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Endocrine Pharmacology Ppt-Merged

The document discusses several classes of endocrine drugs including: 1) Growth hormone drugs used to treat hypopituitarism and pituitary dwarfism. 2) Drugs for hyperpituitarism/gigantism including growth hormone antagonists. 3) Adrenocortical drugs like glucocorticoids and mineralocorticoids used for Addison's disease. 4) Anti-thyroid drugs for treating hyperthyroidism and thyroid hormone replacements for hypothyroidism. 5) Insulin and oral hypoglycemic agents for treating diabetes mellitus.

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0% found this document useful (0 votes)
499 views169 pages

Endocrine Pharmacology Ppt-Merged

The document discusses several classes of endocrine drugs including: 1) Growth hormone drugs used to treat hypopituitarism and pituitary dwarfism. 2) Drugs for hyperpituitarism/gigantism including growth hormone antagonists. 3) Adrenocortical drugs like glucocorticoids and mineralocorticoids used for Addison's disease. 4) Anti-thyroid drugs for treating hyperthyroidism and thyroid hormone replacements for hypothyroidism. 5) Insulin and oral hypoglycemic agents for treating diabetes mellitus.

Uploaded by

Lordgin Openiano
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd
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ENDOCRINE

PHARMA

•  HYPOPITUITARISM
•  PITUITARY DWARFISM
ENDOCRINE DRUGS

•  Somatropin, Somatrem
•  Somatropin and somatrem are hormones of recombinant DNA origin that
are equivalent to human GH. Somatrem is indicated only for the treatment
of children with growth failure due to lack of endogenous GH. Somatropin is
indicated or the treatment of growth failure due to lack of GH or to chronic
renal failure, for treatment of short stature associated with Turner’s
syndrome.
ENDOCRINE DRUGS

•  Individual products vary so follow strictly the manufacturer’s direction before use.
Intramuscular or subcutaneous administration for appropriate distribution of the drug
•  Monitor closely for response to treatment
•  Monitor other hormone function because they may be affected like thyroid function,
and glucose tolerance
•  Monitor closely for adverse effect like hypothyroidism, glucose intolerance and
nutritional imbalance
•  Provide health teaching about the drug, prescribed dosage, therapeutic and adverse
effects to increase client’s and guardian’s understanding and promote compliance
ENDOCRINE DRUGS

•  HYPERPITUITARISM
•  GIGANTISM, ACROMEGALY
ENDOCRINE DRUGS

•  Octreotide, Pegvisomant, Bromocriptine


•  These drugs are growth hormone antagonist. Octerotide ( Sandostatin )
inhibits GH release with less inhibitory effect on insulin release.
Pegvisomant ( Somavert ) is a GH analog, it binds to GH receptors on cells
inhibiting GH effects. It must be given daily subcutaneous injection.
Bromocriptine ( Parlodel ) is a dopamine agonist inhibiting GH secretion in
patients with acromegaly; opposite effects occur in normal individuals
ENDOCRINE DRUGS

•  Follow strictly the manufacturer’s direction for use.


•  Monitor patient’s response to the drug
•  Monitor for adverse effects like hypothyroidism, glucose intolerance, nutritional
imbalance, GI disturbances, dizziness headache and cholecystitis
•  Provide comfort measures
•  Health teaching about drug actions and adverse effects to increase client’s and
guardian’s understanding
ADRENOCORTICAL DRUGS

•  ADDISON’S DISEASE
•  ADRENAL INSUFFICIENCY
ADRENOCORTICAL DRUGS

•  Glucocorticoids and Mineralocorticoids


•  Some synthetic glucocorticoids have mineralocorticoid effects like Hydrocortisone.
Examples of Glucocorticoids include also Cortisone, Prednisone, Dexamethasone,
Budesonide, Beclomathasone. A powerful mineralocorticoid replacement is
Fludrocortisone.
•  These steroids enter target cells and bind to cytoplasmic receptors initiating a complex
reaction that are responsible for anti – inflammatory and immunosuppressive effects.
•  Since the natural steroids or hormones follow a diurnal pattern of release, these steroids
are given following the natural hormone release, two thirds in the morning and one third at
night.
ADRENOCORTICAL DRUGS

•  Avoid sudden withdrawal of steroids to prevent addisonian crisis. Taper the dose if there is a need to
discontinue.
•  Monitor glucose, sodium, potassium levels
•  Monitor vital signs especially BP
•  Follow the regimen and administer following the natural release of hormones
•  Avoid exposure to infection
•  Do not give live virus vaccines because the client is immunosuppressed
•  Monitor CBC
•  Provide health teaching about the drugs, therapeutic and adverse effects to increase client’s or
guardian’s understanding
HYPERTHYROIDISM

•  There are two classification of anti – thyroid drugs.


•  Thioamides – Propylthiouracil (PTU), Methimazole
•  These drugs prevent formation of thyroid hormones within the thyroid cells,
lowering the serum levels of thyroid hormones. They also inhibit the conversion of
T4 to T3 at the cellular level.
•  Iodine solutions – Low doses of iodine are needed in the body for the formation of
thyroid hormone. High doses however, block the thyroid function. Radioactive
iodine destroys thyroid tissues thus decreasing hormone production
ANTI THYROID DRUGS

•  Monitor thyroid hormone levels regularly


•  Monitor for symptoms of hypothyroidism as its primary adverse effects
•  Administer PTU round the clock as ordered to ensure consistent therapeutic levels
•  Administer iodine solution using straw to prevent staining of the teeth. Tablets may be
crushed.
•  Monitor client’s response to the drug
•  Provide health teaching about the drug, therapeutic action and adverse effect.
•  Provide measure to promote good client’s compliance.
HYPOTHYROIDISM

•  Thyroid Hormone replacement


•  Several thyroid hormone replacement products are available. These products
contain both natural and synthetic thyroid hormone. They act to replace low or
absent levels of thyroid hormones and to suppress the overproduction of TSH by
the pituitary. Levothyroxine, a synthetic salt of T4 is the most frequently used
replacement hormone because of its predictable bioavailability and reliability.
Liothyronine is a synthetic salt of T3, rapid onset and long duration of action.
•  These thyroid hormone replacements will increase the metabolic rate of body
tissues, increasing oxygen consumption, respiration and heart rate, growth
hormone and maturation.
THYROID REPLACEMENT

•  Nursing considerations
•  Administer before breakfast to ensure consistent therapeutic levels
•  Advise periodic blood tests to assess levels of thyroid hormones and TSH
•  Monitor for signs of primary adverse effect of hyperthyroidism
•  Monitor vital signs
•  Monitor cardiac response
•  Assess for possible adverse effects like anxiety, skin rash, tachycardia and hypertension
DIABETES MELLITUS

•  Drug therapy is focus on


•  Replace insulin
•  Increase sensitivity of cells to insulin
•  Increase entry of glucose into the cells
•  Decrease absorption of glucose in the GIT
Insulin

INSULIN
Type Example Onset Peak Duration

Very short Aspart, Lispro 15 min 30 to 60 min 2 – 4 hours

Short Regular 30 – 60 min 2 – 4 hours 4 – 6 hours

Intermediate NPH 2 – 4 hours 6 – 8 hours 16 – 20 hours

Long acting Ultralente 6 – 8 hours 12 – 16 hours 20 – 30 hours

Very long Glargine, 1 hour No peak 24 hours


acting Lantus
INSULIN

•  Nursing interventions:
•  Monitor vital signs, tachycardia can occur during insulin reaction
•  Rotate injection sits to prevent lipodystrophy
•  Monitor blood sugar level daily
•  Monitor for glucose control by determining glycosylated hemoglobin test (HBA1c)
periodically
•  Provide health teaching on symptoms of hypoglycemia such as tremors, palpitation,
dizziness, pallor, tachycardia and syncope
ORAL HYPOGLYCEMIC AGENTS
Classification Examples Mechanism of Action
First generation Sulfonylureas Tolbutamide, Chlorpropramide Potentiate insulin action
Second generation Sulfonylurea Glipizide, Glyburide, Glimeperide Potentiate insulin action

Non Sulfonylureas Biguanides decrease hepatic production


Biguanides Metformin of glucose and decreases glucose
Alpha glucosidase inhibitors Acarbose absorption in the small intestine.
Acarbose also decreases absorption of
glucose in the small intestines

Thiazolidinedones Pioglitazone Insulin enhancing agents


Meglitinides Repaglinide Stimulate beta cells to release insulin

DDP-4 Inhibitors Sitagliptin, Linagliptin Increase the level of incretin hormones,


increase insulin secretion and decrease
glucagon secretion to reduce glucose
production
ORAL HYPOGLYCEMIC AGENTS

•  Nursing considerations
•  Determine vital signs. Oral antidiabetic drugs may increase cardiac function and oxygen consumption
which can cause cardiac dysrhythmias,
•  Administer non sulfonylureas with food to minimize GI effects
•  Sulfonylureas are taken before meals
•  Monitor blood glucose level
•  Monitor glycosylated hemoglobin test (HBA1c) for glucose control
•  Provide health teaching about the drug, the name, the prescribed dose, therapeutic and adverse
effects to increase client’s knowledge, lessen anxiety and promote good compliance.
GASTROINTESTINAL PHARMA

•  DRUGS AFFECTING GASTRIC SECRETIONS


•  LAXATIVES AND ANTIDIARRHEAL DRUGS
•  ANTIEMETIC DRUGS
DRUGS AFFECTING GASTRIC SECRETION

•  DRUGS FOR PEPTIC ULCER DISEASE, GASTRITIS AND GERD


•  ANTACIDS
•  H2 RECEPTOR BLOCKERS
•  PROTON PUMP INHIBITORS
•  ANTI PEPTIC DRUGS
LAXATIVES

•  CHEMICAL LAXATIVE
•  BULK LAXATIVES/OSMOTIC LAXATIVE
•  STOOL SOFTENERS
ANTI DIARRHEAL DRUGS

•  LOPERAMIDE
•  OPIATE RELATED DIPHENOXYLATE WITH ATROPINE
ANTI DIARRHEAL DRUGS

q Drowsiness, dizziness, dry mouth, dehydration


q Inhibits gastric motility
q Alcohol is OUT
q Report if there is a narcotic drug history
q Response to drug should be determined prior to driving
q Habit forming, take only prescribed dose
q Electrolytes- monitor with severe diarrhea; encourage clear liquids
q Assess frequency of bowel movements; bowel sounds
ANTI EMETIC DRUGS

•  PATHOGENESIS OF NAUSEA AND VOMITING


•  CHEMORECEPTOR TRIGGER ZONE (CTZ)
ANTI EMETIC DRUGS
•  Phenothiazines – suppress the vomiting center in the medulla
•  Examples:
•  Prochlorperazine, Promethazine
•  Nonphenothiazine – reduce responsiveness of the cells in the CTZ to circulating chemicals
to relieve vomiting
•  Example:
•  Metoclopramide
•  Anticholinergics/Antihistamines – block transmission of impulses to CTZ, very good for
client with vomiting due to vertigo.
•  Examples: Buclizine, Cyclizine, Meclizine
ANTI EMETIC
•  5-HT 3 receptor blockers – block the receptors associated with nausea and vomiting both
locally and centrally (CTZ)
•  Examples: Dolasetron, Ondansetron
•  Substance P/Neurokinin 1 Receptor antagonists – directly act in the CNS to block the
receptors associated with nausea and vomiting little effect on serotonin , dopamine and
corticosteroid receptors
•  Example: Aprepitant
•  Miscellaneous anti emetic drugs
•  Trimethobenzamide HCl
•  Hydroxyzine
•  Dronabinol
• 
ANTI EMETIC

•  Monitor response of the client to the drug


•  Provide safety if CNS effects occur
•  Provide comfort measure including mouth care
•  Provide adequate health teaching about the dug to increase client’s knowledge and
good compliance
RESPIRATORY PHARMA

•  DRUGS FOR UPPER RESPIRATORY TRACT


•  DRUGS FOR LOWER RESPIRATORY TRACT
DRUGS FOR UPPER RESPIRATORY TRACT

•  ANTIHISTAMINE
•  CHLORPHENAMINE, DIPHENHYRAMINE
•  CLARITIN, CITIRIZINE
•  DRUGS FOR COMMON COLDS
•  PHENYLEPHRINE
DRUGS FOR UPPER RESPIRATORY TRACT

•  DRUGS FOR COUGH


•  ANTITUSSIVE DRUGS – DEXTROMETHORPHAN, CODEINE, BUTAMIRATE
•  EXPECTORANT – GUIAFENESIN
•  MUCOLYTIC – CARBOCISTEINE, AMBROXOL, BROMHEXINE
DRUGS FOR LOWER RESPIRATORY TRACT

•  BRONCHODILATORS
•  XANTHINE DERIVATIVES (METHYLXANTHINES)
•  SYMPATHOMIMETIC BRONCHODILATORS
•  ANTICHOLINERGIC BRONCHODILATORS
DRUGS FOR LOWER RESPIRATORY TRACT

q Xanthines
q Aminophylline (theophylline thylenediamine)
q N = 10-20 mcg/ml
q Toxicity:
q >20mcg/mL = NAUSEA (1st sign)
q >35mcg/mL = TREMOR (later sign)
DRUGS FOR LOWER RESPIRATORY TRACT

q ß-2 Agonist (SYMPATHOMIMETIC)


q Short Acting: Albuterol (≤20 mins; lasts 4-6 hrs)
q Long Acting: Terbutaline (lasts 12 hrs)
q Anticholinergics
q Ipatromium Bromide (inhalation)
NURSING CONSIDERATIONS

q Breathing and Coughing Techniques (to remove respiratory secretions and optimize
oxygen exchange)
q Relaxation Techniques (e.g. music)
q Evaluate heart rate and blood pressure
q Appropriate positioning
q Tremors
q Have 8 or more glasses of fluids
q Emphasize no smoking
DRUGS FOR LOWER RESPIRATORY TRACT

•  STEROIDS
q Beclomethasone
q Hydrocortisone
q Prednisone
NURSING CONSIDERATIONS

q Nursing Considerations
q DO NOT use during acute attacks.
q Use bronchodilator before corticosteroid aerosol.
q Hold the inhaled drug for a few seconds before exhaling.
q Allow 1-3 minutes to elapse between each inhalation.
q Rinse mouth with water after.
q Notify provider if sore throat or sore mouth occurs; do not stop abruptly.
q Must taper off gradually under provided supervision.
ANTI ASTHMA DRUGS

•  LEUKOTRIENE RECEPTOR ANTAGONIST


•  MONTELUKAST
•  MAST CELL STABILIZERS
•  CROMOLYN SODIUM
CARDIOVASCULAR PHARMA

•  REVIEW ON CARDIAC PHYSIOLOGY



•  REVIEW ON CARDIAC ACTION POTENTIAL
ANTI HYPERTENSIVE DRUGS

•  GOAL : TO DECREASE BP TO NORMAL


ANTI HYPERTENSIVE DRUGS

•  SECONDARY HYPERTENSION
•  CAUSE : PHEOCHROMOCYTOMA
ANTIHYPERTENSIVE DRUGS

•  IF THE PROBLEM IS INCREASED SNS


•  1. ALPHA ADRENERGIC ANTAGONIST
•  PRAZOSIN
•  DOXAZOSIN
•  TERAZOSIN
ANTIHYPERTENSIVE DRUGS

•  IF THE PROBLEM IS INCREASED SNS


•  2. ALPHA 2 ADRENERGIC AGONIST
•  CLONIDINE
•  METHYLDOPA
ANTIHYPERTENSIVE DRUGS

•  IF THE PROBLEM IS INCREASED SNS


•  3. BETA BLOCKERS
•  PROPRANOLOL
•  METOPROLOL
•  ATENOLOL
ANTIHYPERTENSIVE DRUGS

•  ALTERATION OF R – A – A – S ( RENIN – ANGIOTENSIN – ALDOSTERONE


SYSTEM )
R –A – A – S SYSTEM

ACE

•  RENIN ANGIOTENSINOGEN ANGIOTENSIN 1 ANGIOTENSIN 2


INCREASE BV INCREASE SODIUM & WATER REABSORPTION RECEPTOR

INCREASE BLOOD PRESSURE VASOCONSTRICTION


ANTI HYPERTENSIVE DRUGS

•  IF THE PROBLEM IS ALTERED RAAS


•  4. ACE INHIBITORS
•  CAPTOPRIL
•  QUINAPRIL
•  ENALAPRIL
ANTI HYPERTENSIVE DRUGS

•  IF THE PROBLEM IS ALTERED RAAS


•  2. ANGIOTENSIN RECEPTOR ANTAGONIST
•  LOSARTAN
•  CANDESARTAN
•  TELMISARTAN
ANTIHYPERTENSIVE DRUGS

•  IF THE PROBLEM IS ALTERED RAAS


•  6. DIURETICS
•  THIAZIDE DIURETIC
•  HYDROCHLORTHIAZIDE
ANTIHYPERTENSIVE DRUGS

•  VASODILATORS
•  DIRECT ACTING VASODILATORS
•  INDIRECT ACTING VASODILATORS
ANTIHYPERTENSIVE DRUGS

•  DIRECT ACTING ANTIHYPERTENSIVE DRUGS


•  HYDRALAZINE ( APRESOLINE )
•  NITRATES
•  NITROGLYCERINE
•  ISOSORBIDE DINITRATE OR MONONITRATE
•  NITROPRUSSIDE
ANTIHYPERTENSIVE DRUGS

•  INDIRECT ACTING VASODILATORS ( CALCIUM CHANNEL BLOCKERS)


•  NIFEDIPINE
•  AMLODIPINE
•  FELODIPINE
•  VERAPAMIL
•  DILTIAZEM
ANTI HYPERTENSIVE DRUGS

q The most common side effect of the different antihypertensive drugs is


orthostatic hypotension
q Take meds at regular basis
q Assume sitting or lying position for few minutes
q Change position gradually
q Avoid very warm bath, prolonged sitting or standing
q Avoid tyramine rich food
DRUGS FOR ANGINA

•  ANGINA PECTORIS – IMBALANCE BETWEEN DECREASED OXYGEN AND


INCREASED CARDIAC WORKLOAD
•  GOALS
•  1. TO INCREASE OXYGEN
•  2. TO DECREASE CARDIAC WORKLOAD
DRUGS FOR ANGINA

•  NITROGLYCERINE
•  ISOSORBIDE DINITRATE/MONONITRATE
•  BETA BLOCKERS
•  LONG ACTING CALCIUM CHANNEL BLOCKERS
ANTI ANGINAL DRUGS

q Nitroglycerin intravenous (Nitro-Bid IV, Tridil)


q Sublingual (Nitrostat)
q Topical (Nitro-Bid, Nitrol, Nitrong, Nitrostat)

q Nursing Considerations:
q Make position changes slowly and avoid prolonged standing.
q Oral route, take on an empty stomach with a full glass of water.
q Monitor BP and apical pulse before administration and periodically after dose.
ANTI ANGINAL DRUGS

q Assume sitting or supine position when taking the drug.


q Gradual change of position
q Burning or stinging sensation under the tongue
q Subligual route – onset of action 1-2 minutes; duration is 30 minutes
q Advise to carry 3 tablets always; NOT in pockets
q Store nitroglycerine in cool, dry place; use dark, amber colored air tight container
q Change stock every 6 months
q Observe for side effects: headache, flushed face, dizziness, faintness tachycardia
q Rotate sites of transderm patch
DRUGS FOR DYSRHYTHMIAS

•  CLASS I
•  CLASS II
•  CLASS III
•  CLASS IV
DRUGS FOR DYSRHYTHMIAS

•  CLASS 1
•  ACTS ON PHASE 0 – INHIBITS DEPOLARIZATION OF ABNORMAL RHYTHM
•  LIDOCAINE
DRUG FOR DYSRHYTHMIAS

•  CLASS II – ACTS ON PHASE 4


•  PROLONGED RESTING TO SLOW DOWN IMPULSES AND REMOVE ABNORMAL
RHYTHM
•  PROPRANOLOL
DRUG FOR DYSRHYTHMIAS

•  CLASS III – ACTS ON PHASE 3


•  PROLONG CARDIAC REPOLARIZATION
•  AMIODARONE
DRUGS FOR DYSRHYTHMIAS

•  CLASS IV – ACTS ON PHASE 2


•  BLOCKS CALCIUM ENTRY
•  DILTIAZEM, VERAPAMIL
DRUGS FOR DYSRHYTMIAS

•  FOR HEART BLOCKS


•  ANTICHOLINERGIC DRUGS
•  ATROPINE SULPHATE
DRUGS FOR HEART FAILURE

•  LEFT SIDED AND RIGHT SIDED HEART FAILURE


DRUGS FOR HEART FAILURE

•  1. DIURETICS
•  FUROSEMIDE
•  SPIRONOLACTONE
DRUGS FOR HEART FAILURE

•  2. CARDIOTONIC DRUGS
•  SYMPATHOMIMETIC DRUGS
•  CARDIAC GLYCOSIDES
•  PHOSPHODIESTERASE INHIBITORS
•  MILRINONE
DRUGS FOR HEART FAILURE

•  SYMPATHOMIMETIC DRUG
•  DOPAMINE
•  DOBUTAMINE
DRUGS FOR HEART FAILURE

•  DIGOXIN
•  DIGITALIS
DRUGS FOR HEART FAILURE

•  NURSING CONSIDERATIONS:
•  MONITOR HEART RATE BEFORE ADMINISTRATION
•  MONITOR POTASSIUM LEVEL. NORMAL IS 3.5 – 5.5 meq/L
•  MONITOR ECG
•  MAINTAIN THERAPEUTIC LEVEL ( 0.5 – 1.5 meq/L)
•  DO NOT COMBINED WITH CALCIUM CHANNEL BLOCKERS AND AMIODARONE
•  MONITOR FOR SIGNS OF TOXICITY
•  ANTICIPATE ANTIDOTE : DIGIBIND
DRUGS AFFECTING COAGULATION

•  REVIEW ON HEMOSTASIS
•  VASOCONSTRICTION
•  PLATELET PLUG FORMATION
•  BLOOC COAGULATION
ANTI PLATELET DRUGS

•  ASPIRIN
•  CLOPIDOGREL
ANTOCOAGULANT DRUGS

•  PARENTERAL HEPARIN
•  ANTIDOTE: PROTAMINE SULFATE
•  ORAL WARFARIN
•  ANTIDOTE: VITAMIN K
THROMBOLYTIC DRUGS

•  UROKINASE
•  STREPTOKINASE
•  ALTEPLASE
DRUGS AFFECTING COAGULATION

•  Nursing Considerations:
•  Check VS, platelet count, APTT (N=20-36 sec)
•  Observe for bleeding
•  Review bleeding protocol (i.e. electric razors, soft toothbrushes, etc.)
•  Avoid ASA, may use Acetaminophen
DRUGS AFFECTING COAGULATION

•  Nursing Considerations:
•  CBC, Hgb,Hct - monitor
•  Look for Dysrhythmias
•  Observe for bleeding
•  The vital signs must be monitored
•  Small frequent feeding
ANTIFIBRINOLYTIC DRUGS

•  TRANEXAMIC ACID
•  AMINOCAPROIC ACID
Bachelor of Science in Nursing
NCMA 216 ( PHARMACOLOGY )
COURSE MODULE COURSE UNIT WEEK
2 7 8
AGENTS ACTING ON THE CARDIOVASCULAR SYSTEM

✔ Read course and unit objectives



✔ Read study guide prior to class attendance
✔ Read required learning resources; refer to unit
terminologies for jargons
✔ Proactively participate in classroom discussions
✔ Participate in weekly discussion board (Canvas)
✔ Answer and submit course unit tasks

1. Karch, A. M. (2019). Focus on nursing pharmacology. Lippincott Williams &


Wilkins.
2. Kee, Joyce Le Fuer and Hayer, Evelyn R., Pharmacology: A Nursing
Process Approach, 5th Edition, 2006, by Elsevier ( Singapore) PTE LTD
3. Lilley, Linda lane & Harrington, Scott, Pharmacology and the Nursing
Process, 5th Edition, by Elsevier (Singapore) PTE LTD
4. Rizzo, D. C. (2016) Fundamentals of Anatomy and Physiology 4th edition.
Cengage
At the end of the course unit (CM), learners will be able to:
Cognitive:
1. Understand and explain the physiology of the cardiovascular system.
2. Explain and understand the common disorders affecting the cardiovascular system.
3. Identify and recognize the use of various medication for the management and treatment of
cardiovascular disorders
4. Determine appropriate pharmacological treatment and nursing responsibilities during drug
therapy for clients with problems in cardiovascular function.
Affective:
5. Develop heightened interest in studying Nursing Pharmacology.
6. Manifest professionalism and excellence in planning for safe medication administration.
Psychomotor:
7. Illustrate the use of various medications for the management and treatment of
cardivascular disorders
8. Determine appropriate pharmacological treatment and nursing responsibilities during drug
therapy for clients with problems in cardiovascular dysfunctions.
9. Participate in interactive discussion concerning cardiovascular drugs and nursing
interventions.

▪ Afterload
the pressure that the heart must work against to eject blood during systole (ventricular
contraction)
▪ Baroreceptors
are mechanoreceptors located in the carotid sinus and in the aortic arch and functions to
sense pressure changes by responding to change in the tension of the arterial wall, heart rate
and contractility
▪ Blood pressure
the force exerted by the blood against the endothelial smooth muscle wall
▪ Cardiac cycle
is the period of cardiac muscle relaxation (diastole) followed by a period of contraction
(systole) in the heart
▪ Cardiac output
the amount of blood that is ejected by the heart for every minute
▪ Diastole
resting period when the veins carry blood back to the heart
▪ Dysthythmia
a disruption in cardiac rate of rhythm, also called an arrhythmia
▪ Ischemia
when blood flow to the heart is reduced, preventing the heart muscle from receiving enough
oxygen
▪ Essential hypertension
sustained blood pressure above normal limits with no discernible underlying cause
▪ Inotrope
a drug that increases the force of cardiac contraction
▪ Parasympatholytic
drugs that block the effects of the parasympathetic nervous system
▪ Parasympathomimetics
drugs that mimic the effects of the parasympathetic nervous system
▪ Peripheral vascular resistance (PVR)
also known as systemic vascular resistance (SVR), is the pressure exerted by the endothelial
smooth muscle against the blood
▪ Preload
also known as diastolic filling pressure
is the amount of ventricular stretch at the end of diastole
▪ Renin-angiotensin-aldosterone system
compensatory process that leads to increased blood pressure and blood volume to ensure
perfusion of the kidneys; important in the continual regulation of blood pressure
▪ Stroke volume
amount of blood that is ejected every contraction of the heart, important in determining
blood pressure
▪ Sympathomimetics
drugs that mimic the effects of the sympathetic nervous system
▪ Systole
contraction period when the heart pumps blood out to the arteries for distribution to the
body
▪ Troponin
a muscle protein controlling the interaction of actin and myosin
The heart, a hollow muscle with four chambers comprising two upper atria and two lower ventricles,
pumps oxygenated blood to the body’s cells and also collects waste products from the tissues. The
heart’s conduction (or stimulatory) system consists of the SA node, the AV node, the bundle of His, the
bundle branches, and the Purkinje fibers generate an
impulse, which stimulates the contraction of the heart.
The contraction results to a two-step process called
the cardiac cycle, namely the diastole (relaxation) and
systole (contraction). The cardiovascular system
depends on pressure changes to circulate blood to the
tissues and back to the heart.

DISORDERS OF THE HEART:

I. HYPERTENSION
excessive high blood pressure
Is recognized as a major risk factor for several
potentially lethal cardiac conditions, including
myocardial infarction and heart failure. This can damage the fragile inner lining of blood vessels
and cause a disruption of blood flow to the tissues. It also puts a tremendous strain on the
heart muscle, increasing myocardial oxygen consumption and putting the heart muscle at risk.

BP = Heart rate x stroke volume x peripheral vascular resistance


BP = Cardiac output ( heart rate x stroke volume ) x peripheral vascular
resistance

A. Pathophysiology:
B. Antihypertensive Medications:
Antihypertensive drugs are organized around a clinical indication—the need to
treat a disease—rather than a single receptor type.

a. ACE

INHIBITORS ( … pril )
Captopril (P)
Enalapril
Lisinopril
Perindopril

▪ Pharmacodynamics:
✔ blocks angiotensin-converting enzyme (ACE) from converting angiotensin I to
angiotensin II, leading to;
o a decrease in blood pressure
o a decrease in aldosterone production
o a small increase in serum potassium levels
o sodium and fluid loss.
▪ Indications:
✔ hypertension
✔ heart failure
✔ diabetic nephropathy
✔ left ventricular dysfunction after a myocardial infarction (MI).
▪ Nursing Considerations:
✔ encourage patient to implement lifestyle changes, including weight loss,
smoking cessation, decreased alcohol and salt in the diet, and increased
exercise
✔ administer on an empty stomach 1 hour before or 2 hours after meals
✔ alert the surgeon and mark the patient’s chart prominently if the patient is to
undergo surgery
✔ give the parenteral form of enalapril only if an oral form is not feasible
✔ consult with the prescriber to reduce the dose in patients with renal failure
to account for their
✔ monitor patient carefully for signs of a drop in fluid volume which may lead
to hypotension and other adverse effects

b. ANGIOTENSIN II – RECEPTOR BLOCKERS ( … sartan )


Losartan (P)
Candesartan
Irbesartan
Valsartan
▪ Pharmacodynamics:
✔ selectively blocks the binding of angiotensin II to specific tissue receptors
found in the vascular smooth muscle and adrenal glands
✔ blocks the vasoconstriction and release of aldosterone associated with the
renin–angiotensin–aldosterone system.
▪ Indications:
✔ alone or as part of combination therapy for the treatment of hypertension
✔ diabetic nephropathy with an elevated serum creatinine and proteinuria in
patients with type 2 diabetes and hypertension.
▪ Nursing Considerations:
✔ encourage patient to implement lifestyle changes
✔ administer without regard to meals
✔ alert the surgeon and mark the patient’s chart prominently if the patient is to
undergo surgery
✔ ensure that the female patient is not pregnant before beginning therapy, and
suggest the use of barrier contraceptives while she is taking these drugs
✔ find an alternative method of feeding the baby if the patient is nursing
✔ monitor the patient carefully in any situation that might lead to a drop in
fluid volume

c. CALCIUM CHANNEL BLOCKERS (CCB)


Diltiazem (P)
Amlodipine
Felodipine
Nifedipine
Nicardipine
Verapamil
▪ Pharmacodynamics:
✔ inhibits the movement of calcium ions across the membranes of cardiac and
arterial muscle cells;
o depressing the impulse and leading to slowed conduction,
o decreased myocardial contractility
o dilation of arterioles
✔ resuts to;
o lower blood pressure
o decreases myocardial oxygen consumption.
▪ Indications:
✔ essential hypertension
✔ angina
▪ Nursing Considerations:
✔ encourage lifestyle changes
✔ do not cut, crush, or chew this tablet
✔ give with food if GI upset occurs.
✔ provide comfort and safety measures.
✔ reduce dosage if patient has renal failure.
✔ monitor for any situation that might lead to a drop in blood pressure.
✔ provide support and reassurance to deal with drug effects.
✔ provide patient teaching regarding drug, dosage, adverse effects, signs and
symptoms of problems to report, and safety precautions.
d. VASODILATORS
Nitroprusside (P)
Hydralazine
Minoxidil
▪ Pharmacodynamics:
✔ acts directly on vascular smooth muscle to cause vasodilation and drop of
blood pressure
✔ does not inhibit cardiovascular reflexes and tachycardia
✔ renin release will occur.
▪ Indications:
✔ severe hypertension
✔ maintenance of controlled hypotension during anesthesia
✔ acute heart failure.
▪ Nursing Considerations:
✔ encourage lifestyle changes
✔ monitor BP closely during administration
✔ monitor blood glucose and serum electrolytes
✔ monitor for any situation that might lead to a drop in blood pressure.
✔ provide support and reassurance to deal with drug effects.
✔ provide patient teaching regarding drug, dosage, adverse effects, signs and
symptoms of problems to report, and safety precautions.

e. OTHERS:
i. DIURETICS
Hydrochlorothiazide
Indapamide
Amiloride
Spironolactone
▪ Pharmacodynamics:
✔ increase the excretion of sodium and water from the kidney
✔ decreases blood volume leading to decrease in BP
✔ first line agent in mild hypertension
▪ Indications:
✔ Hypertension
● Nursing considerations:
✔ monitor VS
✔ monitor input and output
✔ weigh the patient daily
✔ monitor for adverse effects

ii. RENIN INHIBITOR


ALISKIREN (P)
▪ Pharmacodynamics:
✔ Inhibits renin leading to
o Decreased plasma renin activity
o Inhibits the conversion of angiotensinogen to angiotensin I
✔ results to;
o decreased BP
o decreased aldosterone release
o decreased sodium reabsorption
▪ Indications:
✔ hypertension
▪ Nursing Considerations:
✔ avoid in the second and third trimesters of pregnancy and used only
in the first trimester if the benefit clearly out weights the risk
✔ advise to use contraceptive while on this drug
✔ advise breastfeeding mothers to find another method of feeding the
baby
✔ monitor serum potassium level for risk of hyperkalemia
✔ monitor closely if taken with furosemide
✔ advise to report any signs of difficulty in breathing or swelling of lips,
face or tongue

iii. Sympathetic Nervous System Blockers:


1. BETA BLOCKERS (…olol)
Acebutolol
Atenolol
Betaxolol
Bisoprolol
Metoprolol
▪ Pharmacodynamics:
✔ compete with the beta receptors ( beta-1 and beta-1 ) of the
sympathetic nervous system
✔ results to;
o vasoconstriction
o decrease heart rate
o decrease cardiac muscle contraction
o increase blood flow to the kidneys
✔ leading to a decrease in the release of renin
▪ Indications:
✔ hypertension
o monotherapy in step 2 treatment or combination with
other antihypertensive drugs
✔ angina
✔ myocardial infarction (MI)
✔ prophylaxis for migraine
▪ Nursing Considerations:
✔ monitor vital signs especially HR and BP before administration
✔ avoid if BP is less than 90/60 mmHg
✔ avoid if HR is less than 60 beats per minute
✔ monitor for adverse effects
✔ caution in patients with hyperglycemia
2. ALPHA- and BETA- BLOCKERS
Carvedilol
Labetalol
Guanabenz
▪ Pharmacodynamics:
✔ Blocks both the alpha- and beta- receptors of the the
sympathetic nervous system
▪ Indications:
✔ Adjunct in the treatment of hypertension
▪ Nursing Considerations:
✔ monitor for adverse effects complain of fatigue, loss of libido,
inability to sleep, and GI and genitourinary disturbances
3. ALPHA-ADRENERGIC BLOCKERS
PHENTOLAMINE
PHENOXYBENZAMINE
✔ Pharmacodynamics:
✔ Inhibits the postsynaptic alpha1-adrenergic receptors,
preventing the feedback control of norepinephrine release
o results in;
▪ increase in the reflex tachycardia
✔ Indications:
✔ diagnose and manage episodes of pheochromocytoma
✔ Nursing Considerations:
✔ not recommended for essential hypertension due to the side
effects
✔ monitor vital signs especially BP
✔ monitor for signs of adverse effects

4. ALPHA-1 ADRENERGIC BLOCKERS


Doxazosin
Prazosin
Terazosin
● Pharmacodynamics:
✔ blocks the postsynaptic alpha1-receptor sites
o results in;
o decreases vascular tone
o promotes vasodilation
▪ leading to a fall in blood pressure
● Indications:
✔ hypertension
✔ benign prostatic hypertrophy (BPH)
● Nursing Considerations:
✔ monitor vital signs
✔ teach patient how to stand or move from lying position in
situation where orthostatic hypotension is an issue

5. ALPHA-2 ADRENERGIC AGONIST


Clonicine
Guanfacine
Methyldopa
● Pharmacodynamics:
✔ stimulates the alpha2-adrenergic receptors in the CNS and
inhibit the cardiovascular centers
✔ results in;
o decrease in sympathetic outflow from the CNS
o decrease in norepinephrine release
o weakening the sympathetic nervous system effects
✔ results in;
o increase in the reflex tachycardia
● Indications:
✔ hypertension

● Nursing considerations:
✔ monitor for signs of reflex hypertension
Site of action of
ANTIHYPERTENSIVE DRUGS

Variety of adverse effects and


toxicities associated with
ANTIHYPERTENSIVE DRUGS

II. ANGINA
refers to a strangling or pressure-like pain
caused by cardiac ischemia. The pain is usually
located substernally, sometimes with radiation to
the neck, shoulder and arm, or epigastrium.
Drugs used in angina exploit two main
strategies: reduction of oxygen demand and
increase of oxygen delivery to the
myocardium.

A. Pathophysiology of Angina:
spasm / obstruction of coronary arteries

myocardial ischemia

reduced O2 supply to myocardium

chest pain : angina pectoris


B. Drugs used for Angina:
a. NITRATES
Nitroglycerine (P)
Isosorbide dinitrate
Isosorbide mononitrate
● Pharmacodynamics:
✔ relaxes vascular smooth muscle with a resultant decrease in venous return
and decrease in arterial blood pressure, reducing the left ventricular
workload and decreasing myocardial oxygen
✔ drug of choice for treating an acute anginal attack.
● Indications:
✔ treatment of acute angina
✔ prophylaxis of angina
✔ intravenous treatment of angina unresponsive to beta-blockers or organic
nitrates
✔ perioperative hypertension
✔ heart failure associated with acute MI
✔ to produce controlled hypotension during surgery
● Nursing considerations:
✔ give sublingual preparations under the tongue or in the buccal pouch, and
encourage the patient not to swallow
✔ ask the patient if the tablet “fizzles” or burns, which indicates potency
✔ always check the expiration date on the bottle and protect the medication
from heat and light
✔ instruct the patient that a sublingual dose may be repeated in 5 minutes if
relief is not felt, for a total of 
three doses; if pain persists, the patient should
go to an emergency room
✔ give sustained-release forms with water, and caution the patient not to chew
or crush them. 

✔ rotate the sites of topical forms to decrease the risk of skin abrasion and
breakdown; monitor for signs of skin breakdown to arrange for appropriate
skin care as needed. 

✔ make sure that translingual spray is used under the tongue and not inhaled
✔ break an amyl nitrate capsule and wave it under the nose of the angina
patient to provide rapid relief using the inhalation form of the drug; this may
be repeated with another capsule in 3 to 5 minutes if needed. 

✔ keep a record of the number of sprays used if a trans- lingual spray form is
used to prevent running out of medication and episodes of untreated angina.

✔ have emergency life support equipment readily available in case of severe
reaction to the drug or myocardial infarction. 

✔ taper the dose gradually (over 4 to 6 weeks) after long-term therapy

b. BETA-BLOCKERS
Metoprolol (P)
Nadolol
Propranolol
● Pharmacodynamics:
✔ competitively blocks beta-adrenergic receptors in the heart and kidneys,
decreasing the influence
of the sympathetic nervous system on these tissues
and the excitability of the heart; decreases cardiac output, which results in a
lowered blood pressure and decreased cardiac workload.
● Indications:
✔ treatment of stable angina pectoris
✔ treatment of hypertension
✔ prevention of reinfarction in myocardial infarction patients
✔ treatment of stable, symptomatic heart failure (HF)
● Nursing considerations:
✔ see nursing considerations of beta blockers in Hypertension

c. CALCIUM CHANNEL BLOCKERS (CCB)


Diltiazem (P)
● Pharmacodynamics:
✔ inhibits the movement of calcium ions across the membranes of myocardial
and arterial muscle cells
o altering the action potential and blocking muscle cell contraction
o depresses myocardial contractility
o slows cardiac impulse formation in the conductive tissues, and relaxes
and dilates arteries
o fall in BP and a decrease in venous return
o decreases the workload of the heart and myocardial oxygen
consumption
✔ relieves the vasospasm of the coronary artery
✔ increasing blood flow to the muscle cells (Prinzmetal angina).
● Indications:
✔ treatment of Prinzmetal angina, effort- associated angina, and chronic
stable angina
✔ to treat essential hypertension
✔ to treat paroxysmal supraventricular tachycardia.
● Nursing considerations:
✔ see nursing consideration of CCB used in hypertension

d. PIPERAZINEACETAMIDE
Ranolazine
● Pharmacodynamics:
✔ mechanism of action is not understood
✔ it does prolong the QT interval, it does not decrease heart rate or blood
pressure, but it does decrease myocardial workload, bringing the supply
and demand for oxygen back into balance.
● Indications:
✔ approved as a first-line treatment for angina or for use in combination with
nitrates, beta-blockers, or amlodipine.
● Nursing considerations
✔ contraindicated for use with any known sensitivity to the drug with
preexisting prolonged QT interval or in combination with drugs that would
prolong QT intervals; and with hepatic impairment and lactation
✔ caution should be used with pregnancy or renal impairment.
✔ Drug–drug interactions can occur with;
o ketoconazole, diltiazem, verapamil, macrolide antibiotics, and HIV
protease inhibitors;
o Digoxin levels may become high if the two drugs are combined; if this
combination is needed, the digoxin dose will need to be decreased
o Tricyclic antidepressants and antipsychotic drug levels may increase if
these agents are combined with ranola- zine; if they are combined,
the dose of these drugs may need to be decreased.
✔ Grapefruit juice should be avoided while taking this drug.
✔ dizziness, headache, nausea, and constipation are the most commonly
experienced adverse effects
✔ patients must be cautioned not to cut, crush, or chew the tablets, which
need to be swallowed whole.
✔ safety
precautions may be
needed if dizziness is
an issue.

III. ARRHYTHMIA
a problem with the
rate or rhythm of the heart

A. Pathophysiology:
involves changes to the automaticity or conductivity of the heart cells
resulting from several factors, including;
a. electrolyte imbalances that alter the action potential
b. decreased oxygen delivery to cells that changes their action potential
c. structural damage that changes the conduction pathway
d. acidosis or waste product accumulation that alters the action potential
e. drugs that alter the action potential or cardiac conduction.

B. Drugs used for Arrhythmia:


affect the action potential of the cardiac cells by altering their automaticity, conductivity,
or both. Because of this effect, antiarrhythmic drugs can also produce new arrhythmias—
that is, they are proarrhythmic.
are used in emergency situations when the hemodynamics arising from the patient’s
arrhythmia are severe and could potentially be fatal.

a. CLASS I ANTIARRHYTHMIC DRUGS


● Class Ia:
Procainamide
Quinidine
● Class Ic
Flecainide
Propafenone
● Class Ib
Lidocaine (P)
Mexiletine

● Pharmacodynamics:
✔ blocks phase 0, blocks sodium channels
✔ decreases depolarization, decreasing automaticity of the ventricular
cells
✔ increases ventricular fibrillation threshold
● Indications:
✔ management of acute ventricular arrhythmias during cardiac surgery
or MI
● Adverse effects:
✔ dizziness, light-headedness, fatigue, arrhythmias, cardiac arrest,
nausea, vomiting, anaphylactoid reactions, hypotension, vasodilation
● Nursing considerations:
✔ Titrate the dose to the smallest amount needed to achieve control of
the arrhythmia
✔ continually monitor cardiac rhythm when initiating or changing dose
✔ ensure that emergency life support equipment is readily available
✔ administer parenteral forms as ordered only if the oral form is not
feasible; expect to switch to the oral form as soon as possible
✔ consult with the prescriber to reduce the dose in patients with renal
or hepatic dysfunction
✔ offer support and encouragement to help the patient deal with the
diagnosis and the drug regimen.
✔ provide thorough patient teaching
✔ establish safety precautions, including side rails, lighting, and noise
control, if CNS effects occur to ensure patient safety
✔ arrange for periodic monitoring of cardiac rhythm 
when the patient
is receiving long-term therapy

b. CLASS II ANTIARRHYTHMIC DRUGS


Acebutolol
Esmolol
Propranolol (P)
● Pharmacodynamics:
✔ competitively blocks beta-adrenergic receptors in the heart and
kidney, has a membrane-stabilizing effect, and decreases the
influence of the sympathetic nervous system
● Indications:
✔ treatment of cardiac arrhythmias, especially supraventricular
tachycardia;
✔ treatment of ventricular tachycardia induced by digitalis or
catecholamines
● Adverse effects:
✔ bradycardia, heart failure, cardiac arrhythmias, heart blocks,
cerebrovascular accident, pulmonary edema, gastric pain,
flatulence, nausea, vomiting, diarrhea, impotence, decreased
exercise tolerance, antinuclear antibody development
● Nursing consideration: please refer Class I agents

c. CLASS III ANTIARRHYTHMIC DRUGS


Amiodarone (P)
Dofetilide
● Pharmacodynamics:
✔ acts directly on heart muscle cells to prolong repolarization and the
refractory period, increasing the threshold for ventricular fibrillation;
also acts on peripheral smooth muscle to decrease peripheral
resistance.
● Indications:
✔ Treatment of life-threatening ventricular arrhythmias
● Adverse effects:
✔ malaise, fatigue, dizziness, heart failure, cardiac arrhythmias, cardiac
arrest, constipation, nausea, vomiting, hepatotoxicity, pulmonary
toxicity, corneal microdeposits, and vision changes.
● Nursing consideration: please refer Class I agents

d. CLASS IV ANTIARRHYTHMIC DRUGS


Diltiazem (P)
Verapamil
● Pharmacodynamics:
✔ blocks the movement of calcium ions across the cell membrane,
depressing the generation of action potentials, delaying phases 1 and
2 of repolarization, and slowing conduction through the AV node.
● Indications:
✔ Treatment of paroxysmal supraventricular tachycardia
✔ atrial fibrillation
✔ atrial flutter.
● Adverse effects:
✔ dizziness, light-headedness, headache, asthenia, peripheral edema,
bradycardia, AV block, flushing, nausea, hepatic injury.
● Nursing consideration: please refer Class I agents

IV. HEART FAILURE (HF):

Muscle physiology:
allows actin
calcium and myosin to muscle fibers
inactivates muscle
enters the form slide
the troponin together contraction
cell actomyosin
bridges

Heart Failure
a condition where the heart is not pumping effectively and blood backs up so
the system becomes congested
A. Pathophysiology:
involves dysfunction of the cardiac muscle, of which the sarcomere is
the basic unit, containing two contractile proteins, actin and myosin
can occur with any of the disorders that damage or overwork the heart
muscle
o Coronary artery disease (CAD)
o Cardiomyopathy
o Hypertension
o Valvular heart disease
C. Signs and Symptoms:

D. Agents used for


Heart Failure :
a. CARDITONIC DRUGS ( INOTROPIC DRUGS )
drugs that affect the intracellular calcium levels in the heart muscle
results in;
✔ increased contractility
✔ increase in contraction
✔ increased cardiac output
✔ increased renal blood flow
✔ increased urine production
o decreases renin release
o interfering with the effects of the renin–angiotensin–
aldosterone system
o increases urine output
o decreased blood volume
✔ decrease in the heart’s workload
✔ relief of HF

i. CARDIAC GLYCOSIDES
Digoxin ( Lanoxin )
derived from digitalis plant
most often used drug to treat HF
✔ Pharmacodynamics:
✔ increases intracellular calcium and allows more calcium to enter
myocardial cells during depolarization
✔ results in;
o a positive inotropic effect
o increased cardiac output and renal perfusion
o a negative chronotropic effect
o decreased conduction velocity through the atrioventricular
(AV) node
✔ decrease in the heart’s workload
✔ relief of HF
● Nursing considerations:
✔ consult with the prescriber about the need for a loading dose when
beginning therapy to achieve desired results as soon as possible. 

✔ monitor apical pulse for 1 full minute before administering the drug
to monitor for adverse effects.
✔ hold the dose if the pulse is less than 60 beats/min in an adult or less
than 90 beats/min in an infant; retake the pulse in 1 hour. If the pulse
remains low, document it, withhold the drug, and notify the
prescriber because the pulse rate could indicate digoxin toxicity
✔ monitor the pulse for any change in quality or rhythm to detect
arrhythmias or early signs of toxicity. 

✔ check the dose and preparation carefully because digoxin has a very
small margin of safety

✔ check pediatric dose with extreme care
✔ have the dose double-checked by another nurse before
administration
✔ follow dilution instructions carefully for intravenous use; use
promptly to avoid drug degradation. 

✔ administer intravenous doses very slowly over at least 5 minutes to
avoid cardiac arrhythmias and adverse effects.
✔ avoid IM administration 

✔ arrange for the patient to be weighed at the same time each day, in
the same clothes
✔ avoid administering the oral drug with food or antacids
✔ maintain emergency equipment on standby:
o potassium salts
o lidocaine (for treatment of arrhythmias)
o phenytoin (for treatment of seizures)
o atropine (to increase heart rate)
o a cardiac monitor, in case severe toxicity
✔ Obtain digoxin level as ordered
✔ monitor the patient for therapeutic digoxin level (0.5–2 ng/mL) 

✔ monitor for adverse effects (vision changes, arrhythmias, HF,
headache, dizziness, drowsiness, GI upset, nausea
✔ Patient teaching on the antidote in case of toxicity (Digoxin immune
Fab) 


ii. PHOSPHODIESTERASE INHIBITORS


Milrinone
✔ Pharmacodynamics:
✔ blocks the enzyme phosphodiesterase
✔ results in;
o an increase in myocardial cell cAMP
o increases calcium levels in the cell
o stronger contraction
o prolonged response to sympathetic stimulation
o directly relaxes vascular smooth muscle.
✔ decrease in the heart’s workload
✔ relief of HF
● Indication:
✔ short-term treatment of HF in patients who have not responded to
digitalis, diuretics, or vasodilators
● Nursing considerations:
✔ protect the drug from light to prevent drug degradation
✔ ensure that patient has a patent intravenous access 
site available to
allow for intravenous administration 
of the drug
✔ monitor pulse and BP frequently 

✔ monitor input and output and record daily weight 

✔ monitor platelet counts before and regularly during 
therapy
✔ inspect the skin for bruising or petechiae
✔ consult with the prescriber about the need to decrease the dose at
the first sign of thrombocytopenia. 

✔ monitor IV injection sites and provide comfort measures 

✔ provide life support equipment on standby in case of severe reaction
to the drug or development of ventricular arrhythmias. 

✔ provide comfort measures 


b. VASODILATORS
i. ACE Inhibitors ( …pril )
✔ Captopril
✔ Enalapril
ii. Nitrates
✔ Nitroglycerine
● Pharmacodynamics:
✔ relax vascular smooth muscle
✔ results in;
o a decrease afterload
o a venous pooling
▪ a decrease preload of the heart
▪ decrease workload
▪ (+) inotropic effect
● Indications:
✔ Hypertension
✔ heart failure
✔ diabetic nephropathy
✔ left ventricular dysfunction after a myocardial infarction (MI).

iii. DIURETICS
▪ Pharmacodynamics:
✔ Increase urine output to reduce blood volume
✔ results in;
o a decrease afterload
o a decrease preload of the heart
o a decrease cardiac workload
▪ (+) inotropic effect
Indications:
✔ hypertension
✔ heart failure

iv. BETA-ADRENERGIC AGONISTS


▪ Pharmacodynamics:
✔ stimulate the beta receptors in the sympathetic nervous system
✔ results in;
o increase calcium flow into the myocardial cell
o (+) inotropic effect
▪ Indications:
✔ Heart failure

Site of action of drugs


used in HEART FAILURE
Variety of adverse effects
and toxicities with
CARDIOTONIC AGENTS

1. Karch, A. M. (2019). Focus on nursing pharmacology. Lippincott Williams &


Wilkins.
3. Kee, Joyce Le Fuer and Hayer, Evelyn R., Pharmacology: A Nursing
Process Approach, 5th Edition, 2006, by Elsevier ( Singapore) PTE LTD
4. Lilley, Linda lane & Harrington, Scott, Pharmacology and the Nursing
Process, 5th Edition, by Elsevier (Singapore) PTE LTD
5. Rizzo, D. C. (2016) Fundamentals of Anatomy and Physiology 4th edition.
Cengage

Lilley, Linda lane & Harrington, Scott, Pharmacology and the Nursing Process, 5th Edition, by
Elsevier (Singapore) PTE LTD
Rizzo, D. C. (2016) Fundamentals of Anatomy and Physiology 4th edition. Cengage

Make a drug study for each drug class using the format below:
CLASSIFICATION DRUGS PHARMACODYNAMICS PHARMACOKINETICS INDICATIONS SIDE EFFECTS / NURSING
INTERACTIONS CONSIDERATIONS

II. Give the rationale for each of the nursing considerations mentioned for each class.
PHARMACOLOGY 2
ELENITA C. MANRIQUE – ARREGLO, RN, MD, MHA
NEUROPHARMACOLOGY

•  REVIEW ON NEUROPHYSIOLOGY
•  NEURONS AND NERVE ACTION POTENTIAL
•  ELECTRICAL NATURE
•  CHEMICAL NATURE
•  NEUROTRANSMITTERS
•  EXCITATORY NEUROTRANSMITTERS
•  INHIBITORY NEUROTRANSMITTERS

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to delete the image and then insert it again.

ANXIOLYTIC DRUGS

•  SEDATIVE HYPNOTIC
•  Mechanism of action – to enhance the effect of GABA (Gamma Amino
Butyric Acid), an inhibitory neurotransmitter to decrease impulses in the
synapses of the brain, therefore decreasing conduction of rapid impulses
causing symptoms of anxiety.

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ANXIOLYTIC DRUGS

•  Barbiturates – drug action is to enhance GABA effect. This is used to be the drug of
choice to manage anxiety but its depressant effect may cause severe respiratory
depression that this is not primarily used for anxiety today
•  Phenobarbital, Secobarbital, Amobarbital

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again. If the red x still appears, you may have to delete the image and then insert it again.

ANXIOLYTIC DRUGS

•  Benzodiazepines – drug action is to enhance GABA effect to cause inhibition of impulse


transmission.
•  Examples: Diazepam, Lorazepam, Clonazepam, Chlordiazepoxide

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ANXIOLYTIC DRUGS

•  Non – Benzodiazepines
•  Paraldehyde, Meprobamate, Chloral hydrate, Zolpidem, Diphenhyramine

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ANXIOLYTIC HYPNOTIC DRUGS

q Nursing Considerations
q Avoid abrupt discontinuation after prolonged use
q Not given if BP is elevated, with renal/hepatic dysfunction, or history of drug abuse
q Xanax (Alprazolam), Ativan (Lorazepam), Serax ( Oxazepam ) - examples with brand names
q Increase in 3Ds - drowsiness, dizziness, and decrease in BP
q Enhance action of GABA
q Teach to rise slowly from supine
q Yes, alcohol and caffeine should be avoided
ANTIPSYCHOTIC DRUGS

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ANTIPSYCHOTIC DRUGS

•  TYPICAL ANTIPSYCHOTIC DRUGS


•  block Dopamine receptors in the limbic system, in the reticular activating system and
the brain. This group of antipsychotic may block all dopamine receptors including those
not associated with psychoses
•  ATYPICAL ANTIPSYCHOTIC DRUGS
•  – block Dopamine and Serotonin receptors. This group will lock only the receptors of
Dopamine and Serotonin which are responsible for occurrence of psychosis making
them more specific drugs for Psychotic disorders
DOPAMINE RECEPTORS

Mane, A. (2017) dopamine receptors: retrieved fro,https://www.slideshare.net/AmbadasMane2/dopamine-72507519


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TYPICAL ANTIPSYCHOTIC DRUGS

•  Typical Antipsychotic drugs: Older drugs, they are less potent and associated with
more adverse effects
•  Examples: Chlorpromazine, Fluphenazine, Thioridazine, Haloperidol
ATYPICAL ANTIPSYCHOTIC DRUGS

•  Typical Antipsychotic drugs: Older drugs, they are less potent and associated with
more adverse effects
•  Examples: Chlorpromazine, Fluphenazine, Thioridazine, Haloperidol
ANTIPSYCHOTIC DRUGS

q Adverse Effects
q Sedation/Sunlight sensitivity
q Tardive dyskinesia, Tachycardia, and Tremors
q Anticholinergic, Agranulocytosis, Addiction
q NMS ( Neuroleptic Malignant Syndrome )
q Cardiac symptoms (orthostatic hypotension),
q EPS ( Extra pyramidal syndrome )
q Endocrine (change in libido)
EXTRA PYRAMIDAL SYMPTOMS

https://www.pinterest.ph/pin/857865428989492668/
Neuroleptic Malignant Syndrome
q Rigidity
q High fever
MNEMONICS
q Autonomic instability F – FEVER
q Unstable BP E – ENCEPHALPATHY
V – VITALS UNSTABLE
q Diaphoresis E – ELEVATED ENZYME (CPK)
q Pallor R – RIGIDITY OF MUSCLES

q Delirium
q Elevated enzymes:
q creatinine and phosphokinase
q Mute
q Agitation to stupor
NMS Management

q Treatment:
q STOP all antipsychotic agents
q Supportive medical care
ANTI SEIZURE DRUGS

Price, S. Antiseizure drugs (2019) Retrieved from: https://www.healtheuropa.eu/nih-study-anti-seizure-drugs-for-epilepsy/95318/


ANTI SEIZURE DRUGS

•  Mechanisms of Action
•  Suppressing sodium influx or deporalarization in the neuron
•  Suppressing calcium influx, preventing electric current generated by calcium
ions
•  Increasing the action of the Gamma Amino Butyric Acid ( GABA ) an
inhibitory neurotransmitter in the brain
ANTI SEIZURE DRUGS

(A picture depicting a synapse showing neurotransmitters from the presynaptic neurons and receptors at the post synaptic neuron) Retrieved from
https://www.ck12.org/biology/nerve-impulse/lesson/Nerve-Cells-and-Nerve-Impulses-MS-LS/
ANTI SEIZURE DRUGS

http://tmedweb.tulane.edu/pharmwiki/lib/exe/fetch.php/antiseizure_drugs.png?cache=
NURSING CONSIDERATIONS

q Nursing Considerations
•  CNS: dizziness, insomnia
•  Antacids decrease
•  Eat food with drug
•  Support group for epileptics
•  Alert tag indicating specific drug
•  Report adverse effects
ANTI PARKINSON’S DRUGS

https://www.drugoffice.gov.hk/eps/do/en/consumer/news_informations/dm_24.html
DOPAMINERGIC DRUGS

•  Dopaminergic drugs – increase the effect of Dopamine at the receptor sites by


increasing the levels of dopamine in the substantia nigra or directly stimulating the
receptors
•  Levodopa with Carbidopa, Amantadine, Bromocriptine
ANTICHOLINERGIC DRUGS

•  oppose the effects of acetylcholine at receptor sites in the substantia nigra.


These anticholinergic drugs have greater affinity with the receptors of
acetylcholine in the CNS than those in the periphery. However, they still
block some receptors at the autonomic nervous system. Blocking the
acetylcholine effect help to normalize the dopamine – acetylcholine
imbalance in the basal ganglia.
•  Diphenhydramine ( Benadryl ), Benztropine ( Cogentin ), Biperiden ( Akineton )
Trihexyphenidyl ( Artane )
ANTI PARKINSON’S DRUGS

q Dopaminergics
q Levodopa

q Nursing Considerations
q Give the drug with meals
q Monitor bowel function
q Instruct to void before taking the drug
q Inform about relapse
ANTI PARKINSON’S DRUGS
q Anticholinergics
q Benztropine (Cogentin)
q Biperiden (Akineton)
q Trihexyphenidyl (Artane)
q Nursing Considerations: Avoid alcohol, eat sugarless candy, use sunglasses
q Dopamine Agonists
•  Amantadine (Symmetrel)
•  Bromocriptine (Parlodel)
•  Pergolide (Permax)
q Nursing Considerations: Slowly rise from supine to standing position, avoid alcohol
MUSCLE RELAXANTS

https://www.epainassist.com/opioid-treatment/medications/what-is-muscle-relaxer-and-list-of-common-
muscle-relaxants
https://www.google.com/search?
q=centrally+acting+muscle+relaxant+drugs&source=lnms&tbm=isch&sa=X&ved=2ahUKEwj_gMmQqpXpAhXayosBHSR6DUYQ_AUoAXoECA0QAw&biw=1280&bih=561#imgrc=IJZa2c7
qOPKNVM
NMJ BLOCKERS

•  1. NON DEPOLARIZING NMJ BLOCKERS


•  2. DEPOLARIZING NMJ BLOCKERS
NMJ BLOCKERS

Bansal, P. NMJ blockers, Retrieved from https://www.slideshare.net/drpranav1/skeletal-muscle-relaxants-


neuromuscular-blocking-agents-neuromuscular-blockers
SPASMOLYTICS

•  1. CENTRALLY – ACTING MUSCLE RELAXANTS


•  2. DIRECT ACTING SKELETAL MUSCLE RELAXANTS
CENTRALLY – ACTING MUSCLE RELAXANTS

•  DIRECTLY SUPPRESS MOTOR NEURONS IN THE CNS


•  BACLOFEN, ORPHENADRINE, TIZANIDINE
DIRECT ACTING SKELETAL MUSCLE
RELAXANTS

•  DECREASE THE RELEASE OF CALCIUM THE SKELETAL MUSCLES


•  DANTROLENE, BOTULINUM TOXIN B
SPASMOLYTICS

q Centrally-acting Muscle Relaxants


q Baclofen (Lioresal)

q Nursing Consideration:
q Monitor respiratory status
q NO ALCOHOL
SPASMOLYTICS

q Direct Acting Skeletal Muscle Relaxants


q Dantrolene sodium (Dantrium)
q Nursing Consideration:
q  STOP if diarrhea becomes severe

[BSN]
[PHARMACOLOGY]
COURSE MODULE COURSE UNIT WEEK
1 5 5
Drugs Affecting the Body System and Nursing Considerations: CNS & ANS

ü Read the course and unit objectives


ü Read the study guide before class begins
ü Read required reading materials and understand terminologies
ü Participate in classroom discussion
ü Participate in discussion board (Canvas)
ü Answer and submit course unit tasks

At the end of the course unit (CU), learners will be able to:
Cognitive:
1. Review anatomy and physiology of the Nervous System
2. Understand the basic concept of diseases affecting the
o Central Nervous System
o Autonomic Nervous System
3. Classify Neurotransmitters that affect nervous function
4. Comprehend the basic impulse transmission in the nervous system to understand
pharmacodynamics of drugs affecting the nervous system
5. Identify classifications of drugs affecting the CNS and ANS
6. Describe the specific actions of drugs and its adverse effects.
7. Understand the pharmacokinetics of drugs affecting the nervous system


8. Determine specific nursing considerations or precautions in safe drug administration
9. Provide appropriate health drug education related to drug therapy
10. Use available clinical evidence that can ensure safe medication administration
Affective
1. Manifest professionalism in and excellence in planning for safe medication process
2. Listen attentively during discussion
3. Respect other’s opinion during discussion and tactfully make clarifications
Psychomotor
1. Participate in an interactive discussion
2. Express suggestions, reactions and opinions in class


ACTION POTENTIAL – this is a rapid change in the membrane potential that explains how
impulses are conducted along the nerves
ANXIETY – feeling of fear, tension or apprehension from known or unknown reasons
DEPRESSION – affective disorders characterized by extreme sadness, hopelessness and
disorganization
MANIA – characterized by period of extreme over activity and excitement
NEUROTRANSMITTERS – chemicals in the nervous system that help in the transmission of
impulses
PALLIATIVE TREATEMENT – control of signs and symptoms of the disease
PARKINSON’S DISEASE – degenerative disease of the nervous system characterized by
lack of neurotransmitter called Dopamine
SCHIZOPHRENIA – most common type of psychotic disorder that may cause impairment o
function of an individual I the society
SEIZURE – abnormal and excessive impulse transmission in the brain
SYNAPTIC TRANSMISSION – conduction of impulses across the junction between neurons

REQUIRED READING
Karch, A. M. (2019). Focus on nursing pharmacology. Lippincott Williams & Wilkins.

Chapters on Drugs affecting CNS and ANS.

All nursing considerations of the given CNS and ANS drugs

Introduction


Drugs affecting the nervous system alter its functions. A thorough review of the anatomy and
physiology of the Central Nervous System and Autonomic System would help students
understand the mechanisms of actions of drugs. The functional unit, neurons basic function is
impulse transmission which happen by electrical and chemical process. Electrical transmission of
impulses happen by action potential and chemical pocess make use of neurotransmitters to
achieve its functions.

Central Nervous System

Brain & Spinal Cord – very important structure of the CNS is its protective mechanisms that not all
chemicals can pass through it, this affects the pharmacodynamics of drugs because some of them
cannot penetrate the CNS. One vital protective structure is the Blood Brain Barrier (BBB). This
represents therapeutic challenge to drug treatment of brain related disorders because a large
percentage of drugs are carried bound to plasma proteins and are unable to cross the brain.

Peripheral Nervous System

Autonomic Nervous System & Somatic Nervous System – Synapses made by the peripheral
nervous system conduct impulses that is chemical in nature. These neurotransmitters have specific
receptors in the neural membrane tos facilitate conduction of nerve impulses. Drugs may act in the
nervous system to either stimulate or block the receptors to correct alterations in the nerovus
functions.

Neurons conduct impulses by Action Potential, the rapid change in the membran potential, this
happens by movement of sodium into the cells causing depolarization and potassium out of the
cells to cause repolarization. This movement of ions facilitated by channels in the cell membranes
will be acted upon by drugs to correct changes in the nervous system causing disease process.

Classifications of Drugs Affecting the CNS

1. Anxiolytic and Hypnotic Drugs

Anxiety is a feeling of tension, nervousness, apprehension or fear that usually involves


unpleasant reactions to a stimulus, whether acutal or unknown. Anxiety is classified as mild,
moderate, severe and panic. Mild anxiety is normal as it helps the person to have wider
perspective and focus on certain activities but increasing anxiety may cause restlessness
and increase sympathetic stress reaction which may cause physical symptoms of the
sympathetic stress reactions. When anxiety becomes moderate, there is a need for drug
treatment.
Sedation is the loss of awareness and reaction to environmental stimuli. Hypnosis is severe
sedation. These conditons occur due to increase excitatory neurotansmitters causing rapid


brain impulse conduction causing restlessness, irritability, loss of concentration, loss of
mental focus and sympathetic responses like palpitations, tremors, diaphoresis, increase
breathing and increase blood pressure.

Drugs for anxiety are called Anxiolytic Drugs or Sedative Hypnotic Agents
Mechanism of action – to enhance the effect of GABA (Gamma Amino Butyric Acid),
an inhibitory neurotransmitter to decrease impulses in the synapses of the brain,
therefore decreasing conduction of rapid impulses causing symptoms of anxiety.
Drug Classifications
o Barbiturates – drug action is to enhance GABA effect. This is used to be the
drug of choice to manage anxiety but its depressant effect may cause severe
respiratory depression that this is not primarily used for anxiety today
§ Pharmacokinetics: Barbiturates are absorbed well, reaching the peak
levels in 20 to 60 minutes. It is metabolized in the liver and excreted in
the urine
§ Contraindications and Cautions: Barbiturates are more addicting than
other anxiolytic drugs. May cause severe CNS depression and
respiratory dysfunction. Contraindicated in pregnant women and
clients with heaptic and renal dysfunction
§ Adverse Effects: CNS depression, paradoxical excitement, anxiety and
hallucinations. Gastrointestinal signs and symptoms like nausea,
voimiting, constipation, diarrhea and epigastric pain. Cardiovascular
effects include bradycardia, hypotension and syncope
§ Examples: Phenobarbital, Secobarbital, Amobarbital
o Benzodiazepines – drug action is to enhance GABA effect to cause inhibition
of impulse transmission.
§ Pharmacokinetics: this is well absorbed in the GIT with peak levels
achieved in 30 minutes. This is lipid soluble and well distributed in the
body crossing the BBB, placenta and breast milk. Metabolized in the
liver and excreted in the urine
§ Contraindications and Cautions: Contraindicated in Clients with allergy
to benzodiazepines, psychosis, clients with acute narrow angle
glaucoma, shock, acute alcohol intoxication which may exacerbate the
depressant effects of the drugs. Contraindicated in pregnancy as this
is known to possible cause cleft lip or palate, inguinal hernia, cardiac
defects, microcephaly or pyloric stenosis if taken during the first
trimester. Caution should be used in the elderly or debilitated patients
an those with hepatic and renal functions
§ Adverse Effects: Sedation,drowsiness, depression, lethargy,
anticholinergic effects like drying of mount, constipation, orthostatic
hypotension, urinary retention, dysrhythmias, blood dyscrasias and


phlebitis. Withdrawal syndrome may occur with abrupt cessation
characterized by nausea, headache, vertigo, malaise and headache.
§ Examples: Diazepam, Lorazepam, Clonazepam

o Non – Benzodiazepines – Other drugs used for anxiety that do not fall under
Benzodiazepine
DRUGS DESCRIPTIONS
o Paraldehyde o Old drug used for Delerium
Tremens, seizures, absorbed and
metabolze in the liver. It has a
distinctve odor and cannot be stored
in plastic containers
o Meprobamate o An old drug used to manage
anxiety for 4 months, works in the
limbic syste, metabolized in the liver
and excreted in the urine
o Chloral hydrate o Frequently used to produce
nocturnal sedation or preoperative
sedation. Unknown mechanis of
action, absorned in the GIT,
metabolized in the liver and excreted
in the urine
o Zolpidem o Used to treat insomnia,
Metabolized in the liver and excreted
in the urine
o Anti histamines – o Used or its drowsiness effect in
Diphenhydramine ( Benadryl) anxiety. With anticholinergic effect.
Promethazine ( Phenergan Used during preoperatively or
postoperatively to decrease use of
narcotics
o Buspirone o No sedative,anticonvulsant, or
muscle relaxant properties, unknown
mechanism of action, reduces anxiety
without many CNS effects. Absorbed
in the GIT, metabolized in the liver an
excreted in the urine
o Beta Blockers – o Decreasing sympathetic effect
Propranolol to lessen signs nd symptoms of
Metoprolol anxiety

Nursing Considerations


o Do not administer intraarterially because of possible serius areriospasm and
gangrene may develop
o Don not mix IV drugs with other drugs
o Give parenteral forms if oral forms are not feasible and switch to oral which is
safer
o Give IV drugs slowly to avoid hypotension effects
o Promote safety measures
o Monitor hepatic and kidney function
o Taper dose of drugs gradually
o Provide comfort measures to help patient tolerate the effects of drugs
o Provide thorough health teaching about drug effects and adverse reactions
o Offer support and encouragement
o For overdose of Benzodiazepine, Flumazenil must be ready as its antidote.

2. Antidepressant Drugs

Feelings of sadness is normal and expected after a tragic event in life. This is an expected
response to a stressor. Since this is a normal process, many people experiencing severe
sadness may develop a depressive disorder unrecognized. People fail to distiguish normal
process of grieving with a major depressive disorder. Depression being an affective disorder
is recognized by its clnical manifestations such as sleep disturbances, they have little
energy, inability to perform daily activity. They may describe overwhelming feelings of
sadness, despair, hopelessness and disorganization.

Pharmacology explains depression by Biogenic Amine Theory. This theory explains that
depression occurs due to decreasing neurotransmitters, norepinephrine, serotonin and
dopamine.

When impulses travel across the synapses, neurotransmitters are released into the
symapse, they bind in the receptors in the post synpatic neural membrane and help impulse
to be conducted. After which, neurotransmitters are removed by enzymes or they may go
back to the presynaptic neuron:

Refer to picture below

In the limbic system which is the area responsible for over all emotion and behavior, there
are three neurotransmitters being released, Norepinephrine, Serotonin and Dopamine. After
impulse is transmitted across the synpase, and enzyme called Mono Amine Oxidase will
remove them. Some however may go back to the pre synaptic neuron the process called
reuptake of Neurotrnasmitters. If they are not available in the synapse, there will be no more
impulse transmission.

Let us go back to Biogenic Amine Theory which explains that depression results from
decreasing neurotransmitter in the limbic system which may happen due possibly to:

1. Overused of neurotransmitters ( Norepinephrine, Dopamine and Serotonin)


2. Increase effect of Mono Amine Oxidase ( MAO ) enzyme
3. Increase reuptake of neurotransmitter back to presynaptinc neuron

If we know the problem in the limbic system that is decreasing neurotransmitters, then we
need to increase them and make them stay in the synaptic cleft. Drugs for hypertension
may achieve its therapeutic effect within 2 – 4 weeks from its oral intake.

Drugs for Depression are called Anti Depressant Drugs

Mechanisms of action
o Inhibit the enzyme Mono Amine Oxidase (MAO)
o Inhibit Reuptake of Neurotransmitters
Drug Classifications
o Tricyclic Antidepressants (TCA) – inhibit presynaptic reuptake of
neurotransmitter, norepinephrine and serotonin, which leads to accumulation
of these neurotransmitters in the synaptic cleft and increased stimulation of
post synpatic receptors
§ Pharmacokinetics: it is abosrbed in the gastrointestinal tract, reaching
the peak in 2 to 4 hours. Widely distributed in the tissue including the


brain. Metabolized in the liver and excreted in the urine. They cross
the placenta and the breast milk.
§ Contraindications and Caution: Contraindicated to those with known
allergy to TCA. Clients with recent myocardial infarction because of its
cardiovascular effects. Caution should be used in clients with
Gastrointestinal and Genitourinary tract disorders. The presence of
hepatic and renal impairment increases toxicity of the drugs.
§ Adverse Effects: CNS effects like sedation, hallucinations, fatigue,
cardiovascular effects, unstable blood pressure, abnormal rhtyhms,
myocaridal infarction, anticholinergic effects like drying of the mouth,
constipation, urinary retention
Remember Mnemonics
C – Cardiovascular effects
A – Anticholinergic effects
S – Sedation
H – Hyotension or Hypertension
• Clinically important drug – drug interactions: The effects of TCA may
increase if combined with Ranitidine, Fluoxetine and Cimetidine
especially the anticholinergic effects. Oral anticoagulant level may
increase if combined with TCA and risk for bleeding increases.
Increase effect with sympathomimetic drugs especially its
cardiovascular effects
• Examples: Imipramine, Amitryptilline, Clomipramine

o Mono Amine Oxidase Inhibitors – these drugs inactivate the enzyme MAO to
increase the neurotransmitters in the synapses.
• Pharamacokinetics: absorbed in the GIT, reaching peak levels in 2 – 3
hours, metabolized in the liver and excreted in the urine. They pass
the placenta and breast milk and not used in pregnancy.
• Contraindications and Cautions: Contraindicated in clients with
cardiovascular disease, hepatic and renal disease. Caution should be
used in psychiatric patients
• Adverse Effects: More adverse effects than other antidepressant
drugs. Dizziness, excitement, nervousness, mania, hyperfexia,
tremors, confusion, insomina, agitation and blurred vision. Liver
toxicity, Cardiovascular toxicity. Anticholinergic effects
• Drug – Drug interaction: Drug interaction with other antidepressant
drugs include hypertensive crisis, coma and severe convulsion. A
period of 6 weeks should elapse after stopping SSRI and beginning
MAOI.
• Drug – Food Interactions: Tyramine – rich food which normally broken
down by MAO enzymes in the GIT amybe absorbed in high


concentration in the resence of MAOI and may cause hypertensive
crisis.
• Examples: Isocarboxazid, Phenelzine, Tranylcypromine

o Selective Serotonin Reuptake Inhibitors (SSRI) – these drug specifically block


the reuptake of serotonin with little or no effect on Norepinpehrine. SSRIs do
not have the many adverse effects of TCAs and MAOIs
• Indications: Depression, Obsessive Compulsive Disorders (OCD)
Panic attacks, Bulemia, Post Traumatic Stress Disorder (PTSD)
• Pharmacokinetics: well absorbed in the GIT, metabolized in the liver
and excreted in the urine or feces. SSRIs are associated with
congenital abnormalities. They passed the placenta and the breastmilk
• Contraindication and Caution: Those with allergy to SSRIs, pregnancy
and lactation.
• Adverse Effects: CNS effects like headache, drowsiness, dizziness,
insomnia, anxiety, tremor, agitation and seizures. Anti cholinergic
effects on the gastrointestinal tract and genitourinary tract.
• Examples: Fluoxetine, Sertraline, Paroxetine

Nursing Considerations
o Limit drug access to potentially suicidal patients to decrease the risk of
overdose
o Monitor the patient for 2 – 4 weeks to ascertain onset and full effects
o Monitor blood pressure and orthostatic blood pressure carefully
o Monitor liver function
o Withold medication dose in client with severe headache that may due
to severe hypertension and cerbrovascular effects
o Have phentolamine or another adrenergic blocker for hypertensive
crisis
o Provide comfort measures to help the client tolerate drug effects
o Privde list of food that is low or no tyramine to clients on MAOI therapy
o Offer support and encouragement to help patients cope with the
disease and drug regimen

3. Psychotherapeutic Drugs

Mental disorders have several classifications. For this course, discussion include only drugs
used for Schizophrenia and Mania, two of the most common psychiatric disorders.

Schizophrenia is the most common type of osychotic disorders. This prevents an individual
in functioning in the society. Some clinical manifestations include, hallucinations, delusions,
paranoia, speech abnormalities and affcetive problems.


Mania is associated with Bipolar illenss. Mania is characterized by periods of extreme
overactivity and excitement

Drugs for mental disorders are called Psychotherapeutic drugs. Drugs for Schizophrenia are
called Anti Psychotic Drugs and for drugs for Mania are called Anti Manic Drugs

Antipsychotic drugs
Mechanisms of Action
o Typical Antipsychotic drugs – block Dopamine receptors in the limbic system,
in the reticular activating system and the brain. This group of antipsychotic
may block all dopamine receptors including those not associated with
psychoses
o Atypical Antipsychotic drugs – block Dopamine and Serotonin receptors. This
group will lock only the receptors of Dopamine and Serotinin which are
responsible for occurrence of psychosis making them more specific drugs for
Psychotic disorders
Drug Classifications
o Typical Antipsychotic drugs: Older drugs, they are less potent and associated
with more adverse effects
§ Examples: Chlorpromazine, Fluphenazine, Thioridazine, Haloperidol
o Typical Antipsychotic drugs: Older drugs, they are less potent and associated
with more adverse effects
§ Examples: Chlorpromazine, Fluphenazine, Thioridazine, Haloperidol
o Pharmacokinetics: Antipsychotic drugs are erratically absorbed in the GIT,
metabolized in the liver and excreted in the bile and urine. Widely distributed
in the tissues, being released up to 6 months after they are discontinued.
Drugs cross the placenta and breast milk so they are not given to pregnant
and lactating mothers
o Contraindications and Cautions: Contraindicated in patients with Parkinson’s
disease, cardiovascular disease, severe hypotension and bone marrow
suppresion
o Adverse Effects include Anti chlinergic effects like drying of the mouthe,
constipation and urinary retention, Sedation effect, Orthostatic hypotension
and extra pyramidal symptoms. Remember the mnemonics ASHE. These are
the most common adverse effects of antipsychotic drugs which are
manifesting more in typical antipsychotic than atypical antipsychotic drugs
A – Anti cholinergic effect
S – Sedation
H – Hypotension
E – Extra pyramidal Symptoms


• Parkinson’s like syndrome, Dystonia, Akathisia, Tardive dyskinesia
these adverse reactions happen because of dopmaine blocking effect
in the basal ganglia altering its function of coordination and fine motor
function.
Other adverse effects may include respiratoy distress like laryngospasms,
bronchospasms and dyspnea. Bone marrow suppresion and blood dyscrasia
are seen in some patients

Nursing Considerations
o Do not allow patients to crush or chew the tablet as it decreases absorption of
the drugs
o Monitor for orthostatic hypotennsion
o Consider warning the patient or the patient’s guardian on the risk of tardive
dyskinesia
o Monitor CBC to check signs of bone marrow suppression
o Provide positioning of legs to decrease discomfort of dyskinesia
o Provide sugarless candies for drying of the mouth
o Encourage the patient to void before taking the dose if urinary retention is a
problem
o Provide safety measures such as side rails and assistance in ambulation if
there are CNS effects
o Provide vison examination to determine ocular changes
o Conduct thorough health teaching on the effects and adverse effects of the
drugs
o Offer support and encouragement to help patients cope with their drug
regimen
Anti Manic Drug - LITHIUM
Mechanism of Action – Lithium alters sodium transport in the nerve and muscle,
inhibit the release of norepinephrine and dopamine slightly and decreases
intraneuronal content of second messengers. The last action may modulate
impulses to control hyperactive state in mania
o Pharmacokinetics: Lithium is absorbed in the GIT. It slowly crosses the BBB.
Dehydration and sodium depletion may cause the kidneys to reabsorb more
Lithim thus increasing serum levels and toxicity. Lithium crosses the palcenta
and breastmilk.
o Contraindications and Cautions: Contraindicated to those with allergy to the
drug, dehydration, hyponatremia and leukemia


o Adverse Effects: Toxicity associated with serum level of Lithium.
( Therapeutic level 0.6 – 1.2 mmol/L)
o Serum level less than 1.5 mmol/L CNS problems including lethargy,
slurred speech, muscle weakness, fine tremor; poluria, beginning
gastric toxicity
o Serum level 1.5 – 2 mmol/L Intensification of the above plus ECG
changes
o Serum levels of 2.0 – 2.5 mmol/LProgression of CNS symptoms to
ataxia, hyperreflexia and seizure, hypotension
o Serum levels more than 2.5 mmol/L complex multi organ toxicity and
death
Other drugs used for Mania
o Aripiprazole – atypical antipsychotic drug
o Lamotrigine – anti convulsive drug
o Olanzapine – atypical antipsychotic drug
o Quetiapine – atypical anti psychotic drug
Nursing Considerations on administration of Lithium
o Daily monitoring of lithium serum levels
o Give the drug with food to alleviate GI irritation
o Ensure that the patient have adequate intake of salt nd fluid
o Monitor closely especially during the initial stage of therapy
o Arrange for small and frequent meals with sugarless lozenges for drying of
mouth
o Provide safety measure like siderails and assistance with ambulation if CNS
effects occur to prevent potential injury
o Offer support and encouragement ot help patient cope with drug regimen

4. Anti – Seizure Drugs

Seizure is a collection of different syndromes characterized by abnormal and excessive


impulse transmission in the brain. Seizures may be primary or secondary. Primary seizure
disorder has no known cause this is often called Epilepsy. Secondary Seizure may be
caused by Cerebrovascular accident, Infections, Brain Tumor, Traumatic Brain Injury, Fever
and a lot more conditions that may alter impulse transmission in the brain. Seizure and
Convulsion are not synonymous. Convulsion is seizure manifesting motor symptoms like
tonic clonic seizure. All convulsions are seizure but not all seizures are convulsions.

Seizure is further classified into Generealized and Partial Seizure. Generalized seizure
beigns in one area of the brain and rapidly spread to both hemispheres of the brain.


Examples of generalized seizure include Tonic – Clonic Seizure formerly known as Grand
Mal Seizure. Partial seizures or focal seizures involve one area of the brain and do not
spread throughout the entire organ. The presenting symptoms depend on exactly where the
excessive electrical discharge is occurring in the brain. Samples include Partial Seizure and
Complex Seizure.

The problems of seizure is excessive impulse transmission in the brain, so the action of the
drug is to decrease impulse transmission, anti seizure drugs cause CNS depression.

Mechanisms of Action
1. Suppressing sodium influx or deporalarization in the neuron
2. Suppressing calcium influx, preventing electric current generated by calcium ions
3. Increasing the action of the Gamma Amino Butyric Acid ( GABA ) an inhibitory
neurotransmitter in the brain

Refer to the figure below:

The figure shows how impulses are transmitted across the synapse. Action potential happen by
sodium influx and potassium efflux, calcium channels open causing release of calcium that
generate electrical activity and nurotransmitters both excitatory and inhibitory regulate impulse
transmission. Excitatory neurotransmitters allow impulses to travel while inhibitory
neurotransmitters stop impulses.

The mechanisms of action of anti seizure drugs occur in the neuronal synapse. Drugs for Seizures
are called Anti – seizure drugs or Anti – convulsive drugs (Anticonvulsant drugs) or Anti – Epileptic
Drugs.

Drug Classifications
o Hydantoins – inhibit sodium influx or depolarization along the nerve fiber.


§ Pharmacokinetics: Hydantoinsa are absorbed in the GIT. . It is higly
protein bound up to 95%. A decrease in serum albumin or proteins
increases free phenytois serum levels. Average half life is 24 hour.
Hydantoins are metabolized to inactive metabolites and excreted in
the liver. Hydantoins are less sedating than Barbiturates and
Benzodiazepines.
§ Adverse Effects: Neurologic and psychiatric effect which include
slurred speech, confusion, depression. Low platelet count and WBC
may happen and gingival hyperplasia (overgrowth of gum tissue or
reddened gums that easily bleeds). Hyperglycemia and less severe
adverse effcts such as nausea, vomiting, constipation, drowsiness,
headache and alopecia
§ Drug – Drug interactions: Hydantoins must not be taken with other anti
seizure drugs because it may increase its CNS depressant effects.
Increase effects of Hydantoins happen in combination with Aspirin,
anticoagulants, Barbiturates, Rifampicin and chronic ingestion of
ethanol. Decreased Hydantoins absorption occur when combined with
Antacids, calcium preparations, sucralfate and some anti cancer
drugs.
§ Examples: Phenytoin,Fosphenytoin, Ethotoin
o Barbiturates - enhanced GABA effect. These drugs are highly sedating and
they may cause severe CNS depression. ( Refer to Anxiolytic Drugs for
detailed discussion )
§ Indications: Anxiety, General Anesthesia and most commonly used for
Generalized Tonic – Clonic Seizure
o Benzodiazepines – enhanced GABA effect. (Refer to Anxiolytic Drugs for
detailed discussion and examples)
§ Indications: For status epilepticus and benign febrile seizure.
Diazepam is not used for long term treatment of seizure. Clonazepam
is good for treatment of Petit Mal Seizure and Myoclonic Seizure
o Succinimides – enhanced effect of GABA, an inhibitory neurotransmitter.
• Examples: Ethosuximide the drug of choice for Petit – Mal or Absence
Seizure with relative few adverse effects than other anti seizure drugs.
Methosuximide
o Valproate or Valproic Acid – reduces electrical acivity by suppressing calclim
influx and enhancing GABA effects the drug of choice for treating myoclonic
seizure
o Other anti- seizure drugs include Carbamazepine, Gabapentin, Lamotrigine,
Levetiracetam. Topiramate. Some of these drugs used for partial seizure may
also be used for treatment of neuropathic pain like Carbamazepine is used for
treatment of Trigeminal Neuralgia.
Nursing Considerations:


o Administer the drug with food to alleviate GI irritations
o Monitor CBC to detect possible bone marriw suppresion
o Evaluate therapeutic blood level to prevent toxicity
o Provide safety measures
o Provide thorough health teaching, including drug name, prescribed dosage
and avoidance of adverse effects
o Suggest that clients wear Medic Alert Bracelet to alert health care workers
about the use of anti epiletpic drugs
o Offer support and encouragement to help the partient cope with the drug
regimen.

5. Anti – Parkinson’s Drugs

Parkinson’s Disease is a degenrative disorder of the central nervous system. There is no


known cause. This is common among elderly 60 years old and above. The disease is
characterized by degeneration of the substantia nigra in the midbrain. A dopamine secreting
neurons in the brain. Therefore there is tremendous decrease of dopamine in the brain
especially affecting the basal ganglia. The basal ganglia is responsible for coordinating fine
motor movement of the body. Alterations in the basal ganglia function results to lack of
coordination, tremors, rigidity and bradykinesia. The neurons of the basal ganglia function
normally when there is a balance between excitatory and inibitory neurotransmitters.
Dopamine in the basal ganglia acts as the inhibitory neurotransmitter and Acetylcholine
produced by higher neuron in the cerebral cortex act as excitatory neurotransmitter.

In Parkinson’s disease an imbalance of neurotransmitters, decreased dopamine and


increased acetylcholine results to clinical manifestions causing incoordination for
unconscious muscle movements including those that control position, posture and
movement

Anti – Parkinson’s drugs should balance the effects of the neurotransmitters. To increase
Dopamine effect and to decrease Acetylcholine effect should control symptoms of
Parkinson’s Disease. These Drugs do not cure the disease but control the symptoms,
hence the use is for palliative treatment.

Mechanisms of Action
1. To increase dopamine effect
2. To supress acetylcholine effect
Drug Classifications
o Dopaminergic drugs – increase the effect of Dopamine at the receptor sites
by increasing the levels of dopamine in the substantia nigra or directly
stimulating the receptors


§ Pharmacokinetics: These drugs are absorbed in the GIT, metabolized
in the liver and excreted in the urine. They cross the placenta and the
breast milk
§ Contraidication and Caution: Contraindicated to clients with allergy to
the drugs and glaucoma as the drug can exacerbate glaucoma.
Caution should be used with any condition that could be exacerbated
by dopamine receptor stimulation such as cardiovascular disease,
bronchial asthma, peptic ulcer disease, urinary tract obstrution and
psychiatric disorders.
§ Adverse Effects: CNS effects include anxiety, nervousness, headache,
malaise, fatigue, confusion, mental changes, blurred vision, muscle
twitching and ataxia. Peripheral effects include anorexia, nausea,
vomiting, diarrhea, constipation, cardiac arrythmias, urinary retention
and bone marrow suppresion
§ Drug – Drug interaction. Dopaminergic drugs combined with MAOI
may increase hypertensive crisis. The combination of levodopa with
Vitamin B6 and phenytoin and dopamine antagonists may lead to
decrease effect of dopaminergic drugs.
§ Examples:
• Levodopa – a precursor of Dopamine. Once levodopa enters
the BBB, it becomes dopamine and will replace the loss od
dopamine. Dopamine itself cannot pass the BBB so a precursor
called Levodopa is used. When this drug was develop, there
was a dramatic reduction in the signs and symptoms of
Parkinson’s disease, however it was found out later that
levodopa can be destroyed by and enzyme called dopa
decarboxylase before they cross the BBB resulting to
decreasing the level of levodopa that may cross the BBB. This
is the reason why another drug is combined with levodopa.
This is Carbidopa. This drug cannot increase the level of
dopamine in the brain but it inhibits the enzyme, dopa
decarboxylase, therefore allowing more levodopa to pass the
BBB. A combination of levodopa and carbidopa (Sinemet) is
still the best drug for Parkinson’s disease.
• Amantadine is adrug that can increase the release of
dopamine. This drug can be effective as long as there is a
possibility of more dopamine release.
• Bromocriptine acts a direct dopamine agonists on dopamine
receptor sites in the substantia nigra.

o Anticholinergic drugs – oppose the effects of acetylcholine at receptor


sites in the substantia nigra. These anticholinergic drugs have greater


affinity with the receptors of acetylcholine in the CNS than those in the
periphery. However, they still block some receptors at the autonomic
nervous sytem. Blocking the acetylcholine effect help to normalize the
dopamine – acetylcholine imbalance in the basal ganglia.
• Pharmacokinetics: drugs absorbed in the GIT, metabolized in
the liver and excreted by cellular pathways. They pass the
placenta and the breast milk
• Contraindications and Cautions: Contraindicated in clients with
Gastro intestinal or Genito urinary obstruction. Caution should
be used in clients with cadiovascular conditions because of its
blocking effect of parasympathetic nervous system
• Adverse Effects: Blocking CNS actylcholine may cause
disorientation, confusion and memory loss. Peripheral
anticholinergic effect include drying of the mouth, constipation,
urinary retention and orthostatic hypotension.
• Drug – Drug interaction: These drugs should not be combined
with other drugs with anti – cholinergic effects like anti –
psychotic, anti – depressant drugs.
• Examples: Diphenhydramine ( Benadryl ), Benztropine
( Cogentin ), Biperiden ( Akineton ) Trihexyphenidyl ( Artane )
These drugs are famous by their brand names. Most often
used for treatment of Parkinson’s like syndrome, an adverse
effect of anti – psychotic drugs.
Nursing Considerations
o Provide sugarless lozenges to relieve drying of the mouth
o Give the drugs with caution in hot weather or with exposure to hot
environemtn because of increase risk for heat prostration
o Give drugs with meals as they may cause GI irritation
o Monitor bowel functions
o Establish safety precautions
o Ensure that the patient voids before taking the drugs if urinary retention is a
problem
o Provide thorough patient teaching about topics such as the drug name and
prescribed dosage, measures help to avoid averse effects, warning signs that
may indicate problems and need for pwriodic monitoring and evaluation to
enhance patient knowledge about drug therapy and to promote compliance
o Offer support and encouragement to help the patient cope up with the
disease and drug regimen

AUTONOMIC NERVOUS SYSTEM


The division of the peripheral nervous system that supply involuntary muscles, glands and other
effectors not innervated by the somatic nervous system. Autonomic nervous system is responsible
for all involuntary actions of the body that the person is not aware of. This is divided into two
divisions:

PARASYMPATHETIC NERVOUS SYSTEM

Parasympathetic nervous system (PNS) comes from the cranio – sacral outflow of the
peripheral nervous system. Cranial nerve X, IX, VII, III participate in the cranial flow.
Majority of the PNS comes from cranial nerve X ( Vagus nerve ). This is the only cranial
nerves that extend up to the thorax and abdomen to supply majority of parasympathetic
innervation, so a vagal stimulation is synanymous with parsympathetic innervation. Sacral
nerves also participate in the PNS to supply mostly the effectors in the pelvic area like
urinary bladder.

The ganglia of the PNS are located near the organ of innervation. The neurons therefore of
the PNS are pre – ganglionic neuron, the neuron from the Cranio – sacral outflow to the
ganglia and the post – ganglionic neuron, the neuron from the ganglia to the organ of
innervations. PNS is responsible for “REST AND DIGEST” involuntary responses of the
body

Impulses transmitted across the synapses of the ganglia are mediated also by the
neurotransmitters.

In the PNS, the neurotransmitter is Acetylcholine. Receptors for acetylcholine are located in
the post synaptic neuronal membrane. These receptors are called cholinergic receptors.
There are 2 tyoes of cholinergic receptors
1. Nicotinic Receptors
2. Muscarinic receptors

SYMPATHETIC NERVOUS SYSTEM

The division of the autonomic nervous system, Sympathetic nervous system (SNS) from the
thoraco- lumbar outflow, spinal nerves from this region send nerve fibers to the sympathetic
ganglia located near the CNS, then post ganglionic neurons send innervation to the
involuntary muscles and glands and other effectors mostly assoicated with involuntary
process in the body.

The preganglionic neuron of the SNS is shorter than PNS and the post ganglionic neuron is
longer than PNS. SNS is responsile for “FIGHT OR FLIGHT” involuntary responses of the
body. Impulses transmitted across the synapses also are mediated by the


neurotransmitters. There are two neurotransmitters in the SNS. Actylcholine and
Epinephrine and Norepinpehrine ( Catecholamines )

Actylcholine is released by the preganglionic neurons, while epinephrine and


norepinephrine are the neurotransmitters released by the post ganglionic neurons, except
for those post ganglionc neurons innervating adrenal medulla, pilo arector muscles, sweat
glands and some smooth muscles of the blood vessels, they have sympathetic innervations
but the neurotransmitter in at the postganglionic neurons is Acetylcholine

Epinephrine and Norepinephrine may also be called Adrenalin and Noradrenaline


respectively or they are being refered to as catecholamines. Their receptors are called
Adrenergic Receptors.

There are 2 types of adrenergic receptors


1. Alpha receptors
2. Beta receptors

Drugs affecting the Autonomic Nervous System are called Autonomic Drugs

Classifications of Autonomic Drugs

Drugs affecting the PNS are called Cholinergic Drugs

Drugs affecting the SNS are called Adrenergic Drugs

In the study of pharmacodynamics, one action of the drugs is its binding with the receptors that
may stimulate the receptors (drugs are called agonist) and drugs that may block the receptors
(drugs are called antagonists). If a student is aware of the responses of the PNS and SNS, it would
be easier to remember drug actions, they would either stimulate the receptors and produce the
same effect or block the receptors or inhibit the effects.

Most of the effectors are innervated by both sympathetic and parasympathetic and in such case
the response of the body is opposite. See examples below:

Effectors SNS PNS


Heart Increase HR Decrease HR
Lungs Bronchodilate Bronchoconstrict
Blood vessels Vasoconstrict Vasodilate


Therefore, if a drug stimulates the receptors for PNS, it is called cholinergic agonist, enhancing
PNS effect so such drug is also referred to as parasympathomimetic drug. A drug that blocks the
cholinergic receptors is called cholinergic antagonist, also called anticholinergic drugs,
inhibiting PNS response and such drug may also be referred to as parasympatholytic drug

If a drug stimulates receptors for SNS, it is called adrenergic agonist, increasing SNS effect so
such drug is also referred to as sympathomimetic drugs. A drug that blocks the adrenergic
receptors decreases SNS responses called adrenergic agonist or it is also called sympatholytic
drugs.

Remember, knowing the responses of the PNS and SNS is very important to understand actions of
autonomic drugs, because these drugs would only stimulate or block the receptors.

Cholinergic drugs – majority of these drugs affect the PNS.


o Direct acting cholinergic agonist – directly stimulates the cholinergic
receptors to increase its effects
§ Pharmacokinetics: well absorbed with relatively short half – life.
Metabolism and excretion may occur at the synaptic level but exact
mechanism is unknown
§ Contraindications and Cautions: These drugs enhance
parasympathetic effect so must not be given to patients with
hypotension, bradycardia or heart block, intestinal obstruction and
urinary retention.
§ Adverse effects: These are related to increase parasympathetic
responses such as bradycardia, diarrhea, urinary incontinence.
Increase sweating may happen because of the acetylcholine present
in the sweat glands.
§ Drug – Drug interaction: Effects of these drugs maybe increase if
combined with anticholinesterase drugs or the indirect acting
cholinergic agonists.
§ Examples
1. Bethanecol – indicated for non – obstructive urinary retention like
in neurogenic bladder
2. Carbachol – indicated for glaucoma, causing pupillary constriction
3. Pilocarpine – indicated for glaucoma, causing pupillary constriction

o Indirect acting cholinergic agonist – this drug increases acetylcholine


effect by inhibiting the action of acetylcholinesterase (an enzyme that
removes acetylcholine in the synapse. If acetylcholinesterase is not removed
in the synaptic cleft, more acetylcholine stays in the synapse stimulating more


receptors, thus enhancing their effects. These drugs are used for treatment of
Myasthenia gravis and Alzheimer’s disease

Myasthenia gravis is an autoimmune disease of the neuromuscular junction


(NMJ). This is characterized by destruction of cholinergic receptors at the NMJ
that will slow down impulses going to the skeletal muscles. This disease is
characterized by the development of muscle weakness and paralysis. To
increase junctional transmission, indirect acting cholinergic agonist inhibits
acetylcholinesterase making more acetylcholine present in the junction to
improve impulse transmission and muscle function. These drugs are also called
anticholinesterase drugs.

Anticholinesterase drugs for Myasthenia gravis include:

Edrophonium HCL (Tensilon) – short acting anticholinesterase drug used to


diagnose the disease. The action lasts for 10 to 20 minutes.

Neostigmine, Physostigmine, Pyridostigmine – long acting anticholinesterase


drugs used for therapeutic purposes. The onset of action starts 20 to 30 minutes
and may last for 3 – 6 hours.

Alzheimer’s Disease is a degenerative disease of the CNS characterized by


loss of neurons in the CNS which may slow down impulse transmission across
the synapses of the CNS. One important cause of this is explained by loss of
acetylcholine receptors in the post synaptic neurons, like myasthenia gravis, less
receptors mean lesser impulse transmission. So anticholinesterase drugs that
inhibit acetylcholinesterase enzyme will increase acetylcholine effect and
promote impulse transmission in the CNS. Can drugs for myasthenia gravis be
used to patients with Alzheimer’s disease? The answer is no simply because
those drugs cannot pass the BBB. Therefore, Alzheimer’s disease will have its
own anticholinesterase drugs.

Acetylcholinesterase drugs used for Alzheimer’s disease are called Anti


Alzheimer’s drugs which include

Rivastigmine
Donepezil
Tacrine


• Pharmacokinetics: These drugs are well absorbed and distributed in the
body. Drugs for myasthenia do not pass the BBB. The drugs are
metabolized in the liver and excreted in the urine.
• Contraindications and Cautions: The drugs are not given to those with
known allergy to the drugs. The drugs may exacerbate bradycardia,
diarrhea and urinary incontinence
• Adverse effects: Exacerbation of parasympathetic effects may be seen in
the patient such as bradycardia, hypotension and incontinence
Nursing Considerations
o Properly administer eye medication
o Slow IV administration to avoid severe cholinergic effects
o Cholinergic agonist oral preparation must be taken with an empty stomach to
decrease nausea and vomiting
o Closely monitor vital signs and exacerbation of parasympathetic effects
o Provide safety measures
o Monitor patients with Alzeimer’s disease for progression of the disease.
Drugs will not cure the disease
o Monitor patients with Myasthenia gravis for underside or overdose of
medication
o Provide health teaching on the name of drugs, its action and adverse effects
to promote client’s understanding and compliance
o Provide emotional support and encouragement to help the patient cope with
drug regimen

o Cholinergic antagonist also being referred to as anticholinergic drug or


parasympatholytic. The drugs act to block the cholinergic receptors in the
PNS. The drugs may also block some cholinergic receptors present in the
SNS.

§ Pharmacokinetics: The drugs are well absorbed and distributed. Drugs


pass the BBB, placenta and breastmilk. The drugs are excreted in the
urine.
§ Contraindications and Cautions: The drugs are not given to patients
with known allergy to the drugs. Should not be used in clients with
cardiovascular, gastrointestinal or genitourinary conditions because
they may exacerbate anticholinergic effect add worsen the conditions.
Contraindicated in client with glaucoma as the drug may cause
pupillary dilation and further increase intraocular pressure. Caution is
used to patients with hepatic or urinary impairment.
§ Adverse effects: These are associated with anticholinergic effects of
drugs such as drying o the mouth, constipation, urinary retention,


tachycardia, mydriasis. Drowsiness, confusion and insomnia are all
related to the CNS effects of anticholinergic drugs
§ Examples:
Atropine – indicated to decrease secretions, treat bradycardia,
pylorospams, ureteral colic, cause pupil dilation (mydriasis) indicated
as preop drug for cataract extraction. Use as antidote for cholinergic
crisis
Dicyclomine – use for hyperactive bowel in adults
Scopolamine – use in motion sickness, indicated to decrease
secretion, pupil dilation

Adrenergic drugs these drugs act to either stimulate or block the adrenergic
receptors in the SNS
o Adrenergic agonist – stimulate the receptors to increase sympathetic effect
and is also referred to as sympathomimetic drugs
o Adrenergic antagonist – block the receptors to decrease sympathetic effect
and is also referred to as sympatholytic drugs

Adrenergic receptors have 2 types and subtypes. Classification is based on their


actual locations in the body. Below are some adrenergic receptor sites and their
specific locations in the body

Types of the Adrenergic Receptors

1. Alpha receptors
a. Alpha 1 receptors
b. Alpha 2 receptors
2. Beta receptor
a. Beta 1 receptors
b. Beta 2 receptors
Study the table below for some important locations of the receptors

RECEPTORS LOCATION
Alpha 1 receptors Vascular smooth muscles, iris, visceral smooth
muscles like the urinary bladder and iris
Alpha 2 receptors CNS neurons, pancreatic islets
Beta 1 receptors Myocardium, Kidneys, CNS neurons
Beta 2 receptors Visceral smooth muscles like in the lungs,
some vascular smooth muscles, CNS neurons


For the sake of the discussion and the given examples of drugs, the effects of some of drugs in
particular receptors will be discussed first.

Alpha 1 receptors when stimulated will cause vasoconstriction, pupillary dilation and closure of
urinary bladder sphincter causing urinary retention.
When the receptors are block? What would be the expected effects?

Alpha 2 receptors in the CNS neurons when stimulated will decrease norepinephrine flow from the
CNS to the SNS therefore decreasing sympathetic response. Take note that this is the drug that
stimulate adrenergic receptors but decreasing SNS effect because the receptors being stimulated
are located in the CNS.

Beta 1 receptors in the heart when stimulated will increase heart rate. When we use a drug that
blocks the receptor, what is the effect?

Beta 2 are located in the lungs, if we use a drug that stimulates receptors, the effect is
bronchodilation, what is the effect if we block the receptor?

Classifications of Adrenergic Agonist Drugs


1. Alpha and Beta adrenergic drugs ( Sympathomimetic drugs ) – these drugs
stimulate all adrenergic receptors to enhance their effects.
• Pharmacokinetics: these drugs are rapidly absorbed, metabolized in the liver
and excreted in the urine. These drugs may cross the placenta and
breastmilk
• Contraindications and Cautions: Should not be given in client with allergy to
these drugs and to patients with pheochromocytoma as the drugs may
exacerbate the signs and symptoms
• Adverse effects: These are all related to increase SNS response like
tachycardia, hypertension, constipation, urinary retention, pupillary dilation
• Examples
o Epinephrine – the drug of choice during CPR, indicated for treatment
of shock
o Dobutamine – used for treatment of congestive heart failure
o Dopamine – usually given for congestive heart failure and cardiogenic
shock
o Norepinephrine – like epinephrine, may be indicated for cardiac arrest

2. Alpha specific adrenergic agonist – these drugs specifically stimulate only the
alpha receptors and not the beta receptors
• Pharmacokinetics: these drugs are well absorbed and distributed, reach peak
levels in 20 to 45 minutes. These drugs are metabolized in the liver and
excreted in the urine


• Contraindications and Cautions: these drugs are not indicated to clients with
allergy to the drugs, those with hypertension and close angle glaucoma.
Caution is used in clients with cardiovascular disease.
• Adverse effects: these are related to the overdose of drugs that may increase
sympathetic effects like hypertension, gastrointestinal depression and
genitourinary effects like urinary retention
• Examples
o Alpha 1 adrenergic agonist – Phenylephrine used for treatment of
common colds and allergy. This drug causes vasoconstriction to
lessen congestion in the nose therefore called decongestants.
o Alpha 2 adrenergic agonist – Clonidine better known for its brand
name as Catapres acting on the CNS neurons to decrease
norepinephrine flow. This drug is indicated for treatment of
hypertension.
3. Beta specific adrenergic agonist – these drugs specifically stimulate the beta
receptors and not the alpha receptors.
• Pharmacokinetics: well absorbed and distributed in the body, metabolized in
the liver and excreted in the urine. The drugs pass the placenta and
breastmilk, use in pregnancy and lactation only if benefits outweigh the risks
• Contraindications and Cautions: The drugs are contraindicated in clients with
allergy to the drugs. Caution is used in clients with cardiovascular disease like
hypertension and tachycardia.
• Adverse effects: These are related to the primary effects of drugs which will
increase sympathetic effects like hypertension and tachycardia.
• Examples
o Isoproterenol – for treatment of cardiogenic shock and heartblock in
transplanted heart.
o Salbutamol – for treatment of obstructive respiratory disease like
COPD and bronchial asthma
Nursing Considerations
o Avoid sudden withdrawal of the drug because it may cause rebound
hypertension, arrhythmias and flushing
o Monitor vital signs especially blood pressure and heart rate
o Avoid comfort measures including rest and environmental control to decrease
CNS irritation.
o Provide adequate health teaching on the name of drug, prescribed dosage,
effects and adverse effects to increase patient’s knowledge and subsequent
compliance.
Classifications of Adrenergic Antagonist Drugs (Sympatholytic drugs)
1. Alpha and Beta adrenergic antagonist – these drugs block all adrenergic
receptors


• Pharmacokinetics: these drugs are well absorbed and distributed in the body,
metabolized in the liver and excreted in the urine and the feces.
• Contraindications and Cautions: These drugs should not be given to clients
with allergy to the drugs. To those with hypotension and bradycardia. Caution
is used in clients with cardiovascular disease and obstructive lung disorders
• Adverse effects: these mainly on the effects of the drugs in the lungs like
bronchospasm, blood vessels causing vasodilation and hypotension.
• Examples
o Carvedilol
o Labetalol
§ Both examples maybe indicated to clients with severe
hypertension caused by pheochromocytoma
2. Alpha adrenergic antagonist – these drugs block only the alpha receptors,
specific drugs act on the alpha 1 and alpha 2 receptors.
• Pharmacokinetics: these drugs are well absorbed and distributed,
metabolized in the liver and excreted in the urine.
• Contraindications and Cautions: The drugs should not be given to clients with
hypotension and urinary incontinence
• Adverse effects: related to the primary action of the drug causing vasodilation
and hypotension
• Examples
o Phentolamine – more specific drug hypertension in
pheochromocytoma, that will have less adverse effects.
3. Alpha 1 selective adrenergic antagonist – these drugs block only the alpha
receptors, specific drugs act on the alpha receptors on the blood vessels and
urinary bladder to case vasodilation for treatment of hypertension and bladder
emptying for treatment of urinary retention. Although some drugs may act in both
blood vessels and urinary bladder at the same time
• Pharmacokinetics: drugs are absorbed in the GIT, metabolized in the liver
and excreted in the urine.
• Contraindications and Cautions: Contraindicated in clients with allergy to the
drugs. This may exacerbate hypotension and urinary incontinence. Caution is
used to clients with cardiovascular disease, gastrointestinal and genitourinary
conditions
• Adverse effects: related to the sympatholytic effect of drugs causing
hypotension and urinary incontinence.
• Examples
o Prazosin – indicated for treatment of hypertension
o Terazosin – indicated for treatment of hypertension and BPH causing
urinary retention
o Doxazosin – indicated for treatment of hypertension and BPH
causing urinary retention


o Alfuzosin indicated for treatment of BPH
o Tamsulosin – indicated for treatment of BPH

4. Beta adrenergic antagonists – these drugs block both beta 1 and beta 2
receptors, particularly affecting both the heart and the lungs, these drugs
increase heart rate and bronchoconstriction of the lungs
5. Beta 1 specific adrenergic antagonist these drugs block specifically beta 1
receptors in the heart. These drugs are most commonly known as beta blockers.
These drugs are indicated to clients with hypertension, dysrhythmias, angina and
use to support cardiac function in clients with congestive heart failure
• Pharmacokinetics: these drugs are absorbed in the gastrointestinal tract and
undergo hepatic metabolism. The presence of food may increase the
bioavailability of some beta blockers. These drugs are known teratogenic in
animals as it passes the placenta and breast milk
• Contraindications and Cautions: Contraindicated in clients with allergy to the
drugs. Caution should be used in clients with bradycardia and heart block as
well on patients with obstructive lung diseases like COPD and bronchial
asthma
• Adverse effects: these are related to the bradycardia and bronchoconstriction
effect of the drug. Gastrointestinal effects like nausea and vomiting,
genitourinary symptoms may be disturbing to clients as well.
• Examples
• Beta adrenergic antagonists or Beta blockers
o Propranolol
o Pindolol
• Beta 1 specific adrenergic antagonists or Beta 1 blockers
o Metoprolol
o Atenolol
Nursing considerations
o Avoid sudden withdrawal of the drug because it may cause rebound
hypertension, arrhythmias and flushing
o Monitor vital signs especially blood pressure and heart rate
o Monitor ECG
o Avoid comfort measures including rest and environmental control to decrease
CNS irritation.
o Provide adequate health teaching on the name of drug, prescribed dosage,
effects and adverse effects to increase patient’s knowledge and subsequent
compliance.


Karch, A. M. (2019). Focus on nursing pharmacology. Lippincott Williams & Wilkins.

Kee, Joyce Le Fuer and Hayer, Evelyn R., Pharmacology: A Nursing Process Approach, 5th Edition,
2006, by Elsevier (Singapore) PTE LTD

Lilley, Linda lane & Harrington, Scott, Pharmacology and the Nursing Process, 5th Edition, by Elsevier
(Singapore) PTE LTD

Rizzo, D. C. (2016) Fundamentals of Anatomy and Physiology 4th edition. Cengage

(A picture depicting a synapse showing neurotransmitters from the presynaptic neurons and receptors
at the post synaptic neuron) Retrieved from https://www.ck12.org/biology/nerve-impulse/lesson/Nerve-
Cells-and-Nerve-Impulses-MS-LS/

Onyekwelu, Kenechukwu (2019) Neuron-neuron interaction-transmission of impulse across the


synapse. (Ethanol) Retrieved from https://www.researchgate.net/figure/Neuron-neuron-interaction-
transmission-of-impulse-across-the-synapse_fig2_330564807

Lilley, Linda lane & Harrington, Scott, Pharmacology and the Nursing Process, 5th Edition, by
Elsevier (Singapore) PTE LTD

Rizzo, D. C. (2016) Fundamentals of Anatomy and Physiology 4th edition. Cengage


• Make a drug study on the individual drugs discussed in this course unit. Write them in an ½
index card and compile them.
• Search new 2 drugs for each classification of CNS and ANS drugs not discussed in this
course unit and include them in the drug study.

Drug study:


DRUG DOSAGE THERAPEUTIC ADVERSE CONTRAINDICATION NURSING
ACTION EFFECTS CONSIDERATIONS

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