0% found this document useful (0 votes)
3 views25 pages

General

general pharma

Uploaded by

Naveed Ahmad
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
0% found this document useful (0 votes)
3 views25 pages

General

general pharma

Uploaded by

Naveed Ahmad
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
You are on page 1/ 25

🧪 Atropine – Overview

Category Details

Drug Class Anticholinergic (Muscarinic antagonist)

Origin Alkaloid derived from Atropa belladonna (deadly nightshade plant)

Mechanism of Action Competitively inhibits muscarinic acetylcholine receptors (M1–M5) → blocks parasympathetic effects

Pharmacokinetics Rapid onset (IV), half-life: 2–3 hours (longer in elderly and liver disease)

💉 Dosage Forms

 Injection: 0.1 mg/mL, 0.5 mg/mL, 1 mg/mL (IV/IM/SC)

 Eye drops: 0.5%, 1% solution

 Oral (rare)

 Premixed autoinjectors (e.g., for organophosphate poisoning)

✅ Indications / Uses

Clinical Use Details

Bradycardia Emergency treatment of symptomatic bradycardia

Pre-anesthesia Reduces secretions, prevents vagal reflexes during surgery

Organophosphate or Nerve Gas Poisoning Antidote (combined with pralidoxime)

Ophthalmic Use Mydriasis and cycloplegia for eye exams

GI Spasms (historical use) Used for IBS, colic (now rarely used due to side effects)

⚠️Contraindications

 Glaucoma (especially narrow-angle)

 Prostatic hypertrophy

 Myasthenia gravis (unless for pre-op use)

 Intestinal or urinary obstruction

 Tachyarrhythmias

⚠️Precautions

 Elderly (risk of confusion, urinary retention)

 Children (sensitive to hyperthermia, CNS effects)

 Heart disease (may worsen ischemia)


 Use with caution in pregnancy category C

💢 Adverse Effects

System Effects

CNS Confusion, delirium, hallucinations (high dose)

Eyes Blurred vision, photophobia

Heart Tachycardia, palpitations

GI Dry mouth, constipation

Skin Dry, flushed skin

Urinary Retention

🔄 Drug Interactions
 Other anticholinergics (e.g., antihistamines, TCAs) → ↑ side effects

 Cholinesterase inhibitors (e.g., neostigmine) → antagonistic

 Amantadine and quinidine → additive anticholinergic effects

💉 Emergency Dosing Examples


Indication Dose

Bradycardia (ACLS) 0.5 mg IV every 3–5 min (max 3 mg)

Organophosphate poisoning 1–2 mg IV every 5–15 min until secretions dry, then maintenance

Pediatric bradycardia 0.02 mg/kg IV (minimum dose 0.1 mg)

🔬 Monitoring Parameters
 HR and ECG

 Secretions (in poisoning cases)

 Mental status (elderly, high doses)

 Intraocular pressure (if used ophthalmically)

🧾 Comparison: Atropine vs Glycopyrrolate vs Scopolamine


Feature Atropine Glycopyrrolate Scopolamine (Hyoscine)
Anticholinergic (quaternary Anticholinergic (tertiary
Drug Class Anticholinergic (antimuscarinic)
ammonium) amine)
Crosses Blood-Brain Barrier? ✅ Yes (CNS effects) ❌ No (does not cross BBB) ✅ Yes (potent CNS effects)
CNS Effects Mild/moderate (restlessness, confusion) None Strong sedation, amnesia,
Feature Atropine Glycopyrrolate Scopolamine (Hyoscine)
dizziness
5–10 mins (IM), 30–60 mins
Onset (IV) Rapid (within 1–2 mins) Rapid (2–3 mins)
(transdermal)
4–6 hours (IM); 72 hours
Duration 30–60 min (bradycardia), up to 4 hours 2–4 hours
(patch)
Bradycardia, OP poisoning, pre-op Pre-op secretion ↓, vagal blockade during Motion sickness, pre-op
Primary Uses
secretion ↓ surgery sedation, nausea
Reduces secretions, prevents
Preanesthetic Use Same use, but less CNS side effects Rare (if sedation is desired)
bradycardia
Motion Sickness/Nausea Not preferred ❌ Not used ✅ Highly effective (patch)
Ophthalmic Use Mydriasis, cycloplegia Rare Rare
✅ Antispasmodic in GI &
GI/Bladder Spasm Sometimes used historically ✅ Common in IBS, antispasmodic use
urinary tract
Pregnancy Category C B C
Route of Administration IV, IM, SC, ophthalmic, oral IV, IM, oral Oral, IM, transdermal patch
Drowsiness, confusion, dry
Notable Adverse Effects Tachycardia, dry mouth, blurred vision Dry mouth, less tachycardia than atropine
mouth, hallucination
Organophosphate Antidote? ✅ Yes ❌ No ❌ Not preferred

🩺 Summary Recommendations

Condition Preferred Drug Reason


Bradycardia (ACLS) Atropine Fast-acting, effective on muscarinic receptors
Pre-anesthetic secretion control Glycopyrrolate No CNS effects, fewer tachycardia risks
Motion sickness Scopolamine (patch) Crosses BBB, effective antiemetic
Organophosphate poisoning Atropine CNS penetration + peripheral action
Avoiding CNS effects (elderly) Glycopyrrolate Safer, no delirium/confusion

⚡ Adrenaline (Epinephrine) – Complete Drug Overview


Category Details

Other Name Epinephrine

Drug Class Sympathomimetic, Adrenergic agonist

Stimulates α1, α2, β1, and β2 adrenergic receptors:


🔹 α1 → Vasoconstriction
Mechanism of Action
🔹 β1 → ↑ HR & contractility
🔹 β2 → Bronchodilation, ↓ inflammatory mediator release

💉 Dosage Forms

 Injection (IM, IV, SC): 1 mg/mL (1:1000), 0.1 mg/mL (1:10,000)


 Auto-injectors (e.g., EpiPen): 0.3 mg (adult), 0.15 mg (pediatric)
 Nebulized: for croup (racemic or L-adrenaline)
 Topical: for hemostasis (combined with local anesthetics)
✅ Indications / Clinical Uses

Condition Use

Anaphylaxis First-line treatment (IM)

Cardiac Arrest (ACLS) IV/IO during CPR for asystole, PEA, VF, VT

Severe Asthma/Croup Nebulized form

Hypotension/Shock As a vasopressor in septic/cardiogenic shock

Local anesthesia adjunct Added to prolong effect and reduce bleeding

Glaucoma (historical) Rarely used anymore

🩺 Common Doses

Indication Dose

Anaphylaxis (Adult) 0.3–0.5 mg IM (1:1000) q5–15 min PRN

Anaphylaxis (Child) 0.01 mg/kg IM (max 0.3 mg)

Cardiac Arrest (Adult) 1 mg IV/IO (1:10,000) every 3–5 min

Nebulized for Croup 0.5 mL/kg of 1:1000 (max 5 mL) diluted in saline

IV infusion (shock) 2–10 mcg/min titrated to BP/HR

⚠️Contraindications

(Mostly relative in emergencies)

 Non-emergency use in patients with:


o Severe hypertension
o Narrow-angle glaucoma
o Hyperthyroidism
o Ischemic heart disease

⚠️Precautions

 Can cause arrhythmias, especially in digitalis or halothane-exposed patients


 Caution in elderly, diabetics, and patients on MAO inhibitors
 Monitor ECG, BP, and perfusion closely during IV use
💢 Adverse Effects

System Effects

Cardiovascular Tachycardia, palpitations, hypertension, arrhythmias

CNS Anxiety, tremor, headache

Metabolic Hyperglycemia, ↑ lactic acid

Local Injection site necrosis (if extravasated)

🔄 Drug Interactions

 Beta-blockers: may cause paradoxical hypertension


 MAO inhibitors: exaggerated response
 TCAs: increased duration of action
 General anesthetics: risk of arrhythmias

🔬 Monitoring Parameters

 Blood pressure, heart rate


 Cardiac rhythm (ECG)
 Blood glucose (in diabetics)
 Potassium (can decrease transiently)

🧾 Storage & Stability

 Protect from light


 Discard if discolored (pink or brown)
 Do not freeze

💊 Drotaverine – Overview
Category Details

Drug Name Drotaverine Hydrochloride

Drug Class Antispasmodic (Selective Phosphodiesterase-4 inhibitor)

Mechanism of Action Inhibits PDE-4 → ↑ cAMP → relaxes smooth muscle (without anticholinergic effects)

💉 Dosage Forms
 Tablets: 40 mg, 80 mg
 Injection (IM/IV): 20 mg/mL, 40 mg/2 mL ampoule

 Syrup: For pediatric use (rare)

✅ Indications / Uses

System Indication

Gynecology Dysmenorrhea, uterine spasms, cervical dilatation

GI Biliary colic, intestinal colic, IBS, pancreatitis

Urology Renal colic, ureteric spasm

Obstetrics Facilitation of labor (cervical dilatation)

Others Spasms during endoscopy or post-op care

🩺 Dosage Guidelines

Route Adult Dose Pediatric Use

Oral 40–80 mg 2–3 times daily Not recommended <12 yrs

IM 40–80 mg every 8 hours Use with caution in children

IV 40–80 mg slowly over 1–2 minutes Must monitor BP (may drop)

⚠️Contraindications

 Severe liver, kidney, or cardiac failure

 Hypotension

 Lactation (limited data)

 Allergy to drotaverine

⚠️Precautions

 Avoid IV use in hypotensive patients (can cause sharp BP drop)

 Use with caution in pregnant women (Category C)

 May mask symptoms of surgical emergencies (e.g., appendicitis)

💢 Adverse Effects
Common Less Common

Nausea, headache Palpitations, dizziness

Hypotension (IV) Allergic reaction (rare)

Flushing Sweating, transient rise in liver enzymes

🔄 Drug Interactions
 May reduce effectiveness of levodopa

 Caution with antihypertensives (additive hypotension)

🤰 Pregnancy & Lactation

 Pregnancy: Category C – Use only if clearly needed

 Lactation: Avoid (no data on excretion in breast milk)

🧾 Comparison With Hyoscine or Mebeverine


Feature Drotaverine Hyoscine Butylbromide Mebeverine

Class PDE-4 inhibitor Anticholinergic Musculotropic antispasmodic

CNS effects None May cause drowsiness Minimal

Pregnancy use Caution (Cat C) Safe in late pregnancy Limited data

Route Oral, IM, IV Oral, IM, IV Oral only

💊 Dexamethasone – Drug Overview


Category Details

Drug Class Corticosteroid (Glucocorticoid)

Mechanism of Action Binds to glucocorticoid receptors → suppresses inflammation, immune response, and cytokine production

Potency ~25–30x more potent than cortisol (long-acting)

Duration Long-acting: biological half-life 36–72 hours

💉 Dosage Forms
 Oral Tablets: 0.5 mg, 2 mg, 4 mg, 6 mg
 Injection (IV/IM): 4 mg/mL, 8 mg/mL, 10 mg/mL

 Ophthalmic Drops: 0.1%

 Topical Cream/Ointment

 Inhaled/Nasal Spray (in combinations)

✅ Indications / Uses

System Indications

Anti-inflammatory Severe allergies, asthma, arthritis, lupus, IBD

Immunosuppression Autoimmune diseases, transplant rejection prevention

Neurological Cerebral edema, brain tumors, spinal cord injury

Endocrine Adrenal insufficiency, congenital adrenal hyperplasia

Cancer Part of chemotherapy regimens (e.g., multiple myeloma, lymphoma)

Obstetrics Fetal lung maturity (preterm labor: 24–34 weeks gestation)

Infections Severe COVID-19, bacterial meningitis (with antibiotics)

ENT/Allergy Acute laryngitis, nasal polyps

🩺 Common Dosing Examples


Indication Typical Adult Dose

Cerebral edema 10 mg IV bolus, then 4 mg IV every 6 hours

COVID-19 (hospitalized) 6 mg once daily (IV or PO) for 10 days

Asthma exacerbation 4–8 mg oral or IV once daily for 5–10 days

Preterm labor (fetal lungs) 6 mg IM every 12 hrs × 4 doses (total 24 mg in 48 hrs)

Arthritis flare 0.75–9 mg/day depending on severity

Allergy/urticaria 4–8 mg/day orally or IM

⚠️Contraindications

 Systemic fungal infections

 Hypersensitivity to dexamethasone

 Caution in: diabetes, hypertension, osteoporosis, peptic ulcer disease, TB

⚠️Precautions

 Long-term use → adrenal suppression, osteoporosis


 Sudden withdrawal → adrenal crisis

 Pregnancy: Category C (safe for fetal lung development but caution in prolonged use)

💢 Adverse Effects

System Effects

Endocrine Cushingoid features, hyperglycemia, adrenal suppression

GI Peptic ulcer, GI bleeding

Bone Osteoporosis, avascular necrosis (hip)

CNS Insomnia, mood swings, psychosis

Eye Cataracts, glaucoma

Immune Increased infection risk

Skin Acne, striae, poor wound healing

🔄 Drug Interactions

 NSAIDs: ↑ GI ulcer risk

 Diuretics: ↑ hypokalemia

 Vaccines: ↓ immune response

 CYP3A4 inducers (e.g., rifampicin, phenytoin): ↓ dexamethasone effect

 CYP3A4 inhibitors (e.g., ketoconazole): ↑ dexamethasone levels

🔬 Monitoring Parameters

 Blood pressure, blood glucose

 Signs of infection

 Electrolytes (esp. potassium)

 Bone mineral density (long-term use)

 Eye pressure (long-term use)

🔁 Glucocorticoid Potency Comparison

Drug Glucocorticoid Potency Mineralocorticoid Potency Duration

Hydrocortisone 1 1 8–12 hrs (short)

Prednisone 4 0.8 12–36 hrs (intermediate)

Dexamethasone 25–30 0 36–72 hrs (long)


Drug Glucocorticoid Potency Mineralocorticoid Potency Duration

🧾 Gynecological Antispasmodics – Comparison Chart


Hyoscine Valethamate
Feature Drotaverine Mebeverine Alverine Citrate
Butylbromide Bromide

Musculotropic
Drug Class PDE-4 inhibitor Anticholinergic
spasmolytic
Anticholinergic Smooth muscle relaxant

↑ cAMP → direct smooth Blocks muscarinic Direct action on GI/UT Antimuscarinic +


Mechanism Calcium channel modulation
muscle relaxation receptors smooth muscle ganglion blocker

CNS Penetration ❌ No ❌ Minimal ❌ No ❌ No ❌ No

Cervical Dilatation ✅ Yes (obstetric use) ✅ Mild effect ❌ No ✅ Common in labor ❌ Rarely

✅ (chronic or IBS-type
Use in Dysmenorrhea ✅ First-line ✅ Second-line ✅ Occasionally ✅ Sometimes
pain)

Use in Labor ✅ To shorten 1st stage ✅ Less effective ❌ Not used ✅ Traditional use ❌ No established benefit

Dry mouth, Dry mouth, blurred


GI Side Effects Minimal Very few Nausea (rare)
constipation vision

Pregnancy Category Category C Category B Category B Category C Category B

Onset of Action Rapid (10–30 min) Rapid (15–30 min) Slower (1–2 hours) Rapid (within 15 min) Moderate

Route of Use Oral, IM, IV Oral, IM, IV Oral only IM, IV Oral

Dry mouth, blurred Nausea, rare allergic Tachycardia,


Adverse Effects Headache, hypotension (IV) Rare
vision reaction anticholinergic

Heart disease,
Notable Cautions Hypotension, liver disease Glaucoma, BPH Liver disease Hepatic impairment
glaucoma

✅ Clinical Uses in Gynecology

Condition Preferred Antispasmodic(s)

Dysmenorrhea Drotaverine, Mebeverine

Labor pain (cervical spasm) Drotaverine, Valethamate, Hyoscine

IBS/functional GI pain with pelvic overlap Mebeverine, Alverine

Preoperative uterine relaxation Hyoscine, Drotaverine

Postoperative spasm (e.g., D&C) Drotaverine, Hyoscine


🧪 Formulations & Dose Examples
Drug Dose (Oral) Dose (Parenteral)

Drotaverine 40–80 mg TID 40–80 mg IM/IV up to 3x/day

Hyoscine Butylbromide 10–20 mg TID 20 mg IM/IV/SC up to 5x/day

Mebeverine 135–200 mg TID ❌ Not available parenterally

Valethamate Bromide ❌ Not preferred orally 8 mg IM/IV every 2–4 hrs in labor

Alverine Citrate 60–120 mg TID ❌ Not available parenterally

🟩 Summary Notes:
 Drotaverine is preferred for dysmenorrhea, early labor, and spasmodic pelvic pain.

 Hyoscine is good for pre-op relaxation, though more side effects.

 Valethamate is older, used in some obstetric protocols for cervical dilatation.

 Mebeverine is effective for patients with visceral hypersensitivity and IBS-like pelvic pain.

 Alverine is rarely used alone, sometimes combined with simethicone

💊 Pheniramine Maleate – Drug Overview

Category Details
Drug Class First-generation antihistamine (H1 receptor antagonist)
Blocks H1 histamine receptors → reduces allergic symptoms (e.g., itching, sneezing,
Mechanism of Action
swelling)

💉 Dosage Forms

 Tablets: 10 mg, 25 mg, 50 mg


 Injection (IM/IV): 22.75 mg/mL (commonly in 2 mL ampoule)
 Syrup: Available for pediatric use (dose varies)

✅ Indications / Uses

System/Condition Use
Allergy Urticaria, allergic rhinitis, hay fever
Anaphylaxis adjunct Used with adrenaline to control allergic reaction
Insect bites Reduces swelling and itching
Respiratory Allergic asthma, mild bronchospasm
System/Condition Use
Dermatology Eczema, contact dermatitis, drug rash
Obstetrics/Gynecology Premedication before anti-D injection or iron sucrose; pruritus of pregnancy

🩺 Dosing Guidelines
Route Adult Dose Pediatric Dose
Oral 25–50 mg 1–3 times/day 0.5–1 mg/kg/day in divided doses (rarely used)
IM/IV 22.75 mg slowly IV or deep IM every 8–12 hours Use with caution — adjust by weight

⚠️Contraindications

 Narrow-angle glaucoma
 Severe liver disease
 Prostatic hypertrophy
 Known hypersensitivity
 Neonates and premature infants

⚠️Precautions

 Sedation: May impair mental alertness


 Avoid in drivers, machine operators
 Use cautiously in elderly, asthmatics, and pregnancy
 Avoid alcohol or other CNS depressants

💢 Adverse Effects

System Adverse Effects


CNS Drowsiness, dizziness, sedation
GI Nausea, dry mouth, constipation
Cardiac Palpitations, tachycardia (at high doses)
Other Blurred vision, urinary retention
Allergy Rarely: hypersensitivity reaction

🔄 Drug Interactions

 Alcohol, benzodiazepines, opioids → ↑ CNS depression


 MAO inhibitors → ↑ anticholinergic effects
 Additive effect with other antihistamines

🤰 Pregnancy & Lactation


 Pregnancy: Category C – Use only if clearly indicated
 Lactation: May pass into breast milk — avoid prolonged use

⏳ Onset and Duration

 Onset: 15–60 minutes (oral), 5–10 minutes (IV/IM)


 Duration: 4–6 hours (short-acting)

🔍 Comparison with Similar Antihistamines

Drug Sedation Use in Pregnancy Duration Route


Pheniramine High Caution (Cat C) 4–6 hrs Oral, IM, IV
Chlorpheniramine Moderate Relatively safer 6–8 hrs Oral
Cetirizine Minimal Safer (Cat B) 12–24 hrs Oral
Loratadine None Safe (Cat B) 24 hrs Oral

💡 Clinical Tip:

Pheniramine is often used as adjunct to adrenaline in anaphylaxis or as premedication before iron infusions or blood
products.

Tranexamic Acid is an antifibrinolytic agent used to treat or prevent excessive bleeding. Below is a comprehensive
overview:

🔹 Drug Name: Tranexamic Acid

Brand names: Cyklokapron, Lysteda, Transamin, etc.

🔹 Class:
 Antifibrinolytic

 Synthetic derivative of the amino acid lysine

🔹 Mechanism of Action:
Tranexamic acid reversibly binds to plasminogen, preventing its conversion to plasmin, an enzyme that breaks down fibrin clots. This stabilizes
blood clots and reduces bleeding.
🔹 Indications / Uses:
Indication Details

Menorrhagia (heavy menstrual bleeding) Oral tablets commonly used

Surgery-related bleeding Cardiac, orthopedic, dental procedures

Trauma-related hemorrhage To reduce bleeding in trauma patients

Hereditary angioedema Off-label

Postpartum hemorrhage IV use

Epistaxis (nosebleeds), Hematuria Topical or systemic use

Dental extraction in hemophilia To reduce bleeding risk

🔹 Dosage Forms:

Form Route

Tablet Oral

Injection (IV) Intravenous

Mouthwash Topical (oral)

Topical solution Mucosal use

🔹 Dosage (Example):
 Menorrhagia: 500–1000 mg orally TID during menstruation (up to 5 days).

 Surgical bleeding: 10–15 mg/kg IV before surgery; may repeat every 8 hours.

🔹 Warnings / Precautions:
 History of thromboembolic disease (e.g., DVT, PE, stroke)

 Renal impairment – dosage adjustment needed

 Seizure risk in high IV doses (especially in cardiac surgery)

 Visual disturbances (e.g., changes in color vision)

🔹 Adverse Effects:

Common Serious
Nausea, vomiting Seizures
Common Serious
Diarrhea Thromboembolism (rare)

Muscle cramps Visual disturbances

Headache Hypotension (if given IV too fast)

🔹 Contraindications:
 Active intravascular clotting

 History of thromboembolic disorders

 Acquired defective color vision

🔹 Drug Interactions:
 Estrogen-containing contraceptives: ↑ risk of thrombosis

 Factor IX concentrates or anti-inhibitor coagulant complexes: ↑ thrombosis risk

🔹 Use in Pregnancy / Lactation:


 Pregnancy Category B (generally safe, used in postpartum hemorrhage)

 Excreted in breast milk in low amounts — caution advised

🔹 Monitoring Parameters:

 Renal function (creatinine)

 Vision (for long-term use)

 Signs of thrombosis

🔹 Summary Chart:

Category Detail
Mechanism Antifibrinolytic, plasminogen inhibitor

Uses Bleeding control in menstruation, surgery, trauma

Route Oral, IV, topical

Common Dose 500–1000 mg TID

Side Effects GI upset, headache, thromboembolism

Caution In DVT history, renal disease


Category Detail

Enoxaparin Sodium is a low molecular weight heparin (LMWH) used primarily for anticoagulation (preventing blood clots).

🧪 Drug Class:

 Low molecular weight heparin (Anticoagulant)

⚙️ Mechanism of Action:

 Inhibits Factor Xa (mainly) and Factor IIa (thrombin) to prevent clot formation.
 Binds to antithrombin III, enhancing its activity.

💉 Dosage Forms:

 Subcutaneous injection (most common)


 IV injection (for acute situations, e.g., STEMI)

📋 Common Indications:
Condition Purpose
Deep vein thrombosis (DVT) Treatment and prophylaxis

Pulmonary embolism (PE) Treatment

Acute coronary syndrome (e.g., unstable angina) Antithrombotic therapy

Post-surgery (orthopedic/abdominal) DVT prophylaxis

During dialysis Prevent clotting in circuit

Pregnant women at risk of thrombosis Anticoagulation in pregnancy

💊 Typical Adult Dosing (Subcutaneous):

 Treatment dose:
o 1 mg/kg every 12 hours
o OR 1.5 mg/kg once daily
 Prophylactic dose:
o 40 mg once daily
o OR 30 mg every 12 hours (orthopedic surgery)

⚠️ Precautions & Warnings:

 Renal impairment (dose adjustment needed)


 Bleeding disorders or risk of bleeding
 Do NOT use with spinal/epidural anesthesia without caution (risk of spinal hematoma)
 Platelet monitoring (risk of heparin-induced thrombocytopenia, though less common than with unfractionated heparin)

❌ Contraindications:

 Active major bleeding


 History of heparin-induced thrombocytopenia (HIT)
 Hypersensitivity to enoxaparin or pork products

🤝 Drug Interactions:

 Other anticoagulants/antiplatelets (↑ bleeding risk)


 NSAIDs (↑ GI bleeding risk)
 Thrombolytics (↑ bleeding)

🧪 Monitoring:

 Not routinely monitored, but:


o Anti-Xa levels in special cases (pregnancy, renal impairment, obesity)
o CBC, platelets, creatinine

🩸 Reversal Agent:

 Protamine sulfate (partially effective, reverses about 60–70%)

🧪 Heparin (Unfractionated Heparin)


📚 Drug Class:
 Anticoagulant

 Natural glycosaminoglycan

⚙️Mechanism of Action:
 Binds to antithrombin III (ATIII) → enhances its ability to inactivate:

o Thrombin (Factor IIa)

o Factor Xa

o Also affects IXa, XIa, and XIIa

 Inhibits conversion of fibrinogen to fibrin → prevents clot formation.

💉 Dosage Forms:
 IV injection/infusion – for rapid anticoagulation

 Subcutaneous injection – for prophylaxis

📋 Common Indications:

Indication Purpose
Deep vein thrombosis (DVT) Treatment or prevention

Pulmonary embolism (PE) Treatment

Acute coronary syndromes (ACS, STEMI/NSTEMI) Anticoagulation during treatment

Atrial fibrillation (AF) Stroke prevention

During/after surgery VTE prophylaxis

Dialysis and ECMO Maintain circuit patency

Line patency (low doses in flushes) Catheter/line care

💊 Typical Dosing:
 IV bolus: 60–70 units/kg (max ~5000 units)

 IV infusion: 12–15 units/kg/hr, adjusted based on aPTT

 Prophylaxis (SC): 5000 units every 8–12 hours

🧪 Monitoring:

Test Purpose
aPTT Activated Partial Thromboplastin Time – main test

CBC Monitor for thrombocytopenia

Platelets Monitor for Heparin-Induced Thrombocytopenia (HIT)

Anti-Xa levels In special cases (e.g., pregnancy, obesity)


⚠️Precautions:
 Careful in renal or hepatic impairment

 Risk of HIT (more common than with LMWH)

 Bleeding risk, especially GI or intracranial

❌ Contraindications:
 Active major bleeding

 History of HIT

 Severe thrombocytopenia

 Hypersensitivity to heparin or pork products

🩸 Antidote / Reversal Agent:


 Protamine sulfate – neutralizes heparin 100%

🔄 Comparison with Enoxaparin (LMWH):


Feature Heparin (UFH) Enoxaparin (LMWH)

Source Natural (porcine) Derived from heparin

Route IV/SC SC only

Onset Immediate (IV) 3–5 hours (SC)

Monitoring aPTT Usually not needed

HIT risk Higher Lower

Half-life Short (~1–2 hours) Longer (~4–6 hours)

Reversal Fully with protamine Partially with protamine

💊 Dopamine
📚 Drug Class:
 Sympathomimetic agent

 Inotropic agent

 Acts on adrenergic and dopaminergic receptors

⚙️Mechanism of Action:
Dopamine acts in a dose-dependent manner:

Dose Receptor Activity Effect


Low (1–2 mcg/kg/min) Dopamine (D1) receptors Renal vasodilation → ↑ renal blood flow, diuresis

Moderate (2–10 mcg/kg/min) β1-adrenergic receptors ↑ Heart rate, ↑ cardiac output (inotropy)

High (>10 mcg/kg/min) α1-adrenergic receptors Vasoconstriction → ↑ blood pressure

📋 Indications:

Condition Purpose
Shock (cardiogenic, septic) Improve blood pressure and perfusion

Heart failure Short-term support (inotropic effect)

Bradycardia (severe, unresponsive) Temporarily increase heart rate

Renal perfusion (low-dose use; now controversial) Previously used to preserve kidney function

💉 Dosage:
 IV infusion only

 Typical starting dose: 2–5 mcg/kg/min

 Titrated up to 20 mcg/kg/min, depending on response

⚠️Precautions & Warnings:


 Tissue necrosis if extravasation occurs → use central line if possible

 Correct hypovolemia before initiating dopamine

 Monitor heart rate, BP, urine output, and ECG

 May worsen arrhythmias or cause tachycardia

❌ Contraindications:
 Pheochromocytoma

 Uncontrolled tachyarrhythmias

 Hypersensitivity to dopamine or sulfites

🤝 Drug Interactions:
 MAO inhibitors (can cause hypertensive crisis)
 Beta-blockers (may blunt cardiac effects)

 General anesthetics (arrhythmogenic potential)

🧪 Monitoring Parameters:

Parameter Why
Blood pressure To titrate dose

Heart rate / ECG To detect arrhythmias

Urine output Assess renal perfusion

Peripheral perfusion Detect vasoconstriction effects

🧯 Adverse Effects:
 Tachycardia

 Arrhythmias (PVCs, VT)

 Hypertension (at high doses)

 Extravasation → tissue necrosis

 Nausea, vomiting

💉 Antidote for Extravasation:


 Phentolamine (α-blocker) injected around the site to reverse vasoconstriction

💉 Dobutamine
📚 Drug Class:
 Inotropic agent

 Synthetic β1-adrenergic agonist (primarily)

⚙️Mechanism of Action:
 Stimulates β1 receptors → ↑ myocardial contractility and cardiac output

 Minor effects on β2 and α1 receptors (mild vasodilation)

 Increases stroke volume more than heart rate (HR)

📋 Indications:
Condition Purpose
Acute decompensated heart failure Improve cardiac output & perfusion

Cardiogenic shock Short-term support of myocardial function

Cardiac stress testing (off-label) In patients unable to exercise

Septic shock (with low cardiac output) As adjunct to vasopressors

💉 Dosage:
 IV infusion only

 Starting dose: 2–5 mcg/kg/min

 Titrated up to 20 mcg/kg/min based on response

🧪 Monitoring Parameters:

Parameter Purpose
BP & HR Detect hypotension, tachycardia

ECG Monitor arrhythmias

Cardiac output Assess therapeutic effect

Urine output Assess end-organ perfusion

⚠️Precautions:
 Use with caution in atrial fibrillation or other tachyarrhythmias

 Can cause hypotension due to mild β2 vasodilation

 Tolerance may develop after prolonged use (>48 hours)

❌ Contraindications:
 Idiopathic hypertrophic subaortic stenosis (IHSS)

 Uncontrolled arrhythmias

 Hypersensitivity to dobutamine or components

🤝 Drug Interactions:
 Beta-blockers ↓ effectiveness

 General anesthetics ↑ arrhythmogenic potential


 MAO inhibitors ↑ risk of hypertension

🧯 Adverse Effects:
 Tachycardia

 Arrhythmias (PVCs, VT)

 Hypertension or hypotension

 Headache

 Angina (due to ↑ O₂ demand)

🩺 Dobutamine vs Dopamine – Key Differences:

Feature Dobutamine Dopamine


Receptors β1 > β2 (minimal α1) D1 → β1 → α1 (dose-dependent)

Effect ↑ Contractility, mild vasodilation Variable: renal, cardiac, or vasopressor

Use Heart failure, cardiogenic shock Shock (esp. with hypotension)

HR effect Mild ↑ Often significant ↑

BP effect Minimal Can increase significantly (high dose)

Risk of extravasation Low High

💉 Noradrenaline (Norepinephrine)
📚 Drug Class:
 Vasopressor

 Sympathomimetic catecholamine

⚙️Mechanism of Action:
 Primarily stimulates α1-adrenergic receptors → vasoconstriction → ↑ systemic vascular resistance (SVR) and blood pressure

 Mild β1 receptor activity → slight increase in heart contractility and heart rate

 Minimal β2 activity (unlike epinephrine)

📋 Indications:

Condition Purpose
Septic shock First-line vasopressor
Condition Purpose

Neurogenic shock Support BP

Hypotension (acute) Unresponsive to fluids

Cardiogenic shock With low BP and vascular tone

During anesthesia Prevent or treat hypotension

💉 Dosage (IV infusion only):


 Initial: 2–4 mcg/min (0.05–0.1 mcg/kg/min)

 Maintenance: Titrate based on MAP (mean arterial pressure), goal: MAP ≥ 65 mmHg

 Usual range: 2–30 mcg/min (or more in severe cases)

Always administer through a central line to avoid extravasation.

🧪 Monitoring Parameters:

Parameter Why
Blood pressure (MAP) To titrate dose

Heart rate Tachycardia or reflex bradycardia

ECG Arrhythmia monitoring

Perfusion (urine output, lactate) Assess tissue oxygenation

Infiltration site Risk of extravasation & necrosis

❌ Contraindications:
 Hypersensitivity to norepinephrine

 Mesenteric or limb ischemia (relative caution)

 Peripheral IV infusion without central access (risk of tissue necrosis)

⚠️Precautions:
 Can cause severe vasoconstriction → risk of digital or gut ischemia

 Must restore fluid volume before use if patient is hypovolemic

 May cause reflex bradycardia


🤝 Drug Interactions:
 MAO inhibitors, TCAs, Linezolid → may potentiate hypertensive effects

 Beta-blockers → may mask cardiac effects

🧯 Adverse Effects:
 Hypertension

 Reflex bradycardia

 Arrhythmias

 Peripheral ischemia (digits, kidneys, bowel)

 Extravasation → local necrosis

💉 Antidote for Extravasation:


 Phentolamine (α-blocker): inject around the site to reverse vasoconstriction

🩺 Comparison: Noradrenaline vs Dopamine vs Dobutamine

Feature Noradrenaline Dopamine Dobutamine


Receptor Target α1 >> β1 D1 → β1 → α1 (dose-dependent) β1 > β2

Main Effect Vasoconstriction Variable: renal, cardiac, vasopressor Inotropy (↑ CO)

BP Effect Strong ↑ Dose-dependent ↑ Mild ↑ or neutral

HR Effect Mild ↑ or ↓ (reflex) Moderate ↑ Mild ↑

First-line in sepsis ✅ ❌ ❌

You might also like