Pharmacology A.
Passive absorption
Occurs mostly by diffusion
- The study or science of drugs
Higher to lower concentration movement
Drug – a chemical agent capable of producing biologic Drug does not require energy to move across
responses within our body the membrane
B. Active absorption
Medication – after a drug is administered Requires carrier such as enzyme or protein to
Drug names: move drug against a concentration gradient.
Requires energy
a. Chemical name – description of drug using the C. Pinocytosis
nomenclature of chemistry Cells carry a drug across their membrane by
b. Generic name – the nonproprietary name; engulfing the drug particles
much shorter and less complex than chemical
name NOTE!
c. Trade name – aka brand names; names under Since the GI tract is composed mostly of lipid
which a drug is marketed and protein, drugs that are fat-soluble passes
rapidly than water-soluble drugs.
BASIC AREAS OF PHARMACOLOGY
Bioavailability – term used to express the
extent of the drug absorption
DRUG ACTION - oral route drugs bioavailability = less than
Pharmaceutic phase 100%
- IV route drugs bioavailability = 100%
- 1st phase of drug action
- drug dosage forms First-pass effect – reduces the bioavailability of
- aka “dissolution” = a drug in a solid form must the drug; some drugs are metabolized in the
be disintegrated into small pieces to dissolve liver before proceeding to the desired site of
into a liquid administration
- how various dosage forms influence the way Factors influencing drug absorption:
the drug is absorbed and how the body
metabolizes the drug Drug administration (route)
- 80 % of drugs are taken by mouth Presence of food
Dosage formulation
Tablets = not 100% drug Stomach acidity
= excipients (fillers and inert substances) are
Rate of blood flow
added
GI motility
= enteric – coated tablet/capsules can remain in Status of absorptive
the stomach because disintegration cannot occur until
alkaline environment is reached
Route of Administration:
Pharmacokinetic phase
A. Enteral
- the study of drug movement throughout the
- Drug is absorbed into the systemic circulation
body
through the mucosa of the stomach and
- four basic pharmacokinetic processes:
small/large intestine
1. Absorption – movement of drug from its
- Sublingual route: drug is placed under the
site of administration into the bloodstream
tongue
- Buccal route: between cheek and gums
Half-life (t1/2)
B. Parenteral
- The time it takes for ½ of the drug
- A general term that means any route of
concentration to be eliminated
administration other than GI tract
4. Excretion – the elimination of drug from the
- Examples: Intravenous injection, intramuscular
body
injection, subcutaneous injections, etc
- Main route of drug elimination is through the
kidneys
C. Topical
- Delivers medication directly into the affected Biliary excretion: excretion of drugs by the intestine
area
- Examples: ointments, patches, eyedrops, Enterohepatic recirculation: when certain drugs are
sprays, inhaler in the bile, they may be reabsorbed int the
bloodstream, returned to the liver and secreted
D. Rectal again in the bile
- Administered through the anus
- Useful for local or systemic drug delivery
Onset, Peak, Duration
- Onset: the time it takes to reach the minimum
2. Distribution – the transport of drug by the effective concentration (MEC) after drug
bloodstream to its site of administration admnitration
- Protein-binding effect: Some drug molecules - Peak: when the drug reaches the highest blood
bound themselves to plasma proteins; or plasma concentration
Albumin – the most common blood - Duration: length of time the drug has a
protein and carries majority of inactive pharmacologic effect
drug molecules
Inactive drug – bounded drug
Active drug – not bounded drug; “free”; Pharmacodynamic phase
causes pharmacologic response
A acid glycoprotein - The study of the way drugs affect the body
Corticosteroid-binding globulin
Factors influencing distribution of drug: Receptor Theory
Malnourishment (causes low serum - Drugs act through receptors by binding to the
albumin level) receptor to produce (initiate) a response or to
Abscesses block (prevent) a response
Exudates - Similar to a key-lock relationship
Body glands - 4 receptor families:
Tumor
Liver disease A.) Kinase-linked receptors
Kidney disease The ligand-binding domain for drug binding is
on the cell surface
The drug activates the enzyme and a response
3. Metabolism – the biotransformation is initiated
- the biochemical alteration of a drug
- Liver: main organ for drug metabolism B.) Ligand-gated ion channels
- Influenced by: The channel spans the cell membrane
Patient’s genetic formation The channel opens to allow flow of ions (i.e. Na,
Diseases K) in and out of the cells
Concurrent use of other
C.) G protein-coupled receptor systems Peak drug level
Three components: receptor, G protein that
- Indicates the rate of absorption of the drug
binds with GTP, and the effector that is either
- Highest plasma concentration of drug at a
an enzyme/channel
specific time
Drug -> receptors -> G protein -> effectors
Trough drug level
D.) Nuclear receptors - Indicates the rate of elimination of the drug
Found in the cell nucleus of the cell membrane - Lowest plasma concentration of a drug
Agonist VS Antagonist
- Agonists: Molecules that activate receptors LOADING DOSES and MAINTENANCE DOSES
Partial Agonists: only has a moderate intrinsic
activity Loading dose
- Antagonists: Molecules that prevents receptor - A higher amount of drug
activation by endogenous regulatory molecules - Often given only once or twice to “prime” the
and drugs bloodstream with a sufficient level of drug
Non competitive antagonists: binds irreversibly Maintenance dose
(permanent) to receptors
Competitive antagonists: binds reversibly to - To keep the plasma drug concentration in the
receptors therapeutic range
Nonspecific and Nonselective Drug Effects
Side effects, Adverse reactions, Toxic effects
Nonspecific drugs
Adverse drug reaction (ADR)
- affects various sites
- Any reaction to a drug that is unexpected and
Nonselective drugs undesirable
- Affects various receptors - Occurs at therapeutic dosages
Side effect
Therapeutic Index and Therapeutic Range (Window) - Unavoidable secondary drug effect produced at
therapeutic doses
Therapeutic index (TI) - Generally predictable
- Expected as part of therapy
- Estimates the margin of safety of a drug
- Examples:
through the use of a ratio that measures
effective (therapeutic) dose (ED) in 50% of Drowsiness caused by antihistamine
people (ED50) and lethal dose (LD) in 50% of Gastric irritation caused by aspirin
people (LD50) Toxicity
- Closer to 1, greater the danger of toxicity
TI = LD50/ED50 - The degree of detrimental physiologic effects
caused by excessive drug dosing
Therapeutic Range (window) - Examples:
- The level of drug between MEC and minimum Respiratory depression from overdose
toxic concentration (the toxic effect) of morphine
Severe hypoglycemia from overdose of
Peak VS trough levels insulin
Allergic reaction - Refers to a rapid decrease of in response to the
drug
- An immune response
- Aka “acute tolerance
- The intensity of the allergic reactions is largely
independent of the dosage
- Examples:
Anaphylaxis
Mild to severe rashes
Paradoxical effect
- Opposite of the intended drug response
- Examples:
Excitement and insomnia for pt given
with benzodiazepines for sedation
Teratogenic Effect
- A drug-induced birth defect
Idiosyncratic
- an uncommon drug response resulting from a
genetic predisposition
- Pharmacogenetics: a study of genetic variations
in drug response and focuses on single-gene
variations
Tolerance
- Decreased responsiveness to a drug as a result
of repeated drug administration
- Pharmacodynamic tolerance: The result of
adaptive processes that occur in response to
chronic receptor occupation; a familiar type of
tolerance due to long-term administration of
drugs such as morphine and heroin
- Metabolic tolerance: a tolerance resulting from
accelerated drug metabolism
- Tachyphylaxis: A reduction in drug
responsiveness brought on by repeated dosing
over a short time
Placebo effect
- A drug response is caused by a psychologic
factors and not by the biochemical and
physiologic properties of the drug
- Depends on the pt’s attitude towards the
medicine
Tachyphylaxis
