Pharmacology Flashcards
What is pharmacokinetics?
The movement of drugs within the body
How the body affects the drug including absorption, distribution, metabolism and excretion
What does pharmacokinetic absorption refer to?
The process of how the drug gets into the bloodstream
Speed of absorption determines onset of action
What are 5 factors that affect absorption?
Route of administration
Formulation/properties (solubility, size, preparation),
Blood flow to administration site
Drug interactions
Ability of drug to cross biological barriers
What route of administration is subject to first pass metabolism?
PO
What route gives immediate and complete bioavailability?
IV
What routes can give local +/- systemic effects?
TD
INH
PR
T (not really systemic)
IN
NEB
What routes are considered rapid?
IV
INH
SL
IN
NEB
What is bioavailability?
The amount of drug that reaches systemic circulation and is available to produce effect
Affected by absorption
What is pharmacokinetic distribution?
How the drug spreads throughout the body and to the site of action once it has been absorbed into the bloodstream
What are 6 factors that affect distribution?
Blood flow to area (more blood = more drug carried)
Tissue permeability (how well drug can cross barriers - lipophilic cross membranes better)
Protein binding (drugs bound to proteins are less distributable)
Blood brain barrier (only some drugs can cross)
Distribution to body compartments (may move to useless spaces e.g. extra cellular fluid)
Metabolism (may be converted to inactive metabolites in liver)
What is pharmacokinetic metabolism?
Process of drug transformation/break down
Affects duration of action and excretion
Primarily takes place in liver (also sweat, bile, renal, lung) via cytochrome P450 enzymes
What is a phase I metabolic reaction?
Drug is modified to make it more water soluble for easier excretion by kidney
What is a phase II metabolic reaction?
Combines drug with a compound to make it more water soluble for easier excretion by kidney
What is an enzyme induction/inhibition metabolic reaction?
Induction: drug increases activity of enzyme which leads to increased metabolism of other drugs
Inhibition: drug decreases activity of enzyme which leads to decreased metabolism of other drugs
What are 4 outcomes of drug metabolism?
Inactivation: converts drug to inactive metabolite
Activation: converts drug to an active form
Toxic metabolite: may convert to a toxic metabolite
Pharmacogenetics: individual genes may cause altered activity