Pharmacology Principles Flashcards
3 phases of pharmacology
Pharmaceutic, Pharmokinetic, Pharmacodynamic
Pharmaceutic phase
Dissolution occurs—drug begins to dissolve in order to be absorbed; tablet—granula—particle—GI solution—absorption
Pharmacokinetic phase
4 stages—absorption into the blood thru the GI tract, distribution at the site of action (effect exerted), metabolism by the liver, excretion by the kidneys (and a small part of the liver)
Cell membrane—phospholipid bilayer
Drug passes thru the cell membrane in the intestinal walls to the blood and travels to the site of action if lipid soluble (needs facilitator if water soluble)
First pass effect
A % of a drug is broken down by the liver in a first pass before systemic circulation; bioavailability of the drug decreases accordingly for drugs that pass thru the GI tract instead of going directly into the blood (IV)
Bioavailability
Amount of drug available in the blood; drugs with lower bioavailability may require higher dose or more frequent dose
Where does the first pass effect NOT occur
IV, highly vascularized tissues like SL, buccal, rectal, parenteral, topical meds
Enteral
By way of the GI tract (PO, oral, rectal, small intestine); first pass occurs
Parenteral meds
SQ, IM, IV, intrathecal (spinal cord), epidural (space around spinal cord); no first pass
Topical meds (transdermal)
Apply to body surfaces; eyes, skin, ears, nose, lungs;no first pass effect occurs
Distribution
Mvt of drug thru body; drug arrives at site of body
What does distribution depend on?
Blood circulation; less blood flow, less circulation; harder to reach tissue (abscesses, tumors, peripheral vascular disease)
Blood brain barrier
Cells in capillary wall in brain have tight junctions that prevent drug passage except for lipid soluble drugs; not fully developed in infants; alcohol and glucose can cross
Protein binding effect
Temporary storage of a drug molecule that lets a drug be available for longer periods of time; unbound drug binds to a protein and becomes bound; binding is reversible and unbound molecules are active and free to exert effect
Goal of dosing
Maintain a steady state of free drug concentrations
Albumin
Primary blood protein that molecules bind to
Hypoalbuminemia
Low protein levels cause by liver disease or malnutrition; more free drug availability and higher chance of overdose and toxicity (drugs that bind highly to proteins will have a stronger effect on people with low protein levels like Coumadin)
Metabolism (biotransformation)
Method by which drugs are inactivated into metabolites; liver converts lipid-soluble drugs into water-soluble metabolites so the kidneys can excrete them