PHARMACOLOGY MIDTERM Flashcards
the study of what the body does to the drug.
- processes of drug undergoes as it reaches and leaves the site of action
PHARMACOKINETICS
movement of drugs from an area of HIGH TO LOW CONCENTRATION WITHOUT ENERGY requiring.
PASSIVE DIFFUSION
measure of the rate and extent of drug into the systemic circulation
BIOVAILABILITY
where does most drug metabolism occur?
LIVER
a family of enzymes that play a key role in phase 1 metabolism
CYTOCHROME
drug administration equals the rate of elimination, typically 4-5 half-lives.
STEADY STATE
higher initial dose of drug given to quickly reach therapeutic levels
LOADING DOSE
constant drug
16%
most drug
curve graph
1ST ORDER
non constant drug
independent concentration
25% - 50%
straight graph
ZERO ORDER
to determine duration of action steady state concentration
HALF- LIFE
drugs move from high to low concentration with the HELP OF CARRIER PROTEINS but NON ENERGY REQUIRING
Ex; VITAMIN B12
FACILITATED DIFFUSION
the movement of drugs across membranes against the concentration with the ENERGY REQUIRING
ACTIVE TRANSPORT
process where large drug molecules are ENGULFED by the cell membrane
ENDOCYTOSIS
it is a CELL DRINKING
PINOCYTOSIS
it is a CELL EATING
PHAGOCYTOSIS
measures of HOW MUCH
- most important
AUC
UNMASK a polar functional groups
PHASE 1
ADDITION of polar group.
PHASE 2
release of drug from the dosage form
LIBERATION
pharmacotechnical factors of liberation
- DISINTEGRATION
- DISSOLUTION
movement of GI concentration to the small intestine.
GET
drugs that increase GI motility
- METOCLOPRAMIDE
- DOMPERIDONE
drugs that decrease GI motility
- ANTICHOLINERGICS
- OPIOIDS
allows determination of the absolute amount of drug absorbed from an EXTRAVASCULAR administered drug product.
ABSOLUTE BIOVAILABILITY
two or more different dosage forms given by the same route of administration
RELATIVE BIOVAILABILITY
maximum plasma concentration reached.
most variable
CMAX
time it takes to reach the Cmax.
least important
measure of rate
TMAX
similarity of the BA of a drug (generic) to the BA of another drug taken as the standard (innovator)
BIOEQUIVALENCE
REVERSIBLE TRANSFER OF DRUG from the systemic circulation to the site of action.
DISTRIBUTION
fraction of the cardiac output that reaches a specific tissue or organ
REGIONAL BLOOD FLOW
hypothetical (apparent) volume of the body fluids required to dissolve a given amount of drug to a concentration equal to that of plasma concentration
VOLUME IOF DISTRIBUTION
active, ADME
unbound (free) drug
ADME
bound drug
Acidic drug
ALBUMIN
basic drug
ex drug: Globulin
ALPHA 1- ACID GLYCOPROTEIN
hormones drug
GLOBULIN
aka. biotransformation
- primary objective to convert a drug to INACTIVE, NONTOXIC, POLAR/WATER-SOLUBLE
METABOLISM
initial metabolism before the drug reaches the systemic circulation
effect: decrease biovailability of drug
FIRST PASS EFFECT/ FIRST PASS METABOLISM
valproic acid
isoniazid
acute alcoholism
azole antifungals
fluoroquinolones
inhibitors of?
ENZYME INHIBITOR
decrease metabolism activity
ENZYME INHIBITION
increase metabolic activity
ENZYME INDUCTION
phenytoin, phenobarbital
rifampicin
carbamazepine
griseofulvin
chronic alcoholism
ENZYME INDUCERS OF enzyme induction
carboxylic acids
salicylic acid
benzoic acid
glycine conjuction of phase 2
macrolide, amiodarone, CCB, azole antifungals, proteases inhibitor, antihistamine
CYP3A4
codeine, dextromethorphan, most antidepressant and ANTI-PSYCHOTICS, debrisoquin
CYP2D6
phenytoin, sulfonylureas, S- Warfarin
CYP2C9
propranolol, PPI, clopidogrel
CYP2C19
acetaminophen, theophylline, caffeine
CYP1A2
what are the 4 main processes of pharmacokinetics?
- absorption
- distribution
- metabolism
- elimination
the drug is absorbed into the bloodstream
absorption
name 4 ways drugs are absorbed
- passive diffusion
- facilitated diffusion
- active transport
- endocytosis
the process of removing the drug from the body, primarily through the kidneys, liver, and bile.
drug elimination
mnemonic helps remember the important ENZYME INDUCERS in drug metabolism
PCRABS - phenytoin, carbamazepine, rifampin, alcohol (chronic use), barbiturates, St. Johns Wort
mnemonic helps remember the important ENZYME INHIBITORS in drug metabolism
GPACMAN - grapefruit, protease inhibitors, azole antifungals, cimetidine, macrolides, amiodarone, non -dihydropyridine calcium channel blockers (diltiazem, verapamil)
mechanism of drug movement across the cell membrane
transport process
