Basic pharmacology Flashcards
What the body does to the drug
Examines the movement and modification of drug over time through the body
Pharmacokinetics
What the drug does to the body
The study of drug-receptor interaction and biological effects
Pharmacodynamics
Pharmacokinetics:
Absorption
Distribution
Metabolism
Elimination
Phase I
Reduction, oxidation, hydrolysis
Yields slightly polar, water-soluble metabolites (active or inactive)
Cytochrome P450
Non-cytochrome P450
Flavin-containing monooxygenase enzymes
Phase II
Conjugation
Yields VERY polar, inactive metabolites that can be easily excreted by kidneys
Glucuronosyltransferases
Glutathione-S-transferases
N-acetyl-transferases
Sulfotransferases
Geriatrics lose which phase first?
Phase I
Drug’s ability to initiate a response after binding to a receptor
Intrinsic activity
Drug has an affinity for a receptor and stimulates it
Full agonist
Drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor as compared to a full agonist
Partial agonist
Drug has an affinity for a receptor but displays little or no intrinsic activity
Antagonist
Competes with agonist for receptor sites, occupies the receptor site- no reaction
Competitive antagonist
Binds to the site other than receptor site and changed the shape of receptor- no reaction
Non-competitive antagonist
Drug acts on a variety of receptors
Nonselective
Efficacy
Maximal effect a drug can produce
Ability of the drug to activate the receptor once it is bound
Potency
Amount of drug needed for a given effect
Depends on:
affinity to receptor
Amount of administered drug that reaches the receptor site
Drugs with _____ ED50 is more potent than the drug with _____ ED50
Low, high
Cell engulfing drug particles
Pinocytosis
More highly protein bound an agent is, the more difficulty it has _____?
Disassociating from the sodium channel.
Causes longer duration of action
Protein bound or unbound can readily cross cell membranes?
Unbound
The free fraction determines the concentration of bound drug on the receptor
Volume of distribution
The volume of total body fluid into which a drug “appears” to distribute
(Amount of drug administered mg) /
(Plasma drug concentration mg/L)=?
Volume of distribution
What is the 60-40-20 rule?
TBW is 60% of body weight
ICF is 40% of body weight
ECF is 20% of body weight
Plasma osmolarity=
2(Na+) + 0.055(glucose) + 0.36(BUN)
Nondepolarizing NMB bind to plasma proteins and are poor lipid soluble, therefore have high plasma concentrations and ____ volume distribution
Low