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32 Cards in this Set

  • Front
  • Back
concentration vs time
PK
Concentration vs effect
PD
Effect vs time
pk/pd
PD: what the _____ does to the______.
Drug, body
Orthosteric interactions
Same site as ligand
Allosteric interactions
Different site than ligand
Antagonism that is surmountable, whether allosteric or orthosteric. Depends on concentration of antagonist and agonist. Requires more ligand to get the effect. Freq at orthosteric site.
Competitive antagonism
Antagonism that is non-surmountable. Binds at either site and alters the max amount of response available b/c the amount of ligand does not affect it.
Non-competitive antagonism
Example of non-competitive antagonist.
Ketamine-nmda receptor, binds at allosteric site, inhibits NT glutamate
Complementary effects: amino glycosides and ?
NDNMBs
PK interactions: what the ______ does to the _______.
Body, drug
PK can involve alterations in:
ADME
_______ determines a drug's duration and intensity of action; also the onset of action in target organ.
Systemic absorption
________ absorption is determined by: surface area avail of capillary membranes to absorb drug; drug's solubility in ISF; aqueous channels in vascular endothelium (watch for d/o of vascular health)
Parenteral
Theoretical volume each drug is distributed into after administration:
Vd
______ is influenced by: lipid solubility, plasma protein binding, and molecular size.
Distribution
First-pass pulmonary uptake can be significant (>65% of dose) for basic lipophilic amines:
lido, propanolol, demerol, fentanyl, sufent, alfent
Parenteral drugs are present dissolved in ____ or bound to ______.
Plasma; protein carriers
The ______ fraction is physiologically active.
Unbound
Highly ______ receive quite a large amount of total dose.
Perfused tissues
Alkaline drugs generally bind to:
alpha 1-acid glycoprotein
Acidic drugs generally bind to:
albumin
Alterations in protein binding _____ is important for drugs that are highly protein-bound.
Capacity
_______ principal phenomenon behind awakening following single doses of anesthesia induction agents.
Redistribution
Drug leaves the brain to less well perfused tissues without sites of ____; pt awakens. Drug is not out of body.
Action
_______ depends on: blood flow, concentration gradient, BBB and its integrity, physiochemistry of the drug (protein binding, lipid solubility, ionization), tissue mass avail, tissue solubility towards the drug, and pH issues.
Tissue distribution
Metabolism of drugs occur primarily in the ____ when it is organ dependent.
Liver
Drugs may be metabolized in the plasma by:
Plasma esterases, Hoffman elimination
Phase I reactions tend to make the drug molecules more _____ and easier to eliminate.
Polar
Drugs may be active or inactive after ______ rxns.
Phase 1
Phase II reactions are _______ which freq inactivates drugs and readies them for excretion.
Conjugation rxns
Slow acetylators means the drug:
hangs around in the body