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