Term
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Definition
ability of drug to bind receptor
can only be compared when two drugs bind to same receptor (have parallel curves)
proximity to y axis, closer = greater affinity (when you have parallel curves) |
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Term
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Definition
dose required to produce a certain magnitude
closer to y axis - more potent (lower dose for same effect) |
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Term
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Definition
how well drug produces response
maximal height of curve |
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Term
| partial agonist (and example) |
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Definition
incapable of eliciting a maximal response, less effective than a full agonist
ex: Buspirone for tx of generalized anxiety without the sedation effects |
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Term
| competitive antagonist + agonist |
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Definition
| causes a PARALLEL RIGHT SHIFT of dose-response curve |
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Term
| competitive antagonist + agonist |
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Definition
causes a PARALLEL RIGHT SHIFT of dose-response curve
aka competitive inhibitor
can be reversed by increasing dose of agonist
decrease affinity, but not max response |
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Term
| noncompetitive antagonist |
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Definition
causes a NONPARALLEL RIGHT SHIFT (downward) in dose response curve
irreversible, usually covalent bonds, always supress the maximal response
can only be overcome with synthesis of new receptors
ex: aspirin, omeprazole, succinylcholine |
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Term
| drugs with therapeutic indices making them highly toxic |
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Definition
TI < 10 means drug is very toxic
*DIGOXIN*
*WARFARIN*
Lithium
Theophylline |
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Term
signaling mechanisms:
intracellular receptors |
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Definition
receptors for steroids, thyroid hormone, Vitamin D
-binding causes dimerization of hormon-receptor complex
-complex translocates to nucleus
-upregulates gene transcription and DNA replication
slower in onset but longer in duration |
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