Term
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Definition
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Term
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Definition
Slow response
-alpha and beta adrenergic, cholinergic, 5-HT, RTK (receptor tyrosine kinase) |
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Term
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Definition
Point where at which receptors can be indirectly affected
-PDE (phosphodiesterases that metabolize cAMP and cGMP)
-AchE (Acetylcholinesterases)
-COX (cyclo-oxidases which break arachidonic acid into PG, PC and TX) |
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Term
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Definition
Direct (act on the receptor)
Indirect (increase agonist by acting as a PDEI/phosphodiesterase inhibitor, AchEI/acetylcholinesterase inhibitor or transport (reuptake) inhibitor.) |
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Term
| PDE III selective inhibitors |
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Definition
| end in -rinone (Am-rinone) except enoximome |
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Term
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Definition
block the receptor, decrease activation
ex: propranolol (beta), naloxon (opioid), flumazenil (benzodiazepin), atropine (Ach) |
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Term
1) Partial agonist
2) Inverse agonist |
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Definition
1) Weaker response than agonist
2) Opposite response as agonist (ex: cAMP down instead of up) |
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Term
| Cytosol/nuclear drug examples |
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Definition
| Steroids, T3/T4, Vitamin A/D, Fibrates and Glitazones |
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Term
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Definition
| First concentration where the drug response is greater than zero. |
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Term
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Definition
| Half maximal effective concentration, measure of potency that is halfway between zero and the max response (in vivo) |
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Term
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Definition
| concentration of drug required for 50% inhibition (in vitro) |
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Term
| Therapeutic index (or ratio) |
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Definition
LD50 (lethal dose for 50% of population)/ED50 (minimum effective dose for 50% of population)
(500 would be safe and effective even at high amounts, 1 would not be safe at an effective concentration) |
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Term
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Definition
| The difference between LD50 and ED50. If the numbers are close, then therapeutic dose monitoring (TDM)is required. Ex: digoxin and lithium |
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Term
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Definition
| If the curve of a drug's concentration vs. response is more to the left, it is more potent. If its max response is greater, it is more efficacious. |
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