Term
| what bonds are necessary to initiate drug-receptor interactions |
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Definition
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Term
| some drugs bind to receptor covalently, this cause long duration of actions. what are some examples? |
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Definition
| phenooxybenzamine,aspirin (COX inhibitor) |
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Term
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Definition
| extra or intracellular macromoleculs that mediate biochem and physiological interactions. |
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Term
| drug receptor theory says |
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Definition
| cellular response is directly proportional to fraction of receptors bound or occupied by the drug. |
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Term
| Law of Mass Action has the following assumptions |
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Definition
1. reverisble interaction
2. receptor exists in only two states
3. drug must bind to each receptor with equal affinity |
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Term
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Definition
| drug conc when half of the receptors are occupied by the drug |
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Term
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Definition
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Term
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Definition
| a proportion rather than a finite number. |
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Term
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Definition
| drug conc that causes half the maximal effect |
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Term
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Definition
| the lower the EC50, the more potent the drug |
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Term
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Definition
| ability of a drug-receptor complex to produce a functional response. |
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Term
| full agonist have an efficacy of ... |
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Definition
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Term
| Antagonists have efficacies of... |
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Definition
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Term
| what type of graph is used to measure EC50 and drug efficacy? |
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Definition
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Term
| what are the three classes of antagonists? |
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Definition
| pharmacological, chemical, and physiological |
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Term
| pharmacological antagonists have ... |
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Definition
| no net effect of the receptor. it has eqaul affinity for the active and inactive receptor confirmations |
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Term
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Definition
| interact directly with the drug. |
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Term
| eg of chemical antagonist |
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Definition
| protamine binds to heparin and neutralizes it, not allowing it to induce a response |
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Term
| physiological antagonists |
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Definition
| act on a site different from the receptor on or in the same cell. |
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Term
| non-competitive antagonists cause... |
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Definition
| a downward shift to the dose response curve. |
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Term
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Definition
| not all receptors must be bound to observe maximal response. |
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Term
| eg of spare receptor system. |
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Definition
| the heart has spare beta-1 receptors. this allows full response to NE even if there is an irreversible antgonist blocking some of the receptors. |
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Term
| What does the spare receptor system tell u about Kd and EC50. |
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Definition
| Kd and EC50 are not always the same. in a spare system the EC 50 is lower than Kd. |
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Term
| What mechanisms have spare receptor systems? |
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Definition
| GPCR, RTKs, and cytokine receptors |
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Term
| What is a quantal dose-response relationship? |
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Definition
| the average amount of drug to reach max effect in 50% of a population. |
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Term
| What is the TI-therapeutic index? |
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Definition
| a ratio of TD50 to ED50 (TD50/ED50) |
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Term
| what does a high TI value signify? |
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Definition
| that the difference bw effective dose is much smaller than the toxic dose. |
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Term
| what are examples of drugs with low TI? these must be closely monitored. |
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Definition
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