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Study of the biochemical and physiological effects of drugs and their mechanism of action, including the relationship between the dose (or concentration) of a drug and the effect it produces. |
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The effects of most drugs results from their reversible association with a functional macromolecular component of the cell, called what? |
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neurotransmitters, hormones, autocoids |
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What are the three types of receptors of endogenous physiological regulatory molecules? |
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Drugs that mimic the effects of endogenous ligands by interaction with the same receptors. |
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Compounds that inhibit the response of a specific agonist by competition for binding sites. |
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They have drug actions NOT mediated by receptors |
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What do these types of drugs have in common?
Antacids
Osmotic diuretics
Chelating Agents |
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100% of the receptors must be occupied |
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With the occupancy theory of drug-receptor interactions the maximal response to the system will require how many of the receptors to be occupied? |
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Which theory of drug-receptor interactions says that a maximal effect can be produced by a drug when only a small proportion of receptor is occupied? |
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What is a measure between the strength of binding between the drug and its receptor? |
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What is the maximum effect of a drug once it is bound called? |
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What refers to the different doses of two drugs that are needed to produce the same effect? |
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What is a drug capable of generating a maximal response? |
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What is a drug that will generate a response, but that response is less than the maximum? |
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What is a drug that reduces the effect of an agonist? |
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Antagonist
*it never produces a response (efficacy) |
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What type of drug will NEVER have an efficacy? |
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Therapeutic Index
*Want this ratio to be BIG - so there is a bigger gap btwn the two |
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What is the ratio between two doses of drugs, one dose that causes an effect that is 50% of the maximum and one dose that is lethal for 50% of the population? |
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What type of drug antagonism is where the agonist and antagonist are fighting for the binding site, if agonist has affinity, it will win. (can affect this by putting more agonist in) – does not change the maximal response. |
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Noncompetetive Antagonist |
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Definition
What type of drug antagonism bings to a site other than the agonist-binding domain. It induces a conformational change in the receptor.
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What type of drug antagonism has two agonists in unrelated reactions, that cause opposite effect and these cancel each other out? |
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What type of drug antagonism has two drugs that bind to one another making both inactive? |
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The inactive one
*agonists would shift it towards the active receptor |
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In the two-state model, the antagonist would shift the equilibrium towards which receptor? |
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Are beta-adrenoceptors more or less sensitive in the elderly? |
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Is the CNS more or less sensitive in the elderly? |
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