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10 Cards in this Set
- Front
- Back
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The magnitude of the maximal effect a drug can produce is what?
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Efficacy
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___________ is a drug that binds, generally with high affinity to a particular type (or subtype) of receptor but is devoid of efficacy
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Antagonist
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________ is a drug that possesses affinity for the receptor it activates/stimulates but has lower efficacy than a full agonist.
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Partial agonist
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How are affinity and efficacy determined from a log dose-response (LDR) curve for a drug?
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The LDR curve is symmetrical at the point at which 50% of the maximum dose is elicited, this is affinity. Efficacy is reflected in the plateau of the LDR curve. Most potent drug (greater affinity for receptor) will be closer to the origin of the LDR plot and will be to the left. If dose rather than drug concentration is used for compression of potency, which is usual, then the higher the dose, the greater the response, which could result in death.
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Which pharmacodynamic parameter of an agonist is changed by the presence of a competitive pharmacological antagonist?
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When a competitive antagonist is present, the affinity of the agonist decreases. The efficacy of the antagonist remains unchanged.
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Log dose-response curves provide information on which of the following terms:
Affinity Efficacy Potency Therapeutic index Pharmacological antagonism |
Affinity - yes
Efficacy - yes Potency - yes Therapeutic index - yes Pharmacological antagonism - yes |
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What is the significance attached to the slope of the LDR curve?
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The slope of the LDR curve indicates the range of dosages over which the drug acts. Steep slope indicates a small increase in dose will produce a large change in intensity of the response. Extremely steep dose response may have important clinical consequences if the upper portion of the drug represents undesirable degree of response.
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On what pharmacodynamic parameter are potency and selectivity of action based?
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Affinity
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By which transport process do drugs penetrate the blood-CSF barrier and enter cerebrospinal fluid?
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Drug penetration takes place solely by passive diffusion.
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What physiochemical property of a drug is required for penetration of the blood-CSF barrier?
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Drug molecules must be non-ionized and free (not bound to albumin)
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