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What is the fundamental principle of pharmacodynamics? |
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Drugs can only modify underlying biochemical or physiological process.
drugs can NOT "create" effects. |
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A drug-receptor complex is necessary to invoke a(n) ... |
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Drug receptors are very.. |
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Drugs (ligands) interact with |
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enzymes, nucleic acids, and membrane receptors |
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Desensitization occurs when |
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Definition
you have too much drug hitting a receptor and you develop a tolerance.
Causes cells to protect themselves from too much drug. You lose the therapeutic affect.
this is a pharmacodynamic response |
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Term
Receptor Occupancy Theory |
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Definition
the magnitude of the effect is assumed to be directly proportional to the [drug]
Basically, the more drug, the more effect
Effect = Rmax x [D]/ Kd + [D] |
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Receptor interaction not static, rather on/off interaction |
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A Dose-Response Curve (DRC) plots.. |
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Definition
the dose of a drug vs. the effect
it is a semi-log plot |
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A Drug-Receptor (D-R) curve shows |
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Definition
potency, efficacy, and slope |
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Term
What are the two molecular properties drugs are classified on, according to their magnitude? |
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Definition
1. Affinity for the receptor (potency) 2. Efficacy once bound to the receptor |
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Definition
AFFINITY for the receptor and EFFICACY Triggers 100% response
it binds to a receptor and elicits a response
Ex: Adrenaline causes 100% bronchial dilation |
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affinity and low efficacy
Ex: Ibuterol. Doesn't give 100% bronchial dilation |
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the maximal response produced by a drug |
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Definition
Effective dose concentration How much drug is required to elicit desired response
Usually the ED50 |
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Clinically, a drug that is more _ is more important than a drug that is _ |
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A maximum agonist response can be achieved in the presence of a competitive antagonist if.. |
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Definition
given at a high enough dose |
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Competitive antagonism shifts the agonist D-R Curve to the right/left? |
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Definition
Right. it decreases the potency, therefore requiring a larger drug concentration to overcome the agonist and achieve the desired affect |
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An agonist can never overcome a _ antagonist |
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Definition
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Factors that affect drug response |
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Definition
resistance, tolerance, tachyphylaxis |
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Definition
a decrease in drug response during repeated administration |
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ACUTE development of tolerance due to rapid repeated administration of some drugs |
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Pharmacokinetic Tolerance is due to what? |
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Definition
a decrease in [drug] at its site of action
Ex: barbiturates, alcohol, phylbutazone |
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Term
Pharmacodynamic tolerance is |
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Definition
the reduced responsiveness to the drug at its site of action Ex: amphetamine, caffeine, nicotine, morphine, barbiturates, alchol
usually drugs that affect behavior or psychological outlook |
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Term
Dose-Response Curve: Quantal responses |
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Definition
Shows the frequency with which a defined effect occurs in a population at a given dose
can express the cumulative frequency with which an effect occurs in a population at a given dose and all lower doses Instead of measuring the degree of response, it measures # of people who have a therapeutic response at some level |
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frequency of desired response and toxic response at various doses
Therapeutic Index = toxic dose/ effective dose |
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small increase in dose is more likely to produce toxic effect |
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large increases in dose are less likely produce toxic effect |
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