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9 Cards in this Set

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  • Back
Why are log scales popular in pharmacology?
The log-scale dose-response curves tend to accentuate the the more interesting elements of the curve.
What are three ways to express the potency/apparent affinity of a drug?
EC50 - the effective concentration, 50%
Kd - the apparent dissociation constant of the drug
IC50 - inhibitor/antagonist conc'n. at 50% reduction of activity
If a drug's Kd and EC50 are the same molar amount, what does it say abou the receptor population being studied?
When Kd = EC50, the receptors are 100% bound.
How is Kd defined?
Kd = ( [D] * [R] ) / [DR] = k2/k1

* k2 = dissociation rate
* k1 = association rate
What are three major components of drug action?
1) Route of administration
2) Receptor affinity
3) Effect of receptor/ligand interaction
How is a competitive antagonist defined?
Competitive antagonists have all the accessibility and affinity, but none of the intrinsic activity.
When does an agonist become an antagonist?
Partial agonists become antagonistic when introduced against full-fledged agonists.
What drug constant forms the basis for therapeutic selectivity?
A drug's Kd across a spectrum of receptors will determine its therapeutic selectivity in the body.
What are spare receptors?
If a receptor pool has yet to saturate, but has reached its maximum response rate, any additional receptors in the pool are said to be "spare." Additional drug/ligand pairs will not enhance the response.