W1D3H4 - Pharmacology: Dose/Response/Therapeutic window

Question 1

competitive antagonist

Answer 1

• reversibly binds at active site (same site as agonist)
• prevents agonist from activating receptor
• decreases potency (increases EC50)
• surmountable: can be overcome by flooding system w/ agonist. Emax (and therefore efficacy) stays same.

Question 2

noncompetitive allosteric antagonist

Answer 2

• binds reversibly or irreversibly at allosteric site (different site from agonist)
• no effect on agonist potency
• decreases agonist efficacy

Question 3

noncompetitive active site antagonist

Answer 3

• irreversibly binds at active site (same site as agonist)
• no effect on agonist potency
• decreases agonist efficacy

Question 4

physiological antagonist

Answer 4

• binds at a different receptor from agonist

- produces opposite physiological effect from the agonist

Question 5

chemical antagonist

Answer 5

• does not interact with a receptor
• interacts directly with the agonist
• removes the agonist from the system, or prevents the agonist from binding to its receptor

Question 6

allosteric modulator

Answer 6

• binds to a site different from agonist
• increases or decreases the affinity of the agonist for the receptor
• OR increases or decreases the level of receptor activation after agonist binding

Question 7

therapeutic index

Answer 7

dose of toxic effect/dose of therapeutic effect

higher the TI, safer the drug

Question 8

therapeutic window

Answer 8

• range of drug dosages that can be used for treatment while staying within the safety range
• from minimum effective dose to minimum toxic dose