W4-2 Pharmacodynamics Flashcards
Agonist
Activates biochemical events, “evokes response”
Most common second messenger system
G-protein coupled receptors
Best known pharmacologic interaction mechanism
Ligand-gated ion channels
Pharmaceuticals often bind ________ proteins in order to ________ transcription
chaperone, inactivate
Major reason for drug-drug interactions
Overlapping 2nd messenger systems
Two types of drugs that do not interact with receptors
Chelating agents
Volatile anesthetics
Antimetabolites
Interfere with DNA/RNA synthesis
What is EC50?
The amount of drug needed to elicit 50% of the maximal response
Affinity
1/Kd (1/dissociation constant)
Potency
Compares relative drug strengths
Antagonist
Inhibits action of agonist, efficacy alpha = 0
Quantal Dose Effect
Population response, “all or nothing” response over very narrow concentration range
Tachyphylaxis
Hyporeactivity induced rapidly after a few doses
Therapeutic index
TI=LD50/ED50
Higher is better
Cyt P-450 types for codeine metabolism
More 2D6 than 3A4
Quinidine reduces 2D6
Grapefruit juice reduces 3A4