Pharmacodynamics Flashcards
Pharmacodynamics
What Meds do to the Body
- Most drugs bind to cell receptors where they initiate reactions that alter cell’s physiology
- Some of a drug’s molecules will find target cell, some distributed, metabolized, and excreted
- Drugs exert primary action at cell level
Medication Actions
Pharmacology at
cell level, organism level, and population level
Drug Receptors
- Proteins/Glycoproteins on cell surface, organelle inside cell, or cytoplasm
- Finite mumber - response plateaud once saturated
- Downregulation/Upregulation
What happens after a drug is bound to the receptor?
- Ion channel opens/closes
- Activate biochemical messengers, second messengers (cAMP, cGMP, C++, Inositol Phosphates) - each signal that passes amplified
- Inhibit/Initiate normal cell function
- Steroids move right into cell w/o help
What is Affinity
Strength of binding b/t drug and receptor
Dissociation Constant (Kp)
Measure of a drug’s affinity for a given receptor.
The concentration of a drug needed for 50% receptor occupancy
What is an Agonist
Drugs that alter physiology of a cell by binding to plasma membrane or intracellular receptors
What is a Strong Agonist
Agonist that causes max effects even though it only occupy a small fraction of receptors
What are Weak Agonists
Agonists that need to be bound to many more recptors than a strong agonist does to produce same effect
Partial Agonist
Drug that fails to produce max effect even when all receptors are occupied
What is an Inverse Agonist
Binds to receptor and causes opposite of an agonist. Doesnt block anything from happening, it just reverses what happens
EX: H2 receptor antagonist
What is an Antagonist?
Inhibit/Block actions caused by agonists
Competetive Antagonist
Competes with Agonist for Receptors
- Agonist cant bind to receptor while its occupied by antagonist
- Antagonism can be overcome by high doses of agonists
- EX: Reversal agents
Noncompetitive Antagonist
Binds to site other than the agonist-binding domain.
- Induces form change in receptor so that agonist no longer recognizes agonist binding domain
- Insurmountable - high doses cant defeat this antagonism
- EX: Warfarin
Irreversible Antagonism
Agents compete with agonists for the agonist-binding receptor
- Antagonists bind permanently to receptor
- Rate of antagonism can be slowed by high # of antagonist
Efficacy
Degree that drug is able to cause max effects
Potency
Amount of drug needed to produce 50% of max effect that its capable of causing
Potency vs. Efficacy
- Potency used to compare drugs in same class.
- Drugs in same class usually have same max efficacy
- Efficacy used to compare drugs with different mechanisms.
Drug-Response Curves
- Graphs magnitude of drug action against concentration/dose of drug needed to induce action
- Represents effects and dose of drug within individual rather than population
- Almost all meds plateau at some point
What must be tested on a drug before they are approved for marketing?
Efficacy and Safety must be tested in animal and human population studies