Chapter 1 - Pharmacology Basic Principles Flashcards
A drug that binds to the receptor, activates it, and causes a cellular response; elicits a response from the receptor
An agonist
A drug that will bind to the receptor but inhibit its activation, preventing a cellular response; blocks endogenous ligand from activating receptor
An antagonist
A drug that binds to the active site
Orthosteric
A drug that does not bind to the active site, but still binds to the receptor
Allosteric
ADME
Absorption, distribution, metabolism, excretion
Are allosteric agonists/inhibitors competitive or non-competitive?
non-competitive
What does it mean when an agonist is “non-competitive”?
It cannot be overcome by a drug binding to the active site to achieve the desired result
What does it mean when an agonist is “competitive”?
The agonist and inhibitor will bind to the same active site
Can a competitive agonist/inhibitor be “overcome”? Why?
Yes because the agonist and inhibitor are both orthosteric and bind at the active site on the receptor
When can an orthosteric antagonist be non-competitive with an agonist?
When the antagonist forms a bond, such as a covalent bond, with the active site on the receptor
Full agonists vs. partial agonists
Partial agonists bind with less affinity; partial agonists act as antagonists in the presence of agonists. In the absence of agonists, partial agonists produce small agonistic effects.
Define Agonist Mimic or Indirect Agonist
bind to intracellular receptors, blocking enzymatic breakdown, thus producing an agonistic effect.
EC50
The drug concentration necessary to achieve 50% of effectiveness
Kd
The drug concentration at which half of all receptors are bound.
Low Kd = high drug/receptor affinity
Shamanism
religious, indigenous practice where shamans communicate with the spirit world in an altered state of consciousness