CHAPTER 2 Flashcards
a drug that activates a receptor by binding to the receptor (a protein) is
an agonist (combination usually reversible)
when the receptor is bound to this…. the effect of the drug is produced
agonist ligand
what is an antagonist
a drug that binds to the receptor without activating the receptor
how do antagonists block the action of agonists
by getting in the way of the agonist, preventing the agonist from binding to the receptor and producing the drug effect
this is present when increasing concentrations of the antagonist progressively inhibit the response to the agonist
competitive antagonism
this is present when, after administration of an antagonist, even high concentrations of agonist cannot completely overcome the antagonism
noncompetitive antagonism
what is one of the many mechanisms that contribute to variability in response to drugs
changing receptor numbers
where are most of the receptors that are most critical for anesthetics interaction located (opioids, IV sedative hypnotics, benzos, beta blockers, catecholamines, & muscle relaxants)
lipid bilayer of cell membranes that interact with membrane bound receptors
what are the other receptors that interact with insulin and steroids
intRAcellular proteins
how do proteins function in the body
catalyze enzymatic reactions & act as ion channels
how does a drug like propofol enhance the receptor activity
increases the sensitivity to the y(gamma)-aminobutyric acid receptor [GABAa] to GABA, the endogenous ligand
what receptor does ketamine decrease the activity of
N-methyl-D-aspartate (NMDA)
what is another way decrease receptor activity
triggering a chain reaction (ex: opioid binding to the u-opioid receptor activates an inhibitory G protein that decreases adenylyl cyclase activity)
what is responsible for the drug effect
the protein’s response to binding of the drug
