basics-idk
What is first-pass effect?
drugs are extensively converted to inactive metabolites during first pass through the gut wall and liver, and have low bioavailability
what graph is curved, what graph is straight?
first order- curved
zero order- straight
selective vs non-selective
selective- acting at a specific receptor in the body in specific organ
non-selective- can act in multiple receptors(organs) in body
does potency increase to the left or right?
to the left
what is tolerance and what are its mechanisms?
chronic, larger doses are required to produce same effect.
1.receptor down-regulation
2.decreased affinity
What organs are linked to metabolism and elimination?
metabolism- liver
elimination- kidney
List in order of highest to lowest bioavailability
oral, intravenous, subcutaneous, intramuscular, sublingual
intravenous, subcutaneous, intramuscular, sublingual, oral
difference between efficacy and affinity
efficacy- how well the drug is working, ability to initiate effect
Affinity- how well is drug binding to a particular receptor
does efficacy increase up or down?
up
what is receptor desensitization?
repeat exposure-> phosphorylation-> receptor changes conformation and becomes desensitized.
what is a agonist & antagonist
Agonist- activates receptors in physiological systems so the drug effects mimic physiological activation. Acts on site of receptor to produce desired effect
Antagonist- blocks receptors or enzymes in physiological systems, the effects are opposite of the normal response
Does first order kinetics have a non-constant or constant half life?
constant
ED50 vs LD50
ED50- dose that produces 50% of max response
LD50- dose that produces 50% death
what does Z represent?
(kris has pic)
non-competitive antagonist
what is a partial agonist?
give an example.
cannot produce the full effect even at a high dose
buprenorphine
what are G-protein coupled receptors?
Work on the outside of the cell- when activated it activates signals on the inside of the cell.
Define each:
Cmax, Tmax, MEC, AUC, duration of action
Cmax- max drug concentration
Tmax- time needed to reach the maximum
MEC- minimum effective concentration
AUC- (area under the curve) measure of total amount of drug during the time course
Duration- how long drug lasts
Therapeutic index equation
LD50/ED50
what does Y represent?
(kris has pic)
competitive antagonist
After chronic exposure to agonists, which of the following occurs?
a. desensitization
b. up-regulation
c.down-regulation
d. supersensitivity
down regulation
Difference between Pharmacokinetics and Pharmacodynamics....
Pharmacokinetics- what the body does to the drug (movement)
Pharmacodynamics- what the drug does to the body (mechanism of action)
What impacts the time for a drug to reach steady state?
half-life
non-competitive inhibition vs competitive inhibition
non-competitive= drug is acting at a different site, changing the conformation
Competitive= drug is acting at the active site of the enzyme, can overcome by adding more substrate.
what does doubling a half-life do?
it takes twice as long for the quantity to decrease by half.
True or false
The smaller the space in a therapeutic index the more lethal the drug can be in smaller doses.
true