General PK/PD

Question 1

What is an agonist

Answer 1

ligand that has same effect on receptor as the endogenous ligand

Question 2

What is an antagonist

Answer 2

ligand that blocks the receptor, neither decreases or increases activity of the receptor

Question 3

what are receptors made out of

Answer 3

large proteins (AAs), some polar some nonpolar

Question 4

3 main types of bonds for drugs? which is the strongest)

Answer 4

covalent ( strongest in aq environment) , electostatic (aka ionic), hydrophobic (weakest)

Question 5

what is a racemic drug?

Answer 5

mix of r/s isomers

Question 6

difference between orthosteric and allosteric binding

Answer 6

ortho: drug binds to same site as endogenous ligand
allo: binds to somwhere else on surface of receptor (can be active or inert)

Question 7

difference between competitive and noncompetitive binding

Answer 7

competitive: bind and inhibit agonist response (can still have same response as agonist, but you need to give a lot more of the drug to see effect)(is surmountable)

noncompetitive: insurmountable because drug binds on allosteric site, changing the shape of the receptor

Question 8

what is a partial agonist?

Answer 8

will bind to same receptor as agonist, but can never reach full effect that pure agonist would elicit.
can act as a full antagonist in presence of full agonist

Question 9

what is an inverse agonist?

Answer 9

further drives the response lower than constitutive activity

Question 10

which plasma proteins bind to drugs in blood stream?

Answer 10

albumin= acidic drugs
alpha 1 acid glycoprotein= basic drugs
lipoproteins= neutral drugs