Basic Principles I and II

Question 1

types of receptors

Answer 1

membrane bound, enzymes, structural macromolecules, intracellular macromolecules, and cell membrane itself

Question 2

reversible drug-receptor bonds

Answer 2

ionic, van der waals, and hydrogen bonds

Question 3

irreversible drug-receptor bonds

Answer 3

covalent bonds

Question 4

receptor amplification and transduction

Answer 4

fractions of seconds of drug-receptor interaction activate G protein activity that lasts for seconds

Question 5

what do G proteins regulate activity of?

Answer 5

distinct effector proteins in the cell. Act as switches that are turned on by the receptor and turn themselves off a few seconds later.

Question 6

second messenger

Answer 6

produce amplification of the drug receptor interaction. Converts an event that happens outside the cell into a change that happens inside the cell. Some second messengers can cause different effects in different tissues

Question 7

structure-activity relationships

Answer 7

the structure of a drug determines how it will fit into the receptor. The better the ffit, the better the stimulation. Sublte changes in structure amongst a class of drugs can greatly influence the drug’s effects

Question 8

dose-response relationships

Answer 8

how to measure and compare drug effects for given doses

Question 9

michaelis menten equation for drugs

Answer 9

Effect = Emax[D]/Kd + [D] Kd is dissociation constant, or the EC 50

Question 10

threshold

Answer 10

beginning of the curve. Dose of agonist at which a response begins

Question 11

slope

Answer 11

rate of rise of the response on the steep portion of the curve. Log of EC50 also relates to affinity

Question 12

maximal asymptote

Answer 12

top of curve. Represents E max for that particular agonist

Question 13

receptor occupancy

Answer 13

intensity of response is proportional to the fraction of receptors occupied

Question 14

intrinsic activity

Answer 14

ability to stimulate the receptor once bound. Relates to structure and influences efficacy and potency

Question 15

spare receptors

Answer 15

not all receptors need to be occupied in order to achieve Emax. Less efficacious agonists may need to occupy more receptors that highly efficacious agonists

Question 16

secondary receptors

Answer 16

outside of the target tissue, may mediate other effects of the drug (side effects)

Question 17

receptor regulation

Answer 17

a cell can up or down regulate a population of receptors by changing the total number of receptors or their sensitivity

Question 18

agonist drugs

Answer 18

bind to receptor and produce a pharmacologic effect. They bind to the receptor and activate the receptor after binding. Better fit to the receptor from more specific structure of the molecule results in more [DR] and an effect at lower doses

Question 19

efficacy

Answer 19

ability of the drug to activate the effector portion of the receptor once the drug is bound to the receptor

Question 20

potency

Answer 20

relates to the amount of drug that is needed for an effect

Question 21

antagonist drugs

Answer 21

block the binding of agonists and prevent the pharmacologic response

Question 22

competitive antagonist

Answer 22

can be overcome by increasing the dose of the agonist

Question 23

simple competitive antagonism

Answer 23

binding of antagonist to receptor is a weak bond and is easily reversed

Question 24

noncompetitive antagonism

Answer 24

receptors remain occupied by antagonist and not enough DR interactions occur to achieve E max. Strong bond

Question 25

pharmacokinetics

Answer 25

time course of drug absorption, actions, and elimination

Question 26

pharmacodynamics

Answer 26

types of drug actions, physiochemical and receptor interactions

Question 27

3 steps to making a drug

Answer 27

1. define physiology of the target tissue
2. create drugs that mimic endogenous agonists
3. test drugs in the target tissue

Question 28

selectivity

Answer 28

property of drug to cause a specific effect, however, few drugs only cause one effect