Receptors and basic pharm

Question 1

the -olol suffix defines drug as a _

Answer 1

beta blocker

Question 2

How many FDA approved drugs are there

Answer 2

3000-6000

point being too many

Question 3

top 10 causes of death in the US
1.
2.
3.
4. accidents
5. stroke
6. alzheimer's and dementia
7. diabetes
8. influenza and pneumonia 
9. kidney disease
10. suicide

Answer 3

1. heart disease
2. cancer
3. chronic lower respiratory disease

Question 4

drugs exert their effects by binding to a _

Answer 4

a receptor (protein)

Question 5

drugs bind to receptors(proteins) and receptors act as a _

Answer 5

signal transducer

they bind a ligand and send some sort of signal to the cell machinery to produce a physiological effect

Question 6

drugs that actively produce a physiological effect are called _

Answer 6

agonists

Question 7

drugs that block the action of agonists (drugs that actively produce effects)

Answer 7

antagonists

Question 8

a binding curve of drug being bound to a receptor vs. free drug concentration looks like a _

Answer 8

a rectangular hyperbola

that has practical implications that we should know

Question 9

having 100% of the receptor bound by drug is a limit approached as the drug concentration _

Answer 9

gets very high

Question 10

the dissociation constant describing drug binding to its receptor is defined as the concentration of drug providing _

Answer 10

the concentration of a drug providing 1/2 maximal binding

Question 11

semilog plots (drug bound to receptor) vs log (free drug) provide _ curves that allow a more complete range of data to be shown

Answer 11

sigmoidal curve

Question 12

a vast majority of drugs function by interacting with _ and either facilitating (agonist drugs) or blocking (anatagonist drugs) their function

Answer 12

receptor proteins

Question 13

the drug _ stimulates salivation by the submaxillary gland

the drug _ blocks this effect

Answer 13

pilocarpine

the drug atropine blocks this effects

Question 14

the beginning of the _ theory of pharmacology

A(pilocarpine)
B(atropine)
Y(receptor)

AY and BY both formed, quantity of AY and BY depending on the relative masses of A and B present and their relative affinity for Y

Answer 14

receptor theory

Question 15

pilocarpine and atropine produce their effects by acting upon _ receptor proteins of salivary glands

Answer 15

muscarinic acetylcholine receptors

this is why muscarininc antagonists (blockers) can produce xerostomia

Question 16

Nicotine acts upon the _ and not upon the axon-endings. It has been shown that _ acts upon the same muscle substance as nicotine.
since this accessory substance is the recipient of stimuli which it transfers to the contractile material. we may speak of it as the receptive substance of the muscle

Answer 16

muscle substance

curare

Question 17

in all cells two consitituents at least must be distinguished

1. substance concerned with _
2. _ especially liable to change and capable of setting the chief substance in action

Answer 17

1. substance concerned with carrying out the cheif functions of the cells, such as contraction secretion, the formation of special metabolic products
2. receptive substances

Question 18

interaction of a drug with a receptor is based on the law of mass action which is

Answer 18

Kd (dissociation constant =

concentration R x concentration of L divided by concentration of RL

Question 19

interaction of a drug with a receptor is based on the law of _

Answer 19

the law of mass action

the proposition that the rate of a chemical reaction is directly proportional to the product of the activities or concentrations of the reactants.[1] It explains and predicts behaviors of solutions in dynamic equilibrium. Specifically, it implies that for a chemical reaction mixture that is in equilibrium, the ratio between the concentration of reactants and products is constant.

Question 20

description of how a plot of drug (L) bound to receptor (R) vs. drug concentration (L) should look

[RL] = [Rt][Lf]/(kd+[Lf])

[RL]/[Rt] = _

thus, 10% to 90% binding takes place over a _ fold concentration range, with 50% binding taking place when the free ligand concentration is equal to the _

Answer 20

law of mass action

= fraction bound
or = [Lf]/9kd+[Lf])

y=x/(c+x)
rectangular hyperbola

over an 81 fold

50% binding when free ligand concentration is equal to kd

Question 21

as Lf approaches infinity, RL/Rt apprroaches 1

what does this mean

Answer 21

once the drug concentration is high enough basically all of he receptor will contain bound drug

Question 22

at RL/Rt = 1/2 , Lf=kd

by definition, the equilibrium or dissociation constant describes the drug concentration required for _ binding to the receptor

Answer 22

1/2 maximal binding

Question 23

is it possible that to drugs L1 and L2 act at the same receptor site but require vastly different concentrations to achieve the same effect?
absolutely. the amount of drug bound to the receptor would depend on both the concentration of drug available for binding as well as the Kd. if drug L1 has a much higher kd than drug L2, more of drug _ will be required to achieve binding equivalent to that of the other

Answer 23

L1

Question 24

if X amount of drug produces a certain effect, 2X amount of drug will produce roughly twice as much of an effect?

Answer 24

no
it depends where you are on the binding curve, if the amount of drug bound to the rececptor is low, doubleing the amount of drug will indeed roughly double the amount of drug bounr to the receptor and could roughly double the effect, however if the amount of drug bound to the receptor is high, doubling the amount of drug would have very little effect

Question 25

graph used to express data over a 1000-fold o more range of drug concentration

Answer 25

semilog plot allows one to plot the full range of results. rectangular hyperbola turns into the familiar sigmoidal plot

Question 26

_ refers to the relative ability of a drug to confer an effect, is a combo of affinity and efficacy

Answer 26

potency

Question 27

law of mass action describes the _ of drugs | it does not accurately describe quantitative aspects of drug _ thus we use the concept or EC50

Answer 27

binding of drugs to receptors not good at drug action

Question 28

Delta = k[Rt][D] / EC50+ [D} this is a representation of dose response data this equation predicts the same shape as the law of mass action when you plot _ vs _ the most important difference is the term _

Answer 28

drug concentration vs effect term EC50 delta - a quantitative representation of the pharmacological effect k[Rt] - represents the pharmacological effect is a function that relates to the amount of receptor(R) and that the max effet is a fxn that relates to the total amount of receptor EC50 - refers to the dose of drug that produces 1/2 max effect [D] - refers to the concentration of drug

Question 29

Delta = k[Rt][D] / EC50+ [D} if delta describes a pharm effect, this equation is sating a max effect is observed when the [D] greatly excedds the EC50 [D]>> EC50 then, deltamax ~kRt there is a max pharm effect, once the drug concentration reaches a certain level addition of more drug does not produce an additional effect if the [D] is equal to the value of EC50 then _

Answer 29

delta0.5 = 1/2kRt this leads to a dose response curve

Question 30

Ec50 is defined as the _

Answer 30

EC50 = [D] that provides 1/2 maximal effect

Question 31

is EC50 the same as Keq since the former produces 1/2 max effect and the latter produces 1/2 max binding to receptor?

Answer 31

no because sometimes (often) one observes 1/2 max effects at less than 1/2 max binding thus EC50 can be less than or equal to Keq

Question 32

how is it that Methadone can prodice a larger opioid effect than Buprenorphine, even when both are given at their optimum concentrations

Answer 32

methadone - full agonist buprenorphrine - partial agonist some agonist are able to activate a higher fraction of receptors than others, INDEPENDENT of their relative binding affinities, in fact some agonists(partial agonists) are sufficiently poor at activation that their best is not good enough to achieve the maximum effect that other agonists (full agonists) can achieve

Question 33

drugs with no efficacy are _

Answer 33

antagonists

Question 34

binding affinity is one factor that determines the _ dependence of drug action. the ability to confer the response (known as _) is another factor

Answer 34

the concentration dependence of drug action efficacy

Question 35

potency refers to the relative ability of a drug to confer an effect 1. the potency of a drug ([D] range where it works) is determined by both its _ and _ 2. drugs with insufficient efficacy will be _ regardless of how well they bind to their receptor.

Answer 35

binding affinity and its efficacy (ability of drug to confer response) 2. partial agonists

Question 36

binding affinity is one factor that determines the concetration dependence of drug _

Answer 36

drug action

Question 37

the ability to confer the response _, is another factor that determines the concentration dependence of drug action

Answer 37

efficacy

Question 38

isoproterenol is the first _

Answer 38

beta selective agonist

Question 39

adrenalin(epi) has _ and _ effects 2 receptors 2 agonists

Answer 39

excitatory effects (vasoconstriction, contraction of uterus) inhibitory effects (inhibi of uterine contraction) 2 receptors - excitatory and inhibitory 2 agonists - sympathin E(excitatory) sy,pathin I (inhib)

Question 40

there are 2 distinct types of adrenotropic receptors as determined by their relative responsiveness to a series of sympathomimetic amines closely related structurally to epinephrine the _ receptor is associated with most of the excitatory fxns and one inhib fxn the _ adrenotropic receptor is associated with most of the inhib fxnx and one excitatory fxn.. _ is the one amine which is the most active on both the alpha and beta receptors

Answer 40

the alpha adrenotropic - most excitatory, one inhib beta - most inhib and one excitatory (Ahlquist considered vasodilation inhibitory) L-epinephrine most active on both the alpha and beta the results support the theory that there is only one adrenergic neurohormone or sympathin and that sympathin is identical with epinephrine

Question 41

characterize receptors by their _ not the nature of their physiological response

Answer 41

by their pharmacology

Question 42

adrenergic receptor AR alpha and beta AR receptors what are they

Answer 42

``` alpha 1-AR ~alpha1A-AR ~alpha1B-AR ~alpha1D-AR alpha 2-AR ~alpha2A-AR ~alpha2B-AR ~alpha2C-AR ``` Beta-AR ~beta1-AR ~beta2-AR ~beta3-AR

Question 43

virtually all receptors are part of a _ one drug can elicit different effects in different contexts 1. this underscores the need for receptor specific agonists and antagonists 2. helps explain the complexity of drug action

Answer 43

gene family