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Pharm 1 - SP19 > Receptors and basic pharm > Flashcards

Receptors and basic pharm Flashcards

1
Q

the -olol suffix defines drug as a _

A

beta blocker

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2
Q

How many FDA approved drugs are there

A

3000-6000

point being too many

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3
Q 
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
A
  1. heart disease
  2. cancer
  3. chronic lower respiratory disease
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4
Q

drugs exert their effects by binding to a _

A

a receptor (protein)

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5
Q

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

A

signal transducer

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

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6
Q

drugs that actively produce a physiological effect are called _

A

agonists

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7
Q

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

A

antagonists

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8
Q

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

A

a rectangular hyperbola

that has practical implications that we should know

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9
Q

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

A

gets very high

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10
Q

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

A

the concentration of a drug providing 1/2 maximal binding

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11
Q

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

A

sigmoidal curve

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12
Q

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

A

receptor proteins

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13
Q

the drug _ stimulates salivation by the submaxillary gland

the drug _ blocks this effect

A

pilocarpine

the drug atropine blocks this effects

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14
Q

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

A

receptor theory

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15
Q

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

A

muscarinic acetylcholine receptors

this is why muscarininc antagonists (blockers) can produce xerostomia

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16
Q

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

A

muscle substance

curare

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17
Q

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
A
  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
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18
Q

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

A

Kd (dissociation constant =

concentration R x concentration of L divided by concentration of RL

19
Q

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

A

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.

20
Q

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 _

A

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

21
Q

as Lf approaches infinity, RL/Rt apprroaches 1

what does this mean

A

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

22
Q

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

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

A

1/2 maximal binding

23
Q

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

A

L1

24
Q

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

A

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

25
Q

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

A

semilog plot

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

26
Q

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

A

potency

27
Q

law of mass action describes the _ of drugs

it does not accurately describe quantitative aspects of drug _ thus we use the concept or EC50

A

binding of drugs to receptors

not good at drug action

28
Q

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 _

A

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

29
Q

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 _

A

delta0.5 = 1/2kRt

this leads to a dose response curve

30
Q

Ec50 is defined as the _

A

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

31
Q

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

A

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

32
Q

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

A

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

33
Q

drugs with no efficacy are _

A

antagonists

34
Q

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

A

the concentration dependence of drug action

efficacy

35
Q

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.
A

binding affinity and its efficacy (ability of drug to confer response)

  1. partial agonists
36
Q

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

A

drug action

37
Q

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

A

efficacy

38
Q

isoproterenol is the first _

A

beta selective agonist

39
Q

adrenalin(epi) has _ and _ effects

2 receptors
2 agonists

A

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)

40
Q

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

A

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

41
Q

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

A

by their pharmacology

42
Q

adrenergic receptor AR

alpha and beta AR receptors what are they

A 
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

43
Q

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
A

gene family

Pharm 1 - SP19 (26 decks)

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