Exam 1 - 1st half Flashcards

1
Q

Pharmacokinetics

A

what the body does to the drug

absorption, distribution, metabolism, excretion

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2
Q

Pharmacodynamics

A

what the drug does to the body

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3
Q

Properties of drugs

A

drug size
shape (stereochemistry)
reactivity
hydrophobicity

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4
Q

greater hydrophobicity means ____ ability to cross biological membranes

A

greater

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5
Q

4 types of drug-receptor interactions

A
  1. g protein couple receptors (main one)
  2. ion channels
  3. transmembrane with cytosolic domains
  4. intracellular receptors
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6
Q

g- protein coupled receptors act in ____ time

A

seconds to minutes

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7
Q

examples of second messengers (2 of them)

A

cAMP

Ca2+ phosphoionisitide signaling

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8
Q

ion channels act in ___ times

A

miliseconds (QUICK)

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9
Q

3 KINDS of ion channels

A

ligand gated
voltage gated
second-messanger regulated

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10
Q

ligand gated channels transmit signal across plasma membrane by _______ transmembrane conductance and changing ____ potential

A

ligand gated channels transmit signal across plasma membrane by increasing transmembrane conductance and changing membrane potential

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11
Q

example of ligand-gated channels

A

nicotinic ACh receptor

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12
Q

transmembrane receptors with cytosolic enzymatic domains (5 kinds)

A
  1. receptor tyrosine kinase (insulin)
  2. receptor tyrosine phosphatases (immunosuppression)
  3. tyrosine kinase -associated
  4. Ser/Thr kinases (cell growth)
  5. guanylyl cyclases (smallest family)
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13
Q

intracellular receptors (3 kinds)

A
  1. enzymes
  2. transcription factors
  3. structural proteins
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14
Q

actions of drugs NOT mediated by receptors (3 kinds)

A
  1. antiacids
  2. agents that affect osmolarity
  3. chelatic agents
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15
Q

greater potency the drug means the concentration needed for the response is

A

smaller

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16
Q

what value does potency get associated with?

A

EC50

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17
Q

the lower the EC50 the _____ the drug

A

more potent

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18
Q

the higher the EC50 the ____ the drug

A

less potent

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19
Q

Emax is known as

A

the maximum response

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20
Q

partial agonists are ____ potent than standard agonsits

A

LESS

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21
Q

antagonist is an agent that binds to a receptor but cannot produce the conformational change necessary to

A

trigger the downstream events

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22
Q

competitive antagonists bind ____ to the receptor

A

REVERSIBLY

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23
Q

With competitive antagonism what kind of shift in the curve do you see?

A

a shift to the right

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24
Q

in competitive antagonist explain what happens to efficacy and potency

A

efficacy stays the same, potency goes DOWN

25
Q

non-competitive antagonists ____ the receptor, its a ____ action

A

non-competitive antagonists inactivates the receptor, its a non-reversible action

26
Q

in non-competitive antagonist explain what happens to efficacy and potency

A

potency stays the same and efficacy goes down

27
Q

physiological antagonism

A

agonist and antagonist acting at 2 independent sites, opposite effects

28
Q

chemical antagonism is caused by combination of

A

agonist with antagonist with resulting in inactivation of the agonist

29
Q

what are the advantages to the spar receptors

A

activation at low concentrations with faster turn of

30
Q

what is the most common mechanism that drugs pass membranes?

A

passive diffusion

31
Q

acidic drugs are better absorbed in the

A

stomach

32
Q

acids with accumulate in

A

basic compartments

33
Q

bases are absorbed in the

A

small intestine

34
Q

bases will accumulate in

A

acidic compartments

35
Q

bioavailability is the measure of the _____ of the orally administered drug that _____ systemic circulation

A

bioavailability is the measure of the percent of the orally administered drug that enters systemic circulation

36
Q

volume of distribution is related the blood _____ to the

A

blood concentration to the amount in the body

37
Q

what 2 properties determine Vd value

A

lipid solubility and binding to plasma proteins

38
Q

high lipid solubility means plasma concentration is low so the Vd is

A

a large value

39
Q

binding to plasma proteins typically results in a what Vd value?

A

a lower value

40
Q

what organ is the most important for excretion?

A

the kidney

41
Q

in renal golmerular filtration what drug is filtered?

A

only the unbound drug

42
Q

renal tubular secretion can be inhibited by what drug?

A

probenecid

43
Q

renal tubular reabsorption is influcened by what properties?

A

nonionized, lipid solubility

44
Q

adding sodium bicarbonate will allow trapping of what kind of drug in the urine ?

A

acidic drugs

45
Q

adding ammonium chloride will allow trapping of what kind of drug in the urine?

A

basic drugs

46
Q

phase 1 metabolism refers to what reactions?

A

oxidation, reduction, hydrolysis

47
Q

phase II metabolism referes to what?

A

functional groups being attached to the drug molecule

48
Q

zero order is constant ____ lost per unit time

A

constant amount lost per unit time

49
Q

first order is constant ___ is lost per unit time

A

constant fraction or % lost per unit time

50
Q

what is a good example of zero order

A

alcohol

51
Q

half life can only be determined for

A

1st order kinetics

52
Q

as 1/2 life increases what decreases?

A

ke (elimiation constant )

53
Q

the elimiation rate constant gives a measure of the

A

rapidity of the drug elimination

54
Q

steady state is when

A

rate of input and rate of ouptu per day are equal

55
Q

elimination kinetics control ____ kinetics

A

accumultion kinetics

56
Q

clearance is only for ____ order kinetics

A

1st order

57
Q

bioavailability is also known as the

A

area under the curve

58
Q

therapeutic index is an estimate of the ____ of the dose needed to produce ___ response from the dose that produces _____

A

therapeutic index is an estimate of the separation of the dose needed to produce desired response from the dose that produces toxicity

59
Q

problems with TI (4)

A
  1. data must be collected in animals
  2. applicability of animal data to humans is uncertain
  3. ED50 is not a realistic dose, ED99 would be better
  4. assumption is that ED and LD curves are parallel and this isn’t always the case