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FA > Pharm > Flashcards

Pharm Flashcards

1
Q

Km - michaelis constant

A

substrate concentration @ 1/2 vmax

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2
Q

high Km

A

low affinity of enzyme for substrate***

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3
Q

high Vmax

A

high enzyme concentration

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4
Q

if a reaction follows michaelis-menten kinetics, what kind of curve will it have?

A

hyperbolic

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5
Q

enzymatic reactions that follow cooperative kinetics - what is an example and what type of curve will they have

A

EX: hemoglobin

sigmoid curve

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6
Q

michaelis-menten kinetics graph

A

Velocity (reaction rate) vs. substrate concenration

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7
Q

lineweaver-burk plot graph

A

1/V vs. 1/[S]

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8
Q

increasing the y-intercept of lineweaver-burk plot

A

decrease Vmax

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9
Q

increase to the right x-intercept of lineweaver-burk plot

A

increase Km = decrease affinity

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10
Q

lineweaver-burk plot y-intercept

A

1/Vmax

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11
Q

lineweaver-burk plot x-intercept

A

1/-Km

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12
Q

lineweaver-burk plot slope

A

Km/Vmax

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13
Q

inhibitors and crossing

A

competitive inhibitors cross eachother competitively, whereas non-competitive inhibitors do not (on 1/v vs. 1/[s] graph)

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14
Q

which enzyme inhibitors resemble substrate

A

competitive inhibitors

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15
Q

which enzyme inhibitors overcome by increase [S]

A

competitive inhibitors

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16
Q

which enzyme inhibitors bind active site

A

competitive inhibitors

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17
Q

which enzyme inhibitors have an effect on Vmax, and what is the effect

A

noncompetitive inhibitors decrease Vmax

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18
Q

which enzyme inhibitors have an effect on Km, and what is the effect

A

competitive inhibitors increase Km (decreasing affinity for substrate)

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19
Q

which enzyme inhibitors decrease potency

A

competitive inhibitors

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20
Q

which enzyme inhibitors decrease efficacy

A

noncompetitive inhibitors

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21
Q

fraction of administered drug that reaches systemic circulation unchanged

A

F = bioavailability

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22
Q

bioavailability for IV dose

A

F = 100%

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23
Q

bioavailability for oral dose

A

F < 100% - incomplete absorption and first-pass metabolism

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24
Q

theoretical fluid volume req to maintain the total absorbed drug amount at the plasma concentration

A

volume of distribution

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25
Q

how to alter vd of plasma protein-bound drugs

A

liver and kidney disease

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26
Q

decreased protein binding’s effect on Vd

A

increases Vd

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27
Q

Vd equation

A

Vd = amount of drug in body/ plasma drug concentration

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28
Q

low Vd (4-8L) distribution and drug types that cause this

A

blood - large/charged molecules; plasma-protein bound

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29
Q

medium Vd distribution and drug types that cause this

A

ECF - small hydrophilic molecules

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30
Q

high Vd distribution and drug types that cause this

A

all tissues - small lipophilic molecules (especially if bound to tissue protein)

31
Q

the time req to change the amount of drug in body by 1/2 during elimination or constant infusion

A

half-life (t 1/2)

32
Q

property of first-order elimination

A

t 1/2

33
Q

drug infused at constant rate takes how long to reach steady state

A

4-5 t 1/2

34
Q

t 1/2 equation

A

t 1/2 = (.7 x Vd) / Cl

35
Q

of half lives –> % remaining

A

1 half life –> 50%
2 half life –> 25%
3 half life –> 12.5%
4 half life –> 6.25%

36
Q

clearance equation

A

rate of elimination of drug/plasma drug concentration = Vd x Ke (elimination constant)

37
Q

clearance may be impaired with what

A

renal, cardiac or hepatic failure

38
Q

loading dose

A

Cp x Vd/F

39
Q

maintenance dose

A

Cp x CL/F

40
Q

Cp

A

target plasma concentration

41
Q

renal/liver disease

A

maintenance dose decreases (loading dose unchanged)

42
Q

time to steady state

A

depends on t 1/2 - independent of dosing freq or size

43
Q

zero order elimination

A

rate of elimination is constant regardless of Cp

constant AMOUNT of drug eliminated per unit time

44
Q

EX of zero order kinetics

A

PEA - phenytoin, ethanol and aspirin(high)

45
Q

capacity limited elimination

A

zero-order kinetics

46
Q

first order elimination

A

rate of elimination is directly proportional to drug concentration - constant FRACTION of drug eliminated per time

47
Q

how does Cp decrease with time in zero order vs. first order

A

zero order = linearly

first order = exponentially

48
Q

flow-dependent elimination

A

first-order kinetics

49
Q

ionized vs neutral species

A

ionized - trapped in urine (pee out)

neutral - can be reabsorbed

50
Q

weak acids

A

trapped in basic env
tx overdose w/ bicarb
EX: phenobarbital, methotrexate, aspirin

51
Q

weak bases

A

trapped in acidic env
tx overdose w/ ammonium chloride
EX: amphetamines

52
Q

phase I of drug metabolism

A

reduction, oxidation, hydrolysis w/ cytochrome P-450 –> slightly polar, water soluble metabolites (still active)

53
Q

phase II of drug metabolism

A

conjugation (glucuronidatoin, acetylation, sulfation) –>very polar, inactive metabolites (pee out)
geriatric patients have GAS - phase 2

54
Q

which phase do geriatric patients lose first

A

phase I

55
Q

patients who are slow acetylators

A

decrease rate of metabolistm –> greater side effects from certain drugs (phase II)

56
Q

maximal effect a drug can produce

A

efficacy

57
Q

amount of drug needed for a given effect

A

potency

58
Q

high-efficacy drug classes

A

analgesic (pain) meds, antibiotics, antihistamines, decongestants

59
Q

partial agonists vs full agonist efficacy

A

partial agonist - decreased efficacy

60
Q

high potency

A

high affinity for receptors

61
Q

highly potent drug classes

A

chemotherapy (cancer) drugs, antihypertensive (BP) drugs, antilipid (cholesterol) drugs

62
Q

receptor binding curve

A

percent of maximum effect (efficacy) vs. agonist dose

63
Q

competitive antagonist

A

shift curve to right –> decreases potency

overcome - increasing concentration of agonist substrate

64
Q

competitive antagonist EX

A

diazepam + flumazenil on GABA R

65
Q

noncompetitive antagonist

A

shift cruve down –> decreases efficacy

66
Q

noncompetitive antagonist EX

A

NE + phenoxybenzamine on alpha-receptors

67
Q

partial agonist

A

acts @ same site as full agonist but w/ reduced maximal effect –> decreased efficacy
potency can increase/decrease (diff variable)

68
Q

partial agonist EX

A

morphine (full agonist) + buprenorphine (partial agonist) at opioid mu-receptors

69
Q

measurement of drug safety

A

therapeutic index

70
Q

TI equation

A

TILE

TI = LD50/ED50 = median lethal dose/median effective dose

71
Q

safer drugs

A

higher TI values

72
Q

drugs w/ low TI values

A

digoxin, lithium, theophylline, warfarin

73
Q

measure of clinical drug safety

A

therapeutic window

range of minimum effect dose –> minimum toxic dose

FA (13 decks)

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