Pharm Flashcards

(73 cards)

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
how to alter vd of plasma protein-bound drugs
liver and kidney disease
26
decreased protein binding's effect on Vd
increases Vd
27
Vd equation
Vd = amount of drug in body/ plasma drug concentration
28
low Vd (4-8L) distribution and drug types that cause this
blood - large/charged molecules; plasma-protein bound
29
medium Vd distribution and drug types that cause this
ECF - small hydrophilic molecules
30
high Vd distribution and drug types that cause this
all tissues - small lipophilic molecules (especially if bound to tissue protein)
31
the time req to change the amount of drug in body by 1/2 during elimination or constant infusion
half-life (t 1/2)
32
property of first-order elimination
t 1/2
33
drug infused at constant rate takes how long to reach steady state
4-5 t 1/2
34
t 1/2 equation
t 1/2 = (.7 x Vd) / Cl
35
of half lives --> % remaining
1 half life --> 50% 2 half life --> 25% 3 half life --> 12.5% 4 half life --> 6.25%
36
clearance equation
rate of elimination of drug/plasma drug concentration = Vd x Ke (elimination constant)
37
clearance may be impaired with what
renal, cardiac or hepatic failure
38
loading dose
Cp x Vd/F
39
maintenance dose
Cp x CL/F
40
Cp
target plasma concentration
41
renal/liver disease
maintenance dose decreases (loading dose unchanged)
42
time to steady state
depends on t 1/2 - independent of dosing freq or size
43
zero order elimination
rate of elimination is constant regardless of Cp | constant AMOUNT of drug eliminated per unit time
44
EX of zero order kinetics
PEA - phenytoin, ethanol and aspirin(high)
45
capacity limited elimination
zero-order kinetics
46
first order elimination
rate of elimination is directly proportional to drug concentration - constant FRACTION of drug eliminated per time
47
how does Cp decrease with time in zero order vs. first order
zero order = linearly | first order = exponentially
48
flow-dependent elimination
first-order kinetics
49
ionized vs neutral species
ionized - trapped in urine (pee out) | neutral - can be reabsorbed
50
weak acids
trapped in basic env tx overdose w/ bicarb EX: phenobarbital, methotrexate, aspirin
51
weak bases
trapped in acidic env tx overdose w/ ammonium chloride EX: amphetamines
52
phase I of drug metabolism
reduction, oxidation, hydrolysis w/ cytochrome P-450 --> slightly polar, water soluble metabolites (still active)
53
phase II of drug metabolism
conjugation (glucuronidatoin, acetylation, sulfation) -->very polar, inactive metabolites (pee out) geriatric patients have GAS - phase 2
54
which phase do geriatric patients lose first
phase I
55
patients who are slow acetylators
decrease rate of metabolistm --> greater side effects from certain drugs (phase II)
56
maximal effect a drug can produce
efficacy
57
amount of drug needed for a given effect
potency
58
high-efficacy drug classes
analgesic (pain) meds, antibiotics, antihistamines, decongestants
59
partial agonists vs full agonist efficacy
partial agonist - decreased efficacy
60
high potency
high affinity for receptors
61
highly potent drug classes
chemotherapy (cancer) drugs, antihypertensive (BP) drugs, antilipid (cholesterol) drugs
62
receptor binding curve
percent of maximum effect (efficacy) vs. agonist dose
63
competitive antagonist
shift curve to right --> decreases potency | overcome - increasing concentration of agonist substrate
64
competitive antagonist EX
diazepam + flumazenil on GABA R
65
noncompetitive antagonist
shift cruve down --> decreases efficacy
66
noncompetitive antagonist EX
NE + phenoxybenzamine on alpha-receptors
67
partial agonist
acts @ same site as full agonist but w/ reduced maximal effect --> decreased efficacy potency can increase/decrease (diff variable)
68
partial agonist EX
morphine (full agonist) + buprenorphine (partial agonist) at opioid mu-receptors
69
measurement of drug safety
therapeutic index
70
TI equation
TILE | TI = LD50/ED50 = median lethal dose/median effective dose
71
safer drugs
higher TI values
72
drugs w/ low TI values
digoxin, lithium, theophylline, warfarin
73
measure of clinical drug safety
therapeutic window | range of minimum effect dose --> minimum toxic dose