Pharm - basics Flashcards

1
Q

competitive inhibitors bind

A

active site

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2
Q

competitive inhibitors affect

A

potency (lower it)

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3
Q

non competitive inhibitors affect

A

efficacy (lower it)

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4
Q

can alter volume of distribution

A

liver and kidney disease

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5
Q

volume of distribution =

A

amount of drug in body/plasma drug concentration

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6
Q

large/charged molecules are distrubted in

A

the blood

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7
Q

small hydrophillic molecules are distributed in the

A

ECF

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8
Q

small lipophillic moclecules are distributed in

A

all tissues

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9
Q

half life =

A

.(07 x volume of distribution)/clearance

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10
Q

a drug infused at a constant rate takes how ling to reach steady state

A

4-5 half lives

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11
Q

clearance =

A

(rate of elimnation of drug/plasma drug concentration)

or

(volume of distribution x elimination constant)

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12
Q

loading dose =

A

target plasma concentration x (volume of distribution/bioavailability)

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13
Q

maintance dose =

A

target plasma concentration x (clearance/bioavailability)

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14
Q

dosage calculation that changes in renal/liver disease

A

maintainance dose (lower)

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15
Q

zero-order elimination drug examples

A

asprin, phenytoin, ethanol

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16
Q

rate of elimination is constant regardless of plasma concentration is called

A

zero order

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17
Q

rate of elimination is directly proportional to drug concentration

A

first order

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18
Q

treat OD of weak acids with

A

bicarb (to trap in urine)

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19
Q

weak acid drug ex:

A

phenobarbital, methotreaxate, asprin

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20
Q

treat OD of weak bases with

A

amonium cholride (traps in urine)

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21
Q

weak base drug ex

A

amphetamines

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22
Q

phase I metabolism results in

A

slightly polar slightly water souable metabolites

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23
Q

phase II metabolism results in

A

very polar, inactive metaboltes that are renally excreted

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24
Q

phase metabolism reactions

A

reduction, oxidation, hydrolysis with cytochrome P450

25
phase II metabolism reactions
conjugation (glucoronidation, acetylation, sulfation)
26
maximal effect a drug can produce
efficacy
27
high efficacy drug classes
pain meds, antibiotics, antihistamines, decongestants
28
amount of drug needed for a given effect
potency
29
high potency drug classes
chemo, HBP drugs, antilipid drugs
30
shifts dose effect curve to right and decreses potency
competive agonist
31
shifts dose effect curve down and decreses efficacy
noncompetetive agonist
32
acts at same site as full agonisyt but with reduced maximal effect
partial agonist
33
cannot be overcome by increasing agonist substrate concentration
noncompetitive antagonist
34
theraputic index=
LD50/ED50
35
drugs with low theraputic indexes
digoxin, lithium, theophylline, warfarin
36
nicotinic ACh receptors are what type
ligand gated Na/K
37
muscarinic ACh receptors are what type
G-protein coupled
38
sympathetic a1 receptor functions
increase: vascular smooth muscle tone, contraction of pupilarry dilator muscle (mydriasis), contract intestinal and bladder sphincter muscle
39
sympathetic a2 receptor functions
lowered: sympathetic outflow, insulin release, lipolysis raised: platelet aggretation
40
sympathetic B1 receptor functions
increase: HR, contractability of heart, lipolysis, increased renin release
41
sympathetic B2 receptor functions
vasodilation, bronchodilation, increased HR and contractability, increased lipolysis and insulin release, lower uterine tone, cilary muscle relaxation, increased aqueous humor production
42
parasympathetic M2 receptor functions
lowers HR and contractability of atria
43
parasympathetic M3 receptor functions
increase exocrine gland secretions, increase gut peristalis, increase bladder contraction, increase bronchoconstriction, miosis, accomidation (increases ciliary muscle contraction)
44
D1 receptor function
relaxes renal vascular smooth muscle
45
D2 receptor function
modulates transmitter release, esp in brain
46
H1 receptor function
nasal and bronchial mucus production, contraction of bronchioles, itching and pain
47
H2 receotor function
gastric acid release
48
V1 receptor functon
vascular smooth muscle contraction
49
V2 receptor function
H20 permability and resbsprption in the collecting tubiles in the kidney
50
prevents tyrosine becoming DOPA
metyrosine
51
prevents dopamine from becoming NE
reserpine
52
prevents NE uptake
cocaine, amphetamine, TCA
53
prevents NE release
guanathidine, bretylium
54
releases extra NE
amphetamine
55
prevents choline uptake
hemicholinium
56
prevents ACh production
vesamicol
57
prevents ACh release
botulism toxin
58
ACh broken down by AChesterase into
choline and acetate