exam I Flashcards

1
Q

percutaneous administration

A

thru skin
lipid soluble (steroids) work much better
slow sustained absorption

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2
Q

enteral

A

via GI
sublingual
oral
rectal

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3
Q

oral

A

aka per os/ PO

absorption varies due to gastric emptying time, food, other drugs

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4
Q

advantages of oral administration

A

mot used
convenient
safe, can recall drug
inexpensive

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5
Q

disadvantages of oral administration

A
slow absorption
variability among different patients and in single patient
can be inactivated by GI 
first pass metabolism
requires conscious cooperative patient
GI irritation
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6
Q

sublingual

A

warm moist environment for rapid drug dissolution
rich blood flow, close to mucosal surface
more rapid absorption than oral
unpleasant taste limits this use

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7
Q

IV advantages

A

no barriers to absorption
rapid onset and subsequent control
unsuitable for non-aqueous
large fluid volumes can be delivered

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8
Q

IV disadvantages

A

high cost, difficult, inconvenient, irreversible, fluid overload, infection, embolism

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9
Q

SQ advantages

A

lower blood flow -> slower absorption -> sustained actions
poorly water soluble drugs and depot preparations
ex- insulin, epinephrine

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10
Q

SQ disadvantages

A

discomfort
inconvenience
injury

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11
Q

IM

A

only barrier capillary wall
time course dictated by water solubility and blood flow, which is generally high in mm
can inject fat soluble, or particulate matter
DEPOT injections
penicillin G
painful, inconvenient

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12
Q

inhalation

A

for lungs

particle size and technique very important

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13
Q

phase I reactions

A

catabolic
more polar metabolite by introducing or unmasking a functional group
oxidation, reductions, hydrolysis, also deamination, desulfuration, dechlorination
MFOs: CYP, FMO, mEH, sEH
products generally more reactive and maybe more toxic then parent drug
enzymes in ER membranes of liver

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14
Q

phase II reactions

A

anabolic
conjugation
significantly faster then phase I
liver

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15
Q

phase I variations

A

ultrafast, normal, or poor metabolizer

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16
Q

phase II variations

A

UDPGT
acetylation issues
TPMT
Serum Cholinesterase

17
Q

UDPGT

A

for excretion of bile
needed to metabolize camptothecin (chemo drug)
people with UGTDA1*28 have 8 copies which reduces transcription -> 5x higher risk for toxicity with chemo therapy

18
Q

acetylation issues

A

slow acetylation- increased risk of developing drug SEL like syndrome and toxicity with TB isoniezid treatment
fast acetylation- decreased effectiveness of TB isoniezid treatment

19
Q

TPMT

A

adds methyl group
needed for metabolism of 6-mercaptopurine and 6- thioguanine ( immunosuprresent for childhood leukemia)
reduced treatment failures

20
Q

serum cholinesterase

A

prolonged postop paralysis after usage of succinylcholine

21
Q

variations in pharmacodynamic responses

A

G6PD deficiency

malignant hyperthermia

22
Q

variations in pharmacokinetics and dynamics

A

warfarin therapy
warfarin blocks recycling of vit K therefore blocking coagulation
most active metabolite phase I detox by CYP2CC9, 20% of whites are deficient in this enzyme
variations in target of warfarin VKORC1 enzyme
B/B require 2x more then A/A
A present in 33% whites, 89% of asians

23
Q

enzyme inducers

A

phenytoin, chronic ethanol, benzopyrene (tabacco), rifampin(TB), PHENOBARBITAL, BARBITUATES

24
Q

enzyme inhibitors

A

grapefruit juice effect
allopurinol
mercaptopurine

25
Q

lead compound

A

chemical with pharmacological or biological activity whose structure is used as a starting point for modifications to improve potenecy, selectivituy, or phamacokinetics

26
Q

no-effect dose

A

max dose at which specified toxic effect is not seen

27
Q

phase 0

A

microdosing

28
Q

phase I

A

25-50 healthy volunteers
unless drug has serious side effects then use the target disease population
usually open, not blind

29
Q

phase II

A

larger group of people with target disease (100-200)
single blind
placebo group
usually fails here

30
Q

phase III

A

300-3000 people with target disease

double blind

31
Q

phase IV

A

must get NDA granted to distribute

post-market study