Pharmacokinetics Flashcards

1
Q

what does ADME stand for

A

absorb
distributes
metabolize
eliminate

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2
Q

what determines the intensity of the drugs effect

A

the concentration at the site of the receptor

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3
Q

what are the routes of administration

A
oral 
IV
subcutaneous
intramuscular
transdermal pathc 
rectal 
inhalation 
sublingual
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4
Q

3 ways drugs cross the cell membrane

A

pass through channels or pores
through membrane with transport system
penetrate directly if lipophilic (most common)

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5
Q

where are transporters found

A

liver
kidney
intestine
brain capillaries

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6
Q

how is 2 compartment model different from one compartment

A

in two drugs are not distributed instantaneously to peripheral, there is a time lag

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7
Q

what kinds of drugs are best described by one compartment model

A

drugs that dont extensively distribute into extravascular tissues

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8
Q

what is another word for bioavailability

A

absorption

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9
Q

describe bioavailability

A

fraction of unchanged drug that reaches the blood

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10
Q

what is drug accumulation

A

inversly proportional to dose lost

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11
Q

describe volume of distribution

A

how drug is distributed in body relative to plasma

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12
Q

define clearance

A

ability of the body to eliminate the drug

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13
Q

what is the drug half life

A

time required to change the amount of drug in the body by one half

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14
Q

what does AUC stand for

A

the area under the curve of a graph of plasma concentration against time

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15
Q

what is the % bioavailability in IV admin

A

100%

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16
Q

what is the first pass effect

A

drugs metabolized and inactivated in the liver

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17
Q

describe enterophepatic cycling

A

body recycles the drug from liver to bile duct back into the intestine, hepatic artery, liver again
prolongs half life

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18
Q

8 factors that influence drug absorption

A
fromulation 
water solubility
lipid solubility 
pka
Gi motility 
posture
others drugs/food
gastric ph
19
Q

is the drug charged or uncharged when passing through a membrane?

A

uncharged

20
Q

acidic drugs require what environment to pass through the membrane

A

acidic environment so they are in the uncharged HA form (dont ionize in acidic)

21
Q

basic drugs require what environment to pass through the membrane

A

alkaline environment so it is in the uncharged form B (dont ionize in basic)

22
Q

how many half lives does it take for a drug to be fully accumulated or eliminated

A

4

23
Q

what is steady state

A

when rate of drug elimination equals rate of administration

24
Q

what does a high volume of distribution represent

A

drug is extensively distributed and not in the plasma

25
Q

what is the loading dose

A

Vd x desired plasma concentration

26
Q

how do you calculate volume of distribution

A

total amount of drug in body/ plasma concentration

27
Q

what is th epurpose of the loading dose

A

reach therapeutic range right away

28
Q

what are the phase 1 reactions

A

oxidation
reduction
hydrolysis

29
Q

what are the phase 2 reactions

A

glucuronidation
sulfation
acetylation

30
Q

what is the result after phase 1 reactions in metabolism

A

usually an inactive metabolite by adding or exposing a polar group

31
Q

what is the result of phase 2 reactions

A

a conjugated derivative

32
Q

what is first order metabolism

A

rate of drug metabolism proportional to dose

33
Q

what is zero irder metabolism

A

enzyme is saturated and the rate of drug metabolism remains constant overtime

34
Q

what are 6 consequences of phase 1 +2 metabolism

A
accelerated renal excretion
drug inactivation 
activation of prodrugs
decreased toxicity 
increased therapeutic action 
increased toxicity
35
Q

define clearance

A

volume of plasma that must lose all the drug it contains in one minute to account for the observed rate of drug elimination

36
Q

how many half lives are required to eliminate a single dose of a drug from the body

A

4-5

37
Q

what is the importance of clearance

A

tells efficiency by which a drug is removed from the body

determining maintenance dose and dosing rate

38
Q

what type of drugs are excreted in urine

A

non lipid soluble
polar
ionized
low MW

39
Q

how does aging affect half life (decreased muscle)

A

decreases half life

40
Q

how does obesity effect half life

A

increases

41
Q

how does pathologic fluid effect half life

A

increases

42
Q

how does induction of cyp450 affect half life?

inhibition?

A

induction decreases

inhibition increases

43
Q

how does organ failure effect half life

A

increases