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?

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

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
what is the loading dose
Vd x desired plasma concentration
26
how do you calculate volume of distribution
total amount of drug in body/ plasma concentration
27
what is th epurpose of the loading dose
reach therapeutic range right away
28
what are the phase 1 reactions
oxidation reduction hydrolysis
29
what are the phase 2 reactions
glucuronidation sulfation acetylation
30
what is the result after phase 1 reactions in metabolism
usually an inactive metabolite by adding or exposing a polar group
31
what is the result of phase 2 reactions
a conjugated derivative
32
what is first order metabolism
rate of drug metabolism proportional to dose
33
what is zero irder metabolism
enzyme is saturated and the rate of drug metabolism remains constant overtime
34
what are 6 consequences of phase 1 +2 metabolism
``` accelerated renal excretion drug inactivation activation of prodrugs decreased toxicity increased therapeutic action increased toxicity ```
35
define clearance
volume of plasma that must lose all the drug it contains in one minute to account for the observed rate of drug elimination
36
how many half lives are required to eliminate a single dose of a drug from the body
4-5
37
what is the importance of clearance
tells efficiency by which a drug is removed from the body | determining maintenance dose and dosing rate
38
what type of drugs are excreted in urine
non lipid soluble polar ionized low MW
39
how does aging affect half life (decreased muscle)
decreases half life
40
how does obesity effect half life
increases
41
how does pathologic fluid effect half life
increases
42
how does induction of cyp450 affect half life? | inhibition?
induction decreases | inhibition increases
43
how does organ failure effect half life
increases