ADME Flashcards

1
Q

F = AUC(non-IV) / AUC(IV) x 100%

A

Bioavailability fraction

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2
Q

determinants of Drug Absorption

A
solubility
concentration
local blood flow
Surface Area
ability to permeate cell membrane
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3
Q

in order to be absorbed, drug must be

process called?

A

dissolved into aqueous phase (of extracellular fluid)

dissolution

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4
Q

rate absorption rates of different drug vehicles

A

Aq soln. > Aq suspension > oily vehicle > pellet/solids

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5
Q

for drugs that easily permeate cell membranes, _________ can be the RLS for absorption

A

local blood flow

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6
Q

5 processes of membrane permeation

A
PASSIVE DIFFUSION
facilitated diffusion
filtration
active transport
pinocytosis/phagocytosis
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7
Q

net rate of diffusion determined by

A
drug size (hydrated radius/MW)
lipid (water partition coefficient)
net charge
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8
Q

______ forms (COOH, NH2) of drugs permeate membranes easily

A

neutral

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9
Q

When Lidocaine is injected into inflamed tissue it becomes a _____ which _____ its onset of action

A

cation

delays

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10
Q

passage through small intercellular gaps between endothelial cells

A

filtration

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11
Q

VRG v. VPG

A

vessel rich group
v.
vessel poor group

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12
Q

in the initial phase of distribution the drug moves to _____ then in the Redistribution phase moves to

A

VRG (brain)

VPG (adipose)

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13
Q

decreases apparent volume of distribution and intensity of clinical effects. But increases half-life and incidence of drug interactions

A

Plasma protein binding

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14
Q

elimination is typically more efficient for

A

hydrophilic drugs

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15
Q

primary organ responsible for biotransformation of most drugs

A

liver

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16
Q

Total Body Clearance

A

theoretical measure of the plasma volume cleared of a drug in a given amt of time.
Vd x Ke
(sum of individual organ rates for first order elimination)

17
Q

Renal clearance involves these 3 processes

clearance =

A

glomerular filtration
tubular secretion
tubular reabsorpton
(GF + TS - TR)

18
Q

tubular _______ is active

tubular ______ is passive

A

secretion

reabsorption

19
Q

First Pass Effect

A

extent to which an orally administered drug is metabolized during its first pass through portal circulation (ranges from 0-100%!)

20
Q

The liver will usually

A

render drugs more polar, increase their solubility in plasma

21
Q

2 Categories of biotransformation by liver?

A

Phase 1 Rxns - (cytochrome P enzymes)

Phase 2 Rxns - (coupling with endogenous substance)

22
Q

Drugs that are metabolized by the same family of hepatic CYP isozymes can?

A

compete as substrates with one another

23
Q

drugs that act as ______ of CYP isozymes, will reduce/prevent the metabolism of other drugs by that family

A

inhibitors

24
Q

drugs that act as ____ of CYP isozymes, cause an elevated rate of drug metabolism by those isozymes

A

inducers

25
Q

metabolism Does/Does not? always lead to drug inactivation?

A

does not

26
Q

use clearance rate of _______ to adjust dose of animal with renal disease

A

creatine