4&5- Pharmacokinetics Flashcards

1
Q

drug delivery via the GI tract

A

enteral administration

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2
Q

drug delivery via a route that does not involve the GI tract. requires piercing the skin

A

parenteral administration

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3
Q

advantage of sublingual and buccal over oral administration

A

sublingual and buccal enter the venous system and therefore bypass 1st exposure

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4
Q

administration via an injection into the subarachnoid space for delivery of drugs into the CNS

A

intrathecal administration

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5
Q

the ________ form is readily able to cross lipid membranes

A

non-ionized form

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6
Q

the non-ionized form of a WA =

A

protonated WA (aka HA)

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7
Q

the non-ionized form of a WB =

A

unprotonated WB (aka B)

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8
Q

where are weak acids better absorbed- stomach or intestine?

A

stomach

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9
Q

where are weak bases better absorbed- stomach or intestine?

A

intestine

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10
Q

when pH

A

protonated form will predominate if the pH is less than the pKa

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11
Q

increase cardiac output = _________ distribution

A

increase

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12
Q

increase regional blood flow = _________ distribution

A

increase

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13
Q

increase capillary permeability = __________ ddistribution

A

increase

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14
Q

increase binding to plasma proteins = _________ distribution

A

decrease ***

*important

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15
Q

increase drug molecule size = _____ distribution

A

decrease

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16
Q

increase lipid solubility of drug = ______ distribution

A

increase

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17
Q

goal of biotransformation

A

make the molecule more water soluble (more polar) for eventual excretion

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18
Q

prodrug

A

makes use of biotransformation to activate the drug

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19
Q

oxidative
reductive
hydrolytic

A

phase 1 biotransformation

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20
Q

cytochrome P450 enzymes

A

phase 1 biotransformation

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21
Q

glucoronidation
sulfation
acetylation

A

phase 2 biotransformation

22
Q

conjugation

A

phase 2 biotransformation

23
Q

first pass effect

A

large percentage of a drug absorbed by stomach or intestine will be carried to the liver by the portal vein and exposed to metabolism before entering circulation –> drug can be inactivated before reaching target

24
Q

primary mechanism of drug elimination

A

renal excretion

25
Q

increase GFR = ________ filtration

A

increase

26
Q

increase binding to plasma prtns = ________ filtration

A

decrease

27
Q

V =

A

volume of distribution

measure of space in body available to contain the drug

28
Q

C =

A

concentration of drug in blood

29
Q

a low volume of distribution indicates…

A

most of the drug stays in the blood circulation

a higher V would indicate that the drug is highly distributed throughout the body or concentrating somewhere

30
Q

CL=

A

clearance

rate of elimination in relation to drug concentration
capacity of drug removal by organs

31
Q

clearance that is independent of drug concentration

A

zero order elimination

32
Q

concentration of drug has saturate the elimination capacity of the system and mimics zero order kinetics

A

capacity limited elimination

33
Q

if dosing rate > elimination rate, the concentration will continue to _________ in blood

A

increase

dangerous for toxic effects

34
Q

constant fraction of drug is eliminated

A

first order elimination

35
Q

the greater the flow the _______ rate of elimination

A

greater

kinetics of flow-limited elimination mimic first order elimination

36
Q

rate of elimination

A

rate of elimination = k

k = 0.693/ t.5

37
Q

accumulation of a drug in the body will be detectable if the dosing interval is shorter than ______ half lives

A

4

38
Q

amount of drug that reaches systemic circulation

A

bioavailability

39
Q

ER =

A

extraction ratio

40
Q

Q =

A

hepatic blood flow (usually 90)

41
Q

F =

A

bioavailability

42
Q

f =

A

extent of absorption (gut)

43
Q

TC =

A

target concentration

44
Q

what is the therapeutic window?

A

concentration range between MEC for desired effects and MEC for toxic effects

45
Q

Css =

A

steady state concentration

point during a dosing regimen when elimination of a drug is equal to bioavailability of drug

should be within the therapeutic window

46
Q

you will always reach the Css within ____ half lives

A

4

47
Q

the time it takes to reach Css is _________ of dose or dosing rate but is ___________ upon the half-life

A

independent

dependent

48
Q

dose needed to maintain steady state concentrations

A

maintenance dose

49
Q

why is decreasing the dosing rate potentially problematic?

A

this will increase the dosing interval and the peak and trough may excede the therapeutic interval with a larger maintenance dose

50
Q

LD =

A

loading dose

initial dose that can be given in order to achieve the target concentration rapidly