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Pharmacology Test #1 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

What does ADME stand for?

A

absorption
distribution
metabolism
elimination

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2
Q

Equation for concentration you need to know

A

[C] = Mass/Volume

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3
Q

define plasma

A

blood without cells

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4
Q

define serum

A

plasma without clotting factors

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5
Q

What’s the makeup of blood?

A

50% cells

50% plasma

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6
Q

Tissues are perfused with?

A

blood not plasma

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7
Q

What kind of drugs are concentrated in RBCs

A

highly lipophilic drugs

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8
Q

Name these terms Cb, Cp, Css, Cu

A 
Cb = [blood]
Cp = [plasma]
Css = [steady state]
Cu = [unbound]
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9
Q

Significance of knowing the [unbound protein]

A

only unbound proteins are active

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10
Q

Pharmacokinetics

A

what the body does to the drug

how does the drug concentration change as it moves through the different compartments of your body

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11
Q

Pharmacodynamics

A

what the drug does to the body

how does the drug exert its effect on your body

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12
Q

Fundamental hypothesis of PK

A

there is a predictable relationship between plasma (or serum) concentration of a drug and its effect

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13
Q

General goals of pharmacokinetics

A

establishing/adjusting dosage regimens
diagnosis of toxicoses
withdrawal times for food safety in babies

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14
Q

Absorption

A

the process of a drug entering the blood/systemic circulation

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15
Q

Distribution

A

the dispersion of a drug throughout fluids and tissues of the body

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16
Q

Metabolism (biotransformation)

A

the irreversible transformation of parent compounds into daughter compounds

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17
Q

Elimination/excretion

A

the removal of the drug from the body

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18
Q

route of elimination/excretion

A

renal/kidney
gut
lung
skin

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19
Q

Drug exposure in the body is a function of what?

A

both drug concentration and the duration time

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20
Q

AUC stands for

A

area under the curve (always of a single dose)

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21
Q

Bioavailability (F)

A

the fraction (%) of the amount of drug entering into the circulating system

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22
Q

Which route of administration has an F of 1

A

intravenous

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23
Q

Which route of administration has a low F

A

oral

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24
Q

What route of administration is faster than oral, but less than 1

A

intramusclar

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25
Q

Equation for F

A

the amount of a drug absorbed into systemic circulation/the amount of a drug administered

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26
Q

Bioavailability is equal to

A

fraction (%) absorbed from gut lumen into the portal vein X fraction (%) escaping first pass metabolism = 1 - hepatic extraction ratio (Eh)

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27
Q

hepatic extraction ratio

A

the fraction of drug extracted by the liver in the first-pass metabolism

28
Q

What does it mean when you say Eh = 0.5

A

50% of the drug will be extracted by the liver

29
Q

Eh =

A

C1 - C2 / C1

30
Q

Another equation for F

A

AUC (P.O.) / AUC (I.V.)

31
Q

For low Eh drugs

A

bioavailability is high
Most of the dose reaches systemic circulation
alteration of the hepatic enzyme activity would not significantly affect the plasma concentration

32
Q

For high Eh drugs

A

bioavailability is low
most of the dose is eliminated by the liver
alteration of the hepatic enzyme activity will significantly affect the plasma concentration

33
Q

When are drugs considered bioequivalent?

A

if the extents and rates of absorption of the drug from them are so similar that there is likely to be no clinically important difference between their effects, either therapeutic or adver

34
Q

Mathematical parameters for considering a drug bioequivalent?

A

if the 90% Cl of the AUC ratio is within the range of 0.8 - 1.25

35
Q

Relative Bioavailability (Fr) =

A

AUC generic / AUC brand

0.8

36
Q

Distribution

A

the dispersion of the absorbed drug form the site of absorption throughout fluids and tissues of the body

37
Q

factors affecting drug distribution

A 
size of organ
blood flow
solubility
binding
MW
38
Q

volume of plasma in the human body

A

~2.5 L

39
Q

total body water volume in the human body

A

40 L

40
Q

total volume of blood in the human body

A

5.6 L

41
Q

Apparent volume of distribution (Vd) is

A

the constant relating the amount of drug in the body to the plasma drug concentration

42
Q

Vd =

A

total amount of drug in the body (A) / plasma drug concentration (Cp)

43
Q

Is Vd constant or related to the drug dose/concentration?

A

For a specific drug and a specific patient, Vd is a constant

44
Q

steady state

A

the condition in which the average total amount of drug in the body remains stable over time of dosing
ex. the rate of drug input = the rate of drug elimination

45
Q

maintenance dose rate (DR)

A

rate (mass/time) of drug input to maintain the drug concentration at the stead state

46
Q

what is a loading dose used for?

A

used to reach the stead state drug concentration more quickly

47
Q

What is Vd important for calculating?

A

loading dose

48
Q

Loading dose =

A

Vd * target plasma concentration

49
Q

metabolism

A

the irreversible transformation of parent compounds into daughter compounds

50
Q

how are most drugs excreted?

A

by the kidneys

51
Q

clearance (CL)

A

the efficiency that the drug (vol) is irreversibly eliminated from the volume of distribution

52
Q

elimination rate (ER)

A

the amount of the drug (mass) is irreversibly eliminated from the dose per unit time

53
Q

Elimination rate constant (K)

A

the fraction of drug vol is irreversibly eliminated from the vol of distribution per unit time

54
Q

Equation for elimination rate (mass/time) =

A

clearance (CL) * plasma concentration (Cp)

55
Q

Equation for elimination rate constant (K) =

A

clearance (CL) / vol of distribution (Vd)

56
Q

increasing the drug plasma concentration will do what to the elimination rate

A

it will proportionately increase the elimination rate

57
Q

maintenance dose rate (DR) =

A

clearance (CL) * steady state drug concentration (Css)

58
Q

When the maintenance dose rate remains the same, changing the clearance will do what to the Css?

A

changing the clearance will proportionately and inversely change the Css

59
Q

When clearance remains stable, increasing the maintenance dose rate will do what to the Css

A

increasing the maintenance dose rate will proportionately increase Css as well

60
Q

clearance is a description of

A

efficiency

61
Q

organ clearance (CL) =

A

organ extraction ratio (E) X organ blood flow (Q)

ex) hepatic: CLh = Eh * Qh

62
Q

for drugs with a high extraction ratio, CL will be mainly determined by

A

organ blood flow (Qh)

63
Q

For drugs with high hepatic extraction, increasing the hepatic metabolism will?

A

decrease bioavailability

no change to the clearance

64
Q

For drugs with low hepatic extraction, increasing the hepatic metabolism will?

A

no change to the bioavailability

clearance will increase

65
Q

What are the implications for blood flow in heart failure?

A

the blood flow is low

Pharmacology Test #1 (5 decks)

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