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2S PC & TC > U3.1 PHARMACOKINETICS > Flashcards

U3.1 PHARMACOKINETICS Flashcards

1
Q

What the body can do to the drug

A

Pharmacokinetics

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2
Q

Dose-concentration relationship

A

Pharmacokinetics

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3
Q

Effects of the biologic system on drugs

A

Pharmacokinetics

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4
Q

T/F Pharmacodynamics deals with the processes of absorption, distribution, [metabolism], and elimination [or excretion] of drugs

A

F

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5
Q

Concentration of a drug at the receptor site [in contrast to drug concentrations that are more rapidly measured, eg, blood]

A

Effective Drug Concentration

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6
Q

The amount of drug waiting to associate with its receptor

A

Effective Drug Concentration

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7
Q

T/F Not all of the drug that the patient takes in would take effect

A

T

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8
Q

3 contributors to plasma concentration

A
  1. Rate of input of the drug by absorption
  2. Rate of distribution to peripheral tissue
  3. Rate of elimination, or loss, from the body
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9
Q

2 basic parameters of pharmacokinetics

A
  1. Volume Distribution (Vd)
  2. Clearance (CL)
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10
Q

measure of the apparent space in the body available to contain the drug

A

Volume distribution

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11
Q

measure of the apparent space in the body available to contain the drug

A

Volume distribution

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12
Q

measure of the ability of the body to eliminate the drug

A

Clearance

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13
Q

related the amount of drug in the body to the concentration of drug (C) in blood of plasma

A

Volume distribution

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14
Q

T/F Initial distribution is in the liver, kidney and brain

A

T

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15
Q

T/F Distribution is faster in muscle, viscera, fat and skin

A

F

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16
Q

T/F Distribution happens in the interstitial and intracellular fluids

A

T

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17
Q

Amount of drug in the body to the plasma/serum concentration

A

Volume Distribution

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18
Q

distribute your
drug inside the tissues

A

Intracellular

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19
Q

distribute drug outside the cells

A

Extracellular

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20
Q

T/F When a drug is avidly bound in peripheral tissues, its concentration in plasma may drop to very low values even if the total amount in the body is large

A

T

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21
Q

↑ Vd = distributed in ___

A

peripheral tissue

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22
Q

Relationship of Vd to plasma volume

When a drug is completely retained in the plasma compartment

A

Volume of distribution (Vd) = plasma volume

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23
Q

Rate of elimination compared to drug concentration (C)

A

Clearance (CL)

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24
Q

Depends on the drug and the organs of elimination in the patient

A

Clearance (CL)

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25
Q

2 major sites of drug elimination

A

Liver & Kidney

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26
Q

↑ Vd = ___ plasma concentration

A

↓ plasma concentration

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27
Q

↑ Vd = distributed to ____ e.g. urine, brain

A

tissues

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28
Q

↓ Vd = stays in the _____ e.g. septicemia

A

blood

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29
Q

T/F In clearance, drugs are eliminated with first-order kinetics

A

T

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30
Q

T/F Clearance is constant and can be calculated via area under the curve (AUC)

A

T

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31
Q

First Order = ___ drug concentration, ___ elimination

A

↑ drug concentration, ↑ elimination

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32
Q

T/F CL = rate of elimination / plasma concentration

A

T

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33
Q

T/F Continuous elimination half-life makes the initial concentration smaller & smaller; thus slowing down elimination.

A

T

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34
Q

Clearance : 2 Types of Elimination

A
  1. Capacity-Limited Elimination
  2. Flow-Dependent Elimination
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35
Q

T/F During capacity-limited elimination, clearance does not remain constant but will vary depending on the concentration of drug that is achieved

A

T

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36
Q

T/F Most drug elimination pathways by metabolism will not become saturated if the dose and therefore the concentration are high
enough.

A

F; it will become saturated

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37
Q

Type of elimination

Some drugs are cleared very readily by the organ of elimination

A

Flow-Dependent Elimination

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38
Q

Type of elimination

When blood flow to an organ does not limit elimination, the relation between elimination rate and concentration (C) is expressed mathematically in equation

A

Capacity-Limited Elimination

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39
Q

Type of elimination

Most of the drug in the blood perfusing the organ is eliminated on the first pass of the drug through the organ.

A

Flow-Dependen elimination

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40
Q

T/F For Flow-Dependent elimination, the elimination of these drugs will thus depend primarily on the rate of drug delivery to the organ of elimination.

A

T

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41
Q

Flow Dependent Elimination

main determinant of drug delivery

A

Blood flow to the organ

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42
Q

Flow Dependent Elimination

important for extensively bound drugs that are highly extracted

A

plasma protein binding and blood cell partitioning

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43
Q

Time it takes for the amount of concentration of a drug to fall to 50% of an earlier measurement

A

Half-Life T1/2

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44
Q

T/F Drugs eliminated by first-order kinetics are constant

A

T

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45
Q

Determines the rate at which blood concentration rises during a constant infusion and falls after administration is stopped.

A

Half-Life T1/2

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46
Q

T/F Drug accumulation happens when repeated drug doses will be accumulated until dosing stops

A

T

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47
Q

inversely proportional to the fraction of
dose lost in each dosing interval

A

Accumulation

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48
Q

drug administration = elimination

A

Steady State Concentration

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49
Q

Dose in = Dose Out

A

Steady State Concentration

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50
Q

of Half lives for the drug to have a steady state

A

4

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51
Q

Fraction of the administered dose of the drug that reaches the systemic circulation

A

Bioavailability

52
Q

Equal to the amount absorbed over the amount administered

A

Bioavailability

53
Q

Bioavailability

Unity or 100%

A

Intravenous administration

54
Q

Bioavailability

< 100%
First-pass elimination by the liver.

A

Oral administration

55
Q

T/F Drugs are more absorbed in the small intestines because it has a larger surface area.

A

T

56
Q

Liver immediately metabolizes and makes it water soluble to make it easier to be excreted via kidneys.

A

First pass metabolism

57
Q

Routes with low bioavailability

A

Sublingual, Rectal, Inhalation or nasal, Transdermal patches

58
Q

T/F Bioavailability is dependent on extent of absorption, first-pass effect, rate of elimination and site of administration.

A

F; extent of absorption, first-pass effect, rate of absoprtion and site of administration

59
Q

Bioavailability route

100% BA; most rapid onset

A

Intravenous (IV)

60
Q

Bioavailability route

75 to < 100; Large volumes often feasible, may be painful

A

Intramuscular (IM)

61
Q

Bioavailability route

75 to < 100; Smaller volumes than IM, may be painful

A

Subcutaneous (SC)

62
Q

Bioavailability route

5 to <100; Most convenient; 1st-pass effect may be important

A

Oral (PO)

63
Q

Bioavailability route

30 to <100; Less first-pass effect than oral

A

Rectal (PR)

64
Q

Bioavailability route

5 to <100; Often very rapid onset

A

Inhalation

65
Q

Bioavailability route

80 to ≤100; Usually very slow absorption, lack of first-pass effect

A

Transdermal

66
Q

Bioavailability route

Prolonged duration of action

A

Transdermal

67
Q

Determined by the site of administration & drug formulation

A

Rate of Absorption

68
Q

Type of drug absorption

Rate is independent of the
amount of drug remaining in the gut.

A

Zero-order drug absorption

69
Q

Type of drug absorption

When the rate of absorption is proportional to the concentration.

A

First-order drug absorption

70
Q

T/F Systemic clearance is not affected by bioavailability

A

T

71
Q

T/F During Oral administration, concentration of drug
metabolites will be increased compared to IV
administration

A

T

72
Q

Alternative Routes

direct access to systemic but not portal veins

A

Sublingual Absorption & Transdermal Route

73
Q

Alternative Route

drain into inferior vena cava, bypassing the liver

A

Lower rectum suppositories

74
Q

Alternative Route

bypass first-pass effect by inhalation to lungs

A

Non-gastrointestinal (“parental”) routes

75
Q

Time Course of Drug Effects

Instantaneous effect

A

Immediate Effect

76
Q

Time Course of Drug Effects

Directly related to concentration

A

Immediate Effect

77
Q

Time Course of Drug Effects

Due to distributional delay

A

Delayed Effect

78
Q

Time Course of Drug Effects

Delayed expression of the physiologic substance needed for the effect.

A

Delayed Effect

79
Q

Time Course of Drug Effects

slow turnover of a physiologic substance that is involved in the expression of the drug effect

A

Delayed Effect

80
Q

Time Course of Drug Effects

Constant infusion

A

Cumulative Effects

81
Q

Time Course of Drug Effects

Aminoglycosides cause renal toxicity if given constantly.

A

Cumulative Effects

82
Q

Time Course of Drug Effects

Intermittent dosing only.

A

Cumulative Effects

83
Q

Fraction of the drug removed from the perfusing blood during passage to the organ

A

Extraction ratio

84
Q

Measure of the elimination of the drug by that organ.

A

Extraction

85
Q

↑ hepatic extraction, __ first-pass effect

A

↑ first-pass effect

86
Q

Drugs are eliminated unchanged or as metabolites

A

Excretion

87
Q

Polar compounds are more efficiently eliminated

A

Excretion

88
Q

The concentration wherein you see the desired
therapeutic effects of the drug

A

Target Concentration

89
Q

T/F Target concentration will also depend on the specific
therapeutic objective

A

T

90
Q

Plan for drug administration over a period

A

Dosage Regimens

91
Q

Achievement of therapeutic levels of the drug in the body without exceeding the minimum toxic concentration

A

Dosage Regimens

92
Q

Dose needed to maintain a steady state of concentration

A

Maintenance Dose

93
Q

Maintain plasma concentration within a specified range
over long periods of therapy

A

Maintenance Dose

94
Q

Most important parameter in defining rational drug dosage

A

Clearance

95
Q

For drugs with long half-lives and longer time to reach a steady state

A

Loading Dose

96
Q

Given to promptly raise the concentration of the drug to the target concentration

A

Loading Dose

97
Q

Important factor to consider in loading dose

A

Volume of distribution

98
Q

↑ volume of distribution, __ loading dose

A

↑ loading dose

99
Q

4 Pharmacokinetic Variables

A
  1. absorption
  2. clearance
  3. volume of distribution
  4. half life
100
Q

Pharmacokinetic Variable

Compliance of patient is important.

A

Absorption

101
Q

Pharmacokinetic Variables

Variations in bioavailability are usually due to variations in metabolism

A

Absorption

102
Q

Pharmacokinetic Variables

Most important parameter in designing dosage regimen.

A

Clearance

103
Q

Pharmacokinetic Variables

may be anticipated when there is major impairment of the function of the kidney, liver, or heart

A

Abnormal clearance

104
Q

Pharmacokinetic Variables

Good indicator of renal function

A

Creatinine Clearance

105
Q

Pharmacokinetic Variables

↑ Vd = ____
↓ Vd = ____

A

↑ Vd = tissues, body waters, extracellular accumulation of body fluids
↓ Vd = plasma

106
Q

Pharmacokinetic Variables

Dependent on clearance and volume of distribution

A

Half-life

107
Q

2 Pharmacodynamic Variables

A
  1. Maximum Effect
  2. Sensitivity
108
Q

Pharmacodynamic Variables

No more increase in effect even if the concentration is
increasing

A

Maximum effect

109
Q

Pharmacodynamic Variables

Increased, exaggerated response to small doses

A

Sensitivity

110
Q

Pharmacodynamic Variables

EC50, the concentration required to produce 50%
of maximum effect

A

Sensitivity

111
Q

More highly protein bound drug will displace the less protein bound drug

A

Plasma binding proteins

112
Q

Acidic drugs bind to ____

A

albumin

113
Q

Basic drugs bind to ____

A

α1-Acid glycoprotein

114
Q

Average total amount of drug in the body does not change over multiple dosing intervals

A

Steady State Concentration

115
Q

Safe opeing between the MEC and MTC of the drug

A

Therapeutic Window

116
Q

used to determine the range of plasma levels that is acceptable when designing a dosing regimen

A

Therapeutic Window

117
Q

Peak and Through Concentrations

determines the desired trough levels of a drug given intermittently

A

MEC : Minimum effective concentration

118
Q

Peak and Through Concentrations

determines the permissible peak plasma concentrations

A

MTC : minimum toxic concentration

119
Q

Most appropriate time to measure drug concentration

A

2 hours

120
Q

T/F With maintenance dose drugs, you’ve already reached the steady state concentration

A

T

121
Q

First Order kinetics

↑ drug concentration, ____ rate of elimination

A

↑ rate of elimination

122
Q

↑ Vd = distributed to tissues, ____ half-life

A

↑ longer half-life

123
Q

↓ Vd = stays in the blood, ____ half-life

A

↓ shorter half-life

124
Q

↑ drug accumulation, ____fraction of the dose lost in each interval

A

↓ fraction of the dose lost in each interval

125
Q

↓ affinity drugs = ____ plasma concentration

A

↑ plasma concentration

2S PC & TC (17 decks)

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