Therapeutic Drug Monitoring (TDM) Flashcards

1
Q

What is the general drug class for methotrexate?

A

Antineoplastic

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2
Q

What is the general drug class for phenobarbital?

A

Anticonvulsant

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3
Q

What is the general drug class for vancomycin?

A

Antibiotic (antimicrobial)

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4
Q

What is the general drug class for ethosuximide?

A

Anticonvulsant

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5
Q

What is the general drug class for digoxin?

A

Cardioactive

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6
Q

What is the general drug class for theophyline

A

Bronchodilator

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7
Q

What is the general drug class for tricyclic antidepressants?

A

Anti-psychotic

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8
Q

What is the general drug class for chloramphenicol?

A

Antibiotic (antimicrobial)

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9
Q

What is the general drug class for quinidine?

A

Cardioactive

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10
Q

What is the general drug class for primidone?

A

Anticonvulsant

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11
Q

What is the general drug class for mycophenolic acid (MPA)?

A

Immunosuppressant

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12
Q

What is the general drug class for aminoglycosides (gentamicin, tobramycin, amikacin, neomycin)?

A

Antibiotic (antimicrobial)

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13
Q

What is the general drug class for alkylating agents?

A

Antineoplastic

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14
Q

What is the general drug class for lithium?

A

Anti-pyschotic

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15
Q

What is the general drug class for valproic acid?

A

Anticonvulsant

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16
Q

What is the general drug class for sirolimus (rapamycin)?

A

Immunosuppressant

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17
Q

What is the general drug class for serotonin-release inhibitors?

A

Anti-psychotic

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18
Q

What is the general drug class for lidocaine?

A

Cardioactive

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19
Q

What is the general drug class for caffeine?

A

Bronchodilator

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20
Q

What is the general drug class for phenytoin?

A

Anticonvulsant

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21
Q

What is the general drug class for tacrolimus (Prograf or FK-506)?

A

Immunosuppressant

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22
Q

What is the general drug class for serotonin-selective reuptake inhibitors (SSRI’s)?

A

Anti-psychotic

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23
Q

What is the general drug class for procainamide?

A

Cardioactive

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24
Q

What is the general drug class for carbamazepine?

A

Anticonvulsant

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25
Q

What is the general drug class for cyclosporine?

A

Immunosuppressant

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26
Q

A chemical used to selectively perturb specific tissues or a specific function of these tissues?

A

Drug

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27
Q

A drug given to produce a DESIRABLE effect

A

Theraapeutic drug

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28
Q

The minimum concentration that one can take to have a desired effectiveness

A

Minimum effective concentration (MEC)

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29
Q

Minimum concentration that one can take to have a toxic effect

A

Minimum toxic concentration

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30
Q

The fraction of a drug taht is absorbed into circulation

A

Bioavailability

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31
Q

When the rate of drug input is equal to the rate of drug elimination

A

Stead-state concentration

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32
Q

Time required for drug concentration to decrease by one-half

A

Half-life

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33
Q

The highest concentration reached after a dose

A

Peak drug level

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34
Q

Lowest drug concentration acheived, usually sampled shortly before teh next scheduled dose

A

Trough drug level

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35
Q

Three purposes of therapeutic drug monitoring

A
  • Check for compliance or non-compliance
  • Initiation and maintenance of the most appropriate dosing regimen for a particular patient
  • Interpreting toxic symptoms of patients to whom a drug is prescribed
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36
Q

Three general tyeps of candidates for therapeutic drug monitoring (TDM)

A
  • Pediatric or geriatric patients
  • Patients w/ other underlying ocnditions
  • Patients on multiple drug therapies
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37
Q

Two general reasons why certain drugs may require monitoring

A
  • ?

- ?

38
Q

Represents the range of drug concentrations w/in which the probability of the desired clinical response is relatively high and the probability of unacceptable toxicity is relatively low

A

Therapeutic range

39
Q

Represents the range of values for a physiologic measurement in healthy persons

A

Reference range

40
Q

List three goals of dosing

A
  • Trough should be reached before giving the next dose
  • Trough should not fall below the MEC
  • Peak should not be above the MTC
41
Q

What are the three general factors that affect drug deposition?

A
  • Biological
  • Physiological
  • Pathological
42
Q

List the condition associated w/ biological factors that affect drug deposition?

A

Genetics (enzyme deficiencies)

43
Q

List at least one of the conditions associated w/ physiological factors that affect drug deposition?

A
  • Body weight and composition
  • Age
  • Temperature (hyper- or hypothermia)
  • Gastric emptying time and gastrointestinal motility
  • Blood flow rates (resting or exercise)
  • Environment (high altitude → ↓ O2 → ↑ RBCs → ↑ “drug carriers”)
  • Nutrition
  • Pregnancy
  • Circadian rhythm
44
Q

List at least one of the conditions associated w/ physiological factors that affect drug deposition?

A
  • Renal impairment
  • Hepatic impairment
  • Cardiac disease and/or congestive heart failure
  • Gastrointestinal disease
  • Burns
  • Shock
  • Trauma
45
Q

Response to a drug that is greater than expected if the drug were administered alone

A

Synergistic drug interaction

46
Q

Response to a drug that is less than expected than if the drug were adminstered alone

A

Antagonistic drug interaction

47
Q

Field of pharmacy which quantitatively studies drug disposition in the body, measuring LADME system for an individual patient, to set a specific dosage regimen for each patient

A

Pharmocokinetics

48
Q

Field of pharmacy which studies the interaction of pharmacologically-active substances w/ target sites and the biochemical and phsyiological consequences leading to therapeutic or adverse effects at the site of action

A

Pharmacodynamics

49
Q

What do the letters in the acronym LADME stand for?

A
L → liberation
A → absorption
D → distribution
M → metabolism
E → elimination
50
Q

Define liberation and the organ system involved

A

Process of a drug passing into solution

- Mouth

51
Q

Explain how liberation works in the LADME system

A
  • Saliva in the mouth causes the disintegration agent to swell, creating channels for the saliva
  • Fast-dissolving granules dissolve and the tablet disintegrates
52
Q

Define absorption and the organ system involved

A

Process of takin ghte drug into the body’s circulation

- GI tract, skin, intramuscular injection, or intrathecal injection

53
Q

Define distribution and the organ system involved

A

How drugs are delivered throughout the bloodstream after being absorbed
- Blood space → enter extravascular fluids → migrate into tissues or organs

54
Q

Define metabolism and the organ system involved

A

Process of biotransformation of the parent drug to one or more metabolites
- Liver and kidney, but also in plasma and muscle tissue

55
Q

Define elimination and the organ system involved

A

Final excretion of drug from the body

- Kidney (urine) and liver (bile and feces)

56
Q

Four sites of drug absorption

A
  • GI tract
  • Small intestine
  • Skin
  • Intramuscular/intrathecal injection
57
Q

When drugs are absorbed from the intestine they are transported by portal circulation to liver where they are substantially metabolized before reaching systemic circulation. This lowers the concentration of active parent drug.

A

First-pass metabolism

58
Q

7 general factors which affect drug distribution

A
  • Binding of drug to circulating blood components
  • Binding of drug to fixed receptors
  • Passage through membrane barriers
  • Ability to dissolve in structural or storage lipids
  • Molecular weight of drug
  • pKa of drug (acidic vs. basic)
  • Condition of patient
59
Q

Drug metabolism

- Two primary and two secondary sites of metabolism

A

Primary: liver and kidney
Secondary: plasma and muscle tissue

60
Q

Drug metabolism – Phase I

- Types of processes

A
  • Oxidation
  • Hydroxylation
  • Reduction
61
Q

Drug metabolism – Phase I

- Usual products

A

Active metabolites

62
Q

Drug metabolism – Phase I

- Change w/ age

A

Greater

63
Q

Drug metabolism –Phase II

- Types of processes

A

Conjugation

64
Q

Drug metabolism – Phase II

- Usual products

A

Inactive metabolites

65
Q

Drug metabolism – Phase II

- Change w/ age

A

Less

66
Q

Drug metabolism

- Differentiation of hepatic enzyme induction and inhibition

A

Inhibition: concentration of drug stays higher
Induction: ?

67
Q

How do zero order kinetics affect drug metabolism?

A
  • Constant AMOUNT per unit of time is metabolized

- Rate doesn’t increase as drug concentration increases

68
Q

How do first order kinetics affect drug metabolism?

A
  • Constant FRACTION per unti of time is metabolized

- Rate increases as drug concentration increases

69
Q

Two major routes of drug elimination

A

Kidney or liver

70
Q

Four minor routes of drug elimination

A
  • Skin (sweat)
  • Lungs (expired air)
  • Mammary glands (milk)
  • Salivary glands
71
Q

Why is protein binding of a drug important for distribution and elimination of a drug?

A

Alteration in protein concentration will alter the free and bound portions of drug in the blood stream.

  • Only FREE drug is available for distribution and elimination
  • Only FREE drug may cross cell membranes or may interact with cellular receptors
72
Q

Three general conditions which may cause altered protein binding of a drug

A
  • Uremia
  • Conditions of acute stress
  • Aging patients
73
Q

How does cardiac disease affect the LADME system?

A

Affects distribution and elimination of the drug

74
Q

How does liver disease affect the LADME?

A

Affects metabolism and elimination of a drug

75
Q

How does renal disease affect the LADME system?

A

Affects metabolism and elimination of a drug

76
Q

?

A

?

77
Q

Steady-state drug levels

- Number of half-lives before steady-state is achieved

A

4-5 half lives

78
Q

Steady-state drug levels

- Importance of monitoring peak and trough drug levels in setting dosing regimens

A

To avoid toxicity

79
Q

Active metabolites of procainamide

A

n-acetyl procainamide (NAPA)

80
Q

Active metabolite of primidone

A

Phenobarbital

81
Q

Active metabolite of theophylline

A

Caffeine

82
Q

Which microorganisms are susceptible to aminoglycosides?

A

Gram-negative

83
Q

What microorganisms are susceptible to chloramphenicol?

A

Gram-negative

84
Q

What microorganisms are susuceptible to vancomycin?

A

Some Gram-positive and some Gram-negative

85
Q

What is the specific disorder treated by lithium therapy?

A

Manic-depressive disorders (bipolar disorders)

86
Q

Organ transplant associated w/ cyclosporine

A
  • Inhibits cytokines that control lymphocyte proliferation
  • Reduces cellular response to Ags
  • Used after BM transplant
87
Q

Organ transplant associated w/ mycophenolic acid (MPA)

A
  • Inhibits transcription in T-lymphocytes

- Used after kidney transplants in combination w/ cyclosproine

88
Q

Organ transplant associated w/ sirolimus (Rapamycin)

A
  • Blocks lymphocyte proliferation due to inhibition of interleukin production
  • Used after kidney transplants
89
Q

Organ transplant associated w/ tacrolimus (Prograf or FK-506)

A
  • Blocks lymphocyte proliferation due to inhibition of interleukin production
  • Used after liver transplantation
90
Q

Why do certain drugs require monitoring?

A
  • Consequences of overdosing and underdosing are serious
  • Small difference b/w a therapeutic and toxic dose
  • Change in patient’s physiologic state that may unpredictably affect drug concentrations
  • Poor relationship b/w dose and circulating concentration but good correlation b/w circulating concentrations adn therapeutic/toxic effects
  • A drug interaction may be or is occurring
  • Monitor of patient compliance
91
Q

What happens when therapeutic drug monitoring is not indicated?

A

If dose and clinical response of patient have a good correlation, therapeutic drug monitoring is not indicated