Therapeutic Drug Markers Flashcards

1
Q

The mechanism of action is defined as the biochemical or physical process that occurs at the ___ to produce the pharmacological effect.

A

site of action.

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2
Q

For drug administration, the parenteral route is defined as…

A

Outside the intestine (i.e., IV, IM, SQ, etc.).

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3
Q

Drug action is ___ mediated at the cellular membrane.

A

receptor.

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4
Q

For drug administration, GI absorption can include…

A

Rectal/suppository.

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5
Q

The rate of absorbance is classified by which two biochemical methods?

A

Passive diffusion and dietary transport mechanism.

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6
Q

Which GI changes can affect drug absorption?

A

GI motility, pH, inflammation, food, and other drugs.

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7
Q

Define first pass metabolism.

A

a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the systemic circulation.

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8
Q

Which drug type correlates with therapeutic and toxic physiological effects? (Bound or Free)

A

Free drug.

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9
Q

Which two factors effect the amount of free drug available?

A

(1) Serum protein level; (2) Competitive binding for the receptor on the transport protein.

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10
Q

What is the major site of metabolic clearance and biotransformation?

A

Liver.

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11
Q

Unmetabolized drugs are termed the ___ compound; metabolized products are termed ___.

A

parent; metabolites.

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12
Q

Define xenobiotic.

A

Exogenous substances (drugs) that are capable of entering the metabolic pathway.

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13
Q

Describe Phase I enzyme reactions.

A

Chemical structure modification produces reactive intermediates.

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14
Q

What is the enzyme responsible for Phase I Enzyme reactions?

A

Cytochrome P450.

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15
Q

Describe Phase II Enzyme reactions.

A

The drug becomes water soluble because of the conjugation of the functional group.

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16
Q

How does the depletion of conjugate groups effect Phase I & II enzyme reactions?

A

Can create a backup of Phase I reactive intermediates which may become toxic.

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17
Q

How are free form drugs and metabolites eliminated by renal clearance?

A

Glomerular filtration - renal secretion through the tubules.

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18
Q

The rate of drug clearance correlates with ___ clearance.

A

creatinine.

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19
Q

How will a decreased GFR effect serum half life and concentration?

A

It will cause it to increase.

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20
Q

An IV bolus of a drug is what type of elimination?

A

First-order.

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21
Q

Define half life.

A

Time required for the concentration to be decreased by one half.

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22
Q

Define the drug distribution rate.

A

How long it takes the drug to distribute throughout the body.

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23
Q

Define minimum effective concentration (MEC).

A

Lowest concentration of the drug in the blood that will produce the desired result.

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24
Q

Define minimum toxic concentration (MTC).

A

The lowest concentration of the drug in the body that will produce an adverse response.

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25
Q

Define the therapeutic index.

A

The ratio of MTC/MEC; varies from drug to drug and patient to patient.

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26
Q

Define the therapeutic window.

A

Range between MEC and MTC.

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27
Q

Define trough.

A

Lowest concentration of drug measured in the blood.

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28
Q

Define peak.

A

Highest concentration of the drug measured in the blood.

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29
Q

The following graph is indicative of what type of elimination?

A

First-order

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30
Q

What is the most important factor of TDM sample collection?

A

Timing; trough or peak.

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31
Q

What samples are collected for TDM testing?

A

Serum or heparin plasma.

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32
Q

Why should gel tubes be avoided for TDMs?

A

They absorb drugs and cause a false decrease.

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33
Q

Why is EDTA avoided for TDM testing?

A

There is a change in distribution of drugs between cells and plasma.

34
Q

Calcium binding anticoagulants can cause changes in ___ between cells and plasma.

A

distribution.

35
Q

What is the most common testing method used for TDM?

A

Immunoassay.

36
Q

What complex lab methods are used for TDM testing?

A

Gas liquid chromatography (GLC); High Performance Liquid Chromatography (HPLC).

37
Q

Digoxin is used to treat…

A

Hear failure & arrhythmias.

38
Q

Therapeutic range of Digoxin.

A

0.8 - 2.0 ng/mL.

39
Q

Mechanism of action for Digoxin.

A

Increases cardiac contractility;
Inhibits Na, K, ATPase membrane pump decreasing intracellular K;
Increases intracellular calcium;
Increases cardiac contractility.

40
Q

3-Procainamide is used to treat…

A

Inappropriate ventricular contractions; tachycardia.

41
Q

Therapeutic range of 3-Procainamide.

A

4 - 12 ug/mL.

42
Q

Mechanism of action for 3-Procainamide.

A

Reduces cardiac excitability;

Increases the threshold membrane potential by blocking K outflow.

43
Q

3-Procainamide testing tests what two metabolites?

A

Procainamide and NAPA.

44
Q

4-Quinidine is used to treat…

A

Many types of arrhythmias after myocardial infarction.

45
Q

Therapeutic range of 4-Quinidine.

A

2 - 5 ug/mL.

46
Q

Mechanism of action of 4-Quinidine.

A

Reduces cardiac excitability;

Increases the threshold membrane potential by blocking K outflow.

47
Q

Aminoglycosides (antibiotics) are used to treat…

A

Aerobic gram negative bacterial infections.

48
Q

What is the mechanism of action for aminoglycosides?

A

Inhibits bacterial protein synthesis by binding the 30S ribosomal subunit.

49
Q

What is the therapeutic range for Gentamicin?

A

Peak: 5 - 8 ug/mL.
Trough: 1 - 12 ug/mL.

50
Q

What collection type should be used for Gentamicin?

A

Serum only.

51
Q

Vancomycin is used to treat…

A

Gram positive and some gram negative Methicillin resistant Staphyloccoci Endocarditis.

52
Q

What is the peak and trough therapeutic range of Vancomycin…

A

Peak: 20 - 40 ug/mL.
Trough: 5 - 10 ug/mL.

53
Q

What is the mechanism of action for Vancomycin?

A

Bactericidal, inhibits cell wall synthesis.

54
Q

Chloramphenicol is used to treat…

A

Broad spectrum antibiotic for resistant bacteria.

Concentrates in the cerebrospinal fluid.

55
Q

Therapeutic range for Chloramphenicol.

A

6 - 12 ug/mL.

56
Q

Mechanism of action for Chloramphenicol.

A

Inhibits bacterial protein synthesis by binding the 50S ribosomal subunit.

57
Q

1-Phenytoin is used to treat…

A

Corrects for grand mall seizures.

58
Q

Therapeutic range for 1-Phenytoin.

A

10 - 20 ug/mL.

59
Q

Mechanism of action for 1-Phenytoin.

A

Reduces synaptic transmission by modulating sodium channels.

60
Q

2-Phenobarbital and Primidone is used to treat…

A

Corrects for all types of seizures except absence (petit mal).

61
Q

Therapeutic range of 2-Phenobarbital and Primidone.

A

Phenobarb: 15 - 40 ug/mL.
Primidone: 5 - 12 ug/mL.

62
Q

What is the mechanism of action of 2-Phenobarbital and Primidone?

A

Reduces synaptic transmission, potentiates inhibition through the GABA receptor, increasing chloride flow.

63
Q

Carbamazepine is used to treat…

A

Seizures and trigeminal neuralgia (facial pain).

64
Q

What is the therapeutic range of Carbamazepine?

A

4 - 12 ug/mL.

65
Q

What is the mechanism of action for Carbamazepine?

A

Reduces synaptic transmission by modulating sodium channels; antidiuretic effect.

66
Q

Valproic acid is used to treat…

A

Petit mal, absence seizures. Used in combination with other antiepileptics.

67
Q

What is the mechanism of action for Valproic acid?

A

Reduces synaptic transmission; GABA transaminase inhibitor, increases GABA inhibition.

68
Q

Lithium is used to treat…

A

Bipolar disorder, manic phase.

69
Q

What is the therapeutic range of Lithium?

A

0.8 - 1.2 mmol/L.

70
Q

What is the mechanism of action of Lithium?

A

Enhances reuptake of catecholamines; sedating effects on the CNS.

71
Q

Tricyclic Antidepressants are used to treat…

A

Depression, insomnia.

72
Q

What is the therapeutic range of tricyclic antidepressants?

A

50 - 150 ng/mL.

73
Q

What is the mechanism of action for tricyclic antidepressants?

A

Inhibition of reuptake of catecholamines in the CNS; positive effect on mood.

74
Q

Theophylline is used to treat…

A

Asthma and COPD.

75
Q

What is the therapeutic range of theophylline?

A

8 - 20 ug/mL.

76
Q

What is the mechanism of action of Theophylline?

A

Relaxes bronchial smooth muscle; antagonist of adenosine receptors in smooth muscle.

77
Q

Caffeine is a minor metabolite of ___.

A

Theophylline.

78
Q

Caffeine is used to treat…

A

Neonate apnea.

79
Q

What is the therapeutic range of caffeine?

A

8 - 14 ug/mL.

80
Q

What is the mechanism of action for caffeine?

A

Relaxes bronchial smooth muscle; antagonist of adenosine receptors in smooth muscle.