Therapeutic Drug Monitoring (TDM | F) Flashcards

1
Q

What are the goals of TDM?

A

1) To ensure that a given drug dosage produces:
a. Maximal therapeutic benefit
b. Minimal toxic adverse effects
2) Must have an appropriate conc. at site of action that produces benefits

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2
Q

True or False

In relation w/ TDM, std dosages are derived from healthy population

A

True

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3
Q

In relation w/ TDM, only the free fraction of drugs can interact w/ site of action, resulting in what?

A

In a biologic response

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4
Q

What are the different routes of administration?

A

1) Injections
a. Circulation = IV (intravenous)
b. Muscles = IM (intramuscular)
c. Skin = SC (subcutaneous)
d. Epidermal
2) Inhaled
3) Absorbed through skin
4) Rectal
5) Oral

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5
Q

What is the most common route of administration?

A

Oral

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6
Q

What is pharmacokinetics?

A

It involves the dynamics associated w/ the movement of drugs across cell membranes

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7
Q

What are the biological events that are involved in pharmacokinetics?

A

1) Absorption
2) Distribution
3) Metabolism / Biotransformation
4) Excretion

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8
Q

What is the relationship present in pharmacokinetics?

A

Relationship of drug conc. to time

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9
Q

The process of pharmacokinetics assists in what?

A

In establishing or modifying a dosage regimen

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10
Q

What is absorption (as 1 of the biological events included in pharmacokinetics)?

A

It is the rate at w/c drug leaves the site of administration and the extent to w/c this happens

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11
Q

What are the different mechanisms of absorption (w/c is 1 of the biological events included in pharmacokinetics)?

A

1) Passive diffusion

2) Active transport

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12
Q

What is the principle of absorption (w/c is 1 of the biological events included in pharmacokinetics)?

A

Limiting factors

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13
Q

What is the route of administration for absorption (w/c is 1 of the biological events included in pharmacokinetics)?

A

Oral administration

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14
Q

Oral administration depends on what (in relation to absorption)?

A

1) Formulation of drug
- > liquid / pill
2) Intestinal motility
3) pH
4) Inflammation
5) Food
6) Presence of other drugs
7) Pt age
8) Pregnancy
9) Concurrent pathologic conditions

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15
Q

Where does metabolism (w/c is 1 of the biological events included in pharmacokinetics) occurs where?

A

In the liver

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16
Q

What is the principle of metabolism (w/c is 1 of the biological events included in pharmacokinetics)?

A

Biotransformation of the parent drug molecule into 1 or more metabolites

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17
Q

What are the metabolites (in relation w/ metabolism)?

A

1) H2O soluble
2) Easily excreted by kidney / liver
3) Pharmacologically active or inactive

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18
Q

The distribution (w/c is 1 of the biological events included in pharmacokinetics) depends on what?

A

1) Blood flow
2) Capillary permeability
a. pH gradients
b. lipid solubility of the drug
3) Binding of drugs to proteins / availability of free fractions
a. Free vs. bound drug
4) Tissue volume

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19
Q

What are the elimination routes (in relation w/ excretion w/c is 1 of the biological events included in pharmacokinetics)?

A

1) Hepatic metabolism
2) Renal filtration
3) Other
a. Skin
b. Lungs
c. Mammary glands
d. Salivary glands

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20
Q

In relation to elimination (w/c is related w/ excretion), fxnal changes in organs can affect what?

A

Elimination rate

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21
Q

Provide an ex of the principle of fxnal changes in organs w/c can affect elimination rate (in relation w/ elimination)

A

Hepatic disease w/ a loss of tissue result in slow rate of clearance w/ a longer half-life

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22
Q

What is elimination half-life (in relation w/ elimination)?

A

It is the time required to reduce the blood lvl conc. to one-half after equilibrium is obtained

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23
Q

In pharmacokinetics, how are most drugs given?

A

Most drugs are given on a scheduled basis (not as a single dosage)
-> oscillation between a max. (peak) and a min. (trough) of serum conc.

24
Q

What is the principle of the goal of dosage regimens (in pharmacokinetics)?

A

Achieve troughs in therapeutic range and peaks that are non-toxic

25
Q

What are the different drug grps?

A

1) Cardioactive
2) Antibiotics
3) Antiepileptic
4) Psychotherapeutic
5) Antiasthmatic
6) Immunosuppressive
7) Antineoplastic
8) Antihypertensive

26
Q

What are the different drugs under the cardioactive drug grp?

A

1) Digoxin
2) Lidocaine
3) Quinidine
4) Procainamide

27
Q

What are the actions of digoxin?

A

1) Used to treat congestive heart failure (CHF)
2) Inhibits Na and K transport within the heart
3) Allows for better cardiac muscle contraction and rhythm

28
Q

What is the characteristic of digoxin?

A

It peaks draw at 2 hrs post dose

29
Q

What are the actions of lidocaine?

A

1) It is used to treat premature ventricular contractions

2) It affects the timing of cardiac contraction

30
Q

What is the characteristic of lidocaine?

A

It is a common dental anesthetic

31
Q

What are the actions of quinidine?

A

1) It is used to treat cardiac arrhythmic problems
2) It inhibits Na and K channels
3) It prevents arrhythmias
4) It prevents atrial flutter
5) It prevents fibrillation

32
Q

What are the actions of procainamide?

A

1) It is used to treat cardiac arrhythmic situations
2) It blocks Na channels
3) It affects cardiac muscle contraction

33
Q

How is procainamide often measured?

A

It is often measured w/ N-Acetyl procainamide (NAPA)

34
Q

What are the different drugs under antibiotics drug grp?

A

1) Aminoglycosides

2) Vancomycin

35
Q

What are the actions of aminoglycosides?

A

1) It is used to treat infections w/ gram-(-) bacteria that are resistant to less toxic antibiotics
2) It inhibits protein synthesis of the microorganism

36
Q

What are the exs of aminoglycosides?

A

1) Gentamicin
2) Tobramycin
3) Amikacin
4) Kanamycin

37
Q

What are the actions of vancomycin?

A

1) It is used to treat infections w/ more resistant gram-(+) cocci and bacilli
2) It inhibits cell wall synthesis

38
Q

What generation antiepileptics (AEDs) are mostly used to treat seizure disorders and epilepsy?

A

1st and 2nd

39
Q

What are the exs of 1st generation AEDs?

A

1) Phenobarbital
- > Barbiturate Primidone its proform
2) Phenytoin
- > = Dilantin
3) Valproic acid
- > = Depakene
4) Carbamazepine
- > = Tegretol

40
Q

What are the exs of 2nd generation AEDs?

A

1) Felbamate
2) Gabapentin
3) Levetiracetam
4) Oxcarbazpine
5) Tigabine
6) Topiramate

41
Q

What are the drugs under the psychotherapeutic drug grp?

A

1) Lithium
2) Tricyclic antidepressants (TCAs)
3) Clozapine

42
Q

What is the action of lithium, TCAs, and clozapine?

A

These are used to treat manic depression (bipolar disorder)

43
Q

What are the drugs under the antiasthmatic drug grp?

A

1) Theophylline
2) Pulmicort
3) Theobromine

44
Q

What is the action of drugs under the antiasthmatic drug grp?

A

These are used to treat neonatal breathing disorders or respiratory disorders (of adults or children)

45
Q

What are the drugs under the immunosuppressive drug grp?

A

1) Cyclosporine

2) Tacrolimus (Prograf)

46
Q

Why is the monitoring of the immunosuppressive drug grp impt?

A

To prevent organ transplant rejection (graft vs. host)

47
Q

What is the action of the immunosuppressive drug grp?

A

These are used to treat autoimmune disease as well

48
Q

What is the sx of choice for cyclosporine?

A

Whole blood

49
Q

Why is whole blood the sx of choice for cyclosporine?

A

Since it sequesters in the RBC

50
Q

What is the action of tacrolimus?

A

It prevents rejection of liver and kidney transplants

51
Q

What is the drug under the antineoplastics drug grp?

A

Methotrexate

52
Q

What is the action of methotrexate?

A

It inhibits DNA synthesis

53
Q

What is the action of the antineoplastics drug grp?

A

It inhibits RNA / DNA synthesis of tumor cells (leading to cell death)

54
Q

What are the actions of the antihypertensive drug grp?

A

1) It is used in treatment of high BP

2) It dilates blood vessels

55
Q

What is the drug under the antihypertensive drug grp?

A

Sodium nitroprusside

56
Q

What is the action of sodium nitroprusside?

A

It is used for short-term control of hypertension

57
Q

What are the techniques for measurement of TDM?

A

1) Immunoassays
2) Gas chromatography
3) Liquid chromatography
4) Mass spectrometry