Therapeutic Drug Monitoring Flashcards

1
Q

What is therapeutic drug monitoring?

A

the measurement of drugs and/or their metabolites in body fluids-usually blood-to maintain therapeutic benefits

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2
Q

What is the definition of drugs (for the purpose of this class)?

A

medications that are prescribed by medical providers

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3
Q

What is the definition of therapeutic range (TR)?

A

the dose, or concentration, range of a drug within which the drug produces the desired therapeutic effect​

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4
Q

What is the result if a drug is outside of the therapeutic range?

A

Inefficacy or toxicity

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5
Q

What are the two main purposes of TDM?

A
  • Ensure correct drug dosages for the T.R.​
  • Identify drug-drug interactions if multiple drugs are taken together
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6
Q

When would TDM be appropriate for a drug?

A
  • The drug has a narrow therapeutic range
  • Marled pharmacokinetic variabilities
  • Critical adverse effects
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7
Q

All of the following are what?

Age​

Gender​

Genetics​

Diet​

Co-administered drugs​

Naturopathic agents

A

Factors that influence drug concentrations and efficacy

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8
Q

Define pharmacokinetics

A

Study of the movement of drugs in the body

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9
Q

What does pharmacokinetics tell us?

A

Provides a time-course of drug concentrations in the body as a function of absorption, distribution, metabolism, and excretion

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10
Q

What is bioavailability?

A

The fraction of the administered dose that eventually reaches its site of action​

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11
Q

The following are all examples of what?

Oral—most common, least invasive​

Intravenous (IV)—most direct & effective​

Intramuscular (IM)​

Subcutaneous (SC)​

Aerosol​

Transdermal patch​

Rectal

A

Routes of administration

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12
Q

What are the three factors that effect the efficiency of absorption from GI tract?

A
  • Dissociation from its administered form​
  • Solubility in GI fluids​
  • Diffusion across GI membranes
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13
Q

T/F:

In order for a drug to passively diffuse from the GI tract to the bloodstream, it must be in the hydrophilic state.

A

FALSE

The drug must be in the hydrophobic state (nonionized)

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14
Q

Drugs will be absorbed in the GI tract ____ in healthy people.

A

Predictably

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15
Q

Weak acids are efficiently absorbed by the __a__; weak bases are absorbed in the __b__

A

a) Stomach

b) intestine

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16
Q

Drug absorption is affected by what?

A

Changes in intestinal motility, pH, inflammation

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17
Q

T/F:

Absorption is not changed wen someone is getting older, becomes pregnant, or develops a pathological condition.

A

FALSE

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18
Q

What is the definition of drug distribution?

A

The movement of a drug between blood circulation and tissues and organs and the relative proportion of the drug in the tissues​

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19
Q

____ ____ affects the ability of a drug to leave circulation

A

Lipid Solubility

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20
Q

What is a free fraction?

A

The portion of a drug that exerts a pharmacologic effect​

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21
Q

Free fractions can diffuse out of the __a__ and into the __b__ and __c__ spaces.

A

a) vasculature

b) interstitial

c) intracellular

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22
Q

What is the formula for drug distribution?

A

The volume of distribution of a drug = (dose of the drug) / (concentration of the drug​)

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23
Q

The following are characteristics of what protein?

Majority of plasma protein constituents​

Major transporter of drugs​

Changes in concentration affects free vs bound

A

Albumin

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24
Q

T/F:

Most drugs are subject to binding with serum protein constituents to form drug-protein complexes

A

TRUE

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25
Only ________ fractions can interact with the site of action to result in a biologic response
Free/unbound
26
All drugs absorbed from the intestine (except rectum) enter what system?
Hepatic portal system
27
What is the first pass effect?
The phenomenon in which a drug is metabolized, results in a reduced concentration o the drug before reaching the circulatory system
28
What are the consequences of impaired liver function?
- Reduced ability to metabolize - Effects ability to perform biotransformation to produce the therapeutically active metabolite of the drug - May require dosing adjustments
29
What are xenobiotics?
Makes up the most drugs. They are exogenous substances capable of entering biochemical pathways that are meant for endogenous substances
30
_____ is the biochemical pathway responsible for a large portion of drug metabolism​
Hepatic mixed function oxidase (MFO) systems
31
What are the two basic function of MFO?
- Involves taking hydrophobic substances & through a series of enzymatic reaction, converts them to water soluble products​ - Products can then be transported into the bile or released into general circulation for elimination by renal filtration
32
Result of Phase 1 reactions in MFO
To produce reactive intermediates
33
Result of Phase 2 reactions in MFO
Conjugate functional groups to reactive sites in water-soluble products
34
T/F: Drug elimination is dependent on the clearance mechanism
FALSE: Independent of clearance mechanism, decreases in the plasma drug concentration most often occur as a first-order process
35
For drugs not secreted or reabsorbed, the elimination rate directly relates to ____
Glomerular Filtration Rate (GFR) A decreased GFR results in increased half life and plasma concentration
36
Many drugs metabolized in the liver are excreted in ____
Bile
37
T/F: When administering drugs on a schedule, you only want the peak blood drug concentration to be in the therapeutic range
FALSE You want to have both peak and trough concentrations to be in the therapeutic range
38
How many doses are typically needed to reach a steady-state oscillation?
5-7 doses
39
What is the definition of pharmacodynamics?
- The study of the biochemical and physiological effects of drugs and their mechanisms of action​ - Describes the relationship between a drug’s concentration at its site of action and its pharmacological responses​
40
What is the single most important factor of specimen collection?
Accurate timing of specimen collection
41
When is the trough typically drawn?
Right before the next dose or random
42
If on oral meds, when is the peak drawn?
1 hour post oral dose
43
If on V medication, when is the peak drawn?
90 min post IV dose
44
T/F: You want to draw peaks only after that 5-7 dose steady oscillation is achieved
TRUE
45
What tube is preferred for medication testing?
Serum (RED)-- NO GEL as it may interfere
46
What tube do you collect for immunosuppressive drug testing?
EDTA WB
47
What is the definition of pharmacogenomics?
The science of studying variations and developing drug therapies to compensate for the genetic differences impacting therapy regimens​
48
What is the difference between a responder and a nonresponder?
Responders will have the benefits of the therapeutic/desired effects of a drug while Nonresponders do not.
49
What is the prominent gene that affects drug metabolism?
Cytochrome P450 (CYP450)
50
What does CYP450 tell us?
Indicates which drug would work best, predicts interactions, or if there would be a benefit
51
Digoxin
One of the most common cardioactive drugs. It is a cardiac glycoside and treats arrythmias and CHF. Inhibits membrane Na-K-ATPase LONG half live as once it is in the tissues it stays
52
Quinidine
Cardioactive Drug Natural from bark to treat arrythmias
53
Disopyramide
Cardioactive Drug Substitute for Quinidine
54
Procainamide and N-Acetylprocainamide
Cardioactive Drug
55
What is NAPA?
Cardioactive Drug The hepatic metabolite of procainamide that works similarly to parent drug
56
Aminoglycosides
Antibiotic Treats gram neg and gram pos infections Inhibits bacterial protein synthesis
57
Gentamicin
Antibiotic Treats GNR - life threatening
58
T/F: Nephrotoxicity is always reversible without compromising renal function
FALSE Nephrotoxicity is USUALLY reversible but it CAN CAUSE renal failure
59
T/F: Ototoxicity is irreversible
TRUE
60
Tobramycin
Antibiotic Treats GNR Ototoxic and nephrotxic
61
Amikacin
Antibiotic Treats severe blood infections
62
Vancomycin
Antibiotic Glycopeptide antibiotic Against GPC and GPR
63
What are adverse effects of vancomycin?
- Redman syndrome (extremity flushing) - Nephrotoxicity - Ototoxicity
64
Antiepileptic Drugs (AEDs)
Treat and suppress seizures Only effective while drug metabolites are in the body TDM is critical
65
Primidone
AED grand mal seizure-- when resistance to other AEDs
66
Phenobarbitol
AED
67
Phenytoin and Free Phenytoin
AED Common treatment for seizure disorder and short term prophylactic agent in brain injury
68
What percentage do we have bound and free form of phenytoin and free phenytoin in the body?
90% bound form 10% free form We need both in the body with some individualism as every body is different
69
Carbamazepine (Tegretol)
AED Severe adverse events (only use if nonresponsive to other AED)
70
Valproic Acid (Depakote)
AED
71
Gabapentin (Neurontin)
AED Used for seizures and pain management
72
Lithium
Psychoactive drug Mood altering and used to treat bipolar, depression, aggresive/self-mutilatin, cluster headache, migraines NO LIHEP TUBES
73
Tricyclic Antidepressants (TCAs)
Psychoactive drug Used to treat depression, insomnia, extreme apathy, loss of libido
74
Clozapine (Clozaril, FazaClo)
Psychoactive drug Treats refractory schizophrenia
75
Olanzapine (Zyprexa)
Psychoactive drug Treats schizophrenia, acute manic episodes, bipolar disorder
76
Immunosuppressive Drugs
TDM used to monitor Immunosuppressive Drugs to prevent organ rejection Most require est. of individual dosage regimens
77
Clyclosporine
Immunosuppressive Drug Suppress graft vs host rejection
78
Tacrolimus FK-506
Immunosuppressive Drug Oral, 100x more potent than cyclosporine
79
Sirolimus
Immunosuppressive Drugs Antifungal agent to prevent graft rejection in kidney transplants
80
Everolimus
Immunosuppressive Drug Derived from Sirolimus Short half live results in a more rapid achievement of steady state pharmacokinetics WB
81
Mycophenolic Acid (MPA)
Immunosuppressive Drug MPA is the active from of Mycophenolate mofetil which is a prodrug that rapidly converts to in the liver to MPA
82
Antineoplastics
Pharmacodynamics are hard to est. so TDM isn't as useful Many rapidly metabolized or incorporated into cellular macromolecular structures​ Delivered dose more relevant than circulating concentrations​
83
Methotrexate
Antineoplastic TDM offers some benefits to est. therapeutic regimen
84
Theophylline
Bronchodilator Used to treat respiratory disorder