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Pharmacology: Exam 3 > Lecture 8: Pharmacogenetics > Flashcards

Lecture 8: Pharmacogenetics Flashcards

1
Q

What is pharmacogenetics?

A

A field concerned with unusual (idiosyncratic) drug responses that have a hereditary basis.

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2
Q

A pharmacogenetically related response is different from an _ or _ phenomenon (an adverse reaction to a drug resulting from previous sensitization to the same drug or a closely related one)

A

Overdose or allergic

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3
Q

Many drugs are metabolized by what?

A

Cytochrome P50 Enzyme

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4
Q

What are tests for determining metabolizer phenotype?

A
  • Desbrisoquine
  • Sparteine
  • Dextromethorphan
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5
Q

What are the four phenotype categories?

A
  • Poor metabolizers (PM)
  • Intermediate metabolizers (IM)
  • Extensive metabolizers (EM)
  • Ultra-rapid metabolizers (UM)
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6
Q

What are genotyping tests for mutant alleles ?

A

Polymerase chain reaction (PCR)

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7
Q

The CYP2D gene clusters on a given allelic DNA fragment may contain between _ copies of functional genes

A

zero to thirteen copies

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8
Q

Which CYP enzymes are pseudogenes and functional gene?

A
  • CYP2D7 and CYPD8 are pseudogenes
  • CYP2D6 is a functional gene
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9
Q

What is located on the long arm of chromosome 22?

A

CYP2D6 and is autosomal

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10
Q

What are major classes of currently used drugs which their metabolism are significantly affected by the CYP2D6 polymorphism? ⭐️

A

Antiarrhythmic agents, B-adrenergic receptor antagonists, anti-psychotics, and tricyclic antidepressent

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11
Q

What happens with patients that take B blockers?

A

is estimated that 15 to 20 percent of patients who undertake therapy with the b-blockers are forced to discontinue their use due to adverse reactions.

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12
Q

Flecanide and propafenone:
1. What type of class?
2. Big or narrow therapeutic window
3. What group does this drug affect with symptoms?

⭐️ ⭐️ ⭐️ ⭐️

A
  1. antiarrhythmic agents
  2. narrow therapeutic window
  3. High concentration (PM) can lead to ventricular tachycardia or fibrillation.
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13
Q

What happens in PM individuals that take tricyclic antidepressants? ⭐️

A

Symptoms of the overdose are sedation and tremors

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14
Q

What is the impact of therapy in fast, intermediate, poor metabolizers with ACTIVE DRUG and INACTIVE metabolite? ⭐️

A
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15
Q

Codeine is an example of a drug that requires what gene for metabolic activation?

A

CYP2D6-> prodrug

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16
Q

Codeine is nearly ineffective as an _ in 5 to 10 percent of population (_).

A

Codeine is nearly ineffective as an analgesic in 5 to 10 percent of population (PM).

17
Q

What is a prodrug that is used for breast cancer? How does it work? How does this drug affect group PM? ⭐️

A
  • Tamoxifen
  • It is a competitive antagonist of estrogen receptor
  • There is a high risk of relapse in PM
18
Q

What is the impact of therapy in fast, intermediate, poor metabolizers with INACTIVE PRODRUG and TOXIC metabolite 🌟

A
19
Q

What is caused by glucose-6-phosphate dehydrogenase deficiency ⭐️

A

Increased Susceptibility to Drug-Induced Hemolysis

20
Q

What drug causes acute hemolysis in approximately 10% of African Americans? ⭐️

A

anti-malarial drug = primaquine

21
Q

Why does the anti-malarial drug primaquine cause acute hemolysis? ⭐️

A

Due to the reduction in the concentration of reduced glutathione (GSH) because there is a Glucose-6-Phosphate Dehydrogenase Deficiency (no NADPH)

22
Q

There are approximately 300 G6PD variants. What are the two main variants?

A
  • A-type → mainly occurs in African Americans
  • More severe type → Mediterranean population (Mediterranean type).
23
Q

What drugs (4) are affected by N-acetyltransferases? ⭐️

A

The metabolism of these drugs is affected:

  • isoniazid
  • procainamide
  • hydralazine
  • caffeine
24
Q

What side is fast acetylaters and slow? ⭐️

A

Left: fast
Right slow

25
Q

What does rocainamide and hydralazine in PM individuals cause? ⭐️

A

Drug-induced Lupus Erythematosus can develop with prolong use of drugs with aromatic amines

Pharmacology: Exam 3 (8 decks)

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