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Med Chem Test 4 > Select Topics > Flashcards

Select Topics Flashcards

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1
Q

What is pharmacogenetics?

A

The individual impact on drug efficacy and toxicity. Genetics dictate enzyme differences across and within species.

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2
Q

What are the observable differences in human pharmacogenetics?

A

Enzyme effectiveness
DDIs
Drug toxicity

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3
Q

What are DMEs exhibiting polymorphisms?

A 
CYP2D6
CYP2C9
CYP2C19
UDP-Glucuronosyl Transferase (UGT 1A1)
NAT2
Thipurine S-MEthyltransferase (TPMT)
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4
Q

What is the consequence of being a CYP2C19 poor metabolizer in the different subpopulations when Mephenytoin is given?

A 
3 Phenotypes(EM, IM, PM)
3-5% Caucasians
12-23% Asians
3% African Americans
are poor metabolizers and thus have sedation when given Mephenytoin.
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5
Q

What subpopulations does CYP2D6 have?

A

PM-poor metabolizers
IM-intermediate metabolizers
EM-extensive metabolizers
UM-ultra-rapid metabolizers

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6
Q

What phenotypic subpopulations does NAT2 have?

A 
Rapid acetylators (Eskimos)
Slow acetylators (Egyptians)
affects Isoniazid
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7
Q

What are NAT2 slow acetylators associated with?

A

10-20% decrease in enzyme amounts in liver cytosol and decrease in NAT2 enzyme activity.

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8
Q

When was the Human Genome Project Established?

A

1990

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9
Q

When was the emergence of pharmacogenomics?

A

1995

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10
Q

What is pharmacogenomics?

A

It involves the genome-wide anaylsis of genetic determinants of drug efficacy and toxicity.
Requires genetic profiling and advocates genetically guided therapy.
Used in chemotherapy.

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11
Q

What is the ultimate goal of pharmacogenomics?

A

Tailored, personalized, individualized drug therapy.

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12
Q

What is polymorphism?

A

Variations in DNA nucleotide sequences

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13
Q

What are the types of polymorphism?

A 
Single nucleotide (A,T,C,G) polymorphism (SNP)
>1 nucleotide changes
Entire gene insertion
Entire gene deletion
Extra gene copies
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14
Q

What are the effects of polymorphism?

A

Lead to disease
Alter protein function (DME)
Ultimately drug therapeutic efficacy is impacted.

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15
Q

Which enzyme has 80 plus different alleles?

A

CYP2D6

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16
Q

What is important about CYP2D6*5?

A

It has deleted nucleotide base pairs in the 2D6 gene
Not a SNP
Results in loss of CYP2D6 function which makes it a poor metabolizer phenotype.

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17
Q

What drugs does CYP2D6*5 affect?

A

Metoprolol, SSRIs, codeine, atomoxetine, tamoxifen, etc. (MS.CAT)

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18
Q

What is important about TPMT*3?

A 
Thiopurine methyltransferase (TPMT)
A SNP(single nucleotide polymorphism)
Results in decreased TPMT activity.
19
Q

What drugs does TPMT*3 affect?

A

Azathiprine, 6-mercaptopurine which causes fatal myelosuppression

20
Q

Genetic testing is suggested because of what polymorphic DMEs?

A

2C19, 2C9, 2D6, TPMT

21
Q

What drugs should genetic testing be suggested for?

A

Warfarin
Atomoxetine
6MP or Azathioprine
Tamoxifen

22
Q

What enzyme should be tested before being given Warfarin?

A

CYP2C9

23
Q

What enzyme should be tested before being given Atomoxetine and Tomoxifen?

A

CYP2D6

24
Q

What enzyme should be tested before being given 6MP or Azathioprine?

A

TPMT

25
Q

What consequences are from PMs(poor metabolizer)?

A

Toxicity

26
Q

What consequences are from UMs(ultra metabolizers)?

A

Therapeutic failure

27
Q

What is metabolomics?

A

Identification of small molecule metabolites in body fluids to create unique ‘fingerprints’

28
Q

Endogenous metabolites (lipids, etc.) are under tight ______ _____.

A

Endogenous metabolites are under tight homeostatic control.

29
Q

What can metabolomics identify?

A

disease markers

metabolism phenotypes

30
Q

What enzyme activities are low in children?

A 
CYP450
1st pass effect low for 1A2, 2C9, & 3A4
MAOB & EHs
ADH
NAT
AA (perhaps due to low glycine)
SULT (almost mature)
DME activity increase with age but can be compromised in malnourished children.
31
Q

What affects pregnancy drug metabolism?

A

Estrogen, progesterone, placental growth, hormones, prolactin, etc.

32
Q

What enzyme changes occur in pregnancy?

A

CYP1A2 activity decreases
CYP2D6 & CYP3A activities increases
UGT1A1/4 & other UGTs activities increase
NAT2 activity decreases.

33
Q

What enzymes are involved in alcohol metabolism?

A

Alcohol dehydrogenase
Catalase
CYP450 or Microsomal Ethanol Oxidizing System (MEOS)

34
Q

What is important about Ethylene Glycol and Diethylene Glycol?

A

Sweet & odor-less liquids
Metabolized by ALDH, ADH to toxic metabolites
Metabolic acidosis
Accidental and intentional poisonings

35
Q

Obesity causes what type of enzyme activities?

A

Decreased CYP450 activities (3A4 &2E1)

Increased Phase II conjugations (UGT, SULT, GST, AA) causes shorter duration of action.

36
Q

What bodily functions are affected by obesity?

A

Cardiac output & liver blood flow increase in obesity.

Altered enterohepatic recirculation.

37
Q

Obesity causes a disruption of drug metabolism and transport which….

A

causes reduced efficacy or increased toxicity.

38
Q

What are antioxidant enzymes?

A

superoxide anion, peroxyl, hydroxyl, alkoxyl, hydroperoxyl, lipid peroxyl, nitric oxide, nitrogen dioxide, hydrogen peroxide, peroxynitrate, peroxynitrite, hypochlorous acid.

39
Q

What is Xanthine Oxidase?

A

Metabolizes purines and pyrimidines.

40
Q

What drugs does Xanthine oxidase affect?

A

Thiopurines &methylxanthines

41
Q

Where are the highest XO levels?

A

liver and intestines

42
Q

What is the rare disease that causes no XO?

A

Xanthinuria

43
Q

Males or Females have more Xanthine oxidase?

A

Males

44
Q

What is the main indication of XO inhibitors is?

A

Hyperuricemia & Gout(precipitation of Na Urate crystals in various tissues)

Med Chem Test 4 (6 decks)

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