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Hematology > Antiplatelets Pharmaco > Flashcards

Antiplatelets Pharmaco Flashcards

1
Q

What is Pharmacogenetics

A

Study of genetic cause of individual variations with drug response

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2
Q

What is pharmacogenomic

A

Genome wide analysis of genetic determinant of drug efficacy and toxicity

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3
Q

Two forms of variability

A

PK variability

PD variability

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4
Q

Differences in those concepts leads to PK variability

A

Absorption
distribution
metabolism
elimination

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5
Q

If variation is due to genes what could be possible causes

A

Single nucleotide polymorphism

insertion /deletion

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6
Q

Frequency of single nucleotide polymorphism in human genome

A

Every hundred to 1000 base pairs

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7
Q

Population with highest number of the population specific polymorphism

A

African Americans

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8
Q

What does pharmacokinetic variability refers to

A

Variability in the amount of drug delivered to a receptor depending on factors such as Absorption Distribution metabolism and excretion

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9
Q

What does Pharmacogenetics Like to focus on in drug pharmacokinetics factors

A

Metabolism

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10
Q

What is the goal of metabolism

A

Conversion of foreign substances or or xenobiotics into water soluble metabolites which are more easily excreted

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11
Q

Enzymes involved in metabolism

A

Xenobiotics metabolizing enzymes

drug metabolizing enzymes

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12
Q

Example of prodrug

A

Codeine into morphine

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13
Q

What is a poor metabolizer phenotype

A

Enzyme deficiency

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14
Q

Can poor metabolizer phenotype lead to toxic drug concentration

A

Yes

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15
Q

Can poor metabolizer phenotype need to save therapeutic effect of prodrug

A

Yes

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16
Q

What is an ultra rapid metabolizer phenotype

A

Has increased in gene copy number with increased expression of active enzyme

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17
Q

Do ultra rapid metabolizers have ineffective drug therapy due to low drug concentration at target sides

A

Yes

18
Q

Do ultra Rapid metabolizer have high therapeutic efficacy when it comes to prodrug

A

Yes

19
Q

Can you have polymorphism of drug transporters in absorption distribution and excretion

A

Yes

20
Q

Two categories of drug metabolizing enzyme

A

Phase 1 functionalizinf enzyme

Phase 2 conjugating enzyme

21
Q

What do phase I enzymes do

A

Introduce or remove functional group in drug through oxidation , reduction or hydrolysis

22
Q

What do phase II enzymes do

A

Transfer moieties from cofactor to a substrate

23
Q

Main phase I enzymes

A

Cyt p450

24
Q

4 phenotypes of patients based on CYP

A

Poor metabolizer - abolished activity
Intermediate metabolizer - reduced activity
Extensive metabolizer - normal activity
Ultra rapid metabolizer - enhanced activity

25
Q

Should you increase or reduce dose of drugs in PM patient metabolized by phase I enzymes

A

Lower

26
Q

Should you increase or reduce dose of drugs in UM patient metabolized by phase I enzymes

A

Increase

27
Q

Main enzymes with high polymorphism

A

CYP2D6
CYP2C9
CYP2C19
Plasma cholinesterase

28
Q

Amtiplagels wirh high variability

A

Clopidogrel
Warfarin
Dabigatran

29
Q

Is clopidogrel a prodrug

A

Yes

30
Q

What is the action of clopidogrel

A

Irreversibly binds to platelet ADP receptor leading to platelet aggregation inhibition

31
Q

Metabolism of clopidogrel

A

CYP450

CYP2C19

32
Q

Enzymes involved in clopidogrel metabolism

A

CYP2C19

33
Q

Loss of function CYP2C19 2 and 3consequence

A

Adverse ischemic event

34
Q

CYP2C19 17 gain of function consequence

A

Higher catalytic effect
Decreased ischemic event
Risk of bleeding

35
Q

Action of warfarin

A

Vitamin K antagonist used in prevention of Venus thromboembolism

36
Q

Enzyme involved in metabolism of warfarin

A

CYP2c9 enzyme

37
Q

What is the function of CYP2C9 2 anD 3 leads to…

A

Increased risk of bleeding by impairing warfarin metabolism

38
Q

Gene responsible for polymorphism of

A

VKORC1

39
Q

If a person has expression of VKORC1 variant , Are they more sensitive or insensitive to warfarin

A

Sensitiv

40
Q

What is the dabigatran Etexilate

A

Prodrug which metabolizes esterases into direct thrombin inhibitor dabigatran

41
Q

What is the polymorphism of dabigatran

A

Single nucleotide polymorphism in CES1 gene Which decreases concentration of dabigatran

Hematology (24 decks)

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