Antiplatelets Pharmaco

Question 1

What is Pharmacogenetics

Answer 1

Study of genetic cause of individual variations with drug response

Question 2

What is pharmacogenomic

Answer 2

Genome wide analysis of genetic determinant of drug efficacy and toxicity

Question 3

Two forms of variability

Answer 3

PK variability

PD variability

Question 4

Differences in those concepts leads to PK variability

Answer 4

Absorption
distribution
metabolism
elimination

Question 5

If variation is due to genes what could be possible causes

Answer 5

Single nucleotide polymorphism

insertion /deletion

Question 6

Frequency of single nucleotide polymorphism in human genome

Answer 6

Every hundred to 1000 base pairs

Question 7

Population with highest number of the population specific polymorphism

Answer 7

African Americans

Question 8

What does pharmacokinetic variability refers to

Answer 8

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

Question 9

What does Pharmacogenetics Like to focus on in drug pharmacokinetics factors

Answer 9

Metabolism

Question 10

What is the goal of metabolism

Answer 10

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

Question 11

Enzymes involved in metabolism

Answer 11

Xenobiotics metabolizing enzymes

drug metabolizing enzymes

Question 12

Example of prodrug

Answer 12

Codeine into morphine

Question 13

What is a poor metabolizer phenotype

Answer 13

Enzyme deficiency

Question 14

Can poor metabolizer phenotype lead to toxic drug concentration

Answer 14

Yes

Question 15

Can poor metabolizer phenotype need to save therapeutic effect of prodrug

Answer 15

Yes

Question 16

What is an ultra rapid metabolizer phenotype

Answer 16

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

Question 17

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

Answer 17

Yes

Question 18

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

Answer 18

Yes

Question 19

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

Answer 19

Yes

Question 20

Two categories of drug metabolizing enzyme

Answer 20

Phase 1 functionalizinf enzyme

Phase 2 conjugating enzyme

Question 21

What do phase I enzymes do

Answer 21

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

Question 22

What do phase II enzymes do

Answer 22

Transfer moieties from cofactor to a substrate

Question 23

Main phase I enzymes

Answer 23

Cyt p450

Question 24

4 phenotypes of patients based on CYP

Answer 24

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

Question 25

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

Answer 25

Lower

Question 26

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

Answer 26

Increase

Question 27

Main enzymes with high polymorphism

Answer 27

CYP2D6 CYP2C9 CYP2C19 Plasma cholinesterase

Question 28

Amtiplagels wirh high variability

Answer 28

Clopidogrel Warfarin Dabigatran

Question 29

Is clopidogrel a prodrug

Answer 29

Yes

Question 30

What is the action of clopidogrel

Answer 30

Irreversibly binds to platelet ADP receptor leading to platelet aggregation inhibition

Question 31

Metabolism of clopidogrel

Answer 31

CYP450 | CYP2C19

Question 32

Enzymes involved in clopidogrel metabolism

Answer 32

CYP2C19

Question 33

Loss of function CYP2C19 2 and 3consequence

Answer 33

Adverse ischemic event

Question 34

CYP2C19 17 gain of function consequence

Answer 34

Higher catalytic effect Decreased ischemic event Risk of bleeding

Question 35

Action of warfarin

Answer 35

Vitamin K antagonist used in prevention of Venus thromboembolism

Question 36

Enzyme involved in metabolism of warfarin

Answer 36

CYP2c9 enzyme

Question 37

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

Answer 37

Increased risk of bleeding by impairing warfarin metabolism

Question 38

Gene responsible for polymorphism of

Answer 38

VKORC1

Question 39

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

Answer 39

Sensitiv

Question 40

What is the dabigatran Etexilate

Answer 40

Prodrug which metabolizes esterases into direct thrombin inhibitor dabigatran

Question 41

What is the polymorphism of dabigatran

Answer 41

Single nucleotide polymorphism in CES1 gene Which decreases concentration of dabigatran