Pharm: CYP enzymes.

Question 1

What do CYP enzymes do?

Answer 1

perform RedOx reactions - PHASE I

Question 2

Where are CYP enzymes?

Answer 2

smooth ER mostly in the liver

Question 3

prodrug

Answer 3

medication that is administered in an inactive or less than fully active form, and is then converted to its active form through a normal metabolic process

Question 4

induction

Answer 4

biotransformation by induced CYP enzymes results in either INCREASED activity of PRODRUGS or ENHANCED ELIMINATION of DRUGS

Question 5

inhibition

Answer 5

results in INCREASED BIOAVAILABILITY of a DRUG or DECREASED activity of PRODRUG

Question 6

polymorphism

Answer 6

genetic change that exists for at least 1% of the population - CYP polymorphism occurs when the biotransforming properties of an enzyme are altered

Question 7

substrate

Answer 7

a substance (drug/medication) acted on by an enzyme

Question 8

Which enzyme is the highest percent of liver CYPs?

Answer 8

3A4

Question 9

CYP1A2 examples

Answer 9

caffeine and theophylline

Question 10

CYP2C9 examples

Answer 10

phenytoin (anti-seizure drug) and warfarin

Question 11

CYP2C19 examples

Answer 11

diazepam

Question 12

CYP2D6 examples

Answer 12

codeine

Question 13

CYP2E1 examples

Answer 13

paracetamol (tylenol)

Question 14

CYP3A4 examples

Answer 14

terfenadine (anti histamine) and verapamil

Question 15

warfarin

Answer 15

used to inhibit the clotting factors 2,7,9,10 - anticoagulant

Question 16

What are inducers of CYP1A2?

Answer 16

smoking, charred food

Question 17

What are inducers of CYP2C9?

Answer 17

rifampicin

Question 18

What are inducers of CYP2C19?

Answer 18

St John’s wort

Question 19

What are inducers of CYP2D6?

Answer 19

rifampicin

Question 20

What are inducers of 3A4?

Answer 20

St. John’s wort

Question 21

What specific drugs are St. John’s wort an inducer of?

Answer 21

diazepam and verapamil

Question 22

What specific drugs are rifampin an inducer of?

Answer 22

codeine, warfarin, phenytoin

Question 23

Normal drugs

Answer 23

caffein, theophylline, verapamil

Question 24

Prodrug

Answer 24

codeine (-> morphine)

Question 25

What is an inhibitor of CYP1A2?

Answer 25

grapefruit juice

Question 26

What is an inhibitor of CYP2C9?

Answer 26

macrolides

Question 27

What is an inhibitor of CYP2C19?

Answer 27

fluoxetine

Question 28

What is an inhibitor of CYP2D6?

Answer 28

quinidine, haloperidol

Question 29

What is an inhibitor of CYP3A4?

Answer 29

ketoconazole (for fungal infections), itraconazole

Question 30

Which 3 enzymes exhibit polymorphisms?

Answer 30

2C9, 2C19, and 2D6

Question 31

Poor metabolizers polymorphisms

Answer 31

2C9 and 2C19 (2D6 is both poor and extensive)

Question 32

African americans show high polymorphism in which enzyme?

Answer 32

2C19, slightly high in 2D6 (diazepam)

Question 33

Asians show polymorphism in which enzyme?

Answer 33

2C19 (diazepam)

Question 34

Caucasians show polymorphism in which enzyme?

Answer 34

2D6 (high percentage don’t make morphine from codeine)