Flashcards in Pharm: CYP enzymes. Deck (34):
What do CYP enzymes do?
perform RedOx reactions - PHASE I
Where are CYP enzymes?
smooth ER mostly in the liver
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
biotransformation by induced CYP enzymes results in either INCREASED activity of PRODRUGS or ENHANCED ELIMINATION of DRUGS
results in INCREASED BIOAVAILABILITY of a DRUG or DECREASED activity of PRODRUG
genetic change that exists for at least 1% of the population - CYP polymorphism occurs when the biotransforming properties of an enzyme are altered
a substance (drug/medication) acted on by an enzyme
Which enzyme is the highest percent of liver CYPs?
caffeine and theophylline
phenytoin (anti-seizure drug) and warfarin
terfenadine (anti histamine) and verapamil
used to inhibit the clotting factors 2,7,9,10 - anticoagulant
What are inducers of CYP1A2?
smoking, charred food
What are inducers of CYP2C9?
What are inducers of CYP2C19?
St John’s wort
What are inducers of CYP2D6?
What are inducers of 3A4?
St. John’s wort
What specific drugs are St. John’s wort an inducer of?
diazepam and verapamil
What specific drugs are rifampin an inducer of?
codeine, warfarin, phenytoin
caffein, theophylline, verapamil
codeine (-> morphine)
What is an inhibitor of CYP1A2?
What is an inhibitor of CYP2C9?
What is an inhibitor of CYP2C19?
What is an inhibitor of CYP2D6?
What is an inhibitor of CYP3A4?
ketoconazole (for fungal infections), itraconazole
Which 3 enzymes exhibit polymorphisms?
2C9, 2C19, and 2D6
Poor metabolizers polymorphisms
2C9 and 2C19 (2D6 is both poor and extensive)
African americans show high polymorphism in which enzyme?
2C19, slightly high in 2D6 (diazepam)
Asians show polymorphism in which enzyme?