Flashcards
Cytochrome P450 (CYP) Enzymes
Cards in this deck (39)
- 1What are the seven major cytochrome p450 (CYP) enzymes that are important to know?1A2, 2A6, 2C9, 2C19, 2D6, 2E1, 3A4
- 2What is a prodrug?An inactive or less than active drug that is converted to its active form via normal metabolic processes (metabolism activates it)
- 3What is induction?Enhanced biotransformation via CYP enzymes, which results in increased activity of prodrugs and enhanced elimination of drugs
- 4What is inhibition?Decreased biotransformation, resulting in decreased activation of prodrugs and increased activity of drugs
- 5What is a polymorphism, with regards to CYP enzymes?A genetic change occurring in at least 1% of the population, resulting in altered biotransformative properties of CYP enzymes
- 6For which of the major CYP enzymes do known polymorphisms exist?2C9, 2C19, and 2D6
- 7Which major CYP enzyme comprises 40-55% of hepatic CYPs?3A4
- 8Which major CYP enzyme comprises only 2% of hepatic CYPs?1A4
- 9Which major CYP enzyme contributes most to the enterocyte CYPs?3A4
- 10Where is 1A4 found, aside from the liver?Lung
- 11Where is 2C9 found, aside from the liver?Nasal mucosa, small intestine, heart
- 12Where is 2C19 found, aside from the liver?Nasal mucosa, small intestine, heart
- 13Where is 2D6 found, aside from the liver?Lung, kidney, small intestine, heart
- 14Where is 2E1 found, aside from the liver?Lung, kidney, small intestine
- 15Where is 3A4 found, aside from the liver?Much in the small intestine, some in the kidney, nasal mucosa, lung, stomach
- 16Order the major CYP enzymes from least to greatest metabolizers of typical drugs1A2 < 2C9 < 2D6 < 3A4
- 17Polymorphisms of which two CYP enzymes are likely to be poor metabolizers?2C9 and 2C19
- 18Polymorphisms of which CYP enzyme is likely to be an ultra extensive metabolizer?2D6
- 19Which population is most likely to have a poor metabolizing polymorphism for 2C19? Compare this population to others in terms of percentages.Aftrican Americans (20%); Asians (15-20%); Whites (3-5%)
- 20Which population is most likely to have a poor metabolizing polymorphism for 2D6? Compare this population to others in terms of percentages.Whites (5-10%); African Americans (2-8%); Asians (<1%)
- 21Which two populations are most likely to have an ultra extensive metabolizing polymorphism for 2D6?Ethiopians (30%); Southern Europeans (10%)
- 22What are two common substrates for 1A2?1. Caffeine
2. Theophylline - 23What are two common inducers for 1A2?1. Smoking
2. Charred foods - 24What is a common inhibitor of 1A2?Grapefruit juice
- 25What are two common substrates for 2C9?1. Phenytoin
2. Warfarin - 26What are three common inducers for 2C9?1. Barbituates
2. Rifampicin
3. St. John's Wort - 27What is a common inhibitor of 2C9?Macrolides
- 28What is a common substrate for 2C19?Diazepam
- 29What is a common inducer for 2C19?St. John's Wort
- 30What is a common inhibitor of 2C19?Fluoxetine
- 31What is a common substrate for 2D6?Codeine, a prodrug
- 32What is a common inducer for 2D6?Rifampin
- 33What are two common inhibitors of 2D6?1. Quinidine
2. Haloperidol - 34What is a common substrate for 2E1?Paracetamol
- 35What is a common inducer for 2E1?Alcohol
- 36What are two common substrates for 3A4?1. Terfenadine (anti-histamine)
2. Verapamil (decreases HR and BP) - 37What is a common inducer for 3A4?St. John's Wort
- 38What are two common inhibitors of 3A4?1. Ketoconazole (anti-fungal)
2. Itraconazole - 39CYP enzymes use what kind of reactions in order to biotransform various molecules?Redox reactions
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- The major cytochrome P450 isozymes and their common substrates, polymorphisms, inducers, and inhibitors
- Created by
- Breanna Felldin
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