10181050
Description
Flashcards by Breanna Felldin, updated more than 1 year ago
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Created by Breanna Felldin
over 6 years ago
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| Question | Answer |
| What are the seven major cytochrome p450 (CYP) enzymes that are important to know? | 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, 3A4 |
| What is a prodrug? | An inactive or less than active drug that is converted to its active form via normal metabolic processes (metabolism activates it) |
| What is induction? | Enhanced biotransformation via CYP enzymes, which results in increased activity of prodrugs and enhanced elimination of drugs |
| What is inhibition? | Decreased biotransformation, resulting in decreased activation of prodrugs and increased activity of drugs |
| What 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 |
| For which of the major CYP enzymes do known polymorphisms exist? | 2C9, 2C19, and 2D6 |
| Which major CYP enzyme comprises 40-55% of hepatic CYPs? | 3A4 |
| Which major CYP enzyme comprises only 2% of hepatic CYPs? | 1A4 |
| Which major CYP enzyme contributes most to the enterocyte CYPs? | 3A4 |
| Where is 1A4 found, aside from the liver? | Lung |
| Where is 2C9 found, aside from the liver? | Nasal mucosa, small intestine, heart |
| Where is 2C19 found, aside from the liver? | Nasal mucosa, small intestine, heart |
| Where is 2D6 found, aside from the liver? | Lung, kidney, small intestine, heart |
| Where is 2E1 found, aside from the liver? | Lung, kidney, small intestine |
| Where is 3A4 found, aside from the liver? | Much in the small intestine, some in the kidney, nasal mucosa, lung, stomach |
| Order the major CYP enzymes from least to greatest metabolizers of typical drugs | 1A2 < 2C9 < 2D6 < 3A4 |
| Polymorphisms of which two CYP enzymes are likely to be poor metabolizers? | 2C9 and 2C19 |
| Polymorphisms of which CYP enzyme is likely to be an ultra extensive metabolizer? | 2D6 |
| Which 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%) |
| Which 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%) |
| Which two populations are most likely to have an ultra extensive metabolizing polymorphism for 2D6? | Ethiopians (30%); Southern Europeans (10%) |
| What are two common substrates for 1A2? | 1. Caffeine 2. Theophylline |
| What are two common inducers for 1A2? | 1. Smoking 2. Charred foods |
| What is a common inhibitor of 1A2? | Grapefruit juice |
| What are two common substrates for 2C9? | 1. Phenytoin 2. Warfarin |
| What are three common inducers for 2C9? | 1. Barbituates 2. Rifampicin 3. St. John's Wort |
| What is a common inhibitor of 2C9? | Macrolides |
| What is a common substrate for 2C19? | Diazepam |
| What is a common inducer for 2C19? | St. John's Wort |
| What is a common inhibitor of 2C19? | Fluoxetine |
| What is a common substrate for 2D6? | Codeine, a prodrug |
| What is a common inducer for 2D6? | Rifampin |
| What are two common inhibitors of 2D6? | 1. Quinidine 2. Haloperidol |
| What is a common substrate for 2E1? | Paracetamol |
| What is a common inducer for 2E1? | Alcohol |
| What are two common substrates for 3A4? | 1. Terfenadine (anti-histamine) 2. Verapamil (decreases HR and BP) |
| What is a common inducer for 3A4? | St. John's Wort |
| What are two common inhibitors of 3A4? | 1. Ketoconazole (anti-fungal) 2. Itraconazole |
| CYP enzymes use what kind of reactions in order to biotransform various molecules? | Redox reactions |
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