Cytochrome P450 (CYP) Enzymes

Pregunta	Respuesta
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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	Creado por Breanna Felldin hace alrededor de 7 años