HomeCoursesMEDSCI 204: Pharmacology and ToxicologyLecture 14 Lecture 14 1. What is pharmacokinetic variablility due to? "sex, age, illness, interactions (food/drugs), genetics"What is pharmacokinetic variablility due to?== "sex, age, illness, interactions (food/drugs), genetics" 2. How does genetic phenotype create pharmacokinetic variability? Drug metabolismHow does genetic phenotype create pharmacokinetic variability?== Drug metabolism 3. What is a poor metabolism trait? Loss of function -> null enzyme activityWhat is a poor metabolism trait?== Loss of function -> null enzyme activity 4. What happens to drug plasma concentration with low hepatic clearance (poor metabolism)? High levels in bloodWhat happens to drug plasma concentration with low hepatic clearance (poor metabolism)?== High levels in blood 5. What effect might a drug with narrow therapeutic index have on a poor metaboliser? Elevated drug levels cause toxicityWhat effect might a drug with narrow therapeutic index have on a poor metaboliser?== Elevated drug levels cause toxicity 6. What type of trait is poor metaboliser? Autosomeal recessiveWhat type of trait is poor metaboliser?== Autosomeal recessive 7. What does omeprazole do? Proton pump inhibitor in parietal cells. Suppresses stomach acid secretion.What does omeprazole do? ==Proton pump inhibitor in parietal cells. Suppresses stomach acid secretion. 8. What enzymes are affected by a poor metabolism trait? CYP 450.00What enzymes are affected by a poor metabolism trait? ==CYP 450.00 9. Will an extensive metaboliser have high concentration of blood or high concentration of metabolites in blood? MetabolitesWill an extensive metaboliser have high concentration of blood or high concentration of metabolites in blood?== Metabolites 10. What drug/metabolite ratio will a poor metaboliser have? highWhat drug/metabolite ratio will a poor metaboliser have?== high 11. What percentage of population is required to have a trait in order for it to be classed as polymorphic? 1%What percentage of population is required to have a trait in order for it to be classed as polymorphic?== 1% 12. What is a polymorphic gene denoted by in literature? *What is a polymorphic gene denoted by in literature? ==* 13. What is *1? wild-type (reference gene)What is *1?== wild-type (reference gene) 14. Does a functional varian necessarily mean clinical effect? NoDoes a functional varian necessarily mean clinical effect?== No 15. What are the varients of CYP450? "*1, *2, *3"What are the varients of CYP450? =="*1, *2, *3" 16. What is CYP2C19 *1/*1? WT/WT: Extensive metaboliserWhat is CYP2C19 *1/*1?== WT/WT: Extensive metaboliser 17. What is CYP2C19 *1/*2? WT/null: intermediateWhat is CYP2C19 *1/*2?== WT/null: intermediate 18. What is CYP2C19 *2/*3? null/null: poor metaboliserWhat is CYP2C19 *2/*3? ==null/null: poor metaboliser 19. What is CYP2C19 *17/*17? promoter/promoter: rapid metaboliserWhat is CYP2C19 *17/*17?== promoter/promoter: rapid metaboliser 20. Whis is a better metaboliser *1/*1 or *1/*17?== *1/*17 21. What is clopidogrel? Antiplatelet/anticlotting agent prodrug used in stent interventionsWhat is clopidogrel?== Antiplatelet/anticlotting agent prodrug used in stent interventions 22. What will happen a person treated with clopidogrel who has CYP219*2? ==Stent thrombosis 23. What will happen a person treated with clopidogrel who has CYP219*17? Increased risk of excessive bleedingWhat will happen a person treated with clopidogrel who has CYP219*17? ==Increased risk of excessive bleeding 24. What does CYP2D6 metabolise? Codeine -> morphineWhat does CYP2D6 metabolise?== Codeine -> morphine 25. What are common null variants of CYP2D6? "*4, *5"What are common null variants of CYP2D6? =="*4, *5" 26. What are common decreased varients of CYP2D6? "*10, *41"What are common decreased varients of CYP2D6? =="*10, *41" 27. Describe is the range of activity scores? "0: null, 0.5: decreased, 1: extensive, 2+: ultrarapid metabolise"Describe is the range of activity scores?== "0: null, 0.5: decreased, 1: extensive, 2+: ultrarapid metabolise" Loading...