HomeCoursesMEDSCI 204: Pharmacology and ToxicologyLecture 6 Lecture 6 1. What is ADME? "Absorption, distribution, metabolism, excretion"What is ADME?== "Absorption, distribution, metabolism, excretion" 2. What is the difference between A and D? "A is bloodstream, D is target"What is the difference between A and D?== "A is bloodstream, D is target" 3. What is IDE? "Input, distribution, elimination"What is IDE?== "Input, distribution, elimination" 4. What is elimination? Metabolism and excretionWhat is elimination?== Metabolism and excretion 5. What is ADME for? Determining concentration of drug in the bodyWhat is ADME for?== Determining concentration of drug in the body 6. What is the largest reason for clinical failure of pre 2000 drugs? ADME processesWhat is the largest reason for clinical failure of pre 2000 drugs?== ADME processes 7. What is the largest reason for clinical failure of drugs today? EfficacyWhat is the largest reason for clinical failure of drugs today?== Efficacy 8. What is the process of drugs entering the body called? DosageWhat is the process of drugs entering the body called?== Dosage 9. What is the process of drugs entering the blood stream called? AbsorptionWhat is the process of drugs entering the blood stream called?== Absorption 10. What factors effect distribution? "Binding to plasma proteins, binding and storage in tissues"What factors effect distribution? =="Binding to plasma proteins, binding and storage in tissues" 11. What are the main modes of metabolism? Plasma -> metabolism -> metabolites -> plasmaWhat are the main modes of metabolism?== Plasma -> metabolism -> metabolites -> plasma 12. What do the ADME processes determine? ConcentrationWhat do the ADME processes determine?== Concentration 13. What are properties that influence ADME? "Solubility, lipophilicity, ionisation"What are properties that influence ADME?== "Solubility, lipophilicity, ionisation" 14. What determines susceptibility to metabolism? Chemical structureWhat determines susceptibility to metabolism?== Chemical structure 15. What is the main organ involved with absorption? GI tractWhat is the main organ involved with absorption?== GI tract 16. What is the main organ involved with metabolism? LiverWhat is the main organ involved with metabolism?== Liver 17. What are the main organs associated with excretion? "Lungs, kidneys"What are the main organs associated with excretion?== "Lungs, kidneys" 18. What are the types of membrane transport? =="Passive diffusion, facilitated diffusion, active transport, endocytosis, filtration" 19. What must exist in order for passive diffusion to take place? "Concentration gradient, drug must be lipophilic, uncharged, small"What must exist in order for passive diffusion to take place?== "Concentration gradient, drug must be lipophilic, uncharged, small" 20. Where does passive diffusion take place? GI tract esp. small intestineWhere does passive diffusion take place?== GI tract esp. small intestine 21. What is the pathway for passive diffusion in GI tract? Gut lumen -> cells lining lumen -> blood streamWhat is the pathway for passive diffusion in GI tract?== Gut lumen -> cells lining lumen -> blood stream 22. What is Fick's rate of diffusion determined by? "Concentration, area membrane, membrane thickness, permeability constant"What is Fick's rate of diffusion determined by? =="Concentration, area membrane, membrane thickness, permeability constant" 23. What is the ionising effect? When a low pH environment provides H+ to drug (acidic drug goes from ion to molecule or basic drug goes from molecule to +ion)What is the ionising effect?== When a low pH environment provides H+ to drug (acidic drug goes from ion to molecule or basic drug goes from molecule to +ion) 24. What environment is conducive to absorption of basic drugs? Higher pH as less ionisation (less +ions)What environment is conducive to absorption of basic drugs?== Higher pH as less ionisation (less +ions) 25. What environment is conducive to absoption of acidic drugs? Low pH as there will be fewer ionised (+ion) acidic drugsWhat environment is conducive to absoption of acidic drugs? ==Low pH as there will be fewer ionised (+ion) acidic drugs 26. Why is less ionisation conducive for diffusion? Molecule is unchargedWhy is less ionisation conducive for diffusion?== Molecule is uncharged 27. What pKa is required for acids to be nonisised? High (acidic)What pKa is required for acids to be nonisised?== High (acidic) 28. What pKa is required for bases to be nonionised? Low (basic)What pKa is required for bases to be nonionised?== Low (basic) 29. What are some proteins that transport drugs through facilitated diffusion? SLC transportersWhat are some proteins that transport drugs through facilitated diffusion?== SLC transporters 30. "Which is faster, passive or facilitated diffusion?" Facilitated unless saturated"Which is faster, passive or facilitated diffusion?"== Facilitated unless saturated 31. What can slow facilitated diffusion? Competitor ligandsWhat can slow facilitated diffusion? ==Competitor ligands 32. What is an example of active transport? "ATP binding cassette (ABC transporter), GFs, hormones, LDL, cytokines"What is an example of active transport?== "ATP binding cassette (ABC transporter), GFs, hormones, LDL, cytokines" 33. What is an example of endocytosis? Drugs with molecular weight <1000What is an example of endocytosis? ==Drugs with molecular weight <1000 34. What are the types of endocytosis?== "Pinocytosis (cell drinking), receptor mediated endocytosis (ligand binds receptor to trigger invagination)" 35. Where does filtration occur? "Blood capillaries, glomerular capillaries, in the liver"Where does filtration occur? =="Blood capillaries, glomerular capillaries, in the liver" Loading...
