HLTH 471 & 671 (2022) - introduction to pharmacology, part 3

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Oct 30, 2023

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Principles of Pharmacology Winter, 2022 HLTH 471/671
Key Points 1) Psychopharmacology defined. 2) Pharmacokinetics. 3) Pharmacodynamics.
Metabolism (i.e., biotransformation), part I - chemical transformation of a drug (generally, enzyme-catalysed) - can occur in several tissues/organs ( liver = major site) - two types: aspirin salicylic acid salicylic-glucuronide phase I phase II Phase I - non-synthetic rx - e.g., redox, hydrolysis Phase II - synthetic rx (conjugation) - e.g., glucuronidation - both phases not always necessary - produce metabolites that are water soluble (and ionised) Pharmacokinetics 11 Guengerich F. (2008) Chem Res Toxicol 21:70-83. Wilkinson G. (2005) New Engl J Med 352:2211- 2221.
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Pharmacokinetics 12 Metabolism (i.e., biotransformation), part II - the chemical transformation of a drug in the liver can be affected by a number of factors: enzyme induction enzyme inhibition drug competition demographic variability liver gall bladder stomach pancrea s hepatic blood flow Ho et al. (2001) J Pharm Pharm Sci 4(3):217-227. Zhao et al. (2014) Seminars Perinatol 38:475-486. Marazziti et al. (2013) CNS Spectrums 18:118-127. Wilkinson G. (2005) N Engl J Med 352(21):2211-2221.
Excretion - products of biotransformation are usually excreted by the kidneys, but may also be released through the lungs or in faeces, sweat, saliva, breastmilk. nephron = functional unit of kidney Pharmacokinetics What would enhance the clearance of a weakly acidic drug from the kidneys? Renal excretion is influenced by glomerular filtration and tubular reabsorption. 13
PHARMACOKINETICS - summary Pharmacokinetics 14
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