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Pharmacology (260)
PCL201H1 (59)
Worlsey (24)
Lecture 16

Lecture 16 Biotransformation I

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Department
Pharmacology
Course
PCL201H1
Professor
Worlsey
Semester
Winter

Description
Drug metabolizing enzymes are like the immune systemCan protect the host organisms from foreign substancesoDME small moleculesoImmune system large substances viruses bacteriaCan harm host organism if not properly regulated and balancedDrug Biotransformationstable or reactive1Produce stable metabolitesaLower PK activity inactivationbIncrease PK activity prodrug activationcRetention of pharmacological activity2Produce reactive metabolitesCovalent binding to cellular macromolecules Toxic consequences cell injury or death carcinogenicity teratogenicityReactive metabolitesundesirable electrophillicInactivation exampleAcetaminophen is active but when metabolized by SULT or UGT becomes inactiveSULT transfers sulfer group from PAPS to acetaminophenUGT transfers glucronic acidInactive Decreased Potency More H20 soluble side groups S G governs duration of effect in bodyActivation exampleAllopurinol is a weak
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