Metabolism of drugs
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This document discusses the biochemistry of drugs in the body. It outlines the common pathways of drug metabolism in the body, including absorption, circulation, and biotransformation of drugs in the liver. The liver plays a key role in drug metabolism through enzymes like cytochrome P450 and through phase I and phase II reactions such as oxidation, reduction, hydroxylation and conjugation with glucuronic acid or amino acids. Drug metabolites are then eliminated from the body.
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2. Factors like age, diet, diseases, genetic factors and simultaneous administration of other drugs can influence drug metabolism by inducing or inhibiting drug-metabolizing enzymes. Metabolism can convert drugs to active, inactive or less active forms.
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2. Pharmacodynamic interactions, where one drug directly or indirectly impacts the effects of another at its site of action. Direct interactions can result in antagonism, addition/summation of effects, or synergism/potentiation.
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Drug metabbolism
Most drug metabolites are less active, but some are more active or toxic. Drug metabolism involves pathways for endogenous substrates and occurs mainly in the liver. Phase I reactions make drugs more polar for excretion or Phase II conjugation. Phase I includes oxidation, reduction, and hydrolysis. Phase II involves conjugating drugs to glucuronide, sulfate, or glutathione for excretion.
BP604T unit 2 notes.docx
This document provides an overview of biotransformation, which is the chemical alteration of drugs in the body. It discusses the objectives and learning outcomes of the course. The main topics covered include the definition of biotransformation, the consequences it can have on drugs, the phases and types of biotransformation reactions (phase I and II), enzymes involved, and the concept of first pass metabolism. Phase I reactions include oxidation, reduction, hydrolysis, and others. Phase II or conjugation reactions attach endogenous substances like glucuronic acid. Enzyme induction and inhibition are also discussed.
Inhibition and induction of drug metabolism
Drug metabolism can be inhibited or induced by other drugs through various mechanisms. Enzyme inhibition decreases drug metabolism and can be direct, by competing for the enzyme's active site, or indirect, such as by repressing enzyme production. Examples include fluvoxamine doubling diazepam's half-life and quinidine inhibiting nifedipine metabolism. Induction increases drug metabolism by stimulating hepatic enzyme production, shortening drug half-lives. Phenobarbital induces the metabolism of warfarin and dexamethasone. Some drugs also interact by inhibiting biliary excretion of other drugs via transporters like P-glycoprotein, increasing their bioavailability and potentially toxicity.
Drug Metabolism.pdf
This document outlines drug metabolism and biotransformation. It discusses the definition of biotransformation and its consequences. The two phases of biotransformation - phase I and phase II - are described. Phase I involves reactions like oxidation, reduction and hydrolysis catalyzed by cytochrome P450 enzymes. Phase II involves conjugation reactions like glucuronidation, acetylation and sulfation catalyzed by transferase enzymes, which aid in drug detoxification and excretion. Factors affecting drug metabolism are also discussed.
Current Issues In Drug Metabolism
This document discusses drug metabolism and its role in adverse drug reactions. It covers the key phases of drug metabolism - phase I involving reactions like hydroxylation and epoxidation, and phase II involving conjugation through glucuronidation and glutathione. The liver plays a central role in drug metabolism but reactive metabolites can cause toxicity. Both predictable and unpredictable adverse reactions are discussed, as well as factors like individual variability in drug response. The roles of bioactivation and specific metabolic pathways in toxicity are also summarized.
pharmacokinetics-ii-170215132744.pdf
This document discusses pharmacokinetics and biotransformation. It covers the four main stages of pharmacokinetics: absorption, distribution, metabolism, and excretion. Metabolism, or biotransformation, involves enzymatic conversion of drugs by the liver and involves two phases - phase I and phase II reactions. Phase I introduces or exposes functional groups through oxidation, reduction or hydrolysis. Phase II involves conjugation through acetylation, methylation, glucuronidation or sulphation. Cytochrome P450 enzymes and microsomal enzymes are involved in phase I reactions. Factors like enzyme induction and inhibition can impact drug metabolism and clearance. Drugs and metabolites are primarily excreted through the kidneys
Pharmacokinetics ii
This document discusses pharmacokinetics and biotransformation. It covers the four main stages of pharmacokinetics: absorption, distribution, metabolism, and excretion. Metabolism, or biotransformation, involves enzymatic conversion of drugs by the liver and involves two phases - phase I and phase II reactions. Phase I introduces or exposes functional groups using oxidation, reduction or hydrolysis. Phase II involves conjugation reactions like glucuronidation and sulfation. Cytochrome P450 enzymes and microsomal enzymes are responsible for many phase I reactions. Factors like enzyme induction and inhibition can impact drug metabolism and clearance from the body.
Microsomal enzyme induction
Microsomal enzymes like cytochrome P450 and UDP glucoronosyl transferases are important for drug metabolism in the liver and other tissues. Cytochrome P450 enzymes catalyze oxidation, reduction, and other phase I reactions. UDP glucoronosyl transferases catalyze phase II conjugation reactions like glucoronidation. Drug metabolism can be induced or inhibited by other drugs and environmental factors, leading to potential drug-drug interactions. A better understanding of an individual's genetic polymorphisms and environmental factors can help optimize drug therapy and avoid adverse reactions.
Inhibition and induction of drug metabolism
This document discusses inhibition and induction of drug metabolism. It describes how some drugs can decrease (inhibit) or increase (induce) the activity of enzymes involved in drug metabolism. Examples are given of drugs that inhibit the metabolism of other drugs, leading to increased levels and potential toxicity. Inhibition can occur directly by interacting with the enzyme or indirectly by other mechanisms. The document also discusses inhibition of biliary secretion, an important route of drug excretion, and how this can cause drug-drug interactions by affecting drug levels.
Hepatic Micrisomal Enzyme System
This document discusses drug metabolism and the clinical relevance of biotransformation. It begins by defining biotransformation as the biochemical reactions that alter drugs within the body, and discusses the roles of microsomal enzymes like cytochrome P450 enzymes and UDP glucuronosyl transferases. It then covers the phases of drug metabolism and the enzymes involved in each phase. Specific cytochrome P450 isoforms and their drug substrates are discussed. The effects of enzyme induction and inhibition on drug metabolism and potential drug interactions are summarized. Factors influencing individual differences in drug metabolism like genetic polymorphisms and environmental factors are briefly mentioned in the conclusion.
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Drug metabolism- General pharmacology - various types
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BIOTRANSFORMATION UNIT -1 DRUG METABOLISM (1).pptx
BIOTRANSFORMATION UNIT -1 DRUG METABOLISM (1).pptx
Metabolism/pharmacokinetics/pharmacy student notes
Metabolism/pharmacokinetics/pharmacy student notes
UNIT I: DRUG METABOLISM: S.Y. B. PHARMACY IV SEMESTER
UNIT I: DRUG METABOLISM: S.Y. B. PHARMACY IV SEMESTER
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Metabolism of drugs
- 2. Amirova Associate Professor at Biochemistry Department of Azerbaijan Medical University, 2021
- 4. WHAT HAPPENS IN THE BODY AFTER ABSORPTION?
- 5. COMMONWAYS OF DRUG METABOLISM INTHE BODY And drug excretion
- 7. Ways of drug circulation
- 10. Biotransformation of drugs in the liver
- 12. IRREPLACEBLE IN BIOTRANSFORMATION ENZYMES:
- 14. Cyt P450 action:
- 17. HYDROLYSIS
- 22. Alkylation:
- 26. Change in activity of drugs activity after biotransformation
- 27. Glucuronic and sulfuric acids in first type of conjugation
- 28. Aryl-sulphatase action. Enzyme uses active form of sulfate - PAPS
- 29. Conjugation with active form of glucuronic acid: UDP- glucuronate
- 31. Second type of conjugation: with non- activated molecules, namely glycine & glutamine
- 32. Synthesis of hippuric acid
- 34. with of salicylic acid
- 35. Product of salicylic acid conjugation with glutamic acid
- 36. Drug induced liver injury
- 37. ELIMINATION OF DRUG METABOLITES
- 38. THANKYOU FOR ATTENTION & SPEND YOURVALUABLETIME