POLYMORPHISM AFFECTING DRUG METABOLISM.pptx
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Polymorphism affecting drug metabolism refers to genetic variations in genes that code for drug-metabolizing enzymes. This can result in altered enzyme function and changes in how drugs are metabolized in the body. The liver is the major site of drug metabolism, through phase I and phase II reactions. Variations in the cytochrome P450 enzyme CYP2D6, which metabolizes around 20-25% of drugs, can lead to poor, intermediate, or ultrarapid metabolism phenotypes. This impacts the efficacy and toxicity of drugs like tamoxifen, codeine, and clopidogrel. Variations in N-acetyltransferase and thiopurine methyltransferase, phase II enzymes, can also affect
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GENETIC POLYMORPHISM IN DRUG METABOLISM.pptx
Genetic Polymorphism is one of the factors that affects the Drug metabolism. Cytochrome P - 450, one of the prominent group of metabolizing enzymes. In this ppt, genetic polymorphism of cytochrome p 450 is discussed.
Genetic polymorphism
Genetic polymorphisms in drug metabolizing enzymes like CYP450 isoenzymes can result in poor, intermediate, extensive, or ultra-rapid metabolism of drugs. The most important polymorphisms are in CYP2D6, CYP2C19, CYP2C9, and CYP3A4/5 which can significantly impact drug efficacy and toxicity risks due to altered metabolism. Genotyping for these polymorphisms provides important information for understanding individual responses to drugs metabolized by these enzymes.
Metabolism,Excretion,prodrug,Therapeutic Drug monitoring
1. Metabolism and excretion are important processes that determine the duration and intensity of a drug's effects in the body. Metabolism involves chemical alteration of drugs through phase I and phase II reactions, while excretion removes drugs and metabolites from the body through renal, hepatic, pulmonary and other routes.
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.
3. Prodrugs are inactive forms administered to deliver the active drug selectively or improve pharmacokinetics. They are converted to active drugs through metabolic processes
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Phenobarbital induces UGT1A1 enzyme.
Phenobarbital is known to induce various drug metabolizing enzymes including UGT1A1. By inducing UGT1A1, it increases the enzyme's activity and ability to conjugate and clear bilirubin, thus lowering bilirubin levels in patients with Crigler-Najjar syndrome type II who have some residual UGT1A1 activity.
Polymorphism affecting drug metabolism .
This document discusses genetic polymorphisms that affect drug metabolism. It begins by defining genetic polymorphism and describing the main types, including single nucleotide polymorphisms, insertions and deletions, and nucleotide repeat polymorphisms. It then discusses how genetic polymorphisms can alter drug metabolism through variations in metabolic enzyme activity and discusses specific examples of polymorphisms in key drug metabolizing enzymes like CYP2D6, CYP2C9, and N-acetyltransferases. The document emphasizes how understanding genetic variations in drug metabolism is important for predicting inter-individual differences in drug responses.
Polymorphism affecting drug metabolism
Polymorphisms in genes encoding drug-metabolizing enzymes can affect individual responses to medications. Genetic variations produce different alleles of genes like CYP2C9, CYP2C19 and CYP2D6, which code for cytochrome P450 enzymes that metabolize many drugs in the liver. These polymorphisms can cause decreased, increased, or absent enzyme expression and activity, leading to subgroups that differ in their ability to metabolize drugs. For example, CYP2C19 polymorphisms are associated with longer half-lives of diazepam, while CYP2C9 variants increase bleeding risk when taking the blood thinner warfarin due to reduced metabolism. Understanding these pharmacogenomic differences can
Genetic polymorphism in drug metabolism
Section 'a' of last chapter in Clinical Pharmacokinetics and Phrmacotherapeutic Drug Monitoring. This is useful for 5th year PHARM D students.
Drug metabolism- General pharmacology - various types
This document discusses drug biotransformation and metabolism. It notes that drugs are chemically altered within the body through processes like oxidation, reduction, hydrolysis, and conjugation. The liver is a major site of drug metabolism, which occurs in two phases - phase I involves processes like oxidation, and phase II involves conjugation reactions to make the drug more water soluble and able to be excreted. Factors like age, diet, disease states, and genetics can impact an individual's drug metabolism. Prodrugs are discussed as inactive forms of drugs that are converted to the active form after metabolism.
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GENETIC POLYMORPHISM IN DRUG METABOLISM.pptx
Genetic Polymorphism is one of the factors that affects the Drug metabolism. Cytochrome P - 450, one of the prominent group of metabolizing enzymes. In this ppt, genetic polymorphism of cytochrome p 450 is discussed.
Genetic polymorphism
Genetic polymorphisms in drug metabolizing enzymes like CYP450 isoenzymes can result in poor, intermediate, extensive, or ultra-rapid metabolism of drugs. The most important polymorphisms are in CYP2D6, CYP2C19, CYP2C9, and CYP3A4/5 which can significantly impact drug efficacy and toxicity risks due to altered metabolism. Genotyping for these polymorphisms provides important information for understanding individual responses to drugs metabolized by these enzymes.
Metabolism,Excretion,prodrug,Therapeutic Drug monitoring
1. Metabolism and excretion are important processes that determine the duration and intensity of a drug's effects in the body. Metabolism involves chemical alteration of drugs through phase I and phase II reactions, while excretion removes drugs and metabolites from the body through renal, hepatic, pulmonary and other routes.
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.
3. Prodrugs are inactive forms administered to deliver the active drug selectively or improve pharmacokinetics. They are converted to active drugs through metabolic processes
Nz pep lecture_jan2016
Phenobarbital induces UGT1A1 enzyme.
Phenobarbital is known to induce various drug metabolizing enzymes including UGT1A1. By inducing UGT1A1, it increases the enzyme's activity and ability to conjugate and clear bilirubin, thus lowering bilirubin levels in patients with Crigler-Najjar syndrome type II who have some residual UGT1A1 activity.
Polymorphism affecting drug metabolism .
This document discusses genetic polymorphisms that affect drug metabolism. It begins by defining genetic polymorphism and describing the main types, including single nucleotide polymorphisms, insertions and deletions, and nucleotide repeat polymorphisms. It then discusses how genetic polymorphisms can alter drug metabolism through variations in metabolic enzyme activity and discusses specific examples of polymorphisms in key drug metabolizing enzymes like CYP2D6, CYP2C9, and N-acetyltransferases. The document emphasizes how understanding genetic variations in drug metabolism is important for predicting inter-individual differences in drug responses.
Polymorphism affecting drug metabolism
Polymorphisms in genes encoding drug-metabolizing enzymes can affect individual responses to medications. Genetic variations produce different alleles of genes like CYP2C9, CYP2C19 and CYP2D6, which code for cytochrome P450 enzymes that metabolize many drugs in the liver. These polymorphisms can cause decreased, increased, or absent enzyme expression and activity, leading to subgroups that differ in their ability to metabolize drugs. For example, CYP2C19 polymorphisms are associated with longer half-lives of diazepam, while CYP2C9 variants increase bleeding risk when taking the blood thinner warfarin due to reduced metabolism. Understanding these pharmacogenomic differences can
Genetic polymorphism in drug metabolism
Section 'a' of last chapter in Clinical Pharmacokinetics and Phrmacotherapeutic Drug Monitoring. This is useful for 5th year PHARM D students.
Drug metabolism- General pharmacology - various types
This document discusses drug biotransformation and metabolism. It notes that drugs are chemically altered within the body through processes like oxidation, reduction, hydrolysis, and conjugation. The liver is a major site of drug metabolism, which occurs in two phases - phase I involves processes like oxidation, and phase II involves conjugation reactions to make the drug more water soluble and able to be excreted. Factors like age, diet, disease states, and genetics can impact an individual's drug metabolism. Prodrugs are discussed as inactive forms of drugs that are converted to the active form after metabolism.
Metabolism of drug
This document discusses drug metabolism and biotransformation. It describes how drugs are structurally modified inside the body through Phase I and Phase II metabolic pathways. Phase I metabolism involves oxidation, reduction and hydrolysis reactions by cytochrome P450 enzymes and flavin monooxygenases. This makes the drugs more hydrophilic but can also activate some drugs. Phase II conjugation reactions like glucuronidation and sulfation catalyzed by transferase enzymes further increases hydrophilicity and promotes excretion of drug metabolites. The liver is the major site of drug metabolism though other tissues also play a role. Enzyme induction and inhibition can impact drug metabolism.
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Genetic polymorphisms can affect how individuals metabolize and respond to drugs. Variations in genes encoding drug metabolizing enzymes, like CYP450 isoforms and dihydropyrimidine dehydrogenase, have been shown to result in decreased, increased, or absent enzyme expression/activity. This can lead to inter-individual differences in drug effects, like a higher risk of toxicity from drugs metabolized by the affected enzymes. Single nucleotide polymorphisms in these genes have been linked to variability in drug dosing requirements, interactions, and treatment outcomes.
Drug metabolism as
Biotransformation, or metabolism, refers to the chemical alteration of drugs in the body. The primary site is the liver, where drugs undergo two main phases of metabolism - phase I and phase II reactions. Phase I reactions like oxidation and hydrolysis functionally alter drugs, while phase II or conjugation reactions make drugs more polar and excretable by conjugating them to other molecules. Many drugs are activated or inactivated in these metabolic pathways. Metabolism can occur in other tissues as well and is mediated by various enzyme systems like the cytochrome P450 enzymes. Drug metabolism can be inhibited or induced, affecting the activity of other drugs a patient may be taking.
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This document discusses drug metabolism. It defines metabolism as the network of chemical processes that maintain life. Drug metabolism occurs through various phases including oxidation, reduction, hydrolysis, and conjugation reactions. These reactions are catalyzed by enzymes like cytochrome P450 and occur mainly in the liver and intestines. The consequences of metabolism can include inactivation of drugs, production of active metabolites, or increased activity as in the case of prodrugs. Factors like genetic polymorphisms and drug interactions can impact the metabolism of drugs.
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The document provides an overview of drug metabolism. It discusses that drug metabolism is important as it converts lipophilic drugs to hydrophilic metabolites that can be readily excreted. The key sites of drug metabolism are the liver, GI tract, lungs and kidneys. Metabolism occurs via phase I and phase II reactions and can activate or deactivate drugs. Factors like enzymes, diet, disease and genetics influence an individual's metabolism. Understanding metabolism is important for drug efficacy, toxicity and interactions.
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The document provides an overview of drug metabolism. It discusses that drug metabolism is important as it converts lipophilic drugs to hydrophilic metabolites that can be readily excreted. The key sites of drug metabolism are the liver, GI tract, lungs and kidneys. Metabolism occurs via phase I and phase II reactions and can activate or deactivate drugs. Factors like enzymes, diet and disease can influence a drug's metabolism. Understanding metabolism is important for predicting drug interactions and toxicity.
Polymorphism affecting Drug Metabolism.pptx
Genetic polymorphisms can profoundly influence drug metabolism, impacting how medications are processed in the body. Variations in genes encoding drug-metabolizing enzymes, like cytochrome P450 (CYP) enzymes, can lead to differences in drug efficacy and safety among individuals. This presentation provides a concise overview of how polymorphisms affect drug metabolism.
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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.
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The document discusses drug metabolism and biotransformation. It notes that the primary site of drug metabolism is the liver, where drugs undergo chemical alterations through reactions like oxidation, reduction, hydrolysis, and conjugation. These reactions are carried out by enzymes like cytochrome P450 and UDP-glucuronosyl transferases. Certain drugs can inhibit or induce these drug-metabolizing enzymes, resulting in clinically significant drug-drug interactions.
Polymorphism affecting drug metabolism
Genetic polymorphisms can affect how individuals metabolize and respond to drugs. Variations in genes encoding drug-metabolizing enzymes like CYP450 isoforms can result in poor, intermediate, extensive, or ultra-rapid metabolizer phenotypes. This impacts how effectively an individual metabolizes and eliminates drugs from the body. The effects of inhibitors and inducers on drug metabolism also differ depending on a person's metabolizer phenotype. Understanding these genetic factors is important for predicting drug responses and interactions between a drug and other substances in an individual.
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This document provides an overview of pharmacogenomics. It defines pharmacogenomics as the study of how genetic variations influence individual drug responses. It discusses how single nucleotide polymorphisms (SNPs) can alter drug metabolism and response. Examples are provided of genes like G6PD, TPMT, CYP2D6 and CYP2C9 that influence drug toxicity and efficacy. Benefits of pharmacogenomics include more powerful and safer drugs through personalized treatment based on an individual's genetic profile. Ethical concerns around privacy, discrimination, and drug availability are also discussed.
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This document discusses biotransformation, or the metabolism of drugs in the body. It covers the key topics of:
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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.
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The document discusses drug metabolism and biotransformation. It notes that the primary site of drug metabolism is the liver, where drugs undergo chemical alterations through reactions like oxidation, reduction, hydrolysis, and conjugation. These reactions are carried out by enzymes like cytochrome P450 and UDP-glucuronosyl transferases. Certain drugs can inhibit or induce these drug-metabolizing enzymes, resulting in clinically significant drug-drug interactions.
Polymorphism affecting drug metabolism
Genetic polymorphisms can affect how individuals metabolize and respond to drugs. Variations in genes encoding drug-metabolizing enzymes like CYP450 isoforms can result in poor, intermediate, extensive, or ultra-rapid metabolizer phenotypes. This impacts how effectively an individual metabolizes and eliminates drugs from the body. The effects of inhibitors and inducers on drug metabolism also differ depending on a person's metabolizer phenotype. Understanding these genetic factors is important for predicting drug responses and interactions between a drug and other substances in an individual.
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Novas diretrizes da OMS para os cuidados perinatais de mais qualidade
Novas diretrizes da OMS para os cuidados perinatais de mais qualidadeProf. Marcus Renato de Carvalho
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
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POLYMORPHISM AFFECTING DRUG METABOLISM.pptx
- 3. Introduction Causes Types Drug metabolism and its types Variation in phase I with examples Variation in phase II with examples Presentation title 3 CONTENT
- 4. Introduction Polymorphism : Genetic difference in drug metabolism are the result of genetically based variation in alleles for gene that code for enzyme responsible for the metabolism of drug . It contains abnormal pairs / multiple /abnormal gene leading to altered enzyme function . Drug Metabolism : Also called Biotransformation . Any chemical alteration of the drug in the body is known as Biotransformation .It covert lipid soluble substance into lipid insoluble substance. SITES of METABOLISM Major site --- Liver Other site of metabolism are : GIT, Lungs ,Kidney,Plasma,Skin , Nasal Mucosa Presentation title 4
- 5. CAUSES Balance between variations created by new mutation and natural selection Frequency dependent selection Multiple niche polymorphism Presentation title 5
- 10. VARIATION IN PHASE I METABOLISM CYTOCHROME P4502D6 • Heme containing enzyme • Superfamily is very large • Represents diverse group of enzyme • Responsible for 20-25 % of drugs metabolism like – Antidepressant , Antiarrthymic drugs , Antipsychotic drugs etc • It has largest phenotypic variations • Have more than 80 allelic variations Presentation title 10
- 11. DIFFERENT ALLELIC AND PHENOTYPIC VARIANTS OF CYP2D6 Presentation title 11 S.NO O PHENOTYPE ALLELIC VARIANTS 1 POOR METABOLISER METABOLISER CYP2D6 2 INTERMEDIATE METABOLISER CYP2D9 3 ULTRARAPID METABOLISER CYP2D1
- 12. EXAMPLES 1. TAMOXIFEN IN BREAST CANCER : Metabolised by these enzymes to form endoxifen . More potent estrogen receptor . The anticancer property of tamoxifen has been largely attributed to this metabolite . It has been found that patients with poor metaboliser phenotype of CYP2D6 have lower level of endoxifen . There are more chance of relapse of cancer in these person 2. CODEINE IN POSTGESTATIONAL WOMEN AS ANALGESIC : Codeine – postgestational women –control pain due to child birth –less quantity excreated in breast milk . In ultra rapid metaboliser high level of morphine are detected in neonates which is fatal . Presentation title 12
- 13. 3. CLOPIDOGREL AS ANTIPLATELET DRUG : Prodrug – metabolised by CYP2C19 –form active metabolite . Hence its variants form CYP2C19*17 – not metabolizes to active form – antiplatelet effect is not observed 4 OMEPRAZOLE IN PEPTIC ULCER 5. WARFARIN AS ANTICOAGULANTOMEPRAZOLE ETC Presentation title 13
- 14. VARIATIONS IN PHASE 2 METABOLISM 1. N-METHYL TRANSFERASE –Variation on this enzyme has been seen in antituberculosis drugs like isoniazid Decrease metabolism of isoniazid in slow acetylator ( variants with decrease N ACETYL TRANSFERASE activity ) leads to neuritis (inflammation of one or more nerve ). Also leads to systemic lupus erythematous 1 Presentation title 14
- 15. 2. THIOPURINE METHYLTRANSFERASE(TPMT) : Purine analogue ( example: 6 – mercaptopurine ) Treat heamatologic malignancies Convert into thioguanine nucleotide Incorporate in DNA strands DNA damage Thioguanine nucleotide metabolised by enzyme tpmt Increase in the level of thioguanine and low level of tpmt = Neutopenia Decrease anticancer activity of purine analogues Presentation title 15
- 16. Thank you MADHU VASHISHT