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  • Metabolisme Obat (Farmako)

    Diunggah oleh

    miftahul jannah
    10 tayangan13 halaman
    Metabolism of drugs involves biotransformation processes that convert non-polar lipid soluble compounds into more polar lipid insoluble compounds. This helps avoid reabsorption in the renal tubules and reduces toxicity. The liver is responsible for the majority of drug metabolism through first pass metabolism. Factors like concurrent drug use, genetic polymorphisms, environment, age, pregnancy, and nutrition can influence drug metabolism by inducing or inhibiting metabolic enzymes. Drug metabolism can result in active metabolites, inactive metabolites, or conversion of prodrugs to active drugs.

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    metabolisme obat-obatan

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    6. Metabolisme Obat (Farmako)

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    Metabolism of drugs involves biotransformation processes that convert non-polar lipid soluble compounds into more polar lipid insoluble compounds. This helps avoid reabsorption in the renal tubules and reduces toxicity. The liver is responsible for the majority of drug metabolism through first pass metabolism. Factors like concurrent drug use, genetic polymorphisms, environment, age, pregnancy, and nutrition can influence drug metabolism by inducing or inhibiting metabolic enzymes. Drug metabolism can result in active metabolites, inactive metabolites, or conversion of prodrugs to active drugs.

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    10 tayangan13 halaman

    Metabolisme Obat (Farmako)

    Diunggah oleh

    miftahul jannah
    Metabolism of drugs involves biotransformation processes that convert non-polar lipid soluble compounds into more polar lipid insoluble compounds. This helps avoid reabsorption in the renal tubules and reduces toxicity. The liver is responsible for the majority of drug metabolism through first pass metabolism. Factors like concurrent drug use, genetic polymorphisms, environment, age, pregnancy, and nutrition can influence drug metabolism by inducing or inhibiting metabolic enzymes. Drug metabolism can result in active metabolites, inactive metabolites, or conversion of prodrugs to active drugs.

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    © All Rights Reserved
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    dari 13

    METABOLISME OBAT

    Departemen Farmakologi
    Fakultas Kedokteran Universitas Tadulako
    METABOLISME OBAT –
    BIOTRANSFORMASI
    Adalah serangkaian proses kompleks yang dapat menurunkan
    tingkat toksik dan meningkatkan eksreksi dari molekul obat atau
    substansi asing saat masuk dalam tubuh
    Senyawa asing  xenobiotika
    Aim: to convert non-polar lipid soluble compounds to polar lipid
    insoluble compounds to avoid reabsorption in renal tubules
    PERAN BIOTRANSFORMASI
    Fase I
    • Obat induk menjadi metabolit yg
    lebih polar dengan
    memperkenalkan atau
    memunculkan suatu gugus
    fungsional (-OH, -NH2, -SH )
    • Kadang termodifikasi atau
    meningkat
    • Sifatnya katabolik
    Conjugation/hydrolysis reactions
    (Phase II)
    • Further modifications to
    compounds to improve
    hydrophilicity
    • Anabolic
    SITES OF DRUG METABOLISM

    • Liver – responsible for the


    majority of drug metabolism
     First pass metabolism
    • Kidney
    • GI
    • Lung
    • Skin
    • Brain
    RESULTS OF BIOTRANSFORMATION
    • Active drug and its metabolite to inactive metabolites – most
    drugs (ibuprofen, paracetamol, chlormphenicol etc.)
    • Active drug to active product (phenacetin – acetminophen or
    paracetamol, morphine to morphine-6-glucoronide, digitoxin
    to digoxin etc.)
    • Inactive drug to active/enhanced activity (prodrug) –
    levodopa - carbidopa, prednisone – prednisolone and
    enalapril – enalaprilat)
    • No toxic or less toxic drug to toxic metabolites (Isonizide to
    Acetyl isoniazide)
    BIOTRANSFORMATION OF DRUGS INTO
    ACTIVE (OR MORE ACTIVE) METABOLITES
    Initial drug Active metabolite
    • Allopurinol • Aloxantin
    • Amitriptilin • Nortriptilin
    • Acetylsalicylic acid • Salicylic acid
    • Butadion • Oxyfenbutazon
    • Diazepam • Dismethyldiazepam
    • Digitoxin • Digoxin
    • Codein • Morphine
    • Cortizol • Hydrocortizon
    • Methyldopa • Methylnoradrenalin
    • Prednison • Prednisolon
    • Novocainamid • N-acetylnovocainamid
    • Propranolol • N-oxypropranolol
    FACTORS AFFECTING BIOTRANSFORMATION

    Concurrent use of drugs: Induction and inhibition


    • Genetic polymorphism
    • Pollutant exposure from environment or industry
    • Pathological status
    • Age
    FACTORS THAT INFLUENCE ON DRUG METABOLISM

    Factor Reaction type


    Age (newborns, Decreasing of metabolism speed
    children, elderly)
    Pregnancy Increasing of metabolism speed
    Genetic factor Various reactions
    Liver pathology Decreasing of excreation speed of drugs, depending on their kinetics, type
    and stage of liver disease, increasing of bioavailability and decreasing of
    excretion speed of orally administered drugs with high hepatic clearence

    GI pathology Changes in metabolism in GI epithelium

    Nutrition Increasing of metabolism speed of certain drugs in case of diet with


    character dominance of proteins and carbohydrates
    Decreasing of metabolism speed in case of heavy digestive disorders linked
    with starvation (total or protein)
    Environment Increasing of metabolism speed if in contact
    with chlorine insecticides
    Alcohol
    — one time Depressing of enzymes that metabolise drugs
    consumption
    — chronic Induction of enzyme system
    consumption
    Smoking Increasing of metabolism of certain drugs (i.e.
    theophyllin)
    Way of Metabolism in liver before entering system
    excretion circulation (first going-through effect) after
    peroral administration of drugs
    Time of Circade changes in drugs metabolism
    introduction of
    drugs
    Interaction of Stimulation and depression of enzyme
    drugs reaction

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