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  • Antimycobacterial Agents

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    Lee bella
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    Isoniazid, rifampin, pyrazinamide, and ethambutol are traditional first-line drugs used to treat tuberculosis. An isoniazid-rifampin combination administered for 9 months cures 95-98% of cases caused by susceptible strains. Isoniazid is the most active drug, penetrating macrophages to target both extracellular and intracellular bacteria. It inhibits mycolic acid synthesis via interactions with kasA and inhA, though mutations can cause resistance. Typical dosing is 5-10 mg/kg daily or 15 mg/kg twice weekly, with pyridoxine supplementation to prevent neuropathy being a potential adverse effect.

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    Isoniazid, rifampin, pyrazinamide, and ethambutol are traditional first-line drugs used to treat tuberculosis. An isoniazid-rifampin combination administered for 9 months cures 95-98% of cases caused by susceptible strains. Isoniazid is the most active drug, penetrating macrophages to target both extracellular and intracellular bacteria. It inhibits mycolic acid synthesis via interactions with kasA and inhA, though mutations can cause resistance. Typical dosing is 5-10 mg/kg daily or 15 mg/kg twice weekly, with pyridoxine supplementation to prevent neuropathy being a potential adverse effect.

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    13 views5 pages

    Antimycobacterial Agents

    Uploaded by

    Lee bella
    Isoniazid, rifampin, pyrazinamide, and ethambutol are traditional first-line drugs used to treat tuberculosis. An isoniazid-rifampin combination administered for 9 months cures 95-98% of cases caused by susceptible strains. Isoniazid is the most active drug, penetrating macrophages to target both extracellular and intracellular bacteria. It inhibits mycolic acid synthesis via interactions with kasA and inhA, though mutations can cause resistance. Typical dosing is 5-10 mg/kg daily or 15 mg/kg twice weekly, with pyridoxine supplementation to prevent neuropathy being a potential adverse effect.

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    © All Rights Reserved
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    of 5

    DRUGS USED IN

    TUBERCULOSIS
    Drugs used in Tuberculosis

    • Isoniazid (INH), rifampin (or other rifamycin), pyrazinamide, and


    ethambutol are the traditional first-line agents for treatment of
    tuberculosis.
    • An isoniazid-rifampin combination administered for 9 months will
    cure 95–98% of cases of tuberculosis caused by susceptible strains.
    ❑ ISONIAZID (Isonicotinic acid hydrazide, H)
    Most active drug for the treatment of tuberculosis
    • Freely soluble in water
    • Bactericidal for actively growing tubercle bacilli.
    • Penetrates into macrophages and is active against both extracellular and
    intracellular organisms.
    ❑ ISONIAZID (Isonicotinic acid hydrazide, H)
    • Mechanism of Action :
    • Inhibits synthesis of mycolic acids.
    • Prodrug activated by katG, the mycobacterial catalase-peroxidase .
    • Forms a covalent complex with an acyl carrier protein (AcpM) and KasA,
    a beta-ketoacyl carrier protein synthetase, which blocks mycolic acid
    synthesis and kills the cell .
    • Resistance:
    • Mutations resulting in overexpression of inhA, which encodes an NADH-
    dependent acyl carrier protein reductase.
    • Mutation or deletion of the katG gene; promoter mutations resulting in
    overexpression of ahpC.
    ISONIAZID (INH)
    PHARMACOKINETICS CLINICAL USES ADVERSE EFFECTS

    Absorption: • Typical dosage of isoniazid is 5 Immunologic Reactions:


    • INH readily absorbed from the GIT. mg/kg/d-10 mg/kg/d (sever Fever and skin rashes are
    Distribution: infection) or 15 mg/kg dose - twice occasionally seen. Drug-
    • All body tissues and fluids including weekly induced systemic lupus
    CSF; crosses placenta, enters breast erythematosus reported.
    milk • Adult dose : 300 mg oral dose O.D.
    Direct Toxicity:
    Metabolism: • Pyridoxine, 25-50 mg/d - • induced hepatitis
    • acetylation by liver N-acetyltransferase, predisposing to neuropathy, an • Clinical hepatitis with loss of
    is genetically determined adverse effect of isoniazid appetite, nausea, vomiting,
    jaundice, and right upper
    Elimination: • Latent tuberculosis : 300 mg/d (5 quadrant pain
    • Half-life elimination: fast acetylators: 30- mg/kg/d) or900 mg twice weekly for • Peripheral neuropathy
    100 min; slow acetylators: 2-3 hr; may 9 months • Central nervous system
    be prolonged with hepatic or severe toxicity.
    renal impairment
    • Excretion: Urine (75-95%); feces.

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