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  • Unit 4 AntiTB Agents

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    Trisha Mallari
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    This document discusses drugs used to treat tuberculosis and leprosy. The primary agents used to treat tuberculosis are isoniazid, rifampin, ethambutol, pyrazinamide, and streptomycin. Secondary agents include capreomycin, cycloserine, ethionamide, and kanamycin. Adverse effects and mechanisms of action are provided for many of the drugs. Rifamycins like rifampin are derived from Streptomyces bacteria and are highly effective against tuberculosis.

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    Important notes about TB.

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    This document discusses drugs used to treat tuberculosis and leprosy. The primary agents used to treat tuberculosis are isoniazid, rifampin, ethambutol, pyrazinamide, and streptomycin. Secondary agents include capreomycin, cycloserine, ethionamide, and kanamycin. Adverse effects and mechanisms of action are provided for many of the drugs. Rifamycins like rifampin are derived from Streptomyces bacteria and are highly effective against tuberculosis.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
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    14 views10 pages

    Unit 4 AntiTB Agents

    Uploaded by

    Trisha Mallari
    This document discusses drugs used to treat tuberculosis and leprosy. The primary agents used to treat tuberculosis are isoniazid, rifampin, ethambutol, pyrazinamide, and streptomycin. Secondary agents include capreomycin, cycloserine, ethionamide, and kanamycin. Adverse effects and mechanisms of action are provided for many of the drugs. Rifamycins like rifampin are derived from Streptomyces bacteria and are highly effective against tuberculosis.

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    © All Rights Reserved
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    of 10

    RALS, MS, RPh, LPT

    Department of Pharmacy, CAMP


    • Treatment of mycobacterial
    infections caused by
    Mycobacterium tuberculosis
    and Mycobacterium leprae

    Mycobacterium tuberculosis
    • Conveyed by droplets, expelled
    by coughing or sneezing, gain
    entry to the body by inhalation
    • Common infection sites: lungs,
    brain, bone, liver, kidney
    STREPTOMYCIN
    KANAMYCIN
    CAPREOMYCIN

    CYCLOSERINE
    ETHIONAMIDE
    ISONIAZID
    RIFAMPICIN
    RIFABUTIN

    P-AMINOSALICYLIC
    ACID
    PRIMARY AGENTS
    • ISONIAZID
    • RIFAMPICIN
    • ETHAMBUTOL
    • PYRAZINAMIDE
    • STREPTOMYCIN

    SECONDARY AGENTS
    • CAPREOMYCIN
    • CYCLOSERINE
    • ETHIONAMIDE
    • KANAMYCIN
    • P-AMINO SALICYLIC ACID
    ISONIAZID ETHIONAMIDE
    • Isonicotinic acid hydrazide • Second drug for the treatment of
    • INH tuberculosis
    • Drug of choice for TB • Treatment of Isoniazid-resistant
    • S/E: peripheral neuropathy, tuberculosis
    hepatotoxicity • S/E: GI intolerance, visual
    • MOA: Inhibits the synthesis of disturbance and hepatotoxicity
    mycolic acid

    PYRAZINAMIDE ETHAMBUTOL
    • PZA (Pyrazinecarboxamide) • Active only against dividing
    • It is not suitable for long term mycobacteria
    therapy • MOA: Inhibition of the incorporation
    • S/E: potential hepatotoxicity of mycolic acids into the cell walls of
    • May interfere with uric acid excretion the mycobacterium.
    • S/E: Retrobulbar neuritis
    AMINO SALICYLIC ACID CLOFAZIMINE
    • MOA: Similar to the sulfonamides • Basic red dye
    • S/E: Gastrointestinal irritation • Mycobacterium leprae
    • Treatment of lepromatous leprosy
    including dapsone-resistant forms of
    the disease.
    • MOA: Bind to the nucleic acids and
    concentrate in reticuloendothelial
    tissue; interfere with the electron
    transport process
    ANTITUBERCULAR ANTIBIOTICS

    RIFAMYCINS: GENERAL PROPERTIES


    • Fermentation of the cultures of Streptomyces mediterranei
    • Ansamycins (contain a macrocyclic ring bridged across two non-
    adjacent positions in an aromatic nucleus).

    RIFAMPIN
    • Rifampicin
    • Most active agent in the clinical use
    for the treatment of tuberculosis
    • S/E: Hepatitis, discoloration of urine,
    stool, saliva, tears and skin; may also
    permanently discolor soft contact
    lenses.
    RIFAMYCINS

    CYCLOSERINE STERILE CAPREOMYCIN SULFATE


    • Streptomyces orchidaceus, S. • Strongly basic cyclic peptide
    garyphalus, and S. lavendulus • Streptomyces capreolus
    • MOA: Preventing the synthesis of • S/E: damage to the 8th cranial nerve
    cross linking peptide in the formation and renal damage
    of bacterial cell walls.

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