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    Chloramphenicol is a broad-spectrum antibacterial agent that inhibits protein synthesis by binding to the 50S subunit of bacteria. It is bacteriostatic but can be bactericidal against some species. Chloramphenicol is rapidly absorbed from the gastrointestinal tract, well distributed throughout the body including crossing the blood-brain barrier, metabolized in the liver, and excreted in the urine. It is effective against a variety of gram-positive and gram-negative bacteria as well as some rickettsiae and anaerobes but has significant toxicities limiting its clinical use.

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    mechanism of action of chloramphenicol

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    medicinal chemistry

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    Chloramphenicol is a broad-spectrum antibacterial agent that inhibits protein synthesis by binding to the 50S subunit of bacteria. It is bacteriostatic but can be bactericidal against some species. Chloramphenicol is rapidly absorbed from the gastrointestinal tract, well distributed throughout the body including crossing the blood-brain barrier, metabolized in the liver, and excreted in the urine. It is effective against a variety of gram-positive and gram-negative bacteria as well as some rickettsiae and anaerobes but has significant toxicities limiting its clinical use.

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    42 views7 pages

    Medicinal Chemistry

    Uploaded by

    deep469
    Chloramphenicol is a broad-spectrum antibacterial agent that inhibits protein synthesis by binding to the 50S subunit of bacteria. It is bacteriostatic but can be bactericidal against some species. Chloramphenicol is rapidly absorbed from the gastrointestinal tract, well distributed throughout the body including crossing the blood-brain barrier, metabolized in the liver, and excreted in the urine. It is effective against a variety of gram-positive and gram-negative bacteria as well as some rickettsiae and anaerobes but has significant toxicities limiting its clinical use.

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    © All Rights Reserved
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    of 7

    B.

    Pharm 4th year


    Semester VII
    MC II
    November 2014

    Antibacterial agents
    Chloramphenicol

    Chloramphenicol

    MOA
    Inhibits protein synthesis ( 50 s subunit )
    Bacteriostatic, bactericidal for some species
    Blacks elongation of proteins by inhibiting
    formation of initiation complexes and
    peptidyltransferase

    Pharmacokinetics

    Rapidly & completely absorbed from GIT


    30 % protein bound
    Metabolized by liver glucuronidation
    Well distributed, including CNS and CSF
    Excreted in urine

    Spectrum of action

    Antibacterial activity
    H. Influenzae
    N. Meningitidis
    S. Pneumoniae
    Ricketsiae
    & B. fragilis

    S. typhi
    E. coli
    V.cholera
    Anaerobes- clostridium

    Clinical uses

    Limited because of potential toxicities


    Anaemia & circulatory collapse in neonates
    Typhoid fever- s. typhi (Quinolones are preffered)
    Meningitis H. influenzae, N. meningitidis, S.
    pneumoniae (Ceftriaxone is preffered )
    Anaerobic infections- B. fragilis (Metronidazole is the
    drug of choice)
    Rickettsial infections Doxycycline is preffered
    Bacterial conjunctivitis (topical )

    Side effects

    Hypersensitivity- low incidence


    May ppt hemolysis in G6PD deficient pts
    Anaemia (fatal )
    Grey baby syndrome
    Suprainfections
    Interaction with other drugs :
    Inhibits liver microsomal enzymes

    Phenytoin
    Tolbutamide
    Chlorpropamide
    Anticoagulants

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