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    Anti-TB Drugs

    Uploaded by

    Ukash sukarman
    Anti TB Drugs

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd

    Anti-TB Drugs

    Uploaded by

    Ukash sukarman
    5 views17 pages
    Anti TB Drugs

    Original Title

    Anti-TB drugs

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    Anti TB Drugs

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    5 views17 pages

    Anti-TB Drugs

    Uploaded by

    Ukash sukarman
    Anti TB Drugs

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 17

    Tuberculosis and Antituberculosis

    (Anti-TB) drugs
    Tuberculosis or pulmonary tuberculosis is caused by
    Mycobacterium Tuberculosis( MTB)
    CLASSIFICATION OF DRUGS
    : base on their efficacies and toxicities
    First-line drugs: Good efficacy, cheap, less
    toxicity and being well tolerated to patients
    (PRIEST) P-pyrazinamide,R-Rifampicin, I-
    Isoniazide,E-ethambutol,S-Streptomycin
    . Second-line drugs:less efficacy,More
    toxicity,veryexpensive, Difficult for patient to tolerate
    Please TAKE Carbon Copy
    P-PAS ( P-aminosalicylicacid) ,T-thioacetazone,A-
    Amikacin,K-Kanamycin,E-ethionamide, C-
    Cyclserine, C-Capreomycin
    Antibiotics used In TB

    a) Aminoglycosides—

    Streptomycin,Kanamycin,Amikacin

    b) Macrolides-RACE

    C) Natural derivative- Rifampicin

    D) Fluroquinolones( FQ)-Ciprofloxacin
    Based on mechanism of action
    1.Mycobacterium Cell wall synthesis blockers
    Mycolic acid synthesis blocker-Isoniazide,Pyrazinamide
    Arabinogalan synthesis blocker-Ethambutol
    Peptidoglycan synthesis blocker- Cycloserine
    2.Drugs inhibiting protein synthesis
    a) By blocking 30 s ribsome- Aminoglycosides
    b) By blocking 50 s ribosome- Macrolides

    3.Drugs inhibiting Nucleic acid synthesis


    a)Inhibiting RNA synthesis- Rifampicin
    b)Inhibiting DNA Synthesis-Fluroquinolones
    4.Drug Inhibiting folic acid synthesis- PAS
    1.Cell wall synthesis blockers
    a) Drugs inhibiting fatty acid ( mycolic acid) layer
    of cell wall
    Example - Isoniazide (INH) , Pyrazinamide

    Isoniazide( INH) - Isonicotinyl hydrazide


    Mechanisam:
    INH inhibits synthesis of mycolic acid ( fatty
    acid layer) in the mycobacterial cell wall- cell wall
    loses its rigidity - acts as bactericidal
    Adverse effects-nephrotoxicity,Hepatotoxicity
    so reduce toxicity it is coadminstrated with
    vitamin B6
    6
    b) Drugs inhibiting arabino galactan layer of cell
    wall Example- Ethambutol( eye toxicity)
    Mechanisam
    Ethambutol inhibits Arabinosyl transferase (AT) enzyme
    there by prevent synthesis of arabinogalactan layer in the
    in the mycobacterial cell wall- (act as Bactrostatic)
    Arabinose + Galactan ( galactose polymer)

    Ethambutol Arabinosyl transferase ( AT)

    Arabino galactan (AG)

    Required for cell wall re rigidity


    c) . Drugs inhibiting peptidoglycan layer of cell
    wall Example- Cycloserine
    Cycloserine inhibits L-alanine racemase
    and D-alanine lygase there by prevent
    synthesis of dipeptide –D-alanyl D-alanine
    L-alanine
    L-alanine racemase

    D-alanine
    Cycloserine
    D-alanine lygase

    D-alanyl-D-alanine
    2.Drugs inhibiting protein synthesis
    A) AMINOGLYCOSIDES- STREPTOMYCIN
     Aminoglycoside - Inhibits protein synthesis by
    blocking to 30 S ribosome subunit
     Bactericidal 5 NOS- 1) No To pregnacy woman
     2) No protein synthesis
     3) Not orally( IM)
     Effective against Aerobic 4) NO- negative-organisaM
    5) NO-
    nephrotoxicty ,Ototoxicity
    2.Drugs inhibiting protein synthesis
    B)MACROLIDES-RACE
     Macrolides - Inhibits protein synthesis by blocking
    to 50 S ribsome subunit
     Bactreostatic
     RACE- Roxithromycin, Azithromycin,
    Clarithromycin,Erythromycin
    3.Drug inhibiting Nucleic acid synthesis

    a) Rifampicin ( m RNA synthesis blocker)


    Broad-spectrum
    It is bactericidal for mycobacteria.
    Mechanism
    RFP inhibits DNA depended RNA polymerase
    (DDRP)and thereby inhibits m RNA synthesis. so
    RFP inhibits transcription process
    Transcription DDRP
    DNA RNA

    Uses – Anti leprotic


    b) Flouroquinolones ( DNA synthesis blocker)
    Broad-spectrum
    It is bactericidal for mycobacteria.
    Mechanism
    Fluroquinolines inhibits DNA Gyragse
    (Topoisomerase-II )and thereby inhibits RNA
    synthesis.
    4. Drug inhibiting Folic acid synthesis

    PAS-(p-amino salicylic acid)

    It act as second line anti TB drug-


    Act as Bactriostaic

    Mechanism
    PAS inhibits DHFR ( dihydrofolate reductase )
    there by inhibits synthesis of folic acid
    4. P-aminosalicylic acid- DHFR blocker

    PAS

    Fansidar- sulfadoxine+ pyrimethamine

    Clotimaxozle- sulfamethoxazole+
    trimethoprim

    14
    PULMONARY TB

    Initial phase –
     INAH+Pyridoxine
     Rifampicin
    2 months
     Ethambutol
     Pyrazinamide

    Continuation phase –
     INAH+Pyridoxine
     Rifampicin 4 months

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