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    O/dr - Ririn FK Unila

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    Nyimas Annissa Mutiara Andini
    This document provides an overview of drugs used to treat tuberculosis (TB) and leprosy. It discusses the first-line anti-TB drugs isoniazid, rifampicin, pyrazinamide, and ethambutol. It describes their mechanisms of action, pharmacokinetics, resistance, and adverse effects. It also discusses the second-line anti-TB drug dapsone and its role along with clofazimine and rifampicin in the WHO recommended triple drug regimen for treating leprosy.

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    O/dr - Ririn FK Unila

    Uploaded by

    Nyimas Annissa Mutiara Andini
    58 views29 pages
    This document provides an overview of drugs used to treat tuberculosis (TB) and leprosy. It discusses the first-line anti-TB drugs isoniazid, rifampicin, pyrazinamide, and ethambutol. It describes their mechanisms of action, pharmacokinetics, resistance, and adverse effects. It also discusses the second-line anti-TB drug dapsone and its role along with clofazimine and rifampicin in the WHO recommended triple drug regimen for treating leprosy.

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    o/dr.ririn fk unila

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    This document provides an overview of drugs used to treat tuberculosis (TB) and leprosy. It discusses the first-line anti-TB drugs isoniazid, rifampicin, pyrazinamide, and ethambutol. It describes their mechanisms of action, pharmacokinetics, resistance, and adverse effects. It also discusses the second-line anti-TB drug dapsone and its role along with clofazimine and rifampicin in the WHO recommended triple drug regimen for treating leprosy.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPSX, PDF, TXT or read online from Scribd
    Download as ppsx, pdf, or txt
    58 views29 pages

    O/dr - Ririn FK Unila

    Uploaded by

    Nyimas Annissa Mutiara Andini
    This document provides an overview of drugs used to treat tuberculosis (TB) and leprosy. It discusses the first-line anti-TB drugs isoniazid, rifampicin, pyrazinamide, and ethambutol. It describes their mechanisms of action, pharmacokinetics, resistance, and adverse effects. It also discusses the second-line anti-TB drug dapsone and its role along with clofazimine and rifampicin in the WHO recommended triple drug regimen for treating leprosy.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPSX, PDF, TXT or read online from Scribd
    Download as ppsx, pdf, or txt
    of 29

    Overview

    INH (H) Ethambutol (E) Pyrazinamide (Z) Rifampicin (R) Dapsone (D) Clofazimine (C)

    For TBC

    For Leprosy

    Overview
    TB is a chronic infection due to M.tuberculosis

    - (acid fast bacilli) mycolic acid


    - slow growth resistant to most AM and need long therapy Monotherapy leads to resistance need combination therapy (> 2 drugs) Long therapy : 6-m 2-y
    3

    Overview
    Long therapy cost compliance Multiple drugs AEs

    treatment failure drug resistance Thats why morbidity & mortality are still high
    Indonesia : the 3rd in the world HIV (+) and poor increase the occurrence of TB
    4

    Overview

    Overview

    Overview

    M.O.A and spectrum: inhibit DNA replication by inhibiting DNA polymerase specific

    10

    RIFAMPICIN
    bactericidal for intra- & extracellular mycobacteria the most active anti TB drug also active for gram (-) sp. TBC, Leprosy, severe gram (-) infection Resistance:
    changes the affinity of the enzyme
    decreased permeability of the mycobacteria
    11

    RIFAMPICIN
    A : p.o well absorbed, esp in empty stomach Dairy food and Antacida (Al, Mg) absorption D: liver by CYP 450 active metabolite Cross BBB in non-inflammed meningen Inducer for CYP 450 !!!

    Orange red color of body fluid (saliva, urine)

    E: bile (and kidney)


    12

    RIFAMPICIN

    GI upset (but not to give with dairy product or antacid!) Coloration of urine, saliva, etc Rash, fever, arthralgia ( uric acid), Hepatitis
    Check for LFT and uric acid regularly Becareful in elderly, alcoholism Drug Interaction!

    13

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    ISONIAZID

    The hydrazide of isonicotinic acid, a synthetic analogue of pyridoxine (B6) MOA ? Unclear inhibit synthesis of mycolic acid Spectra? limited to mycobacteria Bacteriostatic (for dormant) but cidal (for growing)

    Resistance: reduced penetration of the drug


    15

    ISONIAZID

    A : orally, impaired abs if taken with food and antacid D: Widely distributed (include in caseous material), CSF M: liver acetylation (slow and fast) related to AEs and drugs concentrations; involved by genetics E: kidney

    16

    ISONIAZID
    Peripheral neuritis (numbness) B6 Hepatitis (together with R and Z) Skin reaction G-6 PD hemolytic anemia DI: inhibitor CYP

    17

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    PYRAZINAMIDE
    bactericidal anti-TB (active dividing mycobacteria)

    active only in low pH (in early treatment)


    Z hydrolize pyrazinoic acid (active ) PK: oral, well distributed (include CSF) AEs: hepatotoxicity, arthralgia (uric acid)

    19

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    ETHAMBUTOL
    Only for mycobacterium MOA is ?? Bacteristatic Oral kidney AEs : optic neuritis visual acquity and red/green blindness

    CI for children
    Only for the first 2-m of TB treatment
    21

    2nd ANTI TB

    22

    2nd ANTI TB
    inhibit cell wall synthesis (involving D-alanin) liver metabolism, renal excreted AEs: CNS disturbance, epileptic seizure, peripheral neuropathy

    23

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    Overview
    Leprosy (Hansens disease) is caused by M.leprae

    Bacilli from skin or nasal discharge


    2 extreme conditions: skin macules: cell mediated imm is OK
    disseminated lepromatous: cell mediated imm is impaired

    all destruction happen

    WHO: triple drug regimen: R + D + CL


    25

    WHO recommendation
    for tuberculoid leprosy: D + R

    for lepromatous leprosy: D + R + CL (2 - 5years)


    100 mg D + 50 mg C daily (unsupervised at home) + 600 mg R + 300 mg CL monthly (supervised)

    26

    DAPSONE
    Chemically related to sulfonamides Bacteriostatic for M.leprae PK: oral well absorbed wide distribution Long half-life Entero-hepatic circulation urine AEs: a-n-n, allergic, peripheral neuropathy

    Anemia (hemolysis), met-Hb-emia

    27

    CLOFAZIMINE
    A phenazine dye binds to DNA block the template function Bactericid for m.leprae Oral well distributed accumulated in the tissue Effect is delayed after 6-7 weeks Very very long half-life (8-weeks)

    AEs: red-brown discolorization

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