o/dr.ririn fk unila

7/30/2019 o/dr.ririn fk unila

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Overview

INH (H)

Ethambutol (E)

Pyrazinamide (Z)

Rifampicin (R)

Dapsone (D) Clofazimine (C)

For TBC

For Leprosy

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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

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Overview

Long therapycost

Multiple drugs AEs

Thats why morbidity & mortality are still high

Indonesia : the 3rd in the world

HIV (+) and poor increase the occurrence of TB

compliance

treatment failure

drug resistance

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Overview

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Overview


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Overview


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

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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

RIFAMPICIN

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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!

RIFAMPICIN

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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

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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

ISONIAZID

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Peripheral neuritis (numbness) B6

Hepatitis (together with R and Z)

Skin reaction

G-6 PD hemolytic anemia

DI: inhibitor CYP

ISONIAZID

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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

ETHAMBUTOL

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2nd ANTI TB

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2nd ANTI TB

inhibit cell wall synthesis (involving D-alanin)

liver metabolism, renal excreted

AEs: CNS disturbance, epileptic seizure, peripheral

neuropathy

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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

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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)

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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

CLOFAZIMINE

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o/dr.ririn fk unila

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