Second line drugs are less effective, more toxic and costlier.
Para-Amino Salicylic Acid (PAS)
- Second line or reserve drug against Mycobacterium Tuberculosis
- Structurally similar to Sulfonamides and acts through a similar mechanism.
- Tuberculostatic.
Pharmacokinetics
- Well absorbed orally
- Poor concentration in the CSF
- Metabolised in the liver by acetylation
Interactions
- PAS reduces the absorption of Rifampicin
- Competetively inhibits the acetylation of Isoniazid
USE
- Reserve drug for the management of Multi Drug Resistant Tuberculosis
Adverse
- Similar to Sulpha drugs, Including rashes, steven-johnson syndrome, crystalluria etc.
Ethionamide
- Structurally similar to Isoniazid
- Bacteriostatic
- Effective against both Intacellular and extracellular bacilli
- Well absorbed orally, metabolized in the liver and excreted in urine.
Cycloserine
- Inhibits bacterial cell wall synthesis
- Bacteriostatic
- Well absorbed orally, crosses the Blood brain barrier and attains a good concentration in the CSF
- Main adverse effects on the CNS - Headache, confusion, psychosis, depression and suicidal ideation.
Newer anti-tubercular Agents - Only used for treatment of MDR - TB
- Newer Macrolides
- Fluoroquinolones
- Rifabutin
- Rifapentin
Rifabutin
- Derivative of Rifampicin
- Preferred over rifampicin in treatment of tuberculosis in HIV patients on Protease inhibitors as it induces the microsomal enzymes to a lesser extent
- Used in Mycobacterium Avium-Complex in combination with clarithromycin and Ethambutol.
Category:
Pharmacology Notes
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