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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIMYCOBACTERIALS › DRUGS FOR TREATMENT OF TUBERCULOSIS › Combinations of drugs for treatment of tuberculosis
pyrazinamide, ethambutol, protionamide and lomefloxacin
J04AM10
Forms & Strengths
- Fixed-dose combination tablets containing pyrazinamide, ethambutol hydrochloride, protionamide, and lomefloxacin
Adult Dosing
- Dosing is individualized based on patient weight and specific multidrug-resistant tuberculosis (MDR-TB) treatment regimens
- Typically administered as a single daily dose under direct observation (DOT)
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been fully established for this specific fixed-dose combination
- Individual component dosing is preferred in pediatric populations when required
Indications
- Treatment of multidrug-resistant tuberculosis (MDR-TB) caused by susceptible strains of Mycobacterium tuberculosis
Mechanism of Action
- Pyrazinamide disrupts mycobacterial membrane energetics and inhibits translation
- Ethambutol inhibits arabinosyl transferases, disrupting cell wall arabinogalactan synthesis
- Protionamide inhibits mycolic acid synthesis, leading to reduced cell wall integrity
- Lomefloxacin inhibits bacterial DNA gyrase and topoisomerase IV, preventing DNA replication and transcription
Contraindications
- Known hypersensitivity to pyrazinamide, ethambutol, protionamide, fluoroquinolones, or any component of the formulation
- Severe hepatic impairment (for pyrazinamide and protionamide components)
- Optic neuritis (for ethambutol component)
- History of tendinitis or tendon rupture associated with fluoroquinolones
Adverse Reactions
- Hepatotoxicity, ranging from asymptomatic transaminase elevations to severe hepatic necrosis
- Hyperuricemia and acute gouty arthritis (pyrazinamide)
- Optic neuritis characterized by reduced visual acuity and red-green color blindness (ethambutol)
- Gastrointestinal distress, nausea, vomiting, and anorexia
- Central nervous system effects including headache, dizziness, and peripheral neuropathy
- QT prolongation and tendinopathy (lomefloxacin)
Drug Interactions
- Antacids, sucralfate, and multivalent cations reduce absorption of the lomefloxacin component
- Concurrent use with other hepatotoxic drugs increases the risk of severe liver injury
- Pyrazinamide may decrease the serum concentrations of cyclosporine
- Potential additive QT prolongation when combined with other QT-prolonging agents
Curated Content: Needs Vetting Before Put to Clinical Use