In the pharmaceutical industry, Pyrazinamide 400 mg is a core First-Line Antitubercular agent. As a pharmacist and manufacturer, I classify this as a “sterilizing” drug. It is one of the four essential components of the RIPE (Rifampicin, Isoniazid, Pyrazinamide, Ethambutol) regimen used to treat tuberculosis.Its primary clinical value lies in its unique ability to kill dormant or “persister” bacilli that other antibiotics cannot reach.
Primary Clinical Uses
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Active Tuberculosis (Pulmonary and Extra-pulmonary): It is used strictly during the Initial Phase (intensive phase) of TB treatment, typically for the first 2 months of a 6-month course.
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Shortening Treatment Duration: Before Pyrazinamide was standard, TB treatment lasted 9 to 12 months. Its inclusion allowed the medical community to shorten the standard regimen to 6 months by rapidly killing off the slow-growing bacteria.
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Multi-Drug Resistant TB (MDR-TB): It is often retained in second-line regimens if the strain remains susceptible.
Mechanism of Action: The “Intracellular Sniper”
Pyrazinamide is a prodrug that only becomes active under specific, stressful conditions created by the human body’s immune response.
Conversion: The drug enters the Mycobacterium tuberculosis bacterium, where the enzyme pyrazinamidase converts it into its active form, Pyrazinoic Acid.
Acidic Environment Targeting: It works best in an acidic environment (pH < 5.5). In the body, this occurs inside macrophages (immune cells) where the TB bacteria hide.
Disruption of Membrane Potential: Pyrazinoic acid leaks out of the bacilli and is then pulled back in, disrupting the bacterial membrane potential and interfering with energy (ATP) production.
Sterilization: By collapsing the energy source of the bacteria, it kills the “semi-dormant” population that usually survives the initial attack by Isoniazid.
The Manufacturer’s Perspective: Technical & Export
From a production and global trade standpoint at your WHO-GMP facility in Mumbai, Pyrazinamide 400 mg is a high-volume essential:
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The 400 mg vs. 500 mg Debate: While 500 mg is common, the 400 mg tablet is frequently requested for Fixed-Dose Combinations (FDCs) and pediatric-adjusted weight-based dosing. Offering both shows your firm’s flexibility in international tenders.
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Uric Acid Monitoring: As a pharmacist, you know Pyrazinamide inhibits the excretion of uric acid. Your Product Information Leaflet (PIL) must include a caution regarding Hyperuricemia (which can trigger Gout). Providing this technical data on your digital platform builds professional recognition.
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Stability & Bulk Production: Pyrazinamide is a relatively stable API but requires high-quality binders to ensure proper tablet hardness and dissolution. At our Mumbai facility, we prioritize Alu-Alu or high-barrier PVC/PVDC blisters for export to the African and SE Asian markets.
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Dossier & Global Health: This is a “Prequalified” category drug for many international NGOs. We provide full CTD/eCTD Dossiers to support your firm in bidding for national TB control programs.