In the pharmaceutical industry, Leflunomide 20 mg is a potent Disease-Modifying Antirheumatic Drug (DMARD). As a pharmacist, I classify this as an “immunomodulatory” agent. Unlike NSAIDs which only mask pain, Leflunomide is designed to slow down the underlying disease progression and prevent structural joint damage.
Primary Clinical Uses
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Active Rheumatoid Arthritis (RA): The primary indication for reducing signs and symptoms and inhibiting structural damage (joint erosion and joint space narrowing).
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Psoriatic Arthritis (PsA): Used to treat the joint inflammation associated with psoriasis, improving physical function and reducing skin involvement.
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Lupus Nephritis (Off-label): Occasionally used in specialized rheumatology for refractory cases of SLE where other treatments have failed.
Mechanism of Action: Inhibiting Pyrimidine Synthesis
Leflunomide is a prodrug that is rapidly converted in the intestinal wall and liver to its active metabolite, teriflunomide.
Enzyme Inhibition: It inhibits the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH).
Pyrimidine Depletion: This enzyme is essential for the de novo synthesis of uridine monophosphate (rUMP), a building block for DNA and RNA.
Lymphocyte Suppression: Rapidly dividing cells, like activated T-lymphocytes (which cause the inflammation in RA), depend on this de novo pathway. By cutting off their supply of pyrimidines, Leflunomide effectively “starves” the overactive immune cells, reducing joint inflammation without suppressing the rest of the immune system as severely as some other drugs.
The Manufacturer’s Perspective: Technical & Export Details
From a production and global trade standpoint, Leflunomide requires specific professional handling:
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The Loading Dose vs. Maintenance: Historically, a 100 mg “loading dose” was used for three days, but most modern protocols start directly with the 20 mg maintenance dose to reduce GI side effects. In your Product Information Leaflet (PIL), it is vital to reflect current clinical guidelines for your B2B buyers.
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Teratogenicity & “Washout” Procedures: Leflunomide has a very long half-life (up to 2 weeks) and is highly teratogenic. As a manufacturer, we must include strict warnings and the Cholestyramine washout protocol in our documentation to ensure safety for patients of childbearing age.
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Stability for Export: Leflunomide is relatively stable but sensitive to moisture. We utilize Alu-Alu blister packaging at our WHO-GMP facility to ensure a 36-month shelf life for export to Zone IVb regions.
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Dossier Support: This is a high-value item in the rheumatology segment. Our Mumbai facility provides full CTD/eCTD Dossiers to support registration against the innovator (Arava).