Leflunomida Aurovitas (Leflunomide)

Leflunomide is a disease-modifying antirheumatic drug (DMARD) that interferes with lymphocyte proliferation, thereby targeting the inflammatory pathways that drive autoimmune joint disorders.

• Rheumatoid arthritis: reduces joint inflammation, pain, and structural damage, improving functional ability in adult patients with moderate to severe disease.
• Psoriatic arthritis: alleviates skin and joint symptoms, slowing progression of joint erosion and improving quality of life in adult patients with the condition.
• Combination therapy: employed alongside other DMARDs or biologics to achieve better disease control when monotherapy is insufficient.

• Leflunomide is metabolized to its active form, teriflunomide, which inhibits the mitochondrial enzyme dihydroorotate dehydrogenase. This blockade prevents de novo synthesis of pyrimidine nucleotides, limiting proliferation of activated T and B lymphocytes and thereby reducing the autoimmune inflammatory response in the joints. The inhibition is selective for rapidly dividing cells, sparing resting cells, and leads to decreased production of cytokines such as IL‑2 and interferon‑γ, contributing to its immunosuppressive effect.

Leflunomide may cause a range of adverse reactions, varying from mild to severe.

Common Side Effects

• Diarrhea: loose stools or increased frequency.
• Nausea: feeling of sickness or urge to vomit.
• Elevated liver enzymes: increased ALT/AST indicating hepatic stress.
• Hypertension: rise in blood pressure readings.
• Rash: mild skin irritation or itching.

Serious or Rare Side Effects

• Severe liver injury: jaundice, hepatitis, or liver failure.
• Bone marrow suppression: anemia, leukopenia, or thrombocytopenia.
• Pulmonary toxicity: interstitial lung disease or severe respiratory symptoms.

When prescribing Leflunomida Aurovitas, clinicians should observe several precautionary measures to minimize risks.

• Pregnancy contraindication: avoid use in pregnancy due to teratogenic risk (Category X).
• Liver function monitoring: assess baseline hepatic enzymes and repeat periodically.
• Hematologic monitoring: perform complete blood count before and during therapy.
• Drug interactions: avoid concomitant use with teratogenic agents or strong CYP inducers without adjustment.
• Infection risk: monitor for signs of infection and delay treatment in active infections.
• Store at ambient temperature: keep below 25 °C in original packaging, protect from moisture.

Leflunomide can affect the pharmacokinetics of several medicines, requiring careful management.

Major Interactions (Avoid)

• Warfarin: increased anticoagulant effect, may raise INR.
• Methotrexate: additive toxicity, especially hepatic.
• Live vaccines: risk of infection due to immunosuppression.

Moderate Interactions (Monitor Closely)

• CYP3A4 inducers (e.g., rifampin, carbamazepine): reduce teriflunomide levels, decreasing efficacy.
• CYP2C9 inhibitors (e.g., fluconazole): may increase teriflunomide concentrations.
• NSAIDs: may enhance risk of hypertension and renal impairment.