Arava (leflunomide) is a disease-modifying antirheumatic drug (DMARD) specifically indicated for the treatment of adults with active rheumatoid arthritis. As a selective inhibitor of pyrimidine synthesis, it targets rapidly dividing immune cells to reduce inflammation, slow joint damage progression, and improve physical function. This oral medication offers a convenient dosing regimen and demonstrated efficacy in clinical trials, making it a cornerstone therapy for managing moderate to severe disease. Healthcare providers value its well-established safety profile and predictable pharmacokinetics when used according to guidelines.

Features

• Active ingredient: Leflunomide 10mg, 20mg tablets
• Mechanism: Inhibits dihydroorotate dehydrogenase (DHODH), reducing pyrimidine synthesis in activated lymphocytes
• Administration: Oral, once-daily dosing
• Bioavailability: >80% with rapid conversion to active metabolite
• Half-life: Approximately 2 weeks for primary metabolite
• Excretion: Undergoes enterohepatic recycling and fecal elimination

Benefits

• Reduces pain, swelling, and morning stiffness associated with active rheumatoid arthritis
• Slows radiographic progression of joint erosion and cartilage damage
• Improves physical function and quality of life measures
• Offers convenient once-daily oral administration compared to injectable alternatives
• Demonstrates sustained efficacy in long-term clinical studies
• Provides targeted immunomodulation with predictable response patterns

Common use

Arava is primarily prescribed for the management of active rheumatoid arthritis in adults who have had inadequate response to one or more DMARDs. It is frequently used as monotherapy or in combination with other antirheumatic agents, particularly methotrexate, following thorough assessment of patient suitability. The medication is typically initiated after comprehensive rheumatologic evaluation and baseline laboratory testing. Clinical practice guidelines position Arava as a first-line or second-line synthetic DMARD option depending on disease severity, patient comorbidities, and treatment history.

Dosage and direction

The recommended dosing regimen involves an initial loading dose of 100 mg once daily for 3 days, followed by a maintenance dose of 20 mg once daily. For patients who cannot tolerate the 20 mg dose, the maintenance dose may be reduced to 10 mg daily. Administration should occur at approximately the same time each day, with or without food, though consistency in timing relative to meals is advised. The tablets should be swallowed whole with water and not crushed or chewed. Dose adjustments may be necessary based on clinical response, tolerability, and laboratory parameters.

Precautions

Regular monitoring of liver enzymes (ALT) is required before initiation and at least monthly during initial treatment, then periodically thereafter. Complete blood count and blood pressure should be monitored periodically. Patients should be advised that Arava may cause hypertension, which requires ongoing assessment. Due to the long half-life, the drug remains in the system for extended periods after discontinuation. Women of childbearing potential must use reliable contraception during treatment and during drug elimination procedures afterward. Vaccination with live vaccines should be avoided during therapy.

Contraindications

Arava is contraindicated in patients with known hypersensitivity to leflunomide or any component of the formulation. It must not be used in patients with severe hepatic impairment or pre-existing liver disease. The medication is contraindicated in patients with severe immunodeficiency, bone marrow dysplasia, or severe uncontrolled infections. Pregnancy and breastfeeding represent absolute contraindications due to teratogenic risks. Concomitant use with teriflunomide is prohibited. The drug should not be administered to patients with severe hypoproteinemia or those undergoing dialysis.

Possible side effects

Common adverse reactions (≥5%) include diarrhea, nausea, headache, hypertension, alopecia, rash, and respiratory infections. Less frequent but clinically significant side effects may include elevated liver enzymes, weight loss, abdominal pain, back pain, dizziness, and oral ulcers. Serious adverse events, though rare, include hepatotoxicity, severe skin reactions, peripheral neuropathy, interstitial lung disease, and bone marrow suppression. Most side effects are dose-dependent and often manageable with dose reduction or symptomatic treatment.

Drug interaction

Arava interacts significantly with drugs metabolized by CYP2C8 (e.g., repaglinide, paclitaxel) and may increase their plasma concentrations. Concurrent use with other hepatotoxic drugs (including methotrexate) requires enhanced monitoring. Cholestyramine and activated charcoal accelerate elimination of the active metabolite. Warfarin monitoring should be intensified due to potential INR changes. Rifampin may increase leflunomide metabolite levels. The combination with other immunosuppressants may potentiate infection risk. Healthcare providers should conduct comprehensive medication reviews before initiation.

Missed dose

If a dose is missed, patients should take it as soon as remembered on the same day. If remembered the next day, the missed dose should be skipped and the regular schedule resumed. Patients should never double the dose to make up for a missed administration. Consistent daily dosing is important for maintaining therapeutic levels, though the long half-life provides some forgiveness for occasional missed doses. Patients should inform their healthcare provider about pattern of missed doses during follow-up visits.

Overdose

In case of suspected overdose, symptoms may include elevated liver enzymes, gastrointestinal distress, or neurological symptoms. There is no specific antidote for leflunomide overdose. Management involves immediate gastric lavage if ingestion was recent and administration of cholestyramine (8 g three times daily for 24 hours) or activated charcoal to enhance elimination. Supportive care should include monitoring of hepatic and hematological parameters. In severe cases, plasmapheresis may be considered. Patients should seek immediate medical attention and bring the medication container to the emergency department.

Storage

Store Arava tablets at room temperature (15-30°C or 59-86°F) in the original container with the lid tightly closed. Protect from light and moisture. Keep out of reach of children and pets. Do not store in bathroom cabinets where humidity levels fluctuate. Discard any medication that appears discolored or shows signs of degradation. Unused medication should be properly disposed through medication take-back programs rather than flushing or household trash.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for specific dosage recommendations and monitoring requirements. Patients should not alter their treatment regimen without medical supervision. Full prescribing information including boxed warnings should be reviewed before initiation of therapy.

Reviews

Clinical studies demonstrate that approximately 60-65% of patients achieve ACR20 response within 6 months of Arava treatment. Long-term extension studies show sustained efficacy over 2-5 years with maintained radiographic progression inhibition. Patient-reported outcomes indicate significant improvements in pain scores and physical function. Rheumatologists generally report favorable experiences with Arava, particularly noting its predictable response pattern and manageable safety profile with appropriate monitoring. Real-world evidence supports its position as a valuable option in the rheumatoid arthritis treatment algorithm.