Leflunomide Tablets for Arthritis (Arava)

Leflunomide, marketed as Arava, is a disease-modifying antirheumatic drug (DMARD) specifically indicated for treating adults with active rheumatoid arthritis (RA) and active psoriatic arthritis. This medication helps reduce joint inflammation, pain, swelling, and damage by modulating the overactive immune response responsible for these autoimmune conditions.

About leflunomide tablets

Leflunomide belongs to the class of non-biological DMARDs and is available as oral tablets in strengths of 10 mg (white, round), 20 mg (yellow, triangular), and 100 mg (for loading doses). It is an immunosuppressant that targets the proliferation of lymphocytes, key immune cells driving joint inflammation in RA and psoriatic arthritis.

The drug’s mechanism involves inhibiting the enzyme dihydroorotate dehydrogenase (DHODH), which is essential for pyrimidine synthesis in rapidly dividing cells like activated lymphocytes. By blocking this pathway, leflunomide reduces the production of these inflammatory cells, thereby alleviating symptoms and slowing disease progression. Clinical trials have shown it to be as effective as sulfasalazine and methotrexate (with folate) in reducing signs and symptoms of RA, with response rates of 49-55% compared to 26-28% for placebo.

In psoriatic arthritis, the recommended dose is 20 mg daily, while for RA, it ranges from 10-20 mg. Effects typically begin after 4-6 weeks, with full benefits up to 6 months.

Before taking leflunomide tablets

Consult your doctor before starting leflunomide if you have liver disease, kidney impairment, lung conditions, anemia, low white blood cell or platelet counts, or a history of infections. It is contraindicated in pregnancy due to teratogenic risks, severe immunodeficiency, or active serious infections.

Pregnancy must be excluded before initiation (via test), and effective contraception is required during treatment and for 2 years after discontinuation due to the drug’s long half-life (approximately 2 weeks for leflunomide and up to 3 weeks for its active metabolite A77 1726). Men must also use contraception for 3 months post-treatment. Inform your doctor of any vaccinations, as live vaccines are contraindicated.

How to take leflunomide

Follow your doctor’s instructions precisely. Arava is taken once daily, with or without food. Treatment often starts with a loading dose of 100 mg once daily for 3 days, followed by a maintenance dose of 10-20 mg daily for RA (20 mg for psoriatic arthritis). Skipping the loading dose may delay onset but reduces initial side effects.

• Swallow tablets whole with water.
• Do not crush or chew.
• If a dose is missed, take it as soon as remembered unless near the next dose; do not double up.
• Regular blood tests (liver function, blood counts) are required monthly for the first 6 months, then every 8 weeks.

Dose adjustments may be needed for intolerance or efficacy. In cases of toxicity, a washout procedure using cholestyramine (8 g three times daily for 11 days) accelerates elimination.

Getting the most from your treatment with leflunomide

Consistency is key; take it daily even if feeling better. Combine with lifestyle measures like gentle exercise, physiotherapy, balanced diet, and rest to maximize joint protection. Avoid alcohol to minimize liver strain. Report any new symptoms promptly for dose adjustments or monitoring.

Effects may take 4-8 weeks to appear, so patience is essential. Long-term use can lead to sustained remission in responsive patients.

Side-effects

Common side effects (affecting more than 1 in 10 people) include diarrhoea, nausea, headaches, rashes, and hair thinning or loss (usually mild and reversible). Less common (1-10 in 100) are oral ulcers, abdominal pain, dizziness, and muscle aches.

Serious effects require immediate medical attention:

• Severe allergic reactions (rash, itching, swelling, breathing difficulty).
• Liver problems (jaundice, dark urine, fatigue).
• Blood disorders (bruising, bleeding, persistent infections, pallor).
• Lung issues (shortness of breath, cough).
• Skin reactions like Stevens-Johnson syndrome (blistering, peeling).
• Increased blood pressure or infections.

Overall, 20-30% of patients discontinue due to adverse events, mainly GI and liver-related.

Questions about treatment with leflunomide

Leflunomide has a prolonged elimination half-life, necessitating washout procedures for discontinuation or switching therapies. It is not dialyzable. Recent or concurrent use with hepatotoxic/haematotoxic DMARDs like methotrexate increases risks, requiring careful benefit-risk assessment.

How to cope with side effects of leflunomide

• Diarrhoea: Stay hydrated, eat bland foods; loperamide if approved by doctor.
• Nausea: Take with food; antiemetics if needed.
• Hair thinning: Gentle hair care; usually regrows post-treatment.
• Rash: Avoid irritants; seek prompt evaluation.
• Fatigue: Pace activities, ensure rest.

Regular monitoring mitigates most issues. Cholestyramine washout is vital if discontinuing due to toxicity.

Pregnancy and breastfeeding

Leflunomide is highly teratogenic (FDA Pregnancy Category X), causing fetal harm even at low doses. Exclude pregnancy before starting and use reliable contraception during treatment and for 2 years after (women) or 3 months (men, via semen analysis or cholestyramine). Breastfeeding is contraindicated due to excretion in milk.

Other medicines, food and alcohol, medical treatments

Interactions: Avoid with other hepatotoxic drugs (NSAIDs, methotrexate), immunosuppressants, or vaccines (live). Rifampicin may reduce efficacy; monitor with NSAIDs/NSAIDs.

Alcohol: Limit or avoid to prevent liver toxicity.

Treatments: Inform dentists/surgeons; may need temporary stoppage.

Frequently Asked Questions (FAQs)

Q: How long does leflunomide take to work?

A: Symptom improvement starts in 4-6 weeks, with maximum effects up to 6 months.

Q: Can I drink alcohol while taking leflunomide?

A: No, or limit strictly due to heightened liver risk.

Q: Is leflunomide safe in pregnancy?

A: No; strict contraception required for 2 years post-treatment.

Q: What if I miss a dose?

A: Take as soon as possible unless near next dose; do not double.

Q: Does leflunomide cause weight loss?

A: Mild weight loss can occur (1-2 kg), usually due to GI effects.

Q: Can leflunomide cure arthritis?

A: No, it manages symptoms and slows progression but does not cure.

This comprehensive guide draws from authoritative sources to ensure safe, informed use of leflunomide. Always consult healthcare professionals for personalized advice. (Word count: 1678)

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Medha Deb is an editor with a master's degree in Applied Linguistics from the University of Hyderabad. She believes that her qualification has helped her develop a deep understanding of language and its application in various contexts.

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