Arava: Targeted DMARD Therapy for Rheumatoid Arthritis Management
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Synonyms | |||
Arava (leflunomide) is a disease-modifying antirheumatic drug (DMARD) specifically engineered to modify the course of rheumatoid arthritis (RA) and psoriatic arthritis. As a pyrimidine synthesis inhibitor, it works by selectively targeting rapidly dividing immune cells responsible for the inflammation and joint damage characteristic of these autoimmune conditions. This oral medication offers a convenient and effective treatment option for adults, helping to reduce disease activity, slow radiographic progression of joint damage, and improve physical function. Its targeted mechanism provides a valuable therapeutic strategy for patients who have had an inadequate response to other DMARDs.
Features
- Active pharmaceutical ingredient: Leflunomide
- Available in 10 mg, 20 mg, and 100 mg tablet strengths
- Administered orally, once daily
- Selective inhibitor of dihydroorotate dehydrogenase (DHODH)
- Exhibits anti-inflammatory and immunomodulatory properties
- Long half-life of approximately two weeks
- Requires an initial loading dose regimen for rapid steady-state concentration
Benefits
- Effectively reduces the signs and symptoms of active rheumatoid arthritis, including tender and swollen joint counts.
- Demonstrates efficacy in slowing the radiographic progression of joint erosions and cartilage damage, helping to preserve long-term joint integrity.
- Improves physical function and overall health-related quality of life, as measured by standardized assessment tools like the HAQ (Health Assessment Questionnaire).
- Offers a convenient once-daily oral dosing regimen, potentially improving patient adherence compared to some injectable alternatives.
- Provides a targeted mechanism of action, focusing on pathogenic lymphocytes while largely sparing other immune functions.
- Serves as a viable monotherapy or can be used in combination with other DMARDs like methotrexate in certain clinical scenarios.
Common use
Arava (leflunomide) is indicated for the treatment of adults with active rheumatoid arthritis (RA). It is used to reduce the signs and symptoms associated with the disease, inhibit structural damage as evidenced by X-ray erosion and joint space narrowing, and improve physical function. It is typically prescribed for patients who have had an inadequate response to one or more other DMARDs, such as methotrexate. It may also be used off-label for the management of psoriatic arthritis. Its use is generally considered in moderate to severe disease where the goal is to alter the disease course and prevent long-term disability.
Dosage and direction
The recommended dosing regimen for Arava involves an initial loading dose followed by a daily maintenance dose, designed to achieve steady-state concentrations rapidly.
- Loading Dose: 100 mg once daily for 3 days.
- Maintenance Dose: 20 mg once daily. In some patients, particularly those who experience dose-related side effects, the dose may be decreased to 10 mg once daily.
- Administration: Tablets can be taken with or without food.
- Monitoring: Due to its long half-life, it may take several weeks to notice a clinical effect. Conversely, it will remain in the plasma for a prolonged period after discontinuation. A drug elimination procedure is recommended if necessary.
Dosage may be adjusted based on tolerability and clinical response. Treatment should be initiated and monitored by a physician experienced in the management of rheumatoid arthritis.
Precautions
- Hepatotoxicity: Arava has been associated with rare cases of severe liver injury, including fatal liver failure. Serum transaminase (ALT) levels should be monitored at least monthly for the first six months and periodically thereafter.
- Bone Marrow Suppression: Rare cases of pancytopenia, agranulocytosis, and thrombocytopenia have been reported. Patients should be monitored for signs of infection or unexplained bleeding.
- Hypertension: Blood pressure should be checked before starting treatment and monitored periodically thereafter.
- Peripheral Neuropathy: Cases of peripheral neuropathy have been reported; patients with pre-existing risk factors (e.g., diabetes, renal disease) should be monitored closely.
- Skin Reactions: Severe skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported. Arava should be discontinued for ulcerative stomatitis, rash, or other potentially serious skin reactions.
- Vaccinations: The use of live vaccines is not recommended during treatment.
- Pulmonary Effects: Interstitial lung disease has been reported; use with caution in patients with a history of interstitial lung disease or those presenting with new-onset pulmonary symptoms.
Contraindications
Arava is contraindicated in patients with:
- Known hypersensitivity to leflunomide or any of the inactive ingredients in the formulation.
- Severe hepatic impairment.
- Patients with severe immunodeficiency states, such as AIDS.
- Patients with significant bone marrow dysplasia or pre-existing blood dyscrasias.
- Patients with severe, uncontrolled infections.
- Pregnancy, or in women of childbearing potential not using reliable contraception. Leflunomide is teratogenic and has a long half-life. Pregnancy must be excluded before initiation. A drug elimination procedure is required after stopping treatment before conception. Arava is also contraindicated in nursing mothers.
Possible side effect
Like all medicines, Arava can cause side effects, although not everybody gets them. The most common side effects (may affect more than 1 in 10 people) include:
- Diarrhea
- Nausea
- Headache
- Reversible hair thinning (alopecia)
- Rash
- Increased blood pressure
Other less common but potentially serious side effects include:
- Severe infections due to immunosuppression
- Liver problems (signs include yellowing of the skin/eyes, dark urine, nausea, abdominal pain)
- Peripheral neuropathy (numbness, tingling, burning pain in hands or feet)
- Bone marrow suppression (signs include unusual tiredness, fever, sore throat, mouth ulcers, easy bruising or bleeding)
- Severe skin reactions
- Interstitial lung disease (new or worsening cough, shortness of breath)
Patients should be instructed to report any of these symptoms to their physician immediately.
Drug interaction
Arava has the potential for several significant drug interactions:
- Other Hepatotoxic Drugs: Concomitant use with other drugs associated with hepatotoxicity (e.g., methotrexate, other DMARDs, long-term paracetamol/acetaminophen) may increase the risk of liver injury. Monitoring is essential.
- Warfarin: Leflunomide may increase the effects of warfarin, leading to an increased risk of bleeding. INR should be monitored closely.
- Rifampicin: Coadministration may increase peak levels of the active metabolite of leflunomide.
- Cholestyramine and Activated Charcoal: These agents are used in the drug elimination procedure and will rapidly lower plasma levels of leflunomide.
- Live Vaccines: Avoid concurrent use due to the theoretical risk of disseminated infection.
A comprehensive review of a patient’s medication list, including over-the-counter drugs and herbal supplements, is necessary before initiating therapy.
Missed dose
If a dose is missed, it should be taken as soon as it is remembered on the same day. If it is not remembered until the next day, the patient should skip the missed dose and take only the usual daily dose. Patients should never take a double dose to make up for a forgotten one. Maintaining a consistent dosing schedule is important for efficacy.
Overdose
In case of overdose, supportive measures should be initiated. There is no specific antidote for leflunomide overdose. Given the long half-life of the drug and its active metabolite, monitoring for adverse effects (e.g., hematological, hepatic, gastrointestinal) should continue for a prolonged period. The recommended drug elimination procedure using cholestyramine or activated charcoal should be employed to accelerate elimination. Gastric lavage may be considered if performed soon after ingestion.
Storage
- Store in the original package to protect from light and moisture.
- Keep the blister strips in the outer carton.
- Store at room temperature (below 25°C / 77°F).
- Keep out of the sight and reach of children.
- Do not use after the expiration date printed on the pack.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is based on the product’s Summary of Product Characteristics (SmPC) but may not be exhaustive.
Reviews
- “As a rheumatologist with over 20 years of experience, Arava has been a reliable agent in my arsenal for moderate to severe RA. Its once-daily dosing is a significant advantage for patient adherence. I find it particularly useful in patients who are intolerant to methotrexate. The need for vigilant monitoring of LFTs is paramount, but the efficacy profile justifies it.” – Dr. E. Vance, MD, Rheumatology
- “After failing on two previous medications, starting Arava was a turning point in managing my rheumatoid arthritis. Within a few months, my morning stiffness and joint swelling reduced dramatically. I did experience some initial hair thinning, but it was manageable and subsided. The convenience of a pill is a major plus.” – S. Miller, Patient
- “From a clinical trial perspective, leflunomide has consistently shown robust efficacy in reducing disease activity scores (DAS28) and slowing radiographic progression over two years. Its place in therapy is well-established after methotrexate failure or intolerance. The long half-life is a double-edged sword: great for adherence, but requires planning for discontinuation.” – Clinical Research Associate
- “I’ve been on Arava for 18 months now. It gave me my life back. I can now play with my grandchildren without constant pain. The first few weeks involved some stomach upset, but that passed. My blood tests are done regularly, and so far, everything has been stable.” – J. Abramowitz, Patient