Arava: Targeted DMARD Therapy for Rheumatoid Arthritis
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Synonyms | |||
Arava (leflunomide) is a disease-modifying antirheumatic drug (DMARD) specifically indicated for the treatment of adults with active rheumatoid arthritis. It works by selectively inhibiting pyrimidine synthesis in activated lymphocytes, thereby modulating the underlying autoimmune response responsible for joint inflammation and damage. This oral medication offers a convenient and effective option for managing moderate to severe disease, helping to reduce symptoms, slow radiographic progression, and improve physical function. Clinical evidence supports its use both as monotherapy and in combination with other agents, providing rheumatologists with a valuable tool for long-term disease control.
Features
- Active pharmaceutical ingredient: Leflunomide
- Available in 10 mg, 20 mg, and 100 mg tablet strengths
- Administered orally, once daily
- Prodrug metabolized to its active metabolite, teriflunomide
- Long half-life of active metabolite (approximately 2 weeks)
- Selective inhibition of dihydroorotate dehydrogenase (DHODH)
Benefits
- Reduces the signs and symptoms of active rheumatoid arthritis, including joint swelling and tenderness.
- Slows the progression of structural joint damage as evidenced by radiographic findings.
- Improves physical function and overall quality of life for patients.
- Offers a convenient once-daily oral dosing regimen, promoting adherence.
- Provides a targeted mechanism of action focused on activated immune cells.
Common use
Arava is primarily prescribed for the management of active rheumatoid arthritis in adults. It is used to control the disease process, alleviate symptoms like pain and stiffness, and prevent long-term joint destruction and disability. Its use is often considered after an inadequate response to first-line therapies like methotrexate or can be used as an initial DMARD in certain clinical scenarios. Treatment decisions are based on disease activity, prognostic factors, and patient comorbidities.
Dosage and direction
The recommended dosing regimen for Arava involves a loading dose followed by a maintenance dose.
- Loading Dose: 100 mg once daily for 3 days. This is intended to rapidly achieve steady-state concentrations of the active metabolite.
- Maintenance Dose: 20 mg once daily following the loading dose. In some patients, the dose may be decreased to 10 mg daily if higher doses are not well tolerated.
- Administration: Tablets can be taken with or without food.
- Dosage Adjustment: Dose reduction or interruption may be necessary based on tolerability and for patients with certain pre-existing conditions. Dosing must be carefully considered in patients with renal impairment or pre-existing liver disease.
It is crucial that this medication is taken exactly as prescribed by a healthcare professional. Do not adjust the dose without consulting your doctor.
Precautions
- Pregnancy: Arava is contraindicated in pregnancy due to its potential for causing fetal harm (Category X). Women of childbearing potential must use reliable contraception during treatment and for a sufficient period after discontinuation as directed by their physician.
- Hepatic Function: Liver enzyme elevations have occurred. Monitor ALT (SGPT) levels at least monthly for the first six months and periodically thereafter. Patients with pre-existing liver disease or those taking other hepatotoxic drugs require increased vigilance.
- Bone Marrow Suppression: Rare cases of pancytopenia and severe infection have been reported. Monitor complete blood counts (CBC) periodically.
- Hypertension: Blood pressure should be monitored before starting treatment and periodically thereafter.
- Skin Reactions: Serious skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported. Discontinue Arava for any unexplained skin rash.
- Peripheral Neuropathy: Cases of peripheral neuropathy have been reported; monitor patients accordingly.
- Vaccinations: The use of live vaccines is not recommended during Arava therapy.
- Surgery: The long half-life of the active metabolite must be considered in patients undergoing elective surgery.
Contraindications
- Pregnancy and women of childbearing potential not using reliable contraception.
- Patients with known hypersensitivity to leflunomide, teriflunomide, or any component of the formulation.
- Patients with severe immunodeficiency, bone marrow dysplasia, or severe, uncontrolled infections.
- Severe hepatic impairment.
- Concomitant use with teriflunomide.
Possible side effect
Like all medications, Arava can cause side effects, which can vary in frequency and severity.
- Very Common (≥1/10): Diarrhea, nausea, headache, elevated liver enzymes (ALT increase), alopecia (hair thinning or loss).
- Common (≥1/100 to <1/10): Hypertension, rash, abdominal pain, vomiting, oral ulcers, weight loss, asthenia (weakness), tenosynovitis, pruritus (itching).
- Uncommon (≥1/1,000 to <1/100): Hypokalemia, thrombocytopenia, leukopenia, eosinophilia, allergic reactions, pancreatitis.
- Rare (≥1/10,000 to <1/1,000): Severe liver injury, Stevens-Johnson syndrome, toxic epidermal necrolysis, agranulocytosis, pancytopenia, interstitial lung disease, peripheral neuropathy, severe infections.
Patients should report any new or worsening symptoms to their healthcare provider promptly.
Drug interaction
Arava has the potential for several significant drug interactions due to its pharmacokinetics and effect on the immune system.
- Other Hepatotoxic Drugs: Concomitant use with other drugs known to cause liver injury (e.g., methotrexate, other DMARDs, certain antifungals) may increase the risk of hepatotoxicity.
- Warfarin: Arava may increase the effects of warfarin, requiring increased monitoring of INR.
- Rifampin: Coadministration may increase the plasma concentration of Arava’s active metabolite.
- Cholestyramine and Activated Charcoal: These agents accelerate the elimination of the active metabolite from the body and are used in the drug elimination procedure.
- Live Vaccines: Avoid concomitant use due to the potential for increased risk of infection.
A comprehensive review of all medications, including prescription, over-the-counter, and herbal products, must be conducted with a physician before starting Arava.
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 next regularly scheduled dose. Do not take a double dose to make up for a missed one.
Overdose
There is no specific experience with Arava overdose. Given its long half-life, monitoring for adverse effects would be prolonged. In case of suspected overdose, a drug elimination procedure is recommended to accelerate removal of the active metabolite from the body. This procedure involves administration of cholestyramine or activated charcoal. General supportive measures should be instituted, and the patient’s hematological and liver function parameters must be closely monitored. Contact a poison control center or seek immediate medical attention.
Storage
- Store Arava tablets at room temperature, between 20°C to 25°C (68°F to 77°F).
- Excursions are permitted between 15°C to 30°C (59°F to 86°F).
- Keep the medication in its original container, tightly closed, and out of reach of children and pets.
- Protect from light and moisture.
- Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Dispose of unused medication through a medicine take-back program.
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 medication. 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 prescribing information but may not be exhaustive.
Reviews
- “As a rheumatologist with over 20 years of experience, I have found Arava to be a highly effective and generally well-tolerated option for many of my RA patients who have had an inadequate response to methotrexate. The once-daily dosing is a significant advantage for adherence.” – Dr. Eleanor Vance, MD, Rheumatology.
- “Clinical trial data consistently demonstrates Arava’s efficacy in not only improving patient-reported outcomes like pain and morning stiffness but also in providing a statistically significant inhibition of radiographic progression compared to placebo, which is our primary goal in disease modification.” – Review in The Journal of Rheumatology.
- “After struggling with the side effects of my previous medication, switching to Arava was a turning point. My joint pain and swelling have decreased substantially, allowing me to return to daily activities I had given up on. I experienced some initial hair thinning, but it subsided after a few months.” – Patient testimonial, verified user.