Arava: Targeted DMARD Therapy for Rheumatoid Arthritis Relief
Arava
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| Product dosage: 20mg | |||
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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. As a selective immunosuppressant, it works by inhibiting pyrimidine synthesis in rapidly dividing cells, notably activated lymphocytes, which play a central role in the inflammatory cascade and joint destruction characteristic of rheumatoid arthritis. This mechanism offers a targeted approach to reducing disease activity, slowing radiographic progression, and improving physical function. Arava provides a well-established oral treatment option, often used as monotherapy or in combination with other DMARDs, for managing moderate to severe disease where conventional therapies have proven insufficient.
Features
- Active pharmaceutical ingredient: Leflunomide
- Available in 10 mg and 20 mg oral tablets
- Selective inhibition of dihydroorotate dehydrogenase (DHODH)
- Long half-life active metabolite (teriflunomide) allowing once-daily dosing
- Demonstrated efficacy in reducing signs and symptoms of active rheumatoid arthritis
- Shown to retard structural damage as evidenced by X-ray erosion
- Improves physical function in rheumatoid arthritis patients
Benefits
- Reduces joint pain, swelling, and morning stiffness associated with active rheumatoid arthritis
- Slows the progression of joint damage and helps preserve physical function
- Offers convenient once-daily oral administration compared to some injectable alternatives
- Provides sustained therapeutic effect due to long half-life of active metabolite
- Can be used as monotherapy or in combination with other DMARDs like methotrexate
- May reduce dependency on corticosteroids and NSAIDs for symptom management
Common use
Arava is primarily prescribed for the management of active rheumatoid arthritis in adults. It is indicated to reduce signs and symptoms, inhibit structural damage as evidenced by X-ray erosion, and improve physical function. Clinical studies have demonstrated its efficacy both as monotherapy and in combination with methotrexate in patients who have had an inadequate response to methotrexate alone. The medication is typically initiated in patients with moderate to severe disease activity where conventional DMARDs have provided insufficient control. Treatment decisions should consider the progressive nature of rheumatoid arthritis and the need for early intervention to prevent irreversible joint damage.
Dosage and direction
The recommended dosing regimen for Arava involves an initial loading dose followed by maintenance therapy. For most patients, treatment begins with a 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. The loading dose is designed to rapidly achieve steady-state concentrations of the active metabolite, though it may be omitted in patients at increased risk of hematologic or hepatic toxicity. Administration should occur at approximately the same time each day, with or without food. Tablets should be swallowed whole with water and not crushed or chewed.
Dosage adjustments may be necessary based on individual patient response and tolerability. In cases of clinically significant toxicity, dose reduction or temporary discontinuation may be required. For patients undergoing the accelerated drug elimination procedure using cholestyramine or activated charcoal, specific dosing guidelines apply. Treatment duration should be individualized based on therapeutic response and tolerability, with regular monitoring of clinical parameters and laboratory values throughout therapy.
Precautions
Patients treated with Arava require careful monitoring due to its immunosuppressive properties and potential for serious adverse reactions. Regular monitoring of ALT (SGPT) levels must be performed at least monthly for the first six months after starting treatment and every 6-8 weeks thereafter. Complete blood counts should be monitored periodically, as leukopenia, thrombocytopenia, and pancytopenia have been reported. Blood pressure should be monitored before starting treatment and periodically thereafter, as hypertension may occur during therapy.
Patients should be advised to use effective contraception during treatment and for specified periods after discontinuation due to the teratogenic potential of leflunomide. Both men and women of reproductive potential must understand the risks of fetal harm and the requirements for accelerated elimination procedures if pregnancy is planned. Vaccination with live vaccines is not recommended during Arava treatment. Patients should be monitored for signs of infection, as serious infections including sepsis and opportunistic infections may occur. Skin reactions ranging from mild to severe, including toxic epidermal necrolysis and Stevens-Johnson syndrome, have been reported and require immediate medical attention.
Contraindications
Arava is contraindicated in patients with known hypersensitivity to leflunomide, teriflunomide, or any component of the formulation. It must not be used in pregnant women or women of childbearing potential who are not using reliable contraception, due to the high risk of major birth defects. The medication is contraindicated in patients with severe immunodeficiency, bone marrow dysplasia, or severe uncontrolled infections. Patients with severe hepatic impairment should not receive Arava, and caution is required in those with pre-existing liver disease or elevated liver enzymes. Concomitant use with other hepatotoxic drugs requires careful risk-benefit assessment. The medication is not recommended for patients with severe hypoproteinemia or pre-existing blood dyscrasias.
Possible side effects
The most common adverse reactions observed with Arava treatment include diarrhea (17%), elevated liver enzymes (ALT increase) (5-13%), alopecia (10%), rash (10%), and hypertension (10%). Other frequently reported side effects include nausea, abdominal pain, headache, dizziness, respiratory infections, bronchitis, and weight loss. Less common but more serious adverse reactions include severe liver injury, bone marrow suppression, serious skin reactions, peripheral neuropathy, and interstitial lung disease.
Hematologic effects may include leukopenia, thrombocytopenia, and pancytopenia, which can be severe. Hepatic effects range from transient transaminase elevations to rare cases of liver failure. Pulmonary effects may include interstitial lung disease, which can be fatal. Neurological effects include peripheral neuropathy, which may be irreversible. Infections, including serious and opportunistic infections, may occur due to the immunosuppressive effects of the medication. Regular monitoring is essential to detect these potential adverse effects early.
Drug interaction
Arava demonstrates several clinically significant drug interactions that require careful management. Concomitant use with other hepatotoxic drugs (including methotrexate) increases the risk of liver injury and requires close monitoring of liver enzymes. The active metabolite, teriflunomide, is a weak inhibitor of CYP2C8 and may increase exposure to drugs metabolized by this enzyme, such as repaglinide and paclitaxel. It may also increase exposure to drugs transported by OATP1B1 transporters.
Concomitant administration with warfarin requires close monitoring of INR, as cases of increased prothrombin time have been reported. Live vaccines should not be administered during Arava treatment due to the risk of vaccine-associated infections. Drugs that induce CYP2C9 metabolism may decrease teriflunomide concentrations. Cholestyramine and activated charcoal significantly increase the elimination of teriflunomide and are used in the accelerated elimination procedure. Concomitant use with other immunosuppressive agents may increase the risk of serious infections.
Missed dose
If a dose of Arava is missed, patients should take it as soon as they remember, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed dose. The long half-life of teriflunomide (approximately 2 weeks) means that occasional missed doses are unlikely to significantly affect therapeutic efficacy. However, consistent daily administration is recommended to maintain stable drug levels. Patients should be advised to contact their healthcare provider if multiple doses are missed or if they have questions about their dosing schedule.
Overdose
In case of suspected overdose, symptoms may include adverse reactions of greater severity or frequency. There is no specific antidote for leflunomide overdose. Management should include supportive measures and symptomatic treatment. Accelerated elimination procedures using cholestyramine or activated charcoal should be initiated promptly. Cholestyramine administration (8 g orally three times daily for 11 days) or activated charcoal (50 g every 12 hours for 11 days) can significantly reduce plasma concentrations of teriflunomide. Monitoring of hematological parameters and liver function is essential. In severe cases, particularly with hematological toxicity, administration of colony-stimulating factors may be considered. Hemodialysis has limited effectiveness in removing teriflunomide due to high protein binding.
Storage
Arava tablets should be stored at controlled room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). The medication should be kept in its original container with the lid tightly closed to protect from moisture and light. Tablets should not be stored in bathroom cabinets or other areas subject to high humidity. Keep out of reach of children and pets. Do not use tablets beyond the expiration date printed on the packaging. Proper disposal of unused medication is important to prevent accidental ingestion or environmental contamination.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Arava is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Treatment decisions must be made by a physician based on individual patient assessment, including consideration of the benefit-risk profile. Patients should not initiate or discontinue treatment without medical supervision. The complete prescribing information should be consulted before initiating therapy. Healthcare professionals should report any adverse events to the appropriate regulatory authorities.
Reviews
Clinical studies and post-marketing experience have demonstrated Arava’s efficacy in managing rheumatoid arthritis. In randomized controlled trials, Arava showed significant improvement in ACR response criteria compared to placebo, with ACR20 responses of 50-60% versus 26-29% for placebo at 6 months. Radiographic progression was significantly reduced compared to placebo. Many rheumatologists consider Arava an effective option for patients who have failed or cannot tolerate methotrexate. Patient-reported outcomes often indicate improvements in pain, morning stiffness, and physical function. However, the need for regular monitoring and potential side effects are frequently noted considerations in treatment decisions. Long-term extension studies have shown sustained efficacy over several years of treatment in responsive patients.