Arava: Advanced Therapy for Rheumatoid Arthritis Management
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Synonyms | |||
Arava (leflunomide) is a disease-modifying antirheumatic drug (DMARD) specifically engineered to target the underlying mechanisms of rheumatoid arthritis. By selectively inhibiting pyrimidine synthesis in activated lymphocytes, it effectively reduces inflammation, slows joint damage progression, and improves physical function. This oral medication offers a convenient and potent option for adults with moderate to severe active rheumatoid arthritis, providing long-term control where traditional therapies may fall short. Clinical studies demonstrate its efficacy in preserving joint integrity and enhancing quality of life, making it a cornerstone in modern rheumatologic care.
Features
- Active ingredient: Leflunomide 10 mg or 20 mg tablets
- Mechanism: Inhibits dihydroorotate dehydrogenase, reducing autoimmune lymphocyte proliferation
- Administration: Oral, once-daily dosing
- Bioavailability: >80% with high plasma protein binding
- Half-life: Approximately 2 weeks, allowing consistent therapeutic levels
- Metabolism: Hepatic, via CYP450 and non-enzymatic processes
- Excretion: Renal and fecal
Benefits
- Reduces pain, swelling, and tenderness in affected joints
- Slows radiographic progression of joint erosion and cartilage damage
- Improves physical function and mobility in daily activities
- Offers convenient once-daily dosing to support adherence
- Provides an alternative for patients intolerant to methotrexate
- Demonstrates long-term efficacy in maintaining remission
Common use
Arava is indicated for the treatment of adults with active rheumatoid arthritis. It is often prescribed when patients have had an inadequate response to one or more DMARDs, or as a first-line therapy in certain clinical scenarios. It may be used as monotherapy or in combination with other antirheumatic agents, under careful supervision, to achieve optimal disease control.
Dosage and direction
The recommended dosing regimen for Arava 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 may not tolerate the higher dose, a maintenance dose of 10 mg daily can be considered. Tablets should be taken with water, with or without food, at approximately the same time each day. Dosage adjustments may be necessary in patients with hepatic impairment or those taking concomitant medications that interact with leflunomide.
Precautions
Patients should undergo baseline liver function tests (LFTs) and complete blood count before initiation and monitored regularly thereafter. Blood pressure should be monitored due to risk of hypertension. Use with caution in patients with renal impairment, pre-existing liver disease, or immunodeficiency. Vaccination with live vaccines is not recommended during treatment. Women of childbearing potential must use reliable contraception due to teratogenic risk.
Contraindications
Arava is contraindicated in patients with severe hepatic impairment, severe immunodeficiency, or known hypersensitivity to leflunomide or any excipients. It must not be used during pregnancy or in women not using contraception. Concomitant use with teriflunomide or other hepatotoxic drugs is contraindicated.
Possible side effects
Common adverse reactions include diarrhea, nausea, abdominal pain, headache, dizziness, alopecia, rash, and elevated liver enzymes. Less frequently, hypertension, weight loss, respiratory infections, and hematologic abnormalities may occur. Rare but serious side effects include severe liver injury, Stevens-Johnson syndrome, and peripheral neuropathy.
Drug interaction
Leflunomide may interact with warfarin, increasing INR monitoring requirements. Concomitant use with rifampin can elevate leflunomide levels. Cholestyramine and activated charcoal accelerate elimination. Use with other hepatotoxic drugs (e.g., methotrexate, NSAIDs) may increase liver injury risk. Live vaccines should be avoided.
Missed dose
If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose to make up for a missed one. Maintain the regular dosing schedule to ensure consistent therapeutic levels.
Overdose
In case of suspected overdose, discontinue Arava immediately and initiate an accelerated elimination procedure using cholestyramine or activated charcoal. Symptoms may include elevated LFTs, diarrhea, or hematologic changes. Supportive care and monitoring of vital signs and organ function are essential. There is no specific antidote.
Storage
Store Arava tablets at room temperature (15–30°C), in the original container, protected from light and moisture. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging.
Disclaimer
This information is for educational purposes and does not replace professional medical advice. Always consult a healthcare provider for diagnosis, treatment decisions, and personalized guidance. Individual responses to Arava may vary, and only a qualified practitioner can determine its appropriateness based on clinical context and patient history.
Reviews
Clinical trials and post-marketing studies consistently report significant improvement in ACR20/50/70 scores and retardation of joint damage with Arava. Many patients experience enhanced quality of life and functional capacity, though individual tolerance varies. Long-term data support its role as an effective DMARD with a manageable safety profile under appropriate monitoring.