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Arava

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Arava (leflunomide) is a disease-modifying antirheumatic drug (DMARD) used to treat rheumatoid arthritis. It helps reduce joint damage, pain, and swelling, thereby improving physical function. Arava works by slowing down the overactive immune cells that contribute to inflammation within the joints and connective tissues.


Ingredient
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Leflunomide
Reference Brand
Arava
Manufacturer
Sanofi
Product Form
Film-coated Tablet
Regulatory Classification
Rx
Primary Category
Immunosuppressant
Product Category
Antineoplastic and immunomodulating agents, Immunosuppressants, Selective immunosuppressants
Pharmacological Class
Pyrimidine synthesis inhibitors
Manufacturer Description
Used to treat symptoms of arthritis and reduce joint damage.
Mechanism of Action
Leflunomide is a Disease-Modifying Anti-Rheumatic Drug (DMARD). it works by reducing the activity of the immune system, specifically by blocking an enzyme needed for the production of rapidly dividing cells like inflammatory immune cells.
Route of Administration
Oral
Onset Time
4-6 weeks (to see benefit)
Duration
Weeks (long half-life)
Contraindications
Pregnancy, Severe liver impairment, Severe immunodeficiency, Serious infections
Severe Adverse Events
Severe liver damage, Interstitial lung disease, Bone marrow suppression, Severe skin reactions
Common Side Effects
Nausea
Uncommon Side Effects
Diarrhoea, Rash, Weight loss, Increased blood pressure
Drug Interactions
Methotrexate, Warfarin, Rifampicin, Cholestyramine
Pregnancy Safety Warnings
Contraindicated; must use reliable contraception during and after treatment.
Age Restrictions
Not recommended for children under 18.
Storage Guidelines
Keep the bottle tightly closed at room temperature.
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Arava FAQ

Can I travel internationally with Arava tablets?

Yes, you may travel with Arava, but keep the medication in its original packaging with the prescription label visible. Carry a copy of your prescription and a letter from your doctor if you are traveling to countries with strict medication import rules.

How does Arava differ from methotrexate?

Both are DMARDs, but leflunomide primarily inhibits pyrimidine synthesis, whereas methotrexate blocks folate metabolism. Their side-effect profiles and monitoring requirements also differ; for example, leflunomide has a higher risk of liver enzyme elevation, while methotrexate is more associated with mucosal ulceration.

What should I do if I miss a dose while on a loading regimen?

If you miss a loading dose (100 mg), take the missed tablet as soon as you remember on the same day and resume the remaining loading doses as scheduled. Do not double-dose the following day.

Are there any visual changes to the Arava tablets that indicate spoilage?

The tablets should be white to off-white, smooth, and without cracks. Discoloration, powdery surfaces, or broken pieces suggest degradation; discard such tablets and obtain a new supply.

Can I take Arava if I have mild hypertension?

Arava can raise blood pressure in some patients. If you have controlled mild hypertension, your doctor may still prescribe it but will monitor your blood pressure more frequently and may adjust antihypertensive therapy.

Is it safe to combine Arava with over-the-counter pain relievers?

Non-steroidal anti-inflammatory drugs (NSAIDs) are often used for symptom relief in rheumatoid arthritis. They can increase the risk of gastrointestinal irritation when taken with leflunomide, so discuss dosage and gastro-protection strategies with your clinician.

What is the purpose of the cholestyramine washout, and how long does it take?

Cholestyramine binds teriflunomide in the gut, preventing its re-absorption and accelerating elimination. The standard washout course lasts 11 days and reduces plasma teriflunomide levels to <0.02 µg/mL, allowing safer conception.

Does alcohol consumption need to be avoided completely?

Complete avoidance is not mandatory, but excessive alcohol can worsen leflunomide-induced liver toxicity. Moderate consumption (up to one standard drink per day for women, two for men) is generally acceptable, provided liver function is monitored.

Are there generic versions of Arava available in the UK?

Yes, leflunomide is available as a generic medication in 10 mg and 20 mg tablet strengths. Generic products contain the same active ingredient and are subject to the same regulatory standards as the branded version.

What is Arava?

Arava is a brand-name medication that contains the active ingredient leflunomide. It belongs to the class of disease-modifying antirheumatic drugs (DMARDs) used in the management of autoimmune conditions. In the United Kingdom Arava is a prescription-only (Prescription Only Medicine, POM) pill marketed by Hikma Pharmaceuticals and regulated by the Medicines and Healthcare products Regulatory Agency (MHRA).

Arava is available in 10 mg and 20 mg tablet strengths. The tablets are round, film-coated, and intended for oral administration with water.

How Arava Works in the Body

Leflunomide exerts its therapeutic effect by inhibiting the enzyme dihydroorotate dehydrogenase (DHODH). DHODH is essential for the de novo synthesis of pyrimidine nucleotides, which are building blocks of DNA and RNA. By limiting pyrimidine production, leflunomide reduces the proliferation of activated T-lymphocytes and B-lymphocytes-key drivers of autoimmune inflammation.

The drug’s onset of action is typically observed after several weeks, with peak clinical effect emerging around 8-12 weeks of continuous therapy. Leflunomide is well absorbed from the gastrointestinal tract, undergoes extensive first-pass metabolism, and the active metabolite teriflunomide has a long elimination half-life (up to 2 weeks), which contributes to sustained immunomodulation.

Conditions Treated by Arava

Arava is approved by the MHRA for the following indications:

  • Rheumatoid arthritis (RA) in adults when disease-modifying therapy is required.
  • Active psoriatic arthritis (PsA) where joint inflammation is present.

These approvals are based on clinical trials demonstrating reduced joint swelling, improved functional scores, and slowed radiographic progression when leflunomide is added to standard care.

Note: While leflunomide has been investigated for other autoimmune disorders, such uses are not approved in the UK.

Evidence-Based Off-Label Uses

Some peer-reviewed studies have explored leflunomide in conditions such as systemic lupus erythematosus (SLE) and multiple sclerosis (MS). Evidence remains limited, and regulatory agencies have not granted approval for these indications.

Disclaimer: Off-label use of Arava should only occur under the direct supervision of a qualified rheumatologist or specialist, with thorough risk-benefit assessment and appropriate monitoring.

Who Should (and Should Not) Use Arava?

Absolute Contraindications

  • Known hypersensitivity to leflunomide or any tablet excipient.
  • Pregnancy or planned pregnancy (leflunomide is teratogenic).
  • Severe hepatic impairment (Child-Pugh class C).
  • Active serious infections (e.g., tuberculosis, sepsis).

Relative Contraindications

  • Moderate hepatic dysfunction (Child-Pugh A-B).
  • Renal impairment with estimated glomerular filtration rate (eGFR) < 30 mL/min.
  • History of hypersensitivity pneumonitis or interstitial lung disease.
  • Women of child-bearing potential not using reliable contraception.

Special Populations

  • Pregnancy/Lactation: Arava must be stopped at least 2 years before conception; a cholestyramine washout is recommended. It is contraindicated during breastfeeding.
  • Elderly: Dose adjustments may be required based on liver function.
  • Pediatrics: Not approved for use in patients under 18 years of age in the UK.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Diarrhoea or abdominal discomfort.
  • Nausea or loss of appetite.
  • Mild alopecia (hair thinning).
  • Rash, particularly mild maculopapular eruptions.
  • Elevated blood pressure.

These reactions are usually transient and may improve with continued therapy.

Serious Adverse Events

  • Hepatotoxicity: Significant rise in liver enzymes or clinical hepatitis.
  • Bone marrow suppression: Neutropenia, leukopenia, or thrombocytopenia.
  • Pulmonary toxicity: Interstitial lung disease presenting with cough and dyspnoea.
  • Severe infections: Opportunistic infections due to immunosuppression.

Any of the above require immediate medical evaluation and may necessitate drug discontinuation.

Drug Interactions

  • Warfarin: Leflunomide can increase INR; close anticoagulation monitoring is advised.
  • Methotrexate: Combined use may raise liver enzyme levels; dose adjustments and frequent monitoring are recommended.
  • CYP1A2 inducers (e.g., carbamazepine, rifampicin): May reduce leflunomide plasma concentrations, potentially decreasing efficacy.
  • Cholestyramine: Accelerates leflunomide elimination and is used deliberately during washout; concurrent use without intention may lower therapeutic levels.

Food and Lifestyle Interactions

  • Alcohol: Concurrent excessive alcohol intake can exacerbate liver injury; moderation is advised.
  • Sun exposure: Leflunomide may increase photosensitivity; protective clothing and sunscreen are recommended during prolonged outdoor activity.
  • Driving: No direct impairment, but patients experiencing severe fatigue or dizziness should exercise caution.

How to Take Arava

  • Loading Phase: 100 mg (five 20 mg tablets) once daily for the first three days, or 20 mg once daily without a loading dose if a rapid increase in plasma levels is not required.
  • Maintenance Phase: 20 mg once daily is the typical maintenance dose. Some clinicians may start with 10 mg daily for patients with mild disease or hepatic concerns, titrating upward as tolerated.
  • Administration: Swallow tablets whole with a full glass of water. Food does not significantly affect absorption, so the dose may be taken with or without meals.
  • Missed Dose: Take the missed tablet as soon as remembered on the same day; do not double the next dose.
  • Overdose: Symptoms may include nausea, vomiting, diarrhoea, or severe liver injury. Seek urgent medical attention; activated charcoal may be considered if presentation is early.
  • Discontinuation: To terminate therapy rapidly, a cholestyramine washout (4 g three times daily for 11 days) is recommended, especially in women planning pregnancy. Abrupt cessation without washout can result in prolonged drug presence due to the long half-life of teriflunomide.

Dose adjustments are required for patients with moderate hepatic impairment (reduce to 10 mg daily) or renal dysfunction (use caution; no formal dose reduction recommended but monitor closely).

Monitoring and Follow-Up

  • Baseline labs: Liver function tests (ALT, AST, bilirubin), full blood count, serum creatinine, and blood pressure measurement.
  • Routine monitoring: LFTs and CBC at weeks 2, 4, 8, and then every 3 months while on therapy.
  • Pregnancy testing: For women of child-bearing potential, a negative pregnancy test is required before initiation and monthly thereafter.
  • Blood pressure: Check at each clinic visit; antihypertensive therapy may need adjustment.

Prompt reporting of new respiratory symptoms, unexplained fever, or skin eruptions is essential.

Storage and Handling

  • Store tablets at room temperature (15-25 °C), protected from moisture and direct sunlight.
  • Keep the container tightly closed and out of reach of children.
  • Do not use tablets after the expiry date printed on the pack.
  • If a tablet becomes damaged or discoloured, discard it safely and obtain a new supply.

Medication-Specific Glossary

DMARD (Disease-Modifying Antirheumatic Drug)
A class of medications that slow or halt the underlying autoimmune processes causing joint damage, rather than merely relieving symptoms.
Teriflunomide
The active metabolite of leflunomide; shares the same DHODH-inhibiting activity and contributes to the drug’s long-lasting effects.
Pyrimidine Synthesis
The biochemical pathway that creates the nucleotides cytosine, thymine, and uracil; inhibition reduces proliferation of rapidly dividing immune cells.
Cholestyramine Washout
A therapeutic regimen using the bile-acid-binding resin cholestyramine to accelerate removal of teriflunomide from the body, typically employed when rapid drug clearance is required.
Teratogenic
Capable of causing birth defects when exposure occurs during pregnancy.

Medical Disclaimer

This article provides educational information about Arava (leflunomide) and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Arava is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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