LEFLUNOMIDE - Watsons Health





Description: Leflunomide is an immunomodulating agent and DMARD that inhibits pyrimidine synthesis. It inhibits dihydroorotate dehydrogenase enzyme activity resulting in antiproliferative and anti-inflammatory effects.


Absorption: Bioavailability: Approx 82-95%. Time to peak plasma concentration (active metabolite): 6-12 hr.

Distribution: Volume of distribution: 0.13 L/kg. Plasma protein binding (active metabolite): 99% (mainly albumin).

Metabolism: Rapidly converted to active metabolite A77 1726 in GI mucosa and the liver.

Excretion: Via urine (approx 43% as glucuronides) and faeces (approx 48%). Elimination half-life (active metabolite): Approx 14-18 days.

This medication is used to treat rheumatoid arthritis. It helps to reduce the joint damage/pain/swelling and helps you to move better. It weakens your immune system and decreases swelling (inflammation). This may also be used to prevent rejection of organ transplant.


How to use leflunomide

Take this medication by mouth with or without food, usually once daily or as directed by your doctor. Take this medication exactly as prescribed. You may be instructed to take a higher dose for the first 3 days of treatment.


Dosage is based on your medical condition and response to therapy.


Take this medication regularly in order to get the most benefit from it. To help you remember, take it at the same time each day.


After treatment is stopped, a different drug (cholestyramine) may be given as directed to help remove leflunomide from your body. This procedure is used if you need a rapid removal of the drug from your system (e.g., a female/male planning to have children, a person suffering from severe side effects). Without the procedure, the drug may stay in your body for up to 2 years. Consult your doctor or pharmacist for more details.


Inform your doctor if your symptoms persist or worsen.

Leflunomide must not be used during pregnancy.


This drug may rarely cause serious (possibly fatal) liver disease.

Tell your doctor or pharmacist promptly if diarrhea, nausea, and dizziness persist or worsen.


Tell your doctor right away if you have any serious side effects, including:


  • Cough
  • numbness/tingling of hands/feet
  • hair loss
  • chest pain
  • fast/pounding heartbeat
  • increased thirst/urination
  • muscle cramp/pain
  • mental/mood changes
  • vision changes
  • easy bruising/bleeding
  • unusual growths/lumps
  • swollen glands (lymph nodes)
  • unexplained weight loss
  • unusual tiredness



This medication may raise your blood pressure.


This medication owers the body’s immune system or the ability to fight an infection


A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction:


  • rash
  • itching/swelling (especially of the face/tongue/throat)
  • severe dizziness
  • trouble breathing



This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

  • Allergic reaction from this medication
  • Patients with medical history of:
    • immune system disorder (e.g., HIV infection)
    • current/recent infection (e.g., tuberculosis)
    • cancer
    • bone marrow/blood disorder
    • kidney disease
    • liver disease (e.g., hepatitis B or C)
    • alcohol abuse
    • heart disease (e.g., congestive heart failure)
    • high blood pressure
    • lung disease
  • This drug may make you dizzy
  • Do not have immunizations/vaccinations without the consent of your doctor
  • avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose.


  • Avoid contact with people who have illnesses that may spread to others (e.g., flu, chickenpox)
  • This medication must not be used during pregnancy
  • It is not known whether this medication affects the sperm
  • breast-feeding is not recommended while using this drug

Consult your doctor or pharmacist regarding the precautions mentioned above.




Some products that may interact with this drug include:


  • warfarin
  • rifamycins (e.g., rifampin)
  • drugs affecting the liver (e.g., methotrexate)
  • cholestyramine
  • other drugs that weaken the immune system (e.g., tacrolimus, cyclosporine)



Do not take teriflunomide while you are taking leflunomide.

  • If overdose is suspected, contact a poison control center or emergency room immediately.Notes

    Do not share this medication with others.


    A skin test to check for tuberculosis should be performed before you start this medication. While taking this medication, laboratory and/or medical tests (e.g., liver function, blood counts, blood pressure) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.


    Missed Dose

    If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.



    Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.


    Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.




    Available Brands

    Arava [ sanofi-aventis ]

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