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Overview

Leflunomide

Prescription vs OTC : Prescription by Doctor required

About Leflunomide

Leflunomide is an immunosuppressive disease-modifying antirheumatic drug. It is a pyrimidine synthesis inhibitor. It is used to treat rheumatoid arthritis. It functions by reducing joint pain and swelling.

Certain side-effects that you may experience on using Leflunomide are dizziness, nausea, diarrhoea, hair loss, headache, respiratory tract infections, cough, difficulty breathing, stomatitis, fatigue, itchiness and pharyngitis. Should your allergic reactions continue or worsen over time, immediately contact your health care provider.

Before using Leflunomide have a word with your doctor and inform him/her if: you are allergic to any medication, food, substance or any ingredient contained within Leflunomide, you are pregnant, or are planning to become pregnant or are nursing a baby, you have a weak immune system, you have liver, lung or kidney problems and if you are taking any prescription or non-prescription drugs.

The dosage should be ideally prescribed by your doctor. This medication comes in a tablet form. Usually the adult dose for Leflunomide is about 20 mg (maintenance dose) to be taken through the mouth once for over a period of 3 days.

If diabetic, monitor blood sugars closely; this medication may alter glucose levels. There is no human experience with overdosage. Leflunomide is not dialyzable. Cholestyramine and/or activated charcoal enhance elimination of leflunomide's active metabolite (MI).

In cases of significant overdose or toxicity, cholestyramine 8 g every 8 hours for 1-3 days may be administered to enhance elimination. Plasma levels are reduced by approximately 40% in 24 hours and 49% to 65% after 48 hours of cholestyramine dosing.

Take as directed; do not increase dose without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Store medication away from light.

Leflunomide has been associated with teratogenic and embryolethal effects in animal models at low doses. Leflunomide is contraindicated in pregnant women or women of childbearing potential who are not using reliable contraception.

Pregnancy must be excluded prior to initiating treatment. Following treatment, pregnancy should be avoided until the drug elimination procedure is completed.

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    What are the uses of Leflunomide

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    What are the contraindications of Leflunomide ?

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    What are the side effects of Leflunomide ?

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    Key highlights of Leflunomide

    • Is It safe with alcohol?

      Taking Leflunomide with alcohol may cause liver problems.

    • Are there any pregnancy warnings?

      Leflunomide is highly unsafe to use during pregnancy.
      Human and animal studies have shown significant adverse effects on the foetus. Please consult your doctor.

    • Are there any breast-feeding warnings?

      This drug may cause severe fetal defects. Do not breast-feed. Please consult your doctor.

    • Is it safe to drive while on this medicine?

      Caution is advised when driving or operating machinery.

    • Does this affect kidney function?

      No specific dosage adjustment is recommended. There is no clinical experience in the use of Leflunomide in patients with renal impairment. The free fraction of MI is doubled in dialysis patients. Patients should be monitored closely for adverse effects requiring dosage adjustment.

    • Does this affect liver function?

      No specific dosage adjustment is recommended. Since the liver is involved in metabolic activation and subsequent metabolism/elimination of Leflunomide, patients with hepatic impairment should be monitored closely for adverse effects requiring dosage adjustment.

    • What is the onset of action?

      The effect of this medicine is initiated within 2 hours after its administration.

    • How long is the duration of effect?

      The effect of this medicine will remain for about 12 - 14 hours.

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    What are the dosage instructions?

    • Are there any missed dose instructions?

      If you miss a dose of Leflunomide, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    Medicines containing Leflunomide

    Below is the list of medicines, which contains Leflunomide as ingredient

    Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

    How does this medication work?

    Leflunomide is a prodrug with anti-inflammatory and immunosuppressive properties that works by breaking down into its active metabolite A77 1726 once ingested which then blocks an important enzyme for de novo pyrimidine synthesis, dihydroorotate dehydrogenase. This inhibits the growth of activated T-lymphocytes.

      Information given here is based on the salt content of the medicine. Uses and effects of the medicine may vary from person to person. It is advisable to consult a Rheumatologist before using this medicine.

      What are the interactions of Leflunomide ?

      Whenever you take more than one medicine, or mix it with certain foods or beverages, you"re at risk of a drug interaction.

        test
      • Interaction with Medicine

        Decreased effect: Administration of cholestyramine and activated charcoal enhance the elimination of leflunomide's active metabolite.
      • Interaction with Disease

        • Hepatic disease (including seropositive hepatitis B or C patients) may increase risk of hepatotoxicity; immunosuppression may increase the risk of lymphoproliferative disorders or other malignancies;
        • Women of childbearing potential should not receive Leflunomide until pregnancy has been excluded, patients have been counseled concerning fetal risk and reliable contraceptive measures have been confirmed.
        • Caution in renal impairment.
        • Not recommended for patients with severe immune deficiency, bone marrow dysplasia or uncontrolled infection.
        • Has been associated with rare pancytopenia; use with caution in patients with a prior history of significant hematologic abnormalities.
        • Discontinue if evidence of bone marrow suppression occurs, and begin procedure for accelerated removal (cholestyramine and activated charcoal).
        • The use of live vaccines is not recommended.
        • Leflunomide will increase uric acid excretion.

      FAQs about Leflunomide

      • Ques : What is Leflunomide?

        Ans : Leflunomide is an immunosuppressive disease-modifying antirheumatic drug. It is a pyrimidine synthesis inhibitor.

      • Ques : What is Leflunomide used for?

        Ans : It is used to treat rheumatoid arthritis. It functions by reducing joint pain and swelling.

      • Ques : How long do I need to use Leflunomide before I see improvement in my condition?

        Ans : In most of the cases, the average time taken by this medication to reach its peak effect is around 1 day to 1 week. Please consult your doctor for the time period you need to use this medication.

      • Ques : At what frequency do I need to use Leflunomide?

        Ans : This medication is generally used once or twice a day. It is advised to consult your doctor before the usage, as the frequency also depends on the patient's condition.

      • Ques : Should I use Leflunomide empty stomach, before food or after food?

        Ans : This medication is advised to be consumed orally. If you take it on an empty stomach, it might upset the stomach. Please consult the doctor before using it.

      • Ques : What are the instructions for the storage and disposal of Leflunomide?

        Ans : It should be stored at room temperature, away from heat and direct light. Keep it away from the reach of children and pets.

      • Ques : How long does Leflunomide take to work?

        Ans : Usually, Leflunomide starts working soon after taking it. However, it may take some days to kill all the harmful bacteria and make you feel better.

      • Ques : What if I don't get better after using Leflunomide?

        Ans : Inform your doctor if you don't feel better after finishing the full course of treatment. Also, inform him if your symptoms are getting worse while using this medicine.

      • Ques : Can Leflunomide cause weight loss?

        Ans : Yes, Leflunomide may cause weight loss as a common side effect. However, weight loss due to this medicine is usually insignificant. The reason for this reduction in weight could be due to accompanying loss of appetite.

      • Ques : Can Leflunomide cause cancer?

        Ans : Leflunomide may increase your chances of cancer, especially of the lymph system, but this is very rare. The reason could be decreased strength of the immune system caused by Leflunomide.

      References

      • Leflunomide-Drug Information Portal [Internet].druginfo.nlm.nih.gov 2022 [Cited 2 June 2022].Available from:

        https://druginfo.nlm.nih.gov/drugportal/name/leflunomide

      • Leflunomide-DrugBank Online [Internet].go.drugbank.com 2022 [Cited 2 June 2022].Available from:

        https://go.drugbank.com/drugs/DB01097

      • LEFLUNOMIDE Tablet,solution-DailyMed [Internet].dailymed.nlm.nih.gov 2022 [Cited 2 June 2022].Available from:

        https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=LEFLUNOMIDE

      Disclaimer : The information produced here is best of our knowledge and experience and we have tried our best to make it as accurate and up-to-date as possible, but we would like to request that it should not be treated as a substitute for professional advice, diagnosis or treatment.

      Lybrate is a medium to provide our audience with the common information on medicines and does not guarantee its accuracy or exhaustiveness. Even if there is no mention of a warning for any drug or combination, it never means that we are claiming that the drug or combination is safe for consumption without any proper consultation with an expert.

      Lybrate does not take responsibility for any aspect of medicines or treatments. If you have any doubts about your medication, we strongly recommend you to see a doctor immediately.
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      Written ByDrx Hina FirdousPhD (Pharmacology) Pursuing, M.Pharma (Pharmacology), B.Pharma - Certificate in Nutrition and Child CarePharmacology
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      Reviewed ByDr. Garima SharmaMBBS, Master in Healthcare Administration, Diploma in Occupational HealthGeneral Physician
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