Drug information of Leflunomide
Leflunomide affects the immune system and reduces swelling and inflammation in the body. Leflunomide is used to treat the symptoms of rheumatoid arthritis.
Mechanism of effect
Leflunomide is an isoxazole immunomodulatory agent that inhibits dihydroorotate dehydrogenase (a mitochondrial enzyme involved in de novo pyrimidine synthesis) and has antiproliferative activity. Several in vivo and in vitro experimental models have demonstrated an anti-inflammatory effect.
Leflunomide is a pyrimidine synthesis inhibitor indicated in adults for the treatment of active rheumatoid arthritis (RA)
Well absorbed, peak plasma concentrations appear 6-12 hours after dosing Metabolism:Primarily hepatic. Following oral administration, Leflunomide is metabolized to an active metabolite, teriflunomide. Protein binding:>99.3%. The active metabolite is eliminated by further metabolism and subsequent renal excretion as well as by direct biliary excretion. Half life:2 weeks.
Drug indicationsRheumatoid arthritis
Usual Adult Dose for Rheumatoid Arthritis Loading dose: 100 mg orally once a day for 3 days Maintenance: 20 mg orally once a day (If not well tolerated, the dose may be decreased to 10 mg orally once a day)
Drug contraindicationsPregnancy , hypersensitivity to drug or its components. , severe hepatic impairment , being treated with teriflunomide
Side effectsnausea , Headache , abdominal pain , dizziness , vomiting , Hepatic dysfunction , allergic reaction , Diarrhea , asthenia , pruritus , Hypertension , peripheral neuritis , Rhinitis , Stevens-Johnson syndrome , Alopecia , back pain , bronchitis , mouth ulcers , Bone marrow suppression
InteractionsEthinyl estradiol , Paclitaxel , Glutazone , Duloxetine , Repaglinide , Etanercept , Streptozocin , Ifosfamide , Budesonide , Pemethrexed , Terbinafine , Binimetinib , Aflibercept , Abacavir , Atovaquone , Aminosalicylic Acid , Axicabtagene ciloleucel , Pralatrexate , Bendamustine , Nintedanib , Troglitazone , Canakinumab , Basiliximab , Alefacept , Idelalisib , Ivacaftor , Clofarabine , Pyrazinamide , Ibritumomab tiuxetan , Maraviroc , Dantrolene , alectinib , Lenalidomide , Teniposide , Golimumab , Hib vaccine , Peg-interferon alfa 2a , Zalcitabine , Zidovudine , Didanosine , pravastatin , mercaptopurine , Nalthrexone , Vinorelbine , Carbamazepine , cladribine , Chlorambucil , Bisoprolol , Danazol , Dacarbazine , Deflazacort , Riluzole , Glatiramer acetate , Melphalan , Warfarin
1-Leflunomide may cause fetal harm when administered to a pregnant woman.
2-Severe liver injury, including fatal liver failure, has been reported in some patients treated with Leflunomide
3-Leflunomide is not recommended for patients with severe immunodeficiency, bone marrow dysplasia, or severe, uncontrolled infections
Points of recommendation
1-No clinical data are available on the efficacy and safety of vaccinations during Leflunomide treatment. Vaccination with live vaccines is, however, not recommended.
2-Blood pressure should be checked before starting treatment with Leflunomide and monitored periodically thereafter
3-Take without regard to meals.