Leflunomide

Leflunomide Brands

Brand Name	Manufacturer Name	Distributor	Drug Strength	Packaging	Formulation	Formulation Strength	Price
Arava	Sanofi Aventis	Surgipharm Ltd	20mg	30	Tablet	per tablet	KES 7,807
Lefra	Torrent Pharmaceuticals Ltd.	Medox Pharmaceuticals Ltd.	20mg	30	Tablet	per tablet	KES 3,200
Lefra	Torrent Pharmaceuticals Ltd.	Medox Pharmaceuticals Ltd.	200mg	20	Tablet	per tablet	KES 829.65

Leflunomide More info
Mode Of Action	Disease-modifying antirheumatic drug
Drug Indication	Moderate rheumatoid arthritis
Precautions	Renal impairment, impaired bone marrow function such as thrombocytopenia, leucopenia, history of TB, pregnancy (exclude before use), washout procedure before transferring the patient to other disease-modifying antirheumatic drugs.
Contra-Indications	Pregnancy, severe immunodeficiency, severe hepatic disorder, severe hypoproteinaemia.
Side Effects	GI disturbances, weight loss, headache, hypertension, abdominal pain, dizziness, asthenia, alopecia, tenosynovitis, paraesthesia, eczema, Steven-Johnson syndrome, toxic epidermal necrolysis, panceatitis, anaemia, eosinophilia, thrombocytopenia, pancycytopenia, severe infection, skin rash,pruritus, anaphylaxis, interstitial lung disease, taste disturbances.
Dosage	Initially, 100mg OD x 3/7. Maintenance dose: 10-20mg OD. Dosing: Adult Rheumatoid arthritis: Oral: Loading dose: 100 mg/day for 3 days, followed by 20 mg/day; Note: The loading dose may be omitted in patients at increased risk of hepatic or hematologic toxicity (eg, recent concomitant methotrexate). Dosage may be decreased to 10 mg/day in patients who have difficulty tolerating the 20 mg dose. Due to the long half-life of the active metabolite, serum concentrations may require a prolonged period to decline after dosage reduction. CMV disease, resistant to standard antivirals (unlabeled use): Oral: Some authors recommend 100-200 mg/day for 5-7 days, followed by 40-60 mg/day (Avery, 2004; Avery, 2010). Others have utilized the standard rheumatoid arthritis dosing (John, 2004). Adjust dose based on serum concentrations of metabolite and adverse events (Avery, 2008; Avery, 2010; Williams, 2002). Dosing: Geriatric Refer to adult dosing. Dosing: Renal Impairment 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 M1 is doubled in dialysis patients. Patients should be monitored closely for adverse effects requiring dosage adjustment. Dosing: Hepatic Impairment Not recommended for use in patients with pre-existing liver disease or in patients with significant hepatic impairment (ALT >2 times ULN). Patients should have LFTs monitored closely. Discontinue leflunomide if ALT >3 times ULN. Dosing: Adjustment for Toxicity ALT elevations >3 times ULN: Discontinue leflunomide and initiate cholestyramine to enhance elimination. Drug elimination procedure: To achieve nondetectable serum concentrations (<0.02 mg/L) of the active metabolite (M1) of leflunomide administer the following: Cholestyramine: 8 g administered 3 times/day for 11 days. The 11 days do not need to be consecutive unless plasma concentrations need to be lowered rapidly. Verify serum concentrations by 2 separate tests ≥14 days apart. If plasma concentrations are still high, additional cholestyramine treatment may be considered. In healthy volunteers, cholestyramine 8 g administered 3 times/day for 24 hours decreased M1 concentrations by 40% in 24 hours and 49% to 65% in 48 hours. Activated charcoal: 50 g every 6 hours for 24 hours was shown to decrease plasma concentrations of M1 by 37% in 24 hours and 48% in 48 hours.