Leflunomide (Page 7 of 7)
DRUG ABUSE AND DEPENDENCE
Leflunomide has no known potential for abuse or dependence.
OVERDOSAGE
In mouse and rat acute toxicology studies, the minimally toxic dose for oral leflunomide was 200 — 500 mg/kg and 100 mg/kg, respectively (approximately >350 times the maximum recommended human dose, respectively).
There have been reports of chronic overdose in patients taking leflunomide at daily dose up to five times the recommended daily dose and reports of acute overdose in adults or children. There were no adverse events reported in the majority of case reports of overdose. Adverse events were consistent with the safety profile for leflunomide (see ADVERSE REACTIONS). The most frequent adverse events observed were diarrhea, abdominal pain, leukopenia, anemia and elevated liver function tests.
In the event of a significant overdose or toxicity, cholestyramine or charcoal administration is recommended to accelerate elimination (see PRECAUTIONS — General — Need for Drug Elimination).
Studies with both hemodialysis and CAPD (chronic ambulatory peritoneal dialysis) indicate that M1, the primary metabolite of leflunomide, is not dialyzable. (See CLINICAL PHARMACOLOGY – Elimination).
DOSAGE AND ADMINISTRATION
Loading Dose
Due to the long half-life in patients with RA and recommended dosing interval (24 hours), a loading dose is needed to provide steady-state concentrations more rapidly. It is recommended that leflunomide therapy be initiated with a loading dose of one 100 mg tablet per day for 3 days.
Elimination of the loading dose regimen may decrease the risk of adverse events. This could be especially important for patients at increased risk of hematologic or hepatic toxicity, such as those receiving concomitant treatment with methotrexate or other immunosuppressive agents or on such medications in the recent past. (See WARNINGS — Hepatotoxicity).
Maintenance Therapy
Daily dosing of 20 mg is recommended for treatment of patients with RA. A small cohort of patients (n=104), treated with 25 mg/day, experienced a greater incidence of side effects; alopecia, weight loss, liver enzyme elevations. Doses higher than 20 mg/day are not recommended. If dosing at 20 mg/day is not well tolerated clinically, the dose may be decreased to 10 mg daily. Liver enzymes should be monitored and dose adjustments may be necessary (see WARNINGS – Hepatotoxicity). Due to the prolonged half-life of the active metabolite of leflunomide, patients should be carefully observed after dose reduction, since it may take several weeks for metabolite levels to decline.
Monitoring
Hematology parameters and liver enzymes should be monitored (see PRECAUTIONS – Laboratory Tests; WARNINGS – Hepatotoxicity; WARNINGS – Immunosuppression Potential/Bone Marrow Suppression).
HOW SUPPLIED
Leflunomide Tablets, USP in 10 and 20 mg strengths are packaged in bottles.
Strength | Quantity | NDC Number | Description |
10 mg | 30 count bottle | 23155-043-03 | White, round bi-convex tablets debossed with “HP 43” on one side and plain on the other. |
500 count bottle | 23155-043-05 | ||
20 mg | 30 count bottle | 23155-044-03 | White, triangular bi-convex tablets debossed with “HP 44” on one side and plain on the other. |
500 count bottle | 23155-044-05 |
Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Protect from light.
Rx only
Manufactured for:
Heritage Pharmaceuticals Inc.
Edison, NJ 08837
And Relabeled By:
Dispensing Solutions Inc.
3000 West Warner Ave
Santa Ana, CA 92704
United States
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
NDC 68258-2992-03
LEFLUNOMIDE leflunomide tablet | ||||||||||||||||||
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Labeler — Dispensing Solutions, Inc. (066070785) |
Registrant — PSS World Medical, Inc. (101822682) |
Establishment | |||
Name | Address | ID/FEI | Operations |
Dispensing Solutions, Inc. | 066070785 | relabel (68258-2992), repack (68258-2992) |
Revised: 10/2013 Dispensing Solutions, Inc.
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