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PRO-LEFLUNOMIDE is a brand name for Leflunomide, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: PRO-LEFLUNOMIDE (leflunomide tablets) should be used only by physicians who have fully familiarized themselves with the efficacy and safety profile of PRO-LEFLUNOMIDE and who are experienced in the therapy of rheumatoid diseases. PRO-LEFLUNOMIDE is indicated in adults for the treatment of active rheumatoid arthritis.…
Verbatim from this product's HC label. Tap a section to expand.
2 Recommended Dose and Dosage Adjustment Loading Dose Due to the long half-life in patients with rheumatoid arthritis and recommended dosing interval (24 hr), a loading dose is needed to yield steady-state concentrations more rapidly.
It is recommended that PRO-LEFLUNOMIDE therapy be initiated with a loading dose of one 100 mg tablet per day for 3 days. Maintenance Therapy Daily dosing of 20 mg is recommended for treatment of patients with rheumatoid arthritis. 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. Due to the prolonged half-life of the active metabolite of PRO- LEFLUNOMIDE, patients should be carefully observed after dose reduction since it may take several weeks for metabolite levels to decline (See 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests Section).
A treatment effect may be evident after 4 weeks and may further improve up to 4 to 6 months after start of treatment. Geriatric (≥ 65 years) No dosage adjustment is needed in patients over 65 years of age. Pediatrics (< 18 years) The use in patients less than 18 years of age is contraindicated.
Dose Modification for Patient with Renal Impairment Because the kidney plays a role in the elimination of leflunomide, and without sufficient studies of the use of leflunomide in patients with renal insufficiency, caution should be used when considering the administration of PRO-LEFLUNOMIDE to patients with mild renal insufficiency (See 2 CONTRAINDICATIONS Section).
4 Administration PRO-LEFLUNOMIDE tablets should be swallowed whole, with sufficient liquid. PRO- LEFLUNOMIDE can be taken with or without food, without regard to meals, at the same time everyday. 5 Missed Dose If the patient forgot to take a tablet of PRO-LEFLUNOMIDE they should be advised to take it as soon as they remember, unless it is nearly time for their next dose.
The patient should be advised not to double-up on the next dose to make up for the missed dose. 5 OVERDOSE There have been reports of chronic overdose in patients taking leflunomide at daily doses up to five times the recommended daily dose and reports of acute overdose in adults or children.
Section). The most frequent adverse events observed were diarrhea, abdominal pain, leucopenia, anemia and elevated liver function tests. In the event of relevant overdose or toxicity, cholestyramine or activated charcoal administration is recommended.
Cholestyramine given orally at a dose of 8 g three times a day for 24 hours to three healthy volunteers decreased plasma levels of A771726 by approximately 40% in 24 hours and by 49- 65% in 48 hours (See 7 WARNINGS AND PRECAUTIONS, General, Washout Procedures Section).
Administration of activated charcoal (powder made into a suspension) orally or via nasogastric tube (50 g every 6 hours for 24 hours) has been shown to reduce plasma concentrations of the active metabolite, A771726, by 37% in 24 hours and by 48% in 48 hours.
These washout procedures may be repeated if clinically necessary. Studies with both hemodialysis and CAPD (chronic ambulatory peritoneal dialysis) indicate that A771726, the primary metabolite of leflunomide, is not dialyzable. For the most recent information in the management of a suspected drug overdose, contact your regional poison control centre or Health Canada’s toll-free number, 1-844 POISON-X (1- 844-764-7669).
6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING To help ensure the traceability of biologic products, including biosimilars, health professionals should recognise the importance of recording both the brand name and the non-proprietary PRO-LEFLUNOMIDE (Leflunomide Tablets) Page 8 of 82 (active ingredient) name as well as other product-specific identifiers such as the Drug Identification Number (DIN) and the batch/lot number of the product supplied.
Table 1. Dosage Forms, Strengths, Composition and Packaging Route of Administration Dosage Form/Strength/Composition Non-medicinal Ingredients Oral Film-coated tablets 10 mg and 20 mg Colloidal silicon dioxide, corn starch, hydroxypropyl cellulose, hydroxypropyl methylcellulose, lactose anhydrous, lactose monohydrate, magnesium stearate, polyethylene glycol, povidone, titanium dioxide and yellow ferric oxide (20 mg tablet only).
Perioperative Considerations 11/2025 7 WARNINGS AND PRECAUTIONS, Skin 11/2025 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES ...........................................................................................
2 TABLE OF CONTENTS ............................................................................................................. 2 PART I: HEALTHCARE PROFESSIONAL INFORMATION .............................................................
4 1 INDICATIONS .............................................................................................................. 1 Pediatrics.................................................................................................................
2 Geriatrics ................................................................................................................. 4 2 CONTRAINDICATIONS .................................................................................................
4 4 DOSAGE AND ADMINISTRATION................................................................................. 2 Recommended Dose and Dosage Adjustment ....................................................... 4 Administration ........................................................................................................
5 Missed Dose ............................................................................................................ 7 5 OVERDOSE .................................................................................................................
7 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING ................................. 7 7 WARNINGS AND PRECAUTIONS .................................................................................. 1 Special Populations ...............................................................................................
Pro-Leflunomide is contraindicated in: • Patients with known hypersensitivity to leflunomide (especially previous Stevens-Johnson syndrome, toxic epidermal necrolysis or erythema multiforme), to teriflunomide or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container.
For a complete listing, see 6 Dosage Forms, Strengths, Composition, and Packaging section. , AIDS) (See 7 WARNINGS AND PRECAUTIONS, Immune Section). • Patients with impaired bone marrow function or significant anemia, leucopenia, neutropenia or thrombocytopenia due to causes other than rheumatoid arthritis.
• Patients with serious infections. • Patients with moderate to severe renal insufficiency because the kidney plays a role in the elimination of leflunomide. , Disease Modifying Antirheumatic Drugs [DMARDs] such as methotrexate) given the possible risk of increased hepatotoxicity and the role of the PRO-LEFLUNOMIDE (Leflunomide Tablets) Page 5 of 82 liver in activation, elimination and recycling of leflunomide (see 9 DRUG INTERACTIONS Section).
While the mechanism of action of leflunomide and methotrexate are different, their pharmacodynamic action of interfering with cell division is similar. Concomitant treatment with methotrexate and/or other liver and bone marrow toxic medications is associated with an increased risk of serious hepatic or marrow reactions and requires strict vigilance in monitoring (See 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests Section).
If a switch in treatment from leflunomide to another hepatotoxic DMARD is required the washout and monitoring must be adhered to as mentioned in the 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests and General, Washout Procedures sections.
g. in nephrotic syndrome). Since the active metabolite of leflunomide, A771726, is highly protein-bound and cleared via hepatic metabolism and biliary secretion. 02 mg/L). Pregnancy must be excluded before start of treatment with PRO- LEFLUNOMIDE (See 7 WARNINGS AND PRECAUTIONS, Special Populations, Pregnancy section).
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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The majority of the reported overdoses were without adverse events. In cases where adverse events were reported, they were consistent with the safety profile for leflunomide (See 8 ADVERSE REACTIONS Section). The most frequent adverse events observed were diarrhea, abdominal pain, leucopenia, anemia and elevated liver function tests.
In the event of relevant overdose or toxicity, cholestyramine or activated charcoal administration is recommended. Cholestyramine given orally at a dose of 8 g three times a day for 24 hours to three healthy volunteers decreased plasma levels of A771726 by approximately 40% in 24 hours and by 49- 65% in 48 hours (See 7 WARNINGS AND PRECAUTIONS, General, Washout Procedures Section).
Administration of activated charcoal (powder made into a suspension) orally or via nasogastric tube (50 g every 6 hours for 24 hours) has been shown to reduce plasma concentrations of the active metabolite, A771726, by 37% in 24 hours and by 48% in 48 hours.
These washout procedures may be repeated if clinically necessary. Studies with both hemodialysis and CAPD (chronic ambulatory peritoneal dialysis) indicate that A771726, the primary metabolite of leflunomide, is not dialyzable. For the most recent information in the management of a suspected drug overdose, contact your regional poison control centre or Health Canada’s toll-free number, 1-844 POISON-X (1- 844-764-7669).
PRO-LEFLUNOMIDE is available for oral administration as film-coated tablets containing 10 mg or 20 mg of leflunomide. PRO-LEFLUNOMIDE 10 mg tablets are white-coloured, circular, biconvex film-coated tablets plain on one side and “L10” debossed on the other side.
PRO-LEFLUNOMIDE 20 mg tablets are light yellow-coloured, triangular, biconvex, film-coated tablets with “L20” debossed on one side and plain on the other side. PRO-LEFLUNOMIDE tablets in 10 and 20 mg strengths are available in bottles of 30 tablets.
7 WARNINGS AND PRECAUTIONS General The active metabolite of leflunomide, A771726, has a long half-life. g. hepatotoxicity, hematotoxicity or allergic reactions, see below), even if the treatment with Pro-Leflunomide has been stopped.
For the management of the above-mentioned toxicities a washout procedure should be performed. If a severe adverse reaction to Pro-Leflunomide occurs, or if for any other reason A771726 needs to be cleared rapidly from the body, cholestyramine or activated charcoal has to be initiated and continued/repeated as clinically necessary (See 5 OVERDOSE Section).
For suspected severe immunologic/allergic reactions, more prolonged cholestyramine or activated charcoal administration may be necessary to achieve rapid and sufficient clearance (See below the Washout Procedures). g. methotrexate) after treatment with PRO- LEFLUNOMIDE a washout procedure should be performed since there exists a possibility of additive risks of adverse events for a long time after the switching (See below the Washout Procedures and see also the 2 CONTRAINDICATIONS and
1 Pregnancy.......................................................................................................... 2 Breastfeeding ....................................................................................................
3 Pediatrics........................................................................................................... 4 Geriatrics ...........................................................................................................
19 8 ADVERSE REACTIONS................................................................................................ 1 Adverse Reaction Overview .................................................................................. 2 Clinical Trial Adverse Reactions ............................................................................
3 Less Common Clinical Trial Adverse Reactions ..................................................... 5 Post-Market Adverse Reactions............................................................................ 25 9 DRUG INTERACTIONS ...............................................................................................
2 Drug Interactions Overview .................................................................................. 4 Drug-Drug Interactions ......................................................................................... 5 Drug-Food Interactions .........................................................................................
6 Drug-Herb Interactions ......................................................................................... 7 Drug-Laboratory Test Interactions........................................................................ 34 10 CLINICAL PHARMACOLOGY .......................................................................................
1 Mechanism of Action ............................................................................................ 3 Pharmacokinetics ..................................................................................................
35 11 STORAGE, STABILITY AND DISPOSAL ......................................................................... 37 PART II: SCIENTIFIC INFORMATION ......................................................................................
38 13 PHARMACEUTICAL INFORMATION ........................................................................... 38 14 CLINICAL TRIALS .......................................................................................................
1 Clinical Trials by Indication ................................................................................... 2 Comparative Bioavailability Studies ..................................................................... 48 15 MICROBIOLOGY .......................................................................................................
49 16 NON-CLINICAL TOXICOLOGY ..................................................................................... 50 17 SUPPORTING PRODUCT MONOGRAPHS .................................................................... 71 PATIENT MEDICATION INFORMATION .................................................................................
72 PRO-LEFLUNOMIDE (Leflunomide Tablets) Page 4 of 82 PART I: HEALTHCARE PROFESSIONAL INFORMATION 1 INDICATIONS PRO-LEFLUNOMIDE (leflunomide tablets) should be used only by physicians who have fully familiarized themselves with the efficacy and safety profile of PRO-LEFLUNOMIDE and who are experienced in the therapy of rheumatoid diseases.
PRO-LEFLUNOMIDE is indicated in adults for the treatment of active rheumatoid arthritis. 1 Pediatrics The use in patients less than 18 years of age is contraindicated. 2 Geriatrics No dosage adjustment is needed in patients over 65 years of age.
There are no overall differences in effectiveness and safety between elderly […]
• Women who are breast feeding (See 7 WARNINGS AND PRECAUTIONS, Special Populations, Breastfeeding Section). • Patients less than 18 years of age. Male patients should be aware of the possible male-mediated foetal toxicity. Reliable contraception during treatment with PRO-LEFLUNOMIDE should also be guaranteed (See 7 WARNINGS AND PRECAUTIONS, Reproductive Health and Special Population, Pregnancy Section).
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