LEFLUNOMIDE tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

LEFLUNOMIDE (UNII: G162GK9U4W) (LEFLUNOMIDE - UNII:G162GK9U4W)

Available from:

Physicians Total Care, Inc.

INN (International Name):

LEFLUNOMIDE

Composition:

LEFLUNOMIDE 10 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Leflunomide is indicated in adults for the treatment of active rheumatoid arthritis (RA): - to reduce signs and symptoms - to inhibit structural damage as evidenced by X-ray erosions and joint space narrowing - to improve physical function (see CLINICAL STUDIES ). Aspirin, nonsteroidal anti-inflammatory agents and/or low dose corticosteroids may be continued during treatment with leflunomide (see PRECAUTIONS: Drug Interactions: NSAIDs ). The combined use of leflunomide with antimalarials, intramuscular or oral gold, D penicillamine, azathioprine, or methotrexate has not been adequately studied (see WARNINGS: Immunosuppression Potential/Bone Marrow Suppression ). Leflunomide is contraindicated in patients with known hypersensitivity to leflunomide or any of the other components of leflunomide. Leflunomide can cause fetal harm when administered to a pregnant woman. Leflunomide, when administered orally to rats during organogenesis at a dose of 15 mg/kg, was teratogenic (most notably anophthalmia or microophth

Product summary:

Leflunomide tablets, 10 mg are white, round, film-coated tablets, debossed GG on one side and 993 on the reverse side and are supplied as follows: Leflunomide tablets, 20 mg are white, round, film-coated tablets, debossed GG on one side and 994 on the reverse side and are supplied as follows: Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). Dispense in a well-closed container as described in the USP. Protect from light.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LEFLUNOMIDE - LEFLUNOMIDE TABLET, FILM COATED
PHYSICIANS TOTAL CARE, INC.
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LEFLUNOMIDE TABLETS
10 MG AND 20 MG
CONTRAINDICATIONS AND WARNINGS
PREGNANCY MUST BE EXCLUDED BEFORE THE START OF TREATMENT WITH
LEFLUNOMIDE. LEFLUNOMIDE TABLETS ARE CONTRAINDICATED IN
PREGNANT WOMEN, OR WOMEN OF CHILDBEARING POTENTIAL WHO ARE
NOT USING RELIABLE CONTRACEPTION. (SEE CONTRAINDICATIONS AND
WARNINGS.) PREGNANCY MUST BE AVOIDED DURING LEFLUNOMIDE
TREATMENT OR PRIOR TO THE COMPLETION OF THE DRUG ELIMINATION
PROCEDURE AFTER LEFLUNOMIDE TREATMENT.
DESCRIPTION
Leflunomide is a pyrimidine synthesis inhibitor. The chemical name for
leflunomide is N-(4’-
trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide. It has an
empirical formula C
H F N O , a
molecular weight of 270.2 and the following structural formula:
Each leflunomide tablet, for oral administration, contains 10 mg or 20
mg of leflunomide. In addition,
each tablet contains the following inactive ingredients: colloidal
silicon dioxide, crospovidone,
hypromellose, lactose monohydrate, magnesium stearate, polyethylene
glycol, polysorbate 80,
povidone, pregelatinized starch, and titanium dioxide.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Leflunomide is an isoxazole immunomodulatory agent which inhibits
dihydroorotate dehydrogenase (an
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.
PHARMACOKINETICS
Following oral administration, leflunomide is metabolized to an active
metabolite A77 1726 (hereafter
referred to as M1) which is responsible for essentially all of its
activity _in vivo_. Plasma levels of
leflunomide are occasionally seen, at very low levels. Studies of the
pharmacokinetics of leflunomide
have primarily examined the plasma concentrations of this active
metabolite.
ABS ORPTION
Following oral administration, peak levels of the active metabolite,
M1, occurred between 6 to 12 hours
after dosing. Due to the very long half-l