Leflunomide Tablets

This product is an isoxazole immunosuppressant with antiproliferative activity. Its mechanism of action is mainly to inhibit the activity of dihydroorotate dehydrogenase, thereby affecting the pyrimidine synthesis of activated lymphocytes. In vitro and in vivo tests have shown that this product has anti-inflammatory effects. The in vivo activity of leflunomide is mainly produced through its active metabolite A771726 (M1).

The main ingredient of this product is: Leflunomide. Its chemical name is: N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide. Molecular formula: C12H9F3N202 Molecular weight: 270.2

This product is a white film-coated tablet, which appears white after removing the film coating.

(1) Suitable for adults with rheumatoid arthritis, and has a therapeutic effect on improving the condition. (2) Lupus nephritis.

⑴ Adult rheumatoid arthritis: Oral. Due to the long half-life of leflunomide, it is recommended to take the drug every 24 hours. In order to quickly reach a steady-state blood concentration, referring to foreign clinical trial data and combined with the results of Phase I clinical trials, it is recommended to give a loading dose of 50 mg per day for the first three days of treatment, and then give a maintenance dose of 10 mg or 20 mg per day according to the condition. 3 months is a course of treatment. ⑵ Lupus nephritis: Oral. Choose an appropriate dose according to the condition. The recommended dose is once a day, 20-41 mg at a time, and the dose should be appropriately reduced after the condition is relieved.

The main adverse events are diarrhea, itching, reversible liver enzyme (ALT and AST) elevation, hair loss, rash, etc. In foreign clinical trials, among 1,339 patients with rheumatoid arthritis treated with leflunomide, the incidence of adverse events was ge; 3%, including fatigue, abdominal pain, back pain, hypertension, anorexia, diarrhea, indigestion, gastroenteritis, liver enzyme elevation, nausea, oral ulcers, vomiting, weight loss, joint dysfunction, tenosynovitis, dizziness, headache, bronchitis, cough, respiratory tract infection, pharyngitis, hair loss, itching, rash, urinary tract infection, etc. The above adverse events were found in the placebo-controlled or positive-controlled sulfasalazine-treated group and the MTX-treated group. Among them, diarrhea, liver enzyme elevation, hair loss, and rash were more obvious in the leflunomide-treated group, and attention should be paid during application.

It is contraindicated for patients who are allergic to this product and its metabolites and those with severe liver damage.

Precautions for children: The efficacy and safety of this product for children have not been studied, so patients under the age of 18 are not recommended to use this product. Precautions for pregnancy and lactation: Pregnant women and women of childbearing age who have not taken reliable contraceptive measures and lactating women are prohibited from using this product. Precautions for the elderly: This experiment has not been conducted and there are no reliable references.

1 Cholestyramine and activated charcoal Thirteen patients and 96 volunteers were given cholestyramine or activated charcoal, and the plasma Ml concentration decreased rapidly. 2 The hepatotoxic drug leflunomide and other hepatotoxic drugs may increase adverse reactions. It should also be considered that although leflunomide treatment is interrupted, if these drugs are continued without taking drug elimination measures, adverse reactions may also be increased. In a small sample (30 cases) study of the combined use of leflunomide and MTX, 5 cases had a 2-3 times increase in liver enzymes. Among them, 2 cases continued to take the drug and 3 cases discontinued leflunomide treatment, and the increase in enzymes was restored. In another 5 cases, the increase was greater than 3 times, of which 2 cases continued to take the drug and 3 cases discontinued leflunomide treatment, and the increase in enzymes was also restored. 3 Non-steroidal anti-inflammatory drugs In a series of in vitro clinical studies, Ml can increase the concentration of plasma free diclofenac and ibuprofen by 13% to 50%, and the clinical significance of this is still unclear. However, in clinical trials, many cases of simultaneous use of non-steroidal drugs have been observed, and no special effects have been found. 4 In a series of clinical studies, it was found that M1 can increase the plasma free tolbutamide concentration by 13% to 50%, but the clinical significance is still unclear. 5 When single-dose leflunomide and multiple-dose rifampicin are used together, the peak concentration of M1 is higher (about 40%) than when leflunomide is used alone. Since the concentration of M1 may continue to increase with the use of rifampicin, caution should be exercised when the two drugs are used together.

Sealed, light-proof, and stored in a cool and dry place.

10 mg

(1) 10 mg for 36 months (2) 20 mg for 24 months

Suzhou Changzheng-xinkai Pharmaceutical Co., Ltd.

• Founded in:

  2000-04-27

• Address:

  No. 567, Liufeng Road, Hedong Industrial Park, Wuzhong Economic Development Zone, Suzhou

• Tax NO.:

  91320500720535900Q

• Registered Funds:

  38.526778 million yuan

• Email:

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