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).

Leflunomide

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

1. Suitable for adult rheumatoid arthritis, and has the effect of improving the condition. 2. Lupus nephritis.

(1) Adult rheumatoid arthritis: Oral administration. 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 the data of foreign clinical trials and combining 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. Non-steroidal anti-inflammatory drugs or low-dose corticosteroids can continue to be used during the treatment with this drug. (2) Lupus nephritis: Oral administration. Choose an appropriate dose according to the condition. The recommended dose is once a day, 20 to 40 mg at a time, and the dose can be appropriately reduced after the condition improves. It can be used in combination with glucocorticoids, or as prescribed by a doctor.

For the treatment of rheumatoid arthritis: mainly diarrhea, itching, reversible liver enzymes (elevated ALT and AST, hair loss, rash, etc. In foreign clinical trials, adverse events with an incidence of ≥ 3% in 1,339 patients with rheumatoid arthritis treated with leflunomide included: fatigue, abdominal pain, back pain, hypertension, anorexia, diarrhea, indigestion, gastroenteritis, elevated liver enzymes, 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 which diarrhea, elevated liver enzymes, hair loss, and rash were more common in the leflunomide-treated group.

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 yet taken reliable contraceptive measures and lactating women are prohibited from using this product. Precautions for the elderly:

According to literature reports: (1) Cholestyramine and activated carbon: 13 patients and 96 volunteers were given cholestyramine or activated carbon, and the plasma Ml concentration decreased rapidly. (2) The hepatotoxic drug leflunomide and other hepatotoxic drugs may increase adverse reactions when used together. It should also be considered that even if leflunomide treatment is interrupted, continuing to take these drugs without taking drug elimination measures may also increase adverse reactions. In a small sample (30 cases) study of the combined use of leflunomide and MTX, 5 cases showed a 2- to 3-fold 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, among 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 plasma free diclofenac and ibuprofen concentrations 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 Ml 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 Ml is higher (about 40%) than when leflunomide is used alone. Since the concentration of Ml may continue to increase with the use of rifampicin, caution should be exercised when the two drugs are used together.

Protect from light, seal tightly and store in a dry place.

20 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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