Leflunomide Tablets

Leflunomide 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 vivo and in vitro tests have shown that this product has anti-inflammatory effects. The in vivo activity of leflunomide is mainly produced through its active metabolite A771726 (hereinafter referred to as M1).

The main ingredient of this product is leflunomide.

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

It is suitable for adults with rheumatoid arthritis and has the effect of improving the condition.

1. Due to the long half-life of leflunomide, it is recommended to take the drug every 24 hours. 2. In order to quickly reach a steady-state blood concentration, referring to the 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. Non-steroidal anti-inflammatory drugs or low-dose corticosteroids can continue to be used during the treatment of this drug.

The main symptoms are: decreased white blood cell count, itching, decreased appetite, fatigue, dizziness, diarrhea, mild liver damage, rash and nausea. When similar drugs were tested in phase III clinical trials abroad, 1-3% of patients experienced the following adverse reactions: systemic: abscesses, cysts, fever, neck pain, discomfort and pelvic pain; cardiovascular: angina, migraine, palpitations, tachycardia, varicose veins, vasculitis and vasodilation; digestive system: gallstones, colitis, constipation, esophagitis, flatulence, black stools, pharyngitis, salivary gland hypertrophy, gingivitis, stomatitis and irregular teeth; endocrine: diabetes and hyperthyroidism; blood and lymphatic system: anemia (iron deficiency anemia) and purpura; metabolism and nutrition: increased creatine phosphokinase activity, hyperglycemia and hyperlipidemia; musculoskeletal system: arthritis, bone Necrosis, bone pain, bursitis and muscle spasm; Respiratory system: pulmonary discomfort, asthma, dyspnea and epistaxis; Nervous system: anxiety, depression, dry mouth, insomnia, neuralgia, neuritis, sleep disturbance, sweating and vertigo; Skin and appendages: acne, contact dermatitis, fungal dermatitis, hair discoloration, herpes simplex, herpes zoster, maculopapular rash, nail abnormalities, skin discoloration, skin paresthesia, skin nodules, subcutaneous nodules and skin ulcers; Urogenital system: proteinuria, hematuria, cystitis, dysuria, prostatitis and urinary frequency, menstrual disorders, vaginal candidiasis; Sensory system: blurred vision, cataracts, eye discomfort, conjunctivitis, taste perversion.

1. People who are allergic to leflunomide and its metabolites; 2. Pregnant women and women of childbearing age and breastfeeding women who have not yet taken reliable contraceptive measures.

Precautions for children: The efficacy and safety of this product for children have not been studied, so it is recommended that patients under the age of 18 do not use this product. Precautions for pregnancy and lactation: Leflunomide is reproductively toxic and can cause embryo damage. When mice were given 15 mg/kg of leflunomide, the sperm deformity rate of male mice increased significantly, the rate of absorbed and dead embryos of female mice increased, and the rate of live embryos decreased. Therefore, it is contraindicated for pregnant and lactating women. It is contraindicated for women of childbearing age who may become pregnant. Precautions for the elderly: It is not clear yet.

1. When volunteers and patients took cholestyramine or activated charcoal, the level of M1 in the blood decreased significantly. 2. When the hepatotoxic drug leflunomide is used in combination with hepatotoxic drugs, adverse reactions are enhanced. If hepatotoxic drugs are taken without drug elimination after leflunomide treatment, adverse reactions will also be enhanced. Among the 30 patients who used leflunomide and methotrexate in combination, 5 patients had a 2-3 times increase in transaminase, of which 2 continued to use the combined drug and the other 3 stopped leflunomide; in the other 5 patients whose transaminase increased more than 3 times, 2 continued to use the combined drug and the other 3 stopped leflunomide. At the end of the study, the transaminase of 10 patients returned to normal. All patients met the ACR liver biopsy criteria. 3. In vitro tests of non-steroidal antipyretic analgesics showed that M1 could increase the concentration of free diclofenac and ibuprofen by 13-50%. However, in clinical trials, no adverse reactions were enhanced when non-steroidal antipyretic analgesics were used in combination with leflunomide. 4. Tolbutamide in vitro tests show that M1 can increase the concentration of free tolbutamide by 13-50%, and the clinical significance is unclear. 5. Rifampicin The combined use of multiple doses of rifampicin and a single dose of leflunomide increases the free M1 in the blood by 40% compared with the use of leflunomide alone. With the use of rifampicin, the concentration of M1 may continue to increase. Therefore, caution should be exercised when leflunomide and rifampicin are used in combination.

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

(1) 5 mg; (2) 10 mg; (3) 20 mg.

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

Fujian Huitian Biological Pharmacy Co., Ltd.

• Founded in:

  1999-12-22

• Address:

  No. 46, Taijiang Road, Sanyuan District, Sanming City, Fujian Province

• Tax NO.:

  91350400155582666R

• Registered Funds:

  200 million yuan

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