| Customization: | Available |
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| Transport Package: | Drum |
| Specification: | 99% |
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Leflunomide, marketed under the brand name Arava, is a disease-modifying antirheumatic drug (DMARD) used to treat the symptoms of rheumatoid arthritis (RA). It is also used for the prevention of acute and chronic rejection in recipients of solid organ transplants. Leflunomide is a pyrimidine synthesis inhibitor that works by inhibiting the enzyme dihydroorotate dehydrogenase (DHODH), which is involved in the de novo synthesis of pyrimidines. This inhibition affects the proliferation of activated lymphocytes, which are crucial in the autoimmune response seen in conditions like RA.
The drug is well absorbed, with peak plasma concentrations appearing 6-12 hours after dosing. It has a volume of distribution of approximately 0.13 L/kg and is highly protein-bound (>99.3%). Leflunomide is metabolized primarily in the liver and has a half-life of about two weeks. The active metabolite is eliminated through renal excretion and biliary excretion.
Leflunomide is typically initiated with a loading dose of 100 mg per day for three days, followed by a maintenance dose of 20 mg per day. However, if the drug is not well tolerated, the maintenance dose may be decreased to 10 mg per day. It is important to monitor blood pressure, blood cells, and liver function regularly during treatment with leflunomide.
Common side effects of leflunomide may include nausea, diarrhea, stomach pain, headache, abnormal liver function tests, thinning hair, back pain, weakness, rash, and high blood pressure. More serious side effects can occur, such as signs of infection, liver problems, and severe skin reactions. Leflunomide can also cause severe or fatal liver damage, and its use is contraindicated in patients with severe liver disease or those who are pregnant, as it may harm an unborn baby.
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