Leflunomide review

Leflunomide is part of the DMARD class – also known as the disease-modifying antirheumatic drugs. It is a pyrimidine synthesis inhibitor that is both pharmacologically and chemically heterogeneous. It is available in tablet preparations of 10, 20, or 100 mg.

An immunomodulatory drug, Leflunomide inhibits the enzyme known as dihydroorotate dehydrogenase. Previous clinical studies have proven the actual anti-proliferative capabilities of the medication. In addition, a number of experimental models have revealed an anti-inflammatory consequence. The dual effects of Leflunomide are presumed to decelerate the progression of rheumatoid or psoriatic arthritis and to bring about relief/remission of symptoms.

Leflunomide is typically administered as a 20 mg tablet once daily. However, some patients may be prescribed with 10 mg, particularly if they come across side effects along with higher doses of the drug. Time and again, doctors provide a loading dose to be administered when the drug is initially prescribed.

Leflunomide’s loading dose is commonly 100 mg given only once in week for three consecutive weeks over and above the regular daily dosage. Then again, some doctors will prescribe a loading dose of 100 mg per day for the first three days of treatment. Although this approach augments the likelihood of diarrhea, this side effect generally fade away after fulfilling the loading dosage.

Leflunomide is preferably taken with food or milk. It is also vital to take the drug on a regular basis in order to get the best possible benefit. Your physician may also require you to have your blood tested and undergo other health evaluations whilst taking the drug so as to monitor progress and detect any untoward effects.

Partly due to its mechanism of action, Leflunomide may have a number of precautions and contraindications. Since the drug can bring down the immune system’s activity level, taking it can make you more vulnerable to infections. For that reason, you need to avoid making contact with individuals who have contagious illnesses such as the flu or colds.

Alcohol intake alongside Leflunomide treatment can be detrimental to the liver. Consequently, patients with pre-existing conditions of the kidneys or liver and diseases involving the immune system or bone marrow rule out the use of Leflunomide.

Considerable precaution should be observed by women of childbearing age who are not using any contraceptive methods. Pregnancy – either pre-existing or within two years after cessation of Leflunomide treatment – is also contraindicated. On the other hand, male patients who wish to have kids should stop taking the drug after consulting with a doctor. Both men and women are also expected to undergo a wash-out procedure prior to conceiving a baby.

You have to discontinue taking Leflunomide as soon as you notice any of the following severe side effects: an allergic reaction (swelling of the face, lips or tongue; hives; difficulty breathing), changes in the functioning of the liver (jaundice, dark urine, pale stools, fatigue, abdominal pain), dwindled bone marrow function (easy bleeding or bruising, bloody or tarry stools, signs of infection, fever or chills), mouth sores, and skin rash. You also need to seek immediate medical attention the moment the untoward reactions appear.

Less severe side effects, however, are more likely to come about compared to the serious ones. You may continue taking the drug even if you experience any of the following symptoms: increased blood pressure, headache, muscle aches, diarrhea, hair loss, or nausea. Remember to promptly report the occurrence of such reactions to your physician so that the progress of the treatment may be monitored and evaluated.

Leflunomide has the following structural formula:

Chemical structure of leflunomide

• Molecular formula of leflunomide is C12H9F3N2O2
• Chemical IUPAC Name is 5-methyl-N-[4-(trifluoromethyl)phenyl]-oxazole-4-carboxamide
• Molecular weight is 270.207 g/mol
Leflunomide available : 10mg tablets, 20mg tablets

Brand name(s): Arava, Leflunomidum, Lefunomide

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