Leflunomide Pharmacology


About Leflunomide
A pyrimidine synthesis inhibitor, Isoxazole derivative, Disease-modifying Antirheumatic Drug.
Mechanism of Action of Leflunomide
This immunomodulatory drug inhibits dihydroorotate dehydrogenase (an enzyme involved in de novo pyrimidine synthesis) (abbreviation DHODH). It also has anti-inflammatory effect. This double action is slow progression of the disease and to cause remission/relief of symptoms of rheumatoid arthritis and psoriatic arthritis such as joint tenderness and decreased joint and general mobility in human patients.
Pharmacokinets of Leflunomide
Absorption- Well absorbed after oral administration.
Distribution- The active metabolite of drug is widely distributed in the body and extensively (99.3%) binds to the plasma proteins.
Metabolism- Metabolized in the plasma after oral administration into its active metabolites . Then it is metabolized in the liver to its inactive metabolites.
Excretion- Excreted through urine and feces.
Onset of Action for Leflunomide
Duration of Action for Leflunomide
Half Life of Leflunomide
Side Effects of Leflunomide
1. Diarrhea
2. Hair loss
3. Headache
4. Dizziness
5. Upset stomach
6. Vomiting
7. Stomach pain
8. Loss of appetite
9. Weight loss
10. Mouth sores
11. Runny nose
13. Back pain
14. Dry or itchy skin
15. Muscle pain or weakness
16. Flu-like symptoms
17. Urinary tract infection
18. Rash
19. Difficulty breathing
20. Chest pain
21. Increased heart rate
Contra-indications of Leflunomide
1. Hypersensitivity to the drug
2. Immunodeficiency
3. Hypopriteinemia
Special Precautions while taking Leflunomide
1. Blood problems
2. Disease of the immune system
3. Infections
4. Liver disease
5. Renal disease
6. History of TB
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Use with caution
Indications for Leflunomide
1. Rheumatoid arthritis
2. Psoriatic arthritis
Interactions for Leflunomide
Cholesturamine, charcoal: Co-administration with lefulnomide results in rapid and significant decrease in lefulnomide activity.
Rifampicin: Co-administration increases lefulnomide plasma levels.
Hepatotoxic drugs: Co-administration may increase side effects.
NSAIDs: Lefulnomide causes an increase in the free fraction of diclofenac and ibuprofen.
Tolbutamide: Lefulnomide causes increase in the free fraction of tolbutamide.
Typical Dosage for Leflunomide
For rheumatoid arthritis - First, 100 mg once a day for three days, then 20 mg once a day.
Schedule of Leflunomide
Storage Requirements for Leflunomide
Store it at room temperature and away from excess heat and moisture. Keep out of the reach of children.
Effects of Missed Dosage of Leflunomide
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Leflunomide
Give symptomatic and supportive treatment. Administer activated charcoal to reduce the further absorption of drug.

Home Delivery for Leflunomide in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including leflunomide.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for leflunomide and other medicines and health products. Home delivery services for leflunomide may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take leflunomide only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for leflunomide before they complete the sale. You can get this information while placing the order for leflunomide with the pharmacy.

Leflunomide is a generic medicine name and there are several brands available for it. Some of the brands for leflunomide might be better known than leflunomide itself. If the pharmacy that's willing to deliver medicines to your home doesn't have leflunomide in stock, you can ask for one of the branded alternatives for leflunomide.