Class: Musculoskeletal System
Dosage Form: Tablets
Description: For rheumatoid arthritis
Manufacturer: Eva Pharma
Lefulonomide……………20 or 100 mg
Arthfree (leflunomide) is an isoxazole immuno-modulatory agent, which inhibits dihydroorotate dehydrogenase (an enzyme involved in de novo pyrimidine synthesis of the cells involved in the pathogenesis of rheumatoid arthritis) and has antiproliferative and anti-inflammatory effects. Through that Arthfree is suitable for patients with rheumatoid arthritis where it:
- Reduces signs and symptoms of rheumatoid arthritis in the form of reducing the pain, tenderness, inflammation, edema and swelling of the joints, as well as, decreasing morning stiffness
- Inhibits structural damages of the cartilage and joints through decreasing erosions of joints and joint space narrowing
- Improves the physical function of the patients manifested by improvement in the patient ability to perform daily activity such as dressing, arising, eating, walking, hygiene, reach and grip
Arthfree is metabolized, following oral administration, to an active metabolite, which is responsible for essentially all of its activity. The peak level of the active metabolite of Arthfree, occurs between 6 – 12 hours after oral dosing and it is extensively bound (>99.3%) to albumin. This active metabolite is eliminated by further metabolism and subsequent renal excretion as well as by direct biliary excretion.
Arthfree (leflunomide) effects are usually evident by 1 month, stabilized by 3 – 6 months, and continued throughout the course of treatment.
Arthfree is indicated for the treatment of rheumatoid arthritis.
Arthfree is contraindicated in :
- Hypersensitivity to lefulonomide
- Pregnancy and lactation
- Not recommended for patients less than 18 years
The following interactions are to be noted:
- Co-administration of Arthfree with rifampicin increases peak level of the active metabolite of lefulonomide
- Co-administration of Arthfree with hepatotoxic drugs (methotrexate) increases the risk of hepatotoxicity
- Co-administration of cholestyramine & charcoal with lefulonomide result in a rapid and significant decrease in plasma M1 (the active metabolite)
- In vitro studies, M1 was shown to cause increases ranging from 13% to 50% in the free fraction of diclofenac, ibuprofen & tolbutamide in the clinical range.
Dosage and Administration:
It is recommended to initiate therapy with a loading dose of one Arthfree 100 mg tablets once per day for 3 days followed by a maintenance daily dose of one tablet of Arthfree 20 mg tablets once daily.
If dosing at 20 mg/day is not well tolerated clinically, the dose may be decreased to 10 mg daily.
Therapy with lefulonomide might be associated in some cases with mild elevation in liver enzymes (2-fold) and this elevation returns to normal with continuation of therapy. However if the elevation is too high or if levels of liver enzymes are not normalized along therapy, especially in case of concomitant administration of other drugs that affect the liver, dosage adjustment or discontinuation of therapy is advisable. In most of the cases, it is preferable to have a baseline measure for the liver enzymes levels
Caution should be taken when lefulonomide is administered to patients with renal insufficiency. The use of lefulonomide in patients with hepatic insufficiency is not recommended.
Arthfree 20 mg tablets: Box of 1 to 3 strips, each of 10 tablets.
Arthfree 100 mg tablets: Box of 1 strip of 3 tablets.
Store at room temperature, below 25°C.