Generic
Leflunomide
3 brands available in the market
At a glance
Leflunomide is used in the treatment of rheumatoid arthritis and psoriatic arthritis. It slows down disease progression and provides relief from pain, swelling, and redness. It is an immunomodulating agent and DMARD.
Description
Leflunomide is a pyrimidine synthesis inhibitor that inhibits dihydroorotate dehydrogenase enzyme activity, resulting in antiproliferative and anti-inflammatory effects. Rheumatoid arthritis is an autoimmune disease characterized by high T-cell activity. Activated T cells use the de novo pathway for pyrimidine synthesis and are more affected by leflunomide's inhibition. After oral administration, it is rapidly metabolized to A771726, which is the active metabolite.
Indications
- Active rheumatoid arthritis (RA) - reducing signs and symptoms and structural damage
- Psoriatic arthritis
Therapeutic class
Drugs used for Rheumatoid Arthritis
Pharmacological class
Immunomodulator & DMARD
Pharmacology
Leflunomide inhibits de novo pyrimidine synthesis by inhibiting dihydroorotate dehydrogenase, which blocks activated T cell proliferation and produces anti-inflammatory effects.
Mechanism of action
Provides antiproliferative and anti-inflammatory effects by inhibiting pyrimidine synthesis.
Dosage
Adult Dose (Oral):
- Loading dose: 100 mg once daily for 3 days
- Maintenance dose: 10-20 mg once daily
- May be reduced to 10 mg daily if tolerability issues arise
Hepatic Impairment: Contraindicated
Renal Impairment: Mild: No dose adjustment; Moderate-Severe: Contraindicated
Administration
- Swallow tablet whole; do not chew, crush or break
- May be taken with or without food, but at a fixed time is preferable
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as possible. However, if it's almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Diarrhea
- Nausea
- Vomiting
- Abdominal pain
- Headache
- Respiratory infection
- Bronchitis
- Elevated liver enzymes
- Aggravation of pre-existing hypertension
- Alopecia
- Rash
Precautions & warnings
- Highly unsafe during pregnancy - avoid pregnancy
- Do not use during breastfeeding
- Monitor liver function before and during treatment
- Avoid alcohol (risk of liver damage)
- Increased risk of infection - avoid close contact with people with cold or flu
- Caution when driving or activities requiring concentration (may cause dizziness or drowsiness)
Contraindications
- Hypersensitivity to Leflunomide or its components
- Significant hepatic impairment
- Severe uncontrolled infections
- Bone marrow dysplasia
- Pregnancy and lactation
- Concurrent vaccination with live vaccines
Drug interactions
- Cholestyramine and activated charcoal decrease plasma concentration of active metabolite
- Concurrent use with methotrexate and other hepatotoxic drugs increases risk of hepatotoxicity
- Rifampicin increases serum levels of active metabolite
- May enhance adverse effects of live vaccines (potentially fatal)
Food interactions
Alcohol consumption with Leflunomide is unsafe.
Use in pregnancy
Use in Pregnancy: Leflunomide is highly unsafe during pregnancy. Studies on pregnant women and animals have shown significant harmful effects to the developing baby. Completely contraindicated.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Leflunomide is probably unsafe during breastfeeding. The drug may pass into breast milk and harm the baby. Should not be used by nursing mothers.
Pediatric use
Safety and efficacy not established in children.
Geriatric use
Use with caution in elderly; no special dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Mild: No dose adjustment; Moderate-Severe: Contraindicated.
Hepatic Impairment: Contraindicated.
Overdose effects
No human experience with overdose. In case of significant overdose or toxicity, cholestyramine or activated charcoal administration is recommended to accelerate elimination.
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Leflunomide