Home Drug Guide Leflunomide

Drug Guide

Generic Name

Leflunomide

Brand Names Arava

Classification

Therapeutic: Disease-modifying antirheumatic drug (DMARD)

Pharmacological: Immunomodulator

FDA Approved Indications

  • Rheumatoid arthritis

Mechanism of Action

Inhibits pyrimidine synthesis by irreversibly blocking dihydroorotate dehydrogenase, leading to suppression of T-cell proliferation and reduction of inflammatory responses.

Dosage and Administration

Adult: Initially 100 mg once daily for 3 days, then 20 mg once daily.

Pediatric: Not approved for pediatric use.

Geriatric: Adjust dose based on renal and hepatic function; start at lower doses if necessary.

Renal Impairment: Use with caution; dosage adjustments may be necessary.

Hepatic Impairment: Use with caution; contraindicated if severe hepatic impairment.

Pharmacokinetics

Absorption: Well absorbed orally.

Distribution: Widely distributed, protein bound (about 99%).

Metabolism: Primarily hepatic via CYP enzymes.

Excretion: Fecal excretion predominantly; minimal renal excretion.

Half Life: Approximate half-life is 14-18 days, leading to accumulation.

Contraindications

  • Pregnancy, women of childbearing potential not using contraception
  • Severe hepatic impairment

Precautions

  • Liver function should be monitored periodically.
  • Patients should use reliable contraception during and for 2 years after therapy due to teratogenicity.
  • Immunosuppressive effects; increased infection risk.
  • Risk of lymphoma and other malignancies.

Adverse Reactions - Common

  • Diarrhea (Frequent)
  • Transaminitis (elevated liver enzymes) (Common)
  • Alopecia (Common)
  • Nausea (Common)

Adverse Reactions - Serious

  • Hepatotoxicity (Less common but serious)
  • Myelosuppression (neutropenia, thrombocytopenia, anemia) (Less common)
  • Severe infections (Less common)
  • Interstitial lung disease (Rare)

Drug-Drug Interactions

  • Methotrexate (increased risk of hepatotoxicity and myelosuppression)
  • Chloramphenicol (risk of bone marrow suppression)

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor liver function tests, complete blood count, and renal function regularly.

Diagnoses:

  • Risk for infection
  • Impaired skin integrity

Implementation: Advise patients to avoid live vaccines; counsel on contraception; monitor for adverse effects.

Evaluation: Evaluate for signs of hepatotoxicity, infection, and hematologic abnormalities.

Patient/Family Teaching

  • Do not become pregnant during therapy and for 2 years after discontinuation.
  • Report signs of infection, unusual bleeding, or jaundice.
  • Avoid live vaccines during therapy.
  • Take medication exactly as prescribed, even if feeling well.

Special Considerations

Black Box Warnings:

  • Embryo-fetal toxicity; contraindicated during pregnancy and for women trying to conceive.
  • Severe liver injury.

Genetic Factors: Some populations may have differences in metabolism affecting drug levels.

Lab Test Interference: May cause elevated liver enzymes, which should be interpreted carefully.

Overdose Management

Signs/Symptoms: Gastrointestinal symptoms, leukopenia, elevated liver enzymes.

Treatment: Supportive care; activated charcoal if ingestion is recent; possibly administering cholestyramine to reduce absorption.

Storage and Handling

Storage: Store at room temperature, away from moisture and light.

Stability: Stable for the duration of the shelf life as indicated by manufacturer.

🛡️ 5 Critical Medication Safety Tips for Nurses

1

Triple-Check High-Risk Medications

Always have another nurse verify insulin, heparin, warfarin, and chemotherapy drugs. These "high-alert" medications cause the most serious errors. Check concentration, dose calculation, and pump settings twice.

2

Know Look-Alike, Sound-Alike Drugs

Common mix-ups: hydromorphone/morphine, Celebrex/Celexa, Zyprexa/Zyrtec. Always use BOTH generic and brand names, read labels twice, and use barcode scanning when available. One wrong letter can be fatal.

3

Assess Before AND After Giving Meds

Check vitals before cardiac meds, pain levels before analgesics, and blood glucose before insulin. Always reassess within 30 minutes to evaluate effectiveness and watch for adverse reactions.

4

Watch for Drug Interactions

Common dangerous combinations: warfarin + aspirin (bleeding), ACE inhibitors + potassium (hyperkalemia), digoxin + diuretics (toxicity). Always check drug interactions before administering new medications.

5

Educate Your Patients

Teach patients medication names, purposes, major side effects, and what to report. Informed patients catch errors and improve compliance. Always encourage questions - an educated patient is a safer patient.

⚡ Remember: When in doubt, don't give it out! It's always safer to double-check than regret later.

⚠️ Medical Disclaimer

This drug guide is for educational purposes only and is NOT intended for clinical use. Always consult current prescribing information, healthcare providers, and institutional protocols before administering any medication. Do not use this information for patient care decisions.