LEFLUNOMIDE

LEFLUNOMIDE
(le-flu'no-mide)
Arava
Classifications: biologic response modifier; immunomodulator; antiinflammatory;
Therapeutic: disease-modifying antirheumatic drug (dmard)

Pregnancy Category: X

Availability

10 mg, 20 mg, 100 mg tablets

Action

An immunomodulator that demonstrates antiinflammatory effects. Suppression of pyrimidine synthesis in T and B lymphocytes interferes with RNA and protein synthesis in cells that are involved in the inflammatory process within affected joints. Reduction in activity of these lymphocytes leads to reduced cytokine and antibody-mediated destruction of the synovial joints as well as attenuation of the inflammatory process.

Therapeutic Effect

Reduces the S&S of rheumatoid arthritis (RA), retards structural joint damage, and improves physical function.

Uses

Active RA.

Contraindications

Hepatic disease; jaundice; lactase deficiency; hypersensitivity to leflunomide; patients with positive hepatitis B or C serology; malignancy, particularly lymphoproliferative disorders; severe immunosuppression; vaccination, infants; uncontrolled infection; pregnancy (category X), lactation.

Cautious Use

Renal insufficiency; renal failure; alcoholism; immunosuppression; lactase deficiency; infection. Use in patients <18 y has not been fully studied.

Route & Dosage

Rheumatoid Arthritis
Adult: PO Initiate with a loading dose of 100 mg/d x 3 d, then maintenance dose of 20 mg q.d., may decrease to 10 mg/d if higher dose is not tolerated

Administration

Oral
  • Initiate with a 3-d loading dose followed by a lower maintenance dose.

Adverse Effects (≥1%)

Body as a Whole: Allergic reaction, asthenia, flu-like syndrome, infection, pain, back pain, arthralgia, leg cramps, synovitis, tenosynovitis. CNS: Dizziness, headache, paresthesias, peripheral neuropathy. CV: Hypertension, chest pain. GI: Diarrhea, increased LFTs (ALT and AST), abdominal pain, anorexia, dyspepsia, gastroenteritis, nausea, mouth ulcer, vomiting, weight loss, hepatotoxicity. Metabolic: Hypokalemia. Respiratory: Bronchitis, cough, respiratory infection, pharyngitis, pneumonia, rhinitis, sinusitis. Skin: Rash, alopecia, eczema, pruritus, dry skin, Stevens-Johnson syndrome, toxic epidermal necrolysis (rare). Urogenital: UTI.

Interactions

Drug: Rifampin may significantly increase leflunomide levels; cholestyramine, charcoal decrease absorption; caution should be used with other hepatotoxic drugs.

Pharmacokinetics

Absorption: Approximately 80% reaches systemic circulation. Peak: 6–12 h for active metabolite. Distribution: >99% protein bound. Metabolism: Metabolized primarily to M1 (active metabolite). Elimination: 43% in urine, 48% in feces. Half-Life: 19 d for active metabolite.

Nursing Implications

Assessment & Drug Effects

  • Lab tests: Baseline screening to rule out hepatitis B or C; baseline and monthly liver enzymes x 12 mo, then every 6 mo thereafter.
  • Monitor carefully for and report immediately S&S of infection; withhold leflunomide if infection is suspected.
  • Monitor BP and weight periodically. Doses greater than 25 mg/d are associated with a greater incidence of side effects such as alopecia, weight loss, and elevated liver enzymes.

Patient & Family Education

  • Use reliable contraception while taking leflunomide.
  • Note: Both women and men need to discontinue leflunomide and undergo a drug elimination procedure prescribed by the physician BEFORE conception.
  • Withhold drug if you develop an infection and notify the physician before resuming the drug.
  • Notify physician about any of the following: hair loss, weight loss, GI distress, rash, or itching.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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