Names and pronunciation
(leh-floo′noh-mide) Arava
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Individual generic drug information
Extracted information for leflunomide only.
(leh-floo′noh-mide) Arava
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Func. class.: Antirheumatic (DMARDs)
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Chem. class.: Immune modulator, pyrimidine synthesis inhibitor
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ACTION: Inhibits an enzyme involved in pyrimidine synthesis; has antiprolifer- ative, antiinflammatory effect
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USES: RA: to reduce disease process and symptoms
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Unlabeled uses: Juvenile RA, BK virus (viremia or nephropathy; in kidney trans- plant), cytomegalovirus disease (in trans- plant patients resistant to standard antivirals)
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Extracted information for leflunomide only.
CONTRAINDICATIONS: Breast- feeding, hypersensitivity
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Black Box Warning: Pregnancy Precautions: Children, renal disorders, vaccinations, infection, alcoholism, immunosuppression, jaundice, lactase deficiency, hepatic disease L Black Box Warning: Hepatic disease (ALT >2 × ULN) Black Box Warning: Hepatic necrosis/ failure: monitor LFTs, if ALT elevations are >2 × baseline, reduce dose to 10 mg/ day; monitor monthly or more frequently • CBC with differential monthly × 6 mo, then q6-8wk thereafter; pregnancy test; serum electrolytes • Infections: fatal infections can occur • Hypertension: B/P, weight; edema can occur • Stevens-Johnson syndrome, toxic epi- dermal necrolysis: monitor for rash during treatment; if rash with fever, fatigue, joint aches, blisters is present, discontinue im mediately, initiate drug elimination procedure Black Box Warning: Pregnancy: determine that patient is not pregnant before treatment; not to be given to women of childbearing potential who are not using reliable contra- ception, not to use in males who could po- tentially father a child, use barrier protection during therapy and up to 2 yr after last dose Black Box Warning: Pregnancy/breast- feeding: not to become pregnant while taking this product; not to breastfeed while taking this product; men should also discontinue product and begin leflunomide removal protocol if pregnancy is planned HIGH ALERT
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SIDE EFFECTS CNS: Headache, dizziness, insomnia, depression, paresthesia, anxiety, migraine, neuralgia CV: Palpitations, hypertension, chest pain, angina pectoris, peripheral edema EENT: Pharyngitis, oral candidiasis, sto- matitis, dry mouth, blurred vision GI: Nausea, anorexia, vomiting, con- stipation, flatulence, diarrhea, elevated LFTs, hepatotoxicity, weight loss HEMA: Anemia, ecchymosis, hyperlipid- emia INTEG: Rash, pruritus, alopecia, acne, hematoma, herpes infections RESP: Pharyngitis, rhinitis, bronchitis, cough, respiratory infection, pneumonia, sinusitis, interstitial lung disease SYST: Opportunistic/fatal infections, Stevens-Johnson syndrome, toxic epider mal necrolysis, DRESS
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INTERACTIONS Increase: NSAID effect—NSAIDs Increase: hepatotoxicity—hepatotoxic agents, methotrexate Increase: leflunomide levels—rifampin Increase: bleeding risk—warfarin Decrease: antibody response—live virus vaccines Decrease: leflunomide effect—chole- styramine, use for overdose
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Extracted information for leflunomide only.
DOSAGE AND ROUTES Rheumatoid arthritis • Adult: PO Loading dose 100 mg/day × 3 days, maintenance 20 mg/day; may be de- creased to 10 mg/day if not well tolerated Juvenile rheumatoid arthritis (unlabeled) • Adolescent/child >40 kg: PO 20 mg/day • Adolescent/child 20-40 kg: PO 15 mg/day • Adolescent/child 10-19.9 kg: PO 10 mg/day
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Available forms: Tabs 10, 20 mg
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Administer: • With food for GI upset, give same time each day, loading dose is recom- mended • Drug elimination: give cholestyramine 8 g tid × 11 days; check levels
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Extracted information for leflunomide only.
Assess: • Arthritic symptoms: ROM, mobility, swelling of joints at baseline and during treatment • Screen for latent TB before starting treatment; if TB is present, pretreat be- fore using product • Interstitial lung disease: increased or worsening cough, SOB, fever; prod uct may need to be discontinued and drug elimination procedure initiated (rare)
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Evaluate: • Therapeutic response: decreased in- flammation, pain in joints
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That continuing monitoring will be needed • That product must be continued for prescribed time to be effective, that up to a month may be required for im- provement, that other treatment may continue corticosteroids, NSAIDs • To take with food, milk, or antacids to avoid GI upset; to take at same time of day • To use caution when driving because drowsiness, dizziness may occur • To take with a full glass of water to enhance absorption, may continue with correct prescribed treatment with other antiinflammatories • To discuss with health care professional all Rx, OTC, herbals, supplements used • That hair may be lost; review alternatives • To avoid live virus vaccinations during treatment • To notify prescriber of weight loss • Overdose treatment: give cholestyr- amine 8 g tid × 11 days
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Extracted information for leflunomide only.
PHARMACOKINETICS Metabolized in liver to active metabolite, half-life of metabolite 2 wk, excreted in urine, protein binding, 99%, crosses pla- centa, onset 99 min, peak up to 6 min of RA effect
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Filter the extracted dose blocks for this individual drug.
Rheumatoid arthritis
• Adolescent/child >40 kg: PO 20 mg/day
Candidate age grouping · source page 763
Rheumatoid arthritis
• Adolescent/child 20-40 kg: PO 15 mg/day
Candidate age grouping · source page 763
Rheumatoid arthritis
• Adolescent/child 10-19.9 kg: PO 10 mg/day
Candidate age grouping · source page 763