le-FLU-noe-mide
le-FLU-noe-mide
Therapeutic Classification: antirheumatics (DMARDs)
Pharmacologic Classification: immune response modifiers, pyrimidine synthesis inhibitors
Absorption: 80% absorbed following oral administration.
Distribution: Well distributed to tissues.
Protein Binding: 99%.
Half-Life: 14–18 days.
(antirheumatic effect)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO | 1 mo | 3–6 mo | wk–mos‡ |
‡Due to persistence of active metabolite.
Contraindicated in:
Severe hepatic impairment, pre-existing acute or chronic liver disease, or ALT >2 times upper limit of normal (ULN)
;Pregnancy
;Use Cautiously in:
Women of reproductive potential
;Exercise Extreme Caution in:
CV: chest pain, hypertension
Derm: alopecia, rash, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), dry skin, eczema, pruritus, skin ulcers, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)
EENT: pharyngitis, rhinitis, sinusitis
F and E: hypokalemia
GI: diarrhea, nausea, ↑liver enzymes, abdominal pain, anorexia, dyspepsia, gastroenteritis, HEPATOTOXICITY, mouth ulcers, vomiting
MS: arthralgia, back pain, joint disorder, leg cramps, synovitis, tenosynovitis
Neuro: headache, dizziness, paresthesia, peripheral neuropathy, weakness
Resp: bronchitis, cough, ILD, pneumonia
Misc: INFECTION (INCLUDING SEPSIS AND TUBERCULOSIS [TB] REACTIVATION)
Drug-drug:
Methotrexate and other hepatotoxic drugs↑ risk of hepatotoxicity.
Lab Test Considerations:
Verify negative pregnancy test before starting therapy.
Monitor liver function throughout therapy. Assess ALT at baseline, then monthly during initial 6 mo of therapy, then every 6–8 wk. If given concurrently with methotrexate, monitor ALT, AST, and serum albumin monthly. May ↑ ALT and AST, which are usually reversible with ↓ in dose or discontinuation, but may be fatal. If ALT is 2–3 times ULN,↓ dose to 10 mg once daily. Monitor closely after dose ↓; plasma concentrations may not ↓ for several weeks due to long half-life. If ALT ↑ of 2–3 times ULN persists despite dose reduction or if ALT >3 times ULN occurs, discontinue leflunomide and begin accelerated drug elimination procedure (see Implementation).
May cause fetal harm. Advise women of reproductive potential to use effective contraception. If pregnancy is planned or suspected or if breastfeeding, notify health care provider immediately; an accelerated elimination procedure (see Implementation) must be used to ↓ levels more rapidly. Advise patient to avoid breastfeeding during therapy.
NDC Code