ULORIC Dosage & Rx Info | Uses, Side Effects

Uloric Generic Name & Formulations

Legal Class

General Description

Febuxostat 40mg, 80mg; tabs.

Pharmacological Class

Xanthine oxidase inhibitor.

How Supplied

Tabs 40mg—30, 90, 500; 80mg—30, 100, 1000

Manufacturer

Takeda Pharmaceutical Company

Mechanism of Action

Febuxostat, a xanthine oxidase inhibitor, achieves its therapeutic effect by decreasing serum uric acid. It is not expected to inhibit other enzymes involved in purine and pyrimidine synthesis and metabolism at therapeutic concentrations.

Uloric Indications

Indications

Chronic management of hyperuricemia in gout patients who have inadequate response to maximally titrated allopurinol dose, intolerant to allopurinol, or for whom allopurinol therapy is not advisable.

Limitations of Use

Not for treating asymptomatic hyperuricemia.

Uloric Dosage and Administration

Adult

≥18yrs: initially 40mg once daily. Obtain target serum uric acid levels <6mg/dL after 2 weeks of initiating therapy; if not <6mg/dL, increase to 80mg once daily. Gout flare prophylaxis, with an NSAID or colchicine, upon initiation of therapy and for up to 6 months, is recommended. Severe renal impairment: max 40mg once daily.

Children

<18yrs: not established.

Uloric Contraindications

Contraindications

Concomitant azathioprine, mercaptopurine.

Uloric Boxed Warnings

Boxed Warning

Cardiovascular death.

Uloric Warnings/Precautions

Warnings/Precautions

Increased risk of cardiovascular (CV) death; reserve use (see Indications). Monitor for signs/symptoms of CV events. History of CV disease; consider prophylactic low-dose aspirin. Measure LFTs at baseline and if liver injury is suspected; interrupt therapy if ALT or AST >3xULN and investigate cause. Permanently discontinue if liver injury is confirmed without alternate etiology or if serum ALT or AST >3xULN with serum total bilirubin >2xULN without alternative etiologies; for lesser elevations, use with caution. Discontinue if serious skin reactions are suspected (eg, SJS, DRESS, TEN). Severe hepatic impairment. Severe renal impairment (see Adults) or ESRD on dialysis. Secondary hyperuricemia (eg, Lesch-Nyhan syndrome, malignant disease, or in organ transplant recipients): not recommended. Pregnancy. Nursing mothers.

Uloric Pharmacokinetics

Absorption

Maximum plasma concentrations occurred between 1 and 1.5 hours postdose.

Distribution

Mean apparent steady state volume of distribution: approximately 50 L (CV ~40%).
~99.2% serum protein bound.

Metabolism

Extensively metabolized by both conjugation via uridine diphosphate glucuronosyltransferase (UGT) enzymes including UGT1A1, UGT1A3, UGT1A9, and UGT2B7 and oxidation via CYP450 enzymes including CYP1A2, 2C8 and 2C9 and non-P450 enzymes.

Elimination

Renal, fecal.
Half-life: 5–8 hours.

Uloric Interactions

Interactions

See Contraindications. Caution with theophylline. Concomitant cytotoxic chemotherapy: no available data.

Uloric Adverse Reactions

Adverse Reactions

Abnormal LFTs, nausea, arthralgia, rash; gout flares, hepatic failure.

Uloric Clinical Trials

See Literature

Uloric Note

Not Applicable

Uloric Patient Counseling