febuxostat


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febuxostat

Uloric

Pharmacologic class: Xanthine oxidase inhibitor

Therapeutic class: Antigout agent

Pregnancy risk category C

Action

Decreases serum uric acid level

Availability

Tablets: 40 mg, 80 mg

Indications and dosages

Long-term management of hyperuricemia in patients with gout

Adults: Initially, 40 mg P.O. daily; for patients who don't achieve serum uric acid level of less than 6 mg/dl after 2 weeks with 40 mg, give 80 mg P.O. daily

Contraindications

• Concomitant use of azathioprine, mercaptopurine

Precautions

Use cautiously in:
• severe hepatic or renal impairment
• patients with greatly increased rate of urate formation, such as in malignant disease and its treatment and Lesch-Nyhan syndrome (use not recommended)
• concurrent use of theophylline
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).

Administration

• Administer with or without food.

Adverse reactions

CNS: dizziness, nonfatal cerebrovascular accident (CVA)

CV: cardiovascular thromboembolic events (nonfatal myocardial infarction [MI], deaths)

GI: nausea

Hepatic: liver function abnormalities

Musculoskeletal: arthralgia

Skin: rash

Interactions

Drug-drug.Drugs metabolized by xanthine oxidase (such as azathioprine, mercaptopurine): may increase plasma concentrations of these drugs, leading to severe toxicity

Theophylline: altered theophylline metabolism

Drug-diagnostic tests.Alanine aminotransferase, aspartate aminotransferase: increased levels

Patient monitoring

Monitor patient for signs and symptoms of MI or CVA.
• Be aware that gout flares (caused by reduction in serum uric acid levels resulting in mobilization of urate from tissue deposits) may occur. To prevent such flares, provide concurrent prophylactic treatment with a non-steroidal anti-inflammatory drug or colchicine, as prescribed.
• Monitor liver function tests 2 months and 4 months after starting therapy and periodically thereafter.

Patient teaching

• Instruct patient to take drug with or without food.

Instruct patient to immediately report cardiovascular symptoms (such as shortness of breath or chest pain) or strokelike symptoms (such as headache or dizziness) to prescriber.
• Tell patient to inform prescriber of increased gout symptoms or rash.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

febuxostat

(fe-bux-o-stat) ,

Uloric

(trade name)

Classification

Therapeutic: antigout agents
Pharmacologic: xanthine oxidase inhibitors
Pregnancy Category: C

Indications

Chronic management of hyperuricemia in patients with a history of gout.

Action

Decreases production of uric acid by inhibiting xanthine oxidase.

Therapeutic effects

Lowering of serum uric acid levels with resultant decrease in gouty attacks.

Pharmacokinetics

Absorption: Well absorbed (49%) following oral administration.
Distribution: Unknown.
Protein Binding: 99.2%.
Metabolism and Excretion: Extensively metabolized by the liver; minimal renal excretion of unchanged drug, 45% eliminated in feces as unchanged drug, remainder is eliminated in urine and feces as inactive metabolites.
Half-life: 5–8 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POrapid1–1.5 hr*24 hr
*Maximum lowering of uric acid may take 2 wk

Contraindications/Precautions

Contraindicated in: Concurrent azathioprine or mercaptopurine.
Use Cautiously in: Severe renal impairment (CCr <30 mL/min);Severe hepatic impairment; Obstetric: Use only when potential maternal benefit outweighs potential fetal risk; Lactation: Unknown if excreted into breast milk; use caution when breast feeding; Pediatric: Safety in children <18 yr not established.

Adverse Reactions/Side Effects

Gastrointestinal

  • ↑ liver function tests
  • nausea

Dermatologic

  • rash

Musculoskeletal

  • gout flare
  • arthralgia

Interactions

Drug-Drug interaction

Significantly ↑ levels of and risk of serious toxicity from azathioprine and mercaptopurine ; concurrent use is contraindicated.May ↑ levels of theophylline ; use cautiously together.

Route/Dosage

Oral (Adults) 40 mg once daily initially; if serum uric acid does not ↓ to <6 mg/dL, dose should be ↑ to 80 mg once daily.

Availability

Tablets: 40 mg, 80 mg

Nursing implications

Nursing assessment

  • Assess for joint pain and swelling, especially during early therapy. Changing serum uric acid levels from mobilization of urate from tissue deposits may cause gout flares. Use prophylactic NSAID or colchicine therapy for up to 6 mo. If a gout flare occurs, continue febuxostat therapy and treat flare concurrently.
  • Monitor for signs and symptoms of MI and stroke.
  • Lab Test Considerations: Monitor serum uric acid levels prior to, 2 wk after intitiating, and periodically thereafter. If serum uric acid levels are ≥6 mg/dL after 2 wk of daily 40 mg therapy, increase dose to 80 mg daily.
    • Monitor liver function at 2 and 4 mo of therapy and periodically thereafter. May cause ↑ AST, ALT, CPK, LDH, alkaline phosphatase, and creatine.
    • May cause prolonged aPTT and PT, and ↓ hematocrit, hemoglobin, RBC, platelet count, and lymphocyte, neutrohpil counts. May cause ↑ or ↓ WBC.
    • May cause ↓ serum bicarbonate and ↑ serum sodium, glucose, potassium, and TSH levels.
    • May cause ↑ serum cholesterol, triglycerides, amylase, and LDL levels.
    • May cause ↑ BUN and serum creatinine and proteinuria.

Potential Nursing Diagnoses

Chronic pain (Indications)

Implementation

  • Oral: May be taken with or without food and with antacids.

Patient/Family Teaching

  • Instruct patient to take febuxostat as directed. If a gout flare occurs, continue febuxostat and consult health care professional; medications to manage gout flare may be added.
  • Advise patient to notify health care professional if rash, chest pain, shortness of breath, or stroke symptoms (weakness, headache, confusion, slurred speech) occur or if side effects are persistent or bothersome.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products.
  • Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.
  • Emphasize the importance of follow-up lab tests to monitor therapy.

Evaluation/Desired Outcomes

  • Reduction in serum uric acid levels and resultant gout attacks.

febuxostat

A non-purine selective inhibitor of xanthine oxidase that has been tested as an alternative to allopurinol in patients with GOUT and HYPERURICAEMIA.
References in periodicals archive ?
The journal Arthritis & Rheumatology recently reported that the drug febuxostat reduced gout attacks in a double-blind, placebo-controlled study of 314 adults with early gout.
Two medications that prevent the production of uric acid are allopurinol (Zyloprim) and febuxostat (Uloric).
THE URATE-LOWERING THERAPY febuxostat may have a higher risk of heart-related death than does another urate-lowering drug, allopurinol, according to a safety alert from the Food and Drug Administration.
For the study, 110 people with elevated uric acid received one of the following: a placebo, 40 mg daily of the uric-acid lowering drug febuxostat, 500 mg of T.
Other medications, such as allopurinol (Zyloprim) or febuxostat (Uloric), reduce the amount of uric acid produced.
Lesinurad is currently approved under the brand name Zurampic by the FDA and needs to be administered in combination with a xanthine oxidase inhibitor (XOI) like allopurinol or febuxostat for treating hyperuricemia in gout patients who do not achieve the target serum uric acid (sUA) level when treated with a XOI alone.
Among patients with early gout --those experiencing their first gout flare or a second flare that occurred more than 1 year after their first flare--the risk for one or more gout flares during the course of the study was 41% in the placebo group and 29% in the group of patients given febuxostat, a statistically significant difference (P = .
Surgery was recommended, but the patient refused to undergo surgery and chose to receive febuxostat.
This randomized, double-blind, placebo-controlled study evaluated the effects of Ayuric, a natural xanthine oxidase inhibitor, and the prescription gout medication febuxostat on uric acid levels in subjects with hyperuricemia.