Febuxostat Brand Name– Uloric
What is Febuxostat
Febuxostat is an oral, non-purine selective xanthine oxidase inhibitor (XOI).
Febuxostat does not require a dosage adjustment in patients with mild to moderate renal impairment and appears less likely than allopurinol to cause serious hypersensitivity.
Febuxostat shares with allopurinol an increased risk of gout flare during therapy initiation, which necessitates the concurrent use of colchicine, NSAIDs, or corticosteroids for prophylaxis against acute gout attacks.
A boxed warning in the product label warns about a potential increase in cardiovascular death versus allopurinol. Gout patients with established cardiovascular (CV) disease treated with febuxostat had a higher rate of cardiovascular (CV) death compared to those treated with allopurinol in a CV outcomes study.
Because of the increased risk of CV death, febuxostat should only be used in patients who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom allopurinol treatment is not advisable.
Unlike allopurinol, febuxostat has not been studied in patients with secondary hyperuricemia.
Like other chronic gout treatments, the drug is not recommended in patients with asymptomatic hyperuricemia. For chronic gout management, the American College of Rheumatology (ACR) and the European League Against Rheumatism (EULAR) guidelines recommend ULT to achieve a target serum uric acid (sUA) level of less than 6 mg/dL to prevent the formation of crystals and to eliminate crystal deposition, thereby dissolving tophi.
A lower target (less than 5 mg/dL) is recommended for patients with severe disease.
Allopurinol is usually the first-line treatment agent due to effectiveness and cost considerations unless contraindications exist.
Allopurinol and febuxostat appear relatively similar in lowering serum urate concentrations and reducing gout flares with long-term (more than 1 year) of monotherapy use.
Treatment guidelines recommend combination therapy with a uricosuric (e.g., lesinurad) plus a xanthine oxidase inhibitor (XOI) when treatment goals are not met with an XOI alone.
The use of pegloticase is usually reserved for severe, refractory chronic gout.
Indications
- gout
- gouty arthritis
- hyperuricemia
For the chronic management of hyperuricemia in patients with gout (gouty arthritis)
Side Effects
- abdominal pain
- agitation
- alopecia
- anaphylactoid reactions
- anemia
- angina
- angioedema
- anorexia
- anxiety
- appetite stimulation
- arthralgia
- asthenia
- atrial fibrillation
- atrial flutter
- AV block
- blurred vision
- bradycardia
- chest pain (unspecified)
- cholecystitis
- cholelithiasis
- constipation
- cough
- dehydration
- depression
- diabetes mellitus
- diarrhea
- dizziness
- Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
- dysgeusia
- dyspepsia
- dyspnea
- ecchymosis
- edema
- elevated hepatic enzymes
- epistaxis
- erythema multiforme
- fatigue
- flatulence
- flushing
- gastritis
- gastroesophageal reflux
- gout
- Guillain-Barre syndrome
- gynecomastia
- headache
- hematemesis
- hematuria
- hepatic failure
- hepatitis
- hepatomegaly
- hyperamylasemia
- hypercholesterolemia
- hyperglycemia
- hyperhidrosis
- hyperkalemia
- hyperlipidemia
- hypernatremia
- hypertension
- hypertriglyceridemia
- hypoesthesia
- hypokalemia
- hypotension
- impotence (erectile dysfunction)
- infection
- insomnia
- interstitial nephritis
- irritability
- lethargy
- leukocytosis
- leukopenia
- libido decrease
- lymphopenia
- migraine
- musculoskeletal pain
- myalgia
- myocardial infarction
- nasal congestion
- nasal dryness
- nausea
- nephrolithiasis
- neutropenia
- oral ulceration
- palpitations
- pancreatitis
- pancytopenia
- paresthesias
- peptic ulcer
- petechiae
- photosensitivity
- polyuria
- proteinuria
- pruritus
- psychosis
- purpura
- pyuria
- rash
- renal failure (unspecified)
- rhabdomyolysis
- sinus tachycardia
- skin discoloration
- sneezing
- splenomegaly
- steatosis
- Stevens-Johnson syndrome
- stroke
- throat irritation
- thrombocytopenia
- thromboembolism
- tinnitus
- toxic epidermal necrolysis
- tremor
- urinary incontinence
- urinary urgency
- urticaria
- vertigo
- vomiting
- weakness
- weight gain
- weight loss
- xerostomia
Monitoring Parameters
- LFTs
- serum uric acid
Contraindications
- breast-feeding
- cardiac disease
- chemotherapy
- dialysis
- hepatic disease
- Lesch-Nyhan syndrome
- mortality
- myocardial infarction
- neoplastic disease
- pregnancy
- renal failure
- renal impairment
- secondary hyperuricemia
- serious rash
- stroke
Interactions
- Alkylating agents
- Antimetabolites
- Antitumor antibiotics
- Azathioprine
- Carmustine, BCNU
- Chlorambucil
- Cladribine
- Clofarabine
- Cyclophosphamide
- Estramustine
- Fludarabine
- Folate analogs
- Lomustine, CCNU
- Melphalan
- Mercaptopurine, 6-MP
- Mitoxantrone
- Natural Antineoplastics
- Nelarabine
- Pegloticase
- Theophylline, Aminophylline
- Thioguanine, 6-TG
