Class: Agent for gout
- Injection, solution, concentrate 8 mg/mL
Uric acid–specific enzyme (recombinant uricase) that catalyzes the oxidation of uric acid to allantoin, thereby lowering serum uric acid.
Following single IV infusions of 0.5 to 12 mg, max serum concentrations increased in proportion to the administered dose.
Special PopulationsRenal Function Impairment
No formal pharmacokinetic studies were conducted to examine the effects of renal impairment.Hepatic Function Impairment
No formal pharmacokinetic studies were conducted to examine the effects of hepatic impairment.Elderly
Age did not influence the pharmacokinetics of pegloticase.Children
Pharmacokinetics have not been studied in children and adolescents.Gender
Gender did not influence the pharmacokinetics of pegloticase.Weight
Pharmacokinetics of pegloticase were not influenced by weight.
Indications and Usage
For the treatment of chronic gout in adults who are refractory to conventional therapy.
Glucose-6-phosphate dehydrogenase (G6PD) deficiency.
Dosage and AdministrationAdults
IV 8 mg every 2 wk.
- Administer by IV infusion over no less than 120 min via gravity feed, syringe-type pump, or infusion pump.
- Do not administer as an IV push or bolus.
- For dilution, withdraw 1 mL from vial and inject into a single 250 mL bag of sodium chloride 0.9% injection or sodium chloride 0.45% injection for IV infusion. Invert infusion bag several times to ensure mixing. Do not shake.
- Before administration, allow the diluted solution to reach room temperature.
- Visually inspect solution for particulate matter and discoloration before administration, whenever solution and container permit. Do not use vials if either is present.
- Premedicate with antihistamines and corticosteroids prior to administration to reduce the incidence of anaphylaxis and infusion reactions.
- If an infusion reaction occurs during administration, the infusion may be slowed or stopped and restarted at a slower rate.
- Discard any unused portion of product remaining in vial.
- Do not mix or dilute with other drugs.
Store vials in the carton and keep under refrigeration, between 36° and 46°F. Protect from light. Do not shake or freeze. Diluted solution in infusion bags is stable for 4 h at 36° to 46°F and at room temperature (68° to 77°F); however, it is recommended that the diluted solution be stored under refrigeration, not frozen, protected from light, and used within 4 h of dilution.
None well documented.
Nausea (12%); constipation (6%); vomiting (5%).
Gout flare (81%); infusion reaction (26%); contusion or ecchymosis (11%); chest pain (6%).
Anaphylaxis and infusion reactions have been reported to occur during and after administration of pegloticase.
Anaphylaxis may occur with any infusion, including a first infusion, and generally manifests within 2 h of the infusion. However, delayed-type hypersensitivity reactions have also been reported.
Premedicated patients with antihistamines and corticosteroids.
Monitor serum uric acid levels prior to infusions and consider discontinuing treatment if levels increase to above 6 mg/dL, particularly when 2 consecutive levels above 6 mg/dL are observed. Closely monitor patients for an appropriate period of time for anaphylaxis after administration of pegloticase.
Category C .
Safety and efficacy not established.
No dosage adjustment is required.
No dosage adjustment is required.
Cases of CHF exacerbation have been reported. Use with caution and monitor patients closely following infusion.
Contraindicated in patients with G6PD deficiency because of the risk of hemolysis and methemoglobinemia. Screen patients at higher risk of G6PD deficiency (eg, patients of African or Mediterranean ancestry) for G6PD deficiency before starting therapy.
Gout flares may occur and are frequently observed upon initiation of antihyperuricemic therapy.
High antibody titer was associated with a higher incidence of infusion reactions and failure to maintain pegloticase-induced normalization of uric acid.
Because of the immunogenicity of pegloticase, patients receiving re-treatment may be at increased risk of anaphylaxis and infusion reactions. Carefully monitor patients receiving re-treatment after a drug-free interval.
No cases of overdose have been reported.
- Advise patients taking pegloticase to read the Medication Guide before use for the first time and with each subsequent treatment.
- Inform patients that anaphylaxis and infusion reactions can occur at any infusion while on therapy. Counsel patients on the importance of adhering to any prescribed medications to help prevent or lessen the severity of these reactions.
- Educate patients on the signs and symptoms of anaphylaxis, including hemodynamic instability, perioral or lingual edema, rash or urticaria, and wheezing.
- Educate patients on the most common signs and symptoms of an infusion reaction, including chest discomfort, chest pain, dyspnea, erythema, flushing, rash, and urticaria.
- Advise patients to seek medical care immediately if they experience any symptoms of an allergic reaction during or at any time after the infusion.
- Inform patients not to take the medication if they have a condition known as G6PD deficiency and that they may need to be tested to determine if they have G6PD deficiency, unless already known.
- Explain to patients that gout flares may initially increase when starting treatment and that medications to help reduce flares may need to be taken regularly for the first few months after pegloticase is started.
- Advise patients that they should not stop pegloticase therapy if they have a flare.
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