DrugindexOnline^{2nd edition}

Pronouncation: (oh-PRELL-veh-kin)
Class: Interleukin

Trade Names:
Neumega
- Powder for injection 5 mg

Mechanism of Action

Pharmacology

Interleukin 11 (IL-11) is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation, resulting in increased platelet production.

Pharmacokinetics

Absorption

C _max is 17.4 ng/mL. T _max is 3.2 hr.

Distribution

The bioavailability is more than 80%.

Elimination

Renal. The t _½ (terminal) is 6.9 hrs.

Special Populations

Renal Function Impairment

C _max was 2.2-fold higher. AUC was 2.6-fold higher. Clearance was approximately 40% of the value seen in normal renal patients.

Elderly

Clearance decreases with age.

Children

Clearance increases approximately 1.2- to 1.6-fold in infants and children.

Indications and Usage

Prevent severe thrombocytopenia and reduce the need for platelet transfusions following myelosuppressive chemotherapy in patients with nonmyeloid malignancies.

Contraindications

Standard considerations.

Dosage and Administration

Prevent Severe Thrombocytopenia and Reduce the Need for Platelet Transfusions Following Myelosuppressive Chemotherapy in Patients with Nonmyeloid Malignancies
Adults

SC 50 mcg/kg once daily, starting 6 to 24 hr after completing chemotherapy. Continue therapy until the postnadir platelet count is at least 50,000/mm ³ or for a maximum of 21 days. Discontinue oprelvekin at least 2 days before starting the next chemotherapy cycle.

Storage/Stability

Store powder for injection and diluent in refrigerator (36° to 46°F). Protect from light and freezing. Use reconstituted solution within 3 hr of reconstitution and store vial in refrigerator or controlled room temperature (at or below 77°F). Do not freeze or shake reconstituted solution.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Plasma volume expansion; symptomatic atrial arrhythmias, syncope, tachycardia, peripheral edema.

CNS

Headache, fatigue, dizziness.

Dermatologic

Transient rash at injection site.

EENT

Transient visual blurring, papilledema.

GI

Nausea; vomiting; mucositis; diarrhea; oral moniliasis.

Hematologic

Dilutional anemia.

Metabolic

Weight gain.

Respiratory

Dyspnea, rhinitis; increased cough; pharyngitis; pleural effusion.

Miscellaneous

Edema; neutropenic fever; fever.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Fluid retention

Oprelvekin is known to cause fluid retention; use with caution in patients with clinically evident CHF, patients who may be susceptible to developing CHF, and patients with a history of heart failure. Patients have commonly experienced mild to moderate fluid retention as indicated by peripheral edema or dyspnea on exertion. Monitor preexisting fluid collections, including pericardial effusions or ascites. Sudden deaths have occurred in oprelvekin-treated patients receiving chronic diuretic therapy and ifosfamide who developed severe hypokalemia.

Cardiovascular events

Use with caution in patients with a history of atrial arrhythmia. Transient atrial arrhythmias (atrial fibrillation or flutter) have occurred in approximately 10% of patients following treatment with oprelvekin.

Ophthalmologic events

Transient, mild visual blurring has occasionally been reported.

Antibody formation/allergic reactions

A small proportion (1%) of patients developed antibodies to oprelvekin and transient rashes were occasionally observed at the injection site.

Chronic administration

Oprelvekin has been administered safely using the recommended dosing schedule for no more than 6 cycles following chemotherapy. Continuous dosing (2 to 13 wk) in primates produced joint capsule, tendon fibrosis, and periosteal hyperostosis.

Chemotherapy

The safety and efficacy of administering oprelvekin before or concurrently with chemotherapy has not been evaluated.

Overdosage

Symptoms

Doses of oprelvekin more than 50 mcg/kg may be associated with an increased incidence of cardiovascular events in adult patients.

Patient Information

• Instruct people who will be administering oprelvekin as to the proper dose and the method for reconstituting and administering oprelvekin. Instruct patients in the importance of proper disposal and caution against the reuse of needles, syringes, drug product, and diluent.
• Inform patients of the most common adverse reactions associated with oprelvekin administration, including those symptoms related to fluid retention. Mild to moderate peripheral edema and shortness of breath on exertion can occur within the first week of treatment and may continue for the duration of administration. Advise patients who have preexisting pleural or other effusions or a history of CHF to contact their health care provider if dyspnea worsens.
• Most patients who receive oprelvekin develop some anemia.
• Contact health care provider if symptoms attributable to atrial arrhythmia develop and are not transient.
• Advise women of childbearing potential of the possible risks of oprelvekin to the fetus.