Basiliximab

Trade Names:Simulect- Powder for injection 20 mg

Pharmacology

Blocks the interleukin-2 receptor α-chain, which is a critical pathway in allograft rejection.

Pharmacokinetics

Absorption

C _max is about 7.1 mg/L (20 mg IV over 30 min).

Distribution

Vd is about 8.6 L.

Elimination

The t _½ is about 7.2 days. Cl is about 41 mL/h.

Special Populations

Distribution volume and Cl are reduced about 50% compared with adult renal transplant patients.

Indications and Usage

Prophylaxis of acute organ rejection in patients receiving renal transplantation when used as part of an immunosuppressive regimen that includes cyclosporine and corticosteroids.

Contraindications

Standard considerations.

Dosage and Administration

IV 20 mg within 2 h prior to transplantation surgery, followed by 20 mg 4 days after transplantation. Withhold second dose if complications such as severe hypersensitivity reactions to basiliximab or graft rejection occur.

IV 10 mg within 2 h prior to transplantation surgery, followed by 10 mg 4 days after transplantation. Withhold second dose if complications such as severe hypersensitivity reactions to basiliximab or graft rejection occur.

IV 20 mg within 2 h prior to transplantation surgery, followed by 20 mg 4 days after transplantation. Withhold second dose if complications such as severe hypersensitivity reactions to basiliximab or graft rejection occur.

General Advice

• Inspect the bag for particulate matter or solution discoloration; do not use if present.
• Do not shake solution; invert bag gently to avoid foaming.
• Administer diluted solution through central or peripheral IV only over 20 to 30 min using sterile technique.

Storage/Stability

Store lyophilized basiliximab under refrigerated conditions at 2° to 8°C (36° to 46°F). The reconstituted solution can be refrigerated for 24 h or at room temperature for 4 h. Discard reconstituted solution if not used in 24 h. Use the reconstituted solution immediately and dilute as directed.

Drug Interactions

None well documented.

Incompatibility

No data available; do not add or infuse other drugs simultaneously through the same IV line.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension; hypotension; angina pectoris; cardiac failure; abnormal heart sounds; arrhythmia; atrial fibrillation; tachycardia; vascular disorder.

CNS

Headache; tremor; dizziness; insomnia; hypoesthesia; neuropathy; paresthesia; agitation; anxiety; depression; fatigue; malaise.

Dermatologic

Acne; surgical wound complications; cyst; herpes simplex; herpes zoster; hypertrichosis; pruritus; rash; skin ulceration.

GI

Constipation; nausea; diarrhea; abdominal pain; vomiting; dyspepsia; moniliasis; enlarged abdomen; flatulence; gastroenteritis; GI hemorrhage; gum hyperplasia; melena; esophagitis; ulcerative stomatitis.

Genitourinary

Dysuria; UTI; increased nonprotein nitrogen; impotence; genital edema; albuminuria; bladder disorder; hematuria; frequent micturition; oliguria; abnormal renal function; renal tubular necrosis; ureteral disorder; urinary retention.

Hematologic

Anemia; hemorrhage; purpura; thrombocytopenia; thrombosis; polycythemia.

Metabolic-Nutritional

Hyperkalemia; hypokalemia; hyperglycemia; hypoglycemia; hyperuricemia; hypomagnesemia; hypophosphatemia; hypocalcemia; hypercholesterolemia; hyperlipidemia; hyperproteinemia; weight gain; acidosis; dehydration; diabetes mellitus; fluid overload.

Respiratory

Dyspnea; upper respiratory tract infection; coughing; rhinitis; pharyngitis; bronchitis; bronchospasm; abnormal chest sounds; pneumonia; pulmonary disorder; pulmonary edema.

Special Senses

Cataracts; conjunctivitis; abnormal vision; sinusitis.

Miscellaneous

Pain; chest pain; leg pain; back pain; asthenia; arthralgia; arthropathy; bone fracture; cramps; hernia; myalgia; hematoma; edema; peripheral edema; facial edema.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Safety and efficacy not established.

Hypersensitivity

Although not reported, can occur following administration of proteins.

Opportunistic infections/lymphoproliferative disorders

Risk of developing these complications may be increased.

Patient Information

• Instruct patient or family to monitor for signs and symptoms of adverse reactions and report immediately to primary health care provider.
• Instruct family or patient to monitor for signs and symptoms of infections and transplant rejection including fever, pain, and UTIs. Report these symptoms immediately to primary care provider.
• Instruct women of childbearing potential to use effective contraception before beginning therapy, during therapy, and for 2 mo after the completion of therapy.
• Nursing mothers should discontinue nursing prior to using the drug.
• Stress the importance of regular exams and laboratory work.
• Encourage patient to comply with the treatment regimen.

Copyright © 2009 Wolters Kluwer Health.