Simulect

basiliximab

Simulect

Pharmacologic class: Monoclonal antibody

Therapeutic class: Immunosuppressant

Pregnancy risk category B

FDA Box Warning

• Give under supervision of physician experienced in immunosuppressive therapy and management of organ transplant recipients, in facility with adequate diagnostic and treatment resources.

Action

Blocks specific interleukin-2 (IL-2) receptor sites on activated T lymphocytes. Specific binding competitively inhibits IL-2-mediated activation and differentiation of lymphocytes responsible for cell-mediated immunity. Also impairs immunologic response to antigenic challenges.

Availability

Powder for injection: 10 mg, 20 mg in single-use vials

Indications and dosages

Prevention of acute organ rejection in kidney transplantation

Adults and children weighing 35 kg (77 lb) or more: 20 mg I.V. 2 hours before transplantation surgery, then 20 mg I.V. 4 days after surgery. Withhold second dose if complications, hyper-sensitivity reaction, or graft loss occurs.

Children weighing less than 35 kg (77 lb): 10 mg I.V. 2 hours before transplantation surgery, then 10 mg I.V. 4 days after surgery. Withhold second dose if complications, hypersensitivity reaction, or graft loss occurs.

Contraindications

• Hypersensitivity to drug

• Pregnancy or breastfeeding

Precautions

Use cautiously in:

• elderly patients

• females of childbearing age.

Administration

Give by central or peripheral I.V. route only.

• Reconstitute by adding 5 ml of sterile water for injection to vial for bolus injection, or dilute with normal saline solution or dextrose 5% in water to a volume of 50 ml and infuse over 20 to 30 minutes. Discard any remaining product after preparing each dose.

• Don't infuse other drugs simultaneously through same I.V. line.

• Know that drug should be used only as part of regimen that includes cyclosporine and corticosteroids.

Adverse reactions

CNS: headache, insomnia, paresthesia, dizziness, drowsiness, tremor, anxiety, confusion, coma, seizures

CV: palpitations, edema, chest pain, ECG abnormalities, hypotension, hypertension, prolonged QT interval

EENT: blurred vision, eye irritation, tinnitus, earache, epistaxis, nasopharyngitis, sinusitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia, oral blisters, oral candidiasis, GI hemorrhage

GU: urinary incontinence, intermenstrual bleeding, oliguria, renal failure

Hematologic: anemia, disseminated intravascular coagulation, hemorrhage, neutropenia, thrombocytopenia Metabolic: hypokalemia, hypomagnesemia, hyperglycemia, acidosis, hypoglycemia, hyperkalemia

Musculoskeletal: bone, back, neck, or limb pain

Respiratory: dyspnea, cough, hypoxia, tachypnea, hemoptysis, upper respiratory tract infection, pleural effusions

Skin: bruising, pruritus, dermatitis, skin lesions, diaphoresis, night sweats, erythema, hyperpigmentation, urticaria

Other: fever, lymphadenopathy, facial edema, bacterial infection, herpes simplex infection, injection site erythema, hypersensitivity reaction, sepsis

Interactions

Drug-drug. Immunosuppressants: additive immunosuppression

Drug-diagnostic tests. Calcium, glucose, potassium: increased or decreased levels

Hemoglobin, neutrophils, platelets: decreased values

Triglycerides: increased levels

White blood cells: decreased levels

Drug-herbs. Astragalus, echinacea, melatonin: interference with immunosuppressant action

Patient monitoring

Watch for signs and symptoms of hypersensitivity reaction. Keep emergency drugs at hand in case these occur.

• Monitor vital signs and observe patient frequently during I.V. infusion.

• Monitor laboratory values and drug blood level.

Patient teaching

• Teach patient about purpose of therapy. Explain that drug decreases the risk of acute organ rejection.

• Tell patient he may be more susceptible to infection because of drug's immunosuppressant effect.

• Inform patient that he'll need lifelong immunosuppressant drug therapy.

• Advise women of childbearing age to use reliable contraception before, during, and for 2 months after therapy.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

basiliximab

(ba-sil-ix-i-mab) ,

Simulect

(trade name)

Classification

Therapeutic: immunosuppressants
Pharmacologic: monoclonal antibodies
Pregnancy Category: B

Indications

Prevention of acute organ rejection in patients undergoing renal transplantation; used with corticosteroids and cyclosporine.

Action

Binds to and blocks specific interleukin-2 (IL-2) receptor sites on activated T lymphocytes.

Therapeutic effects

Prevention of acute organ rejection following renal transplantation.

Pharmacokinetics

Absorption: IV administration results in complete bioavailability.
Distribution: Unknown.
Metabolism and Excretion: Unknown.
Half-life: 7.2 days.

Time/action profile (effect on immune function)

ROUTEONSETPEAKDURATION
IV2 hrunknown36 days

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Obstetric: May affect fetal developing immune system; Lactation: May enter breast milk.
Use Cautiously in: Women with childbearing potential; Geriatric: Due to greater incidence of infection.

Adverse Reactions/Side Effects

Noted for patients receiving corticosteroids and cyclosporine in addition to basiliximab

Central nervous system

  • dizziness (most frequent)
  • headache (most frequent)
  • insomnia (most frequent)
  • weakness (most frequent)

Ear, Eye, Nose, Throat

  • abnormal vision
  • cataracts

Respiratory

  • coughing (most frequent)

Cardiovascular

  • heart failure (life-threatening)
  • edema (most frequent)
  • hypertension (most frequent)
  • angina
  • arrhythmias
  • hypotension

Gastrointestinal

  • abdominal pain (most frequent)
  • constipation (most frequent)
  • diarrhea (most frequent)
  • dyspepsia (most frequent)
  • moniliasis (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • GI bleeding
  • gingival hyperplasia
  • stomatitis

Dermatologic

  • acne (most frequent)
  • wound complications (most frequent)
  • hypertrichosis
  • pruritus

Endocrinologic

  • hyperglycemia (most frequent)
  • hypoglycemia (most frequent)

Fluid and Electrolyte

  • acidosis (most frequent)
  • hypercholesterolemia (most frequent)
  • hyperkalemia (most frequent)
  • hyperuricemia (most frequent)
  • hypocalcemia (most frequent)
  • hypokalemia (most frequent)
  • hypophosphatemia (most frequent)

Hematologic

  • bleeding
  • coagulation abnormalities

Musculoskeletal

  • back pain (most frequent)
  • leg pain (most frequent)

Neurologic

  • tremor (most frequent)
  • neuropathy
  • paresthesia

Miscellaneous

  • hypersensitivity reactions including anaphylaxis (life-threatening)
  • infection (most frequent)
  • weight gain (most frequent)
  • chills

Interactions

Drug-Drug interaction

Immunosuppression may be ↑ with other immunosuppressants.Concommitant use with echinacea and melatonin may interfere with immunosuppression.

Route/Dosage

Intravenous (Adults and Children ≥35 kg) 20 mg given 2 hr before transplantation; repeated 4 days after transplantation. Second dose should be withheld if complications or graft loss occurs.
Intravenous (Children <35 kg) 10 mg given 2 hr before transplantation; repeated 4 days after transplantation. Second dose should be withheld if complication or graft loss occurs.

Availability

Powder for reconstitution: 20 mg/vial, 10 mg/vial

Nursing implications

Nursing assessment

  • Monitor for signs of anaphylactic or hypersensitivity reactions (hypotension, tachycardia, cardiac failure, dyspnea, wheezing, bronchospasm, pulmonary edema, respiratory failure, urticaria, rash, pruritus, sneezing) at each dose. Onset of symptoms is usually within 24 hr. Resuscitation equipment and medications for treatment of severe hypersensitivity should be readily available. If a severe hypersensitivity reaction occurs, basiliximab therapy should be permanently discontinued. Patients who have previously received basiliximab should only receive subsequent therapy with extreme caution.
  • Monitor for infection (fever, chills, rash, sore throat, purulent discharge, dysuria). Notify physician immediately if these symptoms occur; may necessitate discontinuation of therapy.
  • Lab Test Considerations: May cause ↑ or ↓ hemoglobin, hematocrit, serum glucose, potassium, and calcium concentrations.
    • May cause ↑ serum cholesterol levels.
    • May cause ↑ BUN, serum creatinine, and uric acid concentrations.
    • May cause ↓ serum magnesium, phosphate, and platelet levels.

Potential Nursing Diagnoses

Risk for infection (Side Effects)

Implementation

  • Intravenous Administration
  • pH: Near Neutrality.
  • Basiliximab is usually administered concurrently with cyclosporine and corticosteroids.
    • Reconstitute with 2.5 mL or 5 mL of sterile water for injection for the 10 mg or 20 mg vial, respectively. Shake gently to dissolve powder.
  • Diluent: May be administered undiluted. Bolus administration may be associated with nausea, vomiting, and local reactions (pain).Concentration: 4 mg/mL.
  • Rate: Administer over 20–30 min via peripheral or central line.
  • Intermittent Infusion: Diluent: Dilute further with 25–50 mL of 0.9% NaCl or D5W. Gently invert bag to mix; do not shake, to avoid foaming. Solution is clear to opalescent and colorless; do not administer solutions that are discolored or contain particulate matter. Discard unused portion. Administer within 4 hr or may be refrigerated for up to 24 hr. Discard after 24 hr.Concentration: 0.08–0.16 mg/mL.
  • Rate: Administer over 20–30 min via peripheral or central line.
  • Additive Incompatibility: Do not admix; do not administer in IV line containing other medications.

Patient/Family Teaching

  • Explain purpose of medication to patient. Explain that patient will need to resume lifelong therapy with other immunosuppressive drugs after completion of basiliximab course.
  • May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response is known.
  • Instruct patient to continue to avoid crowds and persons with known infections, because basiliximab also suppresses the immune system.

Evaluation/Desired Outcomes

  • Prevention of acute organ rejection in patients receiving renal transplantation.

basiliximab

A high-affinity, mouse–human chimeric monoclonal antibody raised against the alpha chain (CD25) of the IL-2 receptor on T cells. It is used to prevent or minimise the rejection of transplanted solid organs, and meant to complement other drugs.

Simulect®

Basiliximab, see there.
References in periodicals archive ?
He received Simulect [R], an antibody to the interleukin-2 soluble receptor as an induction agent, as well as standard triple drug immunosuppression therapy based on tacrolimus, MMF, and prednisone.
Basiliximab (Simulect), a chimeric mouse-human monoclonal antibody, blocks the cellular receptor for the cytokine interleukin-2.
Basiliximab (Simulect) is a chimeric mouse-human monoclonal antibody that blocks the cellular receptor for the cytokine interleukin 2.
SangStat, Inc., Fremont, CA announced that an ad hoc independent Data Safety Monitoring Board (DSMB) decided to close the company's comparative kidney transplant study early after an interim analysis revealed significantly fewer rejections in patients treated the Thymoglobulin [Anti-thymocyte globulin, (Rabbit)] versus Novartis' Pharmaceutical's, East Hanover, NJ, Simulect (basiliximab).
Effect of "C2" cyclosporine levels and time to initiation of cyclosporine therapy on outcomes in patients receiving Neoral and Simulect [Abstract].
Novartis Pharmaceuticals, Inc., East Hanover, NJ, announced that severe acute hypersensitivity reactions, including anaphylaxis, have occurred in 17 patients receiving basiliximab (Simulect), a drug administered intravenously as a prophylaxis to prevent transplant rejection.
Novartis Pharma, AG, Basel, Switzerland, announced the scientific Body of the European Medicines Evaluation Agency, the Committee for Proprietary Medicinal Products (CPMP) has recommended extending the label for Simulect (basiliximab), a monoclonal antibody to prevent acute rejection in transplantation.
A multicenter pilot study of early (4 day) steroid cessation in renal transplant recipients under simulect, tacrolimus and sirolimus.
Novartis Pharmaceuticals, Inc., East Hanover, NJ, announced the Food and Drug Administration (FDA) has granted marketing clearance for Simulect (basiliximab) for prevention of acute rejections episodes in renal transplant recipients.
* MMF, Zenapax-MMF, Rapamycin-MMF, Myfortic in place of MMF, Simulect in place of Zenapax
The only Basiliximab product approved to be sold in China is Simulect, the brand-name drug by Novartis.
Patients in the BAS group received induction therapy with basiliximab (Simulect; Novartis, Basel, Switzerland) 20mg intravenously on day 0 intraoperatively after allograft reperfusion and on day 4 after LT.