HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use Rapamune safely and effectively.
See full prescribing information for Rapamune.
RAPAMUNE (sirolimus) ORAL SOLUTION AND TABLETS
Initial U.S. Approval: 1999
WARNING: IMMUNOSUPPRESSION, EXCESS MORTALITY IN DE NOVO LIVER TRANSPLANTATION, AND BRONCHIAL ANASTOMOTIC DEHISCENCE
See Full Prescribing Information for complete Boxed Warning.
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Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression (5.1). Only physicians experienced in immunosuppressive therapy and management of renal transplant patients should use Rapamune.
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The safety and efficacy of Rapamune as immunosuppressive therapy have not been established in de novo liver or lung transplant patients, and therefore, such use is not recommended (5.2, 5.3).
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– Liver Transplantation – Excess mortality, graft loss, and hepatic artery thrombosis (5.2).
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– Lung Transplantation– Bronchial anastomotic dehiscence (5.3).
RECENT MAJOR CHANGES
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Indications and Usage
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Patients at high-immunologic risk (1.1)
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1/2007
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Dosing and Administration
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Tablet administration (2)
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Therapeutic drug monitoring (2.3)
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Patients with hepatic impairment (2.5)
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10/2007
3/2008
3/2008
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Warnings and Precautions
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Increased Susceptibility to Infection and the Possible Development of Lymphoma (5.1)
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Angioedema (5.5)
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Proteinuria (5.9)
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Fluid Accumulation and Wound Healing (5.6)
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10/2007
1/2007
6/2007
10/2007
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Adverse Reactions
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Conversion from Calcineurin Inhibitors to Rapamune in Maintenance Renal Transplant Population (6.4)
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10/2007
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Postmarketing Experience (6.6)
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10/2007
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INDICATIONS AND USAGE
Rapamune is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients aged ≥13 years receiving renal transplants.
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Patients at low- to moderate-immunologic risk: Use initially with cyclosporine (CsA) and corticosteroids. CsA withdrawal is recommended 2-4 months after transplantation (1.1).
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Patients at high-immunologic risk: Use in combination with cyclosporine and corticosteroids for the first 12 months following transplantation (1.1). Safety and efficacy of CsA withdrawal has not been established in high risk patients (1.1, 1.2, 14.3).
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Therapeutic drug monitoring is recommended for all patients (2.3, 5.14).
DOSAGE AND ADMINISTRATION
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Take once daily by mouth, consistently with or without food. Take the initial dose as soon as possible after transplantation and 4 hours after CsA (2, 7.1). Adjust the Rapamune maintenance dose to achieve sirolimus trough concentrations within the target-range (2.3).
Patients at low- to moderate-immunologic risk
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Rapamune and Cyclosporine Combination Therapy: One loading dose of 6 mg on day 1, followed by daily maintenance doses of 2 mg (2.1).
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Rapamune Following Cyclosporine Withdrawal: 2-4 months post-transplantation, withdraw CsA over 4-8 weeks (2.2).
Patients at high-immunologic risk
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Rapamune and Cyclosporine Combination Therapy (for the first 12 months post-transplantation): One loading dose of up to 15 mg on day 1, followed by daily maintenance doses of 5 mg (2.2).
DOSAGE FORMS AND STRENGTHS
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Rapamune Oral Solution: 60 mg per 60 mL in amber glass bottle (3.1).
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Rapamune Tablets: 1 mg, white; 2 mg, yellow-to-beige (3.2).
CONTRAINDICATIONS
Hypersensitivity to Rapamune (4).
WARNINGS AND PRECAUTIONS
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Hypersensitivity Reactions (5.4)
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Angioedema (5.5)
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Fluid Accumulation and Wound Healing (5.6)
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Hyperlipidemia (5.7)
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Renal Function (5.8)
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Proteinuria (5.9)
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Interstitial Lung Disease (5.10)
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De Novo Use Without Cyclosporine (5.11)
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Increased Risk of Calcineurin Inhibitor-induced HUS/TTP/TMA (5.12)
ADVERSE REACTIONS
The most common (> 30%) adverse reactions are: peripheral edema, hypertriglyceridemia, hypertension, hypercholesterolemia, creatinine increased, abdominal pain, diarrhea, headache, fever, urinary tract infection, anemia, nausea, arthralgia, pain, and thrombocytopenia (6).
To report SUSPECTED ADVERSE REACTIONS, contact Wyeth Pharmaceuticals Inc. at 1-800-934-5556 or FD |
