Rapamune Oral Solution

— THERAPEUTIC CATEGORIES —
  • Miscellaneous respiratory disorders
  • Organ rejection prophylaxis
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Rapamune Oral Solution Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Sirolimus 1mg/mL; contains alcohol.

    Pharmacological Class

    Immunosuppressant.

    See Also

    How Supplied

    Tabs—100; Soln—60mL (w. oral syringe)

    Manufacturer

    Pfizer Inc.

    Rapamune Oral Solution Indications

    Indications

    Treatment of lymphangioleiomyomatosis.

    Rapamune Oral Solution Dosage and Administration

    Adult

    Tabs and oral soln are interchangeable up to 2mg. Dilute soln with water or orange juice only. Take once daily, consistently with or without food (absorption increased by high-fat meals). Swallow tabs whole. ≥18yrs: initially 2mg/day. Obtain trough level in 10–20 days; adjust dose to achieve trough concentrations between 5–15ng/mL (see full labeling). Adjust maintenance dose at 7–14 day intervals; once stable dose is achieved, monitor at least every 3 months. Hepatic impairment (mild or moderate): reduce maintenance dose by ⅓; severe: reduce maintenance dose by ½.

    Children

    <18yrs: not established.

    Rapamune Oral Solution Contraindications

    Not Applicable

    Rapamune Oral Solution Boxed Warnings

    Boxed Warning

    Immunosuppression. Use is not recommended in liver or lung transplant patients.

    Rapamune Oral Solution Warnings/Precautions

    Warnings/Precautions

    Liver or lung transplants: not recommended. Should only be used by physicians experienced in immunosuppressive therapy and organ transplant in adequately equipped facilities. Increased risk of infections, lymphomas and other malignancies (eg, skin) may result from immunosuppression. Impaired or delayed wound healing (esp. BMI >30kg/m2). Hepatic impairment. Monitor sirolimus blood concentrations (obtain trough level 3–4 days after a loading dose), renal function, lipids, urine protein and for viral infections (eg, BK virus-associated nephropathy). Antimicrobial prophylaxis for PCP and CMV: see full labeling. Avoid sun, UV light; use high protection sunscreen. Male infertility. Embryo-fetal toxicity. Pregnancy; avoid. Advise females of reproductive potential to use highly effective contraception before, during, and for 12 weeks after therapy. Nursing mothers: not recommended.

    Rapamune Oral Solution Pharmacokinetics

    See Literature

    Rapamune Oral Solution Interactions

    Interactions

    Avoid live vaccines (eg, MMR, polio, BCG, others). Potentiated by cyclosporine, separate dose by 4 hours; increase sirolimus dose after cyclosporine withdrawal. Increased risk of angioedema with ACE-inhibitors. Potentiated by CYP3A4 and/or P-glycoprotein inhibitors (eg, bromocriptine, cisapride, cimetidine, clotrimazole, danazol, diltiazem, fluconazole, letermovir, protease inhibitors, metoclopramide, nicardipine, troleandomycin, verapamil); avoid strong inhibitors (eg, ketoconazole, voriconazole, itraconazole, erythromycin, telithromycin, clarithromycin, grapefruit juice). Antagonized by CYP3A4 and/or P-glycoprotein inducers (eg, carbamazepine, phenobarbital, phenytoin, St. Johns wort); avoid strong inducers (eg, rifampin, rifabutin). Potentiates verapamil. Additive nephrotoxicity with cyclosporine, aminoglycosides, amphotericin B. Increased risk of hemolytic uremic syndrome, thrombotic thrombocytopenic purpura, thrombotic microangiopathy with concomitant calcineurin inhibitor. Increased risk of sirolimus toxicity with cannabidiol; monitor and consider reducing the dose of sirolimus.

    Rapamune Oral Solution Adverse Reactions

    Adverse Reactions

    Stomatitis, diarrhea, abdominal pain, nausea, nasopharyngitis, acne, chest pain, peripheral edema, upper RTI, headache, dizziness, myalgia, hypercholesterolemia; infections (eg, viral), interstitial lung disease, hypersensitivity reactions, angioedema, proteinuria, impaired wound healing, progressive multifocal leukoencephalopathy, malignancies (eg, lymphomas, skin).

    Rapamune Oral Solution Clinical Trials

    See Literature

    Rapamune Oral Solution Note

    Not Applicable

    Rapamune Oral Solution Patient Counseling

    See Literature

    Rapamune Oral Solution Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Sirolimus 1mg/mL; contains alcohol.

    Pharmacological Class

    Immunosuppressant.

    See Also

    How Supplied

    Tabs—100; Soln—60mL (w. oral syringe)

    Manufacturer

    Pfizer Inc.

    Rapamune Oral Solution Indications

    Indications

    Organ rejection prophylaxis in renal transplant patients, in combination with cyclosporine and corticosteroids.

    Limitations of Use

    Cyclosporine withdrawal not studied in patients with Banff Grade 3 acute rejection or vascular rejection before cyclosporine withdrawal, dialysis-dependent, serum creatinine >4.5mg/dL, Black patients, multi-organ transplants, secondary transplants, or those with high panel-reactive antibodies. Not studied >1yr in high-immunologic risk patients. Not established for conversion from calcineurin inhibitors in maintenance renal transplant patients.

    Rapamune Oral Solution Dosage and Administration

    Adult

    Tabs and oral soln are interchangeable up to 2mg. Dilute soln with water or orange juice only. Take once daily, consistently with or without food (absorption increased by high-fat meals). Swallow tabs whole. Give as soon as possible after transplantation in combination with cyclosporine and corticosteroids, 4 hours after cyclosporine dose. Low- to moderate-immunologic risk (≥13yrs): Loading dose: 6mg, maintenance dose: initially 2mg/day. Adjust maintenance dose at 7–14 day intervals to achieve trough concentration target range (see full labeling); max 40mg/day. May give loading dose in addition to new maintenance dose when increasing trough levels; give loading dose over 2 days if maintenance dose plus loading dose is >40mg/day. Withdraw cyclosporine 2–4 months after transplantation progressively over 4–8 weeks; adjust sirolimus dose to achieve trough concentration target range 16–24ng/mL for first year, then 12–20ng/mL thereafter. High-immunologic risk (≥18yrs): Loading dose: up to 15mg on day 1, maintenance dose starting on day 2: initially 5mg/day; obtain trough level between days 5–7, adjust dose to achieve trough concentration target range 10–15ng/mL. Hepatic impairment (mild or moderate): reduce maintenance dose by ⅓; severe: reduce maintenance dose by ½. Low body weight (<40kg): Loading dose: 3mg/m2; maintenance dose: initially 1mg/m2/day.

    Children

    <13yrs: not established.

    Rapamune Oral Solution Contraindications

    Not Applicable

    Rapamune Oral Solution Boxed Warnings

    Boxed Warning

    Immunosuppression. Use is not recommended in liver or lung transplant patients.

    Rapamune Oral Solution Warnings/Precautions

    Warnings/Precautions

    Liver or lung transplants: not recommended. Should only be used by physicians experienced in immunosuppressive therapy and organ transplant in adequately equipped facilities. Increased risk of infections, lymphomas and other malignancies (eg, skin) may result from immunosuppression. Impaired or delayed wound healing (esp. BMI >30kg/m2). Hepatic impairment. Monitor sirolimus blood concentrations (obtain trough level 3–4 days after a loading dose), renal function, lipids, urine protein and for viral infections (eg, BK virus-associated nephropathy). Antimicrobial prophylaxis for PCP and CMV: see full labeling. Avoid sun, UV light; use high protection sunscreen. Male infertility. Embryo-fetal toxicity. Pregnancy; avoid. Advise females of reproductive potential to use highly effective contraception before, during, and for 12 weeks after therapy. Nursing mothers: not recommended.

    Rapamune Oral Solution Pharmacokinetics

    See Literature

    Rapamune Oral Solution Interactions

    Interactions

    Avoid live vaccines (eg, MMR, polio, BCG, others). Potentiated by cyclosporine, separate dose by 4 hours; increase sirolimus dose after cyclosporine withdrawal. Increased risk of angioedema with ACE-inhibitors. Potentiated by CYP3A4 and/or P-glycoprotein inhibitors (eg, bromocriptine, cisapride, cimetidine, clotrimazole, danazol, diltiazem, fluconazole, letermovir, protease inhibitors, metoclopramide, nicardipine, troleandomycin, verapamil); avoid strong inhibitors (eg, ketoconazole, voriconazole, itraconazole, erythromycin, telithromycin, clarithromycin, grapefruit juice). Antagonized by CYP3A4 and/or P-glycoprotein inducers (eg, carbamazepine, phenobarbital, phenytoin, St. Johns wort); avoid strong inducers (eg, rifampin, rifabutin). Potentiates verapamil. Additive nephrotoxicity with cyclosporine, aminoglycosides, amphotericin B. Increased risk of hemolytic uremic syndrome, thrombotic thrombocytopenic purpura, thrombotic microangiopathy with concomitant calcineurin inhibitor. Increased risk of sirolimus toxicity with cannabidiol; monitor and consider reducing the dose of sirolimus.

    Rapamune Oral Solution Adverse Reactions

    Adverse Reactions

    Peripheral edema, hypertriglyceridemia, hypertension, hypercholesterolemia, increased creatinine, constipation, abdominal pain, diarrhea, headache, fever, UTI, anemia, nausea, arthralgia, pain, thrombocytopenia; infections (eg, viral), interstitial lung disease, hypersensitivity reactions, angioedema, proteinuria, impaired wound healing, progressive multifocal leukoencephalopathy, malignancies (eg, lymphomas, skin), azoospermia, oligospermia.

    Rapamune Oral Solution Clinical Trials

    See Literature

    Rapamune Oral Solution Note

    Not Applicable

    Rapamune Oral Solution Patient Counseling

    See Literature

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