Rapamune Side Effects

Generic name: sirolimus

Note: This document contains side effect information about sirolimus. Some of the dosage forms listed on this page may not apply to the brand name Rapamune.

Some side effects of Rapamune may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

For the Consumer

Applies to sirolimus: oral solution, oral tablet

Sirolimus may cause a serious viral infection of the brain that can lead to disability or death. This risk is higher if you have a weak immune system or are receiving certain medicines. Call your doctor right away if you have any change in your mental state, problems with speech or walking, or decreased vision. These symptoms may start gradually and get worse quickly.

Get emergency medical help if you have any of these signs of an allergic reaction while taking sirolimus (the active ingredient contained in Rapamune) hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have a serious side effect such as:

• fast heart rate;

• pain when you breathe, feeling short of breath;

• chest pain, feeling weak or tired;

• coughing up blood or mucus;

• feeling like you might pass out;

• pale skin, easy bruising or bleeding, weakness;

• fever, chills, body aches, flu symptoms;

• night sweats, weight loss;

• swelling in your face, stomach, hands or feet;

• rapid weight gain;

• pain or burning when you urinate; or

• slow healing of a wound.

Less serious side effects of sirolimus may include:

• joint pain;

• nausea, vomiting, diarrhea, constipation, stomach pain;

• headache; or

• acne or skin rash.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

For Healthcare Professionals

Applies to sirolimus: oral solution, oral tablet

Respiratory

Respiratory side effects including dyspnea (22% to 30%), upper respiratory infection (20% to 26%), pharyngitis (16% to 21%), pleural effusion, and alveolar proteinosis have been reported. Cases of interstitial lung disease (including pneumonitis, and infrequently bronchiolitis obliterans organizing pneumonia and pulmonary fibrosis) with no identified infectious etiology and sometimes ending up being fatal have been reported. Bronchial anastomotic dehiscence has also been reported, including fatal cases in lung transplant patients treated with a combination of sirolimus (the active ingredient contained in Rapamune) tacrolimus, and corticosteroids. Three cases of diffuse alveolar hemorrhage have been reported.

It has been recommended that pulmonary toxicity due to sirolimus be included as a part of the differential diagnosis of kidney transplant patients who display signs of interstitial pneumonia.

Metabolic

Metabolic side effects including peripheral edema (54% to 64%), hyperlipidemia (38% to 57%), hypercholesterolemia (35% to 46%), increased creatinine (35% to 40%), edema (16% to 24%), hypophosphatemia (15% to 23%), hypokalemia (11% to 21%), weight gain (8% to 21%), and hyperkalemia (12% to 17%) have been reported. High triglycerides have also been reported.

Cardiovascular

Cardiovascular side effects including hypertension (39% to 49%) and chest pain (16% to 24%) have been reported. There have been reports of pericardial effusion (including hemodynamically significant effusions and tamponade requiring intervention in children and adults). A case of life-threatening coronary artery spasm following sirolimus-eluting stent deployment has also been reported.

Gastrointestinal

Gastrointestinal side effects including diarrhea (25% to 42%), constipation (28% to 38%), abdominal pain (28% to 36%), nausea (25% to 36%), vomiting (19% to 25%), dyspepsia (17% to 25%), and ascites have been reported. A case of sirolimus-induced intractable chronic diarrhea and a case of delayed gastric ulcer healing have also been reported.

General

General side effects including asthenia (22% to 38%), fever (23% to 34%), headache (23% to 34%), and pain (24% to 33%) have been reported.

Hematologic

Hematologic side effects including anemia (23% to 37%), thrombocytopenia (13% to 20%), leukopenia (9% to 15%), capillary leak syndrome, and lymphedema have been reported.

Genitourinary

Genitourinary side effects including urinary tract infection (20% to 26%), proteinuria, and focal segmental glomerulosclerosis have been reported. Azoospermia has also been reported and has been reversible upon discontinuation of in most cases.

Musculoskeletal

Musculoskeletal side effects including arthralgia (25% to 31%) have been reported. A case of premature osteonecrosis and a case of myopathy have also been reported.

Nervous system

Nervous system side effects including tremor (21% to 31%), insomnia (13% to 22%), and progressive multifocal leukoencephalopathy have been reported. A case of posterior reversible encephalopathy syndrome has also been reported.

Dermatologic

Dermatologic side effects including acne (20% to 31%), rash (10% to 20%), and exfoliative dermatitis have been reported. A case of chronic pyogenic periungual infection and a case of chylous ascites have also been reported.

Renal

BK virus associated nephropathy has been associated with serious outcomes, including deteriorating renal function and renal graft loss.

Patients treated with cyclosporine and sirolimus (the active ingredient contained in Rapamune) were reported to have higher serum creatinine levels and lower glomerular filtration rates when compared to patients treated with cyclosporine and placebo or azathioprine controls. The rate of decline in renal function in these studies was greater in patients receiving sirolimus and cyclosporine compared with control therapies.

In patients with delayed graft function, sirolimus may delay recovery of renal function.

Renal side effects have included BK virus associated nephropathy, nephrotic syndrome, higher serum creatinine levels, and lower glomerular filtration rates.

Ocular

The underlying mechanism for severe eyelid edema is unknown.

Ocular side effects including severe eyelid edema have been reported.

Hepatic

Hepatic side effects including hepatotoxicity and hepatic artery thrombosis have been reported. Abnormal liver function tests including increased AST/SGOT, increased ALT/SGPT, hypophosphatemia and hyperglycemia have also been reported.

Hypersensitivity

Hypersensitivity side effects including anaphylactic and anaphylactoid reactions, angioedema, and hypersensitivity vasculitis, have been reported.

Other

Other side effects including lymphedema, tuberculosis, and incisional hernia have been reported. A case of unilateral upper extremity edema has also been reported.

Oncologic

Oncologic side effects have been reported in animal studies including lymphoma, hepatocellular adenoma and carcinoma, and testicular adenoma.

Endocrine

Endocrine side effects have included increased basal and stimulated insulin levels in vitro and insulin content in vitro regardless of culture duration.

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