Sirolimus

DEA Class; Rx

Common Brand Names; Rapamune

• Immunosuppressants

Hypersensitivity to sirolimus or macrolide antibiotics

Concomitant live vaccines

• Peripheral edema, w/ corticosteroids (54-58%)
• Hypertriglyceridemia (45-57%; up to 90% when used with or following cyclosporine)
• Hypercholesterolemia (43-46%; up to 90% when used with or following cyclosporine)
• Constipation (36-38%)
• Arthralgia (25-31%)
• Thrombocytopenia (14-30%)
• Rash (10-20%)
• Hypertension (45-49%)
• Increased creatinine (39-40%)
• Abdominal pain (29-36%)
• Diarrhea (25-35%)
• Headache (34%)
• Fever (23-34%)
• Urinary tract infection (26-33%)
• Anemia (23-33%)
• Nausea (25-31%)
• Arthralgia (25-31%)
• Pain (29-33%)
• Acne (22%)
• Edema (18-20%)
• Sepsis (<20%)
• Lymphocele (<20%)
• Venous thromboembolism (<20%)
• Tachycardia (<20%)
• Stomatitis (<20%)
• Thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (<20%)
• Leukopenia (<20%)
• Abnormal healing (<20%)
• Increased lactic dehydrogenase (<20%)
• Hypokalemia (<20%)
• Hypophoaphatemia (<20%)
• Hyperglycemia (<20%)
• Diabetes mellitus (<20%)
• Bone necrosis (<20%)
• Pneumonia (<20%)
• Epistaxis (<20%)
• Melanoma (<20%)
• Squamous cell carcinoma (<20%)
• Basal cell carcinoma (<20%)
• Pyelonephritis (<20%)
• Ovarian cysts (<20%)
• Menstrual disorders (amenorrhea and menorrhagia) (<20%)

Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions, angioedema, exfoliative dermatitis, and hypersensitivity vasculitis, have been associated with the administration of this drug

Not for liver or lung transplant

Exposure to sunlight and ultraviolet (UV) light should be limited by wearing protective clothing and using a broad spectrum sunscreen with a high protection factor

Progressive multifocal leukoencephalopathy (PML), sometimes fatal, have been reported; commonly presents with hemiparesis, apathy, confusion, cognitive deficiencies, and ataxia

Based on animal studies and mechanism of action, therapy may cause fetal harm when administered to a pregnant woman; in animal studies, mTOR inhibitors caused embryo- fetal toxicity when administered during period of organogenesis at maternal exposures that were equal to or less than human exposures at recommended lowest starting dose; advise pregnant women of potential risk to a fetus; advise women of childbearing potential to avoid becoming pregnant and to use effective contraception while on therapy and for 12 weeks after ending treatment

Associated with development of angioedema; concomitant use of other drugs known to cause angioedema, such as angiotensin-converting enzyme (ACE) inhibitors, may increase risk of developing angioedema; elevated sirolimus levels (with/without concomitant ACE inhibitors) may potentiate angioedema; in some cases, angioedema has resolved upon discontinuation or therapy dose reduction

Consult lab regarding type of assay for drug monitoring; whole blood concentrations are being measured by various chromatographic and immunoassay methodologies; sample concentration values from different assays may not be interchangeable

Can cause fetal harm when administered to pregnant women based on animal studies and the mechanism of action

Data are not available regarding the presence in human milk, the effects on breastfed infants, or the effects on milk production

Sirolimus 

tablet

• 0.5mg
• 1mg
• 2mg

oral solution

• 1mg/mL

topical gel

• 0.2%

injection, lyophilized powder for reconstitution

• 100mg/vial