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GD-SIROLIMUS is a brand name for Sirolimus, supplied as a solution. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: GD-sirolimus (sirolimus oral solution and tablets) is indicated for the prophylaxis of organ rejection in patients receiving allogeneic renal transplants: • In patients at low to moderate immunological risk, it is recommended that GD-sirolimus be used initially in a regimen with cyclosporine and corticosteroids.…
Verbatim from this product's HC label. Tap a section to expand.
). • In patients at high immunologic risk (defined as Black transplant recipients and/or repeat renal transplant recipients who lost a previous allograft for immunologic reason and/or patients with high-panel reactive antibodies (PRA; peak PRA level > 80%), it is recommended that GD-sirolimus be used in combination with cyclosporine and corticosteroids for the first year following transplantation (See 4 DOSAGE AND ADMINISTRATION and 14 CLINICAL TRIALS).
Thereafter, any adjustments to the immunosuppressive regimen should be considered on the basis of the clinical status of the patient. 1 Pediatrics Pediatrics (< 13 years of age): The safety and efficacy of sirolimus in pediatric patients below the age of 13 years have not been established; therefore, Health Canada has not authorized an indication for patients under the age of 13 years.
2 Geriatrics Geriatrics (> 65 years of age): Clinical studies of sirolimus did not include sufficient numbers of patients aged 65 and over to determine whether safety and efficacy differ in this population from younger patients. Based on the finding that blood clearance decreases linearly with age, consideration should be given to reducing the GD-sirolimus dose in patients 65 years of age and over.
2 CONTRAINDICATIONS GD-sirolimus is contraindicated in patients with a hypersensitivity to sirolimus or its derivatives or any ingredient in the formulation, including any non-medicinal ingredient or component of the container. For a complete listing, see
section. During clinical trials, there were two accidental sirolimus (sirolimus oral solution) ingestions, of 120 mg and 150 mg. One patient, receiving 150 mg, experienced an episode of transient atrial fibrillation. The other patient experienced no adverse effects.
General supportive measures should be followed in all cases of overdose. Based on the poor aqueous solubility and high erythrocyte and plasma protein binding of sirolimus, it is anticipated that sirolimus is not dialyzable to any significant extent.
GD®-sirolimus Product Monograph Page 10 of 71 In mice and rats, the acute oral LD50 was greater than 800 mg/kg. For management of a suspected drug overdose, contact your regional poison control centre. 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING Table 1 – Dosage Forms, Strengths, Composition and Packaging Availability of Dosage Forms Oral Solution: GD-sirolimus (sirolimus oral solution) is supplied at a concentration of 1 mg/mL in: • Amber glass bottles of 60 mL The bottles are supplied with an oral syringe adapter for fitting into the neck of the bottle and 30 disposable amber oral syringes and 30 caps for daily dosing.
Tablets:
GD-sirolimus (sirolimus tablets) is available as: • a white, triangular-shaped tablet containing 1 mg sirolimus marked “RAPAMUNE 1 mg” on one side; • a yellow-to-beige triangular-shaped tablet containing 2 mg sirolimus marked “RAPAMUNE 2 mg” on one side, and; • a tan, triangular-shaped tablet containing 5 mg sirolimus marked “RAPAMUNE 5 mg” on one side.
Route of Administration Dosage Form / Strength/Composition Non-medicinal Ingredients Oral Oral Solution: 1 mg/mL Tablets: 1 mg, 2 mg and 5 mg Phosal 50 PG® (ascorbyl palmitate, ethanol, phosphatidyl-choline, propylene glycol, soybean oil fatty acids and sunflower mono and diglycerides) and Polysorbate 80 NF.
04/2023 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES ............................................................................................
2 TABLE OF CONTENTS .............................................................................................................. 2 PART I: HEALTH PROFESSIONAL INFORMATION ......................................................................
4 1 INDICATIONS ............................................................................................................... 4 2 CONTRAINDICATIONS .................................................................................................
4 3 SERIOUS WARNINGS AND PRECAUTIONS BOX ............................................................ 5 4 DOSAGE AND ADMINISTRATION ................................................................................. 9 5 OVERDOSAGE..............................................................................................................
9 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING ............................... 10 7 WARNINGS AND PRECAUTIONS ................................................................................ 17 8 ADVERSE REACTIONS ................................................................................................
29 9 DRUG INTERACTIONS ................................................................................................ 34 10 CLINICAL PHARMACOLOGY .......................................................................................
35 11 STORAGE, STABILITY AND DISPOSAL ......................................................................... 41 12 SPECIAL HANDLING INSTRUCTIONS ........................................................................... 42 PART II: SCIENTIFIC INFORMATION .......................................................................................
GD-sirolimus is contraindicated in patients with a hypersensitivity to sirolimus or its derivatives or any ingredient in the formulation, including any non-medicinal ingredient or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
GD®-sirolimus Product Monograph Page 5 of 71
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Sirolimus in Canada.
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Brand names are compiled from public regulatory records for active-ingredient mapping only. Drugvu is not affiliated with any manufacturer. This is not medical advice.
Calcium Sulfate Anhydrous NF, Carnauba Wax NF, Glyceryl Monooleate, Lactose Monohydrate NF, Magnesium Stearate NF, Microcrystalline Cellulose NF, Pharmaceutical Glaze NF, Polaxamer 188, Polyethylene Glycol 8000 Powdered NF, Polyethylene Glycol Type 20,000, Povidone USP, Vitamin E (dl-alpha tocopherol), Sucrose NF, Talc USP, Titanium Dioxide USP and Ink.
In addition, the 2 mg tablet contains Brown #70 Iron Oxide NF and Yellow #10 Iron Oxide NF; the 5 mg tablet contains Brown #75 Iron Oxide NF, and Yellow #10 Iron Oxide NF. GD®-sirolimus Product Monograph Page 11 of 71 The tablets are supplied in: • Bottles of 100 tablets • Unit dose cartons of 100 tablets (10 blister cards of 10 tablets each) 7 WARNINGS AND PRECAUTIONS Please see 3 SERIOUS WARNINGS AND PRECAUTIONS BOX.
General GD-sirolimus is intended for oral administration only. GD-sirolimus has been approved to be administered concurrently with cyclosporine (liquid and microemulsion) and corticosteroids. The efficacy and safety of the use of sirolimus in combination with other immunosuppressive agents has not been established.
Use in High-Risk Patients The safety and efficacy of cyclosporine withdrawal in high-risk patients have not been adequately studied and it is therefore not recommended. 5 mg/dL), black patients, re-transplants, multi-organ transplants, and patients with high panel of reactive antibodies.
It is recommended that GD-sirolimus be used in combination with cyclosporine and corticosteroids for the first year following transplantation. The safety and efficacy of this combination in high-risk renal transplant patients have not been studied beyond one year.
Therefore, after the first year following transplantation any adjustments to the immunosuppressive regimen should be considered on the basis of the clinical status of the patient (See 1 INDICATIONS, 4 DOSAGE AND ADMINISTRATION, and 14 CLINICAL TRIALS).
Angioedema The concomitant administration of sirolimus and angiotensin-converting enzyme (ACE) inhibitors has resulted in angioneurotic edema-type reactions. Elevated sirolimus levels (with/without concomitant ACE inhibitors) may also potentiate angioedema.
In some cases, the angioedema has resolved upon discontinuation or dose reduction of sirolimus. Antimicrobial Prophylaxis Cytomegalovirus (CMV) prophylaxis is recommended for 3 months after transplantation, particularly for patients at increased risk for CMV infection.
Cases of Pneumocystis carinii pneumonia have been reported in patients not receiving antimicrobial prophylaxis. Therefore, antimicrobial prophylaxis for Pneumocystis carinii pneumonia should be administered for 1 year following transplantation.
Carcinogenesis and Mutagenesis Patients receiving immunosuppression regimens involving combinations of drugs, including GD- sirolimus, as part of an immunosuppression regimen are at increased risk of developing lymphomas and other malignancies, particularly of the skin.
The risk appears to be related to the intensity and GD®-sirolimus Product Monograph Page 12 of 71 duration of immunosuppression rather than to the use of any specific agent. As with all patients at an increased risk for skin cancer, exposure to sunlight and UV light should be limited by wearing protective clothing and using a sunscreen with a high protection factor.
Also, see 16 NON-CLINICAL TOXICOLOGY - Chronic Toxicology - Carcinogenicity, Mutagenicity, Reproductive and Developmental Toxicology.
Cardiovascular Hyperlipidemia:
Increased serum cholesterol and triglycerides requiring treatment may occur in patients treated with GD-sirolimus. The risk/benefit should be considered in patients with established hyperlipidemia before initiating an immunosuppressive regimen including GD-sirolimus.
Drug-Drug Interactions Co-administration of GD-sirolimus with strong inhibitors of CYP3A4 and/or P-glycoprotein (P-gp) (such as ketoconazole, voriconazole, itraconazole, telithromycin, or clarithromycin) or strong inducers of […]
43 13 PHARMACEUTICAL INFORMATION ............................................................................ 43 14 CLINICAL TRIALS ........................................................................................................
53 15 MICROBIOLOGY ........................................................................................................ 56 16 NON-CLINICAL TOXICOLOGY .....................................................................................
56 PATIENT MEDICATION INFORMATION .................................................................................. 60 GD®-sirolimus Product […]