ZEPBOUND (tirzepatide injection) is indicated for once-weekly administration for chronic weight management, including weight loss and weight maintenance, as an adjunct to a reduced-calorie diet and increased physical activity, in adults with obesity (BMI ≥ 30 kg/m²) or overweight (BMI ≥ 27 kg/m²) with at least one weight-related comorbid condition.
About this page. This page summarizes information from Health Canada's product monograph for Zepbound on adverse reactions, warnings, and special populations. It is for informational purposes only and is not a substitute for advice from your prescriber or pharmacist. Always discuss side effects and warnings with your healthcare provider. Read our full medical disclaimer →
Skin and subcutaneous tissue disorders
Vascular disorders
General disorders and administration site conditions
Immune system disorders
Nervous system disorders
Gastrointestinal disorders
No clinical trials have been conducted in pregnancy. Studies in animals (i.e., rats and rabbits) have shown reproductive and developmental toxicity, including harm to fetal development and maternal weight loss. ZEPBOUND is contraindicated during pregnancy. If a patient wishes to become pregnant, ZEPBOUND should be discontinued at least 1 month before a planned pregnancy due to the long half-life of tirzepatide.[9]Section 7.1.1, page 11
In a 5 mg single-dose clinical lactation study, the concentration of tirzepatide in breast milk was found to be either undetectable (limit of detection in breastmilk 4 ng/mL) to very low compared to maternal administered dose and maternal plasma concentrations. There are no available data on the effects of tirzepatide on the breastfed infant or on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for ZEPBOUND and any potential adverse effects on the breastfed infant from ZEPBOUND or from the underlying maternal condition.[10]Section 7.1.2, page 11
The safety and effectiveness of ZEPBOUND have not been established in pediatric patients less than 18 years of age. ZEPBOUND is not indicated for use in pediatric patients.[11]Section 7.1.3, page 11
No dose adjustment is required in patients over 65 years of age. In clinical trials, 246 (8.8%) ZEPBOUND-treated patients were 65 years of age or older and 15 (0.5%) were 75 years of age or older at baseline. No overall differences in safety or efficacy were detected between these patients and younger patients.[12]Section 7.1.4, page 11
In a clinical pharmacology study in subjects with varying degrees of hepatic impairment, no change in tirzepatide pharmacokinetics was observed. However, there is limited clinical experience in patients with mild, moderate, or severe hepatic impairment; therefore, use ZEPBOUND with caution in these patient populations.[13]Section 7.1.5, page 11
In clinical trials, 850 (30.3%) of ZEPBOUND-treated patients had mild renal impairment and 59 (2.1%) had moderate renal impairment at baseline. No patients had severe renal impairment (eGFR <30 mL/min/1.73 m2) at baseline. ZEPBOUND is not recommended in patients with end stage renal impairment due to very limited clinical experience with ZEPBOUND in this population.[14]Section 7.1.6, page 11
ZEPBOUND causes an increase in heart rate. Caution should be observed in patients who have cardiac conditions that might be worsened by an increase in heart rate. There is no therapeutic experience in patients with congestive heart failure New York Heart Association (NYHA) class IV.[5]Section 7, page 8
Patients with type 2 diabetes mellitus receiving ZEPBOUND for weight management in combination with an insulin secretagogue (e.g., a sulfonylurea) or insulin may have an increased risk of hypoglycemia. The risk of hypoglycemia may be lowered by a reduction in the dose of the insulin secretagogue or insulin. The use of ZEPBOUND in combination with other incretin drugs or with other tirzepatide-containing drugs (i.e., Mounjaro) has not been studied and ZEPBOUND should not be used in combination with those drugs.[5]Section 7, page 8
Use of ZEPBOUND has been associated with gastrointestinal adverse reactions, sometimes severe. In clinical trials, severe gastrointestinal adverse reactions were reported more frequently among patients receiving ZEPBOUND (2.7%) than placebo (1.2%). ZEPBOUND has not been studied in patients with severe gastrointestinal disease, including severe gastroparesis, and is therefore not recommended in these patients. Events related to impaired gastric emptying, including severe gastroparesis, have been reported. Events related to malnutrition, including severe events, have been reported in patients receiving ZEPBOUND. Nutritional guidance and, as needed, supplementation or support, should be considered. Discontinuation should be considered for severe or persistent cases.[5]Section 7, page 8
Treatment with ZEPBOUND and GLP-1 receptor agonists is associated with an increased occurrence of acute gallbladder disease. In a pool of 3 placebo-controlled clinical trials of ZEPBOUND, cholelithiasis was reported in 1.1%, cholecystitis in 0.6%, and cholecystectomy in 0.2% of ZEPBOUND-treated patients. Acute gallbladder events were associated with weight reduction. Acute pancreatitis has been observed in patients treated with GLP-1 receptor agonists. In ZEPBOUND placebo-controlled trials, 6 events of acute pancreatitis were confirmed by adjudication in 6 (0.2%) ZEPBOUND-treated patients. If pancreatitis is suspected, ZEPBOUND should be discontinued; if confirmed, ZEPBOUND should not be restarted. ZEPBOUND has not been evaluated in patients with a prior history of pancreatitis.[6]Section 7, page 9
Hypersensitivity reactions have been reported with ZEPBOUND in clinical trials. There have been postmarketing reports of serious hypersensitivity reactions (e.g. anaphylactic reactions and angioedema) in patients treated with tirzepatide. If hypersensitivity reactions occur, discontinue use of ZEPBOUND; treat promptly per standard of care, and monitor until signs and symptoms resolve. Anaphylaxis and angioedema have been reported with GLP-1 receptor agonists. Use ZEPBOUND with caution in patients with a history of angioedema or anaphylaxis with a GLP-1 receptor agonist or related products.[6]Section 7, page 9
Rapid improvement in glucose control has been associated with a temporary worsening of diabetic retinopathy. ZEPBOUND has not been studied in patients with non-proliferative diabetic retinopathy requiring acute therapy, proliferative diabetic retinopathy, or diabetic macular edema, and should be used with caution in these patients, with appropriate monitoring.[6]Section 7, page 9
There have been rare postmarketing reports of pulmonary aspiration in patients receiving GLP-1 receptor agonists undergoing elective surgeries or procedures requiring general anesthesia or deep sedation who had residual gastric contents despite reported adherence to preoperative fasting recommendations. Available data are insufficient to inform recommendations to mitigate the risk of pulmonary aspiration. Instruct patients to inform healthcare providers prior to any planned surgeries or procedures if they are using ZEPBOUND.[6]Section 7, page 9
Suicidal ideation and behaviour have been reported with products which induce weight loss (chronic weight management). Monitor patients treated with ZEPBOUND for the emergence or worsening of depression, suicidal thoughts or behaviours, and/or any unusual changes in mood or behaviour. Discontinue ZEPBOUND in patients who experience suicidal thoughts or behaviours. Avoid ZEPBOUND in patients with a history of suicidal attempts or active suicidal ideation.[7]Section 7, page 10
Tirzepatide has been associated with gastrointestinal adverse reactions, which include nausea, vomiting, and diarrhea. These events may lead to dehydration, which could cause a deterioration in renal function, including acute renal failure. There have been postmarketing reports of acute kidney injury and worsening of chronic renal failure, which may sometimes require hemodialysis. Monitor renal function in patients reporting adverse reactions to ZEPBOUND that could lead to volume depletion.[7]Section 7, page 10
The following adverse reactions have been reported during post-marketing use of tirzepatide (the active ingredient in ZEPBOUND): gastrointestinal disorders — ileus; immune system disorders — anaphylactic reaction; skin and subcutaneous tissue disorders — angioedema; nervous system disorders — dysesthesia; pulmonary — pulmonary aspiration has been reported in patients receiving GLP-1 receptor agonists undergoing elective surgeries or procedures requiring general anesthesia or deep sedation; renal — acute kidney injury. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or to establish a causal relationship to drug exposure.[4]Section 8.5, page 15
Side effects and warnings must be assessed in the context of your personal health history. Discuss any concerns about adverse reactions with your prescriber or pharmacist. Use our pharmacy comparison tool to find and connect with a Canadian pharmacy that carries Zepbound.
Last reviewed May 14, 2026 against the Health Canada Product Monograph dated April 2, 2026. View monograph →