SubcutaneousType 2 diabetes mellitusAdult: As an adjunct to diet and exercise to improve glycaemic control: Monotherapy (if metformin is considered inappropriate) or in combination with other antidiabetic agents: Initially, 2.5 mg once weekly for 4 weeks, then increase to 5 mg once weekly. If additional glycaemic control is needed, dose may be further increased in increments of 2.5 mg at intervals of at least 4 weeks up to Max of 15 mg once weekly. Doses are given without regard to meals at any time of the day, on the same day each week. Treatment recommendations may vary between individual products (refer to specific product guidelines).
SubcutaneousWeight managementAdult: As an adjunct to reduced-calorie diet and increased physical activity in patients with initial BMI of ≥30 kg/m2 (obesity) or with initial BMI of 27-<30 kg/m2 (overweight) in the presence of at least 1 weight-related comorbidity (e.g. hypertension, dyslipidaemia): Initially, 2.5 mg once weekly for 4 weeks, then increase to 5 mg once weekly. If needed, dose may be further increased in increments of 2.5 mg at intervals of at least 4 weeks up to Max of 15 mg once weekly. Doses are given without regard to meals at any time of the day, on the same day each week. Reassess therapy if at least 5% of initial body weight has not been lost after 6 months of treatment at the highest tolerated dose. Treatment recommendations may vary between individual products (refer to specific product guidelines).
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Tirzepatide May be taken with or without food.
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Hypersensitivity. Multiple endocrine neoplasia syndrome type 2 (MEN 2); personal or family history of medullary thyroid carcinoma (MTC).
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Patient with history of pancreatitis; history of anaphylaxis or angioedema with another glucagon-like peptide-1 (GLP-1) receptor agonist; severe gastrointestinal disease, including severe gastroparesis; proliferative diabetic retinopathy, non-proliferative diabetic retinopathy requiring acute therapy, diabetic macular oedema. Patients receiving insulin or insulin secretagogues (e.g. sulfonylurea). Not indicated for use in patients with type 1 diabetes mellitus or diabetic ketoacidosis. Not a substitute for insulin. Patients undergoing surgeries or procedures requiring deep sedation or anaesthesia may have an increased risk of pulmonary aspiration due to residual gastric contents caused by delayed gastric emptying associated with GLP-1 receptor agonists. Tirzepatide is available in various brands that are approved for specific indications in certain countries; these brands may not be interchangeable and must be used according to their approved indication (refer to local product guidelines before administration). Potential misuse of GLP-1 receptor agonists for unauthorised indications such as aesthetic weight loss has been reported; ensure the proper use of this medication as the risks and benefits of using GLP-1 receptor agonists for weight loss outside of the approved indications have not been studied. Renal and hepatic impairment. Pregnancy and lactation.
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Significant: Delayed gastric emptying, which may lead to pulmonary aspiration (particularly in patients undergoing surgery or procedure requiring deep sedation or general anaesthesia); gastrointestinal effects (e.g. nausea, vomiting, diarrhoea) which may lead to severe dehydration or renal function deterioration; acute kidney injury, worsening chronic renal failure; hypoglycaemia; gallbladder disease (e.g. cholelithiasis, cholecystitis); diabetic retinopathy; possible risk of developing MTC or suicidal thoughts; serious hypersensitivity reactions (e.g. anaphylaxis, angioedema).
Cardiac disorders: Sinus tachycardia.
Gastrointestinal disorders: Abdominal pain or distention, constipation, dyspepsia, flatulence, eructation, GERD.
General disorders and administration site conditions: Fatigue, inj site reactions (e.g. pain, erythema, pruritus).
Immune system disorders: Antibody formation.
Investigations: Increased heart rate, serum lipase and serum amylase.
Metabolism and nutrition disorders: Decreased appetite.
Nervous system disorders: Dizziness.
Skin and subcutaneous tissue disorders: Alopecia.
Vascular disorders: Hypotension.
Potentially Fatal: Acute pancreatitis, including haemorrhagic or necrotising pancreatitis.
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SC: Z (Animal studies showed abortion and embryo-foetal toxicity. Generally not recommended. Consult product literature for specific recommendations.)
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This drug may impair the ability to concentrate and react as a result of hypoglycaemia, especially when used in combination with other antidiabetic agents; if affected, do not drive or operate machinery. This drug may also cause gastrointestinal effects (e.g. vomiting, diarrhoea) that may result in dehydration; ensure adequate fluid intake during treatment. Women of childbearing potential using oral hormonal contraceptives may add a barrier contraceptive method for 4 weeks after treatment initiation or after each dose increase, or switch to non-oral contraceptive method.
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Monitor plasma glucose, heart rate, renal function, body weight (when used for weight management), and HbA1c (twice a year for patients who have stable glycaemic control; quarterly for those not meeting the treatment goals or with therapy changes). Closely assess for signs and symptoms of pancreatitis, gallbladder disease, gastrointestinal effects, thyroid tumours, new or worsening depression, suicidal thoughts, and unusual mood/behavioural changes.
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Symptoms: Gastrointestinal effects, including nausea. Management: Symptomatic and supportive treatment.
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Increased risk of hypoglycaemia with insulin or insulin secretagogues (e.g. sulfonylureas). May affect the absorption rate of concomitantly administered oral drugs due to delayed gastric emptying. May reduce the serum concentration and efficacy of oral hormonal contraceptives due to delayed gastric emptying.
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Description:
Mechanism of Action: Tirzepatide is a long-acting dual glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonist. It selectively binds to and activates both GIP and GLP-1 receptors, thereby increasing glucose-dependent insulin secretion, decreasing inappropriate glucagon secretion, and slowing gastric emptying. Additionally, tirzepatide acts on certain areas of the brain to reduce food intake by regulating appetite and modulating fat utilisation.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 8-72 hours. Bioavailability: 80%.
Distribution: Plasma protein binding: 99% to albumin.
Metabolism: Metabolised via proteolytic cleavage of the peptide backbone, β-oxidation of the C20 fatty diacid moiety, and amide hydrolysis.
Excretion: Via urine and faeces (as metabolites). Elimination half-life: Approx 5 days.
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Store between 2-8°C. Do not freeze. Protect from light. If necessary, may be kept below 30°C for up to 21 days (for single-dose vial or pre-filled pen) or up to 30 days (for multiple-dose pre-filled pen).
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A10BX16 - tirzepatide ; Belongs to the class of other blood glucose lowering drugs excluding insulins. Used in the treatment of diabetes.
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Brayfield A, Cadart C (eds). Tirzepatide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/04/2025. GLP-1 and Dual GIP/GLP-1 Receptor Agonists: Potential Risk of Pulmonary Aspiration During General Anaesthesia or Deep Sedation. Medicines & Healthcare products Regulatory Agency. https://www.gov.uk/drug-safety-update. Accessed 07/04/2025. GLP-1 Receptor Agonists: Reminder of the Potential Side Effects and to Be Aware of the Potential for Misuse. Medicines & Healthcare products Regulatory Agency. https://www.gov.uk/drug-safety-update. Accessed 07/04/2025. Joint Formulary Committee. Tirzepatide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/04/2025. Mounjaro 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg and 15 mg Solution for Injection in Pre-filled Pen (Zuellig Pharma Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/04/2025. Mounjaro 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg and 15 mg Solution for Injection in Vial (Zuellig Pharma Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/04/2025. Mounjaro 7.5 mg Solution for Injection in Pre-filled Pen (Eli Lilly Nederland B.V.). MHRA. https://products.mhra.gov.uk. Accessed 07/04/2025. Mounjaro 7.5 mg Solution for Injection in Vial (Eli Lilly Nederland B.V.). MHRA. https://products.mhra.gov.uk. Accessed 07/04/2025. Mounjaro Injection, Solution (Eli Lilly and Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/04/2025. Tirzepatide. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. Accessed 07/04/2025. Tirzepatide. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/04/2025. Zepbound Injection, Solution (Eli Lilly and Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/04/2025.
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