Known brand names include Mounjaro and Zepbound.
A once-weekly injection that acts on two gut hormone receptors. As Mounjaro it lowers blood sugar in type 2 diabetes and cuts the risk of heart attack and stroke in adults at high risk; as Zepbound it helps adults with obesity lose weight and treats moderate to severe sleep apnea in adults with obesity.
Labeled use. Weight reduction and long-term maintenance in adults with obesity, or overweight with a weight-related condition, alongside diet and activity (Zepbound).
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Labeled use. With diet and exercise for glycemic control from age 10, and to reduce major cardiovascular events in adults at high risk (Mounjaro).
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Labeled use. Moderate to severe obstructive sleep apnea in adults with obesity (Zepbound).
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Choose tirzepatide in type 2 diabetes when glucose lowering and weight loss are both priorities, or when a GLP-1 receptor agonist alone has not reached targets, since dual GIP and GLP-1 agonism lowers A1c and weight more than semaglutide 1 mg in head-to-head trials. In obesity it produces larger weight loss than older agents and is the only incretin drug approved for obstructive sleep apnea. Avoid with a history of MTC, MEN 2, pancreatitis, or severe gastroparesis, and never combine it with another GLP-1 drug.
A dual GIP and GLP-1 receptor agonist. It enhances first- and second-phase insulin secretion and lowers glucagon in a glucose-dependent way, improves insulin sensitivity, slows gastric emptying, and reduces food intake. A C20 fatty diacid gives albumin binding and a half-life of about 5 days.
The label does not describe a narrow therapeutic index or direct dosing by measured blood levels of the drug.
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Doses come from the FDA label. Study tool, not for clinical decisions.
None, including end-stage renal disease. Monitor renal function when starting or escalating in patients with renal impairment who report severe GI effects.
Risk of thyroid C-cell tumors. Tirzepatide causes dose- and duration-dependent thyroid C-cell tumors in rats; whether it causes medullary thyroid carcinoma in humans is unknown. Contraindicated with a personal or family history of MTC or with MEN 2. Counsel patients to report a neck mass, trouble swallowing, shortness of breath, or lasting hoarseness.
No specific antidote. Give supportive care based on symptoms and consider contacting Poison Help. Observation may need to be prolonged because the half-life is about 5 days.
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Human data are insufficient; animal studies showed fetal growth reductions and abnormalities at clinical exposures. Use only if the benefit justifies the risk, and weigh the harms of poorly controlled diabetes. Oral hormonal contraceptives may fail for 4 weeks after starting and after each dose increase, so add a barrier method.
In a single-dose lactation study, tirzepatide in breast milk was undetectable or low relative to the maternal dose. There are no data on effects on the infant or on milk production. Weigh the benefits of breastfeeding against the mother's need for the drug.
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Approved for type 2 diabetes from age 10 (Mounjaro), based on a 30-week placebo-controlled trial in 99 patients; vomiting, abdominal pain, and hypoglycemia were more frequent than in adults. The maximum pediatric dose is 10 mg weekly, and the KwikPen is not recommended for self-injection by children. Zepbound is not established in children.
No overall differences in safety or effectiveness between patients 65 and older and younger patients; 30.1% of patients in the seven-trial pool were 65 or older.
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