Tirzepatide (6 brand names, 1 dosage form, 1 route)
Available dosage forms: SOLUTION.
Routes of administration: SUBCUTANEOUS.
Brand Names
- MOUNJARO
- MOUNJARO (AUTOINJECTOR)
- MOUNJARO KWIKPEN
- ZEPBOUND
- ZEPBOUND (AUTOINJECTOR)
- ZEPBOUND KWIKPEN
Boxed Warning
In rats, tirzepatide causes dose-dependent and treatment-duration-dependent thyroid C-cell tumors at clinically relevant exposures. It is unknown whether ZEPBOUND causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans as human relevance of tirzepatide-induced rodent thyroid C-cell tumors has not been determined [see Warnings and Precautions (5.1) and Nonclinical Toxicology (13.1)]. ZEPBOUND is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2) [see Contraindications (4)] . Counsel patients regarding the potential risk for MTC with the use of ZEPBOUND and inform them of symptoms of thyroid tumors (e.g., a mass in the neck, dysphagia, dyspnea, persistent hoarseness). Routine monitoring of serum calcitonin or using thyroid ultrasound is of uncertain value for early detection of MTC in patients treated with ZEPBOUND [see Contraindications (4) and Warnings and Precautions (5.1)].
Indications and Usage
ZEPBOUND® is indicated in combination with a reduced-calorie diet and increased physical activity: to reduce excess body weight and maintain weight reduction long term in adults with obesity or adults with overweight in the presence of at least one weight-related comorbid condition. to treat moderate to severe obstructive sleep apnea (OSA) in adults with obesity.
Contraindications
ZEPBOUND is contraindicated in patients with: A personal or family history of MTC or in patients with MEN 2 [see Warnings and Precautions (5.1)]. Known serious hypersensitivity to tirzepatide or any of the excipients in ZEPBOUND. Serious hypersensitivity reactions, including anaphylaxis and angioedema, have been reported with tirzepatide [see Warnings and Precautions (5.6) and Adverse Reactions (6.2)].
Adverse Reactions
The following serious adverse reactions are described below or elsewhere in the prescribing information: Risk of Thyroid C-cell Tumors [see Warnings and Precautions (5.1)] Severe Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.2)] Acute Kidney Injury Due to Volume Depletion [see Warnings and Precautions (5.3)] Acute Gallbladder Disease [see Warnings and Precautions (5.4)] Acute Pancreatitis [see Warnings and Precautions (5.5)] Hypersensitivity Reactions [see Warnings and Precautions (5.6)] Hypoglycemia [see Warnings and Precautions (5.7)] Diabetic Retinopathy Complications in Patients with Type 2 Diabetes Mellitus [see Warnings and Precautions (5.8)] Pulmonary Aspiration During General Anesthesia or Deep Sedation [see Warnings and Precautions (5.9)]
Mechanism of Action
Tirzepatide is a GIP receptor and GLP-1 receptor agonist. It contains a C20 fatty diacid that enables albumin binding and prolongs the half-life. Tirzepatide selectively binds to and activates both the GIP and GLP-1 receptors, the targets for native GIP and GLP-1. GLP-1 is a physiological regulator of appetite and caloric intake. Nonclinical studies suggest the addition of GIP may further contribute to the regulation of food intake. Both GIP receptors and GLP-1 receptors are found in areas of the brain involved in appetite regulation. Animal studies show that tirzepatide distributes to and activates neurons in brain regions involved in regulation of appetite and food intake.
Overdosage
In the event of an overdosage, contact the Poison Help Line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Appropriate supportive treatment should be initiated according to the patient’s clinical signs and symptoms. A period of observation and treatment for these symptoms may be necessary, taking into account the half-life of tirzepatide of approximately 5 days.