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Zepbound Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Single-dose prefilled pens—4
Manufacturer
Generic Availability
NO
Mechanism of Action
Tirzepatide, a GIP receptor and GLP-1 receptor agonist, is an amino acid with a C20 fatty diacid moiety 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.
Zepbound Indications
Indications
As an adjunct to a reduced calorie diet and increased physical activity for chronic weight management in adults with an initial body mass index (BMI) of ≥30kg/m2 (obesity) or ≥27kg/m2 (overweight) in the presence of at least 1 weight-related comorbid condition (eg, hypertension, T2DM, dyslipidemia, obstructive sleep apnea, cardiovascular disease).
Limitations of Use
Do not use with other tirzepatide-containing products or with any other GLP-1 receptor agonist. Safety and efficacy have not been established with other products for weight management. Not studied in those with a history of pancreatitis.
Zepbound Dosage and Administration
Adult
Give by SC inj in abdomen, thigh, or upper arm; rotate inj sites. Initially 2.5mg once weekly; after 4 weeks, increase to 5mg once weekly. May increase in 2.5mg increments after ≥4 weeks on the current dose; max 15mg once weekly.
Children
<18yrs: not established.
Zepbound Contraindications
Contraindications
History (personal or family) of medullary thyroid carcinoma. Multiple endocrine neoplasia syndrome type 2.
Zepbound Boxed Warnings
Boxed Warning
Risk of thyroid C-cell tumors.
Zepbound Warnings/Precautions
Warnings/Precautions
Risk of thyroid C-cell tumors (including medullary thyroid carcinoma); inform patients of potential risk and symptoms. History of pancreatitis: not studied. Monitor for pancreatitis; discontinue if suspected and do not restart treatment if confirmed. Severe GI disease, including severe gastroparesis: not recommended. Monitor blood glucose prior to and during therapy in those with diabetes. History of diabetic retinopathy; monitor for progression. History of anaphylaxis or angioedema with other GLP-1 receptor agonist. Discontinue if hypersensitivity reactions occur. Perform gallbladder studies and clinical follow-up if cholelithiasis or cholecystitis are suspected. Monitor renal function in patients reporting adverse reactions that could lead to volume depletion. Monitor for emergence or worsening of depression, suicidal thoughts or behaviors, and/or any unusual changes in mood or behavior; discontinue if occurs. History of suicidal attempts or active suicidal ideation: avoid. Pregnancy. Nursing mothers.
Zepbound Pharmacokinetics
Absorption
Median time (range) to maximum plasma concentration: 24 hours (8–72 hours). Mean absolute bioavailability: 80%.
Distribution
Mean apparent steady-state volume of distribution: ~9.7 L. Plasma protein bound: 99% (albumin).
Elimination
Renal, fecal. Half-life: ~5 days. Mean clearance: 0.056 L/h.
Zepbound Interactions
Interactions
Increased risk of hypoglycemia with concomitant insulin secretagogues (eg, sulfonylureas) or insulin; consider reducing dose of these. May affect absorption of concomitant oral drugs (delayed gastric emptying); caution. Monitor drugs with narrow therapeutic index (eg, warfarin). Advise patients using oral hormonal contraceptives to switch to a non-oral contraceptive method or add a barrier method of contraception for 4 weeks after initiation and for 4 weeks after each dose escalation.
Zepbound Adverse Reactions
Adverse Reactions
Nausea, diarrhea, vomiting, constipation, abdominal pain, dyspepsia, inj site reactions, fatigue, hypersensitivity reactions, eructation, hair loss, GERD; acute kidney injury, acute gallbladder disease, acute pancreatitis, hypoglycemia.
Zepbound Clinical Trials
See Literature
Zepbound Note
Not Applicable
Zepbound Patient Counseling
See Literature
