Tirzepatide

Class
Hypoglycemic agents
Subclass
Dual glucose-dependent insulinotropic polypeptide / glucagon-like peptide 1 receptor agonists
Substance name
Tirzepatide
Brand names
Mounjaro®, Zepbound®
Common formulations
Solution for injection
Dosage and administration
Adults patients
Diabetes mellitus type 2
•
Start at: 2.5 mg SC weekly for 4 weeks
•
Maintenance: 5-15 mg SC weekly (Mounjaro®)
Administered subcutaneously in the abdomen, thigh, or upper arm. Administered at any time of day, with or without meals. Titrate in 2.5 mg increments at 4-week intervals as needed for glycemic control.
Obesity
•
Start at: 2.5 mg SC weekly for 4 weeks
•
Maintenance: 5-15 mg SC weekly (Zepbound®)
Administered subcutaneously in the abdomen, thigh, or upper arm. Administered at any time of day, with or without meals. Titrate in 2.5 mg increments at 4-week intervals.
Obstructive sleep apnea in patients with obesity • Moderate-to-severe
•
Start at: 2.5 mg SC weekly for 4 weeks
•
Maintenance: 10-15 mg SC weekly (Zepbound®)
Administered subcutaneously in the abdomen, thigh, or upper arm. Administer at any time of day, with or without meals. Titrate in 2.5 mg increments at 4-week intervals.
Overweight • In the presence of weight-related comorbidities
•
Start at: 2.5 mg SC weekly for 4 weeks
•
Maintenance: 5-15 mg SC weekly (Zepbound®)
Administered subcutaneously in the abdomen, thigh, or upper arm. Administer at any time of day, with or without meals. Titrate in 2.5 mg increments at 4-week intervals.
Indications for use
Labeled indications
Adults
•
Treatment of diabetes mellitus type 2
•
Treatment of obesity
•
Treatment of obstructive sleep apnea in patients with obesity (moderate-to-severe)
•
Treatment of overweight (in the presence of weight-related comorbidities)
Safety risks
Boxed warnings
Thyroid cancer
•
Do not use tirzepatide in patients with a personal or family history of medullary thyroid cancer or in patients with MEN2. Counsel patients regarding the potential risk for and symptoms of medullary thyroid carcinoma.
Contraindications
Hypersensitivity to tirzepatide or its components
T1DM or diabetic ketoacidosis
Warnings and precautions
Acute pancreatitis
•
Maintain a high level of suspicion, as tirzepatide has been associated with an increased risk of acute pancreatitis, including fatal and non-fatal hemorrhagic and necrotizing pancreatitis. Monitor patients for signs and symptoms of pancreatitis. Discontinue tirzepatide if acute pancreatitis is suspected.
Anaphylaxis, angioedema
•
Use caution in patients with a history of anaphylaxis or angioedema with other GLP-1 receptor agonists.
Decreased blood glucose
•
Use caution in patients taking insulin or insulin secretagogues. Consider reducing the insulin or insulin secretagogue dose.
Exacerbation of diabetic retinopathy
•
Maintain a high level of suspicion, as rapid improvement in glucose control has been associated with a temporary worsening of diabetic retinopathy. Monitor for progression of diabetic retinopathy.
Exacerbation of gastrointestinal disorders
•
Maintain a high level of suspicion, as tirzepatide has been associated with an increased risk of gastrointestinal adverse reactions. Avoid using tirzepatide in patients with severe gastrointestinal disorders, including severe gastroparesis.
Gallbladder disease
•
Maintain a high level of suspicion, as tirzepatide has been associated with an increased risk of cholelithiasis and cholecystitis.
Suicidal ideation
•
Maintain a high level of suspicion, as suicidal behavior and ideation have been reported in clinical trials with other chronic weight management products. Monitor for new or worsening depression, suicidal thoughts/behavior, and/or changes in mood or behavior. Avoid using tirzepatide in patients with a history of suicidal attempts or active suicidal ideation. Discontinue tirzepatide if suicidal thoughts or behaviors occur.
Specific populations
Renal impairment
eGFR 0-90 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required. Monitor renal function.
Renal replacement therapy
Any modality
•
Use acceptable. No dose adjustment required. Monitor renal function.
Hepatic impairment
Any severity
•
Use acceptable. No dose adjustment required.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: D
•
Consider safer alternatives. Evidence of fetal harm in humans. Insulin is the preferred first-line treatment for diabetes in pregnancy. Do not use tirzepatide for weight loss during pregnancy.
Breastfeeding
Use only if benefits outweigh potential risks.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
Constipation, diarrhea, loss of appetite, nausea, vomiting, tachycardia
Common 1-10%
•
Abdominal distension, cholelithiasis, ↓ blood glucose, drug hypersensitivity reaction, gastroesophageal reflux, hypotension, ↑ serum lipase, nasopharyngitis, abdominal pain, belching, dizziness, dyspepsia, fatigue, flatulence, hair loss, headache, injection site reactions
Uncommon < 1%
•
Acute kidney injury, acute cholecystitis, acute pancreatitis
Unknown frequency
•
Anaphylaxis, angioedema, ileus, ↑ amylase
Interactions
Drug(s)
Check Interactions
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