INDICATIONS FOR USE

Tirzepatide is FDA approved for type 2 diabetes mellitus to improve glycemic control in adults. It is also indicated for obesity management and related weight-loss applications.

EVIDENCE RATING

✦✦✦ : FDA approved therapy with extensive human efficacy and safety data.

ROUTE OF ADMINISTRATION

• Subcutaneous injection

COMMON INITIAL DOSING REGIMENS

• Standard dosing: start at 2.5 mg weekly for 4 weeks, then increase to 5 mg weekly. Titrate gradually to 10 mg or 15 mg weekly to achieve desired glycemic control or degree of weight loss.

• NOTE: Many patients do not require anything close to the standard dosing. We strongly believe that dosing smaller amounts more frequently results in better outcomes. Each regimen is personalized to the individual patient’s sensitivity and response.

MECHANISM OF ACTION

• Tirzepatide is a dual agonist of glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptors. By activating these pathways, it enhances insulin secretion, suppresses glucagon release, and slows gastric emptying. It also reduces appetite and promotes weight loss through central mechanisms of satiety regulation.

• The combination of GIP and GLP-1 activity may offer synergistic benefits for glycemic control and weight reduction compared to GLP-1 receptor agonists alone.

COMMON SIDE EFFECTS

• Gastrointestinal: Nausea, vomiting, diarrhea, constipation, and abdominal discomfort. These are dose-dependent and often occur during dose escalation.

• Metabolic: Hypoglycemia, primarily when used with insulin or sulfonylureas.

• Injection Site: Mild irritation or redness at the injection site.

• Severe Effects: Rare events include pancreatitis, gallbladder disease, and worsening of diabetic retinopathy in patients with pre-existing disease.

CONTRAINDICATIONS

• Absolute: Personal or family history of medullary thyroid carcinoma (MTC), multiple endocrine neoplasia syndrome type 2 (MEN 2), or hypersensitivity to semaglutide or its excipients.

• Relative: Severe gastrointestinal disease, a history of pancreatitis, or significant renal impairment. Patients with gallbladder disease should be monitored due to the risk of gallstone formation.

NOTES ON EFFICACY / COMPOUNDING

• The average patient completing a course of tirzepatide for weight loss will lose approximately 23% of their body weight.

• Our formulations of tirzepatide are available compounded with Vitamin B6 (to decrease nausea).

LEARN MORE

• Evidence hound? Review our comprehensive listing of PubMed direct links to original research related to this medication.