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ALIMENTARY TRACT AND METABOLISM › DRUGS USED IN DIABETES › BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS › Other blood glucose lowering drugs, excl. insulins
tirzepatide
A10BX16
Forms & Strengths
- Subcutaneous solution in single-dose pen/vial: 2.5 mg/0.5 mL
- Subcutaneous solution in single-dose pen/vial: 5 mg/0.5 mL
- Subcutaneous solution in single-dose pen/vial: 7.5 mg/0.5 mL
- Subcutaneous solution in single-dose pen/vial: 10 mg/0.5 mL
- Subcutaneous solution in single-dose pen/vial: 12.5 mg/0.5 mL
- Subcutaneous solution in single-dose pen/vial: 15 mg/0.5 mL
Adult Dosing
- Type 2 Diabetes Mellitus: Initial 2.5 mg subcutaneously once weekly for 4 weeks, then increase to 5 mg once weekly. May increase in 2.5 mg increments after at least 4 weeks if needed. Maximum dose: 15 mg subcutaneously once weekly.
- Chronic Weight Management: Initial 2.5 mg subcutaneously once weekly for 4 weeks, increase to 5 mg once weekly for 4 weeks. May increase in 2.5 mg increments after at least 4 weeks. Maintenance doses: 5 mg, 10 mg, or 15 mg once weekly. Maximum dose: 15 mg subcutaneously once weekly.
Pediatric Dosing
- Safety and effectiveness in pediatric patients below 18 years of age have not been established.
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
- Chronic weight management in adults with an initial body mass index (BMI) of 30 kg/m² or greater (obesity) or 27 kg/m² or greater (overweight) in the presence of at least one weight-related comorbid condition.
Mechanism of Action
- Dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist.
- Activates GIP and GLP-1 receptors, augmenting glucose-dependent insulin secretion, decreasing inappropriate glucagon secretion, and slowing gastric emptying.
- Reduces food intake and body weight through central appetite suppression mechanisms.
Contraindications
- Personal or family history of medullary thyroid carcinoma (MTC).
- Patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2).
- Known hypersensitivity to tirzepatide or any of its excipients.
Adverse Reactions
- Nausea
- Diarrhea
- Decreased appetite
- Vomiting
- Constipation
- Dyspepsia
- Abdominal pain
- Injection site reactions
- Fatigue
- Hypoglycemia (when used with insulin secretagogues or insulin)
Drug Interactions
- Insulin and insulin secretagogues (e.g., sulfonylureas): Increased risk of hypoglycemia; dose reduction of insulin or secretagogues may be required.
- Oral medications with narrow therapeutic indices or requiring rapid gastrointestinal absorption: Tirzepatide delays gastric emptying and may impact absorption of concomitantly administered oral drugs.
Curated Content: Needs Vetting Before Put to Clinical Use