Generic
Tirzepatide
37 brands available in the market
At a glance
Tirzepatide is a GIP and GLP-1 receptor agonist used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Description
Tirzepatide is a 39-amino-acid modified peptide that selectively binds to and activates both GIP and GLP-1 receptors. It enhances first and second-phase insulin secretion and reduces glucagon levels in a glucose-dependent manner. The C20 fatty diacid moiety enables albumin binding and prolongs the half-life.
Indications
- Type 2 diabetes mellitus (as an adjunct to diet and exercise)
Therapeutic class
GLP-1 Receptor Agonists
Pharmacological class
Dual GIP/GLP-1 Receptor Agonist
Pharmacology
Tirzepatide activates GIP and GLP-1 receptors, enhancing glucose-dependent insulin secretion and reducing glucagon levels. It slows gastric emptying, reduces appetite, and promotes weight loss.
Mechanism of action
Increases insulin secretion and decreases glucagon by activating GIP and GLP-1 receptors.
Dosage
Adult Dose (SC):
- Starting: 2.5 mg once weekly for 4 weeks
- Maintenance: 5 mg once weekly; increase by 2.5 mg every 4 weeks if needed; max 15 mg once weekly
Administration
- Subcutaneous injection (abdomen, thigh, or upper arm)
- Once weekly, any time of day, with or without meals
- Rotate injection sites weekly
- If used with insulin, administer as separate injections; do not mix
Missed dose
- If within 4 days of missed dose, take it as soon as possible; if more than 4 days, skip it
- Resume next dose on the regularly scheduled day
Side effects
Common Side Effects:
- Nausea
- Diarrhea
- Decreased appetite
- Vomiting
- Constipation
- Dyspepsia
- Abdominal pain
Precautions & warnings
- Risk of thyroid C-cell tumors (MTC); contraindicated in personal/family history of MTC or MEN 2
- Do not use in type 1 diabetes or diabetic ketoacidosis
- Monitor for signs of pancreatitis
- Caution in history of diabetic retinopathy
- Monitor renal function with severe GI reactions
- Do not use during pregnancy
Contraindications
- Hypersensitivity to tirzepatide or any component
- Personal or family history of MTC
- Multiple Endocrine Neoplasia syndrome type 2 (MEN 2)
Drug interactions
- Insulin secretagogues (sulfonylureas) or insulin: Increased hypoglycemia risk; consider dose reduction
- Oral medications: Gastric emptying delay may affect absorption
- Oral hormonal contraceptives: Use non-oral or barrier method for 4 weeks
Food interactions
Caution is advised when consuming alcohol with Tirzepatide; consult your doctor.
Use in pregnancy
Use in Pregnancy: May be unsafe; use only if clearly needed; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Adequate information not available; consult your doctor.
Pediatric use
Safety and efficacy not established in children <18 years
Geriatric use
Caution required in elderly patients
Renal / hepatic impairment
Renal Impairment: Monitor renal function with severe GI reactions; consult your doctor.
Hepatic Impairment: Caution required; consult your doctor.
Overdose effects
Overdose may require supportive treatment; half-life approximately 5 days; monitor for symptoms.
Storage conditions
Store at 2-8°C in a refrigerator; do not freeze; protect from light; keep out of reach and sight of children.
Chemical structure
Tirzepatide