ZEPAD 2.5MG/0.5ML INJECTION

Indications

• Type 2 diabetes mellitus
• Diabetes management in adults

Dosage

Children: Refer to the BNF for Children for any paediatric dosing recommendations.

Adults: Refer to the BNF for specific dosing guidelines based on individual patient needs and treatment response.

Mechanism of action

Tirzepatide works by mimicking the action of two incretin hormones, GLP-1 and GIP. Incretins play a crucial role in glucose metabolism by enhancing insulin secretion from the pancreas in a glucose-dependent manner, inhibiting glucagon release, and promoting satiety. The activation of the GLP-1 receptor leads to increased cAMP levels, improved insulin sensitivity, and decreased appetite. By also activating the GIP receptor, tirzepatide further amplifies the insulinotropic effect, contributing to improved glycemic control.

Pharmacodynamics

Tirzepatide's pharmacodynamic profile includes significant reductions in HbA1c levels and body weight in individuals with type 2 diabetes. Its dual receptor activation is associated with enhanced postprandial insulin secretion and reduced fasting and postprandial glucose levels. The effects are dose-dependent and can lead to substantial improvements in glycemic control over time.

Pharmacokinetics

Tirzepatide is administered via subcutaneous injection, with a peak plasma concentration occurring approximately 24 to 72 hours post-dose. It has a half-life of approximately 5 days, allowing for once-weekly dosing. The drug undergoes proteolytic degradation, with metabolites eliminated primarily via the renal route. Steady-state concentrations are achieved after 4 to 5 weeks of consistent dosing, and it demonstrates linear pharmacokinetics within the therapeutic range.

Contra-indications

• Hypersensitivity to tirzepatide or any component of the formulation
• Personal or family history of medullary thyroid carcinoma
• Multiple endocrine neoplasia syndrome type 2

Adverse effects

• Nausea
• Vomiting
• Diarrhoea
• Constipation
• Decreased appetite
• Abdominal pain
• Injection site reactions
• Pancreatitis

Interactions

• May enhance the effects of other antidiabetic medications
• Caution advised with medications that affect gastrointestinal motility

Precautions

• Monitor for signs of pancreatitis
• Consider risk of hypoglycemia when used with insulin or sulfonylureas
• Assess renal function prior to initiation and during treatment
• Evaluate for gallbladder disease prior to treatment

Pregnancy

There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether tirzepatide is excreted in human milk. Caution is advised when administering to nursing women.

Storage

Store in the refrigerator (2°C to 8°C). Do not freeze. Once in use, may be stored at room temperature (up to 30°C) for up to 21 days.

Formulations

• Subcutaneous injection solution