Tirzepatide 10mg Novo

Description

Properties

Tirzepatide is a long-acting, selective agonist of the ‘glucose-dependent insulinotropic polypeptide’ (GIP) and ‘glucagon-like peptide-1’ (GLP-1) receptors. Its activity on the GIP receptor is comparable to the body’s natural GIP hormone, while its activity on the GLP-1 receptor is lower than the body’s natural GLP-1 hormone. Both receptors are present on, among others, the β-cells of the pancreas, the gastrointestinal tract, and the brain. GIP receptors are also found on adipocytes (fat cells).

Glycemic Control

Tirzepatide lowers fasting and post-meal blood glucose levels in type 2 diabetes through various mechanisms. It increases glucose sensitivity of the β-cells in the pancreas, improves first- and second-phase insulin secretion in a glucose-dependent manner, enhances insulin sensitivity, and lowers glucagon levels. Tirzepatide also delays gastric emptying (especially at the beginning of treatment), which slows glucose absorption from meals.

Weight Loss

Tirzepatide activates GIP and GLP-1 receptors on neurons in brain regions involved in regulating appetite and food intake. It also activates GIP receptors on adipocytes, regulating glucose uptake, lipid uptake, and lipolysis. Tirzepatide increases feelings of satiety and fullness while reducing hunger, resulting in decreased energy intake. It also reduces food cravings and preference for high-sugar and high-fat foods. Body weight decreases, mainly due to reduced body fat mass.

Side Effects

Very common (>10%):

• Hypoglycemia (especially when used with sulfonylurea or insulin in type 2 diabetes)

• Nausea, vomiting, abdominal pain, diarrhea, constipation

Common (1-10%):

• Hypersensitivity reactions (e.g., urticaria, eczema)

• Hypoglycemia when used with metformin and SGLT-2 inhibitors

• Dizziness, low blood pressure

• Reduced appetite, indigestion, burping, gastroesophageal reflux disease (GERD), bloating, flatulence

• Hair loss

• Fatigue, injection site reactions (e.g., redness, itching)

• Increased heart rate

• Increased serum lipase or amylase, increased blood calcitonin

Uncommon (0.1-1%):

• Hypoglycemia with metformin in type 2 diabetes

• Weight loss

• Taste disorders, abnormal sensations

• Gallstones, inflammation of gallbladder, acute pancreatitis, delayed gastric emptying

• Injection site pain

Rare (0.01-0.1%):

• Anaphylactic reaction

• Angioedema

Gastrointestinal side effects are usually mild or moderate, are more common during dose escalation, and decrease over time.

Dizziness, low blood pressure, and hair loss mainly occur in patients with obesity or overweight, with or without type 2 diabetes.

Dosage

Type 2 Diabetes Mellitus, Weight Management
Adults (including elderly)

• Subcutaneous injection: starting dose 2.5 mg once weekly.

• After 4 weeks, increase to 5 mg once weekly.

• If needed, increase further in 2.5 mg increments every 4 weeks up to a maximum of 15 mg once weekly.

If added to metformin and/or an SGLT2 inhibitor, maintain the current doses of these medications.

If added to a sulfonylurea and/or insulin, consider lowering the dose of sulfonylurea or insulin to reduce the risk of hypoglycemia; self-monitoring of blood glucose is necessary. Insulin dose reduction should be done gradually.

No dose adjustment is needed in patients with reduced kidney function. Use caution in severe kidney impairment or end-stage renal disease due to insufficient data.

No dose adjustment is needed in patients with reduced liver function. Use caution in severe liver impairment due to insufficient data.