Manufacturer: Dragon Pharma
Pharmaceutical name: Tirzepatide
Pack: 1 vial (5 mg)
Tirzepatide is an agonist for the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor, which has been approved by the FDA for managing type 2 diabetes mellitus. It is crucial to highlight that tirzepatide is not authorized for the treatment of type 1 diabetes mellitus and has not been evaluated in individuals with pancreatitis. As a GIP and GLP-1 receptor agonist, tirzepatide significantly enhances glycemic control in those with type 2 diabetes and contributes to notable weight loss.
Tirzepatide may also be utilized off-label for obesity management. Currently, it is used as a second-line treatment for diabetes, akin to GLP-1 medications such as semaglutide. This medication is administered as a subcutaneous injection once a week, with incremental dose adjustments.
Tirzepatide is a synthetic peptide that acts as a dual agonist for the gastric inhibitory polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) receptors. It consists of 39 amino acids and is an analog of gastric inhibitory polypeptide. Functionally, it promotes insulin secretion from the pancreas, leading to decreased hyperglycemia. Additionally, tirzepatide raises adiponectin levels. Its dual action results in a more significant reduction of hyperglycemia compared to GLP-1 agonists alone and helps reduce appetite.
Pharmacokinetics:
Absorption: Tirzepatide exhibits a bioavailability of roughly 80%, with peak serum levels achieved within 8 to 72 hours.
Distribution: The average apparent steady-state volume of distribution (Vd) for tirzepatide is about 10.3 L, and it has a high affinity for plasma albumin, binding approximately 99% of it.
Metabolism: After injection, the peptide structure experiences proteolytic cleavage, while the C20 fatty diacid is subject to beta-oxidation and amide hydrolysis.
Excretion: Tirzepatide has a half-life of 5 days, permitting once-weekly dosing, and it is eliminated via urine and feces as metabolites.