TIRZEPATIDE

02 March 2024
Volume 6 · Issue 3

Abstract

In this column, Sharon Rees aims to refresh knowledge and interest in some of the commonly used drugs in a series of posts on X. This month she is talking about #tirzepatide

Day 1: Following the diabetes & weight loss successes of GLP-1 agonists such as semaglutide, #tirzepatide is the 1st ‘dual’ incretin drug. Peptide engineering has been used to bring GLP-1 activity into the GIP sequence, permitting agonism of both main gut incretin hormones

Day 2: #tirzepatide is used for diabetes as monotherapy OR in combination with other diabetes drugs. Weekly s.c injection 5-15mg, reduced as needed if added to a sulphonylurea or insulin. Start at 2.5mg & incremental up-titration. Licensed for weight loss in UK in 2023; NICE consultation on use is pending in 2024

Day 3: #tirzepatide is given s.c with good bioavailabilty. It is highly bound to albumin by design to prolong t½. Eliminated by metabolism, where the amino acid sequence is metabolised by proteolysis as well as oxidation/hydrolysis breakdown. Metabolites excreted urine & faeces. Elimination t½ ~ 5 days

Day 4: #tirzepatide provides long-acting agonism of 2 main incretins leading to increased insulin output/duration of action. Improves glycaemic control & weight loss via reduced appetite & increased satiety. Potentiation of glucose-stimulated insulin response allows coordinated control, minimising hypoglycaemic risks

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