Dr Sharon Rees @reesprescribe
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
Dr Sharon Rees @reesprescribe
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
Dr Sharon Rees @reesprescribe
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
Dr Sharon Rees @reesprescribe
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
Dr Sharon Rees @reesprescribe
Day 5: Adverse drug effects; common include GI disturbance, constipation, malaise, nausea, asthenia. Uncommon; acute pancreatitis, cholelithiasis. Risk of DKA when combined with insulin unknown, so caution (NOT exhaustive)
Dr Sharon Rees @reesprescribe
Day 6: Potential for hypoglycaemia when combined with other anti-diabetic agents (lower dose as needed). Delayed gastric emptying can reduce absorption of oral medicines e.g digoxin, warfarin. Also potential impact on absorption of oral contraceptives (additional method recommended). NOT exhaustive
Dr Sharon Rees @reesprescribe
Day 7: Synergism from both incretin actions is believed to produce more weight loss compared to GLP-1 stimulation alone. Triple receptor agonists are in development (with glucagon activity) & there is also interest in GIP receptor antagonism (may cause weight loss). More insight needed to develop drugs targeting this system
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In addition to the posts on X, read the BNF monograph on tirzepatide. Another useful source is the Summary of Product Characteristics for tirzepatide – see links below. Once you have completed this, answer the 10 questions. Submit your answers to reesprescribe@gmail.com. If you answer at least eight out of 10 questions correctly, you will receive your CPD certificate via email.
- Tirzepatide is one of a range of dual incretin agonists TRUE or FALSE?
- Tirzepatide can be combined with all other hypoglycaemic drugs used for diabetes TRUE or FALSE?
- Tirzepatide is licensed for diabetes but not weight loss TRUE or FALSE?
- Tirzepatide is given by a once weekly s.c injection TRUE or FALSE?
- Which of the following is TRUE?
- Tirzepatide has enzymatic action to enhance the incretin system
- Tirzepatide is engineered to mimic both major gut incretins
- Tirzepatide antagonises hormones in the incretin pathway
- Tirzepatide enhances glucagon output and diminishes insulin output
- Dose reduction can be needed when combined with insulin, but no other anti-diabetic drugs TRUE or FALSE?
- Tirzepatide can support weight loss by alterations to appetite and satiety TRUE or FALSE?
- Which of the following is NOT a common adverse drug effect?
- Angioedema
- Constipation
- Nausea
- Malaise
- Tirzepatide might affect the efficacy of the contraceptive pill TRUE or FALSE?
- Which of the following is TRUE?
- Tirzepatide has a high number and range of drug-drug interactions
- Tirzepatide cannot be used in renal impairment
- Tirzepatide is associated with injection site reactions
- Tirzepatide is a long-acting agent
Further reading on #tirzepatide
- https://bnf.nice.org.uk/drugs/tirzepatide/
- https://www.medicines.org.uk/emc/product/14203/smpc#gref