What it does
Trelagliptin is a medication used to help control blood sugar levels in people with type 2 diabetes.
Commonly used for: type 2 diabetes, diabetes mellitus
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 19:56:10 · updated 2026-08-07 02:28:56
About this medicine
Trelagliptin is a medication used to help control blood sugar levels in people with type 2 diabetes.
What it treats
- type 2 diabetes
- diabetes mellitus
How it works
Trelagliptin works by increasing the levels of insulin produced by the body after meals and decreasing the amount of sugar produced by the liver.
Who it's for
This medication is for adults with type 2 diabetes who need help managing their blood sugar levels.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: trelagliptin
BNF-referencedTrelagliptin is a novel, long-acting DPP-4 inhibitor indicated for the management of type 2 diabetes mellitus. By inhibiting the enzyme DPP-4, trelagliptin increases the levels of incretin hormones, which promote insulin secretion and decrease glucagon levels in response to meals, thereby aiding in glycemic control.
Indications
- Type 2 diabetes mellitus
Dosage
Children: Refer to BNF for Children for specific dosing guidelines.
Adults: Refer to BNF for specific dosing guidelines.
Mechanism of action
Trelagliptin selectively inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which is responsible for degrading incretin hormones such as GLP-1 and GIP. By prolonging the action of these hormones, trelagliptin enhances insulin secretion from pancreatic beta cells and suppresses glucagon secretion from alpha cells, leading to improved glucose homeostasis.
Pharmacodynamics
The pharmacodynamic effects of trelagliptin include increased insulin secretion in a glucose-dependent manner, reduced glucagon release, and improved glycemic control. The long duration of action allows for once-weekly dosing, providing sustained pharmacological effects.
Pharmacokinetics
Trelagliptin exhibits linear pharmacokinetics with a terminal half-life of approximately 24-30 hours. After subcutaneous administration, peak plasma concentrations are reached within 24 hours. The drug is primarily eliminated via the kidneys, with a small proportion undergoing hepatic metabolism. The systemic bioavailability is high, allowing for effective oral dosing.
Contra-indications
- Hypersensitivity to trelagliptin or any of its components
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
Adverse effects
- Headache
- Nausea
- Diarrhea
- Hypoglycemia
- Upper respiratory tract infection
- Pancreatitis
- Allergic reactions
Interactions
- May enhance the hypoglycemic effect of other antidiabetic agents
- No significant drug interactions reported with common medications
Precautions
- Use with caution in patients with renal impairment
- Monitor for signs of pancreatitis
- Consider the risk of hypoglycemia when used with other antidiabetic medications
Pregnancy
There is insufficient data on the use of trelagliptin in pregnancy. It should be used only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
It is not known whether trelagliptin is excreted in human milk. Caution should be exercised when trelagliptin is administered to a nursing woman.
Storage
Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.
Formulations
- Tablets
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: trelagliptin
PubChem CID 15983988Molecular formula: C18H20FN5O2
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.