Sitagliptin at a glance
Medicine class
DPP-4 inhibitor, also called a gliptin.
Main use
Improving blood-glucose control in adults with type 2 diabetes.
Food
May be taken with or without food.
Low blood sugar
Uncommon when used alone, but risk increases with insulin or a sulphonylurea.
Kidney function
Kidney function should be checked because sitagliptin is mainly removed through the kidneys.
What is Sitagliptin used for?
Selected UK products are licensed for adults with type 2 diabetes to improve blood-glucose control alongside diet and exercise.
Used alone when blood glucose is inadequately controlled and metformin is unsuitable because of intolerance or a contraindication.
Used with metformin, a sulphonylurea or a thiazolidinedione when existing treatment is insufficient.
Used in certain combinations involving metformin with a sulphonylurea or thiazolidinedione.
Used alongside insulin, with or without metformin, when existing measures are insufficient.
How does Sitagliptin work?
Sitagliptin blocks DPP-4, allowing the incretin hormones GLP-1 and GIP to remain active longer. When glucose is raised, they increase insulin release and reduce glucagon, lowering glucose production by the liver. This glucose-dependent action means sitagliptin alone has a relatively low tendency to cause hypoglycaemia.
Sitagliptin preparations and strengths
Oral solution
Route: Oral
Strengths: 25 mg/mL
Tablet
Route: Oral
Strengths: 25 mg, 50 mg, 100 mg
How to take Sitagliptin
Follow the dispensing label and do not stop treatment without discussing it with the prescriber.
It may be taken with or without food.
Swallow the selected film-coated tablet whole with water.
Measure the oral solution accurately using its supplied oral syringe and refrigerate it as directed on the label.
Do not alter the formulation or amount taken without advice from a prescriber or pharmacist.
Sitagliptin side effects
Common or expected effects
- Headache.
- Low blood sugar, particularly with insulin or a sulphonylurea; symptoms can include sweating, shaking, hunger and confusion.
Get urgent medical advice
- Persistent, severe abdominal pain, which may indicate pancreatitis.
- Swelling of the face or throat, breathing difficulty or collapse, suggesting a serious allergic reaction.
- Blistering, peeling or extensive skin reactions, including possible bullous pemphigoid or Stevens–Johnson syndrome.
- Marked reduction in urine or other symptoms suggesting acute kidney injury.
Sitagliptin in pregnancy
Sitagliptin is not recommended during pregnancy because human safety information is limited. Anyone pregnant or planning pregnancy should ask their diabetes prescriber to review treatment rather than stopping without advice.
Sitagliptin while breastfeeding
Sitagliptin is not usually recommended during breastfeeding because it is unknown how much enters human milk. A prescriber should review the benefits, uncertainties and alternatives, particularly for a newborn or premature baby.
Sitagliptin interactions
Sitagliptin has a generally low potential for clinically important interactions, but some combinations need review or monitoring.
Insulin or sulphonylureas such as gliclazide
The combination increases hypoglycaemia risk, so existing diabetes treatment may need review.
Digoxin
Sitagliptin can slightly increase digoxin exposure; monitor people already at risk of digoxin toxicity.
Potent CYP3A4 inhibitors, including clarithromycin, itraconazole, ketoconazole or ritonavir
They may increase sitagliptin exposure in severe kidney impairment, although the clinical effect is not established.
Common questions about Sitagliptin
Answers are fully visible for fast scanning and source review.
Is sitagliptin hydrochloride monohydrate the same medicine as sitagliptin?
It is a salt form used in some products to provide the active medicine sitagliptin.
Can sitagliptin be taken with food?
Yes. The selected products may be taken with or without food.
Does sitagliptin cause low blood sugar?
It does not usually cause hypoglycaemia when used alone, but risk rises with insulin or a sulphonylurea.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.