Sitagliptin
An oral DPP-4 inhibitor (gliptin) taken once a day to raise mealtime insulin and lower glucagon in type 2 diabetes.
Drug card
- Class
- DPP-4 inhibitor
- How it works
- Blocking the enzyme DPP-4, so gut incretin hormones last longer
- Used for
- Type 2 diabetes
- Known for
- Inflammation of the pancreas (pancreatitis)
- Blistering skin disease (bullous pemphigoid)
- Its name
- -gliptin means a DPP-4 inhibitor (gliptin)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does sitagliptin work?
Sitagliptin is a competitive inhibitor of DPP-4 that spares the related enzymes DPP-8 and DPP-9. One daily dose keeps DPP-4 blocked for 24 hours, so active GLP-1 and GIP levels after meals rise two- to three-fold. About four-fifths is excreted unchanged in the urine, so the dose is lowered in kidney impairment.
Like other DPP-4 inhibitors: DPP-4 inhibitors block dipeptidyl peptidase-4, the enzyme that quickly inactivates the gut incretin hormones GLP-1 and GIP. Active incretin levels after a meal rise two- to three-fold, boosting insulin release and lowering glucagon, but only when glucose is normal or high. On their own they therefore rarely cause hypoglycemia, and body weight does not rise.
Uses
What is sitagliptin used for?
- Type 2 diabetes
Side effects
Side effects of sitagliptin
- Inflammation of the pancreas (pancreatitis)Known forSerious
- Blistering skin disease (bullous pemphigoid)Known forSerious
- Colds and sore throat (nasopharyngitis)
- Headache
- Severe allergic reaction (anaphylaxis)Serious
- Swelling of face and throat (angioedema)Serious
- Stevens-Johnson syndrome and other skin peelingSerious
- Severe, disabling joint pain
- Worse kidney function, including acute kidney injurySerious
- Heart failure (a class warning)Serious
- Hypoglycemia with a sulfonylurea or insulin
- Muscle breakdown (rhabdomyolysis), rareSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Check kidney function before starting and from time to time; the dose is reduced when eGFR is below 45.
- Stop it if pancreatitis is suspected; it has not been studied in people with past pancreatitis.
- Not for type 1 diabetes.
Good to know: Cleared mainly by the kidneys, so unlike linagliptin its dose depends on eGFR. Weight-neutral.
Remember it
A way to remember it
Gliptins guard GLP-1.
DPP-4 normally inactivates GLP-1 and GIP within minutes. Blocking it keeps them active, and because their effect depends on glucose, hypoglycemia is rare unless a sulfonylurea or insulin is added.
Written for biofideX
Its name
-gliptin means DPP-4 inhibitor (gliptin)
Sitagliptin, linagliptin, saxagliptin and vildagliptin block dipeptidyl peptidase-4, so incretin hormones such as GLP-1 last longer.
- Every drug name stem
Its class
DPP-4 inhibitors
Other DPP-4 inhibitors with a card:
Easily mixed up with GLP-1 receptor agonists, SGLT2 inhibitors and sulfonylureas.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Diabetes
Sitagliptin is one of 14 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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