Formulary
Sitagliptin: Indications, Dosing, Side Effects and Interactions
Inhibits dipeptidylpeptidase-4 to increase insulin secretion and lower glucagon secretion.
MedNext Academy | 3 min read
Sitagliptin: Indications, Dosing, Side Effects and Interactions
Inhibits dipeptidylpeptidase-4 to increase insulin secretion and lower glucagon secretion.
Drug action
Inhibits dipeptidylpeptidase-4 to increase insulin secretion and lower glucagon secretion.
Indications and dose
**Type 2 diabetes mellitus as monotherapy (if metformin inappropriate), or in combination with other antidiabetic drugs (including insulin) if existing treatment fails to achieve adequate glycaemic control**
- **Adult** (By Mouth): 100 mg once daily, for further information on use with other antidiabetic drugs-consult product literature.
Cautions
History of pancreatitis
Side effects
Common or very common Headache Uncommon Constipation; dizziness; skin reactions Frequency not known Angioedema; back pain; bullous pemphigoid (discontinue); cutaneous vasculitis; interstitial lung disease; joint disorders; myalgia; pancreatitis acute; renal impairment; Stevens-Johnson syndrome; vomiting Side-effects, further information Discontinue if symptoms of acute pancreatitis occur such as persistent, severe abdominal pain.
Interactions
**Severe interactions:**
- Metabolism may play a more significant role in the elimination of sitagliptin in the setting of severe renal impairment or end-stage renal disease (ESRD).
- For this reason, it is possible that potent CYP3A4 inhibitors (i.e.
**Other interactions (17):**
- Effects of other medicinal products on sitagliptin Clinical data described below suggest that the risk for clinically meaningful interactions by co-administered medicinal products is low.
- In vitro studies indicated that the primary enzyme responsible for the limited metabolism of sitagliptin is CYP3A4, with contribution from CYP2C8.
- In patients with normal renal function, metabolism, including via CYP3A4, plays only a small role in the clearance of sitagliptin.
- In vitro transport studies showed that sitagliptin is a substrate for p-glycoprotein and organic anion transporter-3 (OAT3).
- OAT3 mediated transport of sitagliptin was inhibited in vitro by probenecid, although the risk of clinically meaningful interactions is considered to be low.
- Metformin: Co-administration of multiple twice-daily doses of 1,000 mg metformin with 50 mg sitagliptin did not meaningfully alter the pharmacokinetics of sitagliptin in patients with type 2 diabetes.
Pregnancy
Avoid-toxicity in animal studies.
Breast feeding
Avoid-present in milk in animal studies.
Renal impairment
Dose adjustments Reduce dose to 50 mg once daily if eGFR 30-45 mL/minute/1.73 m 2 . M Reduce dose to 25 mg once daily if eGFR less than 30 mL/minute/1.73 m 2 . M See Prescribing in renal impairment .
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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