Last update Aug. 18, 2017

Sitagliptin Phosphate

Low Risk

Moderately safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.

It promotes pancreatic insulin secretion by inhibiting the DPP-4 enzyme that degrades the intestinal hormone GLP-1 that is activated when eating (Baetta 2011, Scheen 2011).
Oral administration, once daily.
Very low risk of hypoglycemia. Doses 6 times higher than normal for 10 days or 4 times higher for 28 days do not produce side effects (EMA 2016). The most common side effect is rhinopharyngitis.

Since the last update we have not found published data on its excretion in breast milk.

Its pharmacokinetic data (EMA 2016, Scheen 2011): large volume of distribution, moderately high molecular weight and low liposolubility, make it unlikely that it will pass through to breast milk in significant amounts.

Until there is more published data on this drug in relation to breastfeeding, safer known alternatives may be preferable, especially during the neonatal period and in case of prematurity.

Diet, exercise, and breastfeeding improve blood sugar levels.

Among the antidiabetics of this same group, Saxagliptin and Vildagliptin would be preferable due to their short half-life (less than 3 hours).


See below the information of these related products:

  • Maternal Diabetes mellitus (Moderately safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.)
  • Saxagliptin (Moderately safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.)
  • Vildagliptin (Moderately safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.)

Alternatives

  • Acarbose ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Chlorpropamide (Moderately safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.)
  • Glibenclamide ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Hypocaloric Diet ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Maternal Sport ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Metformin Hydrochloride ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Miglitol ( Safe. Compatible. Minimal risk for breastfeeding and infant.)
  • Tolbutamide ( Safe. Compatible. Minimal risk for breastfeeding and infant.)

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Sitagliptin Phosphate in other languages or writings:

Tradenames

Main tradenames from several countries containing Sitagliptin Phosphate in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 87 %
Molecular weight 523 daltons
Protein Binding 38 %
VD 2.8 l/Kg
Tmax 1 - 4 hours
12.4 hours

References

  1. EMA. Sitagliptina. Ficha técnica. 2016 Full text (in our servers)
  2. EMA. Sitagliptin. Drug Summary. 2016 Full text (in our servers)
  3. Golightly LK, Drayna CC, McDermott MT. Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Abstract
  4. Scheen AJ. A review of gliptins in 2011. Expert Opin Pharmacother. 2012 Abstract Full text (link to original source)

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