Last update: Sept. 2, 2017


Low Risk for breastfeeding

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 GLP-1 and GIP intestinal hormones involved in the physiological regulation of glucose, which are activated by eating (EMA 2016, Baetta, 2011, Scheen 2011).
Administered orally once a day.
Very low risk of hypoglycemia in monotherapy. Very low frequency of clinically significant side effects. Dosage up to 120 times higher than normal did not produce side effects (EMA 2016).

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

Its pharmacokinetic data (EMA 2016, Scheen 2011): high volume of distribution and high percentage of protein binding make it unlikely that significant amounts will pass into breast milk, but low molecular weight, low metabolism and its effective elimination half-life of 12 hours would facilitate its possible passing into breast milk.

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:


Suggestions made at e-lactancia are done by APILAM´s pediatricians and pharmacists, and are based on updated scientific publications.
It is not intended to replace the relationship you have with your doctor but to compound it.

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

Linagliptin in other languages or writings:


Main tradenames from several countries containing Linagliptin in its composition:


Variable Value Unit
Oral Bioavail. 30 %
Molecular weight 473 daltons
Protein Binding 70 - 99 %
VD 5,3 - 15,9 l/Kg
Tmax 1 - 3 hours
T1/2 120 - 131 (real: 12) hours


  1. EMA. Linagliptin. Drug Summary. 2017 Full text (in our servers)
  2. EMA. Linagliptina. Ficha técnica. 2017 Full text (in our servers)
  3. Scheen AJ. A review of gliptins in 2011. Expert Opin Pharmacother. 2012 Abstract Full text (link to original source)
  4. Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs. 2011 Abstract
  5. Scheen AJ. Linagliptin for the treatment of type 2 diabetes (pharmacokinetic evaluation). Expert Opin Drug Metab Toxicol. 2011 Abstract

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