Last update April 15, 2024

Bosentan

Very Low Risk

Safe. Compatible. Minimal risk for breastfeeding and infant.

It is an endothelin receptor antagonist. Indicated in the treatment of idiopathic pulmonary arterial hypertension or hypertension associated with connective tissue disease or heart disease. Oral administration twice daily. 

Its pharmacokinetic data (moderately high molecular weight, high percentage of protein binding, high volume of distribution and acidic pKa) explain the very low passage into breast milk observed. (Nauwelaerts 2022)

Its low oral bioavailability makes it difficult to pass into infant plasma from ingested breast milk, except in premature infants and in the immediate neonatal period, where there may be greater intestinal permeability. 

A 30-week preterm infant who was breastfed for 2.5 months on Bosentan and Sildenafil did not have any problems (Molelekwa 2005). An infant breastfed for more than 21 months, with the mother taking Bosentan and Sildenafil from 6 months after birth, had no clinical problems with partial breastfeeding. (Nauwelaerts 2022) 

It is used in Pediatrics from 1 year of age or 10 kg of weight and there are publications with neonatal use and in premature infants with very good tolerance. (Fatima 2018, Pediamecum 2014, Nakwan 2009, Maingourd 2008, Maiya 2006, Rosenzweig 2005, Molelekwa 2005, Barst 2003)

Alternatives

  • Epoprostenol (Possibly safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.)
  • Iloprost (Possibly safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.)

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

Bosentan in other languages or writings:

Tradenames

Main tradenames from several countries containing Bosentan in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 50 %
Molecular weight 552 daltons
Protein Binding 98 %
VD 0.26 l/Kg
Tmax 3 - 5 hours
5 hours
Theoretical Dose 0.0003 - 0.0006 mg/Kg/d
Relative Dose 0.24 %

References

  1. Nauwelaerts N, Ceulemans M, Deferm N, Eerdekens A, Lammens B, Armoudjian Y, Van Calsteren K, Allegaert K, de Vries L, Annaert P, Smits A. Case Report: Bosentan and Sildenafil Exposure in Human Milk - A Contribution From the ConcePTION Project. Front Pharmacol. 2022 Jun 15;13:881084. Abstract Full text (link to original source)
  2. Fatima N, Arshad S, Quddusi AI, Rehman A, Nadeem A, Iqbal I. Comparison Of The Efficacy Of Sildenafil Alone Versus Sildenafil Plus Bosentan In Newborns With Persistent Pulmonary Hypertension. J Ayub Med Coll Abbottabad. 2018 Jul-Sep;30(3):333-336. Abstract
  3. Pediamécum (AEP). Bosentan. Ficha técnica. 2014 Full text (link to original source) Full text (in our servers)
  4. AEMPS. Bosentan. Ficha técnica. 2013 Full text (in our servers)
  5. Nakwan N, Choksuchat D, Saksawad R, Thammachote P, Nakwan N. Successful treatment of persistent pulmonary hypertension of the newborn with bosentan. Acta Paediatr. 2009 Abstract
  6. Goissen C, Ghyselen L, Tourneux P, Krim G, Storme L, Bou P, Maingourd Y. Persistent pulmonary hypertension of the newborn with transposition of the great arteries: successful treatment with bosentan. Eur J Pediatr. 2008 Abstract
  7. Maiya S, Hislop AA, Flynn Y, Haworth SG. Response to bosentan in children with pulmonary hypertension. Heart. 2006 Abstract
  8. Rosenzweig EB, Ivy DD, Widlitz A, Doran A, Claussen LR, Yung D, Abman SH, Morganti A, Nguyen N, Barst RJ. Effects of long-term bosentan in children with pulmonary arterial hypertension. J Am Coll Cardiol. 2005 Abstract
  9. Molelekwa V, Akhter P, McKenna P, Bowen M, Walsh K. Eisenmenger's syndrome in a 27 week pregnancy--management with bosentan and sildenafil. Ir Med J. 2005 Abstract
  10. Dingemanse J, van Giersbergen PL. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet. 2004 Abstract
  11. Barst RJ, Ivy D, Dingemanse J, Widlitz A, Schmitt K, Doran A, Bingaman D, Nguyen N, Gaitonde M, van Giersbergen PL. Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension. Clin Pharmacol Ther. 2003 Abstract

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