Last update May 23, 2024

Nebivolol

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

It is a cardioselective beta blocker β1 adrenérgico which reduces heart rate and blood pressure. Indicated in the treatment of arterial hypertension (AHT) and chronic heart failure. Oral administration once a day.

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

Its pharmacokinetic data (very high percentage of protein binding and large volume of distribution) make transfer to milk in significant quantities unlikely.

It is metabolized through the CYP2D6 isoenzyme. There are fast metabolizing persons (the majority) and other slow ones. Slow metabolism implies an 8-fold higher bioavailability (almost complete), higher plasma concentrations and an elimination half-life up to three times longer than those of rapid metabolizers (AEMPS 2017, FDA 2010), which could lead to greater excretion in breastmilk.

The excretion capacity in milk of beta-blockers is marked by its percentage of protein binding which varies considerably from one to another. (Anderson 2018, Tamargo 2011, Riant 1986)

Beta-blockers are not considered the treatment of choice for hypertension unless migraine or angina prophylaxis coexists. (Anderson 2018)

Until there is more published information on this drug in relation to breastfeeding, known alternatives with a safer pharmacokinetic profile during breastfeeding may be preferable, both in the same group of antihypertensives and others (Anderson 2018, Malachias 2016, Serrano 2015), especially in the neonatal period and in case of prematurity.

The protective role of breastfeeding against maternal hypertension has been proven. (Park 2018).

Alternatives

  • Metoprolol (Safe substance and/or breastfeeding is the best option.)
  • Propranolol (Safe substance and/or breastfeeding is the best option.)

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

Nebivolol is also known as


Nebivolol in other languages or writings:

Tradenames

Main tradenames from several countries containing Nebivolol in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 12 / 96 %
Molecular weight 406 daltons
Protein Binding 98 %
VD 1.5 - 12 l/Kg
pKa 8.2 -
Tmax 1 - 4 hours
10 / 30 hours

References

  1. Park S, Choi NK. Breastfeeding and Maternal Hypertension. Am J Hypertens. 2018 Abstract
  2. Kearney L, Wright P, Fhadil S, Thomas M. Postpartum Cardiomyopathy and Considerations for Breastfeeding. Card Fail Rev. 2018 Abstract Full text (link to original source) Full text (in our servers)
  3. AEMPS (Pharma). Nebivolol. Ficha técnica. 2017 Full text (in our servers)
  4. Serrano Aguayo P, García de Quirós Muñoz JM, Bretón Lesmes I, Cózar León MV. Tratamiento de enfermedades endocrinológicas durante la lactancia. [Endocrinologic diseases management during breastfeeding.] Med Clin (Barc). 2015 Jan 20;144(2):73-9. Abstract
  5. Tamargo Menéndez J, Delpón Mosquera E. Farmacología de los bloqueantes de los receptores β-adrenérgicos. Curso βeta 2011 de Actualización en Betabloqueantes. 2011 Full text (in our servers)
  6. FDA - Forest Ph. Nebivolol. Drug Summary. 2010 Full text (in our servers)
  7. Riant P, Urien S, Albengres E, Duche JC, Tillement JP. High plasma protein binding as a parameter in the selection of betablockers for lactating women. Biochem Pharmacol. 1986 Abstract

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