Last update July 30, 2022

Betaxolol Hydrochloride

Likely Compatibility

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

It is a long-acting cardioselective beta-blocker that is used orally (once a day) in the treatment of hypertension and angina pectoris and, as eye drops (twice a day), to treat glaucoma.

Betaxolol was excreted in the colostrum in an amount that could represent a relative dose of 5 to 10%. (Morselli 1990)

Its low percentage of plasma protein binding and long half-life make it likely that it would pass into breast milk in amounts which could be significant (Riant 1986), although its very wide volume of distribution would make it difficult.

Until more published data is known about this drug in relation to breastfeeding, known safer alternatives are preferable, especially during the neonatal period and in the event of prematurity.

OPHTHALMIC USE:

Following ophthalmic administration of betaxolol 0.5% for 1 week, peak betaxolol plasma concentrations were ≤ 1 ng/mL (nanograms/milliliter). (AEMPS 2019)

Systemic absorption should be minimized by pressing the tear duct (inner corner of the eye) with the finger for 1 to 2 minutes and administering the dose immediately after breastfeeding. (Belkin 2020, Blumen 2020, Méndez 2012)

The small dose and poor plasma absorption of most topical ophthalmological preparations make it unlikely that significant amounts will transfer into breastmilk. Topical use of Betaxolol in the form of eye drops is compatible with breastfeeding.

Alternatives

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

Betaxolol Hydrochloride in other languages or writings:

Tradenames

Main tradenames from several countries containing Betaxolol Hydrochloride in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 89 ± 5 %
Molecular weight 344 daltons
Protein Binding 50 %
VD 4.9 - 8.8 l/Kg
pKa 14.09 -
Tmax 3 (2 - 4) hours
18 (14 - 22) hours
M/P ratio 3 -
Theoretical Dose ≈ 0.001 - 0.007 mg/Kg/d
Relative Dose ≈ 0.7 - 4.3 %

References

  1. Novartis. Betaxolol. Drug Summary. 2020 Full text (in our servers)
  2. Belkin A, Chen T, DeOliveria AR, Johnson SM, Ramulu PY, Buys YM; American Glaucoma Society and the Canadian Glaucoma Society.. A Practical Guide to the Pregnant and Breastfeeding Patient with Glaucoma. Ophthalmol Glaucoma. 2020 Mar - Apr;3(2):79-89. Abstract
  3. Blumen-Ohana E, Sellem E. [Pregnancy & glaucoma: SFO-SFG recommendations]. J Fr Ophtalmol. 2020 Jan;43(1):63-66. Abstract
  4. AEMPS. Betaxolol. Ficha técnica. 2019 Full text (in our servers)
  5. Méndez-Hernández C. Uso de fármacos antiglaucomatosos durante el embarazo y lactancia. [Use of glaucoma medications during pregnancy and breastfeeding]. Arch Soc Esp Oftalmol. 2012 Dec;87(12):389-91. Abstract
  6. 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)
  7. Morselli PL, Boutroy MJ, Bianchetti G, Zipfel A, Boutroy JL, Vert P. Placental transfer and perinatal pharmacokinetics of betaxolol. Eur J Clin Pharmacol. 1990;38(5):477-83. Abstract
  8. 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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