Last update July 30, 2022

Carteolol 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, some arrhythmias and angina pectoris, and, as eye drops (twice a day), to treat glaucoma.

At date of last update were not found published data on its excretion into breast milk.

Its low percentage of plasma protein binding 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 Carteolol 2% for 2 months, peak carteolol plasma concentrations were ≤ 4 ng/mL (nanograms/milliliter). (Bausch 2022, Renard 2005)

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 Carteolol 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

Carteolol Hydrochloride in other languages or writings:

Tradenames

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

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 85 %
Molecular weight 329 daltons
Protein Binding 23 - 30 %
VD 4 (2.5 - 7) l/Kg
pKa 13.4 -
Tmax 2 (1 - 3) hours
3 - 8 hours

References

  1. Bausch. Carteolol. Ficha técnica. 2022 Consulted on July 29, 2022 Full text (in our servers)
  2. 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)
  3. Renard P, Kovalski JL, Cochereau I, Jaulerry S, Williamson W, Elena PP, Lablache Combier M, Allaire C, Siou-Mermet R. Comparison of carteolol plasmatic levels after repeated instillations of long-acting and regular formulations of carteolol 2% in glaucoma patients. Graefes Arch Clin Exp Ophthalmol. 2005 Abstract
  4. 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
  5. Ishizaki T, Ohnishi A, Sasaki T, Kushida K, Horai Y, Chiba K, Suganuma T. Pharmacokinetics and absolute bioavailability of carteolol, a new beta-adrenergic receptor blocking agent. Eur J Clin Pharmacol. 1983 Abstract

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