Is Labetalol Hydrochloride compatible with breastfeeding? Do we have alternatives for Labetalol Hydrochloride?

Labetalol Hydrochloride

August 29, 2018 (Very Low Risk)

Labetalol is a non-cardioselective beta blocker used in the management of hypertension, chronic stable angina pectoris, sympathetic overactivity syndrome associated with severe tetanus, control of blood pressure in patients with pheochromocytoma, in pregnant women with preeclampsia, and for producing controlled hypotension during anesthesia, in order to reduce bleeding resulting from surgical procedures.
Administration is done orally twice daily or intravenously for the emergency treatment of hypertension.

Despite not having a high protein binding (Riant 1986), other pharmacokinetic properties (moderate lipid solubility and high volume of distribution) probably explain that labetalol being excreted in breast milk in clinically insignificant amounts (Hale 2019, Anderson 2018, FDA 2010, Atkinson 1990 y 1988, Lunell 1985, Michael 1979).

Further, its low oral bioavailability would make difficult its passage to the infant’s plasma through breast milk except in premature babies and in the immediate neonatal period during which there may be greater intestinal permeability.

No problems have been observed in term infants whose mothers have received labetalol while breastfeeding (Briggs 2017, AEMPS 2001, Michael 1979). Plasma levels of breast-fed infants whose mothers received labetalol, were very low (Lunell 1985, Michael 1979).

A no well described case of asymptomatic bradycardia is reported in a 26-week-gestation preterm infant and 640 g of birth weight, whose mother took 600 mg of labetalol daily. Through milk, he received 0.1 mg / kg / day of labetalol, which is 1% of the maternal dose and 0.8% of the pediatric dose (Mirpuri 2008).

Oral labetalol does not affect the secretion of prolactin (Barbieri 1982).
Labetalol during pregnancy or delivery, but not during lactation, has been associated with neonatal hypoglycemia (Munshi 1992). The use of labetalol for treatment of hypertension during pregnancy has been associated with Raynaud's phenomenon of the nipples and nipple pain while breastfeeding. Discontinuation of labetalol eliminated the nipple pain (McGuinness 2013).

Some authors do not consider beta-blockers to be drugs of choice for the treatment of hypertension, unless another indication exists simultaneously, such as migraine or angina prophylaxis (Anderson 2018).

Several medical societies, experts and expert consensus, consider the use of this medication safe or probably safe during breastfeeding (Hale 2019 p 418, Briggs 2017, Serrano 2014, Davanzo 2014, Rowe 2013, Podymow 2011, Ghanem 2008).
The American Academy of Pediatrics considers that labetalol is a medication usually compatible with breastfeeding (AAP 2001).

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

Alternatives

Very Low Risk

Compatible. Not risky for breastfeeding or infant.

Low Risk

Moderately safe. Mild risk possible. Follow up recommended. Read the Comment.

High Risk

Poorly safe. Evaluate carefully. Use a safer alternative. Read the Comment.

Very High Risk

Not recommended. Cessation of breastfeeding or alternative.

Synonyms

  • Labetalol

Writings

  • Λαβεταλόλη Υδροχλωρική (Greek)
  • Лабеталола Гидрохлорид (Cyrillic)
  • ラベタロール塩酸塩 (Japanese)
  • C19 H24 N2 O3, HCl (Molecular formula)
  • 5-[1-Hydroxy-2-(1-methyl-3-phenylpropylamino)ethyl]salicylamide hydrochloride (Chemical name)
  • C07AG01 (ATC Code/s)

References

  1. Hale TW. Hale's Medications & Mothers' Milk. Springer Publishing Company. 2019
  2. Park S, Choi NK. Breastfeeding and Maternal Hypertension. Am J Hypertens. 2018Abstract
  3. Anderson PO. Treating Hypertension During Breastfeeding. Breastfeed Med. 2018Abstract
  4. Briggs GG, Freeman RK, Towers CV, Forinash AB. Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk. Wolters Kluwer Health. 11th edition (acces on line) 2017
  5. 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). 2015Abstract
  6. McGuinness N, Cording V. Raynaud's phenomenon of the nipple associated with labetalol use. J Hum Lact. 2013Abstract Full text (link to original source) Full text (in our servers)
  7. Rowe H, Baker T, Hale TW. Maternal medication, drug use, and breastfeeding. Pediatr Clin North Am. 2013 Feb;60(1):275-94. 2013Abstract
  8. 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)
  9. Podymow T, August P. Antihypertensive drugs in pregnancy. Semin Nephrol. 2011Abstract
  10. FDA-Prometheus. Labetalol. Drug Summary. 2010 Full text (in our servers)
  11. Ghanem FA, Movahed A. Use of antihypertensive drugs during pregnancy and lactation. Cardiovasc Ther. 2008Abstract Full text (link to original source) Full text (in our servers)
  12. Mirpuri J, Patel H, Rhee D, Crowley K. What's mom on? A case of bradycardia in a premature infant on breast milk. J Invest Med. 2008;56:409. Poster 203. 2008
  13. AAP - American Academy of Pediatrics Committee on Drugs. Transfer of drugs and other chemicals into human milk. Pediatrics. 2001Abstract Full text (link to original source) Full text (in our servers)
  14. AEMPS-Kern. Labetalol. Ficha técnica. 2001 Full text (in our servers)
  15. Kirsten R, Nelson K, Kirsten D, Heintz B. Clinical pharmacokinetics of vasodilators. Part II. Clin Pharmacokinet. 1998Abstract
  16. Munshi UK, Deorari AK, Paul VK, Singh M. Effects of maternal labetalol on the newborn infant. Indian Pediatr. 1992Abstract
  17. Atkinson H, Begg EJ. Concentrations of beta-blocking drugs in human milk. J Pediatr. 1990Abstract
  18. Atkinson HC, Begg EJ, Darlow BA. Drugs in human milk. Clinical pharmacokinetic considerations. Clin Pharmacokinet. 1988Abstract
  19. 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. 1986Abstract
  20. Lunell NO, Kulas J, Rane A. Transfer of labetalol into amniotic fluid and breast milk in lactating women. Eur J Clin Pharmacol. 1985Abstract
  21. Barbieri C, Larovere MT, Mariotti G, Ferrari C, Caldara R. Prolactin stimulation by intravenous labetalol is mediated inside the central nervous system. Clin Endocrinol (Oxf). 1982Abstract