Last update: Nov. 3, 2018

ラベタロール塩酸塩

Very Low Risk for breastfeeding


Safe. Compatible.
Not risky for breastfeeding or infant.

Labetalol is a non-cardioselective beta-blocker used in the treatment of hypertension, stable chronic angina pectoris, sympathetic overactivity syndrome associated with severe tetanus, the control of blood pressure in patients with pheochromocytoma, in pregnant women with preeclampsia and to produce controlled hypotension during anesthesia in order to reduce bleeding resulting from surgical procedures.
Administration is carried out orally in 2 daily doses or intravenously for the emergency treatment of hypertension.

Despite not having high protein binding (Riant 1986), other pharmacokinetic properties (moderate liposolubility and high volume of distribution) probably explain why labetalol is excreted in breastmilk in clinically insignificant amounts (Hale 2019, Anderson 2018, FDA 2010, Atkinson 1990 and 1988, Lunell 1985, Michael 1979).

In addition, its low oral bioavailability hinders its transfer to infant plasma from breastmilk, except in premature babies and the immediate neonatal period when there may be increased intestinal permeability.

No problems have been observed in term infants whose mothers were prescribed labetalol during breastfeeding (Briggs 2017, AEMPS 2001, Michael 1979). Plasma levels of breastfed babies whose mothers took labetalol were very low (Lunell 1985, Michael 1979).

A poorly documented case of asymptomatic bradycardia has been recorded (poster) in an extremely premature baby of 26 weeks of gestation with 640g birth weight, whose mother took 600 mg of labetalol per day. Through breastmilk, the baby 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 has been associated with neonatal hypoglycemia during pregnancy or delivery, but not during breastfeeding. (Munshi 1992).
The use of labetalol for the treatment of hypertension during pregnancy has been associated with Raynaud's phenomenon and nipple pain during breastfeeding. Discontinuing labetalol eliminated the pain (McGuinness 2013).

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

Several medical associations, experts and expert consensus believe its use to be 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 labetalol to be generally compatible with breastfeeding (AAP 2001).

Alternatives

Suggestions made at e-lactancia are done by APILAM´s pediatricians and pharmacists, and are based on updated scientific publications.
It is not intended to replace the relationship you have with your doctor but to compound it.

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

ラベタロール塩酸塩 is Labetalol Hydrochloride in Japanese.

Is written in other languages:

ラベタロール塩酸塩 is also known as

Group

ラベタロール塩酸塩 belongs to this group or family:

Tradenames

Main tradenames from several countries containing ラベタロール塩酸塩 in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 25 - 40 %
Molecular weight 365 daltons
Protein Binding 50 %
VD 5,1 - 9,4 l/Kg
pKa 8,05 -
Tmax 1 - 2 hours
T1/2 6 - 8 hours
M/P ratio 1 - 2,6 -
Theoretical Dose 0,006 - 0,09 mg/Kg/d
Relative Dose 0,05 - 0,45 %
Relat.Ped.Dose 0,05 - 0,75 %

References

  1. Hale TW. Hale's Medications & Mothers' Milk. Springer Publishing Company. 2019
  2. Anderson PO. Treating Hypertension During Breastfeeding. Breastfeed Med. 2018 Abstract
  3. Park S, Choi NK. Breastfeeding and Maternal Hypertension. Am J Hypertens. 2018 Abstract
  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). 2015 Abstract
  6. Rowe H, Baker T, Hale TW. Maternal medication, drug use, and breastfeeding. Pediatr Clin North Am. 2013 Feb;60(1):275-94. Abstract
  7. McGuinness N, Cording V. Raynaud's phenomenon of the nipple associated with labetalol use. J Hum Lact. 2013 Abstract Full text (link to original source) Full text (in our servers)
  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. 2011 Abstract
  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. 2008 Abstract 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. AEMPS-Kern. Labetalol. Ficha técnica. 2001 Full text (in our servers)
  14. AAP - American Academy of Pediatrics Committee on Drugs. Transfer of drugs and other chemicals into human milk. Pediatrics. 2001 Sep;108(3):776-89. Abstract Full text (link to original source) Full text (in our servers)
  15. Kirsten R, Nelson K, Kirsten D, Heintz B. Clinical pharmacokinetics of vasodilators. Part II. Clin Pharmacokinet. 1998 Abstract
  16. Munshi UK, Deorari AK, Paul VK, Singh M. Effects of maternal labetalol on the newborn infant. Indian Pediatr. 1992 Abstract
  17. Atkinson H, Begg EJ. Concentrations of beta-blocking drugs in human milk. J Pediatr. 1990 Abstract
  18. Atkinson HC, Begg EJ, Darlow BA. Drugs in human milk. Clinical pharmacokinetic considerations. Clin Pharmacokinet. 1988 Abstract
  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. 1986 Abstract
  20. Lunell NO, Kulas J, Rane A. Transfer of labetalol into amniotic fluid and breast milk in lactating women. Eur J Clin Pharmacol. 1985 Abstract
  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). 1982 Abstract

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