Last update: Nov. 3, 2018

Metoprolol

Very Low Risk for breastfeeding


Safe. Compatible.
Minimal risk for breastfeeding and infant.

Metoprolol is a cardioselective beta-blocker used in the treatment of hypertension, angina pectoris, cardiac arrhythmias, myocardial infarction, heart failure, hyperthyroidism and in the prophylaxis of migraine. Administered orally or intravenously, in 1 to 4 daily doses.

Although metoprolol is a weak base (pKa 9.7) with low plasma protein binding and moderate liposolubility and therefore the milk/plasma index is generally high (Ryu 2016, Kulas 1984, Lindeberg 1984, Liedholm 1981, Sandstorm 1983 and 1980), maternal plasma levels are very low so it is excreted in breastmilk in clinically insignificant amounts (Hale 2019, p 505, Ryu 2016, AEMPS 2016, Astra 2014, Yep 2011, Kulas 1984, Lindeberg 1984, Sandstorm 1983, 1980 and 1978).

The concentration of metoprolol in infant plasma is undetectable or very low and unlikely to be clinically significant for babies (Grundmann 2011, Kulas 1984, Lindeberg 1984, Sandstrom 1983).

No side effects have been observed in infants whose mothers were taking metoprolol (Briggs 2017).

Some authors do not consider beta-blockers to be drugs of choice for the treatment of hypertension, unless there is another simultaneous indication, such as migraine or prophylaxis of angina. Caution is needed if metoprolol is used in mothers of premature babies (Anderson 2018).

Several medical associations, experts and expert consensus believe its use to be safe or probably safe during breastfeeding (Alexander 2017, Malachias 2016, Serrano 2014, Davanzo 2014, Rowe 2013, Pringsheim 2012, Ghanem 2008, Tan 2001, Shannon 2000). The American Academy of Pediatrics considers it to be generally compatible with breastfeeding (AAP 2001).

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

Alternatives

Suggestions made at e-lactancia are done by APILAM´s pediatricians and pharmacists, and are based on updated scientific publications.
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Other names

Metoprolol is also known as


Metoprolol in other languages or writings:

Group

Metoprolol belongs to this group or family:

Tradenames

Main tradenames from several countries containing Metoprolol in its composition:

List of 7 tradenames

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 40 - 50 %
Molecular weight 267 daltons
Protein Binding 10 - 12 %
VD 3,2 - 5,6 l/Kg
pKa 9,67 -
Tmax 1,5 - 2 hours
T1/2 3 - 7 hours
M/P ratio 2.4 ± 0.3 -
Theoretical Dose 0,067 mg/Kg/d
Relative Dose 0,5 - 3,8 %
Relat.Ped.Dose 1,1 - 3,3 %

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. 2018 Abstract
  3. Anderson PO. Treating Hypertension During Breastfeeding. Breastfeed Med. 2018 Abstract
  4. 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)
  5. 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
  6. Alexander EK, Pearce EN, Brent GA, Brown RS, Chen H, Dosiou C, Grobman WA, Laurberg P, Lazarus JH, Mandel SJ, Peeters RP, Sullivan S. 2017 Guidelines of the American Thyroid Association for the Diagnosis and Management of Thyroid Disease During Pregnancy and the Postpartum. Thyroid. 2017 Abstract Full text (link to original source) Full text (in our servers)
  7. AEMPS-Recordati. Metoprolol. Ficha técnica. 2016 Full text (in our servers)
  8. Malachias MV, Figueiredo CE, Sass N, Antonello IC, Torloni MR, Bortolotto MRF L. 7th Brazilian Guideline of Arterial Hypertension: Chapter 9 - Arterial Hypertension in pregnancy Arq Bras Cardiol. 2016 Abstract Full text (link to original source) Full text (in our servers)
  9. Ryu RJ, Eyal S, Easterling TR, Caritis SN, Venkataraman R, Hankins G, Rytting E, Thummel K, Kelly EJ, Risler L, Phillips B, Honaker MT, Shen DD, Hebert MF. Pharmacokinetics of metoprolol during pregnancy and lactation. J Clin Pharmacol. 2016 Abstract Full text (link to original source) Full text (in our servers)
  10. 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
  11. Davanzo R, Bua J, Paloni G, Facchina G. Breastfeeding and migraine drugs. Eur J Clin Pharmacol. 2014 Abstract
  12. Astra-Zeneca. Metoprolol (Toprol-XL). Drug Summary. 2014 Full text (in our servers)
  13. Rowe H, Baker T, Hale TW. Maternal medication, drug use, and breastfeeding. Pediatr Clin North Am. 2013 Feb;60(1):275-94. Abstract
  14. Pringsheim T, Davenport W, Mackie G, Worthington I, Aubé M, Christie SN, Gladstone J, Becker WJ; Canadian Headache Society Prophylactic Guidelines Development Group. Canadian Headache Society guideline for migraine prophylaxis. Can J Neurol Sci. 2012 Abstract Full text (in our servers)
  15. 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)
  16. Grundmann M, Kacirova I, Duricova J, Perinova I. Metoprolol and alfa-hydroxymetoprolol concentrations during lactation - a case report. 12th International Congress of Therapeutic Drug Monitoring and Clinical Toxicology Stuttgart, Germany · October 2-6, 2011. Poster 088. Ther Drug Monit. 2011;33:504. P088. 2011
  17. Yep T, Eyal S, Easterling TR, Shen DD, Kelly EJ, Hankins GDV, Caritis S, Risler L, Hebert MF. The pharmacokinetics of metoprolol during pregnancy. American College of Clinical Pharmacy 2011 Annual Meeting. Abstract 471. Pharmacotherapy. 2011;31:439e. 2011 Full text (link to original source) Full text (in our servers)
  18. 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)
  19. Metoprolol. Drugs and Lactation Database (LactMed). 2006 Abstract
  20. 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)
  21. Tan HL, Lie KI. Treatment of tachyarrhythmias during pregnancy and lactation. Eur Heart J. 2001 Abstract Full text (link to original source) Full text (in our servers)
  22. 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
  23. Kulas J, Lunell NO, Rosing U, Stéen B, Rane A. Atenolol and metoprolol. A comparison of their excretion into human breast milk. Acta Obstet Gynecol Scand Suppl. 1984 Abstract
  24. Lindeberg S, Sandström B, Lundborg P, Regårdh CG. Disposition of the adrenergic blocker metoprolol in the late-pregnant woman, the amniotic fluid, the cord blood and the neonate. Acta Obstet Gynecol Scand Suppl. 1984 Abstract
  25. Sandström B, Lindeberg S, Lundborg P, Regårdh CG. Disposition of the adrenergic blocker metoprolol in the late pregnant women, the amniotic fluid, the cord blood and the neonate. Clin Exp Hypertens B. 1983 Abstract
  26. Sandström B. Adrenergic beta-receptor blockers in hypertension of pregnancy. Clin Exp Hypertens B. 1982 Abstract
  27. Liedholm H, Melander A, Bitzén PO, Helm G, Lönnerholm G, Mattiasson I, Nilsson B, Wåhlin-Boll E. Accumulation of atenolol and metoprolol in human breast milk. Eur J Clin Pharmacol. 1981 Abstract
  28. Sandström B, Regårdh CG. Metoprolol excretion into breast milk. Br J Clin Pharmacol. 1980 Abstract Full text (link to original source) Full text (in our servers)
  29. Sandström B. Antihypertensive treatment with the adrenergic beta-receptor blocker metoprolol during pregnancy. Gynecol Invest. 1978 Abstract

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