Is Metoprolol compatible with breastfeeding? Do we have alternatives for Metoprolol?

Metoprolol

August 29, 2018 (Very Low Risk)

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

Although Metoprolol is a weak base (pKa 9.7) with low plasma protein binding and moderate lipid solubility and for this the milk/plasma ratios for metoprolol are in general high (Ryu 2016, Kulas 1984, Lindeberg 1984, Liedholm 1981, Sandstorm 1983 & 1980), the maternal plasma levels are very low, so it is excreted in breast milk in clinically insignificant amounts (Hale 2019, p 505, Ryu 2016, AEMPS 2016, Astra 2014, Yep 2011, Kulas 1984, Lindeberg 1984, Sandstorm 1983, 1980 & 1978).

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

No adverse effects have been seen in breast-fed infants whose mothers were given metoprolol (Briggs 2017)

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. Caution is needed if metoprolol is used in mothers or preterm infants (Anderson 2018).

Several medical societies, experts and expert consensus, consider the use of this medication 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 that it is a medication usually compatible with breast feeding (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

  • Metoprolol fumarate
  • Metoprolol succinate
  • Metoprolol tartrate

Writings

  • Μετοπρολόλη (Greek)
  • ميتوبرولول (Arabic)
  • Метопролол (Cyrillic)
  • 美托洛尔 (Chinese)
  • C15 H25 NO3 (Molecular formula)
  • (±)-1-Isopropylamino-3-[4-(2-methoxyethyl)phenoxy]propan-2-ol IUPAC 1-[4-(2-methoxyethyl)phenoxy]-3-[(propan-2-yl)amino]propan-2-ol (Chemical name)
  • C07AB02 (ATC Code/s)

References

  1. Hale TW. Hale's Medications & Mothers' Milk. Springer Publishing Company. 2019
  2. Anderson PO. Treating Hypertension During Breastfeeding. Breastfeed Med. 2018Abstract
  3. Park S, Choi NK. Breastfeeding and Maternal Hypertension. Am J Hypertens. 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. 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. 2017Abstract Full text (link to original source) Full text (in our servers)
  6. 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. 2016Abstract Full text (link to original source) Full text (in our servers)
  7. AEMPS-Recordati. Metoprolol. Ficha técnica. 2016 Full text (in our servers)
  8. 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. 2016Abstract Full text (link to original source) Full text (in our servers)
  9. 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
  10. Davanzo R, Bua J, Paloni G, Facchina G. Breastfeeding and migraine drugs. Eur J Clin Pharmacol. 2014Abstract
  11. Astra-Zeneca. Metoprolol (Toprol-XL). Drug Summary. 2014 Full text (in our servers)
  12. Rowe H, Baker T, Hale TW. Maternal medication, drug use, and breastfeeding. Pediatr Clin North Am. 2013 Feb;60(1):275-94. 2013Abstract
  13. 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. 2012Abstract Full text (in our servers)
  14. 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
  15. 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)
  16. 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)
  17. 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)
  18. Metoprolol. Drugs and Lactation Database (LactMed). 2006Abstract
  19. 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)
  20. Tan HL, Lie KI. Treatment of tachyarrhythmias during pregnancy and lactation. Eur Heart J. 2001Abstract Full text (link to original source) Full text (in our servers)
  21. Shannon ME, Malecha SE, Cha AJ. Beta blockers and lactation: an update. J Hum Lact. 2000Abstract
  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. 1986Abstract
  23. 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. 1984Abstract
  24. 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. 1984Abstract
  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. 1983Abstract
  26. Sandström B. Adrenergic beta-receptor blockers in hypertension of pregnancy. Clin Exp Hypertens B. 1982Abstract
  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. 1981Abstract
  28. Sandström B, Regårdh CG. Metoprolol excretion into breast milk. Br J Clin Pharmacol. 1980Abstract 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. 1978Abstract