Metoprolol use while Breastfeeding

Drugs containing Metoprolol: Lopressor, Toprol-XL, Metoprolol Tartrate, Metoprolol Succinate ER, Dutoprol, Lopressor HCT

Metoprolol Levels and Effects while Breastfeeding

Summary of Use during Lactation

Because of the low levels of metoprolol in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. Studies on the use of metoprolol during breastfeeding have found no adverse reactions in breastfed infants.

Drug Levels

The excretion of beta-adrenergic blocking drugs into breastmilk is largely determined by their protein binding. Those with low binding are more extensively excreted into breastmilk.[1] Accumulation of the drugs in the infant is related to the fraction excreted in urine. With 10% protein binding, 40% renal excretion and a moderate half-life, metoprolol presents moderately low risk for accumulation in infants.

Maternal Levels. With metoprolol doses of 50 mg orally twice daily, milk levels are usually less than 420 mcg/L.[2][3][4] Five women taking oral metoprolol 100 to 200 mg daily had average milk metoprolol levels of 316 mcg/L.[5] It is estimated that a breastfed infant would receive a dose of about 0.07 mg/kg daily in breastmilk with a maternal dose of 200 mg daily.[4]

Peak milk levels of 106 to 689 mcg/L have been reported following doses of 100 mg orally twice daily.[4][6] Peak milk levels occurred about 30 minutes after peak serum levels, at 1.5 hours after the dose in two patients, and 6 hours after the dose in a third.[6]

Two women who were taking metoprolol (dosage not specified). Milk samples were obtained over one dosage interval. The dosage of metoprolol and alpha-hydroxymetoprolol in breastmilk was less than 2% of the mother's weight-adjusted dose.[7]

Infant Levels. Metoprolol was undetectable (<2.7 mcg/L) in the plasma of 3 infants aged 4, 10 and 60 days after maternal oral doses of 100 mg daily.[2]

Metoprolol serum levels in 3- to 5-day-old breastfed infants ranged from 0.5 to 2.9 mcg/L after maternal doses of 50 or 100 mg twice daily.[3][8]

A woman was taking metoprolol 100 mg daily for hypertension during pregnancy and postpartum. Her breastfed infant's serum concentrations of metoprolol and its active metabolite, alpha-hydroxymetoprolol, were undetectable on days 4 and 182 postpartum.[9]

Effects in Breastfed Infants

A study of mothers taking beta-blockers during nursing found a numerically, but not statistically significant increased number of adverse reactions in those taking any beta-blocker. Although the ages of infants were matched to control infants, the ages of the affected infants were not stated. Of 6 mothers taking metoprolol, none reported adverse effects in her breastfed infant.[10][11]

Possible Effects on Lactation

Relevant published information on the effects of beta-blockade or metoprolol during normal lactation was not found as of the revision date. A study in 6 patients with hyperprolactinemia and galactorrhea found no changes in serum prolactin levels following beta-adrenergic blockade with propranolol.[12]

Alternate Drugs to Consider

Propranolol, Labetalol

References

1. Riant P, Urien S, Albengres E et al. High plasma protein binding as a parameter in the selection of betablockers for lactating women. Biochem Pharmacol. 1986;35:4579-81. PMID: 2878668

2. Kulas J, Lunell NO, Rosing U et al. Atenolol and metoprolol. A comparison of their excretion into human breast milk. Acta Obstet Gynecol Scand Suppl. 1984;suppl 118: 65-9. PMID: 4043203

3. Lindeberg S, Sandstrom B, Lundborg P et al. 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;suppl 118:61-4. PMID: 6587729

4. Sandstrom B, Regardh CG. Metoprolol excretion into breast milk. Br J Clin Pharmacol. 1980;9:518-9. PMID: 7397065

5. Sandstrom B. Antihypertensive treatment with the adrenergic beta-receptor blocker metoprolol during pregnancy. Gynecol Invest. 1978;9:195-204. PMID: 750326

6. Liedholm H, Melander A, Bitzen PO et al. Accumulation of atenolol and metoprolol in human breast milk. Eur J Clin Pharmacol. 1981;20:229-31. PMID: 7286041

7. Yep T, Eyal S, Easterling TR et al. The pharmacokinetics of metoprolol during pregnancy. Pharmacotherapy. 2011;31: 439e. DOI: doi:10.1592/phco.31.10.311e

8. Sandstrom B, Lindeberg S, Lundborg P et al. Disposition of the adrenergic blocker metoprolol in the late pregnant woman, the amniotic fluid, the cord blood and the neonate. Clin Exp Hypertens B. 1983;2:75-82. PMID: 6135523

9. Grundmann M, Kacirova I, Duricova J, Perinova I. Metoprolol and alfa-hydroxymetoprolol concentrations during lactation - a case report. Ther Drug Monit. 2011;33:504. Abstract. DOI: doi:10.1097/01.ftd.0000400651.94145.ba

10. Ho TK, Moretti ME, Schaeffer JK et al. Maternal beta-blocker usage and breast feeding in the neonate. Pediatr Res. 1999;45:67A. Abstract 385.

11. Schimmel MS, Eidelman AI, Wilschanski MA et al. Toxic effects of atenolol consumed during breast feeding. J Pediatr. 1989;114:476-8. PMID: 2921694

12. Board JA, Fierro RJ, Wasserman AJ et al. Effects of alpha- and beta-adrenergic blocking agents on serum prolactin levels in women with hyperprolactinemia and galactorrhea. Am J Obstet Gynecol. 1977;127:285-7. PMID: 556882

Metoprolol Identification

Substance Name

Metoprolol

CAS Registry Number

37350-58-6

Drug Class

  • Antihypertensive Agents
  • Adrenergic Beta-Antagonists
  • Antiarrhythmics

Administrative Information

LactMed Record Number

296

Information from the National Library of Medicine's LactMed Database.

Last Revision Date

2013-09-07

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

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