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Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006-.
CASRN: 177834-92-3
Drug Levels and Effects
Summary of Use during Lactation
Limited information indicates that a maternal dose of eletriptan up to 80 mg daily produces low levels in milk and would not be expected to cause any adverse effects in breastfed infants.
Drug Levels
Eletriptan is metabolized to an active metabolite that has a longer half-life than eletriptan, but its serotonin agonist activity is only about 10% that of eletriptan.
Maternal Levels. Eight lactating women who were at least 1 month postpartum were given a single 80 mg oral dose of eletriptan. An average of 12.9 mcg was excreted in the 24 hours after the dose. At 24 hours, breastmilk levels averaged 1.7 mcg/L. The half-life in milk of eletriptan was 3.6 hours.[1] The active metabolite was not measured in breastmilk.
Three women who were at least 1 month postpartum used eletriptan to treat migraine provided one milk sample before the dose, then additional milk samples at 1, 2, 4, 8, 12 and 24 hours after the dose. Desmethyleletriptan was undetectable (< 1 nM) in milk. One mother took a 20 mg dose. The peak milk level of 18.2 mcg/L occurred at 2 hours after the dose. The average milk level was 5.7 mcg/L and the half-life in milk was 4 hours. Her infant’s daily dosage of eletriptan was 0.9 mcg/kg and the weight-adjusted infant dosage was 0.3% of the maternal dose. The two other women took a 40 mg dose. Peak milk levels of 78.1 and 102.4 mcg/L occurred at 2 hours after the dose and the half-lives in milk were 5.1 and 3.7 hours, respectively. The average milk levels were 24 and 23.5 mcg/L, respectively. Their infants’ daily dosages of eletriptan were 3.6 and 3.5 mcg/kg and their weight-adjusted infant dosages were 0.6% and 0.8% of the maternal dose. The overall average infant dosage was 0.6% of the maternal weight-adjusted dosage.[2]
Infant Levels. Relevant published information was not found as of the revision date.
Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
Alternate Drugs to Consider
References
- 1.
- Research FDA Center for Drug Evaluation and. NDA 21-016. Clinical pharmacology and biopharmaceutics reviews. 2002:8-9. Accessed 1/25/2020. https://www
.accessdata .fda.gov/drugsatfda_docs /nda/2002/21016_Relpax_BioPharmr .pdf. - 2.
- Amundsen S, Nordeng H, Fuskevåg OM, et al. Transfer of triptans into human breast milk and estimation of infant drug exposure through breastfeeding. Basic Clin Pharmacol Toxicol. 2021;128:795–804. [PubMed: 33730376]
Substance Identification
Substance Name
Eletriptan
CAS Registry Number
177834-92-3
Drug Class
Breast Feeding
Serotonin Receptor Agonists
Serotonin 5-HT1 Receptor Agonists
Triptans
Vasoconstrictor Agents
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- The in vivo pharmacological profile of eletriptan (UK-116,044): a potent and novel 5-HT(1B/1D) receptor agonist.[Eur J Pharmacol. 2000]The in vivo pharmacological profile of eletriptan (UK-116,044): a potent and novel 5-HT(1B/1D) receptor agonist.Gupta P, Butler P, Shepperson NB, McHarg A. Eur J Pharmacol. 2000 Jun 9; 398(1):73-81.
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