Also known as (+)-Citalopram, (S)-Citalopram, Escitalopram Oxalate, Escitalopramum, Esertia, S(+)-Citalopram, Seroplex
The active S-stereoisomer of the selective serotonin reuptake inhibitor (SSRI) citalopram with antidepressant, anti-obsessive-compulsive and antibulimic properties. Escitalopram inhibits the reuptake of the neurotransmitter serotonin (5-HT) at the serotonin reuptake pump of the neuronal membrane of the presynaptic cell, thereby increasing levels of 5-HT within the synaptic cleft and enhancing the actions of serotonin on 5HT1A autoreceptors. Unlike other SSRIs, escitalopram appears to not only bind to a primary high-affinity site on the serotonin transporter protein but also to a secondary lower-affinity allosteric site that is considered to stabilize and prolong drug binding.
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Can I take Escitalopram while breastfeeding?
Escitalopram is the S-isomer of the antidepressant, citalopram. Limited information indicates that maternal doses of escitalopram up to 20 mg daily produce low levels in milk and would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months. Based on limited data, escitalopram appears to be preferable to racemic citalopram during breastfeeding because of the lower dosage and milk levels and general lack of adverse reactions in breastfed infants. One case of necrotizing enterocolitis was reported in an breastfed newborn whose mother was taking escitalopram during pregnancy and lactation, but causality was not established. Monitor the infant for drowsiness, especially in younger, exclusively breastfed infants and when using combinations of psychotropic drugs. Mothers taking an SSRI during pregnancy and postpartum may have more difficulty breastfeeding and may need additional breastfeeding support. Breastfed infants exposed to an SSRI during the third trimester of pregnancy have a lower risk of poor neonatal adaptation than formula-fed infants.
Drug levels
Escitalopram is the S -isomer of racemic citalopram which is metabolized to 2 metabolites, each having antidepressant activity considered to be about 13% that of citalopram.[1]
Maternal Levels. Eight women taking escitalopram in an average dosage of 199 mcg/kg daily (10 to 20 mg daily) had 6 to 8 milk steady-state milk samples analyzed over the 24-hour interval after their single daily dose. The average dosage that an exclusively breastfed infant would receive was calculated to be 7.6 mcg/kg of escitalopram and 3 mcg/kg of desmethylcitalopram daily which were 3.9% and 1.7% of the maternal weight-adjusted dosages, respectively. The absolute dosage was about 40% less than a previous study by the same authors with racemic citalopram.[2]
A woman taking escitalopram had milk escitalopram concentrations measured twice. While taking a dosage of 5 mg daily, milk escitalopram was 24.9 mcg/L at 20 hours after the dose. While taking 10 mg escitalopram daily and valproic acid 1200 mg daily, milk escitalopram was 76.1 mcg/L at 15 hours after the dose. Using these two data points, the authors estimated that the infant received 5.1 and 7.7% of the maternal weight-adjusted dosage of escitalopram on these days, respectively.[3]
One woman was taking escitalopram 20 mg daily and reboxetine 4 mg daily orally while nursing her 9.5-month-old infant. She collected milk samples before each breastfeeding session over a 1-day period. The authors estimated that the infant would receive 4.6% of the maternal-weight-adjusted dosage of escitalopram plus desmethylescitalopram.[4]
Infant Levels. One study found that racemic citalopram serum levels in infants were determined by their CYP2C19 genotype, with slow metabolizers more likely to have detectable serum levels.[5] Pharmacogenetics likely plays a part in determining the exposure of breastfed infants to escitalopram also.
In 8 breastfed infants whose mothers were taking an average of 199 mcg/kg daily of escitalopram (10 or 20 mg daily), escitalopram and desmethylescitalopram were undetectable in the serum of 3 infants (<1 mcg/L). The drug and metabolite serum levels were less than 5 mcg/L in all the other infants. Their mothers' serum levels of the drug and metabolite averaged 24 and 20 mcg/L, respectively.[2]
Effects in breastfed infants
Escitalopram is the S -isomer of racemic citalopram which is metabolized to 2 metabolites, each having antidepressant activity considered to be about 13% that of citalopram.[1]
Maternal Levels. Eight women taking escitalopram in an average dosage of 199 mcg/kg daily (10 to 20 mg daily) had 6 to 8 milk steady-state milk samples analyzed over the 24-hour interval after their single daily dose. The average dosage that an exclusively breastfed infant would receive was calculated to be 7.6 mcg/kg of escitalopram and 3 mcg/kg of desmethylcitalopram daily which were 3.9% and 1.7% of the maternal weight-adjusted dosages, respectively. The absolute dosage was about 40% less than a previous study by the same authors with racemic citalopram.[2]
A woman taking escitalopram had milk escitalopram concentrations measured twice. While taking a dosage of 5 mg daily, milk escitalopram was 24.9 mcg/L at 20 hours after the dose. While taking 10 mg escitalopram daily and valproic acid 1200 mg daily, milk escitalopram was 76.1 mcg/L at 15 hours after the dose. Using these two data points, the authors estimated that the infant received 5.1 and 7.7% of the maternal weight-adjusted dosage of escitalopram on these days, respectively.[3]
One woman was taking escitalopram 20 mg daily and reboxetine 4 mg daily orally while nursing her 9.5-month-old infant. She collected milk samples before each breastfeeding session over a 1-day period. The authors estimated that the infant would receive 4.6% of the maternal-weight-adjusted dosage of escitalopram plus desmethylescitalopram.[4]
Infant Levels. One study found that racemic citalopram serum levels in infants were determined by their CYP2C19 genotype, with slow metabolizers more likely to have detectable serum levels.[5] Pharmacogenetics likely plays a part in determining the exposure of breastfed infants to escitalopram also.
In 8 breastfed infants whose mothers were taking an average of 199 mcg/kg daily of escitalopram (10 or 20 mg daily), escitalopram and desmethylescitalopram were undetectable in the serum of 3 infants (<1 mcg/L). The drug and metabolite serum levels were less than 5 mcg/L in all the other infants. Their mothers' serum levels of the drug and metabolite averaged 24 and 20 mcg/L, respectively.[2]
Possible effects on lactation
The SSRI class of drugs, including escitalopram, can cause increased prolactin levels and galactorrhea in nonpregnant, nonnursing patients.[13][14][15][16][17][18][19] Euprolactinemic galactorrhea has also been reported.[20][21] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
In a small prospective study, 8 primiparous women who were taking a serotonin reuptake inhibitor (SRI; 3 taking fluoxetine and 1 each taking citalopram, duloxetine, escitalopram, paroxetine or sertraline) were compared to 423 mothers who were not taking an SRI. Mothers taking an SRI had an onset of milk secretory activation (lactogenesis II) that was delayed by an average of 16.7 hours compared to controls (85.8 hours postpartum in the SRI-treated mothers and 69.1 h in the untreated mothers), which doubled the risk of delayed feeding behavior in the untreated group. However, the delay in lactogenesis II may not be clinically important, since there was no statistically significant difference between the groups in the percentage of mothers experiencing feeding difficulties after day 4 postpartum.[22]
A case control study compared the rate of predominant breastfeeding at 2 weeks postpartum in mothers who took an SSRI antidepressant throughout pregnancy and at delivery (n = 167) or an SSRI during pregnancy only (n = 117) to a control group of mothers who took no antidepressants (n = 182). Among the two groups who had taken an SSRI, 33 took citalopram, 18 took escitalopram, 63 took fluoxetine, 2 took fluvoxamine, 78 took paroxetine, and 87 took sertraline. Among the women who took an SSRI, the breastfeeding rate at 2 weeks postpartum was 27% to 33% lower than mother who did not take antidepressants, with no statistical difference in breastfeeding rates between the SSRI-exposed groups.[23]
Alternate drugs to consider
Nortriptyline, Paroxetine, Sertraline
References
1. Weissman AM, Levy BT, Hartz AJ et al. Pooled analysis of antidepressant levels in lactating mothers, breast milk, and nursing infants. Am J Psychiatry. 2004;161:1066-78. PMID: 15169695
2. Rampono J, Hackett LP, Kristensen JH et al. Transfer of escitalopram and its metabolite demethylescitalopram into breastmilk. Br J Clin Pharmacol. 2006;3:316-22. PMID: 16934048
3. Castberg I, Spigset O. Excretion of escitalopram in breast milk. J Clin Psychopharmacol. 2006;26:536-8. PMID: 16974204
4. Hackett LP, Ilett KF, Rampono J et al. Transfer of reboxetine into breastmilk, its plasma concentrations and lack of adverse effects in the breastfed infant. Eur J Clin Pharmacol. 2006;62:633-8. PMID: 16699799
5. Berle JO, Steen VM, Aamo TO et al. Breastfeeding during maternal antidepressant treatment with serotonin reuptake inhibitors: infant exposure, clinical symptoms, and cytochrome P450 genotypes. J Clin Psychiatry. 2004;65:1228-34. PMID: 15367050
6. Merlob P. Use of escitalopram during lactation. BELTIS Newsl. 2005;Number 13:40-4.
7. Gentile S. Escitalopram late in pregnancy and while breast-feeding. Ann Pharmacother. 2006;40:1696-7. PMID: 16912243
8. Potts AL, Young KL, Carter BS, Shenai JP. Necrotizing enterocolitis associated with in utero and breast milk exposure to the selective serotonin reuptake inhibitor, escitalopram. J Perinatol. 2007;27:120-2. PMID: 17262045
9. Schaefer C, Peters P, Miller RK, eds. Drugs during pregnancy and lactation. Treatment options and risk assessment, 2nd ed. Amsterdam; Boston: Elsevier Academic Press. 2007:714-5.
10. Hale TW, Kendall-Tackett K, Cong Z et al. Discontinuation syndrome in newborns whose mothers took antidepressants while pregnant or breastfeeding. Breastfeed Med. 2010;5:283-8. PMID: 20807106
11. Neuman G, Colantonio D, Delaney S et al. Bupropion and escitalopram during lactation. Ann Pharmacother. 2014;48:928-31. PMID: 24732787
12. Kieviet N, Hoppenbrouwers C, Dolman KM et al. Risk factors for poor neonatal adaptation after exposure to antidepressants in utero. Acta Paediatr. 2015;104:384-91. PMID: 25559357
13. Arya DK, Taylor WS. Lactation associated with fluoxetine treatment. Aust N Z J Psychiatry. 1995;29:697. Letter. PMID: 8825840
14. Egberts ACG, Meyboom RHB, De Koning FHP et al. Non-puerperal lactation associated with antidepressant drug use. Br J Clin Pharmacol. 1997;44:277-81. PMID: 9296322
15. Iancu I, Ratzoni G, Weitzman A et al. More fluoxetine experience. J Am Acad Child Adolesc Psychiatry. 1992;31:755-6. Letter. PMID: 1644743
16. Gonzalez Pablos E, Minguez Martin L, Hernandez Fernandez M et al. [A clinical case of galactorrhoea after citalopram treatment]. Actas Esp Psiquiatr. 2001;29:414. PMID: 11730581
17. Gulsun M, Algul A, Semiz UB et al. A case with euprolactinemic galactorrhea induced by escitalopram. Int J Psychiatry Med. 2007;37:275-8. PMID: 18314855
18. Aggarwal A, Kumar R, Sharma RC, Sharma DD. Escitalopram induced galactorrhoea: a case report. Prog Neuropsychopharmacol Biol Psychiatry. 2010;34:557-8. PMID: 20138200
19. Shim SH, Lee YJ, Lee EC. A case of galactorrhea associated with excitalopram (sic). Psychiatry Investig. 2009;6:230-2. PMID: 20046401
20. Mahasuar R , Majhi P, Ravan JR. Euprolactinemic galactorrhea associated with use of imipramine and escitalopram in a postmenopausal woman. Gen Hosp Psychiatry. 2010;32:341.e11-3. PMID: 20430243
21. Praharaj SK. Euprolactinemic galactorrhea with escitalopram. J Neuropsychiatry Clin Neurosci. 2015;26:E25-6. Letter. PMID: 25093774
22. Marshall AM, Nommsen-Rivers LA, Hernandez LL et al. Serotonin transport and metabolism in the mammary gland modulates secretory activation and involution. J Clin Endocrinol Metab. 2010;95:837-46. PMID: 19965920
23. Gorman JR, Kao K, Chambers CD. Breastfeeding among women exposed to antidepressants during pregnancy. J Hum Lact. 2012;28:181-8. PMID: 22344850
Last Revision Date
20150505
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Source: LactMed – National Library of Medicine (NLM)