Drug Levels and Effects:

Summary of Use during Lactation:

Although no data are available for the use of paliperidone during breastfeeding, it is the active metabolite of risperidone. Risperidone data indicate that the concentrations of paliperidone (9-hydroxyrisperidone) in breastmilk are low, and amounts ingested by the infant are small. Because there is no published experience with paliperidone during breastfeeding and little long-term follow-up data, other agents may be preferred, especially while nursing a newborn or preterm infant. Because paliperidone is available only as a sustained-release product, timing of nursing with respect to doses would not be useful.

Drug Levels:

Paliperidone is 9-hydroxyrisperidone, the active metabolite of risperidone. No studies have measured paliperidone in breastmilk after administration of paliperidone. However, 9-hydroxyrisperidone has been measured in milk and plasma after administration of risperidone.

Maternal Levels.

The manufacturer reports that the average maternal plasma concentration of paliperidone after the maximum dose of 12 mg daily is 45 mcg/L. Using the average milk-to-plasma ratio of 9-hydroxyrisperidone of 0.3 from 3 reports of risperidone use during breastfeeding,[1][2][3] the average milk concentration would be expected to be about 14 mcg/L or 2.1 mcg/kg daily. An exclusively breastfed infant would receive an average of about 1% of the maternal weight-adjusted dosage with this maternal dosage.

Infant Levels.

In 2 breastfed infants (6 weeks and 3.3 months old) whose mothers were taking 2 mg of risperidone twice daily and 1.5 mg daily in 2 divided doses, respectively, risperidone and 9-hydroxyrisperidone were both undetectable (<1 mcg/L) in the serums of the infants.[2]

An infant was breastfed 6 times daily during maternal therapy with risperidone 2 mg once daily. Fifteen hours after the mother's last dose, the infant's plasma levels of risperidone was undetectable and 9-hydroxyrisperidone was 0.1 mcg/L.[3]

Effects in Breastfed Infants:

No published information was found as of the revision date. However, limited data from the use of risperidone during nursing indicate no short- or long-term adverse effects on the infant.[2][3][4]

Possible Effects on Lactation:

Paliperidone has caused elevated prolactin serum levels, gynecomastia, and galactorrhea in patients taking the drug.[5][6][7][8][9] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternate Drugs to Consider:



1. Hill RC, McIvor RJ, Wojnar-Horton RE et al. Risperidone distribution and excretion into human milk: case report and estimated infant exposure during breast-feeding. J Clin Psychopharmacol. 2000;20:285-6. Letter. PMID:10770482
2. Ilett KF, Hackett LP, Kristensen JH et al. Transfer of risperidone and 9-hydroxyrisperidone into human milk. Ann Pharmacother. 2004;38:273-6. PMID:14742766
3. Aichhorn W, Stuppaeck C, Whitworth AB. Risperidone and breast-feeding. J Psychopharmacol. 2005;19: 211-3 . PMID:15728443
4. Ratnayake T, Libretto SE. No complications with risperidone treatment before and throughout pregnancy and during the nursing period. J Clin Psychiatry. 2002;63:76-7. PMID:11838633
5. Davidson M, Emsley R, Kramer M et al. Efficacy, safety and early response of paliperidone extended-release tablets (paliperidone er): results of a 6-week, randomized, placebo-controlled study. Schizophr Res. 2007;93:117-30. PMID:17466492
6. Kane J, Canas F, Kramer M et al. Treatment of schizophrenia with paliperidone extended-release tablets: a 6-week placebo-controlled trial. Schizophr Res. 2007;90:147-61. PMID:17092691
7. Marder SR, Kramer M, Ford L et al. Efficacy and safety of paliperidone extended-release tablets: results of a 6-week, randomized, placebo-controlled study. Biol Psychiatry. 2007;62:1363-70. PMID:17601495
8. Macaluso M, Khan AY. A 19-year-old Black woman with psychotic and depressive symptoms. Psychiatr Ann. 2008;38:312-4.
9. Skopek M, Manoj P. Hyperprolactinaemia during treatment with paliperidone. Australas Psychiatry. 2010;18:261-3. PMID:20429680

Substance Identification:

Substance Name:


CAS Registry Number:


Drug Class:

  • Antipsychotic Agents

  • Administrative Information:

    LactMed Record Number:


    Last Revision Date:

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