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Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-.

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Drugs and Lactation Database (LactMed) [Internet].

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Paliperidone

Last Revision: February 15, 2021.

Estimated reading time: 2 minutes

CASRN: 144598-75-4

image 135072932 in the ncbi pubchem database

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. A safety scoring system finds paliperidone possible to use cautiously during breastfeeding,[1] although others do not recommend it.[2] 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 adult plasma concentration of paliperidone after the maximum dose of 12 mg daily is about 37 mcg/L.[3] Using the average milk-to-plasma ratio of 9-hydroxyrisperidone of 0.3 from 3 reports of risperidone use during breastfeeding,[4-6] the average milk concentration would be expected to be about 11 mcg/L or a dose of 1.7 mcg/kg daily. An exclusively breastfed infant would receive an average of less than 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.[5]

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.[6]

Effects in Breastfed Infants

No published information on paliperidone was found as of the revision date. However, limited data from the use of its parent drug, risperidone, during nursing indicate no short- or long-term adverse effects on the infant.[5-7]

Effects on Lactation and Breastmilk

Paliperidone has caused elevated prolactin serum levels, gynecomastia, and galactorrhea in patients taking the drug.[8-14] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternate Drugs to Consider

Haloperidol, Olanzapine

References

1.
Uguz F. A new safety scoring system for the use of psychotropic drugs during lactation. Am J Ther. 2021;28:e118–e26. [PubMed: 30601177]
2.
Larsen ER, Damkier P, Pedersen LH, et al. Use of psychotropic drugs during pregnancy and breast-feeding. Acta Psychiatr Scand Suppl. 2015:1–28. [PubMed: 26344706]
3.
Food and, Drug, Administration, Drug, approval, package. Invega (paliperidone) extended-release tablets. 2006:127. http://www​.accessdata​.fda.gov/drugsatfda_docs​/nda/2006/021999s000_TOC.cfm.
4.
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. [PubMed: 10770482]
5.
Ilett KF, Hackett LP, Kristensen JH, et al. Transfer of risperidone and 9-hydroxyrisperidone into human milk. Ann Pharmacother. 2004;38:273–6. [PubMed: 14742766]
6.
Aichhorn W, Stuppaeck C, Whitworth AB. Risperidone and breast-feeding. J Psychopharmacol. 2005;19:211–3. [PubMed: 15728443]
7.
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. [PubMed: 11838633]
8.
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. [PubMed: 17466492]
9.
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. [PubMed: 17092691]
10.
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. [PubMed: 17601495]
11.
Macaluso M, Khan AY. A. 19-year-old Black woman with psychotic and depressive symptoms. Psychiatr Ann. 2008;38:312–4. [CrossRef]
12.
Skopek M, Manoj P. Hyperprolactinaemia during treatment with paliperidone. Australas Psychiatry. 2010;18:261–3. [PubMed: 20429680]
13.
Einarson TR, Hemels ME, Nuamah I, et al. An analysis of potentially prolactin-related adverse events and abnormal prolactin values in randomized clinical trials with paliperidone palmitate. Ann Pharmacother. 2012;46:1322–30. [PubMed: 22947594]
14.
Ray I, Jones RM. A. 30-year-old woman with galactorrhea. CMAJ. 2020;192:E397–e8. [PMC free article: PMC7162438] [PubMed: 32392501]

Substance Identification

Substance Name

Paliperidone

CAS Registry Number

144598-75-4

Drug Class

Breast Feeding

Lactation

Antipsychotic Agents

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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