Although low levels of propoxyphene are found in the milk, infant sedation, apnea, bradycardia, and cyanosis have been reported with the maternal use of oral opioids such as propoxyphene in the first week of life. Monitor the infant for drowsiness, adequate weight gain, and developmental milestones, especially in younger, exclusively breastfed infants. Once the mother's milk comes in, it is best to limit maternal intake and to supplement analgesia with a nonnarcotic analgesic, if necessary. If the baby shows signs of increased sleepiness (more than usual), difficulty breastfeeding, breathing difficulties, or limpness, a physician should be contacted immediately.
Propoxyphene is metabolized to active norpropoxyphene (25%) and to several inactive metabolites. Norpropoxyphene has a 30 to 36 hour half-life. The oral bioavailability of norpropoxyphene is unknown. Propoxyphene is available in 2 salt forms: 65 mg of thehydrochlorideform is equivalent to 100 mg of the napsylate.
Six breastfeeding mothers, 5 in the first few days postcesarean section and 1 at 10 months postpartum were given oral propoxyphenehydrochloride130 mg once then 65 mg every 4 hours for 16 hours for a cumulative dose of 390 mg. Breastmilk propoxyphene was measured at 1, 3, 5, 7, and 9 hours after the last dose. Propoxyphene peak levels occurred at 3 hours while norpropoxyphene levels remained fairly constant. An average propoxyphene and norpropoxyphene milk level over the 8-hour collection period was calculated for each patient and varied substantially among patients (range 24 to 210 mcg/L for propoxyphene and 54 to 606 mcg/L for norpropoxyphene). Norpropoxyphene had a longer maternal plasma half-life and thus accumulated in breastmilk more so than propoxyphene. Greater breastmilk production was associated with higher milk levels of both propoxyphene and norpropoxyphene. Using the highest average milk propoxyphene level in this study, an exclusively breastfed infant would receive 32 mcg/kg daily of propoxyphene and 91 mcg/kg daily of norpropoxyphene, equivalent to about 2% of the maternal weight-adjusted dosage.
Relevant published information was not found as of the revision date.
Effects in Breastfed Infants:
In a case-control study of 12 breastfed term newborns with unexplained episodes of apnea, bradycardia or cyanosis during the first week of life, maternal oral propoxyphene use was determined to be the probable cause. A higher proportion of newborns with episodes, 83 compared to 31%, had mothers using opiates, including propoxyphene, for postpartum analgesia. The mean number of doses taken was also higher with mothers of affected newborns taking a mean of 10 doses (range 4 to 22) compared to 5 doses (range 1 to 13) in the control group.
A full-term breastfed infant had mild hypotonia and nursing poorly at 10 days of age; the infant had not regained her birth weight by this time. By 7 days later, the mother had less milk and stopped nursing. The infant's mother had been prescribed 6 capsules daily of propoxyphene 30 mg plus acetaminophen 500 mg for the first 10 days postpartum. Hair samples from the infant were positive for propoxyphene and norpropoxyphene and were higher than the mother's hair sample concentrations. Propoxyphene was probably the cause of the adverse reactions in the infant.
Possible Effects on Lactation:
Narcotics can increase serum prolactin. However, the prolactin level in a mother with established lactation may not affect her ability to breastfeed.
1. Kunka RL, Venkataramanan R, Stern RM et al. Excretion of propoxyphene and norpropoxyphene in breast milk. Clin Pharmacol Ther. 1984;35:675-80. PMID:6713779 2. Kunka RL, Yong CL, Ladik CF et al. Liquid chromatographic determination of propoxyphene and norpropoxyphene in plasma and breast milk. J Pharm Sci. 1985;74:103-4. PMID:3981406 3. Naumburg EG, Meny RG. Breast milk opioids and neonatal apnea. Am J Dis Child. 1988;142:11-2. Letter. PMID:3341293 4. Rigourd V, Amirouche A, Tasseau A et al. Retrospective diagnosis of an adverse drug reaction in a breastfed neonate: liquid chromatography-tandem mass spectrometry quantification of dextropropoxyphene and norpropoxyphene in newborn and maternal hair. J Anal Toxicol. 2008;32:787-9. PMID:19021937 5. Tolis G, Dent R, Guyda H. Opiates, prolactin, and the dopamine receptor. J Clin Endocrinol Metab. 1978;47:200-3. PMID:263291
CAS Registry Number:
LactMed Record Number:
Last Revision Date:
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.