Also known as 3-Isobutyl GABA, CI 1008, CI-1008, Lyrica, PD 144723
A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation.
Originator: NCI Thesaurus | Source: The website of the National Cancer Institute (http://www.cancer.gov)
Can I take Pregabalin while breastfeeding?
Very limited data indicate that amounts of pregabalin in breastmilk are low. If pregabalin is required by the mother of an older infant, it is not a reason to discontinue breastfeeding, but until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
Drug levels
Maternal Levels. In one woman, the breastmilk pregabalin level was about equal to the maternal serum concentration.[1]
Ten women who averaged 35.6 weeks postpartum (range 20 to 43 weeks) were given pregabalin 150 mg every 12 hours for 4 doses. Milk samples were obtained before the last dose and 5 times during the 24 hours after the last dose. Three additional collections were made between 24 and 48 hours after the last dose in 5 of the subjects. The average peak breastmilk pregabalin concentration was 4.63 mg/L and the average breastmilk pregabalin concentration was 2.05 mg/L. The average infant dosage was 0.31 mg/kg/day, or about 7% of the maternal weight-adjusted dosage.[2]
Infant Levels. The breastfed infant of a woman who was taking pregabalin (dose not specified) as an anticonvulsant during pregnancy and breastfeeding had a pregabalin serum concentration of 429 mcg/L at 48 hours postpartum, which was about 8% of the mother’s serum concentration. Some of the infant’s serum concentration could have been derived from transplacental passage, because the pregabalin half-life in this and another newborn averaged 17 hours.[1]
Effects in breastfed infants
Maternal Levels. In one woman, the breastmilk pregabalin level was about equal to the maternal serum concentration.[1]
Ten women who averaged 35.6 weeks postpartum (range 20 to 43 weeks) were given pregabalin 150 mg every 12 hours for 4 doses. Milk samples were obtained before the last dose and 5 times during the 24 hours after the last dose. Three additional collections were made between 24 and 48 hours after the last dose in 5 of the subjects. The average peak breastmilk pregabalin concentration was 4.63 mg/L and the average breastmilk pregabalin concentration was 2.05 mg/L. The average infant dosage was 0.31 mg/kg/day, or about 7% of the maternal weight-adjusted dosage.[2]
Infant Levels. The breastfed infant of a woman who was taking pregabalin (dose not specified) as an anticonvulsant during pregnancy and breastfeeding had a pregabalin serum concentration of 429 mcg/L at 48 hours postpartum, which was about 8% of the mother’s serum concentration. Some of the infant’s serum concentration could have been derived from transplacental passage, because the pregabalin half-life in this and another newborn averaged 17 hours.[1]
Possible effects on lactation
A study randomized pregnant women to either a single dose of pregabalin 150 mg (n = 45), 300 mg (n = 45), or placebo (n = 45) orally 1 hour before induction of anesthesia for an elective cesarean section to reduce postoperative analgesia requirements. Three infants of mothers in the pregabalin 300 mg group had difficulty latching on for breastfeeding for 8 hours after delivery, although none were sedated.[2]
References
1. Ohman I, De Flon P, Tomson T. Pregabalin kinetics in the neonatal period, and during lactation. Epilepsia. 2011;52 (Suppl 6):249-50. Abstract p824.
2. Lockwood PA, Pauer L, Scavone JM et al. The pharmacokinetics of pregabalin in breast milk, plasma, and urine of healthy postpartum women. J Hum Lact . 2016. PMID: 26961752
3. El Kenany S, El Tahan MR. Effect of preoperative pregabalin on post-caesarean delivery analgesia: A dose-response study. Int J Obstet Anesth. 2016;26:24-31. PMID: 26718698
Last Revision Date
20160426
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Source: LactMed – National Library of Medicine (NLM)