Gabapentin is a γ-aminobutyric acid analog formally indicated for the treatment of epilepsy and neuropathic pain that is gaining increased popularity. Gabapentin has been historically considered a safe medication, including during pregnancy and lactation, with low reported concerns for misuse and use disorders. However, new empirical efforts are revealing concerns regarding the safety of widespread gabapentin use, particularly in pregnancy and for individuals with a propensity toward substance misuse. The Food and Drug Administration’s full prescribing information report on gabapentin provides concerning preclinical data and then states that gabapentin is potentially “developmentally toxic” and has an unknown risk of birth impacts. Concerns have also been raised surrounding in utero exposure to gabapentin due to the onset and presentation of atypical and/or difficult to control withdrawal signs and symptoms in neonates, including those dually exposed to opioids, as well as neonatal exposure to gabapentin via breastmilk. Moreover, nonprescribed gabapentin use has become an increasing problem, with opioid use disorder being the greatest risk factor for such misuse. This article summarizes the current literature regarding gabapentin use during pregnancy and related prenatal and neonatal exposure outcomes with special consideration for interactions between gabapentin and opioid use. Taken together, the current literature suggests that gabapentin use should be considered with caution during pregnancy and during the post-partum period. Well-controlled, prospective research studies are needed to determine the extent of the risks and benefits of prescribed and nonprescribed gabapentin exposure to pregnant people and their neonates.