Abstract
Originally marketed under the brand name Neurontin, the anticonvulsant drug gabapentin has become one of the most widely prescribed—and one of the most controversial—drugs in America. On the market for nearly three decades, the drug has been prescribed for everything from chronic cough to chronic pain and hot flashes to bipolar disorder; but is it the real deal, or is it just the brain-child of aggressive marketing, false advertising, and wishful thinking? This critical review will dissect gabapentin down to its molecular roots and trace its wide-ranging effects to better understand the drug and the persons who use it. It will also discuss how gabapentin (and other anticonvulsant drugs) may be doing something more profound than just treating acute symptoms. An emerging hypothesis contends that psychiatric and related function symptoms are driven by pathological hyperactivity in symptom-related circuits in the brain and that the same abnormality may, over time, be driving the development of a plethora of general medical conditions, including diabetes, high blood pressure, cardiovascular disease, autoimmune diseases, dementia, and cancer. Emerging evidence suggests that the underlying physiological abnormality—an inherent hyperexcitability of the neurological system—is very common, and clinical correlation suggests that it is inherited in a classic autosomal dominant distribution. There is also evidence that the abnormality may be reflected in one’s resting vital signs, an observation that could help carriers identify the trait themselves. Gabapentin, together with other pharmacological (and non-pharmacological) interventions that reduce neuronal excitability, may, in addition to their immediate effects, have the potential to prevent the long-term erosive effects of neuronal hyperexcitability by simply turning down the stress response. Recognition of this could usher in history’s greatest campaign in the fight against sickness and disease.
Highlights
According to the New England Journal of Medicine, gabapentin is one of the most popular prescription drugs in America [1]
In conjunction with its illicit use, gabapentin is increasingly being found in tissue samples of persons who have died of drug overdose [5]
From the perspective of the Neuronal Hyperexcitability Hypothesis of Psychiatric Disorders in conjunction with recent gene association studies, gabapentin is primarily treating the reversible consequences of neuronal hyperexcitability; namely, various psychiatric disorders, substance use disorders, and chronic pain disorders
Summary
According to the New England Journal of Medicine, gabapentin is one of the most popular prescription drugs in America [1]. As of August, 2020, gabapentin was the 6th most commonly filled medication at pharmacies [3], with over 400 million prescriptions written between 2004 and 2018 [4]. Introduced in 1993 by Parke-Davis under the brand name Neurontin, gabapentin (Figure 1) has gradually found its way into the treatment of everything from chronic cough to chronic pain and hot flashes to bipolar disorder. American Journal of Clinical and Experimental Medicine 2021; 9(4): 122-134 dealers and persons who struggle with a wide range of substance use disorders [5, 6]. In conjunction with its illicit use, gabapentin is increasingly being found in tissue samples of persons who have died of drug overdose [5]. That begs the question: is gabapentin a dangerous drug? Is it a medical panacea? Or is it something else?
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More From: American Journal of Clinical and Experimental Medicine
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