Gabapentin, sold under brand names like Neurontin and Gralise, is a prescription medication primarily classified as an anticonvulsant. It was initially developed as a treatment for epilepsy to help manage partial seizures, and it is also FDA-approved for treating the nerve pain associated with postherpetic neuralgia, which follows a shingles outbreak. Reports have emerged questioning whether it can produce psychoactive effects or a feeling of being “high,” particularly when used outside of medical guidance. This article explores the nature of gabapentin’s effects, the brain chemistry involved, and the significant dangers associated with its non-prescribed use.
Understanding the Psychoactive Effects
Gabapentin is not designed to produce euphoria, yet it can generate psychoactive effects, especially when taken in high doses that exceed prescribed therapeutic limits. Individuals who misuse the drug often report sensations similar to those caused by central nervous system depressants, such as benzodiazepines or opioids. These reported feelings include a sense of deep relaxation, mild sedation, and a calming effect that can reduce anxiety.
The resulting sensation is sometimes described as a marijuana-like buzz or a feeling of euphoria, which is highly dose-dependent and varies significantly from person to person. Because the drug can slow brain activity, the psychoactive effect may also manifest as altered perception or a feeling of detachment. This potential for non-therapeutic effects is a primary driver for the increasing reports of gabapentin misuse.
The risk of experiencing these effects is particularly elevated when the medication is consumed rapidly or in supratherapeutic amounts, with some misuse doses reaching up to 12,000 mg per day.
How Gabapentin Affects Brain Chemistry
Gabapentin’s psychoactive potential stems from its unique mechanism of action within the central nervous system. The drug works by binding with high affinity to the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels (VGCCs). This binding disrupts the movement of these channels to the cell membrane of presynaptic neurons.
By decreasing the density of VGCCs on the cell surface, gabapentin effectively modulates the release of several excitatory neurotransmitters. Specifically, it inhibits the release of glutamate, which is a powerful excitatory chemical messenger in the brain. Reducing this neuronal hyperexcitability contributes to both its anti-seizure and pain-relieving actions, as well as the sedative and mood-altering effects.
The drug’s structural similarity to the neurotransmitter gamma-aminobutyric acid (GABA) is misleading, as gabapentin does not directly bind to GABA receptors. Instead, its main impact is on the α2δ-1 protein, which plays a role in regulating the communication between neurons. When this communication is dampened, it produces the reduced anxiety and sedation that users associate with the drug’s psychoactive properties.
The Dangers of Non-Prescribed Use
Taking gabapentin outside of a doctor’s supervision or in higher-than-prescribed doses carries significant and potentially fatal risks. A major danger involves the potential for serious drug interactions, particularly when gabapentin is combined with other central nervous system (CNS) depressants. These depressants include common substances like opioids, alcohol, and certain anti-anxiety medications.
When combined, gabapentin and CNS depressants can have an additive effect, leading to dangerously slowed or stopped breathing, a condition known as respiratory depression. Individuals who already have underlying respiratory issues, such as chronic obstructive pulmonary disease (COPD), or those who are elderly, face an even greater risk of severe breathing problems.
Furthermore, long-term non-prescribed use can lead to physical dependence, resulting in severe withdrawal symptoms upon abrupt cessation. Withdrawal is often characterized by intense anxiety, confusion, profuse sweating, and insomnia. For individuals taking the drug for seizure disorders, sudden discontinuation dramatically increases the risk of withdrawal seizures. Misuse is also strongly associated with individuals who have a concurrent opioid use disorder, amplifying the combined risk of death.
Medical Context and Common Side Effects
When gabapentin is used as directed by a healthcare provider for conditions like neuropathic pain or seizures, the side effects are generally manageable. The most frequently reported adverse effects include:
- Feeling tired, dizziness, and somnolence.
- Difficulties with coordination or balance (ataxia).
- Peripheral edema (swelling in the legs and feet).
- Weight gain, nausea, vomiting, and double vision.
These side effects often improve as the body adjusts to the medication. If a person decides to stop taking the drug, they must consult with their doctor to establish a tapering schedule. Abruptly stopping gabapentin can lead to severe adverse reactions, including the risk of withdrawal-induced seizures.