What Drug Category Does Gabapentin Fall Under? An In-depth Look

October 8, 2025 •

2 min read

Over 70 million prescriptions for gabapentin were dispensed in the U.S. in 2021, highlighting its widespread use. To properly understand this medication, it's essential to know what drug category does gabapentin fall under and its unique pharmacological properties.

Quick Summary

Gabapentin belongs to the anticonvulsant class of medications and, more specifically, is a gabapentinoid. It works by affecting nerve signals rather than conventional GABA receptors. The drug is used to treat epilepsy, postherpetic neuralgia, and restless legs syndrome, with varying controlled substance classifications by state.

Key Points

Anticonvulsant Class: Gabapentin is primarily an anticonvulsant, or antiepileptic, medication used to control seizures in people with epilepsy.
Gabapentinoid Designation: More specifically, it is a gabapentinoid, a class of drugs that are structural analogues of GABA but do not act directly on GABA receptors.
Mechanism of Action: It functions by binding to the alpha-2-delta ($\alpha_2\delta$) subunit of voltage-gated calcium channels, which modulates nerve activity and helps treat neuropathic pain and seizures.
Diverse Clinical Uses: In addition to epilepsy, gabapentin is approved to treat postherpetic neuralgia and restless legs syndrome, and is used off-label for other pain conditions and anxiety.
Varying Controlled Status: While not federally controlled in the U.S., many states have reclassified gabapentin as a Schedule V controlled substance due to potential for abuse.
Balancing Benefits and Risks: The medication's benefits, such as pain relief, must be weighed against potential side effects, including dizziness, drowsiness, and serious risks like respiratory depression, especially with opioids.

The Primary Classification: Anticonvulsant

Gabapentin is primarily classified as an anticonvulsant or antiepileptic drug, used to prevent and control seizures. It's used for certain partial-onset seizures in adults and children. Its mechanism is different from older anticonvulsants.

The More Specific Category: Gabapentinoid

More specifically, gabapentin is a gabapentinoid. These drugs are similar in structure to GABA but don't bind to GABA receptors. Gabapentin works by binding to the alpha-2-delta ($\alpha_2\delta$) subunit of voltage-dependent calcium channels. This action may reduce the release of excitatory neurotransmitters, calming nerve cells and helping manage seizures and neuropathic pain.

Therapeutic Uses of Gabapentin

Gabapentin is used for several conditions, both FDA-approved and off-label:

FDA-Approved Uses
- Partial-Onset Seizures: As add-on therapy for epilepsy.
- Postherpetic Neuralgia (PHN): For nerve pain after shingles.
- Restless Legs Syndrome (RLS): An extended-release form is approved for moderate-to-severe RLS.
Common Off-Label Uses
- Other neuropathic pain (e.g., diabetic neuropathy).
- Anxiety disorders.
- Fibromyalgia.

Controlled Substance Status: A Federal vs. State Issue

Federally, gabapentin is not a controlled substance. However, concerns about misuse, especially with opioids, have led many states to reclassify it.

States with Controlled Substance Status

Several states have made gabapentin a Schedule V controlled substance, which means stricter rules for prescribing and dispensing. Examples include Alabama, Kentucky, and Virginia. Many states also use Prescription Drug Monitoring Programs (PDMPs) for gabapentin.

Comparing Gabapentin and Pregabalin

Gabapentin and pregabalin (Lyrica) are both gabapentinoids. Here's a comparison:


Feature	Gabapentin (Neurontin, Gralise)	Pregabalin (Lyrica)
Drug Class	Anticonvulsant, Gabapentinoid	Anticonvulsant, Gabapentinoid
Mechanism of Action	Binds to the $\alpha_2\delta$ subunit of voltage-gated calcium channels.	Binds to the $\alpha_2\delta$ subunit of voltage-gated calcium channels.
FDA-Approved Uses	Partial seizures, PHN, RLS.	Fibromyalgia, diabetic nerve pain, PHN, spinal cord injury nerve pain, seizures.
Absorption	Saturable absorption, lower bioavailability at higher doses.	More rapid and linear absorption.
Controlled Status	Federally non-controlled; Schedule V in several states.	Federally classified as a Schedule V controlled substance.

Potential Side Effects and Risks

Gabapentin can cause side effects. Common ones include:

Dizziness and drowsiness
Fatigue
Headache
Swelling (hands, feet, ankles)
Nausea
Coordination problems

Serious, less common side effects can include:

Breathing problems: Increased risk with opioids or other CNS depressants, especially in older adults or those with respiratory issues.
Suicidal thoughts: A small risk with anticonvulsants.
Severe allergic reactions: Swelling of face, lips, tongue.

Always consult a healthcare provider for full risk information.

Conclusion

Gabapentin is an anticonvulsant and gabapentinoid. Originally for epilepsy, it's effective for neuropathic pain and RLS due to its action on voltage-gated calcium channels. Its controlled status varies by state due to misuse concerns, particularly with opioids. Always use as prescribed and be aware of side effects and local regulations.

[Authoritative Outbound Link]: National Institutes of Health (NIH) Gabapentin information

Frequently Asked Questions

No, gabapentin is not a narcotic. It is an anticonvulsant medication and is not related to opioids or narcotics, although combining it with opioids can be dangerous.

At the federal level in the U.S., gabapentin is not a controlled substance. However, several states have reclassified it as a Schedule V controlled substance due to potential misuse.

Anticonvulsant is a broad drug category for medications that treat seizures. Gabapentinoid is a more specific subcategory for drugs like gabapentin and pregabalin that are structural analogues of GABA but work via a distinct mechanism involving calcium channels.

Gabapentin works by binding to the $\alpha_2\delta$ subunit of voltage-gated calcium channels, which helps to reduce the release of certain excitatory neurotransmitters and calm overactive nerve cells.

Concerns have risen over the potential for gabapentin misuse and abuse, particularly when taken with opioids, which increases the risk of overdose and breathing problems.

Common side effects include dizziness, drowsiness, fatigue, headache, nausea, and swelling in the extremities. These often occur at the beginning of treatment or with higher doses.

Gabapentin is most effective for neuropathic pain, which involves nerve damage. It is not typically used for routine pain from minor injuries or arthritis.