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[Pharmacology](https://durgical.com/en/pharmacology/) · Class

# Gabapentinoids

GABA look-alike medicines that bind a calcium channel subunit and quiet overactive nerves. Used for nerve pain and as add-on seizure treatment.

Updated 2026-11-01

## What they are

Gabapentin and pregabalin, structural relatives of GABA that do not act on GABA receptors. The WHO ATC system files them with the analgesics, because their main use is neuropathic pain (postherpetic neuralgia, diabetic neuropathy); both are also add-on treatment for focal seizures.

## Mechanism of action

They bind the α2δ-1 subunit of voltage-gated calcium channels. This is thought to reduce the number of channels at presynaptic terminals and the calcium-dependent release of excitatory, pain-signalling neurotransmitters in the spinal cord and brain.

Target: α2δ-1 subunit of voltage-gated calcium channels

## Key points

- Not metabolized by the liver: excreted unchanged by the kidneys, so doses are adjusted in kidney disease.
- With opioids or other central nervous system depressants they can cause serious respiratory depression.
- Common effects: dizziness and sleepiness; pregabalin also causes peripheral oedema and weight gain.
- Misuse and dependence occur; pregabalin is a controlled substance in the United States.
- Despite the name, they do not bind GABA receptors or change GABA uptake or breakdown.

## Drugs in this class

- [**Gabapentin** A nerve-pain and add-on seizure medicine that binds a calcium channel subunit. It causes drowsiness and dizziness and… α2δ-1 subunit of voltage-gated calcium channels](https://durgical.com/en/pharmacology/gabapentin/)
- [**Pregabalin** A relative of gabapentin for nerve pain, fibromyalgia and focal seizures. It causes dizziness, sleepiness, swelling… α2δ-1 subunit of voltage-gated calcium channels](https://durgical.com/en/pharmacology/pregabalin/)

## Others in the class

- Mirogabalin

## Test yourself

Think of the answer, then tap the question to see it.

## Where do gabapentin and pregabalin bind?

On the α2δ-1 subunit of voltage-gated calcium channels, which reduces the release of excitatory neurotransmitters. They do not act on GABA receptors.

## Why are gabapentinoid doses reduced in kidney disease?

They are not metabolized and leave the body unchanged in the urine, so they accumulate when kidney function falls.

## Which combination with a gabapentinoid can cause dangerous respiratory depression?

Opioids or other central nervous system depressants, and also underlying respiratory impairment.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N02BF) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [DailyMed - GABAPENTIN capsule](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=16542ee6-0e0e-4d3c-8b32-60ff6ef48846) (DailyMed (U.S. National Library of Medicine), 2026); [DailyMed - PREGABALIN capsule](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e48db3c2-7351-41f2-a451-5a8341c4125c) (DailyMed (U.S. National Library of Medicine), 2026).

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