[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Gabapentinoids](https://durgical.com/en/pharmacology/classes/gabapentinoids/) › Pregabalin

[Pharmacology](https://durgical.com/en/pharmacology/) · [Gabapentinoids](https://durgical.com/en/pharmacology/classes/gabapentinoids/)

# Pregabalin

A relative of gabapentin for nerve pain, fibromyalgia and focal seizures. It causes dizziness, sleepiness, swelling and weight gain.

Updated 2026-11-01

- Class: [Gabapentinoids](https://durgical.com/en/pharmacology/classes/gabapentinoids/)
- Ion channel: α2δ-1 subunit of voltage-gated calcium channels
- ATC code: N02BF02

⇅**α2δ-1 subunit of voltage-gated calcium channels**Pregabalin

ⓘ The figure shows gabapentin, which occupies the same site, bound to the α2δ-1 subunit (from rabbit) in a complex with the human Cav1.2 calcium channel.

**Target in 3D:** α2δ-1 subunit of voltage-gated calcium channels. PDB structure 8FD7 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8FD7) · Drag to rotate · pinch to zoom

## Mechanism of action

Pregabalin binds the α2δ subunit of voltage-gated calcium channels. In models of nerve damage this reduces the calcium-dependent release of pain-signalling neurotransmitters in the spinal cord, possibly by disturbing channel trafficking or reducing calcium currents.

- Binds the α2δ subunit of voltage-gated calcium channels
- Channel trafficking and calcium currents are reduced
- Less release of pain-signalling transmitters in the spinal cord
- Nerve pain and seizures are dampened

## Pharmacokinetics

**Absorption**
Well absorbed by mouth

**Metabolism**
Hardly metabolized

**Elimination**
Mainly unchanged in the urine; the dose is adjusted in kidney disease

**Half-life**
About 6 hours

## Indications

- Neuropathic pain of diabetic peripheral neuropathy or spinal cord injury
- Postherpetic neuralgia (pain after shingles) [Herpes zoster (shingles) →](https://durgical.com/en/conditions/herpes-zoster/)
- Fibromyalgia
- Add-on treatment of focal seizures [Epilepsy and seizures →](https://durgical.com/en/conditions/epilepsy-and-seizures/)

## Adverse effects

### Common

- Dizziness and sleepiness
- Dry mouth and blurred vision
- Peripheral oedema
- Weight gain
- Difficulty concentrating

### Serious (rare, important)

- Angioedema and other hypersensitivity reactions
- Respiratory depression with other sedatives or respiratory impairment
- Misuse and dependence
- Suicidal thoughts

## Contraindications

- Hypersensitivity to pregabalin

## Key interactions

**Opioids and other central nervous system depressants**
Respiratory depression and heavy sedation

**Thiazolidinediones (pioglitazone)**
More oedema and weight gain

**ACE inhibitors**
Higher risk of angioedema

## What is monitored

- Sedation and breathing
- Oedema and weight, especially with heart failure
- Kidney function
- Mood and signs of misuse

## Administration and safety

- Given by mouth
- Controlled medicine in some countries because of misuse risk
- Withdrawn gradually: stopping suddenly can cause insomnia, nausea, headache and anxiety, and more seizures in epilepsy

## Nursing care

- Teach to report swelling of the face, lips or tongue at once
- Watch for ankle swelling and weight gain
- Warn about dizziness and sleepiness before driving
- Check sedation and breathing when opioids are also given

## Pregnancy and breastfeeding

Human data are limited; benefits and risks are weighed with the care team, and there is a pregnancy registry for antiseizure medicines.

## Memory aid

Pregabalin: «Pre-gain» – dizzy, sleepy, puffy and gaining weight.

## Test yourself

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

## Which pain conditions are labelled indications of pregabalin?

Diabetic peripheral neuropathy, postherpetic neuralgia, neuropathic pain after spinal cord injury and fibromyalgia.

## Which antidiabetic class adds to pregabalin's oedema and weight gain?

Thiazolidinediones such as pioglitazone.

## Which serious allergic reaction is listed for pregabalin?

Angioedema, with swelling of the face, lips, tongue or throat; it can threaten the airway.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/pregabalin/)

## Related drugs

- [Gabapentin](https://durgical.com/en/pharmacology/gabapentin/)

## Related conditions

- [Herpes zoster (shingles)](https://durgical.com/en/conditions/herpes-zoster/)
- [Epilepsy and seizures](https://durgical.com/en/conditions/epilepsy-and-seizures/)

[← Back to the class: Gabapentinoids](https://durgical.com/en/pharmacology/classes/gabapentinoids/)

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

Sources: [Pregabalin: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a605045.html) (MedlinePlus (U.S. National Library of Medicine), 2020); [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); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N02BF02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/pregabalin/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/pregabalin/
