Pregabalin !
A relative of gabapentin for nerve pain, fibromyalgia and focal seizures. It causes dizziness, sleepiness, swelling and weight gain.
Updated 2026-11-01
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.
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) →
- Fibromyalgia
- Add-on treatment of focal seizures Epilepsy and seizures →
Adverse effects
Common
- Dizziness and sleepiness
- Dry mouth and blurred vision
- Peripheral oedema
- Weight gain
- Difficulty concentrating
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- Withdrawn gradually: stopping suddenly can cause insomnia, nausea, headache and anxiety, and more seizures in epilepsy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.
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.
Related drugs
Related conditions
← Back to the class: 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 (MedlinePlus (U.S. National Library of Medicine), 2020); DailyMed - PREGABALIN capsule (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.