Gabapentin, the GABA analogue sleeping aid

Gabapentin (also known as Neurontin®) is an analogue of the neurotransmitter GABA; it was originally designed to help with epilepsy and neuropathic pain and has been shown to have efficacy for migraines and even hot flashes; but more recently it has now been shown to be effective as a sleeping drug.

Pain management

Apart from neuropathic pain / migraines, Gabapentin has shown to be effective in reducing the pain levels for about one third of fibromyalgia sufferers, a condition whereby constant pain day and night can be a very debilitating feature of the disease.

In addition, Gabapentin has shown to also benefit pain management conditions for multiple sclerosis.

Side effects

The most common side effects of Gabapentin at ‘regular’ doses are drowsiness and fatigue, (perhaps not surprising when it helps to induce restful sleep). Other side effects, which tend to be dose related, are dizziness and nausea.

Note that Gabapentin should not be discontinued abruptly after long term use. Abrupt withdrawal may provoke withdrawal syndromes, therefore gradual reduction over a period of weeks is recommended if Gabapentin has been in constant regular use.

Contraindications

Antacids reduce the uptake of Gabapentin and therefore should not be taken concurrently.

Gabapentin must not be combined with CNS depressants, nor should Gabapentin be used by children, pregnant or lactating women or those suffering with renal or liver impairment.

Naturally, given the nature of its sleep inducing effects Gabapentin should only be taken when it is safe to do so - when one is ready for bed etc. It should not be combined with alcohol nor taken before driving or operating machinery etc.

Doses

Whilst doses for epilepsy and pain management can vary widely on the condition and need, the typical doses to assist ‘somnolence’ (aiding restful sleep) are 600mg to 900mg an hour before bedtime.

Frequently Asked Questions About Gabapentin

Dear Dr. Dean,

My wife suffers badly from restless legs syndrome? Do you have any suggestions for this exasperating, debilitating condition?

BMC, USA

Dear Sir,

Have her try Gabapentin, before bedtime. Gabapentin is a very effective nerve-stabilizer, and should give her a lot of relief.  It is well-tested to alleviate restless legs.1-3 

The key is the dosage.  This can usually range from 300-1200 mg.  Start with a low dose, and gradually titrate the dose to that which gives her relief, but does not leave her “hung over” in the morning.  Gabapentin is a great sleep-promoter, which actually enhances slow-wave sleep.4  

References:

  1. Happe S, Klösch G, Saletu B, Zeitlhofer J. Treatment of idiopathic restless legs syndrome (RLS) with gabapentin. Neurology. 2001 Nov 13;57(9):1717-9.
  2. Garcia-Borreguero D, Larrosa O, de la Llave Y, Verger K, Masramon X, Hernandez G. Treatment of restless legs syndrome with gabapentin: a double-blind, cross-over study. Neurology. 2002 Nov 26;59(10):1573-9.
  3. Adler CH. Treatment of restless legs syndrome with gabapentin. Clin Neuropharmacol. 1997 Apr;20(2):148-51.
  4. Lo HS, Yang CM, Lo HG, Lee CY, Ting H, Tzang BS. Treatment effects of gabapentin for primary insomnia. Clin Neuropharmacol. 2010 Mar-Apr;33(2):84-90.

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