why does gabapentin help my sleep so much?

[bad1080]

i been trying gabapentin for sleep and it's the only thing to truly make a difference so far. i occasionally take 300mg at 11pm, go to bed around midnight and i am able to get 7h of uninterrupted sleep instead of waking up every 1-1.5h. but i feel very drowsy in the morning (even after falling asleep again and getting up closer to 10am) to the point i have to hold on to something to not tumble. i also take 0.2mg LDN in the evening and 10 drops of THC+CBD (those two alone are not enough to make me sleep through the night).

my questions are, why is it so effective and what are the implications for other things to try (that maybe don't make me as dizzy in the morning)?

edit:
i am guessing this has to do with it:

GABA is an amino acid that is one of the most important neurotransmitters (chemical messengers) that we have in our nervous system. It is essential for maintaining the balance between nerve cell excitation and nerve cell inhibition. GABA acts like a brake in a car and slows down nerve cells that are over-excited. Because it calms the nervous system, it is called an inhibitory neurotransmitter.

from: https://www.drugs.com/drug-class/gamma-aminobutyric-acid-analogs.html

but taking GABA did not help my sleep at all, maybe it was too low of a dose (i took maybe 0.5g)? iirc i read GABA is poorly absorbed through the stomach maybe that has to do with it?

 

[katabasis]

FYI, despite the name, gabapentin does not directly affect GABA receptors like benzos, alcohol, barbiturates, etc. Its primary effect is believed to be mediated by blocking calcium channels, in particular, the α2δ subunit of those channels. This may have a downstream effect of increasing GABAergic signalling, but also has a bunch of other effects, particularly by inhibiting NMDA receptors (which form a complex with the α2δ subunit), as well as generally inhibiting excitatory synapse formation.

I also find gabapentin to have a great benefit for sleep, as well as alleviating the subjective negative effects of ME/CFS. It even has a slightly protective effect against PEM for me, perhaps just by reducing metabolic demands in the brain, and maybe also by reducing muscle tone. I've tried other, broader-spectrum calcium channel blockers like nimodipine (which is primarily used to treat hypertension and to improve brain healing after stroke), and I think there may be a benefit from that one as well, but it has way more side effects, particularly headache, and as a migraine-prone person it's a challenge to explore it more thoroughly.

As for WHY gabapentin is so effective (for sleep, and for other problems I've pointed out), I'm not entirely sure. The literature around α2δ function is pretty opaque, and there's likely a combination of many things happening. If you're looking to investigate similar options, you probably want something that 1) reduces excitation of the nervous system, 2) reduces pain perception (with which α2δ channels are intimately involved), 3) reduces muscle tone and blood pressure, or 4) reduces thrombospondin or other synaptogenic mediators.

I should also warn that gabapentin and other gabapentinoids quickly produce tolerance, and they can be very difficult to wean off of, for at least some people. My preferred usage is only a few times a week, in order to prevent them from becoming ineffective. They're not quite as pernicious as benzodiazepines, but still, tread with caution.

 

[bad1080]

@katabasis thank you very much!

gabapentin does not directly affect GABA receptors

is that why taking GABA is ineffective?

gabapentin and other gabapentinoids quickly produce tolerance

yes i found the effect is already much decreased on a second consecutive night, which is why i only use it occasionally and searching for an alternative

 

[katabasis]

is that why taking GABA is ineffective?

Well, that may have more to do with the fact that GABA does not cross the blood brain barrier. If you take GABAergic drugs that DO cross the blood brain barrier, they may help you sleep more soundly. Though often, this mode of action worsens sleep architecture, which doesn't seem to happen as much with gabapentin.

yes i found the effect is already much decreased on a second consecutive night, which is why i only use it occasionally and searching for an alternative

Personally, I rotate a bunch of different sleep-related supplements which have different mechanisms. Oleamide and skullcap both seem to help. You could also try other gabapentinoids - pregabalin is also popular, though its mechanism is very similar to gabapentin so there would probably be cross-tolerance. Baclofen is also a gabapentinoid, though it acts on GABA-B receptors and not calcium channels - it is used most often as a muscle relaxant. Trying that might be diagnostic for you though, to see if muscle tone is a factor in why gabapentin helps you.

 

[bad1080]

GABA does not cross the blood brain barrier

ah maybe that's what i was (mis-)remembering and not the absorption