Pregablin for opiate dose reduction and tolerance.

[oldirtybizza]

I'm wondering if anyone has any experience or opinions on using Pregabalin for tolerance or dose reduction of opiates?

Pregabalin modulates CNS calcium channels and reduces the release of numerous neurotransmitters, including modifying substance P activity which is known to play a part in opiate tolerance. It's effects are known to be attenuated by NDMA antagonists known to potentiate opiate. A few articles which I can't access mention it's effect on opiates in animal models.

I could put up a bunch of studies and be more detailed but I thought I'd keep it simple, anyone who has any firsthand experience or pharmacological insight would be appreciated.

 

[Hammilton]

If it's similar to gabapentin then it'll decrease absorption of most opioids and require you to increase your dose.

 

[emkee_reinvented]

During the time I was on pregabalin (great med for GAD I may mention) I noticed no difference in effects of Kratom.
But Kratom is a very atypical opioid I know, tolerance builds different and there seems to be a ceiling (for me) and I was on Mirtazepine also and manic and suffering chronic stress (think pseudo psychosis and the like)

I was never sedated enough at that time, and not real good reference material for your question.

 

[endotropic]

If it's similar to gabapentin then it'll decrease absorption of most opioids and require you to increase your dose.

I've never heard of that, any idea why that happens?

 

[oldirtybizza]

^Neither have I. here are some studies relating to Gabapentin and opiate

http://www.ncbi.nlm.nih.gov/pubmed/9313278
This study seems to show increased analgesia in rats that is blocked by naloxone, indicating the addition of gabapentin is enhancing the activity of morph on the Mu receptors

http://www.ncbi.nlm.nih.gov/pubmed/15385372
A quote from this study "We have previously shown that systemic gabapentin (GBP), a non-opioid drug, prevents and reverses tolerance to systemic morphine in the rat." . "Coinjection of GBP with morphine blocked the development of tolerance" "These data support previous evidence that GBP prevents opioid tolerance"

http://www.ucdmc.ucdavis.edu/pain/reviews/gabapentine.html
"However, this study can only suggest that the addition of gabapentin to opiate regimens in the treatment of neuropathic cancer pain increases analgesic efficacy"

http://www.ncbi.nlm.nih.gov/pubmed/22523419
"Gabapentin has been shown to be effective in reducing postoperative narcotic usage, a reduction that may be associated with a reduction in opioid-induced tolerance and hyperalgesia."

 

[MartinFn]

I just can say for sure ,that pregabalin is a very nice potentiator of opiates..


MartinFn

 

[ebola?]

It's pretty likely that blocking calcium channels reduces the efficacy of transmission of pain signals (as it reduces the efficacy of other neural signals).

ebola

 

[SeenSoFar]

I wonder if the fact that Gabapentin/pregabalin prevents the growth of synapses has anything to do with its ability to prevent the development of opioid tolerance.

According to the following study, gabapentin prevents excitatory synaptogenesis:

Gabapentin receptor alpha2delta-1 is a neuronal thrombospondin receptor responsible for excitatory CNS synaptogenesis.
http://www.ncbi.nlm.nih.gov/m/pubmed/19818485/

Synapses are asymmetric cellular adhesions that are critical for nervous system development and function, but the mechanisms that induce their formation are not well understood. We have previously identified thrombospondin as an astrocyte-secreted protein that promotes central nervous system (CNS) synaptogenesis. Here, we identify the neuronal thrombospondin receptor involved in CNS synapse formation as alpha2delta-1, the receptor for the anti-epileptic and analgesic drug gabapentin. We show that the VWF-A domain of alpha2delta-1 interacts with the epidermal growth factor-like repeats common to all thrombospondins. alpha2delta-1 overexpression increases synaptogenesis in vitro and in vivo and is required postsynaptically for thrombospondin- and astrocyte-induced synapse formation in vitro. Gabapentin antagonizes thrombospondin binding to alpha2delta-1 and powerfully inhibits excitatory synapse formation in vitro and in vivo. These findings identify alpha2delta-1 as a receptor involved in excitatory synapse formation and suggest that gabapentin may function therapeutically by blocking new synapse formation.

Any thoughts?

 

[Professer]

I'm wondering if anyone has any experience or opinions on using Pregabalin for tolerance or dose reduction of opiates?

I do.

I was taking 10 mg methadone daily as a self-maintenance thing. I started taking prescribed pregabalin a few days ago and noticed I didn't feel the need to take my daily morning dose. The worst WD symptom I had was a runny nose at first. Maybe some slight physical discomfort but I already had that from chronic RLS and muscle pains/spasms. The pregabalin covered it up well. I was taking a bit more than prescribed (225mg) at first.

That's about all I have to offer here. Nothing on the scientific side, just my subjective experience.