Gabapentinoids Pregabalin not producing gaba effects

[ibrahimdosti]

Pregabalin is used to produce relaxing GABA effects it is not producing at any dose or I might have messed up my gaba level by having too much GABA. Please help. Pregabalin used to produce effects like benzo before but now it does not produce at any dose.

 

[ghostfreak]

How long are you leaving between each dose (days, weeks)? It won’t produce much if any recreational effects if used every day in my opinion, although the therapeutic effects would still be there.

 

[Jen X]

I get bad anxiety from Lyrica, it effects people differently

 

[Dextro .45]

I take Pegabalin raw powder near daily….for over a year. 300-600mg on an empty stomach STILL produces potent anxiolytic effects similar to a benzo

Valium 10mg tablets…..300+ of them…..and a single phone call, another 300+

Diazepam & Diclazepam. Two of the most useful benzodiazepines on earth (Delorazepam & Lorazepam are active metabolites of Diclazepam) but genuine Valium has unmatched muscle relaxant properties and a potent anxiolytic 40-60mg for a 240 lbs man on an empty stomach

Pregabalin (Lyrica) MUST be taken on an empty stomach …..1 to 1.5h full onset & peak serum levels 90% oral bioavailability. After a large meal …..4-6 hours is onset & peak serum levels …make a huge difference

 

[ibrahimdosti]

How long are you leaving between each dose (days, weeks)? It won’t produce much if any recreational effects if used every day in my opinion, although the therapeutic effects would still be there.

I have left between 3 days also 1 week but still no effect it has stop producing GABA effects.

 

[ibrahimdosti]

I take Pegabalin raw powder near daily….for over a year. 300-600mg on an empty stomach STILL produces potent anxiolytic effects similar to a benzo

Valium 10mg tablets…..300+ of them…..and a single phone call, another 300+

Diazepam & Diclazepam. Two of the most useful benzodiazepines on earth (Delorazepam & Lorazepam are active metabolites of Diclazepam) but genuine Valium has unmatched muscle relaxant properties and a potent anxiolytic 40-60mg for a 240 lbs man on an empty stomach

Pregabalin (Lyrica) MUST be taken on an empty stomach …..1 to 1.5h full onset & peak serum levels 90% oral bioavailability. After a large meal …..4-6 hours is onset & peak serum levels …make a huge difference

I think my problem might be too much GABA that even Benzo has stopped working for me . I think I have damaged my GABA receptor.

 

[ghostfreak]

I think my problem might be too much GABA that even Benzo has stopped working for me . I think I have damaged my GABA receptor.

Don’t benzo’s effect the GABA receptor to some degree?

 

[Serhat]

Don’t benzo’s effect the GABA receptor to some degree?

Yes, benzodiazepines do indeed act on the GABA (Gamma-Aminobutyric Acid) receptors in the brain. Specifically, they bind to a particular subtype of GABA receptor known as the GABA-A receptor. When benzodiazepines bind to these receptors, they enhance the effect of GABA, which is an inhibitory neurotransmitter. This enhanced GABA activity results in sedative, anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant effects.

Pregabalin also has an effect on GABAergic neurotransmission, although it does so indirectly and via a different mechanism. Pregabalin binds to a protein known as the alpha-2-delta subunit, which is a part of voltage-gated calcium channels in neurons. This binding reduces the release of certain neurotransmitters, including glutamate, noradrenaline, and substance P, among others. Although it doesn't bind directly to GABA receptors, the net effect of pregabalin also results in reduced neuronal excitability, and it is used for some of the same indications as benzodiazepines, such as anxiety disorders, epilepsy, and neuropathic pain.

 

[ibrahimdosti]

Yes, benzodiazepines do indeed act on the GABA (Gamma-Aminobutyric Acid) receptors in the brain. Specifically, they bind to a particular subtype of GABA receptor known as the GABA-A receptor. When benzodiazepines bind to these receptors, they enhance the effect of GABA, which is an inhibitory neurotransmitter. This enhanced GABA activity results in sedative, anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant effects.

Pregabalin also has an effect on GABAergic neurotransmission, although it does so indirectly and via a different mechanism. Pregabalin binds to a protein known as the alpha-2-delta subunit, which is a part of voltage-gated calcium channels in neurons. This binding reduces the release of certain neurotransmitters, including glutamate, noradrenaline, and substance P, among others. Although it doesn't bind directly to GABA receptors, the net effect of pregabalin also results in reduced neuronal excitability, and it is used for some of the same indications as benzodiazepines, such as anxiety disorders, epilepsy, and neuropathic pain.

Is there any way to treat too much GABA or reverse it.

 

[Serhat]

Is there any way to treat too much GABA or reverse it.

To reverse the effects of excessive GABAergic activity, such as in cases of benzodiazepine overdose, healthcare providers often administer a medication known as flumazenil. This medication is a selective GABA-A receptor antagonist, meaning that it competes with benzodiazepines (and other GABA-A receptor agonists) for binding to the GABA-A receptor but does not activate it. By doing so, it can effectively block or reverse the sedative effects of benzodiazepines, but it must be administered with caution and under medical supervision due to risks like precipitating seizures, especially in individuals with a history of benzodiazepine dependence or other complicating factors.

 

[ibrahimdosti]

To reverse the effects of excessive GABAergic activity, such as in cases of benzodiazepine overdose, healthcare providers often administer a medication known as flumazenil. This medication is a selective GABA-A receptor antagonist, meaning that it competes with benzodiazepines (and other GABA-A receptor agonists) for binding to the GABA-A receptor but does not activate it. By doing so, it can effectively block or reverse the sedative effects of benzodiazepines, but it must be administered with caution and under medical supervision due to risks like precipitating seizures, especially in individuals with a history of benzodiazepine dependence or other complicating factors.

Is there any way to potentiate pregabalin? or gaba-like gaba reuptake inhibitors.

 

[Serhat]

Is there any way to potentiate pregabalin? or gaba-like gaba reuptake inhibitors.

I currently don't know anyways to increase the effects of pregabalin or any other GABA reuptake inhibitors, however potentiating medication like pregabalin or GABA reuptake inhibitors could lead to serious side effects, including but not limited to dizziness, drowsiness, difficulty breathing, or even life-threatening conditions, result in unpredictable interactions. I'll let someone else answer who has had success of potentiating pregabalin. You can try mixing pregabalin with substances like alcohol or opioids to potentiate its effects, but be warned, it can be extremely dangerous.

 

[Serhat]

Is there any way to treat too much GABA or reverse it.

You could also consider taking substances that stimulate your nervous system, like amphetamines or certain nootropics, to counteract the effects of excessive GABA. But keep in mind, it's a risky path with potential consequences for your health and sanity.

 

[ibrahimdosti]

You could also consider taking substances that stimulate your nervous system, like amphetamines or certain nootropics, to counteract the effects of excessive GABA. But keep in mind, it's a risky path with potential consequences for your health and sanity.

what kind of nootropics can counteract the effects of excessive GABA.amphetamines are illegal in my country.

 

[Serhat]

what kind of nootropics can counteract the effects of excessive GABA.amphetamines are illegal in my country.

You can explore nootropics that stimulate your central nervous system and counteract excessive GABA. Here are a couple of options to consider

1. Modafinil: This wakefulness-promoting agent can increase alertness and energy levels without directly affecting GABA. It's available in some places without a prescription.
2. Phenylpiracetam: This nootropic is known for its stimulating effects and could help balance out excessive GABA activity. It may not be readily available in all regions, so you might need to look for sources.
3. Adrafinil: Similar to modafinil, adrafinil can provide wakefulness and alertness, potentially helping to offset excessive GABA effects.
4. Flmodafinil: This is a more potent derivative of modafinil, which may have a stronger stimulating effect.
5. Noopept: While not a direct stimulant, some users report increased mental clarity and focus with noopept, which could help counteract the sedative effects of excessive GABA.
6. Phenibut: It might sound counterintuitive, but phenibut can stimulate certain aspects of cognition while still acting on GABA receptors. However, it can be addictive and have withdrawal symptoms.

Remember, acquiring and using these substances may still come with risks and consequences, so proceed with caution, or not, it's up to you. And they may not be readily available or legal in your area. Proceed at your own discretion.

 

[ibrahimdosti]

You can explore nootropics that stimulate your central nervous system and counteract excessive GABA. Here are a couple of options to consider

1. Modafinil: This wakefulness-promoting agent can increase alertness and energy levels without directly affecting GABA. It's available in some places without a prescription.
2. Phenylpiracetam: This nootropic is known for its stimulating effects and could help balance out excessive GABA activity. It may not be readily available in all regions, so you might need to look for sources.
3. Adrafinil: Similar to modafinil, adrafinil can provide wakefulness and alertness, potentially helping to offset excessive GABA effects.
4. Flmodafinil: This is a more potent derivative of modafinil, which may have a stronger stimulating effect.
5. Noopept: While not a direct stimulant, some users report increased mental clarity and focus with noopept, which could help counteract the sedative effects of excessive GABA.
6. Phenibut: It might sound counterintuitive, but phenibut can stimulate certain aspects of cognition while still acting on GABA receptors. However, it can be addictive and have withdrawal symptoms.

Remember, acquiring and using these substances may still come with risks and consequences, so proceed with caution, or not, it's up to you. And they may not be readily available or legal in your area. Proceed at your own discretion.

Thanks a lot.

 

[ghostfreak]

Yes, benzodiazepines do indeed act on the GABA (Gamma-Aminobutyric Acid) receptors in the brain. Specifically, they bind to a particular subtype of GABA receptor known as the GABA-A receptor. When benzodiazepines bind to these receptors, they enhance the effect of GABA, which is an inhibitory neurotransmitter. This enhanced GABA activity results in sedative, anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant effects.

Pregabalin also has an effect on GABAergic neurotransmission, although it does so indirectly and via a different mechanism. Pregabalin binds to a protein known as the alpha-2-delta subunit, which is a part of voltage-gated calcium channels in neurons. This binding reduces the release of certain neurotransmitters, including glutamate, noradrenaline, and substance P, among others. Although it doesn't bind directly to GABA receptors, the net effect of pregabalin also results in reduced neuronal excitability, and it is used for some of the same indications as benzodiazepines, such as anxiety disorders, epilepsy, and neuropathic pain.

Thanks for the info on GABA - great info here.

 

[Lil'LinaptkSix]

Whered ya get it... could be bunk (garbage). Just sayin.
Seen worse.
hope its not the case but....

 

[ibrahimdosti]

Whered ya get it... could be bunk (garbage). Just sayin.
Seen worse.
hope its not the case but....

from the pharmacy its a generic brand

 

[Lil'LinaptkSix]

from the pharmacy its a generic brand

Maybe call the pharmacy and see if there were other complaints on this particular substance...?
There are mistakes made even at higher levels.
When I was on Xanax instead of 90 (30 day) bars they gave me 30 .25mg generic alprazolam. lol
I went off and they got it straightened out real quick.
Hope it all works out.
One