N&PD Moderators: Skorpio
vigabatrin and benzos and barbs
Slay
Ex-Bluelighter
well, i was reading the "oral gaba" thread a few mins ago and did i search and find something called "vigabatrin" an OTC gaba analog anticonvulsant. i learned that it also inhibits the catabolism of GABA. so i wonder does taking vigabatrin with any benzo or barb or carbamate make any difference or not?
jasoncrest
Bluelighter
elektra said:
One doctor once explained to me that Tiagabine was to GABA what a SRRI was to antidepressants; and that Vigabatrin was to GABA what a MAOI was to antidepressants....
So it raises GABA levels by inhibiting some enzyme or something.
I'm pretty sure it is similar to Tiagabine in many ways, if it's the case, it will STRONGLY potentiate benzos or barbs.
It i surely a good anti-anxiety medication too (like Tiagabine, Pregabalin)
Slay
Ex-Bluelighter
jasoncrest said:
some sources says it causes psychosis and i have cannabis psychosis you think is it a bad idea to potentiate downers with this shit?
Reminisant B
Greenlighter
Wiki
It's no walk in the park with side effects though. Mixing with barbiturates sounds like a recipe for disaster.
Reminisant B
Greenlighter
BNF
Slay
Ex-Bluelighter
fuck me too i already have vision problems
GABAlover
Bluelighter
Guys, you're getting too far ahead here.
"Pharmacodynamics. The mechanism of action is attributed to dose dependent enzyme inhibition of gamma-aminobutyric acid transaminase (GABA-T) and consequent increased levels of the inhibitory neurotransmitter, gamma-aminobutyric acid (GABA). In mice, decreased GABA-T levels in the brain persisted for five days following a single intraperitoneal dose (1,500 mg/kg) and were accompanied by a marked rise in brain GABA concentration.
Animal safety studies carried out in rat, mouse, dog and monkey have indicated that vigabatrin has no significant adverse effects on the liver, kidney, lung, heart or gastrointestinal tract. In the brain, microvacuolation has been observed in white matter tracts of rat, mouse and dog at doses of 30 to 50 mg/kg/day. This effect is caused by a separation of the outer lamellar sheath of myelinated fibres, a change characteristic of intramyelinic oedema.
In both rat and dog (mouse was not tested), the intramyelinic oedema was reversible on stopping vigabatrin treatment. However, in rodents, residual changes consisting of swollen axons and mineralised microbodies have been observed. In the monkey, no lesions were noted after six years of treatment at 50 and 100 mg/kg. In monkeys receiving 300 mg/kg for 16 months, minimal microvacuolation was noted with equivocal differences between treated and control animals. In the dog, results of an electrophysiological study indicate that intramyelinic oedema is associated with increased latency of the somatosensory evoked potential which is reversible when the drug is withdrawn.
Short-term and long-term controlled clinical trials have shown that vigabatrin reduces seizure frequency when given as add-on therapy in patients with epilepsy not controlled satisfactorily by conventional therapy. Efficacy is particularly marked in patients with complex partial seizures.
During long-term clinical follow-up, tests done to confirm lack of significant adverse effects on neurological function include evoked potential studies, magnetic resonance imaging and, in a small number of cases, neuropathological examinations of human brain specimens. Therefore, clinical trials have revealed no evidence in humans of the type of neurotoxicity seen in animal studies. In humans, no tendency towards increased evoked potential latency was observed even on prolonged treatment.
Pharmacokinetics. Vigabatrin is a water soluble compound and is rapidly absorbed from the gastrointestinal tract; absorption is unaffected by the presence of food. The drug is widely distributed with an apparent volume of distribution slightly greater than total body water. Plasma and CSF concentrations are linearly related to dose over the recommended dose range.
There is no direct correlation between plasma concentration and efficacy. Duration of drug effect is thought to be dependent on the rate of enzyme resynthesis rather than the plasma concentration of the drug.
Vigabatrin is eliminated from the plasma with a terminal half-life of five to eight hours with approximately 70% of a single oral dose being recovered in the urine as unchanged drug in the first 24 hours postdose.
Vigabatrin does not induce the hepatic cytochrome P450 enzymes nor is it extensively metabolised or plasma protein bound, therefore drug interactions are unlikely.
Courtesy of MIMS online
Slay
Ex-Bluelighter
^^ the point is theres no point imo after reading all above posters side effects and other sources
hussness
Bluelighter
Is this a reversible or irreversible inhibitor?
Limpet_Chicken
Bluelighter
I wouldn't try either compound with any barb, benzos, possibly, but caerfully of course, barbiturates, unlike benzos, are direct agonists at teh GABAa receptor, so do not need GABA to be present at the receptor to function, thus the overdose risk is far higher, even without potentiation, and also, tolerance develops, but the LD:50 does not increase with it.
Would a reuptake inhibitor actually WORK at all, with a direct agonist, to enhance effectiveness? seeing as direct agonists don't require the presence of GABA to activate the GABAa receptor, does the prescence/lack thereof of GABA alter the activity of barbiturates?
Not, that I would want to try a reuptake inhibitor with a barb even if it did not cause potentiation.
Slay
Ex-Bluelighter
i told about this combo to a friend of mine and she interested very much and tried it. she said the experience is "weird" and unpleasant, specially side effects (like extreme diplopia, extreme blured vision, extreme ataxia, hard to swalllow things (like when your rolling balls), very intense headache after sober up etc). i told her to rite a trip report for TR forum anonymously but she doesnt know english well and aint a bluelighter. i'll learn the details and write a report soon.
Reminisant B
Greenlighter
There is good reason why vigabatrin is not used routinely anymore.
Even as an "exotic" type of downer it seems a stupid choice to play around with and probably very unfun.
