Beitrag von Guitar » 25. Mai 2020, 20:00
[quote="Banjo"]1. Wirkt Phenibut ähnlich bei Alkoholsucht, wie Baclofen? Frage nur, weil ersteres leichter zu erhalten ist.
[/quote]
Phenibut ist tatsächlich in Russland und einigen osteuropäischen Ländern für den Alkoholenzug zugelassen.
[quote=Wikipedia"]Phenibut is used in Russia, Ukraine, Belarus and Latvia as a pharmaceutical drug to treat anxiety and to improve sleep (e.g., in the treatment of insomnia).[5][4] It is also used for various other indications, including the treatment of asthenia, depression, alcoholism, alcohol withdrawal syndrome, post-traumatic stress disorder, stuttering, tics, vestibular disorders, Ménière's disease, dizziness, for the prevention of motion sickness, and for the prevention of anxiety before or after surgical procedures or painful diagnostic tests.[4][5][/quote]
[url=https://en.wikipedia.org/wiki/Phenibut]Quelle[/url]
Aber:
Phenibut acts as a full agonist of the GABAB receptor, similarly to baclofen.[12][13] It has between 30- to 68-fold lower affinity for the GABAB receptor than baclofen, and, in accordance, is used at far higher doses in comparison.[12] (R)-Phenibut has more than 100-fold higher affinity for the GABAB receptor than does (S)-phenibut; hence, (R)-phenibut is the active enantiomer at the GABAB receptor.[14] At very high concentrations, phenibut reportedly also acts as an agonist of the GABAA receptor, which is the receptor responsible for the actions of the benzodiazepines, barbiturates, and alcohol.[15]
Phenibut also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.[8][16] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively).[8] Moreover, (R)-phenibut possesses 4-fold greater affinity for this site than for the GABAB receptor (Ki = 92 μM), while (S)-phenibut does not bind significantly to the GABAB receptor (Ki > 1 mM).[8] As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α2δ subunit-containing VDCCs than with the GABAB receptor (between 5- to 10-fold).[8] For this reason, the actions of phenibut as a α2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid; Ki = 6 μM for the GABAB receptor and Ki = 156 μM for α2δ subunit-containing VDCCs, or a 26-fold difference in affinity).[8][9]
Hier kann sich also, gerade in hohen Dosen, eine Toleranzentwicklung ergeben.