Are there any GABA receptors/subunits that etizolam does downregulate?
From wikipedia:
Etizolam acts as a full agonist at the benzodiazepine receptor to produce its range of therapeutic and adverse effects.[16]
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In addition, etizolam, unlike most benzodiazepines (some of which can increase levels of estradiol), has prolactogenic effects, leading to an increase in blood levels of prolactin.[18]
Full agonist at the benzodiazepine receptor! This doesn't sound very sustainable or desirable due to receptor down regulation...
Also, increasing prolactin will likely lower dopamine levels (perhaps somewhat counteracted by benzo properties) so that's something to be weary of.
Etizolam does NOT seem like a good idea IMO...
wikipedia says it does not downregulate a1 (benzo) receptors:
Abrupt or rapid withdrawal from etizolam, as with benzodiazepines, may result in the appearance of the benzodiazepine withdrawal syndrome, including rebound insomnia.[9]Neuroleptic malignant syndrome, a rare event in benzodiazepine withdrawal, has been documented in a case of abrupt withdrawal from etizolam.[10]
In a study that compared the effectiveness of etizolam, alprazolam, and bromazepam for the treatment of generalized anxiety disorder, all three drugs retained their effectiveness over 2 weeks, but etizolam became more effective from 2 weeks to 4 weeks, a type of reverse tolerance.[11] Administering .5 mg etizolam twice daily did not induce cognitive deficits over 3 weeks when compared to placebo.[12]
When multiple doses of etizolam, or lorazepam, were administered to rat neurons, lorazepam caused downregulation of alpha-1 benzodiazepine binding sites (tolerance/dependence), while etizolam caused an increase in alpha-2 benzodiazepine binding sites (reverse tolerance to anti-anxiety effects).[13] Tolerance to the anticonvulsant effects of lorazepam was observed, but no significant tolerance to the anticonvulsant effects of etizolam was observed.[13] Etizolam therefore has a reduced liability to induce tolerance, and dependence, compared with classic benzodiazepines.[13]
