Misc Why are cyclizine and cyproheptadine virtually unobtainable domestically? (US)

[purplehaze147]

I want them in my medicine cabinet. They look like very useful medicines, but every site says I need a prescription, but they're regulated as OTC. Cyclizine has such a history behind it I just really want to try it, but cyproheptadine looks genuinely useful.

Cyproheptadine has one of the strongest Ki's for the H1 receptor at 0.06nM in humans. It's anticholinergic effects are about the ratio of doxylamine (42nM at H1 490nM at M1; 0.06nM H1 and 12 at M1... Ratios are better at other muscarine sites). It also is a powerful 5HT2 (A,B, and C) antagonist in the 1.5-2.0 nM range. And (probably negative) 8nM at D3. The half-life is on the low end, about the same as diphenhydramine.

 

[JTemperance]

I want them in my medicine cabinet. They look like very useful medicines, but every site says I need a prescription, but they're regulated as OTC. Cyclizine has such a history behind it I just really want to try it, but cyproheptadine looks genuinely useful.

Cyproheptadine has one of the strongest Ki's for the H1 receptor at 0.06nM in humans. It's anticholinergic effects are about the ratio of doxylamine (42nM at H1 490nM at M1; 0.06nM H1 and 12 at M1... Ratios are better at other muscarine sites). It also is a powerful 5HT2 (A,B, and C) antagonist in the 1.5-2.0 nM range. And (probably negative) 8nM at D3. The half-life is on the low end, about the same as diphenhydramine.

I've had an interest in cyproheptadine for a while, it might be time to make some more efforts toward actually getting some. Cyclizine is legendary but the tablets (= hydrochloride) aren't injectable, at least not in any way I'd want to risk, so I'd want to hold out for the ampoules (= lactate) since I get the feeling the PO effects aren't that amazing.