Hydrastine hydrochloride

Dose. Hydrastine hydrochloride was formerly given in doses of 15 to 60 mg. 

Hydrastis extracts and hydrastine hydrochloride have been used for stopping uterine hemorrhage and in relieving menstrual pain. Current use is mainly as components in eyewashes and in certain bitter tonic preparations. 

Hydrastine hydrochloride, C2iH2i06N,HC1, Mol. Wt. 419-9, was official in the B.P.C. 1949. The base is obtained by the usual chloroform extraction in ammoniacal solution, washing, evaporating in the presence of ethanol and drying at 100 x... 

Bicuculline, C2oHi,06N. (Items 1, 9, 10, 13, 14, 18, 20, 23-26, 34, 35, 38 list, p. 169). This alkaloid exists in two forms, m.p. 177° and m.p. 196°, and has [a], ° + 130- 5° (CHCI3). The hydrochloride has m.p. 259° (dec.) and from the methiodide, W-methylbicuculline, plates, m.p. 246°, has been prepared. Bicuculline contains no methoxyl groups it behaves as a lactone and is convertible by alkalis into bicucine, which is possibly the corresponding hydroxy-aeid (see below). It simulates hydrastine in its reactions and differs from that base by CH, indicating that a methylene-dioxy group replaces two methoxyl groups, and this view is supported by comparison of the products of oxidative hydrolysis of the two alkaloids. Both yield hydrastinine (p. 163) as the basic product, but while hydrastine provides as the second product, opianic acid,... 

Hydrastine has been employed (627) in the form of a hydrochloride for uterine and other hemorrhagias in doses of 25 mg 4—5 times daily. Higher doses produce an increase in blood pressure. 

Because of the small number of cularine alkaloids, whose existence was known until very recently, there are very few published studies about their physiological effects. However, studies of the pharmacological activity of (+)-cularine hydrochloride and some comparison with other isoquinoline alkaloids such as papaverine and hydrastine have been reported (76). Dilute solutions of (-t-)-cularine produced marked anesthesia of the rabbit cornea. The effects on smooth muscle included stimulation of the uterus and depression of intestinal motility. Heart tone and contractility were also increased. When injected intravenously into rabbits, (+)-cularine 11 produced a drop in blood pressure which was followed by recovery to the normal level. 

The methylenedioxy group in (—)-j8-hydrastine (23) can be selectively converted to an o-diphenol by treatment with boron trichloride, whereas (9-demethylation without affecting the methylenedioxy function can be accomplished with pyridine hydrochloride in hot pyridine. Boron tribromide cleaves both methylenedioxy and methoxyl groups. Isomerization at C-9 is known to... 

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