D-Pilocarpine

The construction of d-pilocarpine was effected by converting d-Aomopilopoyl chloride (VI COjH COCl) into diazomethyl drhomo-pilopyl ketone (VIII), transformation of the latter by the action of hydro-... 

Answer D. Pilocarpine is present in severed mushroom species including Amanita mus-caria, the ingestion of which is associated with the stimulation of M receptors (parasympathomimetic effects). The activation by pilocarpine of M receptors present on vascular endothelial cells would lead to hypotension (not hypertension) via the release of NO (EDKF). All of the other effects listed are typical of excessive stimulation of M receptors. 

Fig. 4. DSC curves of inserts prepared with poly(vinyl alcohol) PVA-C. Key a) polymer film b) pilocarpine nitrate c) polymer insert containing pilocarpine nitrate d) pilocarpine PAA-salt e,f) polymer insert containing pilocarpine PAA-salt heating and cooling, respectively.

Cushny has compared the action of d- and Z-hyoscyamines with that of atropine, and of d-homatropine with that of dZ-homatropine in antagonising the action of pilocarpine, and finds that the order of activity of the first three is in the ratio 1 40 20, and of the second two in the ratio 4 2-5. He drew attention also to the important influence of the acyl radical in the tropeines, which exercises the maximum effect when it is a hydroxyalkyl aromatic residue and is laevorotatory and in illustration of this point gives the following table of relative activities on the basis of capacity to antagnonise pilocarpine in the salivary fistula dog —... 

The same author found Z-hyoscine sixteen to eighteen times as active as the d-isomeride in antagonising the action of pilocarpine on the termination of nerves in the salivary glands, -while both isomerides are equally active on nerve ends in striated and unstriated muscle and on the central nervous system. 

MF Saettone, D Monti, MT Torracca, P Chetoni, B Giannaccini. (1989). Muco-adhesive liquid ophthalmic vehicles—Evaluation of macromolecular ionic complexes of pilocarpine. Drug Dev Ind Pharm 15 2475-2489. 

Jope RS, Jenden DJ, Ehrlich BE, et al Choline accumulates in erythrocytes during lithium therapy. N Engl J Med 299 833-834, 1978 Jope RS, Jenden DJ, Ehrlich BE, et al Erythrocyte choline concentrations are elevated in manic patients. Proc Natl Acad Sci USA 77 6144-6146, 1980 Jope RS, Morrisett RA, Snead OC Characterization of lithium potentiation of pilocarpine induced status epilepticus in rats. Exp Neurol 91 471-480, 1986 Jordan D, Spyer KM Brainstem integration of cardiovascular and pulmonary afferent activity. Prog Brain Res 67 295-314, 1986... 

Berkowitz, A., Sutton, L., Janowsky, D.S., Gillin, J.C. Pilocarpine, an orally active muscarinic cholinergic agonist, induces REM sleep and reduces delta sleep in normal volunteers. Psychiatry Res. 33. 112—119. 1990. 

Desai, S.D., and J. Blanchard. 2000. Pluronic F127-based ocular delivery system containing biodegradable polyisobutylcyanoacrylate nanocapsules of pilocarpine. Drug Deliv 7 201. 

K. D. Sternitzki, T. Y. Fan, and D. L. Dunn, High-performance liquid chromatographic determination of pilocarpine hydrochloride and its degradation products using a /3-cyclodextrin column, J. Chromatogr., 589 159 (1992). 

Desai, S. D., and Blanchard, J. (1998), Evaluation of pluronic F127-based sustained-release ocular delivery systems for pilocarpine using the albino rabbit eye model, /. Pharm. Sci., 87(10), 1190-1195. 

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