Physostigmine for

Powers JS, Decoskey D, Kahrillas PJ Physostigmine for the treatment of delirium tremens. J Clin Pharmacol 21 57-60, 1981... 

Coelho Filho, J.M. Birks, J. Cochrane Collaboration Physostigmine for Alzheimer s Disease. In The Cochrane Library, Issue 3 2002, Oxford Update Software. 

Coehlo, F. and Birks, J. Physostigmine for Alzheimer s disease, Cochrane Database Syst. Rev., 2, CD001499,... 

F. Use in pregnancy. FDA category C (see p 405). Transient weakness has been noted in neonates whose mothers were treated with physostigmine for myasthenia gravis. 

Johnson has described a method for the estimation of physostigmine in the salicylate for the determination of minute amounts of the alkaloid Ellis, Plaehte and Straus have devised processes depending on (a) inhibition of serum choline-esterase by the alkaloid, or (b) measurement of the colour intensity produced by the conversion of physostigmine to rubreserine in an alkaline medium. i ... 

The miotic effect induced by physostigmine lends itself to investigation of the interrelation of chemical constitution and pharmacological action, and Stedman has devoted much attention to this subject. Eseroline is devoid of miotic activity, so that the latter action in physostigmine must be mainly due to the fact that it is a methylurethane, and, since activity only becomes evident in the urethanes of phenolic bases or phenols with a basic side-chain, a basic nucleus for the urethanes appears also to be essential. 

Pilocarpine is being less used in medicine as a diaphoretic in dropsy and similar diseases because of its depressant action on the heart. It has also been employed as a substitute for physostigmine to contract the pupil and reduce intraocular pressure. It has been used as an antidote to atropine, but it does not antagonise the action of atropine in the central nervous system. 

The relative inaccessibility of physostigmine led to molecular dissection studies to define the parts of the molecule necessary for activity. A surprisingly simple derivative of m-hydroxy-aniline, neostigmine (40), proved to have the same activity as the complex heterocyclic molecule. In addition, this drug has found use as a cholinsterase inhibitor in pathologic conditions such as myasthenia gravis, marked by insufficient muscle tone. Reaction of m-dimethylaminophenol (37) witn pnosgene affords tne... 

The chemical and biological properties of carbamate insecticides (CBs) are described in some detail in the texts of Kuhr and Borough (1976) and Ballantyne and Marrs (1992). An early model for their development was physostigmine, a natural product found in Calabar beans. Many CBs came into use during the 1960s, sometimes as substitutes for banned OC insecticides. 

Released ACh is broken down by membrane-bound acetylcholinesterase, often called the true or specific cholinesterase to distinguish it from butyrylcholinesterase, a pseudo-or non-specific plasma cholinesterase. It is an extremely efficient enzyme with one molecule capable of dealing with something like 10000 molecules of ACh each second, which means a short life and rapid turnover (100 ps) for each molecule of ACh. It seems that about 50% of the choline freed by the hydrolysis of ACh is taken back into the nerve. There is a wide range of anticholinesterases which can be used to prolong and potentiate the action of ACh. Some of these, such as physostigmine, which can cross the blood-brain barrier to produce central effects and neostigmine, which does not readily... 

---