Cholinesterase inhibitors potentiation

When Hie cholinesterase inhibitors are administered with the anticholinergic drugp, there is a potential decrease in activity of the anticholinergic drug. There is an increased risk of toxicity of theophylline when the cholinesterase inhibitors are administered with tacrine There is a synergistic effect when tacrine is administered with succinyl-choline, cholinesterase inhibitors, or cholinergic agonists (eg, bethanechol). 

The courts, however, are not bound by the decision of the Patent Office to issue the patent. In considering whether the application had utility, the Federal Circuit approvingly quoted the district court s determination that the application "did not provide analysis or insight connecting the [summaries of the six references]. .. to galantamine s potential to treat Alzheimer s disease [4]." In conjunction with this analysis, witness testimony given at trial was also considered. For example, the sole inventor testified that "when I submitted this patent, I certainly wasn t sure, and a lot of other people weren t sure, that cholinesterase inhibitors [such as galantamine] would ever work [to treat Alzheimer s disease] [5]." (Emphasis added). 

Effects of Overexposure VX is a lethal cholinesterase inhibitor. Doses which are potentially life-threatening may be only slightly larger than those producing least effects. Death usually occurs within 15 minutes after absorption of a fatal dosage. 

Anger, W. K. (1981). Effects of carbaiyl on variable interval response rates in rats. Neurobehavioral Toxicology 2 21-24. Bear, D. M. (1986). Aggression in cat and human precipitated by a cholinesterase inhibitor. Psychosomatics 27 535-536. Branch, R. A. (1986). Is carbaryl as safe as its reputation Does it have a potential for causing chronic neurotoxicity in humans American Journal cf Medicine 80 659-664. 

Both [2- F] and [4- F]fluorobenzaldehydes are key intermediates in the synthesis of N-[ F]fluorobenzylamines via reductive aminations. This methodo o-gy has been successfully appHed to the preparation of a potential ace y -cholinesterase inhibitor [143] and of fluoro analogues of dexetimide, potent ligand of muscarinic cholinergic receptor [144] (Scheme 23). 

Se/zyres Cholinesterase inhibitors are believed to have some potential to cause generalized convulsions. 

Anticholinesterase agents of all classes can initiate antidromic firing of action potentials in motor neurons, possibly due to an activation of prejunctional ACh receptors that are activated by the elevated synaptic ACh. Quaternary ammonium inhibitors can also act as agonists at these receptors. The initiation of antidromic firing may be a mechanism by which cholinesterase inhibitors produce fasciculation of skeletal muscle. 

Because anticholinesterase agents also inhibit plasma pseudo-ChE, they will potentiate the effects of succinylcholine by inhibiting its breakdown. This is important, for example, when succinylcholine is to be employed in patients who have previously received cholinesterase inhibitors for the treatment of myasthenia gravis or glaucoma. 

Severe cholinergic excess is a medical emergency, especially in rural communities where cholinesterase inhibitor insecticides are commonly used and in cultures where wild mushrooms are commonly eaten. The potential use of cholinesterase inhibitors as chemical warfare "nerve gases" also requires an awareness of the methods for treating acute poisoning (see Chapter 58). 

Ferreri F, Agbokou C, Gauthier S. 2006. Cognitive dysfunctions in schizophrenia Potential benefits of cholinesterase inhibitor adjunctive therapy. J Psychiatry Neurosci 31 ... 

Alzheimer s disease) and donepezil (79). These findings support the potential for combining memantine and cholinesterase inhibitors in patients with Alzheimer s disease. 

To prevent potential clinical deterioration, generally switch from long-term treatment with one cholinesterase inhibitor to another without a washout period... 

There is some evidence that points to an association between Alzheimer s disease and a defict in hrain acetylcholine levels. Considerable attention has thus focused on cholinesterase inhibitors as potential drugs for treating the affliction. The preparation of a relatively simple inhibitor is prepared by acylation of the benzylamine (197) with chloroformamide (198). The resulting urethane is then resolved to afford rivastigmine (199). " ... 

Respiratory ailments, recent exposure to cholinesterase inhibitors, impaired cholinesterase production, or liver malfunction may potentiate the toxicity of dimethoate. Also, high environmental temperatures or exposure of dimethoate to light (visible or UV) may enhance its toxicity. 

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