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Topic: Cholinesterase inhibitor

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	Cholinesterase inhibitor - Wikipedia, the free encyclopedia
		A cholinesterase inhibitor or anticholinesterase is a chemical that inhibits a cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine.
		Anticholinesterases occur naturally as venoms and poisons, are used as weapons in the form of nerve agents, and are used medicinally to treat diseases such as myasthenia gravis and Alzheimer's disease, and as an antidote to anticholinergic poisoning.
		Compounds which function as quasi-irreversible inhibitors of cholinesterase are those most likely to have use as chemical weapons or pesticides.
	en.wikipedia.org /wiki/Anticholinesterase (177 words)

	Hospital Practice: Cholinesterase Inhibitors for Alzheimer's Disease (Site not responding. Last check: 2007-10-09)
		New cholinesterase inhibitors capable of slowing the progression of Alzheimer's disease are being introduced at a rapid pace.
		Although it is not a cholinesterase inhibitor per se, it is gradually converted in the body to 2,2-dichlorovinyl dimethyl phosphate (DDVP), a long-acting inhibitor of both AChE and BuChE.
		Cholinesterase inhibitors may prove useful in treating non-Alzheimer diseases and syndromes characterized by significant disturbance of memory, cognition, and behavior.
	www.hosppract.com /issues/1998/11/stahl.htm (2479 words)

	Cholinesterase (Site not responding. Last check: 2007-10-09)
		Pseudocholinesterase, also known as plasma cholinesterase, butyrylcholinesterase, or (most formally) acylcholine acylhydrolase, found primarily in the liver Both of these compounds catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation.
		A cholinesterase inhibitor is known as an anticholinesterase.
		Because of its essential function, chemicals that interfere with the action of cholinesterase are potent neurotoxin s, causing excessive salivation and eye watering in low doses, followed by muscle spasms and ultimately death.
	www.serebella.com /encyclopedia/article-Cholinesterase.html (203 words)

	Cholinesterase - Wikipedia, the free encyclopedia
		A cholinesterase inhibitor (or "anticholinesterase") suppresses the action of the enzyme.
		Because of its essential function, chemicals that interfere with the action of cholinesterase are potent neurotoxins, causing excessive salivation and eye watering in low doses, followed by muscle spasms and ultimately death (examples are snake venom, sarin and VX).
		One of the most common class of acetylcholinesterase inhibitors are the phosphorus based compounds which are design to bind to the active site of the enzyme, the strucutral requirements are a phosphorus atom bearing two lipophilic groups, a leaving group (such as a halide or thiocyanate) and a terminal oxygen.
	www.wikipedia.org /wiki/Cholinesterase (418 words)

	Resources \| About FDA-approved cholinesterase inhibitors (Site not responding. Last check: 2007-10-09)
		Three cholinesterase inhibitors are commonly prescribed: donepezil (Aricept), approved in 1996; rivastigmine (Exelon), approved in 2000; and galantamine (approved in 2001 under the trade name Reminyl and renamed Razadyne in 2005).
		Cholinesterase inhibitors are designed to increase levels of acetylcholine, a chemical messenger involved in memory, judgment and other thought processes.
		A cholinesterase inhibitor slows the breakdown of acetylcholine by blocking the activity of acetylcholinesterase.
	www.alz.org /Resources/TopicIndex/cholinesteraseinhibitors.asp (838 words)

	Clinical Geriatrics (Site not responding. Last check: 2007-10-09)
		In general, cholinesterase inhibitors can be classified as reversible, irreversible, or pseudoirreversible.6 Reversible inhibitors form only weak ionic bonds within the active site of the cholinesterase, and their half-life of action is equal to their serum half-life.
		Irreversible inhibitors (such as the organophosphates) permanently inactivate the cholinesterase by forming a covalent bond at the active site; the half-life of inhibition for these inhibitors is equal to the time needed to synthesize new cholinesterase (about one to two months).
		Cholinesterase inhibitors have been shown to prolong the time to severe impairment in patients with Alzheimer’s disease, and their use is now considered to be the standard of care in its treatment.
	www.podiatrytoday.com /cg/displayArticle.cfm?articleID=cgac456 (3667 words)

	NASD: Get Cholinesterase Test Now
		Cholinesterase is an enzyme that is needed for the proper function of the human body:s nervous system.
		If the body:s cholinesterase level is decreas d because of exposure to organophosphates or carbamates, the cholinesterase fails to function properly, causing the body:s nervous system to become "jammed up" with unnecessary commands.
		Rosenman points out that a 20 percent decrease of cholinesterase from baseline levels is an indication that a farmer needs to review his or her work practices to minimize any potential health effects.
	www.cdc.gov /nasd/docs/d001101-d001200/d001101/d001101.html (687 words)

	Facts: About FDA-approved cholinesterase inhibitors
		Tacrine (Cognex®), the first cholinesterase inhibitor, was approved in 1993 but is rarely prescribed today because of associated side effects, including possible liver damage.
		Cholinesterase inhibitors are designed to enhance memory and other cognitive functions by influencing certain chemical activities in the brain.
		A cholinesterase inhibitor is designed to stop the activity of acetylcholinesterase, thereby slowing the breakdown of acetylcholine.
	www.alzmass.org /factsheets/AChE_inhibitor_12-15-03.htm (724 words)

	Cholinesterase Inhibition
		Cholinesterase (ko-li-nes-ter-ace) is one of many important enzymes needed for the proper functioning of the nervous systems of humans, other vertebrates, and insects.
		The cholinesterase test is a blood test used to measure the effect of exposure to certain or cholinesterase-affected insecticides.
		A reported change in an individual's cholinesterase level may result from something other than a pesticide exposure, or it may be the result of laboratory error, but this should never be assumed to be the case.
	pmep.cce.cornell.edu /profiles/extoxnet/TIB/cholinesterase.html (2721 words)

	farlow1
		Cholinesterase inhibitors are thought to improve symptoms in patients with AD by blocking acetylcholinesterase raising the levels of acetylcholine at the synapse.
		Cholinesterase inhibitors have been demonstrated to decrease secretion of Ab proteins in both cell line and animal studies, an effect which might delay plaque formation and/or progression of AD.
		Published results of double-blind, placebo-controlled trials of cholinesterase inhibitors and their following open-label studies for periods of time up to 3 years have been reviewed for evidence to support an effect and/or lack of effect on long term disease progression.
	www.siumed.edu /cme/html/farlow1.html (356 words)

	Acetylcholine: AChEase inhibitors
		The cholinesterase inhibitors are widely used to treat glaucoma (a disorder characterized by increased intraocular pressure).
		Another major use of cholinesterase inhibitors is for treatment of myasthenia gravis, an autoimmune disease in which antibodies are formed against the nicotinic receptor at the neuromuscular junction.
		The molecule pralidoxime is a useful antidote for intoxication with cholinesterase inhibitors such as the organophosphates.
	www.neurosci.pharm.utoledo.edu /MBC3320/AChEase.htm (808 words)

	Synopsis of Myasthenia Gravis
		The ability of a short-acting (< 5 minutes) cholinesterase inhibitor (edrophonium) to reverse the presenting symptoms confirms the diagnosis of myasthenia gravis -- patients should show an immediate, short-lived improvement.
		Cholinesterase inhibitors are used to manage the symptoms of the disease.
		Selecting the correct dosage of cholinesterase inhibitor can be difficult, requiring the expertise of a physician experienced at treating this disorder.
	wings.buffalo.edu /aru/MyastheniaGravis.html (505 words)

	032. Mevinphos (FAO Meeting Report PL/1965/10/1)
		Cholinesterase determinations on plasma, erythrocytes and brain all showed inhibition of activity proportional to the dose; e.g., in the brain, 90% of the normal value was found at 6.3 ppm, 40% at 12.5 ppm And 20% at 50 ppm.
		On the basis of statistical analysis it was concluded that the decrease in erythrocyte cholinesterase activity became significant when the diets of males contained 1.1 ppm and that of females 1.3 ppm mevinphos.
		On 5 ppm plasm cholinesterase activity was 90% of normal and brain cholinesterase activity was not affected by 0.3-5.0 ppm in the diet (Cleveland & Treon, 1961; Kettering Lab., 1957c).
	www.inchem.org /documents/jmpr/jmpmono/v065pr32.htm (1174 words)

	BioMed Central \| Full text \| Rational choice of cholinesterase inhibitor for the treatment of Alzheimer's disease in ...
		Cholinesterase inhibitors, such as galantamine, donepezil and rivastigmine are approved for symptomatic treatment of Alzheimer's Disease (AD) in Canada.
		The confidence intervals of the withdrawal adjustment factors for the lower doses of all three cholinesterase inhibitors included a value of one (i.e., withdrawal no different than with placebo), and there is some evidence that slower titration regimens might result in lower discontinuation rates even for the higher doses of these drugs.
		Although there is no evidence to indicate that cholinesterase inhibitors improve survival, if the cognitive benefits are allowed to translate to mortality reductions, all treatments are predicted to increase costs relative to no treatment because the additional survival incurs further costs.
	www.biomedcentral.com /1471-2318/3/6 (4636 words)

	Cholinesterase (Site not responding. Last check: 2007-10-09)
		In biochemistry cholinesterase is a term which refers to of the two enzymes :
		The difference between the two of cholinesterase has to do with their preferences for substrates : the former hydrolyses acetylcholine more quickly; latter hydrolyses butyrylcholine more quickly.
		Because of its essential function chemicals that with the action of cholinesterase are potent neurotoxins causing excessive salivation and eye watering low doses followed by muscle spasms and death.
	www.freeglossary.com /Cholinesterase (196 words)

	Institute for The Study of Aging (Site not responding. Last check: 2007-10-09)
		While the therapeutic impact of cholinesterase inhibitors on patient outcomes is well-documented, little is known about whether therapeutic benefits to the patient help reduce caregiver burden.
		This project estimated the impact of rivastigmine, a cholinesterase inhibitor, on caregiver burden.
		Caregivers of 51patients receiving rivastigmine and with no history of using other cholinesterase inhibitors were compared to caregivers of 604 patients who had never received a cholinesterase inhibitor.
	www.aging-institute.org /outcome_2002b.htm (201 words)

	[No title]
		Cholinesterase inhibitors and Ginkgo extracts - are they comparable in the treatment of dementia?.
		The object of the current study was to compare published efficacy studies of acetyl cholinesterase inhibitors and ginkgo special extract EGb761® (aka TeboninÖ, W. Schwabe, Karlruhe, Germany), with respect to the relevance of their results.
		All studies of cholinesterase inhibitors and EGb761® met the following criteria and were described separately in the paper: only randomized, placebo-controlled studies with a parallel group designed carried out in a double-blind fashion without enrichment or combination therapy, with 24-30 weeks of randomized treatment and with published results.
	www.herbalgram.org /bodywise/herbclip/review.asp?i=42601 (681 words)

	Postgraduate Medicine: Alzheimer's Disease Symposium: Treating Alzheimer's disease
		Cholinesterase inhibitors have been the most widely studied experimental treatment for Alzheimer's disease and are currently the only approved symptomatic treatment.
		Second-generation cholinesterase inhibitors: Donepezil, formerly known as E2020, is a reversible acetylcholinesterase inhibitor that has dose-dependent activity showing greater selectivity for acetylcholinesterase and a longer duration of inhibitory action than tacrine or physostigmine, as well as greater specificity for brain tissue than peripheral tissue.
		Metrifonate (originally developed as an insecticide) is an organophosphorous agent that does not inhibit cholinesterase but acts as a prodrug for the long-acting cholinesterase inhibitor dichlorvos (6).
	www.postgradmed.com /issues/1997/06_97/tariot.htm (2980 words)

	Chronic Neuropsychological Sequelae of Cholinesterase Inhibitors in the Absence of Structural Brain Damage: Two Cases ...
		The main neurotoxic reaction after absorption of cholinesterase inhibitors is acute cholinergic syndrome due to the inhibition of the acetylcholinesterase (AChE) enzyme, which is reversible in case of the carbamates and irreversible in case of OPs.
		In fact, it is difficult to attribute the neuropsychological deficit to pyrethroid intoxication when PVM's diagnosis was overcholinergic syndrome by cholinesterase inhibitors, corroborated by the symptomology presented, which was similar to that previously recorded after intoxications with cholinesterase inhibitors, and the certainty of contact with the carbamate methomyl.
		Nevertheless, it is widely used as a biomarker of both exposure to cholinesterase inhibitors and recovery from acute intoxications.
	ehp.niehs.nih.gov /members/2005/7545/7545.html (4137 words)

	Facts: About FDA-approved cholinesterase inhibitors
		Three cholinesterase inhibitors are commonly prescribed--donepezil (Aricept®), approved in 1996; rivastigmine (Exelon®), approved in 2000; and galantamine (Reminyl®), approved in 2001.
		Symptoms such as nausea, vomiting, loss of appetite, and increased frequency of bowel movements might be expected with any cholinesterase inhibitor.
		It is strongly recommended that a physician who is comfortable and experienced in using these medications monitor patients treated with any of these compounds and that the recommended guidelines be strictly observed.
	www.alzmass.org /factsheets/cholinesterase.htm (695 words)

	DARE abstract20031556 (Site not responding. Last check: 2007-10-09)
		The outcome used in the analysis was the caregiver's WTP for using a cholinesterase inhibitor to delay disease progression and to treat the behavioural symptoms of dementia in patients with AD.
		The four scenarios depicted compared the effects of cholinesterase inhibitors and the effects of no treatment, with participants being asked to derive the maximum they would be willing to pay for treatment.
		Even though the authors referenced the literature from where the effects of cholinesterase inhibitors were derived, more information on how this literature search was undertaken and the quality of the studies retrieved (amongst other factors) should have been included, to increase the internal validity of the study.
	nhscrd.york.ac.uk /online/nhseed/20031556.htm (2416 words)

	Phosphamidon (PDS)
		Cholinesterase activity was inhibited in erythrocytes and brain by 72.05 and 84.15% respectively.
		Inhibition of blood and brain cholinesterases was significant in males and females at 0.25 ml/kg level with the exception of brain cholinesterase activity in females which appeared unaffected at 0.25 ml/kg level.
		Plasma cholinesterase levels were depressed 0-25% in 19 people, 26-50% in 19 other people and over 50% in two people with complete recovery in nine days.
	www.inchem.org /documents/pds/pds/pest74_e.htm (3381 words)

	Journal of Cerebral Blood Flow & Metabolism - Effects of Metrifonate, a Cholinesterase Inhibitor, on Local Cerebral ... (Site not responding. Last check: 2007-10-09)
		A number of studies report that cholinesterase inhibitors such as physostigmine (PHY) and the recently approved agent tacrine (tetrahydroaminoacridine; THA) are moderately effective in some mildly demented AD patients (for review see Lamy, 1994).
		On the other hand, studies on ACh release have shown that the depolarization-induced and the basal release of ACh are significantly decreased in synaptosomal preparations from aged rat brains (Araujo et al., 1990) and that basal ACh release is decreased in cortex and hippocampus in freely moving aged rats (Wu et al., 1988).
		(1972) Inhibition by metrifonate and dichlorvos of cholinesterases in schistosomes.
	www.nature.com /jcbfm/journal/v16/n5/full/9590123a.html (5756 words)

	Clinical Geriatrics (Site not responding. Last check: 2007-10-09)
		With the introduction of rivastigmine this year, another cholinesterase inhibitor is available, but one which also inhibits butyrylcholinesterase.
		Although the current generation of anti-dementia compounds, that is, the cholinesterase inhibitors, are not a cure for Alzheimer's disease, it is important that one not take a therapeutically nihilistic attitude toward these compounds.
		It does seem clear that individuals who are diagnosed early and placed on cholinesterase inhibitors early in the course of the disease and maintained on these medications do better in the long term than do individuals who are not given the benefit of being on these agents.
	www.mmhc.com /cg/displayArticle.cfm?articleID=cgac1021 (588 words)

	034. Parathion (FAO Meeting Report PL/1965/10/1)
		In mammals and plants parathion is readily oxidized to a powerful cholinesterase inhibitor, paraoxon, which is the active form of parathion (Heath, 1961).
		A significant increase in the mean plasma cholinesterase activity without an accompanying change in the erythrocyte cholinesterase activity occurred early in the feeding programs, but the level declined to control values when doses of 0.050 mg/kg body-weight were reached (Rider et al., 1958).
		Erythrocyte cholinesterase activity is a most sensitive indicator of this action of parathion and a wide margin exists between the highest dose without action on cholinesterase activity and the lowest dose needed to cause clinical effect.
	www.inchem.org /documents/jmpr/jmpmono/v065pr34.htm (1824 words)

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