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Cholinesterases inhibitors

The reversible inhibitors, which have a short to moderate duration of action, fall into two categories. Type one, exemplified by edrophonium, forms an ionic bond at the anionic site and a weak hydrogen bond at the esteratic site of acetylcholinesterase. Type two, exemplified by neostigmine, forms an ionic bond at the anionic site and a hydrolyzable covalent bond at the esteratic site. The irreversible inhibitors, exemplified by organophosphorus compounds (diisopropyl fluorophosphate, parathion, [Pg.374]

Passing across blood-brain barrier Well No [Pg.375]

Used to combat the CNS toxicity of numerous anticholinergic drugs Yes No [Pg.375]

Physostigmine (eserine sulfate) causes miosis and spasm of accommodation it also lowers intraocular pressure and hence can be used in the treatment of wide-angle glaucoma. As it is lipid soluble, it penetrates into the brain rapidly, raises the acetylcholine concentration and, in toxic amounts, may cause cholinergic CNS toxicity, which is characterized by restlessness, insomnia, tremors, confusion, ataxia, convulsions, respiratory depression, and circulatory collapse. These effects are reversed by atropine. [Pg.375]

The therapeutic uses of neostigmine include the treatment of atony of the urinary bladder and postoperative abdominal distention. In addition, it antagonizes the action of rf-tubocurarine and curariform drugs. Edrophonium, neostigmine, or pyridostigmine may be used to diagnose myasthenia gravis. Because edrophonium has the shortest duration of action, it is most often used for this purpose. [Pg.375]

GEN ERIC NAME TRADE NAME USES ADVERSE REACTIONS DOSAGE RANGES [Pg.305]

Cholinesterase inhibitors are used to treat the dementia associated with AD. The effectiveness of these dragp varies from individual to individual. The drugp may noticeably diminish the symptoms of AD, the symptoms could improve only slightly, or the symptoms could continue to progress (only at a slower rate). [Pg.305]

Donepezil has the advantage of once-daily administration and appears to be better tolerated than tacrine. Tacrine is particularly harmful to the liver. The new dragp rivastigmine and galantamine, like the other two, are effective in treating mild-to-moderate dementia of AD. [Pg.305]

In most situations, adverse reactions of the cholinesterase inhibitors are mild and are most often experienced early in the treatment. When adverse reactions occur, they tend to disappear gradually as the body gets used to the treatment and generally will not last for more than several days. Adverse reactions of the cholinesterase inhibitors [Pg.305]

Tacrine is particularly damaging to the liver and can result in hepatotoxicity. Because tacrine is more likely to cause adverse reactions and drug interactions, it must be administered more frequently (4 times a day) and is rarely used in current therapy. Donepezil has fewer and milder side effects than tacrine It is considered the agent of first choice However, some patients may achieve a better response with one drug than another. Additional adverse reactions are listed in the Summary Drug Table Cholinesterase Inhibitors. [Pg.305]

Several herbal remedies are thought to be helpful in AD. Ginkgo biloba is a common herb tliat appears to increase blood flow to the brain and has antioxidant properties. The herb is available over tlie counter, but there are no standards in the United States to regulate its quality of effectiveness. No one should take tliis or any otlier herb for AD without first consulting with tlie primary care provider. When ginkgo biloba is used with otlier dru, such as with warfarin or high doses of vitamin E, tliere is a risk for increased bleeding. [Pg.304]

Acetylcholine, a natural chemical in the brain, is required for memory and tliinking. Individuals with AD slowly lose tliis chemical, and as the levels of the chemical decrease, tlie patient experience problems with memory and thinking. The cholinesterase inhibitors act to increase the level of acetylcholine in the CNS by inhibiting its breakdown and slowing neuronal destruction. However, the disease is progressive, and although tliese dru alter the progress of tlie disease, they do not cure the disease The life span of a [Pg.304]


Although controversy exists over the cholinergic involvement in AD dementia, as of 1993 the only AD therapy approved by the U.S. FDA was the cholinesterase inhibitor, tacrine [321-64-2] C 2H 4N2, sold as Cognex (Warner-Lambert). [Pg.96]

Sample pre-treatment. Novel procedures of electrochemical sample treatment have been proposed to decrease the signal interference with native cholinesterase inhibitors present in fruits and vegetables. Polyphenolic compounds were removed by electrolysis with soluble A1 anode followed by the oxidation of thionic pesticides with electrogenerated chlorine. The procedure proposed makes it possible to decrease the background current and the matrix effect by 80-90%. Thus, the detection limits of about 5 ppb of Pai athion-Methyl and Chloropyrifos-Methyl were obtained in spiked grape juice without any additional sepai ation or pre-concentration stages. [Pg.295]

Cholinesterase inhibitor (anti-cholinesterase, ChEI) is a chemical that prevents cholinesterases (ChEs) from breaking down. ACh, which consequently increases the level and duration of action of this neurotransmitter. ChEIs such as organophosphates (esters of phosphoric acid) and carbamates (esters of carbamic acid) - serve as insecticides, pesticides, warfare agents and drugs. [Pg.361]

Monoamine Oxidases and their Inhibitors. Figure 2 Structures of MAO inhibitors. In the top row, the structural similarity between selegiline/L-deprenyl and methamphetamine is shown. Below are the aminoindan series of propargylamine compounds such as rasagiline. Next, the bifunctional MAO and cholinesterase inhibitors (ladostigil) and lastly, the iron chelator-MAO inhibitors. [Pg.785]

List the uses, general drug actions, general adverse reactions, contraindications, precautions, and interactions associated with the administration of the cholinesterase inhibitors. [Pg.304]

Discuss important preadministration and ongoing assessment activities the nurse should perform on the patient taking a cholinesterase inhibitor. [Pg.304]

Discuss ways to promote an optimal response to therapy, how to manage common adverse reactions, and important points to keep in mind when educating patients about the use of the cholinesterase inhibitors. [Pg.304]

The cholinesterase inhibitors are contraindicated in patients with a hypersensitivity to the dru and during pregnancy (Pregnancy Category B) and lactation. [Pg.305]

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). [Pg.306]

The Patient Receiving a Cholinesterase Inhibitor for Mild-to-Moderate Dementia of Alzheimer s Disease... [Pg.306]

A patient receiving a cholinesterase inhibitor may be treated in the hospital, nursing home, or in an outpatient setting. The patient s cognitive ability and functional... [Pg.306]

Ongoing assessment of patients taking the cholinesterase inhibitors includes both mental and physical assessments. Cognitive and functional abilities are assessed using Display 33-1 as a guide. Initial assessments will be compared with the ongoing assessments to monitor die patient s improvement (if any) after taking the cholinesterase inhibitors. [Pg.307]

Widiin 6 weeks of die discontinuation of cholinesterase inhibitor tiierapy, individuals lose any benefit they have received from die drugs. [Pg.308]

Which of die following nursing diagnoses would the nurse most likely place on die care plan of a patient with AD diat is related to adverse reactions of die cholinesterase inhibitors ... [Pg.309]

The cholinesterase inhibitors are more potent and longer acting tiian the direct-acting miotics and are used... [Pg.624]


See other pages where Cholinesterases inhibitors is mentioned: [Pg.207]    [Pg.207]    [Pg.478]    [Pg.428]    [Pg.429]    [Pg.239]    [Pg.339]    [Pg.301]    [Pg.52]    [Pg.526]    [Pg.133]    [Pg.67]    [Pg.360]    [Pg.360]    [Pg.361]    [Pg.799]    [Pg.1174]    [Pg.1489]    [Pg.304]    [Pg.304]    [Pg.304]    [Pg.305]    [Pg.306]    [Pg.307]    [Pg.307]    [Pg.307]    [Pg.309]    [Pg.622]    [Pg.624]    [Pg.626]   
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Applications of cholinesterase inhibitors

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Atropine cholinesterase inhibitor)

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Cholinesterase inhibitor in clover

Cholinesterase inhibitor tolerance

Cholinesterase inhibitors acute effects

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Cholinesterase inhibitors adverse reaction

Cholinesterase inhibitors antagonists

Cholinesterase inhibitors behavioral toxicity

Cholinesterase inhibitors carbamates

Cholinesterase inhibitors cholinomimetics

Cholinesterase inhibitors chronic effects

Cholinesterase inhibitors donepezil

Cholinesterase inhibitors edrophonium

Cholinesterase inhibitors galantamine

Cholinesterase inhibitors glaucoma treatment

Cholinesterase inhibitors history

Cholinesterase inhibitors hypersensitivity

Cholinesterase inhibitors in Alzheimer’s disease

Cholinesterase inhibitors mechanism

Cholinesterase inhibitors metabolic effects

Cholinesterase inhibitors organophosphate

Cholinesterase inhibitors poisoning

Cholinesterase inhibitors potentiation

Cholinesterase inhibitors reproductive toxicity

Cholinesterase inhibitors reversible

Cholinesterase inhibitors rivastigmine

Cholinesterase inhibitors toxicity

Cholinesterase inhibitors toxicology

Cholinesterase inhibitors vapor pressure

Cholinesterase inhibitors, and

Cholinesterase inhibitors, drug

Cholinesterase inhibitors, drug interactions

Cholinesterase inhibitors, specific

Cholinesterase inhibitors, specific agents

Cholinesterase inhibitors. See

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Dementia-related illnesses, cholinesterase inhibitors

Diazepam cholinesterase inhibitors

Glaucoma cholinesterase inhibitors

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Inhibitors of cholinesterase

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Memory cholinesterase inhibitors

Myasthenia gravis cholinesterase inhibitors

Organophosphates cholinesterase inhibitors’ compound

Organophosphorus cholinesterase inhibitors, first

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