Cholinesterase inhibitors. Medical search

Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.

Phenyl esters of carbamic acid or of N-substituted carbamic acids. Structures are similar to PHENYLUREA COMPOUNDS with a carbamate in place of the urea.

Aryl CYCLOPENTANES that are a reduced (protonated) form of INDENES.

A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.

A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.

An aspect of cholinesterase (EC 3.1.1.8).

A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.

An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7.

AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.

A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.

Drugs used to specifically facilitate learning or memory, particularly to prevent the cognitive deficits associated with dementias. These drugs act by a variety of mechanisms. While no potent nootropic drugs have yet been accepted for general use, several are being actively investigated.

A carbamate insecticide with anticholinesterase activity.

A cholinesterase inhibitor that is used as an organothiophosphorus insecticide.

A cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.

A family of hexahydropyridines.

A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.

An organochlorophosphate cholinesterase inhibitor that is used as an insecticide for the control of flies and roaches. It is also used in anthelmintic compositions for animals. (From Merck, 11th ed)

A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)

A highly toxic cholinesterase inhibitor that is used as an acaricide and as an insecticide.

Compounds containing carbon-phosphorus bonds in which the phosphorus component is also bonded to one or more sulfur atoms. Many of these compounds function as CHOLINERGIC AGENTS and as INSECTICIDES.

An organothiophosphate cholinesterase inhibitor that is used as an insecticide and as an acaricide.

An organophosphorus ester compound that produces potent and irreversible inhibition of cholinesterase. It is toxic to the nervous system and is a chemical warfare agent.

An organothiophosphate insecticide.

Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics.

An organophosphorus compound that inhibits cholinesterase. It causes seizures and has been used as a chemical warfare agent.

A potent, long-acting cholinesterase inhibitor used as a miotic in the treatment of glaucoma.

An organophosphate cholinesterase inhibitor that is used as a pesticide.

A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.

Carbamate derivative used as an insecticide, acaricide, and nematocide.

Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.

An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness.

Chemicals that are used to cause the disturbance, disease, or death of humans during WARFARE.

Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here.

Drugs used to reverse the inactivation of cholinesterase caused by organophosphates or sulfonates. They are an important component of therapy in agricultural, industrial, and military poisonings by organophosphates and sulfonates.

Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.

Method of psychotherapeutic treatment based on assumption of patients' personal responsibility for their own behavior. The therapist actively guides patients to accurate self-perception for fulfillment of needs of self-worth and respect for others. (From APA, Thesaurus of Psychological Index Terms, 8th ed.)

A mercaptocholine used as a reagent for the determination of CHOLINESTERASES. It also serves as a highly selective nerve stain.

An aspect of cholinesterases.

Neurologic disorders caused by exposure to toxic substances through ingestion, injection, cutaneous application, or other method. This includes conditions caused by biologic, chemical, and pharmaceutical agents.

A highly fluorescent anti-infective dye used clinically as a topical antiseptic and experimentally as a mutagen, due to its interaction with DNA. It is also used as an intracellular pH indicator.

An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.

A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.

A local anesthetic of the amide type now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1006)

Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.

Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.

One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.

N,N',N'',N'''-Tetraisopropylpyrophosphamide. A specific inhibitor of pseudocholinesterases. It is commonly used experimentally to determine whether pseudo- or acetylcholinesterases are involved in an enzymatic process.

The relationship between the dose of an administered drug and the response of the organism to the drug.

A neurodegenerative disease characterized by dementia, mild parkinsonism, and fluctuations in attention and alertness. The neuropsychiatric manifestations tend to precede the onset of bradykinesia, MUSCLE RIGIDITY, and other extrapyramidal signs. DELUSIONS and visual HALLUCINATIONS are relatively frequent in this condition. Histologic examination reveals LEWY BODIES in the CEREBRAL CORTEX and BRAIN STEM. SENILE PLAQUES and other pathologic features characteristic of ALZHEIMER DISEASE may also be present. (From Neurology 1997;48:376-380; Neurology 1996;47:1113-1124)

Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.

An organophosphorus insecticide that inhibits ACETYLCHOLINESTERASE.

Poisoning due to exposure to ORGANOPHOSPHORUS COMPOUNDS, such as ORGANOPHOSPHATES; ORGANOTHIOPHOSPHATES; and ORGANOTHIOPHOSPHONATES.

Standardized clinical interview used to assess current psychopathology by scaling patient responses to the questions.

Cardiac arrhythmias that are characterized by excessively slow HEART RATE, usually below 50 beats per minute in human adults. They can be classified broadly into SINOATRIAL NODE dysfunction and ATRIOVENTRICULAR BLOCK.

Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of ACETYLCHOLINE, and drugs that affect the survival of cholinergic neurons. The term cholinergic agents is sometimes still used in the narrower sense of MUSCARINIC AGONISTS, although most modern texts discourage that usage.

Various salts of a quaternary ammonium oxime that reconstitute inactivated acetylcholinesterase, especially at the neuromuscular junction, and may cause neuromuscular blockade. They are used as antidotes to organophosphorus poisoning as chlorides, iodides, methanesulfonates (mesylates), or other salts.

A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.

The craniosacral division of the autonomic nervous system. The cell bodies of the parasympathetic preganglionic fibers are in brain stem nuclei and in the sacral spinal cord. They synapse in cranial autonomic ganglia or in terminal ganglia near target organs. The parasympathetic nervous system generally acts to conserve resources and restore homeostasis, often with effects reciprocal to the sympathetic nervous system.

The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.

An organothiophosphate cholinesterase inhibitor that is used as an insecticide.

A carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries.

Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology.

Tests designed to assess neurological function associated with certain behaviors. They are used in diagnosing brain dysfunction or damage and central nervous system disorders or injury.

An imprecise term referring to dementia associated with CEREBROVASCULAR DISORDERS, including CEREBRAL INFARCTION (single or multiple), and conditions associated with chronic BRAIN ISCHEMIA. Diffuse, cortical, and subcortical subtypes have been described. (From Gerontol Geriatr 1998 Feb;31(1):36-44)

A sulfur-containing analog of butyrylcholine which is hydrolyzed by butyrylcholinesterase to butyrate and thiocholine. It is used as a reagent in the determination of butyrylcholinesterase activity.

Disturbances in mental processes related to learning, thinking, reasoning, and judgment.

An agent used as a substrate in assays for cholinesterases, especially to discriminate among enzyme types.

Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)

A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.

The benzoic acid ester of choline.

Amide derivatives of phosphoric acid such as compounds that include the phosphoric triamide (P(=O)(N)(N)(N)) structure.

Intellectual or mental process whereby an organism obtains knowledge.

One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.

Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.

Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.

Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.

The action of a drug that may affect the activity, metabolism, or toxicity of another drug.

Chemicals used to destroy pests of any sort. The concept includes fungicides (FUNGICIDES, INDUSTRIAL); INSECTICIDES; RODENTICIDES; etc.

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.

A carbamate insecticide.

Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.

The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.

A plant family of the order Euphorbiales, subclass Rosidae, class Magnoliopsida. Leaves are alternate, simple, and leathery. Fruits are one- or two-seeded capsules or drupes (stony-pitted fleshy fruits).

Metrifonate increases neuronal excitability in CA1 pyramidal neurons from both young and aging rabbit hippocampus. (1/1796)

The effects of metrifonate, a second generation cholinesterase inhibitor, were examined on CA1 pyramidal neurons from hippocampal slices of young and aging rabbits using current-clamp, intracellular recording techniques. Bath perfusion of metrifonate (10-200 microM) dose-dependently decreased both postburst afterhyperpolarization (AHP) and spike frequency adaptation (accommodation) in neurons from young and aging rabbits (AHP: p < 0.002, young; p < 0.050, aging; accommodation: p < 0.024, young; p < 0.001, aging). These reductions were mediated by muscarinic cholinergic transmission, because they were blocked by addition of atropine (1 microM) to the perfusate. The effects of chronic metrifonate treatment (12 mg/kg for 3 weeks) on CA1 neurons of aging rabbits were also examined ex vivo. Neurons from aging rabbits chronically treated with metrifonate had significantly reduced spike frequency accommodation, compared with vehicle-treated rabbits. Chronic metrifonate treatment did not result in a desensitization to metrifonate ex vivo, because bath perfusion of metrifonate (50 microM) significantly decreased the AHP and accommodation in neurons from both chronically metrifonate- and vehicle-treated aging rabbits. We propose that the facilitating effect of chronic metrifonate treatment on acquisition of hippocampus-dependent tasks such as trace eyeblink conditioning by aging subjects may be caused by this increased excitability of CA1 pyramidal neurons. (+info)

Comparison of two in vitro activation systems for protoxicant organophosphorous esterase inhibitors. (2/1796)

In order to perform in vitro testing of esterase inhibition caused by organophosphorous (OP) protoxicants, simple, reliable methods are needed to convert protoxicants to their esterase-inhibiting forms. Incubation of parathion or chlorpyrifos with 0.05% bromine solution or uninduced rat liver microsomes (RLM) resulted in production of the corresponding oxygen analogs of these OP compounds and markedly increased esterase inhibition in SH-SY5Y human neuroblastoma cells. Neither activation system affected cell viability or the activity of AChE or NTE in the absence of OP compounds. Although parathion and chlorpyrifos were activated by RLM, bromine activation required fewer steps and produced more esterase inhibition for a given concentration of chlorpyrifos. However, RLM activation of OP protoxicants produced metabolites other than oxygen analogs and may, therefore, be more relevant as a surrogate for OP biotransformation in vivo. This methodology makes the use of intact cells for in vitro testing of esterase inhibition caused by protoxicant organophosphate compounds a viable alternative to in vivo tests. (+info)

Anaphylactic bronchoconstriction in BP2 mice: interactions between serotonin and acetylcholine. (3/1796)

1. Immunized BP2 mice developed an acute bronchoconstriction in vivo and airway muscle contraction in vitro in response to ovalbumin (OA) and these contractions were dose dependent. 2. Methysergide or atropine inhibited OA-induced bronchoconstriction in vivo and airway muscle contraction in vitro. 3. Neostigmine potentiated the OA-induced bronchoconstriction in vivo and airway muscle contraction in vitro of BP2 mice. This potentiation was markedly reduced by the administration of methysergide or atropine and when the two antagonists were administered together, the responses were completely inhibited. 4. Neostigmine also potentiated the serotonin (5-HT)- and acetylcholine (ACh)-induced bronchoconstriction and this potentiation was significantly reversed by atropine. 5. These results indicate that OA provokes a bronchoconstriction in immunized BP2 mice by stimulating the release of 5-HT, which in turn acts via the cholinergic mediator, ACh. (+info)

Efficacy and safety of rivastigmine in patients with Alzheimer's disease: international randomised controlled trial. (4/1796)

OBJECTIVES: To assess the effects of rivastigmine on the core domains of Alzheimer's disease. DESIGN: Prospective, randomised, multicentre, double blind, placebo controlled, parallel group trial. Patients received either placebo, 1-4 mg/day (lower dose) rivastigmine, or 6-12 mg/day (higher dose) rivastigmine. Doses were increased in one of two fixed dose ranges (1-4 mg/day or 6-12 mg/day) over the first 12 weeks with a subsequent assessment period of 14 weeks. SETTING: 45 centres in Europe and North America. PARTICIPANTS: 725 patients with mild to moderately severe probable Alzheimer's disease diagnosed according to the Diagnostic and Statistical Manual of Mental Disorders, fourth edition, and the criteria of the National Institute of Neurological and Communicative Disorders and Stroke and the Alzheimer's Disease and Related Disorders Association. OUTCOME MEASURES: Cognitive subscale of the Alzheimer's disease assessment scale, rating on the clinician interview based impression of change incorporating caregiver information scale, and the progressive deterioration scale. RESULTS: At the end of the study cognitive function had deteriorated among those in the placebo group. Scores on the Alzheimer's disease assessment scale improved in patients in the higher dose group when compared with patients taking placebo (P<0.05). Significantly more patients in the higher dose group had improved by 4 points or more than had improved in the placebo group (24% (57/242) v 16% (39/238)). Global function as rated by the clinician interview scale had significantly improved among those in the higher dose group compared with those taking placebo (P<0.001), and significantly more patients in the higher dose group showed improvement than did in the placebo group (37% (80/219) v 20% (46/230)). Mean scores on the progressive deterioration scale improved from baseline in patients in the higher dose group but fell in the placebo group. Adverse events were predominantly gastrointestinal, of mild to moderate severity, transient, and occurred mainly during escalation of the dose. 23% (55/242) of those in the higher dose group, 7% (18/242) of those in the lower dose group, and 7% (16/239) of those in the placebo group discontinued treatment because of adverse events. CONCLUSIONS: Rivastigmine is well tolerated and effective. It improves cognition, participation in activities of daily living, and global evaluation ratings in patients with mild to moderately severe Alzheimer's disease. This is the first treatment to show compelling evidence of efficacy in a predominantly European population. (+info)

The cholinergic hypothesis of Alzheimer's disease: a review of progress. (5/1796)

Alzheimer's disease is one of the most common causes of mental deterioration in elderly people, accounting for around 50%-60% of the overall cases of dementia among persons over 65 years of age. The past two decades have witnessed a considerable research effort directed towards discovering the cause of Alzheimer's disease with the ultimate hope of developing safe and effective pharmacological treatments. This article examines the existing scientific applicability of the original cholinergic hypothesis of Alzheimer's disease by describing the biochemical and histopathological changes of neurotransmitter markers that occur in the brains of patients with Alzheimer's disease both at postmortem and neurosurgical cerebral biopsy and the behavioural consequences of cholinomimetic drugs and cholinergic lesions. Such studies have resulted in the discovery of an association between a decline in learning and memory, and a deficit in excitatory amino acid (EAA) neurotransmission, together with important roles for the cholinergic system in attentional processing and as a modulator of EAA neurotransmission. Accordingly, although there is presently no "cure" for Alzheimer's disease, a large number of potential therapeutic interventions have emerged that are designed to correct loss of presynaptic cholinergic function. A few of these compounds have confirmed efficacy in delaying the deterioration of symptoms of Alzheimer's disease, a valuable treatment target considering the progressive nature of the disease. Indeed, three compounds have received European approval for the treatment of the cognitive symptoms of Alzheimer's disease, first tacrine and more recently, donepezil and rivastigmine, all of which are cholinesterase inhibitors. (+info)

Comparison between huperzine A, tacrine, and E2020 on cholinergic transmission at mouse neuromuscular junction in vitro. (6/1796)

AIM: To compare the effects of huperzine A (Hup A), tacrine, and E2020 on cholinergic transmission at mouse neuromuscular junction in vitro. METHODS: The isolated mouse phrenic nerve-hemidiaphragm preparations were used with the conventional intracellular recording technique. The miniature end-plate potentials (MEPP), the mean quantal content of end-plate potentials (EPP), and the resting membrane potentials of muscle fiber were recorded. RESULTS: Hup A, tacrine, and E2020 at the concentration of 1.0 mumol.L-1 increased the amplitude, time-to-peak, and half-decay time of MEPP in the potencies of E2020 > Hup A > tacrine. Hup A did not significantly change the frequency of MEPP, the appearance of giant MEPP or slow MEPP, the resting membrane potentials, and the mean quantal content of EPP. CONCLUSION: Hup A is a selective and potent cholinesterase inhibitor, by which activity it facilitates the cholinergic transmission at mouse neuromuscular junction, and devoid of pre- and post-synaptic actions. (+info)

Central nervous system-mediated hyperglycemic effects of NIK-247, a cholinesterase inhibitor, and MKC-231, a choline uptake enhancer, in rats. (7/1796)

We investigated the effects of intracerebroventricular administration of NIK-247 (9-amino-2,3,5,6,7,8-hexahydro-1H-cyclo-penta(b)-quinoline monohydrate hydrochloride; a cholinesterase inhibitor) or MKC-231 (2-(2-oxypyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofur o[2,3-b]quinolin-4-yl) acetoamide; a choline uptake enhancer) on plasma glucose level in comparison with that of neostigmine administration in rats. The extents of NIK-247- and MKC-231-induced hyperglycemia were considerably less than that by neostigmine, suggesting that the potencies of the drugs to produce the peripheral hyperglycemia may be pharmacologically negligible. (+info)

Electron paramagnetic resonance reveals altered topography of the active center gorge of acetylcholinesterase after binding of fasciculin to the peripheral site. (8/1796)

Fasciculin, a peptidic toxin from snake venom, inhibits mammalian and fish acetylcholinesterases (AChE) by binding to the peripheral site of the enzyme. This site is located at the rim of a narrow, deep gorge which leads to the active center triad, located at its base. The proposed mechanisms for AChE inhibition by fasciculin include allosteric events resulting in altered conformation of the AChE active center gorge. However, a fasciculin-induced altered topography of the active center gorge has not been directly demonstrated. Using electron paramagnetic resonance with the spin-labeled organophosphate 1-oxyl-2,2,6, 6-tetramethyl-4-piperidinylethylphosphorofluoridate (EtOSL) specifically bound to the catalytic serine of mouse AChE (mAChE), we show that bound fasciculin on mAChE slows down, but does not prevent phosphorylation of the active site serine by EtOSL and protects the gorge conformation against thermal denaturation. Most importantly, a restricted freedom of motion of the spin label bound to the fasciculin-associated mAChE, compared to mAChE, is evidenced. Molecular models of mAChE and fasciculin-associated mAChE with tethered EtOSL enantiomers indicate that this restricted motion is due to greater proximity of the S-EtOSL nitroxide radical to the W86 residue in the fasciculin-associated enzyme. Our results demonstrate a topographical alteration indicative of a restricted conformation of the active center gorge of mAChE with bound fasciculin at its rim. (+info)

It is a cholinesterase inhibitor. Breakdown in soil is 6.1 days in sand, 309 days in water at pH 5.0, 27 days at pH 7.0, and 3 ...

https://en.wikipedia.org/wiki/Methamidophos

It is a Cholinesterase inhibitor. When heated to decomposition, it emits toxic fumes of sulfur oxides and phosphorus oxides. ( ... NTP, 1992) Symptoms of exposure to this type of compound include cholinesterase inhibition, miosis, frontal headache, increased ...

https://en.wikipedia.org/wiki/Malaoxon

The use of medications for treatment of Alzheimer's dementia, such as cholinesterase inhibitors and memantine, has shown small[ ... cholinesterase inhibitors galantamine, donepezil, rivastigmine; and ginkgo biloba extract. The general management of dementia ... These medications include angiotensin converting enzyme inhibitors, diuretics, calcium channel blockers, sympathetic nerve ... inhibitors, angiotensin II receptor antagonists or adrenergic antagonists. Elevated lipid levels, including HDL, were found to ...

https://en.wikipedia.org/wiki/Vascular_dementia

Cholinesterase inhibitors such as donepezil are often used and may be beneficial in mild to moderate disorder. Overall benefit ... Cholinesterase inhibitors are often used early in the disorder course; however, benefit is generally small. Cognitive and ... 2008). "Effectiveness of cholinesterase inhibitors and memantine for treating dementia: evidence review for a clinical practice ... Rodda, J.; Morgan, S.; Walker, Z. (October 2009). "Are cholinesterase inhibitors effective in the management of the behavioral ...

https://en.wikipedia.org/wiki/Dementia

As with other cholinesterase inhibitors, galantamine may not be effective for treating mild cognitive impairment, Alzheimer's ... Birks, J (2006). "Cholinesterase inhibitors for Alzheimer's disease". The Cochrane Database of Systematic Reviews (1): CD005593 ... Galantamine also works as a weak competitive and reversible cholinesterase inhibitor in all areas of the body. By inhibiting ... "Cholinesterase inhibitors for Alzheimer's disease". Cochrane Database of Systematic Reviews (1): CD005593. doi:10.1002/14651858 ...

https://en.wikipedia.org/wiki/Galantamine

Birks, J. (2006). "Cholinesterase inhibitors for Alzheimer's disease". The Cochrane Database of Systematic Reviews (1): ...

https://en.wikipedia.org/wiki/Leucojum_aestivum

It acts as a cholinesterase inhibitor. The commercial product typically exists as a mixture of 70% (Z)-isomer and 30% (E)- ... He collapsed and exhibited significant depression of serum cholinesterase, but recovered completely within 2 days after ...

https://en.wikipedia.org/wiki/Phosphamidon

The chemical is an inhibitor of cholinesterase. If a human's exposure to tetraethyl dithiopyrophosphate is acute, then the ...

https://en.wikipedia.org/wiki/Tetraethyl_dithiopyrophosphate

It produces illness typical of cholinesterase inhibitors. Vomiting, nausea, diarrhea and excessive salivation are some common ... Organophosphates are acetylcholinesterase inhibitors and disrupt the signal transduction at the cholinergic synapse. It is ... There were no effects reported on plasma or red blood cell cholinesterase activity. These results were insufficient to ... Carbophenothion affects the nervous system by inhibiting cholinesterase. There are no signs of chronic or carcinogenic effects ...

https://en.wikipedia.org/wiki/Carbophenothion

Like other cholinesterase inhibitors, it requires doses to be increased gradually over several weeks; this is usually referred ... Jann, M. W.; Shirley, K. L.; Small, G. W. (2002). "Clinical Pharmacokinetics and Pharmacodynamics of Cholinesterase Inhibitors ... Inglis, F. (2002). "The tolerability and safety of cholinesterase inhibitors in the treatment of dementia". International ... Jann, M. W. (2000). "Rivastigmine, a New-Generation Cholinesterase Inhibitor for the Treatment of Alzheimer's Disease". ...

https://en.wikipedia.org/wiki/Rivastigmine

Walker LC, Rosen RF (Jul 2006). "Alzheimer therapeutics-what after the cholinesterase inhibitors?". Age and Ageing. 35 (4): 332 ... "CoMentis BACE Inhibitor Debuts". April 2008. "Merck Presents Results of a Phase I Clinical Trial Evaluating Investigational ... Drugs to block this enzyme (BACE inhibitors) in theory would prevent the buildup of beta-amyloid and (per the Amyloid ... The MEROPS online database for peptidases and their inhibitors: A01.004 beta-Secretase: Molecule of the Month, by David ...

https://en.wikipedia.org/wiki/Beta-secretase_1

It functions as a cholinesterase inhibitor in humans. "ChemSpider". Retrieved January 11, 2013. CID 93516 from PubChem "MSDS ...

https://en.wikipedia.org/wiki/Tebupirimfos

Strength may improve with administration of cholinesterase inhibitors.[citation needed] Berger, in 1876, first reported a case ...

https://en.wikipedia.org/wiki/Fazio–Londe_disease

ISBN 91-87184-39-7. Tammelin, Lars-Erik (1958). Choline esters: substrate and inhibitors of cholinesterases. Stockholm. LIBRIS ... linked to their chemical similarity to the neurotransmitter acetylcholine and their ability to block the enzyme cholinesterase ...

https://en.wikipedia.org/wiki/Lars-Erik_Tammelin

... is a cholinesterase inhibitor used as an insecticide and avicide; for example, against rice stem borers and house ...

https://en.wikipedia.org/wiki/Cyanophos

... monoxon is an inhibitor of the neuro enzyme cholinesterase (ChE), because it contains an active oxygen. Because ChE can ... Ethion monoxon is an inhibitor of the neuro enzyme cholinesterase (ChE). ChE is a facilitator of nerve impulse transmission, ... This mechanism works as follows (see the figure "Inhibition of cholinesterase by ethion monoxon."): a hydroxyl group from a ...

https://en.wikipedia.org/wiki/Ethion

It is a cholinesterase inhibitor and is a positive animal carcinogen. The substance is insoluble in water. Flash point data are ...

https://en.wikipedia.org/wiki/Tetrachlorvinphos

Contribution to the study of the mechanism of action of cholinesterase inhibitors. J. Pharmacol. Exp. Therap. 101: 327-343. ... Ontogenesis of cholinesterases. In: Cholinesterases and Anticholinesterase Agents, G. B. Koelle, Ed., pp. 129 - 186, Handbch. d ... In: Cholinesterases and Anticholinesterase Agents, G. B. Koelle, Ed., pp. 799 -832, Handbch. d. Exper. Pharmakol., Erganzungswk ... These studies contributed to the understanding of the role of cholinesterases as morphogens and "transport" or "scavenger" ...

https://en.wikipedia.org/wiki/Alex_Karczmar

Boxwood [Database] 2015 03-13-2015 [cited 2016 03-01-2016]. Orhan, I.E., et al., Selective cholinesterase inhibitors from Buxus ... McGleenon, B.M., K.B. Dynan, and A.P. Passmore, Acetylcholinesterase inhibitors in Alzheimer's disease. British Journal of ... Murray, A.P., et al., Natural AChE Inhibitors from Plants and their Contribution to Alzheimer's Disease Therapy. Current ... Cyclobuxine could also have a positive effect on Alzheimer's disease, as acetylcholinesterase inhibitors are an important ...

https://en.wikipedia.org/wiki/Cyclobuxine

Myasthenia is treated with immunosuppressants, cholinesterase inhibitors and, in selected cases, thymectomy. Demyelination is ...

https://en.wikipedia.org/wiki/Neuron

RIC-3 also known as resistance to inhibitors of cholinesterase 3 is a chaperone protein that in humans is encoded by the RIC3 ... "Entrez Gene: RIC3 resistance to inhibitors of cholinesterase 3 homolog (C. elegans)". Williams ME, Burton B, Urrutia A, et al ... "Caenorhabditis elegans mutants resistant to inhibitors of acetylcholinesterase". Genetics. 140 (2): 527-35. PMC 1206632 . PMID ...

https://en.wikipedia.org/wiki/RIC3

Calabar bean contains physostigmine, a reversible cholinesterase inhibitor alkaloid. The alkaloid physostigmine acts in effect ... "Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current Neuropharmacology. 11 (3): 315-335. doi:10.2174/ ...

https://en.wikipedia.org/wiki/Physostigma_venenosum

... is an irreversible inhibitor of cholinesterases in vitro. The inhibitory activity of leptophos seems to be related to ... An example of a cholinesterase is the acetylcholinesterase (AChE). This cholinesterase converts the neurotransmitter ...

https://en.wikipedia.org/wiki/Leptophos

Many toxins and venoms produced by plants and animals also contain cholinesterase inhibitors. In clinical use, they are ... They are examples of enzyme inhibitors, and increase the action of acetylcholine by delaying its degradation; some have been ... and rapid inactivation by cholinesterase. However, it is used in the form of eye drops to cause constriction of the pupil ...

https://en.wikipedia.org/wiki/Acetylcholine

Resistance to inhibitors of cholinesterase-8A (Ric-8A), also known as Synembryn-A, is a protein that in humans is encoded by ... Wang L, Guo D, Xing B, Zhang JJ, Shu HB, Guo L, Huang XY (September 2011). "Resistance to inhibitors of cholinesterase-8A (Ric- ... "Entrez Gene: RIC8A resistance to inhibitors of cholinesterase 8 homolog A (C. elegans)". Tall, Gregory G; Krumins Andrejs M; ...

https://en.wikipedia.org/wiki/RIC8A

... is a cholinesterase inhibitor and is toxic to humans. It is classified as a likely human carcinogen by the United ... Carbamate insecticides are slowly reversible inhibitors of the enzyme acetylcholinesterase. They resemble acetylcholine, but ... Extension Toxicology Network Cholinesterase Inhibition - Extension Toxicology Network EPA info EPA factsheet IPCS (WHO) Health ...

https://en.wikipedia.org/wiki/Carbaryl

... is a thiocarbamate cholinesterase inhibitor used as a herbicide. Thiocarbamate Tomlin, C.D.S. (ed.). The Pesticide ...

https://en.wikipedia.org/wiki/Benthiocarb

Historical development of organophosphorus cholinesterase inhibitors." Handbook of Experimental Pharmacology.". Cholinesterases ... It was discovered that TEPP is an inhibitor of cholinesterases. Schrader referred to the studies by Eberhard Gross, who was the ... The cholinesterase forms a very stable complex with TEPP, in which TEPP is covalently bound to the cholinesterase. This is a ... 3-4. "History of organophosphorus cholinesterase inhibitors & reactivators". Military Medical Science Letters. 84 (4): 182-185 ...

https://en.wikipedia.org/wiki/Tetraethyl_pyrophosphate

Petroianu, G.A (2014). Reversible cholinesterase inhibitors as pre-treatment for exposure to organophosphates: assessment using ... Organophosphorus AChE inhibitors can bind temporally to the catalytic site of the enzyme. Because of this binding, AzM cannot ... In mice, AzM causes weight loss, inhibits brain cholinesterase (ChE) and lowers the food consumption of the mice. A decrease of ... At high concentrations AzM itself can be toxic because it can function as a acetylcholinesterase (AChE) inhibitor. But its ...

https://en.wikipedia.org/wiki/Azinphos-methyl

... is a cholinesterase inhibitor which prevents the breakdown of acetylcholine in the synapse. In case of severe ... Aldicarb is a fast-acting cholinesterase inhibitor, causing rapid accumulation of acetylcholine at the synaptic cleft. It is ...

https://en.wikipedia.org/wiki/Aldicarb

is modified to include binding of the inhibitor to the free enzyme:. EI. +. S. ⇌. k. 3. k. −. 3. E. +. S. +. I. ⇌. k. −. 1. k. ... "The Inhibition of Cholinesterase by Physostigmine and Prostigmine". Journal of Biological Chemistry. 146: 85-93. ... is the inhibitor concentration.. V. max. {\displaystyle V_{\max }}. remains the same because the presence of the inhibitor can ... To compute the concentration of competitive inhibitor [. I. ]. {\displaystyle {\ce {[I]}}}. that yields a fraction f. V. 0. {\ ...

https://en.wikipedia.org/wiki/Competitive_inhibition

... because it is not degraded by cholinesterase which normally performs this function. As a result, the muscle cells contract ... UV protectants and specific inhibitors of enzymes.[16][17] ...

https://en.wikipedia.org/wiki/Cyanotoxin

Roberts SB (December 2002). "γ-secretase inhibitors and Alzheimer's disease". Adv. Drug Deliv. Rev. 54 (12): 1579-88. PMID ... Lahiri DK, Chen DM, Lahiri P, Bondy S, Greig NH (November 2005). "Amyloid, cholinesterase, melatonin, and metals and their ... an inhibitor of beta-amyloid(1-42) aggregation". Bioorg. Med. Chem. 10 (11): 3565-9. PMID 12213471. doi:10.1016/S0968-0896(02) ... "New class of inhibitors of amyloid-beta fibril formation. Implications for the mechanism of pathogenesis in Alzheimer's disease ...

https://gl.wikipedia.org/wiki/Amiloide_beta

ATSDR Case Studies in Environmental Medicine: Cholinesterase Inhibitors, Including Insecticides and Chemical Warfare Nerve ... Proteopedia AChE_inhibitors_and_substrates_(Part_II). *Proteopedia AChE bivalent inhibitors AChE_bivalent_inhibitors AChE ... cholinesterase activity. · cholinesterase activity. · protein binding. · collagen binding. · hydrolase activity. · serine ... Massoulie J, Pezzementi L, Bon S, Krejci E, Valette F. Molecular and Cellular Biology of Cholinesterases.. Prog. Brain Res. ...

https://zh.wikipedia.org/zh-tw/乙酰胆碱酯酶

Inhibitors: β-Alanine. *Bafilomycin A1. *Chicago sky blue 6B. *Evans blue. *GABA ...

https://en.wikipedia.org/wiki/GAD_antibodies

... cholinesterase inhibitors for dementia, and modafinil for daytime sleepiness.[84][85] In 2016 pimavanserin was approved for the ... MAO-B inhibitors. MAO-B inhibitors (safinamide, selegiline and rasagiline) increase the amount of dopamine in the basal ganglia ... always combined with a dopa decarboxylase inhibitor and sometimes also with a COMT inhibitor), dopamine agonists and MAO-B ... COMT inhibitors. Tolcapone inhibits the activity COMT, an enzyme which degrades dopamine.[74] It has been used to complement ...

https://en.wikipedia.org/?title=Parkinson's_disease

Like other cholinesterase inhibitors, it requires doses to be increased gradually over several weeks; this is usually referred ... Inglis, F. (2002). "The tolerability and safety of cholinesterase inhibitors in the treatment of dementia". International ... Jann, M. W. (2000). "Rivastigmine, a New-Generation Cholinesterase Inhibitor for the Treatment of Alzheimer's Disease". ... Jann, M. W.; Shirley, K. L.; Small, G. W. (2002). "Clinical Pharmacokinetics and Pharmacodynamics of Cholinesterase Inhibitors ...

https://en.m.wikipedia.org/wiki/Rivastigmine

Acetylcholinesterase inhibitor. *Psychoactive drug. *Ann Silver. *Usu en en.wikibooks.org *Structural Biochemistry/ ... Cholinesterase. *Choline acetyltransferase. *Nicotinic acetylcholine receptor. *Muscarinic acetylcholine receptor. *History of ...

https://ast.wikipedia.org/wiki/Ficheru:Acetylcholine.svg

失智症目前無法治癒[4]。多奈派齊（英语：donepezil）等乙醯膽鹼酯酶抑制劑（英语：cholinesterase inhibitors）類藥物經常用於治療輕至中度失智症[7][17][18]，但這些治療的幫助終歸有限[7][8]。對於失智症患者與照 ... Birks, J. Cholinesterase inhibitors for Alzheimer's disease.. The Cochrane database of systematic reviews. 25 January 2006, (1 ... Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis

https://zh.wikipedia.org/wiki/痴呆

Enkephalinase inhibitors: Amastatin. *BL-2401. *Candoxatril. *D -Phenylalanine. *Dexecadotril (retorphan). *Ecadotril ( ...

https://en.wikipedia.org/wiki/Nalorphine_dinicotinate

Older examples of inhibitors mentioned in the literature include oudenone[45] and aquayamycin.[46] ... Ono M, Okamoto M, Kawabe N, Umezawa H, Takeuchi T (Mar 1971). "Oudenone, a novel tyrosine hydroxylase inhibitor from microbial ... Monoamine reuptake inhibitors • Monoamine releasing agents • Monoamine neurotoxins ...

https://en.wikipedia.org/wiki/Tyrosine_3-monooxygenase

Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and ... Augustinsson, K.-B. (1948). "Cholinesterases. A study in comparative enzymology". Acta Physiol. Scand. 15, Suppl. 2: -. ... Pohanka (2011). "Cholinesterases, a target of pharmacology and toxicology". Biomedical Papers Olomouc 155 (3): 219-229.doi: ... Massoulié J, Perrier N, Noureddine H, Liang D, Bon S (2008). "Old and new questions about cholinesterases". Chem Biol Interact ...

https://sh.wikipedia.org/wiki/Acetilholinesteraza

Parathion was discovered by scientists at IG Farben in the 1940s as a cholinesterase inhibitor insecticide. Propoxur is a ... Xarelto (rivaroxaban) is a small molecule inhibitor of Factor Xa, a key enzyme involved in blood coagulation. In the United ... Trasylol (Aprotinin) Trasylol is a trypsin inhibitor used to control bleeding during major surgery. In a 2006 meeting called by ... Nexavar (sorafenib) is a kinase inhibitor used in the treatment of liver cancer (hepatocellular carcinoma), kidney cancer ( ...

https://en.wikipedia.org/wiki/Bayer_CropScience

Such inhibitors of ion channels serve an important research purpose, by allowing scientists to "turn off" specific channels at ... Main articles: Neuromuscular junction, Acetylcholine receptor, and Cholinesterase enzyme. A special case of a chemical synapse ... However, such inhibitors also make effective neurotoxins, and have been considered for use as chemical weapons. Neurotoxins ... If Xenopus neurons are grown in an environment with RNA synthesis or protein synthesis inhibitors that transition is prevented. ...

https://en.m.wikipedia.org/wiki/Action_potentials

Raina P, Santaguida P, Ismaila A, et al. (2008). "Effectiveness of cholinesterase inhibitors and memantine for treating ... Birks J; Birks, Jacqueline (2006). "Cholinesterase inhibitors for Alzheimer's disease". Cochrane Database Syst Rev (1): ... Stahl SM (2000). "The new cholinesterase inhibitors for Alzheimer's disease, Part 2: illustrating their mechanisms of action". ... Raschetti R, Albanese E, Vanacore N, Maggini M (2007). "Cholinesterase inhibitors in mild cognitive impairment: a systematic ...

https://sw.wikipedia.org/wiki/Ugonjwa_wa_Alzheimer

Cholinesterase *Acetylcholinesterase. *Butyrylcholinesterase. *Pectinesterase. *6-phosphogluconolactonase. *PAF acetylhydrolase ...

https://en.wikipedia.org/wiki/Glucose_6-phosphatase

20 Muscle relaxants (peripherally-acting) and cholinesterase inhibitors. *21 Eye preparations *21.1 Anti-infective agents ...

https://en.wikipedia.org/wiki/List_of_World_Health_Organization_Essential_Medicines

Pohanka M (2011). "Cholinesterases, a target of pharmacology and toxicology". Biomedical Papers Olomouc. 155 (3): 219-229. doi: ... Endogeni inhibitor bola u neuronima je Mir-132 micRNK, što može ograničiti upale u mozgu kao ublažavanje ekspresije ovog ... Augustinsson, K.-B. (1948). "Cholinesterases. A study in comparative enzymology". Acta Physiol. Scand. 15, Suppl. 2: -.. .mw- ... Pohanka (2011). "Cholinesterases, a target of pharmacology and toxicology". Biomedical Papers Olomouc 155 (3): 219-229.doi: ...

https://bs.wikipedia.org/wiki/Acetilholinesteraza

AD inhibitor (Disulfiram. *Calcium carbimide. *Hydrogen cyanamide). *Acamprosate. *Opioid antagonists *Naltrexone. *Nalmefene) ...

https://en.wikipedia.org/wiki/Opioid_antagonist

This cholinesterase inhibitor is not listed in the Annex on Chemicals to the Convention. ... the biomarkers of the cholinesterase inhibitor found in Mr Navalny's blood and urine samples have similar structural ... the OPCW confirmed the presence of a cholinesterase inhibitor from the Novichok group in Navalny's blood and urine samples.[7][ ... clinical findings indicated poisoning with a substance from the group of with a cholinesterase inhibitor, and that they would ...

https://en.wikipedia.org/wiki/Poisoning_of_Alexei_Navalny

This can be a factor in choosing an agent in patients with liver failure,[56] although since cholinesterases are produced in ... ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics *Statins. *Fibrates. *Bile acid ...

https://en.wikipedia.org/wiki/Local_anesthetic

Also indirect D2 agonists, such as dopamine reuptake inhibitors (cocaine, methylphenidate), releasing agents (amphetamine, ...

https://en.wikipedia.org/wiki/Nalorphine

Birks J (January 2006). Birks J (ed.). "Cholinesterase inhibitors for Alzheimer's disease". The Cochrane Database of Systematic ... Stahl SM (November 2000). "The new cholinesterase inhibitors for Alzheimer's disease, Part 2: illustrating their mechanisms of ... "Cholinesterase inhibitors in mild cognitive impairment: a systematic review of randomised trials". PLoS Medicine. 4 (11): e338 ... "Effectiveness of cholinesterase inhibitors and memantine for treating dementia: evidence review for a clinical practice ...

https://en.m.wikipedia.org/wiki/Alzheimer's

Cholinesterase inhibitors for Alzheimer's disease». The Cochrane Database of Systematic Reviews (1): CD005593. PMID 16437532. ... Birks J (2006). «Cholinesterase inhibitors for Alzheimer's disease». The Cochrane Database of Systematic Reviews (1): CD005593 ... Raschetti R, Albanese E, Vanacore N, Maggini M (2007). «Cholinesterase inhibitors in mild cognitive impairment: a systematic ... Stahl SM (2000). «The new cholinesterase inhibitors for Alzheimer's disease, part 2: illustrating their mechanisms of action». ...

https://pt.m.wikipedia.org/wiki/Alzheimer

Cholinesterase inhibitorsEdit. Main article: Cholinesterase inhibitors. Many ACh receptor agonists work indirectly by ... Many toxins and venoms produced by plants and animals also contain cholinesterase inhibitors. In clinical use, they are ... Synthesis inhibitorsEdit. Organic mercurial compounds, such as methylmercury, have a high affinity for sulfhydryl groups, which ... Release inhibitorsEdit. Botulinum toxin (Botox) acts by suppressing the release of acetylcholine, whereas the venom from a ...

https://en.m.wikipedia.org/wiki/Acetylcholine

Birks, J. (2006). "Cholinesterase inhibitors for Alzheimer's disease". The Cochrane Database of Systematic Reviews (1): ...

https://en.wikipedia.org/wiki/Medicinal_plants

... and parathion into inhibitors of cholinesterase by mammalian liver". The Biochemical Journal. 61 (2): 203-9. doi:10.1042/ ... Schradan itself is a weak cholinesterase inhibitor and requires metabolic activation to become active.[2] ...

https://en.wikipedia.org/wiki/Schradan

... is not easily metabolized by cholinesterase, it has a 2 to 5 minute onset of action and its duration of action is 4 ... Carbonic anhydrase inhibitors/. (sulfonamides). *Acetazolamide. *Brinzolamide (+timolol). *Diclofenamide. *Dorzolamide (+ ...

https://en.wikipedia.org/wiki/Carbachol

Increase motivation through use of stimulants, dopamine agonists, or other agents such as cholinesterase inhibitors. ...

https://en.wikipedia.org/wiki/Abulia

... a natural cholinesterase inhibitor from Chinese herbal medicine". Acta Pharmacologica Sinica. 27 (1): 1-26. doi:10.1111/j.1745- ... Huperzine A is extracted from Huperzia serrata.[2] It is a reversible acetylcholinesterase inhibitor[6][7][8][9] and NMDA ... Tang X, He X, Bai D (1999). "Huperzine A: A novel acetylcholinesterase inhibitor". Drugs of the Future. 24 (6): 647. doi: ... there may be possible additive cholinergic effects if huperzine A is taken with other acetylcholinesterase inhibitors or ...

https://en.wikipedia.org/wiki/Huperzine_A

Cholinesterase Inhibitors was found in Washington Manual. The Washington Manual of Medical Therapeutics helps you diagnose and ...

https://www.unboundmedicine.com/washingtonmanual/search?q=Cholinesterase%20Inhibitors

Impact of Cholinesterase Inhibitors on Driving Ability in Healthy Older Adults. The safety and scientific validity of this ...

https://www.clinicaltrials.gov/ct2/show/results/NCT00482001

QSAR Models towards Cholinesterase Inhibitors for the Treatment of Alzheimers Disease: 10.4018/978-1-4666-8136-1.ch010: ... "QSAR Models towards Cholinesterase Inhibitors for the Treatment of Alzheimers Disease." In Quantitative Structure-Activity ... "QSAR Models towards Cholinesterase Inhibitors for the Treatment of Alzheimers Disease." Quantitative Structure-Activity ... QSAR Models towards Cholinesterase Inhibitors for the Treatment of Alzheimers Disease. C. Gopi Mohan (Amrita Institute of ...

https://www.igi-global.com/chapter/qsar-models-towards-cholinesterase-inhibitors-for-the-treatment-of-alzheimers-disease/124475

Despite recognition that cholinesterase inhibitors can provide clinical benefits for patients with Alzheimers disease (AD), ... In such cases, pharmacological differences between available cholinesterase inhibitors provide a good rationale to switch to ... suggesting that a previous failure to respond to another cholinesterase inhibitor did not predict response to galantamine. On ... of available data it is suggested that patients not tolerating or not responding to one particular cholinesterase inhibitor may ...

https://avesis.istanbul.edu.tr/yayin/e14de7c5-1844-4a73-9d96-5ac59f7e406f/switching-cholinesterase-inhibitors-in-patients-with-alzheimers-disease

Cholinesterase inhibitors slow decline in function in Alzheimers Disease (AD): A 2-year observational study in the Sunnybrook ...

https://experts.mcmaster.ca/display/publication1640113

For debate: is the evidence for the efficacy of cholinesterase inhibitors in the symptomatic treatment of Alzheimers disease ... For debate: is the evidence for the efficacy of cholinesterase inhibitors in the symptomatic treatment of Alzheimers disease ... Humans, Alzheimer Disease, Galantamine, Piperidines, Indans, Cholinesterase Inhibitors, Treatment Outcome, Severity of Illness ...

https://www.ndorms.ox.ac.uk/publications/542434

Use with Cholinomimetics and Other Cholinesterase Inhibitors: A synergistic effect may be expected when cholinesterase ... Overdosage with cholinesterase inhibitors can result in cholinergic crisis characterized by severe nausea, vomiting, salivation ... Use with Anticholinergics: Because of their mechanism of action, cholinesterase inhibitors have the potential to interfere with ... Anesthesia: ARICEPT®, as a cholinesterase inhibitor, is likely to exaggerate succinylcholine-type muscle relaxation during ...

https://www.healthyplace.com/alzheimers/medications/aricept-cholinesterase-inhibitor

Cholinesterase Inhibitor? A cholinesterase inhibitor used in the treatment of Alzheimers Disease. Usage, dosage, side-effects ... Use with Cholinomimetics and Other Cholinesterase Inhibitors: A synergistic effect may be expected when cholinesterase ... Exelon is a cholinesterase Inhibitor used in the treatment of Alzheimers Disease. Usage, dosage, side-effects of Exelon. ... Exelon as a cholinesterase inhibitor, is likely to exaggerate succinylcholine-type muscle relaxation during anesthesia. ...

https://www.healthyplace.com/alzheimers/medications/exelon-cholinesterase-inhibitor

This Initial Check will help you assess your current knowledge and skill level about cholinesterase inhibitors. To take the ... While laboratory tests can be used to estimate the exposure to cholinesterase inhibitors (cholinesterase levels and direct ... and Serum Cholinesterase and Direct Measurement of Cholinesterase Inhibitors and Their Metabolic Byproducts. ... This Initial Check will help you assess your current knowledge and skill level about cholinesterase inhibitors. To take the ...

https://www.atsdr.cdc.gov/csem/cholinesterase-inhibitors/initial_check.html

Literature Cited in Cholinesterase Inhibitors: Including Insecticides and Chemical Warfare Nerve Agents ... De Wilde V, Vogelaers D, Colardyn F. Prompt recovery from severe cholinesterase-inhibitor poisoning-remarks on classification ... Namba T. Cholinesterase inhibition by organophosphorus compounds and its clinical effects. Bulletin of the World Health ... Karalliedde L. Cholinesterase estimations revisited: the clinical relevance. European Journal of Anaesthesiology. May 2002;19(5 ...

https://www.atsdr.cdc.gov/csem/cholinesterase-inhibitors/literature_cited.html

Cholinesterase Inhibitors answers are found in the Washington Manual of Medical Therapeutics powered by Unbound Medicine. ... Cholinesterase inhibitors are chemical compounds that inhibit the enzyme cholinesterase. Blockade of AChE function leads to ... Cholinesterase inhibitors are chemical compounds that inhibit the enzyme cholinesterase. Blockade of AChE function leads to ... Cholinesterase Inhibitors. In: Bhat PP, Dretler AA, Gdowski MM, et al, eds. Washington Manual of Medical Therapeutics. Wolters ...

https://www.unboundmedicine.com/washingtonmanual/view/Washington-Manual-of-Medical-Therapeutics/602687/1/Cholinesterase_Inhibitors

Cholinesterase inhibitors may be added to memantine for further beneficial effects on behavioral symptoms and other symptoms of ... Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract ... The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are ...

https://www.drugbank.ca/categories/DBCAT000815

Cholinesterase inhibitors. Class Summary. Cholinesterase inhibitors may be effective in temporarily reversing muscle weakness ... Neostigmine is a longer-acting cholinesterase inhibitor that can be used if a trial of edrophonium is effective; it inhibits ... Evidence supports the trial of cholinesterase-inhibiting drugs, such as edrophonium or neostigmine, as a temporizing measure in ...

https://emedicine.medscape.com/article/771918-medication

The use of cholinesterase inhibitors (ChEIs) has exploded in just a few years, producing golden eggs for several pharmaceutical ... Cholinesterase inhibitor treatment alters the natural history of Alzheimers disease. J Neurol Neurosurg Psychiatry. 2002 Mar; ... Cholinesterase inhibitor treatment alters the natural history of Alzheimers disease. J Neurol Neurosurg Psychiatry. 2002 Mar; ... Cholinesterase Inhibitors Not What Theyre Cracked Up To Be?. Quick Links. *Article ...

https://www.alzforum.org/news/research-news/cholinesterase-inhibitors-not-what-theyre-cracked-be

Cholinesterase inhibitors produce a small benefit on several cognitive and noncognitive function scales. Although data for ... with a cholinesterase inhibitor at the usual recommended dose was compared with placebo or another cholinesterase inhibitor for ... Patients taking a cholinesterase inhibitor are more likely to discontinue treatment as a result of adverse reactions than are ... More patients leave cholinesterase inhibitor treatment groups (29 percent) on account of adverse events than leave the placebo ...

https://www.aafp.org/afp/2006/0901/p747.html

Alzheimer Disease Cholinesterase Inhibitors Drug: cholinesterase inhibitors (CI) (donepezil, galantamine or rivastigmine) Phase ... Cholinesterase Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. Cholinergic Agents. ... Comparison of Therapeutic Strategies With Cholinesterase Inhibitors (SOS TRIAL). The safety and scientific validity of this ... Cholinesterase inhibitors (CI) remain the only drugs with a recognized efficacy in mild to moderate Alzheimers disease (AD) in ...

https://clinicaltrials.gov/ct2/show/study/NCT03454646?term=alzheimer+dijon&rank=14

Methods: Adherence and persistence with cholinesterase inhibitors were assessed by data linkage us ... persistence and continuation beyond 6 months with cholinesterase inhibitors in Australians with Alzheimers disease. ... Aim: To determine adherence, persistence and continuation beyond 6 months with cholinesterase inhibitors in Australians with ... Methods: Adherence and persistence with cholinesterase inhibitors were assessed by data linkage using the Pharmaceutical ...

http://www.biomedsearch.com/nih/Adherence-persistence-continuation-with-cholinesterase/22950587.html

Cholinesterase inhibitors for rarer dementia associated with neurological conditions]. There are various rarer dementias ... The other study found that cholinesterase inhibitor use in the medium-term improved the results of the verbal fluency test (1 ... Cholinesterase inhibitors had no significant impact on improving cognitive level, activities of daily living and quality of ... Cholinesterase inhibitors are beneficial for people with Parkinsons disease and dementia. *Rivastigmine appears to moderately ...

https://www.cochrane.org/CD009444/DEMENTIA_cholinesterase-inhibitors-for-rarer-dementia-associated-with-neurological-conditions

Impact of Cholinesterase Inhibitors on Driving Ability in Healthy Older Adults. The safety and scientific validity of this ... Impact of Cholinesterase Inhibitors on Driving Ability in Healthy Older Adults Official Title ICMJE The Impact of ... The goal of the study is to assess the role of cholinesterase inhibitors in affecting the driving ability of cognitively intact ... We hypothesize that the use of a cholinesterase inhibitor for two weeks will be associated with improvement in safe driving ...

https://www.clinicaltrials.gov/ct2/show/record/NCT00482001?view=results

... guidance does not recommend the use of memantine in combination with cholinesterase inhibitors (acetylcholinesterase inhibitor ... Function (ACDS-ADL19 and ADCS-ADL23). ChEI, cholinesterase inhibitor; ER, extended release; LOCF, last observation carried ... To cite: Farrimond LE, Roberts E, McShane R. Memantine and cholinesterase inhibitor combination therapy for Alzheimers disease ... Memantine and cholinesterase inhibitor combination therapy for Alzheimers disease: a systematic review ...

https://bmjopen.bmj.com/content/2/3/e000917

Effects of Gingko biloba supplementation in Alzheimers disease patients receiving cholinesterase inhibitors: data from the ... associated with additional cognitive and functional benefit in AD patients already in treatment with cholinesterase inhibitors ...

https://www.ncbi.nlm.nih.gov/pubmed/24548724

Cholinesterase Inhibitors. Class Summary. Cholinesterase inhibitors (ChEIs) are used to palliate cholinergic deficiency. All 4 ... Cholinesterase inhibitor treatment and urinary incontinence in Alzheimers disease. J Am Geriatr Soc. 2007 May. 55(5):800-1. [ ... The mainstay of therapy for patients with Alzheimer disease (AD) is the use of centrally acting cholinesterase inhibitors to ... Syncope and its consequences in patients with dementia receiving cholinesterase inhibitors: a population-based cohort study. ...

https://emedicine.medscape.com/article/1134817-medication

Objective: To investigate the possibility that response to cholinesterase inhibitor therapy could be predicted by easily ... This was a cohort study of 160 consecutive outpatients with probable Alzheimers disease who commenced cholinesterase inhibitor ... of MTL thickness derived from CT scanning may be useful in improving the prediction of response to cholinesterase inhibitors in ...

http://connection.ebscohost.com/c/articles/16911284/predicting-outcome-cholinesterase-inhibitor-treatment-alzheimers-disease

Sustained treatment with a cholinesterase inhibitor (ChEI) is used in the management of the symptoms of Alzheimers disease (AD ... Comparison of Cholinesterase Inhibitor Utilization Patterns and Associated Health Care Costs in Alzheimers Disease. ... Comparison of Cholinesterase Inhibitor Utilization Patterns and Associated Health Care Costs in Alzheimers Disease ... Mark, T., Mucha, L., Want, S. S., Cuffel, B., McRae, T., & Del Valle, M. (2008). Comparison of Cholinesterase Inhibitor ...

https://www.rti.org/publication/comparison-cholinesterase-inhibitor-utilization-patterns-and-associated-health-care

Immobilized cholinesterases capillary reactors on-flow screening of selective inhibitors.. [Adriana Ferreira Lopes Vilela, ... The discovery of selective inhibitors for acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) is extremely important ... there is a growing interest in developing rapid and effective assays techniques for cholinesterases (ChE) enzymes ligand ...

https://www.sigmaaldrich.com/catalog/papers/24321276

Resistance to Inhibitors of Cholinesterase 3 (Ric-3) Expression Promotes Selective Protein Associations with the Human α7- ... Resistance to Inhibitors of Cholinesterase 3 (Ric-3) Expression Promotes Selective Protein Associations with the Human α7- ... Resistance to Inhibitors of Cholinesterase 3 (Ric-3) Expression Promotes Selective Protein Associations with the Human α7- ... Resistance to Inhibitors of Cholinesterase 3 (Ric-3) Expression Promotes Selective Protein Associations with the Human α7- ...

https://www.ncbi.nlm.nih.gov/pubmed/26258666

Treated with Cholinesterase Inhibitor. Julia Kheifets, Boris Rozhavsky, Zehava Girsh Solomonovich, Rodman Marianna, and Arie ... cholinesterase inhibitors have been suggested but not tested adequately [3]. Prognosis is good if the patient arrives at the ... a decision was made to treat the patient with a cholinesterase inhibitor. During the first 24 hours the patient received 4 ... and life-threatening TTX poisoning caused by consumption of Lagocephalus sceleratus and treated by cholinesterase inhibitor to ...

https://www.hindawi.com/journals/cricc/2012/782507/

A treatment option for Dementia is cholinesterase Inhibitors. It can be thought of as the drug that inhibits the enzyme that ... Similarly, a cholinesterase inhibitor Cholinesterase inhibitor. A drug which stops the effect of cholinesterase can be thought ... Cholinesterase Inhibitors. Acetyl Choline Acetyl choline. A neurotransmitter released in synapse that is active in the ... It is a cholinesterase inhibitor, making it a drug from the main class of compounds now used to treat people with Alzheimers ...

https://www.dementiaguide.com/aboutdementia/treatments/?pageContent=cholinesterase_inhibitors

Do cholinesterase inhibitors lead to weight loss in older adults with dementia? Heres a wrap up of a large study of patients ... Is cholinesterase inhibitor therapy associated with clinically significant weight loss? Cholinesterase inhibitors are commonly ... Do cholinesterase inhibitors lead to weight loss in older adults with dementia? Heres a wrap up of a large study of patients ... Cholinesterase inhibitors are prescribed often in part because there are no good treatments for dementia, and they are seen as ...

https://www.psychiatrictimes.com/view/weight-loss-associated-cholinesterase-inhibitors-elderly

Efficacy of cholinesterase inhibitors (ChI) in Alzheimers dementia is well established. However, treatment with ChI in ... "Effects of Cholinesterase Inhibitors in Cognition on Parkinsons Disease Dementia: A Systematic Review and Meta-Analysis" ...

https://scirp.org/journal/papercitationdetails.aspx?PaperID=61227&JournalID=1574

To Evaluate the Safety and Effectiveness of Atorvastatin Plus a Cholinesterase Inhibitor in AD Patients.. The safety and ... The purpose of this study is to find out if atovastatin, when taken with a cholinesterase inhibitor, is effective for treating ... To Evaluate the Safety and Effectiveness of Atorvastatin Plus a Cholinesterase Inhibitor in AD Patients.. ... the Efficacy and Safety of Atorvastatin 80 MG Plus an Acetylcholinesterase Inhibitor Versus an Acetylcholinesterase Inhibitor ...

https://clinicaltrials.gov/ct2/show/record/NCT00151502?show_locs=Y

No convincing evidence from one trial of the efficacy of cholinesterase inhibitors for delirium. Delirium is a confusional ... Cholinesterase inhibitors enhance the cholinergic system and there have been reports that they might be beneficial in treating ... Each cholinesterase inhibitor was to be examined separately and together as a group. ... Further trials using cholinesterase inhibitors for the treatment of delirium are needed. ...

http://www.cochrane.org/CD005317/DEMENTIA_no-convincing-evidence-from-one-trial-of-the-efficacy-of-cholinesterase-inhibitors-for-delirium

Use of a cholinesterase inhibitor. Patients were censored if they stopped using the drug (drug cohort) or started using the ... Cholinesterase inhibitors were associated with increased risk for syncope and its consequences in older persons with dementia ... Hirsch C. Cholinesterase inhibitors were associated with increased risk for syncope and its consequences in older persons with ... Review: Cholinesterase inhibitors do not prevent dementia in patients with mild cognitive impairment Annals of Internal ...

https://annals.org/aim/article-abstract/1032760/cholinesterase-inhibitors-were-associated-increased-risk-syncope-its-consequences-older

Effects of a central cholinesterase inhibitor on reducing falls in Parkinson disease. Kathryn A. Chung, Brenna M. Lobb, John G ... Objective: To investigate if a central cholinesterase inhibitor will reduce falling frequency in subjects with Parkinson ... Effects of a central cholinesterase inhibitor on reducing falls in Parkinson disease ...

http://n.neurology.org/content/75/14/1263

Memantine Plus Cholinesterase Inhibitors Improves Psychosis, Neurobehavioral Symptoms in Alzheimer Disease. Share this content: ... CHICAGO - Cholinesterase inhibitors (ChEIs) plus memantine (MEM) may provide a significant benefit for psychosis and ... The effects of memantine added to cholinesterase inhibitors on NPI behavioral domains: pooled post hoc analysis of 3 randomized ...

https://www.neurologyadvisor.com/aaic-2018/alzheimers-disease-psychosis-behavioral-symptoms-treated-with-memantine-cholinesterase-inhibitors/article/782512/

The pharmacological properties of rivastigmine, a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase, and donepezil and galantamine, two AChE-selective inhibitors, are reviewed. (istanbul.edu.tr)
A post hoc analysis of a 5-month trial with galantamine showed that patients had similar efficacy outcomes, whether or not they had received prior anticholinesterase therapy, suggesting that a previous failure to respond to another cholinesterase inhibitor did not predict response to galantamine. (istanbul.edu.tr)

All target compounds are potent acetyl- (AChE) and butyrylcholinesterase (BChE) inhibitors in the nanomolar concentration range. (uni-regensburg.de)
The photoswitchable inhibitor identified might serve as valuable molecular tool to investigate the different biological properties of AChE as well as its role in pathogenesis of AD in in vitro assays. (uni-regensburg.de)

QSAR Models towards Cholinesterase Inhibitors for the Treatment of Alzheimer's Disease. (igi-global.com)
Despite recognition that cholinesterase inhibitors can provide clinical benefits for patients with Alzheimer's disease (AD), the average durations of treatment and beneficial effects are not optimal in all cases. (istanbul.edu.tr)
For debate: is the evidence for the efficacy of cholinesterase inhibitors in the symptomatic treatment of Alzheimer's disease convincing or not? (ox.ac.uk)

Photochromic cholinesterase inhibitors were obtained from cis-1,2-α-dithienylethene-based compounds by incorporating one or two aminopolymethylene tacrine groups. (uni-regensburg.de)
Reversible inhibitors, edrophonium (Tensilon) and tacrine (Cognex), associate with the choline binding domain. (pharmacology2000.com)

Drugs with acetylcholine-like effects (cholinomimetics ) consist of 2 major subgroups on the basis of their mode of action (ie, whether they act directly at the acetylcholine receptor or indirectly through inhibition of cholinesterase). (mhmedical.com)

In such cases, pharmacological differences between available cholinesterase inhibitors provide a good rationale to switch to another drug in the same class. (istanbul.edu.tr)

Neostigmine is a prototype for the indirect-acting cholinesterase inhibitors. (mhmedical.com)
Physostigmine and Neostigmine are acetylcholinesterase inhibitors that form a moderately stable carbamyl-enzyme derivative. (pharmacology2000.com)

Organophosphate acetylcholinesterase inhibitors, such as diisopropyl fluorophosphate (DFP) form stable phosphorylated serine derivatives. (pharmacology2000.com)

Some reversible inhibitors, propidium and fasiculin, a toxic peptide, bind at the peripheral anionic site. (pharmacology2000.com)
Examples of 'reversible' acetylcholinesterase inhibitors that may be used clinically include both carbamylating agents and those that associate only with the choline binding domain. (pharmacology2000.com)
In the case of myasthenia gravis, typically fast-acting reversible acetylcholinesterase inhibitors help with assessing the extent of neuromuscular dysfunction of the disease. (pharmacology2000.com)

This chapter focuses on different Quantitative Structure-Activity Relationship (QSAR) studies carried out for a variety of cholinesterase inhibitors for the treatment of AD. (igi-global.com)

Effectiveness of acetylcholinesterase inhibitors: diagnosis and severity as predictors of response in routine practice. (ox.ac.uk)

The underlying rationale for these concerns is that when acetylcholinesterase inhibitors are administered, the effect is to increase acetylcholine concentration enhancing cholinergic tone or cholinergic effect. (pharmacology2000.com)

For example, acetylcholinesterase inhibitors because they increase local acetylcholine concentration in the heart would be expected to reduce heart rate, just as the physiological transmitter, acetylcholine, would normally cause. (pharmacology2000.com)

In vitro and in vivo studies demonstrate that the inhibition of cholinesterase by rivastigmine is not affected by the concomitant administration of memantine, an N-methyl-D-aspartate receptor antagonist. (healthyplace.com)
CHICAGO - Cholinesterase inhibitors (ChEIs) plus memantine (MEM) may provide a significant benefit for psychosis and neurovegetative behavioral syndromes in patients with Alzheimer disease, according to results of a post-hoc analysis presented at the 2018 Alzheimer's Association International Conference , July 22-26, 2018, in Chicago, Illinois. (neurologyadvisor.com)
Cummings JL, Grossberg GT, Porsteinsson AP, Hendrix S, Ellison N, Kerolous M. The effects of memantine added to cholinesterase inhibitors on NPI behavioral domains: pooled post hoc analysis of 3 randomized controlled trials in patients with moderate to severe AD. (neurologyadvisor.com)
Some of the most commonly prescribed medications used to treat symptoms of AD are cholinesterase inhibitors and memantine. (healthline.com)
Memantine isn't a cholinesterase inhibitor, but it also acts on chemicals in the brain. (healthline.com)
In fact, memantine is often prescribed in combination with a cholinesterase inhibitor. (healthline.com)
The U.S. Food and Drug Administration (FDA) has approved two types of medications - cholinesterase inhibitors (Aricept, Exelon, Razadyne) and memantine (Namenda) - to treat the cognitive symptoms (memory loss, confusion, and problems with thinking and reasoning) of Alzheimer's disease. (alz.org)
There is also a medication that combines one of the cholinesterase inhibitors (donepezil) with memantine called Namzaric. (alz.org)
There is some evidence that individuals with moderate to severe Alzheimer's who are taking a cholinesterase inhibitor might benefit by also taking memantine. (alz.org)
A medication that combines memantine and a cholinesterase inhibitor is available. (alz.org)
Cholinesterase inhibitors , such as rivastigmine and memantine , have demonstrated efficacy in the treatment of behavioral symptoms among patients with DLB, and they are the first-line pharmacologic agents for the management of DLB. (wikidoc.org)

This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. (healthyplace.com)
The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. (drugbank.ca)
When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. (drugbank.ca)
Cholinesterase inhibitors are hypothesised to work by inhibiting the enzyme acetylcholinesterase (AChE) which breaks down the neurotransmitter acetylcholine. (cochrane.org)
The mainstay of therapy for patients with Alzheimer disease (AD) is the use of centrally acting cholinesterase inhibitors to attempt to compensate for the depletion of acetylcholine (ACh) in the cerebral cortex and hippocampus. (medscape.com)
Resistance to Inhibitors of Cholinesterase 3 (Ric-3) Expression Promotes Selective Protein Associations with the Human α7-Nicotinic Acetylcholine R. (nih.gov)
drugs that prevent the degradation of acetylcholine by acetylcholinesterase (also known simply as cholinesterase). (brainscape.com)
It was significantly increased by 1 mM physostigmine (alone or in the presence of acetylcholine) but not by other inhibitors of cholinesterase (neostigmine or edrophonium). (aspetjournals.org)
Cholinesterase breaks apart the neurotransmitter acetylcholine, which is vital for the transmission of nerve impulses. (encyclopedia.com)
Cholinesterase inhibitors are used to reduce the action of cholinesterase, thereby making more acetylcholine available to nerve cells in the brain. (encyclopedia.com)
The use of cholinesterase inhibitors impedes the normal enzymatic breakdown of the little acetylcholine that is present. (encyclopedia.com)
These are not autoimmune disorders, but are caused by defective genes that control proteins in the acetylcholine receptor or in acetyl-cholinesterase. (encyclopedia.com)
We hypothesise that skin vascular response to iontophoresis of acetylcholine, which is partly determined by the level of cholinesterase activity, may be a pre-treatment measure that could predict response to therapy. (biomedcentral.com)
Twenty-four people with probable AD underwent iontophoresis of acetylcholine to the volar surface of the forearm skin prior to treatment with a cholinesterase inhibitor. (biomedcentral.com)
We therefore hypothesised that a person with a relatively fast acetylcholine recovery response could be expected to have high cholinesterase activity and therefore might be a good candidate for response to cholinesterase inhibitor treatment. (biomedcentral.com)
This study attempts to identify the characteristic pattern of change in peripheral blood flow following exposure to iontophoresis of a standard dose of acetylcholine and assess its association with response to cholinesterase inhibitor therapy in people with AD. (biomedcentral.com)
Cholinesterase inhibitors work by increasing acetylcholine, a chemical in your brain that aids in memory and judgment. (healthline.com)
Cholinesterase (Also known as Acetylcholinesterase or AChE) is the enzyme by which Acetylcholine is hydrolyzed, or broken down. (nootriment.com)
Because Cholinesterase, or AChE, targets Acetylcholine in order to break it down, it causes less to be available at any given time. (nootriment.com)
Once Acetylcholine has been released into the synapse, Cholinesterase is there to break it down. (nootriment.com)
Symptomatic treatment for AD and LBD includes cholinesterase inhibitors (ChEIs), which increase synaptic levels of the neurotransmitter, acetylcholine. (biomedcentral.com)
Cholinesterase inhibitors keep acetylcholine around longer at the neuromuscular junction but also in the autonomic nervous system (which controls involuntary bodily functions). (mda.org)
Additionally, cholinesterase inhibitors that are used in myasthenia gravis (MG) , are also used in LEMS to help with symptoms by keeping the chemical acetylcholine around longer at the neuromuscular junction. (mda.org)
Cholinesterase inhibitors block the action of acetylcholinesterase, the enzyme that breaks down acetylcholine. (mda.org)
IT is known that the cholinesterases from various animal tissues are not identical, and it has been proposed that two types of acetylcholine-splitting enzymes exist. (nature.com)
The enzymes from brain and red cells are said to be 'specific' cholinesterases, and in addition a 'non-specific' cholinesterase is said to exist, for example, in human serum, whicji hydrolyses acetylcholine as well as aliphatic esters, for example, tributyrin. (nature.com)
One treatment strategy to enhance the cholinergic function is the use of acetylcholinesterase (AChE, EC 3.1.1.7) inhibitors to increase the amount of acetylcholine, which is present in the synapses between cholinergic neurons [ 6 ]. (mdpi.com)

Cholinesterase inhibitors enhance the cholinergic system and there have been reports that they might be beneficial in treating delirium. (cochrane.org)
Cholinesterase inhibitor toxicity can cause a life-threatening cholinergic crisis. (brainscape.com)
INTRATHECAL administration of cholinergic receptor agonists or cholinesterase inhibitors have an antinociceptive effect in a dose-dependent manner, which is mediated by spinal muscarinic receptors in animals, and this analgesic effect has been confirmed in human studies. (asahq.org)
Therefore, the current study was designed (1) to characterize the effects of spinal cholinesterase inhibitors on nerve injury-induced tactile allodynia and [2] to define the pharmacologic nature of the cholinergic receptors that mediate the effects of this family of agents. (asahq.org)
Through their primary action, cholinesterase inhibitors may be expected to increase gastric acid secretion due to increased cholinergic activity. (drugs.com)
Thus, the focus herein is upon selective cholinesterase (ChE) inhibitors in order to alleviate cholinergic deficits and improve neurotransmission. (mdpi.com)
Cholinergic dysfunction, demonstrated in the late 1970s and early 1980s, led to the introduction of acetylcholinesterase inhibitors (AChEIs) in 1993 (Tacrine) to enhance cholinergic neurotransmission as the first line of treatment against Alzheimer's disease (AD). (cdc.gov)

The first cholinesterase inhibitor (ChEI) approved specifically to treat symptoms of AD was tacrine, but it is no longer used. (biomedcentral.com)
Phenserine, a recently developed cholinesterase inhibitor (ChEI), has been reported to reduce APP levels in vitro and in vivo . (pnas.org)
Phenserine is a recently developed cholinesterase inhibitor (ChEI) currently in clinical trials for treatment of mild to moderate AD. (pnas.org)

One symptom that benefits from the use of cholinesterase inhibitors is called cognition. (encyclopedia.com)
Overall, however, it appears that the cholinesterase inhibitors result in mild improvements in cognition without change in parkinsonian features . (doctorabel.us)

Isosorbide-2-carbamate-5-esters are highly potent and selective butyrylcholinesterase inhibitors with potential utility in the treatment of Alzheimer?s Disease (AD). (tcd.ie)

Cholinesterase inhibitors produce a small benefit on several cognitive and noncognitive function scales. (aafp.org)
The beneficial effect of cholinesterase inhibitors on cognitive function was only observed on a few cognitive function tests for patients with HD, CADASIL or MS. Cholinesterase inhibitors had no significant impact on improving cognitive level, activities of daily living and quality of life in patients with these conditions. (cochrane.org)
Studies that have charted the time course of cognitive changes after taking the various cholinesterase inhibitors have demonstrated that improvements tend to peak about three months after the particular drug is first taken. (encyclopedia.com)
How effective and safe are cholinesterase inhibitors for mild cognitive impairment? (bmj.com)
This makes the inhibition of Cholinesterase an obvious target for enhancing one's cognitive abilities. (nootriment.com)

Subjects above the cut off point for both measures were more likely to be classified as good responders than subjects with only one or no values above the respective cut off points (Ï‡2 = 10.61, df = 1, p=0.001) Conclusions: The DSST and a measure of MTL thickness derived from CT scanning may be useful in improving the prediction of response to cholinesterase inhibitors in subjects with AD. (ebscohost.com)
In particular, we sought to determine whether there a difference over 6 months in the magnitude of change in blood flow between people with AD classed as "responders" or "non-responders" to cholinesterase inhibitor therapy and whether blood flow responses prior to treatment predict response to cholinesterase inhibitors in patients with AD. (biomedcentral.com)

The acute dosage of a cholinesterase inhibitor of 10-7M inhibits acetyl cholinesterase and kills the insect by shutting off its nerves. (stopwestnilesprayingnow.org)
Malathion is an organophosphorous compound that inhibits cholinesterase enzyme activity. (medkoo.com)

ARICEPT® (donepezil hydrochloride) is a reversible inhibitor of the enzyme acetylcholinesterase, known chemically as ( ±)-2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one hydrochloride. (healthyplace.com)

Insecticides containing organophosphates can inhibit cholinesterase and pseudocholinesterase activity. (labtestsonline.org)

More patients leave cholinesterase inhibitor treatment groups (29 percent) on account of adverse events than leave the placebo groups (18 percent). (aafp.org)
There is evidence of more adverse events in total in the patients treated with a cholinesterase inhibitor than with placebo. (aafp.org)
Overall, 78% of patients who started a cholinesterase inhibitor were still taking the drug 12 months later. (psychiatrictimes.com)
Overall, 29% of patients who started cholinesterase inhibitors experienced a weight loss of 10 lb or more in the first year, compared with 23% of the control group. (psychiatrictimes.com)
This corresponds to a number needed to harm of 21 over 1 year, meaning only 21 patients need to be treated with a cholinesterase inhibitor over the course of a year for one patient to experience a 10-lb weight loss. (psychiatrictimes.com)
Clinicians and prescribers should take into account and counsel patients on the possible adverse effects of weight loss when starting a cholinesterase inhibitor, monitor for weight loss if these medications are prescribed, and consider discontinuing cholinesterase inhibitors if significant weight loss occurs. (psychiatrictimes.com)
The decision to prescribe a cholinesterase inhibitor is a complex one and should be made only after a thoughtful and informed discussion with patients and their families about the possible benefits, expected adverse effects, and other risks. (psychiatrictimes.com)
To Evaluate the Safety and Effectiveness of Atorvastatin Plus a Cholinesterase Inhibitor in AD Patients. (clinicaltrials.gov)
Unconfounded, blinded randomised controlled trials, published or unpublished in which treatment with cholinesterase inhibitors was administered and compared with alternative interventions in patients with delirium are included. (cochrane.org)
All outcomes were more frequent in patients who received prescriptions for a cholinesterase inhibitor than in those who did not (Table). (annals.org)
To determine the effect of treatment gaps on the risk of institutionalization or death among community-dwelling elderly patients treated with cholinesterase inhibitors (ChIs). (ovid.com)
On the basis of available data it is suggested that patients not tolerating or not responding to one particular cholinesterase inhibitor may still draw benefits upon switching to another. (istanbul.edu.tr)
ACE inhibitors are used to treat hypertension and heart failure and to protect kidney function in patients with diabetes mellitus. (thefreedictionary.com)
Cholinesterase inhibitors should be prescribed with care to patients with a history of asthma or obstructive pulmonary disease (5.8). (nih.gov)

Evidence supports the trial of cholinesterase-inhibiting drugs, such as edrophonium or neostigmine, as a temporizing measure in a situation of severe cobra venom poisoning with significant neurologic abnormalities until antivenom can be obtained. (medscape.com)
A cholinesterase inhibitor (eg, neostigmine) is used to relieve the crisis. (brainscape.com)

Drugs that inhibit cholinesterases. (drugbank.ca)
ko-lin-S-ter-aze] inhibitors now include three drugs in routine use. (dementiaguide.com)
Cholinesterase inhibitors are drugs that block the activity of an enzyme in the brain called cholinesterase. (encyclopedia.com)
The benefits bestowed by cholinesterase inhibitors last only as long as effective levels of the drugs are present. (encyclopedia.com)
Cholinesterase inhibitors are a new class of supplements and drugs that have been found to offer serious benefits for the way your brain works and stores memories. (nootriment.com)

If you were in TCR's editorial offices, surrounded by boxes of articles about acetylcholinesterase inhibitors (AChEI's), you would quickly develop a sinking sensation. (psychcentral.com)

The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. (nih.gov)
Anti-Cholinesterase Activity of Lycopodium Alkaloids from Vietnamese Huperzia squarrosa (Forst. (mdpi.com)

In moderate-to-severe AD (MMSE ≤15), presence of the BCHE-K variant was associated with late response to cholinesterase inhibitor treatment (P=0.02). (cdc.gov)

Immobilized cholinesterases capillary reactors on-flow screening of selective inhibitors. (sigmaaldrich.com)

What are the three major delayed adverse effects that can follow recovery from the acute cholinesterase toxicity? (cdc.gov)
What is the usual cause of death from acute cholinesterase inhibitor poisoning? (cdc.gov)

The antichymotrypsin, antitrypsin, and anticholinesterase potencies of four homologous series of organophosphorus inhibitors are compared: O-(n-alkyl) methylthiophosphonates, O-(n-alkyl)-S-(n-butyl) methylthiophosphonates, O-(n-alkyl)-S-(β-ethylmercaptoethylene) methylth-iophosphonates, and their methylsulfomethylates. (ovid.com)
In all cases, the antichymotrypsin efficiency was lower, while the antitrypsin-essentially higher than the anticholinesterase activity of the studied inhibitors. (ovid.com)

selective serotonin reuptake inhibitors, tricyclic antidepressants, and monoamine oxidase inhibito. (cram.com)

Donepezil hydrochloride tablets, as a cholinesterase inhibitor, are likely to exaggerate succinylcholine-type muscle relaxation during anesthesia. (drugs.com)

The only clinical indication for the irreversible inhibitors is glaucoma. (brainscape.com)

He is also taking lisinopril, an ACE inhibitor, that blocks the conversion of angiotensin I to angiotensin II (a vasoconstrictor). (cram.com)

The most commonly used cholinesterase inhibitor is pyridostigmine (Mestinon). (mda.org)

Although many types of adverse event were reported, nausea, vomiting, and diarrhea were significantly more frequent in the cholinesterase inhibitor groups than in the placebo groups. (aafp.org)
Given that we know cholinesterase inhibitors cause nausea and anorexia, this finding may not be that surprising. (psychiatrictimes.com)

Cholinesterase inhibitors work to increase the amount of acetyl choline in the brain, where they increase memory performance. (dementiaguide.com)
Cholinesterase inhibitiors work to increase the plasticity of the brain's synapses and have been shown to boost learning skills while affecting the fluid intelligence of the brain. (nootriment.com)

Anatomy2

Organisms2

Diseases7

Chemicals and Drugs67

Analytical, Diagnostic and Therapeutic Techniques and Equipment2

Psychiatry and Psychology9

Phenomena and Processes3

Technology, Industry, Agriculture1

Health Care2

Metrifonate increases neuronal excitability in CA1 pyramidal neurons from both young and aging rabbit hippocampus. (1/1796)

Comparison of two in vitro activation systems for protoxicant organophosphorous esterase inhibitors. (2/1796)

Anaphylactic bronchoconstriction in BP2 mice: interactions between serotonin and acetylcholine. (3/1796)

Efficacy and safety of rivastigmine in patients with Alzheimer's disease: international randomised controlled trial. (4/1796)

The cholinergic hypothesis of Alzheimer's disease: a review of progress. (5/1796)

Comparison between huperzine A, tacrine, and E2020 on cholinergic transmission at mouse neuromuscular junction in vitro. (6/1796)

Central nervous system-mediated hyperglycemic effects of NIK-247, a cholinesterase inhibitor, and MKC-231, a choline uptake enhancer, in rats. (7/1796)

Electron paramagnetic resonance reveals altered topography of the active center gorge of acetylcholinesterase after binding of fasciculin to the peripheral site. (8/1796)

Cholinesterase Inhibitors

Cholinesterases

Phenylcarbamates

Indans

Galantamine

Tacrine

Butyrylcholinesterase

Physostigmine

Acetylcholinesterase

Memantine

Neostigmine

Nootropic Agents

Methomyl

Diazinon

Pyridostigmine Bromide

Piperidines

Edrophonium

Trichlorfon

Alzheimer Disease

Parathion

Organothiophosphorus Compounds

Chlorpyrifos

Sarin

Disulfoton

Insecticides

Soman

Echothiophate Iodide

Paraoxon

Acetylcholine

Aldicarb

Carbamates

Muscarinic Antagonists

Dementia

Chemical Warfare Agents

Parasympathomimetics

Cholinesterase Reactivators

Organophosphorus Compounds

Reality Therapy

Thiocholine

Pseudocholinesterase

Neurotoxicity Syndromes

Aminacrine

Atropine

Choline

Dibucaine

Dopamine Agents

Muscarinic Agonists

Receptors, Muscarinic

Tetraisopropylpyrophosphamide

Dose-Response Relationship, Drug

Lewy Body Disease

Cholinergic Antagonists

Dichlorvos

Organophosphate Poisoning

Mental Status Schedule

Bradycardia

Cholinergic Agents

Pralidoxime Compounds

Succinylcholine

Parasympathetic Nervous System

Brain

Fenitrothion

Carbaryl

Receptors, Cholinergic

Neuropsychological Tests

Dementia, Vascular

Butyrylthiocholine

Cognition Disorders

Acetylthiocholine

Alkaloids

Isoflurophate

Rats, Sprague-Dawley

Double-Blind Method

Excitatory Amino Acid Antagonists

Benzoylcholine

Phosphoramides

Cognition

Receptors, Nicotinic

Neuroprotective Agents

Nicotinic Antagonists