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Cholinesterase Inhibitors

Cholinesterase Inhibitors are a class of pharmaceutical agents that work by blocking the action of cholinesterase enzymes, which are responsible for breaking down the neurotransmitter acetylcholine.
This inhibition leads to an increase in acetylcholine levels in the body, which can have therapeutic effects for conditions such as Alzheimer's disease, myasthenia gravis, and glaucoma.
Cholinesterase Inhibitors are a widely studied and important group of compounds in the field of pharmacology and neuroscience.
They offer potential treatments for a variety of neurological and muscular disorders, and reasearch into their mechanisms and applications is an active area of investigation.

Most cited protocols related to «Cholinesterase Inhibitors»

1
Cognitive Aging in Elderly Type 2 Diabetic Patients
Cited 12 times

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Publication 2014
Aged BLOOD Cholinesterase Inhibitors Cognition Conferences Diabetes Mellitus Diagnosis Ethics Committees, Research Extended Family Family Member Neurologists Patients Physicians Presenile Dementia Primary Care Physicians Psychiatrist Residency
2
ECG Downsampling and HRV Analysis
Cited 10 times
The study utilized ECG signals collected for previously reported research on the utility of HRV in the diagnosis of acute cholinesterase inhibitor poisoning, which involved 83 adult patients who visited an emergency department with the chief complaint of acute poisoning in the earliest period of the patients' stay in the emergency department that provided data of appropriate quality. Emergency treatments, including tracheal intubation, intravenous access, and the first dose of an antidote such as atropine, were given prior to signal acquisition [6 ]. The ECG signals were acquired and digitized at a 1,000-Hz frequency using a custom-built sampling device from the analog ECG output port of a LIFEPAK 20 monitor-defibrillator (Physio-Control, Redmond, WA, USA). The Physio-Toolkit software package was used to process the ECG signals [11 (link)]. The original 1,000-Hz ECG signals were down-sampled to 500-, 250-, 100-, and 50-Hz sampling frequencies with the xform command, which applies linear interpolation when altering sampling frequencies. The timing of QRS waves was detected by the gqrs command and subsequently converted into R–R interval data with the ann2rr command. One case was excluded from further analysis because the gqrs function could not reliably detect QRS complexes from the data on 1,000-Hz signals.
The R–R interval data were analyzed for time-domain, frequency-domain, and nonlinear HRV parameters using Kubios HRV Standard version 3.0 (Kubios Oy Ltd., Kuopio, Finland) from 5-minute sections of the signal tracing [12 (link)]. The HRV parameters used for further analysis and their definitions are summarized in Table 1. Parameters derived from data on the 500-, 250-, 100-, and 50-Hz down-sampled frequencies were compared to those derived from data on 1,000-Hz signals, and Lin's concordance correlation coefficients (CCC) with respective 95% confidence intervals (CI) were calculated. The sampling frequencies were considered unacceptable when the CCCs for the respective parameters were <0.9 [13 (link)14 ]. Bland-Altman analysis was performed to determine the limits of agreement between results from different frequencies. MedCalc Software version 18.2.1 (Med-Calc Software bvba, Ostend, Belgium; http://www.medcalc.org; 2018) was used for statistical analysis.
Kwon O., Jeong J., Kim H.B., Kwon I.H., Park S.Y., Kim J.E, & Choi Y. (2018). Electrocardiogram Sampling Frequency Range Acceptable for Heart Rate Variability Analysis. Healthcare Informatics Research, 24(3), 198-206.
Publication 2018
Adult Antidote Atropine Cholinesterase Inhibitors Defibrillators Diagnosis Intubation, Intratracheal Medical Devices Patients Treatment, Emergency
3
Recruiting Cognitively Impaired Older Adults
Cited 9 times
Volunteers aged 75 years or older were recruited from September 2000 to June 2002 using voter registration and other purchased mailing lists from 4 US communities with academic medical centers: Hagerstown, Maryland (Johns Hopkins); Pittsburgh, Pennsylvania (University of Pittsburgh); Sacramento, California (University of California–Davis); and Winston-Salem and Greensboro, North Carolina (Wake Forest University). All participants were required to identify a proxy willing to be interviewed every 6 months at the time of each study visit. Signed informed consent was obtained from participants and their respective proxies.
Individuals with prevalent dementia (meeting Diagnostic and Statistical Manual of Mental Disorders [Fourth Edition] [DSM-IV] criteria for dementia18 or a score >0.5 on the Clinical Dementia Rating scale19 (link) [CDR]) were excluded from participation. Also excluded were individuals meeting any of the following criteria: (1) currently taking the anticoagulant warfarin; (2) taking cholinesterase inhibitors for cognitive problems or dementia (memantine had not been approved for use in the United States when the study began); (3) unwilling to discontinue taking over-the-counter G biloba for the duration of the study; (4) currently being treated with tricyclic antidepressants, antipsychotics, or other medications with significant psychotropic or central cholinergic effects (the anticholinergic effects of selective serotonin reuptake inhibitors were not believed to be substantial enough to warrant exclusion); (5) daily use of more than 400-IU vitamin E or unwillingness to reduce intake to this level; (6) history of bleeding disorders; (7) hospitalization for depression within the last year or electroconvulsive therapy within last 10 years; (8) history of Parkinson disease or taking anti-Parkinson medications; (9) abnormal thyroid tests, serum creatinine level greater than 2.0 mg/dL (to convert to μmol/L, multiply by 88.4), or liver function tests more than 2 times the upper limit of normal at baseline; (10) baseline vitamin B12 levels 210 pg/mL or lower (to convert to pmol/L, multiply by 0.7378); (11) hematocrit level less than 30%; (12) platelet count lower than 100 ×103/μL; (13) disease-related life expectancy of less than 5 years; or (14) known allergy to G biloba.
The recruitment procedures for the GEM Study have been described elsewhere.17 (link) Participants with mild cognitive impairment (MCI) were not excluded. The criteria for classification of MCI at baseline in the GEM Study were based on guidelines set forth by the International Working Group on Mild Cognitive Impairment.20 ,21 (link) In brief, individuals defined as having baseline MCI met both of the following 2 criteria: (1) impaired at or below the 10th percentile of Cardiovascular Health Study normative data, stratified by age and education, on at least 2 of 10 selected neuropsychological test scores from each cognitive domain, including memory, language, visuospatial abilities, attention, and executive function; and (2) CDR global score of 0.5.
DeKosky S.T., Williamson J.D., Fitzpatrick A.L., Kronmal R.A., Ives D.G., Saxton J.A., Lopez O.L., Burke G., Carlson M.C., Fried L.P., Kuller L.H., Robbins J.A., Tracy R.P., Woolard N.F., Dunn L., Snitz B.E., Nahin R.L, & Furberg C.D. (2008). Ginkgo biloba for Prevention of Dementia: A Randomized Controlled Trial. JAMA : the journal of the American Medical Association, 300(19), 2253-2262.
Publication 2008
Anticholinergic Agents Anticoagulants Antipsychotic Agents Attention Blood Coagulation Disorders Cardiovascular System Cholinergic Effect Cholinesterase Inhibitors Cognition Cognitive Impairments, Mild Creatinine Dementia Drugs, Non-Prescription Electroconvulsive Therapy Executive Function Forests Hospitalization Hypersensitivity inhibitors Liver Function Tests Memantine Memory Neuropsychological Tests Parkinson Disease Pharmaceutical Preparations Platelet Counts, Blood Psychotropic Drugs Serotonin Effect Serum Thyroid Diseases Thyroid Function Tests Tricyclic Antidepressive Agents Vitamin B12 Vitamin E Volumes, Packed Erythrocyte Voluntary Workers Warfarin
4
Depression and Cognitive Deficits in Elderly Patients
Cited 8 times
Seventy four participants (Mean age=80.90; SD=7.48; Range=66–95 yo); 74.32% females) were recruited through collaborating community agencies of Weill-Cornell Institute of Geriatric Psychiatry.
Eligible participants had (1) non-psychotic, unipolar MDD DSM-IV diagnosis (SCID-R)[28 ]; (2) Montgomery Asberg Depression Rating Scale (MADRS) score≥17 [29 (link)] ; (3) at least mild cognitive deficits (age and education-adjusted scaled score of ≤7 on the DRS subscale of Memory or Initiation Perseveration[30 ]); (4) disability (at least 1 impairment in instrumental activities of daily living [31 (link)]); and (5) limited mobility to attend weekly outpatient treatment, based on participant, caregiver or physician’s report. Eligible participants were either: a) not taking antidepressants, cholinesterase inhibitors, or memantine, or b) on a stable dosage for at least 6 weeks prior to study entry without any medical recommendation for medication change in the next 3 months. Pharmacotherapy was uncontrolled and provided by community physicians.
Exclusion criteria included (1) other Axis I psychiatric disorder (except comorbid anxiety disorders); (2) acute or severe medical illness (e.g., metastatic cancer, liver failure); (3) drugs known to cause depression; (4) current involvement in psychotherapy; (5) advanced dementia, i.e. a Mini Mental State Examination score[32 (link)] <17; and (6) aphasia or inability to speak English. The participants provided signed informed consent. Involvement of a caregiver was encouraged but not required (Table 2).
Kiosses D.N., Ravdin L.D., Gross J.J., Raue P., Kotbi N, & Alexopoulos G.S. (2015). Problem Adaptation Therapy (PATH) for Older Adults with Major Depression and Cognitive Impairment: A Randomized Clinical Trial. JAMA psychiatry, 72(1), 22-30.
Publication 2015
Antidepressive Agents Anxiety Disorders Aphasia Care, Ambulatory Cholinesterase Inhibitors Cognition Disorders Dementia Diagnosis Disabled Persons Epistropheus Females Hepatic Insufficiency Memantine Memory Mental Disorders Mini Mental State Examination Neoplasm Metastasis Pharmaceutical Preparations Pharmacotherapy Physicians Psychotherapy Range of Motion, Articular SCID Mice
5
Recruitment and Screening of Cognitive Study
Cited 8 times
A full description of recruitment and screening procedures has been reported previously.1 (link),15 (link),16 (link) Briefly, participants were recruited from September 2000 to May 2002 from 4 US communities: Hagerstown, Maryland; Pittsburgh, Pennsylvania; Sacramento, California; and Winston-Salem and Greensboro, North Carolina. Participants were required to identify a proxy willing to be interviewed at 6-month study visits. Written informed consent was obtained from participants and their proxies.
Individuals with prevalent dementia meeting Diagnostic and Statistical Manual of Mental Disorders (Fourth Edition)17 criteria for dementia or a score greater than 0.5 on the Clinical Dementia Rating (CDR) scale18 (link) were excluded from participation. Also excluded were individuals meeting any of the following criteria: (1) currently taking warfarin; (2) taking cholinesterase inhibitors for cognitive problems or dementia (memantine had not been approved for use in the United States when the study began); (3) unwilling to discontinue over-the-counter G biloba for the duration of the study; (4) current treatment with tricyclic anti-depressants, antipsychotics, or other medications with significant psychotropic or central cholinergic effects; (5) daily use of more than 400 IU of vitamin E or unwillingness to reduce in-take to this level; (6) history of bleeding disorders; (7) hospitalization for depression within the last year or electroconvulsive therapy within the last 10 years; (8) diagnosis of Parkinson disease or taking anti-Parkinson medications; (9) abnormal thyroid, serum creatinine, or liver function test results; (10) low baseline vitamin B12 levels; (11) low hematocrit level; (12) low platelet count; (13) disease-limited life expectancy of less than 5 years; or (14) known allergy to G biloba.
Participants with MCI at baseline were not excluded. Criteria for MCI at baseline were based on published consensus guidelines.19 (link) In brief, participants were defined as having MCI if they had: (1) impairments at or below the 10th percentile of Cardiovascular Health Study normative data, stratified by age and education, on at least 2 of 10 selected neuropsychological test scores from 5 cognitive domains; and (2) a CDR global score of 0.5.20 (link)
Snitz B.E., O'Meara E.S., Carlson M.C., Arnold A.M., Ives D.G., Rapp S.R., Saxton J., Lopez O.L., Dunn L.O., Sink K.M, & DeKosky S.T. (2009). Ginkgo biloba for Preventing Cognitive Decline in Older Adults: A Randomized Trial. JAMA : the journal of the American Medical Association, 302(24), 2663-2670.
Publication 2009
Antipsychotic Agents Blood Coagulation Disorders Cardiovascular System Cholinergic Effect Cholinesterase Inhibitors Cognition Creatinine Diagnosis Drugs, Non-Prescription Electroconvulsive Therapy Hospitalization Hypersensitivity Liver Function Tests Memantine Neuropsychological Tests Parkinson Disease Pharmaceutical Preparations Platelet Counts, Blood Presenile Dementia Psychotropic Drugs Screening Serum Thyroid Diseases Tricyclic Antidepressive Agents Vitamin B12 Vitamin E Volumes, Packed Erythrocyte Warfarin

Most recents protocols related to «Cholinesterase Inhibitors»

1
Anorexia and Frailty in Dementia
The following individuals were eligible if they met all the inclusion criteria: individuals with MCI, as defined by the criteria set out by the Diagnostic and Statistical Manual of Mental Disorders (Fifth Edition) (DSM-5) [22 ], or probable/possible AD, AD with cerebrovascular disease, and mixed dementia as defined by the National Institute on Aging-Alzheimer’s Association criteria [23 ]. The main inclusion criteria were age ≥55 years, outpatients, Neuropsychiatric Inventory (NPI) subcategory scores for ‘anorexia’ ≥3 points, prefrailty or frailty defined as the Japanese version of the Cardiovascular Health Study (J-CHS) criteria, and a global Clinical Dementia Rating (CDR) score of 0.5 or 1.0.
Individuals were excluded if they had severe agitation/aggression, malignant tumor, or other life-threatening diseases, and had major depression, bipolar disorder, schizophrenia, alcoholism, or drug addiction (described in DSM-5) within the past two years. Individuals were also excluded if they had taken medicines containing Polygala Root, Citrus Unshiu Peel, or Kampo medicine, which had indications for anorexia, fatigue, weakness after illness, and upper gastrointestinal disorders such as gastritis, within the past 4 weeks. There were two categories of concomitant drugs administered during the study period. In category 1, continued stable use during the treatment period was allowed for therapeutic agents for dementia (cholinesterase inhibitors) started within the previous 24 weeks, and other effective agents for cognitive decline, frailty, and peptic ulcer started within the previous 4 weeks. For category 2, the use of hypnotics, psychotropic agents, anticonvulsants, effective agents for anorexia, and first-generation antihistamines as rescue drugs were allowed when complications worsened during the study period; however, the dose and frequency of use were kept to a minimum.
Okahara K., Ohsawa M., Haruta-Tsukamoto A., Miyoshi R., Funahashi H., Fukutani Y., Makita S., Matsuo H, & Ishida Y. (2023). Frailty Improvement by Multicomponent Drug, Ninjin’Yoeito, in Mild Cognitive Impairment and Mild Alzheimer’s Disease Patients: An Open-Label Exploratory Study (FRAMINGO). Journal of Alzheimer's Disease Reports, 7(1), 107-117.
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Publication 2023
Alcoholic Intoxication, Chronic Anorexia Anticonvulsants Appetite Depressants Asthenia Bipolar Disorder Cardiovascular System Cerebrovascular Disorders Cholinesterase Inhibitors Citrus Dementia Drug Dependence Fatigue Gastritis Histamine Antagonists Hypnotics Japanese Major Depressive Disorder Malignant Neoplasms Mental Deterioration Mixed Dementias Outpatients Peptic Ulcer Pharmaceutical Preparations Plant Roots Polygala Psychotropic Drugs Schizophrenia Therapeutics Upper Gastrointestinal Tract
2
Alzheimer's Dementia Inclusion Criteria
Patients were eligible for enrollment if they met standard clinical criteria for dementia that was probably due to AD (biomarker tests were not required for patient inclusion) [35 , 36 (link)], had a baseline MMSE score of 12 to 25 (corresponding to mild or moderate dementia), had been treated with a cholinesterase inhibitor, memantine, or both, (representing the standard of care) for a minimum of 6 months prior to screening, and were at least 50 years old. Exclusion criteria included any other cause of dementia not due to AD, severe forms of delusions or delirium, presence of infection, evidence/history of significant psychiatric disorder, and treatment with registered or putative cognitive/memory enhancer or disease modifier (other than donepezil, galantamine, rivastigmine or memantine).
Dubois B., López-Arrieta J., Lipschitz S., Triantafyllos D., Spiru L., Moroz S., Venger O., Vermersch P., Moussy A., Mansfield C.D., Hermine O, & Tsolaki M. (2023). Masitinib for mild-to-moderate Alzheimer’s disease: results from a randomized, placebo-controlled, phase 3, clinical trial. Alzheimer's Research & Therapy, 15, 39.
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Publication 2023
Biological Markers Cholinesterase Inhibitors Delirium Delusions Donepezil Galantamine Infection Memantine Memory Mental Disorders Mini Mental State Examination Nootropic Agents Patients Presenile Dementia Rivastigmine
3
Corticosteroid Tapering in Myasthenia Gravis Patients
The primary efficacy end point for this study was the percent of patients achieving a 50% or greater reduction in CS dose at week 39 from baseline (week 0). Secondary efficacy end points measured from baseline (week 0) to week 39 were the percent reduction in CS daily dose and the time to the first episode of MG worsening (as defined above).
Exploratory end points related to CS therapy included the following: percent of patients achieving a ≥75% reduction in CS dose at week 39, percent of patients achieving a CS dose ≤7.5 mg (prednisone equivalent) at week 39, percent of patients CS-free at week 39, change in fasting serum glucose at week 39 vs baseline, percent of patients with fasting glucose ≤125 mg/dL at week 39 vs baseline, and a change in hemoglobin A1c at week 39 compared with baseline (week 0).
Exploratory end points related to MG were as follows: percent of patients experiencing an MC or worsening of MG requiring hospitalization through week 39 and week 39 through week 45, number of episodes of MG worsening from baseline (week 0) to week 39, changes in a 15-item MG-Quality of Life Instrument (MG-QOL 15) at weeks 39, 42, and 45 compared with baseline (week 0), changes in MG-Activities of Daily Living (MG-ADL) score at weeks 39, 42, and 45 from baseline (week 0), and changes from baseline (week 0) in the activity (binding, blocking, and modulating) of anti-acetylcholine receptor antibodies at week 39 (Covance Central Laboratory, Indianapolis, IN). In addition, the change in serum IgG levels from baseline (week 0) was measured at weeks 9, 24, and 39.
The guide for CS taper was the QMG score.17 (link) A 3-point improvement in the QMG score reflects a clinically significant improvement.19 (link) Study patients taking cholinesterase inhibitors were instructed not to take these medications for 12 hours before QMG testing. The MG-QOL 15 is a measure of mobility, symptoms, general contentment, and emotional well-being as assessed by the patient.20 (link)- (link)22 (link) The MG-ADL score is designed to assess the effects of MG on usual daily activities. A 2-point improvement in MG-ADL was designated as clinically significant.23 (link) The MG Composite scale has been recommended by the MGFA as a quantitative measure for patients with generalized MG.24 (link),25 (link) A 3-point improvement in the MG Composite was correlated with clinical improvement and meaningful improvement to patients.26 (link)
Bril V., Szczudlik A., Vaitkus A., Rozsa C., Kostera-Pruszczyk A., Hon P., Bednarik J., Tyblova M., Köhler W., Toomsoo T., Nowak R.J., Mozaffar T., Freimer M.L., Nicolle M.W., Magnus T., Pulley M.T., Rivner M., Dimachkie M.M., Distad B.J., Pascuzzi R.M., Babiar D., Lin J., Querolt Coll M., Griffin R, & Mondou E. (2023). Randomized Double-Blind Placebo-Controlled Trial of the Corticosteroid-Sparing Effects of Immunoglobulin in Myasthenia Gravis. Neurology, 100(7), e671-e682.
Publication 2023
Anti-Antibodies Cholinergic Receptors Cholinesterase Inhibitors Drug Tapering Emotions Glucose Hemoglobin A, Glycosylated Hospitalization Patients Pharmaceutical Preparations Prednisone Range of Motion, Articular Serum Therapeutics
4
Enhancing Parasympathetic Activity with Pyridostigmine
Total parasympathetic activity has been increased by means of treating the animals with cholinesterase inhibitor pyridostigmine at a daily dose of 40 mg/kg [28 (link)]. The drug was administered intragastrically each day for 6 weeks using commercially available polypropylene feeding tube (Figure 1).
Karpov A.A., Vachrushev N.S., Shilenko L.A., Smirnov S.S., Bunenkov N.S., Butskih M.G., Chervaev A.K., Vaulina D.D., Ivkin D.Y., Moiseeva O.M, & Galagudza M.M. (2023). Sympathetic Denervation and Pharmacological Stimulation of Parasympathetic Nervous System Prevent Pulmonary Vascular Bed Remodeling in Rat Model of Chronic Thromboembolic Pulmonary Hypertension. Journal of Cardiovascular Development and Disease, 10(2), 40.
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Publication 2023
Animals Cholinesterase Inhibitors Pharmaceutical Preparations Polypropylenes Pyridostigmine Tube Feeding
5
Autonomic Modulation in CTEPH Animal Model
On the next day after last MSs or vehicle administration, all survived animals were randomly divided into the following groups (Figure 1):

Healthy animals (INT)—sham surgery has been performed in these animals which received vehicle only;

CTEPH—sham surgery has been performed in these animals with CTEPH;

CTEPH + Sympathetic Denervation (CTEPH + SD)—the animals with CTEPH were subjected to unilateral surgical sympathetic denervation;

CTEPH + Vagal Denervation (CTEPH + VD)—the animals with CTEPH were subjected to unilateral surgical vagal denervation;

CTEPH + Pyridostigmine (CTEPH + PS)—the animals with CTEPH were treated with reversible cholinesterase inhibitor pyridostigmine.

Six weeks after surgery, echocardiography was performed in all animals. Then, hemodynamic measurements were carried out in anesthetized animals, followed by blood sampling, euthanasia and heart and lung harvesting for histological and molecular biology studies.
Karpov A.A., Vachrushev N.S., Shilenko L.A., Smirnov S.S., Bunenkov N.S., Butskih M.G., Chervaev A.K., Vaulina D.D., Ivkin D.Y., Moiseeva O.M, & Galagudza M.M. (2023). Sympathetic Denervation and Pharmacological Stimulation of Parasympathetic Nervous System Prevent Pulmonary Vascular Bed Remodeling in Rat Model of Chronic Thromboembolic Pulmonary Hypertension. Journal of Cardiovascular Development and Disease, 10(2), 40.
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Publication 2023
Animals Cholinesterase Inhibitors Denervation Echocardiography Euthanasia Heart Hemodynamics Lung Operative Surgical Procedures Pneumogastric Nerve Pyridostigmine Sympathectomy

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More about "Cholinesterase Inhibitors"

Cholinesterase Inhibitors, also known as Acetylcholinesterase Inhibitors (AChEIs), are a class of pharmacological agents that work by blocking the action of cholinesterase enzymes.
These enzymes are responsible for breaking down the neurotransmitter acetylcholine (ACh).
By inhibiting cholinesterase, Cholinesterase Inhibitors lead to an increase in ACh levels in the body, which can have therapeutic effects for various conditions.
Conditions that may benefit from Cholinesterase Inhibitor treatment include Alzheimer's disease, myasthenia gravis, and glaucoma.
Cholinesterase Inhibitors are a widely studied and important group of compounds in the fields of pharmacology and neuroscience, offering potential treatments for a variety of neurological and muscular disorders.
Research into the mechanisms and applications of Cholinesterase Inhibitors is an active area of investigation.
Researchers may utilize techniques such as spectrophotometry, using a double beam spectrophotometer, to measure the activity of cholinesterase enzymes and the effects of Cholinesterase Inhibitors.
Compounds like Physostigmine, Acetylthiocholine iodide, and Gallic acid may be used in these studies.
Optimization of research protocols for Cholinesterase Inhibitors is crucial for enhancing reproducibility and accuracy.
AI-driven platforms, such as PubCompare.ai, can help researchers identify the best solutions by comparing protocols from literature, pre-prints, and patents.
This can be particularly useful when working with Electrophorus electricus (electric eel), a source of cholinesterase enzymes, or when using bovine serum albumin (BSA) as a protein source.
Maintaining optimal conditions, such as using Bio-Tek FL 600 for fluorescence measurements and incorporating ascorbic acid as an antioxidant, can also contribute to the success of Cholinesterase Inhibitor research.
By leveraging the insights and tools available, researchers can take their Cholinesterase Inhibitor studies to new heights and unlock the full potential of these important pharmacological agents.