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pyridostigmine bromide

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Description

Pyridostigmine bromide is a cholinesterase inhibitor used to treat myasthenia gravis, a neuromuscular disease. It works by preventing the breakdown of acetylcholine, a neurotransmitter that helps muscles contract. Pyridostigmine bromide is also used to reverse the effects of certain muscle relaxants and to treat certain types of urinary incontinence. It is synthesized through a multi-step process starting with 3-hydroxy-1-methylpyridinium iodide and dimethylaminoethanol. Pyridostigmine bromide is a prescription medication and should only be used under the supervision of a doctor. It is important to note that pyridostigmine bromide can cause side effects, including nausea, vomiting, diarrhea, and muscle weakness. Pyridostigmine bromide is studied to improve its efficacy and reduce its side effects, as well as to explore its potential use in other conditions, such as Alzheimer's disease and Parkinson's disease.'

Pyridostigmine Bromide: 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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID7550
CHEBI ID8666
SCHEMBL ID41147
MeSH IDM0018238

Synonyms (141)

Synonym
MLS001074080
nsc679759
pyridostigmine bromide
nsc-679759
3-{[(dimethylamino)carbonyl]oxy}-1-methylpyridinium bromide
EU-0101035
regonal
bromuro de piridostigmina [inn-spanish]
piridostigmina bromuro [dcit]
pyridinium, 3-(((dimethylamino)carbonyl)oxy)-1-methyl-, bromide
pyridostigmini bromidum [inn-latin]
pyridinium, 3-hydroxyl-1-methyl-, bromide, dimethylcarbamate
einecs 202-929-9
kalymin
3-(dimethylcarbamyloxy)-1-methylpyridinium bromide
1-methyl-3-hydroxypyridinium bromide dimethylcarbamate
3-(((dimethylamino)carbonyl)oxy)-1-methylpyridinium bromide
mestinon bromide
hsdb 3924
bromure de pyridostigmine [inn-french]
kalimin
3-hydroxy-1-methylpyridinium bromide dimethylcarbamate (ester)
3-hydroxy-1-methylpyridinium bromide dimethylcarbamate
carbamic acid, dimethyl-, ester with 3-hydroxy-1-methylpyridinium bromide
dimethylcarbamic acid ester of 3-hydroxy-1-methylpyridinium bromide
pyridinium, 3-hydroxy-1-methyl-, bromide, dimethylcarbamate (ester)
ccris 6798
ro 1-5130
D00487
101-26-8
pyridostigmine bromide (jp17/usp/inn)
mestinon (tn)
NCGC00094324-02
NCGC00094324-03
MLS000028385 ,
smr000058605
SPECTRUM1503240
NCGC00094324-01
NCGC00094324-04
bromide, pyridostigmine
P 9797
HMS2092P14
nsc-758435
ro-1-5130
pyridostigmini bromidum
HMS500K09
P1339
3-(dimethylcarbamoyloxy)-1-methylpyridinium bromide
HMS1922M05
HMS3259M16
HMS3263O11
nsc758435
pharmakon1600-01503240
dtxsid9023540 ,
cas-101-26-8
dtxcid503540
tox21_111266
3-[(dimethylcarbamoyl)oxy]-1-methylpyridin-1-ium bromide
HMS2234D06
CCG-40306
mestinon-sr
bromure de pyridostigmine
nsc 758435
kvi301na53 ,
bromuro de piridostigmina
unii-kvi301na53
piridostigmina bromuro
pyridostigmine bromide [usp:inn:ban:jan]
FT-0603307
LP01035
pyridostigmine bromide [mi]
pyridostigmine bromide [usp-rs]
pyridostigmine bromide [who-dd]
pyridinium, 3-(((dimethylamino)carbonyl)oxy)-1-methyl-, bromide (1:1)
pyridostigmini bromidum [who-ip latin]
pyridostigmine bromide [ep impurity]
pyridostigmine bromide [orange book]
pyridostigmine bromide [jan]
pyridostigmine bromide [ep monograph]
pyridostigmine bromide [who-ip]
pyridostigmine bromide [hsdb]
pyridostigmine bromide [inn]
pyridostigmine bromide [usp monograph]
pyridostigmine bromide [mart.]
S1608
AKOS015895321
HMS3369P02
pyridostigmine (bromide)
HY-B0207A
NC00581
SCHEMBL41147
NCGC00015862-07
tox21_111266_1
tox21_501035
NCGC00261720-01
3-((dimethylcarbamoyl)oxy)-1-methylpyridin-1-ium bromide
pyridinium, 3-[[(dimethylamino)carbonyl]oxy]-1-methyl-, bromide
Q-201644
OPERA_ID_420
3-(dimethylaminocarbonyloxy)-1-methylpyridinium bromide
mfcd00079283
(1-methylpyridin-1-ium-3-yl) n,n-dimethylcarbamate;bromide
AC-8143
SR-01000003072-2
sr-01000003072
pyridostigmine bromide, united states pharmacopeia (usp) reference standard
HMS3651G13
pyridostigmine bromide, european pharmacopoeia (ep) reference standard
SR-01000003072-4
CHEBI:8666
SW199029-2
3-dimethylcarbamoyloxy-1-methylpyridinium bromide;3-dimethylcarbamoyloxy-1-methylpyridinium bromide
pyridostigmine bromide (mestinon)
Q26840825
AS-13164
BCP02148
HMS3884M21
pyridostigminebromine
T71526
3-((dimethylcarbamoyl)oxy)-1-methylpyridin-1-iumbromide
EN300-120686
pyridinium, 3-[[(dimethylamino)carbonyl]oxy]-1-methyl-, bromide (1:1)
Z1269171738
SY108979
3-[(dimethylcarbamoyl)oxy]-1-methylpyridinium bromide
bromure de pyridostigmine (inn-french)
pyridostigmine bromide (ep impurity)
bromuro de piridostigmina (inn-spanish)
pyridostigminii bromidum
carbamic acid,dimethyl-, ester with 3-hydroxy-1-methylpyridinium bromide
pyridostigmine (cation)
pyridostigmine bromide (usp-rs)
pyridostigmine bromide (mart.)
pryidostigmine bromide
pyridostigmine bromide (usp:inn:ban:jan)
n07aa02
pyridostigmini bromidum (inn-latin)
3-dimethylcarbamoyloxy-1-methylpyridinium bromide
pyridostigmine bromide oral
pyridostigmine bromide (ep monograph)
pyridostigmine bromide (usp monograph)

Research Excerpts

Overview

Pyridostigmine bromide (PB) is an FDA-approved drug for the treatment of myasthenia gravis. It is also a prophylactic pre-treatment for organophosphate nerve agent poisoning.

ExcerptReferenceRelevance
"Pyridostigmine bromide is a cholinesterase enzyme inhibitor."( Tailoring Two Chemometric Models for Determination of Three Neuromuscular Combined Medications and Application to Spiked Human Plasma.
Abdelhamid, NS; Anwar, BH; Farid, NF; Magdy, MA, 2023
)
1.63
"Pyridostigmine bromide (PB) is a reversible acetylcholinesterase (AChE) inhibitor and the first-choice for the treatment of symptoms associated with myasthenia gravis and other neuromuscular junction disorders. "( Effects of Pyridostigmine bromide on SH-SY5Y cells: An in vitro neuroblastoma neurotoxicity model.
Azzolin, VF; Barbisan, F; da Cruz, IBM; Duarte, MMFM; Duarte, T; Fortuna, M; Lenz, LS; Teixeira, CF, 2017
)
2.29
"Pyridostigmine bromide (PB) is an FDA-approved drug for the treatment of myasthenia gravis and a prophylactic pre-treatment for organophosphate nerve agent poisoning. "( Carbamate nerve agent prophylatics exhibit distinct toxicological effects in the zebrafish embryo model.
English, E; Fischer, A; Granato, M; McCallion, AS; Parsons, M; Proescher, J; Wolman, M,
)
1.57
"Pyridostigmine bromide (PTB) is a highly soluble and extremely bitter drug. "( Design and evaluation of an economic taste-masked dispersible tablet of pyridostigmine bromide, a highly soluble drug with an extremely bitter taste.
Tan, Q; Teng, Y; Zhang, J; Zhang, L, 2012
)
2.05
"Pyridostigmine bromide (PB) is an anticholinesterase agent whose aqueous solubility is high and which has a short elimination half-life. "( Preparation and in vitro evaluation of pyridostigmine bromide microparticles.
Demirel, M; Hegazy, N; Yazan, Y, 2002
)
2.03
"Pyridostigmine bromide (PYR) is an anticholinesterase drug indicated for the treatment of myasthenia gravis and neuromuscular blockade reversal. "( Pyridostigmine bromide (PYR) alters immune function in B6C3F1 mice.
Allen, CT; Dudley, AC; EuDaly, JG; Gilkeson, GS; Keil, DE; Peden-Adams, MM, 2004
)
3.21
"Pyridostigmine bromide (PB) is a quartenary ammonium compound that inhibits the hydrolysis of acetylcholine by competitive reversible binding to acetylcholinesterase. "( Determination of pyridostigmine bromide and its metabolites in biological samples.
Lai, MH; Lu, J; Moochhala, SM; Tan, D; Zhao, B, 2006
)
2.12
"Pyridostigmine bromide (PB) is a reversible acetylcholinesterase inhibitor that has been used as a pretreatment drug for "Soman" nerve gas poisoning in combat to increase survival. "( An investigation of acetylcholine released in skeletal muscle and protein unbound drug released in blood based on the pyridostigmine bromide (pretreatment drug) sustained-release pellets by microdialysis technique in the rabbit model.
Cham, TM; Cheng, CJ; Chuo, WH; Huang, YT; Lai, TF; Tsai, TH; Tsai, TR, 2007
)
1.99
"Pyridostigmine bromide (PB) is a reversible cholinesterase inhibitor used routinely in the treatment of myasthenia gravis and recently by the US Army as a prophylactic agent against potential nerve gas attack in the Persian Gulf War. "( Potentiation of pyridostigmine bromide toxicity in mice by selected adrenergic agents and caffeine.
Chaney, LA; Hume, AS; Moss, JI; Mozingo, JR; Rockhold, RW, 1997
)
2.09
"Pyridostigmine bromide (PB) is a reversible, peripherally active inhibitor of acetylcholinesterase (AChE) activity, and is recommended by the military as a pretreatment against potential nerve gas exposure. "( Effects of inescapable stress and treatment with pyridostigmine bromide on plasma butyrylcholinesterase and the acoustic startle response in rats.
Beldowicz, D; Guo, W; Natelson, BH; Ottenweller, JE; Servatius, RJ; Zhu, G, 2000
)
2
"Pyridostigmine bromide (PB) is a reversible cholinesterase inhibitor used for treatment of myasthenia gravis and for prophylactic protection against organophosphate nerve agent. "( Reactive oxygen species mediate pyridostigmine-induced neuronal apoptosis: involvement of muscarinic and NMDA receptors.
Borowitz, JL; Isom, GE; Li, L; Shou, Y, 2001
)
1.75

Effects

Pyridostigmine bromide (PB) has been used to protect soldiers from the toxic effects of soman. PB has been associated with improved baroreceptor sensitivity.

ExcerptReferenceRelevance
"Pyridostigmine bromide (PB) has been used to protect soldiers from the toxic effects of soman, a chemical warfare agent. "( Pyridostigmine bromide protection against acetylcholinesterase inhibition by pesticides.
Ankirskaia, A; DePeters, E; Glucksman, G; Henderson, JD; Lam, H; Leong, B; Siddique, I; Tigyi, A; Wilson, BW, 2012
)
3.26
"Pyridostigmine bromide has been associated with improved baroreceptor sensitivity and presents a novel approach to treatment of orthostatic intolerance. "( Pyridostigmine in the treatment of orthostatic intolerance.
Gales, BJ; Gales, MA, 2007
)
1.78

Actions

ExcerptReferenceRelevance
"Pyridostigmine bromide (PB) promotes and then silences cholinergic muscle activity, and disrupts the junctional regions of muscle fibers and associated nerve terminals, in organotypic mouse spinal cord-muscle cultures continuously treated with low concentrations of the drug for up to 14 days. "( Neuromuscular responses to pyridostigmine bromide in organotypic spinal cord-muscle culture.
Drake-Baumann, R; Seil, FJ; Spencer, PS,
)
1.87

Treatment

Treatment with pyridostigmine bromide (PB) increased HRV oscillation of both low frequency (LF: 0.2-0.75 Hz) and high frequency (HF): 0.75-3 Hz. Pretreatment with PB has become part of standard military procedures for protection against the effects of possible chemical warfare attack.

ExcerptReferenceRelevance
"Treatment with pyridostigmine bromide, prednisone, and tacrolimus was initiated."( Case Report: Orbital Myositis and Myasthenia Gravis as Symptoms of Immune Reconstitution Inflammatory Syndrome in a Patient With Human Immunodeficiency Virus Infection.
Wang, Y; Wen, Y; Yang, J; Zhao, N, 2020
)
0.9
"Treatment with pyridostigmine bromide increased HRV oscillation of both low frequency (LF: 0.2-0.75 Hz) and high frequency (HF: 0.75-3 Hz)."( Effects of chronic cholinergic stimulation associated with aerobic physical training on cardiac morphofunctional and autonomic parameters in spontaneously hypertensive rats.
Aguilar, BA; Gardim, CB; Philbois, SV; Souza, HCD; Veiga, AC, 2021
)
0.96
"Pretreatment with pyridostigmine bromide (PB) of human intercostal muscle fibers exposed to the irreversible acetylcholinesterase (AChE) inhibitor soman was investigated."( Protection of human muscle acetylcholinesterase from soman by pyridostigmine bromide.
Follette, D; Graves, G; Henderson, JD; Maselli, RA; Ng, J; Wilson, BW, 2011
)
0.94
"Treatment with pyridostigmine bromide (360 mg/d) in a patient with PV allowed to keep his disease under control at a lower dose of prednisone than that used before starting pyridostigmine bromide treatment."( Pemphigus vulgaris acantholysis ameliorated by cholinergic agonists.
Arredondo, J; Chernyavsky, AI; Grando, SA; Kitajima, Y; Nguyen, VT; Pittelkow, MR, 2004
)
0.66
"Pretreatment with pyridostigmine bromide (PB) has become part of standard military procedures for protection against the effects of possible chemical warfare attack. "( Side effects of low-dose pyridostigmine bromide are not related to cholinesterase inhibition.
Cook, MR; Gerkovich, MM; Graham, C; Sastre, A, 2001
)
0.95
"Pretreatment with pyridostigmine bromide (60 mg orally 60 min before the GHRH injection) significantly increased both baseline GH levels and the GH response to GHRH in all the obese subjects, so that their mean baseline GH, peak GH levels and integrated area under the curve after pyridostigmine bromide plus GHRH were similar to those of the control children after GHRH."( Pyridostigmine counteracts the blunted growth hormone response to growth hormone-releasing hormone of obese children.
Cappa, M; Ghigo, E; Locatelli, V; Loche, S; Müller, EE; Pintor, C; Puggioni, R, 1989
)
0.6

Toxicity

ExcerptReferenceRelevance
" No clinical adverse reactions were observed, confirming the relative safety of the combination of low-dose pyridostigmine with beta-adrenergic blocking agents."( Safety of pyridostigmine in hypertensive patients receiving beta blockers.
Arad, M; Atsmon, J; Rabinowitz, B; Roth, A; Zelinger, J; Zivner, Z, 1992
)
0.28
" LD50 of CMPF was estimated using an up-and-down dose selection procedure and 12 animals."( Evaluation of the toxicity, pathology, and treatment of cyclohexylmethylphosphonofluoridate (CMPF) poisoning in rhesus monkeys.
Dochterman, LW; Gresham, VC; Kaminskis, A; Koplovitz, I; Stewart, JR, 1992
)
0.28
" Thus, 5 mg/kg/day of pyridostigmine bromide appears to be the no observed toxic effect level under the conditions of the present investigation."( Subchronic oral toxicity of pyridostigmine bromide in rats.
Chung, H; Levine, BS; Long, R, 1991
)
0.89
" The effects of continuous pyridostigmine infusion at these dose-rates on the behavioral toxicity of 5 daily repeated low-dose exposures to a toxic organophosphate (soman) were determined not be deleterious; in fact, they were slightly (and variably) protective."( Behavioral toxicity of anticholinesterases in primates: chronic pyridostigmine and soman interactions.
Blick, DW; Brown, GC; Hartgraves, SL; Kerenyi, SZ; Miller, S; Murphy, MR, 1991
)
0.28
"The ability of the carbamates pyridostigmine and physostigmine to protect against the lethal effects of soman, an extremely toxic anticholinesterase agent, was measured in rats, guinea pigs and rabbits."( Effect of carboxylesterase inhibition on carbamate protection against soman toxicity.
Brecht, KM; Lenz, DE; Maxwell, DM; O'Neill, BL, 1988
)
0.27
" This pyridostigmine pretreatment lowered the soman LD50 from 104 micrograms/kg in control animals to 82 micrograms/kg."( Effects of subchronic pyridostigmine pretreatment on the toxicity of soman.
Clement, JG; Shiloff, JD, 1986
)
0.27
" Animals were challenged with 5 x LD50 GF (233 micrograms/kg, IM) following pretreatment with pyridostigmine (0."( Acute toxicity of cyclohexylmethylphosphonofluoridate (CMPF) in rhesus monkeys: serum biochemical and hematologic changes.
Koplovitz, I; Young, GD, 1995
)
0.29
" We hypothesize that test compounds may compete for xenobiotic metabolizing enzymes in the liver and blood and may also compromise the integrity of the blood-brain barrier, leading to an increase in their "effective concentrations" in the nervous system to levels equivalent to the toxic doses of individual compounds."( Increased neurotoxicity following concurrent exposure to pyridostigmine bromide, DEET, and chlorpyrifos.
Abdel-Rahman, AA; Abou-Donia, MB; Jensen, KF; Kurt, TL; Oehme, FW; Wilmarth, KR, 1996
)
0.54
" To investigate toxic interactions between PB and other drugs, male ICR mice received contralateral ip injections of either a selected adrenergic drug or caffeine, followed 15 min later by PB."( Potentiation of pyridostigmine bromide toxicity in mice by selected adrenergic agents and caffeine.
Chaney, LA; Hume, AS; Moss, JI; Mozingo, JR; Rockhold, RW, 1997
)
0.64
" Thus, we conclude that low-dose guanidine therapy is relatively safe and effective for long-term symptomatic treatment of LEMS when it is combined with pyridostigmine."( Low-dose guanidine and pyridostigmine: relatively safe and effective long-term symptomatic therapy in Lambert-Eaton myasthenic syndrome.
Claussen, GC; Head, TC; Kim, DS; Oh, SJ, 1997
)
0.3
" Neither cholinesterase inhibition nor plasma levels of PB predicted side effect scores during the PB week; the best predictor of side effect scores during the PB week was side effect scores during the PL week."( Side effects of low-dose pyridostigmine bromide are not related to cholinesterase inhibition.
Cook, MR; Gerkovich, MM; Graham, C; Sastre, A, 2001
)
0.61
" It is concluded that physical stress (exercise) enhanced the persistent/delayed toxic effects of low-dose sarin and pyridostigmine in specific tissues of mice."( Persistent/delayed toxic effects of low-dose sarin and pyridostigmine under physical stress (exercise) in mice.
Husain, K; Somani, SM, 2004
)
0.32
" Outcomes Included physical performance (handgrip strength and duration, stair climbing, and pull-ups [males] or push-ups [females]), neurocognitive performance (computerized tests), and self-reported adverse effects."( Pyridostigmine, diethyltoluamide, permethrin, and stress: a double-blind, randomized, placebo-controlled trial to assess safety.
Cantilena, LR; Chang, DN; Cherstniakova, SA; Cooper, JA; Deuster, PA; Kamens, DR; Krantz, DS; Kraus, PL; Law, WA; Matulich, W; Roy, MJ; Sato, PA; Seegers, CA; Young, SY, 2006
)
0.33
" Physical and neurocognitive outcome measures and self-reported adverse effects did not significantly differ by exposure group."( Pyridostigmine, diethyltoluamide, permethrin, and stress: a double-blind, randomized, placebo-controlled trial to assess safety.
Cantilena, LR; Chang, DN; Cherstniakova, SA; Cooper, JA; Deuster, PA; Kamens, DR; Krantz, DS; Kraus, PL; Law, WA; Matulich, W; Roy, MJ; Sato, PA; Seegers, CA; Young, SY, 2006
)
0.33
" Fourteen patients (64%) experienced daily cholinergic adverse effects, and muscarinic side effects correlated with AChE activity."( Electrophysiological signs and the prevalence of adverse effects of acetylcholinesterase inhibitors in patients with myasthenia gravis.
Punga, AR; Sawada, M; Stålberg, EV, 2008
)
0.35
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" However, [-]-Huperzine A is toxic at higher doses due to potent AChE inhibition which limits the utilization of its neuroprotective properties."( [+]-Huperzine A protects against soman toxicity in guinea pigs.
Doctor, BP; Jensen, N; Nambiar, MP; Oguntayo, S; Wang, Y; Wei, Y, 2011
)
0.37
" While being generally safe, they cause numerous adverse effects including induction of hyperactivity of urinary bladder and intestines affecting quality of patients life."( Specific inhibition of acetylcholinesterase as an approach to decrease muscarinic side effects during myasthenia gravis treatment.
Ilyin, VI; Kharlamova, AD; Lenina, OA; Nikolsky, EE; Nurtdinov, AR; Petrov, KA; Sitdykova, ME; Zueva, IV, 2018
)
0.48

Pharmacokinetics

ExcerptReferenceRelevance
" 3 The apparent volume of distribution of pyridostigmine was invariably greater than that of neostigmine, and its fast disposition half-life was approximately three times longer."( Plasma clearance of neostigmine and pyridostigmine in the dog.
Baker, PR; Calvey, TN; Chan, K; Macnee, CM; Taylor, K, 1978
)
0.26
" Pyridostigmine was characterized as a drug of relatively long terminal half-life (8."( Pharmacokinetics of pyridostigmine in dogs.
Chung, H; Forrest, TJ; Hawkins, DR; Taylor, T, 1991
)
0.28
" Only in the last few years, since the introduction of highly sensitive and selective analytical procedures based on gas and liquid chromatography, have proper pharmacokinetic studies of these drugs become possible."( Clinical pharmacokinetics of cholinesterase inhibitors.
Aquilonius, SM; Hartvig, P,
)
0.13
"The duration of the antagonism to neuromuscular blockade produced by pyridostigmine is prolonged in elderly patients, and a pharmacokinetic explanation was sought."( Aging alters the pharmacokinetics of pyridostigmine.
Diaz, J; Jamdar, SC; Matteo, RS; Ornstein, E; Ostapkovich, N; Schwartz, AE; Stone, JG, 1995
)
0.29
" A pharmacodynamic model was developed by considering acetylcholinesterase (AChE) inhibition, direct antagonism to the nicotinic receptor, and desensitization of the nicotinic receptor."( Pharmacodynamic analysis of contractile potentiation by cholinesterase inhibitors in rats.
Iga, T; Sawada, Y; Yamamoto, K, 1996
)
0.29
" Population analysis was performed using standard pharmacokinetic and pharmacodynamic models with the nonlinear mixed-effect modeling software (NONMEM)."( Population pharmacokinetics and pharmacodynamics of pyridostigmine bromide for prophylaxis against nerve agents in humans.
Brueckner, RP; Kaminskis, A; Lasseter, KC; Lin, E; Marino, MT; Schuster, BG, 1998
)
0.55
" The half-life period of aminostigmine exceeded considerably that of earlier studied carbamates and correlated with the clinical manifestations of the drug effects."( [New data on the pharmacokinetics of aminostigmine].
Chepur, SV; Panov, PB; Prozorovskiĭ, VB; Vorob'ev-Desiatovskiĭ, NV,
)
0.13
" The resulting pharmacokinetic data were fitted to a single compartment open model with first-order absorption and elimination."( Retrospective population pharmacokinetic/pharmacodynamic analysis of pyridostigmine, a cholinesterase inhibitor, in Chinese males.
Lee, JD; Loke, WK; Moochhala, S; Seng, KY; Zhao, B, 2009
)
0.35
" The pharmacokinetic parameters were calculated with the aid of DAS2."( [Pharmacokinetics of mestinon-phospholipid complex in rats].
Hu, NN; Tan, QY; Yin, HF; Zhang, JQ; Zhang, L, 2012
)
0.38
"Pharmacokinetic parameters of mestinon-phospholipid complex were Tmax 2 h, Cmax 22."( [Pharmacokinetics of mestinon-phospholipid complex in rats].
Hu, NN; Tan, QY; Yin, HF; Zhang, JQ; Zhang, L, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
"We evaluated the effects of iv pretreatment with exogenous GH on the GH response to GHRH either alone or in combination with pyridostigmine in 14 Type I diabetic patients and 6 normal subjects."( Effects of exogenous growth hormone pretreatment on the pituitary growth hormone response to growth hormone-releasing hormone alone or in combination with pyridostigmine in type I diabetic patients.
Bodini, C; Bossoni, S; Cimino, A; Giustina, A; Pizzocolo, G; Schettino, M; Wehrenberg, WB, 1991
)
0.28
"1 kg/m2) before and after 3 months testosterone therapy, we studied the GH response to GHRH (1 microgram/kg iv) alone and combined with pyridostigmine (PD, 120 mg po), a cholinesterase inhibitor which likely inhibits hypothalamic somatostatin release allowing exploration of the maximal somatotrope secretory pool."( Effect of testosterone replacement therapy on the somatotrope responsiveness to GHRH alone or combined with pyridostigmine and on sympathoadrenal activity in patients with hypogonadism.
Carani, C; Coletta, F; Del Rio, G; Ghigo, E; Marrama, P; Procopio, M; Velardo, A; Zizzo, G, 1995
)
0.29
" PANPAL pretreatment did not improve the efficacy of HI-6 in combination with benactyzine on soman-induced anticholinesterase and stressogenic effects."( The influence of pharmacological pretreatment on efficacy of HI-6 oxime in combination with benactyzine in soman poisoning in rats.
Bajgar, J; Kassa, J, 1996
)
0.29
"The effect of methoxime combined with a) atropine, b) benactyzine, c) atropine and natrium thiosulphate, d) atropine and diazepam on antidotal treatment effectiveness was studied in tabun-poisoned mice."( Effect of methoxime combined with anticholinergic, anticonvulsant or anti-HCN drugs in tabun-poisoned mice.
Sevelová, L; Vachek, J, 2003
)
0.32
" To test our hypothesis, we examined the effect of keyhole limpet hemocyanin (KLH) immunization alone or in combination with PY on activation of MKK4 and JNK induced by stress."( Vaccination alone or in combination with pyridostigmine promotes and prolongs activation of stress-activated kinases induced by stress in the mouse brain.
Liu, YF; Perides, G; Wang, D, 2005
)
0.33
" An in vitro cell-resistant assay was used to monitor the potential of test compounds to interact with P-gp."( Interaction of pyridostigmine bromide and N,N-diethyl-m-toluamide alone and in combination with P-glycoprotein expressed in Escherichia coli leaky mutant.
Abou-Donia, MB; El-Masry, EM, 2006
)
0.69
"EA warming therapy combined with western medicine has a significant therapeutic effect on myasthenia gravis."( [Electroacupuncture warming therapy combined with western medicine for treatment of myasthenia gravis and effect on IL-4 level in the patients].
Cui, X; Feng, J; Wang, SH, 2007
)
0.34

Bioavailability

A novel pyridostigmine bromide (PB)-phospholipid nanocomplex (PBPLC) was prepared to increase the bioavailability of PB.

ExcerptReferenceRelevance
" Despite this similarity, there were in general considerable interindividual differences in the bioavailability of pyridostigmine in myasthenic patients."( Plasma pyridostigmine levels in patients with myasthenia gravis.
Calvey, TN; Chan, K, 1977
)
0.26
" The method is used to analyse samples from a bioavailability study by fully automated unattended overnight sample analysis."( Thermospray mass spectrometer as a quantitative specific, sensitive, detector for liquid chromatography. Its application to the analysis of pyridostigmine in human plasma.
Madigan, MJ; Malcolm, SL; Taylor, NL, 1990
)
0.28
" The oral bioavailability of these hydrophilic ionised compounds is low: that of pyridostigmine is approximately 10% and the value for neostigmine is even lower."( Clinical pharmacokinetics of cholinesterase inhibitors.
Aquilonius, SM; Hartvig, P,
)
0.13
" Three poorly controlled patients were studied on a high-dose alternate-day steroid regimen, and a marked decrease in pyridostigmine bioavailability on the same dose of drug was observed in all three."( Plasma pyridostigmine levels in myasthenia gravis.
De Silva, P; Havard, CW; White, MC, 1981
)
0.26
" Pyridostigmine had a higher elimination (2 h-1) than the absorption rate constant (0."( Renal clearance of pyridostigmine in myasthenic patients and volunteers under the influence of ranitidine and pirenzepine.
Breyer-Pfaff, U; Eiermann, B; Maier, U; Schumm, F; Sommer, N; Winne, D, 1993
)
0.29
" In the present study, human volunteers were pretreated with pyridostigmine to attempt to improve the bioavailability of the parent drug."( Lack of bioavailability of mebeverine even after pretreatment with pyridostigmine.
Eloff, JN; Snyman, JR; Sommers, DK; van Wyk, M, 1997
)
0.3
" These experiments suggest that intraarterial perfusion of PB and/or DFP and topical application of DFP or DEET can alter the disposition of [14C]permethrin in skin and possibly its bioavailability in soldiers simultaneously exposed to these chemicals."( Pyridostigmine bromide modulates the dermal disposition of [14C]permethrin.
Baynes, RE; Monteiro-Riviere, NA; Riviere, JE, 2002
)
1.76
" This conclusion explains, at least in part, the increased toxicity and bioavailability of pyridostigmine bromide following combined administration with DEET."( Interaction of pyridostigmine bromide and N,N-diethyl-m-toluamide alone and in combination with P-glycoprotein expressed in Escherichia coli leaky mutant.
Abou-Donia, MB; El-Masry, EM, 2006
)
0.91
" The relative bioavailability F(0-24) was 102."( [Bioequivalence of pyridostigmine bromide dispersible tablets in rabbits].
Cheng, XG; Tan, QY; Wang, H; Zhang, JQ; Zhang, L, 2011
)
0.7
"A novel pyridostigmine bromide (PB)-phospholipid nanocomplex (PBPLC) was prepared to increase the bioavailability of PB."( Role of a novel pyridostigmine bromide-phospholipid nanocomplex in improving oral bioavailability.
Hu, NN; Liu, GD; Lu, LY; Tan, QY; Wang, H; Yin, HF; Zhang, JQ; Zhang, L, 2012
)
1.16
" The relative bioavailability of mestinon-phospholipid complex was 410."( [Pharmacokinetics of mestinon-phospholipid complex in rats].
Hu, NN; Tan, QY; Yin, HF; Zhang, JQ; Zhang, L, 2012
)
0.38
"The oral bioavailability of mestinon increases remarkably when administered as mestinon-phospholipid complex."( [Pharmacokinetics of mestinon-phospholipid complex in rats].
Hu, NN; Tan, QY; Yin, HF; Zhang, JQ; Zhang, L, 2012
)
0.38
" In addition, in the PYR-treated MI group, nitric oxide (NO) bioavailability was increased and attenuated endothelium-dependent relaxations were improved, whereas restored vasodilator responses were inhibited by N(G)-nitro-L-arginine methyl ester."( Pyridostigmine prevents peripheral vascular endothelial dysfunction in rats with myocardial infarction.
Bi, X; He, X; Liu, J; Lu, Y; Qin, F; Yu, X; Zang, W; Zhao, M, 2014
)
0.4
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

In this non-interventional prospective open-label trial, 72 patients with stable myasthenia gravis were switched from instant-release dosage forms of pyridostigmine bromide to SR-Pyr. Proestrous females dosed at 30 mg/kg had much higher pyridsomine bromides than metestrous males and females.

ExcerptRelevanceReference
" All these compounds led to abnormalities of the cervical vertebrae; at higher dosage interference with normal morphogenesis involved the whole vertebral column."( Cholinomimetic teratogens: studies with chicken embryos.
Landauer, W, 1975
)
0.25
" Radical excision of the tumor, if possible, and the remaining thymus, high dosage alternate day prednisone, and radiation therapy, if indicated, seem the treatments of choice."( Myasthenia gravis and invasive thymoma: a 20-year experience.
Brown, WJ; Goldman, AJ; Herrmann, C; Keesey, JC; Mulder, DG, 1975
)
0.25
" This study sought to establish the ability of PD to induce GH release in the rat, determine the dose-response relationship, and test the hypothesis that SS inhibition is the method of action."( Pyridostigmine-mediated growth hormone release: evidence for somatostatin involvement.
Giustina, A; Voltz, DM; Wehrenberg, WB; Wiviott, SD, 1992
)
0.28
" Pretreatment of the mice with a single dose of pyridostigmine prevented the development of jitter after subsequent dosing with an organophosphate."( Protection against the effects of anticholinesterases on the latencies of action potentials in mouse skeletal muscles.
Bamforth, JP; Das, SK; Ferry, CB; Kelly, SS, 1992
)
0.28
" The value of low dosage of pyridostigmine (30 mg three times daily) in preventing peripheral anti-muscarinic side effects of a transdermal controlled-release formulation of hyoscine, was tested in a double-blind placebo-controlled study, involving 47 healthy subjects."( Prevention of peripheral side-effects of transdermal hyoscine by adjunctive therapy with low dosage of pyridostigmine.
Alhalel, A; Alkalay, M; Almog, S; Izraeli, S; Menahem, S; Ruach, M; Tochner, Z; Versano, D; Ziv, I, 1992
)
0.28
"Pyridostigmine has a protective effect against organophosphate poisoning when given in a dosage of 30 mg three times daily causing 20-40% cholinesterase inhibition."( The influence of pyridostigmine administration on human neuromuscular functions--studies in healthy human subjects.
Achiron, A; Ayalon, A; Glikson, M; Glovinski, J; Karni, A; Ram, Z; Revah, M; Sarova-Pinchas, I, 1991
)
0.28
" The aim of the present study was to investigate if an enhancement of the cholinergic tone was able to influence the dose-response relationship between GHRH and GH in normal adult subjects."( The role of cholinergic tone in modulating the growth hormone response to growth hormone-releasing hormone in normal man.
Bodini, C; Bossoni, S; Buffoli, MG; Doga, M; Girelli, A; Giustina, A; Schettino, M; Wehrenberg, WB, 1991
)
0.28
" The present study was undertaken to evaluate the dose-response and time-course effects of acute oral administration of Pyr over a broad dose range (3-40 mg/kg) on the lever pressing of rats maintained under a multiple fixed-ratio (FR-20) time-out schedule of reinforcement for water reward."( Acute effects of oral pyridostigmine bromide on conditioned operant performance in rats.
Lee, JD; Lee, SF; Lin, CH; Liu, WF; Ma, C; Shih, JH, 1991
)
0.6
" In this study we have investigated the effects of PD on the dose-response relationships of GHRH-induced GH secretion in normal subjects."( Effect of enhancement of endogenous cholinergic tone with pyridostigmine on the dose-response relationships of growth hormone (GH)-releasing hormone-induced GH secretion in normal subjects.
Casanueva, FF; Dieguez, C; Muruais, C; Peñalva, A, 1990
)
0.28
"In 18 patients with generalised myasthenia treated with oral pyridostigmine, muscular strength, decrement of neuromuscular transmission in the trapezius muscle on repetitive accessory nerve stimulation, and pyridostigmine plasma level were measured repeatedly during 1-3 dosing intervals."( Neuromuscular function and plasma drug levels in pyridostigmine treatment of myasthenia gravis.
Breyer-Pfaff, U; Brinkmann, A; Maier, U; Schmezer, A; Schumm, F, 1990
)
0.28
" We did not perform any preliminary dose-finding trials to find the optimum dose of pyridostigmine, but gave the drug in a predetermined fixed dosage to each patient."( Acute effects of oral pyridostigmine on memory and cognitive function in SDAT.
Cape, RD; Molloy, DW,
)
0.13
" The correlation of drug dosage with body area ruled out that this difference could be related to the different PD dose in adults and children."( Growth hormone responses to pyridostigmine in normal adults and in normal and short children.
Bertagna, A; Camanni, F; Ghigo, E; Imperiale, E; Massara, F; Mazza, E; Molinatti, P, 1987
)
0.27
" Anticholinesterase medication (nine patients) and corticosteroid dosage (six patients) had been kept constant for a 2-month period."( Effects of repeated doses of intravenous immunoglobulin in myasthenia gravis.
Arsura, EL; Bick, A; Brunner, NG; Grob, D, 1988
)
0.27
"To determine the potencies of neostigmine, pyridostigmine, and edrophonium in reversing pancuronium and d-tubocurarine blockade, dose-response curves were established for first twitch height recovery and train-of-four ratio."( Dose-response curves for edrophonium, neostigmine, and pyridostigmine after pancuronium and d-tubocurarine.
Antzaka, C; Bevan, DR; Donati, F; McCarroll, SM; McCready, D, 1987
)
0.27
" Concentrations of anticholinesterases spanned the clinical range and were extended beyond to establish dose-response curves."( Incomplete reversal of pancuronium neuromuscular blockade by neostigmine, pyridostigmine, and edrophonium.
Bartkowski, RR, 1987
)
0.27
" Dose-response relationships were established from the measurement of first twitch height (T1) ten minutes later."( Neostigmine, pyridostigmine and edrophonium as antagonists of deep pancuronium blockade.
Bevan, DR; Donati, F; Lahoud, J; McCready, D, 1987
)
0.27
" Rats were exposed to pyridostigmine according to 3 dosing schedules: 2 mg/kg ip daily, 5 mg/kg X d by sc infusion, and 25 mg/kg X d by sc infusion."( Decreased tetanic contracture of rat skeletal muscle induced by pyridostigmine.
Anderson, RJ; Chamberlain, WL; Dacko, C; Robertson, DG; Roesner, M, 1986
)
0.27
" Mean t 1/2 of the plasma level decline after oral dosing was 200 minutes, twice as long as the terminal elimination t1/2 after intravenous infusion (97 minutes)."( Pyridostigmine kinetics in healthy subjects and patients with myasthenia gravis.
Breyer-Pfaff, U; Brinkmann, AM; Maier, U; Schumm, F, 1985
)
0.27
" In both species at 30 min after im injection of Py and Ph, a linear relationship was found between percentage of whole blood AChE inhibition and ln dosage of carbamate."( Relationship between reversible acetylcholinesterase inhibition and efficacy against soman lethality.
Anderson, DR; Harris, LW; Lennox, WJ; Talbot, BG, 1985
)
0.27
" Although the severity of the damage varies from fiber to fiber, the variability appears random and not related to a specific fiber type or dosage regimen."( Neuromuscular toxicity of pyridostigmine bromide in the diaphragm, extensor digitorum longus, and soleus muscles of the rat.
Foster, RE; Hudson, CS; Kahng, MW, 1985
)
0.57
" Accordingly, the dose-response relationship, onset and duration of action (n = 60), and pharmacokinetics (n = 22) of neostigmine, pyridostigmine, their metabolites 3-hydroxyphenyltrimethylammonium (PTMA) and 3-hydroxy-N-methylpyridinium (MP), and edrophonium were determined in dogs anesthetized with sodium pentobarbital."( Metabolites of neostigmine and pyridostigmine do not contribute to antagonism of neuromuscular blockade in the dog.
Cronnelly, R; Fisher, DM; Hennis, PJ; Miller, RD; Sharma, M, 1984
)
0.27
" All patients were evaluated from the standpoint of clinical response to thymectomy, and the number and dosage of anti-myasthenic drugs required after operation."( Cervical thymectomy in the treatment of myasthenia gravis.
Donnelly, RJ; Fabri, B; Florence, AM; Hayward, M; Laquaglia, MP, 1984
)
0.27
" A BDF dosage of each carbamate (0."( Toxicity of anticholinesterases: interactions of pyridostigmine and physostigmine with soman.
Anderson, DR; Harris, LW; Lennox, WJ; Swanson, DR; Talbot, BG, 1984
)
0.27
"We measured the fluctuations in plasma pyridostigmine concentration from day to day on 3 consecutive days and hour to hour during 1 day in 11 myasthenic patients, by studying their usual dosage regime."( Steady state kinetics of pyridostigmine in myasthenia gravis.
Flachs, H; Friis, ML; Hvidberg, EF; Paulson, OB; Sørensen, PS, 1984
)
0.27
"125 mg/kg, however, the dose-response curve was not parallel to those for neostigmine or pyridostigmine."( Edrophonium: duration of action and atropine requirement in humans during halothane anesthesia.
Cronnelly, R; Miller, RD; Morris, RB, 1982
)
0.26
" The extent of inhibition was in parallel with the dosage of the drugs used."( The inhibition and protection of cholinesterase by physostigmine and pyridostigmine against Soman poisoning in vivo.
Pei, SQ; Wang, LX; Xia, DY,
)
0.13
"6 ng per ml) of a myasthenic patient over a period of twelve hours with repeated dosing of neostigmine bromide (30 mg) and pyridostigmine bromide (60 mg)."( The simultaneous monitoring of plasma levels of neostigmine and pyridostigmine in man.
Chan, K; Davison, SC; Dehghan, A; Hyman, N; Prentis, RA, 1980
)
0.47
" These findings demonstrate that the PB dosage used by military personnel, as a pharmacological defense against nerve-agent poisoning, should not cause any adverse thermoregulatory or metabolic effects during moderate activity in cold climates."( Pyridostigmine bromide does not alter thermoregulation during exercise in cold air.
Freund, BJ; Roberts, DE; Sawka, MN; Young, AJ, 1994
)
1.73
" After operation the patient became asymptomatic on treatment with low dosage pyridostigmine (3 x 30 mg)."( [Myasthenia gravis in AIDS and neurosyphilis].
Hagenah, R; Schneider, U; Wüllenweber, M, 1993
)
0.29
" administration decreased at high doses of each drug and the dose-response curves were biphasic."( Pharmacodynamic analysis of contractile potentiation by cholinesterase inhibitors in rats.
Iga, T; Sawada, Y; Yamamoto, K, 1996
)
0.29
" Phase I determined the acute oral lethal dose-response relationship of each compound with the vehicle, propylene glycol."( Acute oral toxicity study of pyridostigmine bromide, permethrin, and DEET in the laboratory rat.
Beall, P; Ferguson, JW; Johnson, MS; Leach, G; Lee, R; McCain, WC; Whaley, JE, 1997
)
0.59
" With the present dosage regimen of 30 mg every 8 hours, 30% of individuals may not have red blood cell acetylcholinesterase inhibition > 10% at the time of the trough."( Population pharmacokinetics and pharmacodynamics of pyridostigmine bromide for prophylaxis against nerve agents in humans.
Brueckner, RP; Kaminskis, A; Lasseter, KC; Lin, E; Marino, MT; Schuster, BG, 1998
)
0.55
" Both the duration and the magnitude of the exaggerated startle responses were related to the dosage of PB."( Persistently exaggerated startle responses in rats treated with pyridostigmine bromide.
Beldowicz, D; Guo, W; Natelson, BH; Ottenweller, JE; Servatius, RJ; Zhu, G, 1998
)
0.54
" Proestrous females dosed at 30 mg/kg had much higher pyridostigmine bromide serum levels than metestrous females and males."( Pyridostigmine bromide alters locomotion and thigmotaxis of rats: gender effects.
Cody, BA; Hoy, JB; Karlix, JL; Schmidt, CJ; Tebbett, IR; Toffollo, S; Van Haaren, F; Wielbo, D, 1999
)
1.99
" The required dosage of pyridostigmine had fallen by two thirds after 5 years."( Early and late results after thymectomy in myasthenia gravis: a retrospective study [correction of analysis].
Dauben, HP; Gams, E; Granetzny, A; Heidenreich, F; Klein, M; Madjlessi, F; Schulte, HD, 1999
)
0.3
"05) increased levels of 3-nitrotyrosine starting 24 h after dosing compared with control urine samples."( Induction of urinary excretion of 3-nitrotyrosine, a marker of oxidative stress, following administration of pyridostigmine bromide, DEET (N,N-diethyl-m-toluamide) and permethrin, alone and in combination in rats.
Abou-Donia, MB; Abu-Qare, AW; Suliman, HB, 2001
)
0.52
" Scoping trials were performed to establish appropriate dose-response ranges for sarin and control chemicals."( Actions of pyridostigmine and organophosphate agents on chick cells, mice, and chickens.
Coatney, EM; Henderson, JD; Nieberg, PS; Spencer, PS; Wilson, BW, 2002
)
0.31
" To perform a double-blind, cross-over, dose-response study of PB in 67 healthy, young volunteers (31 women, 36 men)."( Physiological and performance effects of pyridostigmine bromide in healthy volunteers: a dose-response study.
Cook, MR; Gerkovich, MM; Graham, C; Sastre, A, 2002
)
0.58
" Supervised administration of placebo (PL) and PB (every 8 h/5 days) occurred in each of two dosing weeks, separated by a non-dosing week."( Physiological and performance effects of pyridostigmine bromide in healthy volunteers: a dose-response study.
Cook, MR; Gerkovich, MM; Graham, C; Sastre, A, 2002
)
0.58
" Dose-response effects were found only for HF HRV, and RMS error."( Physiological and performance effects of pyridostigmine bromide in healthy volunteers: a dose-response study.
Cook, MR; Gerkovich, MM; Graham, C; Sastre, A, 2002
)
0.58
" Its dosage rate in the treatment of myastenia gravis is frequent due to the short half-life and it exhibits side effects."( Preparation and in vitro evaluation of pyridostigmine bromide microparticles.
Demirel, M; Hegazy, N; Yazan, Y, 2002
)
0.58
" The acute, oral maximum-tolerated dosage (MTD) of pyridostigmine was estimated at 30 mg/kg."( Acute and repeated restraint stress have little effect on pyridostigmine toxicity or brain regional cholinesterase inhibition in rats.
Bressler, J; Pope, C; Pruett, S; Song, X; Tian, H, 2002
)
0.31
" IPPSFs (n=4/treatment) were topically dosed with mixtures of permethrin, DEET, and permethrin/DEET, in ethanol."( Pyridostigmine bromide modulates topical irritant-induced cytokine release from human epidermal keratinocytes and isolated perfused porcine skin.
Baynes, RE; Monteiro-Riviere, NA; Riviere, JE, 2003
)
1.76
"Full toxicologic profiles of chemical mixtures, including dose-response extrapolations to realistic exposures, is a prohibitive analytical problem, even for a restricted class of chemicals."( Protein binding of isofluorophate in vivo after coexposure to multiple chemicals.
Buchholz, BA; Keating, GA; Vogel, JS, 2002
)
0.31
" DEET absorption was enhanced by coinfusion of pyridostigmine bromide and DFP, by the presence of sulfur mustard, or by dosing under complete occlusion."( Percutaneous absorption of topical N,N-diethyl-m-toluamide (DEET): effects of exposure variables and coadministered toxicants.
Baynes, RE; Brooks, JD; Monteiro-Riviere, NA; Riviere, JE; Yeatts, JL, 2003
)
0.58
") was given 60 min after paraoxon dosing and rats were evaluated for cholinergic toxicity just prior to sacrifice 60 min later."( Combined forced running stress and subclinical paraoxon exposure have little effect on pyridostigmine-induced acute toxicity in rats.
Pope, CN; Shaikh, J, 2003
)
0.32
" We evaluated the effects of daily physical (treadmill running) stress or daily exposure to a subclinical dosage of the organophosphate ChE inhibitor paraoxon (PO) on ChE inhibition in blood, diaphragm and selected brain regions in young adult male Sprague-Dawley rats following subacute PYR exposures."( Effects of daily stress or repeated paraoxon exposures on subacute pyridostigmine toxicity in rats.
Chakraborty, D; Karanth, S; Pope, CN; Pruett, S; Shaikh, J, 2003
)
0.32
" We investigated the dose-response effects of these chemicals, alone or in combination, on the sensorimotor performance and cholinergic system of male Sprague-Dawley rats."( Co-exposure to pyridostigmine bromide, DEET, and/or permethrin causes sensorimotor deficit and alterations in brain acetylcholinesterase activity.
Abdel-Rahman, A; Abou-Donia, MB; Bullman, SL; Dechkovskaia, AM; Goldstein, LB; Khan, WA, 2004
)
0.68
"Pyridostigmine has been proposed for the treatment of postural orthostatic tachycardia syndrome in adults at a dose of 60 mg twice daily, but no dosing recommendation exists for children."( Pharmacokinetics of pyridostigmine in a child with postural tachycardia syndrome.
Christians, U; Filler, G; Gow, RM; Jacob, P; Johnson, G; Nadarajah, R; Zhang, YL, 2006
)
0.33
" PB dosing was selected to induce an inhibition of erythrocyte acetylcholinesterase by 30%."( Development of methods to measure humoral immune responses against selected antigens in the common marmoset (Callithrix jacchus) and the effect of pyridostigmine bromide administration.
Brown, AP; Griffiths, GD; Hornby, RJ; Jagger, CP; Pearce, PC; Pritchard, DI; Scott, L; Stoten, A, 2006
)
0.53
"05) among the three dosage forms (IV injection, commercial IR tablets and the PB-SR pellet)."( An investigation of acetylcholine released in skeletal muscle and protein unbound drug released in blood based on the pyridostigmine bromide (pretreatment drug) sustained-release pellets by microdialysis technique in the rabbit model.
Cham, TM; Cheng, CJ; Chuo, WH; Huang, YT; Lai, TF; Tsai, TH; Tsai, TR, 2007
)
0.55
" The dosing of PYD was 60 mg tid for 6 months."( A combination of 6 months of treatment with pyridostigmine and triweekly exercise fails to improve insulin-like growth factor-I levels in fibromyalgia, despite improvement in the acute growth hormone response to exercise.
Bennett, RM; Burckhardt, CS; Deodhar, AA; Hanson, GC; Jones, KD; Perrin, NA, 2007
)
0.34
" There were no significant differences in gender, age, the duration of symptoms before treatment, the dosage of pyridostigmine, and the initial presentations of ptosis or diplopia between the two groups."( Factors associated with insensitivity to pyridostigmine therapy in Thai patients with ocular myasthenia gravis.
Chirapapaisan, N; Chuenkongkaew, W; Tanormrod, S, 2007
)
0.34
" Dosing simulations suggested that 30 mg repeated every six hours might be needed to achieve steady-state trough percentage inhibition above the recommended 10% in healthy Chinese males."( Retrospective population pharmacokinetic/pharmacodynamic analysis of pyridostigmine, a cholinesterase inhibitor, in Chinese males.
Lee, JD; Loke, WK; Moochhala, S; Seng, KY; Zhao, B, 2009
)
0.35
" For Chinese males, the dosing interval may have been shorter than that recommended for the Caucasian population."( Retrospective population pharmacokinetic/pharmacodynamic analysis of pyridostigmine, a cholinesterase inhibitor, in Chinese males.
Lee, JD; Loke, WK; Moochhala, S; Seng, KY; Zhao, B, 2009
)
0.35
" At this time, the dose-response curve for atracurium on the immobilized side was shifted to the left in the pyridostigmine group."( Continuous administration of pyridostigmine improves immobilization-induced neuromuscular weakness.
Blobner, M; Fink, H; Frick, CG; Helming, M; Martyn, JA, 2010
)
0.36
" The sustained-release dosage form of pyridostigmine (SR-Pyr) is only available in a limited number of countries (e."( Benefits from sustained-release pyridostigmine bromide in myasthenia gravis: results of a prospective multicenter open-label trial.
Köhler, W; Sieb, JP, 2010
)
0.64
"In this non-interventional prospective open-label trial, 72 patients with stable myasthenia gravis were switched from instant-release dosage forms of pyridostigmine bromide to SR-Pyr."( Benefits from sustained-release pyridostigmine bromide in myasthenia gravis: results of a prospective multicenter open-label trial.
Köhler, W; Sieb, JP, 2010
)
0.84
" We have assessed in vivo the mortality-reducing efficacy of a group of known AChE inhibitors, when given in equitoxic dosage before exposure to the OPC paraoxon."( Usefulness of administration of non-organophosphate cholinesterase inhibitors before acute exposure to organophosphates: assessment using paraoxon.
Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA; Shafiullah, M, 2013
)
0.39
" In one case, respiratory symptoms were alleviated when pyridostigmine dosage was reduced."( Asthma as a cause of persistent dyspnea in treated myasthenia gravis patients.
Charloux, A; De Sèze, J; Echaniz-Laguna, A; Enache, I; Oswald-Mammosser, M; Philippi, N; Pistea, C, 2012
)
0.38
" If asthma is diagnosed, a bronchodilator treatment should be instituted and a reduction in pyridostigmine dosage should be proposed."( Asthma as a cause of persistent dyspnea in treated myasthenia gravis patients.
Charloux, A; De Sèze, J; Echaniz-Laguna, A; Enache, I; Oswald-Mammosser, M; Philippi, N; Pistea, C, 2012
)
0.38
" Here, an economic complexation technology combined with direct tablet compression method has been developed to meet the requirements of a patient friendly dosage known as taste-masked dispersible tablets loaded PTB (TPDPTs): (1) TPDPTs should have optimal disintegration and good physical resistance (hardness); (2) a low-cost, simple but practical preparation method suitable for industrial production is preferred from a cost perspective."( Design and evaluation of an economic taste-masked dispersible tablet of pyridostigmine bromide, a highly soluble drug with an extremely bitter taste.
Tan, Q; Teng, Y; Zhang, J; Zhang, L, 2012
)
0.61
" Protection was quantified using Cox analysis by determining the relative risk (RR) of death in rats that were administered these AChE inhibitors in equitoxic dosage (25% of LD01) 30 min before azinphos-methyl exposure."( Reversible cholinesterase inhibitors as pre-treatment for exposure to organophosphates: assessment using azinphos-methyl.
Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA, 2015
)
0.42
" The MG foundation of America (MGFA) classification, MGFA post-intervention status, dosage of prednisolone and pyridostigmine, and anti-acetylcholine receptor antibody titers were evaluated."( Two-year outcome of thymectomy in non-thymomatous late-onset myasthenia gravis.
Himuro, K; Kanai, T; Kawaguchi, N; Kuwabara, S; Oda, F; Uzawa, A; Yoshida, S; Yoshino, I, 2015
)
0.42
" The dosage of acetylcholine receptor autoantibodies was normal."( [Juvenile myasthenia gravis in sub-Saharan Africa: a case study of two consanguine sisters born from consanguinity in Togo].
Agba, AI; Apetse, K; Ayena, KD; Balo, KP; Balogou, KA; Diatewa, BM; Domingo, SA; Maneh, N, 2017
)
0.46
" Little is known about the role and dosing of pyridostigmine in pediatric GI motility disorders."( Application of Pyridostigmine in Pediatric Gastrointestinal Motility Disorders: A Case Series.
Camilleri, M; Di Lorenzo, C; Grothe, R; Manini, ML, 2018
)
0.48
" A 42-year-old woman with rheumatoid arthritis (RA) refractory to methotrexate, was treated with adalimumab (ADA), a human monoclonal antibody against the TNF, in a dosage scheme of 40 mg every 14 days subcutaneously."( Adalimumab-induced myasthenia gravis: case-based review.
Drosos, AA; Markatseli, TE; Memi, T; Pelechas, E; Voulgari, PV, 2020
)
0.56
" The dosage of pyridostigmine bromide was reduced for 69."( Effect of treatment with Fufang Huangqi decoction on dose reductions and discontinuation of pyridostigmine bromide tablets, prednisone, and tacrolimus in patients with type I or II myasthenia gravis.
Caifeng, S; Haiou, P; Jingsheng, Z; Wenjun, Q; Xueshi, H; Yi, L; Zhanyou, W, 2022
)
1.29
"Patients with poor Osserman stages, higher preoperative dosage of pyridostigmine bromide, higher ASA score, poor pulmonary function (low DLCO%), and more intraoperative bleeding should be highly vigilant for the occurrence of postoperative myasthenic crisis."( Analysis of influencing factors of postoperative myasthenic crisis in 564 patients with myasthenia gravis in a single center.
Huang, C; Jiao, P; Li, D; Liu, Y; Ma, C; Sun, Y; Tian, W; Tong, H; Wu, F; Wu, J; Wu, Q; Yu, H, 2023
)
1.15
"013), pyridostigmine dosage greater than 240 (P < 0."( Analysis of influencing factors of perioperative myasthenic crisis in 387 myasthenia gravis patients without thymoma in a single center.
Huang, C; Jiao, P; Li, D; Liu, Y; Ma, C; Sun, Y; Tian, W; Tong, H; Wu, F; Wu, J; Wu, Q; Yu, H, 2023
)
0.91
"Patients with poor Osserman classification, history of myasthenic crisis before surgery, larger preoperative dosage of pyridostigmine, and higher ASA scores should be highly alert to the occurrence of postoperative myasthenic crisis."( Analysis of influencing factors of perioperative myasthenic crisis in 387 myasthenia gravis patients without thymoma in a single center.
Huang, C; Jiao, P; Li, D; Liu, Y; Ma, C; Sun, Y; Tian, W; Tong, H; Wu, F; Wu, J; Wu, Q; Yu, H, 2023
)
0.91
" The studies had heterogenous inclusion criteria, dosing regimens and reported outcomes."( Pyridostigmine in chronic intestinal pseudo-obstruction - a systematic review.
Behrenbruch, C; Johnston, M; Keck, JO; Noori, J; Wilkie, BD; Woods, R, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyridinium salt
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.00350.003245.467312,589.2998AID2517
Chain A, Beta-lactamaseEscherichia coli K-12Potency3.98110.044717.8581100.0000AID485341
endonuclease IVEscherichia coliPotency12.58930.707912.432431.6228AID1708
acetylcholinesteraseHomo sapiens (human)Potency10.10640.002541.796015,848.9004AID1347395; AID1347397; AID1347398; AID1347399
RAR-related orphan receptor gammaMus musculus (house mouse)Potency4.28290.006038.004119,952.5996AID1159521; AID1159523
AR proteinHomo sapiens (human)Potency28.22630.000221.22318,912.5098AID743040; AID743054
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.83250.000214.376460.0339AID720691
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.01680.001530.607315,848.9004AID1224821
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.60320.000229.305416,493.5996AID743079
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency2.11300.001024.504861.6448AID743215
alpha-galactosidaseHomo sapiens (human)Potency10.00004.466818.391635.4813AID2107
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.22020.035520.977089.1251AID504332
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency5.62340.00798.23321,122.0200AID2546
gemininHomo sapiens (human)Potency0.81990.004611.374133.4983AID624296
M-phase phosphoprotein 8Homo sapiens (human)Potency0.79430.177824.735279.4328AID488949
lamin isoform A-delta10Homo sapiens (human)Potency0.89130.891312.067628.1838AID1487
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency1.41250.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)13.57000.00000.933210.0000AID1313870; AID465559; AID491761
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (36)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (79)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID212893Acute toxicity was evaluated in rat1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
In vitro and in vivo protection of acetylcholinesterase against organophosphate poisoning by pretreatment with a novel derivative of 1,3,2-dioxaphosphorinane 2-oxide.
AID491761Inhibition of human whole RBC AChE pretreated for 30 mins by Ellman technique2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
AID1313873Acute toxicity in ip dosed mouse measured after 72 hrs2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1313872Selectivity ratio, ratio of IC50 for human plasma BChE to IC50 for human AChE2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
AID1313874Selectivity ratio, ratio of Ki for horse serum BChE to Ki for fetal bovine serum AChE2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
AID465560Inhibition of human plasma BChE after 5 mins by Ellman's method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications.
AID465559Inhibition of human erythrocyte AChE after 5 mins by Ellman's method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications.
AID212892Acute toxicity was evaluated in mouse1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
In vitro and in vivo protection of acetylcholinesterase against organophosphate poisoning by pretreatment with a novel derivative of 1,3,2-dioxaphosphorinane 2-oxide.
AID1313871Inhibition of human plasma BChE assessed as butyrylthiocholine hydrolysis preincubated for 10 mins followed by addition of substrate measured after 2 mins by spectrophotometric method2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID226941Protective ratio of compound (10 mg/kg) against soman poisoning, given subcutaneously to mice 30 min prior to treatment by TAB1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
In vitro and in vivo protection of acetylcholinesterase against organophosphate poisoning by pretreatment with a novel derivative of 1,3,2-dioxaphosphorinane 2-oxide.
AID491762Inhibition of human plasma BChE pretreated for 30 mins by Ellman technique2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
AID1313870Inhibition of human AChE assessed as acetylthiocholine hydrolysis preincubated for 10 mins followed by addition of substrate measured after 2 mins by spectrophotometric method2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
AID491763Selectivity ratio of IC50 for human plasma BChE to IC50 for human whole RBC AChE2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,688)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990457 (27.07)18.7374
1990's432 (25.59)18.2507
2000's359 (21.27)29.6817
2010's321 (19.02)24.3611
2020's119 (7.05)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 65.04

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index65.04 (24.57)
Research Supply Index7.59 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index114.92 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (65.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials179 (9.99%)5.53%
Reviews95 (5.30%)6.00%
Case Studies381 (21.26%)4.05%
Observational5 (0.28%)0.25%
Other1,132 (63.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (36)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effects of Vagal Dysfunction on Gastrointestinal and Inflammatory Pathways in HIV [NCT04353778]Phase 1/Phase 2150 participants (Anticipated)Interventional2020-08-03Recruiting
The Exercise Response to Pharmacologic Cholinergic Stimulation in Myalgic Encephalomyelitis / Chronic Fatigue Syndrome [NCT03674541]Phase 245 participants (Actual)Interventional2020-01-14Completed
Autonomic Neuropathy, Gastrointestinal Motility, and Inflammation in HIV [NCT02850276]Early Phase 176 participants (Actual)Interventional2015-11-30Completed
Double-Blind, Placebo-Controlled Study of Pyridostigmine in Postural Tachycardia Syndrome [NCT00409435]Phase 250 participants (Anticipated)Interventional2006-10-31Recruiting
Pyridostigmine Efficacy and Safety for Treatment of Ileus After Colorectal Surgery (PESTI Trial) [NCT05334485]Phase 2/Phase 350 participants (Anticipated)Interventional2023-12-31Not yet recruiting
Comparison of Effect of Propranolol, Bisoprolol, Pyridosgitmine in Postural Orthostatic Tachycardia Syndrome (POTS) and Prognosis After Medical Treatment [NCT02171988]Phase 4150 participants (Actual)Interventional2014-03-31Completed
Effect of Pyridostigmine (Mestinon) on Muscle Strength in Myasthenia Gravis [NCT03510546]Phase 444 participants (Anticipated)Interventional2018-04-09Recruiting
Study of the Role of Peripheral Acetylcholinesterase Inhibitor Pyridostigmine as Immunomodulators in a Population of Patients Living With Human Immunodeficiency Virus Infection. [NCT03312244]Phase 260 participants (Anticipated)Interventional2019-07-01Suspended(stopped due to Due to COVID-19, effective 3/19/2020 recruitment is halted until further notice)
Gastrointestinal Motility Among Diabetes Patients [NCT02573519]40 participants (Actual)Interventional2015-10-31Terminated(stopped due to Renewal of PET/CT scanners and slow recruitment)
IMproving Symptomatic Treatment With Pyridostigmine and Amifampridine: a Randomized Double-blinded, Placebo Controlled Crossover Trial in Patients With Myasthenia Gravis (IMPACT-MG) [NCT05919407]Phase 324 participants (Anticipated)Interventional2023-03-22Recruiting
The Effects of Normalizing Blood Pressure on Cerebral Blood Flow in Hypotensive Individuals With Spinal Cord Injury [NCT02893553]Phase 241 participants (Actual)Interventional2016-12-31Completed
Prospective Observational Trial to Evaluate Clinical Prognosis and the Risk Factors for Progression for Myasthenia Gravis Patients [NCT04101578]2,000 participants (Anticipated)Observational2017-02-08Recruiting
Pyridostigmine and Its Effects on Autonomic Modulation in Diabetic Patients With Autonomic Neuropathy [NCT00953914]40 participants (Actual)Interventional2005-03-31Completed
Vagal Stimulation in POTS - The Autonomic Inflammatory Reflex (Pilot 3) [NCT03124355]Phase 111 participants (Actual)Interventional2017-09-30Active, not recruiting
A Monocentric Randomized, Controlled, Double Blind, Crossover Phase II Trial to Show Non-inferiority of the Effect of Pyridostigmine Bromide vs. Fludrocortisone on Symptoms of Autonomic Dysregulation in Parkinson's Disease [NCT01993680]Phase 218 participants (Actual)Interventional2012-06-30Completed
Evaluation and Treatment of Autonomic Failure. [NCT00223691]Phase 1389 participants (Actual)Interventional2002-03-31Completed
Addition of Pyridostigmine to Conventional Management of Postdural Puncture Headache [NCT05969119]Phase 430 participants (Anticipated)Interventional2023-07-31Not yet recruiting
Pyridostigmine in Diabetics With Constipation: Randomized, Placebo-controlled, Double-blind Trial [NCT00276406]Phase 1/Phase 230 participants (Actual)Interventional2006-05-31Completed
Safety and Efficacy Study of Anti-cholinesterase Therapy on the Motor Functions in Patients With Spinal Muscular Atrophy Type 3. [NCT02227823]Phase 24 participants (Actual)Interventional2014-07-31Completed
A Phase II, Mono-center, Placebo-controlled, Double-blind, Crossover Trial to Investigate Effect and Efficacy of Pyridostigmine in Dutch Patients With Spinal Muscular Atrophy Types 2, 3 and 4 [NCT02941328]Phase 239 participants (Actual)Interventional2015-12-31Completed
Sleep, Fatigue, and Dexamethosone in Childhood Cancer [NCT00075101]Phase 3134 participants (Anticipated)Interventional2000-09-30Completed
Pilot Study of an ACh-E Inhibitor Upon Immune Activation Markers in HIV-1 Infected Patients Receiving Highly Active Antiretroviral Therapy (HAART) Showing an Incomplete Immune Response. [NCT00518154]Phase 27 participants (Actual)Interventional2007-09-30Completed
Treatment Trial of Droxidopa and Pyridostigmine to Improve Orthostatic Hypotension Without Aggravating Supine Hypertension [NCT01370512]Phase 230 participants (Anticipated)Interventional2011-11-30Suspended(stopped due to Plan to increase enrollment due to preliminary data having lower statistical power than anticipated.)
Pyridostigmine in Patients With Severe Acute Respiratory Syndrome Secondary to SARS-CoV-2 Infection [NCT04343963]Phase 2/Phase 3436 participants (Anticipated)Interventional2020-04-04Recruiting
Comparison of the Effectiveness of Rocuronium - Sugammadex With Succinylcholine-Cisatracurium-Neostigmine in Patients Undergoing Laser Microlaryngeal Surgery [NCT02329964]Phase 480 participants (Actual)Interventional2015-02-28Active, not recruiting
Cardiovagal Baroreflex Deficits Impair Neurovascular Coupling and Cognition in Postural Tachycardia Syndrome [NCT03261570]Early Phase 151 participants (Actual)Interventional2017-07-01Completed
Pyridostigmine for the Treatment of Constipation in Parkinson Disease [NCT05603715]Phase 216 participants (Anticipated)Interventional2022-08-10Recruiting
Pilot Study of the Efficacy of Pyridostigmine for Reversal of Post Injection Dysphonia Following Botulinum Neurotoxin Laryngeal Chemo-Denervation in Spasmodic Dysphonia [NCT05110417]Phase 410 participants (Anticipated)Interventional2021-05-20Recruiting
TheRapeutic Effect of Different immunosuppressAnts on Non-Thymoma Ocular Myasthenia Gravis: a Real-world Study [NCT04182984]200 participants (Anticipated)Observational [Patient Registry]2019-11-04Recruiting
Effectiveness and Safety of Tacrolimus Combined With Low-dose Prednisone for Treatment of Myasthenia Gravis: A Real-world Study [NCT04768465]160 participants (Anticipated)Observational [Patient Registry]2021-01-01Recruiting
Maximizing Exercise Effectiveness in Fibromyalgia [NCT00535587]Phase 2178 participants (Actual)Interventional2002-09-30Completed
Evaluation of Respiratory and Skeletal Muscle Functions in Response to Acetylcholinesterase Inhibitors in Pompe Disease [NCT02357225]Early Phase 12 participants (Actual)Interventional2015-08-31Terminated(stopped due to The drug was ineffective in improving function in Pompe's disease)
Augmentation of Parasympathetic Signaling With Pyridostigmine in Heart Failure [NCT01415921]Phase 233 participants (Actual)Interventional2011-10-31Completed
Using Acetylcholinesterase Inhibitors to Promote Insulin Secretion in Human Beings [NCT03063515]Phase 112 participants (Actual)Interventional2017-04-19Completed
Acetylcholinesterase Inhibition: A Novel Approach in the Treatment of Orthostatic Hypotension in Spinal Cord Injury [NCT02307526]Phase 210 participants (Actual)Interventional2011-01-31Completed
Treatment and Prognosis of Neurogenic Orthostatic Hypotension : A Prospective Randomized Study [NCT02308124]Phase 487 participants (Actual)Interventional2014-11-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00276406 (12) [back to overview]Sense of Completely Emptying Bowels
NCT00276406 (12) [back to overview]Ascending Colon Emptying Half-time (AC t1/2) Measured in Hours
NCT00276406 (12) [back to overview]Colonic Filling at 6 Hours
NCT00276406 (12) [back to overview]Colonic Geometric Center at 24 Hours (GC24) Measured by Scintigraphy
NCT00276406 (12) [back to overview]Colonic Geometric Center at 48 Hours (GC48) as Measured by Scintigraphy
NCT00276406 (12) [back to overview]Gastric Emptying Half-time (GE t1/2)
NCT00276406 (12) [back to overview]QTc Interval Before and After Treatment
NCT00276406 (12) [back to overview]Heart Rate Before and After Treatment
NCT00276406 (12) [back to overview]Stool Frequency Per Week
NCT00276406 (12) [back to overview]Stool Frequency Per Day
NCT00276406 (12) [back to overview]Stool Form/Consistency
NCT00276406 (12) [back to overview]Stool Ease of Passage
NCT00518154 (1) [back to overview]CD4+ Cell Count Change Between Basal and Week 16 of Additive Treatment
NCT00535587 (1) [back to overview]Levels of Growth Hormone Post Exercise
NCT01415921 (2) [back to overview]Post Exercise Heart Rate Recovery
NCT01415921 (2) [back to overview]Baseline Heart Rate Recovery
NCT02307526 (3) [back to overview]Systolic Blood Pressure
NCT02307526 (3) [back to overview]Diastolic Blood Pressure
NCT02307526 (3) [back to overview]Heart Rate
NCT02308124 (5) [back to overview]Changes in Health-related Quality of Life
NCT02308124 (5) [back to overview]Short-form 36 Version 2
NCT02308124 (5) [back to overview]Change in Orthostatic BP Drop
NCT02308124 (5) [back to overview]Change of the Depression Score (Beck Depression Inventory-II )
NCT02308124 (5) [back to overview]Change of the Orthostatic Hypotension Associated Symptom Questionnaire (OH Questionnaire (OHQ)).
NCT02329964 (9) [back to overview]Addition of Neuromuscular Blocking Agents
NCT02329964 (9) [back to overview]Anesthesia Time
NCT02329964 (9) [back to overview]Length of Stay in te Operating Room
NCT02329964 (9) [back to overview]Recovery of T1 to 10%
NCT02329964 (9) [back to overview]Recovery of T1 to 90%
NCT02329964 (9) [back to overview]Surgical Rating Score
NCT02329964 (9) [back to overview]Time to Extubation
NCT02329964 (9) [back to overview]Time to First Spontaneous Breath
NCT02329964 (9) [back to overview]Time to Eye Opening
NCT02850276 (8) [back to overview]Number of Participants With Reduction in Small Intestinal Bacterial Overgrowth (SIBO)
NCT02850276 (8) [back to overview]Change in sCD14 Level
NCT02850276 (8) [back to overview]Change in IL-6 Plasma Level
NCT02850276 (8) [back to overview]Change in Breath Test
NCT02850276 (8) [back to overview]The Composite Autonomic Symptom Score (COMPASS)
NCT02850276 (8) [back to overview]Medical Outcomes Study Questionnaire
NCT02850276 (8) [back to overview]Mean Percent Retention of Gastric Contents on Gastric Emptying Study
NCT02850276 (8) [back to overview]Change in TNFα Level
NCT03674541 (12) [back to overview]Borg Fatigue Scale
NCT03674541 (12) [back to overview]Change in Peak Oxygen Uptake (Peak VO2) Between the First and Second iCPET
NCT03674541 (12) [back to overview]Peak (Ca-vO2)/[Hgb]
NCT03674541 (12) [back to overview]Peak Cardiac Output (Qc)
NCT03674541 (12) [back to overview]Peak Pulmonary Arterial Wedge Pressure (PAWP)
NCT03674541 (12) [back to overview]Peak Stroke Volume (SV)
NCT03674541 (12) [back to overview]Peak Right Atrial Pressure (RAP)
NCT03674541 (12) [back to overview]Ventilatory Efficiency (VE/VCO2)
NCT03674541 (12) [back to overview]Peak-Rest Right Atrial Pressure (RAP)
NCT03674541 (12) [back to overview]Peak-Rest Oxygen Uptake (VO2)
NCT03674541 (12) [back to overview]Borg Dyspnea Scale
NCT03674541 (12) [back to overview]Peak-Rest Cardiac Output (Qc)

Sense of Completely Emptying Bowels

During 9 days of the baseline period and during 17 days of the treatment period, subjects used a daily diary to record whether or not they felt they had completely emptied their bowels(1= Yes; 0= No). Only the 7 days of highest treatment dose will be used for comparison purposes. (NCT00276406)
Timeframe: Daily during baseline period (9 days), Treatment period (7 days)

,
Interventionpercentage of bowel movements (Mean)
BaselineTreatment
Placebo7466
Pyridostigmine8673

[back to top]

Ascending Colon Emptying Half-time (AC t1/2) Measured in Hours

Calculated by linear interpolation of values on the AC emptying curve. (NCT00276406)
Timeframe: Baseline period (days 7-9 ), Treatment period (days 14-17)

,
Interventionhours (Mean)
BaselineTreatment
Placebo20.5918.77
Pyridostigmine16.7310.44

[back to top]

Colonic Filling at 6 Hours

The proportion of a radio-labeled meal in the colon at 6 hours (identifiable by radio-labelled tracer to capsule eaten with meal), measured by scintigraphy. This is an indirect measurement of small-bowel transit time. (NCT00276406)
Timeframe: Baseline period (9 days), Treatment period (7 days)

,
Interventionpercentage of meal (Mean)
BaselineTreatment
Placebo4148
Pyridostigmine3753

[back to top]

Colonic Geometric Center at 24 Hours (GC24) Measured by Scintigraphy

The scintigraphic method is used to measure colonic transit. An isotope is adsorbed on activated charcoal particles and delivered to the colon in a delayed release capsule. Anterior and posterior gamma images of the abdomen are taken hourly for the first 6 hours after the radio-labeled meal, then at 8, 24 and 48 hours. The geometric center (GC) is the weighted average of counts in the different colonic regions. The scale ranges from 1 to 5; a high GC implies faster colonic transit, a GC of 1 implies all isotope is in the ascending colon, and a GC of 5 implies all isotope is in the stool. GC24 is the measurement taken at 24 hours after the radio-labeled meal. (NCT00276406)
Timeframe: Baseline period (days 7-9 ), Treatment period (days 14-17)

,
Interventionunits on a scale (Mean)
BaselineTreatment
Placebo1.981.84
Pyridostigmine1.962.45

[back to top]

Colonic Geometric Center at 48 Hours (GC48) as Measured by Scintigraphy

The scintigraphic method is used to measure colonic transit. An isotope is adsorbed on activated charcoal particles and delivered to the colon in a delayed release capsule. Anterior and posterior gamma images are taken hourly for the first 6 hours after the radio-labeled meal, then at 8, 24 and 48 hours. The geometric center (GC) is the weighted average of counts in the different colonic regions. The scale ranges from 1 to 5; a high GC implies faster colonic transit, a GC of 1 implies all isotope is in the ascending colon, and a GC of 5 implies all isotope is in the stool. GC48 is the measurement taken at 48 hours after the radio-labeled meal. (NCT00276406)
Timeframe: Baseline period (days 7-9 ), Treatment period (days 14-17)

,
Interventionunits on a scale (Mean)
BaselineTreatment
Placebo2.973.26
Pyridostigmine2.923.59

[back to top]

Gastric Emptying Half-time (GE t1/2)

The measure of time for 50 percent of a radio-labeled meal to empty from the stomach. (NCT00276406)
Timeframe: Baseline period (9 days), Treatment period (7 days)

,
Interventionminutes (Mean)
BaselineTreatment
Placebo141121
Pyridostigmine142122

[back to top]

QTc Interval Before and After Treatment

The corrected QT interval (QTc) is a measurement of time (seconds) between the Q and T waves of an heart beat as recorded during an Electrocardiogram (ECG). (NCT00276406)
Timeframe: Baseline period (9 days), Treatment period (7 days)

,
InterventionMilliseconds (Mean)
BaselineTreatment
Placebo420421
Pyridostigmine428415

[back to top]

Heart Rate Before and After Treatment

Heart rate is the number of beats per minute, as recording on an Electrocardiogram (ECG). (NCT00276406)
Timeframe: Baseline period (9 days), Treatment period (7 days)

,
Interventionbeats per minute (Mean)
BaselineTreatment
Placebo7675
Pyridostigmine7466

[back to top]

Stool Frequency Per Week

During 9 days of the baseline period and during 17 days of the treatment period, subjects used a daily diary to record the number of times per day they had a bowel movement. Complete spontaneous bowel movements per week are reported. Only the 7 days of highest treatment dose will be used for comparison purposes. (NCT00276406)
Timeframe: Daily during baseline period (9 days), Treatment period (7 days)

,
InterventionNumber complete bowel movements per week (Mean)
BaselineTreatment
Placebo2.13.1
Pyridostigmine2.14.0

[back to top]

Stool Frequency Per Day

During 9 days of the baseline period and during 17 days of the treatment period, subjects used a daily diary to record the number of times per day they had a bowel movement. Only the 7 days of highest treatment dose will be used for comparison purposes. (NCT00276406)
Timeframe: Daily during baseline period (9 days), Treatment period (7 days)

,
InterventionNumber of bowel movements (Mean)
BaselineTreatment
Placebo1.21.4
Pyridostigmine0.951.5

[back to top]

Stool Form/Consistency

"During 9 days of the baseline period and during 17 days of the treatment period, subjects used a daily diary to record a description of stool consistency according to the Bristol Stool Form Scale (ranging from 1 (hard lumps) to 7 (watery)). The Bristol Stool Scale is a medical aid designed to classify the form of human feces into seven categories or types. Types 1 and 2 indicate constipation with 3 and 4 being the ideal stools especially the latter, as they are the easiest to defecate, and 5-7 tending towards diarrhea." (NCT00276406)
Timeframe: Daily during baseline period (9 days), Treatment period (7 days)

,
Interventionunits on a scale (Mean)
BaselineTreatment
Placebo2.82.6
Pyridostigmine2.53.4

[back to top]

Stool Ease of Passage

During 9 days of the baseline period and during 17 days of the treatment period, subjects used a daily diary to record a description of stool ease of passage of stool, according to the Bristol Stool Form Scale (ranging from 1 (manual disimpaction) to 7 (incontinence)). Only the 7 days at highest treatment dose will be used for comparison purposes. (NCT00276406)
Timeframe: Daily during baseline period (9 days), Treatment period (7 days)

,
Interventionunits on a scale (Mean)
BaselineTreatment
Placebo3.63.5
Pyridostigmine3.53.8

[back to top]

CD4+ Cell Count Change Between Basal and Week 16 of Additive Treatment

Change in total CD4+ T-cell number from baseline to addition of pyridostigmine (NCT00518154)
Timeframe: 16 weeks after initiation of pyridostigmine

InterventionCD4+ T-cell count/uL (Mean)
Pyridostigmine153.2

[back to top]

Levels of Growth Hormone Post Exercise

Serum growth hormone at peak V02/treadmill (NCT00535587)
Timeframe: 6 months

Interventionng/ml (Mean)
Mestinon/Exercise4.95
Placebo Pill/Attention Control1.41

[back to top]

Post Exercise Heart Rate Recovery

Change in heart rate from peak exercise to 1 minute post-exercise (beats per minute) (NCT01415921)
Timeframe: 12 weeks

Interventionbeats per minute (Mean)
Pyridostigmine Bromide38.5
Placebo34.9

[back to top]

Baseline Heart Rate Recovery

Change in peak HR at end of exercise to 1 minute post-exercise (beats per minute) (NCT01415921)
Timeframe: Baseline

Interventionbeats per minute (Mean)
Pyridostigmine Bromide32.5
Placebo30.4

[back to top]

Systolic Blood Pressure

(NCT02307526)
Timeframe: Average systolic blood pressure of 10 minutes supine rest before pyridostigmine and after 45 minutes at 45 degrees after pyridostigmine administration compared to 10 minutes supine rest before tilt and at 45 degrees during no-drug head-up tilt maneuver.

,
Interventionmm Hg (Mean)
Supine Systolic Blood Pressure45 degree Head-up Tilt Systolic Blood Pressure
NO Drug10388
Pyridostigmine Bromide9790

[back to top]

Diastolic Blood Pressure

(NCT02307526)
Timeframe: Average diastolic blood pressure of 10 minutes supine rest before pyridostigmine and after 45 minutes at 45 degrees after pyridostigmine administration compared to 10 minutes supine rest before tilt and at 45 degrees during no-drug head-up tilt maneuver.

,
Interventionmm Hg (Mean)
Supine Diastolic Blood Pressure45 degree Head-up Tilt Diastolic Blood Pressure
NO Drug6663
Pyridostigmine Bromide6464

[back to top]

Heart Rate

(NCT02307526)
Timeframe: Average heart rate of 10 minutes supine rest before pyridostigmine and after 45 minutes at 45 degrees following pyridostigmine administration compared to 10 minutes supine rest before tilt and at 45 degrees during no-drug head-up tilt maneuver.

,
Interventionbpm (Mean)
Supine Heart Rate45 degree Head-up Tilt Heart Rate
NO Drug5572
Pyridostigmine Bromide5266

[back to top] [back to top]

Short-form 36 Version 2

"changes in Short Form (36) Health Survey version 2 (SF-36v2) physical component summary scale (PCS) compared to the baseline~SF-36v2 measures eight HRQOL domains (physical functioning, role limitation caused by physical problems, bodily pain, general health, vitality, social functioning, role limitation caused by emotional problems, and mental health) summarized into two summary scales that are normalized to the population (mean=50, standard deviation=10): the physical component summary scale (PCS) and the mental component summary scale (MCS).20 Better HRQOL is reflected by higher SF-36v2 scores." (NCT02308124)
Timeframe: changes at 3 months after treatment

Interventionpoints (Mean)
Midodrine Only5.6
Pyridostigmine Only4.2
Midodrine + Pyridostigmine2.7

[back to top]

Change in Orthostatic BP Drop

Change of orthostatic SBP and DBP drop after 3-month medical treatment compared to initial results. (NCT02308124)
Timeframe: after 3-month medical treatment

,,
InterventionmmHg (Mean)
Changes in SBP dropChanges in DBP drop
Midodrine + Pyridostigmine8.97.4
Midodrine Only11.17.5
Pyridostigmine Only13.611.1

[back to top]

Change of the Depression Score (Beck Depression Inventory-II )

"Change of the depression score after 3-month medical treatment compared to initial results.~21 multiple-choice questions, each of which can be scored from 0 to 3. Higher score represent higher degree of depression.~Score Normal; 0-13, Mild depression; 14-19, Moderate depression; 20-28, Severe depression; 29-63" (NCT02308124)
Timeframe: after 3-month medical treatment.

Interventionpoints (Mean)
Midodrine Only-6.8
Pyridostigmine Only-7.8
Midodrine + Pyridostigmine-3.5

[back to top]

Change of the Orthostatic Hypotension Associated Symptom Questionnaire (OH Questionnaire (OHQ)).

"Change of the OH associated symptom survey result after 3-month medical treatment compared to initial results.~OHQ questionnaire has two components: the OH daily activity scale (OHDAS), which contains 4 items measuring the impact of OH on daily activities, and the OH symptom assessment (OHSA), which contains 6 items measuring the symptoms of OH (dizziness/light headedness, vision disturbance, weakness, fatigue, trouble concentrating, and head/neck discomfort).This questionnaire reflects the severity of OH-related symptoms on a 10-point scale, with 0 indicating the absence of a symptom and 10 indicating maximal severity.~** OHQ total score minimal 0 ~ maximal 100" (NCT02308124)
Timeframe: after 3-month medical treatment.

Interventionpoints (Mean)
Midodrine Only-16.2
Pyridostigmine Only-17.2
Midodrine + Pyridostigmine-12.6

[back to top]

Addition of Neuromuscular Blocking Agents

"Repeated small boluses or drip of Succinylcholine, or small boluses of nondepolarizing muscle relaxants with intermediate duration are usually followed.~In this protocol, cisatracurium was injected after intubation to maintain neuromuscular blockade during surgery.~We measure the requirement of additive dose of neuromuscular blocker to ensure that neuromuscular blockade remains below T2 during surgery" (NCT02329964)
Timeframe: during surgery

Interventionparticipants (Number)
R-S Group0
S-C-N Group20

[back to top]

Anesthesia Time

time from propofol injection to extubation (NCT02329964)
Timeframe: from the anesthesia start to end

Interventionminutes (Mean)
R-S Group28.4
S-C-N Group35.2

[back to top]

Length of Stay in te Operating Room

LMS surgery has short operation time and ambulatory setting. So the length of stay in the operating room will have significant. We expected the lengh of stay in the operating room is more shorter in R-S group than S-C-N group. (NCT02329964)
Timeframe: time from in to out of the operating room

Interventionminutes (Mean)
R-S Group31.0
S-C-N Group38.6

[back to top]

Recovery of T1 to 10%

we measure the time from the end of surgery to recovery of the TOF 0.1. The end of surgery is defined as the time when the direct laryngoscope, aided by an operation microscope, is removed. (NCT02329964)
Timeframe: from the end of surgery to time when the TOF ratio is 0.1, up to 30 minutes

Interventionseconds (Median)
R-S Group271
S-C-N Group190

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Recovery of T1 to 90%

we measure the time from the end of surgery to recovery of the TOF 0.9. The end of surgery is defined as the time when the direct laryngoscope, aided by an operation microscope, is removed. (NCT02329964)
Timeframe: from the end of surgery(when the surgeon removes the suspension laryngoscope ) to time when the TOF ratio is 0.9, up to 30 minutes

Interventionseconds (Median)
R-S Group377
S-C-N Group240

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Surgical Rating Score

"describe by surgeon under his subjective opinion.~1 - extremely poor conditions 2- poor conditions 3- acceptable conditions 4- good conditions 5- optimal conditions" (NCT02329964)
Timeframe: during surgery

Interventionscore (Median)
R-S Group5.0
S-C-N Group5.0

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Time to Extubation

We expected the emergence time is shorter in R-S group than S-C-N group. So we measure the time from the end of surgery to recovery of the TOF 0.9, and the time from the end of surgery to extubation (NCT02329964)
Timeframe: from the end of surgery to extubate a tracheal tube

Interventionseconds (Median)
R-S Group430
S-C-N Group380

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Time to First Spontaneous Breath

time from end of surgery to first spontaneous breaths (NCT02329964)
Timeframe: from end of surgery to first spontaneous breaths

Interventionseconds (Median)
R-S Group263
S-C-N Group240

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Time to Eye Opening

We expected the emergence time is shorter in R-S group than S-C-N group. So we measure the time from the end of surgery to opening of the eyes to verbal commands. (NCT02329964)
Timeframe: from end of surgery to opening of the eyes to verbal commands

Interventionseconds (Median)
R-S Group340
S-C-N Group300

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Number of Participants With Reduction in Small Intestinal Bacterial Overgrowth (SIBO)

"Number of participants with reduction in Small intestinal bacterial overgrowth (SIBO) assessed with breath testing after 8 weeks of treatment.~The hydrogen breath test for the detection of small intestinal bacterial overgrowth (SIBO), obtained by having participants exhale into a plastic bag. the hydrogen content of the samples is measured using a commercially available analyzer." (NCT02850276)
Timeframe: week 8

InterventionParticipants (Count of Participants)
Pyridostigmine13

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Change in sCD14 Level

Change in sCD14 level at week 8 as compared to baseline. sCD14 is a marker of macrophage activation commonly used as an indirect measure of translocation (NCT02850276)
Timeframe: Baseline and week 8

Interventionmean florescence intensity (Median)
BaselineWeek 8
Pyridostigmine25732095

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Change in IL-6 Plasma Level

Change in IL-6 plasma level at week 8 as compared to baseline. Plasma interleukin-6 (IL-6), an important inflammatory mediator which predicts mortality in HIV as well as multiple medical co-morbidities, presumably via inflammatory mechanisms. (NCT02850276)
Timeframe: Baseline and week 8

Interventionmean florescence intensity (Median)
BaselineWeek 8
Pyridostigmine30.526.5

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Change in Breath Test

Breath Test at week 8 as compared to baseline. Breath test results is the rise in the combined hydrogen and methane during the breath test. (NCT02850276)
Timeframe: baseline and week 8

Interventionppm (Median)
Baselineweek 8
Pyridostigmine2814

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The Composite Autonomic Symptom Score (COMPASS)

The gastrointestinal domain domain score of the COMPASS contains 12 items which reflect gastrointestinal symptoms of autonomic function. It is scored on a total scale of 0-28, with higher numbers reflecting worse symptoms. (NCT02850276)
Timeframe: Baseline and week 8

Interventionscore on a scale (Mean)
BaselineWeek 8
Pyridostigmine88.6

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Medical Outcomes Study Questionnaire

Medical Outcomes Study (MOS-HIV) quality of life questionnaire. It is a 35 item questionnaire covering 11 dimensions of health including physical functioning, role functioning, pain, social functioning, emotional well-being, energy/fatigue, cognitive functioning, general health, health distress, overall QOL, and health transition. The total scale ranges from 0-100 with a higher score representing better functioning and well-being. (NCT02850276)
Timeframe: Baseline and week 8

Interventionscore on a scale (Mean)
BaselineWeek 8
Pyridostigmine66.165

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Mean Percent Retention of Gastric Contents on Gastric Emptying Study

Percent retention of gastric contents on gastric emptying study. GI dysmotility calculated from gastric emptying scintigraphy - measurement of the percent retention of gastric contents at 4 hours. (NCT02850276)
Timeframe: Baseline and week 8

Interventionpercent retention of gastric contents (Mean)
Baselineweek 8
Pyridostigmine32

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Change in TNFα Level

TNFα is a pro-inflammatory cytokine which is induced by components of translocating bacteria. Change in TNFα level at week 8 compared to baseline (NCT02850276)
Timeframe: Baseline and week 8

Interventionmean florescence intensity (Median)
Baselineweek 8
Pyridostigmine134.0117.5

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Borg Fatigue Scale

Difference in perception of fatigue at peak exercise between first and second iCPETs. Used Borg Scale 0 (minimal) to 10 (maximal). (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

Interventionunits on a scale (Mean)
Study Drug - Pyridostigmine0.1
Placebo (Female)-0.6
Placebo (Male)0.4

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Change in Peak Oxygen Uptake (Peak VO2) Between the First and Second iCPET

Define the response of oxygen uptake to pyridostigmine expressed both as mL/min and mL/min/kg. The difference in peak oxygen uptake from first iCPET to second iCPET. Research has shown that ME/CFS patients have inability to reproduce results on two consecutive cardiopulmonary exercise tests(CPET). Traditionally this is demonstrated with a two-day CPET protocol, but in this study we investigate the acute effects of pyridostigmine administration on the early stages of post exertional malaise(PEM). (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

InterventionmL/min (Mean)
Study Drug - Pyridostigmine13.3
Placebo (Female)-40.3
Placebo (Male)111.8

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Peak (Ca-vO2)/[Hgb]

Difference in peak arterial-venous oxygen content difference normalized to hemoglobin (Ca-vO2)/[Hgb] between first and second iCPETs (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

InterventionRatio (Mean)
Study Drug - Pyridostigmine0.0
Placebo (Female)0.0
Placebo (Male)0.0

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Peak Cardiac Output (Qc)

Arterial and mixed-venous blood gases and pH are measured at peak exercise and Qc is calculated using the direct Fick principle Qc=VO2/(Ca-Cv). Change in peak Qc between first and second iCPETs is measured in L/min. (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

InterventionL/min (Mean)
Study Drug - Pyridostigmine0.2
Placebo (Female)-0.2
Placebo (Male)1.1

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Peak Pulmonary Arterial Wedge Pressure (PAWP)

Difference in peak PAWP between first and second iCPETs measured in mmHg (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

Interventionmm Hg (Mean)
Study Drug - Pyridostigmine1.0
Placebo (Female)1.0
Placebo (Male)1.5

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Peak Stroke Volume (SV)

Difference in peak SV between first and second iCPETs measured in mL (NCT03674541)
Timeframe: First iCPEt up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

InterventionmL (Mean)
Study Drug - Pyridostigmine3.0
Placebo (Female)-1.1
Placebo (Male)-12.7

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Peak Right Atrial Pressure (RAP)

Difference in peak RAP between first and second iCPETs measured in mmHg. (NCT03674541)
Timeframe: First iCPEt up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

Interventionmm Hg (Mean)
Study Drug - Pyridostigmine1.2
Placebo (Female)0.1
Placebo (Male)1.7

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Ventilatory Efficiency (VE/VCO2)

Difference in ventilatory efficiency between first and second iCPETs (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

InterventionRatio (Mean)
Study Drug - Pyridostigmine-0.2
Placebo (Female)1.0
Placebo (Male)1.7

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Peak-Rest Right Atrial Pressure (RAP)

Peak versus rest changes in RAP between first and second iCPETs measured in mmHg (NCT03674541)
Timeframe: First iCPEt up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

Interventionmm Hg (Mean)
Study Drug - Pyridostigmine1.0
Placebo (Female)-0.6
Placebo (Male)0.0

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Peak-Rest Oxygen Uptake (VO2)

Peak versus rest changes in oxygen uptake between first and second CPETs expressed as mL/min. (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

InterventionmL/min (Mean)
Study Drug - Pyridostigmine25.9
Placebo (Female)-60.8
Placebo (Male)121.8

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Borg Dyspnea Scale

Difference in perceived dyspnea at peak exercise between first and second iCPETs. Used Borg Scale 0 (minimal) to 10 (maximal). (NCT03674541)
Timeframe: First iCPET up to 30 minutes, 50 minutes rest, second iCPET up to 30 minutes.

Interventionunits on a scale (Mean)
Study Drug - Pyridostigmine-0.1
Placebo (Female)-1.0
Placebo (Male)0.3

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Peak-Rest Cardiac Output (Qc)

Peak versus rest change in cardiac output expressed in L/min between first and second iCPETs. Cardiac output is determined using the direct Fick principle. (NCT03674541)
Timeframe: First iCPET up to 30 min, 50 minutes rest, second iCPET up to 30 minutes

InterventionL/min (Mean)
Study Drug - Pyridostigmine-0.2
Placebo (Female)-1.9
Placebo (Male)0.9

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