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Medicina (Kaunas, Lithuania) Apr 2022: As the use of sugammadex for reversing neuromuscular blockade during general anesthesia increases, additional effects of sugammadex have been reported compared to...
: As the use of sugammadex for reversing neuromuscular blockade during general anesthesia increases, additional effects of sugammadex have been reported compared to cholinesterase inhibitors. Here, we compare the incidence of postoperative catheter-related bladder discomfort (CRBD) between sugammadex and pyridostigmine/glycopyrrolate treatments for reversing neuromuscular blockade. : We retrospectively analyzed patients aged ≥ 18 years who underwent surgery under general anesthesia, received sugammadex or pyridostigmine with glycopyrrolate to reverse neuromuscular blockade, and had a urinary catheter in the post-anesthesia care unit between March 2019 and February 2021. After applying the exclusion criteria, 1179 patients were included in the final analysis. The incidence and severity of CRBD were collected from post-anesthesia recovery records. : The incidence was 13.7% in the sugammadex group ( = 211) and 24.7% in the pyridostigmine group ( = 968). Following propensity score matching, 211 patients each were included in the pyridostigmine and sugammadex matched group (absolute standardized difference (ASD), 0.01-0.05). Compared to the pyridostigmine group, the odds ratio for CRBD occurring in the sugammadex group was 0.568 (95% confidential interval, 0.316-1.021, = 0.059). : Sugammadex has a similar effect on the occurrence of postoperative CRBD compared with pyridostigmine.
Topics: Glycopyrrolate; Humans; Pyridostigmine Bromide; Retrospective Studies; Sugammadex; Urinary Bladder; Urinary Catheters
PubMed: 35630007
DOI: 10.3390/medicina58050590 -
Chemical & Pharmaceutical Bulletin 2012Pyridostigmine bromide (PTB) is a highly soluble and extremely bitter drug. Here, an economic complexation technology combined with direct tablet compression method has... (Clinical Trial)
Clinical Trial
Pyridostigmine bromide (PTB) is a highly soluble and extremely bitter drug. 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. Physicochemical properties of the inclusion complex of PTB with beta-cyclodextrin were investigated by Fourier transformed infrared spectroscopy, differential scanning calorimetry and UV spectroscopy. An orthogonal design was chosen to properly formulate TPDPTs. All volunteers regarded acceptable bitterness of TPDPTs. The properties including disintegration time, weight variation, friability, hardness, dispersible uniformity and drug content of TPDPTs were evaluated. The dissolution profile of TPDPTs in distilled water exhibited a fast rate. Pharmacokinetic results demonstrated that TPDPTs and the commercial tablets were bioequivalent.
Topics: Drug Design; Female; Humans; Male; Molecular Structure; Pyridostigmine Bromide; Reference Values; Solubility; Tablets; Taste; Taste Perception; beta-Cyclodextrins
PubMed: 23207632
DOI: 10.1248/cpb.c12-00629 -
Proceedings of the Royal Society of... Dec 1976
Topics: Child; Child, Preschool; Eye Diseases; Humans; Infant; Male; Myasthenia Gravis; Neostigmine; Pyridostigmine Bromide
PubMed: 1013123
DOI: No ID Found -
Military Medicine Aug 2020
Observational Study
Topics: Asthma; Forced Expiratory Volume; Humans; Pyridostigmine Bromide; Spirometry; Vital Capacity
PubMed: 32207521
DOI: 10.1093/milmed/usaa055 -
The Journal of Pharmacy and Pharmacology Sep 2009We have characterised the population pharmacokinetics-pharmacodynamics of pyridostigmine given as pyridostigmine bromide. (Clinical Trial)
Clinical Trial
OBJECTIVES
We have characterised the population pharmacokinetics-pharmacodynamics of pyridostigmine given as pyridostigmine bromide.
METHODS
Over three days 50 healthy Chinese male subjects each received seven doses of 30 mg pyridostigmine bromide orally (3 x 10 mg every 8 h). Plasma concentrations of pyridostigmine and red blood cell acetylcholinesterase (AChE) activity were determined at various times within the eight hours after the first and the seventh doses. The resulting pharmacokinetic data were fitted to a single compartment open model with first-order absorption and elimination. The pharmacodynamics were modelled using an inhibitory E(max) model. The potential influence of demographic and biological covariates on the model parameters was investigated. Nonlinear mixed effects modelling was performed using NONMEM.
KEY FINDINGS
The apparent clearance and volume of distribution as well as absorption rate constant of plasma pyridostigmine were estimated to be 136 l/h, 130 l and 0.68 1/h, respectively. The maximum red blood cell AChE activity decrease (E(max)) and plasma pyridostigmine concentration producing 50% of this reduction (EC50) were estimated to be 9.32 AChE units per gram haemoglobin and 51.9 ng/ml, respectively. None of the tested covariates were found to be correlated with any of the model parameters. 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.
CONCLUSIONS
The pharmacokinetics and the effects of pyridostigmine on red blood cell AChE activity were described using a mixed effects model. For Chinese males, the dosing interval may have been shorter than that recommended for the Caucasian population. Additional studies are needed to confirm these findings.
Topics: Acetylcholinesterase; Adult; Asian People; Cholinesterase Inhibitors; Drug Dosage Calculations; Humans; Linear Models; Male; Nonlinear Dynamics; Pyridostigmine Bromide
PubMed: 19703368
DOI: 10.1211/jpp/61.09.0008 -
Neurology Feb 1981Plasma concentrations of pyridostigmine were measured after oral administration in 16 patients with myasthenia gravis. The levels varied greatly among both well- and...
Plasma concentrations of pyridostigmine were measured after oral administration in 16 patients with myasthenia gravis. The levels varied greatly among both well- and poorly controlled patients, but were usually higher in the latter group. Absorption of the drug appears to be erratic; its clearance from the plasma is slow and its metabolism could involve an enterohepatic circulation. Drugs such as methylcellulose may prevent absorption. 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. No such changes were demonstrated in a volunteer group taking a lower dose of steroids.
Topics: Biological Availability; Humans; Myasthenia Gravis; Prednisolone; Pyridostigmine Bromide
PubMed: 7193298
DOI: 10.1212/wnl.31.2.145 -
Archives of Dermatology Oct 1980
Topics: Aged; Alopecia; Female; Humans; Myasthenia Gravis; Pyridostigmine Bromide
PubMed: 7425657
DOI: No ID Found -
Anesthesia and Analgesia Oct 1995The duration of the antagonism to neuromuscular blockade produced by pyridostigmine is prolonged in elderly patients, and a pharmacokinetic explanation was sought. Ten...
The duration of the antagonism to neuromuscular blockade produced by pyridostigmine is prolonged in elderly patients, and a pharmacokinetic explanation was sought. Ten elderly (71-85 yr) and 10 younger (21-51 yr) patients were anesthetized with thiopental, nitrous oxide, and isoflurane and paralyzed with a combination of d-tubocurarine and pancuronium. When twitch height returned to 5% of baseline, pyridostigmine 0.25 mg/kg was administered and blood samples were collected intermittently for 6 h. Pyridostigmine plasma concentrations were determined by radioimmunoassay and after an hour were always greater in the elderly than in the younger patients. In both groups, plasma pyridostigmine decrement curves were best described by triexponential equations. Pharmacokinetic analysis revealed that plasma clearance in the elderly group was significantly decreased compared to that in the younger group (6.7 +/- 2.2 vs 9.5 +/- 2.7 mL.kg-1.min-1, P < 0.05). Elimination half-lives and volumes of distribution were not significantly different between groups. We conclude that a possible explanation for the prolonged duration of action of pyridostigmine in the elderly is its slow plasma clearance.
Topics: Adult; Aged; Aged, 80 and over; Aging; Cholinesterase Inhibitors; Female; Half-Life; Humans; Male; Middle Aged; Pyridostigmine Bromide; Radioimmunoassay
PubMed: 7574009
DOI: 10.1097/00000539-199510000-00020 -
Journal of Pharmaceutical and... Sep 2001A simple and reliable method was developed for the quantification of depleted uranium, the anti nerve agent drug pyridostigmine bromide...
A simple and reliable method was developed for the quantification of depleted uranium, the anti nerve agent drug pyridostigmine bromide (PB;3-dimethylaminocarbonyloxy-N-methyl pyridinium bromide) and its metabolite N-methyl-3-hydroxypyridinium bromide in rat plasma and urine. The method involved using solid phase extraction and spectrophotometric determination of uranium, and high performance liquid chromatography (HPLC) with reversed phase C(18) column, and UV detection at 280 nm for PB and its metabolite. Uranium was derivatized using dibenzoylmethane (DBM) then the absorbance was measured at 405 nm. PB and its metabolite were separated using a gradient of 1--40% acetonitrile in 0.1% triflouroacetic acid water solution (pH 3.2) at a flow rate of 0.8 ml/min in a period of 14 min. Limits of detection were 2 ng/ml for uranium and 50 ng/ml for PB and its metabolite. Limits of quantitation were between 10 and 100 ng/ml for uranium and the other two analytes, respectively. Average percentage recovery of five spiked plasma samples were 83.7+/-8.6, 76.8+/-6.7, 79.1+/-7.1, and from urine 82.7+/-8.6, 79.3+/-9.5 and 78.0+/-6.2, for depleted uranium, PB and N-methyl-3-hydroxypyridinium bromide, respectively. The relationship between peak areas and concentration was linear for standards between 100 and 1000 ng/ml for all three analytes. This method was applied to analyze the above chemicals and metabolites following combined administration in rats.
Topics: Administration, Oral; Animals; Cholinesterase Inhibitors; Chromatography, High Pressure Liquid; Injections, Intradermal; Muscle Weakness; Organometallic Compounds; Pyridostigmine Bromide; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Spectrophotometry; Tremor; Uranium
PubMed: 11470205
DOI: 10.1016/s0731-7085(01)00403-4 -
Scientific Reports Aug 2021We investigated hemodynamic, cardiac morphofunctional, and cardiovascular autonomic adaptations in spontaneously hypertensive rats (SHRs) after aerobic physical training...
Effects of chronic cholinergic stimulation associated with aerobic physical training on cardiac morphofunctional and autonomic parameters in spontaneously hypertensive rats.
We investigated hemodynamic, cardiac morphofunctional, and cardiovascular autonomic adaptations in spontaneously hypertensive rats (SHRs) after aerobic physical training associated with chronic cholinergic stimulation. Fifty-four SHRs were divided into two groups: trained and untrained. Each group was further subdivided into three smaller groups: vehicle, treated with pyridostigmine bromide at 5 mg/kg/day, and treated with pyridostigmine bromide at 15 mg/kg/day. The following protocols were assessed: echocardiography, autonomic double pharmacological blockade, heart rate variability (HRV), blood pressure variability (BPV), and baroreflex sensitivity (BRS). Physical training and pyridostigmine bromide reduced BP and HR and increased vagal participation in cardiac autonomic tonic balance. The associated responses were then potentialized. 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). However, the association with physical training attenuated HF oscillations. Additionally, treatment with pyridostigmine bromide also increased LF oscillations of BPV. Both treatment groups promoted morphofunctional adaptations, and associated increased ejection volume, ejection fraction, cardiac output, and cardiac index. In conclusion, the association of pyridostigmine bromide and physical training promoted greater benefits in hemodynamic parameters and increased vagal influence on cardiac autonomic tonic balance. Nonetheless, treatment with pyridostigmine bromide alone seems to negatively affect BPV and the association of treatment negatively influences HRV.
Topics: Animals; Blood Pressure; Cardiac Output; Cholinesterase Inhibitors; Heart; Hypertension; Physical Conditioning, Animal; Pyridostigmine Bromide; Rats; Rats, Inbred SHR; Vagus Nerve
PubMed: 34433865
DOI: 10.1038/s41598-021-96505-2