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Cholinergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Rupali Patil, Aman Upaganlawar
The clinical uses of anti-ChEs are as follows: Neostigmine: At the end of an operation, it reverses the action of nondepolarizing neuromuscular blockers.Pyridostigmine or neostigmine: Treatment of myasthenia gravis.Edrophonium: A short-acting drug, given intravenously in the management of myasthenia gravis and to differentiate between muscle paralysis due to myasthenia gravis or cholinergic crisis at the motor end plate.Donepezil: In Alzheimer’s disease.Ecothiopate: In glaucoma, as an eye drops (Katzung et al., 2009).
Ogilvie Syndrome or Acute Colonic Pseudo-Obstruction
Published in Stephen M. Cohn, Peter Rhee, 50 Landmark Papers, 2019
Matthew J. Forestiere, Kenji Inaba
Treatment begins by allowing nothing by mouth, nasogastric decompression, correction of electrolyte abnormalities, and removal of offending agents. While there is no standard for the duration of a trial of non-interventional management, the risk of perforation increases after failure of conservative treatment for greater than 3 days or when the colon diameter exceeds 12 cm (Vanek and Al-Salti, 1986; Tsirline et al., 2012). For patients who persist with colonic obstruction, the next step in their treatment remains neostigmine. This is a cholinesterase inhibitor that allows more acetylcholine to be present at the synapses for parasympathetic stimulation and increased contractility. When compared to placebo, neostigmine was effective in decompressing the colon in greater than 80% of patients in two randomized trials (Ponec et al., 1999; Van der Spoel et al., 2001). The side effects of neostigmine are not inconsequential and require close monitoring for severe colicky abdominal pain and bradycardia. Polyethylene glycol has also been used and shown to prevent relapse of symptoms after successful colonic decompression with either neostigmine or colonoscopy (Sgouros et al., 2006). Other medical modalities, including tegaserod, erythromycin, metoclopramide, Narcan, and methylnaltrexone, have been reported in individual case reports but have not been confirmed with larger studies.
Therapies
Published in Marc H. De Baets, Hans J.G.H. Oosterhuis, Myasthenia Gravis, 2019
Neostigmine has been applied topically by intranasal administration in patients with generalized myasthenia gravis.96 Topical administration of AChE inhihibitors may indeed be useful in some patients with predominantly oropharyngeal symptoms.97 However, in critical situations, AChE inhibitors should be applied by the i.v. route, because the absorption and distribution of topically applied AChE inhibitors is not reliable enough for crisis management.
Effectiveness of Sugammadex on muscle relaxant reversal in preterm neonates
Published in Egyptian Journal of Anaesthesia, 2023
Ahmed Mohamed Ahmed Elshafie, Ahmed Ezzat Marzouq Sad Elrouby, Yasser Mohamed Osman
A selective muscle relaxant binding agent is called sugammadex. Sugammadex is a hydrophilic exterior that promotes solubility and a hydrophobic interior that encapsulates amino steroidal medicines. It is a donut-shaped cyclodextrin molecule. [3,4] Sugammadex binds to rocuronium with the highest affinity, but it also has a three-fold lower affinity for vecuronium. [5] Pancuronium is not much affected, while the benzylisoquinoliums and succinylcholine classes of muscle relaxants are unaffected. Acetylcholinesterase inhibitors like neostigmine, which compete to stop the breakdown of acetylcholine rather than directly opposing neuromuscular blockers, have long been the go-to antagonists. [6] Because Sugammadex interacts directly with steroidal relaxants, it is the only medicine now on the market that can reverse profound neuromuscular blockade. [6]
Protective effect of valerian extract capsule (VEC) on ethanol- and indomethacin-induced gastric mucosa injury and ameliorative effect of VEC on gastrointestinal motility disorder
Published in Pharmaceutical Biology, 2022
Yuan Feng, Wan Dai, Junyu Ke, Yong Cui, Shuang Li, Jingjing Ma, Wenfeng Guo, Gang Chen, Ning Li, Yanwu Li
After 3 days of adaptive feeding, mice were divided into six groups (n = 20) randomly. The control group (distilled water), model group (distilled water), and VEC-treated groups (248, 496, and 992 mg/kg) were orally administered at a volume of 20 mL/kg once a day for 3 days. The positive control group was given atropine (50 mg/mL) by subcutaneous injection in a volume of 15 mL/kg. Mice fasted for 12 h before the last treatment. The five groups (except the control group) were given neostigmine (0.12 mg/kg) by subcutaneous injection in a volume of 10 mL/kg 30 min after the last medication. After 15 min, carbonic ink (10 mL/kg) was intragastrically administered. After 20 min, the mice were sacrificed. The small intestinal propulsion rate was calculated according to the method described in the previous section.
Sugammadex versus neostigmine for routine reversal of neuromuscular blockade and the effect on perioperative efficiency
Published in Baylor University Medical Center Proceedings, 2022
Andrew P. Moss, Mark F. Powell, Charity J. Morgan, Michelle D. Tubinis
The ability of sugammadex to produce faster recovery from neuromuscular blockade when compared to acetylcholine inhibition has been well established.5,6 To examine the economic impact of sugammadex, studies have often used the time from medication administration to time to train-of-four return = 0.97–9 or time from medication administration to OR exit.10 However, based on pharmacokinetics, neostigmine can and should be administered earlier to better align drug pharmacokinetics and planned extubation time. Thus, a longer reversal time does not necessarily translate into longer time in the OR. Instead, the primary outcome in this analysis was total OR time, which we believe to be a better marker for efficiency and potential cost-effectiveness.