Sugammadex for Reversal of Neuromuscular Blockade: Uses and Limitations

2019 ◽  
Vol 25 (19) ◽  
pp. 2140-2148 ◽  
Author(s):  
Jesse Hawkins ◽  
Sandeep Khanna ◽  
Maged Argalious
Keyword(s):  
Side Effects ◽  
Neuromuscular Blockade ◽  
Mechanism Of Action ◽  
Acetylcholine Receptors ◽  
Review Article ◽  
Muscle Relaxants ◽  
Water Soluble ◽  
Reversal Agent ◽  
Glucose Molecule ◽  
Gamma Cyclodextrin

Sugammadex is a reversal agent that was engineered to reverse the effects of aminosteroid muscle relaxants. It is a modified gamma-cyclodextrin, i.e. a large glucose molecule bound in a ring-like structure. Sugammadex, when injected intravenously, creates a concentration gradient favoring the movement of aminosteroid muscle relaxants from the neuromuscular junction back into the plasma, and then encapsulates the aminosteroid muscle relaxants within its inner structure by forming tight water-soluble complexes. The dissociation of the aminosteroidal muscle relaxant from the post-synaptic acetylcholine receptors is responsible for the termination of neuromuscular blockade. This review article presents the current indication, mechanism of action, limitations, side effects and contraindications of sugammadex. An overview of monitoring of the adequacy of reversal of aminosteroid muscle relaxants with sugammadex is presented. Moreover, the use of sugammadex in special situations, including “cannot intubate cannot oxygenate” scenarios is also described.

scholarly journals COVID-19 Vaccines, What do we know so Far? A Narrative Review

2021 ◽  
Vol 04 (05) ◽  
Author(s):  
Cima Hamieh, MD ◽  
Keyword(s):  
Side Effects ◽  
Mortality Rate ◽  
Mechanism Of Action ◽  
Review Article ◽  
Conspiracy Theories ◽  
Safety And Efficacy ◽  
Large Numbers ◽  
The World ◽  
And Control ◽  
New Vaccines

For more than a year, the world was paralyzed by the COVID-19 pandemic. It wasn’t until the last few months that hope to a return of a quasi-normal way of living was starting to materialize. The era of the COVID-19 vaccines begun, and with it all sorts of concerns and complaints about their safety and efficacy. Large numbers of people believed the conspiracy theories about the new vaccines thus becoming reluctant and sometimes refused to take the new vaccines. Others justified their concern with the relatively short trial periods compared to previous vaccines that used to take years before adoption. Multiple vaccines emerged around the same time, and thus the fight to conquer the market began. Pfizer-BioNTech, Vaxzervria, Moderna, Sputnik, Coronavac, Janssen, all were rapidly distributed to countries around the globe, in order to reduce the mortality rate and control the pandemic. To make things worse, new viral mutations started being detected and thus shed more doubt on the efficacy of these vaccines. This review article summarizes the literature of these vaccines’ pathophysiology, mechanism of action, dosing and schedule, safety profile and lastly the documented side effects of each vaccine. In conclusion, there is no certainty whether these vaccines will prevent infection and more importantly protect against forward transmission. It is sure that the immunity persists for several months, but the exact duration for every vaccine is yet to be determined. For the time being, safety precautions must still be continued; wearing masks, social distancing and avoiding crowded places must be applied.

Initial Studies of a Potent Antiheparin Agent (Ubiquin®)

1968 ◽  
Vol 20 (03/04) ◽  
pp. 588-595 ◽  
Author(s):  
E. B Goodsell ◽  
R. A Krause ◽  
E. T Kimura
Keyword(s):  
Side Effects ◽  
Acute Toxicity ◽  
Propylene Oxide ◽  
Toluidine Blue ◽  
Water Soluble ◽  
Per Se

SummaryUbiquin (oligo-3-(N-methylmorpholinium)-l,2-propylene oxide chloride) is a stable, water soluble, active heparin antagonist producing prompt neutralization when administered in a 1:1 ratio to rats and dogs. Initial studies indicate that it is devoid of any effect on coagulation per se; nor are there any obvious side effects manifested during the process of neutralization. The acute toxicity is less than that of other compounds in use: toluidine blue, protamine and hexadimethrine.

CLINICAL INVESTIGATIONS OF A LONG-ACTING OESTRIOL (POLYOESTRIOL PHOSPHATE)

1961 ◽  
Vol 38 (1) ◽  
pp. 73-87 ◽  
Author(s):  
Christian Lauritzen ◽  
Semih Velibese
Keyword(s):  
Side Effects ◽  
Phosphoric Acid ◽  
Quantitative Data ◽  
Water Soluble ◽  
Cholesterol Concentration ◽  
Experimental Investigations ◽  
Clinical Investigations ◽  
Prolonged Duration ◽  
High Doses ◽  
Long Acting

ABSTRACT A description is given of experimental investigations and preliminary clinical experience with the long-acting oestriol compound polyoestriol phosphate – a water-soluble polymere of oestriol and phosphoric acid. The compound seems to exert all the physiologically important effects of oestriol. Even with high doses the hormone causes no proliferation of the endometrium and no withdrawal bleeding. It has no untoward effect on metabolism. It decreases slightly the cholesterol concentration (to the extent of ⅓–⅕ of the effect produced by long-acting oestradiol esters). The compound has a wide therapeutic range. No side-effects have been observed. Doses of 10 mg or more have a prolonged duration. Additional prolongation of the effect is largely dependent on dosage. To ensure an effect lasting for 4 weeks 40 mg polyoestriol phosphate (corresponding with 30 mg oestriol) is required – an amount which roughly corresponds with physiological quantitative data. The compound, which involves an interesting new principle of prolongation, was most effectively used in the treatment of menopausal symptoms and genital organic disorders. For these indications it can be recommended without reservation.

Nitrogen Mustards as Alkylating Agents: A Review on Chemistry, Mechanism of Action and Current USFDA Status of Drugs

2019 ◽  
Vol 19 (9) ◽  
pp. 1080-1102 ◽  
Author(s):  
Ghansham S. More ◽  
Asha B. Thomas ◽  
Sohan S. Chitlange ◽  
Rabindra K. Nanda ◽  
Rahul L. Gajbhiye
Keyword(s):  
Side Effects ◽  
Mechanism Of Action ◽  
Anticancer Agents ◽  
Nitrogen Mustard ◽  
Alkylating Agents ◽  
Cross Linking ◽  
Nitrogen Mustards ◽  
Information Leaflets ◽  
Anti Cancer ◽  
Approved Drugs

Background & Objective: :Nitrogen mustard derivatives form one of the major classes of anti-cancer agents in USFDA approved drugs list. These are polyfunctional alkylating agents which are distinguished by a unique mechanism of adduct formation with DNA involving cross-linking between guanine N-7 of one strand of DNA with the other. The generated cross-linking is irreversible and leads to cell apoptosis. Hence it is of great interest to explore this class of anticancer alkylating agents.Methods::An exhaustive list of reviews, research articles, patents, books, patient information leaflets, and orange book is presented and the contents related to nitrogen mustard anti-cancer agents have been reviewed. Attempts are made to present synthesis schemes in a simplified manner. The mechanism of action of the drugs and their side effects are also systematically elaborated.Results::This review provides a platform for understanding all aspects of such drugs right from synthesis to their mechanism of action and side effects, and lists USFDA approved ANDA players among alkylating anticancer agents in the current market.Conclusion: :Perusing this article, generic scientists will be able to access literature information in this domain easily to gain insight into the nitrogen mustard alkylating agents for further ANDA development. It will help the scientific and research community to continue their pursuit for the design of newer and novel heterocyclic alkylating agents of this class in the coming future.

scholarly journals NMR Structure and Action on Nicotinic Acetylcholine Receptors of Water-soluble Domain of Human LYNX1

2011 ◽  
Vol 286 (12) ◽  
pp. 10618-10627 ◽  
Author(s):  
Ekaterina N. Lyukmanova ◽  
Zakhar O. Shenkarev ◽  
Mikhail A. Shulepko ◽  
Konstantin S. Mineev ◽  
Dieter D'Hoedt ◽  
...  
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Nmr Structure ◽  
Water Soluble ◽  
Gpi Anchor ◽  
Nicotinic Acetylcholine ◽  
Brain Functions ◽  
The Central Nervous System ◽  
High Concentrations

Discovery of proteins expressed in the central nervous system sharing the three-finger structure with snake α-neurotoxins provoked much interest to their role in brain functions. Prototoxin LYNX1, having homology both to Ly6 proteins and three-finger neurotoxins, is the first identified member of this family membrane-tethered by a GPI anchor, which considerably complicates in vitro studies. We report for the first time the NMR spatial structure for the water-soluble domain of human LYNX1 lacking a GPI anchor (ws-LYNX1) and its concentration-dependent activity on nicotinic acetylcholine receptors (nAChRs). At 5–30 μm, ws-LYNX1 competed with 125I-α-bungarotoxin for binding to the acetylcholine-binding proteins (AChBPs) and to Torpedo nAChR. Exposure of Xenopus oocytes expressing α7 nAChRs to 1 μm ws-LYNX1 enhanced the response to acetylcholine, but no effect was detected on α4β2 and α3β2 nAChRs. Increasing ws-LYNX1 concentration to 10 μm caused a modest inhibition of these three nAChR subtypes. A common feature for ws-LYNX1 and LYNX1 is a decrease of nAChR sensitivity to high concentrations of acetylcholine. NMR and functional analysis both demonstrate that ws-LYNX1 is an appropriate model to shed light on the mechanism of LYNX1 action. Computer modeling, based on ws-LYNX1 NMR structure and AChBP x-ray structure, revealed a possible mode of ws-LYNX1 binding.

Medicinal Plants and Natural Products, More Effective and Safer Pharmacological Treatment for the Management of Obesity

2021 ◽  
Vol 22 ◽  
Author(s):  
Harsha Negi ◽  
Meenakshi Gupta ◽  
Ramanpreet Walia ◽  
Moayad Khataibeh ◽  
Maryam Sarwat
Keyword(s):  
Natural Products ◽  
Weight Gain ◽  
Side Effects ◽  
Medicinal Plants ◽  
Mechanism Of Action ◽  
Pancreatic Lipase ◽  
Herbal Products ◽  
Prevalence Of Obesity ◽  
Herbal Plants ◽  
New Compounds

: Obesity is a major lifestyle disorder and it is correlated with several ailments. The prevalence of obesity has elevated over the years and it has become a global health problem. The drugs presently used for managing obesity have several side-effects associated with them such as diarrhoea, leakage of oily stools, etc. On the contrary, herbal plants and natural products are considered safe for use because they have lesser side effects. New compounds isolated from medicinal plants are screened and identified to determine their effectiveness and potential in preventing abnormal weight gain. In this review, the medicinal plants and natural materials were surveyed across the literature to cover those that have potential for managing and controlling weight gain, and their mechanism of action, active component, and experimental methodologies are also included. These herbal products can be developed as formulations for therapeutic use in obesity. The herbal plants mentioned in the review are classified based on their mechanism of action: inhibition of pancreatic lipase and appetite suppression activities. The ability to inhibit pancreatic lipase enzyme has been used to determine the effectiveness of herbal products for the prevention of abnormal weight gain because of its action on dietary fat and suppression of appetite. This review is an attempt to summarize the herbal plants and natural products that can be used to develop formulations effective in controlling weight gain and obesity.

scholarly journals Update on therapy for superficial mycoses: review article part I

2013 ◽  
Vol 88 (5) ◽  
pp. 764-774 ◽  
Author(s):  
Maria Fernanda Reis Gavazzoni Dias ◽  
Maria Victoria Pinto Quaresma-Santos ◽  
Fred Bernardes-Filho ◽  
Adriana Gutstein da Fonseca Amorim ◽  
Regina Casz Schechtman ◽  
...  
Keyword(s):  
Side Effects ◽  
Drug Interactions ◽  
Fungal Infections ◽  
Review Article ◽  
Practical Approach ◽  
Superficial Mycoses ◽  
World Markets ◽  
The World ◽  
The Right ◽  
Therapeutic Alternatives

Superficial fungal infections of the hair, skin and nails are a major cause of morbidity in the world. Choosing the right treatment is not always simple because of the possibility of drug interactions and side effects. The first part of the article discusses the main treatments for superficial mycoses - keratophytoses, dermatophytosis, candidiasis, with a practical approach to the most commonly-used topical and systemic drugs , referring also to their dosage and duration of use. Promising new, antifungal therapeutic alternatives are also highlighted, as well as available options on the Brazilian and world markets.

The effect of a benzodiazepine, flurazepam, on the response of in vitro skeletal muscle preparations to muscle relaxants: are purines or their receptors involved?

1982 ◽  
Vol 60 (7) ◽  
pp. 877-884 ◽  
Author(s):  
John T. Hamilton ◽  
Peggy A. Stone
Keyword(s):  
Skeletal Muscle ◽  
Phrenic Nerve ◽  
Neuromuscular Blocking ◽  
Muscle Relaxants ◽  
Water Soluble ◽  
Neuromuscular Activity ◽  
Changing Trends ◽  
Low Concentrations ◽  
Partial Blockade

Changing trends in the use of anxiolytic agents and recent reassessment of their neuropharmacological activity has prompted this evaluation of the peripheral neuromuscular activity of the benzodiazepine, flurazepam. In previous reports we have documented peripheral neuromuscular activity of chlordiazepoxide and diazepam on the rat phrenic nerve diaphragm preparation. The water soluble benzodiazepine, flurazepam, has been studied on the rat phrenic nerve diaphragm and frog rectus abdominis in vitro. On the former preparation flurazepam enhanced and then blocked the response to indirect electrical stimulation (0.2 Hz) and readily blocked posttetanic potentiation and prevented the preparation from sustaining a tetanic contracture (30 Hz). On the later preparation, flurazepam blocked in a noncompetitive manner the response of the frog muscle to applied cholinergic agonists. Studies on the rat preparation with the neuromuscular blocking drug succinylcholine have shown an unexpected protection against blockade in preparations pretreated with low concentrations of flurazepam. This was not observed when flurazepam was given prior to d-tubocurarinc. The application of adenosine to rat diaphragms during steady-state partial blockade caused by flurazepam or d-tubocurarine showed an inhibiting action of adenosine which was reversed by theophylline. Pretreatment of rat preparations with dipyridamole significantly enhanced the blocking action of standard concentrations of succinylcholine.These results, along with those in the literature, encourage a reassessment of the action of purines and benzodiazepines on skeletal muscle and encourage a consideration of a possible involvement of purinergic neuromodulation of transmission which is unmasked when the safety factor for transmission is altered by muscle relaxants. The possible clinical significance of protection against succinylcholine by benzodiazepines is noted.

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