Recent advances in intravenous anesthesia and anesthetics

Mahmoud, Mohamed; Mason, Keira P.

doi:10.12688/f1000research.13357.1

Cited by 16 publications

(10 citation statements)

References 61 publications

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“…This leads to the inhibition of the central nervous system. This channel is also the primary target of propofol, which is a commonly used intravenous anesthetic that acts quickly and has a short duration of action [2], which though has its limitations, including injection pain, hemodynamic issues, and risk of a potentially fatal condition known as propofol infusion syndrome (PIS) [3]. To address these limitations and improve the pharmacological and physicochemical properties of drug-receptor binding, propofol was optimized into ciprofol by incorporating a cyclopropyl group [1].…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics, Pharmacodynamics, and Safety of Ciprofol Injectable in Chinese Subjects with Normal or Impaired Renal Function

Tao

Liu

Zhao

et al. 2023

Preprint

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Purpose The study was designed to evaluate the pharmacokinetics (PK), pharmacodynamics (PD) and safety of ciprofol injection in healthy subjects and patients with mild and moderate renal impairment, to provide a reference for the dosage adjustment in these populations. Methods A total of 24 subjects were enrolled in this study. An initial loading dose of ciprofol was 0.4 mg/kg for 1 min, followed by maintenance infusion at a rate of 0.4 mg/kg/h for 30 min were administered to subjects. To evaluate the PK of ciprofol and its metabolite M4, plasma and urine samples were collected. PD was evaluated using a modified observer’s alertness/sedation scale (MOAA/S) in combination with bispectral index (BIS) monitoring. Safety assessments were conducted throughout the trial process. Results The area under the curve (AUC) and maximum concentration (Cmax) of ciprofol in plasma for patients with renal impairment were only slightly higher (0.9- to 1.2-fold) than those subjects in with normal renal function. For the metabolite M4, AUC values were 1.3- and 2.1-fold greater in patients with mild and moderate renal impairment, respectively, than healthy controls. However, increased exposure to M4 in participants with renal impairment may not be clinically significant, as this metabolite is pharmacologically inactive. There was no obvious effect of renal impairment on the PD parameters. The study found that ciprofol injection was well-tolerated, with all AEs reported being mild or moderate in severity. Conclusion No dosage adjustment of ciprofol is necessary for patients with mild-to-moderate renal impairment who receive the injection. Clinical trial registration: NCT04142970(October, 2019).

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Section: Introductionmentioning

confidence: 99%

Pharmacokinetics, Pharmacodynamics, and Safety of Ciprofol Injectable in Chinese Subjects with Normal or Impaired Renal Function

Tao

Liu

Zhao

et al. 2023

Preprint

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“…The provision of general anesthesia through intravenous agents alone is known as total intravenous anesthesia [1]. Propofol and etomidate represent some of the more significant contributions to intravenous anesthetic or sedative agents [2] and are commonly used for induction of general anesthesia prior to rapid sequence intubation in critically ill, hemodynamically unstable patients [3,4]. Propofol, which is an alkylphenol compound, has been a transformative anesthetic agent since its introduction 40 years ago and is still considered to be a near-ideal anesthetic agent.…”

Section: Introductionmentioning

confidence: 99%

“…Propofol, which is an alkylphenol compound, has been a transformative anesthetic agent since its introduction 40 years ago and is still considered to be a near-ideal anesthetic agent. Its success in the clinical setting is a result of its rapid onset, short duration of action, rapid achievement of sedative depth, and complete recovery [2][3][4]. However, it is associated with some adverse reactions, the most important of which include marked respiratory depression, hypotension, hemodynamic instabili-ty, and cardiovascular complications [5][6][7].…”

Section: Introductionmentioning

confidence: 99%

Physical and Chemical Compatibility of Etomidate and Propofol Injectable Emulsions

Wang¹,

Wu²,

Li³

et al. 2021

Pharmacology

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Introduction: The mixture of etomidate and propofol is widely used in clinical practice to improve efficacy of general anesthesia and to minimize side effects. As a thermodynamically unstable system, emulsion is prone to destabilization through mechanisms including coalescence, flocculation, and creaming. Such unwanted phenomenon can induce fat embolism after intravenous administration. This study was aimed to investigate the physical and chemical stability of the mixture of etomidate and propofol in the dosage form of emulsion. Methods: This compatibility study focused on the critical quality attributes (CQAs) of drug-containing emulsions, such as appearance, pH, particle size and distribution, zeta potential, the observation under centrifugation, and drug content and impurity. Results: As the results, there were no significant changes in the CQAs of the mixed emulsions up to 24 h after mixing at refrigeration temperature (4°C), room temperature (25°C), and body temperature (37°C). Conclusions: These results demonstrate that etomidate emulsion is physically and chemically compatible with propofol emulsions up to 24 h at 4°C, 25°C, and 37°C, suggesting that etomidate and propofol can be administrated in mixture without adversely affecting product characteristics, at least in vitro.

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“…In recent years, the continuous improvement of anesthesia technology has enabled more and more surgical operations and invasive examinations to be carried out smoothly [1,2]. Anesthesia is divided into local anesthesia and general anesthesia, and the general anesthesia includes inhalation anesthesia or intravenous anesthesia [3,4].…”

Section: Introductionmentioning

confidence: 99%

Study on the ameliorating effect of miR-221-3p on the nerve cells injury induced by sevoflurane

Wang

Tian

et al. 2020

International Journal of Neuroscience

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Purpose: Sevoflurane is a widely used anesthetics, however, it has been reported that sevoflurane has neurotoxic effects. Studies have shown that miR-221-3p can ameliorate neuron damage. This study was to investigate whether miR-221-3p could reduce the neurotoxic effect of sevoflurane on nerve cells. Materials and methods: The rat hippocampal neuron cells were treated with sevoflurane or cultured normally. And we constructed neuron cells that overexpressed or low expression of miR-221-3p in the presence or absence of sevoflurane. The cells were transfected with CDKN1B or siCDKN1B, and co-transfected with miR-221-3p mimic and CDKN1B or miR-221-3p inhibitor and siCDKN1B. Cell viability and apoptosis were detected by CCK-8 and flow cytometer. Target gene of miR-221-3p were predicted by TargetScan and luciferase reporter assay. The expressions of related genes were detected by western blotting and quantitative real-time polymerase chain reaction. Results: Sevoflurane decreased miR-221-3p level and increased CDKN1B level, inhibited cell viability and promoted apoptosis. Overexpress of miR-221-3p decreased CDKN1B level, up-regulated cell viability and inhibited apoptosis, and reversed the effects of sevoflurane on cell viability and apoptosis, while the effects low expression of miR-221-3p was contrary. CDKN1B was the target gene of miR-221-3p, which inhibited cell viability and promoted apoptosis, and reversed the effects of miR-221-3p mimic, whereas siCDKN1B did the opposite effects. Conclusions: Sevoflurane can cause nerve cell injury, and miR-221-3p may promote cell activity and inhibit apoptosis by inhibiting CDKN1B expression, thereby ameliorating cell injury induced by sevoflurane.

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Recent advances in intravenous anesthesia and anesthetics

Abstract: Anesthesiology, as a field, has made promising advances in the discovery of novel, safe, effective, and efficient methods to deliver care. This review explores refinement in the technology of soft drug development, unique anesthetic delivery systems, and recent drug and device failures.

Cited by 16 publications

References 61 publications

Pharmacokinetics, Pharmacodynamics, and Safety of Ciprofol Injectable in Chinese Subjects with Normal or Impaired Renal Function

Pharmacokinetics, Pharmacodynamics, and Safety of Ciprofol Injectable in Chinese Subjects with Normal or Impaired Renal Function

Physical and Chemical Compatibility of Etomidate and Propofol Injectable Emulsions

Study on the ameliorating effect of miR-221-3p on the nerve cells injury induced by sevoflurane

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