In this work, a series of water-soluble propofol prodrugs were synthesized, and their propofol release rate and pharmacodynamic characteristics were measured. We found that inserting glycolic acid as a linker between propofol and the cyclic amino acid accelerated the release of propofol from prodrugs into the plasma while preserving its safety. In animal experiments, prodrugs (, , and ) were significantly better than fospropofol (the only water-soluble propofol prodrug that has been used clinically) in terms of safety, onset, and duration time of anesthesia. Their molar dose, onset time, and anesthesia duration time were comparable to those of propofol, helping to maintain the clinical benefits of propofol. The experimental results showed the potential of such compounds as water-soluble prodrugs of propofol.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.jmedchem.0c00698 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Efficacy and safety of fospropofol disodium sedation for same-day bidirectional endoscopy in elderly patients: protocol for a prospective, single-center, randomized, double-blind, non-inferiority trial.
Front Pharmacol
August 2024
Department of Anesthesiology, Shanghai Sixth People's Hospital Affiliated to Shanghai Jiaotong University School of Medicine, Shanghai, China.
Article Synopsis
- Fospropofol disodium is a new sedation drug that may offer better effects than traditional propofol, specifically for elderly patients undergoing same-day bidirectional endoscopy.
- The study involves 256 elderly participants, split evenly between fospropofol and propofol groups, to compare sedation success rates, how quickly sedation is achieved, and patient recovery times.
- Researchers aim to determine if fospropofol is as effective and safe as propofol, with hopes of establishing it as a preferred option for sedation in these medical procedures.
Fospropofol disodium versus propofol for long-term sedation during invasive mechanical ventilation: A pilot randomized clinical trial.
J Clin Anesth
August 2024
Department of Critical Care Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, China. Electronic address:
Study Objective: Fospropofol disodium is a propofol prodrug that is water-soluble and has a reduced risk of bacterial contamination and hypertriglyceridemia compared with propofol. Prior to implementing a large randomized trial, we investigated the feasibility, initial efficacy, and safety of fospropofol disodium compared with propofol in long-term mild-to-moderate sedation in intensive care units (ICUs).
Design: Single-centered, prospective, unblind, randomized, parallel-group clinical trial.
Chloromethyl Glycosides as Versatile Synthons to Prepare Glycosyloxymethyl-Prodrugs.
Chemistry
February 2022
Synthetic Organic Chemistry Institute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525, AJ Nijmegen, The Netherlands.
This work investigates the addition of monosaccharides to marketed drugs to improve their pharmacokinetic properties for oral absorption. To this end, a set of chloromethyl glycoside synthons were developed to prepare a variety of glycosyloxymethyl-prodrugs derived from 5-fluorouracil, thioguanine, propofol and losartan. Drug release was studied in vitro using β-glucosidase confirming rapid conversion of the monosaccharide prodrugs to release the parent drug, formaldehyde and the monosaccharide.
View Article and Find Full Text PDFEfficacy and Safety of Fospropofol Disodium for Injection in General Anesthesia Induction for Adult Patients: A Phase 3 Trial.
Front Pharmacol
September 2021
Laboratory of Anesthesia and Critical Care Medicine, Translational Neuroscience Center, West China Hospital of Sichuan University, Chengdu, China.
Fospropofol disodium for injection (Fospropofol) is a prodrug that is metabolized into propofol to produce a general anesthesia effect when administered intravenously. This study aimed to assess the efficacy and safety of Fospropofol in comparison with propofol medium/long-chain fat emulsion injections (propofol-MCT/LCT) for general anesthesia induction in adult patients undergoing elective surgeries. Nine academic medical centers in China.
View Article and Find Full Text PDFOliceridine and its potential to revolutionize GI endoscopy sedation.
Saudi J Anaesth
May 2020
Department of Anesthesiology, Washington University in Saint Louis, 660 South Euclid Avenue, St Louis, MO, USA.
Providing sedation to patients undergoing gastrointestinal (GI) endoscopy is a controversial and emotive issue. The mainstay of sedation is propofol, whose administration is within the sole jurisdiction of anesthesia providers, at least in the USA. Attempts have been made to seize the authority by the GI community.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!