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Anaesthesia and pain relief
Published in Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie, Bailey & Love's Short Practice of Surgery, 2018
Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie
Induction of general anaesthesia is most frequently done by intravenous agents. Propofol has replaced thiopentone as the most widely used induction agent and can be used for maintenance of anaesthesia. Other infrequently used intravenous agents include etomidate and ketamine. Newer agents based on benzodiazepine receptor agonists, etomidate derivatives and fospropofol are still in the experimental stage.
Anesthetic agents: Intravenous
Published in Hemanshu Prabhakar, Charu Mahajan, Indu Kapoor, Manual of Neuroanesthesia, 2017
Propofol (2,6-diisopropylphenol) is also known as “milk of amnesia,” because of its milklike appearance.5 The presently available preparation of propofol is 1% (10 mg/mL), which contains 2.25% glycerol as a tonicity/stabilizing agent, 10% soybean oil, and 1.2% purified egg phospholipid as an emulsifier, with sodium hydroxide to adjust the pH. A local anesthetic such as lignocaine as well as an opioid such as fentanyl can be combined with propofol to decrease the pain.6 A recently developed form of propofol, fospropofol, does not cause pain on intravenous administration like the traditional one.
The prodrug approach in the era of drug design
Published in Expert Opinion on Drug Delivery, 2019
The strategies and aims of prodrugs to be approved in the past decade are reported in Table 1. Phosphorylation to improve aqueous solubility was successfully used in the design of fospropofol, fosaprepitant, and fosnetupitant allowing for injections. On the other hand, gabapentin enacarbil was designed to increase the bioavailability of gabapentin by targeting intestinal transporters monocarboxylate transporter type 1 and sodium-dependent multivitamin transporter.
GABA(A) receptor-targeted drug development -New perspectives in perioperative anesthesia
Published in Expert Opinion on Drug Discovery, 2019
Bernd Antkowiak, Gerhard Rammes
Another way of overcoming the propofol formulation problem is the development of prodrugs that are water soluble. The best know example is fospropofol (GPI5715), which has been approved by the US Food and Drug Administration in 2008 [39]. To be activated, fospropofol must be cleaved by blood phosphatases into inorganic phosphate and propofol. HX0507 and HX0969w are propofol prodrugs that are under evaluation for human use.