Topic
Fospropofol
About: Fospropofol is a research topic. Over the lifetime, 109 publications have been published within this topic receiving 1965 citations. The topic is also known as: Lusedra® & Fospropofol.
Papers published on a yearly basis
Papers
TL;DR: Emergence from sedation is more rapid with propofol than with midazolam, even after long-term administration, which enables better control of the depth of sedation in response to titration and more predictable recovery times.
Abstract: Propofol (Diprivan) is a phenolic derivative with sedative and hypnotic properties but is unrelated to other sedative/hypnotic agents. Formulated as an oil-in-water emulsion for intravenous use, it is highly lipophilic and rapidly crosses the blood-brain barrier resulting in a rapid onset of action. Emergence from sedation is also rapid because of a fast redistribution into peripheral tissues and metabolic clearance. The depth of sedation increases in a dose-dependent manner. In well designed clinical trials in patients receiving sedation in the intensive care unit (ICU) for a variety of indications, propofol provided adequate sedation for a similar proportion of time to midazolam, but the rate of recovery was faster with propofol. Even after periods of prolonged sedation (>72 hours), propofol was generally associated with a faster time to recovery than midazolam. Propofol facilitated better predictability of recovery and an improved control of the depth of sedation in response to titration than midazolam. In patients sedated following head trauma, propofol reduced or maintained intracranial pressure. Propofol is associated with generally good haemodynamic stability but induces a dose-dependent decrease in blood pressure and heart rate. Bolus administration may cause transient hypotension, and slow initial infusions are recommended in most patients. Serum triglyceride concentrations should be monitored during prolonged infusions (>3 days) because of the risk of hypertriglyceridaemia. The administration of 2% propofol can reduce this risk. Strict aseptic technique must be used during the handling of the product to prevent accidental extrinsic microbial contamination. Despite a higher acquisition cost with propofol, most studies of short-term sedation (approximately Conclusion The efficacy of propofol in the sedation of adults in the ICU is well established, and clinical trials have demonstrated a similar quality of sedation to midazolam. Because of a rapid distribution and clearance, the duration of action of propofol is short and recovery is rapid. Emergence from sedation is more rapid with propofol than with midazolam, even after long-term administration (>72 hours), which enables better control of the depth of sedation in response to titration and more predictable recovery times. Thus, for the ICU sedation of adults in a variety of clinical settings, propofol provides effective sedation with a more rapid and predictable emergence time than midazolam.
213 citations
TL;DR: Moderate sedation is a drug‐induced depression of consciousness during which patients respond purposefully to verbal commands with or without light tactile stimulation.
Abstract: Summary
Background
Moderate sedation is a drug-induced depression of consciousness during which patients respond purposefully to verbal commands with or without light tactile stimulation. Moderate sedation is typically accepted in the anaesthesia community as an appropriate target for sedation by non-anaesthesiologists.
Aim
To describe drug regimens that can be successfully and safely targeted to moderate sedation for endoscopy by non-anaesthesiologists.
Results
Moderate sedation can be achieved using narcotics and benzodiazepines. There is interest in some countries in propofol for endoscopy, which is often viewed as an agent for deep sedation. Indeed, propofol cannot be targeted to moderate sedation for endoscopy as a single agent because of coughing during upper endoscopy and pain withdrawal responses during colonoscopy. Pre-treatment with low doses of narcotic and/or benzodiazepine blocks these effects, allowing propofol to be targeted to moderate sedation. Fospropofol, a prodrug of propofol in clinical development, can also be targeted to moderate sedation if co-administered with narcotic.
Conclusion
Moderate sedation provides a safety margin when compared with deep sedation and general anaesthesia. Development of protocols that target agents such as propofol to moderate sedation will expand the sedation agents available to non-anaesthesiologists and help ensure that this expansion occurs safely.
129 citations
TL;DR: AQUAVAN® injection (fospropofol disodium), a phosphorylated prodrug of propofol, is an investigational agent possessing a unique and distinct pharmacokinetic and pharmacodynamic profile, associated with a slightly longer time to peak effect and a more prolonged pharmacodynamic effect.
Abstract: The ability to deliver safe and effective moderate sedation is crucial to the ability to perform invasive procedures. Sedative drugs should have a quick onset of action, provide rapid and clear-headed recovery, and be easy to administer and monitor. A number of drugs have been demonstrated to provide effective sedation for outpatient procedures but since each agent has its own limitations, a thorough knowledge of the available drugs is required to choose the appropriate drug, dose and/or combination regimen for individual patients. Midazolam, propofol, ketamine and sevoflurane are the most frequently used agents, and all have a quick onset of action and rapid recovery. The primary drawback of midazolam is the potential for accumulation of the drug, which can result in prolonged sedation and a hangover effect. The anaesthetics propofol and sevoflurane have recently been used for sedation in procedures of short duration. Although effective, these agents require monitored anaesthesia care. Ketamine is an effective agent, particularly in children, but there is concern regarding emergence reactions. AQUAVAN® injection (fospropofol disodium), a phosphorylated prodrug of propofol, is an investigational agent possessing a unique and distinct pharmacokinetic and pharmacodynamic profile. Compared with propofol emulsion, AQUAVAN® is associated with a slightly longer time to peak effect and a more prolonged pharmacodynamic effect. Advances in the delivery of sedation, including the development of new sedative agents, have the potential to further improve the provision of moderate sedation for a variety of invasive procedures.
124 citations
TL;DR: Fospropofol provided safe and effective sedation for patients undergoing flexible bronchoscopy, and the most frequent adverse events were transient and self-limited paresthesias and pruritus of mild-to-moderate severity.
119 citations
TL;DR: Knowing the metabolism of propofol may lead to the development of new clues to help further toxicological and clinical interpretations and to reduce serious adverse reactions such as respiratory failure, metabolic acidosis, rhabdomyolysis, cardiac bradyarrhythmias, hypotension and myocardial failure.
Abstract: Propofol is an intravenous short-acting anesthetic widely used to induce and maintain general anesthesia and to provide procedural sedation. The potential for propofol dependency and abuse has been recognized, and several cases of accidental overdose and suicide have emerged, mostly among the health professionals. Different studies have demonstrated an unpredictable interindividual variability of propofol pharmacokinetics and pharmacodynamics with forensic and clinical adverse relevant outcomes (e.g., pronounced respiratory and cardiac depression), namely, due to polymorphisms in the UDP-glucuronosyltransferase and cytochrome P450 isoforms and drugs administered concurrently. In this work the pharmacokinetics of propofol and fospropofol with particular focus on metabolic pathways is fully reviewed. It is concluded that knowing the metabolism of propofol may lead to the development of new clues to help further toxicological and clinical interpretations and to reduce serious adverse reactions such as respiratory failure, metabolic acidosis, rhabdomyolysis, cardiac bradyarrhythmias, hypotension and myocardial failure, anaphylaxis, hypertriglyceridemia, renal failure, hepatomegaly, hepatic steatosis, acute pancreatitis, abuse, and death. Particularly, further studies aiming to characterize polymorphic enzymes involved in the metabolic pathway, the development of additional routine forensic toxicological analysis, and the relatively new field of ‘‘omics’’ technology, namely, metabolomics, can offer more in explaining the unpredictable interindividual variability.
76 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2021 | 1 |
| 2020 | 4 |
| 2019 | 1 |
| 2018 | 3 |
| 2017 | 7 |
| 2016 | 2 |