Gina D. Moore, Alyssa M Walker, Robert MacLaren,
Objective: To summarize the published clinical data on fospropofol, critically review the safety and efficacy information, and ... and www.fda.gov . Key search terms included fospropofol, Lusedra, Aquavan, sedative–hypnotic, and monitored anesthesia care. ... clinical trials studying the safety and efficacy of fospropofol were reviewed. Data Synthesis: Fospropofol is a water-soluble prodrug of propofol, a ... from bacterial contamination. Due to its water solubility, fospropofol eliminates some of the known lipid emulsion–associated ...
Tópico(s): Intensive Care Unit Cognitive Disorders
2009 - SAGE Publishing | Annals of Pharmacotherapy
Lawrence B. Cohen, Edward L. Cattau, Allen C. Goetsch, Atul K. Shah, John R. Weber, Douglas K. Rex, Jacqueline Kline,
... study evaluated the safety and efficacy of intravenous fospropofol (6.5 mg/kg vs. 2 mg/kg) ... Anesthesiologists PS1 to PS3) were randomized to receive fospropofol 2 mg/kg, fospropofol 6.5- mg/kg, or midazolam 0.02 ... and safety.Sedation success was higher in the fospropofol 6.5 mg/kg versus 2 mg/kg ... 60% for the midazolam group). Patients in the fospropofol groups had similar memory retention (70% and 82% ... Mean physician satisfaction scores were higher in the fospropofol 6.5-mg/kg group (7.7) than ... 60%) and pruritus (16% vs. 26%) in the fospropofol 6.5 and 2 mg/kg groups, respectively. ...
Tópico(s): Intensive Care Unit Cognitive Disorders
2010 - Lippincott Williams & Wilkins | Journal of Clinical Gastroenterology
Keith Candiotti, Tong J. Gan, Christopher Young, Alex Bekker, Sam T. Sum-Ping, R. Kahn, Philip Lebowitz, Jeffrey J. Littman,
... patients in the intensive care unit have limitations. Fospropofol, a prodrug of propofol, has not been studied ... Ramsay Sedation Score of 2 to 5: (1) fospropofol IV infusion with a bolus and increased infusion rate for agitation events (infusion/bolus); (2) fospropofol IV infusion with an increased infusion rate for ... incidence rates for adverse events were similar between fospropofol groups, and because the study was not powered ... groups for safety variables, adverse events for both fospropofol groups were combined. In the fospropofol groups, 28 ...
Tópico(s): Anesthesia and Neurotoxicity Research
2011 - Lippincott Williams & Wilkins | Anesthesia & Analgesia
Yangyang Zhou, Jing Yang, Jin Liu, Y. Wang, W.S. Zhang,
... performed to compare the efficacy of HX0969w with fospropofol in mice and rats.MethodsWe performed hydrolysis studies ... ED50) and half-maximal lethal doses (LD50) of fospropofol and HX0969w were determined. A pharmacodynamics comparison of ... a longer onset time and shorter duration than fospropofol.ConclusionsSimilar to fospropofol, HX0969w is an effective, water-soluble prodrug that ... sedative–hypnotic effect in mice and rats. Unlike fospropofol, HX0969w releases GHB instead of formaldehyde. Further studies ...
Tópico(s): Anesthesia and Neurotoxicity Research
2013 - Elsevier BV | British Journal of Anaesthesia
J. Fechner, Harald Ihmsen, J. Schüttler, Christian Jeleazcov,
... safety and efficacy of the water-soluble prodrug fospropofol for anesthesia in cardiac surgery and to compare the pharmacodynamic profiles of fospropofol and propofol.Pilot study and a prospective, phase ... were randomized to receive total intravenous anesthesia with fospropofol (n = 8) or propofol (n = 8) combined with ... tests, and vital signs.The total doses of fospropofol and propofol during anesthesia were 11.3±2. ... According to the achieved bispectral index (BIS) values, fospropofol was as effective as propofol in providing general ...
Tópico(s): Cardiac, Anesthesia and Surgical Outcomes
2013 - Elsevier BV | Journal of Cardiothoracic and Vascular Anesthesia
Rui Li, Wensheng Zhang, Jin Liu, Min Tang, Yingying Yang, Nanfu Luo,
... from long duration (≤8 hours) continuous infusion of fospropofol disodium, a novel water-soluble prodrug of propofol, ... Stage 1. 16 rabbits were assigned to receive fospropofol disodium or propofol to measure MIR, using an ... 2. Eighty rabbits were allocated to group F (fospropofol disodium) or group P (propofol), and further subdivided ( ... F4h, F6h, F8h and P2h, P4h, P6h, P8h. Fospropofol or propofol were infused, and tail clamping applied ... oxygen saturation were analyzed. The plasma concentrations of fospropofol disodium, the active metabolite propofol (propofolF) and propofol ...
Tópico(s): Anesthesia and Pain Management
2012 - Elsevier BV | Veterinary Anaesthesia and Analgesia
Krystyna M. Wozniak, James J. Vornov, Bipin Mistry, Ying Wu, Rana Rais, Barbara S. Slusher,
... evaluate, in both animals and human volunteers, whether fospropofol (a water soluble phosphate ester prodrug of propofol) ... provide higher propofol bioavailability through non-intravenous routes.Fospropofol was administered via intravenous, oral and intraduodenal routes ... human volunteers.In rats, bioavailability of propofol from fospropofol delivered orally was found to be appreciable, in ... depending on dose. Availability was especially marked following fospropofol administration via the intraduodenal route, where bioavailability approximated ...
Tópico(s): Veterinary Pharmacology and Anesthesia
2015 - BioMed Central | Journal of Translational Medicine
Ajit Shah, Bipin Mistry, Ekaterina Gibiansky, Leonid Gibiansky,
Editor, GPI 15715 or Aquavan injection (fospropofol disodium; MGI Pharma, Inc., Bloomington, Minnesota, USA) is a water-soluble, phosphono-O-methyl prodrug of propofol for intravenous (i.v.) injection. ... between 2003 and 2005. Following i.v. administration, fospropofol is rapidly metabolized by alkaline phosphatase enzymes, releasing ... concentration) to prevent further in-vitro conversion of fospropofol to propofol by alkaline phosphatase enzymes. This was ... propofolFP and that it did not affect the fospropofol concentrations. The new drug application for fospropofol disodium ...
Tópico(s): Epilepsy research and treatment
2009 - Lippincott Williams & Wilkins | European Journal of Anaesthesiology
Ajit Shah, Bipin Mistry, Ekaterina Gibiansky, Leonid Gibiansky,
To the Editor:— Fospropofol disodium (GPI 15715 or Aquavan® Injection; MGI Pharma, Inc., Bloomington, MN) is a water-soluble, phosphono-O -methyl prodrug ... Anesthesiology between 2003 and 2005.After intravenous administration, fospropofol is rapidly metabolized by alkaline phosphatase enzymes, releasing ... concentration) to prevent further in vitro conversion of fospropofol to propofol by alkaline phosphatase enzymes. This was ... of propofolFPand that it did not affect the fospropofol concentrations. The new drug application for fospropofol disodium ...
Tópico(s): Antibiotics Pharmacokinetics and Efficacy
2008 - Lippincott Williams & Wilkins | Anesthesiology
Ajit Shah, Bipin Mistry, Ekaterina Gibiansky, Leonid Gibiansky,
To the Editor: Fospropofol disodium (GPI 15715 or AQUAVAN® Injection, MGI PHARMA, Bloomington, MN) is a water-soluble, phosphono-O-methyl prodrug of ... routine therapeutic procedures.1–6 Following IV administration, fospropofol is rapidly metabolized by alkaline phosphatase enzymes, releasing ... concentration) to prevent further in vitro conversion of fospropofol to propofol by alkaline phosphatase enzymes. This was ... propofol and that it did not affect the fospropofol concentrations. The new drug application (NDA) for fospropofol ...
Tópico(s): Antibiotics Pharmacokinetics and Efficacy
2008 - Lippincott Williams & Wilkins | Anesthesia & Analgesia
Joseph V. Pergolizzi, Tong J. Gan, Stanford Plavin, Sumedha Labhsetwar, Robert Taylor,
... propofol. Recently approved in the United States is fospropofol, a prodrug of propofol which hydrolyzes in the ... alkaline phosphatase to liberate propofol. Propofol liberated from fospropofol has unique pharmacological properties, but recently retracted pharmacokinetic ( ... difficult to formulate clear conclusions with respect to fospropofol's PK/PD properties. In safety and efficacy clinical studies, fospropofol demonstrated dose-dependent sedation with good rates of ... with good levels of patient and physician acceptance. Fospropofol has been associated with less pain at injection ...
Tópico(s): Anesthesia and Pain Management
2011 - Hindawi Publishing Corporation | Anesthesiology Research and Practice
Philip Yen, Simon Prior, Cara J. Riley, William Johnston, Megann Smiley, Sarat Thikkurissy,
... tolerated by patients and practitioners. This study evaluated fospropofol, a relatively new sedative/hypnotic, in comparison to ... Sixty patients were randomly assigned to either the fospropofol or the midazolam group. Each participant received 1 ... administration of the selected sedative. Those in the fospropofol group received an initial dose of 6.5 ... and (c) hemodynamic stability and adverse effects. The fospropofol group demonstrated shorter physical recovery times than midazolam ... between the 2 drug groups ( P = .123). The fospropofol group had a higher rate of local anesthetic ...
Tópico(s): Anesthesia and Neurotoxicity Research
2013 - Allen Press | Anesthesia Progress
J. Fechner, Harald Ihmsen, Christian Jeleazcov, J. Schüttler,
... a better formulation or a prodrug of propofol. Fospropofol is the first propofol prodrug that has been ... This review describes first published study results of fospropofol with regard to its pharmacokinetics/pharmacodynamics, drug safety, ... all published articles and abstracts containing the words fospropofol or GPI 15715 were included. Results and conclusion: ... an errorness drug assay for propofol liberated from fospropofol is not exactly defined, no clear conclusions can ... drawn from the first published pharmacokinetic/pharmacodynamic studies. Fospropofol was well tolerated in the first two clinical ...
Tópico(s): Cardiac, Anesthesia and Surgical Outcomes
2009 - Taylor & Francis | Expert Opinion on Investigational Drugs
Tong J. Gan, Bradley D. Berry, Evan F. Ekman, Richard C. Muckerman, Neal D. Shore, Robert Hardi,
To evaluate the safety of intravenous (IV) fospropofol when used to provide minimal to moderate sedation in patients undergoing minor surgical procedures. Phase 3, open-label, single-arm study. Multi-center. ... μg before receiving an initial dose of IV fospropofol 6.5 mg/kg. Patients could receive up to 5 supplemental doses of fospropofol 1.63 mg/kg to reach a Modified ... A mean of 2.4 supplemental doses of fospropofol was administered, and in 60% of patients, two or fewer supplemental doses of fospropofol were sufficient to initiate and complete the procedure. ...
Tópico(s): Cardiac, Anesthesia and Surgical Outcomes
2010 - Elsevier BV | Journal of Clinical Anesthesia
Basem Abdelmalak, Ashish K. Khanna, John Tetzlaff,
Fospropofol is an intravenous sedative-anesthetic agent that is FDA-approved for monitored anesthesia care (MAC) sedation ... or therapeutic procedures. As a prodrug of propofol, fospropofol’s pharmacologic activity results from its breakdown by ... who are thus skilled in advanced airway management. Fospropofol has a unique dosing regimen, with a standard ... and 90 kg respectively. Available evidence demonstrates that fospropofol in MAC sedation is successful in patients undergoing esophagogastroscopy, colonoscopy and flexible bronchoscopy. The use of fospropofol is also now being explored in many other ...
Tópico(s): Anesthesia and Pain Management
2012 - Bentham Science Publishers | Current Pharmaceutical Design
Yujun Zhang, Yingying Jiang, Haiyan Wang, Bin Wang, Jun Yang, Yi Kang, Jun Chen, Jin Liu, Wensheng Zhang,
... 29] mg/kg) was similar to that of fospropofol disodium (43.66 [43.57-43.75] mg/ ... to cause LoRR than that of HX0969W and fospropofol. However, the LoRR duration was significantly longer in response to the administration of HX0969W and fospropofol disodium than that caused by propofol. In the pharmacokinetic study, the Cmax of fospropofol was higher than that of HX0969W. HX0969W had ... and a rapid clearance rate than that of fospropofol disodium. There was no significant difference between the ... propofol whether it was released by HX0969W or fospropofol disodium; the Cmax of propofol released by HX0969W ...
Tópico(s): Epilepsy research and treatment
2020 - PeerJ, Inc. | PeerJ
Chao-Meng Wu, Wensheng Zhang, Jin Liu, Weiyi Zhang, Bowen Ke,
Background: Fospropofol disodium for injection (Fospropofol FD ) is a prodrug that is metabolized into propofol to produce a general anesthesia effect when administered intravenously. Objective: This study aimed to assess the efficacy and safety of Fospropofol FD in comparison with propofol medium/long-chain ... 2:1) to the intervention (20 mg/kg Fospropofol FD ) or control (2 mg/kg propofol-MCT/ ... functions or serious adverse events were reported. Conclusion: Fospropofol FD (20 mg/kg) is not inferior to ... use under anesthesiologist monitoring. Impact on Practice Statement: Fospropofol FD can produce a general anesthesia effect and ...
Tópico(s): Intensive Care Unit Cognitive Disorders
2021 - Frontiers Media | Frontiers in Pharmacology
David A. Lubarsky, Eric A. Harris, Keith Candiotti,
Fospropofol, a phosphorylated prodrug version of the popular induction agent propofol, is hydrolyzed in vivo to release active propofol, formaldehyde, and phosphate.Pharmacodynamic studies show fospropofol provides clinically useful sedation and EEG/bispectral index ... common complaint with propofol, was not reported with fospropofol; the major patient complaint was transitory perianal itching ... the drug's administration.Although many clinicians believe fospropofol can safely be given by a registered nurse, ...
Tópico(s): Intensive Care Unit Cognitive Disorders
2009 - Dove Medical Press | Therapeutics and Clinical Risk Management
... Aim To assess the efficacy and safety of fospropofol disodium in providing sedation in patients undergoing colonoscopy. ... multicentre trial evaluated 127 adult patients who received fospropofol (2, 5, 6.5 or 8 mg/kg) ... well as patient‐ and doctor‐rated satisfaction. Results Fospropofol produced a significant dose‐dependent increase in sedation ... ready for discharge and doctor‐rated satisfaction scores. Fospropofol was well tolerated, with most adverse events mild‐ ... Conclusion The 6.5 mg/kg dose of fospropofol provides the ideal balance of efficacy and safety ...
Tópico(s): Anesthesia and Neurotoxicity Research
2008 - Wiley | Alimentary Pharmacology & Therapeutics
Sinan Yavas, David Lizdas, Nikolaus Gravenstein, Samsun Lampotang,
... line simulations to model administration of propofol and fospropofol, a new water-soluble prodrug formulation of propofol. The prodrug formulation of fospropofol leads to a delayed onset to peak concentrations ... propofol. A comparison simulation that overlays administration of fospropofol and propofol allows clinicians to understand the differences of administering fospropofol and traditional propofol. The simulations have the added ... new website demonstrates the pharmacokinetics and pharmacodynamics of fospropofol and shows how it differs from propofol.
Tópico(s): Intensive Care Unit Cognitive Disorders
2008 - Lippincott Williams & Wilkins | Anesthesia & Analgesia
Bingchen Lang, Jun Yang, Yu Wang, Yun Luo, Yi Kang, Jin Liu, Wensheng Zhang,
Phosphate ester prodrugs of propofol (fospropofol, HX0969W) were designed to avoid the unsatisfactory water solubility of the parent drug. However, in previous clinical trials, there were reported ... HCl were synthesized from HX0969. The solubility of fospropofol, HX0969W, HX0969-Gly-F3, and HX0969-Ala-HCl ... doses were given.(1) The water solubility of fospropofol, HX0969W, HX0969-Gly-F3, and HX0969-Ala-HCl ... hepatic enzymes; (3) Compared with the previous prodrugs (fospropofol, HX0969W), the 2 novel compounds (HX0969-Gly-F3, ...
Tópico(s): Ion channel regulation and function
2014 - Lippincott Williams & Wilkins | Anesthesia & Analgesia
Carrie A. Schroeder, Rebecca A. Johnson,
... hypothesized that intracoelomic administration of a new anesthetic, fospropofol, in turtles would result in dose-dependent anesthesia ... LD]) and 50-mg/kg (high-dose [HD]) fospropofol in a crossover design. Respiratory rate, immobility, and ... In part 2, eight turtles were administered HD fospropofol. Immobility and muscle relaxation (front and hind limb) ... all P < 0.05). In part 2, HD fospropofol decreased respiratory rate from 21.5 ± 2.9 ... unpredictable quality and duration of anesthesia with intracoelomic fospropofol, it should be used with caution for general ...
Tópico(s): Analytical Chemistry and Sensors
2013 - American Association of Zoo Veterinarians | Journal of Zoo and Wildlife Medicine
Megan E. Campion, Tong J. Gan,
... procedural sedation. More recently, a new propofol prodrug, fospropofol disodium was also approved in the U.S. as a sedative. Fospropofol is formulated in aqueous solution and has some ... the pharmacology and clinical uses of propofol and fospropofol, as well as the benefits and disadvantages of ...
Tópico(s): Analytical Chemistry and Sensors
2009 - Prous Science | Drugs of today
Michel Struys, J. Fechner, J. Schüttler, H. Schwilden,
... studies on the pharmacokinetic–pharmacodynamic and tolerability of fospropofol had been published.4–9This assay inaccuracy makes ... assay to describe the pharmacokinetics and pharmacodynamics of fospropofol in healthy volunteers and patients. They stated their ... not able to reanalyze the pharmacokinetics–pharmacodynamics of fospropofol in human volunteers within the deadline of 12 ...
Tópico(s): Antibiotics Pharmacokinetics and Efficacy
2010 - Lippincott Williams & Wilkins | Anesthesiology
Michel Struys, J. Fechner, J. Schüttler, H. Schwilden,
... studies on the PK/PD and tolerability of fospropofol had been published.4–9 This assay inaccuracy ... to describe the pharmacokinetics and pharmaco dynamics of fospropofol in healthy volunteers and patients. They stated their ... not able to reanalyze the PK/PD of fospropofol in human volunteers within the deadline of 12 ...
Tópico(s): Cardiac, Anesthesia and Surgical Outcomes
2010 - Lippincott Williams & Wilkins | Anesthesia & Analgesia
Gerard A. Silvestri, Brad D. Vincent, Momen M. Wahidi,
Background Fospropofol disodium is a water-soluble prodrug of propofol. A subset analysis was undertaken of elderly patients (≥65 ... Patients received fentanyl citrate (50 mcg) followed by fospropofol at initial (4.88 mg/kg) and supplemental ( ... but no escalation of care was required. Conclusions Fospropofol provided safe and effective sedation, rapid time to ...
Tópico(s): Nausea and vomiting management
2011 - Lippincott Williams & Wilkins | Journal of Bronchology & Interventional Pulmonology
Sergio D. Bergese, Poorvi Dalal, Rashmi Vandse, Andrew Satlin, Zhengning Lin, Keith Candiotti, LARRY E. COHEN, Tong-Joo Gan,
Fospropofol is a sedative hypnotic with a slower onset and longer duration of action. Fospropofol has demonstrated successful dose-dependent sedation at 6. ... the approved dose or weight-adjusted dose of fospropofol in a 1:1 ratio. Subgroup 1 (n = ...
Tópico(s): Nausea and vomiting management
2012 - Lippincott Williams & Wilkins | American Journal of Therapeutics
... already visible, albeit faintly. Consider the case of fospropofol. The initial marketing plan for this drug was ... proceduralists want to have a drug such as fospropofol that they could use without an anesthesiologist. Some ... taken by the specialty over innovations such as fospropofol could be seen as protectionist or obstructive. Embracing ...
Tópico(s): Hemodynamic Monitoring and Therapy
2009 - Lippincott Williams & Wilkins | Anesthesia & Analgesia
... agents used for endoscopic sedation continues to evolve. Fospropofol (FP), a prodrug of propofol with a slower ... events associated with the novel sedative/hypnotic. Keywords: fospropofol, Aquavan, propofol, sedation, colonoscopy
Tópico(s): Anesthesia and Pain Management
2008 - Dove Medical Press | Therapeutics and Clinical Risk Management
Michelle P. McIntosh, Roger A. Rajewski,
The pharmacokinetics and pharmacodynamics of fospropofol (FP) disodium injection, propofol emulsion (PE), and cyclodextrin-enabled propofol (CDP) solution following bolus parenteral administration in dogs was evaluated. Three ... 3547–3552, 2012 The pharmacokinetics and pharmacodynamics of fospropofol (FP) disodium injection, propofol emulsion (PE), and cyclodextrin- ...
Tópico(s): Anesthesia and Pain Management
2012 - Elsevier BV | Journal of Pharmaceutical Sciences