Literature DB >> 19731849

New drug, fospropofol disodium: a propofol prodrug.

Mark Welliver1, Susan M Rugari.   

Abstract

The use of propofol presents chemical and clinical concerns, including pain on injection, allergy risks, possible bacteria growth, and hyperlipidemia. These concerns have encouraged the search for alternative propofol formulations. Elimination of the soybean oil and lecithin carrier agents is difficult because the highly lipophilic diisopropyl phenol molecule does not dissolve in water. Propofol in aqueous solution would be a preferable alternative to lipid-based emulsions. One formulation of propofol is fospropofol disodium (Lusedra, Eisai Corporation of North America, Woodcliff Lake, New Jersey), previously known as Aquavan (MGI Pharma, Bloomington, Minnesota). Fospropofol is an aqueous solution of a propofol prodrug intended for injection. The discovery and development of this drug may address the concerns with the current propofol emulsion formulations while offering altered pharmacokinetics and pharmacodynamics for sedation. The structure, pharmacokinetics, pharmacodynamics, clinical studies, clinical applications, and implications are discussed.

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Year:  2009        PMID: 19731849

Source DB:  PubMed          Journal:  AANA J        ISSN: 0094-6354


  8 in total

1.  The efficacy of intracoelomic fospropofol in red-eared sliders (Trachemys scripta elegans).

Authors:  Carrie A Schroeder; Rebecca A Johnson
Journal:  J Zoo Wildl Med       Date:  2013-12       Impact factor: 0.776

Review 2.  The rationality for using prodrug approach in drug discovery programs for new xenobiotics: opportunities and challenges.

Authors:  Nuggehally R Srinivas
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2011-03-15       Impact factor: 2.441

3.  Dexmedetomidine as part of balanced anesthesia care in children with malignant hyperthermia risk and egg allergy.

Authors:  Elisabeth Dewhirst; Aymen Naguib; Joseph D Tobias
Journal:  J Pediatr Pharmacol Ther       Date:  2011-04

Review 4.  The Role of GABA Receptor Agonists in Anesthesia and Sedation.

Authors:  Janette Brohan; Basavana G Goudra
Journal:  CNS Drugs       Date:  2017-10       Impact factor: 5.749

5.  Hemodynamic changes following the administration of propofol to facilitate endotracheal intubation during sevoflurane anesthesia.

Authors:  Elisabeth Dewhirst; Christopher Lancaster; Joseph D Tobias
Journal:  Int J Clin Exp Med       Date:  2012-11-18

6.  Fospropofol: clinical pharmacology.

Authors:  Girish M Bengalorkar; K Bhuvana; N Sarala; Tn Kumar
Journal:  J Anaesthesiol Clin Pharmacol       Date:  2011-01

7.  Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers.

Authors:  Krystyna M Wozniak; James J Vornov; Bipin M Mistry; Ying Wu; Rana Rais; Barbara S Slusher
Journal:  J Transl Med       Date:  2015-05-29       Impact factor: 5.531

Review 8.  Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects.

Authors:  Ricardo Jorge Dinis-Oliveira
Journal:  Biomed Res Int       Date:  2018-05-24       Impact factor: 3.411

  8 in total

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