Fospropofol

Mahajan, Rajesh; Mahajan, Bharti; Kaushal, Sandeep

doi:10.4103/0976-500x.99457

Cited by 16 publications

(20 citation statements)

References 14 publications

(33 reference statements)

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“…Only one patient of hypoxemia required the airway assistance (verbal stimulation). Thus, fospropofol showed lower incidences of hypotension, respiratory depression, apnea, and loss of airway patency because of its slower onset of action (Mahajan, Mahajan & Kaushal, 2012). On the basis of the findings in this study, there is no significant difference between HX0969W and fospropofol disodium in pharmacodynamic and pharmacokinetic studies.…”

Section: Discussionmentioning

confidence: 51%

The preclinical pharmacological study on HX0969W, a novel water-soluble pro-drug of propofol, in rats

Zhang

Wang

et al. 2020

PeerJ

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Background. Propofol is the most widely used intravenous sedative-hypnotic anesthetic in clinical practice. However, many serious side effects have been related to its lipid emulsion formulation. The pro-drug design approach was used to develop the watersoluble propofol, which could effectively resolve the limitations associated with the lipid emulsion formulation. Thus, the new water-soluble pro-drug of propofol, HX0969W, was designed and synthesized. The objective of this study was to conduct preclinical pharmacological studies on this novel water-soluble pro-drug of propofol. Methods. The assessment of the loss of the righting reflex (LoRR) was used for the pharmacodynamic study, and liquid chromatography-tandem mass spectrometry and high-performance liquid chromatography-fluorescence were used for the pharmacokinetic study. Results. The potency of HX0969W (ED 50 [95% CI], 46.49 [43.89-49.29] mg/kg) was similar to that of fospropofol disodium (43.66 [43.57-43.75] mg/kg), but was lower than that of propofol (4. 82 [4.8-14.82] mg/kg). Administered with a dose of 2-fold ED 50 , propofol required a shorter time 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 C max of fospropofol was higher than that of HX0969W. HX0969W had a shorter mean residual time and a rapid clearance rate than that of fospropofol disodium. There was no significant difference between the T max of the propofol whether it was released by HX0969W or fospropofol disodium; the C max of propofol released by HX0969W was similar to that of propofol, which was higher than the propofol released by fospropofol disodium. Subjects Anesthesiology and Pain Management, Pharmacology W-. 2020. The preclinical pharmacological study on HX0969W, a novel water-soluble pro-drug of propofol, in rats. PeerJ 8:e8922 http://doi.

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Section: Discussionmentioning

confidence: 51%

The preclinical pharmacological study on HX0969W, a novel water-soluble pro-drug of propofol, in rats

Zhang

Wang

et al. 2020

PeerJ

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“…Sufficient levels of folate and vitamin B12 are necessary to prevent formate toxicity, as these are cofactors for the metabolism of formate to carbon dioxide. 3 There were no treatment-related adverse events besides the well-known burning sensation, and fospropofol was used safely to achieve general anesthesia as well as pre-and postoperative sedation. Clearly, the patient population studied was too small to prove the overall safety of fospropofol for general anesthesia or even long-term sedation.…”

Section: Total Intravenous Anesthesia With Fospropofolmentioning

confidence: 99%

“…2 As propofol is released from fospropofol by hydrolysis, clinical pharmacokinetics of fospropofol compared with propofol are characterized by a longer time to peak effect with lower peak plasma concentrations. 3 Fospropofol compared with propofol has been evaluated in young male volunteers, 4-8 but because of retroactively identified problems with the specific assay measuring the liberated propofol from fospropofol, 9 the pharmacokinetics and pharmacodynamics of fospropofol reported in these studies probably were incorrect, so that the publications were retracted. 10 Until now, no correct pharmacokinetic data about fospropofol pharmacokinetics in humans have been published.…”

mentioning

confidence: 98%

“…10 Until now, no correct pharmacokinetic data about fospropofol pharmacokinetics in humans have been published. 3 Fospropofol also was studied in patients undergoing moderate procedural sedation [11][12][13][14][15] and for sedation in ventilated ICU patients. 2 These studies provided evidence that because of its different pharmacokinetics, fospropofol produces a slower onset of sedative-hypnotic effects and has a prolonged effect compared with propofol.…”

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confidence: 99%

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A Randomized Open-Label Phase I Pilot Study of the Safety and Efficacy of Total Intravenous Anesthesia With Fospropofol for Coronary Artery Bypass Graft Surgery

Fechner

Ihmsen

Schüttler

et al. 2013

Journal of Cardiothoracic and Vascular Anesthesia

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“…The substitution of a noncharged hydroxyl group for a charged phosphate group on the 2,6 diisopropylphenol molecule induces an electronegativity allowing the new molecule to dissolve in water. 11,20,37 This water-soluble drug is gaining popularity among human physicians for sedation during procedures such as bronchoscopy, colonoscopy, and minor surgical procedures. 10,11 However, its use in veterinary species has only recently been reported and no reptile studies have been performed.…”

Section: Introductionmentioning

confidence: 99%

THE EFFICACY OF INTRACOELOMIC FOSPROPOFOL IN RED-EARED SLIDERS (TRACHEMYS SCRIPTA ELEGANS)

Schroeder

Johnson

2013

Journal of Zoo and Wildlife Medicine

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Intravenous anesthetic delivery in reptiles can be challenging; current injectable techniques have varied induction/recovery times and anesthetic quality. This study hypothesized that intracoelomic administration of a new anesthetic, fospropofol, in turtles would result in dose-dependent anesthesia and respiratory depression. A two-part prospective trial using adult red-eared slider turtles (Trachemys scripta) weighing 764±17 g was conducted to 1) determine an effective anesthetic dose, and 2) evaluate the anesthetic quality, duration and respiratory effects of an efficacious dose. In Part 1, six turtles were randomly administered 25 mg kg−1 (low dose: LD) and 50 mg kg−1 (high dose: HD) fospropofol in a cross-over design. Respiratory rate, immobility and muscle relaxation scores were evaluated for 180 minutes. In Part 2, eight turtles were administered HD fospropofol. Immobility and muscle relaxation (front and hind limb) scores, and time to endotracheal intubation/extubation were evaluated until scores returned to baseline. In Part 1, the LD group had significantly lower immobility and muscle relaxation scores versus the HD group over time (both P<0.05); scores were significantly elevated from baseline for 20–120 minutes and 15–180 minutes, respectively (all P<0.05). Although not significantly different between groups (P>0.05), respiratory rate was significantly decreased from baseline from 10–120 minutes (all P<0.05). In Part 2, HD fospropofol decreased respiratory rate from 21.5±2.9 breaths min−1 to 0.1±0.1 breaths min−1, similar to the results in Part 1. Maximal reductions in immobility, front and hind limb motor tone occurred at 39.0±4.1, 30.8±3.6, and 24.0±3.6 minutes, respectively. Intubation in 7/8 turtles occurred at 45.7±5.4 min and extubation at 147.0±23.2 min. However, 2/8 turtles showed prolonged anesthetic effects, requiring resuscitative efforts for recovery. Due to the unpredictable quality and duration of anesthesia with intracoelomic fospropofol, it should be used with caution for general anesthesia in red-eared sliders at the doses and administration route investigated.

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Fospropofol

Cited by 16 publications

References 14 publications

The preclinical pharmacological study on HX0969W, a novel water-soluble pro-drug of propofol, in rats

The preclinical pharmacological study on HX0969W, a novel water-soluble pro-drug of propofol, in rats

A Randomized Open-Label Phase I Pilot Study of the Safety and Efficacy of Total Intravenous Anesthesia With Fospropofol for Coronary Artery Bypass Graft Surgery

THE EFFICACY OF INTRACOELOMIC FOSPROPOFOL IN RED-EARED SLIDERS (TRACHEMYS SCRIPTA ELEGANS)

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