Delving into the Latest Updates on Fospropofol Disodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fospropofol, Fospropofol disodium (USAN), 磷丙泊酚

+ [9]

Target

GABAA receptor

Mechanism

GABAA receptor agonists(Gamma-aminobutyric acid A receptor agonists)

Therapeutic Areas

Other Diseases

Active Indication

AnesthesiaSedation

Inactive Indication

AnalgesiaAnxiety DisordersCarpal Tunnel Syndrome+ [3]

Originator Organization

Eisai Co., Ltd.

Active Organization

Yichang Humanwell Pharmaceuticals Co., Ltd.

Inactive Organization

Eisai, Inc.

West China Hospital

Drug Highest PhaseApproved

First Approval Date

US (08 Dec 2008),

Anesthesia

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC13H21O5P

InChIKeyQVNNONOFASOXQV-UHFFFAOYSA-N

CAS Registry258516-89-1

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STUDY OBJECTIVEFospropofol disodium is a propofol prodrug that is water-soluble and has a reduced risk of bacterial contamination and hypertriglyceridemia compared with propofol. Prior to implementing a large randomized trial, we investigated the feasibility, initial efficacy, and safety of fospropofol disodium compared with propofol in long-term mild-to-moderate sedation in intensive care units (ICUs).DESIGNSingle-centered, prospective, unblind, randomized, parallel-group clinical trial.SETTINGThe general ICU of university-affiliated teaching hospital.PATIENTSAdult patients (n = 60) expected to have mechanical ventilation for >24 h were enrolled and randomly assigned to the fospropofol or propofol group.INTERVENTIONSThe fospropofol group received continuous fospropofol disodium infusions and the propofol group received continuous propofol infusions. The sedation goal was a score of -3 to 0 on the Richmond Agitation and Sedation Scale (RASS).MEASUREMENTSThe primary outcome was the percentage of time spent in the target sedation range without rescue sedation. Safety outcomes were based on adverse events. Blood samples were collected to measure formate concentration in plasma.MAIN RESULTSThe median dose was 4.33 (IQR, 3.08-4.94) mg/kg/h in the fospropofol group and 1.96 (IQR, 1.44-2.94) mg/kg/h in the propofol group. The median percentage of time spent in the target RASS range without rescue sedation was identical in both groups, with 83.33% (IQR, 74.43%-100.00%) in the fospropofol group and 83.33% (IQR, 77.45%-100.00%) in the propofol group (p = 0.887). At least one adverse event was identifed in 23 (76.7%) fospropofol patients and 27 (90.0%) propofol patients. The most common adverse events were tachycardia and hypotension. No paresthesia, catheter-related bloodstream infection or propofol infusion syndrome in both groups was reported. Three patients in the fospropofol group had mild hypertriglyceridemia, and nine patients in propofol group had hypertriglyceridemia (mild in eight patients and moderate in one patient) (10% versus 30%, p = 0.104). The formate concentration in plasma was very low, and no significant difference was identified at any time point between the two groups.CONCLUSIONSFospropofol disodium appears to be a feasible, effective and safe sedative for patients receiving invasive mechanical ventilation with long-term sedation.

01 Jan 2023·Pharmacology

Propofol-Associated Urine Discoloration: Systematic Literature Review

Review

Author: Cortesi, Cinzia ; Milani, Gregorio P ; Lava, Sebastiano A G ; Camozzi, Pietro ; Bianchetti, Mario G ; Lasica, Ana ; Schera, Federica M

Introduction: Propofol occasionally induces a green or pink-cloudy urine discoloration. A lesser-known effect is green discoloration of hair, milk, liver, or stool. We aimed to gain insight into the features of these disturbances. Methods: The terms (“propofol” OR “fospropofol”) AND (“green” OR “pink” OR “cloudy” OR “pink-cloudy”) were searched in Excerpta Medica, MEDLINE/PubMed®, and Web of Sciences databases, with no language limit, from inception up to February 2023 (CRD4202236804). Articles reporting individually documented cases were retained, and data were extracted using a checklist. Results: Seventy-seven original reports documented 95 cases (including 13 subjects ≤18 years of age). Completeness of reporting was satisfactory in 33, good in 35, and excellent in 27 cases. Propofol-associated green urine discoloration was observed in 54 patients. In most instances (n = 21, 39%), propofol was given for ≥24 h. Sometimes, however, the urine discoloration developed after propofol for ≤3 h (n = 12, 22%). Propofol-associated urine discoloration was usually observed during the administration of this agent, but it was at times (n = 11) first recognized ≥3 h after propofol discontinuation. The duration of green urine discoloration was usually ≤24 h after stopping propofol. Propofol-associated green urine discoloration was never associated with worsening kidney function. A pink-cloudy urine discoloration was observed in 32 subjects with an acidic urine pH and increased uric acid excretion given propofol for ≤24 h. A stage I acute kidney injury was observed in 2 cases (6.3%) of propofol-associated pink-cloudy urine discoloration. Nine cases of non-urinary green discoloration were observed: hair (n = 4), breast milk (n = 1), liver (n = 1), stool (n = 1). Conclusion: Propofol is sometimes associated with a green (benign) or pink-cloudy (occasionally associated with mild acute kidney injury) urine discoloration. Rarely, non-urinary green discoloration has been reported.

01 Oct 2020·Digestive Diseases and SciencesQ3 · MEDICINE

Recent Developments in Drugs for GI Endoscopy Sedation

Q3 · MEDICINE

Review

Author: Goudra, Basavana ; Gouda, Gowri ; Mohinder, Preet

Providing sedation for patients undergoing gastrointestinal (GI) endoscopy continues to be a debated topic in both anesthesia and gastroenterology circles. Sedation approaches are widely varied across the globe. While propofol administration is embraced by more endoscopists and patients, its administration evolves controversy. Whereas trained nurses and gastroenterologists are allowed to administer propofol for GI endoscopy sedation in Europe and Asia, it is the sole privilege of anesthesia providers in the USA. However, the costs of anesthesia providers are significant and threaten to derail the screening colonoscopy practice. Efforts were made by both drug and device manufacturers to find alternatives. Fospropofol was one such effort that did not live up to the expectations due to respiratory depressant properties that were similar to propofol. Use of a new tool to administer propofol in the form of Sedasys® was the next experiment that tried to find alternative to anesthesia providers. The device did not succeed due to inadequate sedation. The latest effort is remimazolam, a new benzodiazepine that has quicker recovery profile. In the interim, many drug combinations such as propofol-dexmedetomidine and propofol-ketamine are improving the safety without compromising the quality of sedation. This review attempts to discuss the new drug innovations and drug combinations of existing sedatives for the benefit of readers.

100 Deals associated with Fospropofol Disodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D04257	Fospropofol Disodium	N01AX10	DB06716

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	CN	Yichang Humanwell Pharmaceuticals Co., Ltd.	19 May 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Anesthesia	Preclinical	US	Eisai, Inc.	08 Dec 2008
Consciousness	Preclinical	US	Eisai, Inc.	01 Mar 2006
Carpal Tunnel Syndrome	Preclinical	-	Eisai, Inc.	01 Oct 2004
Analgesia	Preclinical	-	Eisai, Inc.	01 Sep 2004
Anxiety Disorders	Preclinical	-	Eisai, Inc.	01 Sep 2004
Colonic Polyps	Preclinical	-	Eisai, Inc.	01 Sep 2004
Sedation	Preclinical	-	Eisai, Inc.	01 Sep 2004
Sedation	Preclinical	-	Eisai, Inc.	01 Sep 2004
Coronary Artery Disease	Preclinical	-	Eisai, Inc.	01 Feb 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01260142 (CTgov)	Phase 4	Anesthesia	36	Fospropofol (Fospropofol 6.5 mg/kg)	zikgfpfaqb(uyszegdmqi) = hccyoaqrod dcljkfseyk (qavftgrhyn, tcwlwsbsrl - tsfsgllwyl) View more	-	27 Jan 2017
				Fospropofol (Fospropofol 10 mg/kg)	zikgfpfaqb(uyszegdmqi) = tqtaowbjmd dcljkfseyk (qavftgrhyn, irowbtwffa - acsugegxas) View more
NCT01401049 (CTgov)	Phase 4	Pain \| Complication of injection	116	Fospropofol (Fospropofol)	vxxtxutphd(ujzroqvkbk) = anncubrpws kqbjynxxkj (vdbcaqhxub, rtnwidrzgm - iuvyztvzuu) View more	-	26 Jan 2015
				Propofol+Lidocaine (Propofol/Lidocaine)	vxxtxutphd(ujzroqvkbk) = xsaofjmtgt kqbjynxxkj (vdbcaqhxub, nbisjfracb - hibsabgtir) View more
NCT01195103 (CTgov)	Phase 4	Sedation \| occlusions	13	Fentanyl+Fospropofol disodium (10 mg/kg Lusedra)	ccyujwswco(iktzelzbck) = wcdhfcnlhh rurzdoclqz (lqcnsxfsda, xidsimlxqv - aggxjuwrzs) View more	-	29 Mar 2012
				Fentanyl+Fospropofol disodium (6.5 mg/kg Lusedra)	ccyujwswco(iktzelzbck) = ohtfjgwtze rurzdoclqz (lqcnsxfsda, mywxgozqyx - bibhaokeht) View more
NCT00306722 (Pubmed \| Chest)	Phase 3	Sedation	252	Fospropofol 2 mg/kg	trjgavolgy(rbszfyjbdq) = rcuadhafbn pwvcaffmpn (rszqvovfzw ) View more	-	01 Jan 2009
				Fospropofol 6.5 mg/kg	trjgavolgy(rbszfyjbdq) = ykynruivkl pwvcaffmpn (rszqvovfzw ) View more