FOSPROPOFOL DISODIUM CAS 258516-87-9

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Fospropofol disodium, molecular formula C13H19O5P.2Na, CAS 258516-87-9, was approved by the US Food and Drug Administration (FDA) on December 12, 2008 for marketing in Sichuan under the trade name Lusedra. This drug is a sedative hypnotic developed by the American company Elsa, used clinically for the diagnosis or treatment of adult patients. It is intravenous injection of propofol sodium. The cultural scientific name is 2,6-diisopropylphenoxymethyl monoester phosphate disodium salt. This substance reduces cerebral ischemia-reperfusion injury by activating the NO cGMP pathway. In a rat model of focal cerebral ischemia, pretreatment can reduce infarct volume by 30% and improve neurological function scores. Its mechanism involves inhibiting calcium overload, reducing oxidative stress, and anti neuroinflammatory effects, providing new ideas for stroke treatment.

Fospropofol disodium, as the first independently developed Class 1 new drug in China, is a water-soluble precursor drug of propofol. It releases the active ingredient propofol through in vivo metabolism, achieving sedative and anesthetic effects. Its innovative design breaks through the limitations of traditional propofol emulsions and demonstrates unique advantages in clinical applications. The following systematically summarizes its uses and values from five dimensions: anesthesia induction and maintenance, intensive care unit (ICU) sedation, comfort medicine, special patient populations, and future exploration directions.

Anesthesia induction and maintenance: the core choice for stabilizing the circulatory system

 

1. Innovation in anesthesia induction
Phosphopropofol disodium achieves stable blood drug concentration control during anesthesia induction through the "prodrug conversion" mechanism. Its onset time is (2.9 ± 1.1) minutes, with a peak time of (4.8 ± 1.5) minutes, slightly slower than propofol but with a longer duration of action (25-30 minutes), providing anesthesiologists with a more relaxed operating window. Clinical studies have shown that doses of 10-12 mg/kg can meet the induction needs of most patients, and the hemodynamic fluctuations are significantly smaller than those of propofol. For example, in patients undergoing coronary artery bypass grafting, the sedative effect of propofol disodium and propofol is comparable, but the fluctuation amplitude of mean arterial pressure is reduced by 15% -20%, especially suitable for elderly patients and those with unstable cardiovascular function.

 

2. Advantages of anesthesia maintenance
As a maintenance medication, propofol disodium achieves stable anesthesia depth through continuous pump infusion (10-20mg · kg ⁻¹· h ⁻¹). Its metabolite propofol inhibits the central nervous system by enhancing the function of gamma aminobutyric acid (GABA) receptors, while avoiding lipid loading of emulsion formulations. In short-term surgeries such as ureteroscopic lithotripsy, the sedative effect of 6.5mg/kg dose is equivalent to that of etomidate 0.3mg/kg, but the mean arterial pressure is higher 5 minutes after anesthesia induction (89.17 ± 7.08mmHg vs. 85.51 ± 7.74mmHg), significantly reducing the risk of hypotension.

 

3. Convenience and safety of operation
Phosphopropofol disodium is in the form of freeze-dried powder and can be injected after reconstitution, completely avoiding the three major drawbacks of propofol emulsion:

Injection pain: The incidence of injection pain in propofol emulsion is as high as 31.3%, while that in propofol disodium is only 13.3%;
Lipid metabolism disorder: Long term infusion of propofol can lead to hypertriglyceridemia (incidence rate of about 18%), while only 3 cases (10%) were observed in the propofol disodium group;
Risk of infection: Fat emulsion is used as a bacterial culture medium, and there is no hidden danger with propofol disodium phosphate. It does not contain any adsorbent components and is suitable for long-term sedation scenarios such as ECMO.

ICU sedation: the ideal choice for critically ill patients

 

1. Sedation management of mechanically ventilated patients
Phosphopropofol disodium exhibits dose-dependent sedative effects in ICU. Research has shown that doses of 3.0-3.5mg · kg ⁻¹· h ⁻¹ can achieve mild to moderate sedation (RASS score -3-0) in 75% of patients without the need for remedial medication. Compared with propofol, the overall incidence of adverse events was lower (76.7% vs. 90.0%), mainly manifested as mild tachycardia and hypotension, with no reported catheter-related bloodstream infections or propofol infusion syndrome. In deep sedation (RASS score -4-5) studies, a dose of 8mg/kg/h can achieve 100% of the target sedation level and has better hemodynamic stability than propofol.

 

2. Adaptability of critically ill patients with special conditions
Acute respiratory distress syndrome (ARDS): Deep sedation is required to reduce human-machine asynchrony, and propofol disodium reduces the risk of respiratory depression by stabilizing blood drug concentrations;
Extracorporeal membrane oxygenation (ECMO): Traditional emulsions may block the membrane lungs, while propofol disodium as a water-soluble formulation has no such risk and can prolong the service life of the membrane lungs;
Severe acute pancreatitis: Propofol and propofol disodium phosphate are contraindicated in patients with hyperlipidemia to avoid lipid loading, making them the preferred sedative drugs.

 

3. Safety of long-term sedation
In a 72 hour sedation study, there was no significant difference in plasma formate concentration between the propofol group and the propofol group (13 ± 7 μ g/ml vs. 12 ± 6 μ g/ml), far below the toxicity threshold (7-11mg/ml). Its metabolites are excreted through the dual channels of liver and kidney. Patients with liver dysfunction should use medication with caution, but those with kidney dysfunction do not need to adjust the dosage.

Comfortable healthcare: a key role in enhancing patient experience

 

1. Optimization of Digestive Endoscopy Examination
Fospropofol disodium performs well in painless gastroscopy. A randomized controlled trial involving 200 patients showed that the success rate of sedation at a dose of 6.5mg/kg was 96%, and the patient satisfaction score was significantly higher than that of the midazolam group (4.7 ± 0.3 vs. 3.9 ± 0.5). Its advantages lie in:

Smooth onset: Avoiding the "explosive" inhibition of propofol and reducing the risk of respiratory arrest;
Rapid recovery: postoperative recovery time shortened by 20%, reducing observation time;
No injection pain: improves patient acceptance, especially suitable for outpatient short surgeries.

 

2. Applicability of Joint Inspection
For the combined examination of gastroscopy and colonoscopy (requiring 20-30 minutes of anesthesia time), the sustained sedative effect of propofol disodium is significantly better than propofol. Clinical data shows that the anesthesia maintenance time is extended by 15-20 minutes compared to propofol, and the incidence of intraoperative body movement is reduced by 40%, ensuring the integrity of the examination.

 

3. Prevention of Postoperative Nausea and Vomiting (PONV)
Phosphopropofol disodium reduces the risk of PONV by reducing the dosage of opioid drugs. In gynecological laparoscopic surgery, the induction dose is reduced by 30% compared to propofol, and the incidence of postoperative nausea decreases from 25% to 12%, and the incidence of vomiting decreases from 8% to 3%.

Phosphopropofol disodium has become an important innovation in the field of anesthesia and sedation due to its water-soluble prodrug design, stable pharmacokinetic properties, and wide clinical adaptability. The value of anesthesia induction to long-term sedation in ICU, from comfortable medical care to special patient management, is constantly being validated through clinical practice.

The synthetic route of sodium fospropofol disodium: 26 diisocyanate The intermediate O - (chloromethyl) - 26 diisopropyl phenol is obtained from propylphenol as raw material by reacting with chloromethyl methyl sulfide, methylthiomethylation, and chlorination with sulfonyl chloride; The intermediate is condensed with dibenzyl silver phosphate to obtain triester phosphate, which is finally reduced by hydrogenation, deprotected, and neutralized with sodium carbonate solution to obtain sodium propofol. The synthesis route is shown in the figure.

In addition, there are two synthetic methods: 2,6 bivalent phenol reacts with chlorobromomethane in H to obtain the intermediate 0 - (chloromethyl) 2 6 diisopropylphenol, which is then condensed with phosphoric acid, and then treated with sodium hydroxide solution to obtain the target compound disodium phosphate sodium propofol, a water-soluble precursor of propofol, which is metabolized by alkaline phosphatase on the surface of endothelial cells in vivo after intravenous administration to produce the active drug propofol, It quickly achieves balance in the brain tissue, thus playing a dose-dependent sedative and hypnotic role.

In addition, there are two synthetic methods: 2,6 bivalent phenol reacts with chlorobromomethane in H to obtain the intermediate 0 - (chloromethyl) 2 6 diisopropylphenol, which is then condensed with phosphoric acid, and then treated with sodium hydroxide solution to obtain the target compound disodium phosphate sodium propofol, a water-soluble precursor of propofol, which is metabolized by alkaline phosphatase on the surface of endothelial cells in vivo after intravenous administration to produce the active drug propofol, It quickly achieves balance in the brain tissue, thus playing a dose-dependent sedative and hypnotic role.

Phase I clinical study showed that propofol, the active metabolite, could induce stronger anesthetic effect than propofol in fat emulsion. Phase I clinical study showed that propofol, the active metabolite, can effectively maintain the sedation of patients undergoing colonoscopy, while phase II study mainly evaluated the sedation of patients requiring bronchoscopy and minor surgery.

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