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Propofol, a widely used sedative/anesthetic agent, is a phenolic compound known for its rapid onset and brief duration of action. It is highly versatile, employed in various clinical settings for sedation, anesthesia, and more recently, as an investigational treatment.
Propofol is a widely used intravenous medication for anesthesia and sedation, known for its rapid onset and short duration of action. It's commonly employed in medical settings due to these properties.
Originally developed by Imperial Chemical Industries (ICI) as ICI 35868, propofol was formulated into an emulsion to enhance solubility. The commercial version, launched in 1986 under the brand name Diprivan, consists of a 1% propofol solution with soybean oil and phospholipids as emulsifiers. This formulation addresses earlier issues related to hypersensitivity.
Propofol is highly protein-bound, which affects its activity in the body. It undergoes hepatic metabolism through conjugation, leading to a clinical effect that diminishes quickly despite an elimination half-life ranging from 2 to 24 hours.
Developed by veterinarian John B. Glen over 13 years, propofol was recognized with the 2018 Lasker Award for clinical research. Its journey from initial trials in 1977 to market introduction in 1986 highlights its significance in anesthesia.
The medication can cause respiratory depression, hypotension, and pain at injection sites. Rarely, it may lead to propofol infusion syndrome, a severe condition. Formulation components like soybean oil and egg phospholipids pose risks for those with specific allergies.
Recent developments include fospropofol (Lusedra), a water-soluble prodrug, which reduces injection site pain. Additionally, innovative derivatives like ciprofol, showing improved efficacy and fewer side effects, are under Phase III trials. Research also explores propofol's potential in treating treatment-resistant depression.
Developed by John B. Glen over 13 years, propofol was first identified in 1973. Initial formulations using cremophor EL were problematic due to allergic reactions, prompting a reformulation into a soy oil emulsion. This version, named Diprivan, was launched in 1986 and contains 1% propofol, soybean oil, egg phospholipids, glycerol, and sodium hydroxide.
In November 2024, the FDA approved PropofolVet Multidose for dogs, marking a milestone in veterinary medicine. This generic version offers reliable anesthetic properties and aligns with the established efficacy of brand-name counterparts like PropoFlo 28.
Fospropofol, a water-soluble prodrug approved in 2008, reduces injection pain. Ciprofol, a more potent derivative with fewer side effects, is undergoing Phase III trials as of 2022.
Propofol's rapid onset, short recovery time, and minimal nausea compared to opioids make it invaluable in clinical practice. Ongoing research promises further innovations, enhancing its role in both human and veterinary medicine.
In 2024, PropofolVet Multidose was approved for veterinary use in dogs, offering a generic alternative to PropoFlo 28, which has been available since 2011.
Propofol's significance is marked by its efficacy and the recognition of its developer with the Lasker Award. Ongoing research into derivatives like Ciprofol highlights its evolving role in both human and veterinary medicine.