What is propofol?
Propofol is an intravenous, short acting anesthetic with rapid onset of action used in the induction and maintenance of anesthesia. Propofol is also applied as sedative, ex. to ventilated patients in intensive care.
Propofol serves to facilitate rapid and smooth transitions into unconsciousness, allowing medical professionals to perform necessary interventions with precision. Its rapid onset and relatively short duration of action grant an anesthesiologist fine control over the depth of anesthesia, while its swift metabolism by the liver minimizes the risk of prolonged sedation post-procedure.
It was developed some 40 years ago by the former UK company ICI. Propofol was approved in 1986 as an emulsion under the trade name Diprivan® and is used with sophisticated syringe pump systems.
Because of its indisputable efficiency and importance, propofol was listed as an essential drug by the World Health Organization (WHO) in 2016.
How does propofol work?
Propofol mechanism of action
Propofol’s mechanism of action primarily involves its modulation of GABA receptors, leading to enhanced inhibitory neurotransmission in the central nervous system. Structurally, propofol is a lipophilic molecule, which allows it to cross the blood-brain barrier rapidly. Once in the brain, it interacts with GABA-A receptors, a type of ligand-gated ion channel receptor.
Propofol’s interaction with GABA-A receptors allosterically potentiates the receptor’s response to GABA. It enhances the duration and frequency of chloride ion channel openings upon GABA binding, effectively increasing the influx of chloride ions into neurons. This intensified chloride influx hyperpolarizes the neuron’s membrane potential, making it less excitable and reducing the likelihood of action potential generation. This collective inhibition of neuronal firing contributes to the sedative, hypnotic, and anesthetic effects of propofol.
Beyond GABA-A receptors, propofol may also modulate other receptor systems, including those associated with norepinephrine and dopamine, which could further influence its sedative and anesthetic properties. However, these interactions are complex and not fully elucidated.
What are the applications of propofol?
Propofol is most famous for its applications related to anesthesia and sedation:
- Anesthesia: It is an indispensable tool in anesthetizing patients for surgeries ranging from minor to complex, ensuring their comfort and safety under the care of skilled practitioners.
- Procedural sedation: Procedures such as endoscopies, colonoscopies, and certain diagnostic imaging tests often require patient sedation to minimize discomfort and anxiety.
- ICU (intensive care unit) sedation: Patients in critical care units may require sedation to facilitate mechanical ventilation, ease anxiety, and improve patient comfort.
- Sedation for medical interventions: Propofol is often used for sedating patients during various medical interventions, such as cardioversion (restoring normal heart rhythm), bronchoscopy, and wound debridement.
- Veterinary sedation: In veterinary medicine propofol is used for short-time sedation and the induction of endotracheal anesthesia. Propofol is especially recommended for use with sighthounds.
- Refractory Status Epilepticus: Propofol can also be employed in managing refractory status epilepticus—a life-threatening condition characterized by prolonged seizures that do not respond to conventional antiepileptic treatments.
How is propofol produced?
Bachem is a leading propofol manufacturer. We produce the propofol API at our GMP production site in Vionnaz, Switzerland (the former Sochinaz). Propofol or chemically 2,6-diisopropylphenol is synthesized by coupling phenol with acetone using a strong base as catalyst. The reaction is done environment friendly without solvents. The purification is done by distillation using 100% green energy.
The synthesis and purification processes are subject to stringent quality and regulatory standards due to the compound’s medical application.
Who manufactures propofol?
Bachem’s Vionnaz site began developing a manufacturing process for the active ingredient in 1992. A drug master file was submitted to the FDA in September 1994 and actual production began in 2000.
Innovation is a central pillar of Bachem’s success, and we focus on continuous development of more efficient and sustainable production methods for propofol. This includes exploring new catalytic processes and innovative synthetic strategies that reduce waste generation and environmental impact. This enables us to provide customers with a high quality propofol API, with minimized lead time and at the right cost. We have also steadily expanded capacity and our current propofol production capacity serves over 200 million patients per year worldwide.
The supply of propofol, an essential drug on the WHO list, needs to be guaranteed. To strengthen the supply chain, we purchase all starting materials from multiple sources and keep stocks of starting materials and the finished product.
Bachem Regulatory Documentation
2,6-Diisopropylphenol; ICI 35868
Relative Molecular Mass
25 ± 5°C
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