- Ciprofol - Wikipedia
- Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous ...
- CIPROFOL VS PROPOFOL - The anesthesia consultant
- Ciprofol: A Novel Medication from Development towards
- Ciprofol as compared to propofol for sedation and general …
- Efficacy and safety of ciprofol for the sedation/anesthesia in …
- Ciprofol- a game changing intravenous anesthetic or another ...
- Pharmacological Insights and Clinical Applications of Ciprofol: A ...
- Pharmacokinetic and pharmacodynamic properties of ciprofol …
- Ciprofol: A Comprehensive Review of Its Pharmacological …
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Ciprofol (also known as cipepofol, or HSK3486) is a novel 2,6-disubstituted phenol derivative that is used for the intravenous induction of general anesthesia. A short-acting and highly selective γ-aminobutyric acid agonist, ciprofol is 4–6 times more potent than other phenol derivatives such as propofol or fospropofol.
As of 2023, it is still an investigational drug. Manufactured by Haisco Pharmaceutical Group of Chengdu, Sichuan, China, ciprofol has undergone phase I and II trials in Australia and China. In these early studies, ciprofol appears to be comparable in efficacy to propofol and is associated with fewer adverse events.
Physical properties
Ciprofol is an optically active 2,6-disubstituted alkylphenol with a cyclopropylethyl group incorporated at the second carbon atom. This cyclopropyl group increases the steric effects and introduces stereoselective effects over its anesthetic properties. These properties appear to increase the anesthetic potency of ciprofol, when compared with propofol.
Medical use
Ciprofol is used for the intravenous induction of general anesthesia. As of 2023, it is still an investigational drug. Thus far, it has been found to be efficacious as a general anesthetic in patients undergoing gynecological surgery and kidney transplantation, as well as for endoscopic procedures such as bronchoscopy, esophagogastroduodenoscopy and colonoscopy.
Ciprofol has also been used for sedation of critically ill patients undergoing mechanical ventilation in the intensive care unit, as well as for the treatment of agitation and delirium in that patient population. When combined with mild therapeutic hypothermia, ciprofol may also be useful as a cerebral protective agent in the setting of cerebral ischemia-reperfusion injury.
Experimental use
In experimental models of isoproterenol-induced myocardial infarction (using mice as subjects), ciprofol appears to protect the heart against oxidative damage, inflammation and apoptosis of cardiac muscle cells.
Side effects
When compared with propofol, side effects such as pain on injection and respiratory depression appear to be less common with ciprofol.
Pharmacology
= Pharmacokinetics
=Compared to propofol, ciprofol exhibits stronger binding to the GABAA receptor and elicits a greater enhancement of GABAA receptor-mediated neurotransmission.
It is not necessary to adjust the dose in people with mild or moderate renal impairment, or in those with mild or moderate hepatic impairment. In elderly people, a slightly lower dose (0.3 mg/kg) appears to be similar in efficacy to the higher doses administered to younger people but is associated with fewer adverse effects.
= Pharmacodynamics
=Ciprofol exhibits pharmacodynamic properties similar to those of propofol, including both rapid onset and rapid offset. Ciprofol appears to have similar effects upon the respiratory and cardiovascular systems as those propofol. At doses of 0.4 mg/kg to 0.5 mg/kg, ciprofol induces equivalent sedation/anesthesia and has an incidence of adverse events similar to that of propofol 2.0 mg/kg.
Biodegradation and toxicity
Ciprofol is characterized by a rapid onset of action, and predictable absorption, distribution, metabolism, excretion processes. The compound undergoes glucuronidation in the liver, followed by excretion by the kidneys.
References
Further reading
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Ciprofol - Wikipedia
Ciprofol is an optically active 2,6-disubstituted alkylphenol with a cyclopropylethyl group incorporated at the second carbon atom. This cyclopropyl group increases the steric effects and introduces stereoselective effects over its anesthetic properties.
Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous ...
Ciprofol is a short-acting intravenous sedative based on the structural modification of propofol. Ciprofol has high efficacy, good selectivity, and fewer adverse reactions, indicating good clinical application potential.
CIPROFOL VS PROPOFOL - The anesthesia consultant
Dec 31, 2022 · Propofol is used for surgical anesthesia, procedural sedation, and intensive care unit (ICU) sedation. Propofol was FDA-approved in the United States in 1986 and is now off patent. Generic propofol is inexpensive, averaging about $2.27 for a 20 ml vial.
Ciprofol: A Novel Medication from Development towards
Nov 1, 2021 · Ciprofol is a new medication for inducing anesthesia or sedation. According to the results of several clinical trials, ciprofol has a rapid onset, fast and complete functional recovery, and shares similar sedative effects and clinical characteristics with propofol.
Ciprofol as compared to propofol for sedation and general …
Apr 8, 2024 · Ciprofol for sedation or GA may be safer than propofol, though its pharmacokinetics may be less advantageous. Propofol is the most commonly used hypnotic agent used during sedation and general anesthesia (GA) practice, offering faster recovery compared to benzodiazepines.
Efficacy and safety of ciprofol for the sedation/anesthesia in …
Sep 1, 2021 · Ciprofol was safe and well tolerated at doses ranging from 0.1 mg/kg to 0.5 mg/kg. Ciprofol 0.4-0.5 mg/kg induced equivalent sedation/anesthesia and had a similar safety profile to propofol 2.0 mg/kg during colonoscopy without producing serious AEs.
Ciprofol- a game changing intravenous anesthetic or another ...
Ciprofol (working name- HSK3486) is a γ-aminobutyric acid (GABA) receptor agonist and is a novel 2,6-disubstituted phenol derivative like propofol. It is a recently introduced intravenous anesthetic agent which has undergone phase I and II trials in Australia and China.
Pharmacological Insights and Clinical Applications of Ciprofol: A ...
Aug 28, 2024 · Ciprofol (HSK3486) is a novel intravenous anaesthetic developed as an alternative to propofol, offering a safer and more effective option in anaesthesia. It works primarily by modulating the gamma-aminobutyric acid (GABA) receptors in the central nervous system, leading to sedation and hypnosis.
Pharmacokinetic and pharmacodynamic properties of ciprofol …
Ciprofol (HSK3486) is a newly developed structural analog of propofol and a short-acting intravenous drug for induction and maintenance anesthesia in adults. Its application includes anesthesia/sedation during invasive endoscopy and for adult intensive care unit (ICU) patients.
Ciprofol: A Comprehensive Review of Its Pharmacological …
he development of ciprofol (HSK3486), a novel intravenous anesthetic agent designed to retain propofol’s efficacy while improving its safety profile. Objectives. This review evaluates the pharmacological profile, clinical effi.