Propofol is an intravenous anesthetic commonly used to induce general anesthesia before surgery and to induce conscious sedation when given in lower doses. It is a popular medication due to its short onset of action, duration of action, and recovery time following treatment.1 Propofol, however, suffers from certain disadvantages, such as causing pain on injection. Approximately 70% of patients who receive a propofol injection, without first receiving a pretreatment, report pain following injection, a significantly higher rate than the percentage of patients who report pain following injection of other phenol-containing anesthetic agents. Researchers are now investigating a new and similar anesthetic called ciprofol as a potential replacement.
Ciprofol is structurally similar to propofol but does not cause as much pain on injection. Like propofol, ciprofol induces anesthesia by interacting with gamma-aminobutyric acid (GABA) receptors, yet it is more potent and faster acting than propofol.3 Recent evidence suggests that ciprofol exhibits lower rates of injection site pain, though it may cause adverse effects in the respiratory and cardiovascular systems, which propofol has also been known to cause.4
Because ciprofol is a new medication, there does not yet exist a vast body of literature attesting to its efficacy and safety. Still, the few studies that have been published on the topic are encouraging. Teng et al. evaluated the efficacy and safety of ciprofol in patients undergoing a colonoscopy.5 Patients were divided into different ciprofol dosage groups, and several control groups received propofol in different doses for comparison. The researchers found that 0.5 mg/kg dose of ciprofol provided adequate sedation and anesthesia, while adverse events (not precisely defined but likely involving any significant change to blood pressure, heart rate, and blood oxygen saturation) were associated with higher doses. At the same dosage, patients given propofol experienced more adverse events than those given ciprofol. Significantly, the authors found that only 6.8% of patients receiving ciprofol at any dose experienced injection pain, while 55% of propofol patients reported pain. Teng et al. also reported other benefits and disadvantages of ciprofol compared to propofol in their study. Overall, data found ciprofol to be safe and effective.
Chen et al. performed a similar study, except that the patients in their study underwent elective gynecological surgery.6 This study also compared the efficacy and safety of the new anesthetic ciprofol against that of propofol. The two agents were found to induce similar levels of sedation, while propofol was associated with more adverse events. The authors speculate that only propofol causes pain on injection because the aqueous formulation of propofol contains a higher concentration of the anesthetic agent than the ciprofol formulation.
An adjuvant is a medication co-administered with an anesthetic agent to improve the speed or duration of the anesthesia, or to reduce the adverse effects associated with the anesthesia. A team of Chinese and American researchers are interested in the effects of esketamine, the enantiomer, or mirror image, of ketamine, when co-administered with propofol and ciprofol.7 Though they have not yet conducted the study, they published a detailed protocol that can be followed pending approval. Though ciprofol is making waves in the anesthesiology community, it has not yet been approved by the Food and Drug Administration or the European Medicines Agency. The studies mentioned in this article may help ciprofol win regulatory approval.
References
1. McWilliams, K., Keeley, P. W. & Waterhouse, E. T. Propofol for Terminal Sedation in Palliative Care: A Systematic Review. J. Palliat. Med. 13, 73–76 (2010), DOI: 10.1089/jpm.2009.0126
2. Kang, H.-J. et al. Clinical factors affecting the pain on injection of propofol. Korean J. Anesthesiol. 58, 239–243 (2010), DOI: 10.4097/kjae.2010.58.3.239
3. Qin, L. et al. Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics. J. Med. Chem. 60, 3606–3617 (2017), DOI:10.1021/acs.jmedchem.7b00254
4. Li, X. et al. Safety, Pharmacokinetics, and Pharmacodynamics of a Single Bolus of the γ-aminobutyric Acid (GABA) Receptor Potentiator HSK3486 in Healthy Chinese Elderly and Non-elderly. Front. Pharmacol. 12, (2021), DOI: 10.3389/fphar.2021.735700
5. Teng, Y. et al. Efficacy and safety of ciprofol for the sedation/anesthesia in patients undergoing colonoscopy: Phase IIa and IIb multi-center clinical trials. Eur. J. Pharm. Sci. Off. J. Eur. Fed. Pharm. Sci. 164, 105904 (2021), DOI:10.1016/j.ejps.2021.105904
6. Chen, B. et al. The efficacy and safety of ciprofol use for the induction of general anesthesia in patients undergoing gynecological surgery: a prospective randomized controlled study. BMC Anesthesiol. 22, 245 (2022), DOI:10.1186/s12871-022-01782-7
7. Long, Y. et al. Esketamine as an Adjuvant to Ciprofol or Propofol Sedation for Same-Day Bidirectional Endoscopy: Protocol for a Randomized, Double-Blind, Controlled Trial With Factorial Design. Front. Pharmacol. 13, (2022), DOI:10.3389/fphar.2022.821691
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