Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia?

Lu, Ming; Liu, Jian; Wu, Xiaolian; Zhang, Zhiqing

doi:10.1155/2023/7443226

Cited by 46 publications

(50 citation statements)

References 45 publications

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“…Ciprofol is a short-acting intravenous sedative based on the structural modi cation of propofol, whose main mechanism is to activate the postsynaptic GABA-A-Clchannel complex, which causes hyperpolarization of nerve cell membrane through chloride ion in ux, thus causing central nervous system inhibition [15][16][17]. The high selective binding ability of ciprofol to its receptor enables it to achieve the same sedative and anesthetic effects as propofol at a lower dose [18][19][20][21].…”

Section: Discussionmentioning

confidence: 99%

ED50 of Ciprofol Combined with Sufentanil for Fiber Bronchoscopy of Different Patient Populations with Pulmonary Tuberculosis

Pan

Liu

Zhang

et al. 2023

Preprint

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Backgroud: Ciprofol is a promising sedative. At present, there were few clinical studies on the median effective dose (ED50) of ciprofol. The aim of this study was to compare the ED50 of ciprofol for fiberoptic bronchoscopy in pulmonary tuberculosis (TB) patients of different genders and ages. Methods：TB patients who underwent bronchoscopy examination and treatment at The Third People’s Hospital of Changzhou between May 2023 and June 2023 were selected, and divided into four groups according to stratified random method: Group N1 (non-elderly male patients), Group N2 (non-elderly female patients), Group N3 (elderly male patients), and Group N4 (elderly female patients). All patients received intravenous injection of 0.15 μg/kg sufentanil followed by injection of the test dose of ciprofol according to Dixon’s modified sequential method. Fiberoptic bronchoscopy was performed after the disappearance of the eyelash reflex. The initial dose of ciprofol in all four groups of TB patients was 0.4 mg/kg, and the ratio of adjacent doses was 1:1.1. The next patient received a 10% increase in the dose of ciprofol if the patient in the same group experienced positive reactions such as choking cough, frowning, and body movements during the endoscopy process. Otherwise, it was judged as a negative reaction, and the next patient received a 10% decrease in the dose of ciprofol. The transition from a positive reaction to a negative reaction was defined as a turning point, and the study of the group was terminated when seven turning points occurred. Hemodynamic parameters, oxygen saturation and adverse reactions were recorded at different time points in all groups. The Probit regression analysis method was used to calculate the ED50 of ciprofol in the four groups and compare between the groups. Results: The ED50 of ciprofol combined with 0.15 μg/kg sufentanil for bronchoscopy in the four groups were 0.465 mg/kg, 0.433 mg/kg, 0.420 mg/kg and 0.396 mg/kg, respectively. The ED50 of ciprofol in the Group N1 was significantly higher compared with the Group N2 and Group N3 (p<0.05). The ED50 of ciprofol in the Group N4 was significantly lower compared with the Group N2 and Group N3 (p<0.05). Conclusions: The ED50 of ciprofol used for fiber bronchoscopy in patients with TB of different genders and ages was different. Trial registration: The Chinese Clinical Trial Registry, ChiCTR2300071508, Registered on 17 May 2023.

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Section: Discussionmentioning

confidence: 99%

ED50 of Ciprofol Combined with Sufentanil for Fiber Bronchoscopy of Different Patient Populations with Pulmonary Tuberculosis

Pan

Liu

Zhang

et al. 2023

Preprint

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“…Ciprofol is a rapid‐onset anesthetic that takes effect in a dose‐dependent manner, and its efficacy is about four to five times that of propofol 12 . The anesthetic effect falls between that of ciprofol and that of propofol 7 . In the induction of general anesthesia for patients undergoing elective surgery, ciprofol has shown the advantages of rapid onset, minimal response to tracheal intubation, and stable vital signs 11,23 .…”

Section: Discussionmentioning

confidence: 99%

“…[13][14][15] Ciprofol is extensively metabolized after administration; this primarily occurs in the liver through phase I cytochrome P450 (CYP) 2B6 and phase II glucuronosyltransferase 1A9 (UGT1A9). 7,16 A mass balance and biotransformation study showed that the major metabolites in plasma were glucuronic acid-M4 (~79.3% of the total plasma radiation exposure) and that those in urine were M4 and M5-1 (accounting for 51.6% and 19.3% of the dose, respectively) after a single intravenous dose of 0.4 mg/0.8 μCi/kg [ 14 C] ciprofol. 17 By contrast, unchanged ciprofol accounted for only 3.97% of the total radiation exposure and was not detected in urine, which further demonstrated that the major metabolite was M4 and was mainly excreted via the kidneys (84.59%).…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, ciprofol is a promising intravenous anesthetic candidate. Ciprofol has been approved by the China National Medical Products Administration (NMPA) for various indications, including sedation during gastrointestinal endoscopy and general anesthesia 7 . Clinical studies of ciprofol have been conducted in various procedures and settings, including gastroscopy and colonoscopy, 8 fiberoptic bronchoscopy, 9,10 general anesthesia for elective surgery, 11 and mechanical ventilation in the intensive care unit 12 .…”

Section: Introductionmentioning

confidence: 99%

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Drug–drug interaction study of ciprofol and sodium divalproex: Pharmacokinetics, pharmacodynamics, and safety in healthy Chinese subjects

Yang

Zhang

Ruan

et al. 2023

Clinical Translational Sci

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Ciprofol (also known as HSK3486) is a promising intravenous anesthetic candidate derived from propofol and independently developed by Haisco Pharmaceutical Group Co., Ltd. (Chengdu, China). Compared with propofol, ciprofol has the potential to reduce the dose required and the associated risks. Ciprofol is extensively metabolized in vivo, and its interaction with other concurrently administered drugs during clinical application is worthy of attention. Therefore, an open‐label, two‐stage sequential study was performed in healthy subjects who received either a single administration of ciprofol injection or ciprofol injection after oral administration of sodium divalproex. The aim of the study was to evaluate the effects of sodium divalproex on ciprofol with respect to pharmacokinetics, pharmacodynamics, and safety, thus providing a basis for the rational clinical use of ciprofol and sodium divalproex.

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“…Ciprofol exhibits wide tissue distribution, and it has been reported that approximately 95% of the drug is bound to plasma proteins [7]. It is primarily metabolized in the liver by phase II glucuronosyltransferases (UGTs), with UGT1A9 being the main enzyme responsible for the conversion of ciprofol to its major metabolite, M4.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics, Pharmacodynamics, and Safety of Ciprofol Injectable in Chinese Subjects with Normal or Impaired Renal Function

Tao

Liu

Zhao

et al. 2023

Preprint

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Purpose The study was designed to evaluate the pharmacokinetics (PK), pharmacodynamics (PD) and safety of ciprofol injection in healthy subjects and patients with mild and moderate renal impairment, to provide a reference for the dosage adjustment in these populations. Methods A total of 24 subjects were enrolled in this study. An initial loading dose of ciprofol was 0.4 mg/kg for 1 min, followed by maintenance infusion at a rate of 0.4 mg/kg/h for 30 min were administered to subjects. To evaluate the PK of ciprofol and its metabolite M4, plasma and urine samples were collected. PD was evaluated using a modified observer’s alertness/sedation scale (MOAA/S) in combination with bispectral index (BIS) monitoring. Safety assessments were conducted throughout the trial process. Results The area under the curve (AUC) and maximum concentration (Cmax) of ciprofol in plasma for patients with renal impairment were only slightly higher (0.9- to 1.2-fold) than those subjects in with normal renal function. For the metabolite M4, AUC values were 1.3- and 2.1-fold greater in patients with mild and moderate renal impairment, respectively, than healthy controls. However, increased exposure to M4 in participants with renal impairment may not be clinically significant, as this metabolite is pharmacologically inactive. There was no obvious effect of renal impairment on the PD parameters. The study found that ciprofol injection was well-tolerated, with all AEs reported being mild or moderate in severity. Conclusion No dosage adjustment of ciprofol is necessary for patients with mild-to-moderate renal impairment who receive the injection. Clinical trial registration: NCT04142970(October, 2019).

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Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia?

Cited by 46 publications

References 45 publications

ED50 of Ciprofol Combined with Sufentanil for Fiber Bronchoscopy of Different Patient Populations with Pulmonary Tuberculosis

ED50 of Ciprofol Combined with Sufentanil for Fiber Bronchoscopy of Different Patient Populations with Pulmonary Tuberculosis

Drug–drug interaction study of ciprofol and sodium divalproex: Pharmacokinetics, pharmacodynamics, and safety in healthy Chinese subjects

Pharmacokinetics, Pharmacodynamics, and Safety of Ciprofol Injectable in Chinese Subjects with Normal or Impaired Renal Function

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