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Proceedings of the National Academy of... Feb 2021Propofol is a widely used general anesthetic to induce and maintain anesthesia, and its effects are thought to occur through impact on the ligand-gated channels...
Propofol is a widely used general anesthetic to induce and maintain anesthesia, and its effects are thought to occur through impact on the ligand-gated channels including the GABA receptor. Propofol also interacts with a large number of proteins including molecular motors and inhibits kinesin processivity, resulting in significant decrease in the run length for conventional kinesin-1 and kinesin-2. However, the molecular mechanism by which propofol achieves this outcome is not known. The structural transition in the kinesin neck-linker region is crucial for its processivity. In this study, we analyzed the effect of propofol and its fluorine derivative (fropofol) on the transition in the neck-linker region of kinesin. Propofol binds at two crucial surfaces in the leading head: one at the microtubule-binding interface and the other in the neck-linker region. We observed in both the cases the order-disorder transition of the neck-linker was disrupted and kinesin lost its signal for forward movement. In contrast, there was not an effect on the neck-linker transition with propofol binding at the trailing head. Free-energy calculations show that propofol at the microtubule-binding surface significantly reduces the microtubule-binding affinity of the kinesin head. While propofol makes pi-pi stacking and H-bond interactions with the propofol binding cavity, fropofol is unable to make a suitable interaction at this binding surface. Therefore, the binding affinity of fropofol is much lower compared to propofol. Hence, this study provides a mechanism by which propofol disrupts kinesin processivity and identifies transitions in the ATPase stepping cycle likely affected.
Topics: Binding Sites; Kinesins; Mutation; Propofol; Protein Domains
PubMed: 33495322
DOI: 10.1073/pnas.2023659118 -
The Korean Journal of Gastroenterology... Jan 2017Propofol (2,6-diisopropylphenol) is a hypnotic drug with a very rapid onset and offset of action. It has increasingly been used in gastrointestinal endoscopy.... (Review)
Review
Propofol (2,6-diisopropylphenol) is a hypnotic drug with a very rapid onset and offset of action. It has increasingly been used in gastrointestinal endoscopy. Administration of propofol by nurses or endoscopists is commonly referred to as non-anesthesiologist-administered propofol (NAAP). There have been a lot of studies on the safety of NAAP compared with those by anesthesiologists. Safety results of those studies are summarized in this review.
Topics: Anesthesiologists; Endoscopy, Gastrointestinal; Humans; Hypnotics and Sedatives; Propofol
PubMed: 28135791
DOI: 10.4166/kjg.2017.69.1.55 -
Biophysical Model: A Promising Method in the Study of the Mechanism of Propofol: A Narrative Review.Computational Intelligence and... 2022The physiological and neuroregulatory mechanism of propofol is largely based on very limited knowledge. It is one of the important puzzling issues in anesthesiology and... (Review)
Review
The physiological and neuroregulatory mechanism of propofol is largely based on very limited knowledge. It is one of the important puzzling issues in anesthesiology and is of great value in both scientific and clinical fields. It is acknowledged that neural networks which are comprised of a number of neural circuits might be involved in the anesthetic mechanism. However, the mechanism of this hypothesis needs to be further elucidated. With the progress of artificial intelligence, it is more likely to solve this problem through using artificial neural networks to perform temporal waveform data analysis and to construct biophysical computational models. This review focuses on current knowledge regarding the anesthetic mechanism of propofol, an intravenous general anesthetic, by constructing biophysical computational models.
Topics: Anesthetics; Artificial Intelligence; Neural Networks, Computer; Propofol
PubMed: 35619772
DOI: 10.1155/2022/8202869 -
Pediatric Emergency Care Feb 2005
Comparative Study Review
Topics: Child; Conscious Sedation; Humans; Hypnotics and Sedatives; Propofol
PubMed: 15699822
DOI: 10.1097/01.pec.0000159057.57306.0e -
Journal of the American Veterinary... Jun 1994
Review
Topics: Anesthesia; Animals; Cardiovascular System; Central Nervous System; Humans; Propofol; Urogenital System
PubMed: 8077130
DOI: No ID Found -
American Journal of Health-system... Mar 2023The activated partial thromboplastin time (aPTT) is a coagulation assay commonly utilized for monitoring therapeutic heparin anticoagulation. aPTT methods based on... (Observational Study)
Observational Study
PURPOSE
The activated partial thromboplastin time (aPTT) is a coagulation assay commonly utilized for monitoring therapeutic heparin anticoagulation. aPTT methods based on optical detection are vulnerable to spectral interference from hemolysis, icterus, lipemia, and other substances. Intravenous lipid emulsions of primarily 20% have been shown to interfere with multiple clinical laboratory assays, including those measuring aPTT by optical methods, but there is limited data on propofol's effect. The primary objective of this study was to determine the rate of interference of propofol with aPTT measurements in patients receiving both propofol and intravenous heparin.
METHODS
A retrospective observational cohort study of intensive care unit patients who received concomitant propofol and heparin infusions (N = 38 patients) and whose heparin therapy was monitored by aPTT (N = 531 aPTTs) was conducted. Review of the electronic medical record was completed to obtain relevant clinical and laboratory data, while the laboratory information system was queried for analytical interference with the aPTT assay.
RESULTS
A total of 109 aPTTs (21%) spanning 21 patients (55%) had documented aPTT interference. All 21 patients had at least one aPTT requiring ultracentrifugation prior to reporting, and 12 aPTTs from 4 patients were unreportable due to interference. Patients with and without aPTT interference received similar doses of propofol. None of the cases of aPTT interference were caused by hemolysis or hyperbilirubinemia.
CONCLUSION
A potential medication-assay interaction was observed in approximately half of patients who received concomitant propofol and heparin infusions and had aPTT measured for anticoagulation management. Sample ultracentrifugation removes the optical interference in most cases but significantly prolongs aPTT reporting and delays appropriate adjustments to heparin dosing.
Topics: Humans; Heparin; Partial Thromboplastin Time; Propofol; Retrospective Studies; Hemolysis; Anticoagulants
PubMed: 36370416
DOI: 10.1093/ajhp/zxac337 -
Critical Reviews in Analytical Chemistry 2022Propofol (PFL) owing to its excellent inhibitory property of neurotransmitters in CNS by positive modulation of ligand gated ion channels to an integrated chloride... (Review)
Review
Propofol (PFL) owing to its excellent inhibitory property of neurotransmitters in CNS by positive modulation of ligand gated ion channels to an integrated chloride channeled GABA thereby acts as a general anesthetic. It differs from other general anesthetics chemically and pharmacologically as it has lesser side effects compared to other general anesthetics and is most commonly used. The present review focuses on two aspects (a) various analytical methods used in quantification of Propofol in pharmaceutical formulations and (b) various analytical methods used to determine Propofol in biological matrices and some biological markers like hair and end tidal nasal air for forensic purpose to estimate drug concentration in suspected cases. Here the various analytical methods are developed using different parameters and validation of employed methods are discussed. Estimated parameters like the linearity, LOQ (Limit of quantification), % recovery, slope, intercept, validation are discussed for the individual method. The critical quality attributes like the wavelength of detection, columns, flow rate, gas flow, and the sample preparation methods for the determination of PFL by bioanalytical methods are also discussed. Type of electrode, mechanism involved and the potential voltage applied for a particular electrochemical method are also discussed.
Topics: Anesthetics, General; Biomarkers; Chlorides; Drug Compounding; Hair; Ligand-Gated Ion Channels; Propofol; gamma-Aminobutyric Acid
PubMed: 33870775
DOI: 10.1080/10408347.2021.1910927 -
Der Anaesthesist Nov 1998Propofol is known to possess direct antiemetic effects. Its use for induction and maintenance of anaesthesia has been shown to be associated with a lower incidence of... (Review)
Review
Propofol is known to possess direct antiemetic effects. Its use for induction and maintenance of anaesthesia has been shown to be associated with a lower incidence of postoperative nausea and vomiting (PONV) when compared to any other anaesthetic drug or technique. However, its mechanism of action in this context is still not well understood. In this article, the best ways to take advantage of propofol's antiemetic properties are emphasized. The possible effects of propofol on the cerebral cortex, its interactions with the dopaminergic and the serotoninergic systems are evaluated by the known clinical and basic science results. Finally, the advantages and disadvantages of using propofol to decrease the incidence of PONV in clinical practice are discussed.
Topics: Anesthesia; Anesthetics, Intravenous; Antiemetics; Humans; Postoperative Nausea and Vomiting; Propofol
PubMed: 9870087
DOI: 10.1007/s001010050643 -
Critical Care Nurse Dec 2021Propofol is a drug of diversion because of its high-volume use, lack of prescribed control mechanisms, and accessibility. As a result, intensive care unit nurses and...
BACKGROUND
Propofol is a drug of diversion because of its high-volume use, lack of prescribed control mechanisms, and accessibility. As a result, intensive care unit nurses and other health care professionals are placed at unnecessary risk. Decreasing the risk of drug diversion can save lives, licenses, and livelihoods.
LOCAL PROBLEM
Objectives were to reduce the risk of drug diversion and diminish the environmental impact of medication discarded down the sink. Disposing of residual propofol into activated carbon pouches was successful and sustainable in operating rooms at the study institution. Literature findings supported this intervention because of propofol's potential for abuse, ongoing diversion events, ease of access, poor control mechanisms, lack of standardization, excessive waste, and ecological impact.
METHODS
The intensive care unit with the highest propofol use was selected to replicate the propofol disposal process used in the operating rooms. Activated carbon pouches and bottle cap removal tools were located in each intensive care unit room at the nurses' workstation for ease of use. Audits of unsecured waste bins and staff surveys of institutional policy awareness, disposal processes, barriers, and concerns were completed before and after the intervention.
RESULTS
Survey results determined significant concern for drug diversion risk. The pilot project displayed success: 44.1% of propofol bottles in waste bins were full before the intervention and 0% were full afterward.
CONCLUSION
Following institutional approval, this propofol disposal process was replicated in all intensive care units and the emergency department in the study institution.
Topics: Emergency Service, Hospital; Humans; Intensive Care Units; Pharmaceutical Preparations; Pilot Projects; Propofol
PubMed: 34851389
DOI: 10.4037/ccn2021123 -
The British Journal of Psychiatry : the... Dec 1992
Topics: Electroconvulsive Therapy; Humans; Propofol; Retrospective Studies; Seizures; Time Factors
PubMed: 1307869
DOI: 10.1192/bjp.161.6.861a