Further investigation of the rapid-onset and short-duration action of the G protein-biased μ-ligand oliceridine

2021 ◽  
Vol 534 ◽  
pp. 988-994
Author(s):  
Tomohisa Mori ◽  
Yoshinori Takemura ◽  
Takamichi Arima ◽  
Yoshiyuki Iwase ◽  
Michiko Narita ◽  
...  
Keyword(s):  
Peptides ◽  
1992 ◽  
pp. 88-90 ◽  
Author(s):  
H. B. Long ◽  
J. C. Baker ◽  
R. M. Belagaje ◽  
R. D. DiMarchi ◽  
B. H. Frank ◽  
...  

1997 ◽  
Vol 84 (5) ◽  
pp. 1011-1018 ◽  
Author(s):  
Raymond Kahwaji ◽  
David R. Bevan ◽  
George Bikhazi ◽  
Colin A. Shanks ◽  
Robert J. Fragen ◽  
...  

Cephalalgia ◽  
1981 ◽  
Vol 1 (4) ◽  
pp. 209-216 ◽  
Author(s):  
David Russell

A detailed clinical study of 77 spontaneous cluster headache attacks has been carried out. The information was recorded during a period when patients were without medication and with the use of methods which were not dependent on the patients' memory of events. The findings stress the usual rapid onset and termination of attacks, and their short duration. There was a preponderance of attacks beginning during sleep and the majority of daytime attacks began when patients were physically relaxed. No significant difference between nocturnal and daytime attacks was found as regards severity or temporal profiles. A significant positive correlation was found between severity of maximal pain and both duration of maximal pain and total duration of attacks. “Abortive attacks” accounted for 16% of attacks. The apparent spontaneous arrest of these attacks does not appear to be due to special features of patient activity prior to or during attacks, nor are they restricted to a refractory period following more severe attacks.


CNS Spectrums ◽  
2013 ◽  
Vol 18 (5) ◽  
pp. 225-227 ◽  
Author(s):  
Stephen M. Stahl

ISSUE:Reports of rapid-onset but short-duration antidepressant effects in patients with treatment-resistant mood disorders after intravenous administration of ketamine have prompted efforts to find an agent with ketamine's properties that can be administered orally in repeated doses in order to sustain that action. One candidate for this is dextromethorphan, and here the pharmacologic mechanism of action is compared and contrasted with that of ketamine.


1980 ◽  
Vol 8 (2) ◽  
pp. 206-210 ◽  
Author(s):  
Albert Saady ◽  
R. G. Hicks

The EEG was continuously recorded on 43 patients who received Althesin. A basic pattern for this drug, typical of most general anaesthetic agents at a level of light surgical anaesthesia, was established. Four significant levels of change could be discriminated in the EEG following administration of incremental boluses of undiluted Althesin, reflecting deeper levels of anaesthesia. These ranged from a mild slowing of the dominant rhythms to burst-suppression activity at the deepest level reached with larger doses. The EEG demonstrated that althesin has a rapid onset and a short duration and that recovery is rapid and complete after continuous infusion.


1999 ◽  
Vol 91 (5) ◽  
pp. 1311-1311 ◽  
Author(s):  
Neal W. Fleming ◽  
Frances Chung ◽  
Peter S. A. Glass ◽  
John B. Kitts ◽  
Hans Kirkegaard-Nielsen ◽  
...  

Background Currently, the only approved muscle relaxant with a rapid onset and short duration of action is succinylcholine, a drug with some undesirable effects. Rapacuronium is an investigational nondepolarizing relaxant that also has a rapid onset and short duration and consequently should be compared with succinylcholine in its ability to facilitate rapid tracheal intubation. Methods This prospective, randomized clinical trial involved 336 patients. Anesthesia was induced with fentanyl and propofol and either 1.5 mg/kg rapacuronium or 1.0 mg/kg succinylcholine. The goal was to accomplish tracheal intubation by 60 s after administration of the neuromuscular blocking drug. Endotracheal intubation was performed, and conditions were graded by a blinded investigator. Recovery of neuromuscular function was assessed by electromyography. Results Intubation conditions were evaluated in 236 patients. Intubation by 60 s after drug administration occurred in 100% of patients with rapacuronium and in 98% with succinylcholine. Intubation conditions were excellent or good in 87% of patients with rapacuronium and in 95% with succinylcholine (P < 0.05). The time (median and range) to the first recovery of the train-of-four response was 8.0 (2.8-20.0) min with rapacuronium and 5.7 (1.8-17.7) min with succinylcholine (P < 0.05). The overall incidence of adverse effects was similar with both drugs. Conclusions A 1.5-mg/kg dose of rapacuronium effectively facilitates rapid tracheal intubation. It can be considered a valid alternative to 1.0 mg/kg succinylcholine for this purpose.


1998 ◽  
Vol 42 (2) ◽  
pp. 77???78
Author(s):  
RAYMOND KAHWAJI ◽  
DAVID R. BEVAN ◽  
GEORGE BIKHAZI ◽  
COLIN A. SHANKS ◽  
ROBERT J. FRAGEN ◽  
...  

2022 ◽  
Vol 9 (3) ◽  
pp. 3-7
Author(s):  
Uma Advani ◽  
Ravi Prakash ◽  
Parmanand Swami ◽  
Neha Sharma ◽  
Charu Jain ◽  
...  

Abstract Objective: To review the literature on equianalgesic efficacy and better safety(less respiratory depression and gastrointestinal dysfunction) of oliceridine versus opioid analgesic in moderate to severe postoperative pain. Methodology: A comprehensive literature search was conducted in PubMed (January 2021 to March 2021) using keywords as ‘oliceridine’, ‘ligand biased mu receptor agonist’, ‘acute postoperative pain’, ‘conventional opioids’ and ‘morphine’. All English language full text pre-clinical and clinical research articles were searched. In addition, other data source was from ClinicalTrial. Gov. Data Synthesis: Oliceridine is a novel selective µ (mu)-receptor G-protein pathway modulator. G protein biased mu receptor agonists are a new class of opioids exhibiting analgesic properties at par to morphine with less respiratory depressant properties. Oliceridine a first-in-class intravenous (IV) analgesic has received the US FDA approval in August 2020, for management of moderate to severe acute pain in adults. The drug can be administered in cases where the pain is severe enough to require an intravenous opioid and when alternative treatments become inadequate. Oliceridine is an opioid agonist with a rapid onset of action within two to five minutes, was administered via clinician-administered bolus dosing, patient-controlled analgesia (PCA), or a combination of the two. Bolus dosing was initiated at 1 to 2 mg, with supplemental doses of 1 to 3 mg every one to three hours, as needed, based on individual patient need and previous response to oliceridine in management of acute post-operative pain. If oliceridine was administered via PCA, the loading dose was 1.5 mg, the demand dose was 0.5 mg, and the lockout interval (repeat dose)was six minutes. The clinically relevant concentration range of 0 to 35 ng/ml. It is indicated for short-term use only & limited to hospitals or other controlled clinical settings. Oliceridine requires no dosage adjustments in patients with renal impairment as well as in patient with significant medical complications. Therefore, opioids that bias towards G-protein and away from β arrestin signaling should produce analgesia with reduced side effects.


1986 ◽  
Vol 24 (13) ◽  
pp. 51-52

Alfentanil (Rapifen - Janssen) is an intravenous opioid analgesic with a rapid onset and short duration of action. It is recommended for use as a bolus injection during short general anaesthesia or by infusion during longer procedures.1,2


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