Oliceridine as a Novel Selec ve mu-receptor G-protein Pathway Modulator: A Narra ve review

Objec ve: To review the literature on equianalgesic efficacy and be er safety(less respiratory depression and gastrointes nal dysfunc on) of oliceridine versus opioid analgesic in moderate to severe postopera ve 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 postopera ve pain’, ‘conven onal opioids’ and ‘morphine’. All English language full text pre-clinical and clinical research ar cles were searched. In addi on, other data source was from ClinicalTrial. Gov. Data Synthesis: Oliceridine is a novel selec ve μ (mu)receptor G-protein pathway modulator. G protein biased mu receptor agonists are a new class of opioids exhibiting analgesic proper es at par to morphine with less respiratory depressant proper es. 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 alterna ve treatments become inadequate. Oliceridine is an opioid agonist with a rapid onset of ac on within two to fiveminutes, was administered via clinician-administered bolus dosing, pa ent-controlled analgesia (PCA), or a combina on of the two. Bolus dosing was ini ated at 1 to 2 mg, with supplemental doses of 1 to 3 mg every one to three hours, as needed, based on individual pa ent need and previous response to oliceridine in management of acute post-opera ve 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 concentra on range of 0 to 35 ng/ml. It is indicated for short-term use only & limited to hospitals or other controlled clinical se ngs. Oliceridine requires no dosage adjustments in pa ents with renal impairment as well as in pa ent with significant medical complica ons. Therefore, opioids that bias towards Gprotein and away from β arres n signaling should produce analgesia with reduced side effects.