The Medical Letter n. 6 / 2021
Nr. 06 del 15/03/2021
TML n.6 / 2021 UN NUOVO OPPIOIDE PER IL DOLORE GRAVE
L’ oliceridina (Olinvyk-Trevena negli USA; non disponibile in commercio in Italia), un agonista oppioide EV, è stata approvata dalla FDA per la gestione del dolore acuto di gravità tale da richiedere l’uso di un oppioide e per cui le opzioni di trattamento alternative risultino inadeguate.
MECCANISMO D’AZIONE – Il legame di un agonista oppioide ai recettori μ degli oppioidi determina l’attivazione delle proteine G, ritenute il principale mediatore dell’analgesia indotta da oppioidi, e il reclutamento delle β-arrestine, considerate tra le cause degli effetti avversi degli oppioidi. L’oliceridina promuove il legame preferenziale dei recettori μ degli oppioidi con le proteine G, con un’attivazione ridotta della via delle β-arrestine. Negli studi sugli animali, l’oliceridina manteneva l’efficacia analgesica della morfina con tassi inferiori di depressione respiratoria e di effetti avversi GI.
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