Replacement of Current Opioid Drugs Focusing on MOR-Related Strategies
JPT-107519; No of Pages 17 Pharmacology & Therapeutics xxx (2020) xxx Contents lists available at ScienceDirect Pharmacology & Therapeutics journal homepage: www.elsevier.com/locate/pharmthera Replacement of current opioid drugs focusing on MOR-related strategies Jérôme Busserolles a,b, Stéphane Lolignier a,b, Nicolas Kerckhove a,b,c, Célian Bertin a,b,c, Nicolas Authier a,b,c, Alain Eschalier a,b,⁎ a Université Clermont Auvergne, INSERM, CHU, NEURO-DOL Pharmacologie Fondamentale et Clinique de la douleur, F-63000 Clermont-Ferrand, France b Institut ANALGESIA, Faculté de Médecine, F-63000 Clermont-Ferrand, France c Observatoire Français des Médicaments Antalgiques (OFMA), French monitoring centre for analgesic drugs, CHU, F-63000 Clermont-Ferrand, France article info abstract Available online xxxx The scarcity and limited risk/benefit ratio of painkillers available on the market, in addition to the opioid crisis, warrant reflection on new innovation strategies. The pharmacopoeia of analgesics is based on products that are often old and derived from clinical empiricism, with limited efficacy or spectrum of action, or resulting in Keywords: an unsatisfactory tolerability profile. Although they are reference analgesics for nociceptive pain, opioids are sub- Analgesia ject to the same criticism. The use of opium as an analgesic is historical. Morphine was synthesized at the begin- Mu opioid receptors (MORs) ning of the 19th century. The efficacy of opioids is limited in certain painful contexts and these drugs can induce Opioid adverse side effects potentially serious and fatal adverse effects. The current North American opioid crisis, with an ever-rising number Opioid abuse and misuse of deaths by opioid overdose, is a tragic illustration of this.
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