Articles: opioid-analgesics.
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Functional interactions between the mu opioid receptor (MOR) and the metabotropic glutamate receptor 5 (mGluR5) in pain and analgesia have been well established. MMG22 is a bivalent ligand containing MOR agonist (oxymorphamine) and mGluR5 antagonist (MPEP) pharmacophores tethered by a 22-atom linker. MMG22 has been shown to produce potent analgesia in several models of chronic inflammatory and neuropathic pain (NP). ⋯ MMG22 also lacked the central locomotor, respiratory, and anxiolytic side effects of its monomeric pharmacophores. Evaluation of mRNA expression showed the transcripts for both receptors were colocalized in cells in the dorsal horn of the lumbar spinal cord and dorsal root ganglia. Thus, MMG22 reduces hyperalgesia after injury in the SNI model of NP without the typical centrally mediated side effects associated with traditional opioids.
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Anesthesia and analgesia · Sep 2020
Molecular Interaction Between Butorphanol and κ-Opioid Receptor.
The misuse of opioids stems, in part, from inadequate knowledge of molecular interactions between opioids and opioid receptors. It is still unclear why some opioids are far more addictive than others. The κ-opioid receptor (KOR) plays a critical role in modulating pain, addiction, and many other physiological and pathological processes. Butorphanol, an opioid analgesic, is a less addictive opioid with unique pharmacological profiles. In this study, we investigated the interaction between butorphanol and KOR to obtain insights into the safe usage of this medication. ⋯ In conclusion, butorphanol is a partial KOR agonist in the G-protein activation pathway and a potent KOR full agonist in the β-arrestin recruitment pathway. The structure analysis offers insights into the molecular mechanism of KOR interaction and activation by butorphanol.
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The association between surgeon prescribing practices and new persistent postoperative opioid use is not well understood. We examined the association between surgeon prescribing and new persistent use among total hip arthroplasty (THA) patients. ⋯ The development of persistent opioid use after surgery is multifactorial, and surgeon prescribing patterns play an important role. Reducing prescribing and encouraging opioid alternatives could minimize postoperative persistent opioid use.
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Res Social Adm Pharm · Sep 2020
Perception of prescription drug monitoring programs as a prevention tool in primary medical care.
Prescription drug monitoring programs (PDMPs) are primary prevention tools to reduce substance use disorders (SUD) and sequelae. Evidence regarding perceptions of PDMPs from different primary care providers, which may impact PDMP utilization for women, is unavailable. ⋯ These results suggest OB/GYNs view their state's PDMP as less effective than do PCPs, which may present barriers to PDMP utilization and decrease opportunities for SUD interventions. Engagement of all healthcare team members is needed to inform future strategies and policies to increase PDMP effectiveness.