Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594

Conclusions Activation of α4β2 nicotinic acetylcholine receptors by varenicline and ABT 594 counters opioid-induced respiratory depression without interfering with analgesia.Editor ’s PerspectiveWhat We Already Know about This TopicActivation of α4β2 nicotinic acetylcholine receptors by the full agonist A83580 markedly reduced opioid-induced respiratory depression in rats without compromising analgesiaVarenicline, which is used to treat smoking addiction, and ABT 594, which produced analgesia in trials of patients with diabetic peripheral neuropathic pain, are potent, partial agonists of α4β2 nicotinic acetylcholine receptorsWhat This Article Tells Us That Is NewPre- or coadministration of varenicline or ABT 594 with opioids markedly reduced the degree of respiratory depression they caused in ratsVarenicline and ABT 594 reversed moderate to severe respiratory depression produced by fentanyl without interfering with opioid-induced suppression of painAdministration of ABT 594 and varenicline coadministered with a low dose of naloxone reversed respiratory depression and prevented death caused by a bolus lethal dose of fentanyl or the combination of fentanyl and diazepam
Source: Anesthesiology - Category: Anesthesiology Source Type: research