Deaths due to prescription and illicit opioid overdose have been rising at an alarming rate, particularly in the USA. Although naloxone injection is a safe and effective treatment for opioid overdose, it is frequently unavailable in a timely manner due to legal and practical restrictions on its use by laypeople. As a result, an effort spanning decades has resulted in the development of strategi...

Naloxone, an opioid antagonist, augments baroreflex mechanisms in animals; this occurrence suggests that endogenous opioids blunt baroreflex responses. Limited human studies suggest an inhibitory action of endogenous opioids on baroreflex-mediated vagal responses during arterial baroreceptor deactivation. To evaluate the potential effect of endogenous opioids on cardiopulmonary baroreflex mecha...

OBJECTIVE Role of nitric oxide (NO) in reversing morphine anti-nociception has been shown. However, the interaction between NO and naloxone-induced pain in the hippocampus is unknown. The present study aimed to investigate the involvement of molecule NO in naloxone-induced pain and its possible interaction with naloxone into cortical area 1 (CA1) of hippocampus. MATERIALS AND METHODS Male Wis...

OBJECTIVE To evaluate tolerability, safety, and quality-of-life outcomes in non-opioid-pretreated patients with severe chronic low back pain with a neuropathic component receiving tapentadol PR vs. oxycodone/naloxone PR. METHODS Eligible patients (average pain intensity [numerical rating scale] ≥ 6; painDETECT positive/unclear ratings) were randomized to twice-daily tapentadol PR 50 mg or oxy...

Endogenous opioid peptides mediate the effect of suckling on LH and PRL in the domestic pig. However, the role of opioids in modulating GH during lactation in swine is not known. Primiparous sows that had been immunized against GRF(1-29) conjugated to human serum albumin (GRF-HSA, n = 5) or HSA (n = 4) were used to determine changes in GH after naloxone. Treatments were imposed in all sows on d...

OBJECTIVE To compare the quality of life of patients with moderate-to-severe chronic low back pain under treatment with the WHO-step III opioids oxycodone/naloxone, oxycodone, or morphine in routine clinical practice. STUDY DESIGN Prospective, 12-week, randomized, open-label, blinded end-point study in 88 medical centers in Germany. PATIENTS AND METHODS A total of 901 patients requiring aro...

BACKGROUND AND AIMS Take-home naloxone can prevent death from heroin/opioid overdose, but pre-provision is difficult because naloxone is usually given by injection. Non-injectable alternatives, including naloxone nasal sprays, are currently being developed. To be effective, the intranasal (i.n.) spray dose must be adequate but not excessive, and early absorption must be comparable to intramuscu...

Painful stimuli are known to engage an endorphin analgesic system that can be reversed by the opiate antagonist, naloxone. Naloxone, then, should increase the effectiveness of aversive unconditioned stimuli (USs) in Pavlovian fear conditioning. Consistent with this hypothesis, naloxone administered during the acquisition of conditioned suppression in rats enhanced posttrial suppression and prec...

Stressful stimuli, electric footshock (FS), immobilized-water immersion (IW), and cold-water swimming (CWS), produced analgesia and prolonged the pentobarbital hypnosis as well as morphine and clonidine. Naloxone completely antagonized the analgesic effects of morphine and FS and partially that of IW; however, that of clonidine and CWS were not reversed by naloxone. Naloxone eliminated the hypn...

[(3)H]Naloxone, a potent opiate antagonist, binds stereospecifically to opiate-receptor sites in rat-brain tissue. The binding is time, temperature, and pH dependent and saturable with respect to [(3)H]naloxone and tissue concentration. The [(3)H]naloxone-receptor complex formation is bimolecular with a dissociation constant of 20 nM. 15 Opiate agonists and antagonists compete for the same rece...