A highly sensitive method was developed to measure naloxone and its metabolite nornaloxone in human plasma, urine, and human liver microsomes (HLM). Naltrexone-d(3) and oxymorphone-d(3) were used as respective internal standards. Solid-phase extraction, using mixed mode extraction columns and 0.1 M phosphate buffer (pH 5.9), was combined with high-performance liquid chromatography interfaced by...

Sows (N = 16) were infused intravenously for 8 h with saline or naloxone (200 mg/h) or their litters were transiently weaned for 8 h. Before infusion, 200 mg naloxone were administered to elevate quickly concentrations of naloxone. Blood samples were collected from sows at 15 min intervals for 24 h, beginning 8 h before and continuing until 8 h after imposition of treatments during the middle 8...

BACKGROUND Naloxone is standard medication for the treatment of heroin intoxications. No large-scale studies have yet been carried out to determine its toxicity in heroin intoxications. METHODS We have undertaken an investigation as to the frequency, type and degree of severity of complications attributable to naloxone administration. Subjects treated between 1991 and 1993 with naloxone for i...

The effects of the opiate antagonist naloxone on electrophysiological measures of human selective attention were examined utilizing a paradigm which dissociates selective information processing from any concurrent processes of general arousal that may be present. Subjects were injected with naloxone (2 mg, i.v.) or placebo prior to performing a three-channel selective listening task. The measur...

INTRODUCTION Naloxone's use in cardiac arrest has been of recent interest, stimulated by conflicting results in both human case reports and animal studies demonstrating antiarrhythmic and positive ionotropic effects. We hypothesized that naloxone administration during cardiac arrest, in suspected opioid overdosed patients, is associated with a change in cardiac rhythm. METHODS From a database...

BACKGROUND Naloxone has been evidenced widely as a means of reducing mortality resulting from opiate overdose, yet its distribution to drug users remains limited. However, it is drug users who are most likely to be available to administer naloxone at the scene and who have been shown to be willing and motivated to deliver this intervention. The current study builds on a national training evalua...

Opiate receptor inhibition causes adrenergic receptor-mediated increases in aortic pressure, cardiac output, and left ventricular contractile function in right heart failure. To study whether the effects of opiate receptor inhibition are mediated by means of an action on the central opiate system, we administered equimolar doses of naloxone hydrochloride and naloxone methobromide (MeBr) and nor...

We examined two methods of generating a dose-response curve to the opioid receptor antagonist naloxone. In 15 healthy male subjects (18-25 years) plasma adrenocorticotropin (ACTH) responses to five doses of naloxone studied over 5 separate days were compared to plasma ACTH responses to five incremental doses of naloxone studied within a single session. There was a statistically significant posi...

Placebo analgesia involves the endogenous opioid system, as administration of the opioid antagonist naloxone decreases placebo analgesia. To investigate the opioidergic mechanisms that underlie placebo analgesia, we combined naloxone administration with functional magnetic resonance imaging. Naloxone reduced both behavioral and neural placebo effects as well as placebo-induced responses in pain...

Administration of naloxone hydrochloride is the standard treatment for heroin overdose. Naloxone is simple to administer, effective and has a very low risk of harm. Prescribing naloxone to heroin users for later use in case of need is a simple, inexpensive harm-reduction measure that has the potential to reduce mortality from heroin overdose. Some U.S. physicians may be discouraged from distrib...