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Effects of alcohol on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules.

Although contraindicated, coingestion of alcohol and opioids by patients or drug abusers is a major health concern because of dangerous additive and potentially life-threatening sedative and respiratory effects. In addition, alcohol has been shown to disrupt the extended-release characteristics of certain extended-release opioid formulations, releasing a hazardous amount of opioid over a short time period. Morphine sulfate and naltrexone hydrochloride extended release capsules (MS-sNT), which contain naltrexone sequestered in each pellet core, are indicated for management of chronic, moderate …

A double-blind, placebo-controlled study of the opiate antagonist, naltrexone, in the treatment of kleptomania.

BACKGROUND: Kleptomania is a rare psychiatric disorder characterized by recurrent stealing and for which there exists no empirically validated treatments. This study examined the efficacy and tolerability of the opioid antagonist naltrexone in adults with kleptomania who have urges to steal. METHODS: An 8-week, double-blind, placebo-controlled trial was conducted to evaluate the safety and efficacy of oral naltrexone for kleptomania. Twenty-five individuals with DSM-IV kleptomania were randomized to naltrexone (dosing ranging from 50 mg/day to 150 mg/day) or placebo. Twenty-three subjects (92…

Predicting the effect of naltrexone and acamprosate in alcohol-dependent patients using genetic indicators.

Acamprosate and naltrexone are effective medications in the treatment of alcoholism. However, effect sizes are modest. Pharmacogenomics may improve patient-treatment-matching and effect sizes. It is hypothesized that naltrexone exerts its effect through genetic characteristics associated with the dopaminergic/opioidergic positive reinforcement system, whereas acamprosate works through the glutamatergic/GABAergic negative reinforcement system. Alcohol-dependent subjects were randomly assigned to either acamprosate or naltrexone. Subjects participated in a cue-exposure experiment at the day befo…

The effect of naltrexone on amphetamine-induced conditioned place preference and locomotor behaviour in the rat.

Whereas amphetamine and other psychostimulants primarily act on the dopamine system, there is also evidence that other neurotransmitter systems, such as the endogenous opioid system, modulate psychostimulant-induced effects. Several studies have investigated the role of opioid antagonists on cocaine-induced conditioned place preference (CPP), but there is limited information about the interaction with amphetamines. The aim of the present study was to investigate the effect of the opioid receptor antagonist, naltrexone (NTX) on the conditioning, expression and reinstatement of amphetamine-induc…

Overriding the blockade of antinociceptive actions of opioids in rats treated with extended-release naltrexone.

A monthly extended-release formulation of the opioid antagonist naltrexone (XR-NTX) is approved for treatment of alcohol dependence. There is little research regarding overriding chronic (>21 days) competitive opioid receptor blockade with opioids for acute pain. Using the hot plate test after XR-NTX or placebo microsphere administration, rats were treated with an opioid analgesic to determine the dose required to produce the maximum response latency (MRL; 60 s). Rats were later treated with the same opioid to determine any potential effects on respiration rate or locomotor activity. In naïve …

Differential effects of naltrexone on cardiac, subjective and behavioural reactions to acute ethanol intoxication.

OBJECTIVE: Alcohol may have psychomotor stimulant properties during the rising limb of the blood alcohol curve at commonly self-administered doses. Increased heart rate (HR) immediately after alcohol consumption may serve as an indicator or marker of such properties, which appear to be potentially opiate-mediated and dopamine-dependent. Naltrexone, an opiate antagonist, has been used successfully in the treatment of alcoholism and may produce its therapeutic effects through its effects on alcohol metabolism or by blocking alcohol's rewarding effects. We hypothesized that, if naltrexone blocks …

Effect of repeated administrations of heroin, naltrexone, methadone, and alcohol on morphine glucuronidation in the rat.

RATIONALE: Heroin is rapidly metabolized to morphine that in turn is transformed in morphine-3-glucuronide (M3G), an inactive metabolite, an … ole of MOR in these effects of heroin, by examining the effects of methadone, a MOR agonist, and of naltrexone, a MOR antagonist, on morphine glucuronidation. We also investigated the effects of alcohol, which is known to alter drug metabolism and is frequently coabused by heroin addicts. METHODS: Morphine glucuronidation was studied in liver microsomes obt …

Naltrexone effects on alcohol consumption in a clinical laboratory paradigm: temporal effects of drinking.

BACKGROUND: This clinical laboratory study evaluated how the timing of drinking and subjective responses to alcohol are effected by the opioid antagonist naltrexone. METHODS: Forty non-treatment seeking alcoholics were randomly assigned to treatment with 50 mg naltrexone or matching placebo for 7 days. On day 7, they were administered an "initial drink" of alcohol (blood alcohol levels of between 20 and 30 mg%) in a bar-like setting. In a random fashion, half of the subjects in each group (naltrexone and placebo) had either immediate or delayed (40 min) access to up to 8 additional mini-drink…

Influence of chronic Naltrexone treatment on growth hormone and insulin secretion in obese subjects.

OBJECTIVE: Recent studies have demonstrated the restoration of a normal 24 h GH profile induced by a reduction of insulinaemia after weight loss, suggesting a reciprocal relationship between plasma insulin and GH concentrations. We aimed to clarify if an opiate-induced reduction in plasma insulin could affect GH secretion in obesity. DESIGN: We have studied the insulin response to an oral glucose tolerance test (OGTT) and the GH response to GHRH before and after prolonged treatment with Naltrexone (NTX). C-peptide, IGF-I, IGFBP-3 plasma levels and the IGF-I/IGFBP-3 molar ratio were also deter…

An unusual reaction to opioid blockade with naltrexone in a case of post-traumatic stress disorder.

An unusual behavioral and cardiovascular reaction was observed during opioid blockade with naltrexone in a 32-year-old male who met DSM III-R criteria for post-traumatic stress disorder (PTSD). As part of an ongoing placebo-controlled investigation of the effects of naltrexone on laboratory and ambulatory blood pressure reactivity, this participant reported experiencing feelings of rage, explosive behavior, and other unpleasant symptoms. When compared to all other subjects (N = 24), this individual showed significantly greater effects of naltrexone on blood pressure reactivity during the labor…

Effect of naltrexone treatment on insulin secretion, insulin action and postprandial thermogenesis in obesity.

For many years a series of studies has been carried out to evaluate the role of endogenous opioid peptides on glucose metabolism. In this work we studied the influence of endogenous opioid peptides on insulin response to OGTT and glucose-induced thermogenesis before and after a prolonged oral treatment with Naltrexone (50 mg/daily for 6 days), an opioid receptor antagonist, in a group of 9 obese subjects. Moreover in obese patients we evaluated the effect of this anti-opioid drug on insulin secretion and insulin sensitivity during an IVGTT using the minimal model approach. We compared the pre-…

Antagonism by naltrexone of the hypotension and bradycardia induced by alpha-methyldopa in conscious normotensive rats.

The possible role of the endogenous opioid system in the central hypotensive mechanism of action of alpha-methyldopa was investigated. Conscious normotensive Wistar rats were used in this study and all treatments were given intracisternally. Pretreatment with the opiate receptor antagonist naltrexone resulted in a parallel shift to the right of the dose-response curve for alpha-methyldopa, both for blood pressure and heart rate. In addition, when increasing doses of naltrexone and a constant dose of alpha-methyldopa were used the opiate receptor antagonist inhibited dose-dependently alpha-meth…

[Efficacy of the treatment of sleep apnea using naltrexone. A clinical, polygraphic and gasometric study].

Twelve patients with clinical, polysomnographic and oxymetric features of Sleep Apnoea Syndrome (S.A.S.) were recorded, after a 2-week wash-out period, during 2 nights without treatment and 2 nights after receiving 50 mg naltrexone at bed-time. Clinical symptoms improved immediately in four patients, within one month in three patients and after 3 months of treatment in the remaining five ones. Sleep Apnoea index as well as the number, duration and intensity of hypoxic events were dramatically improved by this treatment that has now been prescribed to 25 patients, for more than 2 years in 14 of…

Расширенный выпуск Naltrexone (Vivitrol) Увеличение за навязчивое сексуальное поведение: отчет по делу.

Компульсивное расстройство сексуального поведения (CSBD) было включено в ICD-11 как расстройство импульсного контроля, однако возможности фармакологического лечения по-прежнему ограничены. Налтрексон, антагонист опиоидного рецептора, получивший разрешение на расстройства, связанные с употреблением алкоголя и опиоидов, продемонстрировал многообещающее сексуальное поведение, хотя инъекционный состав с расширенным выпуском не оценивался на этот счет. 54-year-old Женатый мужчина с продолжительным навязчивым сексуальным поведением с острыми симптомами после потери работы, включая навязчивое использ

Совпадение в аннотации оригинала
BackgroundCompulsive sexual behavior disorder (CSBD) was included in the ICD-11 as an impulse control disorder, yet pharmacological treatment options remain limited. Naltrexone, an opioid receptor antagonist approved for alcohol and opioid use disorders, has shown promise for compulsive sexual behaviors, though the extended-release injectable formulation has…

Early cardiovascular and respiratory changes after etorphine immobilization and naltrexone reversal in sheep.

INTRODUCTION: The immediate cardiorespiratory responses to etorphine immobilization and reversal with naltrexone in wildlife are underexplored. OBJECTIVE: To evaluate the early cardiorespiratory changes after etorphine immobilization and reversal with naltrexone in sheep, as a model for wild ungulates. METHODS: Six sheep instrumented with electrical impedance tomography (EIT) belt, arterial and pulmonary arterial catheters were immobilized with intramuscular etorphine (0.05 mg kg-1) and reversed with intravenous naltrexone (1 mg kg-1) 26 min later. Mean pulmonary arterial pressure (MPAP) and…

Nanomolar TLR4 Antagonist CIAC101 Derived from (+)-Naltrexone Blocks Microglial Activation and Methamphetamine Addiction.

Neuroimmune activation via Toll-like receptor 4 (TLR4) contributes to the pathophysiology of substance use disorders. Although (+)-naltrexone can antagonize TLR4 without engaging classical opioid receptors, its modest potency limits translational potential. The dual-site optimization at C3 and N17 was performed and identified CIAC101, an isobutyl-substituted (+)-naltrexone derivative with nanomolar TLR4 antagonism, representing ∼6200-fold higher potency than (+)-naltrexone. CIAC101 dose-dependently blocked lipopolysaccharides-induced NF-κB activation and reduced the expression of pro-inflammat…

Attitudes toward extended-release naltrexone treatment for opioid use disorder among African Americans.

BACKGROUND: Extended-release naltrexone (XR-NTX; Vivitrol®) is a long-acting injectable form of naltrexone, which is a medication used to treat opioid use disorder (OUD). In 2010, XR-NTX received Food and Drug Administration approval to treat OUD, becoming the first non-addictive and non-psychoactive medication for this condition. Because uptake of XR-NTX has been relatively low, less is known regarding how persons with OUD view this form of treatment. And because previous studies tend to rely on samples that lack racial diversity or are conducted outside the United States, we know very little…

Education Intervention to Increase Naltrexone Use Among Adult Inpatients With Alcohol Use Disorder.

Alcohol use disorder (AUD) accounts for high rates of global deaths, disability, and health care spending. Naltrexone is an opioid antagonist used to reduce alcohol cravings. Despite demonstrated safety and efficacy, naltrexone is highly underutilized in a variety of health care settings. The current quality improvement (QI) project aimed to increase knowledge and prescribing behaviors of naltrexone. A chart review of a purposive convenience sample was performed to determine the impact of the intervention. Staff participants completed a pre/posttest and a post-module survey. The primary object…

Patients' experiences of continued treatment with extended-release naltrexone: a Norwegian qualitative study.

BACKGROUND: The opioid antagonist extended-release naltrexone (XR-NTX) in the treatment of opioid use disorder (OUD) is effective in terms of safety, abstinence from opioid use and retention in treatment. However, it is unclear how patients experience and adjust to losing the possibility of achieving an opioid effect. This qualitative study is the first to explore how people with opioid dependence experience XR-NTX treatment, focusing on the process of treatment over time. METHODS: Using a purposive sampling strategy, semi-structured interviews were undertaken with 19 persons with opioid use …

Chronic Naltrexone Therapy Is Associated with Improved Cardiac Function in Volume Overloaded Rats.

PURPOSE: Myocardial opioid receptors were demonstrated in animals and humans and seem to colocalize with membranous and sarcolemmal calcium channels of the excitation-contraction coupling in the left ventricle (LV). Therefore, this study investigated whether blockade of the cardiac opioid system by naltrexone would affect cardiac function and neurohumoral parameters in Wistar rats with volume overload-induced heart failure. METHODS: Volume overload in Wistar rats was induced by an aortocaval fistula (ACF). Left ventricular cardiac opioid receptors were identified by immunohistochemistry and t…