Articles: narcotic-antagonists.
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Zh Nevrol Psikhiatr · Jan 2015
[Alcohol use disorders: current approaches to diagnosis and treatment].
Alcohol abuse and alcoholism are the leading causes of disability, health worsening and increased mortality. Diagnosis of alcohol use disorders is based on the formal criteria of ICD-10 and DSM-V. Sobriety-oriented therapy has extremely low efficiency. ⋯ Serious expectations in addressing unsatisfactory efficiency of alcoholism treatment are associated with WHO reducing alcohol consumption strategy. Nalmefene is the first and still only drug registered as a medicine for reducing alcohol use. Recent studies show that the decrease of alcohol consumption using nalmefene creates opportunities for significant lessening of alcohol-related morbidity, injuries and deaths.
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Nociceptin/orphanin FQ (N/OFQ) controls several biological functions by selectively activating an opioid like receptor named N/OFQ peptide receptor (NOP). Biased agonism is emerging as an important and therapeutically relevant pharmacological concept in the field of G protein coupled receptors including opioids. To evaluate the relevance of this phenomenon in the NOP receptor, we used a bioluminescence resonance energy transfer technology to measure the interactions of the NOP receptor with either G proteins or β-arrestin 2 in the absence and in presence of increasing concentration of ligands. ⋯ Most partial agonists behaved as pure competitive antagonists of receptor/arrestin interaction. Antagonists displayed similar values of potency for NOP/Gβ1 or NOP/β-arrestin 2 interaction. Using N/OFQ as reference ligand we computed the bias factors of NOP ligands and a number of agonists with greater efficacy at G protein coupling were identified.
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J Subst Abuse Treat · Jan 2015
Randomized Controlled Trial Multicenter StudyThe multi-site prescription opioid addiction treatment study: 18-month outcomes.
Despite the high prevalence of prescription opioid dependence in the U. S., little is known about the course of this disorder and long-term response to treatment. We therefore examined 18-month post-randomization outcomes of participants in the Prescription Opioid Addiction Treatment Study, a multi-site, randomized controlled trial examining varying durations of buprenorphine-naloxone treatment and different intensities of counseling for prescription opioid dependence. ⋯ Most participants (65.9%) engaged in substance use disorder treatment during the past year, most commonly opioid agonist therapy (48.8%). Of particular interest in this population, multivariable analysis showed that greater pain severity at baseline was associated with opioid dependence at 18 months. In conclusion, although opioid use outcomes during the treatment trial were poor immediately following a buprenorphine-naloxone taper compared to those during 12 weeks of buprenorphine-naloxone stabilization, opioid use outcomes at 18-month follow-up showed substantial improvement over baseline and were comparable to the rate of successful outcomes during buprenorphine-naloxone stabilization in the treatment trial.
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Nalbuphine is an agonist-antagonist opioid. It causes analgesic and sedative effect and because of ceiling effect it does not cause a respiratory depression. In a perioperative therapy of paediatric patients it may be used for premedication, sedation during diagnostic procedures as well as for postoperative pain treatment. ⋯ After sevoflurane anaesthesia of small children, it reduces the incidences of emergence agitation. Nalbuphine is considered a safe drug, which causes nausea and vomiting less frequently than other opioids. Analgesic effect, the ability to provide moderate sedation and a large margin of safety make that analgesic often used for paediatric patients.