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By Christopher Cook, BA,CADC, SAP Addiction professional. LPC, CADC, CRNP- student, Interventionist, project manager, owner, Director, eval/refer for SUDs/Eating D/o's
D S Wang, G Sternbach, J Varon
The use of the opioid antagonist naloxone is well known to the experienced health care provider. The availability of the longer acting opioid antagonist nalmefene has several potential benefits in clinical practice. Nalmefene has a plasma half-life of almost 11 h, compared to 60-90 min for naloxone. Nalmefene has been shown to reverse opioid intoxication for as long as 8 h, reducing the need for continuous monitoring of intoxicated patients and repeated dosing of naloxone. Single dose administration has also been used effectively in the reversal of opiate-assisted conscious sedation...
May 1998: Journal of Emergency Medicine
Jeremy C Cornelissen, Samuel Obeng, Kenner C Rice, Yan Zhang, S Stevens Negus, Matthew Banks
Receptor theory predicts that fixed-proportion mixtures of a competitive, reversible agonist (e.g. fentanyl) and antagonist (e.g. naltrexone) at a common receptor (e.g. mu opioid receptors; MOR) will result in antagonist proportion-dependent decreases in apparent efficacy of the mixtures and downward shifts in mixture dose-effect functions. The present study tested this hypothesis by evaluating behavioral effects of fixed-proportion fentanyl/naltrexone mixtures in a warm-water tail-withdrawal procedure in rhesus monkeys (n=4)...
January 12, 2018: Journal of Pharmacology and Experimental Therapeutics
Guilherme Carneiro Montes, Bianca Nascimento Monteiro da Silva, Bismarck Rezende, Roberto Takashi Sudo, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Angelo da Cunha Pinto, Bárbara Vasconcellos da Silva, Gisele Zapata-Sudo
5'-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 1-12 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 µmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a µ-opioid antagonist...
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Giovanna Del Vecchio, Viola Spahn, Christoph Stein
Conventional opioids mediate analgesia as well as severe adverse effects via G-protein coupled opioid receptors (OR) in both inflamed (peripheral injured tissue) and healthy (brain, intestinal wall) environments. To exclude side effects, OR activation can be selectively achieved in damaged tissue by lowering the pKa of an opioid ligand to the acidic pH of inflammation. As a result, protonation of the ligand and consequent OR binding and activation of G-proteins is pH- and injury-specific. A novel compound (NFEPP) demonstrates the feasibility of this approach and displays blockade of pain transmission only at the peripheral site of injury, but with lack of central and gastrointestinal adverse effects...
August 16, 2017: ACS Chemical Neuroscience
Abraham Madariaga-Mazón, Andrés F Marmolejo-Valencia, Yangmei Li, Lawrence Toll, Richard A Houghten, Karina Martinez-Mayorga
Biased activation of G-protein-coupled receptors (GPCRs) is shifting drug discovery efforts and appears promising for the development of safer drugs. The most effective analgesics to treat acute pain are agonists of the μ opioid receptor (μ-OR), a member of the GPCR superfamily. However, the analgesic use of opioid drugs, such as morphine, is hindered by adverse effects. Only a few μ-OR agonists have been reported to selectively activate the Gi over β-arrestin signaling pathway, resulting in lower gastrointestinal dysfunction and respiratory suppression...
July 22, 2017: Drug Discovery Today
Xin Liu, Long Zhao, Yuan Wang, Jingjing Zhou, Dan Wang, Yixin Zhang, Xianghui Zhang, Zhaojuan Wang, Dongxu Yang, Lingyun Mou, Rui Wang
Opioid peptides are neuromodulators that bind to opioid receptors and reduce pain sensitivity. Endomorphins are among the most active endogenous opioid peptides, and they have good affinity and selectivity toward the μ opioid receptor. However, their clinical usage is hindered by their inability to cross the blood-brain barrier and their poor in vivo activity after peripheral injection. In order to overcome these defects, we have designed and synthesized a series of novel endomorphin analogs with multiple site modifications...
August 10, 2017: ACS Chemical Neuroscience
Matthew P Prekupec, Peter A Mansky, Michael H Baumann
: Novel synthetic opioids (NSOs) include various analogs of fentanyl and newly emerging non-fentanyl compounds. Together with illicitly manufactured fentanyl (IMF), these drugs have caused a recent spike in overdose deaths, whereas deaths from prescription opioids have stabilized. NSOs are used as stand-alone products, as adulterants in heroin, or as constituents of counterfeit prescription medications. During 2015 alone, there were 9580 deaths from synthetic opioids other than methadone. Most of these fatalities were associated with IMF rather than diverted pharmaceutical fentanyl...
July 2017: Journal of Addiction Medicine
Hoda Soltani, Abbas Pardakhty
Novel drug delivery systems for controlled-release of opioid agonists as a long time painkillers or opioid antagonists for opium, heroin, and alcohol addiction are under development or in clinical use today. In this article, the field of "new drug delivery systems" is momentarily reviewed from the viewpoint of the marketed opioid agonists/antagonists dosage forms today.
April 2016: Addiction & Health
O A Gromova, I Yu Troshin, O A Limanova, A N Gromov, L E Fedotova, K V Rudakov
Hopantenic acid is a well-known nootropic drug similar in its chemical structure to pantothenic acid (vitamin B5). Neurotropic effects of hopantenic acid act through binding with delta- and kappa opioid receptors, modulation of acetylcholine secretion and relationship with dopamine receptors. Besides neurotropic effects, hopantenic acid may modulate the metabolism of prostaglandins, steroids and have antitumor effects.
2015: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Lawrence Toll, Michael R Bruchas, Girolamo Calo', Brian M Cox, Nurulain T Zaveri
The NOP receptor (nociceptin/orphanin FQ opioid peptide receptor) is the most recently discovered member of the opioid receptor family and, together with its endogenous ligand, N/OFQ, make up the fourth members of the opioid receptor and opioid peptide family. Because of its more recent discovery, an understanding of the cellular and behavioral actions induced by NOP receptor activation are less well developed than for the other members of the opioid receptor family. All of these factors are important because NOP receptor activation has a clear modulatory role on mu opioid receptor-mediated actions and thereby affects opioid analgesia, tolerance development, and reward...
April 2016: Pharmacological Reviews
Hui Fan, Teng-Fei Li, Nian Gong, Yong-Xiang Wang
Lamiophlomis rotata (L. rotata, Duyiwei) is an orally available Tibetan analgesic herb widely prescribed in China. Shanzhiside methylester (SM) is a principle effective iridoid glycoside of L. rotata and serves as a small molecule glucagon-like peptide-1 (GLP-1) receptor agonist. This study aims to evaluate the signal mechanisms underlying SM anti-allodynia, determine the ability of SM to induce anti-allodynic tolerance, and illustrate the interactions between SM and morphine, or SM and β-endorphin, in anti-allodynia and anti-allodynic tolerance...
February 2016: Neuropharmacology
Ibrahim Bulduk, Bahdışen Gezer, Mustafa Cengiz
In this study, amount of morphine from poppy capsules (Papaver somniferum) was investigated using ultrasonic assisted extraction (UAE). Response surface methodology was used to estimate effective experimental conditions on the content extraction of poppy capsules. For this purpose, solvent/solid ratio (10-20 mL/500 mg sample), pH (1-13), time (30-60 min), and temperature (30-50°C) were chosen as experimental variables. The affected response is extraction recovery values for morphine from poppy straw...
2015: International Journal of Analytical Chemistry
Shih-Hsien Lin, Kao Chin Chen, Sheng-Yu Lee, Nan Tsing Chiu, I Hui Lee, Po See Chen, Tzung Lieh Yeh, Ru-Band Lu, Chia-Chieh Chen, Mei-Hsiu Liao, Yen Kuang Yang
One of the consequences of heroin dependency is a huge expenditure on drugs. This underlying economic expense may be a grave burden for heroin users and may lead to criminal behavior, which is a huge cost to society. The neuropsychological mechanism related to heroin purchase remains unclear. Based on recent findings and the established dopamine hypothesis of addiction, we speculated that expenditure on heroin and central dopamine activity may be associated. A total of 21 heroin users were enrolled in this study...
March 30, 2015: Psychiatry Research
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