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Fischer, Bradford D. Dykstra Linda A. "Interactions between opioid agonists and glutamate receptor antagonists." Chapel Hill, N.C. : University of North Carolina at Chapel Hill, 2008. http://dc.lib.unc.edu/u?/etd,1694.
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Thesis (Ph. D.)--University of North Carolina at Chapel Hill, 2008.Title from electronic title page (viewed Sep. 16, 2008). "... in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the Department of Psychology Behavioral Neuroscience." Discipline: Psychology; Department/School: Psychology.
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Basti, Vida. "Ligand biased signaling of opioid agonists forphosphorylation and regulation of μ -opioid receptors." Thesis, Uppsala universitet, Farmakologi, 2013. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-192584.
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Abstract Ligand biased signaling of opioid agonists for phosphorylation andregulation of μ -opioid receptors Student: Vida Basti. Supervisor: Prof Macdonald Christie. Departmement of Neuropharmacology, The University of Sydney. Examiner: Prof Ingrid Nylander. Departement of Phamacology, University of Uppsala. Opioid drugs are of great use in the medical practise. The drugs are commonly prescribed formany types of illnesses, mostly in cases of pain management. Although opioids come withmany benefits they are causing a lot of problems as well. The side effects are many andamongst these is tolerance development which may lead to abuse and addiction. Because ofthe fast tolerance development in patients, higher doses up to 10 times the therapeutic doseare being prescribed. This is a major issue in today’s society and must be addressed.Scientists are trying to figure out the mechanism behind tolerance by comparing differenttypes opioid drugs. Some opioids causes tolerance in a much faster rate than others but it isstill uncertain why and what is causing this. Two of the most commonly prescribed opioidsare oxycodone and morphine and so in this rapport these opioids are compared with respectto their capability to cause internalization in neurons. In the experiments a positive control,DAMGO, is being used as well as a negative control. The method being used is an indirectmethod of immunohistochemistry on AtT20 transfected cell culture. The results show thatOxycodone seems to cause no internalization at all in comparison to the control.
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Blackburn, Thomas P. "Renal, vascular and endocrine effects of Kappa opioid agonists." Thesis, University of Manchester, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.237570.
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Moore, Tisha T. "The effects of Kappa Opioid Agonists on Ocular Hydrodynamics." DigitalCommons@Robert W. Woodruff Library, Atlanta University Center, 2000. http://digitalcommons.auctr.edu/dissertations/3602.
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Opioid receptors have been demonstrated to modulate various functions in the eye. This research was designed to determine and compare the effects of kappa agonists on ocular hydrodynamics. Experiments were done to determine the effects of ICI 204,448 (ICI), which is not capable of penetrating the blood-brain barrier, and U-62066 (spiradoline) on: 1) intraocular pressure (IOP) and pupil diameter (PD), 2) pre- (neuronal) and postjunctional sites of action, and 3) atrial natriuretic peptide (ANP) levels in aqueous humor. Dark-adapted New Zealand White (NZW) male, rabbits were used in all experiments. IOP (mmHg) was measured by a pneumatonometer and PDs (mm) were measured by an optistick before each IOP reading. Baseline readings were taken at 1/2 and 0 hours prior to drug adminstration. Post-drug measurements were made at 1/2, 1, 2, 3, 4, and 5 hours after topical drug application. The release of norepinephrine was measured from perfused ICBs and expressed as the percent change of the control. Cyclic AMP concentrations in the ICBs and ANP levels in aqueous were quantified by radioimmunoassay techniques. The kappa antagonist, norbinaltorphimine (nor-BNI), was applied 30 minutes prior to agonist application in all experiments. ICI and spiradoline decreased IOP in a dose-dependent manner in normal rabbits, but only spiradoline showed significant changes in PD. Both kappa agonist inhibited the release of NE from perfused ICBs. Isoproterenol-stimulated cAMP levels in ICBs were lowered by both kappa receptor agonists. ANP levels in the aqueous humor increased in response to the kappa opioid agonists. These data suggest that spiradoline and ICI lower IOP by activating kappa opioid receptors in the eye. The effect of spiradoline on PD indicates that this kappa agonist activates receptors in the eye and/or the brain. The inhibition of NE release and cAMP accumulation in the ICB, suggests pre- and postjunctional sites of action for kappa agonists. The increase of ANP levels in aqeous suggests a role for ANP in lowering IOP. If these drugs can be shown to lower IOP safely and effectively in humans, then they may be utilized in the treatment of glaucoma.
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Rimoy, Gerald Herman. "Studies on the clinical pharmacology of kappa opioid receptor agonists." Thesis, University of Nottingham, 1991. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.305134.
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Altarifi, Ahmad. "EFFECTS OF MU OPIOID RECEPTOR AGONISTS ON INTRACRANIAL SELF-STIMULATION IN THE ABSENCE AND PRESENCE OF “PAIN” IN RATS." VCU Scholars Compass, 2013. http://scholarscompass.vcu.edu/etd/518.
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Pain is a significant health problem. Mu opioid receptor agonists are used clinically as analgesics, but their use is constrained by high abuse liability. Intracranial self-stimulation (ICSS) is a preclinical behavioral procedure that has been used to assess abuse potential of opioids, and drug-induced facilitation of ICSS is interpreted as an abuse-related effect. ICSS can also be used as a behavioral baseline to detect affective dimensions of pain. Specifically, pain-related depression of ICSS can model pain-related depression of behavior and mood, and drug-induced blockade of pain-related ICSS depression can serve as a measure of affective analgesia. This dissertation used mu agonists that vary in efficacy at the mu receptor (methadone> fentanyl> morphine> hydrocodone> buprenorphine> nalbuphine) and compared their effects on ICSS in the absence (phase one) or presence (phase 2) of pain. Adult male Sprague-Dawley rats were equipped with intracranial electrodes targeting the medial forebrain bundle and trained to lever press for brain stimulation. Different frequencies of stimulation maintained a frequency-dependent increase in ICSS rates, and permitted detection of both rate-increasing and rate-decreasing treatment effects. During phase 1, medium- and high-efficacy mu agonists produced initial rate-decreasing effects, followed by abuse-related rate-increasing effects at later time points. Repeated morphine administration produced tolerance to its own rate-decreasing effects, cross-tolerance to rate-decreasing effects of other mu agonists, and enhanced expression of rate-increasing effects. Low efficacy mu agonists only produced rate-increasing effects, which were enhanced after repeated morphine. These results suggest that previous opioid exposure increases expression of abuse-related facilitation of ICSS by mu agonists regardless of efficacy. During phase 2, intraperitoneal administration of lactic acid (1.8%) served as a noxious stimulus to depress ICSS. All mu agonists blocked acid-induced depression of ICSS at doses similar to those that facilitated ICSS in the absence of pain. A higher intensity noxious stimulus (5.6 % acid) produced further depression of ICSS and reduced the antinociceptive potency of both methadone and nalbuphine. Morphine antinociception was resistant to tolerance in the assay of acid-depressed ICSS. Overall, these results provide a basis for comparing determinants of abuse-related opioid effects in the absence of pain with their affective analgesic effects in the presence of pain.
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Asghar, Muhammad Junaid. "Studies on the biased signalling of some novel delta opioid receptor agonists." Thesis, University of Nottingham, 2017. http://eprints.nottingham.ac.uk/40485/.
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The delta opioid receptor (DOR) is a G protein-coupled receptor (GPCR) which is important in the regulation of neuronal function, predominantly via coupling to heterotrimeric Gi/0 proteins. The receptor has been shown to be a potential target for the treatment of chronic pain and affective disorders. Although a large number of opioid agonists exist, their properties vary widely, at least partly due to their differential coupling to post-receptor signalling systems, a phenomenon referred to as ligand-biased signalling or functional selectivity. The aim of the current project was to examine the signalling properties of a set of established and novel DOR agonists in an attempt to identify compounds that have biased signalling profiles. It was hypothesized that DOR agonists with partial efficacy regarding β-arrestin recruitment would be less liable to induce receptor internalization and desensitization of G protein-mediated signalling than full agonists. Chinese hamster ovary (CHO) cells, stably transfected with GFP-tagged human (h)DOR and CHO-K1 and U2OS cells over-expressing hDOR were exposed to a number of novel selective DOR agonists compared with the commercially available agonists, SNC80, ADL5859 and DADLE. The compounds’ potencies and efficacies were measured in four different assay systems; 1. Inhibition of forskolin-stimulated cyclic AMP accumulation, 2. Extracellular signal-regulated kinase (ERK1/2) phosphorylation using an immunocytochemical In-cell Western (I-CW) assay, 3. β-arrestin 2 recruitment and 4. hDOR internalization. The latter two assays employed DiscoverX Enzyme Fragment Complementation technology. An attempt to develop a secreted placental alkaline phosphatase (SPAP) reporter gene assay to measure DOR-mediated cyclic AMP inhibition was not successful. All of the ligands were nearly full agonists in relation to cyclic AMP inhibition although some were less efficacious than the standard SNC80 regarding ERK1/2 activation. Their absolute potencies and rank orders of potency in inhibiting cyclic AMP and activating ERK1/2 were quite different, although both signalling systems were apparently Gi/o- protein mediated. In contrast, the agonists exhibited a full range of efficacies and potencies in both β-arrestin 2 recruitment and hDOR internalization assays and there was a significant correlation between the maximum efficacies of the compounds in the two assays. A potential relationship between β-arrestin 2 recruitment/ hDOR internalization and desensitization of agonist-induced cyclic AMP accumulation was explored. Responses to the highly arrestin-recruiting agonists SNC80 and DADLE desensitized fully after extended exposure, whereas the novel partial agonists PN6047 and OPD00003 resisted desensitization. Bias factors were calculated for the agonist set and both PN6047 and OPD00003 were found to be significantly biased towards G protein-mediated cyclic AMP inhibition. In conclusion, this study reports, for the first time, a detailed characterization of signalling bias for a set of selective DOR agonists in cells over-expressing human DORs. The findings suggest that it is potentially possible to predict wanted and unwanted properties of agonists by determining post-receptor signalling profiles in vitro which will facilitate the discovery and development of novel therapeutics based on the DOR.
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Vanderah, Todd William. "The direct and modulatory antinociceptive actions of endogenous and exogenous opioid delta agonists." Diss., The University of Arizona, 1995. http://hdl.handle.net/10150/187190.
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Opioids are responsible for a number of effects but are employed primarily as analgesics. The discovery of endogenous opioids and multiple receptors have led to a better understanding of how analgesics function, and how both opioid receptors and endogenous ligands are regulated. The hypothesis of this dissertation states that levels of endogenous enkephalins are modulated by stress, inflammation and the endogenous peptide cholecystokinin (CCK) to alter the antinociceptive efficacy of μ and, possibly, δ opioids. Endogenous enkephalin release results in either direct antinociception or synergistically enhances the antinociceptive effects of the μ agonist morphine via δ receptors. This thesis will first detail how the administration of exogenous δ compounds can enhance the antinociceptive effects of a μ agonist. Exposure of mice to a cold-water swim-stress (CWSS) paradigm resulted in direct antinociception that was attenuated by opioid antagonists. Exposure to CWSS for a limited amount of time did not produce significant antinociception, but produced a marked enhancement of morphine antinociception. This enhancement was blocked by the administration of δ antagonists and (Leu⁵) enkephalin antisera. An antisense oligodeoxynucleotide was designed from the δ opioid receptor and administered to animals. Animals treated with the δ antisense and exposed to the CWSS paradigm showed a significant decrease in antinociception. Inflammation produced in the hind-paw of the mouse significantly enhanced the antinociceptive effects of morphine that was inhibited by δ antagonists and (Leu⁵) enkephalin antisera. The administration of a selective CCK(B) antagonist, L365,260 or CCK(B) antisense, enhances the antinociceptive potency of morphine. This enhancement is attenuated by δ antagonists, (Leu⁵) enkephalin antisera, as well as exhibits a two-way cross tolerance with δ agonists. L365,260 and an "enkephalinase" inhibitor, when coadministered, produced significant antinociception that was blocked by a δ antagonist and (Leu⁵) enkephalin antisera. Using polymerase chain reaction in search of a δ opioid receptor subtype, an orphan receptor was cloned and characterized as a member of the G protein-coupled receptor family. These data suggest that stress results in the release of (Leu⁵) enkephalin that enhances the antinociceptive effects of a μ-selective agonist morphine. Release of endogenous enkephalins may be regulated by the interactions of cholecystokinin at the CCK(B)receptor. Such information may lead to appropriate use of opiates in conjunction with CCK antagonists for the management of appropriate pain states.
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Huang, Wei [Verfasser]. "Direct functional effects of opioid agonists on the isolated perfused rat heart / Wei Huang." Berlin : Medizinische Fakultät Charité - Universitätsmedizin Berlin, 2013. http://d-nb.info/1037725727/34.
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Omoniyi, Abimbola T. "The cardiovascular actions of mu and kappa opioid agonists in vivo and in vitro." Thesis, University of Surrey, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.267362.
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Moon, Hyo-Eun. "Differential G protein activation by fusion proteins between the human #delta#-opioid receptor and Gâ†iâ‚α/Gâ†oâ‚α proteins." Thesis, University of Glasgow, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.366183.
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Qian, Xinhua. "Topographical design of the message domain pharmacophore of the delta opioid agonists using designer amino acids and design of non-peptide ligand for opioid receptors." Diss., The University of Arizona, 1995. http://hdl.handle.net/10150/187062.
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A series of highly constrained tyrosine derivatives, 2',6'-dimethyl- β-methyltyrosines (TMTs), was designed and asymmetrically synthesized. Incorporation of the TMT isomers into peptide agonists of δ opioid receptors provide analogues that are highly potent and selectively for δ opioid receptors and have revealed the stereochemical requirements for recognizing opioid δ receptors. Moreover, the combination of conformational studies and pharmacological studies of the peptide analogues provided for the first time the stereochemical requirements for specifically recognizing opioid δ receptor subtypes. The biological active conformation of a highly selective and potent δ opioid agonist, ((2S,3R)-TMT¹) DPDPE, was obtained by NMR studies and computer-assisted modeling. This conformation was then further used for designing novel non-peptide opioid ligands. Thus, this study is another achievement of topographical design of peptide hormones and neurotransmitters. Practically, the results of this study can be used to develop more biological stable pharmaceuticals as strong pain reliever without causing side effects such as physical dependence, respiratory depression, etc.
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Grenald, Shaness A., and Shaness A. Grenald. "Synergistic Actions of Mu-Opioid and CB2 Receptor Agonists in Rodent Models of Acute and Chronic Pain." Diss., The University of Arizona, 2016. http://hdl.handle.net/10150/623184.
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The misuse of prescription opiates is on the rise with combination therapies (e.g. acetaminophen or NSAIDs) resulting in severe liver and kidney damage. In recent years, cannabinoid receptors have been identified as potential modulators of pain and rewarding behaviors associated with cocaine, nicotine and ethanol in preclinical models. Furthermore, activation of cannabinoid 2 (CB2) receptors on immune cells through the inhibition of monoacylglycerol lipase (MAGL), results in increased 2-arachidonylglycerol (2AG) production and analgesia in animal models. Yet, few studies have identified whether mu opioid and CB2 receptor agonists act synergistically to inhibit chronic pain while reducing unwanted side effects including reward liability, or if it could ameliorate the excruciating pain that is poorly managed with by opiates in bone cancer patients. We determined if analgesic synergy exists between the mu-opioid agonist morphine and the selective CB2 agonist, JWH015, or the inhibitor of MAGL, MJN110, in rodent models of acute and chronic inflammatory, post-operative, neuropathic, and cancer-induced bone pain (CIBP) using isobolographic analysis. We also investigated if the MOR-CB2 agonist combination decreased morphine-induced conditioned place preference (CPP) and slowing of gastrointestinal transit. Next, we examined whether JWH015 or the inhibition of MAGL decreased the release of pro-inflammatory mediators by activating nuclear factor kappa enhancer of activated B cells (NFkB), as dysregulation of NFkB is observed in various cancers. Here we show that MOR + CB2 agonism results in a significant synergistic inhibition of preclinical pain while significantly reducing opioid-induced unwanted side effects. The opioid sparing effect of CB2 receptor agonism strongly supports the advancement of a MOR-CB2 agonist combinatorial pain therapy for clinical trials.
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Wooden, Ekaphol. "Synthesis of Novel Biologically Active Peptide Analogues that are Agonists at Opioid Receptors and Antagonists at Cholecystokinin Receptors." Thesis, Tucson, Ariz. : University of Arizona, 2005. http://etd.library.arizona.edu/etd/GetFileServlet?file=file:///data1/pdf/etd/azu%5Fetd%5F1282%5F1%5Fm.pdf&type=application/pdf.
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Kren, Matthew. "The Role of Gonadal Hormones on Opioid Receptor Protein Density in Arthritic Rats." VCU Scholars Compass, 2006. http://hdl.handle.net/10156/1966.
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Duke, Marcus Alan. "The effects of kappa opioid and dopamine agonists on unconditioned behaviors and fos immunoreactivity in preweanling and adult rats." CSUSB ScholarWorks, 1996. https://scholarworks.lib.csusb.edu/etd-project/1209.
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Agnes, Richard S. "New paradigm for drug design: Design and synthesis of novel biologically active peptides that are agonists at opioid receptors and antagonists at cholecystokinin receptors." Diss., The University of Arizona, 2003. http://hdl.handle.net/10150/280340.
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We now know from genomics that many disease states lead to changes in expressed proteins (adaptation/plasticity). Therefore, drug design and discovery based on normal states and single targets often is inadequate or even counter-indicated. Therefore, the "system changes" that have occurred must be considered in any treatment for the disease. Such "systems changes" are clearly evident in neuropathic pain where opioids can actually heighten pain. In these pain states there are increased levels of neurotransmitters such as cholecystokinin (CCK) in which both the peptides and their receptors are increased in pain states. To effectively treat diseases involving "systems changes" a new paradigm for the design of compounds was proposed. In this new approach single peptide or peptidomimetic molecules are designed to interact with multiple receptor targets. For the treatment of pain, a series of linear and cyclic peptides and peptidomimetics were designed based on the overlapping pharmacophores of opioid and CCK ligands. The CCK/opioid analogues were synthesized and evaluated for their biological activities. Several of the CCK/opioid analogues were found to simultaneously interact with opioid receptors as agonists and CCK receptors as antagonists. In addition, the lead compounds have been tested in several pain models and were found to be promising in the treatment of neuropathic pain. Further, the structure-activity relationships of these novel peptides have provided new insights into the requirements for binding and bioactivity at opioid and CCK receptors, as well as the overlapping pharmacophores of CCK and enkephalin.
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LI, YINGXUE. "DESIGN, SYNTHESIS, AND CHARACTERIZATION OF HELICAL OPIOID GLYCOPEPTIDE AGONISTS: THE STUDY OF THE STRUCTURE-ACTIVITY RELATIONSHIP AND TRANSPORT OF GLYCOPEPTIDES RELATED TO BETA-ENDORPHIN AND DYNORPHIN." Diss., The University of Arizona, 2011. http://hdl.handle.net/10150/203033.
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Structure-activity relationships (SAR) of opioid peptide analogues related to endorphin or dynorphin have provided rational and powerful approaches toward the design of peptide therapeutics. A series of glycosylated β-endorphin analogues were designed by modifying the N-terminal “message domain,” the C-terminal “address domain,” and the “linkage domain” between the two, and by altering the intrinsic helix stability of the amphipathic helix that comprises the “address domain.” Further changes were accomplished by altering the charged groups on the side chains of the “address region.” The unglycosylated peptide homologues and variations of the saccharide moieties (monosaccharides vs disaccharides) were also studied. The β- endorphin glycopeptide analogue ¹Tyr- ᵐD-Thr- ³Gly- ⁴Phe- ⁵Leu- ᴸPro- ⁷Asn- ⁸Leu- ʰAib ᶜGlu- ᶜLys- ʰAla- ¹³Leu- ᶜLys-¹⁵Ser[β-O-Glucose]- ¹⁶Leu-NH2, was modified at the indicated positions (m, h, c), and in collaboration with the Bidlack Lab at the Rochester Medical Center, binding affinities Kᵢ were measured using human opioid receptors expressed in CHO cells. All the peptides and glycopeptides were panagonists, showing low nanomolar affinity for the μ, δ and κ-opioid receptors. Helix stability was varied by substituting ʰAib, ʰAla, and ʰGly, which altered membrane affinity, which was correlated with helix stability. Charges on the address side chains were varied by substituting ᶜAsn, ᶜGlu, and ᶜLys. The 15Ser residue bore either a β- Lactoside, a β-D-glucoside or was unglycosylated. These peptides and glycopeptides were studied by circular dichroism (CD) and by 2D-NMR in H₂O buffer (pH = 5.5), in 30% trifluoroethanol in H₂O, and in H₂O containing SDS micelles as a model for biological membranes. In H₂O the glycopeptides and peptides showed only nascent helix behavior and random coil conformations. Chemical Shift Indices (CSI) and nuclear Overhauser effects (NOE) confirmed the helical nature of the “address domains” in the presence of SDS micelles (membrane mimics). Detailed backbone conformations were determined using distance constraints provided by NOE volumes. Based on the CD experiments, most of the β-endorphin analogues showed substantial amounts of helicity in the presence of membrane bilayer models. Several glycopeptides demonstrated penetration of the Blood Brain Barrier (BBB), and produced potent antinociceptive effects in mice after intravenous (i.v.) injection. The amphipathic address domain played a major role in BBB penetration, as reflected by the i.v. activities. The linker also had profound effects on the SAR, and it was possible to produce antinociceptive glycopeptides. In summary, we suggest that this biousian nature is essential for glycopeptides to maintain bioactivities, and the longer, more flexible linkages GABA and DAVA were able to mediate two interactions having lower energy, one interaction between the message segment and opioid receptor’s binding pocket, and another one between the address segment and the cell membrane, to result in higher binding affinities to all three opioid receptors, and significantly increasing analgesia after both i.c.v and i.v. administration. The cyclic linkers restricted D- and L-Pro on the orientation of message segment, relative to the membrane.
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Sousa, Samuel dos Santos [UNESP]. "Infusão contínua intravenosa de cloridrato de xilazina associada ou não à meperidina em jumentos nordestinos (Equus asinus)." Universidade Estadual Paulista (UNESP), 2016. http://hdl.handle.net/11449/144726.
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Existem poucos protocolos para a contenção e sedação de jumentos . Os agonistas alfa-2 são os fármacos mais amplamente administrados e é sabido que essa classe de fármacos pode produzir alguns efeitos deletérios no sistema cardiorrespiratório do animal. Os fármacos da classe dos opioides vêem ganhando espaço na prática anestésica com asininos, pois esses fármacos são utilizados como uma alternativa para a sedação desses animais. Além de produzirem certo grau de sedação, possuem característica analgésica, sem promover efeitos adversos. Na literatura pesquisada não foi encontrado, nenhum estudo sobre o uso associado de xilazina em infusão contínua com meperidina e seus efeitos hemodinâmicos nos muares. Diante deste exposto, objetivou-se estudar os efeitos da associação da infusão contínua da xilazina com bollus intramuscular de meperidina como protocolo de sedação em jumentos. Para tal, foram utilizados seis jumentos, SRD, sendo um macho e cinco fêmeas, com peso médio de 141±23 kg. Os animais foram submetidos a três protocolos experimentais dividos em três grupos, Grupo A: infusão contínua intravenosa de 1,1 mg/kg/hora de xilazina a solução salina por via intramuscular; Grupo B: infusão contínua intravenosa de 0,8 mg/kg/hora de xilazina e solução salina por via intramuscular e Grupo C: infusão contínua intravenosa de 0,8 mg/kg/hora de xilazina e 4 mg/kg de meperidina por via intramuscular. Foi observado redução na frequência respiratória, pressão arterial sistólica nos animais do grupo A e C, diminuição da pressão arterial diastólica e média em todos os grupos. Foi observada redução na altura da cabeça em todos os grupos. A associação da meperidina com xilazina em infusão contínua não provocou alterações cardiorrespiratórias significativas e produziu grau de sedação satisfatório
To the present, there has been few descriptions of anesthetic protocol for restraint and sedation in donkey (Equus asinus). Alpha-2-agonists are widely administered class of drugs. Known to produce some deleterious effects over the cardiopulmonary system. The use of opioids in donkeys has sained popularity anesthetic practicioners, since these drugs are used as an alternative sedative with analgesic characteristics with minimal side effects. To our knowledge, there has not been study evaluating the effects of the association of continuous rate infusion of xilazine with meperidine given intramuscularly over the cardiovascular parameters of donkeys. Therefore, the objective of our study evaluate was to the capacity of sedation and the cardiorespiratory implications of the anesthetic association in donkeys. In order to performe the study, six mixed breed, one male and five females, were used. The average weight has 141 ± 23 kg. The animals were subjected to three experimental protocols. Group A: Continuous intravenous infusion of 1.1 mg / kg / hour of xylazine and saline solution intramuscularly; Group B: Continuous intravenous infusion of 0.8 mg / kg / hour of xylazine and saline solution intramuscularly and Group C: continuous intravenous infusion of 0.8 mg / kg / hour of xylazine and 4 mg / kg of meperidine intramuscularly. Respiratory rate and systolic blood pressure decreased in animals of group A and C. While diastolic blood pressure and mean arterial pressure decreased in all three groups. Head Height lowered following treatment in all groups. The combination of meperidine with continuous rate infusion of xylazine did not cause significant cardiorespiratory implications and produced satisfactory degree of sedation.
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Guilhen, Rafael Costa. "Detomidina isolada e associada à morfina e à metadona para abordagem da cavidade oral em equinos: efeitos sedativos, antinociceptivos e cardiorrespiratórios." Universidade do Oeste Paulista, 2011. http://bdtd.unoeste.br:8080/tede/handle/tede/253.
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Previous issue date: 2011-09-29This study aimed to evaluate the sedative, antinociceptive and cardiopulmonary effects of detomidine alone and in combination with morphine or methadone to the oral cavity approach. Six adult mares were evaluated using a crossover design with at least 7 days between treatments. All the horses were medicated with detomidine (20µg/kg, IV), detomidine (10µg/kg, IV) in combination with morphine (0,1mg/kg, IV) or methadone (0,1mg/kg, IV). Behaviors alteration, sedation degree, oral cavity sensibility, muscle tone of tongue, heart rate, mean arterial blood pressure, arterial blood gases were investigated during 120 minutes. The parametric data were analyzed with ANOVA and Tukey s test, and non parametric data were analyzed with Kruskall-Wallis and Fridman s test with post-Dunn test (P<0,05). In all the treatment groups, the maximum sedative effect was observed between 5 and 60 minutes after drugs administration. The must sedative effect was observed in detomidine horses treated. Respiratory stability was observed in all the groups, with more pronounced cardiovascular changes in DET group. It was concluded that all treatments were satisfactory for oral cavity approach. However, the combination of opioids did not potentiate the sedative effect and, neither increased or prolonged the antinoceptive effect mediate by detomidine.
Objetivou-se avaliar os efeitos sedativos, antinociceptivos e cardiorrespiratórios da administração da detomidina isolada e associada à morfina e metadona para abordagem da cavidade oral de equinos em posição quadrupedal. Foram avaliadas seis éguas, mestiças, adultas, com peso médio de 428±42kg, que foram distribuídas em delineamento de quadrado latino. Cada um dos animais foi tratado com intervalo mínimo de sete dias entre cada avaliação, sendo submetidos aos protocolos de sedação com detomidina (20g/kg, IV) (DET), detomidina (10g/kg, IV) associada a 0,1mg/kg (IV) de morfina (MORF) e detomidina (10g/kg IV) associada a 0,1mg/kg (IV) de metadona (MET). Foram avaliados, através do sistema de escore durante 120 minutos: alteração comportamental, grau de sedação, sensibilidade da cavidade oral, tônus da língua, frequência cardíaca, pressão arterial média, frequência respiratória e variáveis hemogasométricas. A estatística foi realizada com análise de variância, teste de Tukey e análise de medidas repetidas, para as variáveis paramétricas. Para as variáveis não paramétricas foram empregados os testes de Kruskall-Wallis e de Friedmanm com contrastes pelo método de Dunn (P<0,05). O efeito sedativo foi predominante entre 5 e 60 minutos após a administração dos fármacos, em todos os grupos, sendo mais pronunciado no grupo DET. A sensibilidade da cavidade oral e o tônus da língua não diferiram entre os tratamentos. Estabilidade respiratória foi observada em todos os tratamentos, com alterações cardiovasculares mais pronunciadas no grupo DET. Conclui-se que os três tratamentos permitiram a abordagem da cavidade oral, no entanto a associação dos opioides não potencializou o efeito sedativo, bem como não incrementou ou prolongou o efeito antinociceptivo mediado pela detomidina.
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ZHANG, SHENGWEN. "THE OPIOID RECEPTOR-LIKE RECEPTOR ORL1: SIGNALING AND INTERACTION WITH OPIOID RECEPTORS." University of Cincinnati / OhioLINK, 2002. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1029419843.
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Nieland, Nick. "Investigations of derivatives of 14#beta#-amino-7,8-dihydromorphinone." Thesis, University of Bristol, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.265328.
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Groer, Chad E. "Agonist-selective regulation of the mu opioid receptor by βarrestins." The Ohio State University, 2010. http://rave.ohiolink.edu/etdc/view?acc_num=osu1284396146.
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Sousa, Élen Almeida Pedreira de. "Hemodinâmica e efeitos respiratórios e sedativos da associação de detomidina e nalbufina pela via intramuscular em ovinos /." Araçatuba, 2019. http://hdl.handle.net/11449/191270.
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Orientador: Paulo Sergio Patto dos SantosResumo: Objetivou-se com este trabalho avaliar os efeitos na hemodinâmica, respiração, motilidade ruminal e sedação, da associação de detomidina e nalbufina em ovinos. Foram utilizados 8 ovinos hígidos, jovens, fêmeas ou machos, pesando 54,85 ± 20,31kg. Foi instalado na veia jugular esquerda um introdutor e, posteriormente, posicionado um cateter de Swan-Ganz com a extremidade distal alocada no lumen da artéria pulmonar. Foi administrado pela via intramuscular detomidina (10μg/kg) associado a nalbufina (0,1mg/kg). Foram avaliadas FC, PAS, PAD, PAM, PVC, PAPm, IC, IS, IRVS, FR, pH, PaO2, PaCO2, HCO3, TC, sedação e motilidade ruminal antes do início da administração dos fármacos (MB) e a cada quinze minutos após a aplicação durante sessenta minutos (M15, M30, M45 e M60). Houve redução do IC, FR e aumento da PAS, PAPm, temperatura central, PaCO2 e HCO3 após administração dos fármacos. A sedação foi considerada satisfatória durante 45 minutos. Com os resultados obtidos neste estudo, conclui-se que a neuroleptoanalgesia promovida pela associação de detomidina e nalbufina em ovinos, nas doses utilizadas, promove sedação satisfatória. As alterações hemodinâmicas, respiratórias e na motilidade ruminal observadas podem ser bem toleradas por animais sadios.
Abstract: The aim of this study was to evaluate the effects on hemodynamics, respiration, ruminal motility and sedation of the combination of detomidine and nalbuphine in sheep. Were used eight healthy young, female or male sheep, weighing 54.85 ± 20.31kg. A Percutaneous Sheath Introducer was placed in the left jugular vein and then a Swan-Ganz catheter was positioned with the distal port allocated to the lumen of the pulmonary artery. Association of detomidine (10µg/kg) and nalbuphine (0,1mg/kg) was administered intramuscular. HR, SAP, DAP, MAP, CVP, MPAP, CI, SI, SVRI, RR, pH, PaO2, PaCO2, HCO3, CT, sedation and ruminal motility before drug administration (MB) and at each fifteen minutes after application for sixty minutes (M15, M30, M45 and M60). There was a reduction in CI, RR and increase in SAP, mPAP, CT, PaCO2 and HCO3 after drug administration. Sedation was considered satisfactory for 45 minutes. The results of this study allowed us to conclude that neuroleptoanalgesia promoted by the association of detomidine and nalbuphine in sheep at the doses used, promotes satisfactory sedation for short procedures. The hemodynamic, respiratory and ruminal motility changes observed can be well tolerated by healthy animals.
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Rooney, K. F. "Studies on dopamine and opioid receptor subtypes : Their interactions in the C.N.S." Thesis, Cardiff University, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.379197.
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Lui, Wan Thomas. "Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H /." View the Table of Contents & Abstract, 2007. http://sunzi.lib.hku.hk/hkuto/record/B38284157.
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Hayward, Neil James. "Studies on the neuroprotective action of the kappa-opioid agonist enadoline." Thesis, University of Cambridge, 1993. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.307986.
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Cooke, Alexandra Eleanor. "Molecular mechanisms of agonist-induced trafficking of the μ-opioid receptor." Thesis, University of Bristol, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.653070.
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Mu-opioid receptor (MOPr) agonists such as morphine are amongst the most important therapies for the acute relief of moderate to severe pain. However, their clinical efficacy is often compromised due to considerable inter-individual variability, the associated side effects and the development of tolerance and dependence. Numerous molecular mechanisms have been proposed to mediate tolerance to opioids. Although a definitive mechanism remains to be elucidated, desensitization, internalization and resensitization of the MOPr have all been repeatedly implicated as contributing factors. Like most G protein-coupled receptors (GPCRs), MOPr activity is tightly regulated by rapid desensitization and resensitization in response to activation by high efficacy opioid agonists. In contrast, morphine is typically reported to induce little or no acute desensitization or internalization. Howev~r, repeated or chronic administration of morphine results in considerable tolerance that is often greater than that induced by highly efficacious opioids. Despite intensive research into the regulation of the MOPr at the molecular, cellular and systems levels, much still remains to be learned about the mechanisms that underlie tolerance to opioids. The aim of this thesis was to investigate agonist-induced MOPr trafficking at the molecular and cellular level and its relationship to cellular morphine tolerance.
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Lui, Wan Thomas, and 雷雲. "Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2007. http://hub.hku.hk/bib/B45011345.
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Glück, Laura. "Einfluss der Agonist-selektiven Phosphorylierung des μ-Opioid-Rezeptors auf die Antinozizeption und das Suchtverhalten nach Opioid-Applikation." Diss., Ludwig-Maximilians-Universität München, 2014. http://nbn-resolving.de/urn:nbn:de:bvb:19-169154.
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Poon, Wai-hei. "The induction of cellular stress responses by specific Kappa-opioid receptor agonist." Click to view the E-thesis via HKUTO, 2004. http://sunzi.lib.hku.hk/hkuto/record/B31473921.
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Poon, Wai-hei, and 潘偉曦. "The induction of cellular stress responses by specific Kappa-opioid receptor agonist." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2004. http://hub.hku.hk/bib/B31473921.
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Capeyrou, Régine. "Relations structure-fonctions du recepteur opioide de type mu : mecanismes moleculaires impliques dans les effets a long terme des agonistes opioides." Toulouse 3, 1997. http://www.theses.fr/1997TOU30292.
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Galzi, Jean-Luc. "Synthese de sondes photoactivables et marquage irreversible du recepteur des opioides." Université Louis Pasteur (Strasbourg) (1971-2008), 1987. http://www.theses.fr/1987STR13114.
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Wood, Michael D. "Role of k-opioid receptor agonist U-50,488H in consummatory successive negative contrast." Fort Worth, Tex. : Texas Christian University, 2006. http://etd.tcu.edu/etdfiles/available/etd-07262006-161404/unrestricted/wood.pdf.
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Perreault, Melissa Loretta Szechtman Henry. "Coactivation of kappa opioid receptors modulates sensitized responses to the dopamine agonist quinpirole." *McMaster only, 2006.
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Nickel, Frank. "Über die kardioprotektive Wirkung eines d-Opioid-Agonisten [Delta-Opioid-Agonisten] auf das ischämisch-reperfundierte Myokard in Abhängigkeit von freien Radikalen eine Studie an blutperfundierten, isolierten Kaninchenherzen /." [S.l. : s.n.], 2002. http://deposit.ddb.de/cgi-bin/dokserv?idn=966043758.
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Glück, Laura [Verfasser], and Hermann [Akademischer Betreuer] Ammer. "Einfluss der Agonist-selektiven Phosphorylierung des μ-Opioid-Rezeptors auf die Antinozizeption und das Suchtverhalten nach Opioid-Applikation / Laura Glück. Betreuer: Hermann Ammer." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2014. http://d-nb.info/1051776996/34.
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Rutten, Mikal R. "Post treatment with the novel Deltorphin-E, a delta2 opioid receptor agonist, increases recovery and survival following severe hemorrhagic shock in behaving rats." Laramie, Wyo. : University of Wyoming, 2007. http://proquest.umi.com/pqdweb?did=1313914351&sid=1&Fmt=2&clientId=18949&RQT=309&VName=PQD.
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Von, Uexkull Guldenband Alexandra. "Dependence and tolerance in the mouse and guinea pig ileum : interaction between purinoceptor agonists and opioids." Thesis, King's College London (University of London), 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.363470.
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Ochalek, Taylor Anne. "Examining sucrose subjective response among individuals with opioid use disorder." ScholarWorks @ UVM, 2020. https://scholarworks.uvm.edu/graddis/1185.
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Aims: Opioid use disorder (OUD) is associated with significant morbidity and mortality, and opioid agonist treatment (OAT) with methadone or buprenorphine represents the most efficacious treatment. However, data suggest that chronic administration of opioids may be associated with significant weight gain, possibly by altering an organism’s perception of and preference for sweet foods. The primary aim of this laboratory study was to rigorously examine sucrose subjective response among adults receiving OAT and a comparison sample without OUD. As secondary outcomes, we also sought to compare the groups on additional baseline characteristics that may influence subjective sucrose response and weight gain during treatment.
Methods: Participants were 40 adults receiving treatment for OUD (OUD+) and a comparison sample of 40 adults without OUD (OUD-). All participants completed an initial screening visit that included questionnaires on eating behaviors, diet and nutrition, recent substance use, and measurement of body mass index. Eligible participants completed two, same-day outpatient laboratory sessions during which they sampled six experimenter-administered concentrations of sucrose solution (0, 0.1, 0.25, 0.5, 0.75, and 1.0M in distilled water) each three times under double-blind counterbalanced conditions. Following each exposure, participants rated the pleasantness and intensity of each sample using 100-point visual analog scales.
Results: OUD+ participants rated sucrose solutions as less pleasant than OUD- participants (p<0.001). However, this effect was limited to the three lowest sucrose concentrations (0, 0.1, 0.25M), and at higher concentrations there were no group differences. There were no between-group differences on ratings of intensity (p=0.35). Given these baseline group differences in placebo (0M) responding, sucrose response was also examined in terms of change from baseline. In this analysis, there was a significant group effect, with a higher magnitude of change in pleasantness ratings and a lower magnitude of change in intensity ratings from 0M in OUD+ vs. OUD- participants (p’s<0.05). With regard to baseline characteristics that may influence sucrose response and eating behavior more generally, the OUD+ group had a higher prevalence of obesity, food insecurity, unhealthy eating behaviors, high sugar consumption, and nutrition knowledge deficits compared to the OUD- group (p’s<0.05).
Conclusion: Data from preclinical and clinical research have suggested that opioid agonist medications may enhance subjective response to sweet flavors. In the present study, OUD+ participants exhibited a higher magnitude of change in pleasantness ratings from placebo compared to OUD- participants. However, this effect was largely driven by pronounced group differences in perceived pleasantness of essentially unsweet solutions. On the outcome of sucrose intensity, findings were more mixed with no consistent differences between OUD+ and OUD- participants. In contrast, group differences were far more pronounced in participants’ daily eating behaviors and nutrition knowledge, with OUD+ participants presenting with a consistently more severe profile. These data highlight the significant risk factors experienced by OUD+ individuals that extend beyond drug-related risks and may inform future scientific and clinical efforts to improve health outcomes in this vulnerable population.
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Melbostad, Heidi S. "Comparing Family Planning Knowledge Among Females and Males Receiving Opioid Agonist Treatment or Seeking Primary Care Services." ScholarWorks @ UVM, 2019. https://scholarworks.uvm.edu/graddis/1137.
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Background: Approximately 70% of US adults currently receiving opioid agonist treatment (OAT) for opioid use disorder are of reproductive age. Among women receiving OAT at risk of having an unintended pregnancy, typically less than half report any current contraceptive use compared to 90% in the general population. In addition, the rate of unintended pregnancy among women receiving OAT is disproportionately higher than the general population (~80% vs. 45%, respectively). Lack of knowledge about family planning may be contributing to decreased rates of contraceptive use and increased rates of unintended pregnancy among women receiving OAT.
Method: Participants were a convenience sample of women and men receiving OAT or a comparison group receiving primary care (PC) services. Family planning knowledge was assessed with the recently validated Contraceptive Knowledge Assessment (CKA), a self-administered 25-question multiple-choice survey. A two-way ANOVA, with fixed factors (i.e. patient sample and sex), compared the total number of correct responses for all questions and five more specific content areas (p<.05).
Results: Overall, 332 participants completed this survey. The mean percent of total correct responses was significantly lower in the OAT sample (n=167) compared to the PC sample (n=165), 47% vs. 53% correct, respectively (p<.001) or approximately 1.5 questions less. The mean percent of correct responses in four of the five content areas was also lower among the OAT sample compared to the PC sample (ps<.01). The mean percent of total correct responses was significantly higher among women (n=169) than men (n=163), 56% vs. 44% correct, respectively (p<.0001) or approximately 3 questions more. The percent of correct responses in four of the five content areas was also higher among women than men (ps<.01).
Conclusion: Given the substantial discrepancy in rates of contraceptive use and unintended pregnancy between individuals receiving OAT and the general population, it is somewhat unexpected that individuals receiving OAT did not have lower levels of family planning knowledge, although patients in both samples only answered approximately 50% of the questions correctly. Results from the present study suggest deficits in family planning knowledge, while statistically significant, may be less clinically so. Overall, lack of family planning knowledge is likely only playing a small role in population differences in contraceptive use and unintended pregnancy and interventions aimed at decreasing these differences will need to address other barriers to accessing family planning services and utilizing contraception in this population.
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Leinaar, Edward, Billy Brooks, Leigh Johnson, and Arshman Alamian. "Perceived Barriers to Contraceptive Access and Acceptance Among Reproductive-Aged Women Receiving Opioid Agonist Therapy in Northeast Tennessee." Digital Commons @ East Tennessee State University, 2020. https://dc.etsu.edu/etsu-works/8152.
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strong>Objectives: Women with substance use disorders experience unique challenges to contraceptive obtainment and user-dependent method adherence, contributing to higher than average rates of unintended pregnancy. This study estimated the prevalence of barriers to contraception and their associations with contraceptive use and unwanted pregnancies among women receiving opioid agonist therapy (OAT) in northeast Tennessee.
Methods: A cross-sectional survey was piloted among female patients aged 18 to 55 years from 2 OAT clinics. Logistic regression was used to evaluate associations between contraceptive barriers and current contraceptive use and previous unwanted pregnancies among women receiving OAT.
Results: Of 91 participants, most experienced previous pregnancies (97.8%), with more than half reporting unwanted pregnancies (52.8%). Although 60% expressed a strong desire to avoid pregnancy, ambivalence toward becoming pregnant was common (30.0%). Most experienced ≥1 barriers to contraceptive use or obtainment (75.8%), the most prevalent being aversion to adverse effects (53.8%), healthcare provider stigmatization (30.7%), scheduled appointment compliance (30.3%), and prohibitive cost (25.0%). Experience of any contraceptive barrier (adjusted odds ratio [AOR] 8.64, 95% confidence interval [CI] 2.03–36.79) and access to a contraceptive provider (AOR 5.01, 95% CI 1.34–18.77) were positively associated with current use of prescribed contraceptives, whereas prohibitive cost was negatively associated (AOR 0.28, 95% CI 0.08–0.94).
Conclusions: Although most participants desired to avoid pregnancy, ambivalence or uncertainty of pregnancy intention was common. Most experienced barriers to contraception, which were more strongly associated with previous unwanted pregnancy than current contraceptive use. The provision of long-acting reversible contraceptives and contraceptive education at OAT clinics represents an opportunity to reduce the incidence of neonatal abstinence syndrome.
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Leinaar, Edward, Leigh Johnson, Ruby Yadav, Abir Rahman, and Arshmam Alamian. "Healthcare Access, Pregnancy Intention, and Contraceptive Practices Among Reproductive-Aged Women Receiving Opioid Agonist Therapy in Northeast Tennessee." Digital Commons @ East Tennessee State University, 2019. https://dc.etsu.edu/etsu-works/8153.
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Objectives: Women with substance use disorders often experience unique challenges to obtaining contraception and adhering to user-dependent methods. As a result, this at-risk population of women tends to have higher than average rates of unintended pregnancy. The objective of this study was to describe contraceptive use, pregnancy intentions, and adequacy of access to reproductive healthcare among women receiving opioid agonist therapy in northeast Tennessee.
Methods: A cross-sectional survey was piloted among female patients aged 18 to 55 years from two opioid agonist therapy clinics. Descriptive analyses were conducted using logistic regression to evaluate the statistical significance of bivariate associations.
Results: Of 91 participants, 84% reported having health insurance, with 70% perceiving having adequate access to health care. More than half had a history of unwanted pregnancy (53%), among whom few (23.1%) reported the consistent use of contraception at time of conception. Although most desired to avoid pregnancy (90%), only 59% of women reported the current use of regular contraception. Most of those not using regular contraception believed that they were not at risk for pregnancy (54.3%).
Conclusions: Although most participants reported adequate access to health care and a desire to avoid pregnancy, few reported the consistent use of regular contraception. Furthermore, misperceptions regarding pregnancy risk were common among participants. Research is needed to identify barriers to contraceptive acceptance and causes of pregnancy risk misperceptions in this population of women at increased risk of unintended pregnancy.
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Leinaar, Edward, Billy Brooks, Leigh Johnson, and Arsham Alamian. "Perceived Barriers to Contraceptive Access and Acceptance Among Reproductive-Aged Women Receiving Opioid Agonist Therapy in Northeast Tennessee." Digital Commons @ East Tennessee State University, 2019. https://dc.etsu.edu/etsu-works/8182.
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backgroundWomen with opioid use disorder (OUD) experience unique barriers to contraception, contributing to higher than average rates of unintended pregnancy. Rates of neonatal abstinence syndrome (NAS), a drug withdrawal syndrome resulting from antenatal drug exposure, are higher in Tennessee than the nation. Few studies have quantified experience of contraceptive barriers or their associations with contraceptive use among women with OUD.
objectives This study estimated prevalence of barriers to access/acceptance of contraceptive services and their associations with current contraceptive use and unwanted pregnancy among reproductive-aged women in Northeast Tennessee receiving opioid agonist therapy (OAT).
methods A cross-sectional survey was administered to female patients aged 18-55 from two OAT clinics. Logistic regression was used to evaluate associations between contraceptive barriers and current contraceptive use and previous unwanted pregnancies.
results Of 91 participants, most were insured (84.4%), experienced at least one barrier (75.8%), and more than half reported unwanted pregnancies (52.8%). Most desired to avoid pregnancy (60.0%) or were ambivalent (30.0%). Common barriers were side effect aversion (53.8%), provider stigmatization (30.7%), appointment compliance (30.23%), and cost (25.0%). Experience of any barrier (AOR=11.6, 2.25-59.8) and access to a contraceptive provider (AOR=9.78, 1.34-71.7) were positively associated with use, while cost was negatively associated (AOR=0.27, 0.07-0.98). Eight barriers were significantly associated with unwanted pregnancies.
conclusionWhile most participants desired to avoid pregnancy, contraceptive barriers were common. Barriers were more strongly associated with previous unwanted pregnancy than current contraception. Contraceptive provision at OAT clinics may reduce incidence of unwanted pregnancy and NAS in Northeast Tennessee.
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Cornelissen, Jeremy. "Pharmacological assessment of adjuncts to enhance mu-opioid receptor agonist antinociception in male rhesus monkeys: Does one + one = three?" VCU Scholars Compass, 2019. https://scholarscompass.vcu.edu/etd/6115.
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Mu-opioid receptor (MOR) agonists are effective agents for pain management, but are also limited by a number of undesirable effects. One approach to enhance the therapeutic effects and minimize the undesirable effects of MOR agonists may be to combine MOR agonists with an adjunct targeting a different receptor system. This targeted medical approach, known as “combination therapy”, aims to augment the desired effects of the MOR agonist (i.e. antinociception) and/or diminish the undesirable deleterious side effects of the MOR agonist. This dissertation investigated the utility of this approach in an assay of thermal nociception and schedule-controlled responding in male rhesus monkeys with three aims. One aim determined the utility of N-methyl D-aspartate (NMDA) receptor antagonists to selectively enhance MOR agonist antinociception. A second identified the pharmacological determinants of antinociceptive interactions between a nociceptin opioid peptide (NOP) receptor agonist and MOR agonists. A third aim investigated the potential for fixed-proportion mixtures of a competitive MOR antagonist and MOR agonist to manipulate antinociceptive efficacy. Experimental results did not support the utility of NMDA antagonists as adjuncts to selectively enhance MOR agonist antinociception. Furthermore, the antinociceptive interactions between a NOP agonist and MOR agonists were modest and occurred under a narrow range of conditions. Finally, fixed proportion MOR antagonist-agonist mixtures were effective in manipulating antinociceptive in vivo efficacy. In conclusion, this dissertation does not provide strong empirical evidence that a combination therapy approach will result in clinically effective and selective enhancement of MOR agonist analgesia. The dissertation concludes with proposed strategies and novel preclinical methods to enhance preclinical-to-clinical translation of effective candidate analgesics.
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Torres, Chavez Karla Elena 1978. "Mecanismos envolvidos na ação anti-hiperalgésica do agonista opióide mu no tecido periférico." [s.n.], 2012. http://repositorio.unicamp.br/jspui/handle/REPOSIP/290420.
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Orientador: Carlos Amilcar ParadaTexto em português e inglês
Tese (doutorado) - Universidade Estadual de Campinas, Faculdade de Odontologia de Piracicaba
Made available in DSpace on 2018-08-20T10:16:37Z (GMT). No. of bitstreams: 1 TorresChavez_KarlaElena_D.pdf: 3048246 bytes, checksum: 47a94680eba82c1f3eb36fe7add0a488 (MD5) Previous issue date: 2012
Resumo: Os objetivos deste estudo foram: (1) Verificar se a administração local de prostaglandina E2 (PGE2) no tecido periférico aumenta o efeito anti-hiperalgésico da ativação do receptor opióide mu e se este efeito é mediado por um aumento da expressão de receptor opióide mu (2) Testar se o efeito anti-hiperalgésico da ativação do receptor opióide mu no tecido periférico está associada com a diminuição da excitabilidade das fibras-C. De acordo com o objetivo (1)... Observação: O resumo, na íntegra, poderá ser visualizado no texto completo da tese digital
Abstract: The aims of this study were:(1) To verify whether local administration of E2 prostaglandin (PGE2) in peripheral tissue increases the anti-hyperalgesic effect of mu opioid receptor activation and whether this effect is mediated by an increased expression of mu opioid receptor (2) To test if the anti-hyperalgesic effect of the activation of mu opioid receptor in peripheral tissue is associated with the decrease of C-fibers excitability. According to the objective(1)... Note: The complete abstract is available with the full electronic document
Doutorado
Fisiologia Oral
Doutor em Odontologia
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Delay-Goyet, Philippe. "Différenciation biochimique et pharmacologique des récepteurs opioides mu et delta." Paris 5, 1989. http://www.theses.fr/1989PA05P609.
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Serratore, Catherine. "Trends and Patterns in Use of Medications for Opioid Use Disorder in a Commercially Insured Population in the U.S." UKnowledge, 2019. https://uknowledge.uky.edu/pharmacy_etds/108.
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Opioid use disorder (OUD) and opioid overdose are pervasive public health problems in the U.S. Medications for opioid use disorder (MOUD) have been shown effective to reduce OUD morbidity and mortality. Two distinct approaches to MOUD are currently used: agonist therapy (methadone or buprenorphine) or antagonist therapy (naltrexone). Limited information is available about the patterns of use, adherence to therapy, and characteristics of those who use agonist vs. antagonist therapy. The objective of this study is to assess recent trends in MOUD, adherence in use of MOUD, and the characteristics of those who use agonist vs. antagonist therapy in a nationally representative population of commercially insured patients in the U.S.
This retrospective descriptive study utilized data from Truven Marketscan Commercial Claims and Encounters database from years 2011 to 2016. All individuals aged 18 years and older who have a diagnosis of OUD and utilize MOUD at any point during the study period were included. Demographic characteristics of interest included age, gender, geographic region, and type of insurance coverage. Clinical characteristics of interest included diagnosis of OUD and type of MOUD used, including extended – release naltrexone for injection, oral naltrexone, buprenorphine in combination with naloxone, and buprenorphine alone. Descriptive analyses were employed to understand utilization patterns and trends over time and proportion of days covered was used to measure adherence. Frequency and percentage are presented for categorical variables. Adherence of MOUD will be estimated by measuring proportion of days covered. As this study uses de-identified commercial health claims data, it has been determined as not human subjects research by the University of Kentucky’s Office of Research Integrity.
Agonist therapy with buprenorphine or buprenorphine/naloxone was the most common treatment, representing 75.7% of those receiving treatment. Between 2011 and 2016, the percentage of individuals receiving treatment with partial agonist therapy decreased 16.5% to 9.2%, respectively. Meanwhile, the percentage of individuals receiving treatment with antagonist treatment increased from 0.1% in 2011 to 0.3% in 2016. In the analysis of proportion of days covered, all MOUD reported a decrease at both 180 and 365 days. In the commercial population, younger female patients were more likely to be treated with injectable naltrexone. Specifically, in the North Central geographic region, commercial adult patients were more likely to be treated with buprenorphine monotherapy.
Overall, this study found a decrease in use of agonist therapy from 2011 through 2016, with an increase in use of antagonist therapy in the same time period. However, the increase in use of antagonist therapy does not fully account for the decrease in use of agonist therapy, suggesting that since 2011 many patients with OUD still remain untreated. All MOUD types were analyzed and saw a decrease in proportion of days covered, as a measure of adherence, from 2011 to 2016 putting patients at an increased risk for relapse, further complications, emergency visits, and hospitalizations. More information is needed about characteristics of patients who not only seek out treatment for OUD, but also maintain their treatment overtime.
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Dao, Thi Thanh Hà. "Conception et synthèse de macrocycles pouvant s'empiler en nanotubes supramoléculaires ou agir comme agonistes opioïde delta." Thèse, Université de Sherbrooke, 2017. http://hdl.handle.net/11143/10491.
Full textAbstract:
Cet ouvrage porte sur les macrocycles organiques. Une introduction générale sur les propriétés des macrocycles et leurs rôles dans la chimie des matériaux et le développment des médicaments est présentée en premier lieu pour expliquer notre intérêt particulier sur cette classe de molécules.
Le premier chapitre parle d’une nouvelle conception des nanotubes supramoléculaires par auto-assemblage des macrocycles de forme persistante. Nous avons exploité la capacité d’auto-assembler des différents types de cyclopeptides de squelette rigidifié en structures nanotubulaires. Cette approche a aussi été bien étudiée par plusieurs groupes de recherche de la littérature. Une caractéristique commune dans toutes ces conceptions est le besoin des fonctions amides qui sont disposées à l’intérieur du macrocycle et responsables des ponts Hydrogènes intermoléculaires pour diriger l’auto-organisation en nanotubes. Cette approche fonctionnait bien mais trouve limitée dans le cas où la structure cyclique manque des motifs (en particulier les amides) responsables de l’auto-assemblage par exemple les structures π-conjuguées. Pour ce genre de molécules, l’incorporation des longues chaînes latérales alkyles en périphérie du cycle représente la méthode habituelle pour obtenir l’empilement efficace entre les molécules. Par contre, le matériau formé présente souvent un désordre moléculaire et une faible cristallinité. Nous proposons une meilleure conception pour stimuler la croissance unidimensionnelle en ajoutant les fonctions amides susceptibles des liaisons Hydrogène intermoléculaire en périphérie du cycle. La tribenzocyclyne (TBC) est choisie comme échafaudage pour examiner cette stratégie qui n’a jamais été appliquée et rapportée sur un système cyclique pour le même objectif. L’intensité et la directionnalité des interactions Hydrogène supporteraient l’auto-organisation efficace de ces dérivés de TBC en nanotubes comme manifestée par quelques calculs semi-empiriques. De différentes générations de TBC portant des amides latéraux ont été conçues, synthétisées et discutées pour améliorer la synthèse et pouvoir obtenir l’arrangement désiré des molécules. Afin de favoriser la compréhension sur les nanotubes supramoléculaires, une introduction sur la chimie supramoléculaire, les interactions non-covalentes et les différentes approches vers les nanotubes supramoléculaires est résumée en détail.
Toujours concernant les marcocycles, le deuxième chapitre aborde la conception des nouveaux agonistes cycliques ciblant le récepteur opioïde δ (DOPr). Les résultats préliminaires obtenus par notre groupe ont permi de proposer une conformation de Leu-enképhaline (LENK), le ligand endogène activant le DOPr, qui est très probablement celle trouvée dans le site actif de DOPr. En basant sur ce modèle, nous voulons concevoir des macrocycles dont le squelette est fixé plus ou moins vers cette conformation active hypothétique en incorporant les espaceurs appropriés entre les pharmacophores. Les nouvelles molécules sont considérées comme candidats-agonistes sélectifs δ car la conception fixerait la conformation spécifique pour la liaison avec le DOPr au lieu des autres récepteurs opioïdes surtout le μ (MOPr). L’objectif à long terme de ce projet, qui est en collaboration avec le laboratoire du Professeur Louis Gendron, est d’obtenir les agonistes sélectifs δ puissants pour soulager les douleurs sévères et/ou chroniques avec les effets secondaires réduits ou éliminés. Ces effets indésirables constituent le problème majeur qui limite l’efficacité ou suspend la médication des agonistes opioïdes telles que la morphine dans le traitement de la douleur. Pour comprendre mieux l’arrivée des nouveaux macrocycles synthétisés et discutés dans ce chapitre, une introduction générale sur la douleur et les traitements actuels, les récepteurs opioïdes et leur rôle dans la modulation de la douleur est présentée en premier lieu. Les résultats préliminaires par notre groupe et les collaborations sont aussi résumées.
Finalement, une concise annexe sur l’exploration d’une nouvelle conception de nanosphères supramoléculaires est ajoutée en dernier lieu. Ces nanocapsules résulteraient de l’auto-assemblage des dérivés de corannulène portant des amides latéraux, ce qui imitent la structure de la capside sphérique chez plusieurs virus.