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1.
Eur J Pharm Sci ; 162: 105824, 2021 Jul 01.
Article in English | MEDLINE | ID: mdl-33798709

ABSTRACT

Stress is crucially related to the pathophysiology of mood disorders, including depression. Since the effectiveness and number of the current pharmacological options still presents significant limitations, research on new substances is paramount. In rodents, several findings have indicated that corticosterone administration induces the manifestation of behavioral and neurochemical aspects of depression. Recently, riparin III has shown antidepressant-like properties in trials performed on animal models. Thus, our goal was to investigate the effects of riparin III on behavioral tests, monoamines levels, oxidative stress and cytokines levels in chronic corticosterone-induced model of depression. To do this, female swiss mice were treated with subcutaneous administration of corticosterone for 22 days. In addition, for the last 10 days, riparin III or fluvoxamine were also administered per os in specific test groups. Control groups received subcutaneous saline injections or distilled water per os. At the end of the timeline, the animals were killed and their hippocampi, prefrontal cortex, and striatum dissected for neurochemical analysis. Brain changes following corticosterone administration were confirmed, and riparin III could reversed the most abnormal behavioral and neurochemical corticosterone-induced alterations. These results suggest the potential antioxidant, anti-inflammatory and antidepressant effects of riparin III after a chronic stress exposure.


Subject(s)
Depression , Pharmaceutical Preparations , Animals , Behavior, Animal , Benzamides , Corticosterone , Depression/drug therapy , Disease Models, Animal , Female , Mice , Tyramine/analogs & derivatives
2.
Behav Brain Res ; 383: 112487, 2020 04 06.
Article in English | MEDLINE | ID: mdl-31987932

ABSTRACT

Despite recent advances, current antidepressants have considerable limitations: late onset of action and the high profile of refractoriness. Biomedical research with natural products has gained growing interest in the last years, and had provide useful candidates for new antidepressants. Riparins are a group of natural alkamides obtained from Aniba riparia, which had marked neuroactive effects, mainly as antidepressant and antinociceptive agents. We made modifications of the basic structure of riparins, originating a synthetic alkamide, also known as riparin IV (RipIV). RipIV demonstrated a superior analgesic effect than its congeners and a marked antidepressant-like effect. However, the basic mechanism for the central effects of RipIV remains unknown. Here, we aimed to investigate the participation of monoaminergic neurotransmission targets in the antidepressant-like effects of RipIV. To do this, we applied a combined approach of experimental (classical pharmacology and neurochemistry) and computer-aided techniques. Our results demonstrated that RipIV presented antidepressant- and anxiolytic-like effects without modifying locomotion and motor coordination of mice. Also, RipIV increased brain monoamines and their metabolite levels. At the higher dose (100 mg/kg), RipIV increased serotonin concentrations in all studied brain areas, while at the lower one (50 mg/kg), it increased mainly dopamine and noradrenaline levels. When tested with selective receptor antagonists, RipIV antidepressant effect showed dependence of the activation of multiple targets, including D1 and D2 dopamine receptors, 5-HT2A/2, 5-HT3 receptors and α2 adrenergic receptors. Molecular docking demonstrated favorable binding conformation and affinity of RipIV to monoamine oxidase B (MAO-B), serotonin transporter (SERT), α1 receptor, D2 receptor, dopamine transporter (DAT) and at some extent GABA-A receptor. RipIV also presented a computationally predicted favorable pharmacokinetic profile. Therefore, this study demonstrated the involvement of monoaminergic targets in the mechanism of RipIV antidepressant-like action, and provide evidence of it as a promising new antidepressant.


Subject(s)
Anti-Anxiety Agents/pharmacology , Antidepressive Agents/pharmacology , Monoamine Oxidase/drug effects , Receptors, Adrenergic, alpha-2/drug effects , Receptors, Dopamine/drug effects , Receptors, Serotonin/drug effects , Tyramine/analogs & derivatives , Animals , Brain/drug effects , Brain/metabolism , Bupropion/pharmacology , Dopamine/metabolism , Dopamine Plasma Membrane Transport Proteins/drug effects , Dopamine Plasma Membrane Transport Proteins/metabolism , Fluoxetine/pharmacology , Imipramine/pharmacology , Mice , Molecular Docking Simulation , Monoamine Oxidase/metabolism , Norepinephrine/metabolism , Receptor, Serotonin, 5-HT2A/drug effects , Receptor, Serotonin, 5-HT2A/metabolism , Receptors, Adrenergic, alpha-2/metabolism , Receptors, Dopamine/metabolism , Receptors, Dopamine D1 , Receptors, Dopamine D2 , Receptors, GABA-A/drug effects , Receptors, GABA-A/metabolism , Receptors, Serotonin/metabolism , Receptors, Serotonin, 5-HT2/drug effects , Receptors, Serotonin, 5-HT2/metabolism , Receptors, Serotonin, 5-HT3/drug effects , Receptors, Serotonin, 5-HT3/metabolism , Serotonin/metabolism , Serotonin Plasma Membrane Transport Proteins/drug effects , Serotonin Plasma Membrane Transport Proteins/metabolism , Tyramine/pharmacology
3.
Rev. adm. saúde ; 16(64): 89-96, jul-set.2014.
Article in Portuguese | LILACS | ID: lil-784614

ABSTRACT

Com a Política Nacional de Medicamentos, a assistência farmacêutica (AF) tornou-se parte integrante de um conjunto de práticas voltadas para a promoção, prevenção e recuperação de saúde, tendo o medicamento como principal insumo, porém contemplando atividades que extrapolam o simples abastecimento de medicamentos, compreendendo seleção, programação, aquisição, armazenamento, distribuição, prescrição, dispensação e uso. O presente estudo tem como objetivo realizar uma revisão integrativa da literatura no sentido de fornecer um documento de atualização e compilação de dados recentes acerca da gestão da AF do Brasil nos últimos anos. Para a busca dos artigos foram consultadas as bases de dados LILACS, SciELO e MEDLINE, com os descritores “gestão da assistência farmacêutica” e “assistência farmacêutica e gestão”. Os  critérios de inclusão considerados foram: os artigos eletrônicos estarem disponíveis na íntegra, em língua portuguesa e que foram publicados no período compreendido entre 2006 e 2013. Para a coleta de dados dos artigos selecionados, foram utilizados os itens: ano, tipo de estudo, título e objetivo. Foram selecionados oito artigos científicos. Observou-se que, apesar de todos os trabalhos apresentarem objetivos diferentes dentro de uma mesma temática, todos trouxeram à tona um problema comum: a falta de estruturação adequada da AF no Brasil. Ficou evidenciado que a AF é ainda vista como um mero setor de fornecimento de medicamentos. Sugere-se, portanto, uma gestão voltada para atividades de natureza administrativa com AF voltada para o medicamento e usuário...


With the National Drug Policy, the pharmaceutical care (PC) has become an integral part of a set of practices for the promotion, prevention and health recovery, having the drug as the main ingredient, but contemplating activities that extrapolate the mere supply of drugs, including selection, programming, acquisition, storage, distribution, prescription, dispensing and use. This study has as an objective to carry out an integrative literature review in order to provide an updated document and compilation of recent data on the management of the PC in Brazil in recent years. For the search of articles were consulted the databases LILACS, SciELOand MEDLINE with the descriptors “management of pharmaceutical care” and “pharmaceutical care and management”. Inclusion criteria were: electronic articles are available in full in Portuguese and which were published in the period between 2006 and 2013. To collect the data of the selected articles, the following items were used: year, type of study, title and objective. Eight scientific articles were selected. It was observed that, despite all the articles have different objectives within the same theme, all brought to light a common problem: the lack of proper structuring of PC in Brazil. The study revealed that PC is still seen as a mere drug supply sector. Therefore, it is suggested the management focused on administrative activities with PC facing the drug and user...


Subject(s)
Humans , Male , Female , Drug Storage , Health Information Systems , National Drug Policy , Pharmaceutical Services , Pharmaceutical Preparations/supply & distribution , Clinical Protocols , Health Management , Health Promotion , Health Services , Organization and Administration , Public Policy
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