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Multi-drug resistance gene (MDR1) and opioid analgesia in horses Ciência Rural
Natalini,Cláudio Corrêa; Cunha,Anderson Fávaro da; Linardi,Renata Lehn.
Opioid absorption in the intestinal tract as well as its effects in the central nervous system is modulated by the P-glycoprotein (P-gp) encoded in the Multi-drug Resistance gene (MDR1) also named ATP-binding cassete, subfamily B, member 1 (ABCB1). This MDR1 gene acts as a selective pump. The expression of this protein in humans and rodents inhibits cellular uptake of substrate opioids. The presence of the intestinal iso-enzyme CYP3A4 associated with MDR1 gene decreases the opioid analgesic activity due to an increase in intestinal metabolism, with a predicted intestinal first pass extraction around 20% which significantly influences the oral availability of opioids. In the central nervous system, P-gp expression decreases opioid neuronal uptake...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Molecular biology; Opioids; Equine; Gene; MDR1; ABCB1; Analgesia.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100055
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Identification of multi-drug resistance gene (MDR1) in equine ileum Ciência Rural
Natalini,Cláudio Corrêa; Linardi,Renata Lehn.
P-glycoprotein (P-gp) is a membrane transporter encoded in the Multi-drug Resistance (MDR1) gene expressed in several normal tissues and over expressed in tumor cells. P-gp was already identified in different species but not yet in equine. MDR1 gene and P-gp are able to interfere with bioavailability and disposition of several drugs, altering pharmacokinetic and pharmacodinamic of drugs. The presence of the MDR1 and P-gp in the central nervous system blocks the entry of certain drugs in this tissue and reduces drug absorption and enhances drug elimination when P-gp and MDR1 are presented in the gastrointestinal tract. This study showed that the MDR1 gene is present in equine ileum. Future studies on the impact of the P-glycoprotein encoded gene MDR1 on...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Molecular biology; Opioids; Equine; Gene; MDR1; ABCB1.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100048
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Confecção de um modelo experimental in vitro do espaço subaracnóide eqüino para teste de opióides hiperbáricos Ciência Rural
Polydoro,Alexandre da Silva; Raiser,Alceu Gaspar; Natalini,Cláudio Corrêa; Linardi,Renata Lehn.
Com o objetivo de avaliar as características de distribuição de agentes hiperbáricos no líquido cérebro-espinhal (LCE) eqüino, é apresentado um modelo in vitro do espaço subaracnóide confeccionado em policloreto de vinila (PVC) transparente, no qual se adaptou um cateter para a infusão contínua de glicose a 10%, morfina hiperbárica, buprenorfina hiperbárica e metadona hiperbárica marcadas com azul de metileno para permitir a visualização da distribuição destas substâncias no LCE. Avaliaram-se a distância alcançada pelos diferentes agentes minuto a minuto e a forma de distribuição dos mesmos. Todas as substâncias testadas mostraram comportamento de distribuição vertical a partir da extremidade do cateter, quando se deu o início da migração cranial no LCE,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Modelo experimental; Subaracnóide; Anestesia; Hiperbárico.
Ano: 2008 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782008000200014
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First report on spinal hyperbaric opioids in horses Ciência Rural
Polydoro,Alexandre da Silva; Natalini,Cláudio Corrêa; Linardi,Renata Lehn.
This study is the first to report the use of spinal hyperbaric opioids in horses injected through a lumbar-sacral subarachnoid catheter. The injection of hyperbaric subarachnoid morphine and methadone produced short term intense analgesia over the dermatomes of the perineal, sacral, lumbar, and thoracic areas without cardiorespiratory depression, ataxia or central nervous system excitement. The technique involves the use of 10% dextrose as a hyperbaric solvent producing an average hyperbaric solution with a specific gravity of 1030. The use of spinal hyperbaric opioids in horses can be recommended for short term moderate to severe pain management in this species.
Tipo: Info:eu-repo/semantics/article Palavras-chave: Analgesia; Equine; Morphine; Methadone; Buprenorphine; Hyperbaric.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100051
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Multi-drug resistance (MDR1) gene and P-glycoprotein influence on pharmacokinetic and pharmacodymanic of therapeutic drugs Ciência Rural
Linardi,Renata Lehn; Natalini,Cláudio Corrêa.
(MDR1) gene expressed in tumor cells and also in several normal tissues, such as intestine, liver, kidney, blood-brain barrier, spinal cord, and placenta. P-gp has been identified in mice, rat, bovine, monkey, rodents, and human beings and has been receiving a particular clinical relevance because this protein expression limits brain access and intestinal absorption of many drugs. This protein plays a role as a protective barrier against a wide variety of substrates, avoiding drug entry into the central nervous system. P-glycoprotein also interferes with drug bioavailability and disposition, including absorption, distribution, metabolization, and excretion, influencing pharmacokinetic and pharmacodynamic of drugs. Modulation of P-gp may help the efficacy...
Tipo: Info:eu-repo/semantics/article Palavras-chave: MDR1 gene; P-glycoprotein; Therapeutics; Pharmacology.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100056
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Subarachnoidally administered hyperbaric morphine, buprenorphine, methadone, and 10% dextrose on cardiopulmonary function and behavior in horses Ciência Rural
Natalini,Cláudio Corrêa; Linardi,Renata Lehn; Polydoro,Alexandre da Silva.
The study was done to compare the heart rate, arterial blood pressure, arterial blood gases, respiratory rate, body temperature, and behavior after subarachnoid administration of hyperbaric morphine (MorphineD10), buprenorphine (BuprenorphineD10), methadone (Methadone D10), and 10% dextrose (D10) in conscious horses. Six adult horses were studied. Treatments were administered into the lombo-sacral subarachnoid space through an epidural catheter, MorphineD10 at 0.01mg kg-1, BuprenorphineD10 at 0.001mg kg-1, MethadoneD10 at 0.01mg kg-1, and 10% dextrose as a control group. The results showed that there are minimum changes in heart and respiratory rate, blood gases, blood pressure, and body temperature after subarachnoid administration of hyperbaric opioids...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Morphine; Methadone; Buprenorphine; Hyperbaric opioid; Subarachnoid.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000500015
Registros recuperados: 6
Primeira ... 1 ... Última
 

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