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Farmacocinética clínica y farmacodinamia de la dexmedetomidina.
Clinical Pharmacokinetics and Pharmacodynamics of Dexmedetomidine.
Abstract
Dexmedetomidine is an α2-adrenoceptor agonist with sedative, anxiolytic, sympatholytic, and analgesic-sparing effects, and minimal depression of respiratory function. It is potent and highly selective for α2-receptors with an α2:α1 ratio of 1620:1. Hemodynamic effects, which include transient hypertension, bradycardia, and hypotension, result from the drug's peripheral vasoconstrictive and sympatholytic properties. Dexmedetomidine exerts its hypnotic action through activation of central pre- and postsynaptic α2-receptors in the locus coeruleus, thereby inducting a state of unconsciousness similar to natural sleep, with the unique aspect that patients remain easily rousable and cooperative. Dexmedetomidine is rapidly distributed and is mainly hepatically metabolized into inactive metabolites by glucuronidation and hydroxylation. A high inter-individual variability in dexmedetomidine pharmacokinetics has been described, especially in the intensive care unit population. In recent years, multiple pharmacokinetic non-compartmental analyses as well as population pharmacokinetic studies have been performed. Body size, hepatic impairment, and presumably plasma albumin and cardiac output have a significant impact on dexmedetomidinepharmacokinetics. Results regarding other covariates remain inconclusive and warrant further research. Although initially approved for intravenous use for up to 24 h in the adult intensive care unit population only, applications of dexmedetomidine in clinical practice have been widened over the past few years. Procedural sedation with dexmedetomidine was additionally approved by the US Food and Drug Administration in 2003 and dexmedetomidine has appeared useful in multiple off-label applications such as pediatric sedation, intranasal or buccal administration, and use as an adjuvant to local analgesia techniques.
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Utilidad de la dexmedetomidina en diversos contextos en la medicina actual
Dr. Orlando Carrillo-Torres,* Dra. María Guadalupe Pliego-Sánchez,* Dra. María Mónica Gallegos-Allier,* Dra. Lourdes Carmen Santacruz-Martínez*
Rev Mex Anestesiol Vol. 37. No. 1 Enero-Marzo 2014 pp 27-34
Resumen
En los últimos años se han creado fármacos para lograr una adecuada sedación y analgesia en los pacientes antes, durante y después de las intervenciones mé- dicas. Entre estos medicamentos se encuentra la dexmedetomidina, un fármaco altamente selectivo a los receptores alfa-2, que logra, en dosificación adecuada, analgesia, sedación y simpaticolisis sin efectos adversos importantes. Este fármaco se ha utilizado ampliamente en la terapia intensiva, para lo cual fue ideado, pero también se ha utilizado para diversos procedimientos anestesiológicos, ya sean en generales y regionales, así como para sedaciones superficiales y profundas, tanto en los adultos como en la población pediátrica. En esta revisión se abarcarán las generalidades de la dexmedetomidina, así como su uso en las diferentes especialidades hasta el día de hoy. Palabras clave: Alfa-2 agonista, dexmedetomidina, sedación, analgesia.
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Dexmedetomidina: Rol Actual en Anestesia y Cuidados Intensivos
Joana Afonso 1, Flávio Reis 2 Resumen: Afonso J, Reis F
Resumen
Justificativa y objetivos: Actualizar y analizar nuevamente la aplicación de la dexmedetomidina en la anestesia y en los cuidados intensivos. Este trabajo es una revisión bastante exhaustiva de los usos clínicos, farmacología, farmacocinética, mecanismo de acción, y de los efectos adversos de la dexmedetomidina. Contenido: El uso efectivo de los agentes sedativo-hipnóticos y analgésicos, forma parte integral de la comodidad y de la seguridad de los pacientes. La dexmedetomidina es un potente y altamente selectivo agonista de los adrenoceptores α-2 con propiedades simpaticolíticas, sedativas, amnésicas y analgésicas, que se ha venido describiendo como un adyuvante útil y seguro en varias aplicaciones clínicas. Proporciona una "sedación conciente" única, analgésica, y sin depresión respiratoria. Sus usos más comunes ya analizados, incluyen la sedación en la Unidad de Cuidados Intensivos (UCI) (adulta y pediátrica), en Urgencias, anestesia regional y general, neurocirugía, sedación para procedimientos pediá- tricos, intubación por fibra óptica en enfermos despiertos, cirugía cardíaca y cirugía bariátrica. Conclusiones: La dexmedetomidina ofrece la capacidad única de suministrar sedación y analgesia sin depresión respiratoria. Es un agente nuevo con un gran margen de seguridad, excelente capacidad sedativa y moderadas propiedades analgésicas. Aunque su amplio uso sea hoy por hoy, para pacientes de unidades de cuidados intensivos quirúrgicos y no quirúrgicos, la dexmedetomidina parece tener aplicaciones futuras promisorias en las áreas de neuroprotección, cardioprotección y renoprotección. Aunque de todas formas, son necesarios más estudios detallados para definir su rol como sedativo en los enfermos criticos, neuroquirúrgicos y pediátricos, como adyuvante en la anestesia y como sedativo durante los procedimientos. Descriptores: ANALGÉSICOS; Dexmedetomidina; ANALGESIA; ANESTESIA; Cuidados intensivos
Dexmedetomidine: current role in anesthesia and intensive care.
Abstract
BACKGROUND AND OBJECTIVES: To update and review the application of dexmedetomidine in anesthesia and intensive care. This study is a comprehensive review of clinical uses, pharmacology, pharmacokinetics, mechanism of action and adverse effects of dexmedetomidine.CONTENT: The effective use of sedative-hypnotic agents and analgesics is an integral part of comfort and safety of patients. Dexmedetomidine is a potent and highly selective α-2 adrenoceptor agonist with sympatholytic, sedative, amnestic, and analgesic properties, which has been described as a useful and safe adjunct in many clinical applications. It provides a unique "conscious sedation", analgesia, without respiratory depression. The current reviewed uses include sedation at Intensive Care Unit-ICU (both adult and pediatric), emergency department, regional and general anesthesia, neurosurgery, sedation for pediatric procedures, awake fiber-optic intubation, cardiac surgery and bariatric surgery. CONCLUSIONS: Dexmedetomidine offers a unique ability of providing both sedation and analgesia without respiratory depression. It is a new agent with a wide safety margin, excellent sedative capacity and moderate analgesic properties. Although its wide use is currently in patients of surgical and non-surgical intensive care units, dexmedetomidine seems to have promising future applications in neuroprotection, cardioprotection and renoprotection. More detailed studies are required to define its role as sedative in critical, neurosurgical and pediatric patients, as anesthesia adjunct and sedative during procedures.
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Dexmedetomidina: un adyuvante que se adentra en la práctica clínica.
Dexmedetomidine: an adjuvant making large inroads into clinical practice.
Abstract
The introduction of newer more selective α(-2) adrenergic agonist, dexmedetomidine has made a revolution in the field of anesthesia owing to its varied application. The aim of the current review is to highlight the various clinical and pharmacological aspects of dexmedetomidine in daily routine practice of anesthesiology and intensive care besides its potential role in other clinical specialties. This review of dexmedetomidine was carried out after searching the medical literature in Pubmed, Science direct, Scopus, Google scholar and various text books and journal articles using keywords anesthesia, dexmedetomidine, neurosurgery, pediatric surgery, regional dexmedetomidine, anesthesia, regional, neurosurgery, and pediatric surgery. Dexmedetomidine has made its application from a novel sedating agent in the intensive care unit to its use as an adjuvant in various regional anesthetic techniques because of its "cooperative sedation" without any respiratory depression. It has a favorable pharmacokinetic profile suitable to be used in the perioperative period to reduce the requirements of opioids and anesthetic drugs. There are few side-effects of dexmedetomidine, which should always be kept in mind before choosing the patients for its use. The various side-effects associated with dexmedetomidine include, but are not limited to hypotension, bradycardia, worsening of heart block, dry mouth, and nausea. However, large scale randomized controlled trials are still needed to establish various effects of dexmedetomidine and to clearly define its safety profile.
KEYWORDS: Dexmedetomidine; General anesthesia; Regional anesthesia; α−2 adrenergic agonist
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