Brazilian Journal of Anesthesiology
https://app.periodikos.com.br/journal/rba/article/doi/10.1590/S0034-70942002000500012
Brazilian Journal of Anesthesiology
Miscellaneous

Dexmedetomidina: farmacologia e uso clínico

Dexmedetomidine: pharmacology and clinical application

Airton Bagatini; Cláudio Roberto Gomes; Marcelo Zanettini Masella; Gabrielle Rezer

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Resumo

JUSTIFICATIVA E OBJETIVOS: A dexmedetomidina é o mais recente agonista alfa2-adrenérgico em uso clínico. Apresenta rápido início de ação sendo metabolizado no fígado e excretado principalmente pela urina. O objetivo desta revisão é apresentar as características farmacocinéticas e farmacodinâmicas da dexmedetomidina e sua aplicação clínica em cirurgias. CONTEÚDO: São apresentadas as características farmacocinéticas e farmacodinâmicas da dexmedetomidina, comparando-as com a de outras drogas agonistas alfa2-adrenérgicas, que têm como protótipo do grupo a clonidina. São comentados resultados de trabalhos realizados em cirurgias cardíacas, vasculares, neurológicas e ginecológicas. CONCLUSÕES: A dexmedetomidina mostrou ser uma droga inovadora no que diz respeito à sedação e analgesia. Destacam-se como qualidades principais da droga um rápido início de ação e a capacidade de permitir rápida titulação, podendo deste modo variar a profundidade da sedação e da analgesia. Além disso, oferece sinergismo com as demais drogas anestésicas comumente utilizadas, apresentando baixa incidência de efeitos colaterais e mínima depressão respiratória.

Palavras-chave

DROGAS, DROGAS

Abstract

BACKGROUND AND OBJECTIVES: Dexmedetomidine is the newest alpha2-adrenergic agonist for clinical application. It has a fast onset, is metabolized by the liver and mostly excreted by the urine. This review aimed at presenting pharmacokinetic and pharmacodynamic profiles of dexmedetomidine and its clinical applications. CONTENTS: Dexmedetomidine pharmacokinetic and pharmacodynamic profiles are presented and compared to other alpha2-adrenergic agonist drugs, the prototype of which is clonidine. Cardiac, vascular, neurological and gynecologic procedure outcomes are commented. CONCLUSIONS: Dexmedetomidine is an innovative drug for sedation and analgesia. Its major qualities are fast onset and titration, allowing for changes in sedation and analgesia depth. In addition, it has a synergism with commonly used anesthetic drugs, with a low incidence of side effects and minor respiratory depression.

Keywords

DRUGS, DRUGS

References

Maze M. Clinical Uses of alpha2 Agonists: Refresher Courses in Anesthesiology. . 1992;20:132-142.

Hayashi Y, Maze M. Alpha-2 adrenoreceptor agonist and anesthesia. Br J Anaesth. 1993;71:108-118.

Alves TCA, Braz JRC, Vianna PTG. Alfa2-agonistas em Anestesiologia: aspectos clínicos e farmacológicos. Rev Bras Anestesiol. 2000;50:396-404.

Ahlquist RP. A study of the adrenotropic receptors. Am J Phisiol. 1948;153:586-600.

Hall JE, Uhrich TD, Barney JA. Sedative, amnestic, and analgesic properties of small-dose dexmedetomidine infusions. Anesth Analg. 2000;90:699-705.

Graham BA, Hammond DL, Proufit HK. Synergistic interactions between two alpha2-adrenoreceptor agonists, dexmedetomidine and ST-91, in two substrains of Sprague-Dawley rats. Pain. 2000;85:135-143.

Kallio A, Scheinin M, Koulu M. Effects of dexmedetomidine, a selective alphalpha2-adrenorecptor agonist, on hemodynamic control mechanisms. Clin Pharmacol Ther. 1989;46:33-42.

Dick JB, Shafer SL. Dexmedetomidine pharmacokinetics and pharmacodynamics. Anaesth Pharm Review. 1993;1:238-245.

Virtanen R, Savola JM, Saano V. Characterization of selectivity, specificity and potency of medetomidine as an alphalpha2 -adrenoceptor agonist. Eur J Pharmacol. 1988;150:9-14.

Segal IS, Vickery RG, Walton JK. Dexmedetomidine diminishes halothane anesthetic requirements in rats through a postsynaptic alpha2-adrenergic receptor. Anesthesiology. 1988;69:818-823.

Hall EJ, Uhrich TD, Barney JA. Sedative, amnestic, and analgesic properties of small-dose dexmedetomidine infusions. Anesth Analg. 2000;90:699-705.

Talke P, Chen R, Thomas B. The hemodynamic and adrenergic effects of perioperative dexmedetomidine infusion after vascular surgery. Anesth Analg. 2000;90:834-839.

Gertler R, Brown HC, Mitchell DH. Dexmedetomidine: a novel sedative-analgesic agent. BUMC Proceedings. 2001;14:13-21.

Hynynen M, Jalonen J, Heikkila H. Dexmedetomidine infusion improves perioperative adrenergic stability during coronary artery bypass surgery. J Cardiol Vascular Anesth. 1994;8(^s3).

Dyck JB, Shafer SL. Dexmedetomidine pharmacokinetics and pharmacodynamics. . 2000;1:1-5.

Talke PO, Traber DL, Richardson CA. The effect of alpha2-agonist-induced sedation and its reversal with an alpha2 antagonist on organ blood flow in sheep. Anesth Analg. 2000;90:1060-1066.

Jalonen J, Hynynen M, Kuitunen A. Dexmedetomidine as an anesthetic adjunct in coronary artery bypass grafting. Anesthesiology. 1997;86:331-345.

Bloor BC, Ward DS, Maze M. Effects of intravenous dexmedetomidine in humans. Anesthesiology. 1992;77:1134- 1142.

Liu N, Bonnet F, Delaunay L. Partial reversal of the effects of extradural clonidine by oral yohimbine in postoperative patients. Br J Anaesth. 1993;70:515-518.

Dyck JB, Maze M, Haack C. The pharmacokinetics and hemodynamic effects of intravenous and intramuscular dexmedetomidine hydrochloride in adult human volunteers. Anesthesiology. 1993;78:813-852.

Gaumann DM, Brunet PC, Jirounek P. Clonidine enhances the effects of lidocaine on C-fiber action potential. Anesth Analg. 1992;74:719-725.

Butterworth JF, Strichartz GR. The alpha2-adrenergic agonist clonidine and guanfacine produce tonic and phasic block of conduction in rat sciatic nerve fibers. Anesth Analg. 1993;76:259-301.

Spaulding TC, Fielding S, Venafro JJ. Antinociceptive activity of clonidine and its potentiaton of morphine analgesia. Eur J Pharmacol. 1979;58:19-25.

Aantaa R, Jaakola ML, Kallio A. Reduction of the minimum alveolar concentration of isoflurane by dexmedetomidine. Anesthesiology. 1997;86:1055-1060.

Aho M, Erkola O, Kalho A. Dexmedetomidine infusion for maintenance of anesthesia in patients undergoing abdominal hysterectomy. Anesth Analg. 1992;75:940-946.

Jonge A, Timmermans PB, van Zweiten PA. Participation of cardiac presynaptic alpha2-adrenoreceptors in the bradycardic effects of clonidine and analogues. Naunyn Schmiedebergs Arch Pharmacol. 1981;137:8-12.

Ruffolo Jr RR. Distribution and function of peripheral adrenoreceptores on the cardiovascular system. Pharmacol Biochem Beahav. 1985;22:827-833.

Kubo T, Misu Y. Pharmacological characterization on the alpha2-adrenoreceptor responsible for a decrease of blood pressure in the nucleus tractus solitary of the rat. Naunyn Schmiedebergs Arch Pharmacol. 1981;317:120-125.

Flack JW, Bloor BC, Flack WE. - Reduced narcotics requirements by clonidine with improved hemodynamic and adrenergic stability in patient undergoing coronary surgery. Anesthesiology. 1987;67:11-19.

Ernsberger P, Giuliano R, Willette RN. Role of imidazole receptors in the vasopressor response to clonidine analogs in the rostral ventrolateral medulla. J Pharmacol Exp Ther. 1990;253:408-418.

Ferreira AA, Vicente JB, Queiróz Filho LS. Clonidina: medicação pré-operatória ideal para cirurgia oftálmica. Arquivos do Instituto Penido Burnier. 1990;32:7-10.

Bekker AY, Kaufman B, Samir H. The use of dexmedetomidine infusion for awake craniotomy. Anesth Analg. 2001;92:1251-1253.

Bucklin B, Eisenach JC, Tucker B. Pharmocokinetics and dynamic studies of intrathecal, epidural, and intravenous dexmedetomidine. Anesthesiology. 1991;75(3):A662.

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