Anesthesia

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Etomidate

Sat, 11/03/2007 - 12:41 — oxygen
Your Ad Here ETOMIDATE Listen to Audio mechanism of action structure-activity relationships pharmacokinetic effects on organ systems drug interactions MECHAMISM OF ACTION -depresses reticular activating system (RAS) -mimics the inhibitory effects of GABA primarily binding to GABA type A receptor -associated with myoclonus incidence of 30-60% due to disinhibitory effects on the extrapyramidal motor system STRUCTURE-ACTIVITY RELATIONSHIPS -carboxylated imidazole ring -lipid solubility at physiologic pH -water soluable at acidic pH -usually pain on injection due to propylene glycol in which etomidate is dissolved in PHARMACOKINETICS Absorption -only in intravenous form -used primarily for induction of general anesthesia Distribution -very rapid onset of action due to high lipid solubility and high nonionized fraction at physiologic pH -rapid emergence is due to redistribution leading to decreasing plasma concentrations Biotransformation -rapid hydrolysis of etomidate to inactive metabolites by the hepatic microsomal enzymes and plasma esterases -rate of biotransformation of etomidate is five times more rapid than for thiopenthal Excretion -primarily excreted in the urine PHARMACODYNAMICS Effects on Organ Systems Central nervous system -decreases CMR02 -decreases CBF -decreases ICP -generally well maintained CePP due to minimal CVS effects -enhances somatosensory evoked potentials (SSEP) -naseau and vomitting more common with etomidate than other induction agents Cardiovascular system -minimal effects on CVS -may have a slight decline in MAP due to mild reduction in the peripheral vascular resistance -myocardial contractility and cardiac output generally well maintained -not associated with histamine release Respiratory system -less effect on ventilation than other induction agents (ex. barbiturates,benzodiazepines and propofol) -often induction doses of etomidate when used alone may still not result in apnea Endocrine system -enzymes involved in cortisol and aldosterone synthesis may transiently inhibited with induction doses of etomidate -adrenocortical suppresion may occur with long term infusion of etomidate Drug Interactions Fentanyl: increases both plasma levels and half life of etomidate Opiods: decreases myoclonus of etomidate induction

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Etomidate is commonly used in the emergency setting as part of a rapid sequence induction to induce anesthesia or for conscious sedation. It is often used in this setting since it has a rapid onset of action and a low cardiovascular risk profile, and therefore is less likely to cause a significant drop in blood pressure than other induction agents. Etomidate is unlikely to cause hypotension and so is ideal to use as an induction agent with critically-ill patients, such as patients with sepsis, without negative effects from transient worsening of low blood pressure.....

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