[Pharmacokinetics of etomidate]. 1990

J C Levron, and P Assoune
JANSSEN Research Foundation, Laboratoires JANSSEN, Aubervilliers.

Etomidate is the ester of a carboxylated imidazole. This lipophilic (octanol/water partition coefficient: 1000) and weak base (pKa = 4.5) is a potent short-acting hypnotic agent, which can be used for anaesthetic induction or maintenance. The plasma concentration curve fits an open three compartment pharmacokinetic model, with distribution half-lives of 2.6 and 20 min, and terminal elimination half-life of about 4-5 h. Hypnotic plasma concentrations (greater than 0.2 microgram.ml-1) are observed during the intermediate distribution phase (t1/2 approximately 20 min); they reflect the short lasting pharmacodynamic effect. The slow elimination phase is of importance for intravenous infusions lasting more than 2 h; it is recommended to decrease by half the maintenance dose (0.005 mg.kg-1.min-1) so as to prevent a cumulative effect. Etomidate is hydrolysed by hepatic esterases to the corresponding carboxylic acid, which is inactive. The pharmacokinetics of etomidate are altered in the elderly, with a decrease initial distribution volume and clearance (a decreased of 2 ml.min-1.kg-1 every decade) as well as in cirrhotic patients (a 100% increase in terminal half-life).

UI MeSH Term Description Entries
D008103 Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules. Cirrhosis, Liver,Fibrosis, Liver,Hepatic Cirrhosis,Liver Fibrosis,Cirrhosis, Hepatic
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D008723 Methohexital An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. Methohexitone,Brevimytal Natrium,Brevital,Brietal,Brietal-Sodium,Methohexital Sodium,Methohexital, Monosodium Salt,Brietal Sodium,Monosodium Salt Methohexital,Natrium, Brevimytal,Sodium, Methohexital
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D005045 Etomidate Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic. Ethomidate,Hypnomidate,R-26490,Radenarkon,R 26490,R26490
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000367 Age Factors Age as a constituent element or influence contributing to the production of a result. It may be applicable to the cause or the effect of a circumstance. It is used with human or animal concepts but should be differentiated from AGING, a physiological process, and TIME FACTORS which refers only to the passage of time. Age Reporting,Age Factor,Factor, Age,Factors, Age
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D013874 Thiopental A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration. Penthiobarbital,Thiomebumal,Thiopentobarbital,Bomathal,Nesdonal,Pentothal,Pentothal Sodico,Sodipental,Thionembutal,Thiopental Nycomed,Thiopental Sodium,Thiopentone,Tiobarbital Braun,Trapanal

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