Intravenous pharmacokinetic profile in rats of etomidate, a short-acting hypnotic drug. 1976

P J Lewi, and J J Heykants, and P A Janssen

Etomidate is a novel short-acting drug, whose pharmacokinetic profile was studied in 14 organs and tissues after i.v. administration to rats. Four dose levels, ranging from 224 to 1800 mug, were assayed between 1.75 and 112 min after administration. A three-compartment open linear model has been fitted to the plasma concentrations, assuming a central, peripheral and deep compartment. The fast component of the plasma curve, has a half-life of 1.19 min. Brain tissue rapidly enters in equilibrium with plasma and shows the highest concentration. Muscle, subcutaneous fat and possibly skin and connective tissues contribute most to the total amount of drug in the body. Many tissues are heterogeneous and exhibit combinations of central, peripheral and deep compartments. Elimination of etomidate occurs by ester-hydrolysis in plasma and in the liver with approximately equal rate constants. Metabolization of etomidate in the liver is a capacity-limited Michaelis-Menten process.

UI MeSH Term Description Entries
D006993 Hypnotics and Sedatives Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. Hypnotic,Sedative,Sedative and Hypnotic,Sedatives,Hypnotic Effect,Hypnotic Effects,Hypnotics,Sedative Effect,Sedative Effects,Sedatives and Hypnotics,Effect, Hypnotic,Effect, Sedative,Effects, Hypnotic,Effects, Sedative,Hypnotic and Sedative
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D008433 Mathematics The deductive study of shape, quantity, and dependence. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Mathematic
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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