Etomidate Chemical Properties
- Melting point:72-74°C
- alpha D20 +66° (c = 1 in ethanol)
- Boiling point:160-162 °C(Press: 1 Torr)
- Density 1.11±0.1 g/cm3(Predicted)
- storage temp. 2-8°C
- solubility DMSO: >10 mg/mL
- form powder
- pkapKa 4.24(H2O t=25.0) (Uncertain)
- color white
- Merck 14,3881
- CAS DataBase Reference33125-97-2(CAS DataBase Reference)
- NIST Chemistry ReferenceEtomidate(33125-97-2)
Etomidate Usage And Synthesis
- General anestheticsEtomidate is an ultra-short effect non-barbiturate intravenous anesthetic agent allowed to be used in China , it belongs to imidazole derivatives, the appearance is white crystalline powder, melting point 115 ℃, easily soluble in water, methanol, ethanol and propylene glycol, soluble in chloroform, insoluble in acetone, insoluble in ether. Its effects on the central nervous system is similar to barbiturates. Hypnotic effect of Etomidate is strong , and its efficacy is about 12 times higher than thiopental, it has no analgesic effect. It has a rapid onset of anesthesia, after 20 seconds of intravenous injection, it produces anesthesia, anesthesia is maintained for about 5 minutes, it is quick to wake up , increasing the dose will increase the duration of action accordingly. Compared with thiopental ,its anesthesia strength is larger and it has smaller effects on the respiratory and circulatory systems. It is suitable for induction of anesthesia. Intravenous anesthesia, can increase 19% of coronary blood flow and resistance is reduced by 19%. Its obvious advantage is having no negative impact on the cardiovascular system, and it has low toxicity,it has little effect on the respiratory and circulatory system, there is a brief respiratory depression,which makes systolic blood pressure decrease slightly, and make heart rate slightly faster, compared with thiopental, above effects are less, and it has no histamine release effect. It may affect the liver and kidney function and reduce brain oxygen consumption, reduce cerebral blood flow and intracranial pressure. Clinical generally use amount is 0.1~0.4mg/kg, natural wake is 7 to 14 minutes. Distribution half-life is 2.8 minutes, and elimination half-life is 160 minutes. Hydrolyze in the liver and plasma , and the vast majority of metabolites are excreted by the kidneys. The main disadvantages of etomidate is the inhibition of adrenal cortex function, especially after long-term medication.
Induction of anesthesia: quiet, comfortable, heart rate, blood pressure are stable. The usual dose is 0.2~0.3mg/kg. Elderly, frail or critically ill patients can be reduced to 0.1~0.15mg/kg, intravenous drip.It is more suitable for cardiovascular disease, poor cardiac reserve and critically ill patients. Maintenance of intravenous anesthesia or inhalation anesthesia in short surgery or short time heart surgery : intravenous, 0.1~0.2mg/(kg · h). Outpatient minor surgery or special tests: intravenous injection, 0.2~0.3mg/kg.
After the use of the product, there will be clonic muscle contraction, using droperidol or fentanyl before anesthesia can reduce the incidence of myoclonus; if etomidate is used as inducing halothane anesthesia, the amount of halothane should be reduced .
The above information is edited by the chemicalbook of Tian Ye.
- UsesShort-time intravenous anesthetics.
- Chemical PropertiesColourless solid
- UsesEtomidate is a hypnotic.
- UsesA GABAA receptors agonist.
- DefinitionChEBI: The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.
- brand nameAmidate (Hospira);Hypnomidate concentrate;Hypnomidate injection;Hypromidate;Nalgol;Sibu.
- World Health Organization (WHO)Etomidate, a potent hypnotic agent, was introduced in 1977 for use as an intravenous anaesthetic. Its prolonged use can inhibit adrenal steroidogenesis and, following reports of reduced serum cortisol levels unresponsive to ACTH injection, the manufacturer suspended promotion of etomidate for sedation in intensive care in 1983. In 1985 regulatory action taken only in the United Kingdom further restricted use of the drug to induction of anaesthesia. Etomidate remains widely available and is currently registered for induction of anaesthesia in 34 countries and for maintenance of anaesthesia in 17 countries. It has never been registered for sedation.
- Biological FunctionsThe pharmacological properties of etomidate (Amidate) are similar to those of the barbiturates, although its use may provide a greater margin of safety because of its limited effects on the cardiovascular and respiratory systems. Since it has a relatively short elimination halflife (t1/2β = 2.9 hours), in addition to its use as an induction agent, etomidate has been used as a supplement to maintain anesthesia in some critically ill patients. Etomidate is rapidly hydrolyzed in the liver.
- General DescriptionEtomidate is a carboxylated imidazole intended for the inductionof general anesthesia. It is marketed as the morepotent R (+) isomer. It is believed to exert its anestheticeffect via positive modulation of the GABAA receptor. Itis not water soluble and is available in the United States as a2-mg/mL solution containing 35% v/v propylene glycol andin Europe as a soybean oil and medium-chain triglyceridesformulation. The propylene glycol has been associatedwith moderate-to-severe pain on injection and irritation ofthe vascular tissue. A high incidence of skeletal musclemovements were noted in about 32% of patients followingetomidate injection. Case reports of seizures are also foundin the literature.
- Biological ActivityGeneral anesthetic with GABA modulatory and GABA-mimetic actions; selectively interacts with β 2- and β 3-subunit containing GABA A receptors. Short acting and potent hypnotic, with low toxicity.
- Clinical UseEtomidate should only beused for induction of anesthesia when the cardiac benefitsoutweigh the risks associated with adrenal insufficiency.Etomidate is quickly distributed throughout most organsin the body after intravenous administration and the tissueconcentrations equal and sometimes exceed the plasmaconcentrations. The lipid solubility of the drug allows it torapidly penetrate into the brain with peak concentrationsoccurring within 1 minute of administration. Etomidate israpidly metabolized in the plasma and liver via esterases.About 75% of the drug is eliminated in the urine as the inactiveester hydrolyzed carboxylic acid.
- Side effectsEtomidate may cause pain on injection and may produce myoclonic muscle movements in approximately 40% of patients during its use as an induction anesthetic. In addition, etomidate can suppress the adrenocortical response to stress, an effect that may last up to 10 hours.
- Veterinary Drugs and TreatmentsEtomidate may be useful as an alternative to thiopental or propofol for anesthetic induction in small animals, particularly in patients with preexisting cardiac dysfunction, head trauma, or that are critically ill.
- MetabolismEtomidate is hydrolyzed by hepatic esterases to the corresponding inactive carboxylic acid, with subsequent renal and biliary excretion terminating its action. Its apparent elimination half-life is approximately 5 to 6 hours, with a volume of distribution of 5 to 7 L/kg. Changes in hepatic blood flow or hepatic metabolism will have only moderate effects on etomidate disposition. Concerns regarding the ability of etomidate to precipitate myoclonic jerks and inhibit adrenal steroid synthesis have been reported.
Etomidate Preparation Products And Raw materials
- Company Name:Wuhan Wsem Biological Co., Ltd. Gold
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- Company Name:Suzhou Zhongbo Chemical Technology Co., Ltd. Gold
- Tel:13914931156 512-81661176-
- Company Name:J & K SCIENTIFIC LTD.
- Tel:400-666-7788 010-82848833-
- Company Name:Meryer (Shanghai) Chemical Technology Co., Ltd.
- Tel:400-660-8290 21-61259100-
- Company Name:3B Pharmachem (Wuhan) International Co.,Ltd.
- Tel:18930552037 821-50328103-801