部分中文依托咪酯处方资料（仅供参考）
药物类别：神经系统用药
所属类别：全身麻醉药
药物名称：依托咪酯
英文名称：Etomidate
中文别名：
1 甲苄咪酯 
2 甲苄咪唑 
3 乙咪酯
英文别名：Amidate
制剂/规格：
1 注射用乳剂：20mg
2 注射剂：20mg(10m1)
成份：Etomidate 
药理作用：
本品为快速催眠性静脉全身麻醉药，该药仅能催眠，无镇痛作用，但能加强其他麻醉药的镇痛作用。用药后安静、舒适、无兴奋挣扎，且有遗忘现象。在临床剂量范围内(0.1～0.4mg／kg)7～14分钟自然苏醒，较硫喷妥钠快。依托咪酯可减少脑血流量，降低颅内压，并可制止脑缺氧引起的抽搐。
静脉注射依托咪酯后常有心率减慢，收缩压轻度升高，脉压变大，对心血管和呼吸系统影响较小，单次静脉注射量大可引起短期呼吸暂停，对肝、肾功能无明显影响，降低眼压显著，适宜眼科手术。
本品抑制肾上腺皮质激素合成酶，诱导麻醉可引起肾上腺皮质抑制4～8小时。 
药动学：
本品静注后，迅速分布至脑和其他组织，通常在1分钟内起效。保持催眠最低血药浓度一般应在0.2／µg／ml以上，单次注药，血药浓度在30分钟内迅速降低。本品呈三室分布，血浆蛋白结合率较高，78％与白蛋白结合，白蛋白减少，则游离部分增多，3％与球蛋白结合。Vd高达 (24.2±4.2)L／kg。t1/2α(分布半衰期)2.81±1.4分钟，t1/2γ(再分布半衰期) 32.1±16.5分钟，作用时效30～75分钟，t1/2β(消除半衰期)28.7±14分钟，本品在肝脏和血浆中主要被酯酶迅速水解，初30分钟内水解最快，但6小时仍未完全，代谢物80％为混旋-1-(α-甲苄基)-咪唑-5-羧酸酯，有64.3％与 血浆蛋白结合，药理上无效。排泄的第一天为用量的75％经肾由尿排出，13％从胆汁排出。其中85％为代谢物，3％为原药。 
适应症：
静脉全麻诱导药或麻醉辅助药。本品仅供静脉注射，剂量必须个体化。
用法用量：
(1)麻醉诱导：成人常用量按体重0.3mg / kg(范围0.2～0.6mg)，年老体弱和危重病人可酌减，于30～60s内注完。术前给以镇静药，或在全麻诱导前1～2分钟静注芬太尼0.1mg，依托咪酯需要量可酌减。10岁以上小儿用量可参照成人。
(2)麻醉维持：麻醉诱导后可连续每小时静滴0.12～0.2mg／kg，同时静注芬太尼、氟哌利多、芬太尼合剂或吸入全麻药。
(3)门诊手术麻醉：如内镜检查、扁桃腺摘除、人工流产、电击除颤和拔牙等，病人苏醒早，无后遗作用。此外还适用于心功能不全的心血管手术。使用本品须备有复苏设备，并供氧。 
不良反应：
1．本品可抑制肾上腺皮质激素的生物合成，一次性剂量可使。肾上腺皮质对紧张刺激的反应明显减慢约4～6小时，持续使用可能出现暂时性肾上腺皮质功能低下。而呈现水盐失衡、低血压甚至休克。
2．恶心、呕吐主要是由同时或前期给予的阿片类药引起。
3．可能会出现咳嗽、呃逆和寒战、喉痉挛。
4．使用单剂量后可能出现肌阵挛，肌颤发生率约为6％，不自主的肌肉活动发生率可达32％(22.7％～63％)。这一反应可于给药前，使用阿片类或苯二氮卓类(如使用本品1小时前肌注安定或10分钟前静滴安定)来预防。
5．大剂量使用本品或与中枢神经抑制剂合用时，偶见短暂呼吸暂停。
6．注射部位疼痛可达20％(1.2％～42％)，可引起血栓性静脉炎，但若在肘部较大静脉内注射或用乳剂则发生率较低。 
相互作用：
1．抗精神病药、鸦片类、镇静剂及酒精可增强本药的催眠效果。
2．与任何可能引起血压下降的药物合用时均应慎重，以免导致血压剧降，如中枢性抗高血压药、利尿性抗高血压药、钙通道阻滞药、静注硫酸镁、单胺氧化酶抑制药及氯胺酮等。
3．当与芬太尼合用时，可出现不能自制的肌肉强直或阵挛，安定可减少其发生。
4．长期大剂量静脉滴注依托咪酯可抑制肾上腺皮质对促肾上腺素的应激，导致血浆皮质激素低于正常，如遇中毒性休克、多发性创伤或肾上腺皮质功能低下的病人，可同时给予适量的氢化可的松。 
注意事项：
1．依托咪酯注射液不宜稀释后使用。
2．如果用药过量，尤其与吸入麻醉剂合用时，睡眠期可能延长，并可能出现短期呼吸暂停。事先应充分准备好全身麻醉所需的所有设备和药品。
3．癫痫患者慎用。血红素生物合成受损的患者应避免使用，除非用本品的指征十分明确。
4．患者须至少等到用药24小时后方可驾驶或操作机械。
5．麻醉前应用氟哌利多或芬太尼时，可减少肌阵挛的发生。
6．将本品作为氟烷的诱导麻醉剂，宜将氟烷的用量减少。
7．选用粗大静脉注射或在药液中加入利多卡因(0.1mg／kg)预防注射痛。避免注入动脉，因为注入动脉会有危险，静脉旁注射会引起疼痛。
8．在特殊情况下及别无选择时，可用于孕妇。
9．本品可分泌进入乳汁。如果哺乳期必须使用，则应中止哺乳，结束使用24小时后才可开始哺乳。
10．没有作相容性试验之前，不能将本品与其他注射液混合，不能与其他注射液经同一管路同时给药。
11．本品不含抗菌剂，开启后应在无菌条件下迅速抽取和注射，因为脂肪乳会助长微生物生长，未用完部分必须丢弃。用前应摇匀。 
疗效评价：
本品为超短时效的非巴比妥类静脉麻醉药，无镇痛作用，静注后一次臂-脑循环即迅速入睡，其催眠效力比硫喷妥钠强12倍。用于全麻诱导，具有作用快、持续时间短、苏醒迅速而安全、呼吸抑制轻微而短暂、不释放组胺而不引起变态反应、对心血管功能影响小等优点。依托咪酯多次用药无明显蓄积，睡眠持续时间稍有延长。 
AMIDATE (etomidate) injection, solution
[Hospira, Inc.]
SPL UNCLASSIFIED SECTION
Etomidate Injection, USP
2 mg/mL
DESCRIPTION
Amidate (Etomidate Injection, USP) is a sterile, nonpyrogenic solution. Each milliliter contains etomidate, 2 mg, propylene glycol 35% v/v. The pH is 6.0 (4.0 to 7.0).
It is intended for the induction of general anesthesia by intravenous injection.
The drug etomidate is chemically identified as (R)-(+)-ethyl-1-(1-phenylethyl)-1H-imidazole-5-carboxylate and has the following structural formula:
CLINICAL PHARMACOLOGY
Etomidate is a hypnotic drug without analgesic activity. Intravenous injection of etomidate produces hypnosis characterized by a rapid onset of action, usually within one minute. Duration of hypnosis is dose dependent but relatively brief, usually three to five minutes when an average dose of 0.3 mg/kg is employed. Immediate recovery from anesthesia (as assessed by awakening time, time needed to follow simple commands and time to perform simple tests after anesthesia as well as they were performed before anesthesia), based upon data derived from short operative procedures where intravenous etomidate was used for both induction and maintenance of anesthesia, is about as rapid as, or slightly faster than, immediate recovery after similar use of thiopental. These same data revealed that the immediate recovery period will usually be shortened in adult patients by the intravenous administration of approximately 0.1 mg of intravenous fentanyl, one or two minutes before induction of anesthesia, probably because less etomidate is generally required under these circumstances (consult the package insert for fentanyl before using).
The most characteristic effect of intravenous etomidate on the respiratory system is a slight elevation in arterial carbon dioxide tension (PaCO2). See also ADVERSE REACTIONS.
Reduced cortisol plasma levels have been reported with induction doses of 0.3 mg/kg etomidate. These persist for approximately 6 to 8 hours and appear to be unresponsive to ACTH administration.
The intravenous administration of up to 0.6 mg/kg of etomidate to patients with severe cardiovascular disease has little or no effect on myocardial metabolism, cardiac output, peripheral circulation or pulmonary circulation. The hemodynamic effects of etomidate have in most cases been qualitatively similar to those of thiopental sodium, except that the heart rate tended to increase by a moderate amount following administration of thiopental under conditions where there was little or no change in heart rate following administration of etomidate. However, clinical data indicates that etomidate administration in geriatric patients, particularly those with hypertension, may result in decreases in heart rate, cardiac index, and mean arterial blood pressure. There are insufficient data concerning use of etomidate in patients with recent severe trauma or hypovolemia to predict cardiovascular response under such circumstances.
Clinical experience and special studies to date suggest that standard doses of intravenous etomidate ordinarily neither elevate plasma histamine nor cause signs of histamine release.
Limited clinical experience, as well as animal studies, suggests that inadvertent intra-arterial injection of etomidate, unlike thiobarbiturates, will not usually be followed by necrosis of tissue distal to the injection site. Intra-arterial injection of etomidate is, however, not recommended.
Etomidate induction is associated with a transient 20-30% decrease in cerebral blood flow. This reduction in blood flow appears to be uniform in the absence of intracranial space occupying lesions. As with other intravenous induction agents, reduction in cerebral oxygen utilization is roughly proportional to the reduction in cerebral blood flow. In patients with and without intracranial space occupying lesions, etomidate induction is usually followed by a moderate lowering of intracranial pressure, lasting several minutes. All of these studies provided for avoidance of hypercapnia. Information concerning regional cerebral perfusion in patients with intracranial space occupying lesions is too limited to permit definitive conclusions.
Preliminary data suggests that etomidate will usually lower intraocular pressure moderately.
Etomidate is rapidly metabolized in the liver. Minimal hypnotic plasma levels of unchanged drug are equal to or higher than 0.23 μg/mL; they decrease rapidly up to 30 minutes following injection and thereafter more slowly with a half-life value of about 75 minutes. Approximately 75% of the administered dose is excreted in the urine during the first day after injection. The chief metabolite is R-(+)-1-(1-phenylethyl)-1H-imidazole-5-carboxylic acid, resulting from hydrolysis of etomidate, and accounts for about 80% of the urinary excretion. Limited pharmacokinetic data in patients with cirrhosis and esophageal varices suggest that the volume of distribution and elimination half-life of etomidate are approximately double that seen in healthy subjects.
(Reference: H. Van Beem, et. al., Anaesthesia 38 (Supp 38:61-62, July 1983).
In clinical studies, elderly patients demonstrated decreased initial distribution volumes and total clearance of etomidate. Protein binding of etomidate to serum albumin was also significantly decreased in these individuals.
Reduced plasma cortisol and aldosterone levels have been reported following induction doses of etomidate. These results persist for approximately 6-8 hours and appear to be unresponsive to ACTH stimulation. This probably represents blockage of 11 beta-hydroxylation within the adrenal cortex.
(References: 1. R.J. Fragen, et. al., Anesthesiology 61:652-656, 1984. 2. R.L. Wagner & P.F. White, Anesthesiology 61:647-651, 1984. 3. F.H. DeJong, et. al., Clin. Endocrinology and Metabolism 59:(6):1143-1147, 1984, and three additional drafts of Metabolic Studies, all submitted to NDA 18-228 on April 1, 1985).
INDICATIONS AND USAGE
Etomidate is indicated by intravenous injection for the induction of general anesthesia. When considering use of etomidate, the usefulness of its hemodynamic properties (see CLINICAL PHARMACOLOGY) should be weighed against the high frequency of transient skeletal muscle movements (see ADVERSE REACTIONS).
Intravenous etomidate is also indicated for the supplementation of subpotent anesthetic agents, such as nitrous oxide in oxygen, during maintenance of anesthesia for short operative procedures such as dilation and curettage or cervical conization.
CONTRAINDICATIONS
Etomidate is contraindicated in patients who have shown hypersensitivity to it.
WARNINGS
INTRAVENOUS ETOMIDATE SHOULD BE ADMINISTERED ONLY BY PERSONS TRAINED IN THE ADMINISTRATION OF GENERAL ANESTHETICS AND IN THE MANAGEMENT OF COMPLICATIONS ENCOUNTERED DURING THE CONDUCT OF GENERAL ANESTHESIA.
BECAUSE OF THE HAZARDS OF PROLONGED SUPPRESSION OF ENDOGENOUS CORTISOL AND ALDOSTERONE PRODUCTION, THIS FORMULATION IS NOT INTENDED FOR ADMINISTRATION BY PROLONGED INFUSION.
PRECAUTIONS
Do not administer unless solution is clear and container is undamaged. Discard unused portion (see DOSAGE AND ADMINISTRATION).
1. Carcinogenesis, Mutagenesis, Impairment of Fertility: No carcinogenesis or mutagenesis studies have been carried out on etomidate. The results of reproduction studies showed no impairment of fertility in male and female rats when etomidate was given prior to pregnancy at 0.31, 1.25 and 5 mg/kg (approximately 1X, 4X and 16X human dosage).
2. Pregnancy Category C. Etomidate has been shown to have an embryocidal effect in rats when given in doses 1 and 4 times the human dose. There are no adequate and well-controlled studies in pregnant women. Etomidate should be used during pregnancy only if the potential benefit justifies the potential risks to the fetus. Etomidate has not been shown to be teratogenic in animals. Reproduction studies with etomidate have been shown to:
a. Decrease pup survival at 0.3 and 5 mg/kg in rats (approximately 1X and 16X human dosage) and at 1.5 and 4.5 mg/kg in rabbits (approximately 5X and 15X human dosage). No clear dose-related pattern was observed.
b. Increase slightly the number of stillborn fetuses in rats at 0.3 and 1.25 mg/kg (approximately 1X and 4X human dosage).
c. Cause maternal toxicity with deaths of 6/20 rats at 5 mg/kg (approximately 16X human dosage) and 6/20 rabbits at 4.5 mg/kg (approximately 15X human dosage).
3. Labor and Delivery: There are insufficient data to support use of intravenous etomidate in obstetrics, including Caesarean section deliveries. Therefore, such use is not recommended.
4. Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when etomidate is administered to a nursing mother.
5. Pediatric Use: There are inadequate data to make dosage recommendations for induction of anesthesia in patients below the age of ten (10) years; therefore, such use is not recommended (see also DOSAGE AND ADMINISTRATION).
6. Geriatric Use: Clinical data indicates that etomidate may induce cardiac depression in elderly patients, particularly those with hypertension (see CLINICAL PHARMACOLOGY and OTHER ADVERSE OBSERVATIONS, Circulatory System).
Elderly patients may require lower doses of etomidate than younger patients. Age-related differences in phamacokinetic parameters have been observed in clinical studies (see CLINICAL PHARMACOLOGY and DOSAGE AND ADMINISTRATION).
This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and it may be useful to monitor renal function.
7. Plasma Cortisol Levels: Induction doses of etomidate have been associated with reduction in plasma cortisol and aldosterone concentrations (see CLINICAL PHARMACOLOGY). These have not been associated with changes in vital signs or evidence of increased mortality; however, where concern exists for patients undergoing severe stress, exogenous replacement should be considered.
ADVERSE REACTIONS
The most frequent adverse reactions associated with use of intravenous etomidate are transient venous pain on injection and transient skeletal muscle movements, including myoclonus:
1. Transient venous pain was observed immediately following intravenous injection of etomidate in about 20% of the patients, with considerable difference in the reported incidence (1.2% to 42%). This pain is usually described as mild to moderate in severity but it is occasionally judged disturbing. The observation of venous pain is not associated with a more than usual incidence of thrombosis or thrombophlebitis at the injection site. Pain also appears to be less frequently noted when larger, more proximal arm veins are employed and it appears to be more frequently noted when smaller, more distal, hand or wrist veins are employed.
2. Transient skeletal muscle movements were noted following use of intravenous etomidate in about 32% of the patients, with considerable difference in the reported incidence (22.7% to 63%). Most of these observations were judged mild to moderate in severity but some were judged disturbing. The incidence of disturbing movements was less when 0.1 mg of fentanyl was given immediately before induction. These movements have been classified as myoclonic in the majority of cases (74%), but averting movements (7%), tonic movements (10%), and eye movements (9%) have also been reported. No exact classification is available, but these movements may also be placed into three groups by location:
a. Most movements are bilateral. The arms, legs, shoulders, neck, chest wall, trunk and all four extremities have been described in some cases, with one or more of these muscle groups predominating in each individual case. Results of electroencephalographic studies suggest that these muscle movements are a manifestation of disinhibition of cortical activity; cortical electroencephalograms, taken during periods when these muscle movements were observed, have failed to reveal seizure activity.
b. Other movements are described as either unilateral or having a predominance of activity of one side over the other. These movements sometimes resemble a localized response to some stimuli, such as venous pain on injection, in the lightly anesthetized patient (averting movements). Any muscle group or groups may be involved, but a predominance of movement of the arm in which the intravenous infusion is started is frequently noted.
c. Still other movements probably represent a mixture of the first two types.
Skeletal muscle movements appear to be more frequent in patients who also manifest venous pain on injection.
OTHER ADVERSE OBSERVATIONS Respiratory System: Hyperventilation, hypoventilation, apnea of short duration (5 to 90 seconds with spontaneous recovery); laryngospasm, hiccup and snoring suggestive of partial upper airway obstruction have been observed in some patients. These conditions were managed by conventional countermeasures.
Circulatory System: Hypertension, hypotension, tachycardia, bradycardia and other arrhythmias have occasionally been observed during induction and maintenance of anesthesia. One case of severe hypotension and tachycardia, judged to be anaphylactoid in character, has been reported.
(Reference: M. Sold and A. Rothhammer, Anaesthetist 34:208-210, 1985. Submitted to NDA 18-228 on 16 May 1985).
Geriatric patients, particularly those with hypertension, may be at increased risk for the development of cardiac depression following etomidate administration (see CLINICAL PHARMACOLOGY).
Gastrointestinal System: Postoperative nausea and/or vomiting following induction of anesthesia with etomidate is probably no more frequent than the general incidence. When etomidate was used for both induction and maintenance of anesthesia in short procedures such as dilation and curettage, or when insufficient analgesia was provided, the incidence of postoperative nausea and/or vomiting was higher than that noted in control patients who received thiopental.
OVERDOSAGE
Overdosage may occur from too rapid or repeated injections. Too rapid injection may be followed by a fall in blood pressure. No adverse cardiovascular or respiratory effects attributable to etomidate overdose have been reported.
In the event of suspected or apparent overdosage, the drug should be discontinued, a patent airway established (intubate, if necessary) or maintained and oxygen administered with assisted ventilation, if necessary.
The LD50 of etomidate administered intravenously to rats is 20.4 mg/kg.
DOSAGE AND ADMINISTRATION
Etomidate Injection, USP is intended for administration only by the intravenous route (see CLINICAL PHARMACOLOGY). The dose for induction of anesthesia in adult patients and in pediatric patients above the age of ten (10) years will vary between 0.2 and 0.6 mg/kg of body weight, and it must be individualized in each case. The usual dose for induction in these patients is 0.3 mg/kg, injected over a period of 30 to 60 seconds. There are inadequate data to make dosage recommendations for induction of anesthesia in patients below the age of ten (10) years; therefore, such use is not recommended. Geriatric patients may require reduced doses of etomidate.
Smaller increments of intravenous etomidate may be administered to adult patients during short operative procedures to supplement subpotent anesthetic agents, such as nitrous oxide. The dosage employed under these circumstances, although usually smaller than the original induction dose, must be individualized. There are insufficient data to support this use of etomidate for longer adult procedures or for any procedures in pediatric patients; therefore, such use is not recommended. The use of intravenous fentanyl and other neuroactive drugs employed during the conduct of anesthesia may alter the etomidate dosage requirements. Consult the prescribing information for all other such drugs before using.
Premedication: Etomidate Injection, USP is compatible with commonly administered pre-anesthetic medications, which may be employed as indicated. See also CLINICAL PHARMACOLOGY, ADVERSE REACTIONS, and dosage recommendations for maintenance of anesthesia.
Etomidate hypnosis does not significantly alter the usual dosage requirements of neuromuscular blocking agents employed for endotracheal intubation or other purposes shortly after induction of anesthesia.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
To prevent needle-stick injuries, needles should not be recapped, purposely bent, or broken by hand.
HOW SUPPLIED
Amidate™ (Etomidate Injection, USP) is supplied in single-dose containers as follows:
Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]
完整处方资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b7ed5bf8-ba75-44dc-8f81-96b4ad5766be