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 详细处方信息以本药内容附件PDF文件（201892621140836.pdf）的“原文Priscribing Information”为准
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部分艾司唑仑处方资料（仅供参考）

【药品名称】 艾司唑仑

【英文名称】 Estazolam

【

别名】 三唑氮卓；三唑氯安定；舒乐安定；舒坦乐安定；忧虑定；Estazolamum；Eurodin；Surazapam；Surazepam

【类别】 神经系统药物/镇静及催眠药物/苯二氮卓类药物

【剂型】

1.片剂：1mg，2mg；2.注射剂(粉)：2mg。

【 药理作用 】

艾司唑艾司唑仑为高效的苯二氮卓类镇静催眠药，作用于大脑边缘系统和脑干网状结构，并能降低大脑组织氧化过程，加强大脑保护性抑制作用。有较强的镇静、催眠、抗惊厥、抗焦虑作用和较弱的中枢性骨骼肌松弛作用，镇静催眠作用比硝西泮强2.4～4倍。睡醒后精神爽快、无后遗效应。

【 药动学 】

口服吸收良好，1～2h血药浓度达峰值。可迅速分布于全身各组织，以肝、脑的血药浓度最高，可透过胎盘屏障。在肝脏代谢，代谢物经肾排泄，也可泌入乳汁。半衰期β相为2h左右，其代谢物的半衰期β相约为4h。

【 适应证 】

1.主要用于失眠、焦虑、紧张、恐惧。 2.还可用于癫痫和惊厥。 3.麻醉前给药。

【 禁忌证 】

1.重症肌无力患者；2.新生儿。

【 注意事项 】

1.慎用：

(1)老年高血压患者；

(2)心、肝、肾功能不全者；

(3)中枢神经系统处于抑制状态的急性酒精中毒者；

(4)有药物滥用或成瘾史者；

(5)运动过多症患者；

(6)低蛋白血症患者；

(7)严重的精神抑郁者；

(8)急性闭角型青光眼者；

(9)严重慢性阻塞性肺病患者；

(10)孕妇及哺乳妇女。

2.药物对儿童的影响：

本药对小儿特别是幼儿的中枢神经异常敏感，新生儿不易将本类药代谢为无活性的产物，可导致中枢神经持久抑制。

3.药物对老人的影响：老年人的中枢神经对本药也较敏感，可出现呼吸暂停、低血压、心动过缓甚至心脏停搏。

4.药物对妊娠的影响：本药可透过胎盘。在妊娠初期三个月，有增加胎儿致畸的危险，除用作抗癫痫外，在此期间尽量勿用。孕妇长期使用可引起成瘾，使新生儿呈现撤药症状。在妊娠最后数周用于催眠，可使新生儿中枢神经活动有所抑制，在分娩前或分娩时使用本药，可导致新生儿肌张力软弱。

5.药物对哺乳的影响：代谢产物可分泌入乳汁，乳母服用可使婴儿体内本药及其代谢产物积聚，使婴儿嗜睡，甚至喂养困难、体重减轻。

【 不良反应 】

本药使用常规剂量时无明显不良反应。用量过大时，可出现轻微乏力、口干、嗜睡、头胀、头晕等，减小剂量可自行消失。

【 用法用量 】

口服给药：

1.镇静：每次1～2mg，每天3次。

2.催眠：每次1～2mg，睡前服。

3.抗癫痫：每次2～4mg，每天3次。

4.麻醉前给药：每次2～4mg，手术前1h服用。

【 专家点评 】

镇静催眠作用比硝西泮强2.5～4倍，本品特点为作用强、用量小、毒副作用小、对肝、肾功能及骨髓、血、尿常规无影响、治疗安全范围大。

【 药物相互作用 】

1.与全麻药、镇痛药、单胺氧化化酶抑制药、三环类抗抑郁药、可乐定等合用时，可相互增效；阿片类镇痛药的用量至少应先减至1/3，而后按需逐渐增加。

2.与西咪替丁合用时，可使本药清除减慢，血药浓度升高。

3.与酮康唑合用可升高艾司唑仑的血药浓度，增加其不良反应(如过度镇静、乏力、口齿不清、反应迟钝和其他神经精神障碍)，延长其作用时间。

4.与利托那韦合用，可增加本药的血药浓度，有引起过度镇静与抑制呼吸的潜在危险。

5.与易产生依赖性的药物合用，依赖性增加。

6.与钙离子通道拮抗药合用，可使血压下降加重。

7.与卡马西平合用时，由于卡马西平诱导肝微粒体酶，使卡马西平和(或)本药的血药浓度下降，清除半衰期缩短。

8.本药与左旋多巴合用，可降低后者疗效。

9.与扑米酮合用，可引起癫痫发作类型改变，需调整扑米酮的用量。

10.与普萘洛尔合用时，可导致癫痫发作的类型和(或)频率改变，应及时调整剂量，包括普萘洛尔在内的血药浓度可能明显降低。

11.服用本药时饮酒，可使本药增效。

12.烟草中的某些成分可诱导肝药酶，从而加速艾司唑仑经肝脏的代谢清除。

治疗相关疾病

失眠

重症肌无力

低血压

英文：EURODIN 1mg/2mg. TABLETS

ユーロジン1mg/2mg錠

艾司唑仑

日文：ユーロジン1mg/2mg錠

中文：艾司唑仑

有效成分

英文：Estazolam

日文：エスタゾラム

中文：舒乐安定

生产厂家：武田制药

一般名

エスタゾラム（Estazolam）〔JAN〕

[Drug name] estazolam

[English name] Estazolam

[

alias] triazolidine; triazolam chloride; sulpiride; sultanidine; anxiety; Estazolamum; Eurodin; Surazapam; Surazepam

[Category] Nervous system drugs/sedative and hypnotic drugs/benzodiazepines

[Formulation]

1. Tablet: 1 mg, 2 mg; 2. Injection (powder): 2 mg.

[Pharmacological action]

Isostazol is a highly effective benzodiazepine sedative hypnotic agent that acts on the limbic system and brainstem reticular structure, and can reduce the oxidation process of brain tissue and strengthen the protective inhibition of the brain. It has strong sedative, hypnotic, anticonvulsant, anti-anxiety and weaker central skeletal muscle relaxation, and the sedative and hypnotic effect is 2.4 to 4 times stronger than that of nitrite. After waking up, the spirit is refreshing and there is no aftereffect.

[Pharmacokinetics]

Oral absorption was good, and the blood concentration reached a peak at 1 to 2 hours. It can be rapidly distributed in all tissues of the body, with the highest blood concentration in the liver and brain, which can penetrate the placental barrier. Metabolized in the liver, metabolites are excreted in the kidneys and can also be secreted into the milk. The half-life β phase is about 2 h, and the half-life β phase of its metabolite is about 4 h.

[Indications]

1. Mainly used for insomnia, anxiety, nervousness, and fear. 2. Can also be used for epilepsy and convulsions. 3. Administration before anesthesia.

[Contraindications]

1. Patients with myasthenia gravis; 2. Newborns.

[Notes]

1. Use with caution:

(1) elderly hypertensive patients;

(2) Heart, liver, and kidney dysfunction;

(3) Acute alcoholism in which the central nervous system is in a state of inhibition;

(4) Those with a history of drug abuse or addiction;

(5) Patients with hyperkinesia;

(6) Patients with hypoproteinemia;

(7) severe mental depression;

(8) Acute angle-closure glaucoma;

(9) Patients with severe chronic obstructive pulmonary disease;

(10) Pregnant women and lactating women.

2. Effects of drugs on children:

The drug is sensitive to central nervous system abnormalities in children, especially young children. It is not easy for newborns to metabolize this drug into inactive products, which may lead to persistent inhibition of central nervous system.

3. The effect of drugs on the elderly: The central nervous system of the elderly is also sensitive to the drug, and may have apnea, hypotension, bradycardia or even cardiac arrest.

4. The effect of drugs on pregnancy: This drug can pass through the placenta. In the first three months of pregnancy, there is a risk of increasing fetal teratogenicity. In addition to being used as anti-epilepsy, try not to use it during this period. Long-term use of pregnant women can cause addiction, so that newborns show withdrawal symptoms. Hypnosis in the last few weeks of pregnancy can inhibit neonatal central nervous system activity. The use of this medicine before or during childbirth can lead to weak muscle tone in newborns.

5. The effect of drugs on breastfeeding: Metabolites can be secreted into milk. The use of lactating mothers can cause the drug and its metabolites to accumulate in the baby, making the baby sleepy and even feeding and losing weight.

[Adverse Reactions]

There was no significant adverse reaction when the drug was used at regular doses. When the dosage is too large, slight fatigue, dry mouth, lethargy, head swelling, dizziness, etc. may occur, and the dose may be eliminated by itself.

【 Usage and Usage 】

Oral administration:

1. Sedation: 1 to 2 mg each time, 3 times a day.

2. Hypnosis: 1~2mg each time, take it before going to bed.

3. Anti-epilepsy: 2 to 4 mg each time, 3 times a day.

4. Pre-anesthesia administration: 2 to 4 mg each time, 1 hour before surgery.

[Expert Comments]

The sedative and hypnotic effect is 2.5 to 4 times stronger than that of N. sinensis. This product is characterized by strong action, small dosage, small side effects, no effect on liver and kidney function and bone marrow, blood and urine routine, and a wide range of treatment safety.

[Drug Interactions]

1. When combined with general anesthetics, analgesics, monoamine oxidase inhibitors, tricyclic antidepressants, clonidine, etc., it can synergize with each other; the dosage of opioid analgesics should be reduced at least first. To 1/3, and then gradually increase as needed.

2. When combined with cimetidine, the drug can be cleared and the blood concentration is increased.

3. Combined with ketoconazole can increase the plasma concentration of estazolam, increase its adverse reactions (such as excessive sedation, fatigue, slurred speech, unresponsiveness and other neuropsychiatric disorders), prolong its action time .

4. In combination with ritonavir, it can increase the blood concentration of the drug, and has the potential to cause excessive sedation and inhibition of breathing.

5. In combination with drugs that are prone to dependence, the dependence increases.

6. In combination with calcium channel antagonists, blood pressure can be increased.

7. When used in combination with carbamazepine, the carbamazepine induces liver microsomal enzymes, which lowers the blood concentration of carbamazepine and/or the drug, and shortens the elimination half-life.

8. This medicine is combined with levodopa to reduce the efficacy of the latter.

9. In combination with primidone, it can cause changes in the type of seizures, and the dosage of primidone should be adjusted.

10. When combined with propranolol, it can cause changes in the type and/or frequency of seizures. The dose should be adjusted in time, and the plasma concentration including propranolol may be significantly reduced.

11. Drinking alcohol while taking this medicine can make the drug more effective.

12. Certain components of tobacco induce hepatic enzymes, thereby accelerating the metabolic clearance of estazolam through the liver.

Treatment related diseases

Insomnia

Myasthenia gravis

hypotension

English: EURODIN 1mg/2mg. TABLETS

ユーロジン1mg/2mg ingot

Isozolam

Japanese: ユーロジン 1mg/2mg ingot

Chinese: estazolam

Active ingredient

English: Estazolam

Japanese: エスタゾラム

Chinese: Shule Stabilization

Manufacturer: Takeda Pharmaceutical

General name

Eastazolam [JAN]

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 详细处方信息以本药内容附件PDF文件（201892621140836.pdf）的“Prescribing Information”为准
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