药品详细
Remifentanil(瑞芬太尼)
化学结构式图
中文名
瑞芬太尼
英文名
Remifentanil
分子式
C20H28N2O5
化学名
methyl 1-(3-methoxy-3-oxopropyl)-4-(N-phenylpropanamido)piperidine-4-carboxylate
分子量
Average: 376.4467
Monoisotopic: 376.199822016
Monoisotopic: 376.199822016
CAS号
132875-61-7
ATC分类
N01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Remifentanil (marketed by Abbott as Ultiva) is a potent ultra short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is a specific mu-type-opioid receptor agonist. Hence, it causes a reduction in sympathetic nervous system tone, respiratory depression and analgesia.
生产厂家
- Bioniche teoranta
封装厂家
参考
Synthesis Reference | Not Available |
General Reference | Not Available |
剂型
规格
化合物类型
Type | small molecule |
Classes |
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Substructures |
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适应症
药理
Indication | For use during the induction and maintenance of general anesthesia. | ||||||
Pharmacodynamics | Remifentanil is an opioid agonist with rapid onset and peak effect and ultra-short duration of action. The opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone. The analgesic effects of remifentanil are rapid in onset and offset. Its effects and side effects are dose dependent and similar to other opioids. Remifentanil in humans has a rapid blood-brain equilibration half-time of 1 ± 1 minutes (mean ± SD) and a rapid onset of action. | ||||||
Mechanism of action | Remifentanil is a µ-opioid agonist with rapid onset and peak effect, and short duration of action. The µ-opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone. | ||||||
Absorption | Not Available | ||||||
Volume of distribution |
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Protein binding | 70% (bound to plasma proteins) | ||||||
Metabolism |
By hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases.
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Route of elimination | Remifentanil is an esterase-metabolized opioid. The carboxylic acid metabolite is essentially inactive (1/4600 as potent as remifentanil in dogs) and is excreted by the kidneys with an elimination half-life of approximately 90 minutes. | ||||||
Half life | 1-20 minutes | ||||||
Clearance |
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Toxicity | Not Available | ||||||
Affected organisms |
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Pathways |
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理化性质
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State | solid | |||||||||||||||||||||||||||||||||||||||
Experimental Properties |
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Predicted Properties |
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药物相互作用
Drug | Interaction |
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Tranylcypromine | Possible increased risk of serotonin syndrome. |
Triprolidine | The CNS depressants, Triprolidine and Remifentanil, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. |
食物相互作用
Not Available