药品详细
Pentazocine(喷他佐辛)
化学结构式图
中文名
喷他佐辛
英文名
Pentazocine
分子式
C19H27NO
化学名
(1R,9R,13R)-1,13-dimethyl-10-(3-methylbut-2-en-1-yl)-10-azatricyclo[7.3.1.0^{2,7}]trideca-2,4,6-trien-4-ol
分子量
Average: 285.4238
Monoisotopic: 285.209264491
Monoisotopic: 285.209264491
CAS号
359-83-1
ATC分类
N02A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
生产厂家
- Hospira inc
- Sanofi aventis us llc
封装厂家
- A-S Medication Solutions LLC
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Hospira Inc.
- Kaiser Foundation Hospital
- Keltman Pharmaceuticals Inc.
- Mallinckrodt Inc.
- Nucare Pharmaceuticals Inc.
- Ohm Laboratories Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmedix
- Physicians Total Care Inc.
- Ranbaxy Laboratories
- Rebel Distributors Corp.
- Sanofi-Aventis Inc.
- Southwood Pharmaceuticals
- Stat Rx Usa
- Watson Pharmaceuticals
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 the relief of moderate to severe pain. |
| Pharmacodynamics | Pentazocine is a potent analgesic which when administered orally in a 50 mg dose appears equivalent in analgesic effect to 60 mg (1 grain) of codeine. Onset of significant analgesia usually occurs between 15 and 30 minutes after oral administration, and duration of action is usually three hours or longer. Onset and duration of action and the degree of pain relief are related both to dose and the severity of pretreatment pain. Pentazocine weakly antagonizes the analgesic effects of morphine and meperidine; in addition, it produces incomplete reversal of cardiovascular, respiratory, and behavioral depression induced by morphine and meperidine. Pentazocine has about 1/50 the antagonistic activity of nalorphine. It also has sedative activity. |
| Mechanism of action | The preponderance of evidence suggests that pentazocine antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. |
| Absorption | Well absorbed from the gastro-intestinal tract. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Hepatic
|
| Route of elimination | Not Available |
| Half life | 2 to 3 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
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| Pathways | Not Available |
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 |
|---|---|
| Alvimopan | Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan. |
| Triprolidine | The CNS depressants, Triprolidine and Pentazocine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. |
食物相互作用
- Take without regard to meals. Avoid alcohol.
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