药品详细
Naloxone(纳洛酮)
化学结构式图
中文名
纳洛酮
英文名
Naloxone
分子式
C19H21NO4
化学名
(1S,5R,13R,17S)-10,17-dihydroxy-4-(prop-2-en-1-yl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
分子量
Average: 327.3743
Monoisotopic: 327.147058165
Monoisotopic: 327.147058165
CAS号
465-65-6
ATC分类
V03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. [PubChem]
生产厂家
- Abraxis pharmaceutical products
- Astrazeneca lp
- Baxter healthcare corp anesthesia and critical care
- Bristol myers squibb pharma co
- Endo pharmaceuticals inc
- Hospira inc
- International medication system
- International medication systems ltd
- Marsam pharmaceuticals llc
- Smith and nephew solopak div smith and nephew
- Solopak medical products inc
- Watson laboratories inc
- Wyeth ayerst laboratories
封装厂家
- Amphastar Pharmaceuticals
- A-S Medication Solutions LLC
- Bristol-Myers Squibb Co.
- Bryant Ranch Prepack
- Cardinal Health
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Endo Pharmaceuticals Inc.
- General Injectables and Vaccines Inc.
- Hospira Inc.
- Lake Erie Medical and Surgical Supply
- Letco Medical Inc.
- Mallinckrodt Inc.
- Mckesson Corp.
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Reckitt Benckiser Inc.
- Southwood Pharmaceuticals
- Stat Rx Usa
参考
| Synthesis Reference | Not Available |
| General Reference |
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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 complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and the narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol. It is also indicated for the diagnosis of suspected acute opioid overdose. It may also be used as an adjunctive agent to increase blood pressure in the management of septic shock. |
| Pharmacodynamics | Naloxone is an opiate antagonist and prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine. Naloxone is an essentially pure narcotic antagonist, i.e., it does not possess the "agonistic" or morphine-like properties characteristic of other narcotic antagonists; naloxone does not produce respiratory depression, psychotomimetic effects or pupillary constriction. In the absence of narcotics or agonistic effects of other narcotic antagonists, it exhibits essentially no pharmacologic activity. When given intravenously, the onset of action is apparent within 2 minutes. The onset of action is slower if given subcutaneously or intramuscularly. The duration of action also differs between sites of injection and dose. |
| Mechanism of action | While the mechanism of action of naloxone is not fully understood, the preponderance of evidence suggests that naloxone antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. Recently, naloxone has been shown to bind all three opioid receptors (mu, kappa and gamma) but the strongest binding is to the mu receptor. |
| Absorption | Well absorbed following intramuscular injection. |
| Volume of distribution | Following parenteral administration naloxone hydrochloride is rapidly distributed in the body. Naloxone is also very lipophillic and easily crosses the blood-brain-barrier. It can also cross the placenta. |
| Protein binding | Plasma protein binding occurs but is relatively weak. Plasma albumin is the major binding constituent but significant binding of naloxone also occurs to plasma constituents other than albumin. |
| Metabolism |
Naloxone is hepatically metabolized and primarily undergoes glucuronidation to form naloxone-3-glucuronide.
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| Route of elimination | Urine (25%- 40% is excreted as metabolites within 6 hours) |
| Half life | Adults = 30-81 minutes; Neonates = 3.1 ± 0.5 hours. |
| Clearance | Not Available |
| Toxicity | LD50, IV administration, mouse = 150 ± 5 mg/kg; LD50, IV administration, rat = 109 ± 4 mg/kg; |
| 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
食物相互作用
Not Available
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