药品详细
Acetazolamide(乙酰唑胺)
化学结构式图
中文名
乙酰唑胺
英文名
Acetazolamide
分子式
C4H6N4O3S2
化学名
N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
分子量
Average: 222.245
Monoisotopic: 221.988131458
Monoisotopic: 221.988131458
CAS号
59-66-5
ATC分类
S01E 抗青光眼制剂及缩瞳药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)
生产厂家
- Alra laboratories inc
- Ascot hosp pharmaceuticals inc div travenol laboratories inc
- Bedford laboratories div ben venue laboratories inc
- Duramed pharmaceuticals inc sub barr laboratories inc
- Hospira inc
- Lannett co inc
- Mutual pharmaceutical co inc
- Taro pharmaceutical industries ltd
- Vangard laboratories inc div midway medical co
- Watson laboratories inc
- X gen pharmaceuticals inc
- Zydus pharmaceuticals usa inc
封装厂家
- American Cyanamid Co.
- Amerisource Health Services Corp.
- A-S Medication Solutions LLC
- Barr Pharmaceuticals
- Bedford Labs
- Ben Venue Laboratories Inc.
- Cardinal Health
- Direct Dispensing Inc.
- Dispensing Solutions
- DSM Corp.
- Duramed
- Emcure Pharmaceuticals Ltd.
- Heartland Repack Services LLC
- Innovative Manufacturing and Distribution Services Inc.
- Kaiser Foundation Hospital
- Lannett Co. Inc.
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Prescript Pharmaceuticals
- Resource Optimization and Innovation LLC
- Taro Pharmaceuticals USA
- United Research Laboratories Inc.
- Watson Pharmaceuticals
- X-Gen Pharmaceuticals
- Zydus 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 adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma |
| Pharmacodynamics | Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion, in the treatment of certain convulsive disorders and in the promotion of diuresis in instances of abnormal fluid retention. Acetazolamide is not a mercurial diuretic. Rather, it is a nonbacteriostatic sulfonamide possessing a chemical structure and pharmacological activity distinctly different from the bacteriostatic sulfonamides. |
| Mechanism of action | The anticonvulsant activity of Acetazolamide may depend on a direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | 98% |
| Metabolism |
Not Available
|
| Route of elimination | Not Available |
| Half life | 3 to 9 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| 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 |
|---|---|
| Acetylsalicylic acid | Acetylsalicylic acid at high dose increases the effect of the carbonic anhydrase inhibitor, acetazolamide. |
| Bismuth Subsalicylate | The salicylate, bismuth subsalicylate, at high dose increases the effect of the carbonic anhydrase inhibitor, acetazolamide. |
| Brinzolamide | As both brinzolamide and acetazolamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible. |
| Cyclosporine | Acetazolamide may increase the effect and toxicity of cyclosporine. |
| Memantine | Possible increased levels of memantine |
| Tobramycin | Increased risk of nephrotoxicity |
| Topiramate | Additive renal carbonic anhydrase inhibition may occur increasing the risk of crystaluria and renal calculi. Increased risk of nephrolithiasis. Consider altnerate therapy. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
| Triprolidine | The CNS depressants, Triprolidine and Acetazolamide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. |
食物相互作用
- Drink plenty of liquids.
- Take with food; at least 6 hours before bedtime.
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