药品详细
Bumetanide(布美他尼)
化学结构式图
中文名
布美他尼
英文名
Bumetanide
分子式
C17H20N2O5S
化学名
3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid
分子量
Average: 364.416
Monoisotopic: 364.10929245
Monoisotopic: 364.10929245
CAS号
28395-03-1
ATC分类
C03C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A sulfamyl diuretic. [PubChem]
生产厂家
- Baxter healthcare corp anesthesia and critical care
- Bedford laboratories div ben venue laboratories inc
- Hospira inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Sandoz inc
- Teva parenteral medicines inc
- Validus pharmaceuticals inc
封装厂家
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Cardinal Health
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Eon Labs
- F Hoffmann-La Roche Ltd.
- Heartland Repack Services LLC
- Hospira Inc.
- Ivax Pharmaceuticals
- Major Pharmaceuticals
- Mckesson Corp.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Physicians Total Care Inc.
- Sandhills Packaging Inc.
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- Vangard Labs Inc.
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 treatment of edema associated with congestive heart failure, hepatic and renal disease including the nephrotic syndrome. | ||||||
| Pharmacodynamics | Bumetanide is a loop diuretic of the sulfamyl category to treat heart failure. It is often used in patients in whom high doses of furosemide are ineffective. There is however no reason not to use bumetanide as a first choice drug. The main difference between the two substances is in bioavailability. It is said to be a more predictable diuretic, meaning that the predictable absorption is reflected in a more predictable effect. Bumetanide is 40 times more potent than furosemide (for patients with normal renal function). | ||||||
| Mechanism of action | Bumetanide interferes with renal cAMP and/or inhibits the sodium-potassium ATPase pump. Bumetanide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. | ||||||
| Absorption | Bumetanide is completely absorbed (80%), and the absorption is not altered when taken with food. Bioavailability is almost complete. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | 97% | ||||||
| Metabolism |
45% is secreted unchanged. Urinary and biliary metabolites are formed by oxidation of the N-butyl side chain.
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| Route of elimination | Oral administration of carbon-14 labeled Bumex to human volunteers revealed that 81% of the administered radioactivity was excreted in the urine, 45% of it as unchanged drug. Biliary excretion of Bumex amounted to only 2% of the administered dose. | ||||||
| Half life | 60-90 minutes | ||||||
| Clearance |
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| Toxicity | Overdosage can lead to acute profound water loss, volume and electrolyte depletion, dehydration, reduction of blood volume and circulatory collapse with a possibility of vascular thrombosis and embolism. Electrolyte depletion may be manifested by weakness, dizziness, mental confusion, anorexia, lethargy, vomiting and cramps. Treatment consists of replacement of fluid and electrolyte losses by careful monitoring of the urine and electrolyte output and serum electrolyte levels. | ||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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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 |
|---|---|
| Amikacin | Increased ototoxicity |
| Cisplatin | Increased ototoxicity |
| Colesevelam | Bile acid sequestrants such as colesevelam may decrease the absorption of loop diuretics such as bumetanide. Monitor for decreased serum concentrations/therapeutic effects of loop diuretics if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam. |
| Deslanoside | Possible electrolyte variations and arrhythmias |
| Digitoxin | Possible electrolyte variations and arrhythmias |
| Digoxin | Possible electrolyte variations and arrhythmias |
| Gentamicin | Increased ototoxicity |
| Ginseng | Ginseng may decrease the therapeutic effect of diuretic, bumetanide. |
| Ibuprofen | The NSAID, ibuprofen, may antagonize the diuretic and antihypertensive effects of the loop diuretic, bumetanide. |
| Indomethacin | The NSAID, indomethacin, may decrease the diuretic and antihypertensive effects of the loop diuretic, bumetanide. |
| Kanamycin | Increased ototoxicity |
| Netilmicin | Increased ototoxicity |
| Streptomycin | Increased ototoxicity |
| Sulindac | The NSAID, sulindac, decreases the diuretic and antihypertensive effects of the loop diuretic, bumetanide. |
| Tobramycin | Increased ototoxicity |
| Trandolapril | The loop diuretic, Bumetanide, may increase the hypotensive effect of Trandolapril. Bumetanide may also increase the nephrotoxicity of Trandolapril. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
食物相互作用
- Take with food to reduce irritation.
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