药品详细
Bendroflumethiazide(苄氟噻嗪)
化学结构式图
中文名
苄氟噻嗪
英文名
Bendroflumethiazide
分子式
C15H14F3N3O4S2
化学名
3-benzyl-1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2H-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
分子量
Average: 421.415
Monoisotopic: 421.037781946
Monoisotopic: 421.037781946
CAS号
73-48-3
ATC分类
C03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)
生产厂家
- Apothecon inc div bristol myers squibb
封装厂家
- E.R. Squibb and Sons LLC
- King Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Professional Co.
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 high blood pressure and management of edema related to heart failure. | ||||||
Pharmacodynamics | Bendroflumethiazide, a thiazide diuretic, removes excess water from the body by increasing how often you urinate (pass water) and also widens the blood vessels which helps to reduce blood pressure. It inhibits Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. | ||||||
Mechanism of action | As a diuretic, bendroflumethiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like bendroflumethiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of bendroflumethiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. | ||||||
Absorption | Absorbed relatively rapidly after oral administration | ||||||
Volume of distribution | Not Available | ||||||
Protein binding | 96% | ||||||
Metabolism |
Not Available
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Route of elimination | Not Available | ||||||
Half life | 8.5 hours | ||||||
Clearance | Not Available | ||||||
Toxicity | Not Available | ||||||
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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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Deslanoside | Possible electrolyte variations and arrhythmias |
Diazoxide | Significant hyperglycemic effect |
Digitoxin | Possible electrolyte variations and arrhythmias |
Digoxin | Possible electrolyte variations and arrhythmias |
Dofetilide | Increased risk of cardiotoxicity and arrhythmias |
Lithium | The thiazide diuretic, bendroflumethiazide, may increase serum levels of lithium. |
Trandolapril | The thiazide diuretic, Bendroflumethiazide, may increase the hypotensive effect of Trandolapril. Bendroflumethiazide may also increase the nephrotoxicity of Trandolapril. Monitor for postural hypotension at initiation of concomitant therapy and renal dysfunction during chronic therapy. |
Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
食物相互作用
- Take with food to increase bioavailability.