药品详细
Amiloride(阿米洛利)
化学结构式图
中文名
阿米洛利
英文名
Amiloride
分子式
C6H8ClN7O
化学名
3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide
分子量
Average: 229.627
Monoisotopic: 229.04788562
Monoisotopic: 229.04788562
CAS号
2016-88-8
ATC分类
C03D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman’s The Pharmacological Basis of Therapeutics, 9th ed, p705)
生产厂家
- Paddock laboratories inc
- Par pharmaceutical inc
- Sigmapharm laboratories llc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
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适应症
药理
| Indication | For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension. | ||||||
| Pharmacodynamics | Amiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements. | ||||||
| Mechanism of action | Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone. | ||||||
| Absorption | Readily absorbed following oral administration. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Not Available | ||||||
| Metabolism |
Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys.
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| Route of elimination | Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours. | ||||||
| Half life | Plasma half-life varies from 6 to 9 hours. | ||||||
| Clearance | Not Available | ||||||
| Toxicity | No data are available in regard to overdosage in humans. The oral LD50 of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance. | ||||||
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理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
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药物相互作用
| Drug | Interaction |
|---|---|
| Benazepril | Increased risk of hyperkalemia |
| Candesartan | Increased risk of hyperkalemia |
| Captopril | Increased risk of hyperkalemia |
| Cilazapril | Increased risk of hyperkalemia |
| Dihydroquinidine barbiturate | Decreases the antiarrhythmic effect of quinidine |
| Enalapril | Increased risk of hyperkalemia |
| Eplerenone | Increased risk of hyperkalemia. Monitor serum potassium levels during concomitant threapy. |
| Eprosartan | Increased risk of hyperkalemia |
| Forasartan | Increased risk of hyperkalemia |
| Fosinopril | Increased risk of hyperkalemia |
| Irbesartan | Increased risk of hyperkalemia |
| Lisinopril | Increased risk of hyperkalemia |
| Losartan | Increased risk of hyperkalemia |
| Moexipril | Increased risk of hyperkalemia |
| Perindopril | Increased risk of hyperkalemia |
| Polystyrene sulfonate | Risk of alkalosis in renal impairment |
| Potassium | Increased risk of hyperkalemia |
| Quinapril | Increased risk of hyperkalemia |
| Quinidine | Amiloride may decrease the therapeutic effect of quinidine. Monitor for changes in the therapeutic and adverse effects of quinidine if amiloride if initiated, discontinued or dose changed. |
| Quinidine barbiturate | Decreases the antiarrhythmic effect of quinidine |
| Ramipril | Increased risk of hyperkalemia |
| Saprisartan | Increased risk of hyperkalemia |
| Spirapril | Increased risk of hyperkalemia |
| Tasosartan | Increased risk of hyperkalemia |
| Telmisartan | Telmisartan may increase the hyperkalemic effect of Amiloride. Monitor for increased serum potassium concentrations during concomitant therapy. |
| Trandolapril | Increased risk of hyperkalemia. Monitor serum potassium levels. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
| Valsartan | Increased risk of hyperkalemia |
食物相互作用
- Avoid drastic changes in dietary habit.
- Avoid natural licorice.
- Avoid salt substitutes containing potassium.
- Take with food to reduce irritation.
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