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White acicular crystal or crystalline powder, odorless, tasteless. Almost insoluble in water or dilute hydrochloric acid, soluble in ethanol or ethyl acetate, soluble in acetone, glacial acetic acid, slightly soluble in chloroform or ether. Indapamide is currently used in China as an over-the-counter diuretic antihypertensive drug, with good efficacy, stable antihypertensive, less side effects and other advantages. Indapamide has the dual effect of diuretic and calcium antagonism, by inhibiting the Na+ reabsorption of proximal distal convoluted tube. it produces diuretic effect, and blocks the Ca2+ influx. It is highly selective to vascular smooth muscle, dilates peripheral small vessels, and produces hypotensive effect.
But the effect on vascular smooth muscle stronger diuretic effect, below the diuretic doses can step-down, higher doses showed diuretic effect, but no thiazide diuretic shortcomings, namely not cause orthostatic hypotension, flush and reflective tachycardia, on blood picture, metabolism of blood fat, sugar and renal function also had no obvious effect, therapeutic doses of heart rate, cardiac output, no significant changes in electrocardiogram (ecg) were on the central nervous system and plant nerve has no obvious effect. The antihypertensive effect was produced by oral administration for 2-3h, and the effect was maintained for 24h. Diuretic effect appeared for 3h, and reached the maximum effect for 4 ~ 6h.
Different from other diuretics, this product is highly soluble in fat. After oral absorption, it has the highest concentration in liver and kidney plasma, while the concentration in heart, lung, muscle and fat is relatively low. Excretion from the kidneys by metabolites and by 5% protoplasm. Indapamide is suitable for mild and moderate primary hypertension, can also be used for congestive heart failure caused by water sodium retention, with renal failure are also applicable to the patients with high blood pressure, diabetes, hyperlipidemia, use antihypertensive effect is remarkable, and beta blockers used curative effect is better, because have a diuretic effect, can cause hypokalemia, can complement potassium at the same time.
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