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Diuril I.V. (Chlorothiazide Sodium Intravenous) - Description and Clinical Pharmacology

 
 



DESCRIPTION

Intravenous Sodium DIURIL * (Chlorothiazide Sodium) is a diuretic and antihypertensive. It is 6-chloro-2 H -1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide monosodium salt and its molecular weight is 317.71. Its empirical formula is C7H5ClN3NaO4S2 and its structural formula is:

Intravenous Sodium DIURIL is a sterile lyophilized white powder and is supplied in a vial containing:

Chlorothiazide sodium equivalent
to chlorothiazide 0.5 g
Inactive ingredients:
Mannitol 0.25 g
Sodium hydroxide to adjust pH.

DIURIL * (Chlorothiazide) is a diuretic and antihypertensive. It is 6-chloro-2 H -1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide. Its empirical formula is C7H6ClN3O4S2 and its structural formula is:

It is a white, or practically white, crystalline powder with a molecular weight of 295.72, which is very slightly soluble in water, but readily soluble in dilute aqueous sodium hydroxide. It is soluble in urine to the extent of about 150 mg per 100 mL at pH 7.

*Registered trademark of MERCK & CO., INC.

CLINICAL PHARMACOLOGY

The mechanism of the antihypertensive effect of thiazides is unknown. DIURIL (Chlorothiazide) does not usually affect normal blood pressure.

DIURIL (Chlorothiazide) affects the distal renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosage all thiazides are approximately equal in their diuretic efficacy.

DIURIL (Chlorothiazide) increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate.

After oral use diuresis begins within 2 hours, peaks in about 4 hours and lasts about 6 to 12 hours. Following intravenous use of Sodium DIURIL, onset of the diuretic action occurs in 15 minutes and the maximal action in 30 minutes.

PHARMACOKINETICS AND METABOLISM

DIURIL is not metabolized but is eliminated rapidly by the kidney; 96 percent of an intravenous dose is excreted unchanged in the urine within 23 hours. The plasma half-life of chlorothiazide is 45-120 minutes. Chlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.

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