Hydrothiazides - Nonmercurial diuretics

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Chapter: Medicinal Chemistry : Diuretics

Nonmercurial diuretics : Hydrothiazides - Synthesis and Drug Profile - i. Hydrochlorthiazide (Hydride, Aquazide, Bpzide) ii. Hydroflumethiazide (Naturetin, Neonaclex) iii. Bendroflumethiazide (Diucardin, Saluron) iv. Cyclothiazide (Anhydron, Fludil) v. Cyclopenthiazide (Navidrex) vi. Methylclothiazide (Enduron) vii. Trichlormethiazide (Metahydrin, Naqua) viii. Polythiazide (Renese)


SYNTHESIS AND DRUG PROFILE


Nonmercurial diuretics


Hydrothiazides


i. Hydrochlorthiazide (Hydride, Aquazide, Bpzide)


Synthesis


Properties and uses: Hydrochlorthiazide is a white crystalline powder, which is soluble in acetone and dilute alkali hydroxide solutions, but sparingly soluble in alcohol. It is similar to chlorothiazide, but it is ten times more potent. Used in the treatment of oedema associated with congestive heart failure, renal, and hepatic disorders.

Assay: Dissolve the sample in dimethyl sulphoxide and titrate against 0.1 M tetrabutylammonium hydroxide in 2-propanol. Determinine the end point potentiometrically.

Dose: 25 to 200 mg per day; usually 50 mg once or twice daily.

Dosage forms: Hydrochlorthiazide tablets I.P., B.P., Co-amilozide oral solution B.P., Co-amilozide tablets B.P., Co-triamterzide tablets B.P.


ii. Hydroflumethiazide (Naturetin, Neonaclex)


Synthesis


Properties and uses: Hydroflumethiazide is a white crystalline powder, practically insoluble in water and ether, soluble in ethanol. It is a potent oral thiazide diuretic, used in the management of oedema associated with cardiac failure, premenstrual tension, and hepatic cirrhosis.

Assay: Dissolve the sample in anhydrous pyridine and titrate against 0.1 M tetrabutylammonium hydroxide. Determine the end point potentiometrically.

Dose: 25 to 200 mg, usually 50 to 100 mg daily.

Dosage forms: Hydroflumethiazide tablets B.P.


iii. Bendroflumethiazide (Diucardin, Saluron)


Synthesis


Properties and uses: Bendroflumethiazide is a white crystalline powder, practically insoluble in water, soluble in acetone and ethanol. A potent orally effective thiazide diuretic possesses both diuretic and antihypertensive actions.

Assay: Dissolve the sample in dimethyl sulphoxide and titrate against 0.1 M tetrabutylammonium hydroxide in 2-propanol. Determine the end point potentiometrically.

Dose: Initial, diuretic 5 to 20 mg per day; maintenance, 2.5 to 5 mg daily; as antihypertensive, initially 5 to 20 mg per day, maintenance, 2.5 to 15 mg per day.

Dosage forms: Bendroflumethiazide tablets B.P.


iv. Cyclothiazide (Anhydron, Fludil)


Synthesis


Properties and uses: It exists as white, odourless powder, soluble in alcohol or methanol but insoluble in water, chloroform, or ether. Used as both diuretic and antihypertensive.

Dose: Usual initial dose as diuretic, 1 to 2 mg/day; maintenance, 1 to 2 mg on alternate days, or 2 or 3 times/week; as antihypertensive, 2 mg 1 to 3 times daily.


v. Cyclopenthiazide (Navidrex)


Synthesis


Properties and uses: Cyclopenthiazide is a white powder, practically insoluble in water, soluble in acetone and ethanol, very slightly soluble in ether. It is used in the treatment of oedema associated with congestive heart failure and renal and hepatic disorders.

Assay: Dissolve the sample in butylamine and titrate against 0.1 M tetrabutylammonium hydroxide using magneson solution as indicator.

Dose: For oedema, usual, initial dose is 0.5 to 1 mg per day, reduced to 250 to 500 μg/day or 500 μg on alternate days; for hypertension, usually 250 to 500 μg/day either alone, or in conjunction with other antihypertensive agents.

Dosage forms: Cyclopenthiazide tablets B.P.


vi. Methylclothiazide (Enduron)


Synthesis


Properties and uses: It is a white crystalline powder, odourless, tasteless, soluble in water, alcohol, chloroform or ether, and acetone. It is effective as a diuretic and antihypertensive agent. It is about 100 times more potent than chlorothiazide.

Dose: Usual dose maintenance, as diuretic and antihypertensive is 2.5 to 10 mg once per day,


vii. Trichlormethiazide (Metahydrin, Naqua)


Synthesis


Properties and uses: It is a white crystalline powder, odourless, sometimes with a characteristic odour, soluble in water, alcohol, chloroform, or ether. It is used as an antihypertensive agent.

Dose: The usual dose is 2 to 4 mg twice daily; maintenance 2 to 4 mg once/day.


viii. Polythiazide (Renese)


Properties and uses: It is a white crystalline powder with characteristic odour, soluble in water, alcohol, chloroform, or ether, acetone and aqueous alkali carbonates or hydroxides. Used as potent diuretic and antihypertensive agent.

Assay: Dissolve the sample in methanol and measure the absorbance after suitable dilutions at the maxima of 268 nm using ultraviolet spectrophotometer.

Dose: As diuretic, usually 1 to 4 mg/ day; as antihypertensive, 2 to 4 mg as required.

Synthesis


Dosage forms: Polythiazide tablets B.P.


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