CAse inhibitors - Nonmercurial diuretics

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Chapter: Medicinal Chemistry : Diuretics

Nonmercurial diuretics : CAse inhibitors - Synthesis and Drug Profile - i. Acetazolamide (Acetamide, Diamox, Ana) ii. Methazolamide (Neptazane) iii. Ethoxazolamide (Carolrase) iv. Diclofenamide (Daranide, Oratrol) v. Disulfamide (Diluen)


SYNTHESIS AND DRUG PROFILE


Nonmercurial diuretics


CAse inhibitors

Mode of action: CAse is an enzyme that is present in the PT that catalyses the reversible reaction, H2O + CO2 ↔ H2CO3. Carbonic acid spontaneously ionizes as H2 CO3 ↔ H++ HCO . CAse inhibitors reversibly inhibits CAse resulting in the slowing of hydration of CO2 and decrease the availability of H+ to exchange with luminal Na+ through Na+ H+ antiporter.


i. Acetazolamide (Acetamide, Diamox, Ana)


Synthesis


Properties and uses: Acetazolamide is a white crystalline powder, soluble in dilute alkali hydroxide solutions, slightly soluble in water and in alcohol. It is a CAse inhibitor effective for the adjunctive treatment of oedema due to congestive heart failure, drug induced oedema, absence and other centrencephalic epilepsies, chronic simple (open angled) glaucoma, secondary glaucoma when it is desired to lower intra-ocular pressure prior to surgery. Acetazolamide is employed in the treatment of drug-induced oedema, oedema caused by congestive heart failure, and petitmal epilepsy.

Assay: Dissolve the sample in dimethylformamide and titrate against 0.1 M ethanolic sodium hydroxide. Determine the end point potentiometrically.

Dose: Usual dose is 250 mg 2 to 4 times/day.

Dosage forms: Acetazolamide tablets I.P., B.P.


ii. Methazolamide (Neptazane)


Synthesis


Properties and uses: Methazolamide is available as white or yellow crystalline powder with a slight odour, which is soluble in water, in alcohol or in acetone and dimethyl formamide. It is a more potent CA inhibitor than the prototypic acetazolamide and it is seldom used as a diuretic. Methazolamide displays improved penetration into the eye, a property that contributes to its usefulness in the treatment of glaucoma. It is employed in the treatment of drug-induced oedema, oedema caused by congestive heart failure and petitmal epilepsy.

Dose: 100 to 600 mg per day; usually 50 to 100 mg 2 to 3 times/day.


iii. Ethoxazolamide (Carolrase)


Synthesis


Uses: It is mainly used in acute angle-closure glaucoma, chronic simole glaucoma, and secondary glaucoma.

Dose: Usually 125 mg 2 to 4 times per day.


iv. Diclofenamide (Daranide, Oratrol)


Synthesis


Properties and uses: It exists as white crystalline powder with a characteristic odour, soluble in water, sodium hydroxide, alcohol, and ether. Used as a diuretic and for the treatment of primary and the acute phase of secondary glaucoma. It produces less acidotic refractoriness to diuretic action than acetazolamide. It is used for the treatment of both primary and secondary glaucoma.

Dose: 50 to 300 mg per day; usually 25 to 50 mg 1 to 3 times daily.


v. Disulfamide (Diluen)


Synthesis


Uses: It is used in the treatment of oedema.

Dose: For oedema, usual, initial dose is 200 mg per day for 5 days a week or on alternate days, reduced to 100 mg per day.


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