Thiazide Diuretics and Related Drugs

Physiological Disposition of a New Diuretic, 14C-Metolazone, in Dogs

“…The extent to which thiazides and other related diuretics are metabolized in mammals has been reported to be variable. Chlorothiazide, hydrochlorothiazide, flumethiazide, and hydroflumethiazide have been reported to be rapidly excreted without undergoing metabolic transformation (16). By contrast, bendroflumethiadde, trichlormethiazide (16).…”

“…Chlorothiazide, hydrochlorothiazide, flumethiazide, and hydroflumethiazide have been reported to be rapidly excreted without undergoing metabolic transformation (16). By contrast, bendroflumethiadde, trichlormethiazide (16). and polythiazide (16, 20, 21) are partially metabolized by the dog.…”

Diuretics

“…1) evolved from the group of sulfonamide drugs known to inhibit the enzyme carbonic anhydrase. Both are derived from chlorodisulfamoyl-aniline in a condensation reaction with formic acid or formaldehyde, respectively (PETERS and ROCH-RAMEL 1969;NOVELLO and SPRAGUE 1957;SPRAGUE 1958;DESTEVENS 1963;BEYER 1958). Two of the first thiazide-type diuretics synthesized were chlorothiazide and hydrochlorothiazide.…”

“…Two of the first thiazide-type diuretics synthesized were chlorothiazide and hydrochlorothiazide. An excellent detailed account of the history and development of these diuretics and a listing of the structures of 50 thiazides and related diuretics was published in the previous edition of this handbook (PETERS and ROCH-RAMEL 1969). They were selected because of their ability to increase renal chloride and sodium excretion.…”

“…Several excellent and extensive reviews examine the history, structure and chemistry of these agents in great detail (PETERS and ROCH-RAMEL 1969;BEYER and BAER 1961;SPRAGUE 1968;MAREN 1976;ALLEN 1983;LANT 1985). They are benzothiadiazines or analogs and derivatives of the carbonic anhydraseinhibiting sulfonamides.…”