Gastrointestinal Absorption of Spironolactone

Gantt, ClarenceL.; Gochman, Nathan; Dyniewicz, J. M.

doi:10.1016/s0140-6736(62)92126-8

Cited by 25 publications

(9 citation statements)

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“…canrenone failed to improve its efficacy as a mineralocorticoid antagonist. A similar change in physical form increased the activity of spironolactone fourfold (Gantt, Gochman & Dyniewicz, 1962;Shaldon, Ryder & Garsenstein, 1963), further dissociating the activity of spironolactone from canrenone. These results suggest that canrenone is not the principal active metabolite of spironolactone.…”

Section: Antagonism Of Fludrocortisone By Spironolactone and Canrenonementioning

confidence: 94%

Antagonism of fludrocortisone by spironolactone and canrenone [letter].

Huston¹,

Turner²

1976

Brit J Clinical Pharma

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Section: Antagonism Of Fludrocortisone By Spironolactone and Canrenonementioning

confidence: 94%

Antagonism of fludrocortisone by spironolactone and canrenone [letter].

Huston¹,

Turner²

1976

Brit J Clinical Pharma

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“…The 17-spirolactone steroids do not depress adrenal or pituitary function as measured by the 17-hydroxycorticosteroid concentration in the blood and urine, urinary 17-ketosteroids, and urinary aldosterone excretion (10,22,28). The glucuronide-conjugated fraction of the 17-hydroxycorticosteroids in the urine has been reported to decrease during the administration of SC-8109.…”

Section: Other Pharmacological Effectsmentioning

confidence: 98%

The Aldosterone Blocking Effects of Spirolactones

Drill¹

1962

Japanese Journal of Pharmacology

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“…Spironolactone is' an inducer of hepatic microsomal enzyme hydroxylation (section 3.2.5) which is important to remember when drugs which undergo hydroxylation such as warfarin and dicoumarol (bishydroxycoumarin) are administered simultaneously with spironolactone. Gantt, 1962) is highly unspecific. The plasma levels of canrenone after administration of spironolactone appear to be overestimated by a factor of 2 to 5 if they are assayed with fluorimetry instead of HPLC.…”

Section: Plasma Kinetics and Eliminationmentioning

confidence: 99%

Clinical Pharmacokinetics of Diuretics

Beermann¹,

Groschinsky-Grind²

1980

Clinical Pharmacokinetics

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Despite extensive use of diuretics, for only a few have their pharmacokinetics been evaluated.Bendroflumethiazide is completely absorbed and uptake from the gastrointestinal tract is not changed by food. Plasma half-life is about 3h. Apparent volume of distribution averages 1.5£/kg. Up to 'two thirds of the drug is eliminated via non-renal routes. " Hydrochlorothiazide is 65 % absorbed in healthy fasting subjects and 75 % absorbed when given with food. The increased uptake appears to be caused by decreased gastric emptying rate. Absorption is impaired in patients who have undergone intestinal shunt surgery and in some patients with cardiac failure. Plasma half-life averages 10h in subjects with normal renal function. It is prolonged in renal failure as the drug is mainly eliminated via the kidneys in unchanged form. ' " The bioavailability of hydroflumethiazide is at least 50 %. Elimination hal/-life is about 17h in normal subjects and IOh in patients with cardiac failure. The drug is largely eliminated unchanged, in the urine. The half-life of poly thiazide is approximately 26h. About 20 % of an oral dose is cleared via the kidneys. Chlorthalidone is 65 % absorbed. Up to 75 % of a dose is bound to'plasmaproteins and extensively to blood cells. Only 1.4 % of the tota'i amount of the drug in blood is found in plasma.' Plasma half-life averages 40 to 65h. Apparent volume of distribution is close to 300£. This diuretic is mainly eliminated in the urine, although it is metabolised to some extent. Bumetanide is completely absorbed. Up to 96 % is bound to plasma proteins. Apparent volume of distribution ranges from 12 to 35£. Plasma hal/-life is 1.2 to J .5h in healthy subjects and does not appear to be prolonged in renal failure. Renal and non-renal clearance contributes equalfY to its elimination. The uptake of frusemide (furosemide) from the gastrointestinal tract is :about 65 % and is decreased in uraemia and nephrosis. Protein binding is 96 to 98 % and is, diminished in nephrosis. Plasma half-life is approximately 50 minutes in healthy subjects and is prolonged about 3 times in renalfailure. Apparent volumeo/distribution (Vd~rangesfrqm J4 to 11£. Urinary excretion and non-renal elimination contribute almost equally to plasma clearance. The uptake of/ §...mi/ori~is at least 50 % and is diminished when given with food. Plasma half-life averages IOh. Amiloride is essentially eliminated unchanged in'the urine. '

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Gastrointestinal Absorption of Spironolactone

Cited by 25 publications

References 1 publication

Antagonism of fludrocortisone by spironolactone and canrenone [letter].

Antagonism of fludrocortisone by spironolactone and canrenone [letter].

The Aldosterone Blocking Effects of Spirolactones

Clinical Pharmacokinetics of Diuretics

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