Metabolism and Kinetics of the Hypoglycemic Agent Glipizide in Man—Comparison with Glibenclamide

Fuccella, L. M.; Tamassia, V.; Valzelli, G

doi:10.1002/j.1552-4604.1973.tb00255.x

Cited by 40 publications

(24 citation statements)

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“…They show, how- Crooks and Brown (1974) Rupp et al (1969) 1-(2) Crooks and Brown (1975) Schmidt et al (1973) Fucella et al (1973 ever, negligible first-pass hepatic metabolism. Because of the usually complex pathways of the metabolism (fIg.…”

Section: Metabolismmentioning

confidence: 92%

“…Glipizide (fig. Id) is almost completely metabolised, only about 3 to 10% of the administered dose being excreted in the urine as unchanged drug over a 24-hour period (Ambrogi et ai., 1972;Balant et ai., 1973;Fucella et al, 1973;Schmidt et al, 1973). The main metabolites have a similar structure to the derivatives of glibenclamide and they seem to be essentially devoid of hypoglycaemic activity (Tamassia, 1975).…”

Section: Metabolismmentioning

confidence: 98%

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Clinical Pharmacokinetics of Sulphonylurea Hypoglycaemic Drugs

Balant

1981

Clinical Pharmacokinetics

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Section: Metabolismmentioning

confidence: 92%

Section: Metabolismmentioning

confidence: 98%

Clinical Pharmacokinetics of Sulphonylurea Hypoglycaemic Drugs

Balant

1981

Clinical Pharmacokinetics

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“…Glyburide it tightly bound to plasma proteins [30], but whether this agent gains access to the tubule lumen by processes other than limited filtration has not been investigated. The fact that glyburide led to a significant decrease in fluid absorption along the loop of Henle is of interest.…”

Section: Discussionmentioning

confidence: 99%

Effects of Glyburide on Renal Tubule Transport and Potassium-Channel Activity

Wang¹,

Wang²,

Klein-Robbenhaar³

et al. 1995

Kidney Blood Press Res

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Renal clearance, microperfusion and patch-clamp techniques were used to investigate the effects of the K-channel blocker glyburide on electrolyte excretion, the transport properties of the thick ascending limb (TAL) of Henle and K-channel activity in the apical membrane of the TAL and of the cortical collecting tubule. Our data suggest that the K-channel blocker glyburide can inhibit transport of Na and K in the TAL by blocking K recycling across the apical membrane. Additionally, inhibition of K secretion in the collecting ducts occurs by decreasing the activity of apical K channels and prevents kaliuresis.

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“…Hepatic biotransformation is nearly the exclusive pathway of elimination except for about 10%, which is excreted unchanged with urine (FUCCELLA et al 1973;SCHMIDT et al 1973;BALANT et al 1975;PENTIKÄINEN et al 1983). The proportion of a dose found in urine is 65% -87%, 9% _12°;', as 3-cishydroxy-cyclohexyl derivative, 46% -62% in the form of the 4-trans-hydroxycyclohexyl derivative, 1%-2% as the N-acetyl derivative and about 8'Yo as unextractable and unidentified compounds.…”

Section: C) Metabolismmentioning

confidence: 95%

“…UP to 87% of a dose may be excreted with urine, the remainder with feces (FUCCELLA et al 1973), with mean elimination half-lives ranging between 2 and 9 h (SARTOR et al 1980b;WAHLIN-BoLL et al 1982a;HUUPPONEN et al 1982b;PETERSON et al 1982;PENTIKÄINEN et al 1983;KRADJAN et al 1989;lABER et al 1992lABER et al , 1993b. Values for systemic clearance between 33 and 52 ml/min are attained.…”

Section: D) Eliminationmentioning

confidence: 97%