Comparison of the pharmacokinetics of glipizide and glibenclamide in man

Balant, L; Fabré, J; Zahnd, G

doi:10.1007/bf00616416

Cited by 61 publications

(26 citation statements)

References 10 publications

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“…Some studies have measured total radioactivity after giving radiolabelled drug (Balant et al, 1975;Rupp et al, 1972); others have determined immunoreactive glibenclamide (Balant et al, 1977) or employed high performance liquid chromatography (Rogers et al, 1982;WahlinBoll & Melander, 1979) or gas liquid chromatography (Castoldi & Tofanetti, 1979). Use of radioimmunoassay over-estimates glibenclamidederived plasma activity because of crossreactions with hydroxylated metabolites (Pearson, 1985).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic studies of glibenclamide in non‐ insulin dependent diabetes mellitus.

Coppack

Lant

McIntosh

et al. 1990

Brit J Clinical Pharma

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1 The pharmacokinetic and pharmacodynamic properties of oral glibenclamide have been studied in 31 hospitalised in-patients and 79 ambulant out-patients with diabetes mellitus. 2 Breakfast was found to have no significant influence on the kinetic behaviour of glibenclamide or on the effect of this drug on blood glucose utilisation. 3 The time course of glibenclamide kinetics after 20 mg dosing was adequately described by a two-compartment open model, yielding mean half-lives of 3.3 ± 1.5 h (t½/,X) and 9.7 ± 1.2 (t½,z) for the initial and terminal elimination phases respectively. 4 No significant accumulation or change in kinetic profile occurred in patients who had normal renal and hepatic function, were treated continuously with glibenclamide, and then rechallenged after 8-12 weeks.5 Despite inter-individual variations in drug absorption, peak plasma concentrations (Cmax) and the area under the plasma concentration-time curve (AUC(0-24)) were dosedependent over the dose range 5-20 mg. No significant dose-response behaviour was observed in respect of glucose utilisation, suggesting that there is little clinical benefit in using doses of glibenclamide above 5 mg day-'. 6 Comparison of plasma glibenclamide concentrations at different time-bands following doses of 5 and 10 mg showed a wider range in ambulant out-patients than in age-, sexmatched in-patients treated with the same dosages of drug. Mean plasma drug concentrations attained at all time bands up to 8 h after dosing were higher in out-patients than in in-patients, suggesting a tendency to 'over-compliance' by patients in anticipation of attendance at clinic.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic studies of glibenclamide in non‐ insulin dependent diabetes mellitus.

Coppack

Lant

McIntosh

et al. 1990

Brit J Clinical Pharma

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“…These data suggest that glimepiride has different pharmacokinetics and pharmacodynamics to glibenclamide 13 . On the other hand, there are studies 14 comparing the pharmacokinetics activity of glipizide (glibenclamide derivative) with glibenclamide. The results suggest that both drugs are metabolized by liver and kidneys which play roles important in their biotransformation and elimination from plasma.…”

Section: Introductionmentioning

confidence: 99%

Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats

Figueroa‐Valverde¹,

Díaz-Cedillo²,

Lopez-Ramos³

et al. 2012

BIOMED PAP

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Aim. The present study was designed to investigate the activity of two glibenclamide derivatives on glucose concentration. An additional aim was to identify the biodistribution of glibenclamide derivatives in different organs in a diabetic animal model. Methods. The effects of two glibenclamide derivatives on glucose concentration were evaluated in a diabetic animal model. In addition, glibenclamide derivatives were bound to Tc-99m using radioimmunoassay methods. To evaluate the pharmacokinetics of the glibenclamide derivatives over time (15, 30, 45 and 60 min) the Tc-99m-glibenclamide conjugates were used. Results. The results showed that glibenclamide-pregnenolone had greater hypoglycemic activity than glibenclamide or glibenclamide-OH. The data also showed that the biodistribution of Tc-99m-glibenclamide-OH in all organs was less than that of the Tc-99m-glibenclamide-pregnenolone derivative. Conclusions. The glibenclamide-pregnenolone derivative had greater hypoglycemic effects and its biodistribution was wider than glibenclamide-OH. The data suggest that the steroid nucleus may be important to the hypoglycemic activity of the glibenclamide-pregnenolone derivative and this could be related to the degree of lipophilicity induced by the steroid nucleus in the chemical structure of glibenclamide-pregnenolone.

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“…Some glibenclamide pharmacokinetic data have fitted one- (Uihlein & Sistovaris 1982) or two- (Rogers et al 1982) compartment models, but others have found evidence for the existence of a third 'deep' compartment (Balant et al 1975(Balant et al , 1977Rupp et al 1972). If, as most studies indicate, glibenclamide has a short elimination half-life, blood concentrations should be undetectable 24 hours after a dose in the therapeutic range.…”

Section: Distributionmentioning

confidence: 95%

“…Early studies using nonspecific assays tended to overestimate the half-life of glibenclamide with values ranging from 9 to 16 hours (Balant et al 1975;Rupp et al 1972). Later estimates of the elimination half-life vary between 1.4 and 2.3 hours in healthy subjects in studies using specific assays (lngs et al 1981(lngs et al : Matsuda et al 1983Pearson et al 1986).…”

Section: Eliminationmentioning

confidence: 97%

The Relationship Between the Pharmacokinetics and Pharmacodynamic Effects of Oral Hypoglycaemic Drugs

Ferner

Chaplin

1987

Clinical Pharmacokinetics

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Oral hypoglycaemic drugs have widely differing pharmacokinetic properties. Possible pharmacodynamic benefits include greater efficacy and fewer adverse effects. In general, it has not been possible to demonstrate unequivocal differences in clinical efficacy between the sulphonylureas during long term use, although there are clear differences in potency. These differences have been emphasised to the extent that the term 'second-generation' has been used for the most potent sulphonylureas, but there is little to suggest that potency is of any therapeutic significance. Trials to study differences in efficacy have rarely been of acceptable design. They have often used fixed doses of drugs, begging the question of whether true potency ratios have been established for chronic treatment. They have rarely involved substantial numbers of patients in double-blind crossover studies with a suitable washout period. Trials which show that there is a clear relationship between drug concentrations in blood and drug effects (whether therapeutic effects or adverse effects such as severe hypoglycaemia) are generally lacking. Qualitative and semiquantitative analysis of adverse effects supports the concept that drugs with a long half-life (e.g. chlorpropamide), renally excreted active metabolites (e.g. acetohexamide) or unusual properties (e.g. glibenclamide, which accumulates progressively in islet tissue) are more likely to cause prolonged hypoglycaemia, which may be fatal. The major adverse effect of treatment with biguanides is lactic acidosis, and this probably occurs more commonly in patients treated with phenformin than those treated with metformin because of pharmacogenetic variation in phenformin metabolism. The available evidence therefore favours the use of drugs with a short elimination half-life which are extensively metabolised and which have no active metabolites.

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Comparison of the pharmacokinetics of glipizide and glibenclamide in man

Cited by 61 publications

References 10 publications

Pharmacokinetic and pharmacodynamic studies of glibenclamide in non‐ insulin dependent diabetes mellitus.

Pharmacokinetic and pharmacodynamic studies of glibenclamide in non‐ insulin dependent diabetes mellitus.

Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats

The Relationship Between the Pharmacokinetics and Pharmacodynamic Effects of Oral Hypoglycaemic Drugs

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