Stereoselective binding of propranolol enantiomers to human alpha 1‐ acid glycoprotein and human plasma.

Albani, Fiorenzo; Riva, R.; Contin, Manuela; Baruzzi, Agostino

doi:10.1111/j.1365-2125.1984.tb02462.x

Cited by 65 publications

(25 citation statements)

References 12 publications

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“…Although the differences were small, the data nonetheless are consistent with previous reports that have demonstrated the stereoselective binding of (-)-propranolol in young, healthy volunteers (Olanoff et al, 1984;Walle et al, 1983;Albani et al, 1984). We were not, however, able to demonstrate any influence of age itself upon the binding of either of the propranolol enantiomers.…”

Section: Discussionsupporting

confidence: 80%

“…Studies dealing with the stereoselective binding of propranolol in man are, at present, limited and mainly involve young subjects (Olanoff et al, 1984;Walle et al, 1983;Albani et al, 1984). Many elderly individuals receive propranolol and there is evidence to suggest altered pharmacokinetics and/or pharmacological effect in this population (Vestal et al, 1979a;Paxton & Briant, 1984;Schumucker, 1985).…”

Section: Introductionmentioning

confidence: 99%

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Stereoselective binding of propranolol in the elderly.

Colangelo

Chandler

Blouin

1989

Brit J Clinical Pharma

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The influence of age on the stereoselective serum protein binding of propranolol was investigated. Serum was obtained from 10 young (mean age 23 ± 2 years) and ten elderly (mean age 68 ± 2 years) healthy male volunteers. The free fraction of propranolol (fu) was measured by equilibrium dialysis, using tritium labeled (±)-and (-)-propranolol. Thefu values were 0.159 ± 0.049 and 0.148 ± 0.028 (±), 0.135 ± 0.041 and 0.136 ± 0.04 (-), 0.174 ± 0.056 and 0.161 ± 0.028 (+) in the young and elderly subjects, respectively. Serum (xl-acid glycoprotein (AAG) concentrations were 81.4 ± 33.0 and 81.0 ± 21.6 mg 100 mI-' in young and elderly respectively (P > 0.05). Variability in AAG concentration accounted for most of the observed intersubject variability in the binding of both propranolol isomers. The stereoselective binding of propranolol does not appear to be affected by age.

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Section: Discussionsupporting

confidence: 80%

Section: Introductionmentioning

confidence: 99%

Stereoselective binding of propranolol in the elderly.

Colangelo

Chandler

Blouin

1989

Brit J Clinical Pharma

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“…Recently, progress in the development of analytical methods for the efficient resolution of enantiomers has facilitated studies of the differences in the pharmacological properties of the enantiomers of many chiral agents, and it has been shown that such differences can originate from stereoselectivity in their absorption (22), distribution (1,26), receptor binding (23), metabolism (17,18) and/or excretion (10). Among the quinolone antibacterial agents there are many drugs, such as lomefloxacin, sparfloxacin, and OFLX, which possess an asymmetric carbon in their chemical structures.…”

Section: Discussionmentioning

confidence: 99%

Enantioselective disposition of ofloxacin in humans

Okazaki

Kojima

Hakusui

et al. 1991

Antimicrob Agents Chemother

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The enantioselective disposition of ofloxacin (OFLX) was studied in healthy subjects after oral administration of (+/-)-OFLX at a dose of 200 mg. S-(-)-OFLX and R-(+)-OFLX concentrations in serum and urine were measured separately by high-performance liquid chromatography, and various pharmacokinetic parameters were calculated from the data. The ratio of S-(-) to R-(+) enantiomer concentrations in serum showed a increase with time, with S/R ratios of 1.01 at 2 h and 1.31 at 24 h. The terminal elimination half-life of S-(-)-OFLX was 6.9 h, which was significantly greater (P less than 0.05) than that of the R-(+) enantiomer (6.3 h). S-(-)-OFLX also revealed a significantly greater area under the concentration-time curve in serum, mean residence time, and total body clearance than the R-(+) enantiomer did. The renal clearance of S-(-)-OFLX (7.14 liters/h/1.73 m2) was significantly lower than that of the R-(+) enantiomer (7.53 liters/h/1.73 m2). Although the difference in the pharmacokinetic parameters of the enantiomers was small, their disposition in humans was found to be stereoselective. The difference between the enantiomers may be explained by the difference in their renal excretion.

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“…The two different genes which code for AAG in humans, code for two proteins differing by 22 amino acid substitutions [5]. Genetic characterization of the AAG variants [6,13] [22,23].…”

Section: Discussionmentioning

confidence: 99%

Evidence for differences in the binding of drugs to the two main genetic variants of human alpha 1‐acid glycoprotein.

Hervé

Gomas

Duché

et al. 1993

Brit J Clinical Pharma

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1 Human cxl-acid glycoprotein (AAG), a plasma transport protein, has three main genetic variants, Fl, S and A. Native commercial AAG (a mixture of almost equal proportions of these three variants) has been separated by chromatography into variants which correspond to the proteins of the two genes which code for AAG in humans: the A variant and a mixture of the Fl and S variants (60% Fl and 40% S). Their binding properties towards imipramine, warfarin and mifepristone were studied by equilibrium dialysis.

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Stereoselective binding of propranolol enantiomers to human alpha 1‐ acid glycoprotein and human plasma.

Cited by 65 publications

References 12 publications

Stereoselective binding of propranolol in the elderly.

Stereoselective binding of propranolol in the elderly.

Enantioselective disposition of ofloxacin in humans

Evidence for differences in the binding of drugs to the two main genetic variants of human alpha 1‐acid glycoprotein.

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