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Influences of the calcium antagonists nicardipine and nifedipine, and the calcium agonist BAY-K-8644, on the pharmacokinetics of propranolol in rats (1993)

Vercruysse, Isabelle ; Schoors, Danny F. ; Massart, Désiré L. ; [et al.]

Springer

Cardiovascular drugs and therapy 7 (1993), S. 721-726

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ISSN: 1573-7241

Keywords: propranolol ; pharmacokinetics ; nicardipine ; nifedipine ; BAY-K-8644 ; rats

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary To determine the effect of dihydropyridines on the metabolism of propranolol, we studied the effects of a single oral dose of nicardipine, nifedipine, and BAY-K-8644 on the pharmacokinetics of propranolol in male Wistar rats fitted with a catheter in the jugularis vein. Oral propranolol (15 mg/kg and 1.5 mg/kg) and intravenous propranolol (1.5 mg/kg) were administered either alone or together with oral nicardipine (2.5 mg/kg). Oral propranolol (15 mg/kg) was administered with oral nifedipine (1.5 mg/kg) and with oral BAY-K-8644 (1.5 mg/kg). Nicardipine increased significantly the AUC and Cmax of oral propranolol (1.5 mg/kg and 15 mg/kg). However, the plasma concentration time curve of intravenous propranolol (1.5 mg/kg) was unaffected. Nifedipine also significantly increased the AUC and Cmax of oral propranolol (15 mg/kg), whereas with BAY-K-8644 there was only a slight increase in the bioavailability of oral propranolol (15 mg/kg). The results indicate that the dihydropyridine calcium antagonists decrease the metabolism of propranolol as a result of a decrease in first-pass clearance. Although an interaction at the level of cytochrome P450 may also be involved, the results of the present study suggest that the inhibitory effect can be largely attributed to changes in liver blood flow.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00877826

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Enantioselective inhibitory effect of nicardipine on the hepatic clearance of propranolol in man (1994)

Vercruysse, Isabelle ; Belpaire, Frans ; Wynant, Pascal ; [et al.]

New York, NY [u.a.] : Wiley-Blackwell

Chirality 6 (1994), S. 5-10

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ISSN: 0899-0042

Keywords: enantiomers ; propranolol ; enantioselective pharmacokinetics ; protein binding ; nicardipine ; drug-drug interaction ; Chemistry ; Organic Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The influence of a single oral dose of 30 mg nicardipine on the pharmacokinetics of (R)- and (S)-propranolol, given orally as rac-propranolol 80 mg, was studied in 12 healthy volunteers. The plasma concentrations were higher for the (S)-enantiomer than for the (R)-enantiomer. The Clo and the Cl′intr of (S)-propranolol were significantly lower than the Clo and Cl′intr of (R)-propranolol. The unbound fraction of (R)-propranolol was significantly higher than that of (S)-propranolol. Coadministration of nicardipine significantly increased the AUC and Cmax and significantly decreased the Clo and Cl′intr for unbound drug of (R)- and (S)-propranolol. These changes were more important for (R)- than for (S)-propranolol. The protein binding was not altered by nicardipine. The enantioselective effect of nicardipine on the metabolic clearance of propranolol appears to be due to an interaction at the level of the metabolizing enzymes. The effect on blood pressure of rac-propranolol was little affected when nicardipine was coadministered with rac-propranolol, and its bradycardic effect was reduced. © 1994 Wiley-Liss, Inc.

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