Summary
Hydralazine increases the bioavailability of highly lipid- soluble β- adrenoceptor antagonists, but has no significant effect on the pharmacokinetics of β- blockers such as acebutolol or nadolol. The effect of β- blockers on the pharmacokinetics of hydralazine has not previously been investigated. This study describes the reciprocal pharmacokinetic and pharmacodynamic interactions of hydralazine and slow- release oxprenolol in 6 patients with mild- to- moderate hypertension.
The mean area under the blood concentration/time curve for oxprenolol was significantly higher (p < 0.05) when slow- release oxprenolol was coadministered with hydralazine (2856 ± 401 ng/ml · h) than when it was given alone (2020 ± 209 ng/ml · h), but there was no consistent effect of oxprenolol on ‘apparent hydralazine’ kinetics (AUC0–9 1033 ± 233 ng/ ml · h hydralazine alone; 1017 ± 117 ng/ml · h coadministered with slow- release oxprenolol). The increased oxprenolol blood concentrations on combination therapy did not give rise to significantly lower systolic and diastolic blood pressures compared with monotherapy. The effect of hydralazine on oxprenolol kinetics is probably explained by flow- mediated changes rather than metabolic interaction.
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Hawksworth, G.M., Dart, A.M., Chiang, C.S. et al. Effect of Oxprenolol on the Pharmacokinetics and Pharmacodynamics of Hydralazine. Drugs 25 (Suppl 2), 136–140 (1983). https://doi.org/10.2165/00003495-198300252-00039
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DOI: https://doi.org/10.2165/00003495-198300252-00039