Serum binding of nifedipine and verapamil in patients with ischaemic heart disease on monotherapy

Serum free fractions of nifedipine, verapamil and some of their metabolites were measured in patients with ischaemic heart disease receiving single oral dose and chronic monotherapy and were compared with those obtained in vitro. The percentages of unbound nifedipine and verapamil in vitro (concentr...

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Veröffentlicht in:British journal of clinical pharmacology 1989-09, Vol.28 (3), p.357-361
Hauptverfasser: Rumiantsev, DO, Piotrovskii, VK, Metelitsa, VI, Slastnikova, ID, Martsevich Yu, S., Kokurina, EV
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Sprache:eng
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Zusammenfassung:Serum free fractions of nifedipine, verapamil and some of their metabolites were measured in patients with ischaemic heart disease receiving single oral dose and chronic monotherapy and were compared with those obtained in vitro. The percentages of unbound nifedipine and verapamil in vitro (concentration range 50‐200 and 150‐400 ng ml‐1, respectively) were 2.51 and 7.23%, respectively, and did not differ from those found on monotherapy with these drugs (2.05 and 8.08%, respectively), and after single dosing. It is suggested that, during treatment with nifedipine or verapamil, their serum metabolites do not affect binding of the parent drugs to serum proteins.
ISSN:0306-5251
1365-2125
DOI:10.1111/j.1365-2125.1989.tb05438.x