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Digitale Medien

The Clinical Pharmacology of Propafenone (1987)

SMITH, NELLIS A. ; KATES, ROBERT E. ; HARRISON, DONALD C.

Oxford, UK : Blackwell Publishing Ltd

Journal of cardiovascular electrophysiology 1 (1987), S. 0

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ISSN: 1540-8167

Quelle: Blackwell Publishing Journal Backfiles 1879-2005

Thema: Medizin

Notizen: Propafenone is a potent type Ic antiarrhythmic agent that has activity against a wide variety of supraventricular and ventricular arrhythmias. Clinical administration must be individualized, based on an appreciation of propafenone pharmacokinctics and dose-response relationships, which are quite complex. Although a “therapeutic” plasma concentration is achieved in most patients with 300 mg orally every eight hours and plasma concentrations reach steady state after three days, marked interpatient differences in plasma concentrations occur. In addition, the effective plasma concentration required for arrhythmia suppression varies markedly in individual patients. Oral propafenone is subjected to a marked “first-pass” hepatic elimination via a saturable oxidative pathway. This can result in a tenfold increase in plasma concentrations as the dose is increased from 150 to 450 mg. Accumulation of metabolites, notably 5-OH propafenone, probably contributes to the net antiarrhythmic effect of oral propafenone during chronic oral administration. Propafenone may exacerbate ventricular arrhythmias in 20–15% of patients. This does not appear to be dose-dependent, nor is it associated with a definite prolongation in QT interval.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1111/j.1540-8167.1987.tb01443.x

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Digitale Medien

Metabolites of Cardiac Antiarrhythmic Drugs: Their Clinical Role (1984)

KATES, ROBERT E.

Oxford, UK : Blackwell Publishing Ltd

Annals of the New York Academy of Sciences 432 (1984), S. 0

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ISSN: 1749-6632

Quelle: Blackwell Publishing Journal Backfiles 1879-2005

Thema: Allgemeine Naturwissenschaft

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1111/j.1749-6632.1984.tb14510.x

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Digitale Medien

High-performance liquid chromatographic isolation and fast atom bombardment mass spectrometric identification of di-N-desethylamiodarone, a new metabolite of amiodarone in the dog (1984)

Latini, Roberto ; Reginato, Roberto ; Burlingame, Alma L. ; [weitere]

Chichester : Wiley-Blackwell

Biological Mass Spectrometry 11 (1984), S. 466-471

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ISSN: 0306-042X

Schlagwort(e): Chemistry ; Analytical Chemistry and Spectroscopy

Quelle: Wiley InterScience Backfile Collection 1832-2000

Thema: Chemie und Pharmazie

Notizen: Amiodarone is an antiarrhythmic drug which has received considerable attention in recent years. It has been suggested that the unusual pharmacodynamic characteristics of this drug may be due in part to the influence of active metabolites. Using fast atom bombardment (FAB) mass spectrometry we have identified a new metabolite of amiodarone, the di-N-desethyl analog (DDEA). This metabolite was present in the blood of dogs treated with the parent drug, and showed a greater affinity for myocardium than did the parent drug. The unique features of FAB mass spectrometry over electron impact mass spectrometry was an essential element in facilitating the identification of this new metabolite. Whether or not this metabolite has pharmacologic activity or is responsible for some of the side effects occurring during amiodarone administration is not known.

Zusätzliches Material: 6 Ill.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1002/bms.1200110906

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