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Titolo:
DIFFERENCES IN NIFEDIPINE CONCENTRATION-EFFECT RELATIONSHIP BETWEEN CAPSULE AND SLOW-RELEASE TABLET ADMINISTRATION
Autore:
CASTANEDAHERNANDEZ G; HOYOVADILLO C; HERRERA JE;
Indirizzi:
INST POLITECN NACL,CTR INVEST & ESTUDIOS AVANZADOS,DEPT FARMACOL & TOXICOL,APARTADO POSTAL 22026 MEXICO CITY 14000 DF MEXICO HOSP GEN DR MIGUEL SILVA,DEPT INVEST CLIN & BIOMED MORELIA MICHOACAN MEXICO
Titolo Testata:
International journal of clinical pharmacology and therapeutics
fascicolo: 1, volume: 33, anno: 1995,
pagine: 56 - 60
SICI:
0946-1965(1995)33:1<56:DINCRB>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
ISCHEMIC-HEART-DISEASE; PLASMA-CONCENTRATION; HEALTHY-SUBJECTS; PHARMACOKINETICS; HYPERTENSION; DISORDERS;
Keywords:
NIFEDIPINE, CONCENTRATION-EFFECT RELATIONSHIP; NIFEDIPINE, SLOW RELEASE FORMULATIONS; NIFEDIPINE, PHARMACODYNAMICS; NIFEDIPINE, DRUG INPUT RATE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
15
Recensione:
Indirizzi per estratti:
Citazione:
G. Castanedahernandez et al., "DIFFERENCES IN NIFEDIPINE CONCENTRATION-EFFECT RELATIONSHIP BETWEEN CAPSULE AND SLOW-RELEASE TABLET ADMINISTRATION", International journal of clinical pharmacology and therapeutics, 33(1), 1995, pp. 56-60

Abstract

The relationships between nifedipine plasma concentrations and its hypotensive and positive chronotropic effects were studied in healthy volunteers who received either a 10 mg capsule (CAP) or a 20 mg slow release tablet (SRT). Plasma concentrations rose more rapidly after CAP than after SRT, C-max being 131+/-39 and 40+/-7 ng/ml and t(max) being 0.5+/-0.07 and 1.8+/-0.4 h, respectively. Both formulations produced areduction in diastolic blood pressure which exhibited a significant linear correlation (p < 0.01) with nifedipine plasma concentration. However, the slope obtained with SRT was significantly higher than that of CAP (0.24+/-0.05 vs 0.07+/-0.01,p < 0.01). That is, a similar hypotensive effect was produced at a lower concentration with SRT than with CAP. A positive chronotropic effect which exhibited a highly significant correlation with nifedipine plasma concentration (p < 0.0001) was observed with CAP. Conversely, with SRT heart rate increase was smallerand there was no significant correlation with nifedipine plasma concentration (p > 0.45). Since the measured decrease in blood pressure is the outcome of nifedipine-induced vasodilation and of homeostatic responses, results are interpreted as follows. Fast nifedipine input afterCAP induced a brisk change in physiological conditions and hence triggered an important homeostatic response, visualized as heart rate increase, which partially offset the hypotensive effect. With SRT, there was a gradual change in blood pressure producing lesser activation of compensatory mechanisms and therefore the hypotensive effect of nifedipine was less antagonized than with CAP. Nifedipine SRT does not only exhibit pharmacokinetic advantages, but also a more favorable pharmacodynamic profile than CAP.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/09/20 alle ore 11:02:49