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• W2039487761 abstract "Les dihydropyridines ont acquis une position essentielle dans le traitement de l’hypertension artérielle. Les produits de première génération (nifédipine, nicardipine…) avaient tous une pharmacocinétique labile, responsable d’effets secondaires délétères liés à l’activation réflexe des systèmes sympathique et rénine-angiotensine. Des améliorations pharmacocinétiques ont été obtenues par des formulations à libération prolongée pour obtenir des produits mieux adaptés pour contrôler les effets thérapeutiques et réduire les effets secondaires. Il a fallu attendre plus longtemps pour innover sur le plan pharmacodynamique avec la mise au point des dihydropyridines à longue demi-vie plasmatique comme l’amlodipine qui, à coté de leur cinétique stable, sont moins cardiosélectives et donc mieux tolérées chez les insuffisants cardiaques. Avec les dihydropyridines lipophiles aujourd’hui disponibles (lercanidipine et lacidipine), une nouvelle génération est née, apportant un meilleur confort thérapeutique en termes de durée d’action et d’extension des indications, notamment dans l’ischémie myocardique et, on peut l’espérer, dans l’insuffisance cardiaque. Dihydropyridines are among the most widely used drugs for the management of cardiovascular disease. Introduced in the 1960s, dihydropyridines have undergone several changes to optimise their efficacy and safety. Four generations of dihydropyridines are now available. The first-generation (nicardipine) agents have proven efficacy against hypertension. However, because of their short duration and rapid onset of vasodilator action, these drugs were more likely to be associated with adverse effects. The pharmaceutical industry responded to this problem by designing slow-release preparations of the short-acting drugs. These new preparations (second generation) allowed better control of the therapeutic effect and a reduction in some adverse effects. Pharmacodynamic innovation with regard to the dihydropyridines began with the third-generation agents (amlodipine, nitrendipine). These drugs exhibit more stable pharmacokinetics, are less cardioselective and, consequently, well tolerated in patients with heart failure. Highly lipophilic dihydropyridines are now available (lercanidipine, lacidipine). These fourth-generation agents provide a real degree of therapeutic comfort in terms of stable activity, a reduction in adverse effects and a broad therapeutic spectrum, especially in myocardial ischaemia and potentially in congestive heart failure." @default.
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• W2039487761 date "2003-07-01" @default.
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• W2039487761 title "De la première à la quatrième génération de dihydropyridines : vers une meilleure efficacité et une meilleure tolérance" @default.
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• W2039487761 doi "https://doi.org/10.2515/therapie:2003051" @default.
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