Barnidipine and its Pharmacological and Clinical Properties
Barnidipin a jeho farmakologicke a klinicke vlastnosti
Barnidipin je novy blokator kalciovych kanahz skupiny dihydropyridinu, ktery je povazovan za dalsico zastupce tzv. treti generace teto skupiny. Zatimco pouzivani terminu treti generace je v mnoha jinych pripadech spise zavadejici, protoze nevi jasne deklarovano, co se timto zarazenim mysh, v pripade kalciovych blokatoru tomu tak nevi.Blokatory kalciovych kanahz treti generace jsou charakterizovany vyssi selektivitou ve smyslu vazodilatace, pficemz ucinek na kontraktilitu myokardu a prevodni system je zanedbatelny. Dalsi prednosti je pomaly nastup ucineu, ktery neaktivuje sympaticky system. Biologicka dostupnost je nizka, za coz je pravdepodobne zodpovedna presystemova eliminace, neboli tzv. first pass effect. Plazmaticke koncentrace jsou ale stabilni a ucinek je tak dobre predvidatelny. Pomaly nastup a dlouhe trvani ucineu je u latek treti generace dano tim, ze jsou vysoce liposolubilni, dobre pronikaji do fosfolipidove dvojvrstvy biologickych membran, He se kumuluji a vykazuji vyznacny antioxidacni ucinek, cimz zabranuji poskozeni bunecnych membran. Pri redistribuci se latky treti generace dostavaji do tzv. biofaze, He se vazou se svymi specifickymi receptory.Teto charakteristice take odpovidaji farmakokineticke parametry barnidipinu, ktery s vyjimkou biologicke dostupnosti jsou u dalsich dvou dihyropyridinu srovnatelne s barnidipinem a zaroven se vsechny tyto latky podstatne lisi v eliminacnim polocasu od dihydropyridinu prvni generace, nifedipinu. Pokud se jedna o neMdouci uciney, je jejich vyskyt u barnidipinu stejny nebo dokonce i nizsi nez u amlodipinu a lacidipinu.Vzhledem ke sve presne definovatelnosti, ktery je dana obsahem pouheho jedineho enanciomeru, predstavuje barnidipin novou, ucinnou a bezpecnejsi alternativu v 1666
Klíčová slova:
Authors:
Z. Fendrich
Authors place of work:
Katedra farmakologie a toxikologie, Farmaceuticka fakulta Univerzity Karlovy, Hradec Kralove, vedouci katedry prof. MUDr. Z. Fendrich, CSc.
Published in the journal:
Prakt. Lék. 2003; (4): 189-193
Category:
Summary
Barnidipine is a new calcium channel blocker of the dihydropyridine group. It is considered a representative of the so-called third generation of this group. Calcium channel blockers of the third generation are characterized by a greater selectivity in the sense of vasodilatation whereby the effect of the contractility of the heart muscle and conduction system is negligible. Other advantages are a slow onset of action which does not activate the symapthetic system. The biological availability is low. The plasma levels are, however, stable and the effect is thus predictable.
Key words:
calcium channel blocker - dihydropyridine - barnidipine - treatment
Štítky
General practitioner for children and adolescents General practitioner for adultsČlánok vyšiel v časopise
General Practitioner
2003 Číslo 4
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