MIBEFRADIL

BeschreibungPosicor was launched in Argentina, Azerbaijan, Brazil, the Chile, Czech Republic, Denmark, Germany, Ireland, Kazakhstan, the Netherlands, Norway, Peru, the Philippines, Switzerland, Thailand, Turkmenistan, the UK, the US and Venezuela for use in hypertension. It can be assembled in five steps from 4-(1-benzyloxy-Nmethylformamido) butyric acid with o-phenylenediamine and isobutylchloroformate. Posicor binds to calcium channels in a manner that overlaps the Verapamil, SR-33557 and Diltiazem binding site without effecting the dihydropyridine binding site. Thus it blocks a wide variety of calcium channels with selectivity for T-type followed sequentially by L-type. There is also some calcium agonist activity along with sodium and potassium channel activity. It is chemically distinct from the other calcium antagonists (first member of a new catagory of tetralol calcium antagonists). It has the ability to lower heart rate with no negative inotropic effects and is as effective as Amlodipine and more effective than Diltiazem for the treatment of mild to moderate hypertension. Serious drug interactions are possible because Posicor inhibits both CYP2D6 and CYP3A4.

VerwendenMibefradil has been used as a T-type calcium channel blocker in various cells. It has also been used to reduce apoptosis of retinal ganglion cells (RGC) in EphB2-Fc.