. "005.001" . . "5. 1 Farmakodynamick\u00E9 vlastnosti"@cs . . . . . . . . . . "Farmakoterapeutick\u00E1 skupina: vazodilatans, antihypertenzivum.\nATC k\u00F3d : C08CA02\nFelodipin je vysoce vazoselektivn\u00ED blok\u00E1tor v\u00E1pn\u00EDkov\u00E9ho kan\u00E1lu s\u00A0p\u0159eva\u017Euj\u00EDc\u00EDm vaskul\u00E1rn\u00EDm efektem dihydropyridinov\u00E9ho typu, kter\u00FD sni\u017Euje arteri\u00E1ln\u00ED krevn\u00ED tlak sn\u00ED\u017Een\u00EDm perifern\u00ED c\u00E9vn\u00ED rezistence. V terapeutick\u00FDch d\u00E1vk\u00E1ch selektivn\u011B ovliv\u0148uje hladk\u00E9 svaly arteriol a nem\u00E1 p\u0159\u00EDm\u00FD vliv na srde\u010Dn\u00ED kontraktilitu a veden\u00ED vzruch\u016F v p\u0159evodn\u00EDm syst\u00E9mu srdce. Neovliv\u0148uje ani hladk\u00E9 svaly v\u00E9n a adrenergn\u00ED vazomotorick\u00E9 mechanismy, a proto nen\u00ED pod\u00E1v\u00E1n\u00ED felodipinu spojeno s projevy orthostatick\u00E9 hypotenze. Felodipin m\u00E1 vlastn\u00ED m\u00EDrn\u00FD natriuretick\u00FD a diuretick\u00FD \u00FA\u010Dinek, a proto nedoch\u00E1z\u00ED k retenci tekutin v organismu. \nP\u0159\u00EDpravek Presid m\u016F\u017Ee b\u00FDt pou\u017Eit v monoterapii nebo v kombinaci s jin\u00FDmi antihypertenzivy, nap\u0159. betablok\u00E1tory, diuretiky nebo ACE inhibitory, aby do\u0161lo k zes\u00EDlen\u00ED antihypertenzn\u00EDho \u00FA\u010Dinku. Felodipin sni\u017Euje systolick\u00FD i diastolick\u00FD krevn\u00ED tlak a m\u016F\u017Ee b\u00FDt indikov\u00E1n u izolovan\u00E9 systolick\u00E9 hypertenze. Felodipin si zachov\u00E1v\u00E1 svoji antihypertenzn\u00ED \u00FA\u010Dinnost i v kombinaci s nesteroidn\u00EDmi antiflogistiky (NSAID). \nFelodipin m\u00E1 antiangin\u00F3zn\u00ED a antiischemick\u00E9 \u00FA\u010Dinky d\u00EDky sv\u00E9mu vlivu na zlep\u0161en\u00ED rovnov\u00E1hy mezi spot\u0159ebou a saturac\u00ED myokardu kysl\u00EDkem. Felodipin sni\u017Euje koron\u00E1rn\u00ED vaskul\u00E1rn\u00ED rezistenci. Pr\u016Ftok krve koron\u00E1rn\u00EDmi c\u00E9vami a saturace myokardu kysl\u00EDkem jsou zv\u00FD\u0161eny t\u00E9\u017E v d\u016Fsledku dilatace epikardi\u00E1ln\u00EDch arteri\u00ED a arteriol. Felodipin \u00FA\u010Dinn\u011B br\u00E1n\u00ED vzniku a rozvoji spazmu koron\u00E1rn\u00EDch c\u00E9v. Sn\u00ED\u017Een\u00ED syst\u00E9mov\u00E9ho krevn\u00EDho tlaku zp\u016Fsobuje sn\u00ED\u017Een\u00ED dot\u00ED\u017Een\u00ED (afterload) lev\u00E9 komory a sn\u00ED\u017Een\u00ED n\u00E1rok\u016F myokardu na kysl\u00EDk. \nFelodipin zlep\u0161uje toleranci z\u00E1t\u011B\u017Ee a sni\u017Euje v\u00FDskyt angin\u00F3zn\u00EDch z\u00E1chvat\u016F u pacient\u016F se stabiln\u00ED n\u00E1mahovou anginou pectoris (AP). U pacient\u016F s vazospastickou formou AP sni\u017Euje v\u00FDskyt symptomatick\u00E9 a n\u011Bm\u00E9 formy ischemick\u00E9 choroby srde\u010Dn\u00ED. \nFelodipin je \u00FA\u010Dinn\u00FD a je dob\u0159e tolerov\u00E1n u dosp\u011Bl\u00FDch pacient\u016F bez ohledu na v\u011Bk, rasu a tak\u00E9 u pacient\u016F s p\u0159idru\u017Een\u00FDmi chorobami jako bronchi\u00E1ln\u00ED astma a jin\u00E9 obstruk\u010Dn\u00ED choroby plic, po\u0161kozen\u00E1 funkce ledvin, diabetes mellitus, dna, hyperlipid\u00E9mie, Raynaud\u016Fv fenom\u00E9n a u pacient\u016F po transplantaci ledvin. Felodipin nem\u00E1 vliv na glyk\u00E9mii a profil lipid\u016F.\nM\u00EDsto p\u016Fsoben\u00ED a mechanismus \u00FA\u010Dinku: hlavn\u00ED farmakodynamickou charakteristikou felodipinu je vysok\u00E1 m\u00EDra vaskul\u00E1rn\u00ED selektivity. Myogenn\u011B aktivn\u00ED hladk\u00E9 svaly rezisten\u010Dn\u00EDch arteriol jsou zvl\u00E1\u0161t\u011B citliv\u00E9 na p\u016Fsoben\u00ED felodipinu. Felodipin inhibuje elektrickou a kontraktiln\u00ED aktivitu hladk\u00FDch sval\u016F c\u00E9v p\u016Fsoben\u00EDm na kalciov\u00E9 kan\u00E1ly v bun\u011B\u010Dn\u00E9 membr\u00E1n\u011B. \nHemodynamick\u00E9 \u00FA\u010Dinky: prim\u00E1rn\u00EDm hemodynamick\u00FDm \u00FA\u010Dinkem felodipinu je sn\u00ED\u017Een\u00ED celkov\u00E9 perifern\u00ED c\u00E9vn\u00ED rezistence, co\u017E m\u00E1 za n\u00E1sledek sn\u00ED\u017Een\u00ED krevn\u00EDho tlaku. Tento \u00FA\u010Dinek je z\u00E1visl\u00FD na d\u00E1vce. Obecn\u011B je sn\u00ED\u017Een\u00ED krevn\u00EDho tlaku z\u0159ejm\u00E9 2 hodiny po jednor\u00E1zov\u00E9m pod\u00E1n\u00ED a trv\u00E1 alespo\u0148 24 hodin a pom\u011Br T/P dosahuje hodnot zna\u010Dn\u011B vy\u0161\u0161\u00EDch ne\u017E 50%. Existuje pozitivn\u00ED korelace mezi plazmatickou koncentrac\u00ED l\u00E9\u010Diva, \u00FArovn\u00ED sn\u00ED\u017Een\u00ED perifern\u00ED c\u00E9vn\u00ED rezistence a sn\u00ED\u017Een\u00EDm krevn\u00EDho tlaku. \nElektrofyziologick\u00E9 a jin\u00E9 kardi\u00E1ln\u00ED \u00FA\u010Dinky: Felodipin nem\u00E1 v terapeutick\u00FDch d\u00E1vk\u00E1ch vliv na srde\u010Dn\u00ED kontraktilitu, A-V veden\u00ED a na refraktern\u00ED f\u00E1zi A-V uzlu. \nRen\u00E1ln\u00ED \u00FA\u010Dinky: Felodipin m\u00E1 natriuretick\u00FD a diuretick\u00FD \u00FA\u010Dinek, proto\u017Ee sni\u017Euje tubul\u00E1rn\u00ED reabsorpci sod\u00EDku. U n\u011Bkter\u00FDch jin\u00FDch vazodilat\u00E1tor\u016F doch\u00E1z\u00ED p\u0159i pod\u00E1v\u00E1n\u00ED k retenci sod\u00EDku a vody. Felodipin neovliv\u0148uje denn\u00ED exkreci drasl\u00EDku. Ren\u00E1ln\u00ED vaskul\u00E1rn\u00ED rezistence se p\u0159i pod\u00E1v\u00E1n\u00ED felodipinu sni\u017Euje. Norm\u00E1ln\u00ED glomerul\u00E1rn\u00ED filtra\u010Dn\u00ED rychlost (GFR) se nem\u011Bn\u00ED. U pacient\u016F s po\u0161kozenou funkc\u00ED ledvin se v pr\u016Fb\u011Bhu pod\u00E1v\u00E1n\u00ED felodipinu m\u016F\u017Ee GFR zvy\u0161ovat. \nFelodipin je velice dob\u0159e tolerov\u00E1n u pacient\u016F s\u00A0transplantovan\u00FDmi ledvinami.\n"@cs . . .