. . . . . . . . . . "5.1\tFarmakodynamick\u00E9 vlastnosti"@cs . . "Farmakoterapeutick\u00E1 skupina: perindopril a diuretika, \nATC k\u00F3d: C09BA04.\nGleperil Combi je kombinovan\u00FD p\u0159\u00EDpravek obsahuj\u00EDc\u00ED tert-butylaminovou s\u016Fl perindoprilu a indapamid ur\u010Den\u00FD k\u00A0l\u00E9\u010Db\u011B esenci\u00E1ln\u00ED hypertenze u pacient\u016F, u kter\u00FDch krevn\u00ED tlak nen\u00ED adekv\u00E1tn\u011B kontrolov\u00E1n monoterapi\u00ED perindoprilem. Tert-butylaminov\u00E1 s\u016Fl perindoprilu pat\u0159\u00ED mezi inhibitory angiotensin konvertuj\u00EDc\u00EDho enzymu a indapamid mezi diuretikum typu chlorosulfamoylu.\nJeho farmakologick\u00E9 vlastnosti vypl\u00FDvaj\u00ED z vlastnost\u00ED jeho jednotliv\u00FDch slo\u017Eek, k nim\u017E je t\u0159eba p\u0159idat vlastnosti vypl\u00FDvaj\u00EDc\u00ED z aditivn\u00EDho synergick\u00E9ho \u00FA\u010Dinku obou slo\u017Eek p\u0159\u00EDpravku, jsou-li spolu v kombinaci.\nFarmakologick\u00FD mechanismus \u00FA\u010Dinku\nSouvisej\u00EDc\u00ED s\u00A0perindoprilem:\nPerindopril je inhibitor angiotensin-konvertuj\u00EDc\u00EDho enzymu (inhibitor ACE), kter\u00FD konvertuje angiotensin I na vazokonstriktor angiotensin II; konvertuj\u00EDc\u00ED enzym sou\u010Dasn\u011B stimuluje sekreci aldosteronu k\u016Frou nadledvin a stimuluje degradaci bradykininu, vazodilat\u00E1toru, na inaktivn\u00ED heptapeptidy.\nZ\u00A0toho vypl\u00FDv\u00E1:\nsn\u00ED\u017Een\u00ED sekrece aldosteronu,\nzv\u00FD\u0161en\u00ED plazmatick\u00E9 aktivity reninu, p\u0159i\u010Dem\u017E aldosteron ji\u017E neuplat\u0148uje svou negativn\u00ED zp\u011Btnou vazbu,\npokles celkov\u00E9 perifern\u00ED rezistence s preferen\u010Dn\u00EDm \u00FA\u010Dinkem na c\u00E9vn\u00ED \u0159e\u010Di\u0161t\u011B ve svalech a ledvin\u00E1ch, ani\u017E by tento pokles byl doprov\u00E1zen p\u0159i dlouhodob\u00E9 l\u00E9\u010Db\u011B retenc\u00ED soli a vody nebo reflexn\u00ED tachykardi\u00ED.\nAntihypertenzn\u00ED \u00FA\u010Dinek perindoprilu se tak\u00E9 vyskytuje u pacient\u016F s\u00A0n\u00EDzkou nebo norm\u00E1ln\u00ED koncentrac\u00ED reninu.\nPerindopril je \u00FA\u010Dinn\u00FD prost\u0159ednictv\u00EDm sv\u00E9ho aktivn\u00EDho metabolitu, perindopril\u00E1tu. Ostatn\u00ED metabolity jsou inaktivn\u00ED.\nPerindopril sni\u017Euje srde\u010Dn\u00ED pr\u00E1ci:\nvazodilata\u010Dn\u00EDm \u00FA\u010Dinkem na \u017E\u00EDly, kter\u00FD je pravd\u011Bpodobn\u011B zp\u016Fsoben zm\u011Bnami v metabolismu prostaglandin\u016F: sn\u00ED\u017Een\u00ED preloadu,\nsn\u00ED\u017Een\u00EDm celkov\u00E9 perifern\u00ED rezistence: sn\u00ED\u017Een\u00ED afterloadu.\nStudie proveden\u00E9 u pacient\u016F se srde\u010Dn\u00ED insuficienc\u00ED prok\u00E1zaly: \npokles pln\u00EDc\u00EDho tlaku v lev\u00E9 i prav\u00E9 komo\u0159e,\nsn\u00ED\u017Een\u00ED celkov\u00E9 perifern\u00ED vaskul\u00E1rn\u00ED rezistence,\nzv\u00FD\u0161en\u00ED srde\u010Dn\u00EDho v\u00FDdeje a zlep\u0161en\u00ED srde\u010Dn\u00EDho indexu,\nzv\u00FD\u0161en\u00ED region\u00E1ln\u00EDho pr\u016Ftoku krve svaly. \nBylo prok\u00E1z\u00E1no t\u00E9\u017E v\u00FDznamn\u00E9 zlep\u0161en\u00ED z\u00E1t\u011B\u017Eov\u00FDch test\u016F.\nSouvisej\u00EDc\u00ED s\u00A0indapamidem:\nIndapamid je deriv\u00E1t sulfonamid\u016F s indolov\u00FDm kruhem, farmakologicky p\u0159\u00EDbuzn\u00FD thiazidov\u00FDm diuretik\u016Fm. Indapamid inhibuje reabsorpci sod\u00EDku v kortik\u00E1ln\u00EDm dilu\u010Dn\u00EDm segmentu. Zvy\u0161uje vylu\u010Dov\u00E1n\u00ED sod\u00EDku a chlorid\u016F mo\u010D\u00ED a v men\u0161\u00ED m\u00ED\u0159e i vylu\u010Dov\u00E1n\u00ED drasl\u00EDku a ho\u0159\u010D\u00EDku, \u010D\u00EDm\u017E zvy\u0161uje objem mo\u010Di a m\u00E1 antihypertenzn\u00ED \u00FA\u010Dinek.\nCharakteristika antihypertenzn\u00EDho \u00FA\u010Dinku\nSouvisej\u00EDc\u00ED s p\u0159\u00EDpravkem Gleperil Combi:\nU hypertonik\u016F jak\u00E9hokoli v\u011Bku vykazuje Gleperil Combi na d\u00E1vce z\u00E1visl\u00FD antihypertenzn\u00ED \u00FA\u010Dinek na diastolick\u00FD a systolick\u00FD arteri\u00E1ln\u00ED tlak v\u00A0poloze vle\u017Ee i vestoje. Tento antihypertenzn\u00ED \u00FA\u010Dinek p\u0159etrv\u00E1v\u00E1 24 hodin. Sn\u00ED\u017Een\u00ED krevn\u00EDho tlaku je dosa\u017Eeno za necel\u00FD m\u011Bs\u00EDc bez tachyfylaxe; ukon\u010Den\u00ED l\u00E9\u010Dby neprov\u00E1z\u00ED rebound fenom\u00E9n. V\u00A0klinick\u00FDch studi\u00EDch vedlo sou\u010Dasn\u00E9 pod\u00E1v\u00E1n\u00ED perindoprilu a indapamidu ve srovn\u00E1n\u00ED s\u00A0jednotliv\u011B podan\u00FDmi l\u00E1tkami k\u00A0antihypertenzn\u00EDmu \u00FA\u010Dinku synergistick\u00E9 povahy. \nSouvisej\u00EDc\u00ED s perindoprilem:\nPerindopril je \u00FA\u010Dinn\u00FD ve v\u0161ech st\u00E1di\u00EDch arteri\u00E1ln\u00ED hypertenze: m\u00EDrn\u00E9, st\u0159edn\u011B t\u011B\u017Ek\u00E9 i t\u011B\u017Ek\u00E9. Vede ke sn\u00ED\u017Een\u00ED systolick\u00E9ho a diastolick\u00E9ho krevn\u00EDho tlaku v poloze vle\u017Ee i vstoje.\nMaxim\u00E1ln\u00ED antihypertenzn\u00ED \u00FA\u010Dinek nastupuje za 4 a\u017E 6 hodin po po\u017Eit\u00ED jednor\u00E1zov\u00E9 d\u00E1vky a trv\u00E1 nejm\u00E9n\u011B po dobu 24 hodin. \nRezidu\u00E1ln\u00ED blok\u00E1da angiotensin konvertuj\u00EDc\u00EDho enzymu po 24 hodin\u00E1ch je vysok\u00E1: pohybuje se kolem 80 %.\nU pacient\u016F, kte\u0159\u00ED odpov\u00EDdaj\u00ED na l\u00E9\u010Dbu, doch\u00E1z\u00ED k normalizaci krevn\u00EDho tlaku po 1 m\u011Bs\u00EDci l\u00E9\u010Dby bez n\u00E1sledn\u00E9 tachyfylaxe. \nVysazen\u00ED l\u00E9\u010Dby neprov\u00E1z\u00ED rebound fenom\u00E9n.\nPerindopril m\u00E1 vazodilata\u010Dn\u00ED vlastnosti a obnovuje elasticitu hlavn\u00EDho arteri\u00E1ln\u00EDho \u0159e\u010Di\u0161t\u011B, koriguje histomorfologick\u00E9 zm\u011Bny v\u00A0rezistentn\u00EDch art\u00E9ri\u00EDch a vyvol\u00E1v\u00E1 sn\u00ED\u017Een\u00ED hypertrofie lev\u00E9 komory.\nV p\u0159\u00EDpad\u011B pot\u0159eby p\u0159id\u00E1n\u00ED thiazidov\u00E9ho diuretika doch\u00E1z\u00ED k synergistick\u00E9mu aditivn\u00EDmu \u00FA\u010Dinku.\nKombinace inhibitoru angiotensin-konvertuj\u00EDc\u00EDho enzymu a thiazidov\u00E9ho diuretika sni\u017Euje riziko hypokal\u00E9mie vyvolan\u00E9 samotn\u00FDm diuretikem.\nSouvisej\u00EDc\u00ED s indapamidem:\nV monoterapii m\u00E1 indapamid antihypertenzn\u00ED \u00FA\u010Dinek trvaj\u00EDc\u00ED po dobu 24 hodin. Tento \u00FA\u010Dinek se objevuje v\u00A0d\u00E1vk\u00E1ch, kdy jsou diuretick\u00E9 vlastnosti ji\u017E minim\u00E1ln\u00ED.\nAntihypertenzn\u00ED \u00FA\u010Dinek indapamidu m\u00E1 vztah k\u00A0zlep\u0161en\u00ED pru\u017Enosti art\u00E9ri\u00ED a sn\u00ED\u017Een\u00ED celkov\u00E9ho a arteriol\u00E1rn\u00EDho perifern\u00EDho c\u00E9vn\u00EDho odporu.\nIndapamid redukuje hypertrofii lev\u00E9 komory.\nU thiazidov\u00FDch a thiazid\u016Fm podobn\u00FDch diuretik se terapeutick\u00FD \u00FA\u010Dinek nad ur\u010Ditou d\u00E1vkou ji\u017E d\u00E1le nezvy\u0161uje, dos\u00E1hne rovnov\u00E1\u017En\u00E9ho stavu, zat\u00EDmco ne\u017E\u00E1douc\u00ED \u00FA\u010Dinky se d\u00E1le zhor\u0161uj\u00ED. Je-li l\u00E9\u010Dba ne\u00FA\u010Dinn\u00E1, d\u00E1vka by nem\u011Bla b\u00FDt zvy\u0161ov\u00E1na. \nU hypertonik\u016F bylo p\u0159i kr\u00E1tkodob\u00E9m, st\u0159edn\u011B - a dlouhodob\u00E9m pozorov\u00E1n\u00ED zji\u0161t\u011Bno, \u017Ee indapamid:\nneovliv\u0148uje metabolismus lipid\u016F: triglyceridy, LDL- a HDL-cholesterol,\nneovliv\u0148uje metabolismus cukr\u016F, a to dokonce ani u diabetik\u016F s hypertenz\u00ED.\n"@cs . "005.001" . . . . . . . . . . . . . . . . . . . .