Carvedilol: ukuhlaziywa. Imiyalelo yokusetyenziswa, iifanayo, ixabiso

Kuluhlu lwezidakamizwa ezithandwayo zezilwanyana "Carvedilol" sele zifakwe ixesha elide. Izimpendulo zeengcali zichaza njengonyango olulinganiselayo ukungaphumeleli kwentliziyo kunye nokulawulwa kwe-AV-node ngexesha le-fibrillation ye-atrial. Ingasetyenziselwa kakhulu unyango lwexinzelelo lwengqondo, nto leyo eyenza isilwanyana esibalulekileyo. Ngenxa yeso sizathu, iinkampani ezininzi ze-pharmacist zenza i-generic "Carvedilola." Ngamnye wabo unokuzikhethela kwakhe ukukhulula kunye nokudala iziganeko zokwelapha kwigazi. Nangona ngokubanzi bajamelana nomsebenzi wabo.

Ekubeni zonke iziyobisi "i-Carvedilol" zifana neendawo ezixabisekileyo, akukho nto ibaluleke kakhulu ekufuneka ikhethwe kuyo kunyango. Nangona, njengoko uphando lwe-bioequivalence lubonisa, umphumo ogqithiseleyo kunye nobulali uveliswa ngama-generics abizayo kunye nesilwanyana sokuqala. Ngoko ke, injongo yolu hlalutyo kukuchonga amanqaku aphezulu kakhulu aphezulu kunye nexabiso eliphezulu lobuchwephesha.

Uphawu lwesimo semveliso yeyeza

Njengoko izilungiso zokwelapha "iCarvedilol", izifaniso kunye neenjini zaso sele zibonakalise ukuphumelela kwazo. I-medicinal substance ngokwayo iklasi ye-adrenoblockers yamanyathelo axutywayo. Zivimbela iintlobo ezimbini ze-adrenaline kunye ne-norepinephrine receptors: i-beta kunye ne-alpha receptors yohlobo lokuqala. Amandulo ayesentliziyweni, kunye neyokugqibela - kwiimpahla zeemisipha. Ukubavimbela, isichengululo sichaphazela ukuphuhliswa kweziphumo ezininzi zokwelapha.

Akukho zifaniso phakathi kwamachiza e-adrenoblocker kwiklasi kwisiza "Carvedilol". Kukho izinto ezifanayo kuphela kwiindlela zokwenza. Ngokukodwa, isicatshulwa esiseduze nguNebivolol, esinefuthe ekhethekileyo. Kukho neendlela ezilula zokufunda. Baye babeliswa yi-cardioselective, ekhethela i-beta-adrenoreceptors yohlobo lokuqala, iMetoprolol neBisoprolol.

Xa kuthelekiswa ne "Metoprolol", "Carvedilol" iyakhetheka ngakumbi kwi-beta-receptors, ibonisa ukuxhamla kwe-cardiaac beta-adrenoceptors ecishe ifane ne "Bisoprolol". I-Carvedilol nayo i-antioxidant enamandla. Esi siphumo sibaluleke kakhulu ukulungiswa kwodonga lwama-vascular, oluye lwachaphazeleka yienkqubo ze-atherosclerosis. Ngokubaluleka, le propati engumncedisi yeliyobisi ingaphantsi kwento ekhethekileyo ye-Nebivolol. Ubangela ukusetyenziswa kwezinto eziphethwe yi-nitrogen-endothelial factors, kwaye ngoko unako ukukhusela izilonda ze-atherosclerotic zeetriyri.

Farmakodinamika "Carvedilola"

Iyeza zanamhlanje "uCarvedilol" ngenxa yemiphumo yokukhusela i-beta-adrenoreceptors uhlobo lineempembelelo ezilandelayo:

• Iyanciphisa isivumelwano sokuthengiswa kwe-myocardial, ukunciphisa isidingo sesisu senhliziyo kwisondlo kunye ne-oksijini (isenzo sokulwa namanqina);
• Ngaba uyakwazi ukuvimbela i-automatism kunye nokuqhuba (isenzo esichaphazelekayo);
• Ukunciphisa inkqubo ye-renin-angiotensin yomzimba (umthelela okhuselekileyo);
• Iyancipha iqhezu yesiphumo senhliziyo, ukunciphisa izinga lexinzelelo lwegazi;
• Iyakwazi ukwandisa iinqanawa zomzila wesiphelo.

Isiphumo sokugqibela sichaza ngokucacileyo "uCarvedilol". Ukuphononongwa kokusetyenziswa okungapheliyo kweziyobisi kubonisa ukuba kubakho iziphumo ezikhuselekileyo ze-adrenoreceptors-alpha-one subtype. Zifumaneka kwiphonipheral, oko kukuthi, iimpahla ze-muscular. Ukukhusela kwabo kubangela ukwandiswa kwemithambo emincinci. Oku kubangela ukuhla kwe-hydrodynamic yokubambisana komhlaba wonke, okukhokelela ekunciphiseni kwexinzelelo lwegazi kunye nokuphucula ukutya kwesondlo.

Isenzo esifanayo sine "Carvedilol", ama-analog kunye nee-generics zayo, kungekhona nje kwiimisipha zomzimba, kodwa nangentliziyo. Oku kushiya ithuba lokuba ulisebenzise ukusilela kwintliziyo engapheliyo, ecatshulwa yi-ischemia engapheliyo (IHD). Kwaye ekubeni "iCarvedilol" ibhetta-1-blocker ekhethiweyo kunye ne-tropism ye-alpha-1 receptors kunye neepropati ze-antioxidant, isicelo sayo siphezulu ngokubanzi.

Ukusetyenziswa kwe "Carvedilol"

Ekubeni iimpawu ze-pharmacodynamic zeli gciwane zibonisa ukuba "Carvedilol", impendulo malunga nokusetyenziswa kwayo kufuneka iqinisekise ezi ziphumo, okanye zichase izigwebo eziphosakeleyo. Imiphumo emihle yonyango isele ibonakaliswe, ngoko ke akukho nanye inyaniso inokuphikiswa. Ngenxa yesi sizathu, "iCarvedilol" ifanelekile njengesiza esilindelekile kwiimeko ezilandelayo zekliniki:

• Isifo se-Ischemic cardiac;
• Ukungaphumeleli kwintliziyo;
• Tachyarrhythmias;
• I-Angina pectoris, i-infyoction ye-myocardial acute, i-angina engaqinisekanga;
• Uxinzelelo lwengqondo.

Iinkcazo

Isibhengezo esithi "Carvedilol" ubungqina silandela kwimpawu zayo ze-pharmacodynamic. Ngenxa yokunciphisa uxinzelelo lwegazi, ukunciphisa kwangaphambili kunye nokuthunyelwa kwi-myocardium, kwaye nangenxa yempembelelo echaseneyo, isilwanyana singasetyenziswa kwezi zilandelayo:

• Isigulana soxinzelelo lwe-Artertension II kunye ne-III kwonyango olufanelekileyo oluhlangeneyo;
• Uxinzelelo lwe-arterial degree nge-high risk cardiovascular in the form of monotherapy;
• Ngama-tachyarrhymias: uhlobo oluqhubekayo lwe-fibrillation ye-atrial, kunye ne-extrasystole ephindaphindiweyo;
• Ngenxa yesifo senhliziyo esichengeni kunye nembonakalo enzima (stenocardia engaqinisekiyo okanye i-myocardial infarction);
• Ngaphandle kwe-IHD ngaphandle kwembonakalo ebonakalayo (i-angina yoxinzelelo, i-angina eqhubekayo);
• Ukungaphumeleli kwintliziyo engapheliyo, ukususela kwisigaba se-HIIA ngokutsho kweVasilenko-Strazhesko, okanye i-NYHA FC III kwindlela yokudibanisa inonxibelelwano;
• Nge-symptyatic blood pressure ne- sinus tachycardia ehambisana ne-hyperthyroidism okanye ipheochromocytoma.

Iingxoxo ezikhoyo kwiyeza "Carvedilol" zikwahlukana phambi kwezi ziboniso. Zisetyenziselwa kwizifo zentliziyo eziqhelekileyo, oko kukuthi, nge-IHD ne-CHF. Kwakhona, isilwanyana sinokubanzi kwesicelo. Le ngxinxiso ebalulekileyo, nangona iimpawu ezibangelwa yi-hyperthyroidism okanye i-pheochromocytoma, ilawulwa ngempumelelo yi-beta-blockers.

Ukungqinelana

Nangona iphrofayli yokwelapha ebanzi ngaphezu kwe-beta-1-blockers ekhethiweyo, isicatshulwa sinokuchasene nokunciphisa ukusetyenziswa kwayo. "I-Carvedilol" ayinakusetyenziswa kwisenzo sezonyango phambi kwezi meko zilandelayo:

• I-asthma ye-Bronchial, i-COPD ngenxa yengozi yokwanda kwe-bronchospasm;
• Akuvumelekile ukuthatha i-carvedilol ngentlawulo yenhliziyo engaphantsi kwama-50 ngomzuzu ngenxa yengozi ye-bradycardia ebulalayo;
• Akunqunyelwe ukunika i-Carvedilol "kwi-arrhythmias" (CA-blockade, AV blocked 2 na 3 degree degree), ukuba i-pacemaker engapheliyo ayifaki;
• Akwamkelekanga ukumisela izilwanyana ezinobungozi obukhulu;
• Akuvumelekile ukusebenzisa isilwanyana kwi-CHF kunye neklasi ye-IV esebenzayo ngokubhekiselele kwi-NYHA (HIII ngokweVasilenko-Strazhesko) ngenxa yokunyanzeliswa kwekhontrakthi yentliziyo ehlambulukileyo;
• "I-Carvedilol" inqatshelwe ekukhulelweni, i-lactation, kwabantwana abangaphantsi kweminyaka eyi-18 ubudala;
• Akuvumelekanga ukusebenzisa le nkunkuma xa kunokwenzeka ukuba isisombululo esisiphumelelayo kwisithako sayo esisebenzayo okanye inxalenye yefayili yefayili;
• Isiyobisi asisetyenziselwa ukutshitshiswa kwemizimba kunye neSBP ngaphantsi kwama-85 mm Hg. Ubugcisa.

Nangona uhlolo lwe "Carvedilol" lubonisa njengomgangatho kunye nezikhuseli ezikhuselekileyo, kufuneka ulandele ezi ngcebiso. Zenzelwe ukukhusela isiguli kunye neengcali kwiimeko ezingafunekiyo. Ngako oko, oku kungqinelana kwaye akunakukunyanzelwa ngenxa yengozi enkulu yokuphazamiseka okubulalayo kwinto ebalulekileyo yomzimba.

Iziphumo eziPhakathi

Ukuvavanya iziphumo zecala le-"Carvedilol" ukuhlolwa kwakhona akubonakali. Izigulane zizithoba ekuhloleni iiklinikhi nemiphumo emibi. Ngoko ke, kunengqiqo ukuthembela kwiphando lophando. Phakathi kweempembelelo eziphambili, eziqhelekileyo, ezibonakaliswe nge-1 ukuya kwi-10%, zilandelayo:

• Ukususela kwicala le-PNS kunye nenkqubo yesantya ephakathi, kunokwenzeka ukuba uhlakulele ikhanda, utyakekile, ubuthakathaka besifo, izifo zokulala, i-parasthesias njengobonakaliso be-idiosyncrasy;
• Iimpembelelo ze-Cardiovascular (i-bradycardia engapheliyo okanye eqhubekayo okanye i-AV blockade, i-hypotension ye-orthostatic, i-orthostatic hypotension, ngokukhawuleza ukunyuka kwegazi ngenxa yokuphazamiseka kwegazi kwiimisipha ngokuphelisa i-atherosclerosis);
• Izitho zokuphefumula: ukubonakaliswa kwe-dyspnea, ukuxinaniswa kwamanzi, kunye ne-bronchial hyperreactivity okanye izifo eziphazamisayo, i-bronchospasm inokwenzeka;
• Imiphumo emibi evela kwinkqubo yokugaya ibonakaliswa yintlungu yesisu, isicupunu, umlomo owomileyo, isifo sohudo, kwaye ngokungaqhelekanga kukho ukugqithisa okanye ukuhlanza, i-transaminases yesibindi inokunyuka;
• Iprogram ye-hematopoiesis ayifuni ukuphendula kwi-thrombocytopenia okanye i-leukopenia;
• I-eczema, i-pruritus, ukunyanzeliswa kwe-psoriasis, kunye ne-anaphylactoid ezinqabileyo zingasabela.

Kwakhona, ekubeni "iCarvedilol" yinto engaphandle kwimizimba, kunokwenzeka ukuba kuphuhliswe ukusabela okuqhelekileyo. Ibonakalisa nje ngokuba yi-syndrome efana nesifo-mkhuhlane kunye nokuphuhliswa kweentlungu ezisezinyweni, amehlo aomileyo, ukucaphuka kwamanzi. Kule nkalo, "iKarvedilol" ineempembelelo ezininzi ezingaphezu kwe "Metoprolol", nangona ukwenziwa kweeklinikhi kokuqala kudlulileyo kweyesibini.

Izixhobo zokusetyenziswa kwexesha elide elithi "Carvedilol"

Iifom eziphambili zezilwanyana ziyi-capsules kunye namacwecwe. "I-Carvedilol" ithathwa kanye kwimeko yomshushu ophezulu kunye ne-IHD, i-CHF, okanye i-arrhythmia. I-dose yokuqala i-6.25 mg ngosuku, efanelekileyo ukunyanga kwegazi. Xa unyango lwe-CHF, i-IHD okanye i-tachyarrhythmias, kucetyiswa ukuba usebenzise umthamo wokuqala we-6.25 kabini ngosuku. Emva koko, ngokubhaliweyo, i-dose yemihla ngemihla ishintshelwe kwi-25-50 mg.

Isilwanyana sisetyenziswe nanini na kunokwenzeka kwaye xa kukho ukunyamezela. Kufuneka ukulawula i-arrhythmia okanye ukwandisa ubomi kwi-CHF. Olu hlobo lwesilwanyana esithathwe ngokudibanisa ne-diuretics kunye ne-ACE inhibitors landisa ubomi. Kwaye iiphilisi ze-CHF "Carvedilol" zidluliselwa bhetele kune "Bisoprolol." Nangona unyango lufuna ukuyeka ukuqhuba nokuqhuba kwimisebenzi enobungozi, iindlela zokulawula.

IiFom

Ixabiso lonyango "Carvedilol" alilona umqathango wokuzikhethela. Kusebenza ngokugqithiseleyo ukukhetha ifom yefayili ephumelelayo yesigulane esithile. Eyona ndlela ixhaphakileyo kwi-intanethi yasekhaya kunye nakwi-Western intengiso yee-pharmacy ziintlobo ezintathu zonyango lweyeza. Le 25 mg, 12.5 no-6.25 mg. Iipilisi zipakishwe kwiiblisti okanye kwizibhobho zepolymeric. Amayeza athatywa ngaphambi kokutya, ukuba ukuncipha kwenzelwe umsebenzi we dose, ngoko ngexesha lokutya.

Izizukulwana

Izizukulwana zezi ziyobisi ziqulethe "i-Carvedilol" kwifom ethile yokulinganisa ehlangabezana neemfuno ze-bioequivalence xa kuthelekiswa neziyobisi zangaphambili. Kwaye ngoku kwimarike yeekhemisi zasekhaya kukho ubuninzi bama-generics, idibene ezintathu zibe ngokweentengo zabo:

• Ngexabiso eliphezulu (Dilatrend, Coriol, Carvedilol Sandoz);
• Ngexabiso eliphakathi (uCarvelend, Carvedilol Zentiva, Carvedilol Teva);
• Ngamaxabiso aphantsi (Karvedilol-MIK, Karvedilol Belmed, Karvetrend, Karvenal, Vedicardol).

Iindleko ze "Dilatrend" ziyi-ruble engama-450-750, kuxhomekeke kumyinge: 6.25 mg - engabizi ngaphezu kwama-25 mg. Indlela efana nayo iqondwa ngokwemvelo kwimeko yamachiza. Kwi "Coriol" inani lama-ruble ama-250-500, ngokuba "iCarvedilol Sandoz" i-rubles 300-550, ngokuba "iCarvedilol Zentiva" - i-ruble 250-400. "I-Carvedilol Teva" ixabisa i-ruble ka-200-300, "iCarveland" - ii-ruble eziyi-170-330, "uCarvedilol Belmed" - 150-250, "uCarvetrend" - 170-290 ruble.

Ukuba isicatshulwa "Carvedilol" ixabiso alilona uphawu lwekhwalithi, nangona liphakame kakhulu kwiyeza lomphathi oncomekayo. Kwiklinikhi, kukho ukungafani okubalulekileyo phakathi kweziyobisi ezidumiweyo kunye nezasekhaya, ezifanayo kufumaneka. Ngokuqhelekileyo, oogqirha bakhathalele kuphela ukungafani phakathi kwefom yefayili kunye neyokuqala. Ngako oko, kufuneka ukhethe i-generic kwiifomsile, eziza kunciphisa kakhulu intlungu yayo.

Kweminye imilinganiselo, ama-analogs aphantsi angabonakalisa umsebenzi ofanayo wekliniki kwaye asebenza kakuhle kwiinkonzo zentliziyo kunye negazi eliphezulu. Nangona kunjalo, ukuba isiguli sele sithatha i-generic ethile, ngoko kufuneka ishiywe. Ekubeni wayeqhelekile kwiimpawu zefayili kunye neendlela zokunyuka kwinkxalabo ye-plasma yento esebenzayo, ukutshintshwa kwesilwanyana kuya kutshintshisa ibhalansi yakhe. Emva koko kuya kulandelwa ngokucacileyo ukuba le mveliso ayisebenzi okanye ayisebenzi njengoko kuya kuba yinqwenelekayo.

Iiklasi ezifanayo

Amagqabantshintshi eklasi, azalisekise ngokupheleleyo iimfuno zokwelapha, yakha ukhuphiswano lwe "Carvedilol" kwiinkalo ezininzi. Ngokukodwa, ngexinzelelo, kufuneka ukhethe "iBisoprolol" okanye "Nebivolol". Olu hlobo, ngenxa yeendleko zalo eziphezulu, alukwazi ukusetyenziswa zizigulane ezininzi, nangona isilwanyana esiyimpumelelo. Ukuba yonke i-beta-blockers ye-cardioselective ifumaneka, inani labo lokwelapha landa kwinombolo: "Bisoprolol", "Metoprolol", "Carvedilol", "Nebivolol".

"I-Nebivolol" ithathwa njengelona liyeza elona lingcono kakhulu kunyango loxinzelelo lwengqondo, kunye ne "Carvedilol" - unyango lwe-CHF. Akukho nanye kwezinye iziyobisi ezinempembelelo eninzi kwixesha lokukhubazeka kwentliziyo, njengeCarvedilol. Ngenxa yesi sizathu, ngokudibanisa ne-diuretic kunye ne-ACE inhibitor, inako ukwandisa ubomi bomntu.

"I-Carvedilol" i-antiarrhythm ephumelelayo, esebenzisa indlela yokulawula ngokufanelekileyo ukuziphatha kwi-AV node. Oku kubalulekile kwi- fibrillation ye-atrial, xa ubuchule bokubuyisela isigqi kunye nokuyigcina akufumaneki. Kwakhona, nge-fibrillation ye-atrial, "uCarvedilol" unikwe ukulawula isigqi ngexesha lokulungiselelwa kwesigulane kunyango lwe-electropulse.