"I-Acecardol": izinkomba zokusetshenziswa, imiyalelo, ukubuyekezwa, ukufana

Phakathi kwezinto zokwelashwa okulwa ne-antiplatelet, ezisetshenziselwa ukuvimbela izifo ezinomsoco we-cardiovascular, i-acetylsalicylic acid (i-ASA) ibe yindawo esemqoka isikhathi eside. Ehlanganisiwe ngo-1887, sekuyiminyaka engaphezu kwengu-125 esetshenziselwa ukusebenzisana kwezokwelapha njenge-antiaggregant kanye ne-antipyretic. Futhi njengesisetshenziswa somuthi osebenzayo, yingxenye yesidakamizwa esithi "Acecardol", izinkomba zokusetshenziswa okuqhubekayo kancane kancane njengoba kusetshenziselwa izifo eziyinkimbinkimbi yezifo zamathambo.

Isici sesistimu yomkhiqizo wokwelapha

Into esebenzayo yalesi sidakamizwa ngokwezigaba zibhekisela ezindleleni ezivimbela u-aggregation. Kulolu chungechunge, i-ASA iyinkampani ephumelela kakhulu yamakhemikhali, ekwazi ukuqinisekisa ngokuphelele ukuthi akunakwenzeka ukuhlanganiswa kwe-pool yonke yamaplatelet. Ukuhlola izidakamizwa "i-Acecaradol", izinkomba zokusetshenziswa, ama-analog kanye nesimo sawo sokulinganisa kusukela ekubukeni kwe-pharmacodynamics, okulandelayo kuvezwe:

• Into esebenzayo - i-ASA, ukuxazulula umphumela we-antithrombotic ngokumelene nemisipha ye-atherosclerosis;

• Isidakamizwa senziwe kahle kakhulu ekuvimbeleni izifo zenhliziyo;

• Ifomu layo lokulinganisa linciphisa umphumela we-gastro-toxic we-ASA;

• Isidakamizwa sithengeka kakhulu kunontanga enokuncintisana enekhono elifanayo.

Umthelela wokuvimbela i-ASA ngenxa ye-thrombosis ngenxa yokuvimbela ukubunjwa kwe-prostanoids. Ngenxa yokuvinjelwa kwe-COX-1 - i-cyclooxygenase-1 platelets - into eqalayo yokwakhiwa kwe-thrombus - ukuhlukumeza kwamaplatelet wegazi kuphukile. Kukhona ukucindezeleka kokubunjwa kwe-thromboxane A2, okuqala inqubo yokunamathisela iplatelet kwisayithi ewonakele yodonga lwamasongo.

Ukulungiswa nokuhlukaniswa kwe-gastotoxicity

Izinkomba ezibhekiswe ekusetshenzisweni kwe "Acecardol" zihlanganisa ukuvimbela i-thrombosis. Kodwa-ke, ku-ASA, ingxenye esebenzayo yesidakamizwa, kunomphumela ongafaki ohlotshaniswa ne-nonselectivity kuya kwe-cyclooxygenase. Futhi, ukubuyiselwa kwamaseli e-epithelial wepheshana lamathumbu kuphazamiseka. Ukuba ngaphansi kwethonya elinamandla le-acidic esiswini semvelo, zilimazekile kakhulu, okubangela ukuthuthukiswa kwesifo esiswini esingavamile. Ngezinye izikhathi (cishe ngo-3.5% kuwo wonke amacala) lokhu kuphazamisa ukuphuma kwegazi endleleni yokugaya.

Ifomu le-dosage lapho "i-Acecardardol" isetshenziselwa khona, izinkomba zokusetshenziswa zibanzi ngenxa yokuphepha okukhulu. Ihlakazeka futhi igxile kuphela kwi-duodenum, emele uhlobo lwe-ASA lwe-enteric soluble. Ukuxhumana kwakhe namaseli wesisu cishe kukhishwe, ngaleyo ndlela kuvimbela umphumela walo ohlangothini lwe-gastrotoxicity. Umonakalo wendawo wendawo we-"Acecardol" unciphise, ngoba lesi sidakamizwa sesivele sibhekwa njengefomu elungenwe ngaphakathi ngaphakathi njengesimo sokuvimbela i-COX-1. Nakuba ukuvimbela kwe-COX-2 kubonakala futhi emathunjini, engabonakali ukuphazamiseka okukhulu.

Umphumela obalulekile wefomu le-dosage "i-Acecardol" ukuhla kwesimo esisheshayo ekuguleni kwesisu. Ngenxa yokutholakala kwezinto eziphikisana nesikhuhlane ngendlela ye- magnesium hydroxide, amathuba okulimala esiswini ayancipha ngisho nakakhulu. Futhi okwamanje emakethe yemithi ye-Russian Federation, "i-Acecardol" ingenye yemikhiqizo emithathu enezici. Ukuhlala okungabizi kakhulu phakathi kokufanayo, kuyafaneleka ngokufanele ukusetshenziswa okuphakade.

Indawo "i-Acecardola" ekwelapheni kwe-antithrombotic

I-ASA yokuvimbela izenzakalo ze-thrombotic isetshenziselwa ngezifundo ezihlukahlukene zokwelashwa. Ziqinisekisa ukusebenza kwayo ekunciphiseni ukufa kweziguli ezivela ezifweni zamasondo. Ikakhulukazi:

• I-ASA inciphisa ukushona ngo-16% phakathi kweziguli ezingxenyeni eziphezulu ezingozini zomzimba nge-16%

• Ama-25% anciphisa isifo se-ischemic;

• Ngama-25% kunciphisa ingozi ye-thromboembolism yamanzi we-pulmonary namagatsha awo;

• Ngama-29% kunciphisa amathuba okuthuthukisa i-thrombosis ebonakalayo ye-pelvis noma iziphetho;

• Ngama-33% kunciphisa umphumela we-infarction ye-myocardial.

Le miphumela ngokugcwele futhi inikeza izidakamizwa "i-Acecaradol", izinkomba zokusebenzisa okuncane kakhulu kunalokho kokuqeda esiswini se-ASA. Futhi namuhla amandla omphumela we-antithrombotic we-antiplatelet agents omusha kulinganiselwa kuphela ngokuqhathaniswa nawo. Ngakho-ke, "i-Acecaradol", njengendlela ephephile, kufanele ithathe indawo ephakathi kwiphilisi ye-prophylactic yeziguli ngokusho kwezinkomba.

Isiqu seziguli ezinezinkomba zokusetshenziswa

Isidakamizwa esithi "Acecaradol" izinkomba zokusetshenziswa, intengo, ukusebenza kanye nezingozi zokusetshenziswa zilinganiselwe kahle. Lokhu kwenza kube lula ukuthatha i-ASA kule fomu yokulinganisa ngezinhlobo ezahlukene zeziguli ezinezici zobungozi ezivamile. Futhi ukuqedwa kwemiphumela emibi kakhulu kubangela ukuthi umuthi kula macala alandelayo:

• (ACS) ama -syndromes aconary acute ngokuphakama, ukucindezeleka, noma isikhathi esinqunyiwe se-ST ku-cardiogram;

• Ngokuhlukunyezwa okukhulu kokusakaza kwe-cerebral (cerebral) (ONMC);

• Ukuhlaselwa kwe-ischemic (i-TIA) yesikhashana (i-cerebral);

• Uma lezi zifo zidluliselwa ukuze kuvinjelwe amacala avamile;

• Nge-angina pectoris eqinile ngokuvimbela i-ACS;

• Nge-paroxysm noma izinhlobo ezingapheliyo zokufubha kwe-atrial;

• Ngesifo sofuba se-varicose.

Ukulungiswa kwe-pathogenetic yokusetshenziswa kwe- "Acecardol"

Lezi zibonakaliso zokusetshenziswa kwe-"Acecardol" zibangelwa umthelela omtholampilo wesidakamizwa. Isetshenziswe ngempumelelo njengendlela yokuvimbela ukucindezeleka kwemithambo yegazi lapho kutholakala khona ama-platex atherosclerotic engxenyeni engaphansi. Kulezi zingosi, ngenxa yokunciphisa imishanguzo, ukugeleza kwegazi kuphazamiseka, ngokubunjwa kwegazi eligelezayo. Ukucindezela komshini ezindaweni ezithinta i-endothelium thinned kuholela ekusweleni kwayo. Uhlelo lwegazi lwe-coagulation luyabona leli sayithi njengokwephula ubuqotho be-vascular, okudinga ukuvalwa kwayo ngamaplatelet ngokubunjwa kwe-thrombus.

Okunamathiselwe kwamaplatelets kuyisigaba sokubunjwa kokuqala kwe-thrombus, ngemva kwalokho amasondo we-thrombus ezayo azokwakhiwa. Khona-ke, ubukhulu bayo buyanda ngokulibaziseka amangqamuzana egazi. Ukuqedela ukuqeda i-hemostasis kuholela eqinile (endaweni engaphezu kuka-75% yendawo) ekunciphiseni kwe-lumen yomkhumbi. Ngokuvamile lokhu kuvimbela ukugeleza kwegazi emthonjeni, futhi izindawo ezazitholwa ngaphambilini zikwazi ukuthola ischemia. Le nqubo ihambisana ne-ACS ne-ONMI, ngakho-ke ukuvimbela lezi zenzakalo kubaluleke kakhulu ukuze kunciphise ukufa kwabantu abane-atherosclerosis ye-cardiac and brachiocephalic arteries.

I-Farmakodinamika antitromboticheskogo isenzo "I-Acecardola"

Okufakwe ekulungiseleleni "imiyalo ye-Acecaradol" yokusetshenziswa (incazelo yesidakamizwa) ayibonakali umphumela wayo we-pharmacodynamic, kodwa uyayifaka ngokusho kwezimpawu kanye nezimpawu zokwamukelwa. Kodwa-ke, akuchazi umphumela othize we-ASA, ngaleyo ndlela ulahla isiguli sokwaziswa okubalulekile mayelana nendlela yokusebenza. Ama-algorithms alinganiswa nawo afana nalokhu:

• Ukucindezelwa kwe-COX-1 nokuyeka ukuhlanganiswa kwe-prostanoids;

• Ukuvinjelwa okungenakugwetshwa kwe-thromboxane A2 ukukhiqizwa ngamaplatelet;

• Isithiyo sokunamathiselwe kweplatelet ekuphelelweni kokugcina;

• Ukucindezelwa kwezinqubo zokuhlangana kwe-thrombocyte ndawonye;

• Ukungabikho kokwenza i-clothing arterial lumen ye-thrombus.

"Accekarol" ezimweni ezinzima

Futhi, imiyalelo yokusetshenziswa (isifinyeto, incazelo) enamathiselwe ekulungiseleleni "i-Acecardol" ayinikezi ulwazi isiguli mayelana nokusetshenziswa kwayo ngesikhathi sokuthuthukisa ukuphazanyiswa okunzima kwegazi enhliziyweni noma ebuchosheni. Ngokuyinhloko, ngokuthuthukiswa kwesimo se-clinic syndrome se-myocardial noma i-cerebral infarction, i-ASA ingakwazi futhi kufanele isetshenziswe.

Amathebulethi omuthi kufanele ahlolwe (ngesilinganiso sika 150-300 mg), futhi angagwinywa. Uma isiguli sinesidakamizwa esilinganisweni sama-50 mg, khona-ke ngesikhathi sesimo esibucayi kuyadingeka ngesikhathi esifanayo ukuhlaziya amaphilisi angu-3-6, uma isilinganiso singama-100 mg, bese kuthi amaphilisi angu-2-3, uma i-300 mg, bese kuthi ithebhulethi eyodwa. Lokhu kuyisizo esiphuthumayo, okuyinto eyanciphisa kakhulu amathuba okuba nesifo sengculazi esinamandla.

Ukungafani kokusetshenziswa kwe-"Acecardol"

Isidakamizwa esithi "i-Acecardol" (amaphilisi) imfundo ekusetshenzisweni kwezicelo, ukubuyekezwa kochwepheshe kanye nedatha yemithi kuqinisekisa ukulinganisela kwezinselele kanye nezinzuzo zokusetshenziswa. Kodwa-ke, ukuphikisana okuhambisana nezifo ezihambisana nezifo kufanele kuthathwe ngokucabangela uma uthatha isidakamizwa bese uthintana nodokotela. Ukuqhathaniswa kokuhlukaniswa kwehlukaniswe kube unomphela (ngokuphelele) futhi okwesikhashana. Ama-Absolute:

• Ukungaxolisi kwezidakamizwa ku-ASA, ukuthuthukiswa kwe-bronchospasm;

• I-hematoma ye-intracranial yezindawo ezihlukahlukene;

• I-vasculitis ene-Hemorrhagic ;

• Kuvinjelwe ukusebenzisa ezinganeni nasezingane ngenxa yengozi yokuthuthukiswa kwe-Ray's syndrome ;

• Kuvinjelwe ukuthatha abesifazane ngesikhathi se-lactation, ku-trimestre yokuqala neyesithathu yokukhulelwa.

Futhi, ukuphikisana okwesikhashana nokunomlomo kuncane kakhulu:

• Ukuhluleka kwe-Hepatic kanye ne-renal;

• Ukuba khona kwegazi eliqhubekayo, isikhathi sokuqala emva kwesikhathi (ukuphikisana kwesikhashana);

• Ukucindezeleka komzimba ngesikhathi sokuhlupheka, ukucindezeleka okungalawuleki;

• Ulcer of duodenum noma isisu ngenkathi kuqhuma (ukuvinjelwa kwesikhashana).

Imiphumela eminingi ye-Acecardol

Ngaphandle kwemiphumela ejwayelekile futhi efundwe kahle ebangelwa ukuvinjelwa kwe-COX, i-ACK nayo inomunye umphumela. Kwavezwa ngezibalo eziningana zezibalo emdlalweni we-US kanye nezikhungo ezinobungozi. Esikhathini sabo, umphumela omuhle wokusetshenziswa kwe-ASA ekuvimbeleni umdlavuza obulalayo - umdlavuza ogqamile wezizinda ezihlukahlukene - ubonakala.

Manje indlela yokukhonkxa yesenzo sokuzivikela sezinto ezidakamizwa ibonakala. Imibono yabacwaningi abaningi kanye nabahlengikazi bayavumelana ngokubaluleka komphumela wokuvimbela we-COX-2 ezingxenyeni eziphansi zamathumbu. Ukuvimbela ukuhlanganiswa kwe-prostaglandin E2, i-ASA ivumela ngokuhlelekile ukulawula ukufa nokukhiqizwa kwamaseli. Ngendlela, yile nqubo yamaselula eyona eyinhloko ekuthuthukiseni ama-neoplasms we-tumor.

Isiphetho esisekelwe kumaqiniso aqinisekisiwe yilokhu okulandelayo: umuthi "i-Acecaradol", imfundo, isicelo, izazi zezobuchwepheshe mayelana nokuthi yikuphi okuqinisekisa ukusebenza kwawo okulinganiselayo, kungasetshenziswa futhi njenge-agent yokuvimbela ekuvimbeleni izinqubo zesisu ezincane ezingxenyeni eziphansi zamathumbu. Phakathi neminyaka engama-5-12 yokuphatha, ingozi yokufa komdlavuza iyancipha, okuyinto ngokwemvelo ikhulisa isikhathi sokuphila. Noma kunjalo, i-ASA ayikwazi ukusetshenziselwa ukwelashwa nge-adenoma e-colorectal noma i-carcinoma yamathumbu.

Izinto ze-Analog nezinye izinto

Izici zokulungiselela "i-Acecardol": uhlelo lokusebenza, imfundo, ama-analogs, izinkomba zokuphathwa kwe-antithrombotic zivumela ukuzisebenzisela ukwelashwa kweziguli ezahlukene. Kodwa-ke, ochungechungeni lwe-antiplatelet agents, akusiyo kuphela ikhambi. E-Russia, kunezinhlobo ezingaba ngu-20 ze-ASK, ezinye zazo ezikhiqizwa ngendlela yesisu. Zisezingeni lokuphepha eliphansi kune "Acecaradol".

Amafomu emathumbu we-ASA ("Cardiomagnum", "Polokard"), amelwe emakethe yemithi yemithi, aphezulu kakhulu ngentengo. Ukuze umuthi "i-Acecaradol" intengo yonyango wanyangazonke yi-ruble angu-25. Izifaniso ezifanayo ngokufanayo nezindleko ezifanayo zokuvikeleka kwezindleko ezimbili kwezintathu ngaphezulu. Izidakamizwa zangaphandle futhi wenze izikhathi ezimbili noma eziyisihlanu ngaphezulu kunezindleko zokwelashwa kwebhajethi ngaphandle kwezinzuzo ezibonakalayo zesiguli esithatha i- "Acecaradol". Imiyalo yokusetshenziswa, ukwelashwa, ukubuyekezwa, izinkomba zezifanisi zalesi sidakamizwa nazo zifanayo.

Iziphetho mayelana nezinzuzo nezingozi ze-analogues ze "Acecardola"

Ukuhlala engabizi kakhulu, umuthi "i-Acecaradol" uhlangabezana ngokugcwele nezidingo zabahlengikazi. Ingozi yokusetshenziswa kwayo ihambisana nokusetshenziswa kwesicelo esiwusizo njenge-agent antiplatelet. Iphumelela ngokuvimbela i-thrombosis ephindaphindiwe yezinsimbi zenhliziyo nobuchopho, isetshenziswe ekufubeni kwe-atrial, isetshenziselwa imivimbo ye-varicose. Futhi uma kuqhathaniswa nama-analogues wesifunda, inzuzo ye- "Acecardola" inokutholakala kwamanani.

Leli qiniso likhulisa kakhulu ukubaluleka kwesidakamizwa esithi "Acecaradol": intengo yalesi sidakamizwa i-ruble engama-20. Lokhu kuncane kakhulu kunezindleko zamanye ama-antiplatelet agents. Kulesi simo phakathi kwezidakamizwa ze-ASA, ezakhiwe ngendlela evikelekile kakhulu emathunjini emathunjini, ngenani lilinganiselwe "Acecaradol". Kungokwemvelo ukuthi unikezwa ukwelashwa kwezifo okukhulunywe ngenhla, futhi ekuvimbeleni kwabo. Futhi inani lezinhlelo zokusebenza zalo lizokhula kancane kancane.