"Valsartan": imiyalelo yokusetshenziswa. Imithi "i-Valsartan" - ukufana nokubuyekezwa

Isidakamizwa, esibizwa nge "Valsartan", sichaza imiyalelo yokusetshenziswa njengenhlanganisela yeqembu le-pharmacotherapeutic ye-vasodilators yangaphandle. Ukusetshenziswa kwalesi sidakamizwa kunomphumela wokuhlaziya umzimba emzimbeni wesiguli. Futhi, lesi sidakamizwa sinomthelela ophikisayo owenzela i-AT ₁ receptors, okuyiyona eyabangela inqubo yokusebenzisa i-angiotensin II. Ngaphezu kwalokho, umphumela wesifo se-diuretic ungaba nomzimba womuntu njenge-agent ehlanganisiwe, njenge "Valsartan." Ama-analogues alawa makhambi - izidakamizwa "i-Diovan", "Ukukhukhumeza", "i-Tantordio" ne "Valsakor" - anezakhiwo ezifanayo.

Izici zesenzo semithi

Ngokuqondene nezici ezenzakalweni zesimiso sezokwelapha zalesi sidakamizwa esinamagciwane, lokho, ukuba ngumphikisi othize we-angiotensin II receptors, kuvikela ngokuphumelelayo i-AT ₁ receptors futhi kwandisa ukuhlushwa kwe-plasma ye-angiotensin II. Kulesi simo, isidakamizwa esithi "Valsartan" (imfundo yokusetshenziswa ichaza ngokubunjwa kwayo) akuvimbeli i-enzyme yokuguqula i-angiotensin. Futhi, ayikho umsebenzi we-agonistic ngokuphathelene ne-AT ₁ -mukeli. Phakathi kwezinye izinto, i-"Valsartan" yangempela ayivimbeli iziteshi ze-ion kanye nama-receptors wama-hormone, okubaluleke kakhulu ekulawuleni okujwayelekile kwesimiso senhliziyo. Ngaphezu kwalokho, lesi sidakamizwa asinomthelela ezingeni le-thyroglobulin, i-uric acid, i-cholesterol yakho kanye ne-glucose e-plasma yegazi.

Pharmacokinetics yomuthi

Uma sikhuluma nge-pharmacokinetics yesidakamizwa esinamandla kakhulu njengesidakamizwa esithi "i-Valsartan", ngakho-ke, njengomthetho, isheshe iminywe kusukela kumgudu wokugaya emva kokungena, nakuba izinga lokumunca lithembeke ekuhlukeni komuntu ngamunye.

Kulesi simo, umthelela wokuvimbela imithi, njengomthetho, uqala ukugcinwa ngemva kwemizuzu eyikhulu namashumi amabili emva kokuthatha isilinganiso esisodwa semithi, kanti umphumela omkhulu wokwelapha utholakala ngokwesilinganiso phakathi kwamahora amane kuya kwanguyisithupha. I- bioavailability ngokuphelele yalesi sidakamizwa ingaphezu kuka-22%. Ngokuzibophezela, ukubopha amaprotheni egazi (ikakhulukazi ama-albumin) kungama-94-98%. Ukususwa kwe-plasma kwesidakamizwa "i-Valsartan", okubunjwa kwayo kunomthelela oqondile kulokhu, kungu-2 l / h. Leli gciwane eliphikisana ne-antihypertensive likhishwa ikakhulukazi ngamanzi (cishe ngo-70%) futhi, kancane kancane, ngomchamo. Umkhiqizi uphinde ugcizelele ukuthi uma kwenzeka i-bile duct ishiywe noma i-cirrhosis ye-biliary, i-AUC yalesi sidakamizwa iyakhula ngokulinganisa ngesilinganiso sezinto ezimbili. Ngenkathi yezidakamizwa, akukho izinguquko ezakhiweni ze-pharmacokinetic kanye nemingcele ehlonishwayo.

Incazelo yomkhiqizo wokwelapha

Isidakamizwa esinamagciwane "Valsartan" sikhiqizwa (imfundo yokusetshenziswa okuyiyona ehlanganisiwe ephaketheni ngalinye) ngendlela yamathebulethi agqoke ukugqoka ifilimu nesimo se powder omhlophe. Lezi zinto azikho emthethweni emanzini avamile futhi zikwazi ukungena kalula emethanol ne-ethanol. Isisindo samangqamuzana salesi sidakamizwa sincane cishe ngo-430-435. Mayelana nokubunjwa kwaleli vasodilator, izakhi eziyinhloko ezikulo ziqukethe i-angiotensin II receptor blocker kanye ne-thiazide diuretic.

Ububanzi bezidakamizwa

Thatha amaphilisi "imiyalo ye-Valsartan" yokusetshenziswa, ngokuyinhloko, iphakamisa ekubunjweni kokubizwa okuthiwa okuyinkimbinkimbi kubantu ababhekene nesimo esingapheli sokwehluleka kwenhliziyo noma umfutho wegazi ophakeme.

Ngaphezu kwalokho, le nsizakalo ye-antihypertensive ikhonjiswe ukuthi isetshenziselwe ukuthuthukisa ukusinda kwabantu abane-infarction ye-myocardial ephawulekayo (kubandakanya ukungasebenzi kahle kwe-systolic ventricular noma ukwehluleka kwe-ventricular kwesokunxele). Iziguli ezinezifo zenhliziyo ezithatha izidakamizwa zendabuko nazo zivame ukubekwa umuthi "iValsartan". Ama-analogues ale thuluzi angasetshenziswa futhi kuwo wonke amacala abhalwe ngenhla.

Isilinganiso semithi

Ukuthatha odokotela bezidakamizwa ezincelisayo kakhulu bavame ukuphakamisa okukodwa noma kabili ngosuku ngezinkulungwane ezingamashumi ayisishiyagalombili noma amane, ngokulandelana. Uma kungekho umphumela wokwelashwa okudingekayo, isilinganiso sempilo singanyuka. Kodwa-ke, kuyadingeka ukwenza lokhu kancane kancane futhi kuphela odokotela abaya khona. Isilinganiso esiphezulu salesi sidakamizwa singamakhilomitha amathathu namashumi amabili.

Uhlu lwama-contraindications ongawasebenzisa

Sebenzisa lochwepheshe be-tape-vasodilator ngokungavamile ukuthi angasikhuthazi uma kwenzeka umuntu ekhuphula ukuzwela komuntu kunoma iyiphi ingxenye yayo. Ngendlela yokusabela okweqile, kuyadingeka nokugwema ukuthatha amaphilisi e-Valsartan. Isidakamizwa sokuqala akufanele futhi sithathwe ezigulini ezingakafiki eminyakeni eyisishiyagalombili. Isimo sokugcina senziwa ngenxa yokuthi ukuphepha kokusetshenziswa kwalesi sidakamizwa esinamandla okulwa namagciwane kulezi zimo akuqondi kahle.

Isicelo ngesikhathi sokukhulelwa

Memezela izidakamizwa "iValsartan" kwabesifazane abanomntwana, kuqiniswa ngokuphambene. Idatha evela ocwaningweni lwezokwelapha ehleliwe ibonisa ingozi ephezulu kakhulu yemiphumela emibi yalesi sidakamizwa esinamandla okulwa negciwane lesisu. Kodwa-ke, uma kwenzeka isifo esibi esisongela impilo lapho ezinye izidakamizwa eziphephile zingasetshenziselwa, noma zingasebenzi kahle, ukusetshenziswa kwale mithi ye-vasodilator kuvunyelwe. Ngokwehlukana, kufanele kushiwo ngokungavumeleki kokusebenzisa lo mkhiqizo ngenkathi ukondla usana olusanda kuzalwa ngobisi lwebele.

Ukusabela okunzima okungenzeka

Ukusetshenziswa kwezidakamizwa ezinjenge-antihypertensive njenge "Valsartan" kungabangela ukuphathwa ikhanda okukhulu, isizungu, ukukhwehlela nokubuthakathaka. Ngaphezu kwalokho, isiyaluyalu, isifo sohudo, i-hyperkalemia, ukuphelelwa amandla nokulala. Ubuhlungu besisu, i- vertigo, i-neutropenia, i-thrombocytopenia, i-arthralgia, ubuhlungu bomhlane, i-myalgia, i-asthenia ne-edema nayo ingabonakala ngokufanayo ngenxa yokuthatha u-Valsartan. Impendulo evela ezigodini ezazisisebenzisa ngaphambilini ibonisa ukuthi ingozi yokuthuthukisa i-pharyngitis, i-rhinitis, i-sinusitis, izifo ezihlukahlukene zegciwane kanye nezifo ezithinta iphezu eliphezulu lokuphefumula. Phakathi kwezinye izinto, abantu abaningi bane-hyperbilirubinemia, i-hematocrit yehle, i-hypercreatininaemia, ukwanda kwe-urea nitrogen index kanye nokwehla kwe-hemoglobin. Ngaphezu kwalokho, kufanele kukhunjulwe ngaso sonke isikhathi ukuthi ukuphathwa ngesikhathi esisodwa kwe-vasartilator "i-Valsartan" kanye nemithi ephuma eqenjini le-potassium-sparing diuretics lingakhuthaza ukuthuthukiswa kwe-hyperkalemia. Endabeni yokudlula ngokweqile komuthi, izimo ezifana ne-bradycardia, tachycardia, noma hypotension zingabonakala.

Ukuqapha okuyisisekelo

Ekuphetheni, kufanele kushiwo ukuthi kubalulekile ukuhlinzeka, ngokuqapha okukhulu futhi ngokucophelela ngaphansi kokulawulwa kwezokwelapha okuqinile, ukulawulwa kwalesi sidakamizwa esinamandla okulwa namagciwane kuya kweziguli ezinokuntuleka kwe-sodium, ukuphazamiseka kwengqondo, ukuphazamiseka kwesibindi, ukuphazamiseka kwamanye amazwe okuthiwa i-renal arteries noma ukwehla okuphawulekayo emtheni wegazi ojikelezayo. Lokhu ngokuyinhloko kuhlotshaniswa nengozi ephezulu yokuthuthukisa isiguli se-arterial hypotension. Ngaphezu kwalokho, kufaneleka ukunakekelwa okukhethekile kubantu ababhekene ne-biliary cirrhosis noma ukukhubazeka okukhulu kwesibindi somsebenzi. Iziguli ezine-stenosis ye-renal zidinga ukulawulwa njalo phezu kokuhlushwa kwe-urea nitrogen kanye nokuqukethwe kwe-serum creatinine. Kanti futhi, iziguli ezine-bile duct ukuvimbela, ezithatha i-potassium-sparing diuretics, izithako ezikhethekile ze-potassium noma amalungiselelo e-potassium, zidinga ukunakwa okukhethekile. Okokugcina, ngokuqapha okukhulu, kubalulekile ukusebenzisa i-agent ye-antihypertensive "i-Valsartan" kubantu abanomsebenzi wabo ohlobene nokushayela noma yiziphi izimoto, nalabo abanobuchwepheshe babo obuhlobene ngqo nokugxila okukhulu.