Mildronate® (makapisozi, 250 mg) Meldonium

1 kapisozi muli:

yogwira mankhwala - meldonium dihydrate 250 mg,

zokutira - wowuma wa mbatata, colloidal silicon dioxide, calcium stearate, kapisozi (thupi ndi chivindikiro) - titanium dioxide (E 171), gelatin.

Makapisozi a gelatin olimba No. 1 a mtundu woyera. Zomwe zili ndi ufa wowoneka ngati kristalo wonunkhira bwino. The ufa ndi hygroscopic.

Mankhwala

Meldonium imayambira ku carnitine, analogue ya gamma-butyrobetaine (GBB), chinthu chomwe chimapezeka mu khungu lililonse m'thupi la munthu.

Pazinthu zowonjezereka, meldonium imabwezeretsa malire pakati pa kubereka ndi kuchepa kwa mpweya m'maselo, imachotsa kudziunjikira kwa zinthu zopangidwa ndi poizoni m'maselo, kuziteteza kuti zisawonongeke, komanso kukhala ndi mphamvu yamphamvu. Chifukwa chakugwiritsa ntchito, kukana kwa thupi pazipsinjo komanso kuthekanso kubwezeretsa mwachangu mphamvu zosungiramo magetsi.

Mankhwalawa ali ndi mphamvu yolimbikitsa pakatikati kwamanjenje (CNS) - kuwonjezeka kwa ntchito zamagalimoto ndi kupirira kwamthupi. Chifukwa cha malowa, MILDRONAT ® imagwiritsidwanso ntchito kuwonjezera luso la thupi ndi malingaliro.

Mankhwala

Pharmacokinetics

Pambuyo pakumwa pakamwa, mankhwalawa amatengeka mwachangu, bioavailability ndi 78%. Kuzindikira kwamphamvu kwambiri m'madzi a m'magazi kumatheka patatha maola 1-2 mutangoyendetsa. Zimapangidwa mthupi ndi kupangika kwa ziwiri zazikulu

metabolites omwe amuchotsa impso. Hafu ya moyo ukamamwa pakamwa ndi maola 3-6.

Mankhwala

Meldonium (Mildronate ®) ndi analogue yoyambirira ya carnitine gamma butyrobetaine (pano pa GBB), momwe atomu imodzi ya hydrogen imasinthidwa ndi atomu ya nayitrogeni. Zokhudza thupi zimatha kufotokozedwa m'njira ziwiri.

Zotsatira za carnitine kaphatikizidwe

Zotsatira za zoletsa za ntchito ya butyrobetaine hydroxylase, meldonium imachepetsa biosynthesis ya carnitine ndipo motero imalepheretsa kayendedwe ka ma tinthu tambiri tating'onoting'ono tambiri mafuta am'mimba, ma cell, ma acylcarnitine ndi ma acylcoenzyme A. Mikhalidwe ya ischemia, Mildronate ® imabwezeretsa malire pakati pakutulutsa kwa okosijeni ndikugwiritsa ntchito maselo, imachotsa zovuta zoyendera kayendedwe ka ATP, pomwepo munthawi yomweyo kuyambitsa njira ina yopangira mphamvu - glycolysis, yomwe imachitika popanda kugwiritsa ntchito mpweya.

Ndi kuchuluka kowonjezereka chifukwa chogwiritsa ntchito mphamvu kwambiri m'maselo a thupi lathanzi, kuchepa kwakanthawi kwamankhwala amafuta kumachitika. Izi, zimapangitsanso kagayidwe ka mafuta acids, makamaka kaphatikizidwe ka carnitine. The biosynthesis ya carnitine imayendetsedwa ndi kuchuluka kwake kwa plasma ndi nkhawa, koma sizitengera kuchuluka kwa mtsogolo mwa carnitine mu cell. Popeza meldonium imalepheretsa kutembenuka kwa GBB kukhala carnitine, izi zimapangitsa kutsika kwa carnitine m'magazi, zomwe zimapangitsa kuti kapangidwe kake ka carnitine, ndiye kuti, GBB. Ndi kuchepa kwa kuchuluka kwa meldonium, njira ya carnitine biosynthesis imabwezeretseka ndipo kuchuluka kwa mafuta m'chipangacho ndikusintha. Chifukwa chake, maselowo amaphunzitsidwa mokhazikika, zomwe zimapangitsa kuti azikhala ndi moyo wopitilira kuchuluka kwa kuchuluka, momwe mafuta amomwe amapezeka mkati mwake amachepetsedwa nthawi zonse, ndipo katunduyo akatsika, mafuta omwe amapezeka mu acid amabwezeretsedwa mwachangu. Nthawi zambiri, maselo "ophunzitsidwa" mothandizidwa ndi mankhwalawa a Mildronate® amapulumuka nthawi yomwe maselo "osaphunzira" afa.

Mkhalapakati ntchito ya hypothetical GBB-ergic system

Zakhala zikuwonetseredwa kuti m'thupi mumakhala njira yosafotokozeredwa kale yoperekera zikhumbo za mitsempha - dongosolo la GBB-ergic, lomwe limatsimikizira kufalikira kwa kukhudzidwa kwa mitsempha m'maselo amtundu wina. Mkhalapakati wa dongosololi ndiye wotsogola mwachangu wa carnitine - ester wa GBB. Chifukwa cha esterase, izi

mkhalapakati amapatsa ma elekitrodi ku cell, potero kusamutsa kukhudzidwa kwa magetsi, ndipo iko kumasandulika kukhala GBB.

Kuphatikizika kwa GBB ndikotheka mu cell iliyonse yamthupi. Kuthamanga kwake kumayendetsedwa ndi kulimba kwa mphamvu yotsatsira komanso mphamvu, zomwe zimadalira ndende ya carnitine. Chifukwa chake, ndi kuchepa kwa carnitine ndende, kaphatikizidwe ka GBB kamalimbikitsidwa. Chifukwa chake, m'thupi mumakhala zinthu zingapo zachuma zomwe zimapereka kuyankha kokwanira kukwiya kapena kupsinjika: zimayamba ndikulandila kwa chizindikiro kuchokera ku minyewa ya mitsempha (mu mawonekedwe a elekitirodi), yotsatiridwa ndi kapangidwe ka GBB ndi ester yake, yomwe, imanyamula chizindikirocho. pa membatices cell cell. Ma cell a Somatic poyankha kukwiya amapanga mamolekyulu atsopano, ndikupereka kufalikira kwa chizindikiro. Pambuyo pa izi, mawonekedwe a hydrolyzed a GBB omwe akutenga nawo gawo la yogwira amalowa m'chiwindi, impso ndi ma testes, pomwe amasintha kukhala carnitine. Monga tanena kale, meldonium ndi analogue ya GBB, momwe atomu imodzi ya hydrogen imasinthidwa ndi atomu ya nayitrogeni. Popeza meldonium imatha kuwonekera pa GBB-esterase, imatha kukhala "wokambirana". Komabe, GBB-hydroxylase siyimakhudzanso meldonium ndipo chifukwa chake, ikafotokozedwa m'thupi, kuchuluka kwa carnitine sikukula, koma kumachepa. Chifukwa chakuti meldonium imakhala ngati "mkhalapakati" wopanikizika, komanso imachulukitsa zomwe zili mu GBD, zimathandizira kukulitsa kuyankha kwa thupi. Zotsatira zake, zochitika zonse za metabolic m'makina ena, mwachitsanzo, dongosolo lamkati lamanjenje (CNS), limakulanso.

Zizindikiro zogwiritsidwa ntchito

- angina pectoris ndi myocardial infarction (monga gawo la zovuta mankhwala)

- Matenda a mtima osachiritsika.

- pachimake cerebrovascular ngozi (zovuta mankhwala)

- hemophthalmus ndi retinal hemorrhages osiyanasiyana etiologies, thrombosis ya chapakati retin mtsempha ndi nthambi zake, retinopathy zosiyanasiyana etiologies (matenda ashuga, matenda oopsa)

- zochuluka m'maganizo komanso mwakuthupi, kuphatikiza pakati pa othamanga

- achire matenda obwera chifukwa cha uchidakwa (kuphatikizapo mankhwala ena a chidakwa)

Mlingo ndi makonzedwe

Gawani kwa akulu mkati.

Matenda a mtima

Monga gawo la zovuta mankhwala, 0,5-1.0 g patsiku pakamwa, kumwa mankhwala onse nthawi imodzi kapena kugawa mu 2 waukulu. Njira ya mankhwala ndi milungu 4-6.

Cardialgia kumbuyo kwa mtima - ndi pakamwa, 0,25 g 2 kawiri pa tsiku. Njira ya chithandizo ndi masiku 12.

Cerebrovascular ngozi

Pachimake gawo - mlingo jakisoni wa mankhwalawa amagwiritsidwa ntchito masiku 10, ndiye kuti amayamba kumwa mankhwalawo mkati ndi 0,5-1.0 g patsiku. Njira yonse ya chithandizo ndi milungu 4-6.

Matenda owopsa a cerebrovascular - 0,5 g pakamwa patsiku. Njira yonse ya chithandizo ndi milungu 4-6. Maphunziro obwerezedwanso (kawiri kawiri pachaka) amatha kuchitika atakambirana ndi dokotala.

Hemophthalmus ndi retinal hemorrhages a etiologies osiyanasiyana, thrombosis ya chapakati retine mtsempha ndi nthambi zake, retinopathy yosiyanasiyana etiology (matenda ashuga, matenda oopsa)

Mlingo wovomerezeka wa mankhwalawa umagwiritsidwa ntchito masiku 10, ndiye kuti amamwa mankhwalawa pakamwa pa 0,5 g patsiku, kumwa mankhwalawo nthawi imodzi kapena kugawa pakati. Njira ya mankhwala ndi masiku 20.

Kuchulukitsa kwa thupi ndi kwakuthupi, kuphatikiza pakati pa othamanga

Akuluakulu 0,25 ga pakamwa kanayi pa tsiku. Njira ya mankhwala ndi masiku 10-14. Ngati ndi kotheka, mankhwalawa amabwerezedwa pambuyo pa masabata awiri ndi atatu.

Osewera 0,5-1.0 g pakamwa kawiri pa tsiku asanaphunzitsidwe. Kutalika kwa maphunzirowo pakukonzekera ndi masiku 14-21, panthawi ya mpikisano - masiku 10-14.

Matenda osalekeza a mowa

Mkati, 0,5 g 4 pa tsiku. Njira ya chithandizo ndi masiku 7-10.

Contraindication

- Hypersensitivity to the yogwira mankhwala kapena kuzinto zothandizira za mankhwala

- kuchuluka kwazovuta zamkati (kuphwanya chotupa chamkati, zotupa za intracranial)

- mimba ndi mkaka wa m`mawere, chifukwa chosowa deta pa zamankhwala ntchito mankhwala panthawiyi

- ana ndi achinyamata osakwana zaka 18, chifukwa cha kusowa kwa chidziwitso cha kugwiritsa ntchito mankhwalawa munthawi imeneyi

Zochita zamankhwala osokoneza bongo

Imawonjezera mphamvu ya ma coronary dilating agents, mankhwala ena a antihypertensive, mtima glycosides.

Itha kuphatikizidwa ndi antianginal mankhwala, anticoagulants, antiplatelet agents, antiarrhythmic mankhwala, okodzetsa, bronchodilators.

Poona kukula kwa tachycardia wolimbitsa thupi ndi ochepa hypotension, kusamala kuyenera kuchitidwa pophatikizidwa ndi mankhwala omwe ali ndi vuto lofananalo.

Malangizo apadera

Chenjezo liyenera kuchitika mwa odwala omwe ali ndi vuto la chiwindi ndi matenda a impso.

Mildronate ® si mankhwala a mzere woyamba wa matenda oopsa a coronary.

Zambiri za momwe mankhwalawo amatha kuyendetsa magalimoto kapena njira zowopsa

Musamale muyenera kuyendetsa galimoto mukamayendetsa galimoto kapena pamakina oopsa.

Bongo

Milandu yamankhwala osokoneza bongo a Mildronate ® sakudziwika, mankhwalawa ndi oopsa.

Ngati bongo, mankhwala opatsirana.

Kutulutsa Fomu

Makapisozi 250 mg. Makapisozi 10 amawaika pachipala chovundikira cha polyvinyl chloride filimu yokhala ndi poliyo ya polyvinylidene chloride ndi zojambulazo za aluminium. Ma paketi anayi a ma contour cell limodzi ndi malangizo ogwiritsira ntchito boma komanso zilankhulo zaku Russia zimayikidwa mkatoni.

Pharmacokinetics

Pambuyo pakumwa pakamwa, mankhwalawa amatengeka mwachangu, bioavailability ndi 78%. Kuzindikira kwakukulu (C_max) mu madzi am'magazi zimatheka pambuyo pofika maola 1-2. Amapangidwa m'thupi makamaka m'chiwindi ndikupanga ma metabolites awiri akuluakulu omwe amatsitsidwa ndi impso. Hafu ya moyo (T₁/₂) mukamamwa pakamwa, kutengera mlingo, ndi maola 3-6.

Gwiritsani ntchito pa nthawi yoyembekezera komanso nthawi yoyamwitsa

Chitetezo chogwiritsidwa ntchito mwa amayi apakati sichinaphunziridwe, motero, pofuna kupewa zotheka pa mwana wosabadwayo, kugwiritsa ntchito mankhwala kwa amayi apakati kumatsutsana.

Kutulutsa mkaka ndi momwe thanzi la mwana wakhanda silinaphunziridwe, chifukwa chake ngati kuli koyenera, kugwiritsa ntchito mankhwalawa kuyenera kusiya kuyamwitsa.

Zotsatira zoyipa

Meldonium nthawi zambiri imalekeredwa. Komabe, mwa odwala omwe ali ndi vuto lotha kugwiritsidwa ntchito mopitilira muyeso, komanso muzochitika zomwe zimadutsa muyeso womwe umalimbikitsa, zimachitika zosafunikira.
Zochita zosafunikira zamagulu zimayikidwa m'magulu a dongosolo malinga ndi kuchuluka kwa ma frequency: pafupipafupi (> 1/10), nthawi zambiri (> 1/100 ndi 1/1000 ndi 1/10 000 ndi