Roxeracene, pezani, gulani

Zina zamalonda zamankhwala: Roxera

Dzinalo Lopanda Padziko Lonse: Rosuvastatin (Rosuvastatin)

Mlingo: mapiritsi okhala ndi filimu

Chithandizo: rosuvastatin

Gulu la Pharmacotherapeutic: lipid-kuchepetsa mankhwala.

Hypocholesterolemic ndi hypotriglyceridemic mankhwala. HMG CoA reductase inhibitors.

Katundu

Kuchita kwa kukonzekera kwa roxer kumapangidwira kupondaponda ntchito ya microsomal enzyme hydroxymethylglutaryl-CoA reductase, yomwe imakhala chothandizira kwambiri pakuchepetsa magawo a cholesterol synthesis.

Matenda a mtundu wa lipid mbiri (lipid-kutsitsa kwenikweni) chifukwa kuchepa kwa kuchuluka kwa magazi a cholesterol, triglycerides, lipoprotein otsika kwambiri, komanso kuwonjezeka kwa kuchuluka kwa kuphatikizana kwa lipoprotein. Mankhwalawa ndi a gulu la mankhwala "Statins".

Zisonyezero zogwiritsidwa ntchito:

Hypercholesterolemia ya pulayimale (mtundu IIa malinga ndi Fredrickson) kapena dyslipidemia (mtundu IIb malinga ndi Fredrickson) monga chowonjezera pakudya ndi kusakwanira kwa zakudya ndi njira zina zosagwiritsa ntchito mankhwala (mwachitsanzo, zolimbitsa thupi, kuchepa thupi), banja homozygous hypercholesterolemia monga kuwonjezera kwa zakudya ndi zina lipid-kutsitsa mankhwala (mwachitsanzo, LDL-apheresis) kapena ngati chithandizo chotere sichothandiza, hypertriglyceridemia (Fredrickson mtundu IV) monga chowonjezera chakudya, kuti muchepetse kupitilira kwa atherosulinosis ngati Zowonjezera ziwiri zazakudya kwa odwala omwe akuwonetsedwa chithandizo chochepetsa plasma ndende ya Chs ndi Chs-LDL, kupewa kwakukulu kwa mtima wamavuto (stroko, myocardial infarction, arasitalization ya arterialization) mwa odwala akuluakulu opanda matenda opatsirana a matenda am'mitsempha, koma ndi chiwopsezo cha kukula kwake (azaka zopitilira 50 kwa azibambo ndi zopitilira 60 kwa azimayi, kuchuluka kwa mapuloteni a C-reactive (≥2 g / l) pamaso pazinthu zina zowonjezera, monga matenda oopsa Zia, otsika madzi ambiri HDL-Xc, kusuta, oyambirira inatsekeratu mtsempha wamagazi matenda mbiri banja).

Mimba ndi mkaka wa m`mawere - Roxer ali contraindicated mu mimba ndi mkaka wa m`mawere. Amayi azaka zobereka azigwiritsa ntchito njira zokwanira zakulera.

Popeza cholesterol ndi zinthu zopangidwa kuchokera ku cholesterol ndizofunikira pakukula kwa mwana wosabadwayo, chiopsezo choletsa kuyambiranso kwa HMG-CoA kwa mwana wosabadwayo imaposa zabwino zakugwiritsira ntchito mankhwalawa panthawi yapakati.

Ngati muli ndi pakati pamankhwala, kugwiritsa ntchito mankhwalawa kuyenera kuyimitsidwa nthawi yomweyo.

Palibe chidziwitso pakuchuluka kwa rosuvastatin mkaka wa m'mawere (amadziwika kuti zoletsa zina za HMG-CoA reductase zitha kutulutsidwanso mkaka wa m'mawere), kotero kugwiritsa ntchito mankhwalawa kuyenera kusiyidwa panthawi yoyamwitsa.

Zoyipa:

Ndi tsiku lililonse mlingo mpaka 30 mg

Matenda a chiwindi mu gawo logwira (kuphatikiza kuwonjezereka kwa ntchito ya hepatic transaminases ndi kuwonjezereka kwa ntchito ya hepatic transaminases mu seramu yamagazi koposa nthawi 3 poyerekeza ndi VGN), kulephera kwambiri kwaimpso (CC osakwana 30 ml / min), myopathy, kugwiritsa ntchito cyclosporine, odwala odziwikiratu kukonzekera kwa zovuta za myotoxic, kutenga pakati, nthawi yoyamwitsa, kugwiritsa ntchito azimayi azaka zakubadwa omwe sagwiritsa ntchito njira zoyenera za kubereka, kulolera lactose, kusowa kwa lactose PS, shuga-galactose malabsorption syndrome, zaka 18, hypersensitivity kuti rosuvastatin kapena kuti chigawo chilichonse cha mankhwala.

Ndi tsiku lililonse 30 mg kapena kuposa:

zolimbitsa thupi mpaka kufinya kwambiri kwaimpso (CC zosakwana 60 ml / min), hypothyroidism,

matenda a minofu m'mbiri (kuphatikiza mbiri ya banja), myotoxicity ndi HMG-CoA reductase inhibitors kapena ulusi m'mbiri, kumwa kwambiri mowa, mikhalidwe yomwe ingayambitse kuchuluka kwa plasma ndende ya rosuvastatin, kugwiritsa ntchito fuko limodzi odwala a mtundu wa Mongoloid.

Mochenjera ndi tsiku lililonse mpaka 30 mg:

zaka zopitilira 65, kuthana ndi magazi, kuchita opaleshoni yayikulu, kuvulala kwambiri, kusokonezeka kwa ma endocrine kapena ma electrolyte kapena kugwidwa mosagwirizana, kugwiritsa ntchito munthawi yomweyo ndi ezetimibe.

Mlingo ndi makonzedwe:

Mankhwala amatengedwa pakamwa. Osatafuna phukusi kapena kumeza piritsi, kumeza lonse, kutsukidwa ndi madzi, kumatha kutengedwa nthawi iliyonse masana, ngakhale kudya kwambiri.

Asanayambe mankhwala ndi roxer, wodwalayo ayenera kuyamba kutsatira zakudya zapamwamba za hypocholesterolemic ndikupitilizabe kutsatira panthawi ya chithandizo. Mlingo wa mankhwalawa amayenera kusankhidwa payekha kutengera zolinga zamankhwala komanso chithandizo chamankhwala, potsatira malingaliro amtundu uliwonse pa chandamale cha plasma lipid.

Mlingo woyambira wa odwala omwe ayamba kumwa mankhwalawa, kapena kwa odwala omwe atengedwa kuti atenge ma inhibitors ena a HMG-CoA, akhale 5 kapena 10 mg kamodzi patsiku.

Ndi munthawi yomweyo kugwiritsa ntchito mankhwala ndi gemfibrozil, michere, nicotinic acid muyezo wa 1 g patsiku, odwala akulimbikitsidwa koyamba mlingo wa 5 mg. Mukamasankha koyamba mlingo, munthu akuyenera kutsogoleredwa ndi plasma cholesterol ndende ndikuwunika kuopsa kokhala ndi vuto la mtima, komanso kuopsa kwa zotsatira zoyipa kuyeneranso kukumbukiridwa. Ngati ndi kotheka, mlingo utha kuwonjezeka pambuyo pa masabata anayi.

Chifukwa cha kukhazikika kwa zotsatira zoyipa mukamagwiritsa ntchito mlingo wa 40 mg patsiku, poyerekeza ndi mlingo wochepa wa mankhwalawa, kuwonjezereka kwa 40 mg patsiku pambuyo poti mlingo wowonjezera umakhala wokwera kuposa momwe mankhwalawo amathandizira milungu 4 odwala omwe ali ndi vuto lalikulu la hypercholesterolemia ndipo ali pachiwopsezo chachikulu chotenga matenda a mtima (makamaka odwala omwe ali ndi hypercholesterolemia) omwe sanakwaniritse zotsatira zofunika za mankhwala omwe ali ndi 20 mg patsiku, ndipo -rs amene adzakhala kuyang'aniridwa ndi dokotala. Makamaka kuyang'anira odwala omwe amalandira mankhwalawa pa mlingo wa 40 mg patsiku akulimbikitsidwa.

Kugwiritsa ntchito mlingo wa 40 mg patsiku kwa odwala omwe sanakambirane ndi dokotala sikulimbikitsidwa. Pambuyo pamilungu ya 2-4 yothandizidwa ndi / kapena ndi kuchuluka kwa kukonzekera kwa roxer, kuwunika kwa metabolidi ya lipid ndikofunikira (kusintha kwa mlingo ndikofunikira ngati pakufunika).

Odwala omwe ali ndi vuto la aimpso wofatsa kapena pakati, kusintha sikofunikira. Odwala omwe ali ndi vuto lalikulu la impso (CC osakwana 30 ml / min), kugwiritsa ntchito roxer kumatsutsana. Kugwiritsa ntchito mankhwala osapitirira 30 mg tsiku limapangidwa kwa odwala omwe ali ndi pakati komanso kwambiri aimpso osakwanira (CC osakwana 60 ml / min). Kwa odwala omwe amalephera kupezeka aimpso, mankhwalawa amayankhidwa ndi 5 mg tsiku lililonse.

Roxer amatsutsana ndi odwala omwe ali ndi matenda a chiwindi. Palibe zokuchitikirani ndi kugwiritsa ntchito mankhwalawa kwa odwala omwe ali ndi vuto la chiwindi pamwamba pa mfundo za 9 (kalasi C) pamlingo wa Mwana-Pugh.

Odwala opitirira zaka 65 akulimbikitsidwa kuti ayambe kugwiritsa ntchito mankhwalawa ndi 5 mg tsiku lililonse.

Mukamaphunzira ma paracokinetic magawo a rosuvastatin mwa anthu amitundu yosiyanasiyana, kuwonjezereka kwa ndende ya rosuvastatin pakati pa Japan ndi China kudadziwika. Izi zimayenera kukumbukiridwa mukamagwiritsa ntchito mankhwala a Roxer m'magulu odwala. Mukamagwiritsa ntchito Mlingo wa 10 ndi 20 mg patsiku, mlingo woyambirira wa odwala a mtundu wa Mongoloid ndi 5 mg patsiku. Odwala a mtundu wa Mongoloid, kugwiritsa ntchito mankhwala mosokoneza 40 mg ndi kotsutsana.

Kugwiritsa ntchito mankhwala muyezo wa 40 mg ndi contraindicated odwala omwe akukonzekera chitukuko cha myotoxic. Ngati kuli kofunikira kugwiritsa ntchito Mlingo wa 10 ndi 20 mg patsiku, mlingo woyambira wa gulu ili la odwala ndi 5 mg.

Mukamagwiritsa ntchito gemfibrazil, mlingo wa kukonzekera kwa roxer sayenera kupitirira 10 mg patsiku.

Mogwirizana ndi mankhwala ena:

Cyclosporine - pogwiritsa ntchito munthawi yomweyo rosuvastatin ndi cyclosporine, AUC ya rosuvastatin imakhala yokwera kasanu ndi kawiri kuposa momwe amawonera odzipereka athanzi. Kuchuluka kwa plasma kwa rosuvastatin kumadzuka nthawi 11.

Kugwiritsa ntchito pamodzi ndi rosuvastatin sikukhudza kuchuluka kwa cyclosporine m'madzi a m'magazi.

Ma anticoagulants osadziwika - monga ena a HMG-CoA reductase inhibitors, kuyamba rosuvastatin mankhwala kapena kukulitsa mlingo wake mwa odwala omwe sanatenge anticoagulants nthawi yomweyo (mwachitsanzo, warfarin) angayambitse kuwonjezeka kwa MHO. Kuchoka kwa rosuvastatin kapena kuchepetsa kwake kungayambitse kuchepa kwa MHO. Zikatero, kuyang'aniridwa kwa MHO ndikulimbikitsidwa.

Ezetimibe - kugwiritsa ntchito pamodzi kwa rosuvastatin ndi ezetimibe sikuyenda limodzi ndi kusintha kwa AUC kapena Cmax kwa onsewa. Komabe, kulumikizana kwa pharmacodynamic pakati pa rosuvastatin ndi ezetimibe, komwe kumawonetsedwa ndi chiopsezo chowonjezeka cha minyewa yosafunikira, sikungathetsedwe.

Gemfibrozil ndi mankhwala ena otsitsa a lipid - kugwiritsa ntchito nthawi imodzi ya rosuvastatin ndi gemfibrozil kumapangitsa kuti Cmax ndi AUC a rosuvastatin awonjezeke. Gemfibrozil, fenofibrate, michere ina, ndi lipid-kuchepetsa matenda a nicotinic acid (waukulu kapena wofanana ndi 1 g patsiku) adakulitsa chiwopsezo cha myopathy akagwiritsidwa ntchito ndi HMG-CoA reductase inhibitors (mwina chifukwa chakuti amathanso kuyambitsa myopathy akagwiritsidwa ntchito mu monotherapy). Kugwiritsa ntchito munthawi yomweyo mafupa ndi rosuvastatin tsiku lililonse la 30 mg ndi contraindicated. Mwa odwala, chithandizo chimayenera kuyamba ndi 5 mg tsiku lililonse.

HIV protease zoletsa - kugwiritsa ntchito munthawi yomweyo kachilombo ka HIV protease zoletsa kungakulitse kwambiri kuchuluka kwa plasma ya rosuvastatin. Kugwiritsa ntchito nthawi imodzi 20 mg ya rosuvastatin komanso kuphatikiza ziwiri za HIV proteinase inhibitors (400 mg ya lopinavir / 100 mg wa ritonavir) imayendera limodzi ndi kuwonjezeka kwa kufanana kwa AUC (0-24 h) ndi Cmax ya rosuvastatin nthawi 2 ndi 5, motsatana.

Maantacidids - kugwiritsa ntchito nthawi yomweyo rosuvastatin ndi maantacid okhala ndi zotayidwa ndi magnesium hydroxide, kumabweretsa kuchepa kwa plasma ndende ya rosuvastatin ndi pafupifupi 50%. Izi sizitchulidwa kwenikweni ngati maacacid amagwiritsidwa ntchito maola 2 mutatha rosuvastatin.

Erythromycin - kugwiritsa ntchito nthawi yomweyo kwa rosuvastatin ndi erythromycin kumabweretsa kutsika kwa AUC (0-t) wa rosuvastatin ndi 20% ndi Cmax ndi 30%. Kuyanjana kotereku kumatha kuchitika chifukwa cha kuchuluka kwa matumbo chifukwa chogwiritsa ntchito erythromycin.

Njira za kulera za Hormonal / mahomoni obwezeretsanso (HRT) - kugwiritsa ntchito nthawi yomweyo kwa rosuvastatin ndi njira zakulera za mahormoni kumakulitsa AUC ya ethinyl estradiol ndi Norgestrel ndi 26% ndi 34%, motsatana. Kuwonjezeka koteroko kwa plasma kuyenera kuganiziridwanso posankha njira ya kulera kwa mahomoni. Palibe chidziwitso cha pharmacokinetic pakugwiritsa ntchito nthawi imodzi ya rosuvastatin ndi mankhwala othandizira mahomoni, chifukwa chake, zotsatira zomwezi sizingafanane ndikugwiritsa ntchito kuphatikiza uku. Komabe, kuphatikiza uku kunagwiritsidwa ntchito kwambiri panthawi ya mayesero azachipatala ndipo kunavomerezedwa ndi odwala.

Digoxin - Palibe kuyanjana kwakukulu kwa rosuvastatin ndi digoxin amene akuyembekezeka.

Ma Isoenzymes a cytochrome P450 - rosuvastatin sakhala choletsa kapena wochititsa cytochrome P450. Kuphatikiza apo, rosuvastatin ndi gawo lofooka la dongosolo la isoenzyme. Palibe mgwirizano wachipatala pakati pa rosuvastatin ndi fluconazole (choletsa wa isoenzymes CYP2C9 ndi CYP3A4) ndi ketoconazole (choletsa ma isoenzymes CYP2A6 ndi CYP3A4). Kugwiritsa ntchito pamodzi kwa rosuvastatin ndi itraconazole (choletsa kuwala kwa isoenzyme CYP3A4) kumakulitsa AUC ya rosuvastatin ndi 28%, yomwe ndi yoperewera. Chifukwa chake, kulumikizana komwe kumalumikizidwa ndi cytochrome P450 sikuyembekezeredwa.

Bongo:

Chithunzi cha chipatala cha bongo sichimafotokozedwa.

Ndi gawo limodzi la kuchuluka kwa mankhwalawa tsiku lililonse, mapiritsi a pharmacokinetic a rosuvastatin sasintha.

Chithandizo: chisonyezo, kuwunika ntchito za chiwindi ndi ntchito za CPK ndikofunikira, palibe mankhwala enieni, hemodialysis siyothandiza.

Zotsatira zoyipa:

Makamaka pazotsatira zoyipa: nthawi zambiri (> 1/10), nthawi zambiri (> 1/100, koma 1/1000, koma 1/10 000, koma

Zizindikiro zogwiritsidwa ntchito

Kodi chimathandiza Roxer ndi chiyani? Lembani mankhwalawa mu milandu iyi:

dyslipidemia kapena hypercholesterolemia yosakanikirana (monga zakudya ndi kuwonjezera kwa njira zosagwiritsa ntchito mankhwala - kuwonda, kuchita zolimbitsa thupi, ndi zina).
mabanja homozygous hypercholesterolemia (kuwonjezera pa njira yothandizira),
lembani IV hypertriglyceridemia (monga zakudya),
Kukula kwa atherosulinosis odwala amene mankhwala mankhwala kuchepa mu ndende ya Xc ndi Xs-LDL mu plasma,
kupewa chachikulu matenda a mtima (ochepa kusintha, matenda am'mimba, sitiroko) odwala omwe ali ndi chiyembekezo cha matenda amitsempha yamagazi, komanso okalamba,

Malangizo ogwiritsira ntchito Roxer, mlingo

Mlingo umayikidwa payekha, motsogozedwa ndi cholesterol m'madzi a m'magazi. Amamwa mankhwalawo mosasamala chakudya, osambitsidwa ndi madzi. Malinga ndi malangizo, mlingo woyambirira sapitilira 1 piritsi la Roxer 5 mg / 10 mg kamodzi patsiku.

Mlingo wapamwamba ndi 40 mg patsiku.

Kukhazikitsa mlingo waukulu wa 40 mg patsiku ndi kotheka kwa odwala omwe ali ndi vuto lalikulu la hypercholesterolemia komanso omwe ali pachiwopsezo chachikulu cha zovuta zamtima (makamaka munthawi ya mabanja a hypercholesterolemia), momwe zotsatira zosafunikira sizinachitike ndi 20 mg patsiku. Kuchita mankhwala kuyenera kuchitika kokha moyang'aniridwa ndi achipatala.

Kumwa mankhwalawa 40 mg tsiku patsiku kwa odwala omwe sanafunsane ndi dokotala sikulimbikitsidwa. Pambuyo pa masabata 2-4 ogwiritsira ntchito kapena pakukula kulikonse kwa mankhwala, ndikofunikira kuyang'anira mawonetseredwe a lipid metabolism (kusintha kwa mankhwalawa kungakhale kofunikira ngati kuli kofunikira).

Mlingo wa 20 mg / tsiku ndiwokwanira kwaonyamula a genotypes c.521CC kapena s.421AA. Mlingo wapamwamba kwambiri (40 mg) ukhoza kuperekedwa kwa odwala omwe ali ndi kuchuluka kwambiri kwa cholesterol komanso chiwopsezo chodwala mtima.

Kutenga ma anticoagulants (warfarin, etc.) nthawi yomweyo monga statin ingayambitse magazi, komanso mtima wamtima glycosides (mwachitsanzo, digoxin) - kuonjezera ndende yotsirizira.

Zotsatira zochizira zimachitika mkati mwa masiku 5-8, ndipo pazotheka kwambiri - pakadutsa masabata 3-4.

Zotsatira zoyipa

Malinga ndi malangizo ogwiritsira ntchito, kuikidwa kwa Roxer kungakhale limodzi ndi zotsatirazi zoyipa:

Pa mbali ya chitetezo chathupi: angioedema ndi zina zimachitikira ndi hypersensitivity.
Kuchokera ku dongosolo lamanjenje: chizungulire, kupweteka mutu, kuiwalaiwala, polyneuropathy.
Kuchokera m'mimba thirakiti: kupweteka m'mimba, nseru, kudzimbidwa, kapamba, matenda am'mimba, matenda am'mimba, kutsegula m'mimba, kuchuluka kwa hepatic transaminases.
Kuchokera pakhungu: kuyabwa, zidzolo, matenda a Stevens-Jones.
Kuchokera kumafupa ndi minyewa: myalgia, myopathy, rhabdomyolysis.
Kuchokera kwamikodzo dongosolo: proteinuria, hematuria.
General: asthenia.

Contraindication

Amakanizidwa kuti apereke Roxer pazochitika zotsatirazi:

Hypersensitivity to rosuvastatin kapena chilichonse cha mankhwala,
matenda a chiwindi mu gawo yogwira (kuphatikiza kuwonjezereka kwa ntchito ya hepatic transaminases ndi kuwonjezeka kwa zochitika za hepatic transaminases mu seramu yamagazi ndi nthawi zopitilira 3 poyerekeza ndi VGN),
zolimba mpaka zolimba aimpso (creatinine Cl osakwana 60 ml / min),
myopathy
kugwiritsa ntchito cyclosporine,
odwala omwe ali ndi chiyembekezo chotsogola,
mimba, yoyamwitsa,
ntchito kwa akazi amsinkhu wobereka omwe sagwiritsa ntchito njira zokwanira zakulera,
hypothyroidism
mbiri yamatenda am'mimba (kuphatikizapo mbiri ya mabanja),
myotoxicity mukamagwiritsa ntchito mbiri ina ya HMG-CoA reductase inhibitors kapena ma fibrate,
kumwa kwambiri mowa
mikhalidwe yomwe ingayambitse kuchuluka kwa rosuvastatin mu madzi a m'magazi,
kugwiritsa ntchito munthawi yomweyo mafupa,
lactose tsankho, kufupika kwa lactase, shuga-galactose malabsorption syndrome,
Odwala a Mongoloid
wazaka 18.

Bongo

Palibe chidziwitso pazachipatala cha bongo. Kusintha kwa magawo a pharmacokinetic a yogwira ntchito pamene mukumwa Mlingo waukulu sikuwoneka.

Rosuvastatin alibe antiidote imodzi; hemodialysis siyothandiza. Mu nkhani ya bongo, symptomatic mankhwala ikuchitika motsogozedwa chiwindi ntchito ndi creatine phosphokinase ntchito.

Ma analogi a Roxer, mtengo pama pharmacies

Ngati ndi kotheka, mutha kuyika Roxer ndi analogue yogwira ntchito - awa ndi mankhwala:

Rosulip,
Crestor
Rosart,
Reddistatin,
Lipoprime,
Rosuvastatin,
Suvardio
Rosistark,
Rosufast,
Rosucard.

Posankha analogi, ndikofunikira kumvetsetsa kuti malangizo ogwiritsira ntchito Roxer, mtengo ndi kuwunika kwa mankhwala omwe ali ndi zotsatira zofananira sizikugwira ntchito. Ndikofunikira kupeza upangiri wa dokotala komanso kuti usasinthe popanda mankhwala.

Mtengo muma Russian pharmacies: Roxer mapiritsi 5 mg 30 pcs. - kuchokera 384 mpaka 479 rubles, 10 mg 30 pcs. - kuchokera 489 mpaka 503 ma ruble, 15 mg 30pcs. - kuchokera ku ruble 560.

Sungani ku kutentha mpaka 25 ° C. Pewani kufikira ana. Moyo wa alumali ndi zaka zitatu. Mankhwala, chilolezo chachipatala chanyamuka.

Malinga ndi madokotala, Roxer amatsitsa mafuta m'thupi. Amadziwika kuti mankhwalawa amayamba kukhala ndi zotsatira zochizira mwachangu kuposa mankhwala ena omwe ali ndi vuto lofananalo. Ndi kulekerera kwabwino, chithandizo chautali ndizotheka. Mwa zolakwa zimawonetsa kukwera mtengo kwambiri ndi kukulitsa zovuta.

Ndemanga zitatu za "Roxer"

Ndi mapiritsi awa, adatsitsa cholesterol yamagazi m'miyezi iwiri kuchokera pa 9 mpaka 5.8, amatha kulekerera mosavuta (kupatula kupweteka kwapafupipafupi kumadzulo), imakhala modekha, osagwirizana ndi matendawa. Dokotala yemwe adayamwa kuti azimwa nthawi zonse, mtengo wa mankhwalawo ukukhumudwitsa, ndi wokwera mtengo kwa ine.

akayamba kukomoka, siyani kumwa mankhwalawa, amathandizadi wina, koma osati onse.

Ndidayesera. Kusinthaku kudadza kumapeto kwa sabata loyamba, koma mofananamo ndinali pachakudya. Anamwa mankhwalawa kwa nthawi yayitali, pafupifupi zaka 1.5 ndikupumira miyezi iwiri. Cholesterol otsika.

Kutulutsa Fomu

Roxer amapezeka mwa mawonekedwe a mapiritsi okhala ndi mawonekedwe oyera a filimu, omwe amasiyana maonekedwe kutengera kuchuluka kwa zomwe zimagwira mwa iwo:

Mapiritsi okhala ndi zomwe zili rosuvastatin pa mlingo wa 5, 10 kapena 15 mg, wokhala ndi mawonekedwe ozungulira, a biconvex, okhala ndi bevel. Mbali imodzi yolemba yapangidwa yolingana ndi mlingo wa zomwe zimagwira: "5", "10" ndi "15", motero.
Mapiritsi okhala ndi zomwe zili rosuvastatin pa mlingo 20 mg, kuzungulira, biconvex, ndi bevel.
Mapiritsi okhala ndi zomwe zili rosuvastatin pa mlingo wa 30 mg, biconvex, ali ndi mawonekedwe a kapisozi ndi zoopsa mbali zonse ziwiri.
Mapiritsi okhala ndi zomwe zili rosuvastatin pa mlingo wa 40 mg, biconvex, wokhala ndi mawonekedwe a capular.

Pamtambo wa piritsi, zigawo ziwiri zimawonekera bwino, mkati mwake muli oyera.

Zotsatira za pharmacological

The pharmacological zotsatira za mankhwala Roxer umalimbana:

Kuletsa kwa microsomal enzyme ntchito hydroxymethylglutaryl-CoA reductasezomwe zimagwira ngati chothandizira poletsa gawo loyambirira la kaphatikizidwe cholesterol.
Matenda a lipid mbiri (lipid-kutsitsa kwenikweni) pochepetsa magazi kuchuluka kwa onse cholesterol, triglycerides, lipoproteins kachulukidwe kachulukidwe komanso kuchuluka kwa chidwi lipoproteins kukwera kwambiri.

Mankhwalawa ndi a gulu la mankhwala "Madera”.

Pharmacodynamics ndi pharmacokinetics

Kamodzi m'thupi rosuvastatin zimadzetsa zotsatirazi:

Zimathandizira kuchepetsa kutsika kwakweza otsika kachulukidwe lipoprotein cholesterol,
Imathandizira kuchepetsa kukwera kwazonse cholesterol,
Zimathandizira kuchepetsa kukwera kwa triglyceride,
Zimathandizira Kuchulukitsa Kuzindikira kachulukidwe lipoprotein cholesterol,
Zimathandizira kuchepetsa kusamalidwa otsika kachulukidwe lipoprotein apolipoprotein (apoliprotein B),
Zimathandizira kuchepetsa kusamalidwa otsika kachulukidwe lipoprotein cholesterol,
Zimathandizira kuchepetsa kusamalidwa otsika kachulukidwe lipoprotein cholesterol,
Zimathandizira kuchepetsa kusamalidwa otsika kachulukidwe lipoprotein triglycerides,
Zimalimbikitsa Kulimbana magazi plasma apoliprotein A1,
Amachepetsa cholesterol otsika osalimba lipoproteinskuti kachulukidwe lipoprotein cholesterol,
Amachepetsa zigawo zonse cholesterol kuti kachulukidwe lipoprotein cholesterol,
Amachepetsa ziwerengero otsika kachulukidwe lipoprotein cholesterol kuti highensene lipoprotein cholesterol,
Amachepetsa ziwerengero otsika kachulukidwe lipoprotein apolipoprotein (apoliprotein B) kuti apolipoprotein A1.

The kutchulidwa matenda zotsatira za ntchito Roxers amakula sabata pambuyo kuyambika kwa maphunziro a mankhwala. Pafupifupi 90% ya mphamvu yonse ya mankhwala imadziwika pambuyo pa masabata awiri.

Nthawi zambiri zimatenga milungu inayi kuti zitheke, pambuyo pake zimasungidwa nthawi yonse yotsatira yamankhwala.

Zolemba malire plasma rosuvastatin zimadziwika kuti maola asanu mutatha kumwa mapiritsi, chizindikiro chonse cha bioavailability ndi 20%.

Rosuvastatin kwambiri biotransformed mu chiwindikukhala likulu loyambirira cholesterol ndi metabolizing otsika kachulukidwe lipoprotein cholesterol.

Kugulitsa zinthu ndi pafupifupi 134 malita. Pafupifupi 90% rosuvastatin kumangirira ku mapuloteni a plasma (makamaka albin).

Rosuvastatin zimapukusidwa pang'ono (pafupifupi 10%). Mu vitro pogwiritsa ntchito anthu hepatocytes kafukufuku kagayidwe zinthu zinaonetsa kuti zimangoyenera zochepa kagayidwe kutengera dongosolo la cytochrome P450 enzyme. Ndipo iyi kagayidwe sitingawonedwe kukhala ofunikira.

Chachikulu isoenzymekutenga nawo gawo rosuvastatin kagayidwendi CYP 2C9. Pocheperapo pang'ono, iwo amatenga nawo mbali. zoenzymes 2C19, 3A4 ndi 2D6.

Pakukonza kagayidwe, ziwiri zazikulu metabolite:

N-desmethyl yodziwika ndi pafupifupi theka zochita pang'ono poyerekeza ndi rosuvastatin. Ponena za lactone, ndiye imatengedwa ngati mawonekedwe osagwira ntchito m'chipatala.

Rosuvastatin ali ndi zochulukirapo 90% zoletsa kuzitsutsa hydroxymethylglutaryl-CoA reductase (HMG-CoA reductase), yomwe imazungulira mthupi la munthu m'magazi ambiri.

Zowilitsa kwambiri rosuvastatin (pafupifupi 90%) akuwonetsedwa wosasinthika ndi zomwe zilimo matumbo. Pankhaniyi, zonse zotengeka ndi zosasakanizidwa zimachotsedwa.

Zotsalirarosuvastatin chotsekedwa ndi impso ndi mkodzo (pafupifupi 5% - osasinthika).

Hafu ya moyo wa chinthucho ndi pafupifupi maola 20 ndipo sizitengera kuchuluka kwa mankhwalawa. Makamaka chilolezo kuchokera magazi a m'magazi pafupifupi malita 50 pa ola limodzi. Mlozera wosinthika wolingana ndi mtengo wapakati (mgawo wosinthira) ndi 21.7%.

Monga momwe ziliri ndi mankhwala ena omwe amapondereza ntchito hydroxymethylglutaryl-CoA reductaseKugwidwa ndi chiwindirosuvastatin imalimbikitsa kulowerera kwa membrane transporter OATP-S, yomwe imagwira ntchito yofunika kwambiri pakuchotsa zinthu ku chiwindi.

Rosuvastatin yodziwika ndi chiwonetsero chazidalira pokhudzana ndi mlingo, zomwe zimachulukana molingana ndi kuchuluka kwa zinthu.

Kugwiritsidwa ntchito mobwerezabwereza tsiku lililonse la mankhwalawa sikuti kumapangitsa kusintha kwa mapangidwe a mankhwala.

M'badwo wa wodwalayo komanso jenda sizikhudzanso mankhwala a pharmacokinetics. Nthawi yomweyo, kafukufuku adawonetsa kuti mwa odwala a mtundu wa Mongoloid, AUC komanso kuchuluka kwa plasma rosuvastatin pafupifupi owirikiza kawiri kuposa odwala omwe ali mu liwiro la Caucasian.

Amwenye ali ndi zizindikiro zofananira zomwe ndizokwera kwambiri kwa anthu aku Caucasi pafupifupi nthawi 1.3. Palibe zosiyana zikuluzikulu m'ndondomeko za oyimira mtundu wa Negroid ndi Caucasians.

Odwala kulephera kwa aimpso mwa mawonekedwe ofatsa kapena olimbitsa, zizindikiro za kukhathamira kwa rosuvastatin ndi N-desmethyl mu plasma sichikhala osasinthika.

Mitundu yayikulukulephera kwa aimpso chizindikiro cha plasma ndende rosuvastatin kumawonjezera katatu, ndipo chizindikiro cha plasma ndende kwambiri N-desmethyl- pafupifupi nthawi zisanu ndi zinayi poyerekeza ndi zizindikiro zowonetsedwa mwa odzipereka athanzi.

Ndende ya Plasma rosuvastatin mwa odwala omwe anali atapitilira hemodialysispafupifupi kawiri kuposa omwe amadzipereka odzipereka.

At kulephera kwa chiwindichifukwa cha matenda osokoneza bongo a chiwindi, matendawa plasma rosuvastatin okwera modekha.

Odwala omwe matenda awo ali m'gulu A mwana pew lonse, chizindikiro cha ndende yayikulu kwambiri rosuvastatin mu magazi a m'magazi ndipo AUC inakula ndi 60 ndi 5%, motsatana, poyerekeza ndi odwala, chiwindi womwe ndi wathanzi.

Ngati matenda chiwindi Zili m'gulu B la mwana pew lonse, Zizindikiro zimawonjezeka ndi 100 ndi 21%. Kwa odwala omwe matenda awo ali m'gulu C, zambiri sizikupezeka, zomwe zimagwirizanitsidwa ndi kusowa kwa rosuvastatin kwa iwo.

Contraindication

Contraindication poika mapiritsi a Roxer okhala ndi rosuvastatin mu Mlingo wofanana ndi 5, 10 ndi 15 mg ndi:

Hypersensitivity gawo limodzi kapena zingapo za mankhwala,
mafomu ogwira ntchito matenda a chiwindi (kuphatikiza kuphatikiza matenda omwe sanachidziwikirepo), komanso zikhalidwe zomwe zikuwoneka kuti zikuwonjezeka hepatic transaminases, ndi momwe aliyense wa hepatic transaminases ukuwonjezeka osachepera katatu,
matenda a impsokomwe kuchokerako creatinine sizidutsa kuchuluka kwa 30 ml / min,
cholowa chopita patsogolo matenda amitsemphayodziwika ndi kuwonongeka kwa minofu yoyamba (myopathies),
Kugwiritsa ntchito antidepressant Cyclosporin,
wapezeka ndi chiwopsezo chowonjezeka myotoxic zovuta,
tsankho lactose,
kuchepa kwa lactase,
shuga galactose malabsorption,
mimba (Komanso, mankhwalawa saikidwa kwa akazi azaka zoyambira kubereka ngati sagwiritsidwa ntchito kulera),
yoyamwitsa
wazaka 18.

Mapiritsi rosuvastatin 30 ndi 40 mg ndi zotsutsana:

odwala hypersensitivity gawo limodzi kapena zingapo za mankhwala,
odwala omwe ali ndi mitundu yogwira ntchito matenda a chiwindi (kuphatikiza kuphatikiza matenda omwe sanachidziwikirepo), komanso zikhalidwe zomwe zikuwoneka kuti zikuwonjezeka hepatic transaminases, ndi momwe aliyense wa hepatic transaminases ukuwonjezeka osachepera katatu,
matenda a impsokomwe kuchokerako creatinine sizidutsa kuchuluka kwa 60 ml / min,
cholowa chopita patsogolo matenda amitsemphayodziwika ndi kuwonongeka kwa minofu yoyamba (myopathies),
hypothyroidism,
Kugwiritsa ntchito antidepressant Cyclosporin,
wapezeka ndi chiwopsezo chowonjezeka myotoxic zovuta (akakhala m'mbiri ya wodwalayo pali cholembedwa cha poizoni wa minofu yemwe adapangidwa ndi mankhwala ena ochepetsa hydroxymethylglutaryl-CoA reductase kapena kukonzekera zochokera fibroic acid),
uchidakwa
mafomu olemera kulephera kwa chiwindi,
Mtundu wa Mongoloid
phwando munthawi yomweyo michere,
tsankho lactose,
kuchepa kwa lactase,
shuga galactose malabsorption,
mimba (nawonso, mankhwalawa sagwiritsidwa ntchito kwa akazi amisinkhu yakubereka ngati sagwiritsa ntchito njira zakulera),
yoyamwitsa
zaka mpaka 18 ndi okulirapo kuposa 70 zaka.

Zotsatira zoyipa

Zotsatira zoyipa izi zitha kuchitika mukamalandira chithandizo ndi Roxeroy:

zopsinjika chitetezo cha mthupikuphatikizapo zochita chifukwa cha hypersensitivity kuti rosuvastatin kapena zosakaniza zina za mankhwalawa, kuphatikizapo chitukuko angioedema,
zopsinjika m'mimba dongosolo, yomwe imafotokozedwa ngati kudzimbidwa kawirikawiri, kupweteka kwa epigastric dera, nseru, nthawi zina pamatha kuyamba kapamba,
zotupa zomwe zimachitika pakhungu ndi minyewa yodutsa ndipo zimafotokozedwa ngati zotupa pakhungu, kuyabwa pakhungu,urticaria,
chigoba minofu kukomoka, zomwe zimawoneka ngati myalgia (Nthawi zambiri) komanso nthawi zina myopathies ndi rhabdomyolysis,
mavuto ambiri, omwe ambiri amakhala asthenia,
zopsinjika impso ndi kwamikodzo, omwe nthawi zambiri umakhala limodzi ndi kuwonjezeka kwa kuchuluka kwa mapuloteni mumkodzo.

Roxer ikhoza kusintha kusintha kwa magawo a labotale. Chifukwa chake, mutamwa mankhwalawa, zochitika zimatha kuchuluka khalaniinZizindikiro zakumiseche shuga, bilirubinenzyme ya chiwindi gamma glutamyl transpeptidases, zamchere phosphatase, komanso zikuwonetsa kusintha kwa ma plasma a kusintha kwa ma hormone chithokomiro.

Pafupipafupi komanso kuopsa kwa zotsatirapo zake zimadalira mlingo.

Mapiritsi a Roxer: malangizo, ntchito, njira

Asanapereke mankhwala, wodwalayo amakulimbikitsidwa kusinthana ndi zakudya wamba, zomwe cholinga chake ndikuchepetsa cholesterol. Kutsatira izi ndikofunikira komanso nthawi yonse ya chithandizo.

Mlingo umasankhidwa payekha ndi dokotala wopezekapo kutengera cholinga chaumoyo ndi mphamvu yake. Amaloledwa kumwa mankhwalawa nthawi iliyonse, osamangidwa nthawi yakudya.

Piritsi limamezedwa lonse, osapwanya, osafuna kutafuna ndikumwa madzi ambiri.

Odwala ndi hypercholesterolemia muyenera kuyamba kumwa mankhwalawa ndi Mlingo wofanana ndi 5 kapena 10 mg rosuvastatin. Mapiritsi amatengedwa pakamwa kamodzi patsiku. Komanso, izi zimadwalirabe kwa odwala omwe sanalandiridwe ma statins, komanso kwa odwala omwe adachitapo kale mankhwala omwe amapondereza hydroxymethylglutaryl-CoA reductase.

Posankha mtundu woyambira wa Roxers, dokotala amatchera khutu kuzowonetsa cholesterol, imawunikanso zoopsa zachitukuko mtima ndi mavuto.

Muzochitika ngati pakufunika, mlingo ungasinthidwe kukhala wotsatira, komabe, kusintha kotereku kumachitika osati kale kuposa masabata 4 atasankhidwa koyamba.

Popeza kuti zovuta zimadalira mlingo mwachilengedwe, ndipo mukamamwa 40 mg wa rosuvastatin zimachitika pafupipafupi kuposa momwe zimakhalira ndizochepa kwambiri, kuwonjezera mlingo wa tsiku lililonse mpaka 30 kapena 40 mg uyenera kuchitidwa mosamala kwambiri:

odwala oopsa hypercholesterolemia,
odwala omwe amatha kupezeka ndi zovuta kuntchito Mitima ndi mtima dongosolo (makamaka, ngati wodwalayo wapezeka achibale hypercholesterolemia).

Ngati mukumwa Mlingo wocheperako rosuvastatin m'magulu awa odwala sanapereke zotsatira zoyembekezeredwa, pambuyo poika Roxers mu 30 kapena 40 mg patsiku, odwala ayenera kuyang'aniridwa ndi adokotala.

Komanso kuyang'aniridwa kwakanthawi kachipatala kumasonyezedwa ngati chithandizo chimayamba nthawi yomweyo ndi mlingo wa 30 kapena 40 mg.

Malinga ndi malangizo ogwiritsira ntchito, Roxer 20 mg imawonetsedwa ngati mlingo woyambirira wa kupewa matenda Mitima ndi zotengera kwa odwalaomwe ali ndi chiwopsezo chowonjezeka cha matenda amenewa.

Anthu omwe ali ndi vuto lofooka la ntchito impso kusintha kwa mankhwala sikofunikira, komabe, mankhwala amaperekedwa mosamala ku gulu la odwala.

Pankhani yalemala ntchito impso zochepa pakaperekedwe ka chilolezo creatinine mkati mwa 60 ml / mphindi, mankhwalawa amayamba ndi 5 mg. Mlingo waukulu wa mankhwalawa (30 ndi 40 mg) amatsutsana.

Odwala omwe ali ndi vuto lalikulu impsokupereka mankhwala mulingo uliwonse ndi woletsedwa.

Popereka mankhwala operekera roxers kwa odwala omwe ali ndi matenda a chiwindi, zizindikiro za mwana pew lonse osapitirira 7, palibe kuwonjezeka kwawonetsedwe rosuvastatin.

Ngati zizindikiro za matenda operewera chiwindizofanana ndi mfundo za 8 kapena 9 mkati mwana pew lonse, kuwonetsedwa kwa dongosolo kumawonjezeka. Chifukwa chake, musanapereke mankhwala kwa odwala oterowo, kafukufuku wowonjezera amafunika. impso.

Zambiri pochiza odwala omwe zizindikiro zawo zimaposa 9 mfundo mwana pew lonsesikusoweka.

Bongo

Mawonetseredwe azachipatala omwe angachitike ngati mulingo wovomerezeka utaperekedwa ndi mlingo wa mankhwalawo osafotokozeredwa. Patatha kamodzi muyezo wa Roxer muyezo kangapo kuposa womwe wakhazikitsidwa tsiku lililonse, kusintha kwakukulu mu pharmacokinetics rosuvastatin osadziwika.

Ngati bongo ndi zinachitikira Zizindikiro za kuledzera thupi limawonetsa chithandizo ndipo, ngati kuli kotheka, kuikidwa kwa njira yothandizira.

Kuwunikira zochitika kumalimbikitsidwanso. khalaniin ndikupanga mayeso kuti ayese magwiridwe antchito chiwindi.

Kuyenera kusankha kwake hemodialysis ongoyerekeza.

Kuchita

Poika Roxers kuphatikiza Cyclosporine kwambiri AUC rosuvastatin (pafupifupi nthawi zisanu ndi ziwiri), pomwe ndende ya plasma cyclosporine sichimasinthika.

Ndi munthawi yomweyo makonzedwe ndi antagonist mankhwala vitamini K kapena mankhwala osokoneza bongo omwe amathandizira hydroxymethylglutaryl-CoA reductase, kumayambiriro kwa chithandizo, komanso kuwonjezeka kwa mlingo wa tsiku ndi tsiku kudzera pakasinthidwe kake, kuwonjezeka kwa INR (chiwembu chofanizira padziko lonse lapansi) kungadziwike.

Monga lamulo, motsutsana ndi kumbuyo kwa kuchepetsedwa kwa mankhwala ndi titration kapena kusiya kwathunthu mankhwala, ichi chikuchepa.

Ntchito yogwirizana ndi mankhwala ochepetsa lipid Ezetimibe sizimayambitsa kusintha kwa AUC komanso kuchuluka kwa plasma kwa onse a mankhwalawa, komabe, kuthekera kwa kulumikizana kwa pharmacodynamic sikuchotsedwa.

Molumikizana ndi Gemfibrozil ndi mankhwala ena omwe amathandizira kuchepetsa milingo lipidskumakwiyitsa kuwirikiza kawiri mu AUC komanso kuchuluka kwa plasma rosuvastatin.

Kafukufuku wapadera awonetsa kusankhidwa kwawo ndi Fenofibrate mwanjira ina osati moni pakusintha kwa magawo a pharmacokinetic, komabe, mwayi wokhala wolumikizana ndi mankhwala

Lemberani mankhwala Hemfibrozil ndi Fenofibratekomanso mankhwala osokoneza bongo nicotinic acid, pomwe kupangana kwawo ndi zoletsa hydroxymethylglutaryl-CoA reductase onjezerani mwayi wa chitukuko myopathies (zomwe, mwina, ndi chifukwa cha kuthekera kwawo kupangitsa zotulukapo zofananira akapatsidwa mankhwala othandizira monotherapeutic).

Ndi kugwiritsa ntchito pamodzi kwa Roxers ndi mafupa, rosuvastatin Mlingo wofanana 30 ndi 40 mg sunasankhidwe. Koyamba tsiku lililonse rosuvastatin kwa odwala omwe akutenga mafupandi 5 mg.

Kugwiritsa ntchito moyenera mankhwala ndi zoletsa serinemapuloteni kumapangitsa kusintha kuwonekera rosuvastatin. Pazifukwa izi, Roxer sanasankhidwe. HIV- odwala omwe akuchiritsidwa ndi mankhwala osokoneza bongo ma protein a serine.

Mukutenga nthumwi plasma ndende kukonzekera rosuvastatinkuchepetsedwa ndi theka. Kuchepetsa zovuta za izimaantacid Ndikulimbikitsidwa kutenga maola awiri mutatenga mapiritsi a Roxer.

Poyerekeza ndi maziko apadongosolo nthawi imodzi rosuvastatin ndi Erythromycin Mlingo wa AUC rosuvastatin amatsika ndi 20%, ndipo plasma yake ya ndende ili pafupifupi gawo limodzi mwa magawo atatu. Izi zitha kukhala chifukwa chowonjezera kuyenda. matumbophwando lomwe limakwiyitsa Erythromycin.

Ndikusankhidwa kwa Roxers kuphatikiza ndi kulera kwapakati pa mahomoni pakuyendetsa pakamwa, chizindikiro cha AUC ethinyl estradiol ukuwonjezeka ndi 26%, ndi chisonyezo chomwecho cha chindapusa - pofika 34%.

Kuwonjezeka kumeneku kwa milingo ya AUC kuyenera kuganiziridwa posankha mulingo woyenera. kulerapakamwa.

Palibe zambiri za pharmacokinetic zokhudzana ndi kugwiritsidwa ntchito mosiyanasiyana ndi mankhwala othandizira amalo am'magazi, komabe, kuyanjana kwa mgwirizano ndi kuchuluka kwa AUC sikuchotsedwa.

Maphunziro a kuphatikiza kwa rosuvastatin ndi pacemaker Digoxin sizinawonetsetse mgwirizano uliwonse.

Rosuvastatin Zilibe mphamvu komanso zopatsa mphamvu zoenzymes kachitidwe cytochrome P450. Kuphatikiza apo, kagayidwe rosuvastatin motsogozedwa ndiiwo ndi ochepa komanso osawakhudza.

Kuyanjana kwamtundu uliwonse pakati rosuvastatin ndi othandizira Fluconazole ndi Ketoconazolecholetsa ntchito ya cytochrome isoenzymes sichinadziwike.

Kuphatikiza ndi antifungal mankhwala Intraconazole, omwe amalepheretsa ntchito isoenzyme CYP 3A4, imayambitsa kuwonjezeka kwa AUC ya rosuvastatin ndi 28%. Komabe, kuwonjezeka kumeneku sikuti kofunika mu chipatala.

Pharmacokinetics

Nthawi yofika ndende yozama ya plasma (Cmax) ya rosuvastatin m'magazi pambuyo pakukonzekera pakamwa ndi pafupifupi maola 5. Mtheradi bioavailability wa chinthu

20% Metabolism imachitika makamaka m'chiwindi. Kuchuluka kwa magawanidwe kuli pafupifupi 134 malita. Zambiri mwa zinthuzi (pafupifupi 90%) zimagwirana ndi mapuloteni a plasma, makamaka ndi albumin.

Rosuvastatin akudwala kagayidwe kakang'ono (

10%). Katunduyu ndi wa masanjidwe enaake apadera a cytochrome P450. Isoenzyme yayikulu yomwe imakhudzidwa ndi kagayidwe kake ndi isoenzyme CYP2C9. Kuphatikizidwa mu metabolism ya isoenzymes CYP2C19, CYP3A4, CYP2D6 imachitika pang'ono. Ma metabolites odziwika bwino ndi N-desmethylrosuvastatin (ntchito ndi yotsika 2 kuposa rosuvastatin) ndi lactone metabolites (alibe zochitika za pharmacological). Ntchito ya pharmacological yoletsa plasma HMG-CoA reductase imaperekedwa makamaka chifukwa cha rosuvastatin (oposa 90%).

Pafupifupi 90% ya chinthucho chimapukusidwa kudzera m'matumbo osasinthika (kuphatikizapo rosuvastatin), ena - ndi impso. Hafu ya moyo wa chinthu kuchokera m'madzi a m'magazi ndi pafupifupi maora 19 (kuwonjezereka kwa mankhwalawa sikukhudza chisonyezo ichi). Geometric imatanthawuza kutuluka kwa plasma ndi 50 l / h (yokhala ndi kusintha kosiyanasiyana - 21.7%).

Ndi kudya kwa tsiku ndi tsiku, kusintha kwa magawo a pharmacokinetic sikuwoneka. Kuwonekera kwantchito kumawonjezeka molingana ndi mlingo.

Malinga ndi kafukufuku wa pharmacokinetic, mwa odwala a mtundu wa Mongoloid (Japan, Filipinos, Chinese, Koreans and Vietnamese), Median AUC ndi kuchuluka kwakukulu kwa rosuvastatin kuwonjezeka pafupifupi kawiri poyerekeza ndi mpikisano wa Caucasoid, kwa amwenye chokwanira kuti chiwonjezeko cha Median AUC ndi Cmax ndi 1.3.

Odwala okhala ndi creatinine chilolezo (CC) osakwana 30 ml / min, kuchuluka kwa plasma kwa rosuvastatin ndi N-desmethylrosuvastatin m'magazi kumawonjezeka kwambiri.

Odwala matenda a chiwindi osachiritsika, plasma ndende ya rosuvastatin imadzuka pang'ono. Poyerekeza: odwala omwe ali ndi chiwindi chantchito / odwala omwe ali ndi vuto la chiwindi (malinga ndi Mwana-Pugh lonse: 7 kapena mfundo zotsika / 8-9 point) AUC ndi Cmax wa rosuvastatin amawonjezeka ndi 5 ndi 60% / 21 ndi 100%, motero. Zochitika ndi rosuvastatin mwa odwala omwe ali ndi vuto la chiwindi pamwamba pa mfundo za 9 palibe.

Kupanga ndi mawonekedwe a kumasulidwa

Mankhwala Roxer akupezeka mawonekedwe a piritsi pakamwa pakamwa. Mapiritsiwa amakhala atakutidwa ndi filimu yoyera. Kuzungulira, biconvex wokhala ndi bevel, mbali imodzi yolemba "10", yokhazikika. Chofunikira chachikulu pa mankhwalawa ndi rosuvastatin. Zomwe zili mu piritsi limodzi ndi 10 mg. Zina zomwe zikuphatikizidwazo ndi monga:

Macrogol 6000.
Methyl methacrylate kopolymer.
Microcrystalline cellulose.
Colloidal silicon dioxide.
Titanium dioxide
Crospovidone.
Lactose Monohydrate.
Magnesium wakuba.

Mapiritsi a Roxer amayikidwa mu chithuza chamtundu wa zidutswa 10. Phukusi la katoni lili ndi matuza atatu kapena 9 ndi malangizo ogwiritsira ntchito mankhwalawa.

Mankhwala

Chofunikira chachikulu cha mapiritsi a Roxer ndi rosuvastatin, chomwe chimalepheretsa ntchito ya enzyme HMG-CoA reductase, yomwe imayang'anira kaphatikizidwe ka presteror ya mevalonate cholesterol. Imagwira maselo a chiwindi, omwe amayang'anira kapangidwe ka cholesterol ya endo native (yake), chifukwa chomwe mulingo wake m'magazi umachepa. Komanso, motsutsana ndi kagwiritsidwe ntchito ka mankhwala, lipoproteins yotsika kwambiri komanso yotsika kwambiri (imathandizira kuyikika kwa cholesterol m'makoma amitsempha) komanso kuchuluka kwa lipoproteins kumawonjezeka (kuchepetsa kukula kwa njira yogwirira ntchito kwa cholesterol m'makoma a mitsempha).

Mutatenga mapiritsi a Roxer mkati, chophatikiza chimagwira mwachangu, koma osalowa mu magazi. Ndi magazi, amalowa m'maselo a chiwindi (hepatocytes), komwe amakhala ndi mphamvu yochizira. Rosuvastatin samapangidwira ndipo amachotsa osasinthika makamaka ndi ndowe.

Mlingo ndi makonzedwe

Mkati, piritsi sayenera kutafuna kapena kuphwanya, kumeza lonse, kutsukidwa ndi madzi, imatha kutengedwa nthawi iliyonse ya tsiku, mosasamala nthawi yakudya. Asanayambe chithandizo ndi Roxer, wodwalayo ayenera kuyamba kutsatira zakudya zapamwamba za hypocholesterolemic ndikupitilizabe kutsatira panthawi ya chithandizo. Mlingo wa mankhwalawa amayenera kusankhidwa payekha kutengera zolinga zamankhwala komanso chithandizo chamankhwala, potsatira malingaliro amtundu uliwonse pa chandamale cha plasma lipid. Mlingo woyambirira wa odwala omwe ayamba kumwa mankhwalawa, kapena kwa odwala omwe atengedwa kuchokera ku kutenga zina za HMG-CoA reductase, ayenera kukhala 5 kapena 10 mg wa mankhwala a Roxer 1 pa tsiku.

Ndi munthawi yomweyo kugwiritsa ntchito mankhwala ndi gemfibrozil, michere, nicotinic acid mu lipid kutsitsa Mlingo (1 g / tsiku), odwala akulimbikitsidwa koyamba mlingo wa 5 mg / tsiku. Mukamasankha koyamba mlingo, munthu akuyenera kutsogoleredwa ndi plasma cholesterol ndende ndikuwunika kuopsa kokhala ndi vuto la mtima, komanso kuopsa kwa zotsatira zoyipa kuyeneranso kukumbukiridwa. Ngati ndi kotheka, mlingo utha kuwonjezeka pambuyo pa masabata anayi.

Chifukwa cha kukhazikika kwa zotsatira zoyipa mukamagwiritsa ntchito mlingo wa 40 mg / tsiku, poyerekeza ndi Mlingo wochepa wa mankhwalawa, kuwonjezera kuchuluka kwa 40 mg / tsiku kuyenera kuganiziridwa kokha mwa odwala omwe ali ndi vuto lalikulu la hypercholesterolemia komanso omwe ali pachiwopsezo chokhala ndi zovuta zamtima (mtima) makamaka odwala omwe ali ndi mabanja a hypercholesterolemia) omwe sanakwaniritse zotsatira zoyenera za mankhwala ndi 20 mg / tsiku, ndipo adzayang'aniridwa ndi dokotala. Makamaka kuyang'anira odwala omwe amalandira mankhwalawa pa 40 mg / tsiku akulimbikitsidwa.

Kugwiritsa ntchito mlingo wa 40 mg / tsiku kwa odwala omwe sanakambirane ndi dokotala sikulimbikitsidwa. Pambuyo pamankhwala a 2-4 milungu komanso / kapena kuwonjezeka kwa mankhwala a Roxer, kuwunika kagayidwe ka lipid ndikofunikira (kusintha kwa mankhwalawa ndikofunikira).

Odwala omwe ali ndi vuto la impso

Odwala omwe ali ndi vuto la aimpso wofatsa kapena pakati, kusintha sikofunikira. Odwala omwe ali ndi vuto lalikulu la impso (CC osakwana 30 ml / min), kugwiritsa ntchito Roxer kumatsutsana. Kugwiritsidwa ntchito kwa Roxer muyezo woposa 30 mg / tsiku kumatsutsana mwa odwala omwe ali ndi mphamvu yochepa kwambiri ya impso (CC osakwana 60 ml / min). Kwa odwala omwe amalephera kupezeka aimpso, njira yoyamba ya Roxer ndi 5 mg / tsiku.

Gwiritsani ntchito panthawi yoyembekezera komanso poyamwitsa

Mankhwala a Roxer ali contraindicated mu mimba ndi mkaka wa m`mawere.

Amayi azaka zobereka azigwiritsa ntchito njira zokwanira zakulera.

Ngati muli ndi pakati pamankhwala, kugwiritsa ntchito mankhwalawa kuyenera kuyimitsidwa nthawi yomweyo.

Matenda aimpso

Odwala omwe amalandira mlingo waukulu wa rosuvastatin (makamaka 40 mg / tsiku), proteinuria ya tubular imawonedwa, yomwe idapezeka ndikugwiritsa ntchito mayeso ndipo, nthawi zambiri, inali yochepa kapena yochepa. Proteuria yotereyo sisonyeza kupweteka kwambiri kapena kupitirira kwa matenda a impso. Pafupipafupi kuwonongeka kwamphupi komwe kumawonetsedwa mu kafukufuku waposachedwa wa rosuvastatin ndiwokwera ndi mlingo wa 40 mg / tsiku. Odwala omwe amamwa mankhwala a Roxer pa mlingo wa 30 kapena 40 mg / tsiku, tikulimbikitsidwa kuwunika mawonetseredwe aimpso pa mankhwala (osachepera nthawi 1 m'miyezi itatu).

Zokhudza mphamvu ya masculoskeletal system

Mukamagwiritsa ntchito rosuvastatin mu Mlingo wonse, koma makamaka mu Mlingo wopitilira 20 mg / tsiku, zotsatirazi pazotsatira za minofu yam'mimba zimanenedwa: myalgia, myopathy, nthawi zina, rhabdomyolysis. Zochitika kawirikawiri kwambiri za rhabdomyolysis zimadziwika ndi kugwiritsa ntchito nthawi imodzi kwa HMG-CoA reductase ndi ezetimibe zoletsa. Kuphatikiza koteroko kuyenera kugwiritsidwa ntchito mosamala, popeza kulumikizana kwa pharmacodynamic sikungathetsedwe. Monga momwe zimakhalira ndi ma inhibitors ena a HMG-CoA reductase, pafupipafupi ma rhabdomyolysis pakugwiritsa ntchito malonda a Roxer akukwera kwambiri pamene mlingo ndi 40 mg / tsiku.

Kudziwitsa za ntchito za CPK

Ntchito za CPK sizingadziwike pambuyo pakuchita zolimbitsa thupi kwambiri komanso chifukwa cha zifukwa zina zowonjezera zomwe zingachitike, izi zitha kubweretsa kutanthauzira kolakwika kwa zotsatira zake. Ngati ntchito yoyambirira ya CPK ichuruka kwambiri (maulendo 5 kuposa malire apamwamba), kuwunikiranso mobwerezabwereza kuyenera kuchitika pambuyo masiku 5-7. Simungayambe mankhwala ngati zotsatira za kukonzanso zimatsimikizira ntchito zoyambirira za KFK (zopitilira 5 kupitirira malire apamwamba).

Musanayambe mankhwala

Kutengera mlingo wa tsiku ndi tsiku, mankhwala a Roxer ayenera kuikidwa mosamala kwa odwala omwe ali ndi chiopsezo cha myopathy / rhabdomyolysis, kapena kugwiritsa ntchito mankhwalawa ndi contraindicated (onani magawo "Contraindication" ndi "Chenjezo").

Izi ndi monga:

kuwonongeka kwaimpso,
hypothyroidism
mbiri yamatenda am'mimba (kuphatikizapo mbiri ya mabanja),
zotsatira zanga za myotoxic mukamamwa ma HMG-CoA reductase inhibitors kapena ma fiber ena m'mbiri,
kumwa kwambiri
zaka zopitilira 65
Momwe kuchuluka kwa rosuvastatin mu madzi amwazi kumachulukira,
kugwiritsa ntchito munthawi yomweyo ma fiber.

Mu odwala oterowo, ndikofunikira kuyesa kuopsa komanso zabwino zomwe mungapeze pochiritsira. Kuwunikira zamankhwala kumalimbikitsidwanso. Ngati ntchito yoyambirira ya CPK ndi yochulukirapo kuposa kasanu kuposa momwe munakhalira kale, chithandizo ndi Roxer sichiyenera kuyamba.

Munthawi ya mankhwala

Wodwalayo ayenera kudziwitsidwa zakufunika kwakanthawi kuchipatala msanga ukayamba kupweteka, kufooka kwa minofu kapena kukokana, makamaka kuphatikiza ndi malaise ndi malungo. Mwa odwala, ntchito za CPK ziyenera kutsimikizika. Therapy iyenera kutha ngati ntchito ya CPK ikuchulukirachulukira (kangapo ka 5 poyerekeza ndi malire apamwamba) kapena ngati minyewa imatchulidwa komanso imayambitsa kusasangalala tsiku ndi tsiku (ngakhale ntchito ya CPK isapitirire 5 times malire zikhalidwe). Ngati zizindikiro zitha ndipo ntchito ya CPK ibwerera mwakale, kuganiziridwanso kuyenera kuyambiranso kugwiritsa ntchito Roxer kapena HMG-CoA reductase inhibitors mumadontho ochepetsetsa mosamala kuyang'aniridwa ndi achipatala. Kuwunikira ntchito za CPK pakalibe zizindikiro sikungathandize. Milandu yocheperako kwambiri yokhala ndi mycrathy yokhala ndi chitetezo chochepa kwambiri pakuwonetsa kufooka kwa minofu ndikuwonjezera ntchito ya seramu CPK panthawi yamankhwala kapena poyimitsa kugwiritsa ntchito zoletsa za HMG-CoA reductase, kuphatikiza rosuvastatin, zidadziwika. Maphunziro owonjezera a minofu ndi dongosolo lamanjenje, maphunziro a serological, komanso mankhwala a immunosuppress angafunike.

Panalibe zisonyezo zakuchuluka kwa minofu yamafupa mukamamwa mankhwala a rosuvastatin ndi concomitant. Komabe, kuwonjezeka kwa zochitika za myositis ndi myopathy kunanenedwa kwa odwala omwe amatenga zina za HMG-CoA reductase inhibitors kuphatikiza ndi fibroic acid derivatives (mwachitsanzo gemfibrozil), cyclosporine, nicotinic acid mu lipid kutsitsa Mlingo (zoposa 1 g / tsiku), antifungal zotumphukira. azole, HIV protease inhibitors ndi mankhwala a macrolide.

Mukamagwiritsa ntchito zoletsa zina za HMG-CoA reductase, gemfibrozil imawonjezera chiopsezo cha myopathy. Chifukwa chake, kugwiritsa ntchito munthawi yomweyo mankhwala a Roxer ndi gemfibrozil osavomerezeka. Ubwino wa kusintha kwa plasma ndende ya lipids ndi kuphatikiza kwa Roxer wokhala ndi mafupa kapena nicotinic acid mu lipid yotsitsa Mlingo uyenera kuyesedwa bwino poganiza za chiopsezo. Mankhwala Roxer pa mlingo wa 30 mg / tsiku ali contraindicated kuphatikiza mankhwala ndi fibrate. Chifukwa cha kuchuluka kwa matenda a rhabdomyolysis, Roxer sayenera kugwiritsidwa ntchito mwa odwala omwe ali ndi vuto lalikulu lomwe lingayambitse mypathy kapena zochitika zomwe zimayambitsa kukula kwa aimpso (mwachitsanzo, sepsis, hypotension ya arterial, opaleshoni yayikulu, zoopsa, metabolic, endocrine komanso electrolyte kapena kupweteka kosalamulirika).

Zokhudza chiwindi

Kutengera mlingo wa tsiku ndi tsiku, Roxer ayenera kugwiritsidwa ntchito mosamala odwala omwe amamwa kwambiri mowa komanso / kapena mbiri yodwala matenda a chiwindi kapena kugwiritsidwa ntchito kwake kumatsutsana (onani magawo "Contraindication" ndi "Chenjezo").

Ndikulimbikitsidwa kudziwa kuyesedwa kwa chiwindi chisanayambe mankhwala ndi miyezi itatu itayamba. Kugwiritsa ntchito mankhwala Roxer kuyenera kusiyidwa kapena kuti mankhwalawa azitha kuchepetsedwa ngati ntchito ya "chiwindi" mu seramu yamagazi ikukwera katatu kuposa pamlingo wapamwamba.

Odwala a hypercholesterolemia chifukwa cha hypothyroidism kapena nephrotic syndrome, mankhwalawa amayambitsidwa ndi matenda oyambitsidwa ndi Roxer.

Mlingo

Mapiritsi okhala ndi mafilimu 5 mg, 10 mg, 20 mg ndi 40 mg

Piritsi limodzi lili

ntchito yogwira - rosuvastatin calcium 5.21 mg, 10,2 mg, 20,83 mg, kapena 41.66 mg (ofanana ndi 5 mg rosuvastatin, 10 mg, 20 mg ndi 40 mg, motsatana),

muobwera: microcrystalline cellulose, anhydrous lactose, crospovidone, silicon dioxide, colloidal anhydrous, magnesium stearate,

filimu pachimake: wapolisi wamkulu wa botacrylate wa mabotolo, macrogol 6000, titanium dioxide E171, lactose monohydrate.

Mapiritsi ali pozungulira, okhala ndi biconvex pang'ono, wokutidwa ndi filimu yoyera, yolembedwa "5" mbali imodzi komanso bevel (pamlingo wa 5 mg).

Mapiritsi ali pozungulira, okhala ndi biconvex pang'ono, wokutidwa ndi filimu yoyera, yolembedwa "10" mbali imodzi ndikuvekedwa (kwa mulingo wa 10 mg).

Mapiritsi okhala ndi mawonekedwe, zokutidwa ndi filimu yoyera, ndi bevel (pamlingo wa 20 mg).

Mapiritsi okhala ndi mawonekedwe a Capsule okhala ndi biconvex pamwamba, wokutidwa ndi chovala choyera cha filimu (pamlingo wa 40 mg).

Mlingo ndi makonzedwe

Asanayambe kugwiritsa ntchito mankhwala osokoneza bongo, wodwalayo ayenera kukhala pa chakudya chokwanira komanso cholesterol yotsika ndikupitiliza kutsatira izi panthawi ya mankhwala. Mlingo wa mankhwalawa umayikidwa payekha, kutengera zolinga zamankhwala, momwe wodwalayo amayankhira chithandizo. Mulingo woyenera tsiku lililonse umachokera pa 5 mg mpaka 10 mg ndipo amatengedwa kamodzi patsiku. Mlingo womwewo ndi womwewo kwa odwala omwe akutenga ma statins nthawi yoyamba, kapena akusintha kuchokera ku chithandizo ndi HMG inhibitor yina, CoA reductase. Mukamasankha njira yoyambira, ndikofunikira kuganizira kuchuluka koyamba kwa cholesterol ndi chiopsezo cha mtima, komanso chiopsezo chokhala ndi mavuto.

Ngati ndi kotheka, mlingo utha kuwonjezeka pambuyo pa masabata anayi. Popeza kuchuluka kwawonjezereka kwa malipoti osagwirizana pakumatenga 40 mg poyerekeza ndi Mlingo wocheperako, kuchuluka kwa mlingo wa tsiku ndi tsiku mpaka 30 mg kapena 40 mg kuyenera kuganiziridwa kokha kwa odwala omwe ali ndi vuto lalikulu la mtima (makamaka hypercholesterolemia) , momwe sizingatheke kukwaniritsa milingo ya lipid mukamayamwa kwambiri, ndikuwunika. Kuchita chidwi ndi odwala ndikofunikira mukamayamba kumwa Mlingo wa 40 mg kapena 30 mg.

Kuchulukitsa kwa 40 mg kumatheka pokhapokha kuyang'aniridwa ndi dokotala. Mlingo wa 40 mg ndi osavomerezeka kwa odwala omwe sanamwe mankhwalawo. Pambuyo pa masabata a 2 a chithandizo komanso / kapena kuwonjezeka kwa mlingo wa Roxer, kuwunika kwa metabolidi ya lipid ndikofunikira (ngati pakufunika, kusintha kwa mlingo).

Roxera® imatha kutengedwa nthawi iliyonse masana, mosasamala chakudya.

Gwiritsani ntchito mwa okalamba

Odwala opitirira zaka 70 akulimbikitsidwa kuti ayambe kumwa mankhwalawa ndi 5 mg

Mlingo wa odwala ndi aimpso kulephera

Odwala omwe ali ndi vuto la aimpso wofatsa kapena wolimbitsa thupi, kusintha kwa mankhwalawa sikofunikira, mlingo woyenera wa mankhwala ndi 5 mg. Odwala omwe ali ndi vuto laimpso olimbitsa thupi (creatinine chilolezo chosakwana 60 ml / min) - kugwiritsa ntchito mankhwala mu 40 mg ndi kutsutsana. Odwala omwe amalephera kwambiri aimpso (creatinine chilolezo chochepera 30 ml / min), kugwiritsa ntchito Roxer ® kumatsutsana.

Mlingo wa odwala omwe ali ndi chiwindi

Odwala omwe ali ndi ana 7 kapena ochepera ana a Prag, kusintha kwa mankhwalawa sikofunikira. Palibe zokuchitikirani ndi kugwiritsa ntchito mankhwalawa kwa odwala omwe ali ndiopamwamba kuposa 9 pamlingo wa Mwana-Pugh.

Roxer ® imaphatikizidwa kwa odwala omwe ali ndi matenda a chiwindi.

Kuwonjezeka kwachilengedwe kwa rosuvastatin pakati pa Japan ndi China kwadziwika. Mlingo woyambira wodwala waku Asia ndi 5 mg. Kugwiritsa ntchito mankhwalawa pa 30 mg kapena 40 mg ndi contraindicated kwa odwala a ku Asia.

Mlingo wa odwala omwe ali ndi vuto la myopathy

Mlingo woyambira wa odwala omwe ali ndi vuto la myopathy ndi 5 mg. Mlingo wa 40 mg ndi 30 mg ndiwosokoneza mu odwala.