Mankhwala ochokera pagululi ma statins - wotsutsana naye wopikisana ndi molekyulu ya statin, amagwirizanitsidwa ndi gawo la receptor coenzyme A mwachindunji m'malo ophatikizika ndi enzyme iyi, ndipo gawo lake linaletsa kusintha hydroxymethylglutarate mu kupitilira, yomwe ndi yoyang'anira yaphatikizidwe ndi molekyulu cholesterol.

Kuyimitsa ntchito Kuchepetsa kwa CoA amachepetsa okhutira ndi zinthu zina cholesterol ndi kuchuluka kwachulukitsa pantchito LDL receptor, zomwe zimatsogolera kukwezedwa kwa catabolism cholesterol (Xc) LDL. Imakhala ndi kutengera kudalira Hypolipidemic kwenikweni. Mankhwalawa sasokoneza ntchito ya hepatitis / lipoprotein lipase ndi catabolism yamafuta acids.

Akorta ali ndi mphamvu pa endothelium ya mtima khoma (chizindikiro cha preclinical koyambirira atherosulinosis), imagwiranso magazi amitsempha yamagazi, imakhala ndi antiproliferative ndi antioxidant. Kuchuluka kwake kumawonetsedwa patatha masiku 30 chiyambireni mankhwalawa ndikukhazikika pambuyo pake pamlingo womwewo.

Pharmacokinetics

Mankhwala amaphatikizidwa bwino kuchokera kugaya chakudya. Kudya kumachepetsa mayamwidwe, bioavailability - pafupifupi 20%. TCmax imafikiridwa pambuyo - maola 3-5, kugonjetsa chotchinga. Kumangidwa kwakukulu kumapuloteni am magazi (90%). Limadziunjikira m'chiwindi, komwe limapukusidwa kuti N-dimethyl,lactone metabolites. Amamuchotsa m'thupi ndi ndowe zomwe zimapangidwa m'njira zosasinthika.

Zizindikiro zogwiritsidwa ntchito

• Monga chakudya chowonjezera cha hypertriglyceridemia ndi lipid-kutsitsa mankhwala,
• Panthawi yophatikizidwa hypercholesterolemia kapena woyamba hypercholesterolemia, pazovuta, kuphatikiza zakudya ndi njira zina zosagwiritsa ntchito mankhwala (zolimbitsa thupi, kuchepa thupi),
• Pofuna kuti muchepetse kukula atherosulinosis popanga mankhwala a anticholesterol,
• Pofuna kupewa zovuta zamtima mu kukhalapo kwa zinthu zomwe zingayambitse chitukuko Matenda a mtima wa Ischemic.

Contraindication

Kuwonongeka kwa chiwindi / impso, kukhudzidwa kwambiri ndi akorta, myopathynyere mimbaphwando cyclosporine, kuchepa kwa lactase, zaka zosakwana 18.

Gwiritsani ntchito mosamala odwala hypothyroidismpachiwopsezo cha chitukuko myopathies, mu nkhalamba, ochepa hypotensionosalamulirika khunyuwoledzera molumikizana ndi mafupandi kuvulala kambiri.

Malangizo a Akorta ogwiritsira ntchito (Njira ndi Mlingo)

Mankhwala ayenera kumwedwa motsutsana ndi maziko azakudya zomwe zimachepetsa lipid ndipo wodwalayo azitsatira nthawi yonse ya mankhwalawa. Mlingo wa Akorta umasankhidwa molingana ndi chandamale cha lipids komanso malingana ndi zolinga zamankhwala.

Mapiritsi a Acorta tikulimbikitsidwa kuti atenge gawo loyambirira la 10 mg 1 nthawi patsiku kuti athe kuchuluka kwake pakatha milungu 4 ngati kuli kofunikira mpaka 20 mg. Mukamamwa mapiritsi a Acorta, malangizo ogwiritsira ntchito akuwonetsa kufunikira koyang'anira kagayidwe ka lipid ndi kufunika kosintha kwa mlingo.

Kuchita

Kugwirizana kwa mankhwala ndi gemfibrozil kumawonjezera ndende rosuvastatin m'magazi 2. Kugwiritsira ntchito kwa Acort ndi njira yolerera pakamwa kumawonjezera AUC chindapusa ndi ethinyl estradiolzomwe ziyenera kuganiziridwa popanga chithandizo chamankhwala cha mahomoni.

Kuphatikiza kugwiritsa ntchito mankhwalawa erythromycin ukuwonjezeka ndi 20% AUC rosuvastatin. Kutenga ma fibrate ndipo nicotinic acid mu hypolipidemic Mlingo umachulukitsa myopathies. Phwando rosuvastatin ndi maantacidzomwe zikuphatikiza zotayidwa ndi magnesium hydroxideamachepetsa ndende rosuvastatin m'magazi ndi pafupifupi 50%. Chifukwa chake, tikulimbikitsidwa kumwa maantiacid osachepera maola 2 mutatha mapiritsi.

Kutulutsa mawonekedwe ndi kapangidwe kake

Acorta amapangidwa mwanjira ya mapiritsi okhala ndi mawonekedwe a filimu: kuchokera ku pinki kupita ku pinki, kuwala, kuzungulira, biconvex, panthawi yopuma - kuchokera ku kirimu mpaka loyera (ma PC 10. M'matumba, pamatumba okhala ndi zikwama za 1-3 mapepala).

Piritsi 1:

• Zogwira pophika: rosuvastatin - 10 kapena 20 mg (calcium ya rosuvastatin - 10,4 kapena 20.8 mg),
• Zothandiza monga (10/20 mg, motero): lactose monohydrate (shuga mkaka) - 89.5 / 179 mg, cellcrystalline cellulose - 29.82 / 59.64 mg, calcium hydrogen phosphate (E341) - 10.9 / 21.8 mg , crospovidone - 7.5 / 15 mg, magnesium stearate - 1.88 / 3.76 mg,
• Shell (10/20 mg, motero): Opadry II 30K240001 pinki (lactose monohydrate (shuga mkaka) - 2.4 / 4.8 mg, hydroxypropyl methylcellulose (hypromellose) - 1.68 / 3.36 mg, titanium dioxide - 1.413 / 2.826 mg, triacetin (glyceryl triacetate) - 0,48 / 0.96 mg, utoto wofiira wa ironide - 0,027 / 0,054 mg) - 6/12 mg.

Mlingo ndi makonzedwe

Mapiritsi a Acorta amatengedwa pakamwa, mosasamala chakudya, osambitsidwa ndi madzi. Nthawi ya tsiku la kumwa mankhwalawa sizikhudza kutha kwake. Piritsi ndi kutafuna mapiritsi siziyenera kukhala.

Akorta asanaikidwe, wodwalayo ayenera kuyamba kutsatira zakudya zomwe zimachepetsa lipid, zomwe zimayenera kutsatira nthawi yonse yamankhwala.

Dokotala amasankha mtundu wa rosuvastatin payekhapayekha. Zimatsimikiziridwa ndi cholinga cha mankhwala ndi mayankho othandizira, ndipo ziyeneranso kutsatiridwa ndi malingaliro omwe apezeka pakadali pano kuti azigwiritsa ntchito kwambiri.

Pokhapokha atawonetsedwa ndi dokotala, Aorta imatengedwa koyamba kwa 10 mg 1 nthawi patsiku. Posankha mtundu wa mankhwala a cholesterol, anthu aziganiziridwanso, komanso mwayi wokhala ndi zovuta za mtima ndi zovuta zina.

Pakatha mwezi, ngati kuli kotheka, kuchuluka kwowirikiza kawiri kwa mankhwalawa ndikotheka.

Kuwonjezeka kwina kwa tsiku ndi tsiku mlingo (mpaka 40 mg) kumawonetsedwa kwa odwala omwe ali ndi hypercholesterolemia kwambiri ndi chiopsezo cha zovuta zamtima (makamaka odwala omwe ali ndi achibale a hypercholesterolemia), omwe zotsatira zake zamankhwala sizinachitike mutamwa mapiritsi ochepa. Odwala otere ayenera kuyang'aniridwa ndi achipatala, amayeneranso kuwunikira zizindikiro za impso.

Odwala omwe sanakambirane ndi dokotala sanalimbikitsidwe kupereka Akorta pa 40 mg.

Pambuyo pa masabata 2-4 kuyambira pa chiyambi cha mankhwala, komanso ndi kuwonjezeka Mlingo, ndikofunikira kuwunika metabolidi ya lipid. Kutengera ndi zotsatira zake, kusankha kwa mankhwalawa kungasonyezedwe.

Kuwongolera kwa mlingo wa odwala okalamba sikofunikira.

Kuwonjezeka kwachilengedwe kwa rosuvastatin kudadziwika pakati pa China ndi Japan, komwe kuyenera kuganiziridwa popereka mankhwala.

Kwakukulu aimpso kulephera ndi contraindication kuti Akorta Mlingo uliwonse, zolimbitsa - tsiku lililonse 40 mg.

Kwa odwala omwe ali ndi genotypes c.521CC ndi c.421AA, tsiku lililonse mlingo wa Akorta suyenera kupitirira 20 mg.

Odwala omwe ali ndi vuto la chiwindi (maulendo oposa 9 pamakwerero a Mwana-Pugh), palibe chochitika ndi kugwiritsa ntchito mankhwalawa. Contraindication ku chithandizo cha mankhwala ndi matenda a chiwindi omwe amagwira ntchito.

Mulingo wambiri watsiku ndi tsiku wa 40 mg osavomerezeka ngati pali zinthu zina zomwe zingasonyeze kukonzekera kwa wodwala pakukula kwa myopathy.

Chiwopsezo cha myopathy (kuphatikizapo rhabdomyolysis) chikuwonjezeka ndi kuwonjezeka kwa plasma ndende ya rosuvastatin, kuphatikiza chifukwa cha kuphatikiza kwa acorta ndi mankhwala monga cyclosporine, ma protein ena a HIVasease (kuphatikizapo kugwiritsidwa ntchito kwa ritonavir ndi atazanavir, tipranavir ndi / kapena lopinavir). Ngati ndi kotheka, chithandizo chamankhwala chiyenera kukhazikitsidwa. Ngati mukufunika kugwiritsa ntchito Acorta ndi mankhwalawa nthawi imodzi, muyenera kukonza phindu lomwe likuyembekezeredwa ndikuwopsa.

Acorta mapiritsi 10 ndi 20 mg: malangizo ogwiritsira ntchito

Acorta ndi mankhwala omwe ali m'gulu la pharmacological lotchedwa statins. Nthawi zambiri, madokotala amauza anthu omwe ali ndi vuto la atherosulinosis kapena matenda aliwonse a lipid metabolism m'thupi. Mankhwalawa amapezeka ngati mapiritsi ang'onoang'ono okhala ndi filimu. Mtundu wa mapiritsiwo ukhoza kukhala mkati mwa mithunzi yonse ya pinki. Amakhala ozungulira, owongoka mbali zonse, ndipo akaphwanyidwa mkatimo, ndi oyera kapena beige.

Chofunikira chachikulu cha Akorta ndi rosuvastatin. Kuphatikiza pa rosuvastatin, kapangidwe kazinthu kameneka kamagwiritsira ntchito zinthu monga lactose, mapadi, calcium, magnesium, crospovidone. Kuphimba kwamafilimu kwamapiritsiwo kumakhala ndi lactose, hypromellose, titanium dioxide, triacetin ndi utoto womwe umakhala ngati chitsulo. Mapiritsi onse amapezeka mu phukusi lililonse la zidutswa 10.

Limagwirira ntchito

Akorta, kapena,, kaphatikizidwe kake kogwira, rosuvastatin, ndizosankha mosankha wina wa enzyme inayake - hydroxymethylglutaryl-coenzyme A reductase, yomwe m'njira yaying'ono imamveka ngati HMG-CoA. HMG-CoA ndi enzyme yofunika kwambiri yomwe imayang'anira kusintha kwa hydroxy-3-methylglutaryl-coenzyme A ku chinthu chotchedwa mevalonate, kapena mevalonic acid.

Mevalonate ndiwotsogola mwachindunji kwa cholesterol, kuchuluka kwake komwe ndi chiopsezo chachikulu cha atherosulinosis. Kuphatikizika kwa cholesterol ndi kusokonekera kwa otsika kachulukidwe lipoproteins (LDL) kumachitika m'chiwindi. Kuchokera apa zitha kunenedwa molondola kuti chiwindi ndicho chandamale kwambiri chochita ndi mankhwalawa.

Mankhwalawa amathandizira kukulitsa kuchuluka kwa zolandilira zam'mimba zowoneka bwino za maselo a chiwindi, zomwe zimapangitsa kuti zinthu zomwe zimawola chifukwa cha zinthu zawo zowola zisakulire, ndipo lipoproteins zaulere sizilowa m'magazi. Kuphatikiza apo, m'chiwindi, gulu lina la lipoproteins limapangidwanso - kachulukidwe kwambiri (VLDL). Ndi Akorta omwe amalepheretsa kaphatikizidwe kake ndipo amatsogolera kuchepa kwa mulingo wawo m'magazi a anthu.

Rosuvastatin amathandizira kuchepetsa kuchuluka kwa cholesterol yotsika komanso yotsika kwambiri, ndipo nthawi yomweyo imachulukitsa cholesterol "yabwino" - kuchokera ku HDL. Kuchuluka kwa cholesterol yathunthu, ma apolipoproteins B (koma, nawonso, kumawonjezera kuchuluka kwa apolipoproteins A), triglycerides imachepetsedwa kwambiri, kuchuluka kwa cholesterol ya "atherogenic" kwathunthu.

Njira iyi yochitira zinthu ikufotokoza zotsatira zazikulu za mankhwalawa - lipid-kutsitsa (kwenikweni - kuchepetsa kuchuluka kwa mafuta). Zotsatira zake mwachindunji zimatengera mlingo wa mankhwala omwe adokotala adapereka. Kuti mukwaniritse zochizira, ndiye kuti, mothandizidwa mokwanira, ndikofunikira kumwa mankhwalawo kwa sabata limodzi. Kuti mupeze chiwerengero chachikulu, "chodabwitsa", pafupifupi milungu inayi ya kudya pafupipafupi ndikukonzanso kwa mankhwalawo.

Kugwiritsa ntchito Akorta kumayenda bwino ndi mankhwala omwe amachokera ku pharmacological gulu la mankhwala opatsirana ndi lipid, komanso nicotinic acid, omwe amathandizira kukulitsa kuchuluka kwa lipoproteins yapamwamba.

Fomu ya Mlingo:

Piritsi lililonse lili ndi:
ntchito: calcium ya rosuvastatin - 10,4 mg kapena 20,8 mg (potengera zinthu zamadzimadzi, zomwe ndizofanana ndi zomwe zili mu rosuvastatin - 10,0 mg kapena 20.0 mg).
obwera:
Pakatikati:
Mlingo wa 10 mg - lactose monohydrate (mkaka wa shuga) 89.50 mg, microcrystalline cellulose 29.82 mg, calcium hydrogen phosphate (E 341) 10.90 mg, crospovidone 7.50 mg, magnesium stearate 1.88 mg,
Mlingo wa 20 mg - lactose monohydrate (mkaka wa shuga) 179,00 mg, microcrystalline cellulose 59.64 mg, calcium hydrogen phosphate (E 341) 21.80 mg, crospovidone 15.00 mg, magnesium stearate 3.76 mg.

Chigoba:
Mlingo wa 10 mg - OPADRAY II 30K240001 Pink (OPADRAY II 30K240001 Pink) Lactose monohydrate (mkaka wa shuga) 2.40 mg, hypromellose (hydroxypropyl methylcellulose) 1.68 mg, titanium dioxide 1.413 mg, triacetin (glyceryl triacetate) iron oxide red oxide 0,027 mg 6.00 mg,
Mlingo wa 20 mg - OPADRAY II 30K240001 Pink (OPADRAY II 30K240001 Pink) Lactose monohydrate (mkaka wa shuga) 4.80 mg, hypromellose (hydroxypropyl methylcellulose) 3,36 mg, titanium dioxide 2.826 mg, triacetin (glyceryl triacetate) iron oxide red oxide 0,054 mg 12.00 mg.

Mapiritsiwa ndi ophatikizidwa ndi film kuchokera ku pinki yopepuka mpaka pinki, yozungulira, ya biconvex. Pa yopuma kuyambira yoyera mpaka mtundu wa kirimu.

Malangizo ogwiritsira ntchito mankhwalawa

Aorta adalembedwa matenda osiyanasiyana a lipid metabolism.

Chizindikiro chachikulu ndicho kupezeka kwa atherosulinosis.

Mankhwala amagwiritsidwa ntchito ngati kuwonjezera pa zakudya kuti muchepetse mafuta m'thupi komanso otsika kwambiri.

Kuphatikiza pa izi, mankhwalawa amalembedwa:

• Monga wowonjezera prophylactic matenda a mtima dongosolo odwala popanda matenda zizindikiro za matenda a mtima. Izi zimaphatikizapo infernation ya myocardial, stroke, matenda oopsa. Pankhaniyi, zaka za odwala ndizofunika - kwa amuna ndi okulirapo kuposa zaka 50, ndipo kwa akazi opitilira 60. Ndikofunikanso kuganizira kuchuluka kochepa kwa matenda osalimba a lipoprotein cholesterol komanso kupezeka kwa matenda amtima wapachibale kwa abale ake enieni
• Hypercholesterolemia yoyamba malinga ndi Fredricksen kapena mtundu wosakanikirana ndikuwonjezereka kwa cholesterol popanda zifukwa zakunja. Mankhwala amatchulidwa ngati chida chowonjezera, makamaka ngati mankhwala ena, kudya ndi kuchita zolimbitsa thupi sikokwanira kukwaniritsa zotsatira zomwe mukufuna
• Mtundu wachinayi wa hypertriglyceridemia malinga ndi Fredricksen monga gawo lina lophatikiza ndi mankhwala othandizira.

Contraindication kuti agwiritse ntchito Akorty zimatengera mlingo wa mankhwalawa. Pa tsiku lililonse la 10 mpaka 20 mg, mayankho am'mimba, chiwindi matenda, kapena odwala omwe ali pachiwopsezo cha kukokomeza, amatsutsana, komwe kuyezetsa magazi kumafotokozedwa kuti kukuwonjezeka katatu kwa maselo a chiwindi poyerekeza ndi mfundo zapamwamba, gawo lovuta la kulephera kwa impso, matenda a hypersensitivity (lactose), kuchepa kwake kapena kuchepa kwa thupi, kupezeka kwa mbiri ya myopathy (kufooka kwa minofu), kudya kwa mankhwala ofanana ndi Cyclospor mu, mtundu wakubadwa kwa kukula kwa myopathy, nthawi ya pakati ndi mkaka wa m'mawere mwa akazi, msinkhu wawung'ono.

Pamene dort Akorta 40 mg patsiku, zotsatirazi contraindication ziyenera kuwonjezeredwa kwa contraindication pamwambapa:

1. Matenda a chithokomiro - hypothyroidism,
2. Kupezeka mu mbiri ya munthu kapena wachibale wa matenda amisempha yamatenda,
3. Kukula kwa myotoxicity mukamamwa mankhwala omwe ali ndi magawo ofanana,
4. Mowa wambiri,
5. Zinthu zilizonse zomwe zingayambitse kuchuluka kwa rosuvastatin mthupi,
6. Odwala a mtundu wa Mongoloid
7. Ntchito zophatikizika zophatikizika,

Kuphatikiza apo, chosemphana ndi kupezeka kwa thupi la wodwalayo kuzungulira mwamphamvu kwa aimpso.

Acorta Kutulutsa Fomu

Mankhwala amapezeka piritsi. Mawonekedwe a miyala ndi yozungulira, yolumikizana kuchokera mbali ziwiri. ngati phale laphwanyidwa pakati, ndiye kuti pakati pake padzakhala mtundu wa kirimu yoyera.

Chigoba cha mankhwalawo chimachokera ku pinki yopepuka mpaka yapinki yakuda mumtundu wake ndipo mtundu wa chipolopolo umatengera muyeso wa gawo lalikulu la piritsi. Mankhwala akupezeka ndi Mlingo wa rosuvastatin 10,0, 20,0 ndi mamililita 40.0.

Acorta mapiritsi okhala ndi 10 mg wa rosuvastatin:

Zothandiza piritsi ndi mapiritsi a rosuvastatin 10,0 mamililita:

The zikuchokera chipolopolo cha mankhwala Akorta ndi Mlingo wa rosuvastatin 10,0 mamilimita:

Mapiritsi okhala ndi mapiritsi a 10,10 milligram rosuvastatin m'matumba a mapiritsi 10:

• Makatoni okhala ndi malangizo omwe ali ndi matuza 1 (ma PC 10),
• Makatoni awiri matuza (ma PC 10) okhala ndi mawu,
• Makatoni okhala ndi malangizo ogwiritsira ntchito matuza atatu (ma PC 10),

Mapiritsi a pinki acorta cholesterol omwe ali ndi mulingo wa mamilimita 20.0:

Zothandiza piritsi ndi mapiritsi a rosuvastatin 20,0 mamililita:

The zikuchokera chipolopolo cha mankhwala Akorta ndi Mlingo wa rosuvastatin 20.0 mamilimita:

Mapiritsi okhala ndi mapiritsi a rosuvastatin 20,0 mamilimita m'matumba a mapiritsi 10:

• Makatoni okhala ndi malangizo omwe ali ndi matuza 1 (ma PC 10),
• Makatoni 2 matuza (ma PC 10.) Ndi mawu,
• Khadibhodi bokosi ndi malangizo okhala ndi matuza atatu (ma PC 10).

Akorta

Pharmacology

Chithandizo chophatikizidwa mu mankhwala a rosuvastatin ali ndi mphamvu zoletsa ntchito ya enzyme HMG-CoA reductase, ndikuchepetsa kupanga mevalonic acid, omwe amatsogolera kaphatikizidwe ka mamolekyulu a cholesterol m'magawo oyamba opanga maselo a chiwindi (hepatocytes).

Mothandizidwa ndi mankhwalawa, Akorta, kuchuluka kwa cholesterol yomwe imapangidwa imachepetsedwa, yomwe imayambitsa ma LDL receptors, omwe, akayamba kugwira ntchito, amayamba kusaka ma lipoproteins otsika kwambiri, amawagwira ndikuwabweza maselo a chiwindi kuti agwiritsenso ntchito ma asidi a bile.

Chifukwa cha ntchito iyi ya receptors, lipid catabolism imalimbikitsidwa, pali kuchepa kwakukulu kwa cholesterol yotsika kwambiri.

Njirayi imathandizira kuyeretsa magazi m'magazi kuchokera ku cholesterol yaulere.

Chofunikira kwambiri mu mankhwalawa, rosuvastatin amalepheretsa hepatocytes ndikuchepetsa kupanga kwawo ma lipids otsika kwambiri, omwe amachepetsa kaphatikizidwe ka triglycerides.

Mankhwalawa ali ndi kutanthauzira kwachulukidwe ka lipoproteins, kuchepetsa kapangidwe kake ndi maselo a chiwindi, omwe amachepetsa kwambiri kuchuluka kwa maselo olemera a lipoprotein m'magazi ndikuwonjezera kuchuluka kwa maselo osapindulitsa a lipoproteins.

Zotheka kukwaniritsa HMG-CoA reductase kuchokera ku mankhwala Akorta omwe ali ndi mulingo wa mamilimita 10.0 a rosuvastatin:

• Dongosolo lalikulu la cholesterol latsika ndi 36.0%,
• Kachigawo LDL kotsika ndi 52.0%,
• Gawo la triglyceride limachepetsedwa ndi 10,0%,
• Apolipoproteins B amatsika ndi 42.0%,
• Mamolekyulu a lipoproteins apamwamba kwambiri (HDL) amawonjezeka ndi 14.0%,
• Apolipoprotein A kuchuluka ndi 4.0%.

Zowonetsa za HMG-CoA reductase ya mankhwala Akorta ndi rosuvastatin 20 mg:

• Kutsika kwa cholesterol kokwanira ka 40.0%,
• Gawo latsika kwambiri la lipid (LDL) latsika ndi 55.0%,
• Gawo la ma triglyceride mamolekyulu amachepetsedwa ndi 23.0%,
• Apolipoproteins B amatsitsidwa ndi 46.0%,
• Pali kuchuluka kwamamolekyu apamwamba kwambiri (HDL) ndi 8.0%,
• Kuwonjezeka kwa apolipoprotein A ndi 5.0%.

Mphamvu ya lipid yotsitsa thupi ndi yofanana ndi mlingo womwe waperekedwa. Mankhwala achire othandizira akuwonjezeka mkati mwa masiku 7 atangoyamba kumene Acorta.

Pambuyo masiku 14, achire zotsatira zimatheka ndi 90.0%, zomwe zimatsimikizira kusanthula kwachembere popanga magazi a plasma okhala ndi mbiri ya lipid.

100.0% ya achire zotsatira zimapezeka mutamwa mapiritsi a Acorta pamwezi. Pambuyo pakufika pachimake ndikuchepetsa gawo la magawo ofunikira a cholesterol, mankhwala akupitilira kwa mwezi wina.

Gawo lochita rosuvastatin lakhala likuwoneka kuti lothandiza pochiza matenda am'banja komanso omwe siabanja, omwe ali ndi kuchuluka kwa triglycerides kapena opanda gawo lawo lokwera.

Ndiponso, Akorta ndiwothandiza pamitundu yonse iwiri ya matenda ashuga.

Mankhwala

Mankhwala
Rosuvastatin ndi mpikisano wosankha wa hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase, enzyme yomwe imatembenuza 3-hydroxy-3-methylglutaryl-CoA kukhala mevalonate, yomwe ili patsogolo pa cholesterol. Cholinga chachikulu cha ntchito ya rosuvastatin ndi chiwindi, pomwe kaphatikizidwe ka cholesterol (cholesterol) ndi katemera wa otsika kachulukidwe lipoproteins (LDL) amachitika. Rosuvastatin imakulitsa kuchuluka kwa zolandila za LDL pamtunda wa hepatocytes, ndikuwonjezera kukweza ndi chinyengo cha LDL. Zimalepheretsanso kaphatikizidwe kachulukidwe kakang'ono kwambiri ka lipoprotein cholesterol (VLDL) m'maselo a chiwindi, potero kuchepetsa kuchuluka kwa LDL ndi VLDL.
Rosuvastatin amachepetsa kuchuluka kwa cholesterol ya LDL, cholesterol yathunthu ndi triglycerides (TG), imakulitsa kuchuluka kwachulukidwe lipoprotein cholesterol (HDL-C), komanso kumachepetsa kuchuluka kwa cholesterol ya apolipoprotein B (ApoV), cholesterol yopanda HDL (kuchuluka kwa cholesterol yonse) ), Cholesterol-VLDL, TG-VLDL ndikuwonjezera kuchuluka kwa apolipoprotein A-I (ApoA-I). Rosuvastatin amachepetsa kuchuluka kwa cholesterol-LDL / cholesterol-HDL, cholesterol yathunthu / cholesterol-HDL, cholesterol-non-HDL / cholesterol-HDL ndi ApoV / ApoA-I.
Kuchulukitsa kwa lipid kumachitika mwachindunji molingana ndi kuchuluka kwa mlingo womwe umaperekedwa.
The achire zotsatira amakula mkati 1 sabata pambuyo chiyambi cha mankhwala, pambuyo 2 milungu ukufika 90% ya pazotheka kwambiri zotsatira, pazipita achire zotsatira zambiri zimachitika pambuyo 4 milungu ndipo amasungidwa ndi kupitiriza mankhwala.
Kugwiritsa ntchito odwala achikulire omwe ali ndi hypercholesterolemia ya kapena yopanda hypertriglyceridemia (mosasamala mtundu, jenda kapena zaka), kuphatikiza Odwala matenda a shuga komanso chizolowezi cha mabanja hypercholesterolemia.
Mphamvu yowonjezera imawonedwa limodzi ndi fenofibrate (mogwirizana ndi kuchepa kwa kuchuluka kwa TG) ndi nicotinic acid mu lipid kutsitsa Mlingo (woposa 1 g / tsiku) (pokhudzana ndi kuchuluka kwa kuchuluka kwa HDL cholesterol).

Pharmacokinetics
Mafuta: bioavailability mtheradi - 20%. Chakudya chimachepetsa kuyamwa. Nthawi yofika ndende yozizira kwambiri (TCmax) ndi maola 3-5 mutatha kumeza. Imalowa mkati mwa chotchinga chachikulu.
Kugawa: Rosuvastatin imagwidwa makamaka ndi chiwindi, komwe ndi malo a cholesterol synthesis ndi metabolism ya LDL-C. Kugawa voliyumu pafupifupi 134 l. Kuyankhulana ndi mapuloteni am'madzi am'magazi (makamaka ndi albumin) - 90%.
Kupenda: 10% ya mlingo wotengedwa umapukusidwa mu chiwindi. Rosuvastatin ndi gawo lopanda chapakati pazogwiritsa ntchito michere ya cytochrome P450. CYP2C9 ndiye isoenzyme yayikulu yomwe imagwira metabolism ya rosuvastatin, pomwe ma isoenzymes CYP2C19, CYP3A4, CYP2D6 sakukhudzidwa kwambiri ndi kagayidwe kake.
Kuposa 90% ya zochitika zamankhwala zoletsa kufalitsa kwa HMG-CoA reductase zimaperekedwa ndi rosuvastatin, zotsalazo ndi metabolites. Ma metabolites odziwika kwambiri a rosuvastatin ndi N-dismethyl ndi lactone metabolites. N-dismethyl ndi pafupifupi 50% yotsika kuposa rosuvastatin, lactone metabolites ndi pharmacologic yogwira.
Kuswana: yowonetsedwa makamaka mu mawonekedwe osasinthika (90%) kudzera m'matumbo (kuphatikitsanso rosuvastatin), ena onse - ndi impso. Hafu ya moyo (T½) ndi pafupifupi maola 19. Hafu ya moyo sasintha ndi kuchuluka kwa mankhwalawa. Kutengera kwa geometric kumatanthauza chilolezo cha plasma pafupifupi 50 l / h (kutalika kwa masinthidwe 21.7%). Monga ndi zina za HMG-CoA reductase inhibitors, kukonzekera kwa hepatic kwa rosuvastatin kumachitika pa cholesterol membrane transporter (mayendedwe a protein C a organic anions), omwe amathandiza kwambiri pakuchotsa kwa rosuvastatin.
Kuwonetsera kwadongosolo kwa rosuvastatin kumawonjezeka molingana ndi mlingo. Zosintha pama paracokinetic magawo omwe amagwiritsidwa ntchito tsiku ndi tsiku samayang'aniridwa.
Jenda ndi zaka sizikhala ndi vuto lalikulu pa pharmacokinetics ya rosuvastatin.
Kafukufuku wa Pharmacokinetic adawonetsa kuwonjezeka kuwirikiza kawiri mu AUC yapakati (dera lomwe likuyang'aniridwa ndi nthawi yayitali) ndi Cmax (kuchuluka kwa plasma concentration) ya rosuvastatin odwala a mafuko aku Asia (Japan, Chinese, Filipinos, Vietnamese and Koreans) poyerekeza ndi azungu, India odwala adawonetsa kuwonjezeka kwa Median AUC ndi Cmax mu 1, katatu. Kupenda kwa Pharmacokinetic sikunawonetse kusiyana kwakanema kochita kusokonekera pakati pa azungu ndi oyimilira a mtundu wakuda.
Odwala omwe amachepetsa kwambiri aimpso, kuchuluka kwa plasma kwa rosuvastatin kapena N-dysmethyl sikusintha kwambiri. Odwala omwe ali ndi vuto lalikulu la impso (creatinine chilolezo (CC)) Odwala omwe ali ndi vuto la chiwindi
Palibe zokuchitikirani ndi kugwiritsa ntchito mankhwalawa kwa odwala omwe ali ndiopamwamba kuposa 9 pamlingo wa Mwana-Pugh.
Ndi chisamaliro
Mankhwala tsiku lililonse mlingo wa 10 ndi 20 mg: chiopsezo cha myopathy / rhabdomyolysis - kulephera kwa impso, hypothyroidism, mbiri yaumwini kapena banja la matenda obadwa nawo a minofu komanso mbiri yakale yokhudza kupweteka kwa minyewa ndi mafupa ena a HMG-CoA reductase. Momwe mukuwonjezeka plasma ndende ya rosuvastatin, zaka zoposa 65, mbiri ya matenda a chiwindi, sepsis, ochepa hypotension, TWA, zoopsa, kagayidwe kachakudya kwambiri, endocrine kapena matenda electrolyte, kusalankhula khunyu, mpikisano (Mongoloid mtundu), concomitant ntchito fibrates.
Pa tsiku lililonse, 40 mg: kulephera kwa impso (CC oposa 60 ml / min), zaka zopitilira 65, mbiri ya matenda a chiwindi, sepsis, hypotension, opaleshoni yayikulu, zoopsa, metabolic yayikulu, endocrine kapena electrolyte zosokoneza kapena kulanda kosalamulirika.

Zisonyezo za mankhwala Akorta

Mankhwala Rosuvastatin Canon analamula kuti mankhwalawa amathandizanso kutsegula cholesterol index m'magazi:

• Mtundu woyambira wa heterozygous hypercholesterolemia woyamba (mtundu wa 2A malinga ndi Fredrickson),
• Hypercholesterolemia choyambirira si chidziwitso cha banja,
• Hyperlipidemia wosakanikirana (mtundu wa 2B malinga ndi Fredrickson), wogwira ntchito wa rosuvastatin amachita ngati cholumikizira ku cholesterol zakudya,
• Pathology ya dysbetalipoproteinemia (mtundu 3 malinga ndi Fredrickson),
• Etiology ya banja ya hypertriglyceridemia (Fredrickson mtundu 4),
• Ndi mtundu wa homozygous wa cholowa cholowa, umagwiritsidwa ntchito pakudya kapena ndi mankhwala ena a cholesterol. Kapena ngati zakudya za cholesterol sizigwira ntchito,
• Kuletsa kupitirira kwa systemic sclerosis, komanso kuphatikiza zakudya.

Kupewera koyambirira kwa zoterezi:

• Myocardial infaration
• Cerebral stroke cerebral infarction kapena matenda am'mimba,
• Cardiac organ ischemia,
• Ndi kusinthanso,
• Pambuyo pa zaka 50 mwa amuna ndi zaka 60 mwa akazi,
• Kuchepetsa kuphatikiza mapuloteni a C,
• Odwala omwe ali ndi chikonga komanso amamwa mowa,
• Ndi chitukuko cha matenda oopsa,
• Kupewa kosakhazikika kwa angina pectoris, komanso arrhythmias.

Chizindikiro pambuyo sitiroko

Zotsatira zoyipa

Zotsatira zoyipa za thupi zimagawidwa ndi pafupipafupi maphunziro azachipatala:

• Zokwanira kapena nthawi zambiri, izi ndizoposa 1 kwa odwala 10,
• Nthawi zambiri pamakhala vuto limodzi mwa odwala 100,
• Nthawi zambiri pamakhala vuto limodzi mwa odwala 1000,
• Pafupifupi vuto limodzi mwa odwala 10,000,
• Milandu yachilendo kwambiri kapena yokhayokha 1 yokhudza odwala oposa 10,000 omwe amamwa mankhwala a Acorta:

Tachycardia ndi chimodzi mwanjira zoyipa za kumwa mankhwalawa.

Mlingo wa Acorta ndi Ndondomeko Yoyang'anira

Malamulo a kumwa mankhwalawa chifukwa cha cholesterol yayitali:

• Kuyamba kwa mankhwala osokoneza bongo ndi mankhwala a Akorta kumayamba ndi chakudya cha hypocholesterol,
• Njira yonse yochizira ndi Acorta imayendera limodzi ndi chakudya,
• Mlingo wake umasankhidwa ndi dokotala payekha komanso mogwirizana ndi zomwe zikuwonetsedwa ndi milomo.
• Muyenera kumwa piritsi lonse osafuna kutafuna, komanso kumwa ndi madzi ambiri,
• Mlingo woyambirira wa Acorta ndi mamiligamu 10,0, kamodzi patsiku, osalumikizidwa pakudya.
• Onjezani mlingo kapena mankhwalawa, ndi adokotala okhawo omwe angakwanitse kugwiritsa ntchito analogue, koma osapitirira mwezi umodzi atalandira chithandizo,
• Mlingo wambiri patsiku ndi mamiligalamu 40.0, amangoikidwa kuchipatala moyang'aniridwa ndi achipatala nthawi zonse.
• Mlingo wokwanira umangoperekedwa kwa okhawo omwe ali ndi vuto lalikulu la atherosulinosis,
• Pogwiritsa ntchito mankhwala omwe ali ndi kuchuluka kwa mamiligalamu 20.0, yang'anani cholesterol index 2 kawiri pamwezi.
• Komanso, pamlingo wambiri patsiku, penyani mayendedwe a creatine phosphokinase,
• Odwala okalamba safuna kusintha kwa mlingo.

Mulingo waukulu wa mankhwala opezeka piritsi, umakhala wolakwika kwambiri mthupi kuchokera ku kayendetsedwe kake. Mlingo wa Akort wa mamiligalamu 40.0 umayambitsa mavuto ambiri, chifukwa chake muyenera kuyambitsa chithandizo chamankhwala ochepa.

Kwa odwala omwe ali pachiwopsezo chachikulu chotenga mtima, kapena ma pathologies a kayendedwe ka magazi, dokotalayo amatha kukupatsani mankhwala omwe ali ndi mamiligalamu 40.0, koma pokhapokha ngati mankhwala a Akorta kapena mawonekedwe ake omwe ali ndi Mlingo pansipa sanabweretse zotsatira za kuchepetsa mafuta a cholesterol .

Kuwonjezeka kwa mlingo wa mankhwalawa kumatha kuchitika pokhapokha ngati atapezeka ndi matenda a labid.

Kutengera ndi kuyesedwa kwa matenda, dokotala amasankha pakufunika kochulukitsa.

Mulingo waukulu wa mankhwala opezeka piritsi, umakhala wolakwika kwambiri pakumwa mankhwala

Kugwiritsa ntchito mankhwala Akort pa nthawi yapakati

Mankhwala a Akorta sakhazikitsidwa kwa azimayi munthawi yakubala, komanso nthawi yakudya mkaka wa m'mawere.

Amayi amisinkhu yobala panthawi ya mankhwala ndi mankhwala a group la statin ayenera kusamala kuteteza thupi lawo ku malingaliro osakonzekera a mwana.

Ngati mayi wapezeka kuti ali ndi pakati panthawi yomwe amamwa mankhwalawa Akorta, ndiye kuti muyenera kusokoneza mayendedwe ake ndi kuzindikira mayi ndi mwana yemwe sanabadwe.

Malangizo apadera pakusankhidwa kwake

Popereka mankhwala a 40.0 mg kwa odwala, kuwunika pafupipafupi kwa magawo a impso ndikofunikira. Ngati matendawa adawonetsa kuwonjezeka kokhazikika ka 5 mu index ya creatine phosphokinase, ndiye kuti patatha masiku 4 mpaka 5, muyenera kubwereza kuyesanso.

Ngati mutazindikira kuti matenda anu adawonekeranso ndi zotsatira zomwezo, ndiye kuti mankhwalawa omwe ali ndi milimita 40.0 ya Acorta sayenera kuyamba.

Ndikofunikanso kuletsa chithandizo ndi Acorta kwa minofu pathologies, ngati creatine phosphokinase imachulukanso nthawi 5 kapena kuposerapo.

Mulingo wambiri ukabwezeretsedwa ndipo kupweteka kwamisempha kumachepa, chithandizo chitha kuyambiranso, koma ndi mlingo wa Acorta wosaposa mamilimita 20.0. Chithandizo chofananira cha immunosuppressant chitha kuchitikanso.

Ndi kuchuluka kwa mankhwalawa panthawi ya mankhwala ndi Akorta mpaka muyeso waukulu, muziyang'anira ma index a lipid pogwiritsa ntchito mbiri ya lipid, komanso ma cell a chiwindi omwe amapezeka mu seramu.

Ngati wodwala ali ndi index ya glucose apamwamba kuposa 6.0 mmol pa lita imodzi, ndiye kuti chithandizo ndi Acorta chitha kupititsa patsogolo mtundu wachiwiri wa matenda ashuga.

Pa chithandizo, muyenera kuyang'anira shuga m'magazi nthawi zonse.

Mankhwala a Akorta ndi amtundu wa chibadwo chachinayi omwe ali ndi rosuvastatin yogwira, ndipo ali ndi fanizo lochulukirapo la Russia ndi akunja:

Mtengo wamankhwala a Akort ndi analogies

Pomaliza

Kugwiritsa ntchito mankhwala aku Russia kuti muchepetse cholesterol yamagazi kumatha kuikidwa ndi adokotala okha, ndi mlingo womwe wakhazikitsidwa ndi iye, ndipo mankhwalawo sayenera kusintha palokha. Maphunziro a mankhwalawa amaphatikizidwa ndi chakudya choyenera cha cholesterol.

Chithandizo chimachitidwa ndikuwunikira wodwala yemwe akupita komanso kuyesedwa kosalephera kwa cholesterol index.

Sergey, wazaka 54: Zaka 3 zapitazo ndidapezeka ndi atherosulinosis ya miyendo. Zakudyazo sizinachepetse cholesterol yanga, ndipo adotolo adandiuza ma statins. Ndinatenga Krestor kwa miyezi isanu ndi umodzi, koma kumwa mapiritsi awa nthawi zonse kumakhala kodula.

Adafunsa adotolo kuti asinthane ndi ma statin ena, ndipo adandiuza mankhwala a Akort. Ndine wokhutira ndi zotsatira zake, ndipo chifukwa cha mtengo omwe mankhwala aku Russia amandikomera.

Sindimakumana ndi zovuta zilizonse mthupi, kungoyambira pomwepo kudalibe mseru.

Galina, zaka 59: atayamba kusamba, cholesterol yanga imakulirakulira, ndipo ndinayamba kunenepa kwambiri.

Nditatha kudya ma hypocholesterol, ndinakwanitsa kuchepa thupi, koma cholesterol yanga sinatsike kwambiri. Dotolo adandiuza ine mankhwala a Akorta.

Pambuyo pakuthandizidwa miyezi iwiri, cholesterol idabweranso kwawamba, koma ndili pachakudya.

Gwiritsani ntchito pa nthawi yoyembekezera komanso nthawi yoyamwitsa

Mankhwala Akorta ali contraindicated kuti mugwiritse ntchito pa nthawi ya pakati komanso poyamwitsa. Amayi azaka zoyenera kubereka ayenera kugwiritsa ntchito njira zodalirika zakulera. Popeza cholesterol ndi zinthu zina za cholesterol biosynthesis ndizofunikira pakukula kwa fetus, chiwopsezo choteteza HMG-CoA reductase chimaposa zabwino za kugwiritsa ntchito mankhwalawa amayi apakati. Ngati muli ndi pakati pamankhwala, mankhwalawa amayenera kuyimitsidwa nthawi yomweyo. Palibe deta pakugawidwa kwa rosuvastatin mkaka wa m'mawere, chifukwa chake, panthawi yoyamwitsa, mankhwalawa ayenera kusiyidwa.

Mlingo ndi makonzedwe

Asanayambe mankhwala ndi mankhwalawa, wodwalayo ayenera kuyamba kutsatira zakudya zotsika za lipid ndikupitilizabe kutsatira panthawi ya chithandizo. Mlingo wa mankhwalawa amayenera kusankhidwa payekha kutengera zolinga zamankhwala ndi kuyankha, pozindikira zomwe zikuvomerezedwa masiku ano.
Mankhwala Akorta amatengedwa pakamwa, nthawi iliyonse masana, mosasamala chakudya, osafuna kutafuna kapena kupwanya piritsi, kumeza lonse, kumwa ndi madzi.
Mlingo woyambirira wololedwa (pokhapokha utafotokozeredwa mwanjira ina) ndi 10 mg kamodzi tsiku lililonse kwa odwala omwe sanatengere HMG-CoA reductase inhibitors, komanso kwa odwala omwe atumizidwa ku mankhwalawa atachira ndi ena a HMG-CoA reductase inhibitors.
Ngati ndi kotheka, mlingo umatha kuwonjezeka pambuyo pa masabata anayi mpaka 20 mg.
Chifukwa cha kutukuka kwa zoyipa mukamamwa mlingo wa 40 mg, poyerekeza ndi Mlingo wocheperako, kuwonjezereka kwa 40 mg kungachitike kokha mwa odwala omwe ali ndi hypercholesterolemia komanso chiopsezo cha zovuta zamtima (makamaka odwala a hypercholesterolemia ), momwe zotsatira za chithandizo sizinachitike mutamwa 20 mg, ndikuyang'aniridwa ndi achipatala.
Makamaka kuwunika mosamala odwala omwe akulandira mankhwalawa 40 mg akulimbikitsidwa. Mlingo wa 40 mg ndi osavomerezeka kwa odwala omwe sanakumaneko ndi dokotala. Pambuyo pamankhwala a 2-4 milungu komanso / kapena ndi kuchuluka kwa mankhwalawa, kuwunika kwa metabolidi ya lipid ndikofunikira (ngati pakufunika kutero, kusintha kwa mlingo kumafunika).
Odwala kumwa mankhwala 40 mg, tikulimbikitsidwa kuwunika ntchito za aimpso.
Mukamalemba gemfibrozil, mlingo wa rosuvastatin sayenera kupitilira 10 mg / tsiku.
Odwala okalamba safuna kusintha kwa mlingo.
Mukamaphunzira magawo a pharmacokinetic mwa odwala amitundu yosiyanasiyana, kuwonjezereka kwa dongosolo la rosuvastatin pakati pa Japan ndi China kudadziwika. Izi ziyenera kukumbukiridwa popereka rosuvastatin kwa magulu odwala. Kugwiritsa ntchito mankhwalawa 40 mg ndi kwa odwala a mtundu wa Mongoloid.
Odwala omwe ali ndi vuto la impso
Odwala omwe ali ndi vuto la aimpso wofatsa kapena pakati, kusintha sikofunikira. Kugwiritsa ntchito Mlingo uliwonse wa mankhwala Akorta ndi wothandizidwa ndi odwala kwambiri aimpso kulephera kwa creatinine kupitirira 30 ml / min.
Kugwiritsa ntchito mankhwala muyezo wa 40 mg wolekanitsa odwala omwe ali ndi vuto laimpso (creatinine chilolezo chosakwana 60 ml / min).
Odwala omwe ali ndi vuto la chiwindi
Palibe zokuchitikirani ndi kugwiritsa ntchito mankhwalawa kwa odwala omwe ali ndi manambala pamwamba pa 9 pamlingo wa Childe-Pugh. Mankhwala Akorta ali ophatikizika kwa odwala omwe ali ndi matenda a chiwindi omwe amagwira ntchito (kuphatikizapo kuwonjezereka kwa ntchito ya "chiwindi" transaminases, komanso kuwonjezeka kwa ntchito ya "chiwindi" transaminases mu seramu yamagazi koposa katatu poyerekeza ndi malire apamwamba).