Atorvastatin 40 mg - malangizo ogwiritsira ntchito

Atorvastatin 40 mg - mankhwala a lipid-otsitsa ku gulu la ma statins. Limagwirira ntchito ya mankhwala umalimbana kutsitsa cholesterol yamagazi

Piritsi limodzi lokhazikika mu filimu lili:

yogwira mankhwala: atorvastatin calcium calcium, malinga ndi atorvastatin) - 40.0 mg,
zotuluka: microcrystalline cellulose - 103.72 mg, calcium lactose - 100.00 mg, calcium carbonate - 20,00 mg, crospovidone - 15.00 mg, sodium carboxymethyl starch (sodium starch glycolate) - 9.00 mg, hyprolose (hydroxypropyl cellulose) - 6, .00 mg, magnesium stearate - 3.00 mg,
zokutira filimu: hypromellose - 4,500 mg, talc - 1,764 mg, hyprolysis (hydroxypropyl cellulose) - 1,746 mg, titanium dioxide - 0,990 mg kapena kusakaniza kowuma kwa zokutira filimu zokhala ndi hypromellose (50.0%), talc (19.6%), hyprolose (hydroxypropyl cellulose) (19.4%), titanium dioxide (11.0%) - 9,000 mg.

Mapiritsi ozungulira a biconvex, oyera-owoneka oyera kapena pafupifupi oyera. Gawo la mtanda la pakati ndi loyera kapena pafupifupi loyera.

Mankhwala

Atorvastatin ndi mpikisano wosankha wa HMG-CoA reductase, ma enzyme ofunikira omwe amasintha 3-hydroxy-3-methylglutaryl-CoA kukhala mevalonate, choyambirira kwa ma steroid, kuphatikiza cholesterol. Synthetic lipid-kutsitsa wothandizila.

Odwala omwe ali ndi homozygous ndi heterozygous mabanja a hypercholesterolemia, osakhala a mabanja a hypercholesterolemia ndi dyslipidemia wosakanikirana, atorvastatin amachepetsa kuchuluka kwa cholesterol (Ch) yamadzi am'magazi. low-density lipoprotein cholesterol (Cs-LDL) and apolipoprotein B (apo-B), komanso ndende ya lipoproteins yotsika kwambiri (Cs-VLDL) ndi triglycerides (TG), imayambitsa chiwopsezo cha kuchuluka kwambiri kwa milomo ya lipoproteins (Cs-HDL).

Atorvastatin amachepetsa kuchuluka kwa ma Chs ndi Chs-LHNP m'magazi am'magazi, kuletsa kuchepa kwa HMG-CoA ndi cholesterol kaphatikizidwe ka chiwindi ndikuwonjezera kuchuluka kwa "chiwindi" cholandilira cha LDL pamaselo a cell, zomwe zimapangitsa kukulira komanso kutengera kwa Chs-LDL.

Atorvastatin amachepetsa kupanga LDL-C ndi kuchuluka kwa tinthu tambiri ta LDL, timayambitsa kuwonjezereka kwa ntchito ya LDL-receptors kuphatikiza kusintha koyenera mu LDL-particles, komanso kumachepetsa kuyika kwa LDL-C mwa odwala omwe ali ndi homozygous cholowa chamagulu a hypercholesterolemia. amatanthauza.

Atorvastatin mu Mlingo kuyambira 10 mpaka 80 mg amachepetsa kuchuluka kwa ma Chs ndi 30-46%, Chs-LDL - mwa 41-61%, apo-B - ndi 34-50% ndi TG - mwa 14-33%. Zotsatira zamankhwala ndizofanana kwa odwala omwe ali ndi heterozygous Famer hypercholesterolemia, omwe siabanja mitundu ya hypercholesterolemia ndi hyperlipidemia kuphatikizapo mwa odwala matenda a shuga a 2.

Odwala okhala ndi okhazikika hypertriglyceridemia, atorvastatin amachepetsa kuchuluka kwa cholesterol yathunthu, Chs-LDL, Chs-VLDL, apo-B ndi TG ndikuwonjezera kuchuluka kwa Chs-HDL. Odwala omwe ali ndi dysbetalipoproteinsemia, atorvastatin amachepetsa kuchuluka kwa apakati-kachulukidwe lipoprotein cholesterol (Chs-STD).

Odwala omwe ali ndi mtundu wa IIa ndi IIb hyperlipoproteinemia malinga ndi gulu la Fredrickson, mtengo wowonjezereka wa kuchuluka kwa HDL-C munthawi ya chithandizo ndi atorvastatin (10-80 mg) poyerekeza ndi mtengo woyambira ndi 5.1-8.7% ndipo osadalira mlingo. Pali kuchepa kwakukulu kosadalira mlingo: cholesterol / Chs-HDL ndi Chs-LDL / Chs-HDL ndi 29-44% ndi 37-55%, motsatana.

Atorvastatin pa mlingo wa 80 mg kwambiri amachepetsa chiopsezo chotenga matenda a ischemic ndi kufa ndi 16% pambuyo pa maphunziro a sabata 16, ndi chiwopsezo chakugonekedwanso kuchipatala kwa angina pectoris limodzi ndi zizindikiro za myocardial ischemia ndi 26%. Odwala omwe ali ndi magawo osiyanasiyana oyambira a LDL-C (opanda ma wave a Q komanso kulowetsedwa kwa myocardial mwa amuna, akazi, komanso odwala ocheperako zaka 65), atorvastatin amachititsa kuchepa kwa chiwopsezo cha ischemic zovuta ndi kufa.

Kutsika kwa plasma mozungulira kwa LDL-C kumalumikizidwa bwino ndi mlingo wa atorvastatin kuposa ndende ya plasma. Mlingo amasankhidwa poganizira achire zotsatira (onani gawo "Mlingo ndi makonzedwe").

The achire zotsatira zimatheka patatha masabata awiri chiyambireni kuyambika kwa mankhwalawa, chimafika pakatha masabata 4 ndipo chimapitilira nthawi yonse ya chithandizo.

Zogulitsa

Atorvastatin imatengedwa mwachangu pambuyo pakukonzekera kwapakamwa: nthawi yoti ifike pazitsulo zambiri (TCmax) mu plasma yamagazi ndi maola 1-2. Mwa azimayi, kuchuluka kwambiri kwa atorvastatin (Cmax) ndi 20% kuposa, ndipo malo omwe ali munsi mwa ndende (AUC) ndi otsika 10% kuposa amuna. Mlingo wa mayamwidwe ndi ndende mu madzi am`magazi ukuwonjezeka mogwirizana ndi mlingo. Mtheradi wa bioavailability ndi pafupifupi 14%, ndipo dongosolo la bioavailability la zoletsa ntchito motsutsana ndi HMG-CoA reductase lili pafupifupi 30%. Kutsika kwachilengedwe kwa bioavailability kumachitika chifukwa cha kagayidwe kachakudya ka mucous membrane wa m'mimba ndipo / kapena pa "gawo lalikulu" kudzera m'chiwindi. Kudya pang'ono kumachepetsa kuchuluka ndi kuchuluka kwa mayamwidwe a atorvastatin (ndi 25% ndi 9%, motsatana, monga momwe zikuwonekera ndi zotsatira za kutsimikiza kwa Cmax ndi AUC), kuchepa kwa LDL-C kuli kofanana ndi pamene mukumwa atorvastatin pamimba yopanda kanthu. Ngakhale kuti atamwa atorvastatin madzulo, ndende yake ya plasma ndiyotsika (Cmax ndi AUC ndi 30%) kuposa atatha kumwa m'mawa, kuchepa kwa anthu omwe akukhudzidwa ndi LDL-C sikudalira nthawi yatsiku lomwe mankhwalawo amwedwa.

Kupenda

Atorvastatin imapangidwa mwamphamvu kuti apange ortho- ndi para-hydroxylated derivatives ndi zinthu zingapo za beta-oxidation. In vitro, ortho- ndi para-hydroxylated metabolites imalepheretsa kusintha kwa HMG-CoA, kufananizidwa ndi atorvastatin. Ntchito zoletsa kutsutsana ndi HMG-CoA reductase ndi pafupifupi 70% chifukwa cha zochita zama metabolites. Kafukufuku wa in vitro akuwonetsa kuti chiwindi isoenzyme CYP3A4 imachita mbali yofunika kwambiri pakukula kwa atorvastatin. Izi zikutsimikiziridwa ndikuwonjezereka kwa kuchuluka kwa atorvastatin m'madzi am'magazi a anthu pamene akutenga erythromycin, yomwe imalepheretsa iyi isoenzyme.

Kafukufuku wa in vitro awonetsanso kuti atorvastatin ndi choletsa chofooka cha CYP3A4 isoenzyme. Atorvastatin analibe gawo lalikulu pakukhudzidwa kwa plasma ndende ya terfenadine, yomwe imapangidwa makamaka ndi CYP3A4 isoenzyme, chifukwa chake, zovuta zake pa pharmacokinetics zamagawo ena a CYP3A4 isoenzyme ndiwonekere (onani gawo "Kuyanjana ndi mankhwala ena").

Atorvastatin ndi ma metabolites ake amachotseredwa ndi bile pambuyo pa hepatic ndi / kapena metabolism yowonjezera (atorvastatin sakhala ndikuchitika mobwerezabwereza kwambiri). Hafu ya moyo (T1 / 2) ili pafupifupi maola 14, pomwe mphamvu ya atorvastatin yokhudza HMG-CoA reductase ili pafupifupi 70% yotsimikizika ndi ntchito yozungulira metabolites ndipo imatha pafupifupi maola 20-30 chifukwa cha kupezeka kwawo. Mutamwa mankhwalawo mu mkodzo, zosakwana 2% ya mankhwala ovomerezeka amapezeka.

Zizindikiro zogwiritsidwa ntchito

Ngati chowonjezera pakudya kuti muchepetse cholesterol yokwanira, LDL-C, apo-B, ndi triglycerides kwa akulu, achinyamata, ndi ana azaka 10 kapena kuposerapo ndi hypercholesterolemia, kuphatikiza mabanja a hypercholesterolemia (heterozygous version) kapena kuphatikiza (kosakanikirana) Hyperlipidemia ( mitundu IIa ndi IIb malinga ndi gulu la Fredrickson), kuyankha pakudya ndi njira zina zosagwiritsa ntchito mankhwala sizili zokwanira,
Kuchepetsa cholesterol yokwanira, LDL-C mwa akuluakulu omwe ali ndi homozygous Famel hypercholesterolemia monga adjunct to lipid-lowering Therapies (mwachitsanzo LDL-apheresis) kapena, ngati chithandizo chotere sichikupezeka,

Kuteteza Matenda a Mtima:

kupewa zochitika zamtima mu mtima mwa odwala omwe ali pachiwopsezo chachikulu chokhala ndi zochitika zamkati pamtima, kuwonjezera pa kukonza ziwopsezo zina.
kupewa kwachiwiri kwamatenda amtima mwa odwala omwe ali ndi matenda amtima kuti achepetse chiwerengero cha anthu omwalira, matenda amitsempha yam'mimba, sitiroko, kuyambiranso kuchipatala kwa angina pectoris ndi kufunika kosinthanso.

Contraindication

Zoyipa zotsutsana ndi atorvastatin ndi:

Hypersensitivity kuti atorvastatin ndi / kapena chilichonse cha mankhwala,
matenda a chiwindi kapena kuchuluka kwa “chiwindi” transaminases mu madzi am'magazi osadziwika kophatikiza katatu poyerekeza ndi malire apamwamba.
matenda a chiwindi chilichonse etiology,
ntchito kwa akazi amsinkhu wobereka omwe sagwiritsa ntchito njira zokwanira zakulera,
ntchito limodzi ndi fusidic acid,
zaka mpaka zaka 10 - kwa odwala omwe ali ndi heterozygous Famer hypercholesterolemia,
zaka mpaka zaka 18 zikagwiritsidwa ntchito molingana ndi zowonetsera zina (kuthekera ndi chitetezo cha ntchito sizinakhazikitsidwe),
mimba, yoyamwitsa
lactose tsankho, kufupika kwa lactase, shuga-galactose malabsorption.

Atorvastatin atha kupatsidwa mwayi wopita kwa mayi wazaka zakubadwa pokhapokha atadziwika kuti sanakhale woyembekezera komanso kudziwitsidwa za kuwopsa kwa mankhwalawa kwa mwana wosabadwayo.

Mochenjera: kumwa mowa mwauchidakwa, mbiri ya matenda a chiwindi, odwala omwe ali pachiwopsezo cha rhabdomyolysis (kuwonongeka kwa impso, hypothyroidism, cholowa chamkati mwa odwala omwe ali ndi mbiri kapena mbiri yakale, zotsatira zoyipa za HMG reductase inhibitors kapena fibrate pamisempha kale minofu, zaka zopitilira 70, kugwiritsa ntchito munthawi yomweyo mankhwala osokoneza bongo omwe amawonjezera chiopsezo cha myopathy ndi rhabdomyolysis

Mlingo ndi makonzedwe

Mkati. Tengani nthawi iliyonse masana, ngakhale kudya kwambiri.

Musanayambe chithandizo ndi Atorvastatin, muyenera kuyesa kuthana ndi vuto la hypercholesterolemia pogwiritsa ntchito zakudya, masewera olimbitsa thupi komanso kuchepa thupi kwa odwala omwe ali ndi kunenepa kwambiri, komanso chithandizo cha matenda oyambitsidwa.

Popereka mankhwala, wodwalayo ayenera kuvomereza kuti azidya zakudya zaposachedwa za hypocholesterolemic, zomwe ayenera kutsatira nthawi yonse ya chithandizo.

Mlingo wa mankhwalawa umasiyana kuchokera ku 10 mg mpaka 80 mg kamodzi patsiku ndipo umapatsidwa gawo la mankhwala a LDL-Xc, cholinga cha mankhwalawo komanso momwe munthu amathandizira pa mankhwalawo. Mlingo wapamwamba tsiku lililonse wa mankhwala ndi 80 mg.

Kumayambiriro kwa mankhwalawa komanso / kapena pakuwonjezeka kwa mlingo wa Atorvastatin, ndikofunikira kuyang'anira kuchuluka kwa lipids m'magazi am'magazi aliwonse a 2-4 ndikusintha mlingo moyenerera.

Heterozygous achibale hypercholesterolemia

Mlingo woyambirira ndi 10 mg patsiku. Mlingo uyenera kusankhidwa payekhapayekha ndikuwunikira kufunikira kwake sabata iliyonse 4 ndikuwonjezereka kwa 40 mg patsiku. Ndiye kuti mankhwalawa atha kuwonjezeka mpaka kufika pa 80 mg patsiku, kapenanso kuphatikiza kwa mitundu ya asidi ya bile pogwiritsa ntchito atorvastatin muyezo wa 40 mg patsiku ndikotheka.

Gwiritsani ntchito ana ndi achinyamata kuyambira zaka 10 mpaka 18 ndi heterozygous achibale hypercholesterolemia

Mlingo woyambira wabwino ndi 10 mg kamodzi patsiku. Mlingo utha kuwonjezeka mpaka 20 mg patsiku, kutengera zovuta zamatenda. Zochitika ndi mlingo wopitilira 20 mg (wofanana ndi 0,5 mg / kg) ndizochepa. M'pofunika titrate mlingo wa mankhwalawa kutengera cholinga lipid-kutsitsa mankhwala. Kusintha kwa Mlingo kuyenera kuchitika mosiyanasiyana nthawi 1 m'milungu inayi kapena kupitilira.

Gwiritsani ntchito limodzi ndi mankhwala ena

Ngati ndi kotheka, munthawi yomweyo kugwiritsa ntchito cyclosporine, telaprevir kapena kuphatikiza kwa tipranavir / ritonavir, mlingo wa mankhwala Atorvastatin sayenera upambana 10 mg patsiku.

Muyenera kusamala ndikuwonetsetsa kuti mankhwala ochepetsa mphamvu ya atorvastatin azigwiritsidwa ntchito pamene akugwiritsidwa ntchito ndi kachilombo ka HIV proteinase inhibitors, hepatitis C virusaseaseasease inhibitors (boceprevir), clarithromycin ndi itraconazole.

Zotsatira zoyipa

Mukamamwa Atorvastatin, zotsatirazi mavuto zimachitika:

Kuchokera kwamanjenje: kugona, mutu, asthenic syndrome, malaise, chizungulire, zotumphukira zamitsempha, amnesia, paresthesia, Hypesthesia, kupsinjika.
Kuchokera pamimba: kukhumudwa, kutsegula m'mimba, kupweteka kwam'mimba, kukomoka, kugona, kudzimbidwa, kusanza, matenda a chiwindi, hepatitis, kapamba, cholestatic jaundice.
Kuchokera ku minculoskeletal system: myalgia, kupweteka kwa msana, arthralgia, minofu kukokana, myositis, myopathy, rhabdomyolysis.
Zotsatira zoyipa: urticaria, pruritus, zotupa pakhungu, zotupa zamkati, anaphylaxis, polymorphic exudative erythema (kuphatikizapo Stevens-Johnson syndrome), matenda a Laille.
Kuchokera ku ziwalo za hemopoietic: thrombocytopenia.
Kuchokera kumbali ya kagayidwe: hypo- kapena hyperglycemia, kuchuluka kwa seramu CPK.
Kuchokera ku endocrine system: shuga mellitus - pafupipafupi kukula kumadalira kukhalapo kapena kusapezeka kwa zinthu zoopsa (kusala glucose ≥ 5.6, index mass body> 30 kg / m2, kuchuluka kwa triglycerides, mbiri ya matenda oopsa).
Zina: tinnitus, kutopa, kusokonezeka kwa kugonana, zotumphukira, kuchuluka kwa thupi, kupweteka pachifuwa, kuchepa kwa magazi, matenda am'mimba, makamaka ndi kugwiritsidwa ntchito kwa nthawi yayitali, matenda a hemorrhagic (atagwiritsiridwa ntchito Mlingo wambiri komanso CYP3A4 inhibitors) kulephera.

Zizindikiro zochuluka

Zizindikiro zapadera za bongo sizinakhazikitsidwe. Zizindikiro zimatha kuphatikizira kupweteka m'chiwindi, kulephera kwaimpso, kugwiritsa ntchito nthawi yayitali kwa myopathy ndi rhabdomyolysis.

Pankhani ya mankhwala osokoneza bongo, njira zotsatirazi ndizofunikira: kuwunikira ndikusamalira ntchito zofunikira za thupi, komanso kupewa kuyamwa kwa mankhwalawa (gastric lavage, kumwa makala oyambitsa kapena mankhwala oletsa).

Ndi kukula kwa myopathy, kutsatira rhabdomyolysis ndi pachimake aimpso kulephera, mankhwalawa ayenera kuthetsedwa ndipo kulowetsedwa kwa diuretic ndi sodium bicarbonate kunayamba. Rhabdomyolysis ikhoza kuyambitsa hyperkalemia, yomwe imafuna kukhazikika kwa njira ya calcium chloride kapena yankho la calcium gluconate, kulowetsedwa kwa 5% yankho la bingu (glucose) ndi insulin, komanso kugwiritsa ntchito ma resini a potaziyamu.

Popeza mankhwalawa amamangika kumapuloteni a plasma, hemodialysis siyothandiza.

Mlingo

Mapiritsi Ovomerezeka 10 mg, 20 mg ndi 40 mg

Piritsi limodzi lili:

ntchito yogwira - atorvastatin (monga calcium calcium ya trihydrate) 10 mg, 20 mg ndi 40 mg (10.85 mg, 21.70 mg ndi 43.40 mg),

zokopa: calcium carbonate, crospovidone, sodium lauryl sulfate, silicon dioxide, colloidal anhydrous, talc, microcrystalline cellulose,

kapangidwe ka chipolopolo: Opadry II pink (talc, polyethylene glycol, titanium dioxide (E171), mowa wa polyvinyl, chitsulo (III) oxide chikasu (E172), chitsulo (III) oxide ofiira (E172), iron (III) oxide wakuda (E172).

Mapiritsi okhala ndi pinki okhala ndi biconvex pamwamba

Mankhwala

Pharmacokinetics

Atorvastatin imalowa mwachangu pambuyo pakukonzekera kwa pakamwa, ndende yake ya plasma imafika pamlingo wambiri kwa maola 1 - 2. Mgwirizano wa bioavailability wa atorvastatin ndi 95-99%, mtheradi - 12-14%, systemic (wopereka choletsa cha HMG-CoA reductase) - pafupifupi 30 % Kuphatikiza kwachilengedwe kwachilengedwe kumafotokozedwa ndi kutsimikizika kwachulukidwe kamkati ka mucous membrane wam'mimba ndi / kapena metabolism pakadutsa gawo loyambirira kudzera pachiwindi. Mafuta ndi plasma ndende ukuwonjezeka mogwirizana ndi mlingo wa mankhwalawa. Ngakhale kuti akudya ndi chakudya, mayamwidwe amachepetsa (kuchuluka kwa ndende ndi AUC kuli pafupifupi 25 ndi 9%, motero), kutsika kwa cholesterol LDL sikudalira atorvastatin wotengedwa ndi chakudya kapena ayi. Mukamamwa atorvastatin madzulo, ndende yake ya plasma inali yotsika (pafupifupi 30% chifukwa cha kuchuluka kwa ndende ndi AUC) kuposa m'mene mumamwa m'mawa. Komabe, kutsika kwa cholesterol ya LDL sikudalira nthawi yomwe mumwa mankhwalawa.

Kuposa 98% ya mankhwalawa amamangidwa kumapuloteni a plasma. Chiwerengero cha erythrocyte / plasma ndi pafupifupi 0,25, chomwe chimawonetsera kufooka kwa mankhwalawo m'maselo ofiira a magazi.

Atorvastatin imapangidwa kuti itulutsidwe kwa ortho- ndi para-hydroxylated ndi zinthu zosiyanasiyana za beta-oxidised. Mphamvu yoletsa mphamvu ya wachibale wa HMG-CoA reductase pafupifupi 70% imazindikira chifukwa cha zochita za metabolites. Atorvastatin anapezeka kuti ndi choletsa chofooka cha cytochrome P450 ZA4.

Atorvastatin ndi ma metabolites ake amachotsedwa makamaka ndi bile pambuyo pa hepatic ndi / kapena metabolism yowonjezera. Komabe, mankhwalawa sangatengeke pakuwonjezeranso kwina. Hafu yapakati ya moyo wa atorvastatin ndi pafupifupi maola 14, koma nthawi ya inhibitory zochita motsutsana ndi HMG-CoA reductase chifukwa chozungulira yogwira metabolites ndi maola 20-30. Pasanathe 2% ya mlingo wapakamwa wa atorvastatin amamuchotsa mkodzo.

Kuchulukitsidwa kwa plasma kwa atorvastatin mwa okalamba athanzi (wopitilira 65) ndiwokwera kwambiri (pafupifupi 40% ya ndende yayikulu ndi 30% kwa AUC) kuposa mwa achinyamata. Panalibe kusiyanasiyana pakuyenda bwino kwa mankhwalawa ndi atorvastatin mwa odwala okalamba komanso odwala a mibadwo ina.

Kuchulukitsidwa kwa atorvastatin m'madzi am'magazi mwa akazi kumasiyana ndi kuchuluka kwa madzi am'magazi mwa amuna (mwa akazi, kuchuluka kwakukulu kumakhala pafupifupi 20%, ndi AUC - 10% kutsika). Komabe, palibe kusiyana kwakukulu kachipatala komwe kumapezeka chifukwa cha kuchuluka kwa lipid mwa amuna ndi akazi.

Matenda a impso sasokoneza kukhudzana kwa mankhwalawa mu plasma kapena kuchuluka kwa atorvastatin pazambiri za lipid, motero palibe chifukwa chosinthira kwa odwala omwe ali ndi vuto la aimpso. Maphunzirowa sanakhudze odwala omwe amalephera-a-impso kulephera; mwina, hemodialysis sasintha kwambiri kuwonekera kwa atorvastatin, popeza mankhwalawa ali pafupifupi onse pama protein a plasma a magazi.

The kuchuluka kwa atorvastatin mu madzi am`magazi kumawonjezera kwambiri (pazipita ndende - pafupifupi 16 zina, AUC - 11 zina) mwa odwala cirrhosis chiwindi cha uchidakwa etiology.

Mankhwala

Atorvastatin ndi mpikisano wosankha wa HMG-CoA reductase-enzyme, yomwe imayang'anira kuchuluka kwa kusintha kwa HMG-CoA kukhala mevalonate - kalozera wa ma sterols (kuphatikiza cholesterol (cholesterol)). Odwala omwe ali ndi homozygous ndi heterozygous Famer hypercholesterolemia, cholowa monga hypercholesterolemia ndi dyslipidemia, atorvastatin amachepetsa kuchuluka kwa cholesterol, otsika kachulukidwe lipoproteins (LDL) ndi apolipoprotein B (Apo B). Atorvastatin amachepetsa ndende yotsika kwambiri ya lipoproteins (VLDL) ndi triglycerides (TG), komanso imachulukitsa pang'ono zomwe zimakhala ndi cholesterol high density lipoproteins (HDL).

Atorvastatin amachepetsa kuchuluka kwa cholesterol ndi lipoproteins m'magazi a magazi poletsa HMG-CoA reductase, kaphatikizidwe ka cholesterol m'chiwindi ndikuwonjezera kuchuluka kwa zolandilira za LDL pamtunda wa hepatocytes, womwe umatsatiridwa ndi kuwonjezeka ndi kutengera kwa LDL. Atorvastatin imachepetsa kupanga kwa LDL, imayambitsa kuwonjezeredwa kosatha ndi kosatha kwa ntchito ya LDL receptor. Atorvastatin bwino amachepetsa milingo ya LDL odwala omwe ali ndi homozygous Famer hypercholesterolemia, yomwe singagwiritsidwe ntchito moyenera ngati mankhwala a lipid amatsitsa.

Malo oyamba a atorvastatin ndi chiwindi, chomwe chimagwira gawo lalikulu pakuphatikizidwa kwa cholesterol ndi chilolezo cha LDL. Kutsika kwa cholesterol ya LDL kumalumikizana ndi mlingo wa mankhwalawo komanso kugwiritsidwa ntchito kwake mthupi.

Atorvastatin pa mlingo wa 10-80 mg adachepetsa cholesterol yathunthu (pofika 30-46%), LDL cholesterol (pofika 41-61%), Apo B (pofika 34-50%) ndi TG (mwa 14-33%). Zotsatira zake ndizokhazikika kwa odwala omwe ali ndi heterozygous Famer hypercholesterolemia, mtundu wopezeka wa hypercholesterolemia komanso mtundu wosakanikirana wa hyperlipidemia, kuphatikiza odwala omwe samadwala matenda a shuga.

Odwala omwe ali ndi hypertriglyceridemia yokhayokha, atorvastatin amachepetsa kuchuluka kwa cholesterol, LDL cholesterol, VLDL cholesterol, Apo B, TG ndipo kumawonjezera pang'ono mulingo wa cholesterol ya HDL. Odwala omwe ali ndi dysbetalipoproteinemia, atorvastatin amachepetsa chiwindi chomwe chimachepetsa chiwindi.

Odwala omwe ali ndi mtundu wa IIa ndi IIb hyperlipoproteinemia (malinga ndi gulu la Fredrickson), kuchuluka kwapakati pa HDL cholesterol mukamagwiritsa ntchito atorvastatin pa 10-80 mg anali 5.1-8.7% mosasamala. Kuphatikiza apo, panali kuchepa kwakukulu kwakukulu kokhazikika kwa kuchuluka kwa cholesterol / HDL cholesterol ndi HDL cholesterol. Kugwiritsidwa ntchito kwa atorvastatin kumachepetsa chiopsezo cha ischemia ndi kufa kwa odwala omwe ali ndi myocardial infarction popanda Q wave ndi osakhazikika a angina (mosaganizira jenda ndi zaka) ndizofanana molingana ndi mulingo wa cholesterol ya LDL.

Heterozygous zokhudzana ndi hypercholesterolemia mu ana. Mwa anyamata ndi atsikana azaka zapakati pa 10 mpaka 17 ndi heterozygous Famer hypercholesterolemia, kapena hypercholesterolemia, atorvastatin pa mlingo wa 10-20 mg kamodzi patsiku anachepetsa kwambiri cholesterol, LDL cholesterol, TG ndi Apo B m'madzi am'magazi. Komabe, sizinakhudze kwambiri kukula ndi kutha kwa anyamata kapena kutalika kwa msambo kwa atsikana. Chitetezo ndi mphamvu ya Mlingo pamwambapa 20 mg pa mankhwala a ana sichinaphunzire. Mphamvu ya kutalika kwa mankhwala a atorvastatin muubwana pakuchepetsa kuchepa kwa thupi ndi kufa muukalamba sichinakhazikitsidwe.

Mlingo ndi makonzedwe

Musanayambe mankhwala a Atorvastatin, ndikofunikira kudziwa kuchuluka kwa cholesterol m'magazi motsutsana ndi zakudya zoyenera, perekani mankhwala olimbitsa thupi ndikuchita zinthu zofunikira kuchepetsa thupi mwa odwala omwe ali ndi kunenepa kwambiri, komanso kuchitira chithandizo chamatenda oyamba. Pa mankhwala ndi atorvastatin, odwala ayenera kutsatira muyezo hypocholesterolemic zakudya. Mankhwala ndi mankhwala 10 mg wa 80 patsiku kamodzi, tsiku lililonse, koma nthawi yomweyo patsiku, kaya kudya. Mlingo woyambira ndi wokonza ukhoza kupangidwa molingana ndi gawo loyambirira la cholesterol ya LDL, zolinga ndi magwiridwe antchito. Pambuyo pa masabata 2-4 kuyambira pa chiyambi cha chithandizo ndi / kapena kusintha kwa mankhwala ndi Atorvastatin, mbiri ya lipid iyenera kutengedwa ndi kusintha kwa mankhwalawo.

Hypercholesterolemia yoyamba komanso yophatikiza (yophatikizika) hyperlipidemia. Nthawi zambiri, ndikokwanira kupereka mankhwala mu 10 mg kamodzi patsiku. Mphamvu ya mankhwalawa imayamba pambuyo pa masabata awiri, ndipo zotsatira zake zimakhala - pambuyo pa masabata anayi. Kusintha koyenera kumathandizidwa ndi kugwiritsa ntchito mankhwalawa kwa nthawi yayitali.

Homozygous achibale hypercholesterolemia. Mankhwala ndi mankhwala 10 mg mpaka 80 pa tsiku tsiku lililonse, nthawi iliyonse, ngakhale kudya zakudya. Mlingo woyambira ndi kukonza umayikidwa payekhapayekha. Nthawi zambiri, odwala omwe ali ndi homozygous Famer hypercholesterolemia, zotsatira zake zimachitika pogwiritsa ntchito Atorvastatin pa mlingo wa 80 mg kamodzi patsiku.

Heterozygous achibale hypercholesterolemia mu ana (odwala a zaka 10 mpaka 17). Atorvastatin tikulimbikitsidwa koyamba mlingo.

10 mg kamodzi pa tsiku tsiku lililonse. Mlingo woyenera kwambiri ndi 20 mg kamodzi patsiku tsiku lililonse (Mlingo wopitilira 20 mg usanaphunzire mwa odwala a m'badwo uno). Mlingo umayikidwa payekhapayekha, poganizira cholinga cha mankhwala, mankhwalawa amatha kusintha pakadutsa milungu inayi kapena kupitirira apo.

Gwiritsani ntchito odwala omwe ali ndi matenda a impso komanso aimpso kulephera. Matenda a impso sasokoneza kukhudzana kwa atorvastatin kapena kuchepa kwa plasma LDL cholesterol, motero palibe chifukwa chosinthira mlingo.

Gwiritsani ntchito odwala okalamba. Palibe kusiyana pakukhwimitsa chitetezo ndikugwiritsidwa ntchito kwa mankhwalawa pochiza hypercholesterolemia mwa odwala okalamba komanso odwala omwe ali ndi zaka 60.

Odwala omwe ali ndi vuto la chiwindi Mankhwala amakonzedwa mosamala pokhudzana ndi kutsika kwake pakuchotsa mankhwalawa m'thupi. Kuwongolera kwa magawo azachipatala ndi a labotale akuwonetsedwa, ndipo ngati kusintha kwakukuru m'maganizo kwapezeka, mlingo uyenera kuchepetsedwa kapena chithandizo chikuyenera kuyimitsidwa.

Ngati lingaliro lipangidwe pa mgwirizano wa Atorvastatin ndi CYP3A4 zoletsa, ndiye:

Nthawi zonse yambani kulandira mankhwala osachepera 10 mg, onetsetsani kuti mumayang'anira ma seramu lipids musanayambe kumwa mankhwala.

Mutha kusiya kwakanthawi kutenga Atorvastatin ngati zoletsa za CYP3A4 zikuyendetsedwa mwachidule (mwachitsanzo, kanthawi kochepa ka mankhwala othandizira monga clarithromycin).

Malangizo okhudza mlingo waukulu wa Atorvastatin mukamagwiritsa ntchito:

ndi cyclosporine - mlingo sayenera upambana 10 mg,

ndi clarithromycin - mlingo sayenera upambana 20 mg,

ndi itraconazole - mlingo sayenera upambana 40 mg.

Zochita zamankhwala osokoneza bongo

Chiwopsezo cha myopathy chikuwonjezereka panthawi yamankhwala ndimankhwala ena a gululi pomwe ntchito cyclosporine, zotumphukira za fibric acid, erythromycin, antifungals zokhudzana ndi azoles, ndi nicotinic acid.

Maantacid okhala: munthawi yomweyo kuyamwa kwa kuyimitsidwa komwe kuli ndi magnesium ndi aluminium hydroxide kunachepetsa kuchuluka kwa atorvastatin m'madzi am'magazi ndi pafupifupi 35%, komabe, kuchepa kwa cholesterol ya LDL sikunasinthe.

Antipyrine: Atorvastatin sichikhudza pharmacokinetics ya antipyrine, chifukwa chake, kulumikizana ndi mankhwala ena omwe amapangidwa ndi cytochrome isoenzymes yomweyo sayembekezereka.

Amlodipine: mu kuphunzira kwa kuyanjana kwa mankhwala kwa anthu athanzi, munthawi yomweyo makonzedwe a atorvastatin pa mlingo wa 80 mg ndi amlodipine pa 10 mg kunapangitsa kuwonjezeka kwa zotsatira za atorvastatin ndi 18%, zomwe sizinali zofunikira kwambiri pakuchipatala.

Gemfibrozil: chifukwa chowonjezera chiopsezo chotenga myopathy / rhabdomyolysis ndi kugwiritsa ntchito pamodzi kwa HMG-CoA reductase inhibitors ndi gemfibrozil, makonzedwe omwewo a mankhwalawa ayenera kupewedwa.

Ma fiber ena: chifukwa chowonjezera chiopsezo cha myopathy / rhabdomyolysis ndikugwiritsa ntchito munthawi yomweyo HMG-CoA reductase inhibitors okhala ndi ma fibrate, atorvastatin iyenera kuyikidwa mosamala mukamatenga ma fiber.

Nicotinic acid (niacin): chiopsezo chotenga myopathy / rhabdomyolysis chitha kuwonjezeka mukamagwiritsa ntchito atorvastatin molumikizana ndi nicotinic acid, chifukwa chake, munthawi imeneyi, kuganiziridwa kuyenera kuperekedwa pakuchepetsa mulingo wa atorvastatin.

Colestipol: ndi munthawi yomweyo kugwiritsa ntchito colestipol, kuchuluka kwa atorvastatin m'madzi am'magazi kunachepa pafupifupi 25%. Komabe, lipid-kutsitsa mphamvu ya kuphatikiza kwa atorvastatin ndi colestipol imaposa ya aliyense mankhwala payekhapayekha.

Colchicine: ndi munthawi yomweyo kugwiritsa ntchito atorvastatin ndi colchicine, milandu ya myopathy imanenedwa, kuphatikizapo rhabdomyolysis, chifukwa chake, kusamala kuyenera kuchitika pofotokoza atorvastatin ndi colchicine.

Digoxin: mobwerezabwereza makonzedwe a digoxin ndi atorvastatin pa 10 mg, kuchuluka kwa ndende ya digoxin m'madzi a m'magazi sikunasinthe. Komabe, pamene digoxin imagwiritsidwa ntchito limodzi ndi atorvastatin pa mlingo wa 80 mg / tsiku, kuchuluka kwa digoxin kumawonjezeka pafupifupi 20%. Odwala omwe amalandira digoxin osakanikirana ndi atorvastatin amafunikira kuwunika koyenera.

Erythromycin / clarithromycin: ndi munthawi yomweyo kugwiritsa ntchito atorvastatin ndi erythromycin (500 mg kanayi patsiku) kapena clarithromycin (500 mg kawiri patsiku), zomwe zimalepheretsa cytochrome P450 ZA4, kuwonjezeka kwa kuchuluka kwa atorvastatin m'magazi a magazi kumawonedwa.

Azithromycin: ndi munthawi yomweyo kugwiritsa ntchito atorvastatin (10 mg kamodzi patsiku) ndi azithromycin (500 mg / kamodzi patsiku), kuchuluka kwa atorvastatin mu plasma sikunasinthe.

Terfenadine: ndi munthawi yomweyo kugwiritsa ntchito atorvastatin ndi terfenadine, kusintha kwakukulu mu pharmacokinetics ya terfenadine sikunapezeke.

Njira zakulera: mukugwiritsa ntchito atorvastatin ndi kulera kwapakamwa komwe kumakhala ndi norethindrone ndi ethinyl estradiol, kuwonjezeka kwakukulu mu AUC ya norethindrone ndi ethinyl estradiol kumawonedwa ndi pafupifupi 30% ndi 20%, motsatana. Izi ziyenera kuganiziridwa posankha njira yakulera yolerera ya pakamwa ya mayi yemwe akutenga atorvastatin.

Warfarin: pophunzira mogwirizana kwa atorvastatin ndi warfarin, palibe zizindikiro zakugwirizana kwakukulu pamankhwala komwe kunapezeka.

Cimetidine: pophunzira mogwirizana ndi atorvastatin ndi cimetidine, palibe zizindikiro zakugwirizana kwakukulu pamankhwala komwe kunapezeka.

Protease Inhibitors: kugwiritsa ntchito munthawi yomweyo mankhwala a atorvastatin okhala ndi mapuloteni ena otchedwa cytochrome P450 ZA4 inhibitors limodzi ndi kuwonjezeka kwa plasma mozama kwa atorvastatin.

Malangizo pakugwiritsira ntchito mankhwala a atorvastatin ndi HIV proteinase zoletsa:

Kutulutsa mawonekedwe ndi kapangidwe kake

Mankhwala ogulitsa amaperekedwa mwanjira ya mapiritsi mumafakitore. Chithandizo chogwira mankhwalawa ndi atorvastatin calcium calcium (40 mg piritsi lililonse).

Zowonjezera: microcrystalline cellulose, calcium carbonate, StarKap 1500 (pregelatinized starch ndi chimanga wowuma), aerosil, magnesium stearate, titanium dioxide, talc, macrogol, utoto wofiira, iron oxide, utoto wachikasu, iron oxide, mowa wa polyvinyl.

Phukusili lili ndi matuza 1.2 kapena 3 a mapiritsi a 1015 kapena 30.

Kuyanjana kwa mankhwala osokoneza bongo

Kugwiritsa ntchito munthawi yomweyo ndi antibacterial agents (erythromycin ,cacithromycin), mankhwala antifungal (fluconazole, ketoconazole, itraconazole), cyclosporine, michere yama michere imachulukitsa kuchuluka kwa atorvastitis ndi chiopsezo chokhala ndi myalgia.

Kugwiritsa ntchito nthawi yomweyo ndi kuyimitsidwa, komwe kunaphatikizapo magnesium ndi aluminiyamu, kunapangitsa kuchepa kwa kuchuluka kwa atorvastatin. Izi sizinakhudze kuchuluka kwa kutsitsa cholesterol ndi lipoprotein otsika.

Amayi omwe amatenga pakati pakamwa ayenera kuganizira kuti atorvastatin imatha kuwonjezera kuchuluka kwa ethinyl estradiol ndi norethindrone.

Kuphatikizika komwe kumafunikira kusamala: kuphatikiza kwa atorvastatin ndi mankhwala omwe amathandiza kuchepetsa kuchuluka kwa mahomoni a steroid (spironolactone, ketoconazole).

Kusagwirizana kosayenera kwa atorvastatin ndi antihypertensive mankhwala sikunawonedwe.

Pharmacological zochita za atorvastatin 40

Chithandizo chogwira ntchito cha mankhwala chalengeza kuti ntchito ya lipid yatsika ndipo ndi m'gulu la ma statins. Gawo limalepheretsa kuchepa kwa HMG-CoA, puloteni inayake yomwe imasintha mtundu wa A hydroxymethylglutaryl coenzyme kukhala mevalonic acid.

Mankhwalawa amachepetsa mapangidwe a LDL (otsika kachulukidwe lipoproteins) ndikuwonjezera ntchito ya LDL receptors. Kuphatikiza apo, mwa odwala omwe ali ndi hypercholesterolemia, mankhwalawa amachepetsa LDL.

Kuphatikiza apo, mankhwalawa amachepetsa kuchuluka kwa Ho (cholesterol yathunthu) ndikuwonjezera mafuta a cholesterol apamwamba kwambiri a lipoproteins (HDL).

Atorvastatin ali ndi mayamwidwe ambiri. Statin mu plasma imapeza ndende yake yambiri mumphindi 60-120. Kudya pang'ono kumachepetsa kutalika kwa mankhwalawa.

Katunduyu ali ndi bioavailability 12%. Thupi limapukusidwa mu zimakhala za chiwindi. Mankhwala amachotsedwa pamodzi ndi bile. Hafu ya moyo wa atorvastatin ndi maola 14. Pafupifupi 2% ya mankhwalawa ndi impso. Hemodialysis sichikhudza mawonekedwe a pharmacokinetic a mankhwalawa.

Malangizo apadera

Atorvastatin imatha kuyambitsa kuchuluka kwa seramu CPK, yomwe iyenera kukumbukiridwa pakuwonetsetsa kusiyanasiyana kwa kupweteka pachifuwa. Tiyenera kukumbukira kuti kuwonjezeka kwa CPK nthawi 10 poyerekeza ndi chizolowezi, limodzi ndi myalgia ndi kufooka kwa minofu kungagwirizane ndi myopathy, chithandizo chikuyenera kutha.

Pogwiritsa ntchito munthawi yomweyo mankhwala a atorvastatin okhala ndi cytochrome CYP3A4 proteinase inhibitors (cyclosporine, clarithromycin, itraconazole), mlingo woyambirira uyenera kuyambitsidwa ndi 10 mg, panjira yochepa ya mankhwala osokoneza bongo, atorvastatin iyenera kusiyidwa.

Ndikofunikira kuwunika pafupipafupi zizindikiro za chiwindi chisanagwire ntchito mankhwala, pakadutsa milungu 6 ndi 12 atatha kumwa mankhwalawa kapena atakulitsa mlingo, komanso pafupipafupi (miyezi isanu ndi umodzi) munthawi yonse yogwiritsira ntchito (mpaka mtundu wa odwala omwe kuchuluka kwake kwa transaminase kudutsa kwazonse ) Kuwonjezeka kwa hepatic transaminases kumawonedwa makamaka m'miyezi itatu yoyambirira ya mankhwala. Ndikulimbikitsidwa kuti muchepetse mankhwalawo kapena muchepetse mlingo ndi kuwonjezeka kwa AST ndi ALT koposa katatu. Kugwiritsa ntchito atorvastatin kuyenera kusiyidwa kwakanthawi ngati kungachitike kukula kwa matenda azachipatala omwe akuwonetsa kukhalapo kwa myopathy yacute, kapena pamaso pa zinthu zomwe zikuwonetsa kukonzekera kwa kulephera kwa impso chifukwa cha rhabdomyolysis (matenda oopsa, kuchepa kwa magazi, opaleshoni yayikulu, kuvulala, metabolic, endocrine kapena kusokonezeka kwakukulu kwa ma electrolyte) . Odwala akuyenera kuchenjezedwa kuti ayenera kupita kwa dokotala ngati vuto lopanda kufooka kapena kufooka kwa minofu kumachitika, makamaka ngati limodzi ndi malaise kapena malungo.