Atorvastatin (40 mg) Atorvastatin

Atorvastatin 40 MG - wani ƙwayar lipid-rage ƙwayar cuta daga rukuni na statins. Hanyar aiwatar da maganin yana nufin rage jini cholesterol

Tabletaya daga cikin kwamfutar hannu mai rufi ya ƙunshi:

• abu mai aiki: atorvastatin calcium trihydrate (dangane da atorvastatin) - 40.0 mg,
• tsofaffi: microcrystalline cellulose - 103.72 mg, lactose monohydrate - 100,00 mg, kalma carbonate - 20.00 mg, crospovidone - 15.00 mg, sodium carboxymethyl sitaci (sodium sitaci glycolate) - 9.00 mg, hyprolose (hydroxypropyl cellulose) - 6, .00 mg, magnesium stearate - 3.00 mg,
• rufin fim: hypromellose - 4,500 mg, talc - 1,764 mg, hyprolysis (hydroxypropyl cellulose) - 1,746 mg, titanium dioxide - 0,990 MG ko bushewa don fim ɗin da ke dauke da hypromellose (50.0%), talc (19.6%), hyprolose (hydroxypropyl cellulose) (19.4%), titanium dioxide (11.0%) - 9,000 mg.

Alllaji biconvex allunan, fim mai hade da farin ko kusan fararen fata. Pa giciye sashi daga cikin farin fari ne ko kuma fararen fata ne.

Pharmacodynamics

Atorvastatin wani zaɓi ne mai haɓaka mai hana ƙwaƙwalwar HMG-CoA reductase, babban enzyme wanda ke canza 3-hydroxy-3-methylglutaryl-CoA zuwa mevalonate, mai keɓancewa ga steroids, gami da cholesterol. Roba mai saurin maganin rage kiba.

A cikin marasa lafiya tare da homozygous da heterozygous familial hypercholesterolemia, siffofin rashin dangi da hypercholesterolemia da cakuda dyslipidemia, atorvastatin yana rage yawan adadin cholesterol (Ch) a cikin jini na jini. low-density lipoprotein cholesterol (Cs-LDL) da apolipoprotein B (apo-B), kazalika da tattarawar lipoproteins mai ƙarancin ƙarfi (Cs-VLDL) da triglycerides (TG), suna haifar da karuwar taro na lipoprotein cholesterol (Cs-HD).

Atorvastatin yana rage maida hankali kan Chs da Chs-LHNP a cikin jini na jini, yana hana HMG-CoA reductase da cholesterol haɗuwa a cikin hanta da haɓaka adadin "hanta" LDL masu karɓa a farfajiyar tantanin halitta, wanda ke haifar da karuwar haɓakawa da catabolism na Chs-LDL.

Atorvastatin yana rage samarda LDL-C da yawan adadin ƙwayoyin LDL, yana haifar da ƙararraki mai ɗorewa a cikin ayyukan LDL-masu karɓar haɗuwa tare da ingantattun canje-canje a cikin LDL-barbashi, kuma yana rage taro na LDL-C a cikin marasa lafiya tare da homozygous hereditary familial hypercholesterolemia wanda ke da karfin gwiwa tare da sauran yana nufin.

Atorvastatin a cikin allurai na 10 zuwa 80 MG ya rage yawan faduwar Chs ta hanyar 30-46%, Chs-LDL - ta hanyar 41-61%, apo-B - ta hanyar 34-50% da TG - ta hanyar 14-33%. Sakamakon aikin kwantar da hankali sun kasance iri ɗaya a cikin marasa lafiya tare da heterozygous familial hypercholesterolemia, siffofin da ba na iyali na hypercholesterolemia da haɗewar hyperlipidemia, gami a cikin marasa lafiya da nau'in ciwon sukari na 2.

A cikin marasa lafiya da keɓewar hypertriglyceridemia da keɓewa, atorvastatin yana rage yawan adadin cholesterol, Chs-LDL, Chs-VLDL, apo-B da TG kuma yana ƙara yawan haɗakar Chs-HDL. A cikin marasa lafiya tare da dysbetalipoproteinsemia, atorvastatin yana rage yawan ƙwayar lipoprotein matsakaici (Chs-STD).

A cikin marasa lafiya da nau'in IIa da hyblipoproteinemia na IIb kamar yadda aka tsara Fredrickson, matsakaicin darajar haɓakar maida hankali akan HDL-C yayin kulawa tare da atorvastatin (10-80 mg) idan aka kwatanta da ƙimar farko shine 5.1-8.7% kuma ba a dogara da kashi ba. Akwai raguwa mai dogaro-da-gwargwado a cikin rabo: jimlar cholesterol / Chs-HDL da Chs-LDL / Chs-HDL ta 29-44% da 37-55%, bi da bi.

Atorvastatin a kashi na 80 MG yana rage haɗarin ci gaba da rikitarwa mai ƙarancin ischemic da mace-mace ta hanyar 16% bayan karatun 16-mako, da kuma haɗarin sake sakewa zuwa asibiti don angina pectoris tare da alamun cutar myocardial ischemia da 26%. A cikin marasa lafiya da bambancin farko na LDL-C (tare da infarction na myocardial ba tare da raunin Q ba da angina mai tsayayye a cikin maza, mata, da kuma marasa lafiya marasa shekaru da shekaru fiye da 65), atorvastatin yana haifar da raguwa a cikin hadarin rikicewar ischemic da mace-mace.

Rage yawan haɗuwa da ƙwayar plasma na LDL-C shine mafi kyawun dangantaka tare da kashi na atorvastatin fiye da yadda ake haɗuwa da ƙwayar plasma. An zaɓi kashi don yin la’akari da tasirin warkewa (duba sashi "Sashi da gudanarwa").

Ana samun sakamako na warkewa 2 makonni 2 bayan farawar, ya kai matsakaici bayan makonni 4 sannan ya ci gaba a duk tsawon lokacin magani.

Damuwa

Atorvastatin yana shan saurin hanzari bayan sarrafa bakin: lokaci don isa zuwa mafi yawan maida hankali (TCmax) a cikin jini na jini shine 1-2 awanni. A cikin mata, mafi girman yawan atorvastatin (Cmax) ya kai kashi 20%, kuma yankin da ke ƙarƙashin tsarin lokacin taro (AUC) ya ragu da kashi 10% cikin maza. Matsakaicin narkewa da maida hankali a cikin jini na jini yana ƙaruwa daidai gwargwado. Cikakken bayanin bioavailability kusan 14%, kuma ƙirar bioavailability na aikin inhibitory na hanawa HMG-CoA reductase kusan 30%. Systemarancin tsarin bioavailability yana faruwa ne ta hanyar tsarin ƙwayoyin cuta a cikin ƙwayar mucous na ƙwayar jijiyoyin ciki da / ko yayin "jigon farko" ta hanta. Cin dan kadan yana rage ragi da darajar sha na atorvastatin (ta hanyar 25% da 9%, bi da bi, kamar yadda aka tabbatar da sakamakon ƙudurin Cmax da AUC), duk da haka, raguwar LDL-C yayi daidai da na atorvastatin akan komai a ciki. Duk da cewa bayan shan atorvastatin da maraice ƙwayar plasma tana da ƙasa (Cmax da AUC da kusan 30%) fiye da bayan shan ta da safe, raguwar taro LDL-C baya dogara da lokacin ranar da ake shan maganin.

Tsarin rayuwa

Atorvastatin yana da mahimmancin metabolized don ƙirƙirar ortho- da para-hydroxylated Kalam da samfuran beta-hada abubuwa iri-iri. A cikin in vitro, ortho- da para-hydroxylated metabolites suna da tasirin sakamako akan ragewar HMG-CoA, kwatankwacin na atorvastatin. Ayyukan inhibitory na hanawa HMG-CoA reductase kusan kashi 70% ne saboda ayyukan kewaya metabolites. Nazarin cikin vitro ya ba da shawarar cewa hanta na isoenzyme CYP3A4 yana taka muhimmiyar rawa a cikin metabolism na atorvastatin. An tabbatar da wannan ta hanyar karuwa a cikin atorvastatin a cikin jini na mutum yayin shan erythromycin, wanda shine mai hana wannan isoenzyme.

Binciken in vitro ya kuma nuna cewa atorvastatin mai rauni ce ta hana CYP3A4 isoenzyme. Atorvastatin ba shi da tasirin gaske a cikin ƙwayar plasma na terfenadine, wanda aka samar da metabolized musamman ta CYP3A4 isoenzyme, saboda haka, mahimman tasirin sa ga magunguna na sauran abubuwan da ke cikin alakar CYP3A4 ba shi yiwuwa (duba ɓangaren "hulɗa tare da wasu kwayoyi").

Atorvastatin da metabolites din an kebe su musamman tare da bile bayan hepatic da / ko extrahepatic metabolism (atorvastatin baya fuskantar mummunan enterohepatic recirculation). Rabin-rabi (T1 / 2) kusan awa 14 ne, yayin da tasirin hanawar atorvastatin dangane da Htr-CoA ragectase kusan kashi 70% ne da aka ƙaddara ta hanyar motsa jini metabolites kuma yana ɗaukar kimanin sa'o'i 20-30 saboda kasancewar su. Bayan shan miyagun ƙwayoyi, ƙasa da 2% na yarda da maganin ana samun su a cikin fitsari.

Alamu don amfani

• azaman kari don rage cin abinci don rage tasirin cholesterol, LDL-C, apo-B, da triglycerides a cikin manya, matasa, da yara masu shekaru 10 ko mazan su da babban hypercholesterolemia, gami da familial hypercholesterolemia (heterozygous version) ko hade (hade) hyperlipidemia ( nau'ikan IIa da IIb gwargwadon rarrabuwa da Fredrickson), lokacin da amsawar abinci da sauran magungunan marasa magani marasa wadatarwa,
• don rage tasirin cholesterol mai girma, LDL-C a cikin manya tare da hyzycholesterolemia na homozygous a matsayin haɗin kai ga wasu hanyoyin maganin rage ƙwayar cutar lipid (misali LDL-apheresis) ko, idan ba'a sami irin waɗannan jiyya ba,

Yin rigakafin cututtukan zuciya:

• rigakafin abubuwan da suka faru na zuciya da jijiyoyin jini a cikin manya manya a babban hadarin bunkasar abubuwan da ke faruwa na zuciya, ban da gyaran sauran abubuwan hadarin,
• rigakafin sakandare na rikicewar cututtukan zuciya a cikin marasa lafiya da cututtukan zuciya na zuciya don rage jimlar yawan mace-mace, bugun zuciya, bugun jini, sake komawa asibiti don angina pectoris da buƙatar farfadowa.

Contraindications

Magungunan hana amfani da atorvastatin sune:

• hypersensitivity to atorvastatin da / ko kowane ɓangaren magungunan,
• cutar hanta mai aiki ko karuwar aikin “hanta” transaminases a cikin jini na asalin da ba a san shi ba fiye da sau uku idan aka kwatanta da babba na yau da kullun,
• cirrhosis na hanta na kowane etiology,
• amfani a cikin mata masu haihuwa da basa amfani da isasshen hanyoyin samun juna biyu,
• amfani da ma'amala tare da acid na huda,
• shekaru har zuwa 10 - don marasa lafiya tare da heterozygous familial hypercholesterolemia,
• shekaru har zuwa shekaru 18 lokacin da aka yi amfani da wasu alamomi (ba a kafa ingantaccen aiki da amincin amfani ba),
• ciki, shayarwa
• rashin maganin lactose, rashi lactase, glucose-galactose malabsorption.

Ana iya yin Atorvastatin ga macen da ta haihu kawai idan an iya sanin ta da cewa ba ta da juna biyu kuma ta sanar da yiwuwar hadarin da miyagun ƙwayoyi ga tayi.

Tare da taka tsantsan: shan barasa, tarihin cutar hanta, a cikin marasa lafiya da dalilai masu haɗari don rhabdomyolysis (rashi aiki na renal, hypothyroidism, rikicewar ƙwayar tsoka a cikin marasa lafiya tare da tarihin ko tarihin dangi, illa mai guba na HMG reductase inhibitors ko fibrates akan tsoka sun riga sun kasance nama, shekara sama da shekaru 70, amfani da lokaci guda tare da kwayoyi waɗanda ke kara haɗarin kamuwa da cuta da rhabdomyolysis

Sashi da gudanarwa

A ciki. Atauki kowane lokaci na rana, ba tare da la'akari da yawan abincin ba.

Kafin fara magani tare da Atorvastatin, yakamata kuyi ƙoƙarin cimma iko na hypercholesterolemia ta amfani da abincin, motsa jiki da asarar nauyi a cikin marasa lafiya tare da kiba, da kuma maganin cututtukan da ke tattare da cutar.

Lokacin da yake rubuta magani, mai haƙuri yakamata ya bayar da shawarar daidaitaccen tsarin abinci, wanda dole ne ya kasance tare da shi tsawon lokacin magani.

Yawan maganin yana bambanta daga 10 MG zuwa 80 MG sau ɗaya a rana kuma ana sanya shi layin la'akari da farkon tattarawar LDL-Xc, manufar farjin da tasirin mutum akan maganin. Matsakaicin maganin yau da kullun shine 80 MG.

A farkon jiyya da / ko yayin haɓaka yawan ƙwayar Atorvastatin, ya zama dole a kula da yawan ƙwayar lipids a cikin jini a kowane mako na 2-4 kuma daidaita sashi gwargwado.

Heterozygous familial hypercholesterolemia

Maganin farko shine 10 MG kowace rana. Ya kamata a zaɓi kashi ɗin daban-daban kuma ku kimanta dacewa a kowane mako 4 tare da yuwuwar karuwa zuwa 40 MG kowace rana. Sannan za a iya ƙara yawan zuwa adadin zuwa 80 MG kowace rana, ko haɗuwa da jerin abubuwan bile acid tare da amfani da atorvastatin a cikin kashi 40 MG kowace rana mai yiwuwa.

Amfani a cikin yara da matasa daga 10 zuwa 18 tare da heterozygous familial hypercholesterolemia

Maganin farawa shine 10 MG sau ɗaya a rana. Za'a iya ƙara yawan zuwa 20 MG kowace rana, gwargwadon sakamakon asibiti. Warewa tare da kashi fiye da 20 MG (wanda ya yi daidai da kashi na 0.5 mg / kg) yana iyakantacce. Wajibi ne a fitar da kashi na maganin gwargwadon dalilin maganin rage rage kiba. Ya kamata a aiwatar da gyaran fuska gwargwado na 1 lokaci cikin makonni huɗu ko fiye.

Yi amfani dashi a hade tare da wasu kwayoyi

Idan ya cancanta, yin amfani da lokaci ɗaya tare da cyclosporine, telaprevir ko haɗuwa da tipranavir / ritonavir, kashi na miyagun ƙwayoyi Atorvastatin bai kamata ya wuce 10 MG kowace rana ba.

Yakamata a yi taka tsantsan kuma mafi ƙarancin ingancin atorvastatin yakamata a yi amfani dashi yayin da ake amfani da shi tare da masu hana HIV, masu hana garkuwar hepatitis C rigakafin (boceprevir), clarithromycin da itraconazole.

Side effects

Lokacin shan Atorvastatin, waɗannan sakamako masu illa na iya faruwa:

• Daga tsarin juyayi: rashin bacci, ciwon kai, ciwo na asthenic, malaise, dizziness, neuropathy na yanki, amnesia, paresthesia, hypesthesia, depression.
• Daga tsarin narkewa: tashin zuciya, zawo, ciwon ciki, dyspepsia, flatulence, maƙarƙashiya, amai, anorexia, hepatitis, pancreatitis, cholestatic jaundice.
• Daga tsarin musculoskeletal: myalgia, ciwon baya, arthralgia, cramps muscle, myositis, myopathy, rhabdomyolysis.
• Allergic halayen: urticaria, pruritus, fatar fata, rashwar jiki, anaphylaxis, erythema na polymorphic exudative erythema (ciki har da cutar Stevens-Johnson), Laille syndrome.
• Daga gabobin hemopoietic: thrombocytopenia.
• Daga gefen metabolism: hypo- ko hyperglycemia, karuwar ayyukan serum CPK.
• Daga tsarin endocrine: mellitus ciwon sukari - yawan ci gaba zai dogara ne akan kasancewar ko rashin abubuwan haɗari (gulukumi mai azumi ≥ 5.6, ƙididdigar jiki> 30 kg / m2, karuwa a cikin triglycerides, tarihin hauhawar jini).
• Sauran: tinnitus, gajiya, lalatawar jima'i, gurguwar ciki, ƙima mai nauyi, ciwon kirji, alopecia, maganganu na haɓaka cututtukan cututtukan ƙwaƙwalwa, musamman tare da tsawaita amfani, bugun jini (lokacin da aka ɗauka a cikin babban allurai kuma tare da masu hana CYP3A4), na biyu na renal gazawa.

Yawan yawan bayyanar cututtuka

Takamaiman alamun alamun yawan shan ruwa bai cika ba. Kwayar cutar za ta iya haɗawa da jin zafi a hanta, gazawar koda na gazawa, tsawan tsawan yin amfani da ita na myopathy da rhabdomyolysis.

Game da yawan abin sama da ya kamata, matakan gaba daya suna da mahimmanci: saka idanu da kiyaye mahimman ayyukan jiki, da hana kara shan ƙwayoyi (maganin ciwan ciki, shan gawayi ko maganin lasa).

Tare da haɓakar ciwon sankarar myopathy, tare da rhabdomyolysis da kuma rashin nasara na koda, dole ne a soke maganin nan da nan kuma jiko na diuretic da sodium bicarbonate ya fara. Rhabdomyolysis na iya haifar da hyperkalemia, wanda ke buƙatar sarrafawa na ciki na mafita na alli chloride ko mafita na alli glucuate, jiko na 5% bayani na tsawa (glucose) tare da insulin, da kuma amfani da reshen potassium-musayar resins.

Tunda maganin yana da alaƙa da kariyar plasma, hemodialysis ba su da tasiri.

Form sashi

Allunan mai rufi 10 MG, 20 MG da 40 MG

Tabletaya daga cikin kwamfutar hannu ya ƙunshi:

abu mai aiki - atorvastatin (azaman gishirin gishiri na trihydrate) 10 mg, 20 mg da 40 mg (10.85 mg, 21.70 mg da 43.40 mg),

magabata: carbonate carbonate, crospovidone, sodium lauryl sulfate, silicon dioxide, colloidal anhydrous, talc, celclose microcrystalline,

harsashi abun da ke ciki: Opadry II ruwan hoda (talc, polyethylene glycol, titanium dioxide (E171), polyvinyl barasa, baƙin ƙarfe (III) oxide yellow (E172), baƙin ƙarfe (III) oxide ja (E172), baƙin ƙarfe (III) oxide baki (E172).

Allunan mai ruwan hoda masu launin ruwan hoda tare da farfajiyar biconvex

Kayan magunguna

Pharmacokinetics

Atorvastatin yana ɗaukar hanzari bayan kulawa ta baka, ƙwaƙwalwar ƙwayar plasmarsa ya kai matsakaicin matakin na 1 - 2. Aikin dangi na atorvastatin shine 95-99%, cikakkar - 12-14%, tsari (samar da hanawar HMG-CoA reductase) - kimanin 30 % Ana yin bayanin ƙananan ƙirar bioavailability ta hanyar tsabtace tsarin a cikin ƙwayar mucous na ƙwayar hanji da / ko metabolism yayin farkon aikin ta hanta. Orazantawa da kwantar da hankali na plasma yana ƙaruwa da gwargwadon yawan maganin. Duk da gaskiyar cewa lokacin da aka ɗauke shi da abinci, yawan shan miyagun ƙwayoyi yana raguwa (matsakaicin ɗaukar hankali da AUC sun kusan 25 da 9%, bi da bi), raguwar matakin LDL cholesterol bai dogara da atorvastatin da aka ɗauka tare da abinci ba ko a'a. Lokacin ɗaukar atorvastatin da maraice, ƙwayar plasma ta kasance ƙasa (kusan 30% don mafi girman taro da AUC) fiye da lokacin shan safiya. Koyaya, raguwar matakin LDL cholesterol bai dogara da lokacin shan maganin ba.

Fiye da 98% na miyagun ƙwayoyi sun ɗaura wa furotin plasma. Matsayi na erythrocyte / plasma shine kusan 0.25, wanda ke nuna raunin ƙwayar cutar a cikin sel jini.

Atorvastatin yana metabolized zuwa abubuwan da aka samo asali na ortho-da para-hydroxylated da samfuran beta-oxidized daban-daban. Sakamakon inhibitory na miyagun ƙwayoyi dangane da HMG-CoA reductase shine kusan 70% da aka samu saboda ayyukan haɓaka metabolites. Atorvastatin an samo shi mai rauni mai hana cytochrome P450 ZA4.

Atorvastatin da metabolites din an kebe su musamman tare da bile bayan hepatic da / ko metabolhe metabolism. Koyaya, maganin ba mai saukin kamuwa da mahimmancin farfadowa na enterohepatic. Matsakaicin rabin rayuwar atorvastatin kusan sa'o'i 14 ne, amma tsawon lokacin hanawar motsa jiki da hanawa HMG-CoA ragewa saboda yaduwar metabolites mai aiki shine awanni 20-30. Kasa da kashi biyu cikin dari na maganin atorvastatin an fitar dashi a cikin fitsari.

Yawan plasma na atorvastatin a cikin tsofaffi masu lafiya (sama da 65) ya fi girma (kusan 40% don iyakar maida hankali da 30% ga AUC) fiye da matasa. Babu wani bambance-bambance a cikin tasiri na magani tare da atorvastatin a cikin tsofaffi marasa lafiya da marasa lafiya na sauran kungiyoyin shekaru.

Hankalin atorvastatin a cikin jini na jini a cikin mata ya bambanta da maida hankali a cikin jini na jini a cikin maza (a cikin mata, mafi girman yawanci shine kusan 20% mafi girma, kuma AUC - 10% ƙananan). Koyaya, babu bambance-bambance mai mahimmanci na asibiti da aka samo a cikin tasirin matakan lipid a cikin maza da mata.

Cutar cututtukan koda ba ta da tasiri ga ƙwayar ƙwayar cuta a cikin plasma ko tasirin atorvastatin akan matakan lipid, don haka babu buƙatar yin kwaskwarimar kashi a cikin marasa lafiya tare da gazawar koda. Nazarin ba ya rufe marasa lafiya da gazawar matakin ƙarancin ƙayyadadden lokaci; watakila, hemodialysis bai canza ma'anar atorvastatin ba, tunda maganin kusan yana ɗaukar sunadarai na jini.

Hankalin atorvastatin a cikin jini na jini yana ƙaruwa sosai (matsakaici mafi girma - kusan sau 16, AUC - sau 11) a cikin marasa lafiya tare da cirrhosis na hanta na etiology.

Pharmacodynamics

Atorvastatin wani zaɓi ne mai hanawa na ingiza na HMG-CoA reductase-enzyme, wanda ke kayyade yawan canzawar HMG-CoA zuwa mevalonate - mai ƙaddamar da sterols (gami da cholesterol (cholesterol)). A cikin marasa lafiya tare da homozygous da heterozygous familial hypercholesterolemia, wani nau'in da aka gada daga hypercholesterolemia da cakuda dyslipidemia, atorvastatin ya rage yawan adadin cholesterol, low lipoproteins low (LDL) da apolipoprotein B (Apo B). Atorvastatin kuma yana rage yawan ƙwayoyin lipoproteins masu ƙarancin yawa (VLDL) da triglycerides (TG), haka kuma yana ƙara ƙara yawan abubuwan da ke tattare da sinadarin cholesterol mai yawa (HDL).

Atorvastatin yana rage matakin cholesterol da lipoproteins a cikin jini na jini ta hanyar hana HMG-CoA reductase, haɓakar cholesterol a cikin hanta da haɓaka adadin masu karɓar LDL a saman hepatocytes, wanda ke tattare da haɓaka haɓakawa da catabolism na LDL. Atorvastatin yana rage haɓakar LDL, yana haifar da ƙararraki mai ɗorewa kuma mai ɗorewa a cikin ayyukan karɓar LDL. Atorvastatin yadda ya kamata ya rage matakan LDL a cikin marasa lafiya tare da hyzycholesterolemia na homozygous, wanda ba shi da amintacce ga ingantaccen farji tare da magunguna masu rage rage ƙwayoyi.

Shafin farko na aikin atorvastatin shine hanta, wanda ke taka rawa sosai a cikin ayyukan kwayar cutar cholesterol da kawarda LDL. Ragewa daga matakin LDL cholesterol yana daidaitawa tare da adadin maganin kuma maida hankali a jikin mutum.

Atorvastatin a kashi na 1080 mg sun rage matakin jimlar cholesterol (by 30-46%), LDL cholesterol (ta hanyar 41-61%), Apo B (by 34-50%) da TG (by 14-33%). Wannan sakamakon ya tabbata a cikin marasa lafiya da ke fama da cutar heterozygous familial hypercholesterolemia, wani nau'in hypercholesterolemia da aka samu da kuma cakuda hyperlipidemia, gami da marassa lafiyar marasa lafiyar marasa lafiyar insulin-insulin-mellitus.

A cikin marasa lafiya da keɓaɓɓen hypertriglyceridemia, atorvastatin rage matakin jimlar cholesterol, LDL cholesterol, VLDL cholesterol, Apo B, TG kuma ɗan ƙara girman matakin HDL cholesterol. A cikin marasa lafiya da dysbetalipoproteinemia, atorvastatin yana rage matakin ƙwayar cutar cholesterol.

A cikin marasa lafiya da nau'in IIa da hyblipoproteinemia na II (bisa ga rarrabuwa na Fredrickson), matsakaicin matakin karuwa a cikin HDL cholesterol lokacin amfani da atorvastatin a kashi 10-80 mg shine 5.1-8.7%, ba tare da la'akari da sashi ba. Bugu da kari, an sami raguwar yawan dogaro-mai-yawa a cikin yawan adadin cholesterol / HDL cholesterol da HDL cholesterol. Amfani da atorvastatin yana rage haɗarin ischemia da mutuwa a cikin marasa lafiya da infarction na myocardial ba tare da raƙuwar Q da yanayin angina ba tare da matsala ba (ba tare da la'akari da jinsi da shekaru ba) daidai ne da matakin LDL cholesterol.

Heterozygous mai dangantaka da hypercholesterolemia a cikin ilimin yara. A cikin yara maza da mata masu shekaru 10-17 tare da heterozygous familial hypercholesterolemia ko hypercholesterolemia mai tsanani, atorvastatin a kashi 10-20 MG sau ɗaya a rana da muhimmanci rage matakin jimlar cholesterol, LDL cholesterol, TG da Apo B a cikin jini na jini. Koyaya, babu wani tasiri mai tasiri akan girma da balaga a cikin samari ko tsawon lokacin haila a cikin girlsan mata. Amfani da lafiya da ingancin allurai sama da 20 MG don lura da yara ba'a yi binciken su ba. Ba a kafa tasirin lokacin maganin inorvastatin ba a cikin yara game da rage girman cuta da mace-mace a cikin samari.

Sashi da gudanarwa

Kafin fara maganin Atorvastatin, ya zama dole a tantance matakin cholesterol a cikin jini sabanin asalin abincin da yakamata, tsara abubuwan motsa jiki da kuma daukar matakan da zasu rage nauyin jikinsu a cikin masu dauke da kiba, haka kuma gudanar da magani don kamuwa da cututtukan. A yayin jiyya tare da atorvastatin, mara lafiya yakamata a bi tsarin daidaitaccen abinci na hypocholesterolemic. An wajabta maganin a cikin kashi 10 na MG 10 a rana kowace rana, a kowane, amma a lokaci guda na rana, ba tare da la'akari da abincin ba. Za'a iya keɓance na farko da kiyayewa gwargwadon gwargwadon matakin farko na cholesterol na LDL, burin da tasiri na jiyya. Bayan makonni 2-4 daga farkon magani da / ko daidaitawar sashi tare da Atorvastatin, yakamata a ɗauki bayanan lipid kuma an daidaita sashi gwargwado.

Primary hypercholesterolemia da hade (hade) hyperlipidemia. A cikin mafi yawan lokuta, ya isa ya tsara magani a cikin kashi 10 na MG sau ɗaya a rana kowace rana. Sakamakon magani yana haɓaka bayan makonni 2, sakamako mafi girma - bayan makonni 4. Ana samun ingantattun canje-canje da goyan bayan amfani da miyagun ƙwayoyi.

Homozygous familial hypercholesterolemia. An wajabta maganin a cikin kashi 10 zuwa 80 MG sau ɗaya a rana kowace rana, a kowane lokaci, ba tare da la'akari da cin abincin ba. Ana saita allurai na farko da tabbatarwa daban. A cikin mafi yawan lokuta, a cikin marasa lafiya tare da hyzycholesterolemia na homozygous, ana samun sakamako tare da amfani da Atorvastatin a cikin kashi 80 na MG sau ɗaya a rana.

Heterozygous familial hypercholesterolemia a cikin ilimin yara (marasa lafiya masu shekaru 10 zuwa 17). Atorvastatin ana bada shawara a cikin kashi na farko.

10 MG sau ɗaya a rana kowace rana. Matsakaicin shawarar da aka ba da shawarar shine 20 MG sau ɗaya a rana kowace rana (allurai da suka wuce 20 mg ba a yi nazarin su ba a cikin marasa lafiya na wannan rukunin yara). An saita sashi daban-daban, yin la'akari da dalilin maganin, ana iya daidaita sashi tare da tazara tsakanin makonni 4 ko fiye.

Yi amfani a cikin marasa lafiya da cutar koda da gazawar koda. Cutar cututtukan koda ba ta shafi yawan atorvastatin ko ragewa a cikin ƙwayar plasma LDL ba, don haka babu buƙatar daidaita sashi.

Yi amfani a cikin marasa lafiya tsofaffi. Babu bambance-bambance a cikin aminci da tasiri na miyagun ƙwayoyi a cikin lura da hypercholesterolemia a cikin tsofaffi marasa lafiya da marasa lafiya na manya bayan shekarun 60.

Marasa lafiya tare da nakasa aikin hanta an tsara miyagun ƙwayoyi tare da taka tsantsan dangane da jinkirin kawar da miyagun ƙwayoyi daga jikin mutum. Ana nuna ikon sigogin asibiti da dakin gwaje-gwaje, kuma idan an gano manyan canje-canje na ilimin halittu, ya kamata a rage kashi ko magani ya kamata a dakatar.

Idan an yanke shawara game da hadin gwiwar gudanar da Atorvastatin da CYP3A4 inhibitors, to:

Koyaushe fara magani tare da mafi ƙarancin kashi (10 MG), tabbatar da saka idanu a kan lipids mai guba kafin sanya kashi.

Kuna iya dakatar da shan Atorvastatin na ɗan lokaci idan an tsara masu hana CYP3A4 a cikin ɗan gajeren hanya (alal misali, wani ɗan gajeren hanya na ƙwayoyin cuta kamar clarithromycin).

Shawarwarin game da iyakar allurai na Atorvastatin lokacin amfani:

tare da cyclosporine - kashi bai kamata ya wuce 10 MG ba,

tare da clarithromycin - kashi bai kamata ya wuce 20 MG ba,

tare da itraconazole - kashi bai kamata ya wuce 40 MG ba.

Mu'amala da Lafiya

Hadarin myopathy yana ƙaruwa yayin kulawa tare da wasu kwayoyi na wannan aji yayin amfani da cyclosporine, abubuwan da ake amfani da su na fibric acid, erythromycin, antifungals da ke da alaƙa da jijiyoyi, da nicotinic acid.

Antacids: lokaci guda na dakatarwa wanda ya ƙunshi magnesium da hydro hydroxide ya rage yawan atorvastatin a cikin ƙwayar jini da kusan 35%, duk da haka, matakin raguwar cholesterol LDL bai canza ba.

Kwayar cutar ƙwaƙwalwa: Atorvastatin baya tasiri kan magunguna na antipyrine, sabili da haka, hulɗa tare da sauran kwayoyi metabolized by cytochrome isoenzymes iri ɗaya ba a sa ran su.

Amlodipine: a cikin nazarin hulɗa da miyagun ƙwayoyi a cikin mutane masu lafiya, gudanar da atorvastatin lokaci guda a kashi 80 MG da amlodipine a kashi 10 MG ya haifar da karuwa a sakamakon atorvastatin da 18%, wanda ba shi da mahimmancin asibiti.

Gemfibrozil: saboda haɓakar haɗarin haɓaka myopathy / rhabdomyolysis tare da yin amfani da inhibitors na HMG-CoA reductase tare da gemfibrozil, ya kamata a guji kawar da mulkin waɗannan magunguna a lokaci guda.

Sauran zawarawa: saboda karuwar haɗarin myopathy / rhabdomyolysis tare da yin amfani da Hhib-CoA reductase inhibitors tare da fibrates, atorvastatin ya kamata a tsara shi da taka tsantsan lokacin ɗaukar fibrates.

Acid na Nicotinic (niacin): haɗarin haɓakar myopathy / rhabdomyolysis zai iya ƙaruwa lokacin amfani da atorvastatin a hade tare da nicotinic acid, sabili da haka, a cikin wannan yanayin, yakamata a ba da shawara don rage yawan atorvastatin.

Colestipol: tare da amfani da colestipol lokaci guda, yawan atorvastatin a cikin jini yana raguwa da kusan 25%. Koyaya, sakamakon rage rage kiba na haɗin atorvastatin da colestipol sun wuce na kowane ƙwayoyi daban-daban.

Colchicine: tare da amfani da atorvastatin na lokaci daya tare da colchicine, an ba da rahoton maganganu na myopathy, ciki har da rhabdomyolysis, saboda haka ya kamata a yi taka tsantsan lokacin da aka tsara atorvastatin tare da colchicine.

Digoxin: tare da maimaitawa na maganin narkewa da atorvastatin a kashi 10 na mg, daidaitawar digoxin a cikin jini bai canza ba. Kodayake, lokacin da aka yi amfani da digoxin a hade tare da atorvastatin a kashi 80 na MG / rana, yawan narkewar ya karu da kusan 20%. Marasa lafiya da ke karɓar digoxin a hade tare da atorvastatin suna buƙatar saka idanu da suka dace.

Sankarinka / clarithromycin: tare da yin amfani da atorvastatin da erythromycin (500 mg sau hudu a rana) ko clarithromycin (500 mg sau biyu a rana), wanda ke hana cytochrome P450 ZA4, an lura da karuwar taro na atorvastatin a cikin jini na jini.

Azithromycin: tare da amfani da atorvastatin lokaci guda (10 mg sau ɗaya a rana) da azithromycin (500 MG / sau ɗaya a rana), yawan atorvastatin a cikin plasma bai canza ba.

Terfenadine: tare da yin amfani da atorvastatin da terfenadine na lokaci daya, ba a gano canje-canje masu mahimmanci a cikin magungunan likita na terfenadine ba.

Na baka hana: yayin amfani da atorvastatin da maganin hana haihuwa wanda ke dauke da northindrone da ethinyl estradiol, an sami karuwa sosai a cikin AUC na norethindrone da ethinyl estradiol da kusan 30% da 20% bi da bi. Yakamata a yi la’akari da wannan sakamako yayin zabar maganin hana yaduwa ga mace mai shan atorvastatin.

Warfarin: yayin nazarin hulɗa da atorvastatin tare da warfarin, ba a sami alamun ma'amala mai mahimmanci a asibiti ba.

Cimetidine: lokacin da ake nazarin hulɗa da atorvastatin tare da cimetidine, ba a sami alamun mahimmancin hulɗar asibiti ba.

Masu Kariya: amfani da atorvastatin na lokaci daya tare da masu hana kariya wanda aka sani da cytochrome P450 ZA4 inhibitors yana haɗuwa tare da haɓaka yawan ƙwayoyin plasma na atorvastatin.

Shawarwarin gabaɗaya na atorvastatin da masu hana HIV kariya:

Formaddamar da tsari da abun da ke ciki

Ana samar da samfurin magunguna a cikin nau'ikan allunan a cikin magunguna. Abubuwan da ke aiki na miyagun ƙwayoyi shine atorvastatin alli trihydrate (40 mg a kowace kwamfutar hannu).

Ingredientsarin abubuwan da ake amfani da su: microcrystalline cellulose, iron na baƙin ƙarfe, StarKap 1500 hadaddun (sitaci pregelatinized sitaci da sitaci masara), aerosil, magnesium stearate, titanium dioxide, talc, macrogol, fenti mai haske, iron baƙin ƙarfe, launin shuɗi, iron baƙin ƙarfe, barasa na polyvinyl).

Kunshin ya ƙunshi 1.2 ko 3 blisters na 10.15 ko 30 Allunan.

Hulɗa da ƙwayoyi

Amfani na lokaci ɗaya tare da masu hana ƙwayoyin cuta (erythromycin, clarithromycin), magungunan antifungal (fluconazole, ketoconazole, itraconazole), cyclosporine, ƙirar fibroic acid wanda ke haifar da haɗarin atorvastitis da haɗarin haɓaka myalgia.

Amfani na lokaci guda tare da dakatarwa, wanda ya haɗa da magnesium da aluminum, ya ba da gudummawa ga rage yawan atorvastatin. Wannan bai shafi matakin rage darajar cholesterol da ƙarancin lipoproteins mai yawa ba.

Matan da ke yin amfani da maganin hana magana na bakin jini ya kamata suyi la'akari da cewa atorvastatin na iya ƙara haɗuwa da ethinyl estradiol da norethindrone.

Haɗuwa yana buƙatar taka tsantsan: haɗuwa da atorvastatin tare da kwayoyi waɗanda ke taimakawa rage yawan kwantar da hankali na kwayoyin steroid (spironolactone, ketoconazole).

Ba'a lura da ma'amala mara kyau na atorvastatin tare da magungunan antihypertensive.

Aikin magunguna na atorvastatin 40

Abubuwan da ke aiki na miyagun ƙwayoyi suna da aiki mai saurin rage ƙarfin lipid kuma suna cikin rukunan statins. Abun da ke ciki yana hana HMG-CoA reductase, enzyme na musamman wanda ke canza nau'in A hydroxymethylglutaryl coenzyme zuwa mevalonic acid.

Magungunan yana rage haɓakar LDL (ƙarancin lipoproteins mai yawa) kuma yana ƙara matakin ayyukan masu karɓa na LDL. Bugu da ƙari, a cikin marasa lafiya tare da hypercholesterolemia, ƙwayar ta rage LDL.

Bugu da ƙari, ƙwayar ta rage matakin Ho (jimlar cholesterol kuma yana haɓaka yawan ƙwayoyin lipoproteins mai yawa) (HDL).

Atorvastatin yana da babban matakin sha. Statin a cikin plasma ya sami mafi yawan maida hankali a cikin mintuna 60-120. Cin dan kadan yana rage tsawon lokacin shan maganin.

Kayan yana da bioavailability na 12%. Abubuwan yana haɗuwa a cikin kyallen hanta. An cire magungunan tare da bile. Rabin rayuwar atorvastatin sa'o'i 14 ne. Kusan 2% na maganin yana dauke da ƙodan. Kwayar cuta ta jiki ba ta shafi bayanin martaba na magani ba.

Umarni na musamman

Atorvastatin na iya haifar da karuwa a cikin CPK serum, wanda ya kamata a la'akari da shi a cikin bambance-bambancen ganewar ciwon kirji. Ya kamata a ɗauka a cikin zuciya cewa karuwa a cikin CPK ta hanyar sau 10 idan aka kwatanta da na yau da kullun, tare da myalgia da rauni na tsoka na iya hadewa da myopathy, ya kamata a dakatar da jiyya.

Ta hanyar amfani da atorvastatin na lokaci guda tare da cytochrome CYP3A4 protease inhibitors (cyclosporine, clarithromycin, itraconazole), ya kamata a fara amfani da kashi na 10 tare da 10 MG, tare da ɗan gajeren hanya na maganin rigakafi, atorvastatin ya kamata a daina.

Yana da Dole a kai a kai saka idanu kan alamomin aiki hanta kafin magani, 6 da 12 makonni bayan fara miyagun ƙwayoyi ko bayan kara yawan, da kuma lokaci-lokaci (kowane 6 watanni) a duk tsawon lokacin amfani (har zuwa normalization na yanayin marasa lafiya wanda transaminase matakan wuce al'ada ) An lura da karuwa a cikin jigilar hepatic a cikin farkon watanni 3 na farko na maganin miyagun ƙwayoyi. An ba da shawarar soke miyagun ƙwayoyi ko rage kashi tare da karuwa a AST da ALT fiye da sau 3. Yin amfani da atorvastatin ya kamata a dakatar da ɗan lokaci idan akwai alamun ci gaban bayyanar cututtuka da ke nuni da kasancewar myopathy na rashin lafiya, ko kuma a gaban abubuwan da ke haifar da ci gaban matsanancin rashin ƙarfi sakamakon rhabdomyolysis (cututtukan ƙwaƙwalwa, rage karfin jini, tiyata mai yawa, rauni, metabolic, endocrine ko damuwa mai rikicewar damuwa) . Yakamata a gargadi marassa lafiya cewa yakamata su nemi likita kai tsaye idan zafin da ba a bayyana ba ko rauni na tsoka ya faru, musamman idan suna tare da zazzabi ko zazzabi.