Yaya ake amfani da Atorvastatin 10?

Bayanin da ya dace da 26.01.2015

Sunan Latin: Atorvastatin
Lambar ATX: S10AA05
Aiki mai aiki: Gagarinka (Atorvastatinum)
Mai masana'anta: Magungunan CJSC ALSI

Tabletaya daga cikin kwamfutar hannu ya ƙunshi milligramms 21.70 ko 10.85 atorvastatin alli mai narkewa, wanda ya dace da milligram 20 ko 10 na atorvastatin.

A matsayin abubuwanda suka taimaka, Opadra II, magnesium stearate, aerosil, sitaci 1500, lactose, celclosese microcrystalline, carbonate carbonate.

Aikin magunguna

Wannan magani shine hypocholesterolemic - yana gasa da kuma zaɓi yana hana enzyme wanda ke sarrafa ƙimar sauya HMG-CoA zuwa mevalonate, wanda daga baya ya shiga cikin sterols, gami da cholesterol.

Raguwar ƙwayoyin plasma lipoproteins da cholesterol bayan ɗaukar miyagun ƙwayoyi ya kasance sakamakon raguwar aikin cholesterol a cikin hanta da kuma aikin HMG-CoA reductase, da haɓaka matakin masu karɓa na LDL a saman ƙwayoyin hanta, wanda ke ƙara haɓakawa da fatalwa na LDL.

A cikin mutane tare da homozygous da heterozygous familial hypercholesterolemia, cakuda dyslipidemia, da hypercholesterolemia marasa gado, raguwar apolipoprotein B, yawan ƙwayoyin cuta, da ƙananan ƙarancin cholesterol-lipoproteins yayin shan wannan magani.

Wannan magani yana rage damar haɓaka. ischemia da mace-mace a cikin mutane na kowane zamani da ciwon infarction na zuciya ba tare da tsayayyen angina da raunin Q ba.Yana kuma rage yawan hadarin rashin kamuwa da rauni mai yawan gaske, yawan cututtukan zuciya da hadarin kamuwa da cututtukan dabbobi masu cutarwa na zuciya da jijiyoyin jini.

Magunguna da magunguna

Yana da babban narkewa, ana lura da mafi girman hankali a cikin jini bayan daya zuwa awa biyu bayan gudanarwa. Amfani da bioavailability ya yi ƙasa saboda tsabtace tsarin aiki na ƙwayar ciki da kuma tasirin “hanyar farko ta hanta” - kashi 12 cikin ɗari. Kimanin kashi 98 na kashin da aka dauka yana daure ne da garkuwar plasma. Metabolization yana faruwa a cikin hanta tare da samuwar metabolites mai aiki da abubuwa marasa aiki. Rabin rayuwar shine awa 14. Yayin yanayin hemodialysis bai nuna ba.

Contraindications

Kada a sha maganin tare da:

a karkashin shekara 18
ciki da lokacin nono,
gazawar hanta,
cututtukan hanta na aiki ko haɓaka aikin enzymes na “hanta” saboda wasu dalilai marasa tushe,
rashin hankali ga abinda ke ciki na miyagun ƙwayoyi.

Ya kamata a ɗauka tare da cutar tsoka, raunin da ya farubabban tsarin aikin tiyata ba a sarrafa shi ba fargaba, sepsis, jijiyoyin jinirikicewar metabolism da endocrine, damuwa a cikin ma'aunin electrolyte na tsananin tsananin, tarihin cutar hanta da shan barasa.

Side effects

Lokacin shan waɗannan allunan, zaku iya dandana:

tashin hankali gout, mastodynianauyi riba (sosai m)
albuminuria yawan hailahawan jini (mai wuya)
petechiae, ecchymoses, seborrhea, eczemaswearin sweating, xeroderma, alopecia,
Cutar Lyell, cututtukan da suka yawaita erythema, daukar hoto, kumburi da fuska, angioedema, cututtukan mahaifa, tuntuɓar dermatitisfata fitsari da itching (rare),
take hakkin kawo rikici, rashin ƙarfi, rage libido, epididymitis, metrorrhagia, nephrourolithiasis, zubar farji, hematuria, fitar, dysuria,
haɗin gwiwa, tsoka, azabtarwarhabdomyolysis myalgiaarthralgia ciwon kai, anisitis, tendosynovitis, bursitisƙafafun kafafu amosanin gabbai,
gwanaye, goms na jini, melena, zubar jini na hanji, aikin hanta mai rauni, Jazzice cholestatic, maganin ciwon huhu, ciwon duodenal, cutar sankara, biliary colic, hepatitisgastroenteritis, ulcers na mucosa na baka, maƙarƙashiya, esophagitis, stomatitis, amaidysphagia binnewabushewar bakin ciki, haɓaka ko rage ci, ciwon ciki, na ciki, rashin tsoro, zawo ko maƙarƙashiya, ƙwannafi, tashin zuciya,
kumburin hanci, kumburin mahaifa, dyspnea, ciwon huhu, rhinitis, mashako,
thrombocytopenia, lymphadenopathy, anemia,
angina pectoris, arrhythmia, phlebitis, hauhawar jini, hauhawar jini, tashin zuciya, ciwon kirji,
asarar dandano, parosmia, glaucoma, kurma, bashin ciki, damuwa na masauki, bushewar haɗuwa, tinnitus, amblyopia,
asarar sanimaganin ciwan jiki bacin rai, migrainehyperkinesis, facial inna, ataxiadanshi mai danshi amnesiana gefe neuropathy, paresthesia, nasiha, nutsuwa, malaise, asthenia, ciwon kai, tsananin farin ciki, rashin bacci.

Haɗa kai

Gudanarwa na lokaci daya tare da masu hana masu kariya suna ƙara maida hankali ga abu mai aiki a cikin jini. Amfani da haɗin kai tare da kwayoyi waɗanda ke rage taro na kwayoyin steroid endogenous (ciki har da Spironolactone, Ketoconazole da Cimetidine) suna ƙara yiwuwar rage hodar iblis steroid.

Lokacin da aka ɗauka lokaci guda tare da nicotinic acid, erythromycin, fibrates da cyclosporins, yana ƙaruwa da yiwuwar haɓakar cutar kansa yayin da ake bi da wasu kwayoyi na wannan aji.

Simvastatin da Atorvastatin - Wanne ya fi kyau?

Simvastatin Statin halitta ce, kuma Atorvastatin shine mafi mahimmancin Statin zamani na asalin roba. Kodayake suna da hanyoyi na rayuwa daban-daban da kuma tsarin sunadarai, suna da sakamako iri iri. Su ma suna da tasirin sakamako guda ɗaya, amma Simvastatin yafi rahusa fiye da Atorvastatin, don haka ta hanyar farashin Simvastatin shine mafi kyawun zaɓi.

Pharmacokinetics

Nuna rashin hankali yana da girma. Lokacin da ya isa zuwa mafi yawan maida hankali shine 1-2 sa'o'i, matsakaicin maida hankali a cikin mata shine 20% mafi girma, AUC (yanki a ƙarƙashin juji) yana 10% ƙananan, matsakaicin maida hankali a cikin marasa lafiya tare da guguwar giya shine sau 16, AUC ya ninka sau 11 fiye da na al'ada. Abincin dan kadan yana rage gudu da tsawon lokacin shan ƙwayoyi (ta 25% da 9%, bi da bi), amma raguwa a cikin LDL cholesterol yana kama da wannan tare da yin amfani da atorvastatin ba tare da abinci ba. Hankalin atorvastatin lokacin da aka shafa shi da maraice yana ƙasa da safiya (kusan 30%). An bayyana alaƙar layin tsakanin matakin ɗaukar kwayar cutar.

Bioavailability - 14%, tsari na bioavailability na hanawa aiki ta hanawa HMG-CoA rage- 30%. Systemarancin tsarin bioavailability yana faruwa ne ta dalilin tsarin ƙwaƙwalwar ƙwayar cuta a cikin ƙwayar mucous na ƙwayar jijiyoyin ciki da kuma yayin "hanyar farko" ta hanta.

Matsakaicin matsakaiciyar rarraba shine 381 l, haɗin tare da furotin plasma shine 98%. Yana da metabolized a cikin hanta a ƙarƙashin aikin cytochrome P450 CYP3A4, CYP3A5 da CYP3A7 tare da ƙirƙirar metabolites na aiki metabolites (ortho- da kuma abubuwan da aka samar na parahydroxylated, samfuran beta-hada abubuwa). Sakamakon inhibitory na miyagun ƙwayoyi a kan ragewar HMG-CoA shine kusan kashi 70% wanda aka ƙaddara ta hanyar ayyukan kewaya metabolites.

An cire shi cikin bile bayan hepatic da / ko metabolhe metabolism (baya fuskantar matsanancin yanayin maganin cutar ciki).

Rabin rayuwar shine awoyi 14. Ayyukan hana haɓakawa da hanawa HMG-CoA ragewa yai kusan tsawon awanni 20-30, saboda kasancewar metabolites mai aiki. Kasa da 2% na maganin baka an ƙaddara shi a cikin fitsari.

Ba a keɓance shi a lokacin hemodialysis ba.

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 mafi 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,

Rigakafin Cutar 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.

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 kamuwa da cuta (boceprevir), clarithromycin da itraconazole.

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.

Hulɗa da ƙwayoyi

Hadarin da ke tattare da cutar myopathy tare da rhabdomyolysis da rashin cin nasara a lokacin jiyya tare da HMG-CoA reductase inhibitors yana ƙaruwa tare da amfani da cyclosporine, maganin rigakafi (erythromycin, clarithromycin, hipupristine / dalphopristine), hanawar kariya ta HIV itraconazole, ketoconazole), nefazodone. Duk waɗannan magungunan suna hana CenP3A4 isoenzyme, wanda ke cikin metabolism na atorvastatin a cikin hanta. Ana iya yin ma'amala mai kama da wannan tare da yin amfani da atorvastatin lokaci guda tare da fibrates da acid nicotinic a cikin matakan rage ƙwayar lipid (fiye da 1 g kowace rana).

Tare da amfani da lokaci guda tare da masu hana HIV kariya. hepatitis C virus mai hana masu kariya, clarithromycin da itraconazole ya kamata su yi hankali kuma su yi amfani da mafi ƙarancin ingancin atorvastatin.

CYP3A4 Isoenzyme Masu hana masu laifi

Tunda atorvastatin yana metabolized ta hanyar isoenzyme CYP3A4, haɗakar amfani da atorvastatin tare da masu hana ƙwaƙwalwar isoenzyme CYP3A4 na iya haifar da haɓakar ƙwayar plasma na atorvastatin. Matsakaicin ma'amala da tasirin tasirin abu an tabbatar dashi ta hanyar bambance tasirin sakamako akan CYP3A4 isoenzyme.

OATP1B1 jigilar furotin masu hana furotin

Atorvastatin da metabolites sune abubuwan da ke samar da furotin na safarar OATP1B1. OATP1B1 inhibitors (misali, cyclosporine) na iya haɓaka bioavailability na atorvastatin. Hack, amfani da atorvastatin na lokaci guda a kashi 10 na mg da cyclosporine a kashi na 5.2 mg / kg / rana yana haifar da karuwa a cikin atorvastatin a cikin jini na jini ta hanyar 7.7. Ba a san sakamakon hana aikin jigilar cutar hepatic ba tukuna a kan taro na atorvastatin a hepatocytes. Idan ba zai yuwu a guji amfani da irin waɗannan magunguna lokaci guda ba, ana bada shawara don rage kashi da sarrafa tasiri na jiyya.

Gemfibrozil / fibrates

Gabanin tushen amfani da fibrates a cikin monotherapy, ana lura da mummunan halayen lokaci-lokaci, gami da rhabdomyolysis da ke da alaƙa da ƙwayoyin tsoka. Hadarin irin waɗannan halayen yana ƙaruwa tare da yin amfani da fibrates da atorvastatin lokaci guda. Idan amfani da waɗannan magungunan a lokaci guda baza'a iya kauce masa ba, to yakamata ayi amfani da mafi ƙarancin amfanin atorvastatin. kuma kulawa ta yau da kullun game da yanayin haƙuri ya kamata a aiwatar da shi.

Saki siffofin da abun da ke ciki

A cikin kantin magunguna zaka iya samun nau'in magani 1 kawai - a cikin nau'ikan allunan. Kayan aiki yana nufin magungunan ƙwayoyin cuta guda ɗaya. Atorvastatin yana ba da gudummawa ga rage yawan abubuwan da ke cikin kiba, kuma an haɗa wannan sinadarin a cikin shiri a cikin nau'ikan gishiri na alli (alli trihydrate). A cikin ƙirar maganin da ke cikin tambaya, sashi na sashi mai aiki yana rufaffen - 10 MG. Wannan adadin yana cikin kwamfutar hannu 1. Magungunan ba ya nuna illa mai illa saboda kasancewar fim ɗin.

Atorvastatin za'a iya sayansu a cikin kunshin sel. Kowane yana dauke da Allunan 10. Jimlar adadin blister a cikin kwali mai kwali shine 1, 2, 3, 4, 5, ko 10 inji.

Atorvastatin 10 wani abu ne mai inzyme inhibitor wanda yake kai tsaye ya shafi tsarin samar da cholesterol.

Menene aka tsara?

Babban wuraren aikace-aikacen:

haɓaka tasiri na kwayoyi waɗanda aikinsu da nufin rage cholesterol (An wajabta Atorvastatin a matsayin wani ɓangare na kulawa mai wahala), cimma sakamako da ake buƙata tare da maganin rage cin abinci,
lura da tsarin cututtukan zuciya, hana ci gaban rikice-rikice wanda ya haifar da hauhawar jini, hauhawar jini, kumbura da jijiyoyin jini.

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 ruwan hoda mai ruwan hoda tare da farfajiya biconvex

Kare masu hana

Darajar AUC na atorvastatin tana ƙaruwa sosai tare da yin amfani da atorvastatin lokaci ɗaya da wasu haɗuwa da masu hana HIV kariya, da kuma atorvastatin da hepatitis C ƙwaƙwalwar ƙwayar cuta ta hanawa telaprevir. Saboda haka, yin amfani da atorvastatin na lokaci guda a cikin marasa lafiya suna ɗaukar haɗuwa da masu kariya daga kwayar cutar kwayar cutar ta kariya da ke hana ƙwaƙwalwar ƙwayar cuta ta tipranavir da ritonavir ko hepatitis C virus protease inhibitor telaprevir. Yakamata a yi taka tsantsan tare da yin amfani da atorvastatin tare da haɗuwa da masu hana HIV kariya lopinavir da ritonavir, kuma ya kamata a sanya allurai na atorvastatin. Yakamata a yi taka tsantsan tare da amfani da atorvastatin tare da haɗuwa da masu hana HIV kariya, saquinavir da ritonavir, darunavir da ritonavir, fosamprenavir da ritonavir ko fosamprenavir, yayin da yawan atorvastatin bai kamata ya wuce 20 MG ba. A cikin marasa lafiya da ke shan inhibitor na hana garkuwar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar kwayar cutar sinadarai da kwayar cutar sinadarai ta cutar kwayar cutar atorvastatin bai kamata ta wuce mil 40 ba;

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 suna ƙaruwa 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 ƙwayar LDL cholesterol ba ta dogara da lokacin shan magani 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 ma'anar dawowar 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 ita ce 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 da shi a cikin tsofaffi marasa lafiya. 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.

Azithromycin

Tare da yin amfani da atorvastatin na lokaci guda a kashi 10 na mg sau ɗaya a rana da azithromycin a kashi 500 na awo a rana, yawan azithromycin a cikin jini bai canza ba.

Haɗakar amfani da atorvastatin a kashi 40 MG tare da diltiazem a ƙimar 240 MG yana haifar da karuwa a cikin atorvastatin a cikin jini na jini.

CYP3A4 Isoenzyme Inductors

Haɗakar amfani da atorvastatin tare da waɗanda ke haifar da CYP3A4 isoenzyme (alal misali, efavirenz, phenytoin, rifampicin, St John's wort shirye-shiryen) na iya haifar da raguwa a cikin atorvastatin a cikin jini na jini. Sakamakon tsarin na atomatik tare da rifampicin (mai farauta CYP3A4 isoenzyme da mai hana Ortatocyte jigilar furotin mai hana daukar ciki), ana bada shawarar yin amfani da atorvastatin da rifampicin a lokaci guda, tunda ana jinkirta gudanar da atorvastatin bayan daukar rifampicin yana haifar da raguwar yawan jini a atmostat. Koyaya, sakamakon rifampicin akan maida hankali akan atorvastatin a cikin hepatocytes ba a san shi ba kuma idan ba za a iya kawar da amfani da wannan lokaci ba, ya kamata a sa ido sosai game da irin wannan haɗuwa yayin maganin.

Tare da shigarwar atorvastatin lokaci daya da dakatarwa wanda ya ƙunshi magnesium da hydroxides na aluminum, haɗuwa da atorvastatin a cikin jini yana raguwa da kusan 35%, duk da haka, matakin raguwa a cikin LDL-C bai canza ba.

Atorvastatin ba ya tasiri kan magunguna na phenazone, saboda haka, hulɗa tare da wasu kwayoyi metabolized ta enzymes iri ɗaya na tsarin cytochrome P 450 ba a sa ran.

Colestipol

Tare da yin amfani da colestipol na lokaci daya, yawan atorvastatin a cikin jini yana raguwa da kimanin 25%, duk da haka, tasirin rage ƙwayar lipid na haɗuwa da atorvastatin da colestipol sun wuce na kowane ƙwayoyi daban-daban.

Tare da maimaita amfani da digoxin da atorvastatin a kashi 10 a kowace rana, 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 tattarawar digoxin ya karu da kusan 20%, sabili da haka, ya kamata a sa ido a kan marasa lafiya.

Na'urar hana haihuwa

Tare da yin amfani da atorvastatin na lokaci daya da kuma hana hana haihuwa wanda ke dauke da norethisterone da ethinyl estradiol, an sami karuwa mai yawa a cikin AUC na norethisterone 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.

Terfenadine

Atorvastatin tare da yin amfani da lokaci ɗaya ba su da tasiri mai mahimmanci a cikin magunguna na terfenadine.

Yin amfani da atorvastatin lokaci guda tare da warfarin a farkon kwanakin na iya ƙara tasirin warfarin akan coagulation na jini (rage lokacin prothrombin). Wannan tasirin ya ɓace bayan kwanaki 15 na amfani da waɗannan magunguna a lokaci guda.

Tare da yin amfani da atorvastatin lokaci daya a kashi 80 MG da amlodipine a kashi 10 MG, magungunan magunguna na atorvastatin a cikin daidaitattun yanayin bai canza ba.

Fusidic acid

A lokacin karatun bayan tallace-tallace, an lura da maganganun rhabdomyolysis a cikin marasa lafiya da ke daukar mutum-mutumi, gami da atorvastatin da fusidic acid.A cikin marassa lafiya waɗanda amfani da fusidic acid ya zama dole, magani tare da statins ya kamata a dakatar da duk tsawon lokacin amfani da fusidic acid. Za'a iya sake amfani da maganin Statin bayan kwana 7 bayan kashi na ƙarshe na acid na fusidic. A cikin lokuta na musamman, lokacin da aka tsawaita tsarin kulawa tare da fusidic acid ya zama dole, alal misali, don lura da cututtukan cututtuka masu mahimmanci, buƙatar buƙatar yin amfani da atorvastatin da fusidic acid a kowane yanayi kuma a ƙarƙashin tsananin kulawa na likita. Mai haƙuri ya kamata ya nemi likita kai tsaye idan alamun bayyanar rauni, hankali, ko jin zafi sun bayyana.

Amfani da ezetimibe yana da alaƙa da haɓakar halayen masu illa, gami da rhabdomyolysis, daga tsarin musculoskeletal. Hadarin irin waɗannan halayen yana ƙaruwa tare da yin atorvastatin da ezetimibe na lokaci guda. Ana ba da shawarar kulawa da rufewa don waɗannan marasa lafiya.

An ba da rahoton shari'o'in myopathy tare da yin amfani da atorvastatin da colchicine lokaci guda. Tare da haɗin gwiwa tare da waɗannan kwayoyi, ya kamata a yi taka tsantsan.

Lokacin nazarin hulɗa na atorvastatin tare da cimetidine, ba a gano ma'amala mai mahimmanci a asibiti ba.

Sauran hanyoyin kwantar da hankali

Amfani da atorvastatin na lokaci guda tare da kwayoyi waɗanda ke rage maida hankali a cikin kwayoyin steroid na endogenous (gami da cimetidine, ketoconazole, spironolactone) yana ƙara haɗarin rage darajar taro na kwayoyin steroid endogenous (yakamata a yi taka tsantsan).

A cikin nazarin asibiti, an yi amfani da atorvastatin a hade tare da magungunan antihypertensive da estrogens, waɗanda aka wajabta su azaman sauyawa, ba a lura da alamun cudanya marasa mahimmanci a asibiti. Ba a gudanar da nazarin hulɗa tare da takamaiman kwayoyi 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 KFK sau 10 idan aka kwatanta da na yau da kullun, tare da myalgia da rauni na tsoka za a iya danganta su 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 lokaci-lokaci (kowane watanni 6) a duk tsawon lokacin amfani (har zuwa normalization na yanayin marasa lafiya wanda matakan transaminase ya wuce al'ada ) An lura da karuwa a cikin “hepatic” transaminases musamman a 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.

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 kuma nicotinic acid.

Antacids: lokaci guda na dakatarwa wanda ya ƙunshi magnesium da aluminum 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 kulawa na waɗannan kwayoyi 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 yayin ɗaukar fibrates.

Acid na Nicotinic (niacin): haɗarin haɓakar myopathy / rhabdomyolysis zai iya ƙaruwa yayin amfani da atorvastatin a hade tare da nicotinic acid, sabili da haka, a cikin wannan yanayin, ya kamata 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 yin amfani da atorvastatin na lokaci daya tare da colchicine, an ba da rahoton maganganun 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.

Amaryasar / 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 daya (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 northindrone da etinyl 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: lokacin da ake nazarin hulɗa da atorvastatin tare da warfarin, ba a sami alamun mahimmancin hulɗar 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: