Simvastatin: litaelo tsa tšebeliso, li-analogues, litheko le litlhahlobo
Simvastatin ke setlhare se nang le thepa e fokotsang lipid. Fumana sethethefatsi u sebelisa motsoako oa lik'hemik'hale ho sehlahisoa sa enzymatic metabolism ea Aspergillus terreus.
Karolo ea lik'hemik'hale ea ntho ke mofuta o sa sebetseng oa lactone. Ka phetoho ea biochemical, synthet ea cholesterol e etsahala. Tšebeliso ea lithethefatsi e thibela ho bokelloa ha lipid tse chefo haholo 'meleng.
Limolek'hule tsa ntho ena li kenya letsoho ho fokotseheng ha maikutlo a plasma a triglycerides, likaroloana tsa atherogenic tsa lipoprotein, hammoho le boemo ba cholesterol e felletseng. Khatello ea motsoako oa lipids tsa atherogenic e etsahala ka lebaka la khatello ea sebopeho sa cholesterol ho hepatocytes le keketseho ea palo ea meetso ea li-receptor tsa LDL ka membrane ea sele, e lebisang ts'ebetsong le ts'ebelisong ea LDL.
E boetse e eketsa boemo ba lipoprotein tse phahameng haholo, e fokotsa tekanyo ea lipids tsa atherogenic ho antiatherogenic le boemo ba cholesterol ea mahala ho likaroloana tsa antiatherogenic.
Ho ea ka liteko tsa tliliniki, lithethefatsi ha li bake liphetoho tse kahare. Tekanyo ea ho qala ha phello ea kalafo Ho qala hoa ponahatso ke matsatsi a 12-14, phello e phahameng ea kalafo e etsahala khoeli e le ngoe kamora ho qala ts'ebeliso. Matla a teng ka ho sa feleng le kalafo ea nako e telele. Haeba u khaotsa ho sebelisa lithethefatsi, boemo ba cholesterol ea endo native bo khutlela boemong ba bona ba pele.
Sebopeho sa moriana se emeloa ke ntho e sebetsang ea Simvastatin le likarolo tse thusang.
Ntho ena e na le monko o mongata le bioavailability e tlase. Ho kena maling, tlama ho albin. Sebopeho se sebetsang sa lithethefatsi se hlophisoa ke liphetoho tse ikhethileng tsa biochemical.
Metabolism ea Simvastatin e etsahala ho hepatocytes. E na le phello ea "phallo ea mantlha" ka lisele tsa sebete. Ho lahla ho etsahala ka tšilo ea lijo (ho fihlela 60%) ka tsela ea metabolites e sa sebetseng. Karolo e nyane ea ntho e lahloa ke liphio ka sebopeho se holofalitsoeng.
Foromo le sebopeho sa litekanyetso
Simvastatin (INN ka radar - simvastatin) ke ntho e sebetsang e kenyelelitsoeng ho lithethefatsi tse 'maloa tsa lebitso la moetsi oa lihlahisoa tse fapaneng le li-brand tlasa mabitso a fapaneng (Zentiva, Vertex, Star Star le ba bang, ho latela naha). K'holera ke ea moloko oa boraro oa li-statins mme ke moemeli ea fokotsang lipid ea tlase.
Ka lishelefong tsa litlama u ka fumana sethethefatsi se nang le lebitso le tšoanang hantle le ntho e sebetsang - Simvastatin. Sebopeho sa ho lokolloa ha moriana ke pene, se na le mekokotlo e chitja ea biconvex, e koahetsoe ka 'mala o pepeneneng kapa o soeufatsang. Ho ipapisitsoe le khatello ea ntho e sebetsang, matlapa a Simvastatin a fumaneha ka mefuta e fapaneng - 10 le 20 mg ka ngoe.
Cholesterol maling a motho e teng feela ka sebopeho se nang le protheine. Likhomphutha tse joalo li bitsoa lipoprotein. 'Meleng ho na le mefuta e' maloa ea limolek'hule tsena - phahameng, e tlase le e tlase haholo (HDL, LDL le VLDL, ka ho latellana). Kameho e mpe ea k'holeseterole e phahameng e qala ho hlaha ha e hlaha ho metabolism ea lipid. monyetla o hlakileng lebisa ho LDL, seo ho thoeng ke "cholesterol" e mpe.
Phello ea kalafo ea simvastatin e fumanoa haholo ka ho fokotsa karoloana ena ea lipoproteins (LDL). Ka ho thibela ketane ea enzymatic ea HMG - Coenzyme A reductase, lithethefatsi tse ithutoang li fokotsa khatello ea mafura ka har'a lisele ebe li kenya li-receptor bakeng sa lipoprotein tse tlaase le tse tlase haholo (LDL le VLDL). Kahoo, pathogenesis ea hypercholesterolemia e susumetsoa ke mekhoa e 'meli ka nako e le' ngoe - k'holeseterole e bonoa hampe ke lisele mme e tsoa kapele ho tsoa maling le 'meleng ka kakaretso.
Khahlano le nalane ea ho fokotseha hoa karoloana e mpe ea mafura, ho leka-lekana ha lipid ho khutlisetsoa 'me khatello ea khatello ea mohanyetsi, cholesterol e phahameng, e eketseha ka tekano. Ho latela mehloli e fapaneng, keketseho ea HDL kamora thupelo ea phekolo e tla ba ho tloha ho 5 ho isa ho 14%. Simvastatin ha e fokotse k'holeseterole e mpe feela, empa hape e na le phello ea vasoconstrictor. Motsoako ona o thibela ts'ebetso ea ho senyeha ha lebota la vascular, o eketsa ho phahama ha eona le molumo ka lebaka la phello ea antioxidant.
E 'ngoe ea likhopolo tsa nts'etsopele ea atherosulinosis ke ho ruruha. Sepheo sa ho ruruha ke karolo ea tlamo ea ho tsepamisa maikutlo ho atotosolite ho endothelium. Simvastatin e na le matla a ho thibela liphatsa tsa lefutso, ka ho etsa joalo e sirelletsang endothelium ho sclerotherapy, scarring le stenosis. Mehloli e mengata ea mahlale e fana ka maikutlo a hore phello ea ts'ireletso ho endothelium e etsoa khoeli kamora ho qala ha moriana.
Morero oa moriana o etsoa feela ho latela lipontšo tse thata, khetho ea lethal dose ke motho ka mong. Tekanyetso ea ho qala hangata 10 mg mme, ho ea ka bakuli le lingaka, e mamelloa hantle. Tekanyo e phahameng ea letsatsi le letsatsi ke 80 mg. E fuoe maemo a matla a hyperlipidemic. Bakeng sa bakuli ba nang le lefu la sebete kapa la liphio, lethal dose le leholo ha le na letho ebile le 40 mg.
Matšoao a ho sebelisoa
Moriana Simvastatin o laetsoe kalafo ea maemo le mafu a latelang:
- Hypercholesterolemia IIA le mefuta ea IIB ho latela sehlopha sa Fredrickson. Lipalo li fanoa haeba phetoho ea lijo, mekhoa ea bophelo le mehato e meng eo e seng ea lithethefatsi e sa tlise phello e lebelletsoeng ea kalafo. Ba thusa ka k'holeseterole e phahameng e kotsing ea ho ba le lefu la pelo khahlano le methapo ea methapo ea methapo ea mali ea pelo le sebopeho sa lipopae.
- Ts'ebeliso ea bona e na le mabaka a phahameng a ho se feela likhechana tsa cholesterol feela, empa le triglycerides. Ka lebaka la ts'ebetso ea Simvastatin, ho ka khonahala ho fokotsa khatello ea mali ea "TG" (triglycerides) maling ka 25%.
- Simvastatin e laetsoe mohahong o thata oa phepelo ea tlhokomelo bakeng sa ho thibela mathata a methapo ea pelo le - pelo, ho nyekeloa ke pelo, atherosclerosis. Khahlano le nalane ea ts'ebeliso ea meriana ena, boemo ba cholesterol butle-butle bo khutlela ho bo tloaelehileng.
Litokisetso tsohle tsa k'holeseterole li na le matšoao a ikhethang, lethathamo le pharaletseng la litlamorao le li-contraindication, ka hona li ka fanoa ke ngaka feela ka mokhoa o fanoang ke ngaka ka Selatine.
Contraindication
Joalo ka lithethefatsi life kapa life, Simvastatin e na le litlolo tse 'maloa tse thata, tseo ho eona e lokelang ho thibeloa. Maemo ana a kenyelletsa:
- Karolo e sebetsang ea li-pathologies tsa hepatobiliary system, hammoho le keketseho ea nako e telele, e sa phekoloheng ea li-transaminase tsa hepatic tsa tlhaho e sa tsejoeng.
- Maloetse a Myopathic. Ka lebaka la myotoxicity, simvastatin e ka mpefatsa le ho kula hoa mesifa ea mesifa, ho baka rhabdomyolysis le ho se sebetse hantle ha bohloko ka mor'a eona.
- Lilemo tsa bana. Ts'ebetsong ea bana, ha ho na boiphihlelo ka ts'ebeliso ea lithethefatsi ena. Ho saense, ha ho na datha ho lifaele tsa ts'ebetso le polokeho ea Simvastatin ho bakuli ba ka tlase ho lilemo tse 18.
- Ho ima le ho anyesa - ha ho sebelisoe statin bakeng sa cholesterol nakong tsena.
Ka hlokolosi e kholo, simvastatin e laeloa batho ba sebelisang joala hampe - ho tsamaellana le joala ho li-statins ho fokola, ho renal le ho haelloa ke phepo e matla ho ka hlaha kapele haholo.
Litlamorao
Ho tsoa lithong tsa pampitšana ea ka mpeng ho ka ba le bohloko ba ka mpeng, dyspeptic syndromes, ho nyekeloa ke pelo, ho hlatsa le mathata a ka mokokotlong. Ts'ebeliso ea lithethefatsi e ka ama sebete "- ho latela litaelo, keketseho ea nakoana ea li-enzyme tsa sebete (liprotheine tsa mali) lia khoneha.
Ts'ebetso ea methapo e bohareng le e poteletseng e ka arabela ts'ebelisong ea simvastatin ka nts'etsopele ea lefu la limela tsa astheno le li-episode tsa cephalgia, mokhathala, bofokoli ba maikutlo, ho hloka boroko le ho tsekela. Litlamorao tse ling tse mpe tsa Simvastatin li kenyelletsa ho saroloha ha mesifa (maikutlo a ho phahama), kutloelo-bohloko ea ho senyeha ha maikutlo, liphetoho tsa maikutlo.
Ka ho ba le maikutlo a phahameng a motho ka mong ho lintho tse sebetsang kapa tse thusang tsa moriana ona, maikutlo a kulang a ka hlaha. Ho na le mefuta e mengata ea lipontšo tsa bona, empa ho latela lipalo-palo, urticaria, eosinophilia, lefu la ramatiki, angioedema le polymyalgia ea lefu la rheumatoid genesis hangata e ka ba teng.
Letšoao la letlalo la liphetoho tse mpe li ka ba ka mofuta oa 'mala o mofubelu o hlakileng oa erythematous, ho hlohlona le dermatoses. Basebeletsi ba Hypolipidemic ba chefo ho lisele tsa mesifa, ka hona, ka litšobotsi tse 'maloa tsa motho ka mong kapa lipilisi tse phahameng, ponahalo ea myopathies, bohloko ba mesifa, ts'ebetso ea ho ruruha mesifa, bofokoli ba bona le mokhathala. Maemong a sa tloaelehang haholo, rhabdomyolysis e hlaha.
Tekanyetso le tsamaiso
Ho latela tlhahlobo ea mafu, simvastatin e fanoa ka tekanyo e boletsoeng ke ngaka. E fapana pakeng tsa bonyane ba kalafo (10 mg) le boholo ba letsatsi le letsatsi (80 mg). Moriana o lokela ho nooa pele ho lijo, hang ka letsatsi, haholo-holo mantsiboea, o hlatsuoa ka metsi a futhumetseng a kamore. Khetho le tokiso ea lethal dose e etsoa ka nako e sa feteng khoeli e le 'ngoe.
Karabo ea potso ea hore na ho nka Simvastatin ho nka nako e kae ho ntlafatsa bophelo bo botle e ka fanoa feela ke ngaka e eang. Nako ea thupelo e ipapisitse le tlhahlobo ea mali, matla a lefu lena le lipontšo tsa boemo ba lipid - LDL, triglycerides, cholesterol e felletseng.
Nakong ea bokhachane le pelehi
Simvastatin e na le litlamorao tsa teratogenic le fetoto. E khona ho kenella ka har'a placenta, ka hona, ha e laetsoe nakong ea kemaro, e ka baka nts'etsopele ea malformations le "pathologies" ea fetal. Banana ba lilemo tsa ho beleha ba hlokang ho sebelisa lithethefatsi ho tsoa sehlopheng sa li-statins ka mabaka a bophelo bo botle ba tlameha ho latela mekhoa e lekaneng ea thibelo ea bokhachane nakong eohle ea kalafo.
Ts'ebetsong ea bana, lithethefatsi ha li sebelisoe, hobane ha ho na datha e thehiloeng kliniking mabapi le polokeho le katleho ea profil ea Simvastatin bakeng sa bakuli ba bana.
Ka ho se sebetse hantle ha sebete
Hoa hlokahala ho laola ts'ebetso ea sebete ntle le ho qhekella pele ho qala kalafo ea ho fokotsa lipid le nakong ea eona. Matšoao a li-enzyme tsa sebete (serum transaminases) lia hlahlojoa, 'me ho etsoa liteko tse' maloa tse sebetsang tsa sebete. Ka liphetoho tse sa feleng liphellong tsa liteko, sethethefatsi se emisoa.
Ka mosebetsi o sa sebetseng oa renal
Bakuli ba tšoeroeng ke lefu le bobebe kapa le itekanetseng la ho hlaphoheloa kelellong ba lumelloa ho fana ka moriana, empa ho khothalletsoa ho hana tekanyetso e phahameng. Maemong a tebileng a PN (ho se sebetse hantle ka mokokotlo), tumello ea creatinine e ka tlase ho 30 ml ka motsotso, kapa ts'ebeliso ea morao ea lithethefatsi tse kang cyclosporine, fibrate, dinazole, tekanyo e phahameng ea lithethefatsi ke 10 mg ka letsatsi.
Matlapa a Simvastatin: seo moriana o se thusang
Matšoao a ts'ebeliso ea lithethefatsi a kenyelletsa:
- hypercholesterolemia ea mantlha (mofuta oa IIa le IIb) ka ho se sebetse hantle hoa kalafo ea ho ja ka k'holeseterole e tlase le mehato e meng e seng ea lithethefatsi (ho theola boima ba 'mele le ts'ebetso ea' mele) ho batho ba nang le kotsi e eketsehileng ea ho ba le coronary atherossteosis,
- hypertriglyceridemia le hypercholesterolemia ha e lokisoe ke ho ikoetlisa le ho ja lijo tse khethehileng.
- phokotso ea tlatsetso ea mathata a pelo (lefu le potlakileng la tlhaselo ea mokokotlo kapa stroke),
- Thibelo ea myocardial infarction,
- ho fokotsa tsoelo-pele ea coronary atherosulinosis,
- fokotsa kotsi ea lits'ebetso tsa revascularization.
Litaelo tsa ho sebelisoa
"Simvastatin" e nkuoa ka molomo, ka nako ea mantsiboea 1 ka letsatsi e kopane le palo e hlokahalang ea metsi. Nako ea ho sebelisa moriana ha e hloke ho amahanngoa le lijo.
Pele a qala kalafo, mokuli o fuoa lijo tsa hypocholesterol, tse lokelang ho bonoa nakong eohle ea kalafo.
Bakeng sa kalafo ea hypercholesterolemia, tekanyetso e khothalletsoang ea "Simvastatin" e tsoa ho 10 ho isa ho 80 mg hang ka letsatsi ka shoalane. Bakeng sa bakuli ba nang le anomaly ena, tekanyo ea pele ea moriana e khothalletsoang ke 10 mg. Tekanyo e phahameng ea letsatsi le letsatsi ke 80 mg.
Khetho (phetoho) ea lethal dose e hlokahala nako le nako ea libeke tse 4. Ho bakuli ba bangata, phello e nepahetseng ea kalafo ea atleha ha o sebelisa moriana o noang tekong ho fihla ho 20 mg / ka letsatsi.
Phekolo ea bakuli ba nang le lefu la pelo kapa e kotsing e kholo ea kholo ea bona, litekanyetso tse sebetsang tsa lithethefatsi ke 2040 mg / ka letsatsi. Ntlheng ena, lethal dose le khothalelitsoeng ho bakuli ba joalo ke 20 mg / letsatsi. Khetho (phetoho) ea lethal dose e lokela ho etsoa nako le nako ea libeke tse 4. Haeba ho hlokahala, lethalinyana le ka eketsoa ho 40 mg / ka letsatsi.
Bakeng sa bakuli ba nkang verapamil kapa amiodarone ka mokhoa o kopaneng le Simvastatin, tekanyetso ea letsatsi le letsatsi ha ea lokela ho feta 20 mg.
Bakeng sa bakuli ba nang le ho fokola ha 'mele ka tsela e itekanetseng kapa e fokolang, hammoho le bakuli ba tsofetseng, phetoho ea litekanyetso tsa lithethefatsi ha e ea hlokahala.
Ho batho ba nang le homozygous hereditary hypercholesterolemia, tekanyetso ea letsatsi le letsatsi ea Simvastatin ke 80 mg ho litekanyetso tse 3 tse arohaneng (20 mg hoseng, 20 mg ka thapama le 40 mg ka shoalane) kapa 40 mg ka shoalane hang ka letsatsi.
Bakeng sa bakuli ba nang le bothata ba ho phekola renal ba sa foleng kapa ba amohela cyclosporine, gemfibrozil, danazol kapa fiber e meng (ntle le fenofibrate), hammoho le nicotinic acid e kopaneng le moriana, tekanyo e phahameng e khothalletsoang ea lithethefatsi ha ea lokela ho feta 10 mg / letsatsi.
Ketso ea pharmacological
"Simvastatin", litaelo tsa tšebeliso li tsebisa ka sena, - moemeli ea fokotsang lipid a fumanehang ka mokhoa o tsoang sehlahisoa sa belisoa Aspergillus terreus ke lactone e sa sebetseng, o fepuoa 'meleng ho theha hydroxy acid e tsoang ho eona. Metabolite e sebetsang e thibela 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductase), enzyme e thusang ho theoa ha mesvalonate ho tloha HMG-CoA.
Ho tloha ha ho fetoloa hoa HMG-CoA ho mevalonate ke bohato ba pele moqoqong oa k'holeseterole, ts'ebeliso ea simvastatin ha e bake ho bokellana ha "sterols" tse nang le chefo 'meleng. HMG-CoA e tšelisoa habonolo ho acetyl-CoA, e amehang lits'ebetsong tse ngata tsa mantlha 'meleng.
"Simvastatin" e baka ho fokotseha hoa maemo a plasma a triglycerides (TG), lipensiproteins tse tlase (LDL), li-lipoproteins tse fokolang haholo (VLDL) le mefuta e felletseng ea li-hypercholegerolemia, e nang le litaba tse ngata tsa hyperlipidemia. kotsi factor) ka lebaka la thibelo ea synthetic ea cholesterol ka har'a sebete le keketseho ea palo ea li-receptor tsa LDL bokong ba sele, e lebisang ho ho nyoloheng le ho eketseha ha catabolism ea LDL.
E eketsa litaba tsa lipoprotein tse phahameng (HDL) le ho fokotsa karolelano ea LDL / HDL le cholesterol e akaretsang / HDL. Ha e na phello ea mutagenic. Qaleho ea ponahatso ea phello ke libeke tse peli kamora ho qala taolo, kalafo e phahameng e fumaneha kamora libeke tse 'ne tse tšeletseng.
Tšusumetso e pheella ka kalafo e tsoelang pele, ka ho khaotsa ho phekoloa, litaba tsa k'holeseterole butle-butle li khutlela boemong ba tsona ba pele.
Litlamorao
Phekolo e ka baka nts'etsopele ea litlamorao tse sa rateheng tse kang:
- phokolo ea mali
- palpitations
- dyspepsia
- alopecia
- lekhopho la letlalo
- ho hlohlona
- ho hloka boroko
- paresthesia
- ho senyeha hoa mohopolo
- mesifa ea mesifa
- ho tsekela
- hlooho e bohloko
- peripheral neuropathy,
- ho hloleha ha renal haholo (ka lebaka la rhabdomyolysis),
- pancreatitis
- hepatitis
- fokotseha potency
- bofokoli
- bohloko ba ka mpeng
- lets'ollo
- ho nyekeloa, ho hlatsa,
- botlaela
- ho sokela
- ho se sebetse hantle ha sebete,
- myasthenia gravis
- asthenia
- myalgia
- myopathy
- cholestatic jaundice,
- mesifa ea mesifa
- rhabdomyolysis,
- tlolo ea tatso
- pono e fifalitsoeng ea pono
- nts'etsopele ea hypersensitivity syndrome (angioedema, lupus-like syndrome, polymyalgia rheumatism, vasculitis, dermatomyositis, thrombocytopenia, eosinophilia, eketseha ESR, ramatiki, arthralgia, urticaria, photosensitivity, flush ea sefahleho, ho hema ha moea.
Analogues ea lithethefatsi "Simvastatin"
Litlhaku tse felletseng nthong e sebetsang:
- Simlo.
- Sinkard.
- Holvasim.
- Simvacol.
- Simvalimite.
- Zorstat.
- Bareki
- Simvor.
- Simgal.
- Zokor forte.
- Simvakard.
- Simvastatin Chaikafarma.
- Simvastol.
- Zokor.
- Simvastatin Zentiva.
- Actalipid.
- Vasilip.
- Vero Simvastatin.
- Simvastatin Pfizer.
- Atherostat.
- Simvastatin Fereyn.
Sehlopha sa li-statins se kenyeletsa lithethefatsi:
- Tulip.
- Holvasim.
- Holetar.
- Atomax
- Leskol forte.
- Mertenil.
- Bareki
- Pravastatin.
- Rovacor.
- Liptonorm.
- Lovacor.
- Vasilip.
- Atoris.
- Vazator.
- Zorstat.
- Cardiostatin.
- Lovasterol.
- Mevacor.
- Roxer.
- Lipobay.
- Lipona.
- Rosulip.
- Tevastor
- Atorvox.
- Crestor.
- Lovastatin.
- Medostatin.
- Atorvastatin.
- Leskol.
- Liprimar.
- Rosuvastatin.
- Akorta.
- Lipostat.
- Lipoford.
- Rosucard.
- Anvistat.
- Torvazin.
- Apextatin.
- Torvacard.
- Atherostat.
- Atocord.
Maemo a phomolo le theko
Theko e tloaelehileng ea Simvastatin (matlapa a 10 mg No. 30) Moscow ke li-ruble tse 44. Ho la Kiev, o ka reka moriana (20 mg No. 28) bakeng sa li-h Hypnias tse 90. Kazakhstan, litlhare li fana ka analogue ea Vazilip (10 mg No. 28) bakeng sa 2060 tenge. Ho thata ho fumana moriana Minsk. E fumaneha ho lithekisi ka lengolo la ngaka.
About litlhahlobo tsa bakuli "Simvastatin" li fapana. Bareki ba bang ba tiisa hore meriana e hlile e theola cholesterol, empa ka nako e ts'oanang ba hlalosa mefuta e fapaneng e fapaneng e khahlanong le semelo sa phekolo ea hypocholesterol kaofela. Bakuli ba nang le pancreatitis e sa foleng, ba hlokomela keketseho ea khafetsa ea linako tse eketsehileng nakong ea kalafo. Ka kalafo ea nako e telele, ho na le phetoho pontšong ea lipid hore e be betere.
Maikutlo a lingaka le 'ona a arolelanoa. Ba bang ba hlokometse hore moriana o phekola cholesterol ka katleho mme o sebetsa e le mokhoa o motle oa ho thibela atherosclerosis. Ba bang ba lumela hore lithethefatsi li felile, li fanoa ka ho teba ha maikutlo a mabe le ponahalo ea 'maraka oa litlhare oa Atorvastatin le Rosuvastatin, e leng lithethefatsi tse ncha tsa motsoako.
Ho sebelisana le lithethefatsi tse ling
Ts'ebeliso e ts'oanang ea lithethefatsi tse khahlanong le antimycotic joalo ka ketoconazole, itraconazole, tšebeliso ea erythromycin, cytostatics, tekanyetso e kholo ea Vitamin PP (nicotinic acid) ke khang ea ho haptjoa ha Simvastatin. Lithethefatsi tsena tsohle li na le ts'oaetso e phahameng ea myopathies le mathata a mang a mesifa litla-morao. Ha li fanoa ka mokhoa o ts'oanang, ts'oaetso ea tsona ea mesifa e eketsoa, ka hona e batla e imena khafetsa maqhubu a likarolo tsa rhabdomyolysis.
Ka tumellano e ts'oanang ea Simvastatin e nang le lithethefatsi tsa anticoagulant (warfarin, fenprocoumone), ho hlokahala hore ho hlahlojoe coagulogram ea mali khafetsa, kaha li-statins li eketsa phello ea li-anticoagulants. Phetoho ea litekanyetso kapa ho tlohela lithethefatsi e etsoa kamora taolo ea INR.
Ha ho kgothaletswe ka matla ho sebelisa lero la morara ka nako ea kalafo e fokotsang lipid ka lipalo. Boholo bo lumelletsoeng bo fihla ho 250 ml ka letsatsi. Seno sena se secha se na le protheine ea CYP3A4 inhibitor, e fetolang pharmacodynamics le pharmacokinetics ea Simvastatin.
Likarolo tsa ts'ebeliso
Simvastatin ke setlhare se nang le mefuta e mengata ea litla-morao tsa meriana le litla-morao, ka hona se laetsoe ke ngaka feela, ho latela lipontšo tse thata, mme se hasoa libakeng tsa meriana ka taelo ea ngaka feela. Nakong ea kalafo, matšoao a ts'ebetso ea mali a kopantsoeng le mali (INR, APTT, nako ea ho ts'oaroa), profid ea lipid, ts'ebetso ea sebete (ALT, Enst enzymes) le ts'ebetso ea liphio (tlhahiso ea tlhahiso ea tlhahiso eaine, CPK) e hlahlojoa.
Theko ea lithethefatsi
Theko ea simvastatin e leka-lekaneng ebile e theko e tlaase bakeng sa mokuli leha e le ofe. Ho ipapisitsoe le tikoloho le maano a k'hothone ea lithethefatsi, theko e ka fapana. Ka karolelano, litšenyehelo tsa lithethefatsi tsa Russia ke:
- Motsoako 10 mg, likotoana tse 30 ka pakete - ho tloha ho 40 ho isa ho li-ruble tse 70.
- Motsoako 20 mg, likotoana tse 30 ka pakete - ho tloha li-ruble tse 90.
Lithekeng tsa Seukraine, theko ea Simvastatin ke 20-25 UAH le 40 UAH bakeng sa tekanyetso ea 10 le 20 mg, ka ho latellana.
Li-analog tsa simvastatin
Simvastatin e na le sehlopha kaofela 'marakeng oa litlama lipapatso tse felletseng - li-enjene tlasa mabitso a mang a khoebo. Tsena li kenyelletsa Vasilip, Aries, Alkaloid, Simlo, Simvastatin C3, Simgal, Vertex, Simvastol, Zokor. Lithethefatsi tsena ke li-synonyms 'me li ka laeloa ho latela khetho ea ngaka ka boeona, ho sebetsa ha eona ka lichelete le mekhoa eo motho a nang le eona ka phello ea lithethefatsi ho mokuli ea itseng.
Ke eng betra simvastatin kapa atorvastatin
Simvastatin le Atorvastatin ha se ntho e tšoanang. Meriana ena ke ea meloko e fapaneng ea li-statins: Atorvastatin - oa pele, Simvastatin - oa boraro. Li fapana linthong tse sebetsang, matšoao, li-contraindication, ho ikhethang ha tšebelisano le lisebelisoa tse ling tsa bongaka.
Setlahare ka seng se na le niche ea sona ea kalafo le melemo ea sona, ka hona ho fosahetse ho se bapisa. Atorvastatin ke sethethefatsi se sebetsang le se potlakileng se sebetsang ka potlako. Ka hona, haeba ho hlokahala, ho amohela liphetoho tse ntle kapele, o fuoa monyetla. Leha ho le joalo, simvastatin, ke setlhare se bobebe se fanang ka litlamorao tse fokolang mme se amoheloa hore se sebelisoe mehatong e bonolo ea methapo ea methapo le sebete, ho fapana le Atorvastatin.
Phapang ke efe pakeng tsa simvastatin le rosuvastatin
Pakeng tsa simvastatin le rosuvastatin ho na le phapang ea lintho tse sebetsang, boemo ba ts'ebetso, lipontšo, li-contraindication, litla-morao le theko ea theko. Rosuvastatin e sebelisoa khafetsa ho tloha ponong ea thibelo ho bakuli ba nang le nalane e boima ea tsamaiso ea pelo le methapo.
Tlhahlobo
Litlhahlobo tsa lingaka le bakuli ba nkang Simvastatin ha li nke lehlakore. Lingaka li hlokomela bonolo ba moriana - litla-morao tse matla tse bakoang ke lona, li tsamaisana hantle le meriana e meng. Monyetla o moholo oa sethethefatsi ke monyetla oa ho khethoa ha ona le mafu a tšoanang le a liphio kapa sebete ka ponts'o e bonolo kapa e leka-lekaneng ea tsona. Leha ho le joalo, ts'ebetsong ea simvastatin e batla e le tlase ka tsela e nyane ho li-analogues tsa meloko e meng ea li-statins, ka hona, ha e sebelisoe hangata ho phekolo e mabifi.
Pharmacodynamics le pharmacokinetics
Simvastatin e na le sekhahla se phahameng sa ho monya. Khatiso e kholo e tlalehiloe kamora lihora tse 1.5-2,5, empa kamora lihora tse 12 e fokotseha ka 90%. Ho protheine ea plasma, karolo e sebetsang e khona ho tlama ho 95%. Bakeng sa simvastatin le metabolism phello e ikhethileng ea "phallo ea pele" e bonahala ka ts'ebetso ea hepatic, ha, ka lebaka la hydrolysis, e sebetsang e tsoang ho eona, beta-hydroxy acid, e thehoa. Mokhoa o moholo oa ho pepesa ke ho kena ka mpeng. Ka sebopeho se sa sebetseng, karolo ea leshome le metso e mehlano ea ntho e sebetsang e epolloa ka sistimi ea renal.
Mokhoa oa ho nka simvastatin?
Tekanyetso ea letsatsi le letsatsi ea lithethefatsi tsena ho batho ba baholo ke 1 t. (20-40 mg.) 1 leq. ka letsatsi bakeng sa metsotso e 3040. pele o robala, o nwa metsi a mangata.
Tekanyo e phahameng ea letsatsi le letsatsi ha ea lokela ho feta 80 mg. (2 t.), Kaha sena se ka ama bophelo bo botle ba 'mele ka kakaretso.
Nako ea kalafo le tekanyetso ea moriana li khethoa ke ngaka e eang ka botlalo ka bomong ho mokuli ka mong, ho latela boteng ba lefu le itseng la 'mele.
Sebopeho le mofuta oa tokollo
Bahlomphehi, mg
Matlapa a 10/20/40 mg
simvastatin 10/20/40 mg
cellcose ea microcrystalline 70/140/210
ascorbic acid 2,5 / 5 / 7.5
setene sa gelatinized 33.73 / 67.46 / 101.19
stearic acid 1.25 / 2.5 / 3.75
lactose monohydrate 21/42/73
polyvinyl joala 2.33 / 4.66 / 6.99
silicon dioxide 0,75 / 1.50 / 2.25
titanium dioxide 0.97 / 1.94 / 2.91
Oxide e putsoa ea 0.28 / 0.56 / 0.84
oxide ea tšepe e khubelu 0,19 / 0.38 / 057
Tekanyetso le tsamaiso
Pele o qala kalafo, ho ja lijo tsa hypocholesterol hoa tlameha. Simvastatin e nkuoa ka molomo nako e le 'ngoe mantsiboea, e hlatsuoa ka metsi, ho sa tsotelehe lijo tse ngata. Tekanyetso li itšetlehile ka lebaka la ho khethoa ha matlapa:
- Hypercholesterolemia - tekanyetso ea pele ke 10 mg, boholo ke 80 mg. Phetoho ea moriana e etsoa nako e le 'ngoe ka khoeli.
- Ischemia, kotsi ea kholo ea eona ke 20-40 mg.
- Homozygous lefutso la hypercholesterolemia - 20 mg makhetlo a 3 ka letsatsi.
- Li-pathologies tse sa foleng tsa liphio - ha ho na ho feta 10 mg ka letsatsi ka mokhoa o tloaelehileng oa creatinine (3 0,31 ml / min e ka hlahisoang).
- Bakeng sa bakuli ba nkang Verapamil, Amiodarone - tekanyetso ea letsatsi le letsatsi ea 20 mg.
Litaelo tse khethehileng
Matsatsi a pele a 1-3 a ho nka Simvastatin, keketseho ea bilirubin maling le maemo a AST le ALT a ka bonoa. Ka lebaka lena, ho hlokahala ho etsa tlhahlobo ea ultrasound hang ka likhoeli tse 3 (ha u nka 80 mg kapa ho feta). Phekolo e emisa hang ha li-enzyme tsa sebete li feta tse tloaelehileng ka makhetlo a 3. Hypertriglyceridemia ea 1.4, mefuta e 5 ke khang ea tšebeliso ea moriana.
Lithethefatsi li ka baka kholo ea myopathy, litlamorao tsa tsona e le rhabdomyolysis, ts'ebetso ea ho hlaphoheloa ha renal. Matlapa a sebetsa hantle kalafong e rarahaneng ka li-sequestrant tsa bile acid, le monotherapy. Ho sebetsa hantle ha matlapa ho ka matlafatsoa ka ho sebelisa lijo tsa hypocholesterol. Ts'ebeliso ea lero la morara nakong ea kalafo ha e ratehe haholo.
Ho sebelisana le lithethefatsi
Litekanyetso tse phahameng tsa simvastatin le ho nka cyclosporine, danazole e ka baka rhabdomyolysis. Statin e ntlafatsa phello ea li-anticoagulants - Warfarin, Fenprokumon, e ka eketsang kotsi ea ho tsoa mali. Ts'oaetso ea Digoxin e eketseha ha e kopantsoe le takatso ea "statin. Ho thibetsoe ho nka matlapa a nang le gemfibrozil. Kotsi ea myopathy e bakoa ke ho kopana le litlhare tse latelang:
- Nefazodon.
- Erythromycin.
- Clarithromycin
- Li-immunosuppressants.
- Ketoconazole, Itraconazole.
- Fibrate.
- Nicotinic acid e tekanyetso e kholo.
- Li-inhibitors tsa HIV.
Bongata
Matšoao a tekanyetso e feteletseng ha a hlalosoe. Bakeng sa kalafo, ho hlokahala hore o hlohlelletsa ho hlatsa, ho hlatsoa mpa. Se latelang ke pheko ea syndromic ka ho hlokomela li-paramente tsa hepatic. Ka mathata a renal, ho khothalletsoa tšebeliso ea lithethefatsi tsa diuretic, tsamaiso ea methapo ea sodium bicarbonate. Hemodialysis ha e na thuso, empa e ka etsoa ha ho hlokahala. Ka rhabdomyolysis, hyperkalemia e hlaha, e hlokang ho kenella kahare ho calcium chloride le gluconate, insulin e nang le tsoekere.
Lipehelo tsa thekiso le polokelo
Lithethefatsi tsa statin ke sethethefatsi se laeloang. Lifekthering tse ling, lengolo la bongaka le ka 'na la se ke la hlokahala. Moqapi oa matlapa o khothaletsa ho boloka lithethefatsi sebakeng se lefifi, se pholileng ka mocheso oa likhato tse 15 ho isa ho 25. Sehlahisoa se lokela ho sireletsoa ka hloko ho bana. Bophelo ba sefuba sa ntho ke likhoeli tse 24 ho tloha ka letsatsi la ho lokolloa.
Li-analog le sebaka sa lithethefatsi Simvastatin
Ho na le lethathamo la lithethefatsi tse tšoanang ka sebopeho le ketso ea simvastine. Meriana ena e kenyelletsa:
- Vasilip ke analogue e phethahetseng ea sebopeho. E sebelisoa ho phekola hypercholesterolemia, thibelo ea ischemia.
- Simgal - e sebelisoa ho thibela nts'etsopele ea atherosclerosis, myocardial infarction.
- Zokor - e laetsoe ho fokotsa cholesterol ea plasma.
- Holvasim - e khothalletsoa bakeng sa kalafo ea hyperlipidemia e tsoakiloeng, ischemia e sa foleng.
- Sinkard - e sebelisoang ho tsitsisa ho potoloha ha kokoana-hloko ea khoele, e fokotsa monyetla oa lefu.
Boimana (le pelehi)
Simvastatin e hanyetsanoa ka letsoalo ea boimanahobane ho khona ho baka litlolo tse fapaneng tsa nts'etsopele ho masea a sa tsoa hlaha. Nakong ea kalafo, ts'ebeliso ea kemolo. Ha ho na data ea ho kenella ha ntho e sebetsang ka lebese la matsoele. Leha ho le joalo, ho bohlokoa ho hopola hore ho na le kotsi e kholo ea litlamorao tsa simvastatin ho bophelo bo botle ba ngoana.
Tlhahlobo mabapi le Simvastatin (maikutlo a lingaka, bakuli)
Litlhahlobo mabapi le Simvastatin liforong li fapane. Bakuli ba tiisa hore moriana o hlile o theola cholesterol, empa ka nako e ts'oanang o hlalosa karabelo tse fapaneng tse mpe khahlanong le semelo sa thuto eohle ea hypocholesterol. Bakuli ba nang le pancreatitis e sa foleng ba hlokomela keketseho ea khafetsa ea linako tse eketsehileng nakong ea kalafo. Ka kalafo ea nako e telele, ho na le phetoho pontšong ea lipid hore e be betere.
Litlhahlobo tsa lingaka lia arolelanoa. Ba bang ba lumela hore sethethefatsi ke sa "mohlokomeli oa khale" mme se iphetile, se fana ka karabelo e mpe, le ponahalo marakeng oa meriana. Atorvastatin le Rosuvastatine amanang le lithethefatsi tsa moloko o mocha. Ba bang ba hlokometse hore moriana o atleha ho theola cholesterol ka katleho mme o sebetsa e le mokhoa o motle oa ho thibela atherosclerosis.