Raws li kev txheeb cais ntawm kev noj tshuaj nyob thoob plaws ntiaj teb, thawj qhov chaw nrog cov paj tau zoo yog nyob ntawm cov statins txij li nws tau ntawv sau.
Atorvastatin yog thawj qhov tshuaj ntawm qhov kev txiav txim no. Cov tshuaj tau tsim tawm hauv lub Yim Hli 1985 hauv Tebchaws Yelemees.
Statins yog cov tshuaj uas tsim los tawm tsam hypercholesterolemia, thiab atherosclerosis kev tsim los ntawm nws. Lawv qhov kev txiav txim siab yog kho cov lipid profile ntsuas, kho qhov tsis xws luag ntawm phab ntsa vascular thiab txo nws cov o.
Cov nyhuv ntawm statins rau roj biosynthesis
Statins txo cov roj cholesterol los ntawm kev sib xyaw ua ke rau nws cov tshuaj lom neeg txoj sia hauv lub siab.
Rau kev nkag siab zoo ntawm qhov no, nws tsim nyog noj tag nrho cov txheej txheem rau theem.
Muaj ntau tshaj nees nkaum yam koom nrog hauv cov txheej txheem biosynthesis.
Rau qhov yooj yim ntawm kev kawm thiab kev nkag siab, tsuas muaj plaub ntu loj:
- thawj theem yog kev tsub zuj zuj ntawm muaj pes tsawg ntawm cov piam thaj hauv hepatocytes los pib qhov kev tawm tsam, tom qab ntawd cov enzyme HMG-CoA reductase pib muab tso rau hauv cov txheej txheem, nyob rau hauv kev cuam tshuam ntawm kev sib txuas uas hu ua mevalonate yog tsim los ntawm biotransformation;
- tom qab ntawd concentrated mevalonate koom nrog hauv cov txheej txheem phosphorylation, nws muaj nyob rau hauv kev hloov pauv ntawm phosphorus pawg thiab lawv ntes los ntawm adenosine tri-phosphate, rau cov synthesis ntawm lub zog;
- cov theem tom ntej - cov txheej txheem hws - nws muaj nyob rau hauv kev siv cov dej muaj txiaj ntsig thiab kev hloov pauv ntawm mevalonate rau hauv squalene, thiab tom qab ntawd mus rau hauv lanosterol;
- nrog kev tsim ntawm ob daim ntawv cog lus, cov roj carbon atom txuas nrog lanosterol - qhov no yog theem kawg ntawm kev tsim cov roj cholesterol uas tshwm sim hauv tshwj xeeb organelle ntawm hepatocytes - endoplasmic reticulum.
Statins cuam tshuam thawj theem ntawm kev hloov pauv, thaiv lub zog enzyme HMG-CoA reductase thiab yuav luag tag nrho nres mevalonate. Tus txheej txheem no yog tshwm sim rau tag nrho pawg. Yog li nws tau xub tsim los ntawm cov kws tshawb fawb German ntawm Pfizer hauv lub xyoo dhau los.
Tom qab ib xyoo caum ntawm kev sim tshuaj, statins tshwm sim hauv khw muag tshuaj. Thawj tus ntawm lawv yog qhov tshuaj xub pib Atorvastatin, qhov seem tau tshwm sim ntau tom qab thiab yog nws cov ntawv luam - cov no yog cov hu ua generics.
Tus txheej txheem ntawm kev ua haujlwm hauv lub cev
Tevastor yog plaub tiam statin muaj, raws li cov tshuaj nquag, rosuvastatin. Tevastor yog ib qho kev nyiam tshaj plaws los ntawm Atorvastatin hauv cov teb chaws CIS - nws cov neeg ua ntej.
Pharmacodynamics thiab pharmacokinetics piav qhia txog li cas Tevastor ua haujlwm tom qab nws nkag mus rau hauv tib neeg lub cev.
Kev nkag mus ntawm cov hnoos qeev hauv lub plab, cov yam khoom xyaw yog nqa los ntawm cov hlab ntshav thoob plaws lub cev thiab tsub zuj zuj hauv lub siab tom qab tsib teev. Ib nrab-lub neej yog nees nkaum teev, uas txhais tau tias nws yuav siv sijhawm plaub caug teev los ua kom pom tseeb. Cov tshuaj no dhau los ntawm cov txheej txheem hauv ntuj - cov hnyuv tshem tawm 90%, cov seem tshuav yog txia tawm los ntawm lub raum. Nrog kev siv cov tshuaj tsis tu ncua, qhov siab tshaj plaws ua kom tau lub zog tshwm sim rau ib hlis tom qab pib kho.
Yog tias tus neeg mob muaj mob ntev, cov teeb meem pharmacokinetic hloov:
- Nrog rau lub raum ua tsis zoo, thaum creatine tshem tawm txo 4 zaug los yog ntau dua, cov tshuaj ntawm rosuvastatin nce li 9 zaug. Hauv cov neeg mob rau mob hemodialysis, cov ntsuas no nce txog 45%;
- Hauv lub raum me thiab mob raum tsis ua haujlwm, thaum kev tshem tawm yog siab dua 30 millilitres ntawm ib feeb, qhov tseem ceeb ntawm cov tshuaj hauv plasma tseem nyob ntawm cov tshuaj kho mob;
- Nrog tsim lub siab tsis ua haujlwm, kev tshem tawm ib nrab ntawm lub neej nce ntxiv, uas yog, cov khoom siv txuam txuas mus txuas ntxiv kom ncig rau hauv cov ntshav. Qhov no tuaj yeem ua rau qaug dab peg, mob raum, thiab ua rau mob hnyav. Yog li, thaum kho, nws yuav tsum nruj siv cov tshuaj uas kws kho mob tau sau, txhawm rau txhawm rau tiv thaiv kev noj tshuaj ntau dhau thiab tsis pub dhau lub sijhawm mus ntsuas cov kev tswj;
Thaum siv cov tshuaj, nws yuav tsum nco ntsoov tias nyob rau hauv cov neeg ntawm cov haiv neeg Asian, qhov kev nthuav tawm ntawm rosuvastatin qeeb qeeb, yog li lawv yuav tsum tsuas yog cov tshuaj tsawg kawg nkaus.
Cov lus sib xyaw thiab cov ntawv ntau npaum
Cov tsos thiab cov ntsiab lus ntawm cov ntsiav tshuaj nws txawv nyob ntawm seb ntau npaum li cas.
Tevastor 5 milligrams - muaj cov duab sib npaug, xim ntawm kaj daj mus rau txiv kab ntxwv. Muaj cov kev tshoov siab ntawm ob sab ntawm lub ntsiav tshuaj: ntawm ib sab tes hauv daim ntawv N, ntawm qhov tod tes, tus naj npawb 5. Yog tias koj rhuav tshem cov ntsiav tshuaj, koj tuaj yeem pom cov xim dawb sab hauv, suav nrog lub rosuvastatin ntsev;
Tevastor 10 milligrams, 20 milligrams, 40 milligrams - cov ntsiav tshuaj npawv thiab cov tshuaj biconvex. Lub cav sau rau ntawm ib sab yog ib yam, ntawm tus lej nws sau rau tus muab tshuaj nyob hauv lub hlwv. Thaum lub sijhawm ua txhaum, lub chaw dawb yog tseem pom, npog nrog lub plhaub.
Cov tshuaj sib xyaw ntawm Tevastor yog ib yam zoo rau txhua koob tshuaj, qhov sib txawv tsuas yog hauv tus nqi ntawm cov nquag ua haujlwm thiab cov neeg zam:
- rosuvastatin calcium - cov tshuaj nquag, txwv tsis pub cov nquag enzyme uas hloov piam thaj rau hauv mevalonate;
- microcrystalline cellulose - lub ntsej muag o cov hmoov ci, qhia kom ua kom khov ntawm cov plab zom mov;
- lactose yog siv los ua qhov muab tub lim kom nce ntim thiab hnyav, nrog rau cellulose nrawm nrawm;
- povidone thiab crospovidone - phau ntawv thaiv kom ntseeg tau tias nqos zoo;
- sodium stearine fumarate - txhim kho kev muaj npliag, hloov kev ua haujlwm ntawm lub tshuab xovxwm los ntawm kev txo cov nplaum rau lub thev naus laus zis.
Ntxiv rau cov khoom siv no, cov tshuaj muaj cov xim liab thiab xim txiv kab ntxwv kom muab ntsiav tshuaj kom zoo nkauj.
Cov lus qhia rau kev siv tshuaj
Muaj ib daim ntawv teev qee qhov cim tseg ntawm kev siv tshuaj yeeb.
Tag nrho cov cim qhia tau qhia hauv cov lus qhia rau kev siv.
Cov lus qhia no yog ib qho tseem ceeb hauv kev ntim khoom ntawm cov tshuaj muag muag los ntawm cov khw muag tshuaj lub network.
Cov cim tseem ceeb rau kev siv tshuaj yog:
- Lub Koom Haum Me Nyuam Yaus (nrog nws tsuas yog lipoproteins uas tsis muaj tsawg yog txhawb nqa siab) thiab sib xyaw (lipoproteins uas tsis muaj ntau ntau kuj tau nce siab dhau) hypercholesterolemia. Tab sis tsuas yog nyob rau hauv rooj plaub thaum qhov kev nce ntawm kev ua haujlwm hauv lub cev, tso tseg cov kev coj ua tsis zoo thiab kev noj zaub mov tsis tau coj lub txiaj ntsig kom raug;
- Hypertriglycerinemia, nrog rau kev nce ntxiv hauv cov lipoproteins tsawg ntom, yog tias kev noj zaub mov tsis txig tsis txo cov roj cholesterol;
- Atherosclerosis - txhawm rau ua kom cov nyiaj lipoprotein ntau npaum li cas nyob rau hauv daim siab txo cov tshuaj ntawm cov roj cholesterol tsis zoo;
- Txhawm rau tiv thaiv kev txhim kho cov hlab plawv muaj teeb meem ntawm atherosclerosis: mob myocardial infarction, ischemic stroke, angina pectoris, tshwj xeeb tshaj yog nyob rau ntawm qhov muaj feem phom sij - haus luam yeeb, haus cawv, rog dhau ntawm 50 xyoo.
Cov lus qhia rau kev siv tsim kev pom tseeb kev noj tshuaj rau txoj kev noj tshuaj.
Noj ntawm qhov ncauj, haus dej kom ntau, tsis hais noj dab tsi, tsis noj losyog tsoo. Nws raug nquahu kom haus thaum hmo ntuj, vim tias thaum nruab hnub lub sijhawm tso tawm ntawm cov tshuaj tau nrawm dua, thiab cov dej ntau yog nws tawm ntawm lub cev.
Thawj qhov tshuaj yog 5 mg 1 zaug nyob rau ib hnub. Txhua lub hlis, nws yuav tsum tau tswj xyuas lipid thiab tus kws kho mob sab laj. Ua ntej pib kev kho mob, kws kho plawv yuav tsum muab cov lus qhia ua ntej nkag thiab piav qhia txog cov kev mob tshwm sim yuav tsum tsis txhob noj thiab nrhiav kev pab los ntawm lub tsev kho mob.
Tsis tas li ntawd, txhua lub sijhawm ntawm txoj kev kho nws yog ib qho tsim nyog yuav tsum ua raws li kev noj zaub mov hypocholesterol, thiab qhov no txhais tau tias nruj me ntsis rau qhov kev nqus ntawm cov rog, zaub mov kib, qe, hmoov thiab zaub mov qab.
Mob pathological rau ntawm lub cev
Cov kev mob tshwm sim yog cais raws li qhov nquag tshwm sim ntau zaus, tsis tshua muaj thiab tsis tshua muaj heev.
Nquag - ib kis ntawm ib puas tus neeg - kiv taub hau, mob ntawm lub tuam tsev thiab caj dab, kev loj hlob ntawm hom 2 mob ntshav qab zib, xeev siab, ntuav, tso quav tawm, mob leeg, mob asthenic;
Tsis tshua muaj - ib kis rau 1000 tus neeg - kev tsis haum tshuaj rau cov feem ntawm cov tshuaj los ntawm urticaria rau Quincke's edema, mob leeg mob rau daim tawv nqaij (ua mob rau ntawm tus txiav), tawv nqaij ua pob, ua pob txha myopathy;
Muaj tsawg kawg - 1/10000 tus neeg mob - rhabdomyolysis tshwm sim, qhov no yog qhov kev rhuav tshem cov leeg nqaij nrog kev tso cov protein tawm mus rau hauv cov hlab ntshav thiab qhov tshwm sim ntawm lub raum tsis ua haujlwm.
Cov kev ua tsis txuam nrog kev siv tshuaj yog cov xwm txheej hauv qab no:
- Cev xeeb tub - Rosuvastatin yog cov tshuaj lom rau lub cev hauv plab ntau heev vim tias, los ntawm kev thaiv qhov kev sib xyaw ntawm cov cholesterol, nws cuam tshuam nrog kev tsim ntawm phab ntsa. Qhov no, nyeg, yuav ua rau txoj kev loj hlob intrauterine qeeb qeeb, muaj ntau yam hauv nruab nrog cev, thiab ua pa nyuaj siab. Tus me nyuam hauv plab yuav tuag lossis tau yug los nrog qhov ua txhaum tsis zoo, yog li ntawd, nws tau hais kom siv lwm cov tshuaj rau cov neeg mob cev xeeb tub.
- Kev pub mis niam mis - qhov no tsis tau sim hauv cov kev tshawb fawb hauv chav kho mob, yog li qhov kev pheej hmoo tsis txaus ntseeg ua ntej. Lub sijhawm no, cov tshuaj yuav tsum tau tso tseg.
- Cov menyuam yaus thiab tub ntxhais hluas vim tias qhov tsis zoo ua rau lub cev txhawm rau kis tau tus kabmob tsis zoo, yog li ntawd, kev nkag mus rau 18 xyoo txwv tsis pub muaj.
- Mob raum tsis ua haujlwm.
- Kab mob ntawm daim siab, mob ceev lossis mob ntev.
- Hauv kev laus, nws yog ib qhov tsim nyog yuav tsum tau muab tshuaj rau kom ceev faj. Pib noj tshuaj 5 mg, qhov ntau tshaj tsis tshaj 20 mg rau ib hnub nyob rau hauv kev saib xyuas mob nkeeg nruj.
- Tom qab hloov khoom nruab nrog vim kev tsis sib xws ntawm cyclosporine, uas txwv qhov tsis lees txais cov tshuaj tiv thaiv thiab rosuvastatin.
- Ua ke nrog cov tshuaj anticoagulants, txij li Tevastor potentiates lawv qhov kev ua, nce prothrombin lub sijhawm. Qhov no tuaj yeem tiv thaiv nrog los ntshav sab hauv.
- Koj tsis tuaj yeem coj nws nrog lwm cov statins thiab hypocholesterolemic tshuaj vim kev sib xyaw ntawm pharmacokinetics.
- Lactose tsis txaus ntseeg.
Ib qho ntxiv, nws raug txwv tsis pub noj tshuaj yog tias tus neeg mob tau txais tshuaj tiv thaiv tsis haum rau ib qho twg ntawm cov tshuaj.
Cov ntaub ntawv hais txog statins yog muab hauv video hauv tsab xov xwm no.