Ngokusekelwe kwizibalo zokudla izidakamizwa emhlabeni wonke, indawo yokuqala enomugqa omkhulu kuhlala ama-statins selokhu lalinelungelo lobunikazi.
I-Atorvastatin umuthi wokuqala walesi senzo. Umuthi wenziwa ngo-Agasti 1985 eJalimane.
Izimo izidakamizwa eziklanyelwe ukulwa ne-hypercholesterolemia, kanye ne-atherosclerosis ekhula ngenxa yalokho. Isenzo sabo ukulungisa izinkomba zephrofayili ye-lipid, kwelapha iziphazamiso odongeni lwe-vascular futhi kunciphise ukuvuvukala kwayo.
Umphumela wama-statins ku-cholesterol biosynthesis
I-Statins yehlisa i-cholesterol yegazi ngokuzihlanganisa ku-biosynthesis yayo esibindini.
Ukuqonda kangcono lokhu, kufanelekile ukuthatha inqubo yonke ibe izigaba.
Kunezingxenye ezingaphezu kwezingamashumi amabili ezibandakanya inqubo ye-biosynthesis.
Ukuze kube lula ukutadisha nokuqonda, kunezigaba ezine kuphela:
- isigaba sokuqala ukunqwabelana kwenani elilinganayo le-glucose kuma-hepatocytes ukuqala ukusabela, emva kwalokho i-enzyme HMG-CoA reductase iqala ukufakwa kwinqubo, ngaphansi kwethonya lapho ikomidi elibizwa ngokuthi i-mevalonate lenziwa khona nge-biotransformation;
- ke i-mevalonate egxilile ibandakanyeka kwinqubo ye-phosphorylation, iqukethe ekudlulisweni kwamaqembu we-phosphorus kanye nokubanjwa kwawo yi-adenosine tri-phosphate, ekwakhiweni kwemithombo yamandla;
- isigaba esilandelayo - inqubo yokuvuselela - iqukethe ukusetshenziswa kancane kancane kwamanzi nokuguqulwa kwe-mevalonate ibe yi-squalene, bese kuba yi-lanosterol;
- ngokusungulwa kwezibopho eziphindwe kabili, i-athomu lekhabhoni linamathele ku-lanosterol - lesi yisigaba sokugcina sokukhiqizwa kwe-cholesterol esenzeka esikhungweni esikhethekile se-hepatocytes - i-endoplasmic reticulum.
Izimo zithinta isigaba sokuqala soguquko, zivimba ukuncipha kwe-HMG-CoA enzyme futhi kucishe kumise ngokuphelele ukukhiqizwa kwe-mevalonate. Le ndlela ijwayelekile kulo lonke iqembu. Ngakho-ke yaqalwa okokuqala ngososayensi baseJalimane ePfizer eminyakeni eyedlule.
Ngemuva kweshumi lokuvivinywa kwemitholampilo, ama-statin avele emakethe yamakhemisi. Owokuqala wabo kwakuyisidakamizwa sokuqala i-Atorvastatin, abanye bavele ngokuhamba kwesikhathi futhi bangamakhophi ayo - lawa abizwa ngokuthi ama-generics.
Umshini wokusebenza emzimbeni
I-Tevastor yi-statin yesizukulwane sesine enokuthi, njengento esebenzayo, i-rosuvastatin. I-Tevastor ingenye yezinto ezitholakala kakhulu kwe-Atorvastatin emazweni e-CIS - eyandulelayo.
I-Pharmacodynamics ne-pharmacokinetics zichaza ukuthi iTevastor isebenza kanjani ngemuva kokungena emzimbeni womuntu.
Ukungena ngaphakathi kolwelwesi lwesisu, isakhi esisebenzayo sithwalwa ukuphuma kwegazi emzimbeni wonke bese sinqwabelana esibindini ngemuva kwamahora amahlanu. Isigamu sempilo singamahora angamashumi amabili, okusho ukuthi kuzothatha amahora angamashumi amane ukukusula ngokuphelele. Umuthi udonswa ezindleleni zemvelo - amathumbu asusa ama-90%, inani elisele likhishwa yizinso. Ngokusebenzisa umuthi njalo, umphumela omkhulu wokwelapha ubonakaliswa inyanga ngemuva kokuqala kokwelashwa.
Uma isiguli sinezifo ezingamahlalakhona, amapharamitha we-pharmacokinetic ayaguquka:
- Ngokuhluleka okukhulu kwezinso, lapho imvume ye-creatine incipha amahlandla ama-4 noma ngaphezulu, ukuqina kwe-rosuvastatin kukhuphuka ngezikhathi eziyi-9. Ezigulini ezikwi-hemodialysis, lezi zinkomba zikhuphuka ziye kuma-45%;
- Ekwehlulekeni kwe-renal okuncane futhi okulinganiselayo, lapho imvume ingaphezu kwamamilimitha angama-30 ngomzuzu, ukuqoqwa kwezinto ku-plasma kuhleli ezingeni lezokwelapha;
- Ngokuhluleka kwesibindi okuthuthukisiwe, ukukhishwa okukhona kwengxenye yempilo kuyanda, okungukuthi, izingxenye ezisebenzayo ziyaqhubeka nokujikeleza egazini. Lokhu kungadala ukudakwa okungamahlalakhona, ukulimala kwezinso nobuthi obukhulu. Ngakho-ke, ngesikhathi sokwelashwa, kuyadingeka ukuhambisana ngokuqinile nemiyalelo kadokotela, ukuvikela ukusetshenziswa okweqile kanye nesikhathi sokudlula izivivinyo zokulawula;
Lapho usebenzisa umuthi, kufanele kukhunjulwe ukuthi kubantu bomjaho wase-Asia, ukumbiwa kwe-rosuvastatin kuyancipha, ngakho-ke kufanele banikezwe imithamo emincane kuphela.
Ukuqanjwa nefomu lomthamo
Ukubukeka nokuqukethwe kwamatafula kuyahlukahluka ngokuya ngomthamo.
Ama-milligram ama-Tevastor 5 - anomumo oyindilinga, umbala ukusuka ophuzi okhanyayo kuya ku-orange. Kukhona okuvelayo ezinhlangothini zombili zethebhulethi: ngakolunye uhlangothi, ngesimo sencwadi uN, ngakolunye uhlangothi, inombolo 5. Uma wephula isibhebhe, ungabona umnyombo omhlophe ngaphakathi, oqukethe usawoti we-rosuvastatin;
Ama-milligram ama-Tevastor 10, ama-milligram angama-20, ama-milligram angama-40 - amaphilisi ama-pink ayindilinga kanye ne-biconvex. Ukuqoshwa ohlangothini lwezinhlamvu kuyafana, ohlangothini lwamadijithi luhambisana nomthamo okhonjiswe ku-blister. Ngesikhathi sephutha, isikhungo esimhlophe siyabonakala, simbozwe ngegobolondo.
Ukwakheka kweTevastor kuyefana kuwo wonke umthamo, umehluko kuphela enanini lezinto ezisebenzayo nabahlanganyeli:
- i-rosuvastatin calcium - into esebenzayo, ivimba i-enzyme esebenzayo eguqula ushukela ube mevalonate;
- i-microcrystalline cellulose - i-pound baking evuvukalayo, eyethulwa ukukhulisa ubumbano ethambekeni lesisu;
- I-lactose isetshenziswa njenge-filler ukwandisa ivolumu nesisindo, kanye ne-cellulose kusheshisa ukubola;
- i-povidone ne-crospovidone - isigaxa sokuqinisekisa ukugwinya okunethezekile;
- sodium stearine fumarate - kuthuthukisa ukuqina, kusiza umsebenzi emshinini wokuphrinta ngokunciphisa ukunamathela kwizixhobo.
Ngaphezu kwalezi zingxenye, umuthi uqukethe amadayi apinki nawolintshi ukunikeza amaphilisi umbala omnandi.
Imiyalo yokusebenzisa umuthi
Kunohlu oluthile lwezinkomba zokusebenzisa umuthi.
Zonke izinkomba zikhonjiswe kwimiyalo esetshenzisiwe.
Lo mhlahlandlela uyingxenye ebophekile ekufakweni kwezidakamizwa ezithengiswa ngenethiwekhi yasekhemisi.
Izinkomba eziphambili zokusebenzisa umuthi yilezi:
- Amabanga aphansi (anama-lipoprotein aphansi kuphela aphakanyisiwe) futhi axutshwe (ama-lipoprotein aphansi kakhulu nawo aphakeme kakhulu) i-hypercholesterolemia. Kepha kuphela esimeni lapho ukwanda kokuzivocavoca ngokomzimba, ukulahla imikhuba emibi nokudla kokudla kungalethi umphumela ofanele;
- I-Hypertriglycerinemia, ngokunyuka ngasikhathi sinye kwama-lipoprotein aphansi, uma ukudla okuqinile kungazange kwehlise i-cholesterol;
- I-Atherossteosis - ukwandisa inani lama-recensor aphezulu we-lipoprotein ephezulu esibindini ukunciphisa ukwehla kwe-cholesterol embi;
- Ukuvimbela ukuthuthukiswa kwezinkinga zenhliziyo ze-atherosclerosis: infarction ye-acute myocardial, stroke ischemic, i-angina pectoris, ikakhulukazi lapho kunezici zobungozi - ukubhema, ukusebenzisa kabi utshwala, ukukhuluphala ngokweqile, iminyaka yobudala engama-50.
Imiyalo yokusebenzisa isungula imithamo evumelekayo yokuphuza umuthi.
Thatha ngomlomo, uphuze amanzi amaningi, kungakhathaleki ukudla, ngaphandle kokuhlafuna noma ukugqekeza. Kunconywa ukuphuza ebusuku, ngoba phakathi nosuku isidumbu somuthi siyasheshiswa, futhi inani elikhulu laso likhishwa emzimbeni.
Umthamo wokuqala ngu-5 mg 1 isikhathi ngosuku. Njalo ngenyanga, kuyadingeka ukulawula ukulawulwa kwe-lipid nokubonisana nodokotela. Ngaphambi kokuqala ukwelashwa, udokotela wentliziyo uphoqelekile ukuba anikeze umhlahlandlela wokwamukelwa futhi achaze ukuthi yimiphi imiphumela emibi okufanele ayeke ukuthatha nokufuna usizo esikhungweni sezokwelapha.
Ngaphezu kwalokho, sonke isikhathi sokwelashwa kuyadingeka ukunamathela ekudleni kwe-hypocholesterol, futhi lokhu kusho ukukuvimbela ngokuphelele ukungena kwamafutha, ukudla okuthosiwe, amaqanda, ufulawa nokudla okumnandi.
Imiphumela ebuhlungu emzimbeni
Imiphumela emibi ihlukaniswa ngokuya ngemvamisa yokwenzeka njengokujwayelekile, iyivelakancane futhi iyivelakancane.
Imvamisa - icala linye ngabantu abayikhulu - isiyezi, izinhlungu emathempelini nasentanyeni, ukuthuthukiswa kohlobo 2 lwesifo sikashukela, isicanucanu, ukuhlanza, isihlalo sokucasulwa, ubuhlungu bemisipha, i-asthenic syndrome;
I-Rare - icala elilodwa kubantu abayi-1000 - ukusabela komzimba ezingxenyeni zomuthi kusuka ku-urticaria kuya ku-edema kaQuincke, i-pancreatitis eshubile (ukuvuvukala kwamanyikwe), ukuqubuka kwesikhumba, i-myopathy;
Kuqabukela kakhulu - 1/10000 amacala - i-rhabdomyolysis kwenzeka, lokhu kungukubhujiswa kwezicubu zomzimba ngokukhishwa kwamaprotheni abhujisiwe egazini nokuvela kokwehluleka kwe-renal.
Ukuxhumana kokusetshenziswa kwomuthi ngamacala alandelayo:
- Ukukhulelwa - I-Rosuvastatin inobuthi obukhulu kumntwana ngoba ukuvimba ukwakheka kwe-cholesterol, kuphazamisa ukwakheka kodonga lweseli. Lokhu, kuzoholela ekubuyiselweni kokukhula kwe-intrauterine, ukwehluleka kwezitho eziningi, kanye nesifo sokuphefumula sokuphefumula. I-fetus ingafa noma izalwe inezinkinga ezimbi kakhulu, ngakho-ke, kunconywa ngokuqinile ukuthi eminye izidakamizwa inqunyelwe isiguli esikhulelwe.
- Ukuncelisa amabele - lokhu akuhloliswanga ezifundweni zomtholampilo, ngakho-ke ubungozi abubonakali. Ngalesi sikhathi, umuthi kufanele ushiywe.
- Izingane nentsha ngenxa ye-psychanogeneis engaphelele ingathola ukungasebenzi, ngenxa yalokho, ukwamukelwa iminyaka eyi-18 akuvunyelwe.
- Ukwehluleka okukhulu kwezinso.
- Ukulimala kwesibindi, okubi kakhulu noma okungamahlalakhona.
- Ebudaleni, kubalulekile ukunquma umuthi ngokuqapha. Ukuthoma kokuthathwa kwe-5 mg, okungeqi ngaphezu kwama-20 mg ngosuku ngaphansi kokuqashwa okuqinile kwezokwelapha.
- Ngemuva kokufakelwa kwesitho ngenxa yokungasebenzi kwe-cyclosporine, okuthinta ukusabela kokungavunyelwa kanye ne-rosuvastatin.
- Ngokubambisana nama-anticoagulants, njengoba iTevastor inika amandla isenzo sabo, yandisa isikhathi se-prothrombin. Lokhu kungashiswa ukopha kwangaphakathi.
- Awukwazi ukuyithatha namanye ama-statins nezidakamizwa ze-hypocholesterolemic ngenxa yokuhlanganiswa kwe-pharmacokinetics.
- Ukungabekezelelani kwe-lactose.
Ngaphezu kwalokho, kwenqatshelwe ukuphuza umuthi uma isiguli sine-hypersensitivity reaction kunoma yiziphi izingxenye zomuthi.
Imininingwane mayelana nama-statin inikezwe kuvidiyo kule ndatshana.
