"Cyclosporin": yokusetshenziswa. "Cyclosporin A": imfundo. Eye lehla ne cyclosporine

Emvelweni, zikhona izinto okwazi abacindezela amasosha omzimba amaselula kanye humoral emzimbeni isilwane eyenziwa T-lymphocyte. Kungenzeka ngempumelelo ukufeza isitho Ukufakelwa futhi ukwelapha izifo ezihambisana ne kahle omzimba. Omunye cyclosporin esinjalo compounds zemvelo.

incazelo

Ukuvulwa efana ezihlobene cwaningo amagciwane fungal Tolypocladium inflatum futhi Cylindrocarpon lucidum. Kwemiqondo ejenti eziphila abakhuthele ezifana cyclosporin A no C abonise umsebenzi immunological ngokumelene egazi lymphocytic. Lesi sici eyaqala ukutholwa ngawo-1972 ososayensi kusukela "Sandoz" we lab Swiss. Kuye kwatholakala ukuthi isakhiwo amakhemikhali cyclosporine abathathi hlangothi lipophilic endecapeptide eyindilinga nge imakwe ethize isinyathelo immunosuppressive.

Kusekelwe izidakamizwa abe isenzo abakhethayo ku T-lymphocyte ukucindezela amasosha omzimba amaselula kanye humoral. igazi Cyclosporin ithiya ukukhiqizwa kwe lymphokines, okuyinto kunciphisa umsebenzi lymphocyte, kodwa akunamthelela inqubo hematopoiesis kanye nomsebenzi phagocytes, okubonisa ukuthi isenzo ukukhetha enkompolo emzimbeni.

amafomu Isikali

It has ezizofakwa kwikhithi ngemithi equkethe cyclosporin, imfundo manual. Phakathi kwezinye izinto, sifaka imininingwane kwifomu ukukhululwa zomuthi. Amalungiselelo yalolu ketshezi akhiqizwa ifomu:

• Amaphilisi ezithambile nge umthamo 25, 50 no-100 angu;
• oludakayo isixazululo ngomlomo angu 100 cyclosporin ml isixazululo ngasinye;
• uwoyela isixazululo ngomlomo angu 100 cyclosporin ml isixazululo ngasinye;
• ukugxilisa ingqondo womshini isixazululo ukumnika abaphathi nge 50 futhi 650 amamiligremu angaba cyclosporin ngemililitha ngayinye;
• ngeso lehla ne micrograms 500 ngemililitha ka cyclosporine ngayinye.

Kuye ukusetshenziswa ifomu Isikali kuzohluka: kwezokuphatha yangaphakathi, ngoba umjovo, ngoba isicelo nezokusigcoba.

Kukholakala ukuthi izinga ukumuncwa ingxenye esebenzayo, isikhathi ekuqongeleleni emakamu eliphakeme e igazi capsule futhi ikhambi reception yangaphakathi ezibhekwa okulingana.

Izidakamizwa "Tacrolimus": nozakwabo

Ezimakethe ezithaka imithi kukhona izinhlobo eziningi zezidakamizwa ekhiqizwa ngendlela efanayo eyenza imithi, futhi unikeze kakhulu umphumela ofanayo. Isithako asebenzayo okukukho cyclosporine. Yokusetshenziswa bomcondvofana immunodepressorov ucabangela womabili izidakamizwa ukucindezela ukusabela mzimba.

Phakathi nemithi encapsulated e ethambile gelatin igobolondo kanye nezixazululo ketshezi Isidakamizwa yasekuqaleni "Sandimmun Neoral" ezivezwa nkampani Swiss ezithaka imithi "Novartis". I nezinye izidakamizwa kubhekwe kabusha isithombe adalwe ukwakheka kuqala nge cyclosporin izidakamizwa. Analogue ezifana izidakamizwa "Cyclosporin hexane", "Ekoral", "Tsiklopren" "Cyclosporin A", ekhiqizwa ngesimo amaphilisi noma isixazululo imijovo yangaphakathi noma lwamukela.

injongo yabo eyinhloko - ukunciphisa noma ukubandlululwa ukufakelwa kwezitho zangaphakathi noma umnkantsha. Thokozisa them izifo sokuhlasela kwamasosha omzimba, njengoba kufakazelwa exhunywe izidakamizwa "Tacrolimus" yokusetshenziswa. Analogs anezici efanayo, futhi izinkomba ukusetshenziswa.

Lo mshini wezenzo "Cyclosporin A" izidakamizwa

Ngesikhathi inhliziyo yabo bonke isenzo izidakamizwa immunosuppressive kuba nomphumela abakhethayo ku T-lymphocyte. Ayikho ngaphandle kanye izidakamizwa "Cyclosporin A". Umhlahlandlela ngokuningiliziwe ihlanganisa izindlela main imiphumela pharmacodynamic esemazweni esebenzayo, okuyinto sibopha ukuthi zokwakheka yokwamukela phakathi emangqamuzaneni. Inciphisa ukukhiqizwa interleukin futhi interferon kunciphisa ukubonakaliswa receptor ngoba IL-2.

Nomuthi "Cyclosporin A" kunciphisa ukukhiqizwa kwamasosha omzimba sibhekiswe amaseli ayo nezicubu, lapho cabanga alien futhi ababhubhise. Lesi sici ikuvumela ukunciphisa iziyaluyalu immunological nokwehlisa umsebenzi izifo sokuhlasela kwamasosha omzimba.

kahle Omkhulu "Cyclosporin A" maqondana allograft. Isizathu sokuba ukwenqaba kwezicubu utshalwe eziyishumi nemitshingo iyona ukusebenza mzimba T cell elakhiwe. Amemezela ngentshiseko uqale lekufanele akhicitwe ngaphansi umphumela ukufakelwa antigen futhi kuthinte amaseli milisa, okwaholela ekufeni kwabo.

Isenzo immunodepressora kuholela ivimbela isixhumanisi T-amaseli bese okusithiyayo of T-lymphocyte ziphakame ukusabela mzimba. Ngenxa yalokho, ukuphumelela izidakamizwa "Cyclosporin A" (umsebenzisi ibonisa ukuthi leli) kwenzeka kuphela ngemva nokucindezela ukufakelwa antigen. Ngokubhubhisa ubuhlobo antigen omzimba necrosis uvinjelwe ka utshalwe izitho amaseli.

Kungani ukusebenzisa

Izinkomba Zokusetshenziswa "Tacrolimus" yokusetshenziswa zomuthi ihlukaniswe izigaba ezimbili.

Esokuqala ukufakelwa noma ukufakelwa of donor izicubu kanye izitho. A imithi zokunqanda ukwenqaba isitho noma izicubu podsazhennogo. Ngokuvamile, grafts wasebenzisa isikhumba, inhliziyo, umnkantsha, emaphashini, isibindi, izinso, amanyikwe. Mhlawumbe ukusetshenziswa kwezidakamizwa ukuqeda kwenqatshwa lapho namanye amanxusa immunosuppressive. Isigaba sesibili kuyinto isifo sokuhlasela kwamasosha omzimba ifomu ezinzima. Futhi ejenti lomisiwe kahle eliphansi nezinye izidakamizwa.

Ngayiphi izifo esiphatha ngayo izidakamizwa "Tacrolimus"? ukuze isetshenziswe izinkomba kuhlanganise imfundo inike amafomu okukhulu atopic dermatitis kanye neurodermatitis, ukubonakaliswa psoriasis, i-rheumatoid arthritis, nokuthi kuthinta emalungeni ezincane avuvukele. ukusetshenziswa Kunokwenzeka uveitis ezingxenyeni maphakathi kanye ezingemuva iso lapho choroid elikhanyayo futhi i-retina, futhi nephrotic syndrome ne-hormone okuthiwa i-gormonoustoychivoy nemvelo.

imithetho yokwemukelwa

ukwelashwa izidakamizwa Kunconywa kuphela ngaphansi kweso lwezokwelapha esibhedlela. Ngokuvamile ukusebenzisa isicelo sangaphakathi noma ukuvuza emthanjeni, nakuba kubonelelwa kakhulu ukuthola isixazululo bomlomo noma amaphilisi.

Tableware, esetshenziselwa ukulungiselela isixazululo umjovo emthanjeni kumele ezenziwe ngengilazi, esikhundleni chloride polyvinyl ukugwema ukusabela ngamafutha ocolisekileyo.

Ukuze dilution we CONCENTRATE wasebenzisa bokuphila amaphesenti 0.9 isixazululo of sodium chloride noma amaphesenti 5 isixazululo glucose. Dilution luqhutshwa ngezabelo kusuka 1:20 kuya ku-1: 100, kuye ngokuthi injongo. Ngenisa izidakamizwa kancane isikhathi esingamahora amabili kuya kweziyisithupha.

Ngaphambi zitshala izitho noma izicubu owethulwa isixazululo ngaphambili cyclosporin amahora cishe amane kuya kweyishumi. Ukuvimbela ukubonakaliswa iguliswa parallel esimisiwe ukwelashwa antiallergic nezinye immunosuppressants. Ngemuva kwamasonto amabili okuqala ka ekuphathweni emthanjeni zomuthi uhlelo ngomlomo. I umthamo wansuku zonke enqunywe udokotela wakho, kuthathwe izikhathi ezimbili amahora ayishumi nambili.

Amaphilisi Abonayo baphuze lonke ngaphandle kokuvula imvilophi, wageza phansi ngamanzi. Umuthi ewuketshezi ngaphambi kokusetshenziswa buhlanjululwe ku amanzi okuphuza a beaker ingilazi. Leli bhukwana likuchaza ngokuningiliziwe indlela ukukhipha iphakethe nokuthi ukudayela isixazululo iziqu isipetu ngengilazi ibhodlela, ukuze kahle ukhethe isilinganiso esifanele imithi. Ngemva ukuphuza isitsha Ikhambi Ngaleso siyakazwe ngamanzi aphuze ketshezi, ukuthi akukho ukulahleka umthamo.

ukusetshenziswa concomitant is contraindicated izidakamizwa kanye ubhamubhamu juice, okuyinto kunciphisa umphumela izidakamizwa, futhi ngesikhatsi ukwelashwa kungavunyelwa lokugoma ne bukhoma attenuated futhi sera kusukela rubella, uvendle, isimungumungwane, mumps.

Isikali

Lapho utshalwe omdala yokuvuma iqala nge umthamo wansuku zonke 10-14 angu amakhilogramu esisindo ngayinye. Ngemva eziyisikhombisa nane izinsuku ukwelashwa kukalwa lokuhlushwa cyclosporine egazini. Lokhu kuthonywa izinga ukumuncwa futhi ukuguqulwa emzimbeni. Le nkomba kubalulekile ukuqapha ukuze kuvinjelwe imiphumela engemihle futhi ukugwema ekuxhumaneni negative nezinye izidakamizwa. Ngemva kwalokho, umthamo wansuku zonke zomuthi kuyehla kube 3.6 angu amakhilogramu esisindo ngayinye, ihlukaniswe yaba ukusetshenziswa ezimbili. ngaleyo ndlela-plasma okuqukethwe oqabulayo cyclosporin kuhluka nanograms ngemililitha ngayinye 110 kuya 410.

Ngemva ukufakelwa yezinso kokuthola nomuthi e umthamo esingaphansi emithathu kuya kwemine angu amakhilogramu esisindo ngayinye kungabangela ukwenqatshwa.

Umnkantsha transplantation kudinga ukusetshenziswa inhlanganisela cyclosporine futhi methotrexate. Ngemva kwezinsuku ezimbalwa ngaphambi nesineke ukufakelwa iqondiswa nsuku ngemithambo yegazi kusukela 2.5 kuya 5 angu per kilogram esisindo izinto.

Ngemva kwathatha ekwelapheni amaphilisi uqale nge umthamo zonke izinsuku we-12.5 angu amakhilogramu esisindo, okuyinto sathathwa ngayinye njengoba kabili. Engamakhambi eliningi kangangokuthi zomuthi Uthatha izinyanga ezintathu kuya kweziyisithupha. Kancane kancane isidingo ukunciphisa umthamo kwaze kwaba sekupheleni kwesikhathi yokwelashwa.

Ukuqeda isimo sibi usebenzisa komthamo wokuqala nsuku zonke zomuthi kusukela angu amakhilogramu esisindo ngayinye 12.5 kuya ku-15 (ukuthatha izindlela ezimbili). izinsuku ezingamashumi amahlanu ukuchitha Isikali ngamaphesenti angu ezinhlanu ngesonto, futhi ngemva kwezinyanga eziyisihlanu sokuthatha sekugcineni izidakamizwa. olwengeziwe ukwelashwa "Cyclosporin" nomuthi eyenziwa uma ukuphendula okuphindaphindiwe. Yokusetshenziswa, amazwana aqukethe ulwazi mayelana okusinda kwezitho utshalwe (inhliziyo, isibindi). Ngokwezibalo, unyaka owodwa efika amaphesenti ayisishiyagalombili.

Ukwelashwa kwezifo sokuhlasela kwamasosha omzimba kudinga indlela ekhethekile kukhethwa ngemithamo isifo ngasinye.

Ngokuthola "Cyclosporin" ukulungiselela incwadi yeziyalezo uncoma ekwelapheni uveitis ezinzima. Kumele siqale nge umthamo zonke izinsuku we 5-10 angu amakhilogramu esisindo ngayinye futhi unamathele kuso ukunciphisa ukuvuvukala ukuzinza umsebenzi ezibukwayo. Inkambo yokwelashwa ezintathu nesithupha izinyanga. Ngo izilonda kabi lihambisana prednisolone at umthamo micrograms kilogram of isisindo isiguli ngasinye 200 kuya kwangu-600.

Ngo-psoriasis ezinzima umthamo wansuku zonke kuyinto 2.5 milligram amakhilogramu esisindo ngayinye, reception wenziwa izindlela ezimbili. Umthamo luyanda 1 milligram amakhilogramu esisindo ngayinye, kodwa hhayi ngaphezulu kuka-5 angu kilogram per, izinsuku uma ngemva amathathu emva Ukuqalwa okwelashwa, intuthuko. Ukwamukelwa khansela ngemva nje kwamasonto ayisithupha uma kwelashwa ayizwakali.

syndrome Nephrotic nge evamile umsebenzi kwezinso e abadala belashwa usebenzisa umthamo we zemithi 6 angu ngayinye esisindo amakhilogramu ezinganeni - Hlanganisa kufika ku 5 angu amakhilogramu esisindo ngayinye. Uma umsebenzi kwezinso kahle, umthamo - hhayi ningi than 2.5 angu amakhilogramu esisindo ngayinye.

Phakathi ukwelashwa nge okuqukethwe cyclosporin ukugadwa e oketshezini olungenambala lwegazi. Ukuze ngempumelelo zokwelapha okudinga ukuba agxilise ingqondo yayo egazini e isamba 60-160 nanograms ngemililitha ngayinye.

Phakathi nezinyanga ezintathu zokuqala kumele kube ukulawula creatinine ezingeni egazini serum, njengoba landa kule inkomba kungase eyobonisa ukuqala kwe-ukwenqaba a utshalwe isitho noma sezinso. Kubantu abane-izinso abasebenza kahle, ukuhlaziya Kwenziwa kanye ngemva kwezinsuku eziyishumi nane, uma kukhona ukwephulwa, creatinine Inkomba kukalwa zonke izinsuku eziyisikhombisa. Lapho lokuhlushwa inkomba kuka-200 micromoles ilitha abadala futhi ezingaphezu kuka-140 micromoles ilitha izingane eyenziwa ukuqedwa zomuthi.

Ngenxa kungenzeka imiphumela anobuthi zomuthi Kwenziwa ukuqapha ngezikhathi okuqukethwe bilirubin, urea, Amylase, magnesium potassium ion egazini, ama-enzyme isibindi kunqunywa.

rheumatoid arthritis kuyindlela ezinzima phakathi namasonto ayisithupha lokuqala iphathwa ukulungiselela "Cyclosporin" at umthamo 2.5 angu amakhilogramu esisindo ngayinye, kulandelwa ukwelashwa nge umthamo wansuku zonke akufanele idlule 4 angu amakhilogramu esisindo ngayinye. Lapho tolerability abampofu nomuthi kungenzeka ukunciphisa inani layo umthamo ubuncane ngempumelelo. Mhlawumbe inhlanganisela "Ciclosporin" izidakamizwa nge inani elincane corticosteroids noma izidakamizwa nonsteroidal eqeda ukuvuvukala.

amafomu okunzima atopic dermatitis iphathwa ngu nsuku zonke ekuphathweni izidakamizwa e umthamo 2.5 angu amakhilogramu esisindo ngayinye. Uma kungekho ukusebenza ngemva ebekiwe ezilishumi nane umthamo sangemihla - 5 angu amakhilogramu esisindo ngayinye. Uma kukhona ngcono isimo, kutuswa ukuncipha kancane kancane umthamo imithi.

Njengoba lisetshenziswe iso cyclosporine? iso amaconsi

ejenti Immunosuppressive ziye zasetshenziswa zamehlo ukwelapha izinyembezi. Ngenxa yalezi zinjongo, cyclosporine. Eye lehla ekuqukethe (amaphesenti 0.05) imakethwa ngaphansi tradename "Restasis".

Lokhu ejenti kungokwalabo iqembu yemithi esetshenziswayo ukuvikela i-cornea kanye humidification. ukulungiselela akhiqizwa umthamo owodwa we-0.4 milligram izitsha eziyisikhombisa okuqukethwe kwenye ngemililitha solution 500 mg isithako esisebenzayo.

Yini imithi libonisa cyclosporine? Eye amaconsi ukukhiqiza eqeda ukuvuvukala, immunomodulatory umphumela, zivimbela ukukhiqizwa lachrymal uketshezi phakathi keratoconjunctivitis ezomile.

Indlela yokusebenzisa lesi sidakamizwa "Restasis"

Endaweni lapho wasungula indlela "Restasis" aqukethe cyclosporin. Ukusetshenziswa Guide uncoma eyedrops lokuqala nithintithe isitsha ukuthola eyohlobo opaque emulsion emhlophe. Kungaleso sikhathi kuphela lapho usungaqala ukugxilisa amathonsi ku sac conjunctival of iso lesiguli. Le nqubo Kwenziwa kabili ngosuku, njalo ngemva kwamahora nambili. Lapho ebonisa indlela lo izidakamizwa akufanele uthinte emaphethelweni isitsha iso mucosa ukuvimbela ingress ukutheleleka isixazululo. Kubalulekile ukukhumbula ukuthi udinga ukusebenzisa imithi ngokushesha ngemuva kokuvula isitsha, ikhambi asele alisetshenziswa, it is esetshenzisiwe.

Ayikho ikhambi "Restasis" izidakamizwa lapho egqoke contact lens. Basuke isuswe ngaphambi zisebenzisa yesixazululo, futhi kungenziwa reinserted emva kwemizuzu eyishumi nanhlanu kuphela.

Ukusetshenziswa cyclosporine izilwane

Njengamanje, lo ejenti immunosuppressive sisetshenzisiwe futhi ekwelapheni izifo sokuhlasela kwamasosha omzimba e izinja kanye nezinye izilwane.

Ekuqaleni kuphela abantu usebenzisa cyclosporine. "Sandimmune" - isixazululo uwoyela eliqukethe kwakwakhe samanje, lapho esetshenziswa iziguli ezahlukene kubange lokuhlushwa ezahlukene isithako esisebenzayo-plasma.

ifomu ngaphezulu yesimanje sidalwe ke - cyclosporine ultramicronized ( "Neoral"). Kubangela ekwakhekeni microemulsion ngesikhathi ukusebenzisana ketshezi. Lokhu kwaholela ekubeni zibe ngcono ukumuncwa futhi bioavailability zomuthi njengoba kuqhathaniswa ikhambi uwoyela okuyinto asifanele izilwane.

Umdali wefomu lezilwane lomuthi uthathwa njengeNovartis. Imithi elayisensi yanikezwa ngo-2003 ngaphansi kwegama elithi "Atopika", ihloselwe ukwelashwa kwe-atopic dermatitis ezilwaneni. Kuze kube yileso sikhathi, ngokungafaneleki, ama-immunosuppressants asetshenziselwa ukufakelwa izinso ezinkambeni nezinja ukuze kuqedwe izimpawu zezinqubo zokuvuvukala.

Izimpawu ze-atermic dermatitis ngokuvamile zibonakala ezinja ezincane namakati aphakathi kwezinyanga eziyisithupha kuya eminyakeni emithathu. Lesi yisifo esingapheli esibonakala ngokuphindaphindiwe kabusha. Kudinga ukwelashwa kwansuku zonke ngomuthi oqukethe i-cyclosporine. Imiyalo yokusetshenziswa kwezilwane isho ukuthi "Atopika" ibonisa ukuthi kungenzeka ukusebenzisa isikhathi eside ngokuphumelelayo nangokuphepha.

Ngokudla kanye nemithi ngesikhathi esifanayo, kungase kube nezinguquko ekuthandeni, ngakho-ke kunconywa ukuthatha le mithi ngemva kwamahora amabili noma ngaphambi kokudla.

Phakathi kwemiphumela engathandeki ekusetshenzisweni kwalesi sidakamizwa, ngokuvamile kaningi kukhona ukuphazamiseka ohlelweni lokugaya, kepha kubonakala ngesimo esimnene. Ezinye imiphumela emibi yizibonakaliso ze-hypertrichosis, i-gingival hyperplasia kanye ne-dermatitis ephezulu. Njengoba kunciphisa ukuhlolwa kwesidakamizwa, ukunyamalala kwabo kancane kancane kwenzeka.

Ukuphathwa kwe-cyclosporine kunciphisa ukukhula nokuthuthukiswa kwama-causative agents we-staphylococcal infections kanye ne-malasseous dermatitis, emkhakheni wezokwelapha awubangeli ukuhluleka kwe-renal, umfutho wegazi ophezulu, nokwakhiwa kwe-neoplasms. Wonke la maqiniso akhombisa izinga eliphansi lokubhekana nezinkinga ngesikhathi ukwelashwa isikhathi eside kwe-atopic dermatitis ezinja.