"Cyclosporin": imiyalelo ukusetyenziswa. "Cyclosporin A": umyalelo. Wamehlo nge cyclosporine

Kwindalo, kukho izinto ekwaziyo abathintela okukwazi zeselula kunye humoral emzimbeni yezilwanyana lwaqhutywa yi-T-lymphocyte. Oku kungenzeka ukuba afeze ngempumelelo ngaphandle nokufakelwa amalungu omzimba kunye nokunyanga izifo ezinxulumene abanamajoni omzimba kakuhle. Enye loo cyclosporin i imichiza yendalo.

incazelo

Kuvulwa into edityaniswe ekufundweni yatsala nokungunda Tolypocladium inflatum kunye Cylindrocarpon lucidum. Kuhlelwe-arhente eziphilayo esebenzayo ezifana cyclosporin A no-C ukubonisa umsebenzi ngumzimba nxamnye egazi lymphocytic. Olu phawu okokuqala ngo-1972 zizazinzulu ukusuka 'Sandoz "igumbi Swiss. Kuye kwafumaniseka ukuba isakhiwo eekhemikhali cyclosporine yi cala endecapeptide lipophilic elibujikele kunye iphawulwe inyathelo elingqalileyo immunosuppressive.

Oku kusekelwe imithi inyathelo ukuvumbulula T-lymphocyte gqiba okukwazi kumaza humoral. igazi Cyclosporin abangaphangeliyo ukwenziwa lymphokines, leyo kunciphisa umsebenzi lymphocyte, kodwa alunasiphumo kwi inkqubo hematopoiesis kunye nomsebenzi ziiphagocytes, ebonisa ukuba isenzo akhetha umchiza emzimbeni.

iifom balawule

Kufuneka iqhotyoshelwe kule ikhithi ngamayeza equlethe cyclosporin, yemiyalezo. Phakathi kwezinye izinto, oku kuquka iinkcukacha kwifomu release beziyobisi. Amalungiselelo weli ekuveliseni ifomu:

• njengezingxobo ezithambileyo kunye umthamo 25, 50 no 100;
• isisombululo ezinxilisayo ngomlomo 100 neemiligram cyclosporin ml isisombululo nganye;
• oyile isisombululo ngomlomo 100 neemiligram cyclosporin ml isisombululo nganye;
• ingqondo ngenxa eyimveliso isisombululo yolawulo ukumnika nge-50 ne 650 neemiligram cyclosporin milliliter nganye;
• wamehlo kunye micrograms 500 milliliter of cyclosporine nganye.

Kuxhomekeka ngokusetyenziswa kwefom idosi iya kwahluka; kuba nolawulo lwangaphakathi, ngokuba inaliti, ngokuba isicelo mlonyeni.

Kukholelwa ukuba izinga kukufakwa icandelo esebenzayo, ixesha ukuqokelelana xi liphezulu igazi philisi kunye isisombululo ukwamkela lwangaphakathi zijongwa elingana.

Drug "Tacrolimus": nabalingani

Kwimarike zoxubo kukho inani lamachiza eziveliswa ngendlela efanayo amayeza, kwaye unikezele kakhulu kakuhle. Le esisebenza kuzo cyclosporine. Imiyalelo zokusetyenziswa ntonye immunodepressorov sicinga ngendlela efanayo amachiza ukucinezela immune.

Phakathi amayeza anyityiliselwe ngaphakathi a gelatin iqokobhe ethambileyo kunye izisombululo ilulwelo ichiza "Sandimmun Neoral" eziveliswa inkampani Swiss amayeza "Novartis" yokuqala. Ezinye amachiza kuqwalaselwa ngokutsha umfanekiso wadala yi ekwakhiweni wokuqala cyclosporin kweziyobisi. Nucleoside ezifana namachiza "Cyclosporin hexane", "Ekoral", "Tsiklopren" "Cyclosporin A", ekuveliseni ngokohlobo njengezingxobo okanye isisombululo izitofu lwangaphakathi okanye ukufumana.

Zazo eziphambili injongo - ekunciphiseni ukubandlululwa abohlukeneyo ngamalungu angaphakathi okanye lomongo wethambo. Mphathe kwabo izifo samathambo, njengoko oko kungqinwa eqhotyoshelwe i "Tacrolimus" imiyalelo iziyobisi ukuze zisetyenziswe. Analogs babe neempawu ezifana, yaye kubonakala ukuba ukusetyenziswa.

Indlela yokusebenza "Cyclosporin A" iziyobisi

Xa intliziyo yawo onke amanyathelo kweziyobisi immunosuppressive kuba nomphumela ukuvumbulula T-lymphocyte. Akukho ngaphandle kunye neziyobisi "Cyclosporin A". Guide inkcukacha iquka iindlela eziphambili iziphumo pharmacodynamic le icandelo esebenzayo, lona lubopha izinto ukuya iimanyano receptor phakathi kwiiseli. Kunciphisa imveliso interleukin kunye interferon kunciphisa amazwi receptors for IL-2.

Medicament "Cyclosporin A" kunciphisa ukuveliswa omzimba okujoliswe iiseli zayo nezihlunu, babona ezingeyonzalelwane yalapha nokutshabalalisa. Olu phawu ikuvumela ukuba ukunciphisa iingxaki ngumzimba nokunciphisa umsebenzi izifo sokuhlasela.

ukusebenza Enkulu "Cyclosporin A" ngokubhekiselele allograft. Isizathu sokuba ukulahlwa izicwili zilinywe kwaye amalungu i ipoti ye omzimba T wabangela. Ngenkuthalo ukuqala ukuze aveliswe phantsi isiphumo antigen abohlukeneyo yaye kuchaphazela iiseli lenkohlakalo, nisingise ekufeni kwabo.

Action immunodepressora kukhokelela kuthintele unxibelelwano T-iiseli kunye inhibition ka-T-lymphocyte ezivelayo immune. Ngenxa yoko, ukusebenza ichiza "Cyclosporin A" (umsebenzisi ibonisa oku) kwenzeka kuphela emva kokuba kwezithandani antigen yotyando. Ngokutshabalalisa ubudlelwane iantigens omzimba necrosis kumthwalo of zilinywe amalungu iiseli.

Kungani isicelo

Ubungqina obubonakalayo buxela ukuba Sebenzisa "Tacrolimus" imiyalelo ngokusebenzisa ichiza yahlulwe iindidi ezimbini.

Eyokuqala i abohlukeneyo okanye abohlukeneyo befikelwa inyama kunye namaziko. Iyeza osetyenziswayo ukuthintela bazishiya podsazhennogo iqumrhu okanye kwithishyu. Ngokuqhelekileyo, le grafts basebenzisa eluswini, intliziyo, lomongo wethambo, imiphunga, isibindi, intso, injeke. Mhlawumbi ukusetyenziswa kweziyobisi ukuphelisa ukulahlwa xa ezinye izinto immunosuppressive. Udidi lwesibini sisifo samathambo ngendlela kakhulu. Kwakhona arhente ezimiselweyo ukusebenza phantsi namanye amachiza.

Ziziphi izifo esiyiphatha ngayo iziyobisi 'Tacrolimus "? ukuze zisetyenziswe ezibonisa kuquka umyalelo yabela iintlobo nokoyika atopic dermatitis kunye neurodermatitis, izenzo ukhwekhwe, isifo samathambo, kwaye ichaphazela amalungu ezincinane ebushushwini babo. ukusetyenziswa kunokwenzeka uveitis kwi iindawo phakathi nongasemva iso xa choroid asha kunye retina, kwaye nephrotic syndrome kunye enama-gormonoustoychivoy indalo.

imithetho zokwamkelwa

unyango ngamachiza kucetyiswa kuphela phantsi kweliso zonyango esibhedlele. Ngokuqhelekileyo ukusebenzisa isicelo lwangaphakathi okanye ngedriphu efakwa, nangona kukhethwa ukufumana isisombululo ngomlomo okanye njengezingxobo.

Tableware, kusetyenziswa ukulungiselela isisombululo ukuba isitofu efakwa kufuneka zenziwe ngeglasi, endaweni chloride Polyvinyl ukuphepha indlela ngeoli kukaCastor.

Kuba ukuxutywa lo mxube yasebenzisa isisombululo 0.9 ekhulwini komzimba sodium chloride okanye 5 ekhulwini solution iswekile. Ukuxutywa kwenziwa kusenziwa ngokwemilinganiselo ukusuka 1:20 ukuya-1: 100, kuxhomekeka injongo. Yazisa ichiza ngokucotha iiyure ezimbini ukuya kwezintandathu.

Phambi kuhlwayelwe amalungu okanye kwizihlunu kuqaliswa isisombululo ngaphambi cyclosporin iiyure malunga ezine ukuya kwishumi. Ukuthintela obubonakala komzimba ngokunxuseneyo elimisiweyo unyango antiallergic kunye nezinye immunosuppressants. Emva kweeveki ezimbini kulawulo efakwa na ichiza isicelo ngomlomo. Le idosi yemihla ngemihla emiselwe ngugqirha wakho, uthabathe izihlandlo ezimbini iiyure ezilishumi elinambini.

Njengezingxobo basele wonke ngaphandle kokuvula i mvulophu, ahlambe phantsi ngamanzi. Ichiza ikwimo yolwelo phambi kokuba ukusetyenziswa exutywe ibe amanzi okusela kwindawo kwitoti yeglasi. Le ncwadana ichaza iinkcukacha ukuze kucaciswe indlela iphakheji nendlela ukucofa isisombululo izidanga isirinji webhotile iglasi, ukuze ukhethe kakuhle isixa ilungelo amayeza. Emva ukusela isikhongozeli isisombululo eso yoxukuxwa ngamanzi nize nisele ulwelo, ukuba akukho nto kulahlekelwa umthamo.

ukusetyenziswa elimi contraindicated iziyobisi kunye grapefruit juice, leyo kunciphisa isiphumo iziyobisi, nayo ngexesha unyango liyathintelwa ugonyo kunye live okuncitshiswe kunye sera evela rubella, ipoliyo, imasisi, unoqwilikana.

balawule

Xa ufudusiwe ukwamkelwa omdala iqala idosi yemihla ngemihla milligrams 10-14 ikhilogram ubunzima bomzimba ngalinye. Emva kweentsuku ezisixhenxe ukuya elinesine unyango kulinganiswa uyondelelwano lwee- cyclosporine egazini. It iphenjelelwa izinga ukufunxeka kunye nokuguqulwa emzimbeni. Esi salathisi kubalulekile ukuba esweni ukuze kuthintelwe iziphumo ebezingalindelekanga kwaye uphephe nonxibelelwano okubi kunye nezinye iziyobisi. Emva koko, lo idosi yemihla ngemihla ichiza lancitshiswa 3.6 milligrams kwekilogram ubunzima bomzimba ngalinye, yahlulelwe kwii imisebenzi ezimbini. Isiqulatho plasma konwaywa cyclosporin oko yahluka ukusuka nanograms 110 ukuya 410 milliliter nganye.

Emva abohlukeneyo kwizintso abafumana medicament xa umthamo we milligrams ngaphantsi ezintathu ukuya kwezine ikhilogram ubunzima bomzimba nganye kubangele ukwaliwa.

Bone lomongo abohlukeneyo ifuna ukusetyenziswa indibanisela cyclosporine kunye methotrexate. Isibini iintsuku phambi kokuba isigulane esinye ilawulwa mihla yegazi of ukusuka milligrams 2.5 ukuya ku-5 nganye kilogram izinto ubunzima bomzimba.

Emva kokuba lenguqu ukuya nonyango njengezingxobo ziqala idosi yemihla ngemihla milligrams 12.5 ikhilogram ubunzima bomzimba, leyo wasiwa nganye kabini. Amayeza ezinjalo ubungakanani beziyobisi ithatha ukusuka kwiinyanga ezintathu ukuya kwezintandathu. Ngokuthe ngcembe imfuneko ukunciphisa esithathwa de kugqitywe kwexesha imithi.

Ukuze ecaleni imeko etsolo usebenzisa kwedosi yokuqala mihla le ichiza ukusuka milligrams 12.5 ukuya 15 ikhilogram ubunzima bomzimba ngamnye (uthathe iindlela ezimbini). iintsuku ezingamashumi amahlanu ukuchitha lokunciphisa umthamo iipesenti ezintlanu evekini, yaye, emva kweenyanga ezintlanu ukuthatha entanjeni iziyobisi. ezongezelelweyo unyango "Cyclosporin" medicament wayisa kwimeko yokusabela ngokuphindaphindiweyo. Imiyalelo yokusebenzisa, izimvo eziqulathe ulwazi malunga ukusinda amalungu zilinywe (intliziyo, isibindi). Ngokutsho manani, unyaka omnye yena ifikelela asibhozo ekhulwini.

Unyango lwezifo samathambo kufuna indlela ekhethekileyo ukhetho amathamo izifo nganye.

Ngokwamukela "Cyclosporin" ukulungiselela uqeqesho manual icebisa ukuba unyango lwe uveitis kakhulu. Kufuneka uqale idosi yemihla ngemihla milligrams 5-10 ikhilogram ubunzima bomzimba ngalinye yaye ubambelele kuyo ukunciphisa nokudumba kuqheleke umsebenzi olubonakalayo. Ikhosi ye unyango iinyanga ezintathu ukuya elishumi elinesithandathu. Xa izibhaxu yomthonyama ethi idibanise kunye prednisolone xa umthamo we micrograms 200 ukuya 600 ikhilogram ubunzima isiguli ngasinye.

Xa ukhwekhwe kakhulu idosi yemihla ngemihla ngu 2.5 mlligrams kwekilogram ubunzima bomzimba ngalinye, ulwamkelo lwenziwa ngeendlela ezimbini. Idosi ichanekile linyuke nge-1 mlligrams kwekilogram ubunzima bomzimba nganye, kodwa akukho milligrams ngaphezulu kwe-5 kilogram nganye, iintsuku ukuba emva ezingamashumi amathathu emva kokuba ukuqaliswa unyango, akukho ukuphucuka. Ukwamkelwa rhoxisa emva kweeveki ezintandathu ukuba unyango nokungaphumeleli kwawo.

syndrome Nephrotic nge function eziqhelekileyo sezintso abadala uphathwa ngokusebenzisa umthamo ichiza to milligrams 6 kilogram ubunzima bomzimba nganye abantwana - up to milligrams 5 ikhilogram ubunzima bomzimba ngalinye. Ukuba umsebenzi kwezintso kuphazamisekile, idosi - hayi ngaphezulu kwe 2.5 milligrams kwekilogram ubunzima bomzimba ngalinye.

Ngexesha unyango ezinomthamo cyclosporin zibekwe iliso kwi-plasma yegazi. Kuba ukusebenza therapeutic kufuna ingqalelo yayo egazini kwi imali nanograms 60-160 milliliter nganye.

Kwiinyanga ezintathu zokuqala kufuneka ukulawula kwinqanaba creatinine e serum igazi, njengoko ukwanda kwesi salathisi uya kubona ngantoni xa kuqalisa ngokukhatywa ilungu okanye kidney isifo zilinywe. Kuba abantu abaye izintso asebenza kakuhle, uhlalutyo kwakhona emva kweentsuku ezilishumi elinesine kuthwalelwa phandle, ukuba kukho Kukwaphula, isalathiso creatinine ulinganiswa zonke iintsuku ezisixhenxe. Xa uyazikhomba isalathisi ngaphezu micromoles 200 ilitha nganye abadala kunye micromoles ngaphezulu kwama-140 ilitha nganye kubantwana bayithwala ukupheliswa ichiza.

Ngenxa yeziphumo kunokwenzeka yityhefu beziyobisi lwenziwa esweni ngamaxesha ngokuqulathwe yibilirubin, urea, amylase, magnesium potassium ion emagazini, enzyme zesibindi uzimisele.

isifo samathambo luhlobo kakhulu kwiiveki zokuqala ezintandathu ngayo ukulungiselela "Cyclosporin" xa umthamo we milligrams 2.5 ikhilogram ubunzima bomzimba nganye, kulandele unyango kunye idosi yemihla ngemihla mayingagqithi milligrams 4 ikhilogram ubunzima bomzimba ngalinye. Xa tolerability abaziintsizana medicament kunokwenzeka kukunciphisa imali yayo idosi minimum olusebenzayo. Mhlawumbi indibanisela "Ciclosporin" ngamachiza kunye nemali encinane corticosteroids okanye iziyobisi nonsteroidal anti-ukudumba.

iintlobo okunzima atopic dermatitis iphathwa yi imihla ulawulo kweziyobisi umthamo we milligrams 2.5 ikhilogram ubunzima bomzimba ngalinye. Ukuba akukho isiphumo emva kweentsuku ezilishumi elinesine emiselweyo idosi iphezulu yemihla ngemihla - milligrams 5 ikhilogram ubunzima bomzimba ngalinye. Ukuba kukho uphuculo kurhulumente, kucetyiswa nokwehla kancinane ithamo zeyeza.

Njengoko kusetyenziswa iliso cyclosporine? wamehlo

arhente Immunosuppressive ziye zasetyenziswa zamehlo yonyango lweliso owomileyo. Ukuze ezi njongo, cyclosporine. Wamehlo imixholo yawo (0.05 pesenti) ziya kuthengiswa phantsi tradename "Restasis".

Le arhente fanele ukuba iqela ngamayeza asetyenziswa ukukhusela inwebu kunye humidification. ukulungiselela eziveliswa idosi enye ye 0.4 nengqayi mlligrams omxholo kwenye milliliter na isisombululo 500 mg esisebenza.

Yiyiphi imithi ebonisa cyclosporine? wamehlo ukuvelisa anti-ukudumba, isiphumo immunomodulatory, zinqanda imveliso lachrymal secretion ngexesha keratoconjunctivitis owomileyo.

Indlela yokusebenzisa ichiza "Restasis"

Ekuhlaleni kusetyenziswa lithetha "Restasis" equlethe cyclosporin. Usetyenziso Guide icebisa eyedrops kuqala vuthululani igutyana ukufumana emulsion yohlobo olunye ngaphaya emhlophe. Kuphela ke ungakwazi ukuqala ukubethelela ngamathontsi kungena kulo sac conjunctival of iliso yomguli. Le nkqubo yenziwa kabini ngemini, qho kwiiyure ezilishumi elinesibini. Ekusebenziseni ichiza kufuneka ningawachukumisi amazantsi iliso isifo igutyana ukuthintela ukungena zokugula isisombululo. Kubalulekile ukukhumbula ukuba ufuna ukusebenzisa amayeza ngoko nangoko emva kokuvula igutyana, umxube eseleyo ayisetyenziswa, iya isetyenziswa.

Akukho unyango "Restasis" iziyobisi xa enxibe lenses contact. ukuba Banduluka phambi ukusebenzisa yesisombululo, kwaye reinserted emva kwemizuzu elishumi elinesihlanu kuphela.

Ukusetyenziswa cyclosporine izilwanyana

Okwangoku, le arhente immunosuppressive isetyenziswa kwakhona ukuba unyango lwezifo samathambo ezinjeni kunye nezinye izilwanyana.

Ekuqaleni kuphela ngabantu abasebenzisa cyclosporine. "Sandimmune" - isisombululo ioli equlathe umchiza langoku, xa esetyenziswa yi izigulane ezahlukeneyo yabangela xi ezahlukeneyo isithako esisebenzayo kwi plasma.

ifomu wesimanje zadalwa ngoko - cyclosporine ultramicronized ( "Neoral"). Ibangela ukuyilwa kwento microemulsion ngexesha intsebenziswano kunye ulwelo. Oku kwakhokelela kukuphucuka ukufunxeka kunye bioavailability beziyobisi ngokuchaseneyo isicombululo oyile olubalulekileyo ukuba izilwanyana.

Umdali wefom yezilwanyana zezilwanyana ithathwa njengeNovartis. Iyeza elikhutshelwe ilayisenisi linikezelwe ngo-2003 phantsi kwegama elithi "Atopika", lenzelwe unyango lwe-atopic dermatitis kwizilwanyana. Kuze kube ngoko, ngokungafanelekanga, ukuxilongwa kwe-immunosuppressants kusetyenziswe ekutshaleni izintso kwiikati nasezinjaneni ukuze kupheliswe iimpawu zeenkqubo ezivuthayo.

Iimpawu ze-dermatitis ye-atopic zibonakaliswa kwizinja ezisencinane kunye neekati ezineminyaka eli-6 ukuya kwiminyaka emithathu. Esi sifo esingapheli esichazwe ngokuphindaphindiweyo kwakhona. Kudinga unyango obungunaphakade kunye neziyobisi ezine-cyclosporine. Imiyalelo yokusetyenziswa kwezilwanyana ithetha "iAtopika" ibonisa ukuba kungenzeka ukusebenzisa ixesha elide ngokufanelekileyo nangokukhuselekileyo.

Ngokutya ngokufanayo kunye neyeza, kunokukho utshintsho kwi-absorption, ngoko kuyacetyiswa ukuba uthathe eli liyeza emva kweeyure ezimbini okanye ngaphambi kokutya.

Phakathi kwemiphumo engathandekiyo ekusebenziseni kweziyobisi, ngokuqhelekileyo kukho iziphazamiso kwinkqubo yokutya, kodwa zibonakaliswa ngendlela efle. Ezinye iziphumo zempembelelo zibonakaliso ze-hypertrichosis, gingival hyperplasia kunye ne-hyperplastic dermatitis. Ngenxa yokunciphisa kwi-dosing yesilwanyana, ukunyamalala kwabo ngokuqhubekayo kwenzeka.

Ukulawulwa kwe-cyclosporine kunciphisa ukukhula kunye nokuphuhliswa kwee-agent ezenza i-staphylococcal infections kunye ne-malasseous dermatitis, kwimiba yokunyanga ayibangele ukuhluleka kwe-renal, ingozi yexinzelelo, kunye nokubunjwa kwe-nonoplasms. Zonke ezi ngxelo zibonisa izinga eliphantsi lobuncipheko beengxaki ngexesha lotyando lwexesha elide le-dermatitis kwizinja.