SITAGLIPTIN - UMARNIN DON AMFANI, FARASHI, SAKE DUBAWA DA KUMA ALAMUN ANALOGUES

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A cikin pathogenesis na nau'in ciwon sukari na 2, an bambanta manyan hanyoyin guda uku:

Tissue insulin juriya;
Rashin hankali a cikin samar da insulin kwayoyin halitta;
Cikakken ƙwayar glucose ta hanta.

Dogara ga ci gaban irin wannan cuta ta rashin hankali ya ta'allaka ne tare da kwayoyin sel b da c. Karshen ya kuma samar da wani sinadari wanda ke karfafa canzawar glucose zuwa makamashi ga tsokoki da kwakwalwa. Idan rarar da aka samar da shi ya yi saurin raguwa, wannan yana tsokanar hauhawar jini.

Kwayoyin halitta na B-sel sune ke da alhakin samar da glucagon, yawan sa yana haifar da abubuwanda ake bukata don wuce haddi na glucose da hanta. Wucewar glucagon da karancin insulin suna ba da yanayi na tara yawan glucose din da ba ya kariya a cikin jini.

Inganci kula da ciwon sukari na 2 ba zai yiwu ba tare da barga da tsawon lokaci (na tsawon lokacin cutar) kula da metabolism. Yawancin gwaji na kasa da kasa sun tabbatar da cewa diyya na sukari ne kawai ke bayar da halayen shawo kan rikice-rikice tare da kara yawan rayuwar mai ciwon sukari.

Duk da ire-iren magungunan cututtukan cututtukan cututtukan, ba duk marasa lafiya ba ne ke iya samun nasarar wadataccen maganin carbohydrates tare da taimakon su. Dangane da binciken da aka yi a UKPDS mai iko, 45% na masu ciwon sukari sun karbi diyya 100% don rigakafin microangiopathy bayan shekaru 3, kuma kawai 30% bayan shekaru 6.

Wadannan matsaloli sun haifar da buƙatar haɓaka sabon rukuni na kwayoyi waɗanda ba kawai zasu taimaka kawar da matsalolin na rayuwa ba, har ma da kula da farji, yana motsa kayan aikin motsa jiki don daidaita samar da insulin da cutar glycemia.

Magungunan-nau'in cututtukan da za su iya sarrafa nau'in ciwon sukari na 2 ba tare da tayar da hanji ba, canje-canje kwatsam a cikin glycemia, haɗarin cutar hypoglycemia shine sabon ci gaba da masana kera magunguna.

Hasken enzyme na GLP-4 Sitagliptin yana taimaka wa mai ciwon sukari ya kula da ci abinci da kuma nauyin jikin mutum, yana bawa jiki damar iya shawo kan matsalar gubar glucose.

Formaddamar da tsari da abun da ke ciki

Magungunan da aka dogara da sitagliptin tare da sunan cinikin Janavia ana samar da su ne a cikin nau'ikan allunan zagaye tare da ruwan hoda ko launin fata kuma an yi alama da "227" a 100 MG, "112" a 50 MG, "221" a 25 MG. Allunan an cika su cikin akwatunan filastik ko alamuran fensir. Za'a iya samun faranti da yawa a cikin akwati.

Abubuwan da ke aiki mai mahimmanci sitagliptin phosphate hydrate an haɗu da su tare da sirinum croscarmellose, magnesium stearate, cellulose, sodium stearyl fumarate, phosphate hydrogen wanda ba a bayyana ba.

Don sildagliptin, farashin ya dogara da kayan tattarawa, musamman ga allunan 28 kana buƙatar biyan 1,596-1724 rubles. Ana ba da magani ta hanyar magani, rayuwar shiryayye shine shekara 1. Magungunan ba ya buƙatar yanayi na musamman don ajiya. Ana buɗe marufi a ƙofar firiji har wata daya.

Sitagliptinum na Pharmacology

Sitagliptin ya bambanta da sauran magungunan antidiabetic a tsarin aikinsa da tsarin sa. Tare da hana yiwuwar enzyme na DPP-4, mai hanawa ya kara yawan abubuwan ciki na HIP da GLP-1, wanda ke daidaita glucose homeostasis.

Wadannan kwayoyin suna haifar da mucosa na hanji, kuma samar da abubuwan kwanciyar hankali yana ƙaruwa tare da cin abinci mai gina jiki. Idan matakin glucose ya zama al'ada kuma mafi girma, hormones yana haɓaka har zuwa 80% na samar da insulin da ɓoyayyensa ta hanyar β-sel saboda hanyoyin nuna sigina a cikin sel. GLP-1 yana hana babban ɓoyewar ƙwayar glucagon ta sel-sel.

Decreasearin rage yawan glucagon a kan asalin karuwar ƙwayoyin insulin yana tabbatar da rage raguwar ƙwayar glucose a cikin hanta. Wadannan hanyoyin kuma suna tabbatar da daidaituwar glycemia. Ayyukan incretins yana iyakance ta wani yanayi na ilimin, musamman tare da hypoglycemia, ba su shafar ƙirar glucagon da insulin.

Ta amfani da DPP-4, incretins suna hydrolyzed don samar da inert metabolites. Ressara ayyukan wannan enzyme, sitagliptin yana ƙara yawan abubuwan ciki da insulin, rage haɓakar glucagon.

Tare da hyperglycemia, ɗaya daga cikin manyan alamun cututtukan type 2, wannan tsarin aikin yana taimakawa rage ƙoshin jini na glycated, sukari da ke fama da ruwa da kuma glucose bayan nauyin carbohydrate. Doseaya daga cikin kashi na sitagliptin zai iya toshe ayyukan DPP-4 na kwana ɗaya, yana ƙaruwa yaduwar jijiyoyin jini a cikin jini sau 2-3.

Magunguna na sitagliptin

Rashin shan maganin yana faruwa da sauri, tare da bioavailability na 87%. Yawan shaye-shaye bai dogara da lokacin cin abinci da kayan abinci ba, musamman, abinci mai mai mai canzawa baya canza sigogi na magungunan likitanci na abubuwan da ke faruwa.

Mai hanawa ya isa matsakaicin matakin (950 nmol) a cikin awoyi 1-4. Kungiyar AUC ta dogara da kashi, bambanci tsakanin nau'ikan masu ciwon suga ya ragu.

A cikin ma'auni, ƙarin amfani da kwamfutar hannu na 100 MG na ƙara yankin a ƙarƙashin ɓarna na AUC, wanda ke nuna dogaro da yawan kima a kan lokaci, da kashi 14%. Singleaya daga cikin magungunan allunan 100 MG na tabbatar da ƙarfin rarraba 198 l.

Relativelyan ƙaramin sashi na abubuwan maye kamar su metabolized. An gano 6 metabolites cewa rashin karfin hana DPP-4. Enaladdamar da hukunci (QC) - 350 ml / min. Babban ɓangaren magungunan an cire shi ta hanyar ƙwayar kodan (79% a cikin hanyar da ba a canza ba kuma 13% a cikin hanyar metabolites), sauran sune hanjin ciki.

Sakamakon ɗaukar nauyi a kan kodan a cikin masu ciwon sukari tare da wani nau'in ciwon mara (CC - 50-80 ml / min.), Manuniya iri ɗaya ce, tare da CC 30-50 ml / min. An lura da kimar darajar AUC, tare da CC a ƙasa 30 ml / min. - sau hudu. Irin waɗannan yanayin suna ba da shawarar titration kashi.

Tare da cututtukan hepatic na tsananin zafin, Cmax da AUC sun karu da 13% da 21%. A cikin siffofin masu tsauri, magungunan sitagliptin ba su canza sosai ba, tun da kodan sun fara cire maganin.

A cikin masu ciwon sukari na tsufa (65-80 shekaru), sigogi na pharmacokinetic na karuwar kwayoyin halitta na karuwa da kashi 19%. Irin waɗannan ƙimar ba su da mahimmanci a asibiti, saboda haka ba za a buƙaci zakka na ƙa'ida ba.

Wanene yake nuna incretinomimetic

An wajabta magungunan don ciwon sukari na nau'in 2 ban da rage cin abinci mai karko sosai da isasshen ƙwayar tsoka.

Ana amfani dashi azaman magani guda ɗaya da haɗu da jiyya tare da metformin, shirye-shiryen sulfonylurea ko thiazolidinediones. Hakanan yana yiwuwa a yi amfani da alluran rigakafin insulin idan wannan zaɓi yana taimakawa wajen magance matsalar juriyar insulin.

Contraindications don sitagliptin

Kada a rubuta magani:

Tare da babban mutum mai hankali;
Masu fama da cutar siga da nau'in cuta ta 1;
Ciki da shayarwa;
A cikin yanayin ketoacidosis na ciwon sukari;
Ga yara.

Masu ciwon sukari masu dauke da cututtukan cututtukan cututtukan daji suna buƙatar kulawa ta musamman.

Yadda ake ɗauka

Don sitagliptin, umarnin don amfani da shawarar shan maganin kafin abinci. Daidaitaccen sashi iri ɗaya ne ga kowane tsarin kulawa - 100 MG / rana. Idan jigilar shigowa ya karye, kwaya yakamata ya bugu a kowane lokaci, yin ninka kudin bai zama karbuwa ba.

Tare da CC 30-50 ml / min. kashi na farawa na miyagun ƙwayoyi zai zama sau 2 ƙananan - 50 mg / rana., tare da CC a ƙasa 30 ml / min. - sau 4 - 25 MG / rana. (lokaci daya). Lokaci na hemodialysis baya shafar tsarin maganin sitagliptin.

Abubuwan Bala'i

Yin hukunci da sake dubawa, yawancin masu ciwon sukari suna da damuwa game da rashin dyspepsia, damuwa mai sa rai. A cikin gwaje-gwaje na dakin gwaje-gwaje, hyperuricemia, raguwa a cikin ingancin ƙwayar thyroid, kuma an lura da leukocytosis.

Daga cikin sauran tasirin da ba a tsammani ba (ba a tabbatar da haɗin haɗin gwiwa ba tare da tabbatuwa) - cututtuka na numfashi, arthralgia, migraine, nasopharyngitis). Haɓakar haɗarin hypoglycemia yayi daidai da sakamakon da aka samu a cikin ƙungiyar sarrafa placebo.

Taimaka tare da yawan wuce haddi

Game da yawan abin sama da ya kamata, ana cire adadin magungunan da basu da amfani a cikin hanji, ana kulawa da dukkan sigogi masu mahimmanci (gami da ECG). An nuna alamun Symptomatic da tallafi, gami da maganin hemodialysis tare da damar tsawan lokaci (an cire allurai 13.5 a cikin awanni 3-4).

Sakamakon Cutar Magunguna

Tare da yin amfani da sitagliptin na lokaci guda tare da metformin, rosiglitazone, maganin hana haihuwa, glibenclamide, warfarin, simvastatin, magunguna na wannan rukuni na kwayoyi ba su canzawa.

Gudanar da daidaituwa na sitagliptin tare da digoxin baya nuna canji ga yawan magunguna. Ana ba da irin wannan shawarwarin ta hanyar koyarwa da kuma a cikin hulɗa na sitagliptin da cyclosporin, ketoconazole.

Sildagliptin - analogues

Sitagliptin sunan duniya ne na miyagun ƙwayoyi; sunan cinikinsa shi ne Janavius. Ana iya la'akari da analog analog hade da magungunan Yanumet, wanda ya hada da sitagliptin da metformin. Galvus yana cikin rukunin DPP-4 inhibitors (Novartis Pharma AG, Switzerland) tare da kayan aiki mai aiki vildagliptin, farashin 800 rubles.

Magungunan hypoglycemic kuma sun dace da lambar ATX ta matakin 4:

Nesina (Takeda Pharmaceuticals, Amurka, bisa ga bayanan inlogliptin);
Onglisa (Kamfanin Bristol-Myers Squibb, dangane da saxagliptin, farashin - 1800 rubles);
Trazhenta (Kamfanin Kamfanin Bristol-Myers Squibb, Italiya, Burtaniya, tare da sinadarin linagliptin mai aiki), farashi - 1700 rubles.

Ba a haɗa waɗannan magunguna masu mahimmanci a cikin jerin magungunan zaɓe ba? Shin ya cancanci yin gwaji a cikin haɗarinku da haɗarin ku a cikin kasafin ku da lafiyar ku?

Sitagliptin - sake dubawa

Yin hukunci game da rahotanni akan dandalin labarun kasada, Januvius galibi an wajabta shi ga masu ciwon sukari a farkon farkon cutar. Game da sitagliptin, sake dubawar likitoci da marasa lafiya sun nuna cewa yin amfani da incretinomimetic yana da nuances da yawa.

Januvia sabuwar magani ce ta zamani kuma ba duk likitoci bane sun sami isasshen gogewa ta amfani da shi. Har zuwa kwanan nan, metformin shine magani na farko-yanzu; yanzu, an kuma sanya wa littafin tarihin haihuwa kamar yadda ake yin maganin kashe kwayoyin halittu. Idan karfin sa ya isa, kara shi da metformin da sauran magunguna ba bu mai kyau.

Masu ciwon sukari suna korafi cewa maganin ba koyaushe yake biyan bukatun da aka ambata ba, a tsawon lokaci ingancinsa yana raguwa. Matsalar anan bawai amfani da magungunan ba ne, amma a cikin halayen cutar: ciwon sukari na 2 wani cuta ne, mara kamuwa da cuta.

Eugene, Lipetsk. A karshe likita na ya fita hutu. Na kalli rubutaccen sarrafa sukari na, na sanya wa kebabs. Binciken ba ya da kyau, kuma ya ba da shawarar in maye gurbin Diabeton MV tare da Yanuvia. My endocrinologist ya dandana, shi wary duk sabon kayayyakin. Menene fa'idarsa, ban da farashi (sau 6 mafi girma!), Har yanzu ban fahimta ba. Ina shan kwaya na Janavia har tsawon wata daya da safe, 3 da yawa Siofora 500 da rana. sugar sukari yanzu ba ya wuce 7 mm / l, kuma zai dawo da sauri zuwa al'ada bayan cin abinci. A baya, bayan horo mai ƙarfi a cikin dakin motsa jiki, sukari ya faɗi sosai. Yanzu ya isa ga al'ada (5.5 mmol / l) kuma a hankali ya tashi. A matsakaici, ina da alamun irin wannan a gabanin, amma saukad da sukari ya ragu sosai. Ba zan iya faɗi komai ba game da tasirin sakamako - Na yi wata ɗaya a kwantar da hankula.

Duk maganganun suna haifar da ƙarshen yankewa cewa gabatarwar sitagliptin cikin aikin asibiti, wanda ke wakiltar sabon rukuni na kwayoyi, yana ba da cikakkiyar dama don sarrafa nau'in ciwon sukari na 2 a kowane mataki, daga cutar kansa zuwa ƙarin ilimin, tare da sakamakon da ba a gamsu ba daga yin amfani da dabarun diyya na gargajiya.

Rahoton Farfesa A.S. Ametov, endocrinologist-diabetologist game da ka'idar da kuma al'adar amfani da sitagliptin - akan bidiyo.

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