Antidiabetic Dapagliflozin

Jerin magungunan maganin rigakafi a cikin kantin magani (har ma da kayan abinci, ganyen ganye, bitamin), duka takardar sayan magani da wadanda ba a sa musu magani ba, suna da ban sha'awa. Kuma duk da haka, sabbin kwayoyi, bisa ga gwaje-gwajen, sun nuna sakamako mafi gamsarwa. Ofaya daga cikin waɗannan magungunan, wanda ya riga ya saba da masu ciwon sukari, shine Forsiga bisa ga dapagliflozin.

Abun magunguna da nau'in sakin

A cikin cibiyar sadarwar kantin magani, ana sayar da Dapagliflozin kamar allunan launin rawaya. Ya danganta da taron, suna zagaye da juna tare da alamar “5” a gaba da kuma “1427” a gefe guda, ko kuma lu'ulu'u mai kama da alamar "10" da "1428", bi da bi.

A kan farantin karfe daya a cikin sel an sanya inji mai kwakwalwa 10. kwayoyin hana daukar ciki. A kowane kwali na kwali na iya zama 3 ko 9. ire-iren wadannan faranti Akwai guraben blister da guda 14 kowannensu. A cikin kwalin irin wannan farantin zaka iya samun biyu ko hudu.

Rayuwar shiryayye na magani shine shekaru 3. Don dapagliflozin, farashin a cikin sarkar kantin ya kasance daga 2497 rubles.

Babban sashin maganin yana aiki dapagliflozin. Baya ga shi, ana kuma amfani da filler: cellulose, bushe lactose, silicon dioxide, crospovidone, magnesium stearate.

Pharmacology

Abun da ke aiki, dapagliflozin, mai hana mai ƙarfi ne (SGLT2) mai ɗaukar nauyin sodium mai jigilar glucose mai 2. An fitar dashi a cikin kodan, bai bayyana ba a cikin wasu gabobin jikinsu da kyallen takarda (nau'in 70 da aka gwada). SGLT2 shine babban daskararren hannu wanda ke da hannu a cikin reabsorption na glucose.

Wannan tsari bai tsaya tare da ciwon sukari na 2 ba, ba tare da la'akari da hyperglycemia ba. Ta hanyar hana juyar da sinadarin glucose, mai hanawa rage rage kayan maye a cikin kodan kuma an cire shi. Sakamakon wannan hulɗa, sukari yana raguwa - duka a kan komai a ciki kuma bayan motsa jiki, dabi'u na glycosylated haemoglobin suna haɓaka.

Adadin glucose da aka cire ya dogara da yawan adadin sukari mai yawa da ƙimar tacewa na duniya. Inhibitor ba ya shafar asalin halittar glucose. Capabilitiesarfin ƙarfinsa yana da 'yanci daga samarwa da insulin da kuma matsayin ƙwarewar shi.

Gwaje-gwajen tare da magunguna sun tabbatar da haɓaka yanayin ƙirar sel-alhakin alhakin ƙirar insulin halittar jini.

Glucose yana haifar da wannan hanyar yana tsokanar yawan adadin kuzari da asarar nauyi mai yawa, akwai ɗan ƙaramar sakamako.

Magungunan ba ya shafar sauran masu jigilar glucose waɗanda ke rarraba ta ko'ina cikin jiki. Zuwa SGLT2, dapagliflozin yana nuna zaɓin zaɓi na 1,400 sau mafi girma ga takwaransa SGLT1, wanda ke da alhakin ɗaukar glucose a cikin hanji.

Pharmacodynamics

Tare da yin amfani da Forsigi ta masu ciwon sukari da mahalarta lafiya a cikin gwajin, an lura da karuwa a cikin tasirin glucosuric. A cikin takamaiman lambobi, yana kama da wannan: don makonni 12, masu ciwon sukari sun ɗauki maganin a 10 gm / rana. Yayin wannan lokacin, kodan ya cire har zuwa 70 g na glucose, wanda ya isa zuwa 280 kcal / day.

Hakanan ana amfani da magani na Dapagliflozin tare da osmotic diuresis. Tare da tsarin kulawa da aka bayyana, matsalar diuric din ba ta canza shi har tsawon makonni 12 kuma ya zama 375 ml / rana. Tsarin ya kasance tare da lecture na karamin adadin sodium, amma wannan abun baya tasiri abinda ke cikin sa a cikin jini.

Pharmacokinetics

1. Damuwa. Tare da amfani da baka, ana shan maganin a cikin narkewa cikin hanzari kuma kusan 100%. Abincin abinci baya shafar sakamakon shanshi. Ana lura da ganiya mafi yawa na ƙwayoyi a cikin jini bayan sa'o'i 2 lokacin da aka yi amfani da shi akan komai a ciki. Mafi girman kashin maganin, shine mafi girman maida hankali na plasma akan wani lokaci. A kudi na 10 MG / rana. cikakken bioavailability zai zama kusan 78%. A cikin mahalarta lafiya a cikin gwajin, cin abinci ba shi da tasiri a asibiti a kan magunguna.
2. Rarraba. Magani yana ɗaure da garkuwar jini da kimanin kashi 91%. Tare da cututtukan concomitant, alal misali, gazawar renal, wannan alamar tana wanzuwa.
3. Tsarin rayuwa. TЅ a cikin mutane masu lafiya shine sa'o'i 12,0 bayan awo ɗaya na kwamfutar hannu wanda nauyin 10 mg. Dapagliflozin an canza shi zuwa metabolite na inert na dapagliflozin-3-O-glucuronide, wanda ba shi da tasirin magunguna
4. Kiwo. Magunguna tare da metabolites suna fitowa tare da taimakon kodan a cikin ainihin sa. Aƙalla 75% an fesa a cikin fitsari, sauran a cikin hanjin. Kimanin 15% na dapagliflozin yana fitowa da tsabta.

Abubuwa na musamman

Yawan adadin kumburi da kodan ke fitarwa a cikin rikicewar aikin su ya dogara da tsananin cutar. Tare da gabobin lafiya, wannan mai nuna alama shine 85 g, tare da tsari mai haske - 52 g, tare da matsakaici - 18 g, a cikin lokuta masu rauni - 11 g na glucose. Mai hanawa ya ɗaura sunadarai ta hanya guda biyu a cikin masu ciwon sukari da kuma cikin rukuni na sarrafawa. Ba a yi nazarin tasirin maganin hemodialysis ba sakamakon binciken.

A cikin siffofi masu laushi da matsakaitan halayen lalata hanta, likitancokinetics na Cmax da AUC sun bambanta da 12% da 36%. Irin wannan kuskuren ba ya taka rawar asibiti, saboda haka, babu buƙatar rage kashi na wannan rukuni na masu ciwon sukari. A cikin nau'i mai tsanani, waɗannan alamu sun bambanta zuwa 40% da 67%.

A lokacin balaga, ba a lura da wani canji mai girma na bayyanar cutar ba (idan babu wasu dalilai da ke tayar da hoton asibiti). Karancin kodan, mafi girman bayyanar cutar dapagliflozin.

A cikin yanayin kwanciyar hankali, a cikin marasa lafiya da ke fama da ciwon sukari na 2, matsakaicin Cmax da AUC sun fi na maza masu ciwon sukari kashi 22%.

Ba a sami bambance-bambance a cikin sakamakon dangane da zama na Turai, Negroid ko Mongoloid tseren ba.

Tare da nauyin wuce kima, ana nuna alamun ƙarancin sakamako na maganin, amma irin waɗannan kurakurai ba su da mahimmanci a asibiti, suna buƙatar daidaita sashi.

Wanene yake da amfani forsyga

Lokacin da ake canza salon rayuwa (abinci mai ƙarancin carb, isasshen ƙwayar ƙwayar tsoka), don daidaita al'ada glycemia, ana amfani da maganin:

• Tare da monotherapy;
• A layi daya tare da metformin (idan tasirin hypoglycemic bai isa ba);
• A cikin madaidaicin daftarin kewaye.

Contraindications

• Babban hankali ga abubuwan da ke cikin tsari;
• Nau'in cuta guda 1;
• Ketoacidosis;
• Cutar cutar koda.
• Amincewar ƙarancin jini zuwa glucose da lactase;
• Haihuwa da lactation;
• Yara da matasa (babu ingantaccen bayanai);
• Bayan matsanancin rashin lafiya, tare da raunin jini;
• Shekaru tsufa (daga shekaru 75) - a matsayin magani na farko.

Tsarin aikace-aikace na yau da kullun

Algorithm don lura da dapagliflozin likita ne, amma an ba da umarnin daidaitattun bayanai a cikin umarnin don amfani.

1. Monotherapy. Amincewa baya dogara da abinci, tsarin yau da kullun shine 10 MG a lokaci guda.
2. M magani. A hade tare da metformin - 10 MG / rana.
3. Tsarin farko. A wata al'ada ta Metformin 500 MG / rana. Forsigu take 1 shafin. (10g) kowace rana. Idan sakamakon da ake so ba shi ba, ƙara yawan Metformin.
4. Tare da cututtukan hepatic. Masu ciwon sukari tare da dysfunctions mai laushi zuwa matsakaici basa buƙatar daidaita sashi. A cikin nau'i mai tsanani, sun fara da 5 g / rana. Tare da amsawar al'ada na jiki, ana iya ƙara yawan zuwa 10 mg / rana.
5. Tare da mahaukacin mahaifa. A cikin matsakaici da tsauraran tsari, ba a ba da forsig (lokacin da keɓancewar creatinine (CC) <60 ml / min.);
6. Tsufa. A lokacin balaga, lokacin da za su zabi tsarin kulawa, ana samun su ta hanyar girman jini da yanayin kodan.

Side effects

A cikin binciken lafiya na miyagun ƙwayoyi, masu ba da agaji 1,193 waɗanda aka ba Fortigu a 10 MG / rana da 1393 mahalarta waɗanda suka ɗauki placebo sun ɗauki bangare. Matsakaicin tasirin da ba a ke so ba ya kusan iri ɗaya.

Daga cikin abubuwan da ba a san su ba suna buƙatar dakatar da jiyya, an lura da masu zuwa:

• Inara cikin QC - 0.4%;
• Abun da ke cikin tsarin ƙwayar cuta - 0.3%;
• Rashes akan fata - 0.2%;
• Rashin daidaituwa na diski; 0.2%;
• Take hakkin daidaituwa - 0.2%.

An gabatar da cikakkun bayanai na karatun a cikin tebur.

Sharuddan Ea'idodi:

• Sau da yawa -> 0.1;
• Sau da yawa -> 0.01, <0.1;
• Koma baya -> 0.001, <0.01.

Dapagliflozin Reviews

Dangane da binciken da baƙi suka yi game da albarkatun mai, yawancin masu ciwon sukari ba su da sakamako masu illa, sun gamsu da sakamakon magani. Mutane da yawa suna dakatar da farashin kwayoyin, amma jin daɗin kansa wanda ke da alaƙa da shekaru, cututtuka masu haɗuwa, jin daɗin rayuwa gaba ɗaya ba zai iya zama jagora don yanke hukunci game da alƙawarin Forsigi ba.

Wani likita ne kawai zai iya yin magani, shi kuma zai karɓi analogues na dapagliflozin (Jardins, Invokuan) idan hadaddun ba shi da tasiri sosai.

A bidiyon - fasali na Dapagliflozin a matsayin sabon nau'in magani.