Dapagliflozin - za mankhwala osokoneza bongo amitundu iwiri

Makampani odziwika bwino opanga mankhwala akupanga zida zamtundu wa glycemic zatsopano. Imodzi mwa mankhwalawa ndi dapagliflozin. Mankhwalawa adakhala woyimira woyamba wa gulu la zoletsa za SGLT2. Sizikhudza mwachindunji zina zomwe zimayambitsa matenda ashuga; zotsatira zake ndikuchotsa shuga m'magazi kulowa mkodzo. Zotsatira zabwino za dapagliflozin pa onenepa kwambiri komanso kuthamanga kwa magazi zinapezekanso. Zomwe mumagwiritsa ntchito mankhwalawa ku Russia sizidutsa zaka 5, motero ambiri a endocrinologists amakonda mankhwala otsimikiziridwa akale, akuopa zotsatira zoyipa zazitali.

Kukonzekera kwa Dapagliflozin

Dzina lamalonda la Dapagliflozin ndi Forsyga. Kampani yaku Britain AstraZeneca imapanga mapiritsi mogwirizana ndi American Bristol-Myers. Kuti mugwiritse ntchito mosavuta, mankhwalawa ali ndi 2 Mlingo - 5 ndi 10 mg. Zomwe zimapangidwa ndizosavuta kusiyanitsa ndi zabodza. Mapiritsi a Forsig 5 mg ali ndi mawonekedwe ozungulira ndipo zolemba zina zowonjezera "5" ndi "1427"; 10 mg - mawonekedwe a diamondi, olembedwa "10" ndi "1428". Mapiritsi onse awiriwa ndi achikasu.

Malinga ndi malangizo, Forsigu amatha kusungidwa zaka 3. Kwa mwezi wa chithandizo, phukusi limodzi limafunikira, mtengo wake ndi pafupifupi ma ruble 2500. Mwachangu, mu shuga mellitus, Forsigu amayenera kulembedwa kwaulere, chifukwa Dapagliflozin imaphatikizidwa pamndandanda wamankhwala ofunikira. Malinga ndi ndemanga, ndizosowa kwambiri kupeza mankhwala. Forsig imalembedwa ngati pali zotsutsana pakutenga metformin kapena sulfonylurea, ndipo m'njira zina sizingatheke kukwaniritsa shuga wamba.

Forsigi alibe mndandanda wathunthu, popeza chitetezo cha patent chikuchitirabe Dapagliflozin. Zofananira zamagulu zimadziwika kuti Invocana (imakhala ndi canagliflozin SGLT2 inhibitor) ndi Jardins (empagliflozin). Mtengo wa chithandizo ndi mankhwalawa umachokera ku ruble 2800. pamwezi.

Zochita zamankhwala

Impso zathu zimachita nawo gawo limodzi la shuga. Mwa anthu athanzi, mpaka galamu ya glue imasefa tsiku lililonse mu mkodzo woyamba, pafupifupi yonseyo imasungidwanso ndikubwerera m'magazi. Pamene kuchuluka kwa glucose m'matumbo kukwera mu shuga mellitus, kusefera kwake mu impso glomeruli kumakulanso. Atafika pamlingo wina (pafupifupi 10 mmol / l odwala ashuga okhala ndi thanzi labwino), impso zimasiya kubwezeretsanso glucose onse ndikuyamba kuchotsa zochuluka mumkodzo.

Matenda a shuga ndi kupsinjika kudzakhala chinthu chakale

• Matenda a shuga -95%
• Kuthetsa kwa mitsempha thrombosis - 70%
• Kuthetsa kwa kugunda kwamtima kwamphamvu -90%
• Kuthana ndi kuthamanga kwa magazi - 92%
• Kuwonjezeka kwa mphamvu masana, kukonza kugona usiku -97%

Glucose imalowa mkati mwa tinthu tating'onoting'ono tokha, chifukwa chake, onyamula sodium-glucose amatenga nawo mbali machitidwe ake obwezeretsanso. Mtundu umodzi, SGLT2, umangokhala mu gawo limodzi la nephrons pomwe gawo lalikulu la glucose limabwezedwanso. Mu ziwalo zina, SGLT2 sanapezeke. Zochita za Dapagliflozin zimakhazikitsidwa motengera zoletsa (zoletsa) zomwe zimachitika pantchito iyi. Zimagwira kokha pa SGLT2, sizikhudzira onyamula ma analog, chifukwa chake sizisokoneza kagayidwe kazachilengedwe kamphamvu.

Dapagliflozin amalowerera kokha ndi ntchito ya nephrons ya impso. Mutamwa mapiritsiwa, shuga amayambanso kuzimiririka ndipo amayamba kuthira madziwo mkodzo mopitilira muyeso kuposa kale. Glycemia yafupika. Mankhwalawa samakhudza shuga wambiri, chifukwa chake kumwa sayambitsa hypoglycemia.

Kafukufuku akuwonetsa kuti mankhwalawa samangoletsa shuga, komanso amakhudzanso zinthu zina pakukula kwa zovuta za matenda ashuga:

1. Naturalization wa glycemia kumabweretsa kuchepa insulin kukana, pambuyo theka mwezi kutenga index amachepetsa ndi pafupifupi 18%.
2. Pambuyo pakuchepetsa zovuta za glucose m'maselo a beta, kubwezeretsa ntchito zawo kumayamba, kaphatikizidwe ka insulini kumawonjezeka pang'ono.
3. Kusintha kwa shuga kumabweretsa kuchepa kwa zopatsa mphamvu. Malangizowo akuwonetsa kuti mukamagwiritsa ntchito Forsigi 10 mg patsiku, pafupifupi 70 g ya shuga imachotsedwa, yomwe imagwirizana ndi 280 kilocalories. Kupitilira zaka 2 zovomerezeka, kuchepa kwa makilogalamu 4.5 kungayembekezeredwe, komwe 2.8 - chifukwa cha mafuta.
4. Mu odwala matenda ashuga omwe poyamba anali ndi kuthamanga kwa magazi, kuchepa kwake kumawonedwa (systolic amachepetsa pafupifupi 14 mmHg). Kuwona kunachitika kwa zaka 4, zomwe zimachitika nthawi yonseyi. Mphamvu ya Dapagliflozin imagwirizanitsidwa ndi mphamvu yochepa ya kukodzetsa mkodzo (mkodzo wambiri umathiridwa munthawi yomweyo ndi shuga) komanso kuchepa thupi mukamagwiritsa ntchito mankhwalawa.

Pharmacokinetics

Dapagliflozin imatengedwa kwathunthu kuchokera kumimba, kuphatikiza kwa bioavailability kwa pafupifupi 80%. Kuchuluka kwazinthu zambiri m'magazi kumawonedwa pambuyo pa maola awiri ngati mapiritsi aledzera pamimba yopanda kanthu. Mukagwiritsidwa ntchito nthawi yomweyo ndi chakudya, nsonga ya ndende imafikiridwa pambuyo pake, patatha pafupifupi maola atatu. Nthawi yomweyo, kutsitsa kwa shuga sikumasintha, chifukwa chake mapiritsi amatha kuledzera mosasamala nthawi yakudya.

Kuthetsa kwotalika hafu ya moyo ndi maola 13; onse a Dapagliflozin amawachotsa zoposa tsiku limodzi. Pafupifupi 60% ya zinthu zimapukusidwa, zotsalazo zimatuluka osasinthika. Njira yodzifunira ya chimbudzi ndi impso. Mu mkodzo, 75% ya Dapagliflozin ndi ma metabolites ake amapezeka, mu ndowe - 21%.

Zomwe zimachitika mu pharmacokinetics m'magulu osiyanasiyana a odwala matenda ashuga, omwe amawonetsedwa mu malangizo:

• Kuchita bwino kumachepa ndi vuto laimpso. Ndi kulephera kwenikweni kwa aimpso, pafupifupi 52 g ya glucose imachotsedwera patsiku, ndi kulephera kwambiri kwaimpso, osapitirira 11 g;
• chiwindi chikuphatikizidwa mu metabolism ya Dapagliflozin, kotero kuchepa kwake pang'ono kumatsogolera pakuwonjezeka kwazinthu ndi 12%, pafupifupi digiri - ndi 36%. Kukula kotereku sikumawerengedwa ngati kofunika kwambiri ndipo sikutanthauza kusintha kwa Mlingo;
• mwa akazi, kugwiritsa ntchito mankhwalawa kumakhala kwapamwamba kuposa amuna;
• odwala matenda ashuga onenepa kwambiri, zotsatira za mankhwalawo zimacheperachepera.

Zisonyezero zakudikirira

Dapagliflozin adapangira mtundu wa 2 odwala matenda ashuga. Zoyenera kuvomerezeka - kuchepa kwa kuchuluka kwa chakudya mu chakudya, kuchitira zolimbitsa thupi pafupipafupi.

Malinga ndi malangizo, mankhwalawa angagwiritsidwe ntchito:

1. Monga monotherapy. Malinga ndi madotolo, kuikidwa kwa Forsigi kokha kumachitika kawirikawiri.
2. Kuphatikiza pa metformin, ngati sikupereka kuchepa kwakokwanira kwa glucose, ndipo palibe umboni uliwonse wosonyeza mapiritsi omwe amathandizira kupanga insulin.
3. Monga gawo la chithandizo chokwanira chothandizira kukonza chipukuta cha matenda a shuga.

Contraindication

Mndandanda wa contraindication pamankhwala ndi Dapagliflozin malinga ndi wopanga:

Kusankha kwa Mlingo

Muyezo wa tsiku ndi tsiku wa Dapagliflozin ndi 10 mg. Amasankhidwa ngati chithandizo chimayikidwa limodzi ndi mankhwalawa, kapena kuphatikiza ndi Metformin. Mlingo woyambira wa metformin ndi 500 mg, ndiye umakulitsidwa mpaka shuga liperekedwe. Mlingo wa Dapagliflozin mukamagwiritsidwa ntchito ndi mapiritsi ena ampweya wa shuga amatsimikiziridwa ndi adokotala. Malinga ndi ndemanga, odwala onse amapatsidwa 10 mg wa Dapagliflozin, ndipo shuga yamagazi imayendetsedwa ndikusintha mapiritsi a mapiritsi ena.

Kulephera kwambiri kwa chiwindi, malangizo ogwiritsira ntchito amalimbikitsa kuchepetsa kuchuluka kwa mankhwalawa 5 mg. Kulephera kwa impso sikutanthauza kusintha kwa mankhwalawa, ndikuphwanya kwakukulu, mankhwalawo ndi oletsedwa.

Mankhwalawa amamwa kamodzi patsiku, mosasamala nthawi ndi mawonekedwe a chakudyacho.

Zotsatira Zoipa za Dapagliflozin

Kuchiza ndi Dapagliflozin, monga mankhwala ena aliwonse, kumalumikizidwa ndi chiopsezo china chotsatira zoyipa. Mwambiri, mbiri yachitetezo cha mankhwalawa imavoteledwa ngati yabwino. The malangizo alemba zonse zomwe zingachitike, pafupipafupi kutsimikizika:

1. Matenda a genitourinary ali ndi vuto linalake la Dapagliflosin ndi analogues. Zimakhudzana mwachindunji ndi mfundo ya ntchito ya mankhwalawa - kutulutsidwa kwa glucose mkodzo. Chiwopsezo cha matenda chikuyembekezeka ndi 5.7%, pagulu lolamulira - 3,7%. Nthawi zambiri, mavuto amapezeka mwa amayi kumayambiriro kwa chithandizo. Matenda ambiri anali ochepetsetsa pang'ono komanso anali atathetsedwa mwa njira zodziwika bwino. Kuchepa kwa pyelonephritis sikuchulukitsa mankhwala.
2. Osakwana 10% ya odwala, kuchuluka kwa mkodzo kumawonjezeka. Kukula kwapakati ndi 375 ml. Matenda a urin ndi osowa.
3. Osakwana 1% ya odwala matenda ashuga adazindikira kudzimbidwa, kupweteka kumbuyo, thukuta. Chiwopsezo chomwecho cha kuchuluka kwa creatinine kapena urea m'magazi.

Ndemanga za mankhwala

Endocrinologists pa kuthekera kwa Dapagliflozin amayankha bwino, ambiri amati mlingo woyenera umakupatsani mwayi wochepetsa hemoglobin wa glycated ndi 1% kapena kupitirira. Kuperewera kwa mankhwalawa amawaganizira kanthawi kochepa kogwiritsa ntchito, chiwerengero chochepa cha maphunziro atatsatsa malonda. Forsigu pafupifupi samatchulidwa ngati mankhwala okhawo. Madokotala amakonda metformin, glimepiride ndi gliclazide, popeza mankhwalawa ndiokwera mtengo, amaphunziridwa bwino ndikuchotsa kusokonezeka kwakuthupi kokhala ndi matenda ashuga, osangochotsa glucose, monga Forsyga.

Anthu odwala matenda ashuga nawonso saumirira kuti atenge mankhwala atsopano, poopa kupatsirana matenda oyambitsidwa ndi genitourinary sphere. Chiwopsezo cha matenda amenewa m'matenda a shuga ndi chachikulu. Amayi amawona kuti pakuwonjezeka kwa matenda ashuga, kuchuluka kwa vaginitis ndi cystitis kumawonjezera, ndipo amawopa kupititsa patsogolo mawonekedwe awo ndi Dapagliflozin. Chofunika kwambiri kwa odwala ndi kukwera mtengo kwa Forsigi ndi kusowa kwa zotchipa.