Antidiabetesic Dapagliflozin

Mndandanda wa mankhwala othandizira odwala matenda ashuga (komanso mankhwala othandizira pakudya, mankhwala azitsamba, mavitamini), mankhwala onse komanso osalemba, ndiwodabwitsa. Ndipo komabe, mankhwala atsopano, malinga ndi kuyesera, adawonetsa zotsimikizika zambiri. Imodzi mwa mankhwalawa, omwe amadziwa kale odwala matenda ashuga, ndi Forsiga yozikidwa pa dapagliflozin.

Kuphatikizika kwa mankhwalawo komanso mawonekedwe a kumasulidwa

Pulogalamu yamasamba, Dapagliflozin amagulitsidwa ngati mapiritsi achikasu. Kutengera ndi unyinji, ali ozungulira okhala ndi zilembo zokhala ndi "5" kutsogolo ndi "1427" mbali inayo, kapena diamondi zopangidwa ndi zilembo za "10" ndi "1428", motsatana.

Pa mbale imodzi m'maselo anaikamo ma PC 10. mapiritsi. Phukusi lililonse la makatoni mungathe kukhala ndi mbale zotere zitatu kapena 9. Pali matuza ndi zidutswa 14 chimodzi. Mu bokosi lamasewera otere mungapeze awiri kapena anayi.

Alumali moyo wa mankhwalawa ndi zaka zitatu. Kwa dapagliflozin, mtengo womwe umapezeka m'matumba a pharmacy ndi 2497 rubles.

Chofunikira chachikulu cha mankhwalawa ndi dapagliflozin. Kuphatikiza apo, mafilimuwa amagwiritsidwanso ntchito: cellulose, lactose youma, silicon dioxide, crospovidone, magnesium stearate.

Pharmacology

Chosakaniza chophatikizika, dapagliflozin, ndi choletsa choletsa (SGLT2) cha transporter yodalira shuga 2. Chotsimikiziridwa mu impso, sichimawoneka m'ziwalo zina ndi matupi ena (mitundu 70 yoyesedwa). SGLT2 ndiye chonyamula chachikulu mu glucose reabsorption.

Njirayi siyimayima ndi matenda amtundu wa 2, kaya ndi hyperglycemia. Poletsa kutulutsa kwa glucose, ma inhibitor amachepetsa kubwezeretsanso kwa impso ndipo amamuchotsa. Chifukwa cha kuyanjana uku, shuga amachepetsa - onse pamimba yopanda kanthu komanso atatha kuchita masewera olimbitsa thupi, zomwe zimapangitsa glycosylated hemoglobin kusintha.

Kuchuluka kwa glucose omwe amachotsedwa kumadalira kuchuluka kwa shuga komanso kuchuluka kwa kusefedwa kwa glomerular. The inhibitor sikukhudza kupanga kwachilengedwe kwa shuga. Mphamvu zake ndizosagwirizana ndi kupanga kwa insulin komanso kuchuluka kwa chidwi chake.

Kuyesera kwa mankhwalawa kunatsimikizira kusintha kwa boma la ma b-cell omwe amachititsa kuti pakhale insulin.

Kudzala kwa glucose mwanjira imeneyi kumakwiyitsa calorie kumwa ndi kuwonda kwambiri, pali pang'ono okodzetsa.

Mankhwalawa samakhudza ma glucose ena omwe amayendetsa thupi lonse. Kupanga SGLT2, dapagliflozin imawonetsa kukwezeka nthawi 1,400 kuposa mzake mnzake SGLT1, yemwe amachititsa kuti shuga ayambe kuyamwa.

Mankhwala

Pogwiritsa ntchito Forsigi ndi odwala matenda ashuga komanso omwe ali ndiumoyo woyeserera, kuwonjezereka kwa glucosuric zotsatira kunadziwika. Manambala enieni, zimawoneka motere: kwa masabata 12, odwala matenda ashuga adamwa mankhwalawa 10 gm / tsiku.Kanthawi imeneyi, impso zimachotsa mpaka 70 g shuga, wokwanira 280 kcal / tsiku.

Chithandizo cha Dapagliflozin chimathandizidwanso ndi osmotic diuresis. Ndi njira yofotokozedwera yamankhwala, mayendedwe a diuric sanasinthe kwa masabata 12 ndipo anali 375 ml / tsiku. Mchitidwewu unkatsatiridwa ndi kukoka kwa sodium wochepa, koma izi sizikhudza zomwe zili m'magazi.

Pharmacokinetics

1. Zogulitsa. Pogwiritsa ntchito pakamwa, mankhwalawa amalowetsedwa m'matumbo oyaka msanga komanso pafupifupi 100%. Kudya zakudya sizimakhudzana ndi mayamwidwe. Kuchuluka kwa mankhwala omwe amapezeka m'magazi kumawonedwa pambuyo pa maola 2 mutagwiritsidwa ntchito pamimba yopanda kanthu. Mulingo wamphamvu wa mankhwalawa, umakulanso kuchuluka kwa plasma kwakanthawi. Mulingo wa 10 mg / tsiku. mtheradi bioavailability adzakhala pafupifupi 78%. Mwaumoyo omwe mumayesedwa, kudya sikunawakhudze kwambiri pamankhwala a pharmacokinetics.
2. Kugawa. Mankhwala amamangidwa kumapuloteni a magazi ndi pafupifupi 91%. Ndi matenda ophatikizika, mwachitsanzo, kulephera kwa impso, chizindikiro ichi chimatsalira.
3. Kupenda. TЅ mwa anthu athanzi ndi maola 12,0 pambuyo piritsi limodzi la piritsi 10 mg. Dapagliflozin imasinthidwa kukhala inert metabolite ya dapagliflozin-3-O-glucuronide, yopanda pharmacological
4. Kuswana. Mankhwala okhala ndi metabolites amatuluka mothandizidwa ndi impso mu mawonekedwe ake oyambirira. Pafupifupi 75% imachotsedwa mu mkodzo, ena onse m'matumbo. Pafupifupi 15% ya dapagliflozin imatuluka mwangwiro.

Milandu yapadera

Kuchuluka kwa glucose komwe impso zimachita bwino pamavuto amachitidwe awo zimatengera kuuma kwa matenda. Ndi ziwalo zathanzi, chizindikiro ichi ndi 85 g, ndi mawonekedwe opepuka - 52 g, ndi pafupifupi - 18 g, muzovuta kwambiri - 11 g shuga. Inhibitor imamangiriza mapuloteni momwemonso onse odwala matenda ashuga komanso m'gulu lolamulira. Zotsatira za hemodialysis pazotsatira zamankhwala sizinaphunzire.

Mwa mitundu yofatsa komanso yolimba ya kukanika kwa chiwindi, pharmacokinetics ya Cmax ndi AUC imasiyana ndi 12% ndi 36%. Choyipa chotere sichichita gawo lazachipatala, motero, palibe chifukwa chochepetsera muyeso wa gulu la odwala matenda ashuga. Mawonekedwe owopsa, zizindikirozi zimasiyana mpaka 40% ndi 67%.

Mukakula, kusintha kwakukulu kwa mawonekedwe a mankhwalawo sikunawonedwe (ngati palibe zifukwa zina zowonjezera chithunzi cha chipatala). Zofooka zofooka, ndizomwe zimakweza dapagliflozin.

Okhazikika, odwala omwe ali ndi matenda a shuga a 2, pafupifupi Cmax ndi AUC ndi apamwamba kuposa omwe ali ndi anthu odwala matenda ashuga ndi 22%.

Zosiyana pazotsatira kutengera mtundu wa European, Negroid kapena Mongoloid sizinapezeke.

Ndi kulemera mopitirira muyeso, zisonyezo zochepa za momwe mankhwalawo amalembedwera, koma zolakwika zotere sizofunikira kwambiri, zomwe zimafunikira kusintha kwa mlingo.

Ndani othandiza forsyga

Posintha njira yamoyo (zakudya zama carb ochepa, minyewa yokwanira), kuti glycemia isinthe, mankhwalawa amagwiritsidwa ntchito:

• Ndi monotherapy;
• Kufanana ndi metformin (ngati zotsatira za hypoglycemic sizokwanira);
• M'gawo loyambirira lophatikizika.

Contraindication

• Kuzindikira kwakukulu pazomwe zimapangidwira;
• Mtundu woyamba wa shuga;
• Ketoacidosis;
• Matenda akulu aimpso;
• Matupi kusalolera kwa glucose ndi lactase;
• Mimba ndi mkaka wa m`mawere;
• Ana ndi unyamata (palibe deta yodalirika);
• Pambuyo pachimake matenda, limodzi ndi kuchepa kwa magazi;
• Zaka za Senile (kuyambira zaka 75) - ngati woyamba mankhwala.

Njira zoyenera zochitira

Algorithm yochizira dapagliflozin ndi dokotala, koma malangizo okhazikika amaperekedwa mogwirizana ndi malangizo omwe angagwiritsidwe ntchito.

1. Monotherapy. Kulandila sikudalira chakudya, chizolowezi cha tsiku ndi tsiku ndi 10 mg panthawi imodzi.
2. Chithandizo chokwanira. Kuphatikiza ndi metformin - 10 mg / tsiku.
3. Chiwembu choyambirira. Nthawi zonse, Metformin 500 mg / tsiku. Forsigu amatenga 1 tabu. (10g) patsiku. Ngati zotsatira zomwe mukufuna sizikhala, onjezerani kuchuluka kwa Metformin.
4. Ndi hepatic pathologies. Anthu odwala matenda ashuga ofatsa osakwanira chiwindi safuna kusintha kwa mlingo. Mowonda kwambiri, amayamba ndi 5 g / tsiku .. Ndi mawonekedwe abwinobwino a thupi, chizolowezi chimatha kuchuluka mpaka 10 mg / tsiku.
5. Ndi matenda a impso. Mwa mawonekedwe olimbitsa komanso ovuta, Forsig sanalembedwe (pamene creatinine chilolezo (CC) <60 ml / min.);
6. Ukalamba. Paubwino, posankha mtundu wa mankhwala, amatsogozedwa ndi kuchuluka kwa magazi ndi zomwe impso zimachita.

Zotsatira zoyipa

Kafukufuku wachitetezo cha mankhwalawa adakhudza odzipereka 1,193 omwe adapatsidwa Fortigu pa 10 mg / tsiku, ndi omwe anali nawo 1393 omwe adatenga placebo. Pafupipafupi pazosayenera zotsatira zinali zofanana.

Mwa zina zomwe sizinachitike mwadzidzidzi zomwe zimafuna kuti ntchito ichotsekedwe, zotsatirazi zinaonedwa:

• Kuchuluka kwa QC - 0,4%;
• Matenda a genitourinary system - 0,3%;
• Kuwala pakhungu - 0,2%;
• Matenda a Dyspeptic; 0.2%;
• Kuphwanya mgwirizano, 0%.

Zambiri za phunziroli zimaperekedwa pagome.

Makhalidwe Akuwunika:

• Nthawi zambiri -> 0,1;
• Nthawi zambiri -> 0,01, <0,1;
• Nthawi zambiri -> 0.001, <0.01.

Ndemanga za Dapagliflozin

Malinga ndi kafukufuku wa alendo omwe amapeza zinthu zofunikira, odwala matenda ashuga ambiri alibe mavuto, amakhutira ndi zotsatirazi. Ambiri amaimitsidwa ndi mtengo wamapiritsi, koma malingaliro ake okhudzana ndi ukalamba, matenda opatsirana, thanzi labwino silingakhale chitsogozo chogamula kusankha kwa Forsigi.

Njira yakuchiritsira payokha ikhoza kupangidwa ndi dokotala, amadzatenga analogi ya dapagliflozin (Jardins, Attokuan) ngati zovuta sizokwanira.

Kanemayo - mawonekedwe a Dapagliflozin ngati mtundu watsopano wamankhwala.