Antidiabetesic Dapagliflozin

Matenda a shuga ndi gulu lalikulu la matenda omwe amapezeka osiyanasiyana. Mbali yodziwika bwino yamitundu yonse ya matenda ashuga ndi hyperglycemia - shuga wamagazi ambiri. Hyperglycemia imachitika pamtundu wa insulin yokwanira kapena insulin (insulin siyitha kukwaniritsa zosowa zonse za thupi, kapena kulibe).
Insulin ndi mahormoni, "fungulo" lomwe limatha kutsegula maselo kuti likwaniritse shuga moyenera. Ichinso chofunikira pakudya komanso kugwiritsa ntchito bwino njira zonse mthupi. Insulin imapangidwa ndi zida zapadera - maselo a pancreatic beta. Pali mitundu iwiri ya insulin yopanga - basal secretion (yofunikira, yofunika, kupereka shuga yoyenera yamagazi popanda kudya chakudya) ndi postprandial (pancreatic insulin yopanga imakhudzidwa ndi chakudya, pakakhala zosowa pokonzekera shuga wambiri).

Ngati odwala ayamba kupezeka ndi matenda a shuga, ndikofunikira kudziwa kuti ndi mitundu yanji yamatenda omwe amachitika pambuyo pake. Ambiri omwe ali ndi matenda a shuga amtundu 1 ndi mtundu 2. Pochita, palinso ena, koma siofala kwambiri.

Kodi kuchitira matenda a shuga 1?

Matenda a shuga a Type 1 amatchedwa mtundu wodalira insulini. Chifukwa cha kuwonongeka kwa maselo a pancreatic beta, kupanga insulin kumatha. Kwa odwala omwe ali ndi matendawa, pakufunika kuperekera insulin pafupipafupi. Anthu omwe ali ndi matenda amtundu woyamba a shuga amatembenukira kuchipatala. Izi zikutanthauza kuti insulin yayitali, yoyerekeza kubisika kwa insal insulin, imayendetsedwa madzulo (kapena m'mawa ndi madzulo), ndipo masana, monga lamulo, asanadye chakudya, "insulin yochepa" "imawonjezeredwa" kuti muchepetse postprandial glycemia.

Odwala ena agwiritsa bwino ntchito pampu ya insulin. Ichi ndi chipangizo chomwe chimapereka insulini nthawi zonse molingana ndi zosowa za wodwala molunjika ku dermis, komwe imalowetsedwa.

Kodi kuchitira matenda a shuga a 2?

Matenda a 2 a shuga, mosiyana ndi oyamba, ndi a insulini okha. Izi zikutanthauza kuti kapamba amatulutsa insulini, koma kuchuluka kwa kapangidwe kake sikokwanira mokwanira zofunikira za thupi kapena minyewa yake singathenso kuchitapo kanthu (mwaukadaulo umatchedwa insulin kukana).

Mankhwala otani?

Maziko othandizira mtundu wa 2 matenda a shuga , Glinides, komanso mapiritsi). Pakadali pano, mankhwalawa amagwiritsidwanso ntchito potengera mphamvu ya pulogalamu ya maretretin ndipo, pamapeto pake, pakuchotsa shuga wambiri mthupi ndi mkodzo (Glyflosins). Othandizira ambiri ochokera m'maguluwa amagwiritsidwa ntchito ngati mapiritsi othandizira. Chifukwa chake, mankhwalawa amatchedwa mankhwala opatsirana pakamwa.

Metformin ndi woyamba kusankha pa matenda a shuga a 2. Amakonzanso shuga pokonza minofu ya mafupa. Ngati mphamvu ya mankhwalawa sikokwanira, ndiye kuti othandizira ena odwala matenda a shuga atha kuwonjezeredwa. Zotsatira zoyipa za mankhwalawa ndizosowa. Odwala owonjezereka amatha kudwala matenda otsegula m'mimba, kusanza, nseru, kutsekemera kwazitsulo. Zotsatira zosafunikira pamtunda wam'mimba zimatha kuchepetsedwa ndikumwa mankhwalawa mukatha kudya, monga lamulo, pambuyo pa chithandizo cha milungu 2-3, amayamba kufooka. Metformin imatha kutumikiridwa mpaka katatu pa tsiku. Mowa suyenera kuikidwa pakumwa mankhwalawa. Mankhwala amapezeka monga mapiritsi.

Gulu la glitazone limaphatikizapo chinthu pioglitazone, mankhwala omwe samangowonjezera chidwi cha minyewa kupita ku insulin, komanso amathandizira pakuwoneka kwamafuta m'magazi, kuthamanga kwa magazi ndikuletsa kuperewera kwambiri kwa mapuloteni ndi impso. Mankhwalawa, angagwiritsidwe ntchito kokha (ngati wodwalayo akuletsa Metformin), kapena atha kuphatikizidwa ndi othandizira ena am'kamwa. Zotsatira zoyipa za mankhwala zimaphatikizira kudzikundikira kwamadzi m'thupi, kunenepa kwambiri, kuphatikizapo mankhwala - hypoglycemia. Mankhwala osokoneza bongo m'gululi amapangidwa ngati mapiritsi.

Sulfonylureas

Magulu ochokera ku Sulfonylurea ndi zinthu zatsopano zomwe zimapangitsa kuti inshuwaransi ya beta ipangidwe ndi insulin. Mankhwalawa nthawi zambiri amagwiritsidwa ntchito pophatikiza mitundu yachiwiri ya matenda ashuga. Mapiritsi okhala ndi mankhwala a sulfonylurea amatengedwa makamaka mkati mwa theka la ola musanadye. Ngati mankhwala ena pagululi aphatikizidwa ndi mapiritsi othandizira omasulira, mankhwalawa atha kumwa nthawi yomweyo musanadye kapena panthawi ya chakudya.

Zochokera ku Sulfonylurea zimatha kuyanjana ndi mankhwala ena omwe wodwala amatenga, kuphatikiza mankhwala osokoneza bongo. Chifukwa chake, ndikofunikira kuti adokotala azindikire mankhwala onse omwe amamwa. Zotsatira zoyipa kwambiri ndizo hypoglycemia ndi kuwonda. Ngati chithandizo cha nthawi yayitali chikhala ndi kukonzekera kwakukulu kwa sulfonylurea, insulin yomwe ili m'matumba amatha kutsirizika, chifukwa chake insulin imayambitsidwa ndi minyewa ya wodwala. Kukonzekera ndi zotumphukira za sulfonylurea - mapiritsi. Mowa sugwirizana ndi gulu ili la mankhwala!

Pakadali pano pali magulu a mankhwala osokoneza bongo omwe ali ndi msika pamsika womwe ali ndi zotsatirazi zogwira ntchito: Glimepiride, Gliclazide, Glipizide ndi Gliburide.

Magulu a Clinid amachita pa maselo a beta a isch a Langerhans chimodzimodzi ndi sulfonylureas. Ndiye kuti, amathandizira pakuwonjezeka kwa insulin katulutsidwe. Ma glinid amatengedwa mosasamala kanthu za chakudya. Fomuyo ndi miyala.

Zinthu zomwe zimakhudza dongosolo la maretretin

Ma incretins ndi zinthu zatsopano zamtundu wa mapuloteni kapena mahomoni ndipo zimapangidwa mucous nembanemba am'mimba atatha kudya. Kuchokera m'matumbo am'mimba, amadzipereka m'magazi. Ntchito yayikulu ya ma insretins ndikusunga kuchuluka kwa shuga m'magazi.

Glucan-peptide-1 (dzina lamankhwala limapezeka mu mawonekedwe a GLP-1) ndiye "retret "yofunika kwambiri, komwe gulu lonse la mankhwala limapezeka. GLP-1 imapangidwa ndimatumbo am'mimba mutatha kudya. Ngati kapangidwe kake ndi chimbudzi chake chikugwira ntchito moyenera, chimamasula 70% ya insulini yofunikira pokonza shuga womwe umapezeka mu chakudya. Mtundu wobala ndi magome.

Glyphlosins

Glyphlosins ndi gulu laposachedwa la mankhwalawa pochiza matenda a shuga a mtundu wachiwiri. Amamangirira zigawo zina za impso, zomwe zimabweretsa kuwonjezeka kwamkodzo wa glucose. Chifukwa cha njirayi, ndizotheka kupewa kuchuluka kwa shuga mu mkodzo ndikuchepetsa kuchuluka kwa shuga m'magazi.

Pakadali pano, Dapagliflozin, Kanagliflosin ndi Empagliflosin adalembetsedwa pamsika.

Dapagliflozin ndi Empagliflozin amatengedwa ngati gawo limodzi tsiku lililonse, mosasamala za kudya, ndipo amathanso kuphatikizidwa ndi mankhwala ena amkamwa a antidiabetes. Mawonekedwe ake ndi mapiritsi.

Kanagliflozin imayendetsedwa ngati kumwa kamodzi tsiku lililonse, makamaka pakudya koyamba. Oyenera kuphatikiza ndi ena othandizira pakamwa. Amapangidwa monga mapiritsi.

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 mankhwala ndi zaka 3. Kwa dapagliflozin, mtengo mumtundu wa mankhwala amachokera ku 2497 rubles.

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

Pharmacology

Chosakaniza chophatikizika, dapagliflozin, ndi choletsa inhibitor (SGLT2) cha transporter yodalira shuga 2. Chotsimikiziridwa mu impso, sichimawoneka m'ziwalo zina ndi matupi ena (mitundu 70 yoyesedwa). SGLT2 ndiye chonyamulira chachikulu chomwe chimakhudzidwa ndi kubwezeretsa shuga.

Njirayi siyimayima ndi matenda amtundu wa 2, mosasamala za hyperglycemia. Mwa kulepheretsa mayendedwe a glucose, ma inhibitor amachepetsa kugwiranso ntchito kwa impsoyo 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 owonjezera 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 mkhalidwe wa 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. Mpaka SGLT2, dapagliflozin imawonetsa kukongola kwakanthawi 1,400 kuposa 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 unkaphatikizidwa ndi kukoka kwa sodium wochepa, koma izi sizikhudza zomwe zili m'magazi.

Pharmacokinetics

1. Zogulitsa. Mukamamwa pakamwa, mankhwalawa amalowetsedwa m'matumbo mwake mwachangu ndipo pafupifupi 100%. Nthawi ya Chakudya sichikhudza zotsatira za 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 ma pharmacokinetics a mankhwalawa.
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 omwe ali ndi metabolites amasiya mothandizidwa ndi impso momwe adalili kale. Pafupifupi 75% imachotsedwa mu mkodzo, ena onse m'matumbo. Pafupifupi 15% ya dapagliflozin imatuluka mwangwiro

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 omwe ali ndi matenda ashuga komanso gulu. Zotsatira za hemodialysis pazotsatira zamankhwala sizinaphunzire.

Mwa mitundu yofatsa komanso yolimba ya kukanika kwa chiwindi, ma pharmacokinetics a Cmax ndi AUC amasiyana 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.

Contraindication

• Kuzindikira kwakukulu pazomwe zimapangidwira,
• Mtundu woyamba wa shuga
• Ketoacidosis
• Matenda akulu a impso,
• Matenda amtundu wa glucose ndi lactase,
• Mimba komanso kuyamwa,
• Ana ndi achinyamata (osakhala ndi data 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 osagwiritsa ntchito chiwindi safuna kusintha kwa mlingo. Mowonda kwambiri, amayamba ndi 5 g / tsiku .. Ndi mawonekedwe abwinobwino a thupi, mawonekedwewo amatha kuwonjezeredwa mpaka 10 mg / tsiku.
5. Ndi matenda a impso. Ndi mawonekedwe olimbitsa komanso okhwima, Forsig sanalembedwe (pamene creatinine chilolezo (CC)) zoyipa

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

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

• Kuchuluka kwa QC - 0,4%,
• Zofooka za genitourinary system - 0,3%,
• Zotupa pakhungu - 0,2%,
• Matenda a Dyspeptic, 0%
• Kuphwanya mgwirizano, 0%.

Zambiri za phunziroli zimaperekedwa pagome.

• Nthawi zambiri -> 0,1,
• Nthawi zambiri -> 0.01, 0.001,

Mtundu wa kachitidwe ndi ziwalo

Matenda komanso infestationsVulvovaginitis, balanitisKubala Matenda a metabolism komanso zakudyaHypoglycemia (pamodzi ndi mankhwala)W ludzu Matenda Am'mimbaKuyenda kwa matumbo Chiwonetsero cha khunguKutukwana Dongosolo laumisecheUlulu wammbuyo Dongosolo la genitourinaryDysuriaNocturia Zambiri ZamalondaDyslipidemia, mkulu hematocritKukula kwa QC ndi urea wamagazi

Ndemanga za Dapagliflozin

Malinga ndi kafukufuku wa alendo omwe amapeza zinthu zofunikira, odwala matenda ashuga ambiri alibe zotsatira zoyipa, 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 adokotala; amasankhanso kufanana kwa dapagliflozin (Jardins, Attokuan) ngati zovuta sizokwanira.

Kanemayo - mawonekedwe a Dapagliflozin ngati mtundu watsopano wamankhwala.

Kugwiritsa ntchito Dapagliflozin

Type 2 shuga mellitus kuwonjezera pa zakudya ndi masewera olimbitsa thupi kuti muthe kuyendetsa bwino glycemic control:

- zowonjezera pamankhwala a metformin, sulfonylurea zotumphukira (kuphatikiza ndi metformin), thiazolidinediones, DPP-4 zoletsa (kuphatikiza ndi metformin), kukonzekera kwa insulini (kuphatikiza ndi limodzi kapena mankhwala awiri a hypoglycemic ogwiritsira ntchito pakamwa) pakakhala kuti palibe chitetezo chokwanira cha glycemic,

- Kuyambitsa kuphatikiza mankhwala ndi metformin, ngati mankhwalawa alangizidwa.

Mimba komanso kuyamwa

Gawo la FDA la mwana wakhanda ndi C.

Dapagliflozin imakhudzana ndi pakati panthawi yoyembekezera (gwiritsani ntchito panthawi yomwe mwakhala simunaphunzire). Ngati amayi apezeka kuti ali ndi pakati, mankhwala a dapagliflozin ayenera kusiyidwa.

Sizikudziwika ngati dapagliflozin ndi / kapena ma metabolites ake osagwira amapita mkaka wa m'mawere. Chiwopsezo cha akhanda / makanda sichingadziwike kuti. Dapagliflozin ndi contraindified mu nthawi yoyamwitsa.

Zotsatira zoyipa za Dapagliflozin

Chitetezo cha Mbiri Yachitetezo

Kuwunikira komwe kunakonzedweratu kwa zomwe zidasungidwazo kunaphatikizapo zotsatira za maphunziro 12 oyendetsedwa ndi placebo momwe odwala 1193 adatenga dapagliflozin pa mlingo wa 10 mg ndipo odwala 1393 adalandira placebo.

Zomwe zimachitika pazochitika zoyipa (zamanthawi yochepa) kwa odwala omwe amatenga 10 mg dapagliflozin zinali zofanana ndi zomwe zimachitika mgulu la placebo. Kuchuluka kwa zovuta zomwe zimatsogolera pakuchepetsa kwa chithandizo chamankhwala kunali kochepa komanso koyenera pakati pa magulu azachipatala. Zochitika zodziwika bwino kwambiri zomwe zidapangitsa kuti discapinuation ya dapagliflozin atengere mlingo wa 10 mg ndizowonjezereka m'magazi a creatinine ndende (0.4%), matenda amkodzo thirakiti (0.3%), nseru (0,2%), chizungulire (0, 2%) ndi zidzolo (0.2%). Wodwala wina akutenga dapagliflozin adawonetsa chitukuko chochitika choopsa kuchokera pachiwindi ndi kupezeka kwa mankhwala a chiwindi ndi / kapena autoimmune hepatitis.

Choyipa chodziwika kwambiri chinali hypoglycemia, kukula komwe kudalira mtundu wa chithandizo chamankhwala chomwe chimagwiritsidwa ntchito pa kafukufuku aliyense. Zowopsa za hypoglycemia zinali zofanana m'magulu azithandizo, kuphatikizapo placebo.

Zotsatira zoyipa zomwe zimayesedwa pamayeso azachipatala omwe amayendetsedwa ndi placebo zimaperekedwa pansipa (chithandizo chanthawi yochepa mpaka masabata 24 osatengera wina wowonjezera hypoglycemic). Palibe wa iwo omwe amadalira mlingo. Pafupipafupi pazochitika zoyipa zimaperekedwa munjira ya ma gradation otsatirawa: pafupipafupi (≥1 / 10), nthawi zambiri (≥1 / 100, 1,2, kwamikodzo thirakiti matenda 1, infrequently - vulvovaginal kuyabwa.

Kuchokera kumbali ya kagayidwe kazakudya ndi matenda: nthawi zambiri - hypoglycemia (akagwiritsidwa ntchito pophatikizana ndi sulfonylurea kapena insulin) 1, modabwitsa - kuchepa kwa BCC 1.4, ludzu.

Kuchokera m'mimba: pafupipafupi - kudzimbidwa.

Pa khungu ndi subcutaneous minofu: pafupipafupi - thukuta linakula.

Kuchokera minofu ndi mafupa ofunikira: nthawi zambiri ululu wammbuyo.

Kuchokera ku impso ndi kwamkodzo thirakiti: Nthawi zambiri - dysuria, polyuria 3, pafupipafupi - nocturia.

Zambiri zasayansi: dyslipidemia 5, kuchuluka kwa hematocrit 6, kuchuluka kwa kuchuluka kwa creatinine m'magazi, kuwonjezeka kwa ndende ya urea m'magazi.

1 Onani gawo loyenera pansipa kuti mumve zambiri.

2 Vulvovaginitis, balanitis ndi zina zofanana ndi matenda amtunduwu zimaphatikizapo, mwachitsanzo, mawu ofotokozedweratu otsatirawa: kachilombo ka fungvovaginal fungal, matenda apakhungu, balanitis, fungal matenda opatsirana maliseche, vulvovaginal candidiasis, vulvovaginitis, candida balanitis, maliseche candidiasis, maliseche ziwalo amuna, matenda a penile, vulvitis, bakiteriya vaginitis, vulvar abscess.

3 Polyuria imaphatikizapo mawu omwe amakonda: polakiuria, polyuria ndi kutulutsa mkodzo wowonjezera.

Kuchepa kwa bcc kumaphatikiza, mwachitsanzo, mawu ofotokozedweratu: chisowa cham'madzi, hypovolemia, ochepa hypotension.

5 Kusintha kwapakati pazisonyezo zotsatirazi monga kuchuluka kwa zoyambira m'gulu la 10 mg dapagliflozin ndi gulu la placebo, motere: Chs chonse - 1.4 poyerekeza ndi -0.4%, Chs-HDL - 5.5 poyerekeza ndi 3,8%, Chs-LDL - 2.7 poyerekeza -1.9%, triglycerides -5.4 poyerekeza -0.7%.

Zosintha zapakati pa hematocrit kuchokera pazoyambira zinali 2.15% mgulu la 10 mg dapagliflozin poyerekeza -0.4% pagulu la placebo.

Kufotokozera kwa zoyipa zomwe zasankhidwa

Hypoglycemia. Kuchuluka kwa hypoglycemia kudalira mtundu wa chithandizo chamankhwala chomwe chimagwiritsidwa ntchito pa kafukufuku aliyense.

M'maphunziro a dapagliflozin monga monotherapy, kuphatikiza mankhwala ophatikizika ndi metformin kwa masabata a 102, ziwonetserozo za episode of hypoglycemia ofanana zinali zofanana (BCC. Zotsatira zoyipa zomwe zimakhudzana ndi kuchepa kwa bcc (kuphatikiza malipoti a kuchepa kwa madzi m'thupi, hypovolemia, kapena ochepa hypotension) zimadziwika mu 0.8 ndi 0.4% ya odwala omwe amatenga dapagliflozin 10 mg ndi placebo, motero; zovuta zazikulu zimadziwika mu bcc, zomwe nthawi zambiri zimalembetsedwa ngati ochepa hypotension yowonekera mu 1.5 ndi 0,4% ya odwala omwe amatenga dapagliflozin ndi placebo, motero (onani "Precautions").

Kuchita

Zodzikongoletsera. Dapagliflozin imatha kupititsa patsogolo okodzetsa a thiazide ndi zida zotulutsa komanso kuonjezera ngozi yakuchepa kwa magazi ndi vuto la mtima (onani "Precautions").

Insulin ndi mankhwala omwe amalimbikitsa katulutsidwe ka insulin. Poyerekeza ndi kagwiritsidwe ntchito ka insulin ndi mankhwala omwe amachititsa kuti pakhale chitetezo cha insulin, hypoglycemia ikhoza kuchitika. Chifukwa chake, kuti muchepetse chiopsezo cha hypoglycemia ndi kuphatikiza kwa dapagliflozin ndi insulin kapena mankhwala omwe amachulukitsa kubisika kwa insulini, pangafunike kuchepetsa kuchuluka kwa insulin kapena mankhwala omwe amachititsa secretion ya insulin (onani "Zotsatira zoyipa").

Kagayidwe ka dapagliflozin makamaka kamachitika ndi glucuronide conjugation mothandizidwa ndi UGT1A9.

Pakufufuza mu vitro dapagliflozin sanalepheretse isoenzymes ya cytochrome P450 system CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 ndipo sizinachititse isoenzymes CYP1A CYP12 CYPY2Y2Y2Y2Y2Y2Y2Y2Y2Y2Y2Y1 / CYP32. Mwakutero, zotsatira za dapagliflozin pakuvomerezeka kwa mankhwala ophatikizika omwe amakonzedwa ndi ma isoenzymes sikuyembekezeredwa.

Zotsatira za mankhwala ena pa dapagliflozin. Kafukufuku wokhudzana ndi odzipereka athanzi labwino, makamaka kumwa kamodzi kwa dapagliflozin, adawonetsa kuti metformin, pioglitazone, sitagliptin, glimepiride, voglibose, hydrochlorothiazide, bumetanide, valsartan, kapena simvastatin sizikhudza dapaglapinagin pharmacokinetics.

Pambuyo pa kuphatikiza kwa dapagliflozin ndi rifampicin, woyambitsa othandizira osiyanasiyana othandizira ndi ma enzyme omwe amapangira mankhwala, 22% inayamba kuwonekera pang'onopang'ono (AUC) ya dapagliflozin idadziwika kuti kulibe vuto lililonse latsiku ndi impso. Sikulimbikitsidwa kusintha mlingo wa dapagliflozin.

Zotsatira zazikulu zamankhwala zikagwiritsidwa ntchito ndi inducers zina (mwachitsanzo carbamazepine, phenytoin, phenobarbital) sizimayembekezeredwa.

Pambuyo pakuphatikizidwa kwa dapagliflozin ndi mefenamic acid (UGT1A9 inhibitor), kuwonjezereka kwa 55% kwawonekera kwa chiwonetsero cha dapagliflozin kunadziwika, koma popanda chiwonetsero chazofunikira kwambiri pakuwonetsa kwa shuga kwa impso tsiku ndi tsiku. Sikulimbikitsidwa kusintha mlingo wa dapagliflozin.

Zotsatira za dapagliflozin pa mankhwala ena. Pakufufuza komwe kudachitika odzipereka athanzi labwino, makamaka omwe adatenga limodzi mlingo, dapagliflozin sizinakhudze pharmacokinetics ya metformin, pioglitazone, sitagliptin, glimepiride, hydrochlorothiazide, bumetanide, valsartan, digoxin (gawo lapansi la P-varnarfin, varfarbacate, varfarate pot, farfarbacate, varfarbacate, varfarbacate, varfarbacifate, varfarbacate ) kapena pa anticoagulant zotsatira, zoyesedwa ndi INR. Kugwiritsa ntchito mlingo umodzi wa dapagliflozin 20 mg ndi simvastatin (gawo laling'ono la CYP3A4 isoenzyme) kunapangitsa kuchuluka kwa 19% ya simvastatin AUC ndi 31% simvastatin acid AUC. Kuchuluka kwa simvastatin ndi simvastatin acid sikumveka kwakukulu.

Zotsatira za kusuta, kudya, kumwa mankhwala azitsamba ndi kumwa mowa pa pharmacokinetics ya dapagliflozin sizinaphunzire.

Bongo

Dapagliflozin ndiyotetezeka komanso yolekeredwa bwino ndi odzipereka athanzi limodzi ndi mlingo umodzi wofika 500 mg (50 nthawi ya mlingo woyenera). Glucose anali kutsimikiza mu mkodzo atatha kutsata (osachepera masiku 5 atatha kumwa 500 mg), pomwe kunalibe milandu yakusowa magazi, kuchepa kwa magazi, kusowa kwa magazi kwa electrolyte, kuperewera kwakukulu pakubwera kwa QTc. Zovuta za hypoglycemia zinali zofanana ndi pafupipafupi ndi placebo. M'maphunziro azachipatala odzipereka omwe ali ndi thanzi labwino komanso odwala omwe ali ndi matenda a shuga a mtundu wa 2 omwe adatenga dapagliflozin kamodzi pa mlingo wa mpaka 100 mg (kangapo mlingo woperekedwa) kwa masabata awiri, zochitika za hypoglycemia zinali zapamwamba pang'ono kuposa ndi placebo, ndipo osati zimatengera mlingo. Zomwe zimachitika pazochitika zoyipa, kuphatikiza kuchepa kwa madzi m'thupi kapena kuchepa kwa thupi, zinali zofanana ndi pafupipafupi pagulu la placebo, popanda kusintha kwakukulu kokhudzana ndi kuchuluka kwa magawo a labotale, kuphatikiza ma seramu ambiri a ma elekitirodiya ndi ma biomarkers a ntchito ya impso.

Pankhani ya bongo, ndikofunikira kuchita kukonza mankhwala, kuganizira momwe wodwalayo alili. Kutulutsa kwa dapagliflozin ndi hemodialysis sikunaphunzire.

Mosamala Dapagliflozin

Odwala ndi mkhutu aimpso ntchito

Mphamvu ya dapagliflozin imatengera ntchito yaimpso, ndipo izi zimachepetsedwa mwa odwala omwe ali ndi kuchepa kwa aimpso ndipo mwina sapezeka mwa odwala omwe ali ndi vuto laimpso. Mwa odwala omwe ali ndi vuto lochepa kwambiri laimpso (Cl creatinine 2), kuchuluka kwakukulu kwa odwala omwe amalandila dapagliflozin adawonetsa kuwonjezeka kwa kuchuluka kwa creatinine, phosphorous, PTH ndi ochepa hypotension kuposa odwala omwe akulandira placebo. Dapagliflozin imalekanitsidwa kwa odwala omwe ali ndi kuchepa kwapakati kapena koopsa aimpso (Cl creatinine 2). Dapagliflozin sichinaphunzitsidwe kulephera kwambiri kwaimpso (Cl creatinine 2) kapena kulephera kwa impso.

Ndikulimbikitsidwa kuti muziyang'anira ntchito ya impso motere:

- isanayambike mankhwala a dapagliflozin ndi nthawi 1 pachaka pambuyo pake (onani "Zotsatira zoyipa", "Pharmacodynamics" ndi "Pharmacokinetics"),

- musanamwe mankhwala omwe angakuthandizeni kuchepetsa matenda a impso, komanso nthawi ndi nthawi.

- vuto laimpso pafupi ndi zolimbitsa, pafupifupi kawiri pachaka. Ngati matenda a impso amachepa m'munsimu Cl creatinine 2, siyani kumwa dapagliflozin.

Odwala omwe ali ndi vuto la chiwindi

M'maphunziro azachipatala, zowerengeka zapezeka pakugwiritsa ntchito dapagliflozin mwa odwala omwe ali ndi vuto la chiwindi. Kuwonetsedwa kwa dapagliflozin kumachulukitsidwa kwa odwala omwe ali ndi vuto lalikulu la chiwindi (onani "Malingaliro pazogwiritsidwa ntchito" ndi "Pharmacokinetics").

Odwala omwe ali pachiwopsezo cha kuchepa kwa bcc, kukulitsa kwa ochepa hypotension ndi / kapena kukhudzika kwa elekitirodi

Malinga ndi momwe amagwirira ntchito, dapagliflozin imakulitsa diuresis, limodzi ndi kuchepa kwapang'onopang'ono kwa kuthamanga kwa magazi (onani "Pharmacodynamics"). The diuretic zotsatira zitha kutchulidwa kwambiri kwa odwala omwe ali ndi kuchuluka kwa shuga m'magazi.

Dapagliflozin imalekanitsidwa kwa odwala omwe amatenga magazi m'thupi (onani "Kulumikizana"), kapena ndi BCC yochepetsedwa, mwachitsanzo, chifukwa cha matenda owopsa (monga matenda am'mimba).

Chenjezo liyenera kuchitika kwa odwala omwe kuchepa kwa kuthamanga kwa magazi chifukwa cha dapagliflozin kungakhale pachiwopsezo, mwachitsanzo, mwa odwala omwe ali ndi mbiri ya matenda amtima, mbiri yakale ya hypotension, kulandira antihypertensive chithandizo, kapena odwala okalamba.

Mukamatenga dapagliflozin, kuwunika mosamala dziko la BCC komanso kuchuluka kwa ma elekitirodi (mwachitsanzo, kuwunika kwa thupi, kuyeza magazi, mayeso a labotale, kuphatikizapo hematocrit) kumalimbikitsidwa motsutsana ndi maziko azikhalidwe zomwe zingayambitse kuchepa kwa bcc. Kutsika kwa BCC, kuchepa kwa dapagliflozin ndikulimbikitsidwa mpaka izi zitakonzedwa (onani "Zotsatira zoyipa").

Pogulitsa pambuyo pa kugwiritsidwa ntchito kwa dapagliflozin, ketoacidosis imanenedwapo, kuphatikizapo odwala matenda ashuga ketoacidosis, odwala omwe ali ndi mtundu woyamba 1 ndi 2 matenda a shuga, amatenga dapagliflozin ndi zina zoletsa za SGLT2, ngakhale kuti ubale wa causal sunakhazikitsidwe. Dapagliflozin sinafotokozeredwe zochizira odwala matenda a shuga 1.

Odwala omwe akutenga dapagliflozin ndi zizindikiro ndi zizindikiro za ketoacidosis, kuphatikizapo nseru, kusanza, kupweteka kwam'mimba, malaise, ndi kufupika kwa mpweya, ayenera kuyang'ana kupezeka kwa ketoacidosis, ngakhale magazi a glucose ali pansi pa 14 mmol / L. Ngati ketoacidosis ikukayikiridwa, kuganiziridwanso kuyenera kusiya kapena kusiya kwakanthawi ntchito dapagliflozin ndikuwunika wodwalayo mwachangu.

Zambiri zomwe zimayambitsa chitukuko cha ketoacidosis zimaphatikizapo magwiridwe antchito a maselo a beta chifukwa cha kuperewera kwa kapamba (mwachitsanzo, matenda a shuga 1, mellitus, kapamba kapenanso mbiri ya opaleshoni yapamba), kuchepa kwa insulin, kuchepa kwa chakudya cha caloric, kapena kuchuluka kwakufunika kwa chakudya insulin chifukwa cha matenda, matenda kapena opaleshoni, komanso uchidakwa. Dapagliflozin iyenera kugwiritsidwa ntchito mosamala mu odwala.

Matenda amitsempha.

Mukamasanthula deta yophatikiza kugwiritsa ntchito dapagliflozin, mpaka milungu 24 ya matenda a kwamikodzo amatchulidwa kawirikawiri ndikugwiritsa ntchito dapagliflozin pa 10 mg poyerekeza ndi placebo (onani "Zotsatira zoyipa"). Kukula kwa pyelonephritis kunadziwika kwambiri, komanso pafupipafupi pagulu lolamulira. Kuchuluka kwa shuga kwa impso kumatha kugwirizanitsidwa ndi chiopsezo chotenga matenda amkodzo thirakiti, chifukwa chake, mankhwalawa a pyelonephritis kapena urosepsis, kuthekera kwa kusiya kwakanthawi kwa chithandizo cha dapagliflozin kuyenera kuganiziridwanso (onani "Zotsatira zoyipa").

Urosepsis ndi pyelonephritis. Pogulitsa malonda pambuyo pa dapagliflozin, matenda oopsa a kwamikodzo, kuphatikizapo urosepsis ndi pyelonephritis, omwe amafunikira kuchipatala odwala omwe akutenga dapagliflozin ndi ena oletsa ma SGLT2. Chithandizo cha ma SGLT2 inhibitors chimawonjezera chiopsezo chotenga matenda amkodzo thirakiti. Odwala amayenera kuwunikidwa kuti awone zizindikiro ndi matenda amkodzo thirakiti ndipo ngati akuwonetsedwa, akuyenera kulandira chithandizo mwachangu (onani "Zotsatira zoyipa").

Odwala okalamba amatha kukhala ndi vuto laimpso komanso / kapena kugwiritsa ntchito antihypertensive mankhwala omwe amatha kuthana ndi vuto la impso, monga ACE inhibitors ndi mtundu II ARA 1. Kwa odwala okalamba, malingaliro omwewo a vuto laimpso amathandizanso kwa anthu onse odwala (onani"Zotsatira zoyipa" ndi "Pharmacodynamics").

Mu gulu la odwala azaka zapakati pa ≥65, kuchuluka kwakukulu kwa odwala omwe amalandila dapagliflozin kunayambika zotsatira zosakhudzika zomwe zimakhudzana ndi vuto laimpso kapena kulephera kwaimpso poyerekeza ndi placebo. Njira zoyipa zomwe zimakhudzana ndi vuto laimpso kuwonjezeka kwa kuchuluka kwa seramu creatinine, milandu yambiri inali yochepa komanso yosinthika (onani "Zotsatira zoyipa").

Kwa odwala okalamba, chiwopsezo cha kuchepa kwa BCC chingakhale chambiri, ndipo okodzetsa amakhala ndi mwayi wotengedwa. Ambiri mwa odwala ≥65 wazaka zakubadwa yemwe adalandira dapagliflozin adakumana ndi zovuta zotsutsana ndi kuchepa kwa BCC (onani "Zotsatira zoyipa").

Zochitika ndi dapagliflozin mwa odwala azaka 75 ndi akulu ndizochepa. Amakanizidwa kuti ayambe mankhwala a dapagliflozin mwa anthuwa (onani "Pharmacokinetics").

Kulephera kwamtima kosalekeza

Zochitika pakugwiritsa ntchito dapagliflozin mwa odwala CHF I - II ogwira ntchito mkalasi molingana ndi gulu NYHA ochepa, komanso munthawi ya mayesero azachipatala, dapagliflozin sanagwiritsidwe ntchito mwa odwala omwe ali ndi kalasi yogwira III - IV CHF NYHA.

Kuchuluka kwa hematocrit

Mukamagwiritsa ntchito dapagliflozin, kuwonjezereka kwa hematocrit kunawonedwa (onani "Zotsatira zoyipa"), chifukwa chake ayenera kusamala mwa odwala omwe ali ndi kuchuluka kwa hematocrit.

Kuyesa kwa mayeso a mkodzo

Chifukwa cha limagwirira a dapagliflozin, zotsatira za kuwunika kwa mkodzo kwa glucose mwa odwala omwe akutenga dapagliflozin adzakhala abwino.

Zotsatira za kutsimikiza kwa 1,5-anhydroglucitol

Kuunika kwa glycemic control pogwiritsa ntchito kutsimikiza kwa 1,5-anhydroglucitol sikulimbikitsidwa, popeza muyeso wa 1,5-anhydroglucitol ndi njira yosadalirika kwa odwala omwe akutenga ma SGLT2 zoletsa. Njira zina ziyenera kugwiritsidwa ntchito poyesa kuwongolera kwa glycemic.

Kukopa pa kuyendetsa magalimoto ndi kugwira ntchito ndi njira. Kafukufuku wofufuza momwe mphamvu ya dapagliflozin ikuyendera magalimoto ndikugwira ntchito ndi machitidwe sanachitike.

Kufotokozera za mankhwalawa

Dapagliflozin ndi potent (Kihibitilamu wosasinthika (Ki) wa 0,55 nM), mtundu womwe umasinthanso mtundu wa 2 sodium glucose cotransporter inhibitor (SGLT2). SGLT2 imawonetsedwa moyenera mu impso ndipo sapezeka m'matumbo ena opitilira 70 (kuphatikizanso chiwindi, minofu yamatumbo, minofu ya adipose, gland ya mammary, chikhodzodzo ndi ubongo).

SGLT2 ndiye chonyamula chachikulu cha glucose reabsorption mu aimpso tubules. Glucose reabsorption mu aimpso tubules kwa odwala omwe ali ndi matenda a shuga 2 mellitus (T2DM) akupitiliza ngakhale hyperglycemia. Mwa kuletsa kusinthika kwa impso m'magazi, dapagliflozin imachepetsa kugwedezeka kwa impso tubules, zomwe zimapangitsa kuti shuga akhale impso.

Kuchotsa glucose (glucosuric athari) kumachitika mutamwa mankhwala oyamba, umapitirira kwa maola 24 otsatira ndikupitilira chithandizo chonse. Kuchuluka kwa shuga komwe impso zimapangidwa chifukwa cha njirayi kumadalira kuchuluka kwa shuga m'magazi komanso kuchuluka kwa kusefedwa kwa glomerular (GFR).

Dapagliflozin sichimasokoneza kupanga kwachilendo kwa glucose amkati poyankha hypoglycemia. Zotsatira za dapagliflozin ndizodziyimira payekha paz insulin komanso insulin sensitivity. M'maphunziro a zamankhwala a Dapagliflozin * (Dapagliflozin *) ™, kusintha kwa ntchito ya function-cell kunadziwika (kuyesedwa kwa HOMA, kuwunika kwa homeostasis).

Kuwonongeka kwa shuga ndi impso zomwe zimayambitsidwa ndi dapagliflozin limodzi ndi kuchepa kwa zopatsa mphamvu komanso kuchepa kwa thupi. Dapagliflozin zoletsa wa sodium glucose cotransport limodzi ndi ofooka okodzetsa ndi osakhalitsa natriuretic zotsatira.

Dapagliflozin ilibe gawo lililonse kwa anthu ena omwe amayendetsa glucose omwe amatengera glucose kuzinthu zotumphukira ndikuwonetsa kupitirira 1,400 nthawi yayikulu pakusankha kwa SGLT2 kuposa SGLT1, transporter yayikulu yamatumbo yomwe imayendetsa mayamwidwe a glucose.

Atamwa dapagliflozin ndi odzipereka athanzi komanso odwala matenda amtundu wa 2, kuwonjezeka kwa glucose komwe anapatsidwa ndi impso kunawonedwa. Pamene dapagliflozin amatengedwa pa mlingo wa 10 mg / tsiku kwa masabata 12, mwa odwala T2DM, pafupifupi 70 g ya glucose adamuchotsa impso patsiku (zomwe zimafanana ndi 280 kcal / tsiku). Odwala omwe ali ndi matenda a shuga a mtundu wa 2 omwe adatenga dapagliflozin pa 10 mg / tsiku kwa nthawi yayitali (mpaka zaka ziwiri), shuga wa mayamwidwe adasungidwa panthawi yonse ya mankhwala.

Kuchulukanso kwa shuga kwa impso ndi dapagliflozin kumathandizanso kuti osmotic diuresis ndi kuchuluka kwa mkodzo kuchuluka. Kuwonjezeka kwa kuchuluka kwa mkodzo kwa odwala omwe ali ndi matenda amtundu wa 2 akumamwa dapagliflozin pa 10 mg / tsiku lokhalokha kwa masabata 12 ndipo limafikira pafupifupi 375 ml / tsiku. Kuchuluka kwa kuchuluka kwa mkodzo kumayendera limodzi ndi kuchepa kwa pang'onopang'ono kwa impso, komwe sikunapangitse kusintha kwa kuchuluka kwa sodium mu seramu yamagazi.

Kuwunikira komwe kumakonzedwa pazotsatira za maphunziro 13 olamulidwa ndi placebo akuwonetsa kuchepa kwa magazi a systolic (SBP) a 3.7 mm Hg. ndi diastolic magazi (DBP) pa 1.8 mm Hg pa sabata la 24 la dapagliflozin Therapy pa 10 mg / tsiku poyerekeza ndi kuchepa kwa SBP ndi DBP ndi 0,5 mm Hg. pagulu la placebo. Kutsika kofananako kwa kuthamanga kwa magazi kunawonedwa m'milungu ya 104 ya chithandizo.

Mukamagwiritsa ntchito dapagliflozin pa 10 mg / tsiku kwa odwala omwe ali ndi matenda a shuga 2 omwe ali ndi vuto losakwanira glycemic komanso matenda oopsa, kulandira angiotensin II receptor blockers, ACE inhibitors kuphatikiza ndi mankhwala ena a antihypertensive, kuchepa kwa hemoglobin ya glycosylated ndi 3.1% ndi kuchepa kwa SBP ndi 4.3 mm Hg. Pambuyo pa milungu 12 ya mankhwala poyerekeza ndi placebo.

Njira yayikulu yochizira matenda ashuga

Kuphatikiza pa njira zamankhwala, chithandizo chosagwiritsa ntchito mankhwalawa ndikofunikira kwambiri. Madokotala amalimbikitsa kudya kwapadera, masewera olimbitsa thupi, ndi zochitika zina zomwe cholinga chake ndicholemetsa thupi. Izi zimathandizira kuchepetsa kuchuluka kwa insulin, kuchepetsa kuwonongeka kwa zinthu zofunika kwambiri za thupi pama cell β. Koma njira zotere zimapereka zotsatira zabwino pokhapokha matendawa atadwala. Odwala ambiri amafuna mankhwala.

Malingaliro a chithandizo cha hypoglycemic amadalira Zizindikiro zamatenda ndi momwe wodwalayo alili. Ngati kuchuluka kwa hemoglobin ya glycated ili mu 6.5 - 7.0%, monotherapy imaloledwa, ndipo ndalama zimasankhidwa ndi chiopsezo chochepa cha zotsatira zoyipa.

Asanawonekere muzochita zamankhwala, Forksig adalembedwa:

• biguanides (metformin),
• DPP-4 inhibitors (depeptidide peptidase-4) - Saxagliptin, Vildagliptin,
• glinids (Repaglinide, Nateglinide),
• glucagon-ngati peptide analogues (aGPP) - Exenatide, Lyraglutid,
• insulin

Ngati pali zotsutsana pakutenga mankhwalawa, njira zina zochiritsira zosagwiritsidwa ntchito pogwiritsa ntchito sulfonylureas, dongo, ndi zina zinagwiritsiridwa ntchito.

Pa gawo loyambirira la glycated hemoglobin wa 7.5 - 9.0%, kuphatikiza mankhwalawa ndi mankhwala angapo a hypoglycemic, omwe amakhudza mbali zosiyanasiyana za pathogenesis ya mtundu 2 matenda a shuga, ndikofunikira. Komabe, kuphatikiza kwa metformin komwe kumagwiritsidwa ntchito ndi ma hypoglycemic othandizira nthawi zambiri kumapangitsa kuti thupi la wodwalayo liwonjezeke komanso zinthu zina zovuta. Koma kuphatikiza kwa Metformin Forksig, m'malo mwake, kumayambitsa kuwonongeka kwa minofu ya subcutaneous ndi visceral adipose.

Pamene glycated hemoglobin imaposa 9,0%, wodwalayo amangofunika chithandizo cha insulin, nthawi zina kuphatikiza ndi ena othandizira a hypoglycemic.

Koma akatswiri amavomereza kuti mankhwala omwe kale anali ogwiritsidwa ntchito sioyenera kulandira chithandizo chamanthawi yayitali. Chifukwa chake, patatha zaka zitatu, theka lokhalo la odwala ndi lomwe limapereka chithandizo chokwanira, ndipo patatha zaka 9 - kotala.

Kugwiritsa ntchito Forxiga pochiza matenda ashuga

Chimodzi mwa mankhwala akuluakulu omwe amagwiritsidwabe ntchito pochiza matenda amtundu wa II ndi Metformin. Chida chake chimakhudza:

• chiwindi insulin kukana,
• njira ya gluconeogeneis,
• minofu kumverera kwa insulin.

Metformin kwenikweni sikuti imabweretsa kuchuluka kwa thupi, sikuyambitsa hypoglycemia. Koma gawo limodzi mwa magawo atatu a odwala limanenanso za zovuta zomwe zimachitika m'matumbo. Ndipo nthawi zina, zovuta zimayambitsa kusiya mankhwala. Kuphatikiza apo, Metformin nthawi zambiri imagwiritsidwa ntchito limodzi ndi mankhwala ena.

Poterepa, zotsatira za Forxiga zimadalira glucose. Zotsatira za kubwezeretsanso m'mimba zimachepetsedwa ndikuchepera pomwe kuchuluka kwa shuga m'magazi m'munsi mwa 5 mmol / L. Nthawi yomweyo, ngati mulingo wa glycemia ndi 13.9 mmol / L, kubwezeretsanso kumachulukitsa mpaka 70%, ndipo pa 16.7 mmol / L - mpaka 80%. Chifukwa chake, poyerekeza ndi mankhwala ena ochepetsa shuga, chiopsezo cha hypoglycemia sichikupezeka.

Musanagwiritse ntchito mankhwalawa, muyenera kufunsa dokotala nthawi zonse. Ndondomeko yeniyeni ya chithandizo imatha kupangidwa pokhapokha mayeso atatha.

Kukonzekera kwa glyphlosin

Zoletsa zimayambitsa impso ndipo zimayambitsa secretion wa shuga mu mkodzo. Chifukwa cha izi, pali kuchepa kwa glucose wamagazi, zopatsa mphamvu zowonjezera zimatenthedwa, zomwe zimatsogolera kuonda.

Mankhwala a SGLT-2, monga Jardins, Attokana, Xigduo, Wokanamet ndi achatsopano motero, sizotsatira zoyipa zonse zomwe zimamveka bwino.

Mankhwalawa ndi a gulu la SGLT2 inhibitors (dzina loyamba, mwachitsanzo, Forsig ndi malonda, lachiwiri likufanana ndi dzina la Dapagliflosin yogwira ntchito).

Tikukulimbikitsani kuti muwerenge: momwe mungatenge metformin

Ingitor ya SGLT-2 imateteza impsozo isanabwezeretsenso shuga m'magazi. Chifukwa chake, impso zimatha kuchepetsa kuchuluka kwa shuga m'magazi ndikuthandizira kuchotsa zochuluka kuchokera mthupi ndi mkodzo.

Werengani zambiri: Jardiance - kuteteza mtima

Impso za munthu pokonza zosefera choyamba zimachotsa shuga m'magazi ndikulola magaziwo kuti azimwenso, osagwira ntchito nthawi zonse. Munthawi yachilendo, makinawa amakakamiza thupi kugwiritsa ntchito michere yonse.

Mwa anthu omwe ali ndi shuga wambiri, gawo laling'ono la glucose silingabwezedwe, koma amamuwonjezera mkodzo, kuteteza pang'ono ku hyperglycemia. Komabe, onyamula shuga - mapuloteni am'magulu a sodium - amapanga pafupifupi 90% ya mpweya wosefedwayo kubwerera m'magazi.

Kugwira bwino ntchito kwa mankhwalawa othandizira kuchepetsa shuga kwachitika pamsonkhano wa Association of Nephrologists pa World Kidney Day pa Marichi 13, 2017. Komabe, ndi matenda oopsa a impso, amalembedwa mosamala kwambiri.

Muyenera kudziwa: za mankhwala ochepetsa shuga a m'badwo watsopano wa ma protein - GLP-1

Zolemba zogwiritsira ntchito

Buku lamalangizo

pa kugwiritsa ntchito mankhwalawa

ntchito zamankhwala

mapiritsi okhala ndi filimu

dapagliflozin propanediol monohydrate 6.150 mg, yowerengedwa monga Dapagliflozin * (Dapagliflozin *) 5 mg

microcrystalline cellulose 85.725 mg, anactrous lactose 25,000 mg, crospovidone 5,000 mg, silicon dioxide 1,875 mg, magnesium stearate 1,250 mg,

II chikasu 5,000 mg (polyvinyl mowa pang'ono hydrolyzed 2,000 mg, titanium dioxide 1,47 mg, macrogol 3350 1,010 mg, talc 0,740 mg, utoto wa iron oxide chikasu 0,073 mg).

dapagliflozin propanediol monohydrate 12.30 mg, yowerengedwa monga Dapagliflozin * (Dapagliflozin *) 10 mg

microcrystalline cellulose 171.45 mg, anactrous lactose 50.00 mg, crospovidone 1000 mg, silicon dioxide 3.75 mg, magnesium stearate 2.50 mg,

Chikasu chachikasu 10,00 mg (mowa wa polyvinyl pang'ono hydrolyzed 4.00 mg, titanium dioxide 2.35 mg, macrogol 3350 2.02 mg, talc 1.48 mg, utoto wa ayoni wachikasu 0,15 mg).

Mapiritsi ozungulira a biconvex atakulungidwa ndi nembanemba wachikasu, olembedwa "5" mbali imodzi ndi "1427" mbali inayo.

Mapiritsi a Rhomboid biconvex opakidwa utoto wachikasu wachikaso, olembedwa "10" mbali imodzi ndi "1428" mbali inayo.

Hypoglycemic wothandizira pakamwa - lembani 2 glucose transporter inhibitor

Dapagliflozin * (Dapagliflozin *) ndi wamankhwala (inhibitory pafupipafupi (Ki) wa 0.55 nM), mtundu wosankha-mtundu wa 2 glucose cotransporter inhibitor (SGLT2). SGLT2 imawonetsedwa moyenera mu impso ndipo sapezeka m'matumbo ena opitilira 70 (kuphatikizanso chiwindi, minofu yamatumbo, minofu ya adipose, gland ya mammary, chikhodzodzo, ndi ubongo).

SGLT2 ndiye chonyamula chachikulu cha glucose reabsorption mu aimpso tubules. Glucose reabsorption mu aimpso tubules kwa odwala omwe ali ndi matenda a shuga 2 mellitus (T2DM) akupitiliza ngakhale hyperglycemia. Mwa kuletsa kusinthika kwa shuga kwaimpso, Dapagliflozin * (Dapagliflozin *) amachepetsa kubwezeretsanso kwa impso tubules, komwe kumapangitsa kutsekemera kwa impso.

Kuchotsa glucose (glucosuric athari) kumachitika mutamwa mankhwala oyamba, umapitirira kwa maola 24 otsatira ndikupitilira chithandizo chonse. Kuchuluka kwa shuga komwe impso zimapangidwa chifukwa cha njirayi kumadalira kuchuluka kwa shuga m'magazi komanso kuchuluka kwa kusefedwa kwa glomerular (GFR).

Ntchito ya cell ya Beta idayenda bwino (kuyesedwa kwa NOMA, kuwunika kwa homeostasis).

Kuwonongeka kwa shuga ndi impso zomwe zimayambitsidwa ndi dapagliflozin limodzi ndi kuchepa kwa zopatsa mphamvu komanso kuchepa kwa thupi. Dapagliflozin zoletsa wa sodium glucose cotransport limodzi ndi ofooka okodzetsa ndi osakhalitsa natriuretic zotsatira.

Dapagliflozin * (Dapagliflozin *) ilibe nazo vuto kwa mayendedwe ena a shuga omwe amayendetsa glucose kupita ku zotumphukira ndipo amapitilira nthawi zoposa 1,400 posankha SGLT2 kuposa SGLT1, transporter yayikulu yamatumbo yomwe imayendetsa mayamwidwe a glucose.

Atamwa dapagliflozin ndi odzipereka athanzi komanso odwala matenda amtundu wa 2, kuwonjezeka kwa glucose komwe anapatsidwa ndi impso kunawonedwa. Pamene dapagliflozin amatengedwa pa mlingo wa 10 mg / tsiku kwa masabata 12, mwa odwala T2DM, pafupifupi 70 g ya shuga patsiku idachotsedwa ndi impso (zomwe zimafanana ndi 280 kcal / tsiku). Odwala omwe ali ndi matenda a shuga a mtundu wa 2 omwe adamwa Dapagliflozin * (Dapagliflozin *) pa mlingo wa 10 mg / tsiku kwa nthawi yayitali (mpaka zaka 2), zotupa za glucose zimasungidwa nthawi yonseyi.

Kuchulukanso kwa shuga kwa impso ndi dapagliflozin kumathandizanso kuti osmotic diuresis ndi kuchuluka kwa mkodzo kuchuluka. Kuwonjezeka kwa kuchuluka kwa mkodzo kwa odwala omwe ali ndi matenda amtundu wa 2 omwe adamwa Dapagliflozin * (Dapagliflozin *) pa mlingo wa 10 mg / tsiku, anapitilira kwa milungu 12 ndipo anakwana pafupifupi 375 ml / tsiku. Kuchuluka kwa kuchuluka kwa mkodzo kumayendera limodzi ndi kuwonjezeka kwa pang'onopang'ono komanso kwa impso, komwe sikunachititse kuti kusintha kwa sodium mu seramu yamagazi.

Pambuyo pakukonzekera pakamwa, Dapagliflozin * (Dapagliflozin *) imatengedwa mwachangu komanso kwathunthu m'matumbo am'mimba ndipo imatha kutengedwa nthawi yonse ya chakudya komanso kunja kwake. Kuchuluka kwa dapagliflozin m'madzi am'magazi (Stax) nthawi zambiri kumachitika mkati mwa maola 2 mutatha kudya.Makhalidwe a Cmax ndi AUC (dera lomwe lili pansi pa nthawi yopondera) amawonjezeka molingana ndi mlingo wa dapagliflozin.

Mtheradi bioavailability wa dapagliflozin akaperekedwa pakamwa pa 10 mg ndi 78%. Kudya kunali ndi zolimbitsa pa pharmacokinetics ya dapagliflozin mwa odzipereka athanzi. Zakudya zamafuta kwambiri zimachepetsa Stax ya dapagliflozin ndi 50%, idakulitsa Ttah (nthawi yofika ndende yambiri ya plasma) pafupifupi ola limodzi, koma sizinakhudze AUC poyerekeza ndi kusala kudya. Kusintha kumeneku sikofunikira pachipatala.

Dapagliflozin * (Dapagliflozin *) ali pafupi 91% zomanga thupi ndi mapuloteni. Odwala omwe ali ndi matenda osiyanasiyana, mwachitsanzo, omwe ali ndi vuto laimpso kapena kwa chiwindi, chizindikiro ichi sichinasinthe.

Dapagliflozin * (Dapagliflozin *) ndi glucoside yolumikizidwa ndi C yomwe aglycon yake imalumikizidwa ndi glucose ndi mgwirizano wa kaboni kaboni, womwe umatsimikizira kukhazikika kwake pakulimbana ndi glucosidases. Wapakati wama plasma hafu ya moyo (T½) mwa odzipereka athanzi anali 12,9 patatha ola limodzi dapagliflozin pakamwa pa 10 mg. Dapagliflozin * (Dapagliflozin *) imapangidwa kuti ipange metabolite yosagwira kwambiri ya dapagliflozin-3-O-glucuronide.

Pambuyo pakamwa 50 mg ya 14C-dapagliflozin, 61% ya mankhwalawo amatengedwa kuti dapagliflozin-3-O-glucuronide, yomwe imapangitsa 42% ya kuchuluka kwa placma radioacaction (AUC

) - Mankhwala osasinthika amawerengera 39% ya kuchuluka kwa madzi am'magazi. Zigawo za metabolites zomwe zatsala payekhapayekha sizidutsa 5% ya kuchuluka kwa madzi am'magazi. Dapagliflozin-3-O-glucuronide ndi ma metabolites ena alibe mankhwala. Dapagliflozin-3-O-glucuronide imapangidwa ndi enzyme uridine diphosphate glucuronosylasease 1A9 (UGT1A9), yomwe imapezeka m'chiwindi ndi impso, ndipo CYP cytochrome isoenzymes sakukhudzidwa ndi metabolism.

Dapagliflozin * (Dapagliflozin *) ndipo ma metabolites ake amachotsedwa makamaka ndi impso, ndipo ndi ochepa okha omwe amaperekedwa osasinthika. Mutatha 50 mg

C-dapagliflozin adapezeka kuti ali ndi ma radio 96% - 75% mkodzo ndi 21% mu ndowe. Pafupifupi pafupifupi 15% ya ma radioac opezeka mu ndowe adawerengedwa ndi Dapagliflozin * (Dapagliflozin *).

Pa equilibrium (ndikutanthauza AUC), kuwonekera kwa makonzedwe a dapagliflozin mwa odwala omwe ali ndi matenda a shuga a 2 komanso ofatsa, ochepa kapena ochepa aimpso (monga momwe iohexol chilolezo) anali 32%, 60%, ndi 87% kuposa omwe amapezeka ndi odwala matenda a shuga 2 impso, motero. Kuchuluka kwa shuga kwa impso masana mutatenga dapagliflozin mu ofanana kumadalira boma la impso.

Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri ndi aimpso kugwira ntchito, komanso mofatsa, pang'ono kapena pang'ono, aimpso, 85, 52, 18 ndi 11 ga glucose adachotsedwera patsiku, motero. Panalibe kusiyana pakumanga kwa dapagliflozin kupangira mapuloteni mu odzipereka athanzi komanso odwala omwe amalephera kupweteka aimpso. Sizikudziwika ngati hemodialysis imakhudzana ndi mawonekedwe a dapagliflozin.

Odwala omwe ali ndi kuchepa pang'ono kapena kosakwanira kwa hepatic, kuchuluka kwa Cmax ndi AUC ya dapagliflozin anali 12% ndi 36% apamwamba, motsatana, poyerekeza ndi odzipereka athanzi. Kusiyana kumeneku sikofunikira mwakuthupi, chifukwa chake, kusintha kwa dapagliflozin kwaofatsa komanso kosakwanira kwa hepatic sikofunikira.

Panalibe kuwonjezeka kwakadwala kovuta kwambiri kwa odwala omwe ali ndi zaka zosakwana 70 (pokhapokha ngati zifukwa zina sizakukhudzidwa). Komabe, kuwonjezeka kwawonetsero kungayembekezeredwe chifukwa kuchepa kwa ntchito yaimpso yolumikizidwa ndi zaka. Zambiri zowonekera kwa odwala azaka zopitilira 70 ndizosakwanira.

Mwa akazi, AUC wamba pamlingo wofanana ndi 22% kuposa kuposa amuna.

Palibe kusiyana kwakukulu pakumwonekera kwatsatanetsatane komwe kunapezeka pakati pa oimira amipikisano ya Caucasian, Negroid ndi Mongoloid.

Makhalidwe otsika kwambiri ndi kulemera kwamphamvu kwa thupi adadziwika. Chifukwa chake, mwa odwala omwe ali ndi thupi lozama, kuwonekera pang'ono kungadziwike, ndipo mwa odwala omwe ali ndi thupi lochulukirapo - kuchepa kwa chiwonetsero cha dapagliflozin. Komabe, kusiyana kumeneku sikofunikira mwamaganizidwe.

Mtengo wa mankhwalawo komanso momwe mungagule

Mutha kugula Forksig m'masitolo ogulitsa mankhwala ku Moscow, St. Petersburg ndi m'mizinda ina ya Russia. Koma kugulitsa mankhwala kumatheka pokhapokha ngati mwalandira mankhwala. Kuphatikiza apo, mtengo wa mankhwalawo ndiwokwera pang'ono kuposa ku Europe. Mutha kugula choyambirira cha Forxiga kuchokera kwa kugulitsa ndikugulitsa ku adilesi yomwe mwatsimikiza.

Ngati mulingo wofunikira mulibe, mankhwalawo amabweretsedwa mwachindunji ndi Germany. Mtengo wa phukusi lomwe lili ndi miyala 28 ndi ma euro 90. Ndikopindulitsa kugula bokosi la mapiritsi 98 a ma euro 160.

Alendo amawunika

Sergey Viktorovich Ozertsev, endocrinologist: "M'mbuyomu, odwala matenda ashuga a 2 amayenera kusankha njira yoyenera yolandirira kwa nthawi yayitali. Nthawi yomweyo, amakumana ndi hypoglycemia ndi zovuta zina. The munthawi yomweyo mankhwala angapo mankhwala nthawi zambiri limodzi ndi kulumpha mapiritsi, kuphwanya mlingo.

Olga, wazaka 42: “Matenda a shuga adapezeka ali ndi zaka 35. Dokotala adalangiza za kudya mosamalitsa (ndinali ndimavuto akulu onenepa). Ndidakwanitsa kuchepetsa thupi, kuyang'anira kwambiri zakudya zanga, koma shuga adakulirakonso. Poyamba, dokotalayo adapereka lingaliro la mankhwala otsika mtengo komanso osavuta, koma adamva kuwawa chifukwa cha zovuta zake. Chifukwa chake, ndidaganiza zogulira Forksigu ndipo sizinatayike. Ndimamwa kamodzi patsiku. Amva bwino, shuga ndi wabwinobwino. ”

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 zimapangidwira ndizosavuta kusiyanitsa ndi zabodza. Mapiritsi a Forsig 5 mg ali ndi mawonekedwe ozungulira ndipo olembedwa "5" ndi "1427", 10 mg ndi 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 ma analogu athunthu, 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.

Glucose yekha sangalowe mumalowedwe am'mimba, motero, onyamula sodium-glucose amatenga nawo mbali pazinthu zake zobwezeretsanso. Mtundu umodzi, SGLT2, umangokhala mu gawo limodzi la nephrons pomwe kuchuluka kwa glucose kumabwezedwanso. Mu ziwalo zina, SGLT2 sanapezeke. Zochita za Dapagliflozin zimakhazikitsidwa motengera zoletsa (zoletsa) zomwe zimachitika pantchito iyi. Zimagwira kokha pa SGLT2, sizimakhudzira 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 pama cell 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 zakulamulira, 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 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 nthawi yomweyo ndi shuga) komanso kuchepa thupi mukamagwiritsa ntchito mankhwalawa.

Zisonyezero zakudikirira

Dapagliflozin adapangira mtundu wa 2 odwala matenda ashuga. Zofunikira - kuchepa kwa kuchuluka kwa chakudya chamagulu m'zakudya, kuchita masewera olimbitsa 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 kupatsidwa kwa mapiritsi omwe amathandizira kupanga insulin.
3. Monga gawo la chithandizo chokwanira chothandizira kukonza chipukuta cha matenda a shuga.

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 kutsimikiza:

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 wokhazikika umatha kuchepetsa hemoglobin wa 1% kapena kuposerapo. Kuperewera kwa mankhwalawa amawaganizira kanthawi kochepa kogwiritsa ntchito, maphunziro ochepa otsatsa malonda. Forsigu pafupifupi samatchulidwa ngati mankhwala okhawo. Madokotala amakonda metformin, glimepiride ndi gliclazide, popeza mankhwalawa ndiokwera mtengo, amaphunziridwa bwino ndikuchotsa zovuta zamagulu omwe ali ndi matenda ashuga, ndipo osangochotsa glucose, monga Forsyga.

Anthu odwala matenda ashuga nawonso saumirira kuti atenge mankhwala atsopano, poopa kupatsirana matenda oyambitsidwa ndi bacteria. 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.

Onetsetsani kuti mwaphunzira! Kodi mukuganiza kuti kuyamwa kwa mapiritsi ndi insulini kwa nthawi yonse yokhayo ndi njira yokhayo yothanirana ndi shuga? Sichowona! Mutha kutsimikizira izi nokha ndikuyamba kuzigwiritsa ntchito. werengani zambiri >>

Dapagliflozin (Forsyga)

Type 2 shuga - matenda omwe amalumikizidwa ndi chiwopsezo chowonjezereka cha matenda amkodzo thirakiti (UTIs) ndi matenda amtundu, monga vulvovaginitis ndi balanitis mwa azimayi komanso matenda opha ziwalo zam'mimba mwa amuna 33, 34. Kuopsa kwa matendawa kumachitika kokha chifukwa cha glucosuria. Zinthu monga kukanika kwa chitetezo cha m'thupi, glycosylation wa maselo a uroepithelial nawonso ndiofunikira.

Kutengera ndi izi, dapagliflozin idavomerezedwa ndi FDA itavomerezedwa ndi European Medicines Agency (EMEA) 16, 39.

Pomaliza

Kafukufuku wofufuza ndi zamankhwala akuwonetsa mawonekedwe owoneka bwino a SGLT2 inhibitors. Gululi la mankhwalawa limapereka njira zatsopano za insulin zodziyimira pakukonza glycemia mu mtundu wa 2 wa shuga wolekerera bwino, kusakhalapo kwa zotsatira zoyipa pa kulemera kwa thupi, chiwopsezo cha hypoglycemia ndi zovuta zina zoyipa.

Mankhwala a Forsig (dapagliflozin) m'maphunziro atatha masabata 104 adawonetsa kukhathamiritsa kwakutali kwa glycemic, kuchepa kwakanenepa makamaka chifukwa cha mafuta ambiri komanso chiopsezo chochepa cha mikhalidwe ya hypoglycemic. Forsiga ndi njira ina yofananira ndi sulfonylureas mwa odwala omwe sanakwaniritse zolinga zawo ndi metformin monotherapy.