Jardins: malangizo ogwiritsira ntchito, ma analogi ndi ndemanga, mitengo yamafesi ku Russia

Kugwiritsa ntchito kwa empagliflozin pa nthawi ya pakati kumapangidwa chifukwa cha kusakwanira kwa chidziwitso chokwanira ndi chitetezo.
Zambiri zomwe zimapezeka mu preclinical maphunziro mu zinyama zimasonyezera kulowa kwa empagliflozin mkaka wa m'mawere. Ngozi yokhala ndi ana akhanda ndi ana pa nthawi yoyamwitsa sichimakhudzidwa. Kugwiritsa ntchito empagliflozin nthawi yoyamwitsa kumatsutsana. Ngati pakufunika kugwiritsa ntchito empagliflozin nthawi yoyamwitsa, kuyamwitsa kuyenera kuyimitsidwa.

Mlingo ndi makonzedwe

Monotherapy kapena kuphatikiza mankhwala
Mlingo woyambira wabwino ndi 10 mg (piritsi 1 limodzi ndi 10 mg) kamodzi patsiku, pakamwa.
Ngati mlingo wa tsiku ndi tsiku wa 10 mg usaperekenso vuto lokwanira la glycemic, muyezo ungathe kuchuluka kwa 25 mg (piritsi 1 limodzi ndi 25 mg kamodzi patsiku). Mlingo wambiri watsiku ndi tsiku ndi 25 mg.
Mankhwala JARDINS amatha kumwedwa mosasamala chakudyacho nthawi iliyonse ya tsiku.
Zochita zodumphapo kumwa kamodzi kapena zingapo za mankhwala
Pakulumpha mlingo, wodwalayo ayenera kumwa mankhwalawa akakumbukira izi.
Osamwa kawiri pa tsiku limodzi.
Magulu apadera a odwala
Pakulephera kwa impso ndi GFR kuchokera pa 45 mpaka 90 ml / mphindi / 1.73 m2, kusintha kwa mankhwalawa sikofunikira.
Odwala omwe amalephera kupweteka aimpso ndi GFR osakwana 45 ml / min / 1.73 m2 ali osavomerezeka kuti agwiritse ntchito mankhwalawa chifukwa chosakwanira.
Odwala ndi mkhutu chiwindi ntchito kusintha kusintha sikofunikira.

Bongo

Zizindikiro
Pa mayeso azachipatala omwe amayendetsedwa, mulingo umodzi wa empagliflozin womwe umafikira 800 mg (katatu pamiyeso yolowa tsiku ndi tsiku) mu odzipereka athanzi komanso Mlingo wambiri womwe umafikira 100 mg (4 times the maximum tsiku mlingo) odwala omwe ali ndi matenda a shuga a 2 amaleredwa bwino. Kuchuluka kwamkodzo kwamkodzo kuchuluka sikudalira mlingo ndipo kunalibe matendawo. Palibe chokuchitikirani ndi mlingo woposa 800 mg.
Chithandizo
Pankhani ya mankhwala osokoneza bongo, tikulimbikitsidwa kuti mankhwalawa osachiritsika achotsedwe m'matumbo, kuwunika ndi kuthandizira matenda kumachitika.

Kuchita ndi mankhwala ena
Mu vitro kugwiritsa ntchito mankhwala
Empagliflozin sikuletsa, kutsatsa, kapena kuyambitsa CYP450 isoenzymes. Njira yayikulu yogwiritsira ntchito kagayidwe ka mankhwala kaumunthu ndi glucuronidation pogwiritsa ntchito uridine-5'-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9. Empagliflozin sikuletsa UGT1A1. Kugwiritsa ntchito mankhwala osokoneza bongo a empagliflozin ndi mankhwala omwe ali gawo lapansi la CYP450 ndi UGT1A1 isoenzymes amawonedwa ngati osatheka.
Empagliflozin ndi gawo lapansi la glycoprotein P (P-gp) ndi mapuloteni odana ndi khansa ya m'mawere (BCRP). koma mu zochizira Mlingo sichiletsa mapuloteni awa. Kutengera ndi kafukufuku wochokera mu maphunziro a in vitro, akukhulupirira kuti kuthekera kwa empagliflozin kulumikizana ndi mankhwala omwe ali gawo lapansi la glycoprotein P (P-gp) ndizokayikitsa. Empagliflozin ndi gawo lapansi lonyamula ma organic anionic: OATZ, OATP1B1 ndi OATP1VZ, koma si gawo laling'ono lonyamula anionic 1 (OAT1) ndi organic cationic onyamula 2 (OST2). Komabe, kulumikizana kwa mankhwala a empagliflozin ndi mankhwala omwe ali ophatikizana ndi mapuloteni onyamula omwe afotokozedwa pamwambapa ndiwowona kuti sangayike.
Mu vivo kuyanjana kwa mankhwala osokoneza bongo
Ma pharmacokinetics a empagliflozin sasintha mwa odzipereka athanzi akagwiritsidwa ntchito limodzi ndi metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, torasemide ndi hydrochlorothiazide. Kugwiritsa ntchito kwa empagliflozin ndi gemfibrozil, rifampicin ndi probenecid kukuwonetsa kuwonjezeka kwa AUC ya empagliflozin ndi 59%, 35% ndi 53%, komabe, zosinthazi sizinawonedwe ngati zamankhwala.
Empagliflozin ilibe gawo lililonse pama pharmacokinetics a metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin. digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide ndi kulera kwamlomo.
Zodzikongoletsera
Empagliflozin imatha kukongoletsa kukodzetsa kwa thiazide ndi "loop" diuretics, yomwe imatha kukulitsa vuto lakusowa kwamadzi ndi magazi ochepa.
Insulin ndi mankhwala omwe amathandizira kubisalira kwake
Insulin ndi mankhwala omwe amathandizira kubisika kwake, monga sulfonylureas, amatha kukulitsa chiopsezo cha hypoglycemia. Chifukwa chake, kugwiritsa ntchito nthawi imodzimodzi ya empagliflozin ndi insulin ndi mankhwala omwe amathandizira kutulutsa kwake, zingakhale zofunikira kuti muchepetse mlingo wawo, kuti mupewe chiopsezo cha hypoglycemia.

Malangizo apadera

Mankhwala JARDINS ali osavomerezeka kwa odwala omwe ali ndi matenda a shuga 1 komanso kuthandizira matenda ashuga a ketoacidosis.
Mulingo wambiri watsiku ndi tsiku wa JARDINS uli ndi 113 mg wa lactose, kotero mankhwalawa sayenera kugwiritsidwa ntchito mwa odwala omwe ali ndi vuto laling'ono monga kuperewera kwa lactase, tsankho lactose, glucose-galactose malabsorption.
Kafukufuku wachipatala awonetsa kuti chithandizo ndi empagliflozin sichimabweretsa chiwopsezo cha mtima. Kugwiritsa ntchito mphamvu ya empagliflozin pa 25 mg sikupangitsa kuti pakhale nthawi yayitali ya QT.
Pogwiritsa ntchito limodzi mankhwala JARDINS omwe ali ndi zotumphukira za sulfonylurea kapena insulin, kuchepetsedwa kwa mankhwala a sulfonylurea / insulin kungafunike chifukwa cha chiopsezo cha hypoglycemia.
Osaphunzitsidwa kuphatikiza kwa mankhwala a hypoglycemic
Empagliflozin sanaphunziridwe limodzi ndi glucagon-peptide 1 analogues (GLP-1).
Impso ntchito kuwunika
Mphamvu ya mankhwala JARDINS zimatengera ntchito ya impso. Chifukwa chake, tikulimbikitsidwa kuwunika ntchito ya impso isanakhazikitsidwe komanso nthawi ya mankhwala (osachepera kamodzi pachaka), komanso asanaikidwe pochiza, yomwe ingasokoneze ntchito ya impso. Odwala omwe ali ndi vuto la impso (GFR ochepera 45 mlmin). kumwa mankhwala ali osavomerezeka.
Odwala okalamba
Odwala azaka zapakati pa 75 ndi kupitirira ali ndi chiopsezo chowonjezeka chakumadzi. Mu odwala omwe amathandizidwa ndi empagliflozin, zovuta zoyipa zomwe zimayambitsidwa ndi hypovolemia nthawi zambiri zimawonedwa (poyerekeza ndi odwala omwe akulandira placebo). Kukumana ndi kugwiritsa ntchito kwa empagliflozin mwa odwala opitilira zaka 85 kumakhala kochepa, motero, sikulimbikitsidwa kupereka mankhwala a DZHARDINS kwa odwala omwe ali ndi zaka 85.
Gwiritsani ntchito odwala omwe ali pachiwopsezo cha kukhala ndi hypovolemia
Malinga ndi kayendedwe ka kayendedwe, kayendetsedwe ka mankhwala JARDINS kumatha kutsitsa magazi moyenera. Chifukwa chake, mankhwalawa ayenera kugwiritsidwa ntchito mosamala ngati vuto la kuchepa kwa magazi ndilosafunikira, mwachitsanzo, odwala omwe ali ndi matenda amtima, odwala omwe amamwa antihypertensive mankhwala (omwe ali ndi mbiri yakale ya hypotension), komanso odwala omwe ali ndi zaka zoposa 75.
Zikachitika kuti wodwalayo akumwa mankhwala JARDINS. zinthu zomwe zingayambitse kuchepa kwa madzimadzi (mwachitsanzo, ndi matenda am'mimba), chikhalidwe cha wodwalayo, kuthamanga kwa magazi kuyenera kuyang'aniridwa mosamala, komanso hematocrit ndi usawa wa electrolyte. Pangafunike kwakanthawi, mpaka kubwezeretsa bwino madzi, kusiya mankhwala.
Matenda amitsempha
Zotsatira zoyipa monga matenda amkodzo thirakiti anali wofanana ndi empagliflozin pa 25 mg ndi placebo, komanso wokwera ndi empagliflozin pa 10 mg. Matenda a kwamkodzo ovuta (monga pyelonephritis ndi urosepsis) amawonedwanso pafupipafupi ngati odwala akutenga empagliflozin ndi placebo. Pankhani ya matenda ovuta kwamikodzo, kuyimitsidwa kwakanthawi kwa mankhwala a empagliflozin ndikofunikira.
Urinalysis Laborator
Malinga ndi limagwirira zake odwala kumwa mankhwala JARDINS, shuga mu mkodzo mtima.

Zokhudza mphamvu pakutha kuyendetsa magalimoto ndi zida
Kafukufuku wamankhwala wokhudzana ndi mphamvu ya empagliflozin pa kuyendetsa magalimoto ndi machitidwe sanachitike. Odwala ayenera kusamala poyendetsa magalimoto ndi maginito, popeza mukamagwiritsa ntchito mankhwala JARDINS (makamaka kuphatikiza ndi zotumphukira za sulfonylurea ndi / kapena insulin), hypoglycemia imayamba.

Ogonjera a Jardins

NovoNorm (mapiritsi) Kutalika: 163

Analogue ndiotsika mtengo kuchokera ku ma ruble 59.

NovoNorm ndimakonzedwe a piritsi kuchokera ku gulu lomwelo lamankhwala, koma pogwiritsa ntchito njira ina. Repaglinide imagwiritsidwa ntchito pano pa mulingo wa 0,5 mpaka 2 mg. Zizindikiro zakupangira zikufanana, koma ma contraindication amasiyana chifukwa cha ma DV osiyanasiyana pamapiritsi, kotero werengani malangizo mosamala ndikuwonana ndi dokotala.

Diagninide (mapiritsi) Kutalika: 142

Diagninide ndi chi Russia cholowa mmalo amtundu womwewo ndi mapiritsi amodzi phukusi lililonse. The kapangidwe ndi Mlingo wa yogwira mankhwala amakhalanso osiyana Jardins, koma mankhwala mankhwala 2 matenda osagwira ntchito zolimbitsa thupi ndi zakudya.

Zambiri pazamankhwala, kapangidwe kake

Mankhwala Jardins amagwiritsidwa ntchito kuwongolera shuga m'magazi panthawi ya monotherapy. Kuphatikiza apo, chida ichi chitha kugwiritsidwa ntchito ngati gawo pa zovuta pakuchiza matenda ashuga.

Chida ichi chitha kugwiritsidwa ntchito limodzi ndi mankhwala ena a hypoglycemic. Mankhwalawa atha kuphatikizira insulin kapena metformin.

Mankhwala pamsika wa mankhwala a pharmacological amagulitsidwa m'mitundu iwiri yosiyanasiyana muyezo wa mankhwala omwe amapanga.

Kutengera mlingo wa mankhwala othandizira, piritsi limodzi lokonzekera limatha kukhala ndi 10 kapena 30 mg ya mankhwala othandizira.

Kuphatikiza pazomwe zimagwira, zida zotsatirazi zimaphatikizidwa piritsi limodzi lamankhwala:

• lactose monohydrate,
• cellcrystalline mapadi,
• Hyprolose
• sodium croscarmellose,
• silika
• magnesium wakuba.

Mapiritsi a mankhwalawa ndi zokutira, zomwe zimakhala ndi izi:

1. Opadra chikasu,
2. hypopellose,
3. titanium dioxide
4. talcum ufa
5. macrogol 400,
6. iron oxide ndi chikasu.

Mukamagwiritsa ntchito mankhwalawa, muyenera kukumbukira kuti kugwiritsa ntchito Jardins kuti shuga asakhale m'magazi a wodwala wodwala matenda a mtundu wa 2 sikungapulumutse munthu kudwala.

Chachikulu pharmacological zimatha mankhwala

Mankhwala Jardins nthawi zambiri amagwiritsidwa ntchito ngati mankhwala amakono kukonza shuga yayikulu yamagazi mwa munthu yemwe ali ndi matenda a shuga a 2.

Ndemanga ya akatswiri azachipatala akuwonetsa kuti chida ichi chimapangitsa kuti azitha kuwongolera bwino zomwe zili mthupi la wodwalayo ndikupeza zotsatira zabwino.

Empagliflozin, yemwe ali gawo lalikulu la mankhwalawo, ndiwosankha, wogwiritsidwanso ntchito wampikisano wothamanga wa transporter wapadera wama protein.

Izi zimawongolera kutha kuwongolera kuchuluka kwa shuga mthupi la wodwala yemwe ali ndi matenda ashuga a 2. Zomwe zimagwiritsidwa ntchito ndi mankhwalawa ndikuti zimathandizira kuchepetsa kufalikira kwa glucose pamagulu a impso. Mukamagwiritsa ntchito mankhwalawa, shuga mumkodzo amachulukana, zomwe zimapangitsa kuti magazi athetse msanga m'thupi.

Kugwiritsa ntchito mankhwalawa sikungawononge ntchito ya maselo a beta. Pulogalamu yogwira imakhala ndi phindu pancreatic minofu, yomwe imathandizira kukonza magwiridwe ake.

Kukhazikitsidwa kwa empagliflozin m'thupi kumakhudza bwino njira yopsereza mafuta komanso kumathandizira kuchepetsa kulemera kwa wodwala yemwe ali ndi matenda ashuga a 2. Izi zowonjezera chifukwa chogwiritsa ntchito mankhwalawa ndizofunikira kwambiri kwa anthu omwe ali onenepa kwambiri ndi matenda a shuga a 2.

Hafu ya moyo wa yogwira mankhwala amapangidwa kwa maola 12. Mlingo wokhazikika mthupi la wogwira ntchito limodzi ndi mlingo umodzi wa mankhwalawa patsiku umatheka mukalandira mlingo wachisanu.

Kuchokera m'thupi laumunthu, mpaka 96% ya mankhwalawo omwe amwedwa amachotsedwa. Excretion ya metabolites imachitika pogwiritsa ntchito matumbo ndi impso. Kudzera m'matumbo, pawiri yogwira imachotsedwa osasinthika. Mukapukusidwa kudzera mu impso, ndi 50% yokha ya mankhwala omwe amagwiritsidwa ntchito omwe amachotsedwa osasinthika.

The ndende ya yogwira pawiri mu thupi amathandizidwa kwambiri ndi kupezeka kwa wodwalayo aimpso kapena kwa chiwindi ntchito.

Kulemera kwa thupi la munthu, jenda ndi zaka zake sizimakhudza kwambiri pharmacokinetics yogwira mankhwala.

Malangizo ogwiritsira ntchito mankhwalawa

Mankhwalawa amagwiritsidwa ntchito popangira mankhwala a mono - kapena zovuta. Mlingo woyenera ndi 10 mg - piritsi limodzi patsiku. Mankhwala amaperekedwa pakamwa.

Ngati tsiku ndi tsiku 10 mg yalephera kupereka yachilendo matenda a glycemic, mlingo womwe umagwiritsidwa ntchito umatha kuchuluka mpaka 25 mg pa tsiku. Mulingo wovomerezeka wa mankhwalawa ukhoza kukhala 25 mg.

Mankhwalawa amaloledwa kumwa nthawi iliyonse, mosasamala mtundu wa chakudya.

Ngati mukusowa nthawi yomwe mumamwa mankhwalawa, simuyenera kumwa kawiri mlingo wa mankhwalawa patsiku.

Ndi kulephera kwakukulu kwa aimpso, mankhwalawa samalimbikitsidwa, chifukwa chosagwira ntchito chifukwa chogwiritsa ntchito mankhwalawa.

Ngati wodwala ali ndi vuto la chiwindi, lomwe limawoneka ngati kulephera kwa chiwindi, kusintha kwa mankhwalawa kwa mankhwalawa sikofunikira.

Sitikulimbikitsidwa kugwiritsa ntchito mankhwalawa mukanyamula mwana ndikuyamwitsa, chifukwa chosowa chidziwitso pakuchita bwino komanso chitetezo cha mankhwalawa kwa mayi ndi mwana panthawiyi.

Pankhani ya kulephera kwa impso, mphamvu ya mankhwalawa imatengera kuchuluka kwa kulephera kugwira ntchito.

Ndikulimbikitsidwa kuti muwoneke ntchito ya impso musanagwiritse ntchito mankhwala, ndipo tikulimbikitsidwa kuti muziwonetsetsa ntchito ya impso kamodzi pachaka pogwiritsira ntchito Jardins.

Ndi zoletsedwa kugwiritsa ntchito mankhwalawa muubwana. Kuletsa kugwiritsa ntchito kumagwiranso kwa odwala onse osakwana zaka 18. Izi ndichifukwa chosowa kafukufuku pazantchito ndi chitetezo.

Sikulimbikitsidwa kugwiritsa ntchito mankhwalawa pochiza odwala azaka zopitilira 75. Izi nthawi zambiri zimagwirizanitsidwa ndi kukula kwakukulu kwa mkhalidwe wakusowa kwamadzi.

Simuyenera kugwiritsa ntchito chida pochiza odwala omwe ali ndi matenda a shuga 1 komanso odwala matenda ashuga a ketoacidosis.

Pogwiritsa ntchito mlingo woyenera wa mankhwala a Jardins, pafupifupi 113 mg ya lactose imalowa m'thupi la wodwalayo.

Chida ichi sichiyenera kugwiritsidwa ntchito ngati wodwala ali ndi vuto lactase, lactose tsankho kapena glucose-galactose malabsorption m'thupi.

Zotsatira zoyipa ndi contraindication mukamagwiritsa ntchito mankhwalawa

Zotsatira zoyipa kwambiri za kutenga empagliflozin ndikoyamba kwa zizindikiro za hypoglycemia.

Nthawi zambiri, zotsatira zoyipa za hypoglycemia zimadziwonetsera pogwiritsa ntchito mankhwala osakanikirana ndi sulfonylurea kapena ndi insulin.

Kuphatikiza pa hypoglycemia, odwala omwe amagwiritsa ntchito empagliflozin amatha kulimbana ndi zovuta zingapo.

Zotsatira zoyipa zomwe mukugwiritsa ntchito mankhwalawa ndi izi:

1. Maonekedwe a matenda opatsirana komanso ma parasitic monga vulvovaginitis, balanitis, vagidi candidiasis, ndi matenda amkodzo thirakiti.
2. Zotsatira za kusintha kwa kagayidwe kazakudya mthupi, hypovolemia ikhoza kuchitika.
3. Kuwonjezeka kwakukulu pokodza.
4. Kupezeka kwa zizindikiro za kuchepa madzi m'thupi, komwe nthawi zambiri kumawonedwa ndi kugwiritsa ntchito mankhwalawa okalamba.

Ndemanga za mankhwalawa, anthu omwe amawagwiritsa ntchito, akuwonetsa kuti zovuta zina mthupi la wodwalayo ndizosowa kwambiri. Zizindikiro zoyambirira za zotsatira zoyipa zikaonekera, muyenera kusiya kumwa mankhwalawo ndikupempha thandizo kwa dokotala.

Mfundo zazikuluzikulu zogwiritsa ntchito mankhwalawa ndi izi:

• mtundu 1 shuga
• otsika ochepa kwambiri
• matenda ashuga ketoacidosis,
• lactose tsankho,
• Mimba ndi kuyamwa
• mkhalidwe wamthupi womwe umawopseza kupezeka kwa madzi m'thupi.

Musanagwiritse ntchito mankhwalawa, muyenera kufunsa dokotala ndikuwunikira thupi kuti mupeze zotsutsana zilizonse.

Mgwirizano wa mankhwalawa, mtengo wake komanso kuyanjana ndi mankhwala ena

Pa msika wa mankhwala ku Russia, ndi mankhwala a Jardins okha, omwe amapangidwa pamaziko a empagliflozin, omwe amagulitsidwa. Kuchokera pomwe titha kunena kuti palibe fanizo la mankhwalawa pamsika waku Russia. Othandizira ena omwe ali ndi machitidwe a hypoglycemic ali ndi zotsatira zosiyana mthupi.

Mtengo wa mankhwalawa umatengera dera lomwe amagulitsa mankhwalawo, komanso kwa amene akuwapatsa mankhwalawo. Mtengo wapakati wa mankhwalawa Jardins ku Russia umachokera ku 850 mpaka 1030 rubles.

Mukamagwiritsa ntchito mankhwalawa, tiyenera kukumbukira kuti amatha kupatsa mphamvu diuretic yamagwiritsidwe ntchito ena a thiazide okodzetsa, omwe angathandize kukulitsa kuchepa kwa madzi m'thupi komanso kuwononga thupi.

Chosafunikira ndikuphatikizidwa kwa Jardins ndi mankhwala omwe amapangidwa kuti azithamanga magazi.

Kugwiritsa ntchito pamodzi kwa mankhwala a insulin, Jardins ndi mankhwala omwe amachititsa kuti mahomoni achilengedwe azitha kupanga mawonekedwe a hypoglycemia. Pochita mankhwala osokoneza bongo, kusintha mosamala kwa mankhwalawa komanso kuyamwa kwa mankhwala omwe amayang'aniridwa ndi adokotala amafunikira. Ndipo vidiyo yomwe yatchulidwa munkhaniyi ikamba za matenda a shuga.

Mitengo ya ma jardins ku malo ogulitsa mankhwala ku Moscow

Madokotala amawunika za ma jardins

Imagwira kwambiri polimbana ndi glycemia, imathandizira kuchepetsa thupi.

Chiwopsezo chowonjezeka cha zovuta za urogenital.

Mankhwalawa ali ndi phindu pa glycemia, koma amafunika ukhondo nthawi zonse, zomwe sizingatheke kwa odwala onse. Popanda kuwona malamulo a mankhwala azakudya, zomwe zikuwonetsa za kagayidwe kazachilengedwe zimatheka mwa odwala omwe alibe kuwonjezeka kwakukulu kwa glycemia. Kuchepetsa kudya kwa calorie chifukwa kuchotsedwa kwa shuga mumkodzo ndi njira ina yabwino, komabe, yoperewera nthawi.

Ndi mankhwala abwino kwa odwala omwe ali ndi matenda osokoneza bongo.

Mkodzo mwa odwala ndi madzi a shuga, omwe amachepetsa kwambiri matenda amtunduwu. Odwala ayenera kutsatira ukhondo mosamalitsa. Ndikufuna kukumbukira lipoti la FDA lonena za chiopsezo chachikulu cha matenda am'mimba chifukwa cha chiwopsezo chachikulu cha matenda obadwa nawo.

Mankhwalawa ndi mtundu wa kusintha kwa mtima. Matenda a shuga amayamba pang'onopang'ono kukhala nthambi yamatenda a mtima, ndipo ndi yoyamba kukhala yogwira mtima yolimbana ndi matenda osokoneza bongo omwe ali ndi maubwino owonekera pokhudzana ndi mphamvu yake pamtima.

Hypoglycemic yabwino kwambiri yamatenda a shuga 1. Zimayenda bwino ndi mankhwala ena a hypoglycemic ndi insulin. Imakhala ndi njira yosakongoletsa.

Mtengo uli pamwamba pa avareji.

Imagwira ntchito bwino. Odwala amadziwa kuphweka kwa kugwiritsidwa ntchito - 1 nthawi patsiku, zomwe zimathandiza kwambiri kutsatira wodwalayo.

Mankhwala "Jardins" ndi othandiza kwambiri pakadali pano pochiza matenda ashuga. Mankhwalawa adalembetsedwa ku Russian Federation. Odwala ambiri amachitcha "mapiritsi a insulin." Zotsatira zimawonekera mofulumira. Masiku ano, mankhwalawa ndi njira ina yosinthira insulin.

Ndemanga za Jardins Odwala

Matendawa akhazikitsidwa kuyambira chaka cha 2012. Shuga sanatsike ndi mankhwala aliwonse, chifukwa chake, adayikidwa mwachangu kwa insulin zaka 3. Poyamba inkasunga mayunitsi 16-16, kenako 18-16, ndi miyezi 4 yapitayo. Mayunitsi 22-18 Koma adotolo sasintha mankhwalawa, amangokulitsa mlingo. Ndipo zidachitika, a Jardins adachita zothandizira, kupereka mayeso. Pambuyo masiku atatu, shuga - 10 mayunitsi, ndi magawo 8. Ndili ndi mphamvu komanso chidwi chamoyo! Koma ndi mwezi, iwo samalemba kwaulere, palibe njira yoti mugule nokha. Koma ndikulimbikitsa kwambiri, kwa iwo omwe alibe kupita patsogolo mu chithandizo, zithandizadi.

Pharmacology

Oral hypoglycemic mankhwala. Empagliflozin ndiwosinthika, wogwira ntchito kwambiri, wosankha komanso wampikisano wa mtundu wa 2 wodutsa glucose woperekera ndende ndikufunikira kuti tiletse 50% ya ntchito ya enzyme (IC₅₀), lofanana ndi 1.3 nmol. Kusankha kwa empagliflozin ndi okwera 5,000 kuchulukirapo kuposa mtundu wa glucose wopatsirana ndi sodium yemwe amachititsa kuti shuga ayambe kuyamwa.

Kuphatikiza apo, zidapezeka kuti empagliflozin imasankha kwambiri anthu ena okhathamira omwe amayendetsa glucose homeostasis m'malo osiyanasiyana.

Mtundu 2 wa glucose wopatsirana ndi sodium ndiye puloteni yonyamula kwambiri yomwe imapangitsa kuti shuga ayambidwenso kuchokera ku chimpso chamadzimadzi kulowa m'magazi.

Empagliflozin imathandizira kuwongolera kwa glycemic mwa odwala omwe ali ndi matenda a shuga 2 ndikuchepetsa reghorpose glucose. Kuchuluka kwa shuga komwe impso zimagwiritsidwa ntchito m'njira imeneyi zimadalira kuchuluka kwa shuga m'magazi ndi GFR. Kuletsa kwa sodium wodalira wa mtundu 2 shuga mwa odwala matenda ashuga a 2 ndi hyperglycemia kumabweretsa kuchotsedwa kwa shuga ndi impso.

M'mayesero azachipatala, zidapezeka kuti odwala omwe ali ndi matenda amtundu wa 2, kuchuluka kwa shuga mwa impso kumawonjezeka atangomaliza muyezo woyamba wa mankhwala a empagliflozin, izi zimachitika kwa maola 24. Kuwonjezeka kwa shuga kwa impso kumapitirirabe mpaka kumapeto kwa nyengo ya milungu 4. kugwiritsa ntchito empagliflozin pa mlingo wa 25 mg 1 nthawi / tsiku, pafupifupi, pafupifupi 78 g / tsiku. Odwala omwe ali ndi matenda a shuga 2, kuwonjezeka kwa kuchuluka kwa shuga ndi impso kunayambitsa kutsika kwamphamvu kwa shuga m'magazi a m'magazi.

Empagliflozin amachepetsa kuchuluka kwa shuga m'magazi am'magazi posala kudya komanso mukatha kudya.

Limagwirira a empagliflozin sizitengera magwiridwe antchito a pancreatic β-cell ndi insulin metabolism. Zotsatira zabwino za empagliflozin pazodziwitsa za ntchito za cells-cell zidadziwika, kuphatikizapo index ya HOMA-β (chitsanzo pakuwunika homeostasis) komanso kuchuluka kwa proinsulin kuti insulin. Kuphatikiza apo, kuchotsa kwa shuga ndi impso kumayambitsa kuchepa kwa zopatsa mphamvu, komwe kumayendetsedwa ndi kuchepa kwa kuchuluka kwa minofu ya adipose komanso kuchepa kwa thupi.

Glucosuria yomwe imagwiritsidwa ntchito pa empagliflozin imayendera limodzi ndi kuwonjezeka pang'ono kwa diuresis, zomwe zimapangitsa kuchepa kwambiri kwa magazi.

M'maphunziro azachipatala komwe empagliflozin adagwiritsidwa ntchito ngati monotherapy, kuphatikiza mankhwala ophatikizika ndi metformin, kuphatikiza mankhwala ophatikizidwa ndi metformin mwa odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga, kuphatikiza mankhwala ophatikizika ndi metformin ndi sulfonylurea, kuphatikiza mankhwalawa ndi pioglitazone +/- metformin linagliptin odwala omwe ali ndi mtundu wachiwiri wa matenda ashuga a 2, kuphatikiza mankhwala ndi linagliptin, omwe adawonjezeredwa ku mankhwala a metformin, palimodzi FDI yokhala ndi metformin motsutsana ndi glimepiride (deta kuchokera ku kafukufuku wazaka 2), kuphatikiza mankhwala ophatikizira ndi insulin (ma insulin angapo a insulin) +/- metformin, kuphatikiza mankhwalawa ndi basal insulin, kuphatikiza chithandizo ndi dipeptidyl peptidase-4 inhibitor (DPP-4), metformin +/- mankhwala ena amkamwa a hypoglycemic awonetsedwa kuti ali ndi kuchepa kwakukulu kwa glycosylated hemoglobin (Hb_A1c), kuchepa kwa chidwi cha kutsika kwa shuga m'magazi, komanso kuchepa kwa kuthamanga kwa magazi ndi kunenepa kwambiri kwa thupi.

Pharmacokinetics

Ma pharmacokinetics a empagliflozin adaphunziridwa kwathunthu mu odzipereka athanzi komanso odwala omwe ali ndi matenda a shuga a mtundu wachiwiri.

Pambuyo pakuyamwa, empagliflozin imatengeka mwachangu, C_max empagliflozin m'madzi am'magazi amafikira pambuyo maola 1.5. Kenako, kuchuluka kwa empagliflozin mu plasma kumachepa biphasic. AUC wamba pa nthawi yokhazikika ya plasma anali 4740 nmol × h / l, ndi mtengo wa C_max - 687 nmol / L. Kudya sikukhala ndi vuto lililonse pama pharmacokinetics a empagliflozin.

Ma pharmacokinetics a empagliflozin mwa odzipereka athanzi komanso mwa odwala omwe ali ndi matenda a shuga 2 amakhala ofanana.

V_d Mu nthawi ya ndende yolimba m'madzi am'magazi mumapanga pafupifupi 73.8 l. Pambuyo pakulankhula pakamwa ndi odzipereka othandiza olembedwa enagliflozin 14 C, kumanga mapuloteni a plasma anali 85%. Mukamagwiritsa ntchito empagliflozin 1 nthawi / tsiku C_ss mu plasma adakwaniritsidwa pambuyo lachisanu.

Njira yayikulu yogwiritsira ntchito mphamvu ya metabolaguriflozin mwa anthu ndi glucuronidation ndikuchita nawo uridine-5'-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9. Ma metabolites omwe amadziwika kwambiri a empagliflozin ndi ma glucuronic conjugates atatu (2-O, 3-O ndi 6-O glucuronide). Mphamvu ya metabolite iliyonse imakhala yochepa (zosakwana 10% ya mphamvu yonse ya empagliflozin).

T_1/2 ndi pafupifupi maola 12.4. Atalembera enagliflozin 14 C olembedwa modzipereka, pafupifupi 96% ya mankhwalawa idachotsedwa (m'matumbo - 41%, impso - 54%). Kudzera m'matumbo, mankhwala ambiri omwe adalembedwa kuti anali osasinthika sanasinthidwe. Hafu imodzi yokha yolembedwa yomwe idatulutsidwa ndi impso ndi yosasinthika.

Pharmacokinetics pamagulu apadera a odwala

Odwala omwe ali ndi vuto lochepa, ochepa komanso owonjezera aimpso (30 2) komanso odwala omwe amalephera kusintha kwa impso, AUC ya empagliflozin inakula pafupifupi 18%, 20%, 66%, ndi 48%, motero, poyerekeza ndi odwala omwe ali ndi vuto labwinobwino impso. Odwala ndi zolimbitsa aimpso kulephera ndi odwala end-siteji aimpso kulephera C_max empagliflozin mu plasma inali yofanana ndi mfundo zofanana mwa odwala omwe ali ndi vuto laimpso. Odwala wofatsa kwambiri aimpso kulephera_max empagliflozin mu plasma anali pafupifupi 20% kuposa kuposa odwala wamba yachilendo ntchito. Zotsatira za kusanthula kwa anthu a zakumwa zamtundu wa anthu zidawonetsa kuti chiwonetsero chonse cha empagliflozin chatsika ndikuchepa kwa GFR, zomwe zidapangitsa kuti chiwopsezo cha mankhwalawo chikwanire.

Odwala omwe ali ndi vuto lochepa, modekha, komanso zovuta kwa chiwindi (malinga ndi gulu la ana-Pugh), mfundo za AUC za empagliflozin zidakula pafupifupi 23%, 47%, ndi 75%, motsatana, ndi C_max pafupifupi 4%, 23% ndi 48%, motero (poyerekeza ndi odwala omwe ali ndi chiwindi chambiri).

BMI, jenda, mtundu, komanso zaka sizinakhale ndi vuto lililonse pakamerokamziki.

Maphunziro a pharmacokinetics a empagliflozin mwa ana sanachitike.

Kutulutsa Fomu

Mapiritsiwa ndi filimu yokutidwa ndi mtundu wachikaso chopepuka, chozungulira, cha biconvex, chokhala ndi mbali zokutidwa, cholembedwa ndi chizindikiro cha kampani mbali inayo ndi "S10" mbali inayo.

Omwe amathandizira: lactose monohydrate - 162,5 mg, microcrystalline cellulose - 62,5 mg, hyprolose (hydroxypropyl cellulose) - 7.5 mg, croscarmellose sodium - 5 mg, colloidal silicon dioxide - 1.25 mg, magnesium stearate - 1.25 mg.

Mapangidwe a Shell: Opadry chikasu (02B38190) - 7 mg (hypromellose 2910 - 3.5 mg, titanium dioxide - 1.733 mg, talc - 1.4 mg, macrogol 400 - 0,35 mg, iron oxide chikasu - 0,018 mg).

Ma PC 10 - matuza (1) - mapaketi a makatoni.
Ma PC 10 - matuza (3) - mapaketi a makatoni.

Mankhwala amatengedwa pakamwa, nthawi iliyonse masana, mosasamala kanthu za kudya.

Mlingo woyambira wabwino ndi 10 mg 1 nthawi / tsiku. Ngati mlingo wa tsiku ndi tsiku wa 10 mg usaperekedwe koyenera kwa glycemic, muyezo ungathe kuchuluka kwa 25 mg 1 nthawi / tsiku.

Mlingo wambiri watsiku ndi tsiku ndi 25 mg.

Pakulumpha mlingo, wodwalayo ayenera kumwa mankhwalawa akakumbukira izi. Osamwa kawiri pa tsiku limodzi.

Kwa odwala omwe ali ndi vuto la impso ndi GFR kuchokera pa45 mpaka 90 ml / mphindi / 1.73 m 2, kusintha kwa mankhwalawa sikofunikira. Odwala omwe ali ndi vuto la impso ndi GFR 2, kugwiritsa ntchito mankhwalawa sikulimbikitsidwa chifukwa chosakwanira.

Odwala ndi mkhutu chiwindi ntchito kusintha kusintha sikofunikira.

Kuchita

Empagliflozin imatha kupititsa patsogolo okodzetsa a thiazide ndi "loop" okodzetsa, omwe, nawonso, amatha kukulitsa kuchepa kwa madzi m'thupi komanso ochepa hypotension.

Insulin ndi mankhwala omwe amathandizira kubisika kwake, monga sulfonylureas, amatha kukulitsa chiopsezo cha hypoglycemia. Chifukwa chake, kugwiritsa ntchito nthawi imodzimodzi ya empagliflozin ndi insulin ndi mankhwala omwe amathandizira kutulutsa kwake, zingakhale zofunikira kuti muchepetse mlingo wawo, kuti mupewe chiopsezo cha hypoglycemia.

Mu vitro kugwiritsa ntchito mankhwala. Empagliflozin sikuletsa, kutsatsa, kapena kuyambitsa CYP450 isoenzymes. Njira yayikulu yogwiritsira ntchito metabolism ya empagliflozin mwa anthu ndi glucuronidation ndi kutenga nawo uridine-5'-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9. Empagliflozin sikuletsa UGT1A1. Kugwiritsa ntchito mankhwala osokoneza bongo a empagliflozin ndi mankhwala omwe ali gawo lapansi la CYP450 ndi UGT1A1 isoenzymes amawonedwa ngati osatheka.

Empagliflozin ndi gawo limodzi la P-glycoprotein komanso kukana kwa khansa ya m'mawere komwe kumatsimikiza mapuloteni (BCRP), koma sikuletsa mapuloteni awa pamankhwala ochepetsa. Kutengera ndi kafukufuku wochokera ku maphunziro a in vitro, akukhulupirira kuti kuthekera kwa empagliflozin kulumikizana ndi mankhwala omwe ali gawo lapansi la P-glycoprotein ndikokayikitsa. Empagliflozin ndi gawo lapansi lonyamula ma organic anionic: OAT3, OATP1B1 ndi OATP1B3, koma si gawo laling'ono lonyamula anionic 1 (OAT1) ndi organic cationic onyamula 2 (OST2). Komabe, kulumikizana kwa mankhwala a empagliflozin ndi mankhwala omwe ali gawo lapansi kwa mapuloteni onyamula omwe atchulidwa pamwambawa ndiwowona kuti sangayike.

Mu vivo kuyanjana kwa mankhwala osokoneza bongo. Ndi kuphatikiza kwa empagliflozin ndi mankhwala ena omwe amagwiritsidwa ntchito, palibe zofunika kwambiri pakubwera kwamachitidwe a pharmacokinetic. Zotsatira za kafukufuku wa pharmacokinetic zikuwonetsa kuti palibe chifukwa chosintha mlingo wa mankhwala a Jardins ® pomwe amagwiritsidwa ntchito ndi mankhwala omwe amagwiritsidwa ntchito masiku onse.

Ma pharmacokinetics a empagliflozin sasintha mwa odzipereka athanzi akagwiritsidwa ntchito limodzi ndi metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, torasemide ndi hydrochlorothiazide. Kugwiritsa ntchito kwa empagliflozin ndi gemfibrozil, rifampicin ndi probenecid kukuwonetsa kuwonjezeka kwa AUC ya empagliflozin ndi 59%, 35% ndi 53%, komabe, zosinthazi sizinawonedwe ngati zamankhwala.

Empagliflozin ilibe gawo lalikulu pakumera kwa pharmacokinetics ya metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide ndi njira yolerera pakamwa mwa odzipereka athanzi.

Zotsatira zoyipa

Zomwe zimachitika nthawi zambiri zovuta kwa odwala omwe amalandila empagliflozin kapena placebo zinali zofanananso ndi mayesero azachipatala. Chotsatira chovuta kwambiri chinali hypoglycemia, chomwe chimagwiritsidwa ntchito ndi empagliflozin kuphatikiza ndi sulfonylurea kapena insulin.

Zotsatira zoyipa zomwe zimawoneka mwa odwala omwe amalandila empagliflozin mu maphunziro oyendetsedwa ndi placebo amaperekedwa pansipa molingana ndi gulu la ziwalo ndi machitidwe ndi njira zomwe zimakondedwa ndi MedDRA zosonyeza kutsutsana kwawo kokwanira. Magawo a pafupipafupi amafotokozedwa motere: Nthawi zambiri (≥1 / 10), nthawi zambiri (kuchokera ≥1 / 100 mpaka 2,

Mochenjera: odwala omwe ali ndi chiopsezo chokhala ndi hypovolemia (kugwiritsa ntchito mankhwala a antihypertensive omwe ali ndi mbiri yokhudzana ndi ochepa ochepa), omwe ali ndi matenda am'mimba omwe amachititsa kuti magazi asatayike, matenda amtundu wa genitourinary, ogwiritsira ntchito limodzi ndi sulfonylureas kapena insulin, zakudya zamagulu ochepa a ketoacidosis mbiri yakale, zochitika zazinsinsi za maselo a pancreatic beta, odwala azaka zopitilira 75.

Mimba komanso kuyamwa

Kugwiritsa ntchito kwa empagliflozin pa nthawi ya pakati kumapangidwa chifukwa cha kusakwanira kwa chidziwitso chokwanira ndi chitetezo.

Kugwiritsa ntchito empagliflozin nthawi yoyamwitsa kumatsutsana. Zambiri zomwe zimapezeka mu preclinical maphunziro mu nyama zimadzipatula za empagliflozin mkaka wa m'mawere. Chiwopsezo chokhala pachiwopsezo cha ana akhanda ndi ana oyamwitsa sichimachotsedwa. Ngati kuli kofunika kugwiritsa ntchito empagliflozin panthawi yotsekemera, kuyamwitsa kuyenera kuyimitsidwa.

Gwiritsani ntchito ntchito yolakwika yaimpso

Kugwiritsa ntchito bwino kwa mankhwala a Jardins ® kumadalira ntchito ya impso. Chifukwa chake, tikulimbikitsidwa kuwunika ntchito ya impso isanakhazikitsidwe komanso nthawi yanthawi yamankhwala (osachepera 1 pachaka), komanso asanaikidwe pochiza, yomwe ingasokoneze ntchito ya impso.

Kwa odwala omwe ali ndi vuto la impso ndi GFR kuchokera pa45 mpaka 90 ml / mphindi / 1.73 m 2, kusintha kwa mankhwalawa sikofunikira. Odwala omwe ali ndi vuto la impso ndi GFR 2, kugwiritsa ntchito mankhwalawa sikulimbikitsidwa chifukwa chosakwanira.

Gwiritsani ntchito odwala okalamba

Odwala azaka 75 ndi kupitirira amakhala ndi chiopsezo chowonjezera cha madzi m'thupi. Odwala omwe amathandizidwa ndi empagliflozin, zovuta zoyipa zomwe zimayambitsidwa ndi hypovolemia zimawonedwa pafupipafupi (poyerekeza ndi odwala omwe akulandira placebo).

Zomwe zimachitika ndi empagliflozin mwa odwala opitilira zaka 85 ndizochepa, motero, sikulimbikitsidwa kupereka mankhwala Jardins ® kwa odwala a m'badwo uno.