Amaryl® (4 mg) Glimepiride

Kufotokozera za mtundu wa kipimo

Amaryl ® 1 mg: mapiritsi amtundu wapinki, oblong, athyathyathya okhala ndi mzere wogawa mbali zonse ziwiri. Zolemba "NMK"h"Mbali ziwiri.

Amaryl ® 2 mg: mapiritsi obiriwira, oblong, osalala okhala ndi mzere wogawanika mbali zonse ziwiri. Zolemba "NMM"h"Mbali ziwiri.

Amaryl ® 3 mg: Mapiritsi ake ndi achikaso achikasu, owala, lathyathyathya ndi mzere wogaula mbali zonse ziwiri. Zolemba "NMN"h"Mbali ziwiri.

Amaryl ® 4 mg: mapiritsi amtambo, oblong, osalala ndi mzere wogawanika mbali zonse ziwiri. Zolemba "NMO"h"Mbali ziwiri.

Mankhwala

Glimepiride imachepetsa kuchuluka kwa shuga m'magazi, makamaka chifukwa cha kukondoweza kwa kutulutsa kwa insulin m'maselo a beta. Zotsatira zake zimaphatikizidwa makamaka ndi kuwongolera kwa kuthekera kwa ma cell a pancreatic beta poyankha kukondoweza kwa thupi ndi glucose. Poyerekeza ndi glibenclamide, kutenga milingo yotsika ya glimepiride kumapangitsa kuti insulini itulutsidwe pomwe ikukwaniritsa kuchepa pafupifupi kwa ndende yamagazi. Izi zimapereka umboni wothandizira kukhalapo kwa extrapancreatic hypoglycemic zotsatira mu glimepiride (kuchuluka kwa chidwi cha minofu kupita ku insulin ndi insulin-mimetic effect).

Katemera wa insulin. Monga zochokera ku sulfonylurea zina zonse, glimepiride imayang'anira kubisala kwa insulin mwakuchita ndi njira zamtundu wa potaziyamu wa ATP pama cell a beta-cell. Mosiyana ndi zotumphukira zina za sulfonylurea, glimepiride imadzisankhira mapuloteni omwe ali ndi kulemera kwa 65 kilodaltons (kDa) yomwe imapezeka m'zipinda za cell za pancreatic beta. Kuchita uku kwa glimepiride ndi mapuloteni omwe amamangiriza kwa iwo kumayendetsa kutsegulidwa kapena kutseka kwa njira zamtundu wa potaziyamu za ATP.

Glimepiride amatseka njira zam potaziyamu. Izi zimayambitsa kukhumudwitsidwa kwa maselo a beta ndipo zimatsogolera kutsegulidwa kwa njira zopangira calcium komanso kumva kashiamu kulowa m'selo. Zotsatira zake, kuwonjezeka kwa intracellular calcium ndende kumapangitsa kuti insulin itulutsidwe ndi exocytosis.

Glimepiride imathamanga mwachangu motero imakhala yolumikizana ndipo imamasulidwa ku mgwirizano womwe uli ndi zomanga thupi kuposa glibenclamide. Amaganizira kuti nyumbayi yomwe ili ndi chiwopsezo chachikulu kwambiri cha glimepiride yokhala ndi mapuloteni omanga kwa iyo imatsimikizira mphamvu yake yotengeka ya maselo a beta ku glucose ndi chitetezo chawo ku kukomoka komanso kufooka msanga.

Zomwe zimawonjezera chidwi cha minofu ku insulin. Glimepiride imapititsa patsogolo zotsatira za insulin pa mayamwidwe a glucose mwa zotumphukira zimakhala.

Insulinomimetic kwenikweni. Glimepiride imakhala ndi zotsatira zofanana ndi zomwe zimapangitsa kuti insulini ikhale ndi mayamwidwe amtunduwu komanso kutulutsidwa kwa glucose ku chiwindi.

Glucose wa Peripheral umatengedwa ndikuwutumiza mu ma cell a minofu ndi adipocytes. Glimepiride imawonjezera mwachindunji kuchuluka kwamamolekyu omwe amayendetsa glucose m'matumbo a plasma a maselo am'mimba ndi adipocytes. Kuwonjezeka kwa kudya kwamaselo am'magazi kumabweretsa kutseguka kwa glycosylphosphatidylinositol-enieni phospholipase C. Zotsatira zake, ndende ya calcium ya intracellular imachepa, ndikupangitsa kuchepa kwa ntchito ya protein kinase A, yomwe imayambitsa kukondoweza kwa metabolism ya glucose.

Glimepiride amalepheretsa shuga kuti chiwindi chiwonjezeke ndi kuchuluka kwa fructose-2,6-bisphosphate, zomwe zimalepheretsa gluconeogeneis.

Zokhudza kuphatikizidwa kwa kupatsidwa zinthu za m'mwazi. Glimepiride amachepetsa kuphatikiza kwa mapulateleti mu vitro ndi mu vivo . Izi zikuwoneka kuti zimagwirizanitsidwa ndi kusankha kwa COX, komwe kumayambitsa mapangidwe a thromboxane A, chinthu chofunikira kwambiri cha kuphatikizira kwa maselo.

Antiatherogenic zotsatira za mankhwala. Glimepiride imathandizira kuti mitundu ya lipid ikhale yachulukidwe, imachepetsa zomwe zili mu malondialdehyde m'magazi, zomwe zimapangitsa kuchepa kwakukulu kwa lipid peroxidation. Mu nyama, glimepiride imabweretsa kuchepa kwakukulu kwa mapangidwe a atherosranceotic malo.

Kuchepetsa nkhawa ya oxidative, omwe amapezeka pafupipafupi kwa odwala omwe ali ndi mtundu wa matenda a shuga 2. Glimepiride imawonjezera zomwe zili za io-tocopherol amkati, ntchito ya catalase, glutathione peroxidase ndi superoxide dismutase.

Zokhudza mtima. Kudzera mu njira zamtundu wa potaziyamu wa ATP (onani pamwambapa), zochokera ku sulfonylurea zimakhudzanso CCC. Poyerekeza ndi miyambo yachikhalidwe ya sulfonylurea, glimepiride imakhala yotsika kwambiri ku CCC, yomwe ingafotokozedwe ndi chikhalidwe chake cholumikizana ndi mapuloteni omanga a njira za potaziyamu a ATP.

Mwa odzipereka athanzi labwino, mlingo woyenera wa glimepiride ndi 0,6 mg. Mphamvu ya glimepiride ndi kumwa modalira ndi kubereka. Kuyankha kwakuthupi pakulimbitsa thupi (kuchepa kwa insulin katemera) wokhala ndi glimepiride kumakhalabe.

Palibe kusiyana kwakukulu pazotsatira zake, kutengera kuti mankhwalawo adatengedwa mphindi 30 asanadye kapena nthawi yomweyo asanadye. Odwala omwe ali ndi matenda ashuga, kuwongolera kokwanira kwa metabolic kumatha kupezeka mkati mwa maola 24 ndi mlingo umodzi. Kuphatikiza apo, pakufufuza kwachipatala, odwala 12 mwa 16 omwe ali ndi vuto la aimpso (Cl creatinine 4-99 ml / min) adakwaniranso.

Kuphatikiza mankhwala ndi metformin. Odwala omwe ali osakwanira kagayidwe kachakudya pogwiritsa ntchito kuchuluka kwa glimepiride, kuphatikiza mankhwalawa ndi glimepiride ndi metformin kungayambike. M'maphunziro awiri, popanga mankhwala osakanikirana, zimatsimikiziridwa kuti kuwongolera kwa metabolic kuli bwino kuposa momwe amathandizira aliyense mwa mankhwalawa mosiyana.

Kuphatikiza mankhwala ndi insulin. Odwala osakwanira kagayidwe kachakudya, munthawi yomweyo mankhwala a insulin angayambike ndi mlingo waukulu wa glimepiride. Malinga ndi zotsatira za kafukufuku awiri, ndikugwiritsa ntchito kuphatikiza uku, kusintha komweku pakukonzekera metabolic kumatheka monga momwe mungagwiritsire ntchito insulin imodzi yokha, komabe, chithandizo chothandizirana chimafunikira kuchuluka kwa insulini.

Gwiritsani ntchito ana. Palibe deta yokwanira pakukwaniritsidwa kwakanthawi komanso chitetezo cha mankhwala kwa ana.

Pharmacokinetics

Kugwiritsa ntchito glimepiride mobwerezabwereza tsiku lililonse 4 mg C_max mu seramu imafikiridwa pambuyo pafupifupi maola 2,5 ndipo ndi 309 ng / ml. Pali ubale womwe ulipo pakati pa mlingo ndi C_max glimepiride mu plasma, komanso pakati pa mlingo ndi AUC. Mukamwetsa glimepiride mtheradi bioavailability wathunthu. Kudya kulibe vuto lililonse chifukwa chonyamula, kupatula kutsika pang'ono pang'onopang'ono. Glimepiride amadziwika ndi V wotsika kwambiri_d (pafupifupi 8.8 L), pafupifupi wofanana ndi V_d albin, yogwirizana kwambiri ndi mapuloteni a plasma (oposa 99%) ndi chilolezo chochepa (pafupifupi 48 ml / min). Wapakati T_1/2 , wozindikira seramu moyenera nthawi zonse mobwerezabwereza mankhwala, pafupifupi maola 5-8. Mutatha kumwa kwambiri, pali kuwonjezeka pang'ono kwa T_1/2 .

Pambuyo pa limodzi mlingo wa glimepiride, 58% ya mankhwalawa amachotsedwa impso ndi 35% ya mlingo kudzera m'matumbo. Glimepiride yosasinthika mumkodzo sadziwika.

Mu mkodzo ndi ndowe, ma metabolites awiri adadziwika omwe amapangidwa chifukwa cha kagayidwe kachakudya mu chiwindi (makamaka mothandizidwa ndi CYP2C9), imodzi mwa izo inali yochokera ku hydroxy, ndipo inayo imachokera ku carboxy. Pambuyo pakuyamwa kwa glimepiride, matendawa T_1/2 Mwa metabolites awa anali 3-5 ndi 5-6 h, motsatana.

Glimepiride amamuchotsa mkaka wa m'mawere ndikuwoloka chotchinga.

Kuyerekeza kwa osakwatiwa komanso angapo (kamodzi patsiku) makonzedwe a glimepiride sanawonetse kusiyana kwakukulu pama parachetinetic magawo, kusiyana kwawo kochepa kwambiri pakati pa odwala osiyanasiyana kumawonedwa. Palibe kuchuluka kwakukulu kwa mankhwalawa.

Ma paracokinetic magawo ndi ofanana mwa odwala azikhalidwe zosiyanasiyana komanso azaka zosiyanasiyana. Odwala omwe ali ndi vuto la aimpso (okhala ndi vuto lochepera la creatinine), amakhala ndi chizolowezi chomakulitsa chiwonetsero cha glimepiride ndi kuchepa kwake mozama kwambiri mu seramu yamagazi, yomwe, mwanjira zonse, imachitika chifukwa chothana ndi mankhwalawa chifukwa chotsika mapuloteni. Chifukwa chake, m'gulu lino la odwala palibe chiopsezo chowonjezereka cha mankhwalawa.

Contraindication

Hypersensitivity glimepiride kapena mankhwala othandizira aliwonse, mankhwala ena a sulfonylurea kapena mankhwala a sulfonamide (chiopsezo cha hypersensitivity reaction),

mtundu 1 shuga

matenda ashuga ketoacidosis, matenda a shuga komanso chikomokere,

kukanika kwambiri kwa chiwindi (kusowa kwazachipatala),

kwambiri aimpso kuwonongeka, kuphatikizapo mwa odwala hemodialysis (kusowa kwazachipatala),

Matenda obadwa nawo monga galactose tsankho, kuchepa kwa lactase kapena malabsorption a glucose-galactose,

zaka za ana (kusowa kwa kachipatala).

milungu yoyamba mankhwala (chiwopsezo cha hypoglycemia). Ngati pali zovuta zomwe zingayambitse kukula kwa hypoglycemia (onani gawo "Malangizo Apadera"), kusintha kwa glimepiride kapena chithandizo chonse chofunikira chitha,

ndi matenda wamba nthawi yamankhwala kapena kusintha kwa moyo wa odwala (kusintha kadyedwe ndi nthawi ya chakudya, kuchuluka kapena kuchepa kwa zochitika zolimbitsa thupi),

ndi shuga-6-phosphate dehydrogenase akusowa,

Ndi malabsorption chakudya ndi mankhwala m'mimba thirakiti (m'mimba kutsekeka, matumbo paresis).

Mtundu woyamba wa shuga. - Matenda a shuga a ketoacidosis, matenda a shuga komanso chikomokere. - Hypersensitivity glimepiride kapena mankhwala ena aliwonse othandizira, ku mankhwala ena a sulfonylurea kapena kukonzekera kwina kwa sulufilide (chiwopsezo cha zochita za hypersensitivity). - Kuwonongeka kwakukulu kwa chiwindi ntchito (kusowa kwazachipatala). - Kuwonongeka kwakukulu kwa aimpso, kuphatikizira odwala omwe akudwala hemodialysis (kusowa kwachipatala). - Mimba komanso kuyamwa. - Zaka za ana (kusowa kwa kachipatala). - Matenda obadwa nawo monga galactose tsankho, kuchepa kwa lactase kapena mal gluorpose-galactose malabsorption.

Mimba komanso kuyamwa

Glimepiride ndi contraindicated mwa amayi apakati. Ngati mayi wapezeka kuti ali ndi pakati kapena pokhapokha ngati ali ndi pakati, mkazi ayenera kuthandizidwa ndi insulin.

Glimepiride imadutsa mkaka wa m'mawere, kotero sichingatengere mkaka wa mkaka. Pankhaniyi, muyenera kusinthana ndi insulin kapena kusiya kuyamwitsa.

Zotsatira zoyipa

Pafupipafupi zotsatira zoyipa zimatsimikizidwa malinga ndi gulu la WHO: nthawi zambiri (≥10%), nthawi zambiri (≥1%, ® hypoglycemia ikhoza kupezeka, yomwe, monga momwe ena amachokera ku sulfonylurea, amatha kupitilira.

Zizindikiro za hypoglycemia ndi izi: kupweteka mutu, njala, kusanza, kusanza, kumva kutopa, kugona, kusokonezeka kwa tulo, kuda nkhawa, kukwiya, kusokonezeka kwamaganizidwe ndi kuthamanga kwa zochitika zama psychomotor, kupsinjika, kusokonezeka, kusokonezeka kwa mawu, aphasia, kuwonongeka kowoneka, kunjenjemera, paresis, kusokonezeka kwa malingaliro, chizungulire, kulephera kudziletsa, kusowa chithandizo, chisangalalo, kupindika kwa m'mimba, kukayikira kapena kutaya chikumbumtima, mpaka kukomoka, kupuma kosazama, bradycardia.

Kuphatikiza apo, pakhoza kuwonetsedwa kwa kutsutsa kwa adrenergic poyankha kukula kwa hypoglycemia, monga kutulutsa thukuta, khungu lozizira komanso lonyowa, nkhawa zambiri, tachycardia, kuthamanga kwa magazi, angina pectoris, palpitations ndi kusokonekera kwa mtima.

Kuwonetsedwa kuchipatala kwa hypoglycemia yayikulu ikhoza kukhala yofanana ndi sitiroko. Zizindikiro za hypoglycemia pafupifupi nthawi zambiri zimatha atatha.

Kulemera. Mukamamwa glimepiride, monga zotumphukira zina za sulfonylurea, kuwonjezeka kwa thupi ndikotheka (pafupipafupi sikudziwika).

Kuchokera kumbali ya gawo la masomphenyawo: pa mankhwala (makamaka pachiyambipo), kuwonongeka kwapang'onopang'ono chifukwa cha kusintha kwa ndende yamagazi kumawonedwa. Zomwe zimayambitsa ndikusintha kwakanthawi kwa ma lens, kutengera kuchuluka kwa shuga m'magazi, ndipo chifukwa cha izi, kusintha kwa mndandanda wa ma lenses.

Kuchokera m'mimba: osowa - nseru, kusanza, kumva kupsinjika kapena kusefukira dera la epigastric, kupweteka kwam'mimba, kutsekula m'mimba.

Pa mbali ya chiwindi ndi biliary thirakiti: Nthawi zina, chiwindi, kuchuluka kwa michere ya chiwindi ndi / kapena cholestasis ndi jaundice, komwe kumatha kupitilira pachiwopsezo cha chiwopsezo cha moyo, koma kumatha kupitilira chitukuko chitatha mankhwala.

Mbali ya magazi ndi zamitsempha yamagazi: kawirikawiri thrombocytopenia, nthawi zina - leukopenia, hemolytic magazi, erythrocytopenia, granulocytopenia, agranulocytosis ndi pancytopenia. Pogwiritsa ntchito malonda pambuyo pa malonda, milandu ya thrombocytopenia yoopsa yokhala ndi ma cellels osakwana 10,000 / μl ndi thrombocytopenic purpura (pafupipafupi osadziwika) yanenedwa.

Kuchokera ku chitetezo chamthupi: kawirikawiri - matupi awo sagwirizana ndi pseudo-matupi awo, monga pruritus, urticaria, zotupa pakhungu. Kusintha koteroko kumakhala kofatsa nthawi zonse, koma kumatha kupweteka kambiri komanso kupuma movutikira, kutsika kwamphamvu kwa kuthamanga kwa magazi, komwe nthawi zina kumayamba kugwedezeka kwa anaphylactic. Ngati zizindikiro za urticaria zikuwoneka, pitani kuchipatala msanga. Mtanda-ziwengo zimatheka ndi zotumphukira zina za sulfonylurea, sulfonamides kapena zina zofanana, nthawi zina matupi awo saviyo vasculitis.

Pa khungu ndi subcutaneous minofu: Nthawi zina - photosensitivity, pafupipafupi sizikudziwika - alopecia.

Zambiri zasayansi: Nthawi zina - hyponatremia.

Kuchita

Glimepiride imapangidwa ndi cytochrome P4502C9 (CYP2C9), yomwe iyenera kukumbukiridwa ikagwiritsidwa ntchito nthawi yomweyo ndi inducers (mwachitsanzo rifampicin) kapena ma inhibitors (mwachitsanzo fluconazole) CYP2C9.

Kuthekera kwa hypoglycemic kanthu, nthawi zina, kukula kwa hypoglycemia komwe kumayenderana ndi ichi imatha kuthandizidwa ikaphatikizidwa ndi imodzi mwazomwezi: Mao zoletsa, fluconazole, para-aminosalicylic acid, pentoxifylline (mlingo waukulu wa makolo), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, clarithromycin n, sulfonamides, tetracyclines, tritocqualin, trophosphamide.

Kuchepa kwa hypoglycemic kanthu ndi kuwonjezereka kwokhudzana ndi kuchuluka kwa shuga m'magazi Itha kuthandizidwa mukaphatikizidwa ndi imodzi mwamankhwala awa: acetazolamide, barbiturates, GCS, diazoxide, diuretics, epinephrine ndi mankhwala ena a sympathomimetic, glucagon, laxatives (ogwiritsa ntchito nthawi yayitali), nicotinic acid (muyezo waukulu), estrogens ndi progestogens, phenothiazines, phenytoin, rifampicin, mahomoni okhala ndi chithokomiro.

Zotchinga N₂histamine receptors, beta-blockers, clonidine ndi reserpine kutha kuwongolera ndi kufooketsa mphamvu ya hypoglycemic ya glimepiride. Mothandizidwa ndi othandizira achifundo, monga beta-blockers, clonidine, guanethidine ndi reserpine, zizindikiro za kutsutsa kwa adrenergic poyankha hypoglycemia zitha kuchepetsedwa kapena kulibe.

Ngakhale mukumwa glimepiride, kuwonjezeka kapena kufooka kwa zochita za coumarin zitha kuonedwa.

Kumwa kamodzi kapena kosapatsa thanzi ikhoza kuwongolera ndikuchepetsa mphamvu ya hypoglycemic ya glimepiride.

Otsatira a bile acid kwa chafer chimagwira glimepiride ndikuchepetsa kuyamwa kwa glimepiride osachepera maola 4 musanatenge chafer, palibe kuyanjana kumawonedwa. Chifukwa chake, glimepiride iyenera kumwedwa osachepera maola 4 musanatenge magudumu.

Mlingo ndi makonzedwe

Kutenga Amaril ®

Mkati osafuna kutafuna, kutsuka ndi madzi okwanira (pafupifupi makapu 0,5). Ngati ndi kotheka, mapiritsi a Amaril ® amatha kugawidwa pamodzi ndi zoopsa m'magawo awiri ofanana.

Monga lamulo, mlingo wa Amaril ® umatsimikiziridwa ndi kutsata kwa shuga m'magazi. Mlingo wotsika kwambiri wokwanira kukwaniritsa zoyenera za metabolic uyenera kugwiritsidwa ntchito.

Pa mankhwala ndi Amaril ®, ndikofunikira kudziwa pafupipafupi kuchuluka kwa shuga m'magazi. Kuphatikiza apo, kuwunika pafupipafupi milingo ya hemoglobin ya glycosylated kumalimbikitsidwa.

Kukhazikika kwa mankhwala osokoneza bongo, mwachitsanzo, kudumpha mlingo wotsatira, sikuyenera kuthandizidwa ndi kudya kwina kwa mlingo waukulu.

Zochita za wodwalayo pakafunika zolakwa mukamamwa mankhwalawo (makamaka, podumpha mlingo wotsatira kapena kudumpha chakudya) kapena ngati sizotheka kumwa mankhwalawo ayenera kukambirana ndi wodwalayo ndi dokotala pasadakhale.

Koyamba mlingo ndi kusankha kwa mankhwala

Mlingo woyambirira ndi 1 mg ya glimepiride 1 nthawi patsiku.

Ngati ndi kotheka, tsiku lililonse mlingo ungakulidwe pang'onopang'ono (pakadutsa masabata 1-2). Ndikulimbikitsidwa kuti kuwonjezeka kwa mlingo kuchitidwa ndikuwonetsetsa kuchuluka kwa shuga wamagazi komanso mogwirizana ndi gawo lotsatira la kuchuluka kwa 1 mg - 2 mg - 3 mg - 4 mg - 6 mg (mg8 mg).

Mlingo umakhala pakati pa odwala omwe ali ndi shuga wambiri

Nthawi zambiri, tsiku lililonse odwala omwe amalamulidwa ndi shuga wambiri amawongolera kuti ndi 4 mg mg glimepiride. Mlingo wa tsiku ndi tsiku wopitilira 6 mg umagwira kwambiri mwa ochepa ochepa odwala.

Nthawi yomwe mumamwa mankhwalawa ndikugawa zamankhwala tsiku lonse limatsimikiziridwa ndi dokotala, kutengera moyo wa wodwalayo panthawi yopatsidwa (nthawi yakudya, kuchuluka kwa zochitika zolimbitsa thupi).

Nthawi zambiri, mlingo umodzi wa mankhwalawa masana ndi wokwanira. Ndikulimbikitsidwa kuti pankhaniyi, mlingo wonse wa mankhwalawo uyenera kumwedwa musanadye chakudya cham'mawa chokwanira, kapena ngati sichinatenge panthawiyo, musanadye chakudya chachikulu choyamba. Ndikofunika kuti musadumphe chakudya mutamwa mapiritsi.

Popeza kuyendetsa bwino kagayidwe kachakudya kumalumikizidwa ndi kukhudzika kwa insulin, kufunika kwa glimepiride kumatha kuchepa panthawi ya chithandizo. Kuti mupewe kukula kwa hypoglycemia, ndikofunikira kuchepetsa mlingo kapena kusiya kumwa Amaril ®.

Momwe mankhwalawa a glimepiride angafunikire:

- Kuchepetsa thupi la wodwala,

- kusintha kwa moyo wa wodwalayo (kusintha kadyedwe, nthawi ya chakudya, kuchuluka kwa zochita zolimbitsa thupi),

- kutuluka kwa zinthu zina zomwe zimatsogolera kukukula kwa hypoglycemia kapena hyperglycemia (onani gawo "Malangizo apadera").

Chithandizo cha glimepiride nthawi zambiri chimachitika kwa nthawi yayitali.

Kusamutsa kwa wodwala kuchokera kwa wothandizira wina wa hypoglycemic wothandizira pakamwa kupita ku Amaryl ®

Palibe ubale weniweni pakati pa Mlingo wa Amaril ® ndi othandizira ena a hypoglycemic pakamwa. Wothandizanso wina wa hypoglycemic pakakonzedwe kamlomo ndikusinthidwa ndi Amaril ®, tikulimbikitsidwa kuti njira yoyendetsera kayendetsedwe kake ndi chimodzimodzi ndi koyamba kwa Amaril ®, i.e. mankhwalawa amayenera kuyamba ndi mlingo wochepa wa 1 mg (ngakhale wodwalayo atamupititsa ku Amaryl ® ndi mlingo wokwanira wa mankhwala ena a hypoglycemic pakumwa pakamwa). Kuchulukitsa kwa mlingo uliwonse kuyenera kuchitika m'magawo, kukumbukira kuyankha kwa glimepiride molingana ndi malangizo omwe ali pamwambawa.

M'pofunika kuganizira mphamvu ndi kutalika kwa zotsatira za m'mbuyomu hypoglycemic wothandizira pakamwa. Kulowetsa chithandizo kungafunike kuti mupewe zovuta zilizonse zomwe zingapangitse chiopsezo cha hypoglycemia.

Gwiritsani ntchito limodzi ndi metformin

Odwala omwe ali ndi matenda osokoneza bongo omwe amawongolera osakwanira, akalandira mlingo waukulu wa glimepiride kapena metformin, mankhwalawa atha kuphatikizana ndi mankhwalawa. Pankhaniyi, chithandizo cham'mbuyomu chomwe chili ndi glimepiride kapena metformin chimapitilira mlingo womwewo, ndipo mlingo wowonjezereka wa metformin kapena glimepiride umayamba ndi mlingo wochepa, womwe umasungidwa malinga ndi gawo lazomwe limayang'anira metabolic mpaka mlingo waukulu wa tsiku lililonse. Kuphatikiza mankhwala kuyenera kuyang'aniridwa ndi achipatala.

Gwiritsani ntchito limodzi ndi insulin

Odwala omwe ali ndi matenda osokoneza bongo omwe amawongolera osakwanira, insulin imatha kuperekedwa nthawi yomweyo mutatenga mlingo waukulu wa tsiku ndi tsiku wa glimepiride. Pankhaniyi, mlingo womaliza wa glimepiride woperekedwa kwa wodwala amakhalabe wosasinthika. Pankhaniyi, chithandizo cha insulin chimayamba ndi milingo yotsika, yomwe imayamba kuwonjezeka pang'onopang'ono motsogozedwa ndi glucose m'magazi. Chithandizo chophatikiza chimafunika kuyang'aniridwa mosamala ndi madokotala.

Gwiritsani ntchito odwala omwe ali ndi impso. Pali chidziwitso chochepa pakugwiritsa ntchito mankhwalawa odwala omwe ali ndi vuto la aimpso. Odwala omwe ali ndi vuto la impso amatha kukhudzidwa kwambiri ndi hypoglycemic zotsatira za glimepiride (onani magawo "Pharmacokinetics", "Contraindication").

Gwiritsani ntchito odwala omwe ali ndi vuto la chiwindi. Pali zambiri zochepa pakugwiritsa ntchito mankhwalawa kulephera kwa chiwindi (onani gawo "Contraindication").

Gwiritsani ntchito ana. Zambiri pa kugwiritsa ntchito mankhwalawa kwa ana sikokwanira.

Bongo

Zizindikiro pachimake kwambiri, komanso chithandizo chambiri chotenga nthawi yayitali kwambiri cha glimepiride, chingayambitse matenda oopsa kwambiri obwera chifukwa cha hypoglycemia.

Chithandizo: mutagwiritsa ntchito bongo mopitirira muyeso, muyenera kudziwitsa dokotala wanu nthawi yomweyo. Hypoglycemia nthawi zambiri imatha kuimitsidwa msanga chifukwa cha kudya zakudya zamagulu (shuga kapena chidutswa cha shuga, msuzi wa zipatso kapena tiyi). Pankhaniyi, wodwalayo ayenera kukhala ndi shuga pafupifupi 20 g (zidutswa 4 za shuga). Zomakoma sizothandiza pochita hypoglycemia.

Mpaka pomwe dokotala angaganize kuti wodwalayo ali pachiwopsezo, wodwalayo amafunika kuyang'aniridwa mosamala ndi madokotala. Tiyenera kukumbukira kuti hypoglycemia imatha kuyambiranso pambuyo poyambitsanso koyamba magazi a magazi.

Wodwala yemwe akudwala matenda ashuga amathandizidwa ndi madotolo osiyanasiyana (mwachitsanzo, pakakhala kuchipatala pambuyo pangozi, atadwala kumapeto kwa sabata), ayenera kuwauza za matenda ake ndi chithandizo cham'mbuyomu.

Nthawi zina kuchipatala wodwala angafunike, ngakhale pokhapokha ngati pakufunika kusamala. Kuchuluka kwa mankhwala osokoneza bongo kwambiri komanso kuwonetsa kozama monga kuwonongeka kwa chikumbumtima kapena matenda ena okhudzana ndi mitsempha ndikofunikira kuchipatala ndipo amafunikira chithandizo chamankhwala ndi kuchipatala.

Ngati wodwalayo sakudziŵa kanthu, jakisoni wamkati wokhazikika wa dextrose (glucose) ndikofunikira (kwa akulu, kuyambira 40 ml ya yankho la 20%). Ngati njira ina achikulire, mtsempha wa magazi, kulowerera kapena kutsekeka kwa glucagon ndikotheka, mwachitsanzo, pa mlingo wa 0.5-1 mg.

Mankhwala a hypoglycemia chifukwa cha mwangozi a Amaril ® ndi makanda kapena ana aang'ono, mlingo wa dextrose womwe umayendetsedwa uyenera kusinthidwa molingana ndi mwayi wa hyperglycemia wowopsa, ndikuwongolera kwa dextrose kuyenera kuchitika pang'onopang'ono poyang'anira kuchuluka kwa shuga m'magazi.

Pankhani ya overdose ya Amaril ®, chapamimba thonje ndi kukhathamira kwa makala omwe adalowetsedwa angafunike.

Pambuyo pobwezeretsa mwachangu kuchuluka kwa shuga m'magazi, kulowetsedwa kwamphamvu kwa dextrose njira yotsikira ndikufunika kuti muchepetse kuyambiranso kwa hypoglycemia. Kuchuluka kwa shuga m'magazi mwa odwala oterowo kuyenera kuyang'aniridwa pafupipafupi kwa maola 24. Muzochitika zazikulu kwambiri za hypoglycemia, chiopsezo chochepetsa kuchuluka kwa glucose m'magazi mpaka kuchuluka kwa hypoglycemic kumatha masiku angapo.

Malangizo apadera

M'magawo apadera ovuta a nkhawa, monga kuvutika maganizo, chithandizo cha opaleshoni, matenda a febrile fever, metabolic control ikhoza kudwala kwambiri odwala matenda a shuga, ndipo angafunikire kusinthidwa kwakanthawi kuti alandire insulin kuti azitha kuyendetsa bwino metabolism.

M'milungu yoyamba ya chithandizo, chiopsezo chokhala ndi hypoglycemia chitha kuchuluka, chifukwa chake, kuyang'anira kuchuluka kwa shuga m'magazi ndikofunikira pakadali pano.

Zomwe zimayambitsa chiopsezo cha hypoglycemia zimaphatikizapo:

- kusafuna kapena kulephera kwa wodwala (nthawi zambiri kumawonedwa mwa odwala okalamba) kuti azithandizana ndi dokotala,

- kuperewera kwa zakudya m'thupi, kudya mosazolowereka kapena kudumpha chakudya,

- Kusagwirizana pakati pa zolimbitsa thupi ndi chakudya

- zakumwa zoledzeretsa, makamaka kuphatikiza ndi zomwe zimatsala,

- kwambiri aimpso kuwonongeka,

- kukanika kwa chiwindi (odwala omwe ali ndi vuto lalikulu la chiwindi, kusinthika kwa mankhwala a insulin akuwonetsedwa, osachepera mpaka kupezeka kwa metabolic),

- zovuta zina zowonongeka za endocrine zomwe zimaphwanya chakudya cha carbohydrate metabolism kapena adrenergic mogwirizana ndi hypoglycemia (mwachitsanzo, kusowa kwina kwa chithokomiro cha chithokomiro komanso chimbudzi cha anterior, adrenal insuffence.

- kulandira munthawi yomweyo mankhwala ena (onani. "Kuyanjana"),

- Kulandila kwa glimepiride posakhala zizindikiro zakulandila kwake.

Kuchiza ndi zotumphukira za sulfonylurea, zomwe zimaphatikizapo glimepiride, kungayambitse kukula kwa hemolytic anemia, chifukwa chake, odwala omwe ali ndi vuto la glucose-6-phosphate dehydrogenase ayenera kusamala makamaka pokhazikitsa glimepiride ndipo ndibwino kugwiritsa ntchito othandizira a hypoglycemic omwe siabwino.

Pamaso pa zinthu zomwe zili pachiwopsezo cha hypoglycemia, kusintha kwa glimepiride kapena chithandizo chonse chofunikira kungafunike. Izi zimagwiranso ntchito pakupezeka kwa matenda omwe amakumana nawo panthawi yamankhwala kapena kusintha kwa moyo wa odwala.

Zizindikiro za hypoglycemia zomwe zimawonetsa kuwukira kwa thupi chifukwa cha hypoglycemia (onani "Zotsatira zoyipa") zitha kukhala zofatsa kapena kusapezeka ndi kukula kwapang'onopang'ono kwa hypoglycemia, odwala okalamba, odwala omwe ali ndi vuto la neuronomic, kapena odwala omwe amalandila beta adrenoblockers, clonidine, reserpine, guanethidine ndi othandizira ena achifundo.

Hypoglycemia imatha kuthetsedwa mwachangu ndi kupezeka msanga kwa chakudya cham'mimba chambiri (glucose kapena sucrose).

Monga momwe ena amachokera ku sulfonylurea, ngakhale atakwanitsa kupumula kwa hypoglycemia, hypoglycemia ikhoza kuyambiranso. Chifukwa chake, odwala ayenera kuyang'aniridwa mosalekeza.

Mu hypoglycemia yayikulu, chithandizo chamanthawi yomweyo ndikuyang'aniridwa kuchipatala chofunikira, ndipo nthawi zina, kugonekedwa kwa odwala kuchipatala.

Mankhwalawa glimepiride, kuwunika pafupipafupi kwa chiwindi ndi chithunzi cha magazi (makamaka kuchuluka kwa leukocytes ndi mapulateleti) kumafunika.

Popeza zovuta zina, monga hypoglycemia, kusintha kwakukuru mu chithunzi cha magazi, zovuta zina za thupi, kulephera kwa chiwindi, pamikhalidwe inayake ikhoza kuwopseza moyo, ngati mukuchitika zosakhumudwitsa kapena zowopsa, wodwalayo ayenera kudziwitsa dokotala wopezekapo za iwo ndipo osatero Mulimonsemo, musapitilize kumwa mankhwalawo osalimbikitsa.

Kukopa pa kuyendetsa magalimoto ndi njila zina. Pankhani ya kukula kwa hypoglycemia kapena hyperglycemia, makamaka kumayambiriro kwa mankhwalawa kapena kusintha kwa mankhwalawa, kapena mankhwalawa akapanda kumwa mankhwala pafupipafupi, kuchepa kwa chidwi ndi kuthamanga kwa zochitika zama psychomotor ndikotheka. Izi zitha kulepheretsa wodwala kuyendetsa magalimoto kapena njira zina.

Kutulutsa Fomu

Mapiritsi, 1 mg, 2 mg, 3 mg, 4 mg.

Mlingo wa 1 mg

30 mapiritsi mu chithuza cha PVC / aluminium zojambulazo. 1, 2, 3 kapena 4 bl. anayikidwa mu katoni.

Mlingo wa 2 mg, 3 mg, 4 mg

15 tabu. mu chithuza cha PVC / aluminium zojambulazo. Pa 2, 4, 6 kapena 8 bl. anayikidwa mu katoni.

Wopanga

Sanofi S.p.A., Italy. Stabilimento di Scoppito, Strada Statale 17, km 22, I-67019 Scoppito (L'Aquilla), Italy.

Bungwe lovomerezeka lomwe dzina lake limalembetsedwa. Sanofi-Aventis Deutschland GmbH, Germany

Zodandaula za ogula ziyenera kutumizidwa ku adilesi ku Russia. 125009, Moscow, st. Tverskaya, 22.

Tele. ((495) 721-14-00, fakisi: (495) 721-14-11.

Mlingo

Piritsi limodzi la 4 mg lili

ntchito yogwira - glimepiride 4 mg

obwera: lactose monohydrate, sodium starch glycolate (mtundu A), povidone 25000, cellcrystalline cellulose, magnesium stearate, indigo carmine aluminium varnish (E 132).

Mapiritsi, oboweka mawonekedwe, okhala ndi lathyathyathya mbali zonse ziwiri, opepuka amtambo wautoto wokhala ndi cholakwika kumbali zonse ziwiri ndi logo ya NMO / logo ya kampani kapena logo ya kampani / NMO.

Amaril mapiritsi 4 mg Itha kugawidwa muyezo waukulu.

Mankhwala

Pharmacokinetics

Glimepiride amadziwika ndi bioavailability wathunthu pakamwa. Kudya kulibe vuto lililonse pakumwedwa kwa mankhwalawa, limodzi ndi kuchepa pang'ono chabe kwa mayamwidwe. Maximum serum concentrations (Cmax) amakwaniritsidwa pafupifupi maola 2,5 pambuyo pakumwa pakamwa (pafupifupi 0,3 μg / ml wokhala ndi Mlingo wambiri wa 4 mg patsiku), kuwonetsa mgwirizano womwe ulipo pakati pa mlingo ndi Cmax ndi AUC ( dera pansi pa ndende motsutsana nthawi yopindika).

Glimepiride ili ndi voliyumu yotsika kwambiri (pafupifupi ma 8.8 malita), pafupifupi yolingana ndi mwayi wogawa albumin, mapuloteni ambiri omanga (> 99%) komanso chilolezo chotsika (pafupifupi 48 ml / min.). M'maphunziro oyesa, glimepiride amachotseredwa mkaka wa m'mawere. Glimepiride amatha kudutsa placenta. Mlingo wolowerera kudzera mu chotchinga cha magazi ndi chochepa.

Biotransformation ndi chimbudzi

Hafu yayikulu kwambiri ya theka la moyo wa seramu yoyenera imagwiritsidwa ntchito mobwerezabwereza ndi pafupifupi maola 5-8. Atamwa mankhwalawa muyezo waukulu, mioyo yayitali pang'ono idadziwika. Pakadutsa mphindi imodzi yokha ya radioactive isotope-cholembedwa glimepiride, 58% ya radioactivity idapezeka mumkodzo ndi 35% mu ndowe. Zinthu zosasinthika mkodzo sizinapezeke. Ma metabolites awiri adadziwika mu mkodzo ndi ndowe, mwachidziwikire kukhala zopangidwa ndi hepatic metabolism (puloteni yayikulu ya CYP2C9): zotulutsidwa za hydroxy ndi carboxy. Pambuyo pakamwa makonzedwe a glimepiride, kuchotseratu kwa terminal miyoyo ya metabolites awa anali 3-6 ndi maola 5-6, motero.

Kufananitsa zotsatira zomwe zapezedwa ndikuvomerezedwa kamodzi komanso kawiri pazomwe zimafotokozedwa kamodzi sizinawonetse kusiyana kwakukulu pamalingaliro a pharmacokinetics, amadziwika ndi kusiyanasiyana kwapadera kwamalingaliro. Kuchuluka kwakukulu kwa glimepiride sikunawonedwe.

Magawo a pharmacokinetic anali ofanana mwa amuna ndi akazi, komanso mwa achinyamata ndi achikulire (opitilira zaka 65) odwala. Odwala omwe ali ndi lowinine clearance, panali chizolowezi chowonjezera chilolezo cha glimepiride ndi kutsika kwapakati kwa seramu, makamaka chifukwa chofulumira chifukwa chotuluka kwa protein. Kuphatikiza apo, kuchepa kwa impso excretion kwa metabolites awiri akuluakulu adadziwika. Mwambiri, chiopsezo chowonjezereka cha kudzikundikira kwa mankhwala mwa odwala awa sichikuyembekezeredwa.

Magawo a pharmacokinetic mwa odwala asanu omwe alibe matenda ashuga atatha opaleshoni pamiyendo ya bile anali ofanana ndi omwe amawonekera mwa anthu athanzi.

Kafukufuku wofufuza za pharmacokinetics, chitetezo, ndi kulolerana kwa glimepiride omwe amatengedwa kamodzi pa mlingo wa 1 mg mwa 30 odwala omwe ali ndi ana (ana 4 wazaka 12-16 wazaka 26 ndi ana azaka za 12 mpaka 17) omwe ali ndi mtundu wa 2 matenda a shuga adawonetsa pafupifupi AUC mfundo (0 -last.), Cmax ndi t1 / 2, zofanana ndi zomwe zimawonedwa kale mwa akulu.

Mankhwala

Glimepiride ndi hypoglycemic ya mkamwa yogwira gulu la zotumphuka za sulfonylurea. Itha kugwiritsidwa ntchito ngati matenda osokoneza bongo omwe amadalira shuga.

Kuchita kwa glimepiride makamaka kumathandizira kubisalira kwa insulin ndi maselo a beta a kapamba.

Monga momwe zimapezekera ndi zinthu zina za sulfonylurea, izi zimachitika chifukwa cha kuwonjezereka kwa mayankho a pancreatic beta kukwiya ndi kuchuluka kwa glucose. Kuphatikiza apo, glimepiride, mwachiwonekere, ili ndi kutchulidwa kochulukirapo, komwe kumadziwika ndi zina zomwe zimachokera ku sulfonylurea.

Zotsatira za Sulfonylurea zimayendetsa katulutsidwe ka insulin potseka njira za ATP zotsekemera za potaum cell ya beta-cell. Kutsekedwa kwa njira za potaziyamu kumapangitsa kuchepa kwa maselo a beta ndipo mwa kutsegulira njira za calcium kumawonjezera kuchuluka kwa calcium m'maselo. Izi zimapangitsa kuti amasulidwe a insulin ndi exocytosis.

Glimepiride yokhala ndi chiwopsezo chachikulu kwambiri chomwe chimamangidwa kumapuloteni am'maselo a maselo a beta, omwe amalumikizidwa ndi njira zamtundu wa potaziyamu wa ATP, koma amasiyana ndi tsamba lomwe limamangidwa nthawi zonse.

Zotsatira za extrapancreatic zimaphatikizapo, mwachitsanzo, kukonza chidwi cha zotumphukira kuti insulini ikhale pansi ndikuchepetsa kuchuluka kwa insulin yolandidwa ndi chiwindi.

Kulowetsedwa kwa glucose m'magazi ndi zotumphukira minofu ndi minyewa yamafuta kumachitika chifukwa cha mapuloteni apadera a mayendedwe omwe amapezeka m'matumbo am'mimba. Kutenga kwa glucose m'misempha imeneyi ndi gawo lochepetsa kuchuluka kwa shuga m'magazi. Glimepiride mofulumira imachulukitsa kuchuluka kwa ma glucose transporter mamolekyu mu cell membranes a minofu ndi maselo amafuta, zomwe zimayambitsa kukhudzidwa kwa glucose.

Glimepiride imathandizira ntchito yeniyeni ya glycosyl phosphatidylinositol phospholipase C, yomwe imatha kuphatikizana ndi mankhwala olexandis ndi glycogeneis pama cell am'magazi. Glimepiride imalepheretsa kupanga kwa glucose m'chiwindi mwa kuchulukitsa kuchuluka kwa chidwi cha fructose-2,6-bisphosphate, komwe, ndipo, kumalepheretsa gluconeogeneis.

Mwa anthu athanzi labwino, mlingo woyamwa wothandiza ndi pafupifupi 0.6 mg. Glimepiride imadziwika ndi mlingo wodalira komanso kubereka. Kuyankha kwakuthupi pakuchita zolimbitsa thupi mwamphamvu, kuchepa kwa insulin katemera, kumakhalabe ndi kugwiritsa ntchito glimepiride.

Kusiyanitsa kwakukulu mu mtundu wa chochitikacho pakumwa mankhwalawo kwa mphindi 30 ndipo nthawi yomweyo chakudya chisanachitike. Odwala omwe ali ndi matenda a shuga, kupatsidwa mphamvu yokwanira ya metabolic mkati mwa maola 24 kungatheke pogwiritsa ntchito mankhwalawa kamodzi patsiku.

Hydroxymetabolite ya glimepiride, ngakhale idayambitsa kuchepa kwakukulu koma kwakukulu m'magazi a seramu mwa anthu athanzi, imayang'anira gawo laling'ono lonselo la mankhwala.

Kuphatikiza Therapy ndi Metformin

Kafukufuku wina, odwala omwe ali ndi vuto losakwanira pa metformin pamlingo waukulu wogwiritsidwa ntchito ndi glimepiride adawonetsa kusintha kwa metabolic control poyerekeza ndi metformin monotherapy.

Kuphatikiza mankhwala ndi insulin

Pakadali pano, pali zochepa zochepa pazamankhwala othandizira osakanikirana ndi insulin. Odwala omwe ali ndi osakwanira kuwongolera matenda pazambiri mlingo wa glimepiride akhoza zotchulidwa concomitant insulin. M'maphunziro awiri, kuphatikiza mankhwala kunaphatikizidwa ndi kusintha kwa kagayidwe kachakudya komwe kamayenderana ndi insulin monotherapy, koma kuphatikiza mankhwalawa kunafunikira kugwiritsa ntchito insulin yapakati.

Kafukufuku wamasabata 24 adachitika ndikuwongolera mwachangu (glimepiride mu Mlingo mpaka 8 mg pa tsiku kapena metformin mu Mlingo mpaka 2,000 mg pa tsiku) mwa ana 285 (azaka 8 mpaka 17) omwe ali ndi matenda a shuga a 2.

Kulandila kwa glimepiride ndi metformin kunatsagana ndi kuchepa kwakukulu kwa HbA1c poyerekeza ndi gawo loyambirira (glimepiride - 0.95 (СО 0.41), metformin -1.39 (СО 0.40). Komabe, mitengo ya kusintha kwa HbA1c poyerekeza ndi gawo loyambirira lomwe lili mgulu la glimepiride silinakumane ndi zotsutsa zomwe sizotsika ndi metformin. Kusiyana pakati pamagulu azithandizo anali 0.44% pokomera metformin. Mulingo wapamwamba (1.05) wa chidaliro cha 95% cha kusiyana pamalingaliro anali pamwamba pa 0.3% ya malire osachita bwino.

Poyerekeza ndi chithandizo chamankhwala a glimepiride mwa ana, panalibe zisonyezo zakusintha kwatsopano poyerekeza ndi zomwe zimawonedwa mwa odwala akuluakulu omwe ali ndi matenda a shuga 2. Zomwe zimapangitsa kuti mankhwalawa agwiritsidwe ntchito kwa nthawi yayitali odwala sapezeka.