ComboGliz Ikani mapiritsi a 500

Dzinalo:Kutalika kwa nthawi ya Kombiglyze

Kupanga ndi mawonekedwe a kumasulidwa

Filimu Yotulutsira Kutulutsidwa Kwa Makanema Piritsi limodzi lili ndi 1000 mg ya metformin, 2,5 mg wa saxagliptin.

Mu matuza 28 kapena 56 mapiritsi. Atakwezedwa m'makatoni.

Mapiritsi okhala ndi mafilimu okonzedwa osintha, 1000 mg + 5 mg. Mu phukusi la mapiritsi 28 kapena 56.

Mapiritsi okhala ndi mawonekedwe otulutsidwa otulutsa mafilimu, 500 mg + 5 mg. Mu phukusi la mapiritsi 28 kapena 56.

Zachipatala ndi gulu la mankhwala

Oral hypoglycemic mankhwala

Gulu la Pharmacotherapeutic

Wophatikiza wa hypoglycemic wophatikizira pakamwa (dipeptidyl peptidase-4-inhibitor + biguanide)

Zotsatira za pharmacological

Combogliz Prolong imaphatikiza mankhwala awiri a hypoglycemic omwe ali ndi njira zowonjezerapo zowongolera glycemic control mwa odwala omwe ali ndi mtundu wa 2 shuga mellitus (DM2): saxagliptin, dipeptyl peptidase 4 inhibitor (DPP-4), ndi metformin, woimira kalasi yayikulu.

Poyankha kudya kwakudya kuchokera m'matumbo aang'ono, mahomoni amtundu wa impretin amatulutsidwa m'magazi, monga glucagon-peptide-1 (GLP-1) ndi insulinotropic polypeptide (HIP) ya glucose. Ma mahomoniwa amalimbikitsa kutulutsa kwa insulin kuchokera ku maselo a pancreatic beta, kutengera kuchuluka kwa shuga m'magazi, koma samapangidwira ndi enzyme DPP-4 kwa mphindi zingapo. GLP-1 imachepetsa kubisalira kwa glucagon m'maselo a alpha, ndikuchepetsa kupanga shuga kwa chiwindi. Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri, anthu ambiri omwe amakhala ndi GLP-1 amatsitsidwa, koma mayankho a insulin ku GLP-1 amakhalabe. Saxagliptin, wokhala mpikisano wopikisana ndi DPP-4, amachepetsa mphamvu ya kuchuluka kwa ma impretin, potero amawonjezera kuchuluka kwawo m'magazi ndikupangitsa kutsika kwama glucose posachedwa kudya.

Metformin ndi mankhwala osokoneza bongo a hypoglycemic omwe amapititsa patsogolo kulekerera kwa glucose kwa odwala omwe ali ndi matenda a shuga a 2, amachepetsa kuyambira kwa shuga ndi postprandial glucose. Metformin imachepetsa kupanga shuga ndi chiwindi, imachepetsa mayamwidwe am'matumbo m'matumbo ndikukulitsa kumva kwa insulin, kukulitsa kuphatikizika kwa magazi ndi kugwiritsa ntchito shuga. Mosiyana ndi kukonzekera kwa sulfonylurea, metformin sayambitsa hypoglycemia kwa odwala omwe ali ndi matenda a shuga a 2 kapena anthu athanzi (kupatula pazochitika zina, onani zigawo "Precautions" ndi "Maupangiri apadera"), ndi hyperinsulinemia. Pakati pa mankhwala a metformin, kutulutsidwa kwa insulin kumakhalabe kosasinthika, ngakhale kusala kwa insulin komanso kuyankha zakudya masana kumatha kuchepa.

Pharmacokinetics

Ma pharmacokinetics a saxagliptin ndi metabolite yake yogwira, 5-hydroxy-saxagliptin, ndiwofanana mu odzipereka athanzi komanso odwala omwe ali ndi matenda a shuga a 2. Makhalidwe a C max ndi dera lomwe lili pansi pa AUC pamapindikira a saxagliptin ndi metabolite yake yogwira plasma inachulukanso mokwanira muyezo kuchokera pa 2.5 mg mpaka 400 mg. Pambuyo pakukonzekera kamlomo kamodzi kwa saxagliptin pa mlingo wa 5 mg ndi odzipereka athanzi, avareji ya AUC ya saxagliptin ndi metabolite yake yayikulu anali 78 ng * h / ml ndi 214 ng * h / ml, ndipo mfundo za C max mu plasma zinali 24 ng / ml ndi 47 ng / ml motero. Kusintha kwapakati pa AUC ndi C max kwa saxagliptin ndipo metabolite yake yogwira inali yochepera 25%.

Pogwiritsa ntchito mankhwalawa mobwerezabwereza kamodzi patsiku pa mlingo uliwonse, palibe umboni wowoneka bwino wa saxagliptin kapena metabolite yake yogwira. Palibe kudalira kwa chilolezo cha saxagliptin ndi metabolite yogwira pa mlingo ndi nthawi yomwe imagwiritsidwa ntchito masiku 14 kamodzi pa tsiku kuchokera pa 2,5 mg mpaka 400 mg ya saxagliptin.

Ndi max, kutulutsidwa kwa metformin kumatheka pakati pa maola 7. Mafuta a metformin kuchokera pamapiritsi osinthidwa amasulidwa amawonjezereka ndi 50% mukamamwa ndi zakudya. Pakufanana, AUC ndi Cmax a metformin amasulidwe amasintha osati molingana ndi gawo la mlingo kuchokera pa 500 mpaka 2000 mg. Pambuyo pa kutsata mobwerezabwereza, kutulutsidwa kwa metformin sikunadziunjike mu plasma. Metformin imachotsedwa osasinthika ndi impso ndipo samapangidwira m'chiwindi.

Pambuyo pakukonzekera pakamwa, osachepera 75% ya muyezo wa saxagliptin. Kudya sizinakhudze kwambiri pharmacokinetics ya saxagliptin mwa odzipereka athanzi. Zakudya zamafuta kwambiri sizinakhudze C max ya saxagliptin, pomwe AUC inakula ndi 27% poyerekeza ndi kusala kudya. Nthawi yofika C max (T max) ya saxagliptin inachulukitsa pafupifupi maola 0,5 mukamamwa mankhwalawo ndi chakudya koma poyerekeza ndi kusala kudya. Komabe, zosinthazi sizofunikira mthupi.

Pambuyo pakukonzekera kamodzi kwamlomo wa metformin kumasulidwa, C max imatheka pambuyo pa maola 7, pamtunda kuchokera maola 4 mpaka 8. AUC ndi Cmax a metformin amasulidwe kumasulidwa sikuchulukako molingana ndi kuchuluka kwa mlingo kuchokera pa 500 mpaka 2000 mg. Kuchuluka kwa mankhwala omwe amapezeka m'madzi am'magazi ndi 0,6, 1.1, 1.4 ndi 1.8 μg / ml pamene mukumwa Mlingo wa 500, 1000, 1500 ndi 2000 mg kamodzi patsiku, motero. Ngakhale kuchuluka kwa mayamwidwe (oyesedwa ndi AUC) a metformin kuchokera pama mapiritsi otulutsidwa a metformin kumawonjezera pafupifupi 50% akamamwa ndi chakudya, kudya zakudya sizinakhudze C max ndi T max a metformin. Zakudya zotsika komanso zamafuta kwambiri zimakhudzanso zomwe zimachitika pa pharmacokinetics ya metformin yotulutsidwa.

Kumangidwa kwa saxagliptin ndi metabolite yake yayikulu m'mapuloteni a seramu sikofunikira, chifukwa chake, titha kulingaliridwa kuti kugawa kwa saxagliptin ndikusintha kwa kapangidwe ka mapuloteni a seramu yamagazi omwe amawonekera mu hepatic kapena aimpso kulephera sikungasinthe.

Kafukufuku wamagawidwe a metformin amasinthidwe sanachitike, komabe, kuchuluka kowonekera kwa kugawa kwa metformin pambuyo pakulankhula kamodzi kwamlomo wa mapiritsi a metformin kutulutsidwa kwaposachedwa kwa mapiritsi a 850 mg pafupifupi 654 ± 358 L. Metformin imamangiriza pang'ono mapuloteni a plasma.

Saxagliptin imapangidwa makamaka ndi kutengapo gawo kwa ma isoenzymes a cytochrome P450 ZA4 / 5 (CYP3A4 / 5) ndi mapangidwe a metabolite yogwira, mphamvu yotsutsa yomwe motsutsana ndi DPP-4 ndi yofupika kawiri kuposa saxagliptin.

Kafukufuku yemwe adapangidwira kamodzi pamankhwala osokoneza bongo kwa odzipereka athanzi amawonetsa kuti metformin sinafotokozeredwe ndi impso, samapukusidwa mu chiwindi (metabolites samapezeka mwa anthu), ndipo samatulutsidwa m'matumbo.

Saxagliptin imakumbidwa impso kudzera m'matumbo. Mlingo umodzi wa 50 mg wolembedwa 14 C-saxagliptin, 24% ya mankhwalawa idachotsedwa ndi impso ngati saxagliptin wosasinthika ndi 36% monga metabolite yayikulu ya saxagliptin. Ma radioactivine omwe apezeka mumkodzo amafanana ndi 75% ya mlingo womwe unatengedwa.

Chilolezo chapakati cha saxagliptin chinali pafupifupi 230 ml / mphindi, kuchuluka kwa kusefera kwa glomerular kunali pafupifupi 120 ml / mphindi. Pa metabolite yayikulu, chilolezo cha impso chinali chofanana ndi tanthauzo la kusefera kwa glomerular. Pafupifupi 22% ya ma radioacaction athu onse adapezeka mu ndowe.

Chilolezo cha renal chimakhala chamtunda pafupifupi 3.5 kuposa chilengedwe cha clearinine chilolezo (CC), zomwe zikuwonetsa kuti kubisala kwa tubular ndiyo njira yayikulu yodziwira metformin.Pambuyo pakulowetsa, pafupifupi 90% ya mankhwala odziwikirawa amachotseredwa impso m'masiku 24 oyambirira, ndi theka la moyo kuchokera ku plasma pafupifupi maola 6.2. M'magazi, theka la moyo ndi pafupifupi maola 17.6, chifukwa chake, erythrocyte misa ikhoza kukhala gawo logawidwa.

Pharmacokinetics mwapadera matenda

Sitikulimbikitsidwa kugwiritsa ntchito Combogliz Kutalika kwa odwala omwe ali ndi vuto la impso (onani gawo "Contraindication").

Odwala omwe ali ndi vuto lofooka la aimpso, mfundo za AUC za saxagliptin ndi metabolite yogwira anali 20% ndi 70% (motsatana) apamwamba kuposa zomwe AUC imachita mwa odwala omwe ali ndi vuto laimpso. Popeza kuwonjezeka kotereku sikumvekedwa kukhala kofunika kwambiri, sikulimbikitsidwa kusintha saxagliptin mwa odwala omwe ali ndi vuto laimpso.

Odwala omwe ali ndi vuto la impso (malinga ndi zotsatira za muyeso wa QC), theka la moyo wa metformin kuchokera ku plasma ndi kutalika kwa magazi ndi chilolezo cha impso umachepa mogwirizana ndi kuchepa kwa QC.

Odwala omwe ali ndi vuto lochepa kwambiri, loletsa komanso la hepatic kwambiri, panalibe kusintha kwakukulu pama pharmacokinetics a saxagliptin, kotero kusintha kwa mlingo kwa odwala kotere sikofunikira.

Palibe maphunziro a pharmacokinetic a metformin mwa odwala omwe ali ndi kuwonongeka kwa hepatic.

Kukonza mlingo wa saxagliptin malinga ndi jenda la odwala sikofunikira.

M'maphunziro azachipatala odwala omwe ali ndi matenda a shuga a 2, zotsatira za hypoglycemic za metformin mwa amuna ndi akazi zinali zofanana.

Odwala a zaka zapakati pa 65-80, panalibe kusiyana kwakukulu mu pharmacokinetics ya saxagliptin poyerekeza ndi odwala aang'ono (azaka 18 mpaka 40), motero kusintha kwa odwala okalamba sikofunikira. Komabe, ziyenera kukumbukiridwa kuti m'gulu ili la odwala, kuchepa kwa ntchito yaimpso ndikothekera (onani magawo "Mlingo ndi Ulamuliro" ndi "Maupangiri Apadera").

Zambiri zochepa kuchokera ku maphunziro olamulidwa a pharmacokinetics of metformin mwa odzipereka achikulire ogwira ntchito amati chiwonetsero chonse cha plasma chikucheperachepera, T 1/2 imawonjezeka, ndipo C imakulirakulira poyerekeza ndi zofunikira za magawo amenewa mwa odzipereka achinyamata athanzi. Malinga ndi izi, kusintha kwa ma pharmacokinetics a metformin ndi kukula msinkhu makamaka chifukwa cha kusintha kwa impso. Kuchulukitsa kwa Combogliz sikuyenera kutumizidwa kwa odwala azaka zopitilira 80, pokhapokha ngati ntchito yachilendo yatsitsi imatsimikiziridwa ndi zotsatira za QC.

Maphunziro a pharmacokinetics a saxagliptin mwa ana sanachitike.

Kafukufuku wa pharmacokinetics of metformin amasulidwa amasungidwe mwa ana sanachitike.

Mtundu ndi Fuko

Sitikulimbikitsidwa kusintha mlingo wa saxagliptin kutengera mtundu wa wodwalayo.

Sipanapezeke maphunziro a pharmacokinetics a metformin kutengera mtundu wa odwala.

Type 2 shuga mellitus wophatikizidwa ndi zakudya komanso masewera olimbitsa thupi kuti muzitha kuyendetsa bwino glycemic.

Contraindication kugwiritsa ntchito mankhwala Combogliz Kutalika

Kuchulukitsa kwa chidwi cha munthu aliyense pazinthu zilizonse za mankhwala, kuopsa kwa hypersensitivity (anaphylaxis kapena angioedema) kwa DPP-4 zoletsa, mtundu 1 wa matenda osokoneza bongo (osaphunzira glucose-galactose malabsorption, kutenga pakati, mkaka wa m`mawere, osakwana zaka 18 (chitetezo ndi mphamvu sanaphunzire), impso, serum creatinine creat1.5 mg / dl kwa amuna, ≥1.4 mg / dl kwa akazi cystin kapena kuchepa kwa chilolezo cha creatinine), kuphatikizapo zomwe zimayambika chifukwa cha mtima wolephera (kugwedezeka), matenda amitsempha yam'mimba komanso septicemia, matenda omwe ali ndi vuto la impso: kutsitsa madzi m'mimba (kusanza, kutsekula m'mimba),malungo, matenda opatsirana, matenda a hypoxia (mantha, sepsis, matenda a impso, matenda a bronchopulmonary), pachimake kapena matenda a metabolic acidosis, kuphatikizapo matenda ashuga a ketoacidosis, omwe ali ndi chifuwa chachikulu kapena matenda osokonekera omwe angayambitse matenda kukula kwa minofu hypoxia (kupuma kulephera, mtima kulephera, pachimake infarction), opaleshoni yayikulu ndi zoopsa (pamene insulin mankhwala akusonyeza), chiwindi ntchito uchidakwa wambiri ndi poyizoni wa ethanol, lactic acidosis (kuphatikizapo mbiri), nthawi yosachepera maola 48 isanachitike komanso mkati mwa maola 48 mutachitika maphunziro a radioisotope kapena radiology ndikuyambitsa othandizira ayodini wokhala ndi mankhwala osakanikirana, kutsatira zakudya zochepa zama calorie (5% ya odwala, omwe adalandira metformin yotulutsidwa, ndikukula pafupipafupi kuposa gulu la placebo, anali ndi m'mimba komanso kusanza / kusanza.

Zotsatira zotsatirazi zidanenedwera pakutsatsa kugwiritsidwa ntchito kwa saxagliptin: pachimake pancreatitis ndi hypersensitivity reaction, anaphylaxis, angioedema, zidzolo ndi urticaria. Ndizosatheka kuwerengera pafupipafupi kukula kwa zinthuzi, popeza mauthenga adalandilidwa mosawerengeka kuchokera kwa anthu osadziwika (onani zigawo "Contraindication" ndi "Malangizo apadera a kutenga Combogliz Kutalika»).

Chiwerengero chonse cha ma lymphocyte

Saxagliptin

Mukamagwiritsa ntchito saxagliptin, kuchepa kwapakati pa kuchuluka kwa ma mankhwalawa kumawonedwa. Mukamasanthula kafukufuku wophatikizidwa wa masabata makumi awiri ndi awiri, maphunziro owongoleredwa ndi malo, kutsika kwapakati pa 100 ndi ma cell 120 / μl ya kuchuluka kwathunthu kwa ma lymphocyte kuchokera ku chiwerengero choyambirira cha maselo a 2200 / μl adawonedwa ndikugwiritsa ntchito saxagliptin pa mlingo wa 5 mg ndi 10 mg, poyerekeza, poyerekeza ndi placebo. Zofananazo zimawonedwa pakumwa saxagliptin pa 5 mg mu kuphatikiza koyamba ndi metformin poyerekeza ndi metformin monotherapy. Panalibe kusiyana pakati pa 2,5 mg saxagliptin ndi placebo. Gawo la odwala omwe kuchuluka kwa ma lymphocyte anali ≤ 750 maselo / μl anali 0,5%, 1.5%, 1.4%, ndi 0,4% m'magulu azachipatala a saxagliptin pa mlingo wa 2.5 mg, pa 5 mg , pa mlingo wa 10 mg ndi placebo, motero. Odwala ambiri omwe amagwiritsa ntchito saxagliptin mobwerezabwereza, sanayambenso kuyambiranso, koma mwa odwala ena kuchuluka kwa ma lymphocyte kunachepa kachiwiri ndi kuyambiranso kwa mankhwala ndi saxagliptin, komwe kunapangitsa kuti saxagliptin ithe. Kutsika kwa kuchuluka kwa ma lymphocyte sikunayendetsedwe ndi mawonetsedwe azachipatala.

Zomwe zimapangitsa kuchepa kwa chiwerengero cha ma lymphocyte pa saxagliptin chithandizo chofanana ndi placebo sizikudziwika. Pakakhala matenda osazolowereka kapena osakhalitsa, ndikofunikira kuyeza kuchuluka kwa ma lymphocyte. Mavuto a saxagliptin pa kuchuluka kwa ma lymphocyte odwala omwe ali ndi vuto lambiri la mankhwalawa (mwachitsanzo, kachilombo ka chitetezo cha munthu) sikadziwika.

Saxagliptin

Saxagliptin sanali ndi vuto lachipatala kapena lachiwonetsero pakuwonekera kwa maselo a m'magulu asanu ndi m'modzi amaso awiri, owongolera mayesero azachipatala otetezeka komanso ogwira ntchito.

Vitamini B Kukhazikika₁₂

Mu maphunziro azachipatala olamulidwa a metformin wokhala ndi masabata a 29, pafupifupi 7% ya odwala adawonetsa kuchepa kwa seramu kale kuposa kutsata kwachilendo kwa vitamini B₁₂ kumakhalidwe abwino popanda chiwonetsero chachipatala. Komabe, kuchepa kotereku sikumayendera limodzi ndi kukula kwa magazi m'thupi ndipo kumatha msanga pambuyo pakuchotsa ma metformin kapena kuchuluka kwa vitamini B₁₂.

Mimba komanso kuyamwa

Chifukwa chakuti kugwiritsidwa ntchito kwa mankhwala a Combogliz Prolong pa nthawi ya pakati sikunaphunzire, mankhwalawa sayenera kutumikiridwa panthawi yomwe ali ndi pakati.

Sizikudziwika ngati saxagliptin kapena metformin akadutsa mkaka wa m'mawere.Popeza kuthekera kwa kulowa kwa mankhwala a Combogliz Kutalika mu mkaka wa m'mawere sikumayikidwa padera, kugwiritsa ntchito mankhwalawa panthawi ya mkaka wa m`mawere kumatsutsana.

Gwiritsani ntchito mankhwalawa chiwindi chogwiritsa ntchito mankhwalawa chifukwa cha kukanika kwa chiwindi chimagwira.

Kugwiritsa ntchito mankhwala kwa ana

Kugwiritsa ntchito mankhwalawa kumakwiriridwa ana osakwana zaka 18 (chitetezo ndi kuchita bwino sizinaphunzire).

Gwiritsani ntchito odwala okalamba

Popeza saxagliptin ndi metformin amatha kuperewera pang'ono ndi impso, ndipo odwala okalamba kuchepa kwa impso, mwina Combogliz Prolong iyenera kugwiritsidwa ntchito mosamala okalamba.

Malangizo apadera a kutenga Combogliz Kutalika

Lactic acidosis ndi osowa, zovuta kagayidwe kachakudya zomwe zimayamba chifukwa chakuwunika kwa metformin panthawi ya mankhwala a Combogliz Prolong. Ndi chitukuko cha lactic acidosis chifukwa chogwiritsa ntchito metformin, kugwiritsidwa ntchito kwake mu plasma ya magazi kumaposa 5 μg / ml.

Odwala omwe ali ndi matenda ashuga, lactic acidosis nthawi zambiri imayamba ndi kulephera kwambiri kwaimpso, kuphatikizapo chifukwa cha kubadwa kwa impso komanso kusakwanira kwa impso, makamaka mukamamwa mankhwala angapo. Odwala omwe ali ndi vuto la mtima, makamaka odwala omwe ali ndi vuto losakhazikika la angina kapena mtima wovuta komanso chiopsezo cha hypoperfusion ndi hypoxemia, pamakhala chiwopsezo cha lactic acidosis. Chiwopsezo chokhala ndi lactic acidosis imachulukana molingana ndi kuchuluka kwa kulephera kwa impso komanso zaka za wodwalayo. Kuwunikira pafupipafupi kwa ntchito yaimpso kwa odwala omwe akutenga metformin kuyenera kuchitika ndipo mlingo wofunikira wa metformin uyenera kutumikiridwa. Odwala okalamba, kuwunika ntchito yaimpso ndikofunikira. Metformin sayenera kutumizidwa kwa odwala azaka makumi asanu ndi atatu ndi okulirapo ngati vuto la impso likulephera (malinga ndi data ya QC), popeza odwalawa amakonda kwambiri lactic acidosis. Kuphatikiza apo, mankhwala a metformin amayenera kutha yomweyo ngati machitidwe omwe akuphatikizidwa ndi hypoxemia, kufooka kapena sepsis akayamba. Popeza kulephera kwa chiwindi kungachepetse kuthana ndi kukhazikika kwa lactate, metformin sayenera kutumizidwa kwa odwala omwe ali ndi matenda am'chipatala kapena a labotale matenda a chiwindi.

Kukhazikika kwa lactic acidosis nthawi zambiri kumakhala kosadziwika ndipo kumayendera limodzi ndi zizindikiro zopanda pake, monga malaise, myalgia, kulephera kupuma, kuwuma kwambiri, kupweteka komanso kusasangalala pamimba. Hypothermia, hypotension, ndi bradyarrhythmia yolimbana ndi vuto limatha. Wodwala ayenera kufotokozera mwansanga zonsezo kwa dotolo. Ngati zizindikiro zotere zapezeka, njira ya metformin iyenera kusiyidwa, kuyang'anira ma seramu elekitirodi, matupi a ketone, shuga wamagazi, ndipo ngati akuwonetsa, magazi a pH, ndende ya lactate ndende ya metformin m'magazi. Zizindikiro zam'mimba zomwe zimayamba kumapeto kwa mankhwala a metformin zimatha chifukwa cha lactic acidosis kapena matenda ena.

Kusala kudya kwa plousma kotupa kumapangitsa kuti magazi azigundika pamwamba pamlingo wambiri koma ochepera 5 mmol / L odwala omwe akutenga metformin angatchule chitukuko cha lactic acidosis, komanso mwina chifukwa cha zifukwa zina, monga matenda a shuga osakwanira, kunenepa kwambiri, kulimbitsa thupi kwambiri katundu.

Kukhalapo kwa lactic acidosis kuyenera kuwunika mu odwala onse omwe ali ndi matenda osokoneza bongo komanso metabolic acidosis popanda zizindikiro za ketoacidosis (ketonuria ndi ketonemia). Lactic acidosis imafunikira chithandizo kuchipatala. Ngati lactic acidosis yapezeka mwa wodwala yemwe akutenga metformin, muyenera kusiya kumwa mankhwalawo nthawi yomweyo ndikuyamba kutsatira njira zothandizira.Ndikulimbikitsidwa kuti dialysis iyambike nthawi yomweyo kuti ikonze acidosis ndi metformin yowonjezera.

Monga mukudziwa, mowa umapangitsa mphamvu ya metformin pa lactate metabolism, yomwe imawonjezera chiopsezo cha lactic acidosis. Chepetsani kumwa mowa mukamamwa Combogliz Prolong.

Kutalika kwa Combogliz sikulimbikitsidwa kwa odwala omwe ali ndi matenda azachipatala komanso a labotale chifukwa cha chiwopsezo cha lactic acidosis.

Kuyesa kwa impso

Musanayambe mankhwala ndi Combogliz Prolong ndipo pafupifupi pachaka, ndikofunikira kuyang'ana impso. Odwala omwe akuyembekezeredwa kuti aimpso, ntchito ya impso iyenera kuyesedwa pafupipafupi ndipo chithandizo chokhala ndi Combogliz Prolong ziyenera kusiyidwa ngati chizindikiro cha kulephera kwa impso chikuwonekera.

Muyenera kuyimitsa kanthawi kogwiritsa ntchito mankhwalawa Combogliz Prote musanayambe kuchita opareshoni iliyonse (kupatula njira zazing'ono zomwe sizikugwirizana ndi kuchepetsa kumwa ndi zakumwa zina), osayambiranso kugwiritsidwa ntchito mpaka wodwala atatha kumwa mankhwalawo mkati ndikuti ntchito yachilendo ya impso itsimikizirika .

Sinthani mu kachipatala ka odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga

Wodwala T2DM, yemwe kale ankawongolera nthawi ya mankhwala ndi Combogliz Pronge, ndipo wapatuka m'magawo a labotale kapena amatenga matenda (makamaka pakudziwika bwino), zizindikiro za ketoacidosis kapena lactic acidosis ziyenera kuwunikiridwa nthawi yomweyo. Kuunika kuyenera kuphatikizira kutsimikiza kwa ma elekitiroma mu seramu yamagazi, ma ketoni, shuga wamagazi ndipo, ngati akuwonetsa, magazi pH, kutsata kwa lactate, pyruvate ndi metformin. Ngati mtundu wina wa acidosis wapezeka, Combogliz Prolong iyenera kusiyidwa pomwepo ndipo mankhwala enanso a hypoglycemic atchulidwa.

Kugwiritsa ntchito mankhwala omwe angayambitse hypoglycemia

Mankhwala omwe amalimbikitsa katemera wa insulin, monga sulfonylureas, amatha kuyambitsa hypoglycemia. Chifukwa chake, kuti muchepetse chiopsezo cha hypoglycemia mukamaphatikizidwa ndi saxagliptin, zingakhale zofunikira kuchepetsa mlingo wa mankhwala omwe amalimbikitsa katemera wa insulin.

Hypoglycemia siimakula mwa odwala omwe amangotenga metformin mwa njira yokhayo, koma imatha kukhala ndi vuto losakwanira la chakudya, pamene ntchito yolimbitsa thupi siziwalitsidwa ndi kudya kwa carbohydrate, kapena kugwiritsa ntchito limodzi ndi mankhwala ena a hypoglycemic (monga sulfonylureas ndi insulin. Okalamba, odwala ovutitsidwa kapena osadyetsedwa bwino komanso odwala omwe adrenal kapena pituitary insuffidence kapena kuledzera amakonda kwambiri zovuta za hypoglycemic. Mwa okalamba ndi odwala omwe amatenga beta-blockers, kuzindikira kwa hypoglycemia kumatha kukhala kovuta.

Thercomitant chithandizo chokhudza impso kapena kugawa kwa metformin

Mankhwala olumikizana (monga mankhwala a cationic, omwe amathandizidwa ndi kubisala mu impso tubules), omwe angayambitse ntchito ya impso, amatsogolera kusintha kwakukulu kwa hemodynamic kapena kusokoneza kugawa kwa metformin (onani gawo "Kuyanjana ndi mankhwala ena"), kuyenera kugwiritsidwa ntchito mosamala.

Radiological maphunziro ndi intravascular makonzedwe a ayodini osiyanitsa ena

Mukamachititsa maphunziro a radiology ndi intravascular management ya iodine okhala ndi mitundu yosiyanitsa, mapangidwe owopsa aimpso adadziwika, omwe amatha kukhala limodzi ndi chitukuko cha lactic acidosis odwala omwe amalandila metformin. Odwala omwe akukonzekera kuchita kafukufukuyu ayenera kusiya Combogliz Prolong Therapy mkati mwa maola 48 asanachite izi, kukana kumwa mankhwalawa mkati mwa maola 48 pambuyo pa njirayi, ndikuyambiranso chithandizo pokhapokha ngati njira yotsimikizika ya impso itsimikizika.

Mtima kugwa (mantha) kwa komwe kunachokera, kugundika kwa mtima, pachimake infarction ndi zina zokhala ndi hypoxia ndi lactic acidosis kungayambitse azotemia prerenal. Ndi chitukuko cha zochitika zoterezi, ndikofunikira kusiya yomweyo mankhwala ndi Combogliz Pronge.

Shuga wamagazi

Thupi, kuvulala, matenda, opaleshoni imatha kuyambitsa kuphwanya kwa magazi m'thupi, lomwe m'mbuyomu limawongolera mothandizidwa ndi mankhwala a Combogliz Prolong. Muzochitika izi, kuchoka kwakanthawi kwa chithandizo komanso kusamutsa wodwala kupita ku insulin chithandizo kungafunike. Pambuyo kukhazikika kwa kuchuluka kwa shuga m'magazi ndikusintha momwe wodwalayo alili, chithandizo ndi Combogliz Prolong chitha kuyambiranso.

Mukatsatsa malonda ogwiritsa ntchito saxagliptin, zochitika zazikulu za hypersensitivity zimadziwika, kuphatikizapo anaphylaxis ndi angioedema. Ndi kukula kwa vuto lalikulu la hypersensitivity, kugwiritsa ntchito mankhwalawa kuyenera kusiyidwa, zifukwa zina zomwe zingayambitse chitukuko cha mankhwalawa ziyenera kuyesedwa, ndipo njira zina zochizira matenda ashuga ziyenera kuyikidwa (onani "Contraindication" ndi "Zotsatira zoyipa»).

Pogwiritsa ntchito saxagliptin atangogulitsa, zalandiridwa mwadzidzidzi za milandu yamatenda owononga pancreatitis. Odwala omwe atenga Combogliz Kutalika amayenera kudziwitsidwa za mawonekedwe a kupweteka kwa kapamba: kupweteka kwakali, m'mimba. Ngati mukukayikira kukula kwa kapamba, muyenera kusiya kumwa mankhwala a Combogliz Prolong (onani zigawo "Mochenjera" ndi "Zotsatira zoyipa»).

Kukopa pa kuyendetsa magalimoto ndi kayendedwe kazinthu

Kafukufuku wokhudzana ndi saxagliptin pakutha kuyendetsa magalimoto ndi kayendedwe kazinthu sikunachitike.

Kumbukirani kuti saxagliptin ikhoza kupweteketsa mutu.

Bongo

Ndi kugwiritsa ntchito mankhwalawa kwa nthawi yayitali mpaka 80 peresenti kuposa momwe amalimbikitsira, sikuonetsa matendawa.

Pankhani ya mankhwala osokoneza bongo, mankhwala othandizira ayenera kugwiritsidwa ntchito. Saxagliptin ndi metabolite yake yayikulu imapukusidwa ndi hemodialysis (kuchuluka kwa excretion: 23% ya mlingo mu maola 4).

Pakhala pali milandu yambiri ya metformin, kuphatikizapo kutenga zoposa 50. Hypoglycemia imayamba pafupifupi 10% ya milandu, koma mgwirizano wake ndi metformin sunakhazikitsidwe. Mu 32% ya milandu yochuluka ya metformin, odwala anali ndi lactic acidosis. Metformin imachotsedwa pakayimbidwe, pomwe chilolezo chimafika 170 ml / min.

Kuchita ndi Mankhwala Ena

Mankhwala ena amachulukitsa hyperglycemia (thiazide ndi ma diuretics ena, glucocorticosteroids, phenothiazines, kukonzekera kwa mahomoni a chithokomiro, estrogens, njira zakulera zamkati, phenytoin, nicotinic acid, sympathomimetics, pang'onopang'ono calcium blockers ndi isoniazid). Mukamayamwa kapena kusiya mankhwala ngati wodwala akutenga Combogliz Prolong, yang'anirani kuchuluka kwa shuga m'magazi. Mlingo womangidwa wa metformin ku mapuloteni amadzi a m'magazi ndi ochepa, kotero sizingatheke kuti azilumikizana ndi mankhwala omwe amaphatikizidwa kwambiri ndi mapuloteni a plasma, monga salicylates, sulfonamides, chloramphenicol ndi probenecid (mosiyana ndi zomwe zimachokera ku sulfonylurea, zomwe zimamangidwa kwambiri. ndi mapuloteni a seramu).

Zowonetsa za isoenzymes CYP3A4 / 5

Rifampicin amachepetsa kwambiri ma saxagliptin osasintha AUC ya metabolite yake yogwira, 5-hydroxy-saxagliptin. Rifampicin sichikuwakhudza kuletsa kwa DPP-4 m'magazi a magazi munthawi yamahora a 24 a chithandizo.

CYP3A4 / 5 Isoenzyme Inhibitors

Diltiazem imakulitsa mphamvu ya saxagliptin ikagwiritsidwa ntchito limodzi.Kuwonjezeka kwa kuchuluka kwa saxagliptin m'madzi a m'magazi kuyembekezeredwa ndikugwiritsa ntchito amprenavir, aprepitant, erythromycin, fluconazole, fosamprenavir, madzi a mphesa ndi verapamil, komabe, kumwa kwa saxagliptin sikulimbikitsidwa. Ketoconazole amachulukitsa kuchuluka kwa saxagliptin mu plasma. Kuwonjezeka kofananako kwa kuchuluka kwa saxagliptin m'madzi a m'magazi kuyembekezeredwa pamene ma inhibizes ambiri a nzoenzymes CYP3A4 / 5 amagwiritsidwa ntchito (mwachitsanzo, atazanavir ,cacithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir ndi telithromycin. Mukaphatikizidwa ndi inhibitor yamphamvu ya CYP3A4 / 5 isoenzymes, mlingo wa saxagliptin uyenera kuchepetsedwa kukhala 2.5 mg.

Mankhwala a Cationic (mwachitsanzo, amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterone, trimethoprim kapena vancomycin), omwe amachotseredwa ndi impso kudzera mu kusefera kwa glomerular, akhoza kungogwirizana ndi metformin, kupikisana mayendedwe wamba. Mu maphunziro okhudzana ndi mankhwala a metformin ndi cimetidine kamodzi komanso mobwerezabwereza kayendetsedwe ka mankhwalawa, kuyanjana kwa metformin ndi cimetidine pakumwa pakamwa mu odzipereka athanzi kunawonedwa, kuwonjezeka kwa 60% pazowonjezera za metformin mu plasma ndi magazi athunthu ndi kuwonjezeka kwa 40% kwa AUC ya metformin mu plasma ndi kwathunthu magazi. Pakuphunzira ndi mtundu umodzi wa mankhwalawa, palibe chomwe chinasintha mu theka-moyo. Metformin sichikhudza pharmacokinetics ya cimetidine. Ndikulimbikitsidwa kuyang'anira odwala mosamala, ndipo ngati ndi kotheka, sinthani muyezo wa odwala omwe amamwa mankhwala a cationic omwe amuchotsa kudzera mu proximal renal tubule system.

Pakufufuza kwakukhudzana ndi kumwa kwa kamodzi kwa mankhwalawa odwala omwe ali ndi matenda a shuga a 2, kugwiritsa ntchito metformin ndi glibenclamide sikukhudza pharmacokinetics kapena pharmacodynamics.

Pakufufuza kwa kuyanjana kwa mankhwala a metformin ndi furosemide ndi mlingo umodzi wa mankhwalawo, wopangidwa pa odzipereka athanzi, kuyanjana kwawo kwa pharmacokinetic kuwululidwa. Furosemide imachulukitsa C_max metformin mu plasma ndi magazi ndi 22% ndi AUC m'magazi ndi 15% popanda kusintha kwakukulu kwa impso chilolezo cha metformin. Mukamamwa ndi metformin C_max ndi AUC ya furosemide imachepetsedwa ndi 31% ndi 12%, motero, ndipo theka la moyo limatsitsidwa ndi 32% popanda kusintha kwawonekera kwa impso kwa furosemide. Palibe deta pakukhudzana kwa metformin ndi furosemide pogwiritsa ntchito nthawi yayitali.

Pophunzira za kuyanjana kwa mankhwala a metformin ndi nifedipine ndi mlingo umodzi wa mankhwalawa, wopangidwa pa odzipereka athanzi, nifedipine imawonjezera C_max metformin mu plasma ndi 20% ndi AUC ndi 9%, ndipo imakulitsa kuchulukitsidwa ndi impso. T_max ndi T_1/2 sizinasinthe. Nifedipine imawonjezera mayamwidwe a metformin. Metformin ilibe gawo lililonse pa pharmacokinetics ya nifedipine.

Saxagliptin ndi Metformin

Kugwiritsa ntchito limodzi mphamvu ya saxagliptin (100 mg) ndi metformin (1000 mg) sikukhudza kwambiri pharmacokinetics ya saxagliptin kapena metformin odzipereka athanzi.

Palibe maphunziro apadera a pharmacokinetic okhudzana ndi kugwiritsa ntchito mankhwala kwa Combogliz Prolong, ngakhale maphunziro otere adachitidwa ndi zigawo zake: saxagliptin ndi metformin.

Zotsatira za mankhwala ena pa saxagliptin

Glibenclamide: Kugwiritsa ntchito kamodzi kwa saxagliptin (10 mg) ndi glibenclamide (5 mg), gawo laling'ono la isoenzyme CYP2C9, C_max saxagliptin ndi 8%, komabe, saucagliptin AUC sasintha.

Pioglitazone: Kugwiritsidwa ntchito mobwerezabwereza kwa saxagliptin kamodzi patsiku (10 mg) ndi pioglitazone (45 mg), gawo laling'ono la isoenzyme CYP2C8 (wamphamvu) ndi CYP3A4 (ofooka), sizikuwakhudza pharmacokinetics a saxagliptin.

Digoxin: Kugwiritsidwa ntchito mobwerezabwereza kwa saxagliptin kamodzi patsiku (10 mg) ndi digoxin (0.25 mg), gawo lapansili la P-glycoprotein, sikukhudza ma pharmacokinetics a saxagliptin.

Simvastatin: Kugwiritsidwa ntchito mobwerezabwereza kwa saxagliptin kamodzi patsiku (10 mg) ndi simvastatin (40 mg), gawo lapansi la CYP3A4 / 5 isoenzymes, kuchuluka C_max saxagliptin ndi 21%, koma saxagliptin AUC sasintha.

Diltiazem: Kugwiritsa ntchito limodzi kophatikizira kwa saxagliptin (10 mg) ndi diltiazem (360 mg wowerengeka wa mulingo wofanana muyezo), inhibitor ya CYP3A4 / 5 isoenzymes, kumawonjezera C_max saxagliptin ndi 63%, ndi AUC - 2.1 zina. Izi zimatsatana ndi kuchepa kofananira kwa C_max ndi AUC ya metabolite yogwira ndi 44% ndi 36%, motsatana.

Ketoconazole: Kugwiritsa ntchito limodzi mlingo wa saxagliptin (100 mg) ndi ketoconazole (200 mg maola 12 aliwonse molingana), kumawonjezeka_max ndi AUC ya saxagliptin 2.4 ndi 3.7 nthawi, motsatana. Izi zimatsatana ndi kuchepa kofananira kwa C_max ndi AUC ya metabolite yogwira ndi 96% ndi 90%, motero.

Rifampicin: Kugwiritsa ntchito limodzi mlingo wa saxagliptin (5 mg) ndi rifampicin (600 mg kamodzi patsiku mu ofanana)_max ndi AUC ya saxagliptin ndi 53% ndi 76%, motero, ndi kuwonjezeka kofananira kwa C_max(39%), koma popanda kusintha kwakukulu mu AUC ya metabolite yogwira.

Omeprazole: Kuphatikiza kosiyanasiyana kwa saxagliptin pa mlingo wa 10 mg kamodzi patsiku ndi omeprazole pa mlingo wa 40 mg, gawo lapansi la isoenzyme CYP2C19 (lolimba) ndi isoenzyme CYP3A4 (ofooka), inhibitor ya isoenzyme CYP2C19 ndi inducer MRP-3ok.

Aluminium hydroxide + magnesium hydroxide + simethicone: Kugwiritsa ntchito limodzi mphamvu ya saxagliptin (10 mg) ndi kuyimitsidwa komwe kumakhala ndi aluminium hydroxide (2400 mg), magnesium hydroxide (2400 mg) ndi simethicone (240 mg) otsitsa C_max saxagliptin ndi 26%, komabe saxagliptin AUC sasintha.

Famotidine: Kutenga muyezo umodzi wa saxagliptin (10 mg) patatha maola atatu mutamwa limodzi la famotidine (40 mg), choletsa hOCT-1, hOCT-2, ndi hOCT-3, kumawonjezera C_max saxagliptin ndi 14%, komabe, saucagliptin AUC sasintha.

Mankhwala Okhala Pamalo a Pharmacy

Mankhwala ndi mankhwala.

Migwirizano ndi magwiritsidwe akusungidwa

Kutentha kopitilira 30 ° C. Pewani kufikira ana. Moyo wa alumali ndi zaka zitatu.

Kugwiritsa ntchito mankhwala Combogliz kutalika pokhapokha malinga ndi dokotala, malangizo ndi omwe amaperekedwa!

Kutulutsa mawonekedwe, kapangidwe kake ndi ma CD

Amapezeka m'mitundu itatu yamatumbo (mg):

• metformin - 1000, saxagliptin - 2,5,
• metformin - 1000, saxagliptin - 5.0,
• metformin - 500, saxagliptin - 5.0.

Zowonjezera:

• magnesium wakuba,
• carmellose sodium
• hypromellose.

Pali mapiritsi 7 pachimake, pakatoni kolumikizidwa koyambira koyamba kumatha kukhala matuza 4 kapena 8.

Zotsatira za pharmacological

Mapiritsi okhala ndi machitidwe ophatikizidwa, kumasulidwa kosinthidwa ndi zomwe zili ndi zosakaniza ziwiri zomwe zimathandizana.

Metformin ndi biguanide. Imalepheretsa gluconeogeneis, imasokoneza makutidwe ndi okosijeni a mafutawa ndikuwonjezera chidwi cha zolandilira kulandira insulin. Kugwiritsa ntchito shuga m'magazi kumathandizidwanso. Gawolo silikhudza zomwe zili ndi insulin m'magazi pawokha, sizoyambitsa hypoglycemia. Zimathandizanso kaphatikizidwe ka glycogen. Kuchulukitsa kwa shuga chifukwa chowonekera maselo. Kuphatikiza apo, mankhwalawa amatha kuchepetsa kuchuluka kwa shuga m'matumbo am'mimba, chifukwa cha zomwe zimapangitsa kuchepetsa thupi. Athandizenso kusintha magazi.

Saxagliptin imawonjezera kutulutsidwa kwa mahomoni enieni - ma insretins. Amalimbikitsa kutulutsidwa kwa insulini kuchokera ku cell ya beta ya kapamba ndikuchepetsa kupanga kwa glucagon mmenemo. Kuthekera kwakukulu kwa saxagliptin ndikuchepetsa shuga m'mimba yopanda kanthu komanso chakudya.Komanso, kumasulidwa kwa m'mimba ndikulepheretsa, kotero kuti pakhale kutalikirana kwakukulu. Zimathandizanso kuchepetsa kuchepa kwa odwala matenda ashuga.

Chifukwa cha kumasulidwa kosinthidwa, chiopsezo cha zovuta kuchokera m'matumbo am'mimba chimachepetsedwa.

Contraindication

• Hypersensitivity pamagawo ake,
• Mbiri yakusokosera kwa anaphylactic,
• Mtundu woyamba wa shuga
• Lactose tsankho,
• Chithandizo cha insulin
• Kafukufuku pogwiritsa ntchito zinthu zopangidwa ndi ayodini (maola 48 asanafike ndi pambuyo pake),
• Matenda a impso ndi kwa chiwindi,
• Matenda owopsa, opatsirana komanso opatsirana,
• Matenda a shuga ketoacidosis
• Mbiri yakale yokoma
• Kuopsa kwa minofu hypoxia,
• Mbiri ya lactic acidosis,
• Zakudya zochepa zopatsa mphamvu
• Mimba komanso kuyamwa
• Osakwana zaka 18
• Mowa

Malangizo ogwiritsira ntchito (njira ndi Mlingo)

Amasankhidwa payekha kutengera umboni.

Tengani nthawi 1 patsiku nthawi imodzi. Chipolopolo sichiyenera kusweka, chifukwa izi zimakhudza kuchuluka kwa kumasulidwa. Imwani madzi ambiri.

Chithandizo chimayamba ndi mapiritsi a 500 + 2.5 mg, ndiye amatha kuwonjezereka mpaka 1000 + 5 mg. Zolemba malire - 2000 + 5 mg. Onjezani mlingo pang'onopang'ono kuti muchepetse zotsatira zosafunikira.

Ngati izi zisanachitike, wodwalayo adathandizidwa ndi othandizira omwe ali ndi zinthu izi, koma payokha, mlingo wake umasankhidwa molingana ndi woyamba. Zokhudza momwe thupi lasinthira kuchokera ku mankhwala ena a hypoglycemic kupita ku mankhwalawa silinaphunzire.

Zotsatira zoyipa

• Mutu, migraine,
• Matenda a genitourinary
• Kupweteka kwam'mimba
• Sinusitis
• Kusanza ndi kusanza
• Kutsegula m'mimba
• Kutupa
• Hypoglycemia (wochokera ku saxagliptin),
• Urticaria,
• Supombocytopenia
• Thupi lawo siligwirizana
• Nasopharyngitis,
• Gastroenteritis
• Pancreatitis
• Mavuto okoma
• Zachisangalalo.

Amachotsedwa mwina mwa kusintha mlingo, kapena kusiya mankhwala.

Bongo

Ngati chizolowezi chitha, lactic acidosis imatha kuchitika. Izi zili ndi zovuta zowopsa - ngakhale imfa. Ngati pali kukaikira kulikonse, wodwalayo ayenera kuchipatala. Chipatala chimapereka hemodialysis ndi dalili.

• myalgia
• kulephera kupuma
• kugona kwambiri
• kupweteka m'mimba
• kununkhira kwa acetone kuchokera mkamwa.

Mukamamwa mankhwala ena, makamaka chifukwa cha sulfonylurea, chiopsezo cha hypoglycemia chimawonjezeka. Zizindikiro zake: kufooka, khungu, khungu lodzala (mpaka kukomoka), njala, kusokonekera, ndi ena. Fomu yosavuta imachotsa kudya zakudya zotsekemera. Zapakati komanso zowopsa - jakisoni wa shuga kapena dextrose solution. Ndikofunikira kuti munthu azindikire, kenako kufunsa dokotala kuti musinthe mlingo.

Kuyanjana kwa mankhwala osokoneza bongo

Imalimbikitsa ntchito yogwira ntchito:

• aluminium hydroxide,
• pioglitazone
• magnesium hydroxide,
• rifampicin
• GKS,
• nicotinic acid
• simethicone
• estrogens
• thiazide okodzeya,
• mahomoni a chithokomiro,
• isoniazid
• phenothiazines,
• phenytoin
• amphanomachul
• blockers of pang'onopang'ono calcium njira.

Chepetsani kugwiritsa ntchito bwino zinthu:

• diltiazem
• fukuchiyama
• amprenavir
• verapamil
• erythromycin
• ketoconazole,
• aprepitant
• glibenclamide,
• zochokera sulfonylurea,
• msuzi wa mphesa
• genotidine
• isoenzymes CYP3A4 / 5,
• mangochinos
• kukonzekera kwa cationic
• nifedipine
• Mowa.

Dokotala wopezekapo amayenera kudziwa chithandizo ndi mankhwalawa popereka mankhwala.

Malangizo apadera

Popeza mankhwalawa amachotsa impso, tikulimbikitsidwa kuyesedwa pafupipafupi ndikuwunika momwe alili kuti apewe zovuta. Izi zimachitika makamaka kwa okalamba.

Odwala pambuyo pa zaka 60, lactic acidosis imachitika pafupipafupi. Kuyang'aniridwa ndi katswiri ndikofunikira.

Kuthekera kwa kukhala ndi kapamba kumakulirakulira. Chizindikiro chachikulu ndi kupweteka kwakanthawi, m'mimba.

Wodwala ayenera kudziwa zizindikiro za zovuta komanso athe kupereka thandizo.

Ngati ndi kotheka, njira zopangira opaleshoni yaumunthu zimasamutsidwa ku insulin.

Palibe maphunziro omwe adachitika pazokhudza kuyendetsa galimoto. Komabe, pophatikiza chithandizo, chiopsezo cha hypoglycemia ziyenera kukumbukiridwa. Saxagliptin imatha kupweteketsanso mutu komanso mutu. Lingaliro la kuthekera koyendetsa galimoto kapena kugwira ntchito ndi machitidwe amapangidwa ndi katswiri.

Fananizani ndi fanizo

Mankhwalawa ali ndi misonkho ingapo pamapangidwe ndi katundu. Kukhala kofunikira kuzidziwa bwino.

"Yanumet." Mtengo - kuchokera ku ma ruble 2830 a mapiritsi a 56. Kuphatikizikako kumaphatikizapo metformin ndi sitagliptin. Amapanga kampani Merck Sharp ndi Dome, USA. Itha kugwiritsidwa ntchito molumikizana ndi insulin, komabe, zambiri zoyipa ndi contraindication. Osamalembera ana ndi amayi apakati. Ambiri amalemba kuti mankhwalawa amachepetsa thupi mosavuta.

Galvus Met. Mtengo - 1500 rubles ndi pamwambapa. Muli ndi metformin ndi vildagliptin. Wopanga - "Novartis", Switzerland. Ndiotsika mtengo, ngakhale malo ake siosiyana ndi "Comboglize". Mndandanda wa contraindication ndi ofanana.

"Comboglize Xr." Ilinso ndi mawonekedwe ofanana. Amaperekedwa ndi kampani ya AstraZeneca, Great Britain. Mtengo udzafunika ma ruble 1650 pa paketi iliyonse. Analogue oyandikana kwambiri ndi katundu. Zotsatira zonse zoyipa ndi contraindication ndizofanana.

Glibomet. Mankhwala opangidwa ndi kampani "Berlin Chemie", Germany. Mtengo - ma ruble 350 pa phukusi lililonse. Zosakaniza zogwira ntchito - glibenclamide ndi metformin. Siwothandiza aliyense. Zoletsa zambiri kugwiritsa ntchito.

Bagomet. Mapiritsi a Metformin ndi glibenclamide okhala ndi miyala. Mtengo - kuchokera ku ma ruble 160. Ali ndi chochita chowonjezera, amapangidwa ndi kampani Chemistry Montpellier, Argentina. Kuphatikiza kwakukulu ndi mtengo wotsika wokhala ndi katundu wofanana. Contraindations ndi ofanana.

Chisankho chosinthira ku mankhwala ena chimapangidwa ndi adotolo. Kudzipatsa nokha koletsedwa!

Kwambiri pali malingaliro abwino a mankhwalawo. Zokhazo zoyipa ndizokwera mtengo. Komanso pakuwunika kumadziwika kuti iwo omwe adatenga metformin iyi asanayerekezedwe ndi boma lapitalo ali ndi zovuta zochepa. Kuchepetsa thupi kumawonedwanso, komanso ndi zakudya.

Victor: “Ndakhala ndikugwiritsa ntchito mapiritsi a metformin kwazaka zambiri. Anasiya kupereka zomwe akufunazo, adotolo adatchulanso kukonzekera kwa Combogliz Prolong. Zomwe ndimakonda: mwachangu amapereka zotsatira, ingomwa piritsi limodzi patsiku. Amakhala ndi miyeso yabwinobwino komanso shuga. Zomwe sindimakonda: pali zovuta zina, makamaka ngati mumaphwanya zakudya. Zimathandiza kwambiri, ngakhale kuti zimawononga ndalama zambiri. ”

Alexandra: “Ndimadwala matenda ashuga komanso wodziwa zambiri. Posachedwa, ndimangogwiritsa ntchito mankhwala ochokera kunja. Tsopano ndikuvomereza Combogliz Kutalika. Mankhwalawa ndiabwino, ndilibe mavuto. Ndiwosavuta kulandira, mtengo / mtundu wake ndi zonse. ”

Pomaliza

Mankhwalawa ndi othandiza kwambiri. Chifukwa cha zomwe zamasulidwazo, zimathandizira kupewa kukula kwa mavuto ndi m'mimba. Ndemanga kuchokera kwa ogwiritsa ntchito mankhwala ndi akatswiri ndizabwino kwambiri. Zokhazo zoyipa ndizokwera mtengo komanso kufunikira kwa dongosolo mu mankhwala. Kupanda kutero, ndi mankhwala abwino a shuga.

Njira yogwiritsira ntchito

Akuluakulu: Ndimamwa pakamwa nthawi imodzi / tsiku ndikudya. Mlingo uyenera kusankhidwa payekha.
Monga mankhwala ophatikiza ndi saxagliptin ndi metformin, muyezo wa saxagliptin ndi 5 mg 1 nthawi / tsiku. Mlingo woyamba wa metformin wosinthika kumasulidwa ndi 500 mg 1 nthawi / tsiku, utha kuwonjezereka mpaka 2000 mg 1 nthawi / tsiku.
Mlingo wa metformin ukuwonjezeka pang'onopang'ono kuti muchepetse chiopsezo cha zotsatira zoyipa kuchokera m'mimba.
Mulingo wambiri watsiku ndi tsiku: saxagliptin 5 mg ndi masinthidwe otulutsidwa a 2000 mg.

- Type 2 shuga mellitus wophatikizidwa ndi zakudya komanso masewera olimbitsa thupi kuti muzitha kuyendetsa bwino glycemic control.

Fomu ya Mlingo:

Piritsi limodzi yokutidwa ndi kanema ndi kutulutsidwa kosinthidwa

1000 mg + 2,5 mg ili.

Zinthu zogwira ntchito: metformin hydrochloride 1000 mg + saxagliptin 2.5 mg

Pakatikati pa cholembapo: metformin hydrochloride yosakanikirana ndi 0,5% ya magnesium yotentha 1005.0 mg (1000.0 mg metformin hydrochloride + 5.0 mg magnesium stearate), sodium carmellose 50.0 mg, hypromellose 2208 393.0 mg, magnesium stearate 2.0 mg

utoto woyamba wa zokutira za chipolopolo (zoteteza): Opadry II woyera (% m / m) 130,5 mg polyvinyl mowa pang'ono hydrolyzed 40.00%, titanium dioxide 25.00%, macrogol 3350 20.20%, talc 14.80%, 1 M yankho la hydrochloric acid kuti pH 2 , 0 ± 0.3 *,

wachiwiri wosanjikiza wa chipolopolo (chogwira): saxagliptin 2.5 mg, Opadray II yoyera 20,0 mg, 1 M hydrochloric acid yankho la pH 2.0 ± 0.3 *,

kanema wa kanema (wachitatu wosanjikiza (mtundu)): Opadry II wachikasu (% m / m) 48.0 mg polyvinyl mowa pang'ono hydrolyzed 40.00%, titanium dioxide 24.25%, macrogol 3350 2020%, talc 14.80%, utoto wachitsulo wachikasu 0,75% , 1 M yankho la hydrochloric acid kuti pH 2.0 ± 0.3 *,

inki yolemba: inki Opacode buluu ** (% m / m) 0,03 mg indigo carmine aluminium varnish 16.00%, shellac

45% (20% esterified) mu ethanol 55.40%, komaanol 15.00%, propylene glycol 10.50%, isopropanol 3.00%, 28% yankho la ammonium hydroxide 0.10%.

Piritsi limodzi la 500 mg + 5 mg lojambulidwa lili.

Zinthu zogwira ntchito: metformin hydrochloride 500 mg + saxagliptin 5 mg

Pakatikati pa cholembapo: metformin hydrochloride mu osakaniza 0,5% magnesium stearate 502.5 mg (500.0 mg metformin hydrochloride + 2,5 mg magnesium stearate), sodium carmellose 50.0 mg, hypromellose 2208 358.0 mg, hypromellose 2910 10.0 mg, microcrystalline cellulose 102.0 mg, magnesium stearate 1.0 mg,

utoto woyamba wa zokutira za chipolopolo (zoteteza): Opadry II Woyera (% m / m) 99.0 mg polyvinyl mowa pang'ono hydrolyzed 40.00%, titanium dioxide 25.00%, macrogol 3350 20.20%, talc 14.80%, 1 M yankho la hydrochloric acid kuti pH 2 , 0 ± 0.3 *, bi yachiwiri yosanjikiza (yogwira): saxagliptin 5.0 mg, Opadry II yoyera 20,0 mg, 1 M yankho la hydrochloric acid kuti pH 2.0 ± 0.3 *,

kanema wa kanema (wachitatu wosanjikiza (mtundu)): Opadry II tawny (% m / m) 33.0 mg polyvinyl mowa pang'ono hydrolyzed 40.00%, macrogol 3350 20,20%, titanium dioxide 19.58%, talc 14.80%, utoto wachitsulo wachikasu 5, 00% ndi utoto wa iron oxide ofiira 0,42%, 1 M yankho la hydrochloric acid kuti pH 2.0 ± 0.3 *,

inki yolemba: inki Opacode buluu ** (% m / m) 0,03 mg indigo carmine aluminium varnish 16.00%, shellac

45% (20% esterified) mu ethanol 55.40%, komaanol 15.00%, propylene glycol 10.50%, isopropanol 3.00%, 28% yankho la ammonium hydroxide 0.10%.

Piritsi limodzi lokhathamira la 1000 mg + 5 mg lili ndi:

Zinthu zogwira ntchito: hydrochloride 1000 mg + saxagliptin 5 mg Pakatikati pa cholembapo: metformin hydrochloride yosakanikirana ndi 0,5% ya magnesium yotentha 1005.0 mg (1000.0 mg metformin hydrochloride + 5.0 mg magnesium stearate), sodium carmellose 50.0 mg, hypromellose 2208 393.0 mg, magnesium stearate 2.0 mg

utoto woyamba wa zokutira za chipolopolo (zoteteza): Opadry II woyera (% m / m) 130,5 mg polyvinyl mowa pang'ono hydrolyzed 40.00%, titanium dioxide 25.00%, macrogol 3350 20.20%, talc 14.80%, 1 M yankho la hydrochloric acid kuti pH 2 , 0 ± 0.3 *,

wachiwiri wosanjikiza wa chipolopolo (chogwira): saxagliptin 5.0 mg, Opadry II Woyera 20.0 mg, 1 M yankho la hydrochloric acid kuti pH 2.0 ± 0.3 *,

kanema wa kanema (wachitatu wosanjikiza (mtundu)): Opadry II pink (% m / m) 48.0 mg polyvinyl mowa pang'ono hydrolyzed 40.00%, titanium dioxide 24.25%, macrogol 3350 20.20%, talc 14.80%, utoto wa iron utayidi wofiira 0,75% , 1 M yankho la hydrochloric acid kuti pH 2.0 ± 0.3 *,

inki yolemba: inki Opacode buluu ** (% m / m) 0,03 mg indigo carmine aluminium varnish 16.00%, shellac

45% (20% esterified) mu ethanol 55.40%, komaanol 15.00%, propylene glycol 10.50%, isopropanol 3.00%, 28% yankho la ammonium hydroxide 0.10%.

* Ngati ndi kotheka, njira ya 1 M sodium hydroxide ingagwiritsidwe ntchito kusintha pH.
** Ngati ndi kotheka, mowa wa isopropanol umawonjezeredwa ku inki panthawi yolembera. Zotsatira za indigo carmine aluminium varnish ndi shellac zimangokhala pamapiritsi pomwe zalembedwa. Zinthu zosungunulira zomwe zimaphatikizidwa ndi inki zimachotsedwa pakupanga.

Mapiritsi a 1000 mg + 2,5 mg:

Mapiritsi okhala ndi mawonekedwe a biconvex a Capsule, opakidwa utoto kuyambira wachikasu kupita ku chikaso chowoneka chikaso, ndi mawu oti "2,5 / 1000" mbali ina ndi "4222" mbali inayi, inki ya buluu.

500 mg + 5 mg mapiritsi:
Mapiritsi okhala ndi mawonekedwe a biconvex wooneka ngati Capsule, wopangidwa kuchokera ku bulauni mpaka bulauni, pomwe mawu akuti "5/500" mbali ina ndi "4221" mbali inayi, inki ya buluu.

Mapiritsi a 1000 mg + 5 mg:
Mapiritsi okhala ndi mawonekedwe a biconvex wa Capsule, wokutidwa ndi membala wamakanema apinki, wokhala ndi mawu akuti "5/1000" mbali imodzi ndi "4223" mbali inayi, inki yabuluu.

ZOCHULUKITSA ZA ZAULERE

Mankhwala

Njira yamachitidwe
Combogliz Prolong ® imaphatikiza mankhwala awiri a hypoglycemic omwe ali ndi njira zowonjezera kuchitira patsogolo glycemic control mwa odwala omwe ali ndi mtundu wa 2 shuga mellitus (T2DM): saxagliptin, dipeptidyl peptidase 4 inhibitor (DPP-4), ndi metformin, woimira kalasi yayikulu.

Saxagliptin
Poyankha kudya kwakudya kuchokera m'matumbo aang'ono, mahomoni amtundu wa impretin amatulutsidwa m'magazi, monga glucagon-peptide-1 (GLP-1) ndi insulinotropic polypeptide (HIP) ya glucose. Ma mahomoniwa amalimbikitsa kutulutsa kwa insulin kuchokera ku maselo a pancreatic beta, kutengera kuchuluka kwa shuga m'magazi, koma samapangidwira ndi enzyme DPP-4 kwa mphindi zingapo. GLP-1 imachepetsa kubisalira kwa glucagon m'maselo a alpha, ndikuchepetsa kupanga shuga kwa chiwindi. Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri, anthu ambiri omwe amakhala ndi GLP-1 amatsitsidwa, koma mayankho a insulin ku GLP-1 amakhalabe. Saxagliptin, wokhala mpikisano wopikisana ndi DPP-4, amachepetsa mphamvu ya kuchuluka kwa ma impretin, potero amawonjezera kuchuluka kwawo m'magazi ndikupangitsa kutsika kwama glucose posachedwa kudya.

Metformin
Metformin ndi mankhwala osokoneza bongo a hypoglycemic omwe amapititsa patsogolo kulekerera kwa glucose kwa odwala omwe ali ndi matenda a shuga a 2, amachepetsa kuyambira kwa shuga ndi postprandial glucose. Metformin imachepetsa kupanga shuga ndi chiwindi, imachepetsa mayamwidwe am'matumbo m'matumbo ndikukulitsa kumva kwa insulin, kukulitsa kuphatikizika kwa magazi ndi kugwiritsa ntchito shuga. Mosiyana ndi kukonzekera kwa sulfonylurea, metformin sayambitsa hypoglycemia kwa odwala omwe ali ndi matenda a shuga a 2 kapena anthu athanzi (kupatula pazochitika zina, onani zigawo "Precautions" ndi "Maupangiri apadera"), ndi hyperinsulinemia. Pakati pa mankhwala a metformin, kutulutsidwa kwa insulin kumakhalabe kosasinthika, ngakhale kusala kwa insulin komanso kuyankha zakudya masana kumatha kuchepa.

Kuchita Mwachipatala ndi Chitetezo

Saxagliptin M'maso awiri akhungu, osasankhidwa, mayesero azachipatala, mankhwala a saxagliptin adalandiridwa ndi oposa 17,000 odwala T2DM.

Zotsatira za mtima
Kafukufuku wa SAVOR (Kuwunika kwa Zotsatira za Mtima mu Matenda a Odwala Kutenga Saxagliptin) adawunika zotsatira za mtima mu 16492 odwala T2DM (12959 odwala omwe ali ndi vuto la mtima (CVD), odwala 3533 omwe ali ndi chiwopsezo cha mtima zambiri kupsinjika kwa mtima) ndi mfundo za 6.5% ≤ HbA1c 14 C-saxagliptin 24% ya kuchuluka kwa impso ndi impso ngati saxagliptin osasinthika ndi 36% monga metabolite yayikulu ya saxagliptin. Ma radioactivine omwe apezeka mumkodzo amafanana ndi 75% ya mlingo womwe unatengedwa. Chilolezo chapakati cha saxagliptin chinali pafupifupi 230 ml / mphindi, kuchuluka kwa kusefera kwa glomerular kunali pafupifupi 120 ml / mphindi. Pa metabolite yayikulu, chilolezo cha impso chinali chofanana ndi tanthauzo la kusefera kwa glomerular. Pafupifupi 22% ya ma radioacaction athu onse adapezeka mu ndowe.

Metformin
Chilolezo cha renal chimakhala chamtunda pafupifupi 3.5 kuposa chilengedwe cha clearinine chilolezo (CC), zomwe zikuwonetsa kuti kubisala kwa tubular ndiyo njira yayikulu yodziwira metformin.Pambuyo pakulowetsa, pafupifupi 90% ya mankhwala odziwikirawa amachotseredwa impso m'masiku 24 oyambirira, ndi theka la moyo kuchokera ku plasma pafupifupi maola 6.2. M'magazi, theka la moyo ndi pafupifupi maola 17.6, chifukwa chake, erythrocyte misa ikhoza kukhala gawo logawidwa.

Pharmacokinetics mwapadera matenda

Kulephera kwina
Sikulimbikitsidwa kugwiritsa ntchito Combogliz Prolong® mwa odwala omwe ali ndi vuto la impso (onani gawo "Contraindication").

Saxagliptin
Odwala omwe ali ndi vuto lofooka la aimpso, mfundo za AUC za saxagliptin ndi metabolite yogwira anali 20% ndi 70% (motsatana) apamwamba kuposa zomwe AUC imachita mwa odwala omwe ali ndi vuto laimpso. Popeza kuwonjezeka kotereku sikumvekedwa kukhala kofunika kwambiri, sikulimbikitsidwa kusintha saxagliptin mwa odwala omwe ali ndi vuto laimpso.

Metformin
Odwala omwe ali ndi vuto la impso (malinga ndi zotsatira za muyeso wa QC), theka la moyo wa metformin kuchokera ku plasma ndi kutalika kwa magazi ndi chilolezo cha impso umachepa mogwirizana ndi kuchepa kwa QC.

Saxagliptin
Odwala omwe ali ndi vuto lochepa kwambiri, loletsa komanso la hepatic kwambiri, panalibe kusintha kwakukulu pama pharmacokinetics a saxagliptin, kotero kusintha kwa mlingo kwa odwala kotere sikofunikira.

Metformin
Sipanapezeke maphunziro a metacokinetic a metformin mwa odwala omwe ali ndi kuwonongeka kwa hepatic.

Saxagliptin
Kukonza mlingo wa saxagliptin malinga ndi jenda la odwala sikofunikira.

Metformin
M'maphunziro azachipatala odwala omwe ali ndi matenda a shuga a 2, zotsatira za hypoglycemic za metformin mwa amuna ndi akazi zinali zofanana.

Saxagliptin
Odwala a zaka zapakati pa 65-80, panalibe kusiyana kwakukulu mu pharmacokinetics ya saxagliptin poyerekeza ndi odwala aang'ono (azaka 18 mpaka 40), motero kusintha kwa odwala okalamba sikofunikira. Komabe, ziyenera kukumbukiridwa kuti m'gulu ili la odwala, kuchepa kwa ntchito yaimpso ndikothekera (onani magawo "Mlingo ndi Ulamuliro" ndi "Maupangiri Apadera").

Metformin
Zambiri zochepa kuchokera ku maphunziro olamulidwa a pharmacokinetics of metformin mwa odzipereka achikulire odzipereka amati chiwonetsero chokwanira cha plasma chikuchepa, theka la moyo limangowonjezeka, ndipo Cmax imawonjezeka poyerekeza ndi mawonekedwe a magawo awa mu odzipereka achinyamata achinyamata. Malinga ndi izi, kusintha kwa ma pharmacokinetics a metformin ndi kukula msinkhu makamaka chifukwa cha kusintha kwa impso. Combogliz Prolong® sayenera kulembedwa kwa odwala omwe ali ndi zaka zopitilira 80, pokhapokha ngati ntchito yachilendo yachilengedwe imatsimikiziridwa ndi zotsatira za muyeso wa QC.

Saxagliptin
Maphunziro a pharmacokinetics a saxagliptin mwa ana sanachitike.

Metformin
Kafukufuku wa pharmacokinetics of metformin amasulidwa amasungidwe mwa ana sanachitike.

Mtundu ndi Fuko

Saxagliptin Sitikulimbikitsidwa kusintha mlingo wa saxagliptin kutengera mtundu wa wodwalayo.

Metformin
Sipanapezeke maphunziro a pharmacokinetics a metformin kutengera mtundu wa odwala.

Type 2 shuga mellitus wophatikizidwa ndi zakudya komanso masewera olimbitsa thupi kuti muzitha kuyendetsa bwino glycemic.

MALANGIZO OTHANDIZA

• Kuchulukitsa chidwi kwa munthu aliyense pazinthu zilizonse za mankhwala,
• Kusintha kwakukulu kwa Hypersensitivity (anaphylaxis kapena angioedema) kwa DPP-4 zoletsa,
• Type 1 shuga mellitus (musanaphunzire)
• Gwiritsani ntchito ndi insulin (simunaphunzire)
• Congenital galactose tsankho, lactase akusowa ndi shuga-galactose malabsorption,
• Mimba, kuyamwa,
• Zofika zaka 18 (chitetezo ndi kusawerengeka),
• Kuwonongeka kwa impso (serum creatinine ≥1.5 mg / dL kwa amuna, ≥1.4 mg / dL kwa akazi kapena kuchepa kwa chilolezo cha creatinine), kuphatikizapo zomwe zimayambitsidwa ndi kuperewera kwa mtima ndi mantha (manjenje), kupweteka kwapakati pa mtima ndi kupindika kwa septicemia,
• Matenda owopsa omwe amakhala ndi chiopsezo chokhala ndi vuto la impso: kuchepa magazi (ndi kusanza, kutsekula m'mimba), kutentha thupi, matenda opatsirana, mikhalidwe ya hypoxia (mantha, sepsis, matenda a impso, bronchopulmonary matenda).
• Pachimake kapena matenda metabolic acidosis, kuphatikiza matenda ashuga a ketoacidosis, kapena opanda chikomokere
• Matenda akufotokozera za matenda owopsa komanso osachiritsika omwe angayambitse kukula kwa minofu hypoxia (kupuma kulephera, mtima kulephera, kulowetsedwa kwadzuwa),
• Kuchita opaleshoni yayikulu ndikuvulaza (chithandizo cha insulin chikusonyeza)
• Kuchepa kwa chiwindi,
• Uchidakwa wambiri ndi poyizoni wa ethanol,
• Lactic acidosis (kuphatikizapo mbiri),
• Nthawi yosachepera maola 48 asanafike komanso mkati mwa maola 48 mutachita maphunziro a radioisotope kapena x-ray ndikuyambitsa ntchito zotsutsana ndi ayodini.
• Kutsatira Zakudya Zochepa-Kalori (Odwala Okalamba
  Popeza saxagliptin ndi metformin amatha kuperewera pang'ono ndi impso, ndipo mwa odwala okalamba kuchepa kwa mphamvu yaimpso kuyenera, Combogliz Prolong® iyenera kugwiritsidwa ntchito mosamala mwa okalamba.

Saxagliptin
Panalibe kusiyana pakukhwimitsa chitetezo kapena kugwiritsa ntchito mankhwalawa kwa odwala> zaka 65,> 75 wazaka, ndi odwala achichepere.
Metformin
Kafukufuku wolamulidwa wa metformin sanaphatikizepo chiwerengero chokwanira cha odwala okalamba kuti athe kudziwa kusiyana pakumayesedwa poyerekeza ndi odwala achichepere, ngakhale zovuta zamankhwala sizinayambitse kusiyana poyankha odwala okalamba ndi achinyamata. Monga mukudziwa, metformin imachotsedwa kwambiri ndi impso, chifukwa chake pali chiopsezo chokhala ndi zovuta zovuta kwa odwala omwe ali ndi vuto la impso. Comboglyz Prolong ® iyenera kugwiritsidwa ntchito pokhapokha kwa odwala omwe ali ndi vuto lachilendo. Mlingo woyamba wa metformin uyenera kuperekedwa kwa odwala okalamba, poganizira kuchepa kwa impso. Kusintha kwa mlingo uliwonse kuyenera kuchitika pambuyo popenda mosamala aimpso.

Chitetezo ndi kufunika kwa mankhwalawa kwa odwala ochepera zaka 18 sizinaphunzire.

ZOTHANDIZA ZONSE

Zotsatira zoyipa zamaphunziro a glycemic control zikagwiritsidwa ntchitosaxagliptin mu monotherapy ndipo akaphatikizidwa ndi mankhwala ena

Saxagliptin
Gome 1 ikufotokozera mwachidule zochitika zoyipa zomwe zimawonedwa pamayeso azachipatala (mosasamala kanthu kuti wofufuzayo adayesa momwe ziliri) mu ≥5% ya odwala omwe amalandila saxagliptin 5 mg, komanso pafupipafupi kuposa gulu la placebo, malinga ndi kusanthula kophatikizidwa kwa kafukufuku wamasabata 24 .

Gome 1. Zochitika zoyipa

Saxagliptin5mgN = 882

MaloN = 799

Matenda opumira kwambiri a m'mapapo

Matenda amitsempha

Kafukufuku 5 omwe amayang'aniridwa ndi placebo omwe adaphatikizidwa pakuwunikira ndi maphunziro awiri ophatikiza ma monotherapy komanso maphunziro amodzi othandizira othandizira ophatikizidwa ndi saxagliptin ku metformin, thiazolidinedione kapena glibenclamide. Odwala omwe amatenga saxagliptin pa mlingo wa 2,5 mg, kupweteka kwamutu (6.5%) ndiye chokhacho chokhacho chomwe chimadziwika ndi pafupipafupi> 5%, ndikupanga pafupipafupi kuposa gulu la placebo.

Malinga ndi kuphatikiza komweku, zochitika zowopsa zomwe zimachitika mu> 2% ya odwala omwe amatenga saxagliptin pa 2,5 mg kapena saxagliptin pa mlingo wa 5 mg ndi kukulira> 1% pafupipafupi kuposa gulu la placebo linaphatikizanso sinusitis (2, 9% ndi 2.6% poyerekeza ndi 1.6%, motsatana), kupweteka kwam'mimba (2.4% ndi 1.7% poyerekeza ndi 0.5%), gastroenteritis (1.9% ndi 2.3 % poyerekeza ndi 0.9%) ndi kusanza (2.2% ndi 2.3% poyerekeza ndi 1.3%).

Zovuta za fractures zinali 1.0 ndi 0,6 pa 100 zaka-odwala, motero, mukamamwa saxagliptin (kusanthula kwapadera kwa 2,5 mg, 5 mg ndi 10 mg) ndi placebo. Pafupipafupi fractures odwala omwe akutenga saxagliptin sizinawonjezeke pakapita nthawi. Chiyanjano cha causal sichinakhazikitsidwe, ndipo kafukufuku wamakedzana sanawonetse zotsatira zosafunikira za saxagliptin pamafupa.

Pa pulogalamu yachipatala, kukulitsa kwa thrombocytopenia kogwirizana ndi kupezeka kwa idiopathic thrombocytopenic purpura kunawonedwa. Kugwirizana pakati pa chitukuko cha izi ndi kayendetsedwe ka saxagliptin sikudziwika.

Zochitika zoyipa zomwe zimakhudzana ndi mgwirizano wa saxagliptin ndi metformin pochiza odwala omwe ali ndi matenda a shuga a 2 omwe sanalandire chithandizo cham'maphunziro a glycemic controlSaxagliptin
Gawo 2 limaliza mwachidule zochitika zovuta zomwe zidawonedwa (mosasamala kanthu za ubale wapamalo wofufuzayo) mu ≥ 5% ya odwala omwe akuchita nawo kafukufuku wowonjezera wa masabata 24 ndi kuwongolera kogwiritsidwa ntchito kophatikizika kwa saxagliptin ndi metformin mwa odwala omwe sanalandire chithandizo.

Gome 2. Zochitika zoyipa

Kuchuluka(%)la odwala

Saxagliptin5mg+metformin*N = 320

Metformin* N = 328

* Mlingo woyambirira wa metformin 500 mg / tsiku unakulitsidwa mpaka mlingo waukulu wa 2000 mg / tsiku.

Odwala omwe amalandila saxagliptin kuwonjezera pa chithandizo cha metformin kapena njira yoyambirira yophatikizira, kutsegula m'mimba kunali chokhacho chokhacho chomwe chimachitika mu ≥ 5% ya odwala m'gulu lililonse. Zomwe zimayambitsa matenda otsekula m'mimba zinali 9.9%, 5.8% ndi 11.2% mu saxagliptin gulu 2,5 mg, saxagliptin 5 mg ndi placebo, motero, pophunzira za saxagliptin kuti metformin, chiwopsezo cha matenda otsekula m'mimba chinali 6.9% ndi 7.3% mu gulu lophatikiza mankhwala omwe ali ndi saxagliptin 5 mg ndi metformin ndi gulu la metformin monotherapy pophunzira mankhwala oyamba ndi metformin.

Hypoglycemia

Saxagliptin
Zambiri zokhudzana ndi hypoglycemia ngati chochitika chovuta zinasonkhanitsidwa pamaziko a malipoti a hypoglycemia; kuchuluka kwa kuchuluka kwa shuga sikunafunike. Zomwe zimachitika mu hypoglycemia pogwiritsa ntchito saxagliptin 2.5 mg, saxagliptin 5 mg ndi placebo (zonse monga monotherapy) zinali 4%, 5.6% ndi 4.1%, motero, ndi 7.8%, 5.8% ndi 5 %, motero, ndi kuwonjezera kwa metformin. Kuchuluka kwa hypoglycemia kunali 3,4% mwa odwala omwe sanapezeke kale omwe amatenga saxagliptin pa mlingo wa 5 mg wophatikizidwa ndi metformin, ndi 4% mwa odwala omwe amapezeka pa metformin monotherapy.

Hypersensitivity zimachitika

Saxagliptin
Pakufufuza kwamaphunziro asanu ophatikizidwa, zochitika zotsutsana ndi hypersensitivity (monga urticaria ndi nkhope ya edema) zinaonedwa mu 1.5%, 1.5% ndi 0.4% ya odwala omwe amalandila saxagliptin pa mlingo wa 2,5 mg, saxagliptin pa mlingo 5 mg ndi placebo, motero. Malinga ndi ofufuza, palibe chilichonse mwazinthu izi zomwe odwala omwe amalandila saxagliptin amafuna kuti agonekere kuchipatala ndipo sanawopseze miyoyo ya odwala. Pakuwunika kwakasinkhidwe kameneka, wodwala m'modzi yemwe amalandila saxagliptin sanatengedwe nawo phunzirolo chifukwa chotukukira urticaria ndi mtima wambiri.

Zisonyezero zamagulu olimbitsa thupi

Saxagliptin
Odwala omwe adalandira saxagliptin ngati monotherapy kapena osakanikirana ndi metformin, palibe kusintha kwakufunika kwakuwonekera kwakutithandiza pakuwonekera.

Monotherapy

Metformin
M'maphunziro omwe amayendetsedwa ndi placebo, zochitika zovutitsa kwambiri zomwe zimawonedwa mu> 5% ya odwala omwe adalandira metformin yotulutsidwa ndikulimidwa pafupipafupi kuposa momwe gulu la placebo lidataya ndi mseru / kusanza.

Magulu Osiyanasiyana a Saxagliptin mu SAVOR Study

Mu kafukufuku wa SAVOR, odwala 8240 adalandira saxagliptin pa mlingo wa 2,5 mg kapena 5 mg kamodzi tsiku lililonse, ndipo odwala 8173 adalandira placebo.Nthawi yayitali ya mankhwala a saxagliptin, mosasamala ndi kusokonezeka kwa chithandizo, panali zaka 1.8. Mu odwala 3698 (45%), kutalika kwa mankhwala a saxagliptin anali zaka 2-3. Zomwe zimachitika pazochitika zoyipa motsatira kafukufukuyu pagulu la odwala omwe akutenga saxagliptin (72,5%) anali ofanana ndi zomwe zimachitika mu gulu la placebo (72.2%).

Pafupipafupi kuleka kwa mankhwala chifukwa cha zovuta sizinachitike ngati odwala amatenga saxagliptin (4,9%) ndi placebo (5%). Kafukufuku wa SAVOR adawunika zotsatira za saxagliptin pakachitika zovuta zamtima. Kuonjezera saxagliptin ku mankhwala sanakuwonetse kuchulukitsa zovuta za mtima (monga kufa ndi mtima, infarction ya nonfatal myocardial, nonfatal ischemic stroke mwa odwala T2DM poyerekeza ndi placebo (RR 1.00, 95% CI 0, 89, 1.12, P Mtheradi wa ma lymphocyte

Saxagliptin
Mukamagwiritsa ntchito saxagliptin, kuchepa kwapakati pa kuchuluka kwa ma mankhwalawa kumawonedwa. Mukamasanthula kafukufuku wophatikizidwa wa masabata makumi awiri ndi awiri, maphunziro owongoleredwa ndi malo, kutsika kwapakati pa 100 ndi ma cell 120 / μl ya kuchuluka kwathunthu kwa ma lymphocyte kuchokera ku chiwerengero choyambirira cha maselo a 2200 / μl amawonetsedwa ndi saxagliptin pa mlingo wa 5 mg ndi 10 mg, poyerekeza ndi placebo . Zofananazo zimawonedwa pakumwa saxagliptin pa 5 mg mu kuphatikiza koyamba ndi metformin poyerekeza ndi metformin monotherapy. Panalibe kusiyana pakati pa 2,5 mg saxagliptin ndi placebo. Gawo la odwala omwe kuchuluka kwa ma lymphocyte anali ≤ 750 maselo / μl anali 0,5%, 1.5%, 1.4%, ndi 0,4% m'magulu azachipatala a saxagliptin pa mlingo wa 2.5 mg, pa 5 mg , pa mlingo wa 10 mg ndi placebo, motero. Odwala ambiri omwe amagwiritsa ntchito saxagliptin mobwerezabwereza, sanayambenso kuyambiranso, koma mwa odwala ena kuchuluka kwa ma lymphocyte kunachepa kachiwiri ndi kuyambiranso kwa mankhwala ndi saxagliptin, komwe kunapangitsa kuti saxagliptin ithe. Kutsika kwa kuchuluka kwa ma lymphocyte sikunayendetsedwe ndi mawonetsedwe azachipatala.

Mu kafukufuku wa SAVOR, kuchepa kwa kuchuluka kwa ma lymphocyte m'gulu la saxagliptin kumaonedwa mu 0.5% ya odwala, omwe ali mgulu la placebo - mu 0.4% ya odwala.

Zomwe zimapangitsa kuchepa kwa chiwerengero cha ma lymphocyte pa saxagliptin chithandizo chofanana ndi placebo sizikudziwika. Pakakhala matenda osazolowereka kapena osakhalitsa, ndikofunikira kuyeza kuchuluka kwa ma lymphocyte. Mavuto a saxagliptin pa kuchuluka kwa ma lymphocyte odwala omwe ali ndi vuto lambiri la mankhwalawa (mwachitsanzo, kachilombo ka chitetezo cha munthu) sikadziwika.

Saxagliptin
Saxagliptin sanali ndi vuto lachipatala kapena lachiwonetsero pakuwonekera kwa maselo a m'magulu asanu ndi m'modzi amaso awiri, owongolera mayesero azachipatala otetezeka komanso ogwira ntchito.

Vitamini B12 Concentration

Mu maphunziro azachipatala olamulidwa a metformin okhala ndi masabata 29, pafupifupi 7% ya odwala adawonetsa kuchepa kwa seramu kale kuposa kutsata kwachilendo kwa Vitamini B12 ku mfundo zapamwamba popanda mawonekedwe owonekera. Komabe, kuchepa kotereku sikumayendera limodzi ndi kukula kwa kuchepa kwa magazi m'thupi ndipo kumachira msanga pambuyo pakuchotsedwa kwa metformin kapena kuchuluka kwa vitamini B12.

CHONCHO

Ndi kugwiritsa ntchito mankhwalawa kwa nthawi yayitali mpaka 80 peresenti kuposa momwe amalimbikitsira, sikuonetsa matendawa.

Pankhani ya mankhwala osokoneza bongo, mankhwala othandizira ayenera kugwiritsidwa ntchito. Saxagliptin ndi metabolite yake yayikulu imapukusidwa ndi hemodialysis (kuchuluka kwa excretion: 23% ya mlingo mu maola 4).

Metformin
Pakhala pali milandu yambiri ya metformin, kuphatikizapo kutenga zoposa 50. Hypoglycemia imayamba pafupifupi 10% ya milandu, koma mgwirizano wake ndi metformin sunakhazikitsidwe. Mu 32% ya milandu yochuluka ya metformin, odwala anali ndi lactic acidosis. Metformin imachotsedwa pakayimbidwe, pomwe chilolezo chimafika 170 ml / min.

KUTENGA KWA ZINSINSI ZINA KAPENA ZINSINSI ZINA ZA KUPANGIRA

Metabolism ya Saxagliptin imayang'aniridwa makamaka ndi cytochrome P450 3A4 / 5 isoenzyme system (CYP3A4 / 5). Kafukufuku wa in vitro awonetsa kuti saxagliptin ndi metabolite yake yayikulu sichikuletsa CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 ndi 3A4 isoenzymes ndipo osalimbikitsa CYP1A2, 2B6, 2C9, ndi 3A4 isoenzymes. Chifukwa chake, zotsatira za saxagliptin pakuvomerezeka kwa mankhwala mu metabolism yomwe ma isoenzymes omwe akukhudzidwa sakuyembekezeredwa ngati agwiritsidwa ntchito limodzi. Saxagliptin sikuti ndi cholepheretsa kapena chosokoneza P-gp.

Metformin
Mankhwala ena amachulukitsa hyperglycemia (thiazide ndi ma diuretics ena, glucocorticosteroids, phenothiazines, kukonzekera kwa mahomoni a chithokomiro, estrogens, njira zakulera zamkati, phenytoin, nicotinic acid, sympathomimetics, pang'onopang'ono calcium blockers ndi isoniazid). Popereka kapena kuletsa mankhwalawa kwa wodwala amene akutenga Combogliz Prolong®, kuchuluka kwa shuga wamagazi kuyenera kuyang'aniridwa mosamala. Mlingo womangidwa wa metformin ku mapuloteni amadzi a m'magazi ndi ochepa, kotero sizingatheke kuti azilumikizana ndi mankhwala omwe amaphatikizidwa kwambiri ndi mapuloteni a plasma, monga salicylates, sulfonamides, chloramphenicol ndi probenecid (mosiyana ndi zomwe zimachokera ku sulfonylurea, zomwe zimamangidwa kwambiri. ndi mapuloteni a seramu).

Zowonetsa za isoenzymes CYP3A4 / 5

Saxagliptin
Rifampicin amachepetsa kwambiri ma saxagliptin osasintha AUC ya metabolite yake yogwira, 5-hydroxy-saxagliptin. Rifampicin sichikuwakhudza kuletsa kwa DPP-4 m'magazi a magazi munthawi yamahora a 24 a chithandizo.

CYP3A4 / 5 Isoenzyme Inhibitors

Saxagliptin
Diltiazem imakulitsa mphamvu ya saxagliptin ikagwiritsidwa ntchito limodzi. Kuwonjezeka kwa kuchuluka kwa saxagliptin m'madzi a m'magazi kuyembekezeredwa ndikugwiritsa ntchito amprenavir, aprepitant, erythromycin, fluconazole, fosamprenavir, madzi a mphesa ndi verapamil, komabe, kumwa kwa saxagliptin sikulimbikitsidwa.

Ketoconazole amachulukitsa kuchuluka kwa saxagliptin mu plasma. Kuwonjezeka kofananako kwa kuchuluka kwa saxagliptin m'madzi a m'magazi kuyembekezeredwa pamene ma inhibitors ena amphamvu a CYP3A4 / 5 isoenzymes amagwiritsidwa ntchito (mwachitsanzo, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir ndi telithromycin. Mukaphatikizidwa ndi inhibitor yamphamvu ya CYP3A4 / 5 isoenzymes, mlingo wa saxagliptin uyenera kuchepetsedwa kukhala 2.5 mg.

Metformin
Mankhwala a Cationic (mwachitsanzo, amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamteren, trimethoprim kapena vancomycin), omwe amachotseredwa ndi impso kudzera mu kusefera kwa glomerular, akhoza kungogwirizana ndi metformin, kupikisana mayendedwe wamba. Mu maphunziro okhudzana ndi mankhwala a metformin ndi cimetidine kamodzi komanso mobwerezabwereza mankhwala, metformin ndi cimetidine amawonetsedwa ngati amaperekedwa mwaumoyo mwa odzipereka athanzi, ndikuwonjezereka kwa 60% kwa kuchuluka kwa metformin mu plasma ndi magazi athunthu komanso kuwonjezeka kwa 40% kwa AUC ya metformin mu plasma ndi kwathunthu magazi. Pakuphunzira ndi mtundu umodzi wa mankhwalawa, palibe chomwe chinasintha mu theka-moyo. Metformin sichikhudza pharmacokinetics ya cimetidine. Ndikulimbikitsidwa kuyang'anira odwala mosamala, ndipo ngati ndi kotheka, sinthani muyezo wa odwala omwe amamwa mankhwala a cationic omwe amuchotsa kudzera mu proximal renal tubule system.

Metformin
Pakufufuza kwakukhudzana ndi kumwa kwa kamodzi kwa mankhwalawa odwala omwe ali ndi matenda a shuga a 2, kugwiritsa ntchito metformin ndi glibenclamide sikukhudza pharmacokinetics kapena pharmacodynamics.

Metformin
Pakufufuza kwa kuyanjana kwa mankhwala a metformin ndi furosemide ndi mlingo umodzi wa mankhwalawo, wopangidwa pa odzipereka athanzi, kuyanjana kwawo kwa pharmacokinetic kuwululidwa. Furosemide imawonjezera Cmax ya metformin mu plasma ndi magazi ndi 22% ndi AUC m'magazi ndi 15% popanda kusintha kwakukulu kwa impso chilolezo cha metformin. Akaphatikizidwa ndi metformin, Cmax ndi AUC ya furosemide imatsika ndi 31% ndi 12%, motero, ndipo theka la moyo limatsika ndi 32% popanda kusintha kooneka m'gulu la furosemide. Palibe deta pakukhudzana kwa metformin ndi furosemide pogwiritsa ntchito nthawi yayitali.

Metformin
Pakufufuza momwe mankhwala a metformin amaphatikizidwira ndi nifedipine limodzi ndi gawo limodzi la mankhwalawa, omwe amapangidwa ndi gawo la odzipereka athanzi, nifedipine imawonjezera Cmax ya plasma metformin ndi 20% ndi AUC ndi 9%, ndikuwonjezera kuchulukitsidwa ndi impso. Tmax ndi kuthetsa theka la moyo sizinasinthe. Nifedipine imawonjezera mayamwidwe a metformin. Metformin ilibe gawo lililonse pa pharmacokinetics ya nifedipine.

Saxagliptin ndi Metformin
Kugwiritsa ntchito limodzi mphamvu ya saxagliptin (100 mg) ndi metformin (1000 mg) sikukhudza kwambiri pharmacokinetics ya saxagliptin kapena metformin odzipereka athanzi. Palibe maphunziro apadera a pharmacokinetic okhudzana ndi mankhwala omwe amagwiritsidwa ntchito ndi Combogliz Prolong® adachitapo, ngakhale kafukufuku wotere wachitika ndi zigawo zake payekha: saxagliptin ndi metformin.

Zotsatira za mankhwala ena pa saxagliptin

Glibenclamide: Kugwiritsa ntchito kamodzi kwa saxagliptin (10 mg) ndi glibenclamide (5 mg), gawo laling'ono la CYP2C9 isoenzyme, kukulitsa Cmax ya saxagliptin ndi 8%, koma AUC ya saxagliptin sizinasinthe.
Pioglitazone: Kugwiritsidwa ntchito mobwerezabwereza kwa saxagliptin kamodzi patsiku (10 mg) ndi pioglitazone (45 mg), gawo laling'ono la isoenzyme CYP2C8 (wamphamvu) ndi CYP3A4 (ofooka), silikuwakhudza pharmacokinetics a saxagliptin.
Digoxin: Kugwiritsidwa ntchito mobwerezabwereza kwa saxagliptin kamodzi patsiku (10 mg) ndi digoxin (0.25 mg), gawo lapansili la P-glycoprotein, sikukhudza ma pharmacokinetics a saxagliptin.
Simvastatin: Kugwiritsidwa ntchito mobwerezabwereza kwa saxagliptin kamodzi patsiku (10 mg) ndi simvastatin (40 mg), gawo lapansi la CYP3A4 / 5 eyeenzymes, kuchuluka kwa Saxagliptin ndi 21%, koma AUC ya saxagliptin sizinasinthe.
Diltiazem: Kugwiritsa ntchito limodzi kophatikizira kwa saxagliptin (10 mg) ndi diltiazem (360 mg wa nthawi yayitali pakulingana), inhibitor ya CYP3A4 / 5 isoenzymes, imachulukitsa Stax ya saxagliptin ndi 63%, ndi AUC nthawi 2.1. Izi zimatsatiridwa ndi kuchepa kofananira kwa Stax ndi AUC ya metabolite yogwira ndi 44% ndi 36%, motsatana.
Ketoconazole: Kugwiritsa ntchito limodzi mlingo wa saxagliptin (100 mg) ndi ketoconazole (200 mg maola 12 aliwonse molingana) kumawonjezera Stax ndi AUC ya saxagliptin 2.4 ndi 3.7 nthawi, motero. Izi zimatsatiridwa ndi kuchepa kofananira kwa Stax ndi AUC ya metabolite yogwira ndi 96% ndi 90%, motsatana.
Rifampicin: Kugwiritsa ntchito limodzi mlingo wa saxagliptin (5 mg) ndi rifampicin (600 mg kamodzi patsiku muyezo) kumachepetsa Stax ndi AUC ya saxagliptin ndi 53% ndi 76%, motsatana, ndi kuwonjezeka kofananira kwa Stax (39%), koma popanda kusintha kwakukulu mu AUC yogwira metabolite.
Omeprazole: Kuphatikizidwa kochulukirapo kwa saxagliptin pa 10 mg kamodzi patsiku ndi omeprazole pa 40 mg, gawo limodzi la isoenzyme CYP2C19 (lolimba) ndi isoenzyme CYP3A4 (ofooka), inhibitor ya isoenzyme CYP2C19 ndi inducer MRP-3lok.

Aluminium hydroxide + magnesium hydroxide + simethicone:
Kugwiritsa ntchito limodzi kwaminyewa ya saxagliptin (10 mg) ndi kuyimitsidwa komwe kuli ndi aluminium hydroxide (2400 mg), magnesium hydroxide (2400 mg) ndi simethicone (240 mg) kumachepetsa Stax ya saxagliptin ndi 26%, komabe saxagliptin AUC sasintha.

Famotidine: Kutenga muyezo umodzi wa saxagliptin (10 mg) patatha maola atatu mutatha kumwa kamodzi kwa famotidine (40 mg), choletsa hOCT-1, hOCT-2, ndi HOCT-3, kumawonjezera Cmax ya saxagliptin ndi 14%, komabe saxagliptin AUC sasintha.

Kutulutsa mawonekedwe ndi kapangidwe kake

Fomu ya Mlingo - mapiritsi otulutsidwa osinthidwa, makatoni okhala ndi makatoni 4 a mapiritsi 7 ndi malangizo ogwiritsira ntchito Combolize Pronge, kuphatikiza mapiritsi a 1000 + 2.5 mg - matuza 8 a mapiritsi 7):

• Mlingo wa 1000 mg + 2.5 mg: kapangidwe kake, biconvex, makanema ojambula kuchokera ku utoto wachikasu, kuwala kwa inki mbali imodzi kudalembedwa "2,5 / 1000", mbali inayo - "4222",
• Mlingo wa 500 mg + 5 mg: kapangidwe kake kolimba, biconvex, chovala cha kanema kuyambira bulauni mpaka bulawuni, wokhala ndi inki wabuluu mbali inayo amalembedwa "5/500", mbali inayo - "4221",
• Mlingo wa 1000 mg + 5 mg: kapangidwe ka kapangidwe kake, biconvex, malaya apinki, pinki inki kumbali imodzi amalembedwa "5/1000", mbali inayo - "4223".

Zinthu zomwe zimagwira piritsi limodzi:

• metformin hydrochloride - 1000 mg + saxagliptin - 2,5 mg,
• metformin hydrochloride - 500 mg + saxagliptin - 5 mg,
• metformin hydrochloride - 1000 mg + saxagliptin - 5 mg.

Zomwe zimapangidwira piritsi limodzi lokhazikika, kutulutsa filimu (1000 mg + 2.5 mg / 500 mg + 5 mg / 1000 mg + 5 mg):

• piritsi yayikulu: metformin hydrochloride mu chisakanizo ndi 0,5% ya magnesium stearate - 1005 / 502.5 / 1005 mg, sodium carmellose - 50/50/50 mg, hypromellose 2208 - 393/358 / 393 mg, hypromellose 2910 - 0/10 / 0 mg, magnesium stearate - 2/1/2 mg, microcrystalline cellulose - 0/102/0 mg,
• wosanjikiza woyamba: (woteteza): Opadry II Woyera (% m / m) - 130,5 / 99 / 130.5 mg (pang'ono hydrolyzed polyvinyl mowa - 40%, titanium dioxide - 25%, macrogol 3350 - 20.2% , talc - 14.8%), 1M hydrochloric acid solution - mpaka pH 2 ± 0.3,
• gawo lina lachiwiri la zigoba zotumphukira (yogwira): saxagliptin - 2,5 / 5/5 mg, Opadry II yoyera - 20/20/20 mg, 1M yankho la hydrochloric acid - mpaka pH 2 ± 0,3,
• inki yolemba: Opacode inki ya buluu (% m / m) - 0,03 / 0,03 / 0,03 mg (indigo carmine aluminium varnish - 16%, shellac

45% mu ethanol - 55.4%, butanol - 15%, propylene glycol - 10,5%, isopropanol - 3%, 28% yankho la ammonium hydroxide - 0,1%.

Gawo lachitatu (mtundu) wa utoto wa zigamba:

• 1000 + 2,5 mg: Opadry II wachikasu (% m / m) - 48 mg (pang'ono hydrolyzed polyvinyl mowa - 40%, titanium dioxide - 24.25%, macrogol 3350 - 20.2%, talc - 14.8% , utoto wachikasu chitsulo okusayidi - 0,75%), 1M hydrochloric acid solution - mpaka pH 2 ± 0,3,
• 1000 + 5 mg: Opadry II tan (% m / m) - 33 mg (pang'ono hydrolyzed polyvinyl mowa - 40%, macrogol 3350 - 20.2%, titanium dioxide - 19.58%, talc - 14.8% , utoto wachikasu chitsulo okusayidi - 5%, utoto wofiira utoto okusayidi - 0,42%), 1M yankho la hydrochloric acid - mpaka pH 2 ± 0,3,
• 500 + 5 mg: Opadry II pinki (% m / m) - 48 mg (pang'ono hydrolyzed polyvinyl mowa - 40%, titanium dioxide - 24.25%, macrogol 3350 - 20.2%, talc - 14.8%, wofiyira utoto wa okusayidi - 0,75%), 1M yankho la hydrochloric acid kukhala pH ya 2 ± 0,3.

MALANGIZO OTHANDIZA

Lactic acidosis

Lactic acidosis ndi osowa, zovuta kagayidwe kachakudya kamene kamatha kukhazikitsidwa chifukwa chakuwunikira kwa metformin panthawi ya mankhwala a Combogliz Prolong®. Ndi chitukuko cha lactic acidosis chifukwa chogwiritsa ntchito metformin, kugwiritsidwa ntchito kwake mu plasma ya magazi kumaposa 5 μg / ml.

Odwala omwe ali ndi matenda ashuga, lactic acidosis nthawi zambiri imayamba ndi kulephera kwambiri kwaimpso, kuphatikizapo chifukwa cha kubadwa kwa impso komanso kusakwanira kwa impso, makamaka mukamamwa mankhwala angapo. Odwala omwe ali ndi vuto la mtima, makamaka odwala omwe ali ndi vuto losakhazikika la angina kapena mtima wovuta komanso chiopsezo cha hypoperfusion ndi hypoxemia, pamakhala chiwopsezo cha lactic acidosis. Chiwopsezo chokhala ndi lactic acidosis imachulukana molingana ndi kuchuluka kwa kulephera kwa impso komanso zaka za wodwalayo.

Kuwunikira pafupipafupi kwa ntchito yaimpso kwa odwala omwe akutenga metformin kuyenera kuchitika ndipo mlingo wofunikira wa metformin uyenera kutumikiridwa. Odwala okalamba, kuwunika ntchito yaimpso ndikofunikira. Metformin sayenera kutumizidwa kwa odwala azaka makumi asanu ndi atatu ndi okulirapo ngati vuto la impso limalephera (malinga ndi data ya QC), popeza odwalawa amakonda kukhala ndi lactic acidosis.Kuphatikiza apo, mankhwala a metformin amayenera kutha yomweyo ngati machitidwe omwe akuphatikizidwa ndi hypoxemia, kufooka kapena sepsis akayamba. Popeza kulephera kwa chiwindi kungachepetse kuthana ndi kukhazikika kwa lactate, metformin sayenera kutumizidwa kwa odwala omwe ali ndi matenda am'chipatala kapena a labotale matenda a chiwindi.

Kukhazikika kwa lactic acidosis nthawi zambiri kumakhala kosadziwika ndipo kumayendera limodzi ndi zizindikiro zopanda pake, monga malaise, myalgia, kulephera kupuma, kuwuma kwambiri, kupweteka komanso kusasangalala pamimba. Hypothermia, hypotension, ndi bradyarrhythmia yolimbana ndi vuto limatha. Wodwala amayenera kufotokozera dokotala zonse mwazizindikirozi. Ngati zizindikiro zotere zapezeka, njira ya metformin iyenera kusiyidwa, kuyang'anira ma seramu elekitirodi, matupi a ketone, shuga wamagazi, ndipo ngati akuwonetsa, magazi a pH, ndende ya lactate ndende ya metformin m'magazi. Zizindikiro zam'mimba zomwe zimayamba kumapeto kwa mankhwala a metformin zimatha chifukwa cha lactic acidosis kapena matenda ena.

Kusala kudya kwa plousma kotsekemera kumachitika ndende pamwamba pamlingo wabwinobwino koma m'munsi mwa 5 mmol / l mwa odwala omwe akutenga metformin kumatha kuwonetsa kukulira kwa lactic acidosis, komanso chifukwa cha zifukwa zina, monga matenda osokoneza bongo a shuga. katundu.

Kukhalapo kwa lactic acidosis kuyenera kuwunika mu odwala onse omwe ali ndi matenda osokoneza bongo komanso metabolic acidosis popanda zizindikiro za ketoacidosis (ketonuria ndi ketonemia).

Lactic acidosis imafunikira chithandizo kuchipatala. Ngati lactic acidosis yapezeka mwa wodwala yemwe akutenga metformin, muyenera kusiya kumwa mankhwalawo nthawi yomweyo ndikuyamba kutsatira njira zothandizira. Ndikulimbikitsidwa kuti dialysis iyambike nthawi yomweyo kuti ikonze acidosis ndi metformin yowonjezera.

Monga mukudziwa, mowa umapangitsa mphamvu ya metformin pa lactate metabolism, yomwe imawonjezera chiopsezo cha lactic acidosis. Chepetsani kumwa mowa mukamamwa Combogliz Prolong®.

Kulephera kwa chiwindi

Kugwiritsa ntchito mankhwalawa Combogliz Prolong® imaphatikizidwa kwa odwala omwe ali ndi matenda azachipatala komanso a labotale chifukwa cha chiwopsezo cha lactic acidosis.

Kuyesa kwa impso

Musanayambe chithandizo ndi Combogliz Prolong® komanso osachepera pachaka, ndikofunikira kuyang'ana ntchito ya impso. Odwala omwe akuyembekezeredwa kuti aimpso ntchito, ntchito yaimpso iyenera kuyesedwa pafupipafupi ndipo chithandizo cha Combogliz Prolong® chiyenera kusiyidwa ngati chizindikiro cha kulephera kwa impso chikuwonekera.

Njira zopangira opaleshoni

Muyenera kusiya kwakanthawi kumwa Combogliz Prolong® musanagwiritse ntchito opareshoni iliyonse (kupatula njira zazing'ono zomwe sizikugwirizana ndi kuchepetsa kudya ndi madzi akumwa), osayambiranso ntchito mpaka wodwalayo atha kumwa mankhwalawo mkati ndikuti ntchito yokhazikika itatsimikizika impso.

Sinthani mu kachipatala ka odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga

Wodwala T2DM, yemwe m'mbuyomu anali wolamulidwa bwino ndi Combogliz Prolong ® komanso yemwe amapatuka magawo a labotale kapena amatenga matenda (makamaka pakudziwika bwino), zizindikiro za ketoacidosis kapena lactic acidosis ziyenera kuwunikiridwa nthawi yomweyo. Kuunika kuyenera kuphatikizira kutsimikiza kwa ma elekitiroma mu seramu yamagazi, ma ketoni, shuga wamagazi ndipo, ngati akuwonetsa, magazi pH, kutsata kwa lactate, pyruvate ndi metformin. Ngati mtundu wina wa acidosis wapezeka, muyenera kusiya Combogliz Prolong® nthawi yomweyo ndikuperekanso mankhwala ena a hypoglycemic.

Kugwiritsa ntchito mankhwala omwe angayambitse hypoglycemia

Saxagliptin
Zochokera ku sulfonylureas ndi insulin zingayambitse hypoglycemia.Chifukwa chake, kuti muchepetse chiopsezo cha hypoglycemia mukamagwiritsa ntchito saxagliptin, kuchepetsa kufotokozera kwa sulfonylurea kapena insulin.
Metformin
Hypoglycemia siimakula mwa odwala omwe amangotenga metformin mwa njira yokhayo, koma imatha kukhala ndi vuto losakwanira la chakudya, pamene ntchito yolimbitsa thupi siziwalitsidwa ndi kudya kwa carbohydrate, kapena kugwiritsa ntchito limodzi ndi mankhwala ena a hypoglycemic (monga sulfonylureas ndi insulin. Okalamba, odwala ofooka kapena operewera bwino ndipo odwala omwe ali ndi adrenal kapena pituitary insufflication kapena kuledzera amakhala osamala kwambiri ndi zotsatira za hypoglycemic. Mwa okalamba ndi odwala omwe amatenga beta-blockers, kuzindikira kwa hypoglycemia kumatha kukhala kovuta.

Thercomitant chithandizo chokhudza impso kapena kugawa kwa metformin

Chenjezo limalangizidwa kugwiritsa ntchito mankhwala olumikizana (monga mankhwala a cationic omwe amathandizidwa ndi secretion mu renal tubules), omwe angayambitse ntchito ya impso, amabweretsa kusintha kwakukulu kwa hemodynamic kapena kusokoneza kugawa kwa metformin (onani gawo "Kuyanjana ndi mankhwala ena").

Radiological maphunziro ndi intravascular makonzedwe a ayodini osiyanitsa ena

Mukamachititsa maphunziro a radiology ndi intravascular management ya iodine okhala ndi mitundu yosiyanitsa, mapangidwe owopsa aimpso adadziwika, omwe amatha kukhala limodzi ndi chitukuko cha lactic acidosis odwala omwe amalandila metformin. Odwala omwe akupangidwira phunziroli ayenera kuletsa chithandizo cha Combogliz Prolong® mkati mwa maola 48 asanachite izi, kukana kumwa mankhwalawa patatha maola 48 pambuyo pa njirayi, ndikuyambiranso chithandizo pokhapokha atatsimikizira kuti imagwira ntchito impso.

Mikhalidwe ya Hypoxic

Mtima kugwa (mantha) kwa komwe kunachokera, kugundika kwa mtima, pachimake infarction ndi zina zokhala ndi hypoxia ndi lactic acidosis kungayambitse azotemia prerenal. Ndi chitukuko cha zinthu zoterezi, ndikofunikira kusiya yomweyo mankhwala ndi Combogliz Prolong®.

Kusintha kwa shuga wamagazi

Thupi, zoopsa, matenda, opaleshoni imatha kusintha kusintha kwa magazi m'magazi, omwe kale adatha kuwongolera mothandizidwa ndi mankhwala a Combogliz Prolong®. Muzochitika izi, kuchoka kwakanthawi kwa chithandizo komanso kusamutsa wodwala kupita ku insulin chithandizo kungafunike. Pambuyo kukhazikika kwa kuchuluka kwa shuga m'magazi ndikusintha momwe wodwalayo alili, chithandizo ndi Combogliz Prolong® chitha kuyambiranso.

Hypersensitivity zimachitika

Mukatsatsa malonda ogwiritsa ntchito saxagliptin, zochitika zazikulu za hypersensitivity zimadziwika, kuphatikizapo anaphylaxis ndi angioedema. Ngati vuto lalikulu la hypersensitivity likuchitika, muyenera kusiya kugwiritsa ntchito mankhwalawa, kuwunika zina zomwe zingayambitse zomwe zimachitika, ndikupatseni njira zina zothandizira odwala matenda a shuga (onani zigawo za "Contraindication" ndi "Zotsatira Zowopsa").

Pancreatitis

Pogwiritsa ntchito saxagliptin atangogulitsa, zalandiridwa mwadzidzidzi za milandu yamatenda owononga pancreatitis. Odwala omwe akutenga Combogliz Prolong® ayenera kudziwitsidwa za zomwe zimayambitsa kupweteka kwa kapamba: kupweteka kwakali, m'mimba kwambiri. Ngati mukukayikira kukula kwa kapamba, muyenera kusiya kumwa Combogliz Prolong® (onani magawo "Mosamala" ndi "Zotsatira zoyipa").
Mlingo wa kapamba mu kafukufuku wa SAVOR, wotsimikiziridwa malinga ndi ndondomeko ya kafukufukuyu, anali 0,3% m'magulu a saxagliptin ndi placebo pagulu la odwala onse osakhazikika.

Odwala okalamba

Mwa odwala 16492 omwe adasinthidwa mwapadera mu kafukufuku wa SAVOR, odwala 8561 (51.9%) anali ndi zaka 65 kapena kupitirira, ndipo odwala 2330 (14.1%) anali azaka 75 kapena kupitirira. Mwa awa, odwala 4290 azaka zapakati pa 65 ndi akulu ndi 1169 odwala wazaka 75 ndi akulu omwe adalandira saxagliptin. Malinga ndi kafukufuku wazachipatala, zothandiza komanso zodzitetezera mwa odwala azaka zapakati pa 65 ndi kupitirira, zaka 75 ndi akulu sizinasiyane ndi zofananira zomwezo mwa odwala omwe ali ndi zaka zochepa.

Kulephera kwa mtima

Kafukufuku wa SAVOR adawona kuwonjezeka kwa kugonekedwa kwa hospital hospital chifukwa cha kulephera kwa mtima mu gulu la saxagliptin poyerekeza ndi gulu la placebo, ngakhale kuti ubale wa causal sunakhazikitsidwe. Chenjezo liyenera kuchitika mukamagwiritsa ntchito Combogliz Prolong® kwa odwala omwe ali pachiwopsezo cha mtima kulephera, monga mbiri yolephera kwapakati kapena kupweteka kwambiri kwaimpso. Odwala ayenera kudziwitsidwa ndi zomwe zimachitika chifukwa cha kulephera kwa mtima komanso kufunika kofotokozera zizindikiro izi mwachangu (onani Pharmacodynamics, Clinical ufanisi ndi Chitetezo).

Arthralgia

Malipoti a malonda a pambuyo pofotokoza ululu wophatikizidwa, kuphatikiza ululu waukulu, mukamagwiritsa ntchito DPP-4 inhibitors. Odwala, mpumulo wa chizindikiro unawonedwa atasiya kumwa mankhwalawo, ndipo mwa wodwala payekhapayekha zizindikiro zimawonedwanso poyambanso kugwiritsa ntchito chimodzimodzi kapena inhibitor ina ya DPP-4. Kuyamba kwa zizindikiro mutayamba kugwiritsa ntchito mankhwalawa kumatha kufulumira kapena kudziwika motsutsana ndi maziko a chithandizo cha nthawi yayitali. Ndi kukula kwa ululu wolumikizika kwambiri, kuyenera kopitilira mankhwalawa m'thupi lililonse kuyenera kuyesedwa (onani gawo "Zotsatira zoyipa").

KUMVETSA KWAULERE KUTI MUZILIMBITSA ZINSINSI NDI NTCHITO NDI MIYANI

Kafukufuku wokhudzana ndi saxagliptin pakutha kuyendetsa magalimoto ndi kayendedwe ka kayendedwe sanachitike. Kumbukirani kuti saxagliptin ikhoza kupweteketsa mutu.

Mankhwala

Combogliz Prolong imaphatikiza ma othandizira awiri a hypoglycemic omwe amagwira ntchito yolumikizira mogwirizana kuti apititse patsogolo kulumikizana kwa glycemic kwa odwala omwe ali ndi matenda a 2 matenda a shuga (mtundu 2 matenda osokoneza bongo): saxagliptin, choletsa wa DPP-4 (dipeptidyl peptidase 4), ndi metformin, yomwe ili m'gulu khwawa.

Saxagliptin

Kuchokera m'matumbo ang'onoang'ono, poyankha kudya, mahomoni, ma protein, monga GLP-1 (glucagon-peptide-1) ndi HIP (glucose-insulinotropic polypeptide) amatulutsidwa m'magazi.

Hormones-incretins imalimbikitsa kutulutsidwa kwa insulin kuchokera ku cell ya beta ya kapamba, zomwe zimatengera kuchuluka kwa glucose m'magazi, koma amalephera kwa mphindi zingapo ndi enzyme DPP-4. Kuchita kwa GLP-1 ndikuyembekezeranso kuchepetsa kubisala kwa glucagon m'maselo a alpha a kapamba, omwe amachititsa kutsika kwa kupanga kwa chiwindi mu chiwindi. Kuzunza kwa GLP-1 kwa odwala omwe ali ndi matenda a shuga 2 kumachepa, koma kuyankha kwa insulin ku GLP-1 kumasungidwa. Saxagliptin, monga mpikisano wopikisana ndi DPP-4, amachepetsa mphamvu ya kuchuluka kwa ma impretin, potero amawonjezera kuchuluka kwawo m'magazi, ndipo amatsogolera kutsika kwa kuchuluka kwa glucose pamimba yopanda kanthu ndikatha kudya.

Metformin ndi mankhwala osokoneza bongo a hypoglycemic omwe amapititsa patsogolo kulekerera kwa glucose kwa odwala omwe ali ndi matenda amtundu wa 2 (pochepetsa kutsalira kwa shuga ndi postprandial glucose).

Kuchita bwino kwamankhwala a metformin kumachepetsa kupanga kwa chiwindi ndi chiwindi, kufooketsa mayamwidwe am'matumbo m'matumbo, ndikuwonjezera kuchepa kwa insulin (kuperewera kwa magazi ndi kugwiritsa ntchito shuga).

Metformin, mosiyana ndi kukonzekera kwa sulfonylurea, sikumayambitsa hyperinsulinemia ndi hypoglycemia mwa odwala omwe ali ndi matenda a shuga a 2 kapena anthu athanzi (kusiyapo ndi zochitika zina zapadera). Katulutsidwe ka insulin panthawi ya mankhwala a metformin sikusintha, ngakhale kuti pakhoza kukhala kuchepa kwa kuchuluka kwa insulin pamimba yopanda kanthu komanso poyankha chakudya masana.

MALO A ISSUE

Mapiritsi okwana 1000 osinthidwa

7 mapiritsi pachimake pa zotayidwa zojambulazo, matuza 4 kapena 8 okhala ndi malangizo

gwiritsani ntchito katoni yoyang'anira makatoni oyamba.

500 mg + 5 mg mapiritsi okhala ndi mafilimu
7 mapiritsi pachimake pa zotayidwa zojambulazo, matuza 4 okhala ndi malangizo ogwiritsidwira ntchito pabokosi lamakatoni poyang'anira kutsegula koyamba.

1000 mg + 5 mg mapiritsi okhala ndi mafilimu
7 mapiritsi pachimake pa zotayidwa zojambulazo, matuza 4 okhala ndi malangizo ogwiritsidwira ntchito pabokosi lamakatoni poyang'anira kutsegula koyamba.

Kutentha kopitilira 30 ° C. Pewani kufikira ana.

WOPHUNZITSA, WODZICHEKA (WOPHUNZITSIRA WOPHUNZITSIRA), PACKER (Wachiwiri (WOTSITIRA) KUPANGITSA), KUPANGITSA ZINTHAZO ZABWINO

AstraZeneca Pharmaceuticals LP, USA
4601 Highway 62 East, Mount Vernon, Indiana, 47620, USA
AstraZeneca Pharmaceuticals LP, USA
4601 Highway 62 East, Mount Vernon, Indiana, 47620, USA

Dzina, adilesi ya bungwe lovomerezedwa ndi yemwe ali ndi mwiniwake kapena mwiniwake wa satifiketi yolembetsera mankhwala kuti agwiritse ntchito kuchipatala kuvomera zomwe ogula akufuna:

Chiyimidwe cha AstraZeneca UK Limited, UK, ku Moscow ndi AstraZeneca Pharmaceuticals LLC
125284 Moscow, st. Kuthamanga, 3, p. 1.

Pharmacological mawonekedwe a mankhwalawa

Combogliz Prolong ndi kuphatikizika kwa saxagliptin ndi metformin, kupatsa madokotala ndi anthu odwala matenda ashuga mwayi watsopano wowongolera mbiri yawo ya glycemic.

Kutalika kwa Combogliz: malangizo ogwiritsira ntchito

Dokotala amasankha dongosolo la kayendetsedwe ndi kumwa payekhapayekha payekha, poganizira zomwe zimayimira glucometer, thanzi labwino, msinkhu wa odwala matenda ashuga, momwe munthu angamve pamapiritsi. Mwambiri, malangizowa amapereka malingaliro amenewo.

Mankhwala okhazikika nthawi zambiri amatengedwa 1 r / tsiku. nthawi yomweyo.

Imwani piritsi m'mawa kapena madzulo, osakupera. Kwa mitundu yosinthika yosinthidwa, kukhulupirika kwa zigoba kumatenga gawo lalikulu.

Mlingo wake ndiwofanana, ngati kuyambira kungakhale piritsi limodzi (500 mg ya metformin + 2,5 mg wa saxagliptin), ngati chiwongolero chonse cha glycemic sichingatheke, mlingo umakulitsidwa mapiritsi 2 (1000 mg ya metformin + 5 mg ya saxagliptin).

Ndi munthawi yomweyo kugwiritsa ntchito mankhwala pochiza matenda ophatikizika, zotsatira za kuyanjana kwawo ziyenera kukumbukiridwa. Makamaka, ndi munthawi yomweyo makonda a zoletsa za CYP3A4 / 5 isoenzymes (Indinavir, Ketoconazole, Nefazodon, Itraconazole, Atazanavir), osachepera mlingo wa saxagliptin ndi mankhwala - 2.5 mg.

Mankhwala motengera metformin yokhala ndi zotsatira zazitali zosakhudzana ndi zovuta zam'mimba ndizochepa kwambiri poyerekezera ndi kutulutsidwa mwachangu. Momwe thupi limasinthira kwatsopano, sizopweteka m'mimba Mlingo titration zizichitika pang'onopang'ono, milungu iwiri iliyonse.

Kusintha kwina kulikonse kwamikhalidwe kuyenera kukumbukiridwa mukakonza momwe mankhwalawo amathandizira, motero ndikofunikira kudziwitsa adokotala za iwo munthawi yake.

Analogs Kombiglyce Prolong

Kwa Combogliz Prolong, analogue yokhala ndi zosakaniza zomwezo zingakhale Comboglis XR, yomwe imapangidwa ku Italy ndi UK. Mtengo wa analogue umachokera ku 1650 rubles. (Mapiritsi 28 a 1000 mg a metformin ndi 2,5 mg wa saxagliptin).

Zotsatira zowonjezera zachipatala za Avandamet, Yanumet, Glimecomb, GalvusMet ndi Bagomet kuphatikiza ndizochiritsanso.

Lembani mankhwala potengera gawo limodzi logwira ntchito monga Glyformin Prolong, Glucofage, Metadiene, Sofamet, Diaformin Od, Ongliza, Matospanin, Metfogamma, Siofora.

Ndani akuwonetsedwa mankhwalawo

Kutalika kwa Combogliz ndikolembedwera mtundu wa matenda ashuga a 2 kuti achepetse kuwongolera kwa glycemic monga chowonjezera pa chakudya chochepa cha carb ndi zochitika zolimbitsa thupi zokwanira, ngati kusintha kwamachitidwe sikupereka zotsatira zomwe mukufuna komanso kuphatikizidwa kwa saxagliptin ndi metformin ndikoyenera kwa wodwalayo.

Mtheradi ndi zotsutsana pachibale

Ngakhale mankhwala omwe ali ndi chitetezo chambiri, chomwe ndi Combogliz Prolong, sinafotokozeredwe kuti munthu azitsutsa komanso asakanikirane ndi zosakaniza za formula.

1. Mankhwalawa sawonetsedwa kwa amayi apakati komanso oyembekezera (amasunthidwa kwakanthawi kwa insulin), chifukwa chosowa umboni wokwanira chifukwa chogwira ntchito, samaperekedwa kwa ana.
2. Mankhwalawa sioyenera odwala matenda ashuga omwe ali ndi mtundu woyamba wa matenda.
3. Pochita kuwonongeka kwa impso, komanso mikhalidwe yomwe imawakwiyitsa, mankhwalawa sanatumizidwenso.
4. Osagwiritsa ntchito mankhwalawa kuchiza odwala omwe ali ndi matenda omwe amachititsa kufa ndi mpweya wa minofu ya minyewa.
5. Ndi ketoacidosis (mawonekedwe a matenda ashuga) okhala ndi chikomokere kapena chosatha, mankhwalawa samatengedwa kwakanthawi.
6. Mapiritsi amathetsedwa panthawi yochita, ndikuvulala kwambiri, kupsa kwambiri. Kuyesedwa kwa X-ray yokhala ndi zikwangwani zokhala ndi ayodini mu diabetes kungawononge impso, motero kumasinthidwanso kukhala insulin. Pazonse, chithandizo cha insulin chimawonetsedwa kwa maola 48 asanafike komanso maola 48 pambuyo pa njirazi, makamaka, zonse zimatengera momwe impso ili komanso thanzi la wodwalayo.
7. Ma pathologies a chiwindi, lactic acidosis ndi kudalira mowa amakhalanso pamndandanda wa contraindication. Simungathe kupereka mankhwalawa kwa odwala omwe ali ndi ma genetic galactose tsankho.

Chidwi chachikulu chiyenera kuperekedwa kwa odwala matenda ashuga okalamba, makamaka kuperewera kwa chakudya, kapamba ndi masewera olimbitsa thupi omwe angayambitse hypoglycemia.

Zotheka zosafunikira komanso mankhwala osokoneza bongo ambiri

Saxagliptin yokhala ndi magawo osiyanasiyana amomwe amatha kupangitsa zinthu:

• Sinusitis
• Gastroenteritis
• Kutupa kumaso,
• Pancreatitis
• Urticaria.

Kafukufuku wa Laborator awonetsa kuchepa kwa mayamwidwe a Vitamini B12 ndikugwiritsa ntchito mankhwalawa kwa nthawi yayitali, komanso kuchepa kwa kuchuluka kwa ma lymphocyte. Milandu yamankhwala osokoneza bongo ndi osakwatira, nthawi zambiri amapezeka ndi kugwiritsa ntchito nthawi yayitali saxagliptin. Mankhwalawa sayambitsa kuledzera, ndi kuchuluka kwa mankhwalawa, hemodialysis imagwira. Mofananamo, chithandizo chamankhwala chimachitika.

Mankhwala osokoneza bongo a metformin ndi ochulukirapo, oopsa kwambiri ndi lactic acidosis.. Mutha kuzindikira momwe mulili ndi izi:

1. Kutha
2. Kupuma pang'ono
3. Kupweteka kwam'mimba
4. Kuthamanga kwa magazi
5. Hypothermia,
6. Minofu kukokana
7. Kusokonezeka kwa mtima.

Panthawi yovuta, kusokonezeka kwa chikumbumtima, kukomoka, kukhazikika mtima komanso kukhazikika. Wovutikayo amafunikira kuchipatala mwachangu, popanda chithandizo chokwanira, amatha kumwalira. Metformin yowonjezera imachotsedwanso ndi hemodialysis, ndikofunikira kulingalira kuti clearinine chilolezo chimafikira 170 ml / min.

Munthu wodwala matenda ashuga akamakwaniritsa malingaliro onse a dokotala, amachepetsa chiopsezo chovuta kwambiri. Pankhani ya Combogliz yotalikilapo, sikovuta kutsatira dongosolo la mankhwalawa.

Zosankha zothandizira kucheza ndi mankhwala ena

Mukamapangira njira ya mankhwala a Combogliz Prolong, ndikofunikira kuchenjeza endocrinologist za mankhwala onse omwe munthu wodwala matenda ashuga amatenga pofuna kuchiza matenda oyanjana. Ena mwa iwo amatha kupititsa patsogolo mphamvu zotsitsa shuga za Comboglize, ena akuletsa ntchito zake.

Kuti mudziwe zambiri, mutha kuyang'ana patebulo.

Kupititsa patsogolo kwa Hyperglycemic

Rifampicin, Pioglitazone, Magnesium ndi Aluminium Hydroxides / SimethiconeGCS, diuretics, nicotinic acid

mahomoni a chithokomiro, isoniazid, sympathomimetics, phenothiazines, estrogens, phenytoin, calcium blockers

Perekani zochitika za hypoglycemic

Amprenavir, Diltiazem, Erythromycin, Fluconazole, Aprepitant, Verapamil, madzi a mphesa, Ketoconazole, mankhwala a sulfonylurea, Glibenclamide, Ketoconazole, CYP3A 4/5 isoenzymes, FamotidineMankhwala a Cationic, Furosemide, mankhwala opangidwa ndi ethanol, Nifedipine

Amprenavir, Diltiazem, Erythromycin, Fluconazole, Aprepitant, Verapamil, madzi a mphesa, Ketoconazole, mankhwala a sulfonylurea, Glibenclamide, Ketoconazole, CYP3A 4/5 isoenzymes, Famotidine
Mankhwala a Cationic, Furosemide, mankhwala opangidwa ndi ethanol, Nifedipine

Ndizachidziwikire kuti kuyesa kudzifufuza komanso kudzipatsa mankhwala ndi Combogliz Prolong kumatha kukhala ndi zotsatirapo zoyipa m'moyo.

Kutalika kwa Combogliz: ndemanga za anthu odwala matenda ashuga

Madokotala omwe amawunika momwe mankhwalawo amathandizira ndi mankhwala a Combogliz Pronge amawona kuti ndi osiyana, ndipo odwala matenda ashuga nawonso amakayikira momwe angathere.

Kuwongolera kwathunthu matenda a shuga kumafuna njira yolumikizira: zakudya zamafuta ochepa, kuwunika tsiku ndi tsiku kuwerenga kwa glucometer, kuchita masewera olimbitsa thupi mokwanira ndi thandizo la mankhwala. Kuphatikiza uku kokha komwe titha kuwerengera za 100% zotsatira za Combogliz Prolong.

Mu kanemayo, pulofesa-endocrinologist A.S. Ametov amalankhula za mfundo zamakono zoyendetsera matenda a shuga a 2.

Pharmacokinetics

Bioequivalence ndi momwe chakudya chimaphatikizira ndi zinthu zomwe zimapangidwa ndi Comboglize Prolong zimadziwika ndi odwala potsatira zakudya zamafuta ochepa, zomwe zimapatsa 324 kcal ndi kapangidwe kazakudya ndipo zili ndi mapuloteni - 11.1%, mafuta - 10,5%, chakudya - 78.4%. Pansi pa izi zakudya zopatsa thanzi, m'maphunziro athanzi, malinga ndi zotsatira za kafukufuku, kufufuza kwa mapangidwe a pharmacokinetics osakanikirana a metformin + saxagliptin m'mapiritsi ndi mapiritsi a payekha osinthika a saxagliptin ndi metformin mu Mlingo wofanana.

Zochitika zapadera zamankhwala

Kugwiritsa ntchito Combogliz Prolong yokhala ndi kulephera kwa impso ndikusokoneza chiwindi sikulimbikitsidwa.

Odwala a zaka zapakati pa 65-80, palibe kusiyana kwakukulu m'mafakisoni a saxagliptin omwe amapezeka poyerekeza ndi odwala aang'ono (azaka za 18 mpaka 40), motero, kusintha kwa mlingo kwa odwala okalamba sikofunikira. Komabe, ziyenera kukumbukiridwa kuti m'gulu ili la odwala, kuchepa kwa impso ndizotheka kwambiri. M'badwo uliwonse, sikofunikira kupereka Combogliz Kutalika mpaka ntchito yachilengedwe yotsimikizika.

Odwala a zaka zopitilira 80 amalephera kumwa mankhwalawa, pokhapokha ngati abwinobwino aimpso amatsimikiziridwa ndi muyeso wa creatinine chilolezo.

Kafukufuku wa pharmacokinetics wa yogwira zinthu Comboglize Prolong mu ana sanachitike.

Zotsatira zoyipa za saxagliptin zolembedwa mu kafukufuku wa SAVOR

Chiwerengero cha odwala omwe adayamba kudwala kwambiri hypoglycemia panthawi ya chithandizo (hypoglycemia, chomwe chimafuna kuti athandizidwe ndi ena) anali okwera m'gulu la saxagliptin poyerekeza ndi gulu la placebo.

Chiwopsezo chowonjezeka cha kukhala ndi hypoglycemia ambiri, komanso hypoglycemia yayikulu pagulu la saxagliptin, amawonedwa kwambiri mwa odwala omwe amalandila sulfonylurea, koma osati mwa odwala omwe alandila metformin kapena insulin ngati chithandizo chachikulu.

Pazonse, chiopsezo chowonjezereka cha hypoglycemia, komanso hypoglycemia yayikulu, imadziwika kwambiri kwa odwala omwe ali ndi basana glycated hemoglobin (HbAlc) wochepera 7%.

Ntchito yotsatsa

Pa kuwunika pambuyo pakutsatsa, chitukuko cha zotsatirazi zotsatirapo zinajambulidwa: pancreatitis pachimake, hypersensitivity reaction (kuphatikizapo anaphylaxis, angioedema, zidzolo ndi urticaria) ndi arthralgia. Ndizosadalirika kuwunika kufalikira kwa izi.

Pogwiritsa ntchito saxagliptin, kuchepa kwapakati pamankhwala omwe amadziwika ndi kuchuluka kwa mankhwalawa amadziwika.Nthawi zambiri, kugwiritsa ntchito saxagliptin mobwerezabwereza, palibe kubwereza komwe kunawonedwa, ngakhale mwa odwala ena kuchuluka kwa ma lymphocyte kunachepa pambuyo poyambiranso mankhwala ndi saxagliptin, komwe kunayambitsa kusiya mankhwala. Kutsika kwa kuchuluka kwa ma lymphocyte sikumayendetsedwa ndi chiwonetsero chazachipatala. Zomwe zimayambitsa kuphwanya izi sizikudziwika. Pakakhala matenda atatenga nthawi yayitali kapena osazolowereka, chiwerengero cha ma lymphocyte chiyenera kuyesedwa. Mavuto a saxagliptin pa kuchuluka kwa ma lymphocyte odwala omwe ali ndi vuto lambiri chifukwa cha kuchuluka kwawo (kuphatikizapo kachilombo ka anti immunodeficiency virus) sikudziwika.

M'maphunziro azachipatala a metformin, pafupifupi 7% ya odwala adawonetsa kuchepa kwa seramu ya vitamini B₁₂ (kale zinali zabwinobwino) kumalingaliro achilendo omwe samatsatiridwa ndi chiwonetsero chachipatala. Komanso, kuchepa kotereku kwa magazi m'thupi kumayendera limodzi ndi kawirikawiri, atatha kuchotsa metformin kapena kuchuluka kwa vitamini B₁₂ anachira msanga.

Mu vuto laimpso

Zotsatira za Combogliz Kutalika kwa mbali ya ntchito impso:

• kuvulala kwa impso (serum creatinine: amuna ≥ 1.5 mg / dl, akazi ,
• matenda pachimake, pomwe pali chiopsezo cha mkhutu aimpso ntchito.