Comboglizzen, pezani, gulani

Dzina la malonda akukonzekera: Kutalika kwa Komboglize

Dongosolo losavomerezeka: Metformin (metformin) + Saxagliptin (saxagliptin)

Fomu ya Mlingo: Mapiritsi okhala ndi mafilimu

Chithandizo: Metformin hydrochloride + saxagliptin

Gulu la Pharmacotherapeutic: Hypoglycemic wothandizila kukonzekera pakamwa (dipeptidyl peptidase 4 inhibitor + biguanide).

Katundu

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 (DM2): saxagliptin, dipeptidyl 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 ma cell a pancreatic beta, zomwe zimatengera kuchuluka kwa glucose m'magazi, koma samapangidwa ndi enzyme ya DPP-4 kwa mphindi zingapo. GLP-1 imachepetsa kubisalira kwa glucagon m'maselo a alpha, ndikuchepetsa kupanga kwa 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 mayamwidwe 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.

Zisonyezero zogwiritsidwa ntchito:

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

Zoyipa:

- Kuchulukitsa chidwi kwa munthu aliyense pazinthu zilizonse za mankhwala,

- Zotsatira zazikulu za hypersensitivity (anaphylaxis kapena angioedema) kwa DPP-4 zoletsa,

- Type 1 matenda a shuga (musawerenge)

- Gwiritsani ntchito molumikizana ndi insulin (simunaphunzire),

- Congenital galactose tsankho, lactase akusowa ndi shuga-galactose malabsorption,

- Zaka mpaka 18 (chitetezo ndi kusachita bwino sizinaphunzire),

- Kulephera kwamkati (serum creatinine ≥1.5 mg / dl kwa amuna, ≥1.4 mg / dl kwa akazi kapena kuchepetsedwa chilolezo cha creatinine), kuphatikizapo zomwe zimayambitsidwa ndi kuperewera kwa mtima ndi mantha (mantha), 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, matenda a bronchopulmonary),

- pachimake kapena matenda metabolic acidosis, kuphatikizapo matenda ashuga a ketoacidosis, okhala ndi chikomokere kapena opanda kukomoka,

- Matenda akuwonetsa za matenda owopsa komanso osachiritsika omwe angayambitse kukula kwa minofu hypoxia (kupuma kulephera, mtima kulephera, kulowetsedwa kwapanjira),

- Opaleshoni yayikulu ndi kuvulala (pamene chithandizo cha insulin chikusonyezedwa),

- chiwindi ntchito,

- Chakumwa choledzeretsa komanso poyizoni wa ethanol,

- Lactic acidosis (kuphatikizapo mbiri),

- Nthawi yosachepera maola 48 isanachitike komanso mkati mwa maola 48 mutachita maphunziro a radioisotope kapena x-ray ndikuyambitsa ntchito zotsutsana ndi ayodini.

- Kuthana ndi chakudya cha hypocaloric (5% ya odwala omwe adalandira metformin yotulutsidwa ndikumapangidwa pafupipafupi kuposa momwe gulu la placebo lidadwala matenda am'mimba komanso kusanza / kusanza.

Zotsatira zotsatirazi zidanenedwera pakutsatsa kugwiritsidwa ntchito kwa saxagliptin: pachimake pancreatitis ndi hypersensitivity reaction, kuphatikizapo anaphylaxis, angioedema, zidzolo ndi urticaria. Ndizosatheka kuwerengera pafupipafupi kukula kwa zinthuzi, popeza mauthenga adalandiridwa mosawerengeka kuchokera kwa anthu osadziwika (onani zigawo "Contraindication" ndi "Maupangiri Apadera").

Chiwerengero chonse cha ma lymphocyte

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 othandizira saxagliptin pa mlingo wa 2,5 mg, pa 5 mg. , pa mlingo wa 10 mg ndi placebo, motero. Odwala ambiri omwe amagwiritsidwa ntchito mobwerezabwereza saxagliptin, palibe kubwereza komwe kunawoneka, ngakhale kuti 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 chiwonetsero chazachipatala.

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 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 adakumana ndi kuchepa kwa kuchuluka kwa seramu isanachitike kuchuluka kwa vitamini B12 ku miyezo yapamwamba yopanda mawonekedwe. Komabe, kuchepa kotereku sikumachitika kawirikawiri limodzi ndi kukula kwa kuchepa kwa magazi ndipo kumachira msanga pambuyo pakuchotsedwa kwa metformin kapena kudya vitamini B12 kochulukirapo.

Bongo

Ndi kugwiritsa ntchito mankhwalawa kwa nthawi yayitali mpaka 80 peresenti kuposa momwe analimbikitsira, 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 imachotsedwedwa pa dialysis, pomwe chilolezo chikufika pa 170 ml / min.

Tsiku lotha ntchito: Zaka zitatu

Zoyenera kufalitsa kuchokera kuma fakitoli: Ndi mankhwala.

Wopanga: Bristol Myers squibb, USA