Linagliptin ndi wothandizira pakamwa wa hypoglycemic yemwe amatha kuletsa enzyme dipeptidylpetitase-4. Enzyme iyi imathandizira nawo pakuyambitsa mahomoni a incretin.
Ma mahomoni oterewa m'thupi la munthu ndi glucapeptide-1 ndi insulinotropic polypeptide. Izi zophatikiza zama bioactive zimawonongeka mwachangu ndi enzyme.
Mitundu yonse iwiri ya maretretin imatsimikizira kukhazikika kwa njira zomwe zimayang'anira gawo lama glucose pamlingo womwe umatsimikizira magwiridwe antchito a thupi lonse.
The kapangidwe ndi Mlingo mawonekedwe
Mankhwala odziwika kwambiri omwe ali ndi linagliptin ndi mankhwala a dzina lomweli.
The zikuchokera mankhwala zikuphatikizira waukulu yogwira thunthu - linagliptin. Mlingo umodzi wa mankhwalawa uli ndi 5 mg yogwira ntchito.
Kuphatikiza pa chophatikizira chachikulu, mankhwalawa ali ndi zowonjezera zina.
Zothandiza pazinthu zomwe zimapangidwa ndi mankhwalawa ndi motere:
- Mannitolum.
- Wowuma pregelatinized.
- Wowuma chimanga.
- Colovidone.
- Magnesium wakuba.
Mankhwalawa ndi piritsi yolumikizidwa ndi filimu yofunikira.
Zomwe amapanga penti yapadera ya piritsi lililonse imaphatikizanso izi:
- Opadra pinki;
- hypromellose;
- titanium dioxide;
- talc;
- macrogol 6000;
- oxide wachitsulo ndi wofiyira.
Mankhwala amapezeka mu mawonekedwe a mapiritsi okhala ndi mawonekedwe ozungulira. Mapiritsi adalowetsa m'mbali komanso filimu. Chipolopolo cha phale ndichopepuka. Chipolopolocho chimalembedwa ndi chizindikiro cha kampani yopanga BI pamalo amodzi ndi D5 mbali inayo.
Mapiritsi amapezeka m'matumba a masamba a zidutswa 10 chilichonse. Mabulogu amadzaza katoni. Phukusi lililonse lili ndi matuza atatu. Onetsetsani kuti muphatikiza malangizo ogwiritsira ntchito mankhwalawa piritsi lililonse la mankhwalawa.
Kusungidwa kwa mankhwalawa kuyenera kuchitika m'malo amdima osachepera 25 digiri Celsius.
Malo osungira mankhwalawa sayenera kupezeka kwa ana. Alumali moyo wa mankhwala ndi zaka 3.
Pharmacodynamics ndi pharmacokinetics a mankhwala
Pambuyo pakukonzekera kwa pakamwa kwa thupi, Linagliptin amamangiriza kugwira dipeptidyl peptidase-4.
Chomangira chovuta chomwe chimapangidwanso chimatha kusintha. Kulumikizana kwa enzyme ndi linagliptin kumabweretsa kuwonjezeka kwa kuchuluka kwa ma insretin m'thupi ndipo kumathandizira kuti azichita ntchito yawo kwakanthawi.
Zotsatira za mankhwalawa ndi kuchepa kwa kupanga kwa glucagon ndikuwonjezereka kwa insulin, ndipo izi zimatsimikizira kuchuluka kwa shuga mthupi la munthu.
Mukamagwiritsa ntchito Linagliptin, kuchepa kwa glucose hemoglobin komanso kuchepa kwa glucose m'madzi a m'magazi kunakhazikitsidwa molondola.
Mutatha kumwa mankhwalawa, imamwidwa mwachangu. Pazipita ndende ya mankhwalawa m'madzi a m'magazi amatheka 1.5 mawola.
Kutsika kwa zomwe linagliptin kumachitika pamagawo awiri. Kutha kwa theka la moyo ndikutalika ndipo kuli pafupifupi maola 100. Izi ndichifukwa choti mankhwalawa amapanga zovuta kukhazikika ndi enzyme DPP-4. Chifukwa chakuti kulumikizana ndi enzyme ndikusintha kwadzakenso kwa mankhwala mthupi sikumachitika.
Pankhani yogwiritsira ntchito Linagliptin pakakhala kuchuluka kwa 5 mg patsiku, nthawi imodzi yokhazikika yokhazikika yogwira mankhwala imatheka m'thupi la wodwalayo mutatenga 3 Mlingo wa mankhwalawa.
Mtheradi bioavailability wa mankhwala pafupifupi 30%. Ngati linagliptin imatengedwa nthawi yomweyo monga chakudya chamafuta, ndiye kuti chakudya chotere sichikhudza mayamwidwe anu.
Kuchotsa mankhwala m'thupi kumachitika makamaka m'matumbo. Pafupifupi 5% imachotseredwa kudzera mu imkodzo ndi impso.
Zizindikiro ndi contraindication kugwiritsa ntchito mankhwalawa
Chizindikiro pakugwiritsa ntchito linagliptin ndiko kupezeka kwa mtundu II wa shuga wodwala.
Pa monotherapy, linagliptin imagwiritsidwa ntchito kwa odwala omwe sangathe kuwongolera kuchuluka kwa glycemia mthupi mothandizidwa ndi zakudya komanso zolimbitsa thupi.
Kugwiritsa ntchito mankhwalawa kumalimbikitsidwa ngati wodwala wachita tsankho kapena ngati pali zotsutsana pakugwiritsa ntchito metformin chifukwa cha kulephera kwa aimpso kwa wodwala.
Mankhwala tikulimbikitsidwa othandizira awiri othandizira kuphatikiza ndi metformin, sulfonylurea zotumphukira kapena thiazolidinedione, pochitika kuti kugwiritsa ntchito mankhwala othandizira pakudya, masewera olimbitsa thupi ndi monotherapy ndi mankhwala omwe akuwonetsedwa akupezeka kuti ndi osathandiza.
Ndizomveka kugwiritsa ntchito Linagliptin monga gawo limodzi la zinthu zitatu zomwe zingapangidwe ngati chakudya, masewera olimbitsa thupi, chithandizo cha monotherapy kapena ziwiri zokha sizinapatse zotsatira zabwino.
N`zotheka kugwiritsa ntchito mankhwalawa limodzi ndi insulin, pochita zinthu zambiri zamankhwala othandizira odwala matenda ashuga, chifukwa zosagwiritsa ntchito mankhwalawa olimbitsa thupi komanso njira zopewera insulin yopanda mankhwala
Milandu yayikulu yomwe imagwiritsidwa ntchito popanga mankhwala ndi:
- kupezeka kwa thupi la wodwala matenda a shuga 1;
- chitukuko cha matenda ashuga ketoacidosis;
- nthawi ya pakati ndi mkaka wa m`mawere;
- zaka zodwala zimakhala zosakwana 18;
- kukhalapo kwa hypersensitivity kuti achite pa zinthu zilizonse za mankhwala.
Linagliptin ali oletsedwa kugwiritsa ntchito panthawi ya kukomoka ndi mkaka wa mkaka. Izi ndichifukwa choti chinthu chomwe chikugwirira ntchito, chikalowa m'magazi a wodwalayo, chimatha kudutsana ndi zotchinga, komanso amatha kulowa mkaka wa m'mawere nthawi ya mkaka wa m'mawere.
Ngati kuli kofunikira kugwiritsa ntchito mankhwalawa panthawi yoyamwa, kuyamwitsa kuyenera kuyimitsidwa nthawi yomweyo.
Malangizo ogwiritsira ntchito mankhwalawa
Malangizo ogwiritsira ntchito mankhwalawa akuwonetsa kuti Linagliptin amagwiritsidwa ntchito pochiza mtundu wa 2 shuga mellitus mu mlingo wa 5 mg kamodzi patsiku, ndiye piritsi limodzi. Mankhwala amatengedwa pakamwa.
Ngati mukusowa nthawi yomwe mumamwa mankhwalawa, muyenera kumwa nthawi yomweyo wodwala akakumbukira izi. Mlingo wawiri wa mankhwalawo waletsedwa.
Mukamamwa mankhwalawa, kutengera umunthu wake, zotsatira zoyipa zimachitika.
Zotsatira zoyipa zomwe zimachitika mthupi la wodwalayo zimakhudza:
- Chitetezo cha mthupi.
- Ziwalo zopumira.
- Matumbo a m'mimba.
Kuphatikiza apo, ndizotheka kukulitsa matenda opatsirana mthupi, monga nasopharyngitis.
Pogwiritsa ntchito Linagliptin kuphatikiza ndi Metformin, zotsatirazi zingachitike:
- mawonekedwe a hypersensitivity;
- kupezeka kwa chifuwa;
- chitukuko cha kapamba
- mawonekedwe a matenda opatsirana.
Pankhani yogwiritsa ntchito mankhwalawa limodzi ndi sulfonylureas yaposachedwa, ndizotheka kuti thupi likhale ndi zovuta zokhudzana ndi kugwira ntchito:
- Chitetezo cha mthupi.
- Njira zachikhalidwe.
- Njira yothandizira.
- Ziwalo zam'mimba.
Pankhani yogwiritsira ntchito Linagptin kuphatikiza ndi Pioglipazone, chitukuko cha zovuta zotsatirazi tingaone:
- mawonekedwe a hypersensitivity;
- Hyperlipidemia mu shuga;
- kupezeka kwa chifuwa;
- kapamba
- matenda opatsirana;
- kunenepa.
Pogwiritsa ntchito Linagliptin kuphatikiza ndi insulin panthawi yamankhwala, zotsatirazi zimabweretsa thupi la wodwalayo:
- Kukula kwa hypersensitivity m'thupi.
- Maonekedwe akutsokomola komanso kusokonezeka kwa njira yopumira.
- Kuchokera mu chakudya chamagaya, mawonekedwe a kapamba ndi kudzimbidwa ndikotheka.
- Matenda opatsirana amatha kuchitika.
Pankhani yogwiritsidwa ntchito kwa Linagliptin wa mtundu wachiwiri wowongolera matenda a shuga kuphatikiza ndi Metformin ndi zotumphukira zochokera mu mtima, Hypersensitivity, hypoglycemia, mawonekedwe a chifuwa, kuwoneka kwa zizindikiro za kapamba ndi kuwonjezeka kwa thupi.
Kuphatikiza pazotsatira zoyipa izi, mawonekedwe ndi chitukuko cha angioedema, urticaria, kapamba kapamba, zotupa pakhungu m'thupi la wodwalayo ndizotheka.
Ngati mankhwala osokoneza bongo agwiritsidwa ntchito, njira zomwe zimagwiritsidwa ntchito pokonzera thupi ziyenera kugwiritsidwa ntchito.
Njira zoterezi ndikuchotsa mankhwalawa m'thupi ndi mankhwala othandizira.
Kugwirizana kwa linagliptin ndi mankhwala ena
Ndi makonzedwe a Metformin 850 omwe ali ndi Linagliptin, kuchepa kwakukulu kwamlingo wa shuga m'thupi la wodwalayo kumachitika.
Ma pharmacokinetics a mankhwalawa akagwiritsidwa ntchito limodzi ndi zotumphukira za m'badwo waposachedwa sizinasinthe kwenikweni.
Mukamagwiritsa ntchito mankhwala othandizira a thiazolidinediones, palibe kusintha kwakukulu kwa pharmacokinetics. Izi zikusonyeza kuti linagliptin si choletsa CYP2C8.
Kugwiritsidwa ntchito kwa ritonavir mu zovuta kuchipatala sikuti kumabweretsa kusintha kwakukulu mu pharmacodynamics ndi pharmacokinetics of linagliptin.
Kugwiritsa ntchito Linagliptin mobwerezabwereza ndi Rifampicin kumapangitsa kuchepa pang'ono kwa ntchito ya mankhwala
Linagliptin amatsutsana pa matenda a matenda a shuga 1 kapena matenda a shuga a ketoacidosis.
Pafupipafupi kukula kwa chikhalidwe cha hypoglycemia m'thupi la wodwalayo panthawi ya monotherapy kumakhala kochepa.
Kuchepa kwa hyperglycemia kumawonjezereka ngati Linagliptin amagwiritsidwa ntchito molumikizana ndi mankhwala omwe amachokera ku sulfonylureas a m'badwo waposachedwa. Pachifukwa ichi, chisamaliro chapadera chimayenera kutengedwa ndi chithandizo chovuta.
Ngati ndi kotheka, mlingo wa mankhwalawa womwe umayenera kutengedwa uyenera kusinthidwa kuti mupewe kukula kwa zizindikiro za hypoglycemia.
Kugwiritsidwa ntchito kwa linagliptin sikukhudzana ndi zovuta mu ntchito ya mtima.
Linagliptin angagwiritsidwe ntchito pochiza matenda a shuga kwa odwala omwe amalephera kwambiri aimpso.
Pogwiritsa ntchito Linagliptin, kuchepa kwakukulu pazomwe zili ndi glycosylated hemoglobin ndi glucose kudya.
Ngati akukayikira kukula kwa kapamba m'thupi, kugwiritsa ntchito mankhwalawa kuyenera kuyimitsidwa nthawi yomweyo.
Ndemanga za mankhwala, mawonekedwe ake komanso mtengo wake
Mankhwalawa, omwe akuphatikiza linagliptin, ali ndi dzina lazamalonda padziko lonse lapansi la Trazhenta.
Wopanga mankhwalawa ndi Beringer Ingelheim Roxane Inc., ku United States. Kuphatikiza apo, mankhwalawa amapangidwa ndi Austria. Mankhwala amaperekedwa kuchokera ku malo ogulitsa mankhwalawa pamaziko a mankhwala omwe madokotala amakupatsani.
Maganizo a odwala pamankhwala ambiri amakhala abwino. Ndemanga zoyipa nthawi zambiri zimagwirizanitsidwa ndi kugwiritsa ntchito mankhwalawa ndikuphwanya malangizo ogwiritsira ntchito, omwe amayambitsa bongo kapena mawonekedwe a zovuta zina.
Mtengo wa mankhwalawo uli ndi mtengo wosiyana kutengera wopanga, wogulitsa, komanso dera lomwe mankhwalawo amagulitsidwa ku Russia.
Linagliptin 5 mg No. 30 opangidwa ndi Beringer Ingelheim Roxane Inc., USA ku Russia ali ndi mtengo wapakati m'chigawo cha 1760 rubles.
Linagliptin m'mapiritsi 5 mg phukusi la zidutswa 30 zopangidwa ku Austria ku Russian Federation ali ndi mtengo wapakati pamtunda kuchokera 1648 mpaka 1724 rubles.
Mafanizo a Trazhenta ya mankhwala, omwe ali linagliptin, ndi Januvia, Onglisa ndi Galvus. Mankhwalawa ali ndi zosakaniza zingapo zomwe zimagwira, koma momwe zimakhudzira thupi ndizofanana ndi zomwe Trazhenta amakhala nazo mthupi.
Dziwani zambiri zamankhwala a shuga omwe ali mu vidiyoyi.
