Trazhenta (dzina ladziko lonse Trajenta) ndi gulu latsopano la mankhwala othandizira odwala matenda ashuga. Ma Dhib-4 ma inhibitors omwe ali ndi njira yoyendetsera pakamwa agwiritsidwa ntchito bwino kuthana ndi matenda a shuga a 2;
Gawo logwira la mankhwala ndi linagliptin. Ubwino wake umayamikiridwa makamaka ndi odwala matenda ashuga omwe ali ndi matenda a impso, chifukwa mankhwalawa samawakhudza.
Trazhenta - mawonekedwe ndi mawonekedwe
Opanga, BOEHRINGER INGELHEIM PHARMA (Germany) ndi BOEHRINGER INGELHEIM ROXANE (USA), amatulutsa mankhwalawo ngati mapiritsi ofiira owoneka bwino. Chizindikiro cha wopanga omwe amateteza mankhwalawa kuchokera ku zinsomba amalembedwa mbali imodzi, ndipo cholembedwa "D5" chidalemba mbali inayo.
Iliyonse mwa iwo imakhala ndi 5 mg ya yogwira linagliptin ndi mafayilo osiyanasiyana monga wowuma, utoto, hypromellose, magnesium stearate, Copovidone, macrogol.
Chotumphukira chilichonse cha aluminium chimanyamula mapiritsi 7 kapena 10 a mankhwala a Trazhenta, chithunzi chake chikhoza kuwonedwa m'gawoli. Mu bokosi amatha kukhala osiyana - kuchokera pama mbale awiri mpaka asanu ndi atatu. Ngati pali maselo 10 okhala ndi mapiritsi pachimake, ndiye kuti pali timbale 3 motere.
Pharmacology
Kuthekera kwa mankhwalawa kumatheka bwino chifukwa cha zoletsa za ntchito ya dipeptidyl peptidase (DPP-4). Enzyme iyi imawononga
pa mahomoni HIP ndi GLP-1, omwe amachita mbali yayikulu pakuyang'anira shuga. Ma insretins amalimbikitsa kupanga kwa insulin, kuthandizira kuwongolera glycemia, ndikuletsa kubisala kwa glucagon. Zochita zawo zimakhala zakanthawi kochepa; pambuyo pake, HIP ndi GLP-1 imawononga ma enzyme. Trazhenta imagwirizananso ndi DPP-4, izi zimakupatsani mwayi wokhala ndi thanzi la ma impretins komanso kuwonjezera kuchuluka kwa magwiridwe ake.
Makina amakopa a Trazhenty ndi ofanana ndi mfundo za ntchito ya ma analogu ena - Januvius, Galvus, Ongliza. HIP ndi GLP-1 zimapangidwa pamene michere ilowa m'thupi. Mphamvu ya mankhwalawa sikugwirizana ndi kukonzekera kwawo, mankhwalawa amangowonjezera kutalikirana kwawo. Chifukwa cha machitidwe awa, Trazhenta, monga ma incretinomimetics ena, samayambitsa kupepuka kwa hypoglycemia ndipo uwu ndi mwayi wofunikira kwambiri kuposa magulu ena a mankhwala a hypoglycemic.
Ngati shuga sangachuluke kwambiri, ma insretins amathandizira kupanga insulin ya insulin mwa β-cell. Horoni GLP-1, yomwe ili ndi mndandanda wofunikira kwambiri poyerekeza ndi GUI, imalepheretsa kuphatikiza kwa glucagon m'maselo a chiwindi. Njira zonsezi zimathandiza kukhazikika glycemia pamlingo woyenera - kuchepetsa glycosylated hemoglobin, shuga komanso shuga m'magazi pambuyo pochita masewera olimbitsa thupi kwa maola awiri. Mu zovuta mankhwala a metformin ndi sulfonylurea kukonzekera, glycemic magawo bwino popanda zovuta kuwonda.
Pharmacokinetics
Pambuyo polowa m'matumbo, mankhwalawa amatengeka mwachangu, Cmax imawonedwa pambuyo pa ola limodzi ndi theka. Ndendeyi imachepera m'magawo awiri.
Kugwiritsa ntchito mapiritsi ndi chakudya kapena padera pa pharmacokinetics yamankhwala sikukhudza. The bioavailability wa mankhwala mpaka 30%. Peresenti yaying'ono imapangidwa, 5% imakumbidwa ndi impso, 85% yochotsa ndowe. Matenda aliwonse a impso safuna kuti munthu atenge mankhwala kapena kusintha kwa mankhwala. Zolemba za pharmacokinetics muubwana sizinaphunzire.
Kodi mankhwala a ndani
Trazent imasankhidwa ngati mankhwala mzere woyamba kapena kuphatikiza ndimankhwala ena ochepetsa shuga.
- Monotherapy. Ngati wodwala matenda ashuga samalola kugwiritsa ntchito mankhwala osokoneza bongo a mitundu yayikulu monga metformin (mwachitsanzo, ndi aimpso kapena kusalolera kwa ziwalo zake), ndikusinthidwa kwa njira ya moyo sikubweretsa zotsatira zomwe mukufuna.
- Zigawo ziwiri. Trazent imayikidwa limodzi ndi sulfonylurea kukonzekera, metformin, thiazolidatediones. Ngati wodwala ali ndi insulin, incretinomimetic ikhoza kuwonjezeranso.
- Njira zitatu. Ngati chithandizo cham'mbuyomu cha mankhwala othandizira sichigwira ntchito mokwanira, Trazhenta imaphatikizidwa ndi insulin ndi mtundu wina wa mankhwala opatsirana pogwiritsa ntchito njira zina.
Yemwe sanapatsidwe Trazhent
Linagliptin amatsutsana chifukwa cha anthu odwala matenda ashuga:
- Mtundu woyamba wa shuga;
- Ketoacidosis wokwiyitsidwa ndi matenda ashuga;
- Oyembekezera ndi kuyamwa;
- Ana ndi unyamata;
- Hypersensitivity pazomwe zimapangidwira.
Zotsatira zoyipa
Pa maziko akutenga linagliptin, mavuto amayamba:
- Nasopharyngitis (matenda osachiritsika);
- Kuzonda kuzizira;
- Hypersensitivity;
- Pancreatitis
- Kuwonjezeka kwa triglycerol (akaphatikizidwa ndi mankhwala a gulu la sulfonylurea);
- Kuchulukitsa kwa LDL (pogwiritsa ntchito pioglitazone);
- Kukula kwa thupi;
- Zizindikiro za Hypoglycemic (motsutsana ndi maziko a mankhwala awiri komanso atatu).
Pafupipafupi komanso kuchuluka kwa zovuta zomwe zimachitika mutatha kudya Trazhenta ndizofanana ndi kuchuluka kwa zotsatira zoyipa mutagwiritsa ntchito placebo. Nthawi zambiri, zotsatira zoyipa zimawonetsedwa katatu mu zovuta za Trazhenta zokhala ndi metformin komanso sulfonylurea.
Mankhwalawa amatha kuyambitsa zovuta kumalumikizana, izi ndizofunikira kuziganizira mukamayendetsa magalimoto ndi magwiridwe antchito.
Bongo
Ophunzira adapatsidwa mapiritsi a 120 (600 mg) panthawi imodzi. Mankhwala osokoneza bongo amodzi sanakhudze thanzi la odzipereka ochokera ku gulu loyendetsa bwino. Pakati pa odwala matenda ashuga, milandu ya bongo yochulukirapo sanalembedwe ndi ziwerengero zamankhwala. Ndipo komabe, ngati mwangozi kapena mukugwiritsa ntchito mwanjira inayake ma Mlingo angapo nthawi imodzi, wovutikayo amafunika kuti azitsuka m'mimba ndi matumbo kuti achotse gawo losagwiritsidwa ntchito la mankhwalawo, apatseni ma sorbets ndi mankhwala ena molingana ndi zizindikirazo, onetsani adotolo.
Momwe mungamwe mankhwalawa
Mosamala mogwirizana ndi malangizo ogwiritsira ntchito ayenera kumwedwa katatu patsiku, piritsi 1 (5 mg). Ngati mankhwalawa agwiritsidwa ntchito pazovuta zovuta mogwirizana ndi metformin, ndiye kuti mlingo wotsiriza umakhalabe.
Anthu odwala matenda ashuga aimpso kapena a hepatic osakwanira safuna kusintha kwa mlingo. Zizolowezi sizosiyana kwa odwala azaka zokhwima. Mu senile (wazaka 80), Trazhent sanatchulidwe chifukwa cha kusowa kwa chidziwitso m'chipani cha m'badwo uno.
Ngati nthawi yakumwa mankhwalawo yakusowa, muyenera kumwa piritsi mwachangu. Ndikosatheka kubwereza zomwezo. Kugwiritsa ntchito mankhwalawa sikugwirizana ndi nthawi yakudya.
Mphamvu ya trazhenti pa mimba ndi mkaka wa m`mawere
Zotsatira zakugwiritsa ntchito mankhwalawa ndi amayi apakati sizofalitsidwa. Pakadali pano, kafukufuku wachitika pa nyama zokhazokha, ndipo palibe zolemba za poizoni zomwe zalembedwa. Ndipo komabe, panthawi yoyembekezera, azimayi sapatsidwa mankhwala.
Poyeserera nyama, zidapezeka kuti mankhwalawo amatha kulowa mkaka wa mayi. Chifukwa chake, munthawi yakudyetsa azimayi, Trazhent sanalembedwe. Ngati boma laumoyo likufuna mankhwala otere, mwana amamuthandizira zakudya zopanda pake.
Kafukufuku wazokhudza mphamvu ya mankhwala pakubala mwana sanatengeke. Kuyesera komweko pa nyama sikunawonetse vuto lililonse mbali iyi.
Kuyanjana kwa mankhwala osokoneza bongo
Kugwiritsa ntchito munthawi yomweyo kwa Trazhenta ndi Metformin, ngakhale mlingo utakhala wokwera kuposa muyezo, sizinayambitse kusiyana kwakukulu mu pharmacokinetics yamankhwala.
Kugwiritsa ntchito pamodzi kwa Pioglitazone sikusinthanso mphamvu ya pharmacokinetic ya mankhwala onse awiri.
Chithandizo chovuta ndi Glibenclamide sichowopsa kwa Trazhenta, chifukwa chomaliza, Cmax chimachepera pang'ono (ndi 14%).
Zotsatira zofananazo zimawonetsedwa ndi mankhwala ena a gulu la sulfonylurea.
Kuphatikiza kwa ritonavir + linagliptin kumachulukitsa Cmax katatu, kusintha kotereku sikutanthauza kusintha kwa mlingo.
Kuphatikiza ndi Rifampicin kumayambitsa kuchepa kwa Cmax Trazenti. Mwapang'onopang'ono, mawonekedwe azachipatala amasungidwa, koma mankhwalawa sagwira ntchito 100%.
Siowopsa kudziwa Digoxin nthawi yomweyo ngati lynagliptin: ma pharmacokinetics a mankhwala onsewa sasintha.
Trazhent sichikhudza kuthekera kwa Varfavin.
Kusintha kocheperako kumawonedwa limodzi ndi kugwiritsidwa ntchito kwa linagliptin ndi simvastatin, koma mlingidwe wa incretin samakhudza kwambiri mawonekedwe ake.
Poyerekeza ndi chithandizo cha mankhwala ndi Trazhenta, njira zakulera za pakamwa zitha kugwiritsidwa ntchito momasuka.
Malangizo owonjezera
Matendawa satchulidwa mtundu 1 wa shuga komanso ketoacidosis, vuto la matenda ashuga.
Chiwopsezo cha zochitika za hypoglycemic pambuyo pa chithandizo cha linagliptin, chogwiritsidwa ntchito ngati monotherapy, ndizokwanira kuchuluka kwa milandu yotere ndi placebo.
Kuyesa kwa zamankhwala kwawonetsa kuti pafupipafupi momwe zimachitika mu hypoglycemia mukamagwiritsa ntchito Trezhenta pophatikiza mankhwala samaganiziridwa, popeza zovuta sizimayambitsa linagliptin, koma metformin ndi mankhwala a gulu la thiazolidinedione.
Chenjezo liyenera kuonedwa posankha Trazhenta osakanikirana ndi mankhwala a gulu la sulfonylurea, chifukwa amachititsa hypoglycemia. Pangozi yayikulu, ndikofunikira kusintha mlingo wa mankhwala a gulu la sulfonylurea.
Linagliptin sikukhudza mwayi wopanga matenda a mtima ndi mtsempha wamagazi.
Kuphatikiza mankhwala, Trazhent angagwiritsidwe ntchito ngakhale kwambiri mkhutu aimpso ntchito.
Odwala achikulire (zaka zopitilira 70), chithandizo cha Trezenta chinawonetsa zotsatira zabwino za HbA1c: hemoglobin yoyambirira inali 7.8%, yomaliza - 7.2%.
Mankhwalawa samatulutsa chiwopsezo cha mtima. Malo oyambira omwe amakhala ndi pafupipafupi komanso nthawi yomwe amwalira, matenda a mtima, sitiroko, osakhazikika a angina pectoris omwe amafunikira kuchipatala, odwala matenda ashuga omwe amatenga linagliptin sanali kawirikawiri komanso mochedwa kuposa odzipereka pagulu lolamulira omwe adalandira mankhwala a placebo kapena kuyerekezera.
Nthawi zina, kugwiritsa ntchito linagliptin kumayambitsa kupweteka kwa pachimake kapamba.
Ngati pali zizindikiro (zopweteka kwambiri za epigastrium, dyspepsia, kufooka kwathunthu), mankhwalawa ayenera kuyimitsidwa ndikufunsani dokotala.
Kafukufuku wokhudzana ndi kufalikira kwa Trazhenta pa luso loyendetsa magalimoto ndi magwiridwe antchito ambiri sanayendetsedwe, koma chifukwa cha kulumikizidwa komwe kungatheke, imwani mankhwalawo ngati pakufunika, mwachidwi kwambiri komanso mosamala mwachangu.
Analogs ndi mtengo wamankhwala
Kwa Trazhenta wa mankhwala, mtengo wake umachokera ku ruble 1500-1800 wama mapiritsi 30 ndi mlingo wa 5 mg. Mankhwala omwe mumalandira amamasulidwa.
Zofanizira za gulu lomwelo la DPP-4 zoletsa zimaphatikizapo Januvia zozikidwa pa sungliptin, Onglizu zochokera ku saxagliptin ndi Galvus wokhala ndi vildagliptin yogwira. Mankhwalawa amafanana ndi code ya ATX level 4.
Zofanana ndi izi zimaperekedwa ndi mankhwalawa Sitagliptin, Alogliptin, Saksagliptin, Vildagliptin.
Palibe zofunikira zina pakusungidwa kwa Trazenti m'malangizo. Kwa zaka zitatu (malinga ndi nthawi yomwe ntchito yake imatha), mapiritsiwa amasungidwa kutentha kwa chipinda (mpaka +25 degrees) m'malo amdima osapezedwa ndi ana. Mankhwala omwe atha ntchito sangathe kugwiritsidwa ntchito, ayenera kutayidwa.
Anthu odwala matenda ashuga komanso madokotala za Trazhent
Kuchita kwakukulu kwa Trazenti pakuphatikizana kosiyanasiyana kunatsimikiziridwa ndi maphunziro apadziko lonse komanso machitidwe azachipatala. Endocrinologists amakonda kugwiritsa ntchito linagliptin ngati mankhwala a mzere woyamba kapena kuphatikiza pamodzi. Ndi chizolowezi cha hypoglycemia (kulimbitsa thupi mwamphamvu, kusowa zakudya m'thupi), m'malo mwa mankhwala a sulfonylurea, amapatsidwa mankhwala a Trazent, pali ndemanga zamankhwala omwe mumalandira pakulimbana ndi insulin komanso kunenepa kwambiri. Anthu ambiri omwe ali ndi matenda ashuga amalandila mankhwalawa ngati gawo la zovuta mankhwala, motero nkovuta kuyesa momwe amagwirira ntchito, koma ambiri, aliyense amasangalala ndi zotsatirazi.
Zoletsa za DPP-4, zomwe Trazhenta ndi yake, zimasiyanitsidwa osati ndi mphamvu ya antidiabetes, komanso chiwopsezo chowonjezeka, popeza sizipangitsa vuto la hypoglycemic, sizithandiza kukulitsa kulemera, komanso sizikukulitsa kulephera kwa impso. Mpaka pano, gulu la mankhwalawa limawerengedwa kuti ndi imodzi mwazabwino kwambiri pakuwongolera matenda ashuga a mtundu 2.
