Noho ka Sitagliptin e kaohi i ka momona a me ke kaumaha o ke kino

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I nā pathogenesis o ke ʻano maʻi type 2, ʻokoʻa ʻekolu mau ʻano hana:

  1. Tissue insulin pale;
  2. Loaʻa i ka hana o ka insulin endogenous;
  3. Hoʻohui nui i nā hōʻailona o ka glucose e nā pepeka.

ʻO ke kuleana no ka hoʻomohala ʻana i ua maʻi maʻi kūlike e waiho pū ana me nā c a me nā sela o ka pancreas. Hoʻopau ka mea hope loa i kahi hormone e hoʻonāukiuki i ka huli ʻana o ka glucose i ka ikehu no nā māhu a me ka lolo. Inā lohi ka helu o kāna hana, hoʻonāukiuki kēia ma ka hyperglycemia.

Na B-cells ke kuleana no ka hana ʻana o glucagon, ʻo ka hapanui ʻo ia i hana i ka ʻikepili no ka huna ʻana o ka pona e ka ate. ʻO ka glucagon nui a me ka nele o ka insulin e hāʻawi i nā kūlana no ka hōʻiliʻili o nā glucose i loaʻa ʻole i ka kahe koko.

ʻAʻole hiki ke mālama maikaʻi ʻia ka mālama ʻana i ka maʻi diabetes type 2 me ka ʻole o ka lōʻihi a me ka lōʻihi (no ka manawa holoʻokoʻa o ka maʻi) ka mālama ʻana o nā pakano kalepa. ʻO nā hoʻokolohua nui ma waena o ke ao nei e hōʻoia i ka uku gula wale nō e hoʻolako i nā kūlana no ka pale ʻana i nā hoʻopiʻi a hoʻonui i ke manaʻolana o ke ola maʻi.

ʻOiai me nā ʻano lāʻau āpau o antidiabetic, ʻaʻole ka poʻe maʻi āpau e hoʻokō i ka uku kūnaehana o nā kalepona me kā lākou kōkua. Wahi a kahi haʻawina UKPDS limau, ua loaʻa he 45% o nā maʻi maʻi i ka uku 100% no ka pale ʻana o ka microangiopathy ma hope o 3 mau makahiki, a he 30% wale nō ma hope o 6 mau makahiki.

Ke hoʻohālikelike nei kēia mau pilikia i ka pono e hoʻomohala i kahi papa wai hou no ka lāʻau lapaʻau e hiki ʻole ke kōkua wale nō e hoʻopau i nā pilikia metabolic, akā mālama pū nō hoʻi i ka pancreas, hoʻokuʻi i ka ʻoihana physiological e hoʻoponopono i ka hana insulin a me ka glycemia.

ʻO nā lāʻau lapaʻau ʻano nui i hiki ke hoʻoponopono i ka maʻi diabetes type 2 me ka hoʻoluhi ʻole ʻana o ka pancreas, nā loli koke i ka glycemia, ka ʻalā o ka hypoglycemia i nā hanana hou loa e nā lāʻau lapaʻau.

ʻO ka GLP-4 enzyme inhibitor Sitagliptin e kōkua i kahi maʻi maʻi e hoʻomalu i ka leʻaleʻa a me ke kaumaha o ke kino, e hāʻawi ana i ke kino me ka hiki ke kūʻokoʻa kūʻokoʻa i ka pilikia o ka hoʻoneʻe o ka glucose.

E hoʻokuʻu i ke ʻano a me ka ʻano

ʻO ka lāʻau lapaʻau e pili ana i ka sitagliptin me ka inoa kālepa ʻo Januvia i hana ʻia i ke ʻano o nā papa pōʻai me ka ʻulaʻula a i ka beige hue a hōʻailona ʻia i ka "227" no 100 mg, "112" ma kahi 50 mg, "221" no 25 mg. Hoʻopili ʻia nā papa ma nā pahu plastik a i ʻole nā ​​hihia penikala. Hiki i kekahi mau papa i kahi pahu.

Hoʻopili ʻia ka mea hoʻoneʻe sitagliptin phosphate hydrate me ka sodium croscarmellose, magnesium stearate, cellulose, sodium stearyl fumarate, unrefined calcium hydrogen phosphate.

No ka sildagliptin, hilinaʻi ke kumukūʻai ma ke kīʻaha, inā paha no nā papa 28 e pono ai ʻoe e uku i ka 1,596-1724 rubles. Hāʻawi ʻia kekahi lāʻau lapaʻau, ʻaina ka ola o ka noho papa. ʻAʻole pono ka lāʻau lapaʻau i nā kūlana kūikawā no ka mālama. Mālama ʻia ka ʻōmū wehe ma ka puka o ka pahu pouaka i hoʻokahi mahina.

Lapaʻau Sitagliptinum

ʻOkoʻa ka Sitagliptin mai i nā lāʻau lapaʻau hou antidiabetic i kāna ʻano hana a me kona ʻano. Ke hōʻike nei i ka hiki o ka hoʻonaninani o ka DPP-4, hoʻonui ka mea hoʻomohala i nā mea o ka hua i hoʻohui ʻia HIP a me GLP-1, e hoʻoponopono i ka glucose homeostasis.

Hoʻāla ʻia kēia mau hormones e ka mucosa ʻōpū, a hoʻonui ʻia ka hoʻoulu ʻana o nā huaole me ka makemake o nā mea kanu. Inā he kūleʻa a kiʻekiʻe ka pae glucose, e piʻi ka nui o nā hormones a i ka 80% o ka hana o ka insulin a me kāna neʻe ʻana e β-cells ma muli o ka hōʻailona hōʻailona i nā hana pūnaehana i loko o nā hale. Hoʻopili ʻia ka GLP-1 i ka mea huna kiʻekiʻe o ka testosteroneagon e nā b-cell.

ʻO ka emi ʻana o ke kaʻe o ka glucoseagon e kūʻē i ka mua o ka hoʻonui ʻana i ka nui o ka insulin i mea e hōʻemi ai i ka hoʻokaʻawale i nā mea huna glucose i loko o ka ate. Ke hana nei kēia mau hana a hōʻoia i ka maʻamau o ka glycemia. Hoʻohālikelike ʻia ka hana o nā incretins e kekahi ʻano pilikino, me ka hypoglycemia, ʻaʻole lākou e pili i ka synthesis o ka glucoseagon a me ka insulin.

Ke hoʻohana nei iā DPP-4, e hoʻokaʻawale ʻia nā kūmaha pane e hana i nā metabolites inert. Ke hāpai nei i nā hana o kēia enima, hoʻonui ʻia ka sitagliptin i ka ʻike o incretins a me ka insulin, e hoʻoneʻe ana i ka hana o glucagon.

Me ka hyperglycemia, kekahi o nā hōʻailona nui o ka diabetes type 2, ʻo kēia ʻano hana e kōkua i ka hōʻemi ʻana i ka pae o ka hemoglobin glycated, ke kōʻai holi a me ka glucose ma hope o ka ukana o ka haʻaleka. Hoʻokahi i hoʻokahi dosis o sitagliptin hiki ke kāohi i ka hana o DPP-4 i hoʻokahi lā, e hoʻonui ana i ka kahe o ka nui o nā hua i loko o ke kahe koko e 2-3 mau manawa.

Pharmacokinetics o sitagliptin

Hoʻopuka koke kahi komo o ka lāʻau, me ka bioavailability o 87%. ʻAʻole paʻa i ka manawa lawe ʻole i ka manawa e hoʻokomo a me ka ʻano o ka meaʻai, i ka mea kūikawā, ʻaʻole e loli nā meaʻai momona i nā parekela pharmacokinetic o ka mimetin mimetin.

E hiki aku ka mea paʻa i kona kiʻekiʻe loa (950 nmol) i nā hola 1-4. Aia i ka AUC e hilinaʻi ana i ka nui o ka maʻi, he haʻahaʻa ka hoʻololi ʻana ma waena o nā ʻano like ʻole o nā maʻi maʻi.

Ma ka hoʻohālikelike, hoʻonui ʻia ka hoʻohana hou o kahi papa 100 mg i ka ʻona ma lalo o ka AUC curve, e hōʻike ana i ka hilinaʻi o nā kaila apana i ka manawa, ʻo 14%. ʻO kahi waihona hoʻokahi o nā papa āpau o 100 mg e hōʻoia i ka laha unihue o 198 l.

Ua hoʻohuihui ʻia kahi ʻāpana liʻiliʻi o ka incretin mimetic. Ua hōʻike ʻia nā metabolites he nele i ka hiki ke pale aku i ka DPP-4. Hoʻolaha ʻo Renal (QC) - 350 ml / min. ʻO ka hapa nui o ka lāʻau lapaʻau ke hoʻopau ʻia e nā keiki (79% i loko o ke ʻano o ke ʻano a me ka 13% i loko o nā ʻano o nā metabolites), ke koena ka mea i hoʻopau ʻia e nā ʻāpana.

I ka ʻike ʻana o ka hana kaumaha ma luna o nā pēpē i loko o kahi maʻi maʻi me kahi ala koʻikoʻi (CC - 50-80 ml / min.), Ua like nā hōʻailona me ka CC 30-50 ml / min. ua nānā ʻia kahi kānalua o nā waiwai AUC, me kahi CC ma lalo o 30 ml / min - ʻehā mau manawa. Manaʻo kēia mau ʻano i ka dosis titration.

Me nā ala hepatic o ka hōʻeha paʻakikī, hoʻonuiʻia ka Cmax a me AUC ma ka 13% a me 21%. Ma nā hiʻohiʻona koʻikoʻi, ʻaʻole loli nui ka pharmacokinetics o sitagliptin, no ka mea, ua hoʻopuka mua ʻia ka lāʻau lapaʻau e nā keiki.

I nā maʻi maʻi o ka wā pākeke (65-80 mau makahiki), ʻo nā hiʻohiʻona pharmacokinetic o ka nui o ka minamina o ka penetenika me 19%. ʻAʻole koʻikoʻi nā mea like i kēlā me kēia, no laila ʻaʻole pono nā titration o keʻano.

ʻO wai e hōʻike ʻia ana ʻo ka incretinomimetic

Ua kuhikuhi ʻia ka lāʻau lapaʻau no ka maʻi maʻamau o ka 2 ma kahi o ka lāʻau haʻahaʻa-haʻahaʻa a me ka hana ʻoi ʻana.

Hoʻohana ʻia ia ma ka lāʻau hoʻokahi a hui pū ʻia me ka metformin, sulfonylurea hoʻomākaukau a i ʻole thiazolidinediones. Hiki nō hoʻi ia ke hoʻohana i ka hoʻoponopono ʻana i nā inikini insulin inā he kōkua kēia koho i ka hoʻoponopono ʻana i ka pilikia o ka pale ʻana i ka insulin.

ʻO nā maʻi no ka sitagliptin

Mai kuhikuhi i nā lāʻau lapaʻau:

  • Me ka kiʻekiʻe o ka naʻau kūʻokoʻa;
  • Maʻa maʻi maʻi me nā maʻi ʻano ʻehā;
  • ʻO ka ʻōpū a me ka umauma;
  • I ka'āina diabetes ketoacidosis;
  • I na keiki.

ʻO ka maʻi Diabetics me kahi ʻano maʻamau o ka papa lāʻau i ʻole e nānā pono.

Pehea e lawe ai

No ka sitagliptin, ʻo nā ʻōlelo e pili ai ka hoʻohana ʻana i ka inu ʻana i ka lāʻau lapaʻau ma mua o ka papaʻaina. ʻO ka maʻa maʻamau he like ia no ka hoʻoponopono lāʻau hou - 100 mg / lā. Inā wāwahi ʻia ka papa inoa o ka hoʻopono, pono e inu ʻia ka pōpoki i kēlā me kēia manawa, ʻaʻole ʻae ʻia ka pālua i ka hopena.

Me ka CC 30-50 ml / min. ka hoʻomaka hoʻomaka ʻana o ka lāʻau lapaʻau 2 mau manawa haʻahaʻa - 50 mg / lā., me CC ma lalo o 30 ml / min. - 4 manawa - 25 mg / lā. (one-one). ʻAʻole pili ka manawa o ka hemodialysis i ka hoʻoponopono regode sitagliptin.

Nā hanana pōʻino

E hoʻoholo ana i nā loiloi, ʻo ka hapa nui o nā maʻi maʻi āpau e hopohopo nei e pili ana i ka dyspepsia, huhū hewa. Ma nā hoʻokolohua hōʻoia, ua ʻike ʻia ka hyperuricemia, kahi hōʻemi i ka maikaʻi o ka gland thyroid, a me ka leukocytosis.

Ma waena o nā hopena ʻē aʻe ʻole i ʻike ʻia (kahi pilina me ka incretin mimetic i kū ʻole ʻia) - nā maʻi ʻeha, ʻeka ʻo Arthralgia, migraine, nasopharyngitis). Hoʻohālikelike ka ulu ʻana o ka hypoglycemia me nā hopena i ka pūʻulu hoʻomalu placebo.

Kōkua me ka overdose

Ma ka hihia o kahi overdose, lawe ʻia aku ka nui o ka lāʻau kī ʻole ʻia mai ka gastrointestinal tract, nā kākuhi koʻikoʻi (a me ka ECG) ka nānā ʻia. Hōʻike ʻia nā ʻano symptomatic a me ke kākoʻo kākoʻo, e komo pū ai ka hemodialysis me nā hiki ke lōʻihi (13.5 doses o ka lāʻau lapaʻau i nā hola 3-4).

Nā hopena hoʻopuka lāʻau lapaʻau

Me ka hana o ka sitagliptin me ka metformin, rosiglitazone, contraceptives waha, glibenclamide, warfarin, simvastatin, ka pharmacokinetics o kēia ʻano o nā lāʻau i loli.

ʻO ka hoʻokele ʻana o sitagliptin me ka digoxin ʻaʻole ia e hoʻopiʻi i kahi loli i ka nui o nā lāʻau lapaʻau. Hāʻawi ʻia nā ʻano like ʻole e ka ʻōlelo aʻo a me ka hoʻopili ʻana o ka sitagliptin a me cyclosporin, ketoconazole.

Sildagliptin - hui kikowaena

ʻO Sitagliptin ka inoa honua no ka lāʻau lapaʻau, ʻo kona inoa kālepa ʻo Januvius. Hiki i kahi analogue ke manaʻo ʻia i ka lāʻau lapaʻau i hoʻohui ʻia ʻo Yanumet, aia kahi me ka sitagliptin a me ka metformin. No Galvus ka pūʻulu o ka DPP-4 inhibitors (Novartis Pharma AG, Switzerland) me ka vildagliptin hāmeʻa ikaika, ke kumukūʻai 800 rubles.

ʻO nā lāʻau Hypoglycemic kūpono hoʻi no ke code ATX o ka pae 4:

  • Nesina (Takeda Pharmaceuticals, USA, e pili ana i ka alogliptin);
  • Onglisa (ʻO Bristol-Myers Squibb Company, e pili ana i ka saxagliptin, kumukūʻai - 1800 rubles);
  • ʻO Trazhenta (ʻO Bristol-Myers Squibb Company, ʻAmelika, Pelekane, me ka linagliptin ʻano ikaika), kumukūʻai - 1700 rubles.

ʻAʻole paʻa kēia mau lāʻau lapaʻau i loko o ka papa inoa o nā lāʻau lapaʻau kūikawā; mea pono anei ia e hoʻomaʻamaʻa i kou pilikino a me ke kūpaʻa me kāu kumukūʻai a me ke olakino?

ʻO Sitagliptin - nā loiloi

Ma ka hoʻopiʻi ʻana ma nā hōʻike e pili ana i nā kumuhana temala, ua helu pinepine ʻia ʻo Januvius i nā maʻi maʻi maʻi i ka manawa mua o ka maʻi. E pili ana i sitagliptin, nā hōʻike o nā kauka a me nā mea maʻi e hōʻike ana he nui nā nuances o ka hoʻohana ʻana i ka incretinomimetic.

ʻO Lavvia kahi lāʻau lapaʻau hou hou a ʻaʻole i loaʻa i nā kauka āpau ke loaʻa ka ʻike me ka hoʻohana. A hiki i kēia manawa, ʻo ka metformin ka laʻa mua loa; Inā lawa nā mea hiki, e hoʻohui pū iā ia me ka metformin a me nā lāʻau lapaʻau ʻē aʻe.

Hoʻopiʻi ka maʻi maʻi i ʻole e hālāwai ka lāʻau lapaʻau i nā koi i ʻōlelo ʻia, i ka wā i emi ka pono o ke kūpono. ʻAʻole ka pilikia ma aneʻi no ka hoʻohana ʻana i nā pā, akā i nā ʻano o nā maʻi: ʻo ke ʻano type type 2 he ʻano maʻi ʻano holomua.

Eugene, Lipetsk. Ma ka hope ua hele aku koʻu kauka i ka hoʻomaha. Nānā wau i kaʻu diary control gula, mālama ʻia no ka barbecue. ʻAʻole maikaʻi nā ʻili o nā loiloi, a ua ʻōlelo ʻo ia iaʻu e hoʻololi i ka Diabeton MV me Yanuvia. Uaʻike koʻu endocrinologist, ua makaʻala ʻo ia i nā huahana hou a pau. He aha kona pōmaikaʻi, ma waho o ka uku (6 mau manawa ke kiʻekiʻe!), ʻAʻole wau e maopopo. Hoinu wau i ka paila o Januvia no hoʻokahi mahina i ke kakahiaka, 3 hou Siofora 500 i ka lā, ʻoi ka honu pōloli ma mua o ka 7 mmol / l, a hoʻi koke ia i ka maʻamau maʻa o ka ʻai ʻana. Ma mua, ma hope o ke aʻo ikaika ʻana i ka hana lepa, hāʻule nui ke kō. I kēia manawa ke hōʻea nei i ka maʻamau (5.5 mmol / l) a kū aʻe i luna. I ka awelika, loaʻa iaʻu nā hōʻailona like ʻole ma mua, akā ua emi maoli ka hāʻule o ke kō. ʻAʻole hiki iaʻu ke ʻōlelo i kekahi mea e pili ana i nā hopena ʻokoʻa - ua noho mālie wau i hoʻokahi mahina.

Ke pili nei nā ʻōlelo āpau i ka hoʻomaka ʻana o ka sitagliptin i loko o ka hana lapaʻau, ka mea e hōʻike nei i ka papa hou o nā lāʻau lapaʻau hou, e loaʻa ana i ka manawa kūpono no ka mālama ʻana i ka maʻi type 2 i kēlā me kēia manawa, mai prediabetes a me nā hopena hou, me nā hopena maikaʻi ʻole mai ka hoʻohana ʻana i nā kumu uku lapaʻau glycemic kūlohelohe.

Hoike a Profesor A.S. Ametov, endocrinologist-diabetesologist e pili ana i ka ʻatikala a me ka hana o ka hoʻohana ʻana i sitagliptin - ma ke wikiō.

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