Ke ʻano lāʻau Lixumia: nā ʻōlelo no ka hoʻohana ʻana

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

Nā mea kūʻai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2.7 mg, hydrochloric acid solution 1 M a i kahi pākia wai pākana wai pākaha 1 M - a hiki i ka pH 4.5, wai d / a - hiki i ka 1 ml.

3 ml - mau kāleka (1) - peni syringe (1) - nā pā o ka pahu paʻi.

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

Nā mea kūʻai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2.7 mg, hydrochloric acid solution 1 M a i kahi pākia wai pākana wai pākaha 1 M - a hiki i ka pH 4.5, wai d / a - hiki i ka 1 ml.

3 ml - mau kāleka (1) - peni syringe (1) - nā pā o ka pahu paʻi.
3 ml - mau kāleka (1) - peni syringe (2) - nā pā kāleka.
3 ml - mau kāleka (1) - peni syringe (6) - nā pākeke o ke kāleka.

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

Nā mea kūʻai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2.7 mg, hydrochloric acid solution 1 M a i kahi pākia wai pākana wai pākaha 1 M - a hiki i ka pH 4.5, wai d / a - hiki i ka 1 ml.

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

Nā mea kūʻai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2.7 mg, hydrochloric acid solution 1 M a i kahi pākia wai pākana wai pākaha 1 M - a hiki i ka pH 4.5, wai d / a - hiki i ka 1 ml.

3 ml - mau kāleka (2) me kahi hoʻonā o 0,05 mg / ml (10 μg / dosis) a me 0.1 mg / ml (20 μg / mauʻu) - penikala syringe (2) - nā pākeke o ka pāpū.

Nā hōʻailona no ka hoʻohana ʻana

ʻO ka maʻi mellitus type 2 i ka pākeke e hoʻokō i ka mana glycemic i loko o nā poʻe maʻi e ʻike ʻole ʻia e ka maʻi mellitus e ka hoʻomau ʻia ʻana o ka maʻi hypoglycemic.

Ke kumu o Lixumia i hui pū me nā huaʻōlelo hypoglycemic waha e hōʻike nei:

- ka lāʻau lapaʻau hypoglycemic oral o ka hui sulfonylurea,

- ka hui ʻana o kēia mau lāʻau.

Ua kauoha ʻia ʻo Lixumia i ka hui pū me ka insulin basal:

- i hui pū me ka lālani hypoglycemic oral o ka hui sulfonylurea.

Nā Hoʻohui

- Hoʻonui i ka naʻau pono pilikino i ka waiwai ikaika a i ʻole o nā mea i hoʻowalewale o ka lāʻau lapaʻau.

- ʻO ka manawa o ka lactation (umauma umauma).

- nā maʻi hōʻeha o ka gastrointestinal tract, me nā gastroparesis.

- hōʻeha maikaʻi o ka renal (ʻoi aku ka hana ma kahi o 30 ml / min).

- nā keiki a me nā ʻōpio ma lalo o 18 makahiki.

Me ka mōʻaukala o ka pancreatitis, pono e hoʻohana ʻia ʻo Lixumia me ka akahele.

Pehea e hoʻohana ai: dosis a me ke ʻano o ka mālama ʻana

ʻO ka ʻōlelo mua a Lixumia ʻo 10 mcg hoʻokahi i ka lā no 14 lā. A laila e hoʻonui ʻia ka lāʻau i ka mālama mālama ʻia o 20 mcg i hoʻokahi lā.

Ke hoʻohui ʻia kahi lāʻau lapaʻau i kahi lāʻau metformin e hoʻomau nei, hiki ke hoʻomau ka metformin me ka ʻole o ka hoʻololi ʻana i kona ʻano.

Ke hoʻohui ʻia ʻo Lixumia i ka lāʻau paʻa me ka lāʻau hypoglycemic oral o ka hui sulfonylurea a i ʻole ka hui ʻana o ka lāʻau hypoglycemic oral o ka hui o ka sulfonylurea a me ka insulin basal, kahi hoʻemi ʻia ka hopena o ka lāʻau hypoglycemic oral o ka hui o ka sulfonylurea a i ka basal insulin hiki ke manaʻo e hōʻemi i ka hopena o ka hypoglycemia.

ʻAʻole pono ka hoʻohana ʻana o Lixumia i ka nānā koʻikoʻi o ka neʻe o ka glucose i ke koko. Eia nō naʻe, i ka wā e hoʻohana pū ʻia me ka lālani hypoglycemic oral o ka hui sulfonylurea a i ʻole basal insulin, ka nānā ʻana o ka glucose o ke koko a i ʻole ka nānā pono ʻana (ka hoʻomalu ʻia e ka mea maʻi) o ka hoʻoliʻi ʻana o ka hoʻokaʻa glucose lā e koi ʻia e hoʻoponopono i ka ʻai ʻana o ka lāʻau hypoglycemic oral o ka hui o ka sulfonylurea a i ʻole basal insulin.

Nā hui ahonui kūikawā

Nā keiki a me nā ʻōpio ma lalo o nā makahiki he 18: i kēia manawa, ke palekana a me ka pono o ka lāʻau lapaʻau i kēia pūʻulu o nā maʻi ʻaʻole i aʻo ʻia.

Nā wa kahiko: ʻaʻohe pono o ka hoʻoponopono hoʻoponopono ʻia ma muli o ka makahiki o ka mea maʻi.

ʻO nā mea maʻi me ka nele o ka ate: ʻaʻole i koi ʻia ka hoʻoponopono ʻana i nā maʻi i nā mea maʻi me ka maikaʻi ʻole o ka ate.

ʻO nā mea maʻi me ka hiki ʻole o ka renal: ʻaʻole i koi ʻia ka hoʻoponopono ʻana i ka wai i loko o nā mea maʻi me ka maikaʻi ʻole o ka renal (ʻoi aku ka hana ʻana o ka creinine 50-80 ml / min) a me ka hoʻomaʻamaʻa renal moderate (clearanine clearance 30-50 ml / min). ʻAʻoheʻike therapeutic me Lixumia i nā mea maʻi me ka hōʻeha o ka renal koʻikoʻi (ʻo ka creinine clearance e emi mai ma mua o 30 ml / min) a i ʻole ka hopena hope loa o ka hanana, a no laila ke hoʻohana nei i ka lāʻau lapaʻau ma kēia pūʻulu o nā mea maʻi.

Hoʻohana ʻia ʻo Lixumia i 1 manawa i kēlā me kēia lā ma mua o 1 mau hola ma mua o ka pāʻina mua i ka lā a i ʻole 1 hola ma mua o ka pāʻina ahiahi. Inā kāpī ʻia ka makeʻe ma hope aʻe, e lawe ʻia ma loko o 1 mau hola ma mua o ka ʻai ʻokoʻa.

Hoʻohana ʻia ka lāʻau i ka subcutaneously ma ka ʻūhā, ka ʻōpū a i ʻole poʻohiwi paha. ʻAʻole pono ke hoʻokele ʻia ʻo Lixumia a i ʻole intramuscularly.

Ma mua o ka hoʻohana ʻana, pono e mālama i ka peni penikala ʻo Lixumia i loko o kahi friji i ke mahana o 2-8 ° C i loko o kāna pale e pale ai mai ka ʻike ʻana i ka mālamalama. Ma hope o ka hoʻohana mua ʻana, pono e mālama ʻia ka peni kinipiko i kahi mahana ʻaʻole 30% C. Ma hope o kēlā me kēia hoʻohana ʻana, pono e pani ʻia ka peni ʻuli me ka pāpale e pale ai iā ia mai ka ʻike ʻana i ka mālamalama. ʻAʻole pono e mālama i ka penu syringe me kahi pūpū e hoʻopili ʻia. Mai hoʻohana i ka peni ʻo ka syringe inā ua maloʻo ia.

E hoʻokuʻu ʻia ka Lixumia Syringe Pen ma hope o 14 lā.

Ka hana lāʻau lapaʻau

ʻO ka mahele hoʻoikaika o Lixumia lixisenatide he ikaika ikaika a me ka selon agonist o ke kīkona-like peptide-1 (GLP-1). ʻO ka GLP-1 ka mea i hopu ʻia no ka GLP-1 maoli, he hormone endogenous o ka ʻōlelo huna kūloko, kahi potentiates glucose i hilinaʻi i ka insulin a nā beta-cells o ka pancreatic pulupulu. Hoʻohui ka hopena o ka lixisenatide me kona ʻano kikoʻī me nā mea hoʻokipa GLP-1, e alakaʻi ana i ka hoʻonui nui ʻana o ka ʻike intracellular monophosphate cyclic (cAMP). Hoʻokomo ʻo Lixisenatide i ka hana huna ʻana o ka insulin i nā hua beta o nā mokupuni pancreatic i pane ai i ka hyperglycemia. Ke hoʻoneʻe nei ka nānāʻana o ka glucose i ke koko ma nā kumu maʻamau, ka hopena o ka hoʻoulu ʻana o ka huna ʻana i ka insulin, e hoʻoneʻe ana i ka hopena o ka hypoglycemia. I ka hyperglycemia, ka lixisenatide pale pinepine i ka huna ʻana i ke kihi o ka glucoseagon, eia naʻe, ke ʻano pale o ka pale ʻana o ka hoʻokahe i ka hopena o hypagonlycemia e pane ana i nā koena hypoglycemia.

Hōʻike ʻia ka hoʻohālikelike i ka hana insulinotropic o lixisenatide, me ka hoʻonui ʻana o ka biosynthesis insulin a me ka hoʻoulu ʻana i nā hua beta o nā mokupuni pancreatic i nā holoholona. Lohi ʻo Lixisenatide i ka emi ʻana o ka wahī, ma laila e hōʻemi ai i ka nui o ka hoʻonui ʻana o ka glucose koko ma hope o ka ʻai ʻana. Hiki ke hopena i ka hoʻomaha ʻana i ka gastric hiki ke hāʻawi pū i ka pohō kaumaha.

I ka manawa i lawelawe ʻia i hoʻokahi lā i nā mea maʻi me ka diabetes mellitus type 2, e hoʻomaikaʻi ai ka lixisenatide i ka mana glycemic ma o ka ulu wikiwiki ʻana ma hope o kona keʻena a me ka hoʻokaʻawale ʻana o ke kaila o ka glucose koko ma hope o kaʻai a me ka ʻōpū.

E hoʻokuʻu i ke ʻano, ka hoʻonohonoho ʻana a me ka pōpoki

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

1 ml o ka hoʻonā i loaʻa:

mea waiwai: lixisenatide - 0.05 mg,

nā mea waiwai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2,7 mg, kahawai hulu wai pākahi 1 M a i ʻole ka pāʻina sodiumxide hopena 1 M - a hiki i ka pH 4.5, ka wai d / a - a i ml

3 ml - mau kāleka (1) - peni syringe (1) - nā pā o ka pahu paʻi.

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

1 ml o ka hoʻonā i loaʻa:

mea waiwai: lixisenatide - 0.1 mg,

nā mea waiwai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2,7 mg, kahawai hulu wai pākahi 1 M a i ʻole ka pāʻina sodiumxide hopena 1 M - a hiki i ka pH 4.5, ka wai d / a - a i ml

3 ml - mau kāleka (1) - peni syringe (1) - nā pā o ka pahu paʻi.
3 ml - mau kāleka (1) - peni syringe (2) - nā pā kāleka.
3 ml - mau kāleka (1) - peni syringe (6) - nā pākeke o ke kāleka.

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

1 ml o ka hoʻonā i loaʻa:

mea waiwai: lixisenatide - 0.05 mg,

nā mea waiwai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2,7 mg, kahawai hulu wai pākahi 1 M a i ʻole ka pāʻina sodiumxide hopena 1 M - a hiki i ka pH 4.5, ka wai d / a - a i ml

ʻO ke kūleʻa no ka hoʻokele sc, he ʻulaʻula ʻole.

1 ml o ka hoʻonā i loaʻa:

mea waiwai: lixisenatide - 0.1 mg,

nā mea waiwai: ka glycerol 85% - 18 mg, sodium acetate trihydrate - 3,5 mg, methionine - 3 mg, metacresol - 2,7 mg, kahawai hulu wai pākahi 1 M a i ʻole ka pāʻina sodiumxide hopena 1 M - a hiki i ka pH 4.5, ka wai d / a - a i ml

3 ml - mau kāleka (2) me kahi hoʻonā o 0,05 mg / ml (10 μg / dosis) a me 0.1 mg / ml (20 μg / mauʻu) - penikala syringe (2) - nā pākeke o ka pāpū.

ʻO ka maʻi mellitus type 2 i ka pākeke e hoʻokō i ka mana glycemic i loko o nā poʻe maʻi e ʻike ʻole ʻia e ka maʻi mellitus e ka hoʻomau ʻia ʻana o ka maʻi hypoglycemic.

Hōʻike ʻia ʻo Lixumia i ka hui pū me nā huaʻōlelo hypoglycemic waha o kēia lā:

- ka lāʻau lapaʻau hypoglycemic oral o ka hui sulfonylurea,

- ka hui ʻana o kēia mau lāʻau.

Hōʻike ʻia ʻo Lixumia i ka hui pū me ka insulin basal:

- i hui pū me metformin,

- i hui pū me ka lālani hypoglycemic oral o ka hui sulfonylurea.

Ka hoʻohana ʻana o Lixumia i ka wā hāpai a me ka lactation

Nā wahine hānau keiki.
ʻAʻole ʻōlelo ʻo Lixumia i nā wahine o nā keiki hānai keiki ʻaʻole i hoʻohana i nā contraceptives.
Kahawai
ʻAʻole lawa nā data ma ka hoʻohana ʻana o Lixumia i nā wahine hāpai. Ua hōʻike ʻia nā haʻawina preclinical i nā mānoanoa reproduction.
ʻAʻole maopopo ka ʻike nui i ke kanaka.
ʻAʻole pono e hoʻohana ʻo Lixumia i ka wā hāpai. Ma kahi o ka ʻōlelo, ua ʻōlelo ʻia mai ka insulin.
Inā makemake ka mea maʻi e hāpai a hāpai a hāpai paha, ua hoʻōki ʻia ka lāʻau me Lixumia.
Hoʻokaumana.
ʻAʻole i ʻike ʻia inā hoʻokomo ʻo Lixumia i ka waiū umauma o ke kanaka. ʻAʻole pono e hoʻohana ʻo Lixumia i ka wā lactation.
Pūnaewele.
ʻAʻole hōʻike nā haʻawina preclinical i kahi hopena maikaʻi i ka ulu ʻana.

ʻO Lixisenatide kahi mea pili i koho ʻia no nā mea hoʻokipa GLP-1 (e like me peptide-1). ʻO ka mea maʻi GLP-1 kahi pahuhopu maoli no ka GLP-1 kūlohelohe, he endogenous incretin hormone e potentiates glucose e hilinaʻi nei i ka huna a ka maʻi e ka pancreatic beta cells.
Hoʻopili ʻia ka hopena o ka lixisenatide e kahi hōʻike pilikino me nā mea hoʻokipa GLP-1, e alakaʻi ana i ka hoʻonui i ka intracellular cyclic adenosine monophosphate (cAMP).
Hoʻolaha ʻo Lixisenatide i ka huna ʻana i ka insulin i ka wā e hoʻonui ka nui o ke kō o ke koko, akā ʻaʻole me ka normoglycemia, kahi e hoʻohālikelike ai i ka hopena o ka hypoglycemia.
I ka manawa like, kau ʻia ka ʻikepili glucagon. Me ka hypoglycemia, mālama ʻia kahi ʻoihana hoʻolaʻa o ka hoʻonaʻauao glucagon.
Hāʻawi ʻo Lixisenatide i ka haʻalele ʻana o ka ʻōpū, hoʻemi ʻia ka wikiwiki i loaʻa i ka glucose i ka meaʻai ke kahe koko.
ʻO nā hopena Pharmacodynamic.
Ke hoʻohana ʻia i hoʻokahi lā i ka poʻe maʻi me ka maʻi diabetes type 2, hoʻomaikaʻi ka lixisenatide i ka mana glycemic ma muli o nā hopena koke a lōʻihi loa o ka hoʻohaʻahaʻa ʻana i nā kukuna glucose ma hope o ka ʻaina a ma ka ʻōpū ʻole.
Ua hōʻoia ʻia kēia hopena ma ka glucose postprandial i loko o kahi haʻawina 4-pule, i hoʻohālikelike ʻia me ka liraglutide 1.8 mg hoʻokahi manawa i ka lā me ka hui pū me ka metformin. Hoʻomaka mai ka pae mua o ka mākaukau PPK 0: 30–4: 30 h
ʻO ka glucose glucose ma hope o ka ʻai ʻaʻai ʻana:
–12.61 hola * mmol / L (-227.25 hola * mg / dL) i loko o ka lixisenatide pūʻulu a me -4.04 hola * mmol / L (–72.83 hola * mg / dl) i ka hui liraglutide.
Ua hōʻoia ʻia i kēia ma ke aʻo he 8 mau wiki i hoʻohālikelike ʻia i ka liraglutide i ʻōlelo ʻia ma mua o ka ʻaina kakahiaka i hui pū me ka glargine insulin a i ʻole ʻole metformin.
Maikaʻi pono ʻo ka haukapila.
Nā hopena o Lixumia i ka hoʻomohala glycemic hoʻohālikelike ʻia me exenatide i loiloi ʻia i loko o kahi ʻeono i hoʻoholo ʻia, ʻelua pāpū, pālua, ʻohiʻohi ʻia a me ka hoʻokaʻawale pahuhopu āpau, wehe ʻana i ka hōʻike me ka mana paʻa.
Ua komo nā noiʻi i ka poʻe 3825 me nā maʻi maʻi type (2445 nā mea maʻi me ka lixisenatide), 48.2% o nā kāne a me 51.8% o nā wahine.
768 nā mea maʻi (447 randomized e hoʻohana i ka lixisenatide) he ≥65 mau makahiki, a he 103 nā maʻi (57 randomized to use lixisenatide) were75 makahiki.
I ka pau ʻana o nā haʻawina III paʻa, ua hōʻike ʻia ma ka hopena o ka papa mālama 24-wiki ma mua, ʻoi aku ka 90% o ka nui o ka poʻe maʻi i hiki i ka mālama mau i ka mālama mālama ʻia o Lixumia 20 μg hoʻokahi i hoʻokahi lā.
ʻO ka control glycemic.
Hoʻohui hui hou i ka hoʻohana ʻana i nā lāʻau antidiabetic waha.
I ka hopena o ka hopena mālama 24 mau hebedoma, ʻo Lixumia i hui pū me ka metformin, sulfonylurea, pioglitazone, a hui pū ʻana me kēia mau lāʻau i hōʻike i ka emi nui o ka wikiwiki o ka plasma HbA1c, kūmole i ka glucose glucose wikiwiki a me ka glucose o ka hapaha postprandial 2-hola. ʻO ka hōʻemi ʻana o HbA1c i mea nui i ka wā i mālama ʻia ai ka lāʻau i hoʻokahi manawa i ka lā, inā paha me ka mea i ke kakahiaka nui a i ke ahiahi paha.
ʻO ka hoʻolaha ʻana i ka HbA1c i lōʻihi i nā haʻawina lōʻihi a hala 76 mau pule.
Hoʻohui kūikawā i hui pū me ka metformin kūʻokoʻa wale nō.
Papa 2: nā haʻawina hoʻokele placebo i hui pū me ka metformin (hopena 24-pule).
I loko o ka noiʻi ʻana me ka mana hoʻomohala nui ma ka hopena o ka hopena mālama 24 nui hebedoma, ʻo ka hoʻohana ʻana o Lixumia i hoʻokahi manawa i ka lā e hōʻike ana i ka emi ʻana o ka pae HbA1c o -0.79% hoʻohālikelike ʻia -0.96% i ka wā e hoʻohana ai iā Exenatide pālua i kēlā me kēia lā, me ka awelika hōʻokoʻa o ka mālama ʻana 0.17% (95% pilina hilinaʻi (CI): 0.033, 0.297) a me kahi pālua like like o nā maʻi i loaʻa i kahi pae HbA1c ma lalo o 7% ma ka hui lixisenatide (48.5%)
a ma ka hui exenatide (49.8%).
I ka nui o ka mālama manawa 24-mau pule, ʻo ka hōʻeha o ka maʻi pākaukau ʻo 24.5% i loko o ka lixisenatide pūʻulu hoʻohālikelike ʻia me 35.1% i ka hui o exenatide pākahi i ka lā, a me ka ulu ʻana o ka hypoglycemia hōʻailona a me ka lixisenatide he 2.5% hoʻohālikelike ʻia me ka 7.9% ma ka hui exenatide.
I loko o kahi hōʻike 24-pule wehe, ua hāʻawi ʻia ʻo lixisenatide ma mua o ka papa ʻaina nui a ʻaʻole hoʻi i emi ʻole ka lixisenatide i hāʻawi ʻia ma mua o ka ʻaina kakahiaka ma ke ʻano o ka hōʻemi.
ʻO ka HbA1c (loli i ka palena o ka hopena mai ka pae mua: -0.65% hoʻohālikelike me 0.74%). ʻO ka hoʻēmi ʻana ma HbA1c i nānā ʻia ʻo ia ma ke ʻano o ka ʻai nui (ʻaina kakahiaka, ʻaina awakea, a me ka pāʻina). I ka hopena o ke aʻo ʻana, ʻo 43.6% (nā hui kīʻaha nui) a me 42.8% (hui ʻaina kakahiaka) o nā mea maʻi i loaʻa ma lalo o 7% HbA1c. Ua hōʻike ʻia kahi maʻi i ka 14.7% a me 15.5% o nā mea maʻi, a me ka hypoglycemia hōʻailona ma 5.8% a me 2.2% o nā mea maʻi i ka pāʻina nui a me nā pāʻina kakahiaka.
Hoʻohui hou aku i ka hoʻohui pū ʻana me ka sulfonylurea a i ʻole me ka hui pū me ka metformin.
Papa 3: ʻO ka haʻawina hoʻokele placebo i hui pū me ka sulfonylurea (hopena 24-pule).
Hoʻohui hou aku i ka hoʻohui pū ʻana me pioglitazone a i hui pū ʻia me metformin.
I loko o kahi haʻawina hōʻike maʻi ma nā maʻi e ʻike ʻole i ka loaʻa ʻana ma ka pioglitazone, ka hoʻohui o lixisenatide i pioglitazone i hui pū a i ʻole metformin a i ka hopena o ka hopena mālama 24 mau he hopena i hopena ia i ka hōʻemi o ka HbA1c mai ka punawai e 0.90% i hoʻohālikelike ʻia me ka hoʻohaʻahaʻa ʻana. mai ka pae mua o 0.34% i ka hui placebo. I ka hopena o ka mālama mālama 24-wiki ma hope, he 52.3% o nā maʻi e loaʻa ana i ka lixisenatide he HbA1
c nā emi ma lalo o 7% i hoʻohālikelike ʻia me 26,4% i ka hui placebo.
I ka wā nui o ka hopena pule 24 he mau pule, ʻike ʻia ka loiloi he 23,5% i ka hui lixisenatide hoʻohālikelike ʻia me 10,6% i ka hui plasebo, nā hihia o ka hypoglycemia hōʻailona ma 3.4% o nā mea maʻi i mālama ʻia me ka lixisenatide, i hoʻohālikelike ʻia me 1.2% pūpū hoʻonohonoho.
ʻO ka hui pū kekahi me ka insulin basal Lixumia, i hoʻohuihui ʻia me ka insulin basal wale nō, a i hui pū ʻia me ka basal insulin a me ka metformin, a i hui pū ʻia me ka basal insulin a me ka sulfonylurea, i hopena i ka hoʻoliʻina nui statistically i HbA1c a me 2 mau hola postprandial glucose ma hope o ka hoʻāʻo. ʻai ʻai plasebo.
Papa 4: ʻO nā haʻawina hoʻokele placebo i hui pū me ka insulin basal (hopena 24-pule).
Ua hoʻokele ʻia kahi haʻawina ma nā maʻi e loaʻa ʻole i ka insulin, ka mea i ʻole o lākou i mālama i nā ʻaina antidiabetic waha. Ua komo pū ʻia kēia noiʻi i kahi manawa mākaukau he 12 mau pule me ka hoʻomehana ʻana o ka glucose glargine a me ka titration a me ka mālama manawa 24-wiki i loko o ka mea e loaʻa ai i nā mea maʻi a lixisenatide a i kahi papa paha i ka hui pū me ka insulin glargine a metformin me i ʻole thiazolidinediones. I loko o kēia manawa, hoʻomehana mau ka insulin glargine.
I ka wā hoʻomākaukau o 12 mau hebedoma, ʻo ka hoʻohui a me ka titration o ka glargine insulin e alakaʻi i kahi hōʻemi i ka HbA1c o kahi o 1%.
ʻO ka hoʻohui i ka lixisenatide ka hopena i ka hōʻemi nui loa i ka HbA1 mai ka 0.71% i ka hui lixisenatide hoʻohālikelike ʻia me 0.40% i ka hui plasebo. Ma ka hopena o ka mālama mālama 24-wiki, he 56.3% o nā mea maʻi e hoʻohana ana i ka lixisenatide kahi hōkū HbA1 ma kahi o 7% e hoʻohālikelike ʻia me 38.5% i ka hui plasebo.
I ka manawa o 24 pule pule, ʻo 22.4% o nā mea maʻi i mālama ʻia me ka lixisenatide i hōʻike ʻia ma kahi o ka hypoglycemia symptomatic hoʻokahi, i hoʻohālikelike ʻia me 13.5% i ka hui plasebo.
Ua hoʻonui ʻia ka ulu o ka hypoglycemia i loko o nā wiki 6 mua o ka mālama ʻana i ka lixisenatide pūʻulu, a ua like ia me ka hui pletebo.
Ka ʻoli ʻana o ka glucose glucose.
I loko o kahi haʻawina hoʻokele pletebo i ka hopena o ka mālama 24-pule, ka hoʻokeo ʻana i ka hoʻōla glucose plasma mai ka palena hana i loaʻa me ka hana ʻo Lixumia mai 0.42 mmol / L a i ka 1,19 mmol / L.
ʻO ke pae o ka glucose postprandial.
Ma kahi o Lixumia ka hopena i hōʻemi ʻia i ka glucose i hoʻihoʻi ʻia i ka 2 mau hola ma hope o ka pāʻina hoʻāʻo ʻana, ua ʻoi aku ka maikaʻi o ka placebo, me ka manaʻo ʻole o ka hana maʻamau.
Ma ka laulā, i nā ʻikepili āpau kahi i ana ai i nā pae o ka glucose postprandial, me Lixumia i ka pau o ka mālama 24-wiki, ʻo ka hōʻemi ʻana mai ka pae ʻana mai ka palena mai 4.51 a 7.96 mmol / L. Mai 26.2% a 46.8% o nā mea maʻi, ʻo ka hala o ka glucose i kau iho nei mau hola he 2 ma lalo o 7.8 mmol / L (140.4 mg / dl).
Kau ka paona.
I ka hopena o ka hopena mālama 24 mau hebedoma mua loa, ʻo Lixumia i hui pū me ka metformin a me / a i ʻole ka sulfonylurea i nā hoʻokolohua āpau i alakaʻi i ka hoʻololi mau loa i ke kaupaona ʻana o ke kino e kū ana mai –1.76 kg a i -2.96 kg. ʻO ka hoʻololi ʻana i ke kaumaha o ke kino mai ka pae mua ma ka pae mai -0.38 kg a –1.80 kg i nānā ʻia i nā mea maʻi e loaʻa ana i ka lixisenatide i hui pū ʻia me ka nui o nā kūlike o ka insulin basal, a i hui pū me ka metformin a i ʻole sulfonylurea.
I nā poʻe maʻi i hoʻomaka mua i ka hoʻohana ʻana i ka insulin, i ka hui lixisenatide, ua noho kino ʻole ke kino o ke kino, akā, ma ka hui pletebo i hōʻike ʻia.
Ma nā haʻawina lōʻihi e lōʻihi a hiki i ka 76 wiki, e hoʻomau ana ka nui o ka paona.
ʻAʻole hilinaʻi ka mea kaupaona i ka neʻe ʻana o ka mokuʻala a me ka luaʻi.
Koiā hana Beta.
Ua hōʻike ʻia nā haʻawina hauoli o Lixumia i ka hana hoʻonā beta hoʻoponopono hou e like me ke ana ʻia e ka loiloi loiloi cell cellostatic home (HOMO-β / HOMA-β).
ʻO ka hoʻihoʻi hou i ka hana mua o ka mea huna o ka insulin a me ka hoʻomaikaʻi ʻana i ka lua o ka hana huna o ka insulin i ka pane ʻana i kahi inikini bolus intravenous e pili ana i ka glucose i mālama ʻia ma hope o hoʻokahi awhi hoʻokahi o Lixumia i loko o nā mea maʻi me ka maʻi diabetes type 2 (n = 20).
ʻO ka loiloi o ka ʻōnaehana cardiovascular.
I nā hoʻokolohua āpau i hoʻomalu ʻia i ka maʻi III, ʻaʻole i hōʻike ʻia nā mea maʻi me ka maʻi diabetes type 2 i ka hoʻonui o ka nui o ka puʻuwai ma waena.
I ka papa hoʻokele hoʻomalu i ka pletebo i hoʻolaʻa ʻia e placebo, ua nui ka emi o ka nui o ka systolic a me ka diastolic blood pressure, kēlā me kēia manawa, i ka 2.1 mm RT. ʻAniā. a i oi aku mm 1,5mmHg. ʻAniā.
Meta-kaʻo ʻana o nā hanana cardiovascular kū hoʻokahi i ka make (make ma muli o nā kumu cardiovascular, nonfatal myocardial infarction, nonfatal stroke, hospitalization due to unstable angina, hospitalization due to heart heart and revascularization of coronary arteries) in 8 placebo-control trial of the III phase, ka mea i loaʻa i nā poʻe maʻi o 2,673 me ka maʻi diabetes type 2 e loaʻa ana i ka lixisenatide a me 1,448 nā mea maʻi e loaʻa ana i ka placebo i hōʻike i ka palena o ka waihona o 1.03 (95% interval interval 0.64, 1.66) no ka lixis Atid hoʻohālike me ka placebo.
ʻO ka nui o nā hanana i nā hoʻokolohua lapaʻau he liʻiliʻi (1.9% i nā mea maʻi e loaʻa ana i ka lixisenatide a me 1,8% i loko o nā maʻi e loaʻa ana i ka placebo), ʻaʻole ia e ʻae i nā hopena hopena.
ʻO ka hōʻeha ʻana o nā hanana cardiovascular kūwaho (lixisenatide versus plasebo) ʻo: ka make ma muli o nā kumu cardiovascular (0.3% kū'ē i 0.3%), infarction myocardial nonfatal (0.4% kū'ē i 0.4 %), non-fatal stroke (0.7% hoʻohālikelike ʻia me 0.4%), nā mālama maʻi ma muli o ka angina hiki ʻole (0 hoʻohālikelike ʻia i 0.1%), hoʻokipa maʻi ma muli o ka puʻuwai naʻau (0.1% hoʻohālikelike ʻia i 0) , coronary arasiale revascularization (0.7% kūlike 1.0%).
Pharmacokinetics: Hoʻopuka.
Ma hope o ka hoʻomalu ʻana i ka subcutaneous i nā poʻe maʻi me ka maʻi diabetes type 2, ʻo ka wikiwiki o ka emi ʻana o ka lixisenatide, inā hoʻi i ka ʻimi i ka lawelawe. Ka nānā ʻole o ka pāʻana a inā paha i hoʻohana ʻia ka lixisenatide ma hoʻokahi a i ʻole ka nui o nā koina, i nā mea maʻi me ka maʻi type 2, ʻo ka pākāwā tmax ka 1 i ka 3.5 mau hola. No ka mālamaʻana i ka hoʻokele subcutaneous o lixisenatide i ka ʻōpū, ka ʻūhā a me nā poʻohiwi paha, ʻaʻohe ʻano nui o ke kikowaena o ka pā o ka hoʻopili ʻana.
Kahele.
ʻO Lixisenatide kahi pae paʻakikī o ka nakinaki ʻana (55%) i nā protein o kānaka.
ʻO ka nui ʻike ka laha ma hope o ka hoʻokele subutaneus o lixisenatide (Vz / F) ma kahi o 100 L.
ʻO Biotransformation a me ka hoʻopuka.
E like me ka peptide, ua hoʻopio ʻia ka lixisenatide e ka kānana glomerular i ukali ʻia e ka puna tubular me ka wā e hōʻeha nei ka metabolic, ke alakaʻi nei i ka hoʻokumu ʻana o nā peptides liʻiliʻi a me nā waikawa amino, ka mea i hoʻohui pū ʻia i ka protein metabolism. Ma hope o ka hoʻomoe ʻana i ka nui o nā maʻi i nā maʻi me ka diabetes type 2, ʻo ka ʻokoʻa hapalua hapalua hapalua-ola ka palena o 3 mau hola a me ka nui o nā hoʻomaʻamaʻa ʻike (CL / F) ma kahi o 35 l / h.
Nā Pākuʻi Nui:
ʻO ka maʻi me ka hana renal impaired.
I nā mea maʻi me ka hana renal maʻamau a me nā mea maʻi me ka hana ʻole o ka papalū ʻula (ʻo ka hana maʻa ma ka helu ʻana i hōʻuluʻulu ʻia e ka ʻōlelo ʻo Cockcroft-Gault, 50-80 ml / min), ʻaʻohe ʻano nui i ka Cmax a me PPK o ka lixisenatide. I nā mea maʻi me ka maʻi renal éduction maʻalahi (hōʻea i hana ma kahi o 30-50 ml / min), ʻo ka AUC hōʻailona (wahi ma lalo o ka pihi) i hoʻonui ʻia i ka 24%, a i nā mea maʻi me ka maʻi haneli kino (hana ʻana o ka creinine o 15-30 ml / min) - e 46 %
ʻO nā mea maʻi me ka hana pūlima hemahema.
No ka mea, ua hoʻopiʻi ʻia ka lixisenatide e nā ʻōpū, ʻaʻole i komo nā mea maʻi me ka maʻi lela paʻa ʻole a hopena i loko o nā haʻawina ʻo pharmacokinetic. ʻAʻole manaʻo ʻia ka neʻe hematic e pili i ka pharmacokinetics o lixisenatide.
Paul
ʻAʻohe hopena koʻikoʻi ʻo Gender i ka pharmacokinetics o lixisenatide.
Kāhea.
Wahi a nā hopena o nā haʻawina pharmacokinetic i nā poʻe maʻi o ka lāhui Caucasian, Iapana a me Kaina, ʻaʻole i loaʻa i ka hopena koʻikoʻi ka hopena o ka pharmacokinetics o lixisenatide.
ʻO nā maʻi maʻi.
ʻAʻole loaʻa kahi hopena koʻikoʻi o ka makahiki ma ka pharmacokinetics o lixisenatide. Ma kahi noiʻi pharmacokinetic ma nā maʻi maʻi maʻi ʻole maʻi maʻi, ka hoʻohana ʻana o ka lixisenatide 20 gg i loko o ka hui o nā mea maʻi (11 mau mea maʻi 65 a 74 mau makahiki he 7 mau mea maʻi ʻoono he ʻ75 makahiki), e alakaʻi ana i ka piʻi maʻamau o ka PPC o ka lixisenatide e 29%. hoʻohālikelike ʻia me 18 nā mea maʻi 18 a 45 paha mau makahiki he mea paha, ua pili ʻia me ka hoʻēmi ʻia ʻana o ka hana hula ma ka ʻelemakule.
Kau ka paona.
ʻAʻole loaʻa ka hopena o ke kino i ka hopena koʻikoʻi ma ka hōʻike ʻo PPK no ka lixisenatide.

Nā ʻihi ʻaoʻao o Liksumiya

ʻO ka wehewehe pōkole o ka ʻaoʻao palekana.
ʻOi aku ma mua o ka 2,600 mau mea maʻi ma 8 mau haʻawina nui i hoʻokele ʻia i ka papa lālau a i ka hana III paha me ka mana ikaika i loaʻa iā Lixumia i loko o ka monotherapy a i hui pū paha me metformin, sulfonylurea (me ka ʻole a metformin) a i ʻole basal insulin (me ka ʻole o ka metformin a me ka sulfonylurea a i ʻole me ia ʻole).
ʻO nā hana ʻino i hōʻike ʻia i ka wā o ka hoʻokolohua ʻana i nā maʻi ma ke ʻano he nausea, luaʻi, a me nā hōʻeha. ʻO ka pane ka maʻa mau a maʻalahi.
Aia nō kekahi mau hihia a ka ha hypoglycemia (i ka wā i hoʻohana ʻia ai ʻo Lixumia i hui pū me ka sulfonylurea a me / a me ke ʻano basal) a me ke poʻo.
Ua nānā ʻia nā hopena alerine i ka 0.4% o nā mea maʻi e hoʻohana ana iā Lixumia.
Aia ma lalo iho nā hopena ʻino i loaʻa ai i ka pinepine o> 5%, inā ʻoi aku ka nui o ka ulu ʻana ma waena o nā mea maʻi e loaʻa iā Lixumia ma waena o nā mea maʻi e loaʻa ana i nā lāʻau hoʻohālikelike āpau, i hui pū ʻia ka hopena ʻino me ka pinepine o ≥1% ma ka hui o nā maʻi e loaʻa ana iā Lixumia. ina he 2 mau koina ka nui o ka hiki ana mai o ka pinepine o ka hui o na mea maʻi e loaʻa ana i nā lāʻau lapaʻau hoʻohālikelike āpau.
ʻO nā hopena hoʻonā i hoʻokumu ʻia i nā hoʻokolokolo plebo-control and phase III me ka hoʻomohala paʻa i ka wā o ka mālama lapaʻau holoʻokoʻa (me ka nui o nā manawa ma mua o ka 24 ma ka manawa lapaʻau nui 24 mau pule i nā haʻawina me ≥76 mau pule o ka holoʻokoʻa).
Hoʻopaʻa pinepine ʻia (≥1 / 10):
- ka hypoglycemia (i hui pū me ka sulfonylurea a me / a i ke ʻano basal)
lie kanikela
- nausea, luaʻi, ʻeha
I nā manawa pinepine (≥1 / 100 ma mua o ka maʻi - ka maʻi, ke kaumaha o ke ala o ka ʻōpū, cystitis, maʻi maʻi
- hypoglycemia (i hui pū me ka metformin kūʻokoʻa)
- ʻeha, mau ka ʻeha
- dyspepsia
- ʻeha hope
- ʻeha ma ka wahi i ʻōlelo ʻia
Hoʻohālikelike (≥1 / 1000 a - i ka hopena anaphylactic
- urticaria

ʻO ka ho'ākāka o kēlā me kēia ʻino maikaʻi ʻole:
Hypoglycemia.
I nā mea maʻi e lawe ana iā Lixumia ma ka monotherapy, ua hele mai ka hōʻailona hypoglycemia ma 1.7% o nā mea maʻi e loaʻa ana i ka lixisenatide, a ma ka 1.6% o nā mea maʻi e loaʻa ana i ka placebo. I ka manawa i hoʻohana ʻia ai ʻo Lixumia i ka hui pū me ka metformin i ka wā mālama holoʻokoʻa, hele mai ka hōʻailona hypoglycemia ma ka 7.0% o nā maʻi e loaʻa ana i ka lixisenatide a me 4.8% o nā maʻi e loaʻa ana i ka placebo.
I nā mea maʻi e lawe ana iā Lixumia i hui pū me ka sulfonylurea a me ka metformin, hele mai ka hōʻailona hypoglycemia i ka 22.0% o nā mea maʻi e loaʻa ana i ka lixisenatide a me 18,4% o nā mea maʻi e loaʻa ana i ka placebo (3.6% kūʻokoʻa kūʻokoʻa) i ka wā mālama holoʻokoʻa. I ka manawa i hoʻohana ʻia ai ʻo Lixumia i hui pū me ka insulin basal me ʻole a i ʻole ka metformin i ka wā mālama holoʻokoʻa, hele mai ka hōʻailona hypoglycemia ma ka 42.1% o nā mea maʻi me ka lixisenatide a ma ka 38.9% o ka poʻe i loaʻa i ka placebo (3.2% o ka ʻokoʻa kūʻokoʻa).
I ka manawa i hoʻohana ʻia ʻo Lixumia i ka hui pū me ka sulfonylurea i ka manawa holoʻokoʻa holoʻokoʻa, hele mai ka hōʻailona hypoglycemia i ka 22.7% o nā maʻi e loaʻa ana i ka lixisenatide, hoʻohālikelike ʻia me 15.2% e loaʻa ana i ka placebo (7.5% kūʻokoʻa kūʻokoʻa). I ka manawa i hoʻohana ʻia ʻo Lixumia i hui pū me ka sulfonylurea a me ka insulin basal, hele mai ka hōʻailona hypoglycemia ma 47.2% o nā maʻi e loaʻa ana i ka lixisenatide, hoʻohālikelike ʻia me 21.6% e loaʻa ana i ka placebo (25.6% o ka ʻokoʻa kūʻokoʻa).
Ma keʻano holoʻokoʻa, i ka wā o ka mālama lapaʻau āpau i nā aʻo hoʻokele i ka plasebo o ka manawa III, ʻo ka nui o ka hōʻeha o ka hypoglycemia maʻi (0.4% i nā mea maʻi i mālama ʻia me lixisenatide a me 0.2% i nā mea maʻi i mālama ʻia me ka pletebo).
Nā kipi o ka gastrointestinal tract.
I ka hana nui o 24-wiki lapaʻau, ʻae a me ka luaʻi, ʻo ia ka nui loa o ka hōʻike. Ua ʻoi aku ka kiʻekiʻe o ka uha i ka lixisenatide pūʻulu (26.1%) i hoʻohālikelike ʻia i ka hui plasebo (6.2%), a ua piʻi ke kiʻekiʻe o ka luaʻi ma ka lixisenatide pūʻulu (10.5%) hoʻohālikelike i ka hui plasebo (1.8 %).
ʻO ka maʻi ka hapanui a me ka transient a hele i loko o nā 3 mau pule mua ma hope o ka hoʻomaka ʻana o ka mālama ʻana. Ma hope aku, ma hope o nā hebedoma e hiki mai ana, e hoʻohaʻahaʻa i ka lohi.
Nā wahi hōʻike ma ka wahi ʻōlelo.
I loko o ka manawa lapaʻau nui 24-pule, ua loaʻa nā hopena ma ke kahua maʻi i ka 3.9% o nā mea maʻi e loaʻa ana iā Lixumia, a ua ʻike ʻia hoʻi nā ʻano ma ka wahi i ka maʻi lapaʻau ma ka 1,4% o nā mea maʻi e loaʻa ana i ka placebo.
ʻO ka hapanui o nā hopena kūpono mai ka hōʻeha a ʻaʻole i hoʻōki ka hana.
Immunogenicity
Ma muli o nā ʻano maʻi immunogenic o nā lāʻau e loaʻa ai ka protein a me ka peptides, ma hope o ka mālama ʻana me Lixumia, hiki i nā mea maʻi ke hoʻomohala i nā antibodies i ka lixisenatide, a ma ka hopena o ka hopena pule 24-pule ma nā haʻawina i hoʻomoe ʻia ma plebo i 69.8% o nā mea maʻi e loaʻa ana i ka lixisenatide, ua hoʻokumu ʻia ke kūlana antibody kūpono. I ka hopena o ka manawa lapaʻau o ka wiki holoʻokoʻa 76, ua like ka like o ka nui o ka maʻi o nā maʻi seropositive. I ka hopena o ka hopena mālama 24 mau pule he nui, ma ka 32.2% o nā mea maʻi me ke kūlana antibi i ke ʻano, ua ʻoi aku ka pae ʻana o ka antibody ma lalo o ka palena palena o ka lehulehu ana, a ma ka hopena o ke ana o ka lā mālama 76-wiki i 44.7% o nā mea maʻi, ua hoʻokiʻoki ʻia ka antibody ma luna o ka palena palena o ka helu . ^ E Ha yM. Ma hope o ka pau ʻana o ka mālama ʻana, hoʻomau ka nānā ʻana i kekahi o nā mea maʻi seropositive, i loko o 3 mau mahina ua hoʻemi ka hapa pakeneka ma kahi o 90%, a ma hope o 6 mau mahina a ʻoi aʻe paha a hiki i 30%.
ʻO ka loli i ka HbA1c mai ka palena kahua e like me ka kūlike o ke kūlana antibody (maikaʻi a maikaʻi ʻole paha).
ʻO nā mea maʻi me ka helu HbA1c i loaʻa i ka lixisenatide, ʻo 79.3% paha i loaʻa i kahi kūlana antibody maikaʻi ʻole a i ʻole ke ʻano o ka ʻohiʻohi ʻana ma lalo o ka palena o ka helu ana, ʻoiai ko 20.7% o nā mea maʻi i loaʻa i ka ʻōpū o ka antibody.Ma loko o ka hui o nā mea maʻi (5.2%) me ka kiʻekiʻe o ka ʻōpū o ka antibody, ʻo ka nui o ka hoʻonui ʻia ʻana o ka HbA1c ma ka hebedoma 24 a me ka pule i loko o ka nui o ke ana o ka maʻi lapaʻau, akā, aia kahi ʻano pane glycemic, a ʻaʻole i hōʻemi ka 1,9%. HbA1c.
ʻAʻole ʻae ke kūlana o nā antibodies (maikaʻi a maikaʻi paha) e wānana i ka emi ʻana o ka HbA1c i nā maʻi maʻi pilikino.
ʻAʻohe ʻano iki o ka ʻike palekana palekana i ka maʻi, me ka ʻike ʻole i ke kūlana antibody, koe wale nō no ka hoʻonui ʻana o ka nui o nā hopena ma ka wahi maʻi (ʻoi aku ka manawa mālama, 4.7% i nā mea maʻi me ke kūlana antibody kūpono, hoʻohālikelike ʻia me 2.5% nā mea maʻi seronegative). ʻO ka hapanui o ka pane ma ka wahi i ʻōlelo ʻia, ʻoluʻolu ʻole i ke kūlana antibody.
ʻAʻohe mea hoʻoliʻi ka hoʻohālikelike ʻana i nā kūlohelohe maoli a i ʻole ka endogenous GLP-1.
Allergic hopena pili.
I ka wā nui o ka mālama 24-wiki, pili i nā hopena alia i ka lixisenatide (e like me ka anaphylactic reaksi, angioedema, a me urticaria) i loaʻa i ka 0.4% o nā mea maʻi i mālama ʻia me lixisenatide, ʻoiai paha ka hopena o ke alaka i hele liʻiliʻi i 0.1% o nā maʻi e loaʻa ana i ka placebo.
Ua hoʻokū ʻia nā hopena anaphylactic i ka 0.2% o nā mea maʻi e loaʻa ana i ka lixisenatide, i hoʻohālikelike ʻia me ka waiho ʻole ʻana o nā hopena i ka hui plasebo.
ʻO ka hapa nui o nā maʻi kūlohelohe i hoʻonohonoho ʻia i ka paʻakikī. ʻO kahi hihia o ka anaphylactoid ʻano mea i hoʻokumu ʻia ma ka wā o nā hoʻokolohua lapaʻau o lixisenatide.
ʻAne hoihoi.
Ma nā haʻawina e pili ana i nā limahana olakino, ka nui o ka neʻe ʻana ma ka naʻau o ka puʻuwai e nānā ma hope o ke alakaʻi ʻana o 20 μg o lixisenatide. ʻO ka arrhythmia o Cardiac, inā paha, ka tachycardia (0.8% hoʻohālikelike ʻia me ka hōʻea ʻana o ka lāʻau lapaʻau.
I ka manawa nui o ka mālama 24-wiki lapaʻau, ʻo ka ulu ʻana o ka hoʻopau ʻana ma muli o nā hanana pōʻino, ʻo 7.4% i loko o ka hui Lixumia i hoʻohālikelike ʻia me 3.2% i ka hui plasebo. ʻO ka hopena maʻamau e pili ana i ka hoʻokuʻu ʻana i ka mālama ʻana i ka hui lixisenatide i loko o ka maʻi (3.1%) a me ka luaʻi (1.2%).
Ke hōʻike nei i nā manaʻo maikaʻiʻole.
He mea nui ia e hōʻike i nā pōʻino i hopohopo ma hope o ka hoʻopaʻa inoa ʻana i ka lāʻau lapaʻau. Hāʻawi kēia iā ʻoe e hoʻomau i ka nānā ʻana i ka uku o ka pōmaikaʻi / hōʻemi i ka lāʻau. Noi ʻia nā limahana olakino e hōʻike i nā pōʻino i manaʻo ʻia ma o ka ʻōnaehana hoʻolaha ninaninau.

ʻAʻoheʻike therapeutic i hoʻohana me ka hoʻohana ʻana o lixisenatide i nā maʻi me nā maʻi 1 type mellitus; ʻaʻole pono e hoʻohana ʻia i kēia mau maʻi.
ʻAʻole pono e hoʻohana ʻo Lixisenatide e mālama i ka maʻi maʻi ketoacidosis maʻi.
ʻO ka pancreatitis acute.
ʻO ka hoʻohana ʻana i ka agonists receptor-like peptide-1 (GLP-1) i hoʻopili ʻia me ka hopena o ka hoʻomohala ʻana i ka maʻi pancreatitis.
Ua hōʻike ʻia he mau hanana nui o ka pancreatitis me ka hoʻohana ʻana i ka lixisenatide, ʻoiai ʻaʻole i hoʻokū ʻia kahi pilina kumu.
Pono e hoʻomaopopo i ka mea maʻi e pili ana i nā hōʻailona maʻamau o ka maʻi pancreatitis: ka hoʻomau, hōʻeha o ka ʻōpū nui. Inā kānalua ka pancreatitis, pono ia e pani i ka hoʻohana ʻana i ka lixisenatide, inā ua hoʻopaʻa ʻia ka maʻi pancreatitis, ʻaʻole pono ke hoʻomau ʻia ka hoʻohana ʻana o ka lixisenatide. Pono e hoʻomaʻemaʻe ʻia i ka wā i hoʻohana ʻia ai i nā mea maʻi ma hope o ka maʻi pancreatitis.
ʻO nā maʻi maʻi gastrointestinal.
ʻO ka hoʻohana ʻana i nā agonists o nā mea hoʻokipa GLP-1 e pili ana me nā hopena ʻino loa mai ka gastrointestinal tract.
ʻAʻole i aʻo ʻia ʻo Lixisenatide i nā mea maʻi i nā maʻi maʻi gastrointestinal, me loko o ka gastroparesis koʻikoʻi, a no kēia kumu, ʻaʻole i ʻōlelo ʻia ka hoʻohana ʻana o ka lixisenatide.
Hola paʻa kino hana.
Aia keʻike i ke kaupaona ʻana i ka mea maʻi me ka hana ʻana o ka maʻi lēpaʻa (ʻo ka cleinine clearance 30-50 ml / min), ʻaʻohe mea e loaʻa ai ka hopena therapeutic i nā maʻi me ka hana ʻole o ka maʻi homa (ʻo ka hana ma lalo o ka hana ma kahi o 30 ml / min) a i loko o ka poʻe maʻi ma ke kahua o ka maʻi. nā pōpō. I nā mea maʻi me ka hana renal moderate, pono e hoʻohana ʻia ʻo Lixumia me ka akahele. I ka poʻe maʻi me ka hana renal impaired koʻikoʻi a i ʻole nā ​​mea maʻi i ka ʻoihana kūleʻa o ka maʻi ʻōiwi, ʻaʻole ʻia ka hoʻohana ʻana (e nānā "Dosage and Administration" a me "Pharmacokinetics").
Hypoglycemia.
ʻO nā maʻi e loaʻa ana iā Lixumia me ka sulfonylurea a i ʻole ka basal insulin e loaʻa paha ka piʻi nui o ka hypoglycemia. No ka hōʻemi i ka hopena o ka hypoglycemia, hiki ke hoʻemi i ka nui o ka sulfonylurea a i ʻole ke basal insulin (e ʻike i "Dosage and Administration"). ʻAʻole pono e hoʻohana ʻo Lixumia i ka hui pū me ka insulin basal a me ka sulfonylurea ma muli o ka hoʻonui nui o ka hypoglycemia.
Nā lāʻau lapaʻau hoʻohuli
Ke hoʻoluhi nei i ka hoʻomaha ʻana o nā ʻōpū o ka gastric me ka hoʻohana ʻana i ka lixisenatide e hōʻemi ʻia i ka helu o ka hoʻoulu ʻana o nā lāʻau lapaʻau. I nā mea maʻi e loaʻa ana i nā lāʻau lapaʻau e koi ai i ka hoʻoulu ʻana o ka gastrointestinal, ka nānā ʻana o nā mea lapaʻau, a i nā lāʻau lapaʻau me kahi pākīkī liʻiliʻi pōkole, pono e hoʻohana ʻia ʻo Lixumia me ka akahele. Hāʻawi ʻia nā ʻōlelo loiloi kūikawā e pili ana i ka hoʻohana ʻana i ia mau lāʻau i ka mahele "Nā Pānaʻi Kūloko".
ʻO nā lōluhi i hoʻonohonoho ʻole ʻia.
ʻAʻole i aʻo ʻia ʻo Lixisenatide me ka mea hoʻohui me dipeptidyl peptidase-4 (DPP-4) inhibitors.
He palena liʻiliʻi ka ʻike ʻana i nā maʻi me ka puʻuwai naʻau congestive.
Naʻu?
ʻO ka poʻe maʻi e loaʻa ana i ka mālama ʻana me Lixumia e hoʻomaopopo pono i ka hopena o ka hopena o ka ʻōpio ma muli o nā hopena maikaʻi loa mai ka gastrointestinal tract a mālama pono i ka pale ʻana i ka hypovolemia.
Nā mea kūʻai.
Loaʻa ka lāʻau lāʻau i ka metacresol, hiki i nā mea kūlohelohe.
Nā wahine hānau keiki.
ʻAʻole ʻōlelo ʻo Lixumia i nā wahine o nā keiki hānai keiki ʻaʻole i hoʻohana i nā contraceptives.
Kahawai
ʻAʻole lawa nā data ma ka hoʻohana ʻana o Lixumia i nā wahine hāpai. Ua hōʻike ʻia nā haʻawina preclinical i nā mānoanoa reproduction.
ʻAʻole maopopo ka ʻike nui i ke kanaka.
ʻAʻole pono e hoʻohana ʻo Lixumia i ka wā hāpai. Ma kahi o ka ʻōlelo, ua ʻōlelo ʻia mai ka insulin.
Inā makemake ka mea maʻi e hāpai a hāpai a hāpai paha, ua hoʻōki ʻia ka lāʻau me Lixumia.
Hoʻokaumana.
ʻAʻole i ʻike ʻia inā hoʻokomo ʻo Lixumia i ka waiū umauma o ke kanaka. ʻAʻole pono e hoʻohana ʻo Lixumia i ka wā lactation.
Pūnaewele.
ʻAʻole hōʻike nā haʻawina preclinical i kahi hopena maikaʻi i ka ulu ʻana.
Nā hiʻohiʻona o ka hopena o ka lāʻau lapaʻau ma ka hiki ke hoʻokau i kahi kaʻa a lawelawe paha.
ʻAʻole pili ʻo Lyskumia a i ʻole ia i kahi hopena iki i ka hiki ke kahe i kahi kaʻa a mīkini paha. I ka manawa e lawe pū ʻia me ka sulfonylurea a i ʻole basal insulin, pono e aʻo ʻia nā mea maʻi e mālama i ka pale ʻana e pale aku ai i ka hypoglycemia i ke holo ʻana a i ka hoʻohana ʻana i nā mīkini.

Nā kūlana mālama.
E kūʻai ma kahi mahana o 2 degere a hiki i ka 8 mau degere C ma kahi wahi ʻino. Mai hoʻokaʻawale. E mālama i kahi manuahi.
Ma hope o ka hoʻohana mua ʻana, hiki ke hoʻohana ʻia i ka peni ʻo ka syringe no 14 mau lā ma ke aniani ʻaʻole eʻoi aku ma mua o 30 tikelika C. Mai hoʻokaʻawale.
Mai mālama i nā keiki.

Nā ʻōkuhi no ka hoʻohana syringe pen Lixumia
Ma mua o ka hoʻohana ʻana i ka penikala ʻāhane Lixumia, e heluhelu pono i nā ʻōlelo.
Mālama i kēia mau ʻōlelo olakino no ka hoʻohana ʻana i ka lāʻau lapaʻau no ka haʻi aku e hiki mai ana.
ʻO Lixumia kahi peni syringe mua i hoʻopiha ʻia no ka inikohu e loaʻa ana he 14 mau kakona. ʻO kēlā me kēia pākēneka aia 10 g a 20 μg o lixisenatide ma 0.2 ml.
• Hana i kahi hōʻeha hoʻokahi no kēlā me kēia lā.
• Aia i kēlā me kēia peni penikala Lixumium he 14 mau ʻōlelo piha mua. ʻAʻole pono ia mau pākahi i ana e hoʻopaʻa ʻia.
• Ma mua o ka hoʻohana ʻana i ka peni syringe, e nīnau aku i kāu kauka e pili ana i ka lawelawe ʻana i ka lāʻau lapaʻau.
• Inā 'aʻole hiki ke hahai iā' oe i nā kuhikuhi, a 'aʻole hiki iāʻoe ke kūʻai i ka peni like (no ka mea, inā he pilikia kou kiʻi), e lawe i ke kōkua o waho.
• ʻO kēia peni wale nō hoʻokahi wale nō. Hooleia ka ke ana ana.
• E ʻike mau i ka hana ʻana i ka hōʻailona e hoʻopaʻa pono ai ʻole ʻiliʻili ʻo Lixumia. E nānā pū i ka mālama paʻa ʻana.
Hiki ke hōʻeha ka hoʻohana ʻana i ka lāʻau.
• mai hoʻokaʻawale i ke kahe mai ka pahu pahu me ka hoʻohana ʻana i kahi syringe. ʻIke Hana
• E hoʻohana pono i nā pūlima pono e hoʻohana ʻia me Lixumia. E hoʻohana i nā mea pono pono mai ka 29 a 32 i ka peni ʻo Lixumia syringe ʻoi aku ka maikaʻi inā nīnau ʻoe i kāu kauka e pili ana i ka lōʻihi a me ke ana o ka pono.
• Inā hoʻopaʻa ʻia ʻo ia me ke kōkua i waho, pono e mālama pono e mālama i ka mea me ka pono. Inā ʻaʻole, hiki i ka hoʻouna.
• No kēlā me kēia inikini, hoʻohana pono i kahi lāʻau hou e pale aku ai i ka maʻi o Lixumia a i ʻole ke kūʻai ʻia.

Nā hōʻailona o ka lāʻau Lixumia

ʻO ka maʻi mellitus type 2 i ka pākeke e hoʻokō i ka mana glycemic i loko o nā poʻe maʻi e ʻike ʻole ʻia e ka maʻi mellitus e ka hoʻomau ʻia ʻana o ka maʻi hypoglycemic.

Hōʻike ʻia ʻo Lixumia i ka hui pū me nā huaʻōlelo hypoglycemic waha o kēia lā:

• metformin
• ka lāʻau hypoglycemic waha o ka hui sulfonylurea,
• ka hui ʻana o kēia mau lāʻau.

Hōʻike ʻia ʻo Lixumia i ka hui pū me ka insulin basal:

• in kahiki,
• i ka hui me metformin,
• i ka hui pū ʻana me kahi lāʻau kūlohelohe hypoglycemic o ka hui sulfonylurea.

Ka hoʻoponopono ʻia ʻana

ʻO ka ma mua mua he 10 micrograms o Lixumia i hoʻokahi manawa no ka lā 14.

A laila e hoʻonui ʻia ka lāʻau o Lixumia i 20 mcg i hoʻokahi lā. Kākoʻo kēia ʻāpana.

I ka manawa e hoʻohui pū ʻia ʻo Lixumia i kahi lāʻau metformin i loaʻa, hiki ke hoʻomau ʻia ʻo Metformin me ka loli ʻole o kona ʻano.

Ke hoʻohui ʻia ʻo Lixumia i ka lāʻau paʻa me ka lāʻau hypoglycemic oral o ka hui sulfonylurea a i ʻole ka hui ʻana o ka lālani hypoglycemic oral o ka hui o ka sulfonylurea a me ka insulin basal, e hōʻemi i ka hopena o ka hypoglycemia, hiki iā ʻoe ke noʻonoʻo i ka hōʻemi ʻana i ka hopena o ka lāʻau hypoglycemic oral o ka hui o ka sulfonylurea. Nā ʻōlelo kikoʻī ".

ʻAʻole pono ka hoʻohana ʻana i ka lāʻau Lixumia i ka nānā koʻikoʻi o ka neʻe o ka glucose i ke koko. Eia nō naʻe, i ka wā e hoʻohana pū ʻia me ka lālani hypoglycemic oral o ka hui sulfonylurea a i ʻole basal insulin, ka nānā ʻana o ka glucose o ke koko a i ʻole ka nānā pono ʻana (ka hoʻomalu ʻia e ka mea maʻi) o ka hoʻoliʻi ʻana o ka hoʻokaʻa glucose lā e koi ʻia e hoʻoponopono i ka ʻai ʻana o ka lāʻau hypoglycemic oral o ka hui o ka sulfonylurea a i ʻole basal insulin.

Nā hui ahonui kūikawā

Nā keiki a me nā ʻōpio ma lalo o 18

I kēia manawa, ʻo ka palekana a me ka loaʻa o ka lāʻau Lixumia i nā maʻi ma lalo o nā makahiki 18, ʻaʻole i aʻo ʻia ʻo ia.

Poʻe kānaka

ʻAʻole koi kekahi hoʻoponopono hoʻoponopono e koi ʻia ma ke ʻano o ka makahiki o ka mea maʻi.

ʻO nā maʻi me ka palaualohi maʻa

ʻAʻole koi ka hoʻoponopono hoʻoponopono ʻana i nā maʻi me nā hemahema o ka ate.

ʻO nā mea maʻi me ka maikaʻi ʻole o ka pūpū

ʻAʻole koi ʻia ka hoʻoponopono ʻana ma nā maʻi i nā mea maʻi me ka maikaʻi ʻole o ka renal (hōʻea i ka hana maanina 50-80 ml / min) a me ka hoʻomaʻamaʻa ʻana i ka renal moderate (clearanine clearance 30-50 ml / min).

ʻAʻoheʻike therapeutic me ka hoʻohana ʻana o Lixumia i nā mea maʻi me ka hōʻeha o ka renal maikaʻi ʻole (clearanine clearance emi mai i ka 30 ml / min) a i ʻole ka hopena ʻole o ka hanana, a no laila ka hoʻohana ʻana o Lixumia ma kēia pūʻulu o nā maʻi.

Hoʻohana ʻia ka lāʻau Lixumia i ka manawa 1 i ka lā ma mua o ka hola 1 ma mua o ka pāʻina mua i ka lā a i ʻole 1 hola ma mua o ka pāʻina ahiahi. Inā kāpī ʻia ka makeʻe ma hope aʻe, e lawe ʻia ma loko o 1 mau hola ma mua o ka ʻai ʻokoʻa. Hoʻohana ʻia ka lāʻau Lixumia a subcutaneously ma ka ʻāʻī, ka ʻōpū a i ʻole poʻohiwi paha. ʻAʻole hiki ke hoʻokele ʻia ka lāʻau Lixumia i ka hana intravenously a me intramuscularly. Ma mua o ka hoʻohana ʻana, pono e mālama i ka peni penikala ʻo Lixumia i loko o kahi friji i ke mahana o 2-8 ° C i loko o kāna pale e pale ai mai ka ʻike ʻana i ka mālamalama. Ma hope o ka hoʻohana mua ʻana, pono e mālama ʻia ka penikala ʻauhau ma Lixumia i kahi mahana ʻaʻole hohonu 30 ° C. Ma hope o kēlā me kēia hoʻohana, pono ke pani ʻia ʻo ka peni ʻo ka Lixumium me kahi pāpale i mea e pale ai i ka ʻike. ʻAʻole pono e mālama i ka Lixumia Syringe Pen me nā pāpale e hoʻopili ʻia. Mai hoʻohana i ka penina penu ʻo Lixumia i pau ia.

E hoʻokuʻu ʻia ka Lixumia Syringe Pen ma hope o 14 lā.

Loaʻa ka hopena

ʻO ka hapanui o nā hopena ʻokoʻa (HP) i hoʻoholo ʻia e like me: pinepine: ≥10%, pinepine: ≥1% - 76 mau wiki) i hele a me ka pinepine o> 5% (inā ua kiʻekiʻe ko lākou ʻōuli ma nā maʻi e lawe ana iā Lixumia i hoʻohālikelike ʻia me nā mea maʻi. ka lawe ʻana i nā lāʻau lapaʻau ʻē aʻe āpau, me ka plasebo), a me ka nūnē hoʻi o> 1% i nā mea maʻi ma ka pūʻulu Lixumia, inā ʻoi ka nui o ko lākou manawa ʻoi aku ka 2 o ka loaʻa ʻana o kēia HP i nā mea maʻi e loaʻa ana i kekahi o nā ʻano hoʻohālikelike (me ka pletebo) . ^ E Ha yM.

Nā maʻi maʻi a me nā maʻi parasit

ʻO ka maʻi pāpaʻi, nā ʻaoʻao ʻeha o ke ake ʻana.

ʻO ka huʻihuʻi me ka meaʻaiʻaiʻai

ʻO ka hypoglycemia e hana pū ana me nā maʻi lapaʻau (i ka wā e hoʻohana ai ʻo Lixumia i ka hui pū me ka lāʻau hypoglycemic waha o ka hui sulfonylurea a me / a i ʻole basal insulin).

ʻO nā maʻi o ka pūnao

Nā maʻi Gastrointestinal

ʻAno, hoʻopuka, ka ʻeha.

ʻO nā maʻi me ka hoʻopili ʻana o nā musculoskeletal

I nā mea maʻi e loaʻa ana iā Lixumia ma monotherapy a i hui pū me ka metformin, hypoglycemia me nā hōʻike kulana i ulu pinepine ʻia, a ʻo ka pinepine o nā maʻi i loaʻa iā Lixumia e like me kēlā me ka pletebo i ka wā mālama holoʻokoʻa.

I nā maʻi i hoʻolako ʻia ʻo Lixumia i hui pū me kahi lāʻau hypoglycemic waha o ka hui sulfonylurea a i ʻole basal insulin, ka ʻeha o ka hypoglycemia, ka mea i hui pū ʻia e nā maʻi maʻi.

I ka manawa holoʻokoʻa o ka mālama ʻana me Lixumia, ʻo ka nui o ka ulu ʻana o ka hypoglycemia e hana pū ana me nā maʻi maʻi ʻoi aku ka kiʻekiʻe ma mua o ka placebo, i ka manawa ua hoʻohana ʻia ʻo Lixumia e hui pū.

• me kahi lāʻau lapaʻau hypoglycemic waha o ka hui sulfonylurea a me ka metformin,
• me ka insulin monotherapy monotherapy,
• me ka hui pū ʻana o ka insulin basal a me ka metformin.

I ka manawa holoʻokoʻa o ka wā i hoʻohana ʻia ai ʻo Lixumia i hui pū me ka monotherapy me ka lāʻau hypoglycemic waha o ka hui o ka sulfonylurea, hypoglycemia me nā hōʻike pilikino i hana ʻia ma ka 22.7% o nā mea maʻi i mālama ʻia me Lixumia a ma 15.2% o nā mea maʻi i loaʻa iā pletebo.I ka manawa i hoʻohana ʻia ai ʻo Lixumia i ka hui pū ʻana me ka lālani hypoglycemic waha o ka hui sulfonylurea a me ka insulin basal, hypoglycemia me nā hōʻike hōʻike i loaʻa i ka 47.2% o nā mea maʻi i mālama ʻia me lixisenatide, a ma 21.6% o nā mea maʻi i mālama ʻia me ka pletebo.

Ma ka holoʻokoʻa, ma ka manawa holoʻokoʻa o ka lawe ʻana i ka lāʻau lapaʻau ma ka hoʻokolohua mau i nā maʻi haukapila III, ʻo ka hōʻeha o ka hypoglycemia koʻikoʻi me nā hōʻike hōʻike like ʻana me ka "infrequent" gradation (i ka 0.4% i nā maʻi nā maʻi e loaʻa iā Lixumia a ma 0.2% i nā mea maʻi e loaʻa ana i ka placebo) . ^ E Ha yM.

Nā maʻi Gastrointestinal

ʻO ka maʻi a me ka luaʻi, ʻo ka HP ka mea i hōʻike pinepine ʻia ma ka manawa mālama 24-pule. ʻO ke koʻikoʻi o ka maʻi pālahalaha ke kiʻekiʻe aku i nā maʻi nā maʻi me Lixumia (26.1%) ma mua o nā mea maʻi i mālama ʻia me ka placebo (6.2%) ʻO ka ulu ʻana o ka hoʻopuka a ʻoi aku ka kiʻekiʻe o nā maʻi i mālama ʻia me Lixumia (10,5%) ma mua o nā mea maʻi i mālama ʻia me ka pletebo (1.8%). ʻO kēia mau HPs i ka maʻalahi a me ka transient a hele i loko o nā 3 mau pule mua ma hope o ka hoʻomaka ʻana i ka mālama ʻana. I nā hebedoma e hiki mai ana, ua ʻoki koke lākou.

I ka poʻe maʻi i mālama ʻia me Lixumia, ʻoi aku ka liʻiliʻi o ka maʻi pākau (24.5%) ma mua o nā mea maʻi i mālama ʻia me ka exenatide 2 mau manawa i kahi lā (35.1%), a me ka nui o nā HP ʻē mai ka gastrointestinal tract i loko o nā ʻelua nā hui lapaʻau i like like ʻole.

Nā wahi hōʻike ma ka wahi ʻōlelo

ʻO nā hōʻike ma ka wahi maʻi ma kahi o ka mālama ʻia 24-pule i nānā ʻia ma 3.9% o nā mea maʻi e loaʻa ana iā Lixumia, ʻoiai i nā mea maʻi e loaʻa ana i ka placebo, ua nānā ʻia lākou me ka pinepine o 1,4%. ʻO ka hapanui o nā hopena kūpono mai ka hōʻeha a ʻaʻole i hoʻōki ka hana.

Ma muli o nā mea e mau ai ka maʻi immunogenic o nā lāʻau i loaʻa nā protein a i nā peptides, ma hope o ka mālama ʻana me Lixumia i nā mea maʻi, hiki i ka hoʻokumu ʻana i nā antibodies i ka lixisenatide. I ka pau ʻana o ka hopena mālama 24 mau hebedoma, i loko o kahi hōʻike hoʻomalu i waiho i ka placebo, ua loaʻa he 69,4% o nā mea maʻi me ka lixisenatide mau hopena kūpono no ka hiki ʻana o nā antibodies i ka lixisenatide. Eia nō naʻe, ʻo ka loli i ka HbA 1c index, hoʻohālikelike me ka mea ma mua o ka hoʻohana ʻana i ka lixisenatide, he mea like ʻole ia, me ka hopena o ka hopena maikaʻi a maikaʻi ʻole paha o ka loiloi no ka hiki ʻana i nā antibodies i ka lixisenatide. ʻO nā mea maʻi i mālama ʻia me ka lixisenatide nona ka helu HbA 1c, ʻo 79.3% kahi hōʻike maikaʻi ʻole no ka hiki ʻana o nā antibodies i ka lixisenatide a i ʻole ka titī o nā antibodies i ka lixisenatide ma lalo o ka palena haʻahaʻa no kona helu ʻana, aʻo ke koena 20,7% o nā mea maʻi. ka nui titers o nā antibodies e lixisenatide.

ʻAʻohe ʻokoʻa ʻole i ka ʻike palekana palekana i nā maʻi me ka mea e pili ana i ke kūlana o nā antibodies i ka lixisenatide, koe wale nō ke hoʻonui ʻana i nā ʻano o ka hopena ma ka wahi i hoʻopaʻa ʻia ai i nā maʻi maʻi anti-antibody. ʻO ka hapanui o nā hopena ma ka wahi maʻi ʻoi aku ka mālie, me ka hele ʻole a me ka ʻole o nā antibodies i ka lixisenatide.

ʻAʻohe mea hoʻohālikelike anti-immunological me ka glandona maoli a i ʻole he endogenous GLP-1.

ʻO nā maʻi e pili ana i ka maʻi me ka hoʻohana ʻana i ka lixisenatide (e like me ka anaphylactic reaksi, angioedema, a me urticaria) i ka manawa nui o ka mālama 24-wiki i nānā ʻia ma ka 0.4% o nā mea maʻi i mālama ʻia me Lixumia, i hoʻohālikelike ʻia me ka hapa haʻahaʻa o 0.1% o nā mea maʻi. ma ka hui placebo.

Hoʻolaha ma mua o ka lāʻau

ʻO ke alapine o ka wehe ʻana i nā lāʻau ma muli o nā hopena hōʻino he 7.4% i loko o ka hui Lixumia a me 3.2% i ka hui pletebo. ʻO nā HP pinepine e alakaʻi i ka huki ʻana i ka mālama ʻana ma ka pūʻulu Lixumia o ka nausea (3.1%) a me ka lua a me ka lua (1.2%).

Pākuʻi helu

ʻO ka hopena no ka hoʻonā ʻana,05 mg / ml a me 0.1 mg / ml

1 ml o ka hoʻonā i loaʻa:

mea kūlohelohe - lixisenatide 0.05 mg a i ʻole 0.10 mg

nā mea waiwai: 85% glycerin, sodium acetate trihydrate, L-methionine, metacresol, hydrochloric acid, sodium hydroxide, wai no ka hōʻemi.

ʻAihea ʻāpana kala ʻole.

ʻO nā waiwai Pharmacological

Ma hope o ka hoʻomalu ʻana i ka subcutaneous i nā poʻe maʻi me ka maʻi diabetes type 2, ʻo ka wikiwiki o ka emi ʻana o ka lixisenatide, inā hoʻi i ka ʻimi i ka lawelawe. Ka nānā ʻole o ka pāʻana a inā paha i hoʻohana ʻia ka lixisenatide ma hoʻokahi a i ʻole ka nui o nā koina, i nā mea maʻi me ka maʻi type 2, ʻo ka pākāwā tmax ka 1 i ka 3.5 mau hola. No ka mālamaʻana i ka hoʻokele subcutaneous o lixisenatide i ka ʻōpū, ka ʻūhā a me nā poʻohiwi paha, ʻaʻohe ʻano nui o ke kikowaena o ka pā o ka hoʻopili ʻana.

ʻO Lixisenatide kahi pae paʻakikī o ka nakinaki ʻana (55%) i nā protein o kānaka.

ʻO ka nui ʻike ka laha ma hope o ka hoʻokele subutaneus o lixisenatide (Vz / F) ma kahi o 100 L.

ʻO Biotransformation a me ka hoʻopuka

E like me ka peptide, ua hoʻopio ʻia ka lixisenatide e ka kānana glomerular i ukali ʻia e ka puna tubular me ka wā e hōʻeha nei ka metabolic, ke alakaʻi nei i ka hoʻokumu ʻana o nā peptides liʻiliʻi a me nā waikawa amino, ka mea i hoʻohui pū ʻia i ka protein metabolism.

Ma hope o ka hoʻomoe ʻana i ka nui o nā maʻi i nā maʻi me ka diabetes type 2, ʻo ka ʻokoʻa hapalua hapalua hapalua-ola ka palena o 3 mau hola a me ka nui o nā hoʻomaʻamaʻa ʻike (CL / F) ma kahi o 35 l / h.

ʻO ka maʻi me ka hana renal impaired

I nā maʻi me ka liʻiliʻi (clearanine clearance i hoʻohālikelike ʻia me ka laikini ʻo Cockcroft-Gault, he 60-90 ml / min), hōʻemi (hoʻonaninani ʻo ka creinine he 30-60 ml / min) a me nā hōʻeha o ka hana hōʻeha nui (ʻo ka hana maʻaina he 15-30 ml / min), AUC (ka pae ma lalo o ka neʻe ʻana o ka manawa curve) hoʻonui ʻia e 46%, 51% a 87%, ia manawa.

ʻO nā mea maʻi me ka hana pūlima hemahema

No ka mea, ua hoʻopiʻi ʻia ka lixisenatide e nā ʻōpū, ʻaʻole i komo nā mea maʻi me ka maʻi lela paʻa ʻole a hopena i loko o nā haʻawina ʻo pharmacokinetic. ʻAʻole manaʻo ʻia ka neʻe hematic e pili i ka pharmacokinetics o lixisenatide.

ʻAʻohe hopena koʻikoʻi ʻo Gender i ka pharmacokinetics o lixisenatide.

Wahi a nā hopena o nā haʻawina pharmacokinetic i nā poʻe maʻi o ka lāhui Caucasian, Iapana a me Kaina, ʻaʻole i loaʻa i ka hopena koʻikoʻi ka hopena o ka pharmacokinetics o lixisenatide.

ʻAʻole loaʻa kahi hopena koʻikoʻi o ka makahiki ma ka pharmacokinetics o lixisenatide. Ma kahi noiʻi pharmacokinetic ma nā maʻi maʻi maʻi ʻole maʻi maʻi, ka hoʻohana ʻana o ka lixisenatide 20 μg ma ka hui o nā mea maʻi (11 mau mea maʻi 65 a 74 mau makahiki he 7 mau maʻi maʻi ʻo 75 mau makahiki), e alakaʻi ana i ka piʻi maʻamau o ka PPK o lixisenatide e 29%. hoʻohālikelike ʻia me 18 nā mea maʻi 18 a 45 paha mau makahiki he mea paha, ua pili ʻia me ka hoʻēmi ʻia ʻana o ka hana hula ma ka ʻelemakule.

ʻAʻole loaʻa ka hopena o ke kino i ka hopena koʻikoʻi ma ka hōʻike ʻo PPK no ka lixisenatide.

ʻO Lixisenatide kahi mea pili i koho ʻia no nā mea hoʻokipa GLP-1 (e like me peptide-1). ʻO ka mea maʻi GLP-1 kahi pahuhopu maoli no ka GLP-1 kūlohelohe, he endogenous incretin hormone e potentiates glucose e hilinaʻi nei i ka huna a ka maʻi e ka pancreatic beta cells.

Hoʻopili ʻia ka hopena o ka lixisenatide e kahi hōʻike pilikino me nā mea hoʻokipa GLP-1, e alakaʻi ana i ka hoʻonui i ka intracellular cyclic adenosine monophosphate (cAMP). Hoʻolaha ʻo Lixisenatide i ka huna ʻana i ka insulin i ka wā e hoʻonui ka nui o ke kō o ke koko, akā ʻaʻole me ka normoglycemia, kahi e hoʻohālikelike ai i ka hopena o ka hypoglycemia.

I ka manawa like, kau ʻia ka ʻikepili glucagon. Me ka hypoglycemia, mālama ʻia kahi ʻoihana hoʻolaʻa o ka hoʻonaʻauao glucagon. Hāʻawi ʻo Lixisenatide i ka haʻalele ʻana o ka ʻōpū, hoʻemi ʻia ka wikiwiki i loaʻa i ka glucose i ka meaʻai ke kahe koko.

Ke hoʻohana ʻia i hoʻokahi lā i ka poʻe maʻi me ka maʻi diabetes type 2, hoʻomaikaʻi ka lixisenatide i ka mana glycemic ma muli o nā hopena koke a lōʻihi loa o ka hoʻohaʻahaʻa ʻana i nā kukuna glucose ma hope o ka ʻaina a ma ka ʻōpū ʻole.

Ua hōʻoia ʻia kēia hopena ma ka glucose postprandial i loko o kahi haʻawina 4-pule, i hoʻohālikelike ʻia me ka liraglutide 1.8 mg hoʻokahi manawa i ka lā me ka hui pū me ka metformin. ʻO ka emi ʻana mai ka pae mua o ka ʻōlelo PPC 0: 30–4: 30 h o ka glucose o ka plasma ma hope o ka ʻaʻa ʻana o ka hōʻike.

–12.61 hola * mmol / L (-227.25 hola * mg / dL) i ka lixisenatide hui a me nā

- 4.04 hola * mmol / L (–72.83 hola * mg / dL) i ka hui liraglutide. Ua hōʻoia ʻia i kēia ma ke aʻo he 8 mau wiki i hoʻohālikelike ʻia i ka liraglutide i ʻōlelo ʻia ma mua o ka ʻaina kakahiaka i hui pū me ka glargine insulin a i ʻole ʻole metformin.

He mākaukau me ka palekana

I ka pau ʻana o nā haʻawina III paʻa, ua hōʻike ʻia ma ka hopena o ka papa mālama 24-wiki ma mua, ʻoi aku ka 90% o ka nui o ka poʻe maʻi i hiki i ka mālama mau i ka mālama mālama ʻia o Lixumia 20 μg hoʻokahi i hoʻokahi lā.

Hoʻohui hui hou me nā lāʻau antidiabetic waha

I ka hopena o ka hopena mālama 24 mau hebedoma mua loa me Lixumia, i hui pū me ka metformin, sulfonylurea, pioglitazone, a hui pū ʻana paha i kēia mau lāʻau, hōʻike i ka nui o ka statistically i ka hookeokeo ʻana i ka plasma HbA1c a me ka glucose o ka hola 2 mau hola ma hope o kahi hoʻāʻo ʻana e hoʻohālikelike ʻia me ka placebo. ʻO ka hōʻemi ʻana o HbA1c i mea nui i ka wā i mālama ʻia ai ka lāʻau i hoʻokahi manawa i ka lā, inā paha me ka mea i ke kakahiaka nui a i ke ahiahi paha. ʻO ka hoʻolaha ʻana i ka HbA1c i lōʻihi i nā haʻawina lōʻihi a hala 76 mau pule.

Hoʻolaha kūpaʻa postprandial Glucose

Ma kahi o Lixumia ka hopena i hoʻoemi ʻia i ka glucose ma hope o ka lōʻihi o ka hoʻāʻo ʻana ma 2 mau hola ma hope o ka ʻai ʻaʻai, he ʻoi aku ka maikaʻi ma ka placebo, me ka manaʻo ʻole o ka hana maʻamau.

I ka hopena o ka hopena mālama 24 mau hebedoma mua loa, ʻo Lixumia i hui pū me ka metformin a me / a i ʻole ka sulfonylurea i nā hoʻokolohua āpau i alakaʻi i ka hoʻololi mau loa i ke kaupaona ʻana o ke kino e kū ana mai –1.76 kg a i -2.96 kg.

ʻO ka hoʻololi ʻana i ke kaumaha o ke kino mai ka pae mua ma ka pae mai - 0.38 kg a -1.80 kg i nānā ʻia i nā mea maʻi e loaʻa ana i ka lixisenatide i hui pū ʻia me ka nui o ka manaʻo o ka insulin basal, a i hui pū me ka metformin a i ʻole sulfonylurea.

I nā poʻe maʻi i hoʻomaka mua i ka hoʻohana ʻana i ka insulin, i ka hui lixisenatide, ua noho kino ʻole ke kino o ke kino, akā, ma ka hui pletebo i hōʻike ʻia. Ma nā haʻawina lōʻihi e lōʻihi a hiki i ka 76 wiki, e hoʻomau ana ka nui o ka paona.

Ua hōʻike ʻia nā haʻawina hauoli o Lixumia i ka hana hoʻonā beta hoʻoponopono hou e like me ke ana ʻia e ka loiloi loiloi cell cellostatic home (HOMO-β / HOMA-β).

ʻO ka loiloi Cardiovascular

I nā hoʻokolohua āpau i hoʻomalu ʻia i ka maʻi III, ʻaʻole i hōʻike ʻia nā mea maʻi me ka maʻi diabetes type 2 i ka hoʻonui o ka nui o ka puʻuwai ma waena.

Poʻe kānaka

Nā kānaka ʻokoʻa ≥70 makahiki

Ua hoʻomaikaʻi nui ʻo Lixisenatide i nā kiʻekiʻe o ka hemoglobin glycated (HbA1c) (-0.64% hoʻohālikelike ʻia me ka placebo, 95% interval interval (CI): -0.810% a -0.464%, p

Nā hopena ʻona o ka hopena o Lixumium

ʻO ka hōʻikepili Palekana Pūnaewele

ʻOi aku ma mua o ka 2,600 mau mea maʻi ma 8 mau haʻawina nui i hoʻokele ʻia i ka papa lālani a i ʻole ka hoʻokele III me ka mana ikaika i loaʻa iā Lixumia i ka monotherapy a i hui pū paha me metformin, sulfonylurea (me ka ʻole a metformin) a i ʻole basal insulin (me ka ʻole o ka metformin a me ka sulfonylurea) a i ʻole a ʻole).

ʻO nā hana ʻino i hōʻike ʻia i ka wā o ka hoʻokolohua ʻana i nā maʻi ma ke ʻano he nausea, luaʻi, a me nā hōʻeha. ʻO ka pane ka maʻa mau a maʻalahi.

Aia nō kekahi mau hihia a ka ha hypoglycemia (i ka wā i hoʻohana ʻia ai ʻo Lixumia i hui pū me ka sulfonylurea a me / a me ke ʻano basal) a me ke poʻo. Ua nānā ʻia nā hopena alerine i ka 0.4% o nā mea maʻi e hoʻohana ana iā Lixumia.

Aia ma lalo iho nā hopena ʻino i hana ʻia me ka pinepine o> 5%, inā ʻoi aku ka nui o ka ulu ʻana ma waena o nā poʻe maʻi e loaʻa ana iā Lixumia ma waena o nā mea maʻi e loaʻa ana i nā lāʻau hoʻohālikelike āpau, i hui pū ʻia ka hopena ʻino me ka pinepine o ≥ 1% ma ka hui o nā maʻi e loaʻa ana iā Lixumia, ina he 2 mau koina ka nui o ka hiki ana mai o ka pinepine o ka hui o na mea maʻi e loaʻa ana i nā lāʻau lapaʻau hoʻohālikelike āpau.

ʻO nā hopena maikaʻi loa i hoʻokū ʻia ma nā hoʻokolokolo ma plebo-control and phase III me ka hoʻomohala paʻa i ka wā o ka mālama lapaʻau holoʻokoʻa (me ka nui o nā manawa ma mua o ka 24 ma ka manawa lapaʻau nui 24 mau pule i nā haʻawina me ≥ 76 mau pule o ka holoʻokoʻa).

• hypoglycemia (i hui pū me ka sulfonylurea a me / a i ʻole ke basal insulin)

• lie kanikela

• kikala, holo maikaʻi, ʻōpū

Pinepine (≥ 1/100 a 5% momona payday bolsan zhalymsyz reperar berylgen, hunter payda boli zhіlіgі barlyқ salistyru drug taryn alғan edelushіler toptara arasynda zhіlіlіndydydelda 1%

Placebo-baқılanatyn әne belsendi baқylanatyn III phase ғ zertteulerde bүkіl emdela kezeңi boyina (bүkіl emdeudің ≥ 76 aptasynda zertteulerde negizy-24

Nā ʻōlelo kikoʻī

I nā mea maʻi e loaʻa ana iā Lixumia ma monotherapy a i hui pū me ka metformin, hypoglycemia me nā hōʻike kulana i ulu pinepine ʻia, a ʻo ka pinepine o nā maʻi i loaʻa iā Lixumia e like me kēlā me ka pletebo i ka wā mālama holoʻokoʻa.

I nā maʻi i hoʻolako ʻia ʻo Lixumia i hui pū me kahi lāʻau hypoglycemic waha o ka hui sulfonylurea a i ʻole basal insulin, ka ʻeha o ka hypoglycemia, ka mea i hui pū ʻia e nā maʻi maʻi.

I ka manawa holoʻokoʻa o ka mālama ʻana me Lixumia, ʻo ka nui o ka ulu ʻana o ka hypoglycemia e hana pū ana me nā maʻi maʻi ʻoi aku ka kiʻekiʻe ma mua o ka placebo, i ka manawa ua hoʻohana ʻia ʻo Lixumia e hui pū.

- me kahi lāʻau lapaʻau hypoglycemic oral o ka hui sulfonylurea a me ka metformin,

- me ka monotherapy me ka insulin basal,

- me ka hui pū ʻana o ka insulin basal a me ka metformin.

I ka manawa holoʻokoʻa o ka wā i hoʻohana ʻia ai ʻo Lixumia i hui pū me ka monotherapy me ka lāʻau hypoglycemic waha o ka hui o ka sulfonylurea, hypoglycemia me nā hōʻike pilikino i hana ʻia ma ka 22.7% o nā mea maʻi i mālama ʻia me Lixumia a ma 15.2% o nā mea maʻi i loaʻa iā pletebo. I ka manawa i hoʻohana ʻia ai ʻo Lixumia i ka hui pū ʻana me ka lālani hypoglycemic waha o ka hui sulfonylurea a me ka insulin basal, hypoglycemia me nā hōʻike hōʻike i loaʻa i ka 47.2% o nā mea maʻi i mālama ʻia me lixisenatide, a ma 21.6% o nā mea maʻi i mālama ʻia me ka pletebo.

Ma keʻano holoʻokoʻa, no ka manawa holoʻokoʻa o ka lawe ʻana i ka lāʻau lapaʻau ma ka hoʻokolohua mau i nā maʻi haukapila III, ʻo ka ulu ʻana o ka hypoglycemia koʻikoʻi me nā hōʻike maʻi e pili ana i ka hana "jarang".

Ma muli o nā mea e mau ai ka maʻi immunogenic o nā lāʻau i loaʻa nā protein a i nā peptides, ma hope o ka mālama ʻana me Lixumia i nā mea maʻi, hiki i ka hoʻokumu ʻana i nā antibodies i ka lixisenatide. I ka pau ʻana o ka mālama manawa 24-pule, ma nā haʻawina i hoʻomalu ʻia e placebo, he 69,4% o nā mea maʻi i mālama ʻia me lixisenatide he mau hopena kūpono no ka hiki ʻana o antibodies i ka lixisenatide.Eia nō naʻe, ʻo ka hoʻololi i ka index HbA1c, hoʻohālikelike me ka mea ma mua o ka hoʻohana ʻana i ka lixisenatide, he mea like ʻole ia, me ka hopena o ka hopena maikaʻi a maikaʻi ʻole paha o ka loiloi no ka hiki ʻana i nā antibodies i ka lixisenatide. No nā mea maʻi i mālama ʻia me ka lixisenatide me ka helu HbA1c, ʻo 79.3% kahi hōʻike maikaʻi ʻole no ka hiki ʻana o nā antibodies i ka lixisenatide a i ʻole ka titī o nā antibodies i ka lixisenatide ma lalo o ka palena haʻahaʻa o kona helu ana, a ʻo ke koena 20,7% o nā mea maʻi i loaʻa i ka nui ʻike kumumea i nā ʻāpana o nā antibodies i ka lixisenatide.

ʻAʻohe ʻokoʻa ʻole i ka ʻike palekana palekana i nā maʻi me ka mea e pili ana i ke kūlana o nā antibodies i ka lixisenatide, koe wale nō ke hoʻonui ʻana i nā ʻano o ka hopena ma ka wahi i hoʻopaʻa ʻia ai i nā maʻi maʻi anti-antibody. ʻO ka hapanui o nā hopena ma ka wahi maʻi ʻoi aku ka mālie, me ka hele ʻole a me ka ʻole o nā antibodies i ka lixisenatide.

ʻAʻohe mea hoʻohālikelike anti-immunological me ka glandona maoli a i ʻole he endogenous GLP-1.

ʻLoe a me ke kākele

Initial dosis: hoʻomaka ke ʻano me 10 mcg Lixumia i hoʻokahi lā no 14 lā.

Ka mālama mālama ʻana: ka ʻoihana o ka mālama mālama paʻa o 20 mcg Lixumia i hoʻokahi lā i ka lā 15.

No kahi papa mālama mālama pono ʻia, ʻoi aku ka hoʻohana ʻai ʻana o Lixumia i 20 mcg. No ka hoʻomaka mua ʻana, hoʻohana ʻia kahi hopena o 10 μg Lixumia i hoʻohana ʻia.

Hoʻokomo ʻia ʻo Liksumiya i hoʻokahi manawa i ka lā, hoʻokahi hola ma mua o ka pāʻina ʻana. ʻOi aku ka maikaʻi, ke mālama ʻia nei ka ʻōlelo Lixumia i kēlā me kēia lā ma mua o ka pāʻina like, i ke manawa ua koho ʻia ka manawa kūpono loa o ka hoʻokele. Inā hala kahi dosis o Lixumia, pono e hoʻolilo ʻia kahi manawa ma hoʻokahi hola ma mua o ka papaʻai e hiki mai ana.

I ke koho ʻana iā Lixumia, i ka hoʻohui ʻana no ka loaʻa ʻana o ka mālama ʻana me ka metformin, hiki nō i ke ʻano o ka metformin ke loli.

Ma ke kuhikuhi ʻana iā Lixumia, i ka loaʻa ʻana o ka mālama ʻana me ka sulfonylurea a i ʻole ke basal insulin, e hoʻemi ʻia kahi nui o ka sulfonylurea a i ʻole basal insulin e hōʻemi i ka hopena o ka hypoglycemia.

ʻAʻole pono ke kuhikuhi ʻo Lixumia i ka hui pū me ka insulin basal a me ka sulfonylurea ma muli o ka nui o ka piʻi o ka hypoglycemia (e nānā i "ʻōlelo aʻoaʻo".

ʻAʻole pono ka hoʻohana ʻana o Lixumia i ka nānā kūikawā ʻana i nā pae glucose o ke koko. Eia nō naʻe, i ka hoʻohana ʻana i ka hui me ka sulfonylurea a i ʻole ke basal insulin, e nānā ana i ka glucose o ke koko a i ʻole mālama pono iā ʻoe iho i ke kahe o ke koko e pono ai i ka hoʻoponopono ʻana i ka maʻi o ka sulfonylurea a i ʻole basal insulin.

Kuhi ʻia no ke ʻano o ka makahiki, ʻaʻole pono ka hoʻoponopono ʻana o ka lāʻau.

ʻO ka maʻi me ka hana renal impaired

I nā mea maʻi me ka hoʻōla kaumaha a i ʻole ka hopena, ʻaʻole i koi ʻia ka hoʻoponopono ʻana. ʻAʻoheʻike therapeutic i loko o nā mea maʻi me ka hana ʻole o ka maʻi hanalula (ʻo ka hana hōʻoki i hana ʻia ma lalo o 30 ml / min) a i loko o nā mea maʻi me ka maʻi hope o ka maʻi hope, a no kēia kumu, ʻaʻole i ʻōlelo ʻia ʻo Lixumia i kēia mau hui o nā maʻi.

ʻO nā mea maʻi me ka hana pūlima hemahema

No ka poʻe maʻi me ka hana pūpū o ka maʻi hemahema, ʻaʻole pono ka hoʻoponopono ʻana. Ka maʻi ʻōpiopio

ʻAʻole paʻa i ka palekana a me ka hana pono o ka lixisenatide ma nā keiki a me nā ʻōpio ma lalo o 18 makahiki o kona mau makahiki. ʻAʻohe ʻikepili i ʻole.

Kahi alanui hoʻokele

Ua hōʻike ʻia ʻo Lycumum no ka hoʻokele subutaneus ma ka ʻāʻī, ka ʻōpū a me ka poʻohiwi paha. ʻAʻole hiki iā ʻoe ke komo i ka intravenously a i ʻole intramuscularly.

ʻAʻole pono e hoʻohana ʻo Lixumia i ʻaopo ʻia. Hiki ke hoʻohana ʻia ʻo Liksumiya me nā ngika waila mai 29 a 32 mau caliber no kahi peni syringe. ʻAʻole pili ʻia nā pulima penikala Syringe.

Pono e aʻo i ka mea maʻi e hoʻolei i ka pono ma hope o kēlā me kēia hoʻohana e like me nā koi o ke kānāwai kūloko kūloko a mālama i ka peni ʻo ka syringe me kahi huʻu ʻole i hoʻokomo ʻia. E kōkua ana kēia i ka pale ʻana a me ke kahakaha ʻana o ka pono. Hoʻohana ʻia ka peni no ka mea hoʻokahi wale nō ka maʻi.

ʻO kekahi lāʻau lapaʻau a hoʻohana ʻole ʻia paha e hoʻokaʻawale ʻia e like me nā kānāwai kūloko kūloko.

I ka loaʻa ʻole o nā haʻawina hoʻokolohua, ʻaʻole pono e kāwili ʻia ka lāʻau lapaʻau me nā lāʻau ʻē aʻe.

Hoʻopili i nā lāʻau lapaʻau

ʻO Lixisenatide he peptide ʻaʻole i hoʻohālikelike ʻia me ka komo ʻana o ka cytochrome P450. I loko o nā haʻawina vitro, ʻaʻole i hoʻopilikia ka lixisenatide i ka hana o nā cytochrome hōʻike ʻia P450 a me nā mea lawe kanaka.

Ke hoʻoluhi nei i ka hoʻomaha ʻana o nā ʻōpū o ka gastric me ka hoʻohana ʻana i ka lixisenatide e hōʻemi ʻia i ka helu o ka hoʻoulu ʻana o nā lāʻau lapaʻau. E mālama pono e mālama i nā maʻi e loaʻa ana i nā lāʻau lapaʻau me nā mākī liʻiliʻi a i ʻole nā ​​lāʻau lapaʻau e koi pono ai ka nānā ʻana i nā lāʻau lapaʻau, ʻoiai inā hoʻomaka ka mālama ʻana me ka lixisenatide. No ka lixisenatide, pono e lawe ʻia kēia mau lāʻau i ke ala maʻamau. Inā pono e kiʻi ʻia nā lāʻau lapaʻau me ka meaʻai, pono e kuhikuhi ʻia nā mea maʻi e lawe iā lākou i ka meaʻai i ka manawa hiki ke hoʻohana ʻole ʻia ka lixisenatide.

No nā lāʻau lapaʻau waha, e like me ka antibiotics, ka mea, me ka noʻonoʻo pono ʻana i ka hana pono, e hilinaʻi ana i ka lūlū ʻana o ka paepae, pono e hoʻomaopopo ʻia nā mea maʻi e lawe i kahi manawa i hala 1 a i ʻole 4 mau hola ma hope o ka loaʻa o ka lixisenatide.

Pākuʻi wai hoʻohālikelike i loko o ka ʻōpū e pili ana i nā mea pili i ka hoʻowalewale ʻana i ka ʻōpū ma mua e hoʻohana ʻia i 1 hola ma mua a i ʻole 4 mau hola ma hope o ka loaʻa ʻana o ka lixisenatide

Ua hoʻohana ʻia ʻo Paracetamol me he laʻa lāʻau hoʻohālike e loiloi i ka hopena o ka lixisenatide ma ka haʻalele ʻana i nā ʻike o ka gastric. Ma hope o hoʻokahi ka wai o ka paracetamol 1000 mg i hoʻohana ʻia, ua hoʻomau ka wahi ma lalo o ka pihi (PPC) a me ka t1 / 2 o ka paracetamol i loli ʻole, i ka manawa o kona hoʻohana ʻana (ma mua a i ʻole ma hope o ka inake o lixisenatide). I ka manawa i hoʻohana ʻia ai he 1 hola a i ʻole mau hola 4 ma hope o 10 μg o ka lixisenatide, ua emi iho ka palena o Cmax o ka paracetamol, ma kēlā me kēia, e ka 29% a me 31%, a ua hoʻolōʻihi ʻia ka waiwai o tmax, ma kēlā me kēia, ma ka 2.0 a me 1,75 hola. Me ka hoʻohana ʻana o 20 μg o ka nui o ka mālama mālama, ua wānana ʻia kahi lohi o ka tmax a me kahi laʻana i Cmax o ka paracetamol.

ʻAʻohe hopena i ka Cmax a me ka tmax o ka paracetamol i ka wā i hoʻohana ai ka paracetamol i ka hola 1 i mua o ka hoʻohanaʻana o lixisenatide.

Hāʻawi i ka ʻikepili i luna, ʻaʻohe pono o ka hoʻoponopono ʻana i nā hapa o paracetamol, akā pili ka Tmax i nānā ʻia i ka wā i manaʻo ʻia ai nā paracetamol i nā hola he 1-4 ma hope o ka lawe ʻana i ka lixisenatide e noʻonoʻo inā pono kahi hoʻomaka wikiwiki o ka hana no ka hoʻoponopono pono.

Ma hope o ka noi ʻana i hoʻokahi waihona o ka ʻekemu kūlohelohe (ethinyl estradiol 0.03 mg / levonorgestrel 0.15 mg) 1 hola ma mua a i ʻole 11 mau hola ma hope o ka noi ʻana o 10 gg o ka lixisenatide, Smax, PPC, t1 / 2 a me ka tmax o ka ethinyl estradiol a me levonorgestrel i loli ʻole.

ʻO ka hoʻohana ʻana o ka maʻi paʻakai 1 mau hola a i ʻole 4 mau hola ma hope o ka hoʻohana ʻana i ka lixisenatide ʻaʻole i hoʻopilikia i ka AUC a me ka t1 / 2 o ka ethinyl estradiol a me levonorgestrel, aʻo ka Cmax o ka ethinyl estradiol i emi, i kēlā me kēia, ma ka 52% a 39%, a me ka Cmax o ka levonorgestrel i pau e 46%, i kēlā me kēia. a 20%, a me ka waihona waiwai o ka tmax ua neʻe i ka holo i nā hola 1-3.

ʻO ka emi ʻana o Cmax ka palena o ka pilina kaukaʻi ʻana, a ʻaʻole pono ka hoʻoponopono ʻana o ka hoʻoponopono ʻana i kahi maʻi paʻakai.

Ke hoʻohana nei i 20 μg o ka lixisenatide me ka hui pū me 40 mg o ka atorvastatin i kakahiaka ma 6 mau lā, ʻaʻole i loli ka hopena o ka atorvastatin, ʻoiai Cmax i emi i ka 31% a me ka tmax i hoʻonui ʻia e 3.25 hola.

ʻAʻole i ʻike ʻia kēlā hoʻonui like no ka tmax inā i hoʻohana ʻia ʻo atorvastatin i ke ahiahi, a i ka lixisenatide ma ke kakahiaka, akā ʻo PPK a me Cmax o atorvastatin, ma kēlā me kēia, hoʻonui ʻia ka 27% a 66%.

ʻAʻole he koʻikoʻi nā loli o kēia mau hoʻololi, a no laila, ʻaʻole pono ka hoʻoponopono ʻana i ka maʻi atorvastatin i ka wā i hoʻohana ʻia ai me ka lixisenatide.

ʻO Warfarin a me nā mea hoʻohua ʻē aʻe

Ma hope o ka hoʻohana concomitant o 25 mg o warfarin me nā nui o nā lixisenatide 20 μg, ʻaʻohe hopena i ka AUC a i INR (pālākē maʻamau o ka honua), aʻo ka Cmax hōʻemi e ka 19% a hoʻonui i ka tmax i 7 mau hola.

Aia e pili ana i kēia mau hopena, ʻaʻole pono ka hoʻoponopono ʻia o ka warfarin i ka wā i hoʻohana ʻia ai me ka lixisenatide, akā naʻe, mālama pinepine ʻia ka INR i nā poʻe maʻi e lawe nei i ka warfarin a me / a i ʻole e kō ai i nā derivatives Coumarin i ka wā i hoʻomaka ai a i ka hopena o ka lapaʻau lixisenatide.

Ma hope o ka hoʻohana pū ʻana o ka lixisenatide 20 μg a me 0.25 mg o ka digoxin i loko o ka mokuʻināʻau, ʻaʻole i loli ka manaʻo o PPC o ka digoxin. Ua hoʻonuiʻia ke kumukūʻai o ka tmax o ka digoxin i nā hola 1,5, a ua emi ka nui o Cmax e 26%.

Hoʻokumu ʻia ma kēia mau hualoaʻa, ʻaʻole pono ka hoʻoponopono ʻana o ka hoʻoneʻe o ka digoxin i ka wā e hoʻohana ʻia ai me ka lixisenatide.

Ma hope o ka hoʻohana pū ʻana o ka lixisenatide 20 μg a me 5 mg o ka ramipril no nā lā 6, ua hoʻonui ʻia ka PPK ramipril ma kahi o 21%, aʻo ka Cmax i emi iho e 63%. ʻAʻole loli nā ʻōlima o ka PPC a me Cmax o ka metabolite ikaika (ramiprilat). ʻO ka tmax o ka ramipril a me ka ramiprilat i hoʻonui e hoʻonui i ka aneane 2.5 mau hola.

Hoʻokumu ʻia kēia mau hualoaʻa, ʻaʻole pono ka hoʻoponopono ʻana o ka wai maʻi ramipril i ka wā e hoʻohana ʻia ai me ka lixisenatide.

Ke keu

I loko o nā hoʻokolohua lapaʻau, mālama ʻia nā kumu o ka lixisenatide a hiki i 30 mcg i kēlā me kēia lā i nā mea maʻi me ka diabetes type 2 i kahi mau noi 13. Ua hoʻonui ʻia ka ulu ʻana o ka ʻeha gastrointestinal.

Ma kahi o kahi overdose, e like me nā hōʻailona lāʻau a me nā hōʻailona, ​​pono e hoʻomaka ka mea maʻi i ke kākoʻo kākoʻo kūpono, a me ka nui o ka lixisenatide e hoʻemi ʻia i ka lāʻau i kuhikuhi ʻia.