Aktos bụ nkwadebe hypoglycemic nke usoro thiazolidinedione, nsonaazụ nke dabere na ọnụnọ insulin. Ọ bụ agonist na-ahọrọ nke gamma ndị na-anabata ihe gamma nke peroxisome na-agbasa ozi (PPAR-γ). A na-enweta ndị na-anabata PPAR-in na adipose, anụ ahụ akwara na imeju. Mgbapụta nke ndị nabatara ọgwụ nuklia nke PPAR mod na-emegharị ntụgharị nke ọtụtụ mkpụrụ ndụ ihe ọmụmụ insulin na-etinye aka na nchịkwa glucose na metabolism metabolism.

Actos na-ebelata insulin na-eguzogide n’akpụ anụ ahụ na imeju, na-eme ka mmụba na ojiji nke glucose na-adabere na umeji mbelata na ntọhapụ nke glucose site na imeju. N'adịghị ka nkwadebe nke sulfonylurea, pioglitazone anaghị akpali mkpali insulin site na mkpụrụ ndụ beta pancreatic.

N'ime ndị ọrịa nwere ụdị ọrịa shuga 2 nke mellitus, mbelata nke insulin na-eguzogide ọgwụ n'okpuru ọrụ ọgwụ Actos na-eme ka mbelata glucose n'ọbara, mbelata ọkwa insulin na plasma na ndekọ HbA1C. Na njikọta sulfonylurea, metformin ma ọ bụ insulin, ọgwụ ahụ na-eme ka nchịkwa glycemic dịkwuo mma.

N'ime ndị ọrịa nwere ụdị ọrịa shuga 2 nke nwere oke ike lipid metabolism n'oge ọgwụgwọ ọgwụ ahụ, enwere mbelata triglycerides na mmụba nke ọdịnaya lipoproteins dị elu. N'otu oge ahụ, a na-ahụta mgbanwe na ọkwa nke lipoproteins dị ala na nchịkọta cholesterol dị ala na ndị ọrịa a.

Egwu. Mgbe ewere ya n’afọ na-enweghị isi, a na-ahụ pioglitazone n’ọbara ọbara mgbe minit 30 gasịrị, a na-ahụ ịta ahụhụ kachasị mgbe awa 2 gachara. Nri na-ebute obere oge ịbanye na ntinye uche kachasị, nke a na-ahụ mgbe awa 3-4 gachara, mana nri anaghị agbanwe njupụta zuru oke.

Nkesa. Olu pụtara (Vd / F) nke pioglitazone mgbe ị nwesịrị otu ọgwụ bụ ọkara 0.63 ± 0.41 (pụtara ± SD squared) l / n'arọ ahụ. Pioglitazone nwere ọtụtụ ihe nchebe mmadụ na - akpata ya (> 99%), ọkachasị albumin. Ọ dị oke obere, ọ na-ejikọ ya na protein ndị ọzọ. A na - ejikọtakwa metabolites nke pioglitazone M-III na M-IV n'ụzọ dị mkpa na serum albumin (> 98%).

Metabolism. Pioglitazone bụ metabolized kpụ ọkụ n'ọnụ n'ihi nsonaazụ hydroxylation na mmeghachi nke oxidation na nguzobe metabolites: metabolites M-II, M-IV (ihe dị iche iche pioglitazone hydroxide) na M-III (pagoglitazone keri iche iche). A na-agbanwe metabolites akụkụ ụfọdụ na conjugates nke glucuronic ma ọ bụ sọlfọm acid. Mgbe nchịkwa ọgwụ a ugboro ugboro, na mgbakwunye na pioglitazone, metabolites nke M-III na M-IV, nke bụ akụrụngwa ndị metụtara ya, ka a na-ahụ n'ọbara ọbara. Na nguzozi, itinye uche nke pioglitazone bụ 30% -50% nke mkpokọta mkpokọta na ọbara yana site na 20% ruo 25% nke mpaghara n'ogo n'okpuru usoro ọgwụ.

A na-eme metabolism nke pioglitazone site na isi isoforms nke cytochrome P450 (CYP2C8 na CYP3A4). N'ime ọmụmụ in vitro, pioglitazone anaghị egbochi ọrụ P450. Emebeghị nnyocha banyere mmetụta nke pioglitazone na ọrụ nke enzymes ndị a n'ime ụmụ mmadụ.

Ojiji. Mgbe ịwesịrị, ihe dịka 15% -30% nke pioglitazone bụ mmamịrị. A na - ahụpụta ihe pioglitazone na - agbanweghi agbanwe site na akụrụ, a na - apịpụta ya ọkachasị n'ụdị metabolites na conjugates ha. Mgbe etinyere ya n’ime, a na-apịpụta ihe ka ukwuu n’ime ọgwụ ahụ na bile, ma n’ụdị na-agbanweghi agbanwe ma n’ụdị nke metabolites, wee si n’arụ ahụ nwee ọnya.

Nkezi ọkara ndụ nke pioglitazone na ngụkọta pioglitazone (pioglitazone na metabolites na-arụ ọrụ) sitere na awa 3 ruo 7 wee site na awa 16 ruo 24 n'otu n'otu. Mkpokọta ihe zuru ezu bụ 5-7 l / awa.

A na –echeta ngụkọta ngụ nke pioglitazone na serum ka nọ n ’ọrịrị dị elu awa iri abụọ na anọ mgbe ọ gbasasịrị otu ụbọchị.

Ofzọ nke ngwa

Ekwesịrị iji ihe ndị a na-akpọ Actos otu ugboro n'ụbọchị, n'agbanyeghị nri oriri.

Ọ bụ dibia a ka edobere ọgwụ a n’otu n’otu.

Monotherapy na Aktos n'ime ndị ọrịa na-enwetaghị ụgwọ ọrịa mamịrị na ọgwụgwọ nri na mmega ahụ na 15 mg ma ọ bụ 30 mg otu ugboro kwa ụbọchị. Ọ bụrụ na ọ dị mkpa, enwere ike ịbawanye ogwu ahụ ruo 45 mg otu ugboro n'ụbọchị. Ọ bụrụ na monotherapy na ọgwụ adịghị arụ ọrụ, enwere ike ịtụle ohere ọgwụgwọ nkwonkwo.

Nchịkwa nke sulfonylureas. Ọgwụ na aktos jikọtara na sulfonylurea nwere ike ịmalite na 15 mg ma ọ bụ 30 mg otu ugboro kwa ụbọchị. Na nmalite ọgwụgwọ Aktos, enwere ike ịhapụ dose nke sulfonylurea na-agbanweghị. Site na mmepe nke hypoglycemia, a ghaghị belata dose nke sulfonylurea.

Metformin. Ọgwụ na aktos jikọtara ya na metformin nwere ike ibido na 15 mg ma ọ bụ 30 mg otu ugboro n'ụbọchị. Na nmalite ọgwụgwọ Aktos, a pụrụ ịhapụ dose nke metformin ịhapụ ịgbanwe. Mmepe nke hypoglycemia na nchikota a aputaghi, ya mere, odi nkpa idozi nguzo nke metformin.

Insulin Ọgwụ na aktos jikọtara ya na insulin nwere ike ịmalite na 15 mg ma ọ bụ 30 mg otu ugboro kwa ụbọchị. Na nmalite ịgwọ ọrịa ọgwụ Aktos, enwere ike ịhapụ ọgwụ insulin na-agbanweghị. N'ime ndị ọrịa na-anata Actos na insulin, ya na mmepe nke hypoglycemia ma ọ bụ mbelata ọkwa glucose plasma na-erughị 100 mg / dl, enwere ike belata ogo insulin na 10% -25%. Imeghari insulin ozo kwesiri ime ya n’otu n’otu dabere na mbelata glycemia.

Ọgwụ Aktos nwere monotherapy ekwesịghị gafere 45 mg / ụbọchị.

Na njikọta ọgwụ, ọgwụ Aktos ekwesịghị gafere 30 mg / ụbọchị.

N'ime ndị ọrịa nwere nsogbu gbasara akụrụ, a chọghị imezi dose nke Actos. Ihe omuma banyere ojiji nke Aktos na ọgwụ thiazolidinedione ndị ọzọ adịghị.

Ihe ngbanwe

• hypersensitivity na pioglitazone ma ọ bụ otu n'ime mmiri ọgwụ ahụ,
• ụdị shuga 1
• ọrịa mamịrị ketoacidosis,
• ime, inye ụmụ ara,
• oke obi ike III-IV ogo dị ka NYHA (New York Heart Association),
• afọ ruo afọ 18.

Ọrịa Edema, anaemia, ọdịda imeju (mmụba nke ogo enzymes 1-2.5 karịa karịa oke elu nke nkịtị), nkụda obi.

Mmetụta akụkụ

N'ime ndị ọrịa na-ewere Actos na insulin ma ọ bụ ọgwụ ọgwụ hypoglycemic ndị ọzọ, mmepe nke hypoglycemia ga-ekwe omume (na 2% nke ikpe yana njikọta na sulfonylurea, 8-15% nke ikpe yana ngwakọta na insulin).

Ugboro nke anaemia na monotherapy na ọgwụgwọ njikọta na Actos sitere na 1% ruo 1.6% nke ikpe.

Actos nwere ike ime ka mbelata nke hemoglobin (2-4%) na hematocrit. Mgbanwe ndị a ka a na-ahụkarị izu 4-12 ka mmalite nke ọgwụgwọ wee nọgide na-adịgide. Ha adịghị emetụta mmetụta ọ bụla dị n'ọbara na-adịkarị n'ọbara ma na-abụkarị n'ihi mmụba nke olu plasma.

Ugboro nke mmepe edema na monotherapy bụ 4.8%, yana ọgwụgwọ yana insulin - 15.3%. Oge nke ịba ụba n’arụ mgbe ị na-ewere Actos dị nkezi 5%.

Ugboro nke mmụba na ọrụ nke hepatic enzymes alanine aminotransferase (ALT)> ugboro 3 site na oke nke ụkpụrụ bụ ihe dịka 0.25%.

N’oge na-adịkarịghị anya, ịkọpụta ma ọ bụ nmepe nke ọrịa mamịrị na-arịa ọrịa shuga, tinyere mmụba dị n ’anya na-ahụ. Azubeghi ntuzi aka nke itolite uto oria nke pioglitazone. Ndị dọkịta kwesịrị ịtụle ohere nke ịmalite ịmụ asụsụ ma ọ bụrụ na ndị ọrịa na-eme mkpesa na mbelata visual acuity.

N'ime ọmụmụ ihe ndị na-achịkwa ịmịnye mmadụ ọgwụ na United States, ihe kpatara nsogbu ụbụrụ na-emetụta oke mmụba nke ọbara agbagobeghi n'etiti ndị ọrịa e mesoro Actos naanị yana njikọ ya na sulfonylurea, metformin, ma ọ bụ placebo. Na omumu ihe omumu, ya na ochichi aktos na nke insulin n’otu obere onu ogugu ndi nwere oria obi, enwere nsogbu nke obi obi. Ndị ọrịa nwere nkụda mmụọ nke III na nke ọrụ III dịka nhazi ọkwa NYHA (Yorktù Obi New York) esonyeghị na ule ọgwụ banyere iji ọgwụ ọjọọ eme ihe, ya mere, Aktos bụ contraindicated maka ìgwè ndị ọrịa a.

Dabere na data azụmaahịa maka Aktos, a kọwo akụkọ banyere ọrịa nkụchi obi na ndị ọrịa, n'agbanyeghị ihe ngosipụta nke ọrịa obi dị adị.

Jiri n’oge ime na inye nwa ara

Emebeghi ihe omumu oma na nke oma na ndi nwanyi ime. Amabeghị ma Aktos dị na mmiri ara ara, yabụ, ụmụ nwanyị na-enye ara akaghi aka Aktos.

Ọ bụrụ na ọ dị mkpa, na ịhapụ ịhapụ ọgwụ n’oge ị na-a breastụ ara, a ga-akwụsị ịhapụ inye ya ara.

Dodoụbiga ya ókè

Dodoụbiga ọgwụ ókè nke aktos nwere ọgwụ monotherapy anaghị eso ya na nrịba ama nke mgbaàmà ọria.

Dodoụbiga ihe omume ókè nke Actos na sulfonylurea nwere ike jikọta ya na mmepe nke akara nke hypoglycemia. Enweghị ọgwụgwọ a kapịrị ọnụ maka ịdoụbiga mmanya ókè. Achọrọ ọgwụgwọ Symptomatic (dịka ọmụmaatụ, ọgwụgwọ hypoglycemia).

Mmekọrịta na ọgwụ ndị ọzọ

Mgbe ejikọtara na sulfonylurea ma ọ bụ insulin, hypoglycemia nwere ike ịmalite.

Ndị na-egbochi CYP2C8 (dịka gemfibrozil) nwere ike iwelie mpaghara ahụ n'okpuru usoro mkpịsị uche pioglitazone n'oge oge (AUC), ebe ndị na - abanye CYP2C8 (dịka egamampicin) nwere ike ibelata pioglitazone AUC. Njikọ njikọta nke pioglitazone na gemfibrozil na-eduga na mmụba okpukpu atọ na AUC nke pioglitazone. Ebe ọ bụ na mmụba a nwere ike ibute mmụba dabere na mmeghachi omume na-adịghị mma nke pioglitazone, nchịkwa nke ọgwụ a na gemfibrozil nwere ike ịchọ mbelata dose pioglitazone.

Nchikota pioglitazone na rifampicin na-eduga na mbelata 54% na AUC nke pioglitazone. Njikọ dị otú a nwere ike ịchọ mmụba na pioglitazone iji nweta nsonaazụ.

N'ime ndị ọrịa na-ewere Actos na ọgwụ mgbochi, ọnụ na ịdị irè nke mgbochi afọ.

Enweghị mgbanwe na pharmacokinetics na pharmacodynamics mgbe ị na-ewere Actos na glipizide, digoxin, anticoagulants na-apụtachaghị ìhè, metformin. Na vitro ketoconazole na-egbochi metabolism nke pioglitazone.

Enweghi data na mmekorita nke pharmacokinetic nke Actos na erythromycin, astemizole, calcium channel blockers, cisapride, corticosteroids, cyclosporine, ọgwụ egbugbere ọnụ (statins), tacrolimus, triazolam, trimethrexate, ketoconazole, na itraconazole.

Ọnọdụ nchekwa

O were okpomoku di 15-30 Celsius n’ebe ebe anabataghi ya. Mee ka ụmụaka ghara iru. Ndepụta B.

Ndụ shelf afọ 3.

Ọnọdụ ndenye ọgwụ.

Ihe na-arụ ọrụ: pioglitazone hydrochloride nke 15 mg, 30 mg ma ọ bụ 45 mg nke pioglitazone,

Ndị pụrụ iche: lactose monohydrate, cellulose hydroxypropyl, calcium carboxymethyl cellulose na magnesium stearate.

Mpempe mwepụta

Ọgwụ dị n'ụdị mbadamba na 15, 30 na 45 mg. Mbadamba nkume ndị ahụ na-acha ọcha, gbaa gburugburu, a oghere dị n'otu akụkụ na ihe e dere “Actos” n'akụkụ nke ọzọ. A na-ere ọgwụ ahụ na mbadamba 30 n'ime karama.

Ọnụahịa Aktos nwere ntuziaka sitere na 1990 ruo 3300 rubles. Ọ dabere na oke ọgwụ dị na vial ahụ na ọkwa nke ihe na-arụ ọrụ n'ime ya.

Ihe kachasị dị mkpa nke ọgwụ ahụ bụ pioglitazone hydrochloride. Enwere ike ịchọta ya na mbadamba ụrọ nke Actos 15, 30 na 45 mg. Otu n'ime ihe enyemaka nke ọgwụ ahụ bụ:

• celloslose nke carboxymeth,
• hydroxypropyl cellulose,
• lactose monohydrate,
• calcium na magnesium stearate.

Ntụziaka maka ojiji

Site na monotherapy, a na-eji doses nke 15 na 30 mg. N'ọnọdụ ndị siri ike, a na-eji nwayọọ nwayọọ amụba ahụ ruo 45 mg kwa ụbọchị.

N'oge nhazi ahụ, dịka ntuziaka ahụ si dị, a na-eji Aktos eme ihe na 15 mg. Ọnụnọ nke ọnọdụ hypoglycemic bụ oge iji belata usoro ị theụ ọgwụ.

Usoro ọgwụgwọ a na-agwakọta na ọgwụ insulin na-agakọ na 30 mg kwa ụbọchị. A na -ebelata onodu ogwu nke 10-20% n'ihe banyere ịbelata ogo ogo glucose ọbara.

Njirimara ngwa

Iji ngwaahịa a contraindicated n'oge gestation na nri. N'ihi eziokwu ahụ bụ na enwebeghị nnyocha ọmụmụ a na-achịkwa banyere nchekwa nke iji ọgwụ n'oge a, ndị dọkịta amaghị mmetụta pioglitazone ga-enwe n'ahụ ahụ nwa ahụ. Maka nke a, ọ bụrụ na ọ dị mkpa ngwa ngwa iji ọgwụ n'oge ara, a ga-enyefe nwatakịrị ahụ ka ọ na-enye ya ọgwụ ndị na-agwakọta.

Ejighi Actos na ọgwụgwọ ụmụaka na ndị ntorobịa erubeghị afọ 18. Na mgbakwunye, a na-enye ndị mmadụ karịrị afọ iri isii oke oke nlezianya.

N'ime ndị ọrịa nwere usoro ịgba ọgwụ mmanụ na iguzogide insulin n'oge menopause, ọgwụ ahụ na-akwalite mmepe nke ovulation. N'okwu a, ndị ọrịa nwanyị nwere ohere dị ukwuu maka ịtụrụ ime.

Dabere na ntuziaka maka ojiji nke Actos n'ọnọdụ ụfọdụ, pioglitazone na-eduga n'ịba ụba mmiri n'ime ahụ. Nke a na - eduga n’ịzụ oke ike akwara obi. Na ọnụnọ nke ihe mgbaàmà nke usoro a, a na-akwụsị ọgwụ ahụ.

Mgbe nyochachara nke ọma, a na-enye ndị ọrịa ọgwụ vaskụla, yana ọrịa imeju na akụrụ. Ndị ọrịa na-ewere Ketoconazole na Aktosom kwesịrị ilebara shuga ọbara anya.

Mmekọrịta na ọgwụ ndị ọzọ

Ngwá ọrụ na-ebelata mmetụta nke mgbochi ụbụrụ n'ọnụ n'ihi mbelata ọkwa nke norethindrone na ethinylextradiol site na 25-30%. N'ihi ojiji nke Digoxin, Glipizide, anticoagulant na-apụtaghị ìhè na metformin, a naghị ahụ mgbanwe ọgwụ. N'ime ndị ọrịa na-ewere ketoconazole, enwere mwepu nke usoro metabolic metụtara pioglitazone.

Nsonaazụ

N'ihi ọgwụgwọ a na - enwe ụdị insulin na - enweghị nsogbu, a na - ahụta mmetụta ndị ọrịa na - eme ka pioglitazone na - akpasu iwe. N'ime ha, ihe ndị kachasị ewu ewu bụ:

• Usoro ọbara: mbelata nke hematocrit na haemoglobin, yana ọrịa anaemia, nke a na - edekarịkarịrị ọnwa 1-3 mgbe mmalite ọgwụ. Mgbanwe ndị a na-egosi mmụba nke olu mmiri plasma na n'ọbara.
• Ọrịa afọ na - afọ iri: ịba ụba nke enzymes imeju, mmepe nke ịba ọcha n'anya ọgwụ ga-ekwe omume.
• Usoro endocrine: ọnọdụ hypoglycemic.Ihe puru omume na mbelata ọbara shuga n’ihi nkwonkwo nkwonkwo n'oge a na-a administrationụ ọgwụ nke ọgwụ antidiedi bụ 2-3%, na mgbe ị na - eji insulin - 10-15% nke ikpe.
• Nsogbu systemic. Ndị a gụnyere mmepe nke edema, mgbanwe na uru ahụ nke onye ọrịa, yana mbelata nke ọrụ nwa oge nke creatine phosphokinase. Ihe ọghọm ịfụfụ site na iji mbadamba Actos na-abawanye n'oge ọgwụgwọ ọgwụ insulin na-ejikọ.

N'ihe banyere mmepe nke mmetụta dị iche iche, ị kwesịrị ịchọrọ enyemaka ozugbo site n'aka ndị ọkachamara ọkachamara. Mgbanwe mgbanwe dị na ọnụọgụ nke ndị na - ahụ ihe hypoglycemic nwere ike iduga n'ọrịa ahụ na ịmalite nke nsogbu ndị a na - agbanwe agbanwe.

Emeputa

Mwepụta nke ọgwụ mgbochi antioxonia n'okpuru aha akara Actos bụ ụlọ ọrụ ọgwụ America bụ Eli Lilly. E hiwere ụlọ ọrụ ahụ na 1876, a makwaara ya dị ka onye nrụpụta mbụ iji guzobe ọgwụ mmepụta nke insulin n'okpuru aha Humalog na Humulin. Brandlọ ọrụ ọzọ bụ ụlọ ọrụ Prozac, nke a na-ejikarị iji na-agwọ ọrịa nwere nkụda mmụọ.

Mgbe mmepe nke ọgwụ Aktos na ọdịdị nke ọgwụ dị na ahịa, ụlọ ọrụ ọgwụ ọzọ - Takeda Pharmaceutical Company Ltd., otu n'ime ụlọ ọrụ Asia kachasị na nwere ọfịs na Europe na North America, natara ikike ịhapụ ọgwụ ahụ.

Nkọwa na ihe mejupụtara

Ọnụ ọgụgụ nke isi ihe dị na nkwadebe bụ 15 mg, 30 mg na 45 mg na ngwugwu 196 na mbadamba 28. Ihe dị n'ime ọgwụ ahụ bụ pioglitazone n'ụdị nnu hydrochloride. Dika ihe ndi inyeaka, a na-eji lactose, cellulose, calcium na magnesium eme ihe.

Na agbanyeghị usoro onunu ogwu a, ogwu nwere udidi gbara gburu gburu. N’aka aka, enwere ihe osise na ndi ozo ma obu ndi ozo.

Mlọ ọgwụ

Mmetụta ọgwụ a nwere n'ahụ anụ ahụ bụ n'ihi mmekọrịta dị n'etiti otu ndị na - anabata ya - PRAP, nke na - ahazi usoro nkwụpụta site na imechi otu ihe akpọrọ akpọ ligand. Pioglitazone bụ ụdị ligand maka ndị nnabata PRAP dị na mpaghara akwara, eriri olu na umeji.

N'ihi nrụpụta nke pioglitazone-receptor complex, mkpụrụ ndụ ihe “arụpụtara” bụ nke na-achịkwa glucose biotransformation kpọmkwem (ma, n'ihi nke a, na-achịkwa itinye uche ya na ọbara) yana metabolism metabolism.

N'otu oge, Aktos nwere ụdị na-esote nsonaazụ physiological:

• na anụ adi adi - na - achịkwa ihe dị iche nke adipocytes, glucose na - eme site na anụ ahụ na oke nke ụkwara nke necrosis factor type α,
• niime ụlọnga - eme ka ihe banyere ala ha buru ihe,
• n’ime arịa - na-eweghachi ọrụ ọrụ nke endothelium, na-ebelata atherogenicity nke lipids,
• na imeju - na - achịkwa imepụta glucose na lipoproteins nke ukwuu, na-ebelata insulin iguzogide hepatocytes,
• n’ime akụrụ - na - eme ka akụrụngwa rụọ ọrụ na arụmọrụ nke glomeruli.

N'ihi mweghachi nke insulin na -akpata anụ ahụ na-emebi emebi, ịdị ukwuu nke mwepụ insulin na-adabere na-abawanye ma, n'ihi ya, imepụta insulin n'ime imeju na-ebelata. N'okwu a, a na-enweta mmetụta hypoglycemic n'emebighị ọrụ ọrụ nke mkpụrụ ndụ reat-pancreatic.

N'ime ụdị nnwale nke ụdị shuga 2 n'ime anụmanụ, pioglitazone belata hyperglycemia, hyperinsulinemia. Nke a bụ naanị ọgwụ sitere na otu nke triazolidinediones nke na-ahazi ọkwa nke triglycerides n'ọbara na profaịlụ lipid n'ihi ụba lipoproteins. Ya mere, mgbe ị na-ewere Aktos, ikike atherogenic nke dyslipidemia na ndị ọrịa nwere ọrịa shuga mellitus belatara nke ukwuu.

Mlọ ọgwụ

Mgbe ewere ya na usoro ọgwụgwọ, enwere ike ịta ahụhụ nke pioglitazone n'onwe ya na ngwaahịa biotransformation n'ime otu izu. N'otu oge ahụ, ọkwa nke ihe ike nọ n'ọrụ mụbara na njikọta na mmụba na dose nke ọgwụ.

Orkpachara anya. Mgbe nchịkwa ọnụ na-enweghị ọnụ, a na-achọpụta ntinye nke ihe na-arụ ọrụ n'ime ọbara mgbe ọkara elekere gachara, edere ọnụ ọgụgụ kacha elu mgbe awa 2 gachara. Mgbe ị na-a theụ ọgwụ ahụ mgbe nri gachara, oge a nwere ike ịbawanye ma ọ nweghị mmetụta dị ukwuu na oke nnabata ikpeazụ.

Nkesa. Ogologo njuputa nkesa ruru 1.04 l / n'arọ. Pioglitazone (yana ngwaahịa nke mgbanwe metabolic) ya na - ejikọ ya na albumin.

Biotransformation. Uzo mbu nke mmeghachiri ndu ihe banyere mmiri bu hydroxylation na / ma obu oxidation. Na-esote, metabolites na-eji ịta mmiri na glucuronidation emekọta ahụ. A na --akpokọta ngwakọ na nsonaazụ nke biotransformation nwekwara ọgwụgwọ ịgwọ ọrịa. A na-eme metabolism nke pioglitazone site na ntinye nke enzymes hepatic P450 (CYP2C8, CYP1A1 na CYP3A4) na microsomes.

Mwepu. Ruo n’ime otu ụzọ n’ụzọ atọ nke pioglitazone anabatara na mmamịrị. Ọ na-abụkarị mmamịrị, a na-ewepụ ọgwụ ahụ n'ụdị metabolites dị mkpa na conjugates nke abụọ ha. Site n'iji ihe nlere anya mee ihe, ikuku nke pioglitazone na - agbanweghi agbanwe. Oge ikpochapu sitere na awa (maka ụdị ọgwụ izizi) ruo otu ụbọchị (maka ngwaahịa biotransformation na-arụ ọrụ). Usoro ikpochapụ ruru 7 l / h.

Pharmacokinetics n'ụdị ndị ọrịa pụrụ iche. N'iburu ọdịda ezumike ụlọ, mkpochapụ ọkara ndụ anaghị agbanwe. Ma na mwepụ nke creatinine erughị 30 ml / min, a na-eji ọgwụ akpachara anya. Ọrịa imeju na-emetụta paramginetic paramg nke pioglitazone nke ọgwụ ọgwụ. Ya mere, mgbe ị gafere ọkwa transaminases na ALT karịa ugboro 2, a naghị eji ọgwụ ahụ eme ihe.

Achọpụtaghị data maka iji ngwaahịa a na nwata na oge uto (ruo afọ 18). N'ime ndị ọrịa agadi, enwere mgbanwe na ọgwụ ọgwụ ọgwụ, mana ha enweghị ihe dị mkpa maka idozi dose.

Mgbe a na-a drugụ ọgwụ ahụ na usoro onunu ogwu ka ọ dị elu karịa etu nke ndị mmadụ kwuru maka ya, onweghị data enwetara na ọrịa carcinogenicity, mutagenicity ma ọ bụ nsonaazụ nke Aktos na ọmụmụ.

Banyere ihe eji arụ ọrụ

Aha kemịkal nke pioglitazone bụ (()) - 5 - ((4- (2- (5-ethyl-2-pyridinyl) ethoxy) phenyl) methyl) -2,4-) thiazolidinedione monohydrochloride. Isi di iche na uzo ihe si na uzo Metformin na sulfonylurea. Nri ahụ nwere ike ịdị n'ụdị isomers abụọ na-adịghị iche na ọrụ ọgwụgwọ.

Na mpụga, pioglitazone bụ ntụ ntụ na-esi ísì ụtọ. Empkpụrụ ikike ahụ bụ С19Н20N2O3SˑHCl, ịdị arọ molecula 392.90 daltons. Nsogbu na N, N-dimethylfomamide, soluble na ethanol anhydrous, acetone. Ọ fọrọ nke nta insoluble na mmiri na insoluble na ether. Koodu ATX A10BG03.

Etu esi eji: usoro onunu ogwu na usoro ọgwụgwọ

N'ime, oge 1 kwa ụbọchị (n'agbanyeghị nri nri). Monotherapy: 15-30 mg, ọ bụrụ na ọ dị mkpa, enwere ike ịgbatị dose ahụ gaa na 45 mg / ụbọchị. Ngwakọta ọgwụ: mmanụ n'ụkpụrụ sulfonylurea, metformin - ọgwụgwọ na pioglitazone na-amalite site na 15 mg ma ọ bụ 30 mg (ọ bụrụ na hypoglycemia mere, belata dose nke sulfonylurea ma ọ bụ metformin). Ọgwụgwọ yana insulin: usoro izizi bụ 15-30 mg / ụbọchị, ọ̀tụ̀tụ̀ insulin na-adịgide otu ma ọ bụ belata 10-25% (ọ bụrụ na onye ọrịa ahụ na-akọ hypoglycemia, ma ọ bụ plasma glucose concentrated na-erughị 100 mg / dl).

Omume ọgwụ

Hypoglycemic n'ụlọnga nke usoro thiazolidinedione maka nchịkwa ọnụ. Mbelata insulin iguzogide, na-abawanye oriri nke glucose na-adabere ma belata mwepụta nke glucose site na imeju. Na-ebelata nkezi TG, na-eme ka itinye uche nke HDL na cholesterol dịkwuo elu. N'adịghị ka sulfonylurea, ọ naghị akpali insulin mkpuchi. Họrọ na-akpali ndị nnabata gamma nke piroxisome proliferator na-arụ ọrụ (PPAR). A na - achọta ndị na - anabata PPAR na anụ ahụ na - arụ ọrụ dị mkpa na usoro nke insulin (adipose, anụ ahụ akwara na akwara). Ọrụ nke ndị na-anabata ọgwụ nuklia nke PPAR na-emegharị ntụgharị nke ọtụtụ mkpụrụ ndụ ihe ọmụmụ insulin na-etinye aka na nchịkwa nke glucose ọbara na metabolism metabolism.

Ntụziaka pụrụ iche

A na-egosipụta mmetụta hypoglycemic naanị n'ihu ọnụnọ insulin. N'ime ndị ọrịa nwere insulin na-eguzogide ọgwụ na usoro nke anovulatory n'oge premenopausal, ọgwụgwọ nwere ike ibute ovulation. Nsonaazụ nke imeziwanye ọgụgụ ndị ọrịa a ka insulin bụrụ ihe egwu dị na ime ọ bụrụ na ejighị ezigbo mgbochi. N'oge ọgwụgwọ, mmụba nke olu plasma na mmepe nke hypertrophy nke akwara obi (n'ihi ebugo ya) ga-ekwe omume. Tupu mmalite na ọnwa abụọ ọ bụla n'afọ mbụ nke ọgwụgwọ, ọ dị mkpa iji nyochaa ọrụ nke ALT.

Nhọrọ

Etu usoro maka ọgwụgwọ ụdị ọrịa shuga abụọ na-arịa ọrịa shuga, na mgbakwunye na ị na-ewere Actos, ekwesịrị ịgụnye usoro ọgwụgwọ nri na mmega ahụ akwadoro. Nke a dị mkpa ọ bụghị naanị na mmalite nke ụdị ọrịa shuga 2 ọrịa shuga, kamakwa. iji kwado ike ịgwọ ọrịa ọgwụ.

Fegwọ arụmọrụ ọgwụ dị mma ka ị chọpụta ọkwa nke HbAic, nke kachasị gosipụta njikwa glycemic ruo ogologo oge, ma e jiri ya na mkpebi siri ike nke naanị glycemia na-ebu ọnụ. HbA1C na-egosipụta glycemia n'ime ọnwa abụọ na atọ gara aga.

A na-atụ aro ọgwụgwọ na Aktos ruo oge zuru ezu iji chọpụta mgbanwe dị na ọkwa HbA1C (ọnwa atọ), ma ọ bụrụ na enweghi mmebi na njikwa glycemic. N'ime ndị ọrịa nwere insulin iguzogide na usoro nke anovulatory n'oge premenopausal, ọgwụgwọ na thiazolidinediones, gụnyere ọgwụ Aktos, nwere ike ibute ovulation. Nsonaazụ nke imeziwanye ọgụgụ ndị ọrịa a ka insulin bụrụ ihe egwu dị na ime ọ bụrụ na ejighị ezigbo mgbochi.

Ekwesịrị iji nlezianya mee ihe maka ndị ọrịa nwere edema.

Pioglitazone nwere ike ibute njigide mmiri n'ime ahụ, ma mgbe ejiri ya dịka monotherapy yana yana ọgwụ ndị ọzọ na-alụso ọrịa ọgụ, gụnyere insulin. Idebe onwe onye n’arụ n’ahụ nwere ike iduba mmadụ n’iru ma ọ bụ mee ka ọ kawanye njọ n’ọkpụkpụ obi. Ọ dị mkpa ịchịkwa ọnụnọ nke ihe mgbaàmà na akara nke nkụda obi, ọkachasị yana mbelata obi.

N'ihe banyere nbibi ọ bụla na ọrụ gbasara obi, a ga-akwụsị pioglitazone.

A kọwara usoro nke nkụda obi na iji pioglitazone yana njikọ insulin.

Ebe ọ bụ na ọgwụ mgbochi mkpali na steroidal na pioglitazone na-ebute njigide mmiri n'ime ahụ, njikwa njikọta nke ọgwụ ndị a nwere ike ịbawanye ohere nke edema.

Ekwesịrị ilebara anya nke ọma mgbe ị na-edepụta ọgwụ ahụ nye ndị ọrịa nwere ọrịa obi, gụnyere infarction myocardial, angina pectoris, cardiomyopathy na ọnọdụ ọbara na-enye aka na mmepe nke ọdịda obi.

Ebe ọ bụ na mmụba nke olu na-ekesa ọbara nwere ike ibute ngwa ngwa edema ma kpatara ma ọ bụ nwekwuo ngosipụta nke nkụchi obi, a ga-akwụ ụgwọ nlebara anya na ndị a:

Ekwesighi inye ndị ọrịa nwere nkụda mmụọ akụrụngwa Aktos mbadamba ma ọ bụ nwee nkụda obi.

Ọ dị mkpa iji nlezianya nyochaa ndị ọrịa na-ewere Actos. N'ihe banyere edema, mmụba dị ukwuu na ahụ mmadụ, ọdịdị nke ihe mgbaàmà nke obi obi, wdg, ekwesịrị ime ihe mmegwara, dịka ọmụmaatụ, kwụsị ị Akụ ọgwụ Aktos, depụta loop diuretics (furosemide, wdg).

Ọ dị mkpa ịkụziri onye ọrịa banyere edema, mmụba dị ukwuu n’arụ ahụ, ma ọ bụ mgbanwe mgbanwe ọ bụla nwere ike ịpụta mgbe ị na-ewere Actos, ka onye ọrịa ahụ kwụsị ị takingụ ọgwụ ahụ ozugbo ma gakwuru dọkịta.

Ebe ọ bụ na ị Akụ ọgwụ ọgwụ Aktos nwere ike ibute ndagwurugwu na ECG ma nwekwuo oke kadio-thoracic, ndekọ ECG kwa oge dị mkpa. Ọ bụrụ na achọtara ihe na - adịghị mkpa, ekwesịrị ịtụleghachi usoro nke ọgwụ ahụ, enwere ike wepu ya ma ọ bụ wedata ya obere oge.

N'ime ndị ọrịa niile, tupu ọgwụgwọ ya na Aktos, a ga-ekpebi ọkwa ALT, ekwesịrị ịme nyocha a kwa ọnwa abụọ na afọ mbụ nke ọgwụgwọ yana mgbe oge gafere.

Ekwesịrị ime nyocha iji chọpụta ọrụ umeji ma ọ bụrụ na onye ọrịa ebulite mgbaama na-atụ aro ọrụ imeju, dịka ọmụmaatụ, ọgbụgbọ, ọgbụgbọ, mgbu afọ, ike ọgwụgwụ, enweghị agụụ, mmamịrị gbara ọchịchịrị. Mkpebi banyere ịga n'ihu ọgwụgwọ ya na Aktos kwesịrị ịdabere na data nyocha, na-eburu n'uche usoro plọg.

N'ihe banyere jaundice, a ga-akwụsị ịhapụ ị withụ ọgwụ ahụ.

Ekwesighi ịmalite ọgwụgwọ na Aktos ma ọ bụrụ na onye ọrịa ahụ gosipụtara ngosipụta ọgwụgwọ nke ụzọ ọrụ ike nke ọrịa imeju ma ọ bụ ọkwa ALT gafere oke nke ụkpụrụ ahụ site na oge 2.5.

A ga-enyocha ndị ọrịa nwere ọkwa dị elu nke enzymes imeju (ọkwa ALT 1-2.5 karịa oke elu nke nkịtị) tupu ọgwụgwọ ma ọ bụ n'oge ọgwụgwọ na Aktos iji chọpụta ihe kpatara mmụba nke ọkwa enzyme ndị a. Ekwesịrị ịmalite ma ọ bụ n'ihu ọgwụgwọ na Aktos nwere ndị ọrịa nwere mmụba dị elu na ọkwa nke enzymes imeju na ịkpachara anya.

Na nke a, a na-atụ aro ka ị na-agbakarị ndị na-ahụ maka onyonyo a na-eleba anya na ọmụmụ gbasara ọrụ enzymes “imeju”. Maka ihe mmụba na ọkwa ọbara serminase (ALT> ihe dị ka okpukpu abụọ karịa oke dị elu nke iwu), ekwesịrị ileba anya na-arụ ọrụ nke imeju ọtụtụ oge ruo mgbe ọkwa ahụ ga-alaghachi na nkịtị ma ọ bụ ọkwa ndị a hụrụ tupu ọgwụgwọ.

Ọ bụrụ na ọkwa ALT dị elu karịa ogo elu nke ụkpụrụ, mgbe ahụ, a ga-eme nnwale nke abụọ iji chọpụta ọkwa ALT ozugbo enwere ike. Ọ bụrụ na edobere ọkwa ALT na ogo 3 karịa nke elu karịa nke kwesịrị, mgbe ahụ ịkwesịrị ịhapụ ọgwụ na Aktos. Tupu ịmalite ọgwụgwọ na Aktos na ọnwa 2 ọ bụla n'afọ mbụ nke ọgwụgwọ, a na-atụ aro ka nyochaa ọkwa nke ALT.

A ga-enyocha ndị ọrịa na-anata ketoconazole na Actos mgbe niile maka glucose.

Tebụl usoro ọgwụgwọ

Nkwụsị nke ọgwụgwọ

Ikekwe naanị na uche nke dọkịta.

N'ime usoro analogues nke ọgwụ ọgwụ Aktos mbụ, ndị dọkịta nwere ike inye ọgwụ ndị a:

• Amalvia (Teva, Israel),
• Astrozone (Onye na-ere ọgwụ - Leksredstva, Russia),
• Diab-Norm (onye nnọchite anya KRKA, Russia),
• Pioglar (Ranbaxy, India),
• Pioglite (ụlọ ọrụ Sun na-emepụta ọgwụ, India),
• Piouno (WOCKHARDT, India).

Aha ndebanye aha ndị a na Russian Federation.

Ọnụahịa na ebe ịzụta

Na Russia, Aktos debara aha ya na mbido, mana ugbu a nkwekọrịta akwụkwọ ikike enyerela ikike ya, ọgwụ ahụ naanị na Europe. Amachibidoro ire ire ahịa na ụlọ ahịa na Moscow, St. Petersburg na obodo ndị ọzọ nke mba a machibidoro iwu.

Ma ị nwere ike ịgwa ọgwụ ka ọ dị site na Germany na mbufe na Russia, kpọtụrụ ụlọ ọrụ na-ahụ maka enyemaka maka enyemaka. Ihe nkwakọ ngwaahịa nke mbadamba 196 nke nwere 30 mg dị ihe dịka 260 euro (ewezuga njem nke usoro ahụ). Nwere ike ịzụta mbadamba Aktos 30 mg na ọnụ ahịa nke ihe dịka euro 30 maka mkpụrụ 28.

Ndi dibia nyocha

Oksana Ivanovna Kolesnikova, endocrinologist

Site na ahụmịhe nke m, enwere m ike ikwu na ọbụnadị Aktosom monotherapy na mbido ọrịa ahụ, ọkachasị yana nri na mmega ahụ, nwere ike ịnwe ọkwa glucose. N'okwu a, ọgwụ ọgwụ anaghị akpata nsonaazụ.

Etu esi ere ahia adighi nma

Iji zere ịzụta ngwaahịa adịgboroja, ị ga-ahọrọ onye ọka iwu tụkwasịrị obi nke ga-eweta akwụkwọ ego mbụ sitere na ụlọ ahịa ọgwụ si mba ọzọ ma wepụta oge nnyefe zuru oke maka ọgwụ na Russia. Na nnata, ikwesiri inyocha nnabata nke akara a na ngwugwu ma were mbadamba nkume belata.

Nsonaazụ nnwale nke Clinical

A na-atụle arụmọrụ nke pioglitazone dị ka monotherapy yana yana njikọta metformin na nyocha ụlọ ọgwụ metụtara ndị ọrịa 85. E kee ndị ọrịa ụzọ abụọ, nke 3% kwụsịrị ọgwụgwọ ejikọtara ya na mmepe nke nnukwu nsogbu. Mgbe izu 12 gasị, ọkwa glucose gbadara n’etiti ndị ọrịa niile fọdụrụ n’ime nnwale ahụ.

Enwetara nsonaazụ ndị yiri nke a n'ọmụmụ metụtara ndị ọrịa 800. Ntinye uche nke HbAlc dara site na 1.4% ma ọ bụ karịa. Ọzọkwa chọpụtara mbelata lipoproteins dịkarịsịrị nta, kọlestrọl ọnụ ala, ebe n'otu oge ahụ, mkpụrụ ndụ nke lipoproteins dị elu mụbara.

Hypoglycemic ọgwụ Aktos: ntuziaka, ọnụahịa na nyocha na ọgwụ

Didị ndị ọrịa shuga 2dị nke abụọ ga-ewere ọgwụ hypoglycemic maka ndụ iji nọgide na-enwe ahụike nkịtị ma gbochie nsogbu nke ọrịa ahụ.

Ọtụtụ ndị dọkịta na-enye ndụmọdụ iji Actos. Nke a bụ ọgwụ nje thiazolidinedione. A tụlere atụmatụ na nyocha nke ọgwụ a n'isiokwu ahụ.

Ngwakọta ọgwụ ahụ

Isi ihe dị na Actos bụ pioglitazone hydrochloride. Ihe inyeaka bụ lactose monohydrate, magnesium stearate, calcium carboxymethyl cellulose, hydroxypropyl cellulose.

Actos 15 mg

A na-emepụta ọgwụ ahụ n'ụdị mbadamba. Enwere mbadamba nkume nwere ihe dị ike na mkpokọta nke 15, 30 na 45 mg. Capsules gbara gburugburu n'ụdị, biconvex, nwere agba ọcha. A na-adọpụ "ACTOS" n'otu akụkụ, yana "15", "30" ma ọ bụ "45" n'akụkụ nke ọzọ.

Ezubere Actos maka ịgwọ ndị nwere ọrịa shuga na-arịa ọrịa shuga. A na-eji ya na capsu ndị ọzọ na-akpali mmepụta insulin, inje nke homonụ ma ọ bụ dị ka monotherapy.

A na-eji ọgwụ ahụ dabere na nri siri ike, mmega ahụ zuru oke.

Vidiyo ndị metụtara

Banyere ụdị ọgwụ eji eme shuga na vidiyo:

N'ihi ya, Actos na-ebelata oke mkpokọta nke glycemia na plasma, mkpa ịba insulin. Mana ọgwụ hypoglycemic adabaraghị onye ọ bụla, a naghị anabata ya nke ọma dịka akụkụ nke njikọta ọgwụgwọ.

N'ihi ya, a nwaakwa ahụike gị ma zụta ọgwụ na ndụmọdụ nke ndị enyi. Ọ bụ ọkachamara ga-eme mkpebi banyere ikwekọrịta ịgwọ ọrịa shuga na Actos.

Uzo esi ewere Actos

A na-ekpebi usoro onunu ogwu n’otu n’otu, 1 mbadamba / ụbọchị, n’agbanyeghi nri. Dịka ọgwụ monotherapy, enyere ọgwụ Aktos ka ọ bụrụ na nri antidiabetic adịghị arụ ọrụ nke ọma, na-amalite site na 15 mg / ụbọchị. Usoro ịba ụba na-abawanye na ọkwa. Oke kachasị kwa ụbọchị bụ 45 mg. Site na usoro ọgwụgwọ ya ezughi ezu, a na-enye ọgwụ ndị ọzọ.

Mgbe ị na-ehiwe ọgwụgwọ njikọta, a na-ebelata ọgwụ mbụ nke pioglitazone na 15 ma ọ bụ 30 mg / ụbọchị. Mgbe agbakọtara Aktos na metformin, ihe ize ndụ nke hypoglycemia dị ala. Mgbe agwakọtara na sulfonylurea na insulin, achọrọ njikwa glycemic. Usoro kasịnụ nke ọgwụ a na usoro ọgwụgwọ siri ike agaghị agafe 30 mg / ụbọchị.