Aktos kukonzekera kwa pakamwa kwa hypoglycemic ya mndandanda wa thiazolidinedione, momwe zotsatira zake zimatengera kukhalapo kwa insulin. Ndi agonist yosankha bwino kwambiri ya gamma receptors yokhazikitsidwa ndi peroxisome proliferator (PPAR-γ). Ma receptors a PPAR-γ amapezeka mu adipose, minofu ya minofu ndi chiwindi. Kutsegula kwa zida za nyukiliya za PPARγ modulates module ya mitundu ingapo yamtundu wa insulin yomwe ikukhudzidwa ndi kayendedwe ka glucose ndi lipid metabolism

Actos amachepetsa kukana kwa insulini mu chiwopsezo cha zotumphukira ndi chiwindi, zomwe zimapangitsa kuti chiwonetsero cha glucose chodalira insulin ndi kuchepa kwamasulidwe a shuga chiwindi. Mosiyana ndi kukonzekera kwa sulfonylurea, pioglitazone simalimbikitsa kubisalira kwa insulin mwa maselo a pancreatic beta.

Odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga, kuchepa kwa insulin chifukwa cha mankhwala a Actos amachititsa kuchepa kwa kuchuluka kwa shuga m'magazi, kuchepa kwa insulini mu plasma ndi index ya HbA1C. Kuphatikiza ndi sulfonylurea kukonzekera, metformin kapena insulin, mankhwalawa amathandizira kuwongolera kwa glycemic.

Odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga omwe ali ndi vuto la lipid metabolism panthawi yamankhwala, pali kuchepa kwa triglycerides ndi kuwonjezereka kwa zomwe zimakhala kwambiri osalimba a lipoproteins. Nthawi yomweyo, kusintha kwa milingo yokhala ndi osachepera lipoprotein ndi cholesterol yathunthu mwa odwala sikuwonedwa.

Zogulitsa. Akamamwa pamimba yopanda kanthu, pioglitazone imadziwika mu seramu ya magazi pambuyo pa mphindi 30, kuchuluka kwakukulu kumachitika pambuyo pa maola awiri. Kudya kumayambitsa kuchepa pang'ono pofika pazovuta zambiri, zomwe zimawonedwa pambuyo pa maola 3-4, koma chakudya sichisintha mayamwidwe athunthu.

Kugawa. Kuchulukitsa komwe kumawoneka (Vd / F) kwa pioglitazone pambuyo pa kumwa kamodzi kumakhala pafupifupi 0.63 ± 0.41 (kutanthauza ± SD squared) l / kg thupi. Pioglitazone imamangidwa makamaka pamapuloteni a seramu a anthu (> 99%), makamaka a albin. Pocheperako, zimagwirizanitsa ndi mapuloteni ena a seramu. Ma metabolites a pioglitazone M-III ndi M-IV amakhudzidwanso kwambiri ndi serum albin (> 98%).

Kupenda. Pioglitazone imapangidwa mwamphamvu kwambiri chifukwa cha hydroxylation ndi oxidation zimachitika ndi mapangidwe a metabolites: metabolites M-II, M-IV (pioglitazone hydroxide derivatives) ndi M-III (pioglitazone keto derivatives). Ma metabolabolite nawonso amasinthidwa pang'ono kukhala ma conjugates a glucuronic kapena sulfuric acid. Pambuyo popereka mankhwala mobwerezabwereza, kuphatikiza pioglitazone, metabolites ya M-III ndi M-IV, omwe ali othandizira kwambiri, amapezeka mu seramu yamagazi. Mothandizana, kuchuluka kwa pioglitazone ndi 30% -50% ya kuchuluka kwathunthu mumsinga komanso kuchokera 20% mpaka 25% ya malo onse omwe amapangidwira.

Metabolite ya hepatic ya pioglitazone imachitika ndi isoforms yayikulu ya cytochrome P450 (CYP2C8 ndi CYP3A4). Pakufufuza kwa in vitro, pioglitazone sichiletsa ntchito ya P450. Kafukufuku wokhudzana ndi ntchito ya pioglitazone pazomwe zimachitika mwa ma enzymes mwa anthu sanachitidwe.

Kuswana. Pambuyo pakulowetsa, pafupifupi 15% -30% ya mlingo wa pioglitazone umapezeka mkodzo. Mlingo wosasunthika wa pioglitazone wosasinthika umatulutsidwa kudzera mu impso, umapukusidwa makamaka mu mawonekedwe a metabolites ndi ma conjugates. Mukamamwa, ambiri mwa mankhwalawa amachotsedwa mu ndulu, zonse osasinthika komanso mawonekedwe a metabolites, ndikuchotsa m'thupi ndi ndowe.

Pakati theka la moyo wa pioglitazone ndi pioglitazone yathunthu (pioglitazone ndi metabolites yogwira) imayambira maola atatu mpaka 7 komanso kuchokera maola 16 mpaka 24, motsatana. Chilolezo chonse ndi 5-7 l / ola.

Kuzindikira kwa pioglitazone kwathunthu mu seramu kumakhalabe pamalo okwera maola 24 pambuyo pa tsiku limodzi.

Njira yogwiritsira ntchito

Actos ayenera kumwedwa kamodzi patsiku, mosasamala kanthu zakudya.

Mlingo wa mankhwalawa umayikidwa ndi dokotala payekhapayekha.

Monotherapy ndi Aktos mwa odwala omwe kulipira shuga sikumatheka ndi chithandizo chamankhwala ndipo masewera olimbitsa thupi amathanso kuyamba ndi 15 mg kapena 30 mg kamodzi tsiku lililonse. Ngati ndi kotheka, mlingo umatha kuwonjezeka pang'onopang'ono mpaka 45 mg kamodzi patsiku. Ngati monotherapy ndi mankhwalawa singathandize, mwayi wophatikizira mankhwala uyenera kuganiziridwanso.

Zothandiza kuchokera ku sulfonylureas. Kuchiza ndi Aktos osakanikirana ndi sulfonylurea kumatha kuyamba ndi 15 mg kapena 30 mg kamodzi tsiku lililonse. Kumayambiriro kwa chithandizo ndi Aktos, mlingo wa sulfonylurea ungasiyidwe osasinthika. Ndi chitukuko cha hypoglycemia, mlingo wa sulfonylurea uyenera kuchepetsedwa.

Metformin. Kuchiza ndi Aktos osakanikirana ndi metformin kumatha kuyamba ndi 15 mg kapena 30 mg kamodzi patsiku. Kumayambiriro kwa chithandizo ndi Aktos, mlingo wa metformin ukhoza kusunthidwa osasinthika. Kukula kwa hypoglycemia ndi kuphatikiza uku sikungatheke, chifukwa chake, kufunika kwa kusintha kwa mlingo wa metformin sikungatheke.

Insulin Kuchiza ndi Aktos osakanikirana ndi insulin kumatha kuyamba ndi 15 mg kapena 30 mg kamodzi tsiku lililonse. Kumayambiriro kwa mankhwalawa ndi Aktos, mlingo wa insulin ungasiyidwe osasinthika. Odwala omwe amalandira Actos ndi insulin, ndi kukula kwa hypoglycemia kapena kuchepa kwa glucose wambiri mpaka osachepera 100 mg / dl, mlingo wa insulin ungachepetse 10% -25%. Chinanso cha kusintha kwa insulin kuyenera kuchitika payekhapokha potengera kuchepa kwa glycemia.

Mlingo wa Aktos wokhala ndi monotherapy sayenera kupitirira 45 mg / tsiku.

Kuphatikiza mankhwala, mlingo wa Aktos suyenera kupitirira 30 mg / tsiku.

Odwala aimpso kulephera, kusintha kwa Actos sikofunikira. Zambiri pakugwiritsa ntchito Aktos kuphatikiza ndimankhwala ena a thiazolidatedione palibe.

Contraindication

• Hypersensitivity pioglitazone kapena chimodzi mwazinthu za mankhwala,
• mtundu 1 shuga
• matenda ashuga ketoacidosis,
• mimba, yoyamwitsa,
• kulephera kwamtima kwambiri kwa III-IV digiri malinga ndi NYHA (New York Heart Association),
• wazaka 18.

Matenda a Edema, kuchepa kwa magazi, kuchepa kwa chiwindi (kuchuluka kwa michere ya chiwindi 1-2.5 nthawi yayitali kuposa malire apamwamba), kulephera kwa mtima.

Zotsatira zoyipa

Odwala omwe amatenga ma Actos osakanikirana ndi insulin kapena mankhwala ena a hypoglycemic, chitukuko cha hypoglycemia chimatheka (2% milandu ndikuphatikizana ndi sulfonylurea, 8-15% ya milandu yophatikizana ndi insulin).

Pafupipafupi magazi m'thupi mu monotherapy ndi kuphatikiza mankhwala ndi Actos amachokera ku 1% mpaka 1.6% ya milandu.

Actos amatha kuyambitsa kuchepa kwa hemoglobin (2-4%) ndi hematocrit. Kusintha kumeneku kumawonedwa pakadatha masabata 4-12 chiyambireni mankhwala ndikukhazikika. Samalumikizidwa ndi zovuta zilizonse zamatenda a hematological ndipo nthawi zambiri zimachitika chifukwa cha kuchuluka kwa plasma.

Pafupipafupi kukula kwa edema ndi monotherapy ndi 4.8%, ndi chithandizo cha mankhwala limodzi ndi insulin - 15,3%. Pafupipafupi kuchuluka kwa thupi ndikumatenga Actos kumakhala pafupifupi 5%.

Pafupipafupi kuchuluka kwa ntchito ya hepatic Enzymes alanine aminotransferase (ALT)> katatu kuchokera kumalire apamwamba ndi pafupifupi 0.25%.

Osati kawirikawiri, kutukuka kapena kupita patsogolo kwa matenda ashuga a macular edema, limodzi ndi kuchepa kwa kuwona kwa chidwi. Kudalira kwachindunji kwa chitukuko cha macular edema pakudya pioglitazone sikunakhazikitsidwe. Madokotala ayenera kuganizira kuthekera kotukula macular edema ngati odwala akudandaula chifukwa cha kuchepa kowonekera.

M'maphunziro omwe amayendetsedwa ndi placebo ku United States, kuchuluka kwa zotsatira zoyipa zamagetsi zomwe zimakhudzana ndikuwonjezereka kwa magazi ambiri sizinasiyane mwa odwala omwe amachitidwa ndi Actos okha komanso kuphatikiza ndi sulfonylurea, metformin, kapena placebo. Mu kafukufuku wazachipatala, munthawi yomweyo ndikupereka mankhwala Aktos ndi insulin ochepa odwala omwe anali ndi mbiri yamatenda a mtima, panali zochitika za mtima wovuta. Odwala omwe ali ndi vuto la mtima la magawo a III ndi IV omwe amagwira ntchito molingana ndi gulu la NYHA (New York Heart Association) sanatenge nawo mbali pazoyeserera zamankhwala pakugwiritsa ntchito mankhwalawa, chifukwa chake, Aktos amatsutsana ndi gulu ili la odwala.

Malinga ndi tsatanetsatane wa malonda a Aktos, milandu yodwalika ya mtima idanenedwa mwa odwala, mosasamala kanthu za zizindikiro zamatenda amtima omwe adalipo kale.

Gwiritsani ntchito panthawi yoyembekezera komanso poyamwitsa

Maphunziro okwanira komanso owongoleredwa moyenera mwa amayi apakati sanachitike. Sizikudziwika ngati Aktos amachotsedwa mkaka wa m'mawere, chifukwa chake, Aktos sayenera kutengedwa ndi amayi omwe akuyamwitsa.

Ngati ndi kotheka, kuikidwa kwa mankhwalawa panthawi yoyamwitsa, kuyamwitsa kuyenera kutha.

Bongo

Mankhwala osokoneza bongo a Aktos omwe ali ndi monotherapy samayendera limodzi ndi kupezeka kwa zizindikiro zapadera za matenda.

Mankhwala osokoneza bongo a Actos osakanikirana ndi sulfonylurea amatha kuphatikizidwa ndi kukula kwa zizindikiro za hypoglycemia. Palibe chithandizo chenicheni cha bongo. Syndrome dalili zimafunika (mwachitsanzo, chithandizo cha hypoglycemia).

Kuchita ndi mankhwala ena

Akaphatikizidwa ndi sulfonylurea kapena insulin, hypoglycemia imayamba.

CYP2C8 inhibitors (mwachitsanzo gemfibrozil) ikhoza kuwonjezera malowa m'mbali mwa pioglitazone concentration motsutsana ndi nthawi ya AUC), pomwe CYP2C8 inducers (mwachitsanzo rifampicin) imatha kuchepetsa pioglitazone AUC. Kuphatikizika kwa pioglitazone ndi gemfibrozil kumabweretsa kuwonjezeka katatu kwa AUC ya pioglitazone. Popeza kuwonjezeka kumeneku kungapangitse kuwonjezeka kwa mlingo wa pioglitazone, kugwiritsa ntchito mankhwalawa ndi gemfibrozil kungafunike kuchepa kwa pioglitazone.

Kugwiritsa ntchito kwa pioglitazone ndi rifampicin kumabweretsa kutsika kwa 54% mu AUC ya pioglitazone. Kuphatikiza koteroko kungafunike kuwonjezeka kwa mlingo wa pioglitazone kuti akwaniritse matenda.

Odwala omwe amatenga ma Actos ndi njira zakulera zapakati, kuchepa kwa mphamvu zakulera ndikotheka.

Palibe kusintha kwa pharmacokinetics ndi pharmacodynamics pomwe mukumwa ma Actos omwe amakhala ndi glipizide, digoxin, anticoagulants, metformin. Mu vitro ketoconazole linalake ndipo tikulephera kagayidwe ka pioglitazone.

Palibe chidziwitso cha kuphatikiza kwa pharmacokinetic kwa Actos omwe ali ndi erythromycin, astemizole, calcium blockers blockers, cisapride, corticosteroids, cyclosporine, lipid-lowering drug (statins), tacrolimus, triazolam, trimethrexate, ketoconazole, ndi itraconazole.

Malo osungira

Kutentha kwa 15-30 ° C pamalo otetezedwa ku chinyezi ndi kuwala. Pewani kufikira ana. Mndandanda B.

Alumali moyo 3 zaka.

Zomwe zalembedwa.

Chithandizo chogwira: pioglitazone hydrochloride yofanana ndi 15 mg, 30 mg kapena 45 mg ya pioglitazone,

Omwe amathandizira: lactose monohydrate, hydroxypropyl cellulose, calcium carboxymethyl cellulose ndi magnesium stearate.

Kutulutsa Fomu

Mankhwalawa amapezeka mu mawonekedwe a piritsi pa 15, 30 ndi 45 mg. Mapiritsiwo ndi oyera, wozungulira bwino, woboola mbali imodzi ndipo mawu akuti "Actos" mbali inayo. Mankhwalawa amagulitsidwa m'mapiritsi 30 m'mabotolo.

Mtengo wa Aktos ndi malangizo ndi wochokera ku 1990 mpaka 3300 rubles. Zimatengera kuchuluka kwa mankhwalawo mu vial ndi kuchuluka kwa zinthu zomwe zimagwira.

Chofunikira chachikulu pa mankhwalawa ndi pioglitazone hydrochloride. Itha kupezeka pamapiritsi a Actos 15, 30 ndi 45 mg. Zina mwazinthu zothandizira za mankhwalawa ndi:

• carboxymethyl cellulose,
• hydroxypropyl cellulose,
• lactose monohydrate,
• calcium ndi magnesium stearate.

Malangizo ogwiritsira ntchito

Ndi monotherapy, Mlingo wa 15 ndi 30 mg umagwiritsidwa ntchito. Woopsa milandu, mlingo umakulitsidwa pang'onopang'ono mpaka 45 mg tsiku lililonse.

Panthawi yamavuto, malinga ndi malangizo, Aktos amagwiritsidwa ntchito muyezo wa 15 mg. Kukhalapo kwa zinthu za hypoglycemic ndi mwayi wochepetsa kuchuluka kwa mankhwalawa.

Kuphatikiza chithandizo ndi insulin kukonzekera kumayendetsedwa ndi mlingo wa 30 mg patsiku. Mlingo wa mankhwalawa umachepetsedwa ndi 10-20% pang'onopang'ono kuchepa kwamagazi a shuga.

Zolemba ntchito

Kugwiritsa ntchito kwazinthu zomwe zimapangidwa kumayesedwa pakhungu ndi kudya. Chifukwa chakuti pakhala palibe maphunziro owongoleredwa okhudza kugwiritsa ntchito mankhwalawa nthawi izi, madokotala sakudziwa kuti pioglitazone ingakhudze bwanji thupi la mwana. Pachifukwa ichi, ngati pakufunika kugwiritsa ntchito mankhwalawa nthawi ya mkaka wa m`mawere, mwana ayenera kupita ku kudyetsa ndi zosakaniza kupanga.

Actos sagwiritsidwa ntchito pochiza ana ndi achinyamata ochepera zaka 18. Kuphatikiza apo, anthu opitilira 60 amakhala mosamala kwambiri.

Odwala ndi anovulatory kuzungulira ndi insulin kukana pa kusintha kwa thupi, mankhwala amalimbikitsa kukula kwa ovulation. Pankhaniyi, odwala azimayi ali ndi chiopsezo chowonjezereka cha kutenga pakati.

Malinga ndi malangizo ogwiritsira ntchito Actos nthawi zina, pioglitazone imapangitsa kuti madzi azikhala mokwanira m'thupi. Izi zimapangitsa kuti pakhale kulephera kwa minofu ya mtima. Pamaso pa zizindikiro za matenda amtunduwu, mankhwalawa amasiya.

Mukawunika mozama, mankhwalawa amaperekedwa kwa anthu omwe ali ndi mtima wamitsempha yamagazi, komanso matenda a chiwindi ndi impso. Odwala omwe amatenga Ketoconazole osakanikirana ndi Aktosom ayenera kuwunika shuga wamagazi pafupipafupi.

Kuchita ndi mankhwala ena

Chidachi chimachepetsa kwambiri mphamvu zakulera pakamwa chifukwa kuchepa kwa msana wa norethindrone ndi ethinylextradiol ndi 25-30%. Chifukwa cha kugwiritsa ntchito Digoxin, Glipizide, anticoagulant komanso metformin, kusintha kwa mankhwala sikuwunikidwa. Odwala omwe amatenga ketoconazole, pali kuponderezedwa kwa kagayidwe kachakudya ka pioglitazone.

Zotsatira zoyipa

Chifukwa cha mankhwalawa chifukwa cha matenda omwe amadzisokoneza okha insulin, zotsatira zoyipa zimawonedwa mwa odwala omwe amakwiya chifukwa cha pioglitazone. Pakati pawo, omwe ali ambiri ndi:

• Dongosolo la magazi: kuchepa kwa hematocrit ndi hemoglobin, komanso magazi m'thupi, omwe nthawi zambiri amalembedwa patangotha ​​miyezi itatu chichitikireni mankhwala. Kusintha kumeneku kukuwonetsa kuchuluka kwamadzi am'madzi a m'magazi.
• M`mimba thirakiti: kuchuluka secretion wa chiwindi michere, kukula kwa mankhwala a chiwindi ndi kotheka.
• Dongosolo la endocrine: machitidwe a hypoglycemic.Kuchepa kwa kuchepa kwa shuga m'magazi chifukwa cha kuphatikiza mankhwalawa pakumwa mankhwala a antidiabetic ndi 2-3%, ndipo mukamagwiritsa ntchito insulin - 10-15% milandu.
• Zovuta zamachitidwe. Izi zimaphatikizira kukula kwa edema, kusintha kwa thupi la wodwalayo, komanso kuchepa kwa zochitika zaposachedwa za creatine phosphokinase. Kuopsa kwa puffness ndi kugwiritsa ntchito mapiritsi a Actos kumawonjezeka panthawi yophatikiza ndi mankhwala a insulin.

Ngati mukuyambitsa mavuto, muyenera kufunafuna chithandizo kuchokera kwa akatswiri akatswiri. Kusintha kwayekha kwa mlingo wa hypoglycemic othandizira kungayambitse kukula kwa matendawa ndikupanga zovuta zosasinthika.

Wopanga

Kutulutsidwa kwa mankhwala othandizira odwala matenda ashuga omwe amadziwika ndi dzina loti Actos amatsogozedwa ndi kampani yaku America ya mankhwala a Eli Lilly Company. Bungweli lidakhazikitsidwa mu 1876 ndipo limadziwika kuti ndi woyamba kupanga kukhazikitsa ma insulin popanga mayina a Humalog ndi Humulin. Mtundu wina wa kampaniyo ndi Prozac ya mankhwala, omwe amagwiritsidwa ntchito kwambiri pochiza matenda ovutika maganizo.

Pambuyo pakupanga mankhwala Aktos ndikuwoneka kwa mankhwalawo pamsika, kampani ina yopanga mankhwala - Takeda Pharmaceutical Company Ltd., imodzi mwa makampani akuluakulu ku Asia omwe ali ndi maofesi ku Europe ndi North America, adalandira chilolezo chomasula mankhwalawo.

Kufotokozera ndi kapangidwe

Kuchuluka kwa zosakaniza zazikulu pakukonzekera ndi 15 mg, 30 mg ndi 45 mg m'mapaketi a 196 ndi mapiritsi 28. The yogwira pophika mankhwala ndi pioglitazone mu mawonekedwe a hydrochloride mchere. Monga zida zothandizira, lactose, cellulose, calcium ndi magnesium amagwiritsidwa ntchito.

Mosasamala Mlingo, mapiritsiwo amakhala ndi mawonekedwe ozungulira, oyera oyera. Kumbali imodzi, pali zolemba za ACTOS; mbali inayo, kuchuluka kwa gawo la mankhwala lomwe likusonyeza.

Mankhwala

Mphamvu ya mankhwalawa minofu imachitika chifukwa cha kulumikizana kwa gulu linalake la ma receptors - PRAP, yomwe imayang'anira mawonekedwe a jini poyankha kumangika ku chinthu china chotchedwa ligand. Peoglitazone ndi ligand yotero ya PRAP receptors yomwe ili mu lipid wosanjikiza, ulusi wa minofu ndi chiwindi.

Zotsatira zamapangidwe a pioglitazone-receptor zovuta, majini "amamangidwa" mwachindunji omwe amayang'anira mwachindunji glucose biotransfform (ndipo, chifukwa chake, amawongolera kuyika kwake mu seramu yamagazi) ndi lipid metabolism.

Nthawi yomweyo, Aktos ali ndi zotsatirazi zowoneka bwino pazokhudza thupi:

• mu adipose minofu - imayang'anira kusiyanasiyana kwa ma adipocytes, kukoka kwa glucose pogwiritsa ntchito minofu yam'mimba komanso kugawa kwa chotupa necrosis factor mtundu wa α,
• m'maselo a β - sinthani ma morphology ndi kapangidwe kake,
• m'matumba - kubwezeretsa magwiridwe antchito a endothelium, kumachepetsa mphamvu ya lipids,
• mu chiwindi - imayendetsa ndikupanga shuga ndi lipoprotein ochepa kachulukidwe, kumachepetsa kukana kwa insulini wa hepatocytes,
• mu impso - imasinthasintha mawonekedwe ake ndi magwiridwe antchito a glomeruli.

Chifukwa chobwezeretsanso kukana kwa insulini mu zotumphukira za minofu, kuchuluka kwa insulin komwe kumadalira glucose kumawonjezeka ndipo, motero, kupanga kwa insulin m'chiwindi kumachepa. Pankhaniyi, zotsatira za hypoglycemic zimatheka popanda kukhudzidwa ndi zochitika za pancreatic β-cell.

Mu mitundu yoyesera ya mtundu 2 wa shuga mu nyama, pioglitazone amachepetsa kwambiri hyperglycemia, hyperinsulinemia. Awa ndi mankhwala okhawo omwe gulu la triazolidinediones limapangitsa kuti matenda a triglycerides m'magazi ndi lipid azikhala chifukwa cha kupindika kwambiri ma lipoproteins. Chifukwa chake, mutatenga Aktos, mphamvu ya atysgenipic ya dyslipidemia mwa odwala omwe ali ndi matenda osokoneza bongo amachepetsa kwambiri.

Pharmacokinetics

Mukamamwa mankhwala ochepetsa mphamvu, magawo onse a pioglitazone pawokha komanso zinthu zomwe amapanga mu biotransfform amafikira sabata limodzi. Nthawi yomweyo, mulingo wa zinthu zomwe zimagwira ntchito zimachulukana pakukwaniritsidwa ndi kuwonjezeka kwa mlingo wa mankhwalawa.

Mafuta. Pambuyo pakukonzekera pakamwa pamimba yopanda kanthu, mphamvu yoyeserera yogwira ntchito m'magazi imapezeka pambuyo pa theka la ola, nsonga imalembedwa pambuyo pa maola awiri. Mukamamwa mapilitsi mukatha kudya, nthawi imeneyi imawonjezeka koma ilibe gawo lililonse pamagawo omaliza a mayamwidwe.

Kugawa. Voliyumu yapakati yogawa ili ndi 1.04 l / kg. Pioglitazone (komanso zinthu zomwe zimasintha mu metabolic) zimangofunika kwathunthu ku serum albin.

Biotransformation. Njira zikuluzikulu zakusintha kwachilengedwe ndi hydroxylation ndi / kapena makutidwe ndi okosijeni. Pambuyo pake, metabolites imalumikizidwa ndi magulu a sulfate ndi glucuronidation. Mapangidwe omwe amapangidwa chifukwa cha biotransfform amakhalanso ndi ntchito yochizira. Kagayidwe ka pioglitazone kumachitika ndi kutenga kwa hepatic Enzymes P450 (CYP2C8, CYP1A1 ndi CYP3A4) ndi ma microsomes.

Kuthetsa. Mpaka gawo limodzi mwa magawo atatu a pioglitazone ovomerezeka amapezeka mu mkodzo. Makamaka ndi mkodzo, mankhwalawa amachotsedwa mu mawonekedwe a metabolites oyambira ndi ma sekondale awo achiwiri. Ndi bile, chofufumimba cha pioglitazone chosasinthika chimachitika. Nthawi ya kufafaniza imayambira maola ambiri (kwa mtundu woyamba wa mankhwalawa) mpaka tsiku (la mankhwala othandizira biotransfform). Chilolezo cha Systemic chimafika pa 7 l / h.

Pharmacokinetics m'magulu apadera a odwala. Ndi kulephera kwa aimpso, kuwongolera hafu ya moyo sikusintha. Koma ndi creatinine chilolezo chochepera 30 ml / min, mankhwalawa amatchulidwa mosamala. Zilonda zam'mimba zimakhudza magawo a pharmacokinetic a pioglitazone. Chifukwa chake, pochita kuchuluka kwa transaminases ndi ALT nthawi zopitilira 2, mankhwalawa sagwiritsidwa ntchito.

Zambiri pazakugwiritsa ntchito mankhwalawa muubwana ndi unyamata (mpaka zaka 18) sizinaperekedwe. Mwa odwala okalamba, pali kusintha kwa mankhwala a pharmacokinetics, koma ndizofunikira pakuwongolera mlingo.

Mankhwalawa akaperekedwa muyezo wokwera kwambiri kuposa zofanana ndi zomwe anthu amalimbikitsa, palibe zomwe zimapezeka pa carcinogenicity, mutagenicity kapena mphamvu ya Aktos pa chonde.

Zokhudza ntchito

Dzina la mankhwala a pioglitazone ndi (()) - 5 - ((4- (5-ethyl-2-pyridinyl) ethoxy) phenyl) methyl) -2,4-) thiazolidinedione monohydrochloride. Zosiyana kachitidwe ka zochita ndi Metformin ndi sulfonylurea kukonzekera. Thupi limatha kukhala ngati ma isomers awiri omwe samasiyana muzochita zochizira.

Kunja, pioglitazone ndi ufa wopanda pake wa crystalline. Fomula yamphamvu ndi 19191920N2O3SˑHCl, kulemera kwa maselo 392.90 daltons. Soluble mu N, N-dimethylfomamide, sungunuka pang'ono mu anhydrous ethanol, acetone. Imasungunuka m'madzi ndipo siyopanda kanthu mu ether. Nambala ya ATX A10BG03.

Momwe mungagwiritsire ntchito: Mlingo ndi njira ya chithandizo

Mkati, 1 nthawi patsiku (mosasamala kanthu za kudya kwakatundu). Monotherapy: 15-30 mg, ngati kuli kotheka, mlingo umatha kukhala wokwanira mpaka 45 mg / tsiku. Kuphatikiza mankhwala: mankhwala a sulfonylurea, mankhwala a metformin - mankhwala a pioglitazone amayamba ndi 15 mg kapena 30 mg (ngati hypoglycemia imachitika, muchepetse mlingo wa sulfonylurea kapena metformin). Chithandizo chophatikiza ndi insulin: mlingo woyambirira ndi 15-30 mg / tsiku, mlingo wa insulini umakhalabe womwewo kapena umachepa ndi 10-25% (ngati wodwalayo apereka hypoglycemia, kapena plasma glucose protein ikutsikira osakwana 100 mg / dl).

Zotsatira za pharmacological

Hypoglycemic wothandizira wa mndandanda wa thiazolidinedione woperekera pakamwa. Kuchepetsa kukana kwa insulin, kumawonjezera kudya kwa glucose wodalira insulin komanso kumachepetsa kutulutsa shuga. Imachepetsa pafupifupi TG, imawonjezera ndende ya HDL ndi cholesterol. Mosiyana ndi sulfonylurea, simalimbikitsa kubisalira kwa insulin. Mosankha bwino kumapangitsa kuti ma gamma receptors akhazikitsidwe ndi peroxisome proliferator (PPAR). Ma receptor a PPAR amapezeka mu minyewa yomwe imagwira gawo lofunikira kwambiri mu zochita za insulin (adipose, minofu yamatumbo ndi chiwindi). Kutsegula kwa zida za nyukiliya za PPAR kumasintha magwiritsidwe amitundu yambiri yolimbana ndi insulin yomwe imakhudzana ndi kayendedwe ka magazi a glucose ndi lipid metabolism.

Malangizo apadera

Mphamvu ya hypoglycemic imawonetsedwa pamaso pa insulin. Odwala omwe ali ndi insulin, komanso amayambira kutsika kwa nthawi ya premenopausal, mankhwalawa amatha kuyambitsa mazira. Zotsatira zakonzanso chidwi cha odwala kuti apange insulini ndi chiopsezo cha kutenga mimba ngati sikokwanira kugwiritsa ntchito njira zakulera. Pa chithandizo, kuwonjezeka kwa kuchuluka kwa plasma ndi chitukuko cha hypertrophy ya minofu ya mtima (chifukwa chodzaza) ndizotheka. Asanayambe komanso miyezi iwiri iliyonse pachaka choyamba cha chithandizo, ndikofunikira kuwunika ntchito za ALT.

Zosankha

Njira zingapo zochizira mtundu wachiwiri wa matenda ashuga, kuphatikiza pa kutenga ma Actos, ziyeneranso kuphatikiza mankhwala othandizira pakudya ndi masewera olimbitsa thupi. Izi ndizofunikira osati pachiyambi cha mtundu wa matenda a shuga 2, komanso. kukhalabe chothandiza cha mankhwala othandizira.

Kugwiritsa ntchito kwa mankhwala othandizira ndikofunikira kuyesa kuchuluka kwa HbAic, komwe ndiko chizindikiro chabwino kwambiri pakulamulira glycemic kwa nthawi yayitali, poyerekeza ndi kutsimikiza kwa glycemia wokha. HbA1C imawonetsa glycemia m'miyezi iwiri kapena itatu yapitayo.

Kuchiza ndi Aktos kumalimbikitsidwa kwakanthawi kokwanira kuti athe kuyesa kusintha kwa HbA1C mulingo (miyezi 3), ngati palibe kuwonongeka pakulamulira kwa glycemic. Odwala omwe ali ndi insulin, ndipo amayambira kuzungulira pang'onopang'ono, mankhwalawa ndi thiazolidatediones, kuphatikizapo mankhwala a Aktos, amatha kuyambitsa mazira. Zotsatira zakonzanso chidwi cha odwala kuti apange insulini ndi chiopsezo cha kutenga mimba ngati sikokwanira kugwiritsa ntchito njira zakulera.

Actos ayenera kugwiritsidwa ntchito mosamala odwala ndi edema.

Pioglitazone imatha kuyambitsa kusungunuka kwa madzi m'thupi, onse amagwiritsidwa ntchito ngati monotherapy komanso kuphatikiza ndi mankhwala ena ophatikiza shuga, kuphatikizapo insulin. Kusungika kwamphamvu m'thupi kumatha kubweretsa kukulira kapena kukulira kwa maphunziro a mtima omwe alipo. Ndikofunikira kuwongolera kupezeka kwa zizindikiro ndi zizindikiro za kulephera kwa mtima, makamaka ndi malo ochepetsa a mtima.

Potha kuwonongeka mu ntchito zamtima, pioglitazone iyenera kusiyidwa.

Milandu yakulephera kwa mtima kugwiritsa ntchito pioglitazone kuphatikiza ndi insulin amafotokozedwa.

Popeza mankhwala osapweteka a anti-yotupa komanso pioglitazone amachititsa kuti magazi azisungika m'thupi, kuphatikizira kwa mankhwalawa kumatha kuwonjezera ngozi ya edema.

Kusamalidwa kwapadera kuyenera kuchitika popereka mankhwala kwa odwala omwe ali ndi matenda a mtima, kuphatikizapo myocardial infarction, angina pectoris, cardiomyopathy ndi matenda oopsa omwe amathandizira kukulitsa kulephera kwa mtima.

Popeza kuwonjezeka kwa magazi ozungulira kungayambitse kukulira kwa edema ndikupangitsa kapena kukulitsa mawonekedwe a kulephera kwa mtima, chidwi chachikulu chiyenera kulipira ku izi:

Mapiritsi a Aktos sayenera kutumizidwa kwa odwala omwe ali ndi vuto la mtima kapena omwe ali ndi vuto la mtima.

Kuyang'anira odwala akutenga ma Actos ndikofunikira. Zikakhala edema, kuchuluka kwambiri kwa thupi, kuwoneka kwa zizindikiro zakulephera kwa mtima, ndi zina, njira zobwezera ziyenera kutengedwa, mwachitsanzo, kusiya kumwa mankhwala a Aktos, perekani diopture (furosemide, etc.).

Ndikofunikira kuphunzitsa wodwalayo za edema, kuchuluka kwambiri kwa thupi, kapena kusintha kwa zizindikilo zomwe zingachitike mutatenga Actos, kotero kuti wodwalayo amasiya kumwa mankhwalawo mosavuta ndikuwonana ndi dokotala.

Popeza kugwiritsa ntchito mankhwala Aktos kumatha kuyambitsa kupatuka mu ECG ndikukulitsa kuchuluka kwa Cardio -acac, kuyenera kujambulidwa nthawi ndi nthawi kwa ECG ndikofunikira. Ngati zonyansa zikupezeka, mawonekedwe a mankhwalawa amayenera kuwunikiranso, kuthekera kwachotsedwa kwake kwakanthawi kapena kuchepetsa mlingo.

Odwala onse, asanalandire chithandizo ndi Aktos, mulingo wa ALT uyenera kutsimikiziridwa, ndipo kuwunikiraku kuyenera kuchitika miyezi iwiri iliyonse pachaka choyamba cha chithandizo komanso pambuyo pake.

Kuyesedwa kuti mupeze chiwindi kugwira ntchito kuyeneranso kuchitidwa ngati wodwala akukhala ndi vuto losonyeza kuti chiwindi chimagwira, mwachitsanzo, nseru, kusanza, kupweteka m'mimba, kutopa, kusowa kwa chakudya, mkodzo wakuda. Lingaliro la kupitiliza kwa mankhwala ndi Aktos liyenera kutengera deta ya chipatala, poganizira magawo a labotale.

Mlandu wa jaundice, chithandizo ndi mankhwalawa ziyenera kusiyiratu.

Kuchiza ndi Aktos sikuyenera kuyambika ngati wodwala akuwonetsa kuwonetsa komwe matendawa amagwira kapena matenda a ALT aposa malire apamwamba a pafupipafupi ndi 2,5.

Odwala omwe ali ndi ma enzymes okwera molondola kwambiri (ALT mulingo wa 1-2.5 nthawi yayitali kuposa malire apamwamba) musanalandire chithandizo kapena nthawi ya chithandizo ndi Aktos amafunika kuwunika kuti adziwe chomwe chikuwonjezera kuchuluka kwa michere iyi. Kukhazikitsa kapena kupitiliza kwa mankhwala ndi Aktos odwala omwe ali ndi kuwonjezeka kwapang'onopang'ono pamlingo wa michere ya chiwindi kuyenera kuchitika mosamala.

Poterepa, tikulimbikitsidwa kuwunika pafupipafupi chithunzi cha matenda ndi kuphunzira za ntchito za "chiwindi" michere. Ngati chiwopsezo cha kuchuluka kwa ma seramu transaminase (ALT> 2,5 nthawi zambiri kuposa malire apamwamba), kuwunika kwa chiwindi kuyenera kuchitidwa pafupipafupi mpaka msana ubwerere kwazinthu zofunikira kapena pamlingo womwe unawonedwa chisanachitike chithandizo.

Ngati mulingo wa ALT ndiwokwera katatu kuposa malire apamwamba, ndiye kuti kuyesa kwachiwiri kuti mupeze mulingo wa ALT kuyenera kuchitika posachedwa. Ngati milingo ya ALT imasungidwa katatu pamlingo wapamwamba, ndiye kuti chithandizo ndi Aktos ziyenera kusiya. Musanayambe mankhwala ndi Aktos ndi miyezi iwiri iliyonse pachaka choyamba cha chithandizo, tikulimbikitsidwa kuwunika kuchuluka kwa ALT.

Odwala omwe amalandila ketoconazole mogwirizana ndi Actos ayenera kuyang'aniridwa pafupipafupi ndi shuga.

Tebulo tchati

Kusiya mankhwala

Mwina pokhapokha malinga ndi dokotala.

Mwa mawonekedwe ofanana ndi mankhwala oyamba a Aktos, madokotala amatha kupereka mankhwala awa:

• Amalvia (Teva, Israel),
• Astrozone (Pharmstandard - Leksredstva, Russia),
• Diab-Norm (woimira KRKA, Russia),
• Pioglar (Ranbaxy, India),
• Pioglite (Malo Ogulitsa Zoyenera ku Sun, India),
• Piouno (WOCKHARDT, India).

Zofanizira zonsezi zidalembetsedwa ku Russian Federation.

Mtengo ndi kugula

Ku Russia, Aktos adalembetsedwa poyamba, koma pakali pano mgwirizano wamalayisensi udatha, ndipo mankhwalawo akupezeka ku Europe kokha. Kugulitsa ku malo ogulitsa mankhwala ku Moscow, St. Petersburg ndi m'mizinda inanso ya dzikolo ndizoletsedwa.

Koma mutha kuyitanitsa mankhwalawo mwachindunji kuchokera ku Germany ndikupereka ku Russia, kulumikizana ndi makampani apakati kuti mupeze thandizo. Malongedzedwe a mapiritsi a 196 okhala ndi mlingo wa 30 mg ndi pafupifupi 260 euro (kuphatikiza kayendedwe ka dongosolo). Mutha kugula mapiritsi a Aktos 30 mg pamtengo wa 30 30 muma 28.

Madokotala amafufuza

Oksana Ivanovna Kolesnikova, endocrinologist

Kuchokera pa zomwe ndakumana nazo, nditha kunena kuti ngakhale Aktosom monotherapy m'magawo oyamba a matendawa, makamaka pophatikiza zakudya ndi masewera olimbitsa thupi, amatha kukhalabe ndi shuga. Pankhaniyi, mankhwalawa samayambitsa mavuto.

Osagula zabodza

Pofuna kupewa kugulitsa zinthu zachinyengo, muyenera kusankha mkhalapakati wodalirika yemwe angakupatseni zikalata zoyambirira kuchokera ku malo ena achilendo ndikuperekanso nthawi yokwanira yochotsetsera mankhwalawa ku Russia. Mukalandira, muyenera kutsimikizira kutsata kwa zilembo phukusi ndi chithuza ndi miyala.

Zotsatira zakuchipatala

Kuchita bwino kwa pioglitazone monga monotherapy komanso kuphatikiza ndi metformin kunayesedwa pamayesero azachipatala omwe amakhala ndi odwala 85. Odwala adagawika m'magulu awiri, pomwe 3% adayimitsa chithandizo chophatikizidwa chifukwa chotukuka kwambiri. Pambuyo pa milungu 12, kuchuluka kwa glucose kunachepa mwa onse odwala otsala pamayesowa.

Zotsatira zofananazo zidapezeka mu kafukufuku wokhudza odwala 800. Kuzunza kwa HbAlc kudatsika ndi 1.4% kapena kuposa. Adanenanso kuchepa kwamankhwala ochepa kwambiri a lipoproteins, cholesterol yathunthu, pomwe nthawi yomweyo, lipoproteins yapamwamba inachuluka.

Hypoglycemic mankhwala Aktos: malangizo, mtengo, ndemanga

Anthu odwala matenda amtundu wa 2 ayenera kumwa mankhwala a hypoglycemic kuti akhale ndi thanzi labwino komanso kupewa mavuto a matendawa.

Madokotala ambiri amalangiza pogwiritsa ntchito Actos. Ichi ndi mankhwala a thiazolidatedione apakamwa. Makhalidwe ake ndi kuwunikira kwa mankhwalawa kwatchulidwa m'nkhaniyi.

The zikuchokera mankhwala

Gawo lalikulu la Actos ndi pioglitazone hydrochloride. Zinthu zothandiza ndi lactose monohydrate, magnesium stearate, calcium carboxymethyl cellulose, hydroxypropyl cellulose.

Machitidwe 15 mg

Mankhwala amapezeka piritsi. Pali mapiritsi okhala ndi chinthu chogwiritsidwa ntchito mwa 15, 30 ndi 45 mg. Makapisozi ozungulira mozungulira, biconvex, okhala ndi mtundu woyera. "ACTOS" imakodwa mbali imodzi, ndipo "15", "30" kapena "45" mbali inayo.

Actos adapangira kuti azichitira anthu omwe ali ndi matenda a shuga a insulin odziimira okha. Amagwiritsidwa ntchito limodzi ndi makapisozi ena omwe amathandizira kupanga insulin, jakisoni wa mahomoni, kapena ngati monotherapy.

Mankhwalawa amagwiritsidwa ntchito pokhapokha ngati mudya zakudya zowonjezera, zokwanira zolimbitsa thupi.

Makanema okhudzana nawo

Zokhudza mitundu ya mankhwala omwe amagwiritsidwa ntchito posokoneza bongo mu video:

Chifukwa chake, Actos amachepetsa kwambiri kuchuluka kwa glycemia mu plasma, kufunika kwa insulin. Koma mankhwala a hypoglycemic sioyenera aliyense, ndipo nthawi zambiri samaloledwa monga gawo la mankhwala ophatikiza.

Chifukwa chake, musayese thanzi lanu ndikugula mankhwala pamalangizo a anzanu. Lingaliro pazoyenera kuchiza matenda a shuga ndi Actos liyenera kupangidwa ndi katswiri.

Momwe mungatenge Actos

Mlingo umatsimikiziridwa payekhapayekha, piritsi limodzi / tsiku, mosasamala chakudya. Monga monotherapy, Aktos amalembedwa ngati zakudya zodwala sizothandiza, kuyambira 15 mg / tsiku. Mlingo ukuwonjezeka m'magawo. Mlingo wapamwamba wa tsiku ndi tsiku ndi 45 mg. Ndi osakwanira achire, mankhwala owonjezera amalembedwa.

Mukakhazikitsa mankhwala ophatikiza, mlingo woyambirira wa pioglitazone umachepetsedwa mpaka 15 kapena 30 mg / tsiku. Aktos akaphatikizidwa ndi metformin, chiopsezo cha hypoglycemia ndi chochepa. Akaphatikizidwa ndi sulfonylurea ndi insulin, kuwongolera glycemic kumafunika. Mlingo wokwanira wa mankhwalawa mu zovuta mankhwala sangathe kupitirira 30 mg / tsiku.