Umarnin don amfani da "Pioglitazone", tsarin aikin, abun da ke ciki, analogues, farashin, alamu, contraindications, sakamako masu illa da kuma sake dubawa

Littafin koyarwa

• Rijistar Rijistar Rijista: Ranbaxy Laboratories, Ltd. (Indiya)

Wakili mai magana da yalwar jini, mai samo asali daga jerin thiazolidinedione. Mai ƙarfi, mai zaɓin agonist na masu karɓar gamma wanda mai kunna peroxisome ya kunna (PPAR-gamma). Ana samun masu karɓa na PPAR gamma a cikin adipose, ƙwayar tsoka da a cikin hanta. Kunna mai karɓar makaman nukiliya PPAR-gamma yana daidaita jigilar adadin kwayoyin halittar-insulin-ins da ke aiki da kulawar glucose da ƙwaƙwalwar ƙwayar ƙwayar cuta. Yana rage juriya ga insulin a cikin kasusuwa na ciki da hanta, sakamakon wannan akwai karuwa a yawan amfani da insulin-da-glucose da kuma raguwar samarda glucose a cikin hanta. Ba kamar magungunan sulfonylurea ba, pioglitazone baya motsa ƙwayar insulin ta hanyar ƙwayoyin beta na pancreatic.

A cikin nau'in 2 na ciwon sukari na mellitus (wanda ba shi da insulin-insulin ba), raguwar juriya na insulin a ƙarƙashin aikin pioglitazone yana haifar da raguwa a cikin kwantar da hankali na glucose jini, raguwar insulin plasma da haemoglobin A 1c (haemoglobin glycated, HbA 1c).

A cikin nau'in 2 na ciwon sukari na mellitus (wanda ba shi da insulin-insulin) tare da raunin ƙwayar ƙwayar cuta ta lipid wanda ke hade da amfani da pioglitazone, akwai raguwa a cikin TG da karuwa a HDL. A lokaci guda, matakin LDL da jimlar cholesterol a cikin waɗannan marasa lafiya ba su canzawa.

Bayan shigowa cikin komai a ciki, ana gano pioglitazone a cikin jini a cikin jini bayan mintuna 30. C max a cikin plasma an kai shi bayan sa'o'i 2. Lokacin cin abinci, an sami ƙara ƙarancin lokacin don isa zuwa C max har zuwa awanni 3-4, amma matakin shaƙar bai canza ba.

Bayan kashi ɗaya, bayyanar V d na pioglitazone averages 0.63 ± 0.41 l / kg. Haɗa kai ga furotin ɗan adam, akasarinsu tare da albumin, ya zarce kashi 99%, ɗaukar nauyin wasu sunadarai ba su da ƙima. Hakanan kuma metabolites na pioglitazone M-III da M-IV suma suna da alaƙa da serum albumin - sama da 98%.

Pioglitazone yana da cikakken metabolized a cikin hanta ta hanyar hydroxylation da hadawan abu da iskar shaka. Metabolites M-II, M-IV (abubuwan da ke haifar da hydroxy na pioglitazone) da M-III (abubuwan da ake samo asali na pioglitazone) suna nuna ayyukan magunguna a cikin nau'ikan dabbobi na nau'in ciwon sukari na 2. An kuma canza hanyoyin samar da kwayoyin dan adam cikin hadewar su da sinadarin glucuronic ko sulfuric acid.

Hanyar metabolism na pioglitazone a cikin hanta yana faruwa tare da halayen isoenzymes CYP2C8 da CYP3A4.

T 1/2 na pioglitazone wanda ba a canza shi ba shine 3-7 hours, jimlar pioglitazone (pioglitazone da aiki metabolites) shine 16-24 hours. Cirewar pioglitazone shine 5-7 l / h.

Bayan gudanarwar baka, kusan 15-30% na kashi na pioglitazone ana samun su a cikin fitsari. Extremelyan ƙananan ƙwayoyin pioglitazone suna ƙare da kodan, galibi a cikin hanyar metabolites da conjugates. An yi imanin cewa lokacin da aka saka shi, yawancin kashi ana cire shi cikin bile, duka canzawa kuma a cikin nau'in metabolites, kuma an keɓe shi daga jiki tare da feces.

Yawan kwalliya na pioglitazone da aiki metabolites a cikin jijiyoyin jini ya kasance a cikin babban matakin 24 awa bayan tsari guda na yau da kullun.

Type 2 ciwon sukari mellitus (mara insulin).

Oauki baki a cikin kashi 30 na MG 1 lokaci / rana. An saita tsawon lokacin jiyya daban daban.

Matsakaicin kashi a cikin maganin haɗin kai shine 30 MG / rana.

Daga gefen metabolism: hypoglycemia na iya haɓaka (daga m zuwa mai tsanani).

Daga tsarin hawan jini: anaemia, raguwar haemoglobin da bashin jini suna yiwuwa.

Daga tsarin narkewa: da wuya - ƙara yawan ayyukan ALT.

Pioglitazone yana contraindicated a cikin ciki da kuma lactation.

A cikin marasa lafiya da juriya na insulin da kuma sake zagayowar anovulatory a cikin premenopausal lokacin, jiyya tare da thiazolidinediones, gami da pioglitazone, na iya haifar da ovulation. Wannan yana kara hadarin samun ciki idan ba ayi amfani da isasshen rigakafin.

A cikin binciken dabbobi, an nuna cewa pioglitazone bashi da tasirin teratogenic kuma baya cutar da haihuwa.

Lokacin amfani da wani tsararren magani na thiazolidinedione lokaci guda tare da maganin hana haihuwa, an lura da raguwa a cikin taro na ethinyl estradiol da northindrone a cikin plasma da kusan 30%. Saboda haka, tare da yin amfani da pioglitazone tare da maganin hana haihuwa, yana yiwuwa a rage tasirin hana haihuwa.

Ketoconazole yana hana metabolic hanta na pioglitazone.

Bai kamata a yi amfani da Pioglitazone ba a gaban bayyanar cututtuka na cutar cututtukan hanta a cikin aiki mai aiki ko tare da karuwa a cikin ayyukan ALT sau 2.5 sama da VGN. Tare da ƙara girman aiki na enzymes na hanta (ALT ƙasa da sau 2.5 fiye da VGN), ya kamata a bincika marasa lafiya kafin ko lokacin jiyya tare da pioglitazone don sanin dalilin karuwar. Tare da haɓaka matsakaici a cikin aikin enzyme na hanta, ya kamata a fara magani tare da taka tsantsan ko ci gaba. A wannan yanayin, ana ba da shawarar ƙarin sa ido akan hoto na asibiti da kuma nazarin matakan ayyukan hanta enzymes.

Game da karuwa a cikin ayyukan transaminases a cikin magani (ALT> sau 2.5 fiye da VGN), ya kamata a gudanar da aikin kula da hanta fiye da kullun kuma har sai matakin ya dawo al'ada ko kuma alamun da aka lura kafin magani. Idan aikin ALT ya ninka VGN sau 3, to, gwaji na biyu don sanin ayyukan ALT yakamata a aiwatar da wuri-wuri. Idan ayyukan ALT ya kasance a matakin 3 sau> VGN pioglitazone ya kamata a daina.

A lokacin jiyya, idan akwai tuhuma game da haɓakar aikin hanta mai rauni (bayyanar tashin zuciya, amai, ciwon ciki, gajiya, rashin ci, fitsari mai duhu), ya kamata a ƙaddara gwajin aikin hanta. Ya kamata a dauki shawarar kan ci gaba da cutar ta pioglitazone a kan tushen bayanan asibiti, yin la'akari da sigogi na dakin gwaje-gwaje. Game da jaundice, ya kamata a dakatar da pioglitazone.

Bai kamata a yi amfani da Pioglitazone ba a gaban bayyanar cututtuka na cutar cututtukan hanta a cikin aiki mai aiki ko tare da karuwa a cikin ayyukan ALT sau 2.5 sama da VGN. Tare da ƙara girman aiki na enzymes na hanta (ALT ƙasa da sau 2.5 fiye da VGN), ya kamata a bincika marasa lafiya kafin ko lokacin jiyya tare da pioglitazone don sanin dalilin karuwar. Tare da haɓaka matsakaici a cikin aikin enzyme na hanta, ya kamata a fara magani tare da taka tsantsan ko ci gaba. A wannan yanayin, ana ba da shawarar ƙarin sa ido akan hoto na asibiti da kuma nazarin matakan ayyukan hanta enzymes.

Game da karuwa a cikin ayyukan transaminases a cikin magani (ALT> sau 2.5 fiye da VGN), ya kamata a gudanar da aikin kula da hanta fiye da kullun kuma har sai matakin ya dawo al'ada ko kuma alamun da aka lura kafin magani. Idan aikin ALT ya ninka VGN sau 3, to, gwaji na biyu don sanin ayyukan ALT yakamata a aiwatar da wuri-wuri. Idan ayyukan ALT ya kasance a matakin 3 sau> VGN pioglitazone ya kamata a daina.

A lokacin jiyya, idan akwai tuhuma game da haɓakar aikin hanta mai rauni (bayyanar tashin zuciya, amai, ciwon ciki, gajiya, rashin ci, fitsari mai duhu), ya kamata a ƙaddara gwajin aikin hanta. Ya kamata a dauki shawarar kan ci gaba da cutar ta pioglitazone a kan tushen bayanan asibiti, yin la'akari da sigogi na dakin gwaje-gwaje. Game da jaundice, ya kamata a dakatar da pioglitazone.

Tare da taka tsantsan, ya kamata a yi amfani da pioglitazone a cikin marasa lafiya da edema.

Haɓaka cutar anemia, raguwar haemoglobin da raguwa a cikin ƙwayar cuta na jini yana iya alaƙa da haɓaka da ƙwayar plasma kuma kar a bayyanar da wani tasirin sakamako na cutar.

Idan ya cancanta, yin amfani da ketoconazole na lokaci daya yakamata a kula sosai da matakin glycemia.

Ba a lura da lokuta masu yawa na karuwa na wucin gadi a cikin aikin CPK ba dangane da tushen amfani da pioglitazone, wanda ba shi da sakamako na asibiti. Ba a san dangantakar waɗannan halayen tare da pioglitazone ba.

Matsakaicin ƙimar bilirubin, AST, ALT, alkaline phosphatase da GGT sun ragu yayin gwaji a ƙarshen maganin pioglitazone idan aka kwatanta da irin waɗannan alamomi kafin magani.

Kafin fara magani da kuma lokacin farkon shekarar magani (kowane wata 2) sannan kuma lokaci-lokaci, ya kamata a sa ido kan ayyukan ALT.

A cikin nazarin gwaji, pioglitazone ba mutagenic bane.

Ba'a bada shawarar amfani da pioglitazone a cikin yara ba.

Fom ɗin saki

Akwai "Pioglitazone" a cikin nau'i na allunan 15, 30 da 45 MG. An amince da samfurin a cikin Rasha don maganin cututtukan type 2, ko dai azaman monotherapy, ko a hade tare da sauran wakilai na bakin jini ko insulin. A cikin EU, akwai madaidaicin tsari don maganin: yakamata a yi amfani da miyagun ƙwayoyi a lokuta da ba a bi da su ba.

Magunguna da magunguna: bayanin matakin

A cikin 1999, an amince da sayar da magani. A shekara ta 2010, an cire rosiglitazone daga kasuwa bisa shawarar Hukumar Kula da Magungunan Turai bayan gano cewa ta haifar da karuwar hadarin zuciya. Tun shekara ta 2010, pioglitazone ce kawai samfurin da aka sayar, kodayake ana shakkar amincinsa kuma an dakatar da amfani da shi a kasashe da dama, ciki har da Faransa, saboda yiwuwar cutar kansa.

Thiazolidinediones - wani rukuni na wasu sunadarai wadanda ke jawo hankulan jikin kwayoyin halitta ga aikin insulin. Ba sa shafar ɓarin insulin a cikin farji. Magungunan suna ɗaure wa mai karɓa na makaman nukiliya a cikin hanta, mai da ƙwayoyin tsoka, wanda ke haifar da karuwar masu karɓar insulin kuma sabili da haka, hankali. A cikin wadannan kyallen takarda, ana hanzarta daukar abubuwa da kuma lalatawar glucose, kuma ana yin saurin gluconeogenesis.

Bayan gudanarwar baka, an cimma iyakar yawan plasma cikin sa'o'i biyu. Abubuwan samfuran abinci suna jinkirta sha, amma kada ku rage adadin kayan masarufi masu amfani. Bioavailability shine kashi 83%. Magungunan yana hydroxylated kuma oxidized a cikin hanta ta hanyar tsarin cytochrome P450. Magungunan sun kasance sunadarai ta hanyar CYP2C8 / 9 da CYP3A4, kazalika da CYP1A1 / 2. 3 cikin 6 da aka gano metabolites suna aiki a cikin magunguna kuma suna da tasirin hypoglycemic. Rabin rayuwar kayan daga 5 zuwa 6 hours, kuma metabolite mai aiki yana daga sa'o'i 16 zuwa 24. Tare da rashin isasshen ƙwayar cuta, ƙwayoyin magunguna suna canzawa daban, a cikin jini yana da ƙari, ɓangaren sinadarai na pioglitazone yana ƙaruwa.

Manuniya da contraindications

Kimanin mutane 4,500 da ke da nau'in ciwon sukari na 2 sun dauki pioglitazone a matsayin wani ɓangare na binciken su. A cikin hanyar monotherapy, an riga an kwatanta pioglitazone da placebo. An kuma gwada haɗin pioglitazone tare da sulfonylureas, metformin da insulin sosai. Meta-nazarce-nazarcen sun hada da karatuttukan dogon lokaci (na bude) wanda masu ciwon sukari suka karbi pioglitazone na makwanni 72. Saboda jarabawar asibiti ba kasafai ake buga dalla-dalla ba, mafi yawan bayanan sun fito ne daga takaddama ko abubuwan ƙira.

An kwatanta magani da placebo a cikin karatun makafi da yawa har zuwa tsawon makonni 26. Studyaya daga cikin binciken wanda mutane 408 suka halarta an buga cikakke. Ana iya taƙaita sakamakon kamar haka: a cikin kewayon daga 15 zuwa 45 MG / rana, pioglitazone ya haifar da raguwar tallafin-kashi a cikin HbA1c da glucose jini.

Don kwatanta kai tsaye tare da wani wakilin maganin cututtukan ƙwayar cuta, kawai taƙaitaccen bayani yana samuwa: nazarin makircin-mako-mako na mako-mako 26-marasa lafiya tare da marasa lafiya 263 sun nuna ƙarancin inganci idan aka kwatanta da glibenclamide.

Magungunan yana contraindicated a cikin ciki da kuma lactation, da kuma a cikin yara da matasa. Pioglitazone yana contraindicated a cikin marasa lafiya da tashin hankali, ciwon sukari-dogara da ciwon sukari, gazawar zuciya, matsakaici da kuma tsananin hepatopathy, da ciwon sukari ketoacidosis. Lokacin shan magani, kuna buƙatar saka idanu akan aikin hanta koyaushe don guje wa ci gaban halayen masu wahala.

Side effects

Kamar kowane glitazones, pioglitazone yana riƙe da ruwa a cikin jiki, wanda zai iya bayyana kansa a cikin edema da anemia; yayin da ya faru da faduwar zuciya na baya, rikice rikice na iya faruwa - huhun huhun. An kuma ba da rahoton Pioglitazone don haifar da ciwon kai, cututtukan jijiyoyin jiki, tsoka, haɗin gwiwa, da ƙafafun kafa. A cikin karatun na dogon lokaci, matsakaicin nauyin da aka samu shine 5%, wanda ke da alaƙa ba kawai tare da riƙe ruwa ba, har ma da haɓaka nama na adipose.

Pioglitazone monotherapy bai bayyana da alaƙa da haɗarin haɗarin hypoglycemia ba. Koyaya, pioglitazone yana ƙaruwa mai saurin kamuwa da ƙwaƙwalwar ƙwaƙwalwar ƙwayar ƙwaƙwalwa ko insulin, wanda ke ƙara haɗarin hypoglycemia tare da irin waɗannan hanyoyin maganin.

A wasu marasa lafiya, transaminases ya karu. Lalacewa a hanta da aka lura lokacin shan wasu glitazones ba a gano shi ba lokacin shan maganin. Jimlar cholesterol na iya ƙaruwa, amma HDL da LDL ba su canzawa.

A watan Satumbar 2010, Hukumar Kula da Abinci da Magunguna ta Amurka ta ba da shawarar gwada wani magani don hadarin kamuwa da cutar mafitsara. Tun da farko a cikin karatun asibiti guda biyu, an lura da karuwar cutar kansa tare da magani. Masana ilimin kimiyya sun kammala cewa babu wata alaƙar mahimmanci ta dangantaka tsakanin shan miyagun ƙwayoyi da haɓaka cutar kansa.

Sashi da yawan abin sama da ya kamata

Ana ɗaukar Pioglitazone sau ɗaya a rana. Shafin farko da aka ba da shawarar shi ne daga 15 zuwa 30 MG / rana, sashi na iya karuwa a hankali akan makonni da yawa. Tun da troglitazone yana da hepatotoxic, ya kamata a sa ido a cikin enzymes hanta a kai a kai yayin shan magunguna don dalilai na aminci. Bai kamata a yi amfani da Pioglitazone don alamun cututtukan hanta ba.

A halin yanzu, har yanzu akwai sauran saiti a cikin amfani da waɗannan sabbin abubuwa masu tsada, tunda ba a yi nazari sosai game da rikice-rikice da fa'idodin su ba.

Haɗa kai

Babu ma'amala da aka bayyana. Koyaya, za a iya samun damar hulɗa don abubuwan da ke hana ko haifar da mahimmancin enzymes biyu masu lalata - CYP2C8 / 9 da CYP3A4. Ba'a ba da shawarar a haɗa fluconazole tare da magani ba.

Nazarin ra'ayi na ƙwararren likita da masu ciwon sukari.

Pioglitazone magani ne mai tsada wanda aka wajabta wa marasa lafiya da rashin ƙarfi na metformin.Magungunan zai iya samun sakamako na hepatotoxic, saboda haka marasa lafiya suna buƙatar bincika hanta a kai a kai kuma su ba da rahoton duk canje-canje a cikin yanayin ga likita.

Boris Mikhailovich, likitan diabetologist

Ya dauki metformin da sauran magunguna waɗanda ba su taimaka ba. Daga metformin, ciki na ya ji ciwo duk rana, saboda haka dole in ƙi. Na gabatar da “Pioglar”, na sha tsawon watanni 4 kuma naji bayyanannuwar ci gaba - glycemia ya saba kuma lafiyar ta ta inganta. Ba na lura da m halayen.

Farashi (a cikin Tarayyar Rasha)

Farashin kowane wata na Pioglar (daga 15 zuwa 45 mg / rana) yana daga 2000 zuwa 3500 rubles. Don haka, pioglitazone, a matsayin mai mulkin, yana da rahusa fiye da rosiglitazone (4-8 mg / rana), wanda farashin daga 2300 zuwa 4000 rubles kowace wata.

Hankali! Ana ba da magani sosai bisa ga umarnin likita. Kafin amfani, nemi ƙwararren likita.