Kufotokozera kwa Viktoza, malangizo ogwiritsa ntchito, chithunzi
Fomu ya Mlingo - yankho la subcutaneous makonzedwe: osakhala amtundu kapena pafupifupi color (3 ml aliyense * m'magalapota amgalasi, omwe amasindikizidwa mu cholembera cha pulasitiki chotayika cha jakisoni wambiri, mu cholembera 1, 2 kapena 3 syringe pensulo).
* Mu 1 syringe cholembera (3 ml) muli mulingo 10 wa 1.8 mg, 15 Mlingo wa 1.2 mg kapena 30 Mlingo wa 0,6 mg.
Ntchito yogwira: liraglutide, mu 1 ml - 6 mg.
Zothandiza: hydrochloric acid / sodium hydroxide q.s., sodium hydrogen phosphate dihydrate, phenol, propylene glycol, madzi a jekeseni.
Mankhwala
Liraglutide ndi analogue ya anthu GLP-1 (glucagon-like peptide-1). Kupangidwa ndi njira yogwiritsira ntchito biotechnology ya recombinant DNA (deoxyribonucleic acid) pogwiritsa ntchito Saccharomyces cerevisiae strain, yomwe ili ndi 97% ya Homology yaumunthu ya GLP-1, imamanga ndikuyambitsa zolandirira za GLP-1 mwa anthu.
RecPoror ya GLP-1 ndi chandamale cha omwe ali ndi chibadwa cha GLP-1, chomwe ndi hormone yakumapeto ya insretin yomwe imalimbitsa secretion ya glucose yomwe imadalira glucose m'maselo a pancreatic β-cell. Poyerekeza ndi mbadwa za GLP-1, ma pharmacodynamic ndi ma pharmacokinetic Mbiri ya liraglutide amalola kuti ziziyendetsedwa kamodzi patsiku.
Ndi jakisoni wotsekemera, mawonekedwe a chinthucho amakhala motengera njira zitatu:
- kuyanjana, komwe kumapereka kuyimitsidwa kwa liraglutide,
- zomatira albin,
- kuchuluka kwa kukhazikika kwa enzymatic motsutsana ndi DPP-4 (dipeptidyl peptidase-4) ndi NEP (enzyme neutral endopeptidase), yomwe imapangitsa T yayitali1/2 (theka-moyo) wa chinthu kuchokera plasma.
Zotsatira za liraglutide zimakhazikitsidwa pakuyanjana ndi ma GLP-1 receptors enieni, chifukwa chomwe kuchuluka kwa cAMP (cyclic adenosine monophosphate) kumakulirakulira. Mothandizidwa ndi chinthucho, kukhudzika kwa glucose komwe kumapangitsa kuti insulin itulutsidwe kumawonedwa, ndipo ntchito ya pancreatic β-cell imayenda bwino. Nthawi yomweyo, kutsanulira kwa glucose komwe kumachitika mobisa kwambiri. Chifukwa chake, ndi kuchuluka kwa shuga m'magazi, kubisala kwa glucagon kumachepetsa ndipo kutulutsidwa kwa insulin kumalimbikitsidwa.
Komabe, odwala omwe ali ndi hypoglycemia, liraglutide amatsitsa insulin secretion popanda kuletsa secretion wa glucagon. Njira yochepetsera glycemia imaphatikizaponso kuchepetsedwa pang'ono kwa kutsuka kwa m'mimba. Pogwiritsa ntchito njira zomwe zimayambitsa kuchepa kwa njala komanso kuchepa kwa mphamvu yamagetsi, liraglutide imabweretsa kuchepa kwa minofu ya adipose komanso kuwonda.
GLP-1 ndi owongolera azakudya ndi zama calorie, zolandilira za peptidezi zimapezeka m'malo angapo aubongo omwe akukhudzidwa ndi kayendetsedwe kazakudya.
Mukamachititsa maphunziro a nyama, zidapezeka kuti kudzera mwa kuphatikiza mwachindunji kwa zolandila za GLP-1, liraglutide imathandizira zizindikiritso ndikuchepetsa ma siginolo am'manja, potero kumatsogolera kuwonda.
Komanso, malinga ndi maphunziro a nyama, liraglutide imachedwetsa kukula kwa matenda ashuga. Katunduyu ndiwothandiza kwambiri pakukondweretsedwa kwapadera kwa pancreatic β-cell ndikulepheretsa imfa ya β-cell (apoptosis), yomwe imayambitsa ma cytokines ndi mafuta acids aulere. Chifukwa chake, liraglutide imawonjezera insulin biosynthesis ndikuwonjezera kuchuluka kwa β-cell. Pambuyo polimbitsa shuga ndende, liraglutide imasiya kuwonjezera kuchuluka kwa ma pancreatic β-cell.
Wovutitsayo amakhala ndi nthawi yayitali ya maola 24 ndikuwongolera kuwongolera kwa glycemic, komwe kumatheka chifukwa chochepetsa kuchuluka kwa shuga m'magazi ndikatha kudya ndi shuga yachiwiri.
Pharmacokinetics
Pambuyo pa kayendetsedwe ka subcutaneous, kuyamwa kwa liraglutide kumayamba pang'onopang'ono, Tmax (nthawi yoti mufikire kuchuluka kwa ndende) mu plasma ndi maola 8-12. Cmax (kuchuluka kwa ndende) mu plasma pambuyo kukhazikitsa limodzi mlingo wa 0.6 mg ndi 9,4 nmol / L. Mukamagwiritsa ntchito mlingo wa 1.8 mg pafupifupi Css (equilibrium concentration) mu plasma imafika pafupifupi 34 nmol / L. Kuwonekera kwa chinthu kumathandizidwa molingana ndi mlingo. The intra-payekha payekha kusintha kwa AUC (dera pansi pa ndende nthawi pamapindikira) pambuyo makonzedwe a liraglutide limodzi mlingo 11%. Mtheradi bioavailability pafupifupi 55%.
Zikuwoneka Vd (kuchuluka kwa magawidwe) a liraglutide mu minofu yokhala ndi njira yotsogola yoperekera ndi 11-17 l, mtengo wapakati wa Vd pambuyo mtsempha wa magazi makonzedwe - 0,07 l / kg. Kumanga kwofunikira kwa liraglutide ndi mapuloteni a plasma kumadziwika (> 98%).
Kagayidwe ka liraglutide kumachitika ngati mapuloteni akuluakulu, osatenga nawo mbali monga njira yodziwitsira chiwalo chilichonse. Maola 24 pambuyo pa kuperekedwa kwa mlingo umodzi, mankhwala osasinthidwawo amakhalabe gawo lalikulu la plasma. Ma metabolites awiri adapezeka mu plasma (≤ 9 ndi ≤ 5% ya mlingo wonse).
Liraglutide wosasintha pambuyo makonzedwe a 3 H-liraglutide mu mkodzo kapena ndowe sichitsimikizike. Kachigawo kochepa chabe ka metabolites komwe kamakhudzana ndi thunthu kamakhudzidwa ndi impso kapena matumbo (6 ndi 5%, motsatana). Pambuyo subcutaneous makonzedwe a limodzi liraglutide, pafupifupi chilolezo cha thupi pafupifupi 1,2 l / h pochotsa T1/2 pafupifupi maola 13.
Zizindikiro zogwiritsidwa ntchito
Malinga ndi malangizo, Viktoza amagwiritsidwa ntchito pa matenda a shuga 2 kuphatikiza zakudya komanso masewera olimbitsa thupi kuti akwaniritse kuwongolera kwa glycemic.
Njira zotheka kugwiritsa ntchito mankhwalawa:
- monotherapy
- kuphatikiza chithandizo chamankhwala amodzi kapena angapo amkamwa hypoglycemic othandizira (thiazolidinediones, sulfonylureas, metformin) mwa odwala omwe alephera kukwaniritsa machitidwe oyenera a glycemic panthawi yamankhwala am'mbuyomu,
- kuphatikiza mankhwala a basal insulin odwala omwe alephera kukwaniritsa bwino glycemic control pogwiritsa ntchito Victoza osakanikirana ndi metformin.
Contraindication
- matenda ashuga ketoacidosis,
- mtundu 1 shuga
- angapo endocrine neoplasia mtundu 2,
- chiwindi ntchito,
- kuvulala kwambiri aimpso,
- diabetic gastroparesis,
- matenda amatupa,
- Kulephera kwamtima kwa mtima kwa III - kalasi yogwira ntchito malinga ndi gulu la New York Cardiology Association (NYHA),
- mbiri yodwala khansa ya chithokomiro, kuphatikizapo banja,
- wazaka 18
- mimba ndi mkaka wa m`mawere
- Hypersensitivity ku gawo lililonse la Victoza.
- matenda a chithokomiro
- kulephera kwamtima kwa I - II gulu lothandiza malinga ndi gulu la NYHA,
- zaka zopitilira 75.
Malangizo ogwiritsira ntchito Victoza: njira ndi mlingo
Victoza amayenera kutumikiridwa mosabereka m'mimba, phewa kapena ntchafu kamodzi patsiku, ngakhale zakudya. Malo ndi nthawi ya jekeseni imatha kusinthidwa popanda kusintha kwa mlingo, komabe, ndikofunikira kuperekera mankhwalawa pafupifupi nthawi yomweyo, yomwe ili yabwino kwambiri kwa wodwalayo.
Kupititsa patsogolo kulekerera kwamatumbo, chithandizo chimalimbikitsidwa ndi mlingo wa tsiku lililonse wa 0,6 mg. Pambuyo pa sabata yochepa, mlingo umakulitsidwa ku 1,2 mg. Ngati ndi kotheka, pofuna kukwaniritsa njira yabwino kwambiri yolamulira glycemic, poganizira luso la Victoza, kuwonjezeka kwa mlingo mpaka 1.8 mg ndikotheka patatha sabata limodzi. Kugwiritsa ntchito Mlingo wapamwamba sikulimbikitsidwa.
Mankhwalawa amatha kuikidwa kuwonjezera pa mankhwala omwe akupitilira ndi metformin kapena kuphatikiza mankhwala ndi metformin osakanikirana ndi thiazolidinedione. Mlingo womaliza suyenera kusintha.
Wowonongera amatha kuwonjezeredwa ku mankhwala omwe alipo a sulfonylurea kapena mankhwala a metformin osakanikirana ndi mankhwala a sulfonylurea. Pankhaniyi, kuti muchepetse mwayi wokhala ndi hypoglycemia yosafunikira, mlingo wa zotumphukira za sulfonylurea ziyenera kuchepetsedwa.
Victoza amathanso kuwonjezeredwa ndi basal insulin, koma kuti muchepetse chiopsezo cha hypoglycemia, ndikofunikira kuchepetsa mlingo wa insulin.
Ngati mwasowa mlingo:
- Ngati maola opitilira 12 asanadutse, muyenera kulowa muyezo womwe mwasowa posachedwa,
- ngati maola opitilira 12 adatha, mlingo wotsatira uyenera kuperekedwa tsiku lotsatira panthawi yoyenera, mwachitsanzo, sikofunikira kulipiritsa mlingo womwe wakuphayo popereka muyeso wowonjezera kapena wowirikiza.
Malangizo ogwiritsira ntchito Victoza (Njira ndi Mlingo)
S / c imalowetsedwa m'mimba / ntchafu kamodzi patsiku, ngakhale chakudya.
Ndikofunika kulowa nthawi yomweyo. Tsamba la jakisoni limasiyana. Mankhwala sangathe kulowa / mkati ndi / m.
Amayamba chithandizo ndi 0,6 mg patsiku. Pambuyo pa sabata, mlingo umakulitsidwa ku 1,2 mg. Ngati ndi kotheka, kuti muthane ndi vuto labwino kwambiri la glycemic, onjezerani 1.8 mg pambuyo pa sabata. Mlingo pamwambapa 1.8 mg ndi osayenera.
Nthawi zambiri amagwiritsidwa ntchito kuwonjezera pa chithandizo Metforminkapena Metformin+ PizzMlingo wam'mbuyomu. Akaphatikizidwa ndi mankhwala a sulfonylurea, mlingo wotsiriza uyenera kuchepetsedwa, chifukwa osayenera hypoglycemia.
Mothandizidwa ndi kuyamwa kwa mankhwala opitilira 40 mgyezo wamba, nseru kwambiri ndi kusanza zimayamba. Chithandizo cha Syndrome chimachitika.
Mukutenga Paracetamol Mlingo wa chomaliza suyenera kusintha.
Sizimayambitsa kusintha kwakukulu mu pharmacokinetics Atorvastatin.
Mlingo Griseofulvin kugwiritsa ntchito Victoza munthawi yomweyo sikofunikira.
Komanso palibe kukonza Dozlisinoprilndi Digoxin.
Kuletsa kubereka Ethinyl estradiolndi Levonorgestrel pamene kutenga ndi Viktoza sikusintha.
Kugwiritsa ntchito mankhwala osokoneza bongo Insulinndi Warfarin osati kuphunzira.
Yoperekedwa ndi mankhwala.
Kusungidwa mufiriji pa 2-8 ° C; kusungidwa m'chipinda chosungiramo kutentha kuposa 30 ° C ndikovomerezeka.
Analogs: Liraglutide, Baeta(ofanana momwe amagwirira ntchito, koma zomwe zimagwira ndizosiyana).
Ndemanga za madotolo za Viktoz amabwera kudzavomereza kuti mankhwalawa amayenera kugwiritsidwa ntchito molingana ndi zofunikira komanso pokhapokha ngati adokotala akuwalangiza. Kafukufuku awonetsa kuti mankhwala othandizira odwala matenda amtundu wa 2, Baeta ndi Victoza, ndi othandiza kuchepetsa kunenepa kwambiri. Izi ndizofunikira chifukwa ntchito yofunika kwambiri pothandizira odwala omwe ali ndi vutoli ndi kuwonda.
Mankhwalawa amapangidwira KUTHENGA matenda ashugandi kupewa zovuta zake, zimakhudza mtima wamtima. Sizingochepetsa kuchuluka kwa shuga, komanso kubwezeretsa kupanga kwa insulin mwa odwala matenda ashuga. Poyeserera nyama, zinatsimikiziridwa kuti mothandizidwa ndi kapangidwe ka maselo a beta ndikugwira ntchito kwawo zimabwezeretseka. Kugwiritsa ntchito mankhwalawa kumalola njira yovomerezeka yothandizira Type 2 shuga.
Viktoza wochepetsa thupi mwa odwala ena omwe ali ndi matenda ashuga adagwiritsidwa ntchito ngati monotherapy. Odwala onse adazindikira kuchepa kwakudya. Zizindikiro zamagalasi am'magazi masana zinali zopanda malire, momwe zimakhalira kubwerera mwezi umodzi triglycerides.
Mankhwalawa adapangidwa pa mlingo wa 0,6 mg kamodzi patsiku kwa sabata, ndiye kuti mlingowo unakwezedwa mpaka 1.2 mg. Kutalika kwa chithandizo ndi chaka chimodzi. Zotsatira zabwino zimawonedwa ndi kuphatikiza mankhwala ndi Metformin. M'mwezi woyamba wa chithandizo, odwala ena adataya 8 kg. Madotolo amachenjeza kuti asamangotsatira mankhwalawa kwa omwe akufuna kuchepa thupi. Kugwiritsa ntchito kumakhala ndi ngozi khansa ya chithokomiro ndi zochitika kapamba.
Ndemanga pamapulogalamu nthawi zambiri zimakhala zoipa. Kutaya kambiri kumalemera pafupifupi 1 kg pamwezi, osachepera 10 kg kwa miyezi isanu ndi umodzi. Funso lomwe likufunsidwa mwachangu: kodi pali tanthauzo lililonse kusokoneza metabolism chifukwa cha 1 kg pamwezi? Ngakhale kuti zakudya ndi masewera olimbitsa thupi zimafunikirabe.
"Kupotoza kagayidwe ... ayi."
"Ndikuvomereza kuti chithandizo chamankhwala ndikofunikira kuti magawo atatu a minyewa ya thupi athe, pamene metabolism itasokonekera, koma apa? Sindikumvetsa ... "
"Ku Israel, mankhwalawa amalembedwa PAMODZI kwa odwala matenda ashuga omwe ali ndi shuga. Ungopeza chophikacho. "
“Palibe chabwino pankhani imeneyi. Kwa miyezi itatu + 5 kg. Koma sindinatengereko kuti ndichepe thupi, ndili ndi matenda ashuga. ”
Mutha kugula ku Victoza ku Moscow m'mafakitala ambiri. Mtengo wa yankho la jakisoni mu cholembera cha 3 ml No. 2 m'masitolo osiyanasiyana opangira mankhwala amachokera ku rubles 7187. mpaka 11258 rub.
Njira yothetsera makonzedwe a sc wopanda mtundu kapena pafupifupi wopanda utoto, wowonekera.
Omwe amathandizira: sodium hydrogen phosphate dihydrate - 1.42 mg, propylene glycol - 14 mg, phenol - 5.5 mg, hydrochloric acid / sodium hydroxide - q.s., madzi a jakisoni - mpaka 1 ml.
3 ml - makatoni agalasi (1) - ma cholembera a syringe (1) - mapaketi a makatoni.
3 ml - makatoni agalasi (1) - ma cholembera a syringe (2) - mapaketi a makatoni.
3 ml - makatoni agalasi (1) - ma cholembera a syringe (3) - mapaketi a makatoni.
Hypoglycemic wothandizira. Liraglutide ndi analogue ya glucagon yofanana ndi peptide-1 (GLP-1), yopangidwa ndi recombinant DNA biotechnology pogwiritsa ntchito Saccharomyces cerevisiae strain, yomwe ili ndi 97% ya Homology ya anthu ndi GLP-1, yomwe imamanga ndikuyambitsa zolandirira za GLP-1 mwa anthu. Receptor ya GLP-1 imagwira ntchito ngati chandamale cha mbadwa za GLP-1, ma endreteni am'mimba amkati, omwe amathandizira secretion ya shuga ya glucose omwe amadalira maselo a pancreatic beta. Mosiyana ndi mbadwa ya GLP-1, ma pharmacokinetic ndi ma pharmacodynamic Mbiri ya liraglutide amalola kuti ziziperekedwa kwa odwala tsiku lililonse 1 nthawi / tsiku.
Mbiri yayitali ya liraglutide pakubaya kwapansipansi imaperekedwa ndi njira zitatu: kudziphatikiza, komwe kumapangitsa kuti mankhwalawa achedwe, kumangiriza ku albumin komanso kuchuluka kwakukulu kwa enzymatic pokhudzana ndi dipeptidyl peptidase-4 (DPP-4) ndi ndale endopeptidase enzyme (NEP) , chifukwa chomwe moyo wautali wa mankhwalawo umatheka. Kuchita kwa liraglutide kumachitika chifukwa cha kulumikizana ndi ma receptors ena a GLP-1, chifukwa chomwe kuchuluka kwa cyclic cAMP adenosine monophosphate kumakwera. Mothandizidwa ndi liraglutide, kukhudzana ndi shuga kwa insulin katulutsidwe kumachitika. Nthawi yomweyo, liraglutide imapumira shuga wambiri wodalira shuga. Chifukwa chake, ndi kuchuluka kwa kuchuluka kwa shuga m'magazi, insulin katulutsidwe imakhudzidwa ndipo katulutsidwe wa glucagon amakakamizidwa. Komabe, pa hypoglycemia, liraglutide amachepetsa katemera wa insulin, koma sayimitsa katulutsidwe wa glucagon. Njira yochepetsera glycemia imaphatikizanso kuchepetsedwa pang'ono kwa madzi am'mimba. Liraglutide amachepetsa thupi komanso amachepetsa mafuta m'thupi pogwiritsa ntchito zida zomwe zimapangitsa kuchepa kwa njala komanso kugwiritsa ntchito mphamvu zochepa.
Liraglutide ali ndi nthawi yayitali ya maola 24 ndipo amakonzanso kayendedwe ka glycemic pochepetsa kuchuluka kwa shuga m'magazi ndikatha kudya odwala omwe ali ndi matenda a shuga a 2.
Ndi kuwonjezeka kwa ndende ya magazi, liraglutide imawonjezera katemera wa insulin. Mukamagwiritsa ntchito shuga wa kulowetsedwa kwa shuga, kutsekeka kwa insulin pambuyo pakumwa mlingo umodzi wa liraglutide kwa odwala omwe ali ndi matenda a shuga 2 kumawonjezera pamlingo wofanana ndi omwe amakhala ndi maphunziro abwino.
Liraglutide monga gawo la mankhwala ophatikiza ndi metformin, glimepiride kapena kuphatikiza kwa metformin ndi rosiglitazone kwa masabata 26 kunapangitsa kuchuluka kwakukulu (p 98%).
Kwa maola 24 pambuyo pa kuperekedwa kwa odzipereka athanzi limodzi la 3 H-liraglutide yolembedwa ndi radioot isotope, gawo lalikulu la plasma silinasinthe liraglutide. Ma metabolites awiri a plasma adapezeka (≤ 9% ndi ≤ 5% ya kuchuluka kwa plasma radioacaction). Liraglutide imapangidwa pang'onopang'ono ngati mapuloteni akuluakulu.
Mlingo wa 3 H-liraglutide utaperekedwa, liraglutide wosasinthika sanapezeka mumkodzo kapena ndowe. Kachigawo kochepa chabe kamene kamayendetsedwa ndi radioactivity mwa ma metabolites omwe amalumikizana ndi liraglutide (6% ndi 5%, motero) ndi impso kapena matumbo. Zinthu zokhala ndi wailesi zimapukutidwa ndi impso kapena matumbo, makamaka masiku 6 kapena 6 atatha kumwa mankhwalawa, ndipo ndi metabolites atatu. Wapakati chilolezo kuchokera thupi pambuyo sc makonzedwe a liraglutide limodzi mlingo pafupifupi 1,2 l / h ndi kuchotsedwa theka moyo pafupifupi 13 maola.
Zambiri kuchokera ku kafukufuku wa pharmacokinetic pagulu la odzipereka athanzi komanso kusanthula kwa data ya pharmacokinetic yomwe imapezeka mwa odwala (azaka 18 mpaka 80) akuwonetsa kuti zaka sizikhala ndi vuto lalikulu pakukhudzana ndi pharmacokinetic katundu wa liraglutide.
Kafukufuku wogwiritsa ntchito anthu ku pharmacokinetic kuwunika kwa zotsatira za liraglutide mwa odwala amtundu wakuda, wakuda, waku Asia, ndi ku Spain akuonetsa kuti mafuko alibe gawo lalikulu pokhudzana ndi pharmacokinetic katundu wa liraglutide.
Kuwonetsedwa kwa liraglutide mwa odwala ofatsa kwambiri osakhazikika pachiwindi kunachepetsedwa ndi 13-23% poyerekeza ndi omwe ali mgululi la mitu yathanzi. Odwala omwe ali ndi vuto losakwanira kwa hepatic (malinga ndi gulu la ana-Pugh, matenda oopsa> ma point 9), kuwonetsa kwa liraglutide kunali kotsika kwambiri (ndi 44%).
Dzina la malonda: Victoza ®
INN: Liraglutide
Kufotokozera
Mtundu wopanda mawonekedwe kapena pafupifupi wopanda mawonekedwe owonekera.
Nambala ya ATX - A10BX07.
Mankhwala
Liraglutide ali ndi nthawi yayitali ya maola 24 ndipo amakonzanso kayendedwe ka glycemic pochepetsa kuchuluka kwa shuga m'magazi ndikatha kudya odwala omwe ali ndi matenda a shuga a 2.
Kutupa kwa inshuwaransi
Ndi kuwonjezeka kwa ndende ya magazi, liraglutide imawonjezera katemera wa insulin. Mukamagwiritsa ntchito mankhwala osokoneza bongo a glucose kulowetsedwa, insulin katulutsidwe pambuyo pokhazikitsa limodzi muyezo wa liraglutide kwa odwala omwe ali ndi matenda a shuga 2 amawonjezera pamlingo wofanana ndi wophunzitsidwa bwino (mkuyu. 1).
Victoza: malangizo ogwiritsa ntchito ndi kuwunikira
Dzina lachi Latin: Victoza
Code ya ATX: A10BX07
Zogwira pophika: liraglutide (Liraglutide)
Wopanga: Novo Nordisk, A / C (Novo Nordisk, A / S) (Denmark)
Sinthani mafotokozedwe ndi chithunzi: 08/15/2018
Mitengo muma pharmacies: kuchokera ku 10 500 ma ruble.
Wopondera ndi agonist wa glucagon-polypeptide (GLP) receptors, othandizira a hypoglycemic.
Fomu ya Mlingo - yankho la subcutaneous makonzedwe: osakhala amtundu kapena pafupifupi color (3 ml aliyense * m'magalapota amgalasi, omwe amasindikizidwa mu cholembera cha pulasitiki chotayika cha jakisoni wambiri, mu cholembera 1, 2 kapena 3 syringe pensulo).
* Mu 1 syringe cholembera (3 ml) muli mulingo 10 wa 1.8 mg, 15 Mlingo wa 1.2 mg kapena 30 Mlingo wa 0,6 mg.
Ntchito yogwira: liraglutide, mu 1 ml - 6 mg.
Zothandiza: hydrochloric acid / sodium hydroxide q.s., sodium hydrogen phosphate dihydrate, phenol, propylene glycol, madzi a jekeseni.
Liraglutide ndi analogue ya anthu GLP-1 (glucagon-like peptide-1). Kupangidwa ndi njira yogwiritsira ntchito biotechnology ya recombinant DNA (deoxyribonucleic acid) pogwiritsa ntchito Saccharomyces cerevisiae strain, yomwe ili ndi 97% ya Homology yaumunthu ya GLP-1, imamanga ndikuyambitsa zolandirira za GLP-1 mwa anthu.
RecPoror ya GLP-1 ndi chandamale cha omwe ali ndi chibadwa cha GLP-1, chomwe ndi hormone yakumapeto ya insretin yomwe imalimbitsa secretion ya glucose yomwe imadalira glucose m'maselo a pancreatic β-cell. Poyerekeza ndi mbadwa za GLP-1, ma pharmacodynamic ndi ma pharmacokinetic Mbiri ya liraglutide amalola kuti ziziyendetsedwa kamodzi patsiku.
Ndi jakisoni wotsekemera, mawonekedwe a chinthucho amakhala motengera njira zitatu:
- kuyanjana, komwe kumapereka kuyimitsidwa kwa liraglutide,
- zomatira albin,
- kuchuluka kwa kukhazikika kwa enzymatic motsutsana ndi DPP-4 (dipeptidyl peptidase-4) ndi NEP (enzyme neutral endopeptidase), yomwe imapangitsa T yayitali1/2 (theka-moyo) wa chinthu kuchokera plasma.
Zotsatira za liraglutide zimakhazikitsidwa pakuyanjana ndi ma GLP-1 receptors enieni, chifukwa chomwe kuchuluka kwa cAMP (cyclic adenosine monophosphate) kumakulirakulira. Mothandizidwa ndi chinthucho, kukhudzika kwa glucose komwe kumapangitsa kuti insulin itulutsidwe kumawonedwa, ndipo ntchito ya pancreatic β-cell imayenda bwino. Nthawi yomweyo, kutsanulira kwa glucose komwe kumachitika mobisa kwambiri. Chifukwa chake, ndi kuchuluka kwa shuga m'magazi, kubisala kwa glucagon kumachepetsa ndipo kutulutsidwa kwa insulin kumalimbikitsidwa.
Komabe, odwala omwe ali ndi hypoglycemia, liraglutide amatsitsa insulin secretion popanda kuletsa secretion wa glucagon. Njira yochepetsera glycemia imaphatikizaponso kuchepetsedwa pang'ono kwa kutsuka kwa m'mimba. Pogwiritsa ntchito njira zomwe zimayambitsa kuchepa kwa njala komanso kuchepa kwa mphamvu yamagetsi, liraglutide imabweretsa kuchepa kwa minofu ya adipose komanso kuwonda.
GLP-1 ndi owongolera azakudya ndi zama calorie, zolandilira za peptidezi zimapezeka m'malo angapo aubongo omwe akukhudzidwa ndi kayendetsedwe kazakudya.
Mukamachititsa maphunziro a nyama, zidapezeka kuti kudzera mwa kuphatikiza mwachindunji kwa zolandila za GLP-1, liraglutide imathandizira zizindikiritso ndikuchepetsa ma siginolo am'manja, potero kumatsogolera kuwonda.
Komanso, malinga ndi maphunziro a nyama, liraglutide imachedwetsa kukula kwa matenda ashuga. Katunduyu ndiwothandiza kwambiri pakukondweretsedwa kwapadera kwa pancreatic β-cell ndikulepheretsa imfa ya β-cell (apoptosis), yomwe imayambitsa ma cytokines ndi mafuta acids aulere. Chifukwa chake, liraglutide imawonjezera insulin biosynthesis ndikuwonjezera kuchuluka kwa β-cell. Pambuyo polimbitsa shuga ndende, liraglutide imasiya kuwonjezera kuchuluka kwa ma pancreatic β-cell.
Wovutitsayo amakhala ndi nthawi yayitali ya maola 24 ndikuwongolera kuwongolera kwa glycemic, komwe kumatheka chifukwa chochepetsa kuchuluka kwa shuga m'magazi ndikatha kudya ndi shuga yachiwiri.
Pambuyo pa kayendetsedwe ka subcutaneous, kuyamwa kwa liraglutide kumayamba pang'onopang'ono, Tmax (nthawi yoti mufikire kuchuluka kwa ndende) mu plasma ndi maola 8-12. Cmax (kuchuluka kwa ndende) mu plasma pambuyo kukhazikitsa limodzi mlingo wa 0.6 mg ndi 9,4 nmol / L. Mukamagwiritsa ntchito mlingo wa 1.8 mg pafupifupi Css (equilibrium concentration) mu plasma imafika pafupifupi 34 nmol / L. Kuwonekera kwa chinthu kumathandizidwa molingana ndi mlingo. The intra-payekha payekha kusintha kwa AUC (dera pansi pa ndende nthawi pamapindikira) pambuyo makonzedwe a liraglutide limodzi mlingo 11%. Mtheradi bioavailability pafupifupi 55%.
Zikuwoneka Vd (kuchuluka kwa magawidwe) a liraglutide mu minofu yokhala ndi njira yotsogola yoperekera ndi 11-17 l, mtengo wapakati wa Vd pambuyo mtsempha wa magazi makonzedwe - 0,07 l / kg. Kumanga kwofunikira kwa liraglutide ndi mapuloteni a plasma kumadziwika (> 98%).
Kagayidwe ka liraglutide kumachitika ngati mapuloteni akuluakulu, osatenga nawo mbali monga njira yodziwitsira chiwalo chilichonse. Maola 24 pambuyo pa kuperekedwa kwa mlingo umodzi, mankhwala osasinthidwawo amakhalabe gawo lalikulu la plasma. Ma metabolites awiri adapezeka mu plasma (≤ 9 ndi ≤ 5% ya mlingo wonse).
Liraglutide wosasintha pambuyo makonzedwe a 3 H-liraglutide mu mkodzo kapena ndowe sichitsimikizike. Kachigawo kochepa chabe ka metabolites komwe kamakhudzana ndi thunthu kamakhudzidwa ndi impso kapena matumbo (6 ndi 5%, motsatana). Pambuyo subcutaneous makonzedwe a limodzi liraglutide, pafupifupi chilolezo cha thupi pafupifupi 1,2 l / h pochotsa T1/2 pafupifupi maola 13.
Malinga ndi malangizo, Viktoza amagwiritsidwa ntchito pa matenda a shuga 2 kuphatikiza zakudya komanso masewera olimbitsa thupi kuti akwaniritse kuwongolera kwa glycemic.
Njira zotheka kugwiritsa ntchito mankhwalawa:
- monotherapy
- kuphatikiza chithandizo chamankhwala amodzi kapena angapo amkamwa hypoglycemic othandizira (thiazolidinediones, sulfonylureas, metformin) mwa odwala omwe alephera kukwaniritsa machitidwe oyenera a glycemic panthawi yamankhwala am'mbuyomu,
- kuphatikiza mankhwala a basal insulin odwala omwe alephera kukwaniritsa bwino glycemic control pogwiritsa ntchito Victoza osakanikirana ndi metformin.
- matenda ashuga ketoacidosis,
- mtundu 1 shuga
- angapo endocrine neoplasia mtundu 2,
- chiwindi ntchito,
- kuvulala kwambiri aimpso,
- diabetic gastroparesis,
- matenda amatupa,
- Kulephera kwamtima kwa mtima kwa III - kalasi yogwira ntchito malinga ndi gulu la New York Cardiology Association (NYHA),
- mbiri yodwala khansa ya chithokomiro, kuphatikizapo banja,
- wazaka 18
- mimba ndi mkaka wa m`mawere
- Hypersensitivity ku gawo lililonse la Victoza.
- matenda a chithokomiro
- kulephera kwamtima kwa I - II gulu lothandiza malinga ndi gulu la NYHA,
- zaka zopitilira 75.
Maupangiri ogwiritsira ntchito mankhwala osokoneza bongo
Cholembera chilichonse cha syringe chimapangidwa kuti chizigwiritsa ntchito payekha.
Mankhwalawa amayenera kuperekedwa pogwiritsa ntchito singano mpaka 8 mm kutalika mpaka 32G wandiweyani (osaphatikizidwa, motero wogulidwa payokha). Ma cholembera a syringe amaphatikizidwa ndi singano zotayira za NovoTvist ndi NovoFayn.
Victoza sayenera kuperekedwa ngati yankho likuwoneka losiyana ndi madzi owoneka bwino, osakonda kopanda utoto.
Simungathe kulowa mankhwalawa ngati chayamba kuzizira.
Osasunga cholembera ndi singano yomata. Pambuyo pa jekeseni aliyense, amayenera kutayidwa. Kuchita izi kumalepheretsa kutayikira, kuipitsidwa ndi matenda a mankhwalawo, komanso kumatsimikizira kulondola kwa dosing.
Victoza: malongosoledwe, malangizo ogwiritsira ntchito, chithunzi
Mankhwala Victoza akuwonetsedwa kuti agwiritsidwe ntchito kwa odwala omwe ali ndi mtundu wachiwiri wa matenda osokoneza bongo monga chothandiza. Imagwiritsidwa ntchito nthawi yomweyo ndi chakudya komanso kuwonjezera zolimbitsa thupi kuchititsa matenda a shuga.
Liraglutide yomwe ndi gawo la mankhwalawa imakhudza kulemera kwa thupi ndi mafuta m'thupi. Imagwira mbali zina zamanjenje zapakati zomwe zimayambitsa njala. Wovutitsayo amathandiza wodwalayo kuti azimva kutalika kwa nthawi yayitali pochepetsa kugwiritsa ntchito mphamvu.
Mankhwalawa amatha kugwiritsidwa ntchito ngati mankhwala odziimira pawokha, kapena osakanikirana ndi mankhwala ena. Ngati mankhwalawa ali ndi mankhwala okhala ndi metformin, sulfonylureas kapena thiazolidatediones, komanso kukonzekera kwa insulini kulibe vuto, ndiye kuti Victoza angalembedwe mankhwala omwe adamwa kale.
Mankhwala ndikugwiritsa ntchito mankhwalawa amayi apakati kapena oyembekezera
Mankhwala okhala ndi liraglutide ali osavomerezeka kuti agwiritsidwe ntchito panthawi yomwe muli ndi pakati komanso pokonzekera. Munthawi imeneyi, shuga abwinobwino azisamalidwa ndi mankhwala omwe ali ndi insulin. Ngati wodwalayo adagwiritsa ntchito Victoza, ndiye kuti pambuyo pake kutenga pakati kuyenera kuyimitsidwa nthawi yomweyo.
Zotsatira za mankhwalawa paubwino wa mkaka wa m'mawere sizikudziwika. Mukadyetsa, kutenga Viktoza sikulimbikitsidwa.
Zotsatira zoyipa
Poyesa Victoza, odwala nthawi zambiri amadandaula za mavuto am'mimba. Adanenanso kusanza, kutsegula m'mimba, kudzimbidwa, kupweteka pamimba. Izi zimawonedwa mwa odwala kumayambiriro kwa makonzedwe kumayambiriro kwa kayendetsedwe ka mankhwala. M'tsogolomu, pafupipafupi zotsatirapo zoyipa zotere zidachepetsedwa kwambiri, ndipo mkhalidwe wa wodwalayo umakhala wokhazikika.
Zotsatira zoyipa za kupuma zimawonedwa nthawi zambiri, pafupifupi 10% ya odwala. Amakhala ndi matenda amtundu wa kupuma kwamatumbo. Mukamamwa mankhwalawa, odwala ena amadandaula chifukwa cha mutu wopitilira.
Pogwiritsa ntchito mankhwala osokoneza bongo osiyanasiyana, hypoclycemia imayamba. Kwenikweni, izi zimadziwika ndi chithandizo chanthawi imodzi ndi Viktoza komanso mankhwala osokoneza bongo omwe amapezeka kuchokera ku sulfonylurea.
Zotsatira zoyipa zilizonse zomwe zimachitika mukamamwa mankhwalawa ndi chidule.
Zotsatira zonse zomwe zidafotokozedwa mwachidule patebulopo zidadziwika nthawi yayitali ya gawo lachitatu la mankhwalawa Victoza, komanso kutengera mauthenga obwera nawo. Zotsatira zoyesedwa mu kafukufuku wanthawi yayitali zimapezeka odwala opitilira 5% omwe amatenga Victoza, poyerekeza ndi odwala omwe akuchita mankhwala ena.
Komanso pathebulopo tafotokozanso zotsatira zoyipa zomwe zimapezeka mwa opitilira 1% ya odwala ndipo pafupipafupi kukula kwawoko ndi kawiri konse kakulidwe kazomwe umamwa ena. Zotsatira zonse zoyipa patebulopo zimagawika m'magulu potengera ziwalo komanso pafupipafupi zomwe zimachitika.
Hypoglycemia
Zotsatira zoyipa za odwala omwe Victoza anali wofatsa. Pankhani ya odwala matenda a shuga ndi mankhwalawa okha, kupezeka kwa hypoglycemia sikunenedwe.
Zotsatira zoyipa, zomwe zimafotokozedwa ndi kuchuluka kwambiri kwa hypoglycemia, zimawonedwa panthawi yovuta ya mankhwala a Viktoza pokonzekera zomwe zimachokera ku sulfonylurea.
Mankhwala osokoneza bongo omwe ali ndi liraglutide ndi mankhwala omwe alibe sulfonylurea samapereka zotsatira zoyipa za hypoglycemia.
Matumbo
Njira zoyipa zoyambira kuchokera m'matumbo am'mimba zambiri zimasonyezedwa ndikusanza, mseru ndi m'mimba. Iwo anali opepuka mwachilengedwe ndipo anali ofanana ndi gawo loyamba la chithandizo. Pambuyo pake panali kuchepa kwa zomwe zimachitika chifukwa cha zovuta izi. Milandu yakuchotsedwa kwa mankhwalawa chifukwa cha zovuta zomwe zimachitika m'matumbo am'mimba sizinalembedwe.
Pakufufuzidwa kwanthawi yayitali kwa odwala omwe amatenga Victoza osakanikirana ndi metformin, 20% yokha idadandaula za vuto limodzi la nseru panthawi ya chithandizo, pafupifupi 12% ya matenda otsegula m'mimba.
Mankhwala osakanikirana ndi mankhwala okhala ndi liraglutide ndi zotumphukira za sulfonylurea adabweretsa zotsatirapo zotsatirazi: 9% ya odwala amadandaula ndi mseru akumwa mankhwala, ndipo pafupifupi 8% adadandaula za matenda otsegula m'mimba.
Poyerekeza zomwe zimachitika mukamamwa mankhwala a Viktoza ndi mankhwala ena omwe ali ofanana ndi mankhwala omwe amapezeka, zotsatira zoyipa zimadziwika mu 8% ya odwala omwe amatenga Victoza ndi 3.5 - akumamwa mankhwala ena.
Chiwerengero cha zoyipa za anthu okalamba chinali zapamwamba pang'ono. Matenda okhala ndi vuto limodzi, monga kulephera kwa impso, amakhudzanso zomwe zimachitika.
Pancreatitis
Muzochita zachipatala, milandu ingapo yonyansa yamankhwala imapangidwa ndikukula ndikuchulukirachulukira kwa kapamba akuti. Komabe, kuchuluka kwa odwala omwe matendawa adapezeka chifukwa chotenga Victoza ndi ochepera 0.2%.
Chifukwa cha kuchepa kwakukulu kwa izi komanso chifukwa chakuti kapamba ndi vuto la shuga, sizokayikitsa kutsimikizira kapena kutsutsa izi.
Chithokomiro
Chifukwa chophunzira momwe mankhwalawa amathandizira odwala, zomwe zimapangitsa kuti chithokomiro chizigwira. Kuwona kunachitika kumayambiriro kwa maphunzirowa ndikugwiritsa ntchito liraglutide kwa nthawi yayitali, placebo ndi mankhwala ena.
Kuchuluka kwa zoyipa zomwe anali motere:
- liraglutide - 33,5,
- placebo - 30,
- mankhwala ena - 21.7
Kukula kwa mfundo izi ndi kuchuluka kwa zovuta zomwe zimakhudzidwa zaka 1000 zomwe munthu amagwiritsa ntchito ndalama. Mukamamwa mankhwalawa, pamakhala chiopsezo chokhala ndi vuto lalikulu la chithokomiro.
Zina mwazotsatira zoyipa kwambiri, madotolo amawona kuchuluka kwa magazi a calcitonin, goiter komanso ma neoplasms osiyanasiyana a chithokomiro.
Mukamamwa Victoza, odwala adanenanso kuti thupi siligwirizana. Pakati pawo, khungu loyenda, urticaria, mitundu yosiyanasiyana ya totupa imatha kusiyanitsidwa. Mwa milandu yayikulu, milandu ingapo ya anaphylactic imadziwika ndi izi:
- kutsika kwa magazi,
- kutupa
- kupuma movutikira
- kuchuluka kwa mtima.
Mankhwala osokoneza bongo
Malinga ndi malipoti ofufuza zamankhwala, nkhani imodzi ya mankhwala osokoneza bongo idalembedwa. Mlingo wake udaposa 40 nthawi yoyenera. Mphamvu ya bongo anali kwambiri mseru komanso kusanza. Zodabwitsa monga hypoglycemia sizinadziwike.
Pambuyo pa chithandizo choyenera, kuchira kwathunthu kwa wodwalayo komanso kusapezeka kwathunthu kwa mankhwala osokoneza bongo adadziwika. Pankhani ya bongo, ndikofunikira kutsatira malangizo a madokotala ndikugwiritsa ntchito mankhwala oyenerera.
Kugwirizana kwa Victoza ndi Mankhwala Ena
Pounika momwe liraglutide imathandizira matenda a shuga, kuchepa kwake ndi zinthu zina zomwe zimapanga mankhwalawo kunadziwika. Zinadziwikanso kuti liraglutide imakhudzanso kupopera kwa mankhwala ena chifukwa chovuta kutulutsa m'mimba.
Kugwiritsa ntchito pamodzi kwa paracetamol ndi Victoza sikufuna kusintha kwa mankhwalawa. Zomwezi zimagwiranso ntchito pa mankhwalawa: atorvastatin, griseofulvin, lisinopril, kulera kwapakamwa. Panthawi yogwiritsidwa ntchito molumikizana ndi mankhwala amtunduwu, kuchepa kwa mphamvu yawo sikunawonedwenso.
Kuti muthandizike kwambiri, nthawi zina, kupatsidwa insulin ndi Viktoza ndi mankhwala. Kuyanjana kwa mankhwalawa sikunaphunzirepo kale.
Popeza kafukufuku wokhudza kuphatikiza kwa Viktoza ndi mankhwala ena sanachitike, madokotala salimbikitsidwa kumwa mankhwalawa nthawi imodzi.
Kugwiritsa ntchito mankhwala ndi kumwa
Mankhwalawa amapaka jekeseni pang'ono m'chiuno, mkono wapamwamba, kapena pamimba. Mankhwala, jakisoni wa nthawi 1 patsiku ndikokwanira nthawi iliyonse, mosasamala kanthu za kudya. Nthawi ya jakisoni ndi malo ake jakisoni amatha kusinthidwa ndi wodwalayo payokha. Pankhaniyi, ndikofunikira kutsatira mlingo wa mankhwalawo.
Ngakhale kuti nthawi yopanda jekeseni siyofunika, timalimbikitsidwabe kuperekera mankhwalawa nthawi yomweyo, yomwe ili yoyenera kwa wodwalayo.
Zofunika! Victoza sagwiritsidwa ntchito kudzera m'mitsempha kapena m'mitsempha.
Madokotala amalimbikitsa kuyambitsa chithandizo ndi 0,6 mg ya liraglutide patsiku. Pang'onopang'ono, mlingo wa mankhwalawa uyenera kuchuluka. Pambuyo pa sabata la mankhwala, mlingo wake uyenera kuwonjezeka ndi 2 times. Ngati pakufunika, wodwalayo atha kuwonjezera mlingo wa 1.8 mg mlungu wamawa kuti akwaniritse zotsatira zabwino zamankhwala. Kuwonjezeka kwina kwa mankhwalawa osavomerezeka sikulimbikitsidwa.
Wowonongera amatha kugwiritsidwa ntchito ngati chowonjezera cha mankhwala omwe ali ndi metformin kapena chithandizo chovuta ndi metformin ndi thiazolidinedione. Pankhaniyi, mlingo wa mankhwalawa ukhoza kusiidwa pamlingo womwewo popanda kusintha.
Kugwiritsa ntchito Viktoza monga mankhwala osokoneza bongo okhala ndi sulfonylurea kapena njira yovuta yokhala ndi mankhwalawa, ndikofunikira kuti muchepetse kuchuluka kwa sulfonylurea, popeza kugwiritsidwa ntchito kwa mankhwalawa m'miyeso yapitayi kungayambitse hypoglycemia.
Kuti musinthe mlingo wa Viktoza tsiku ndi tsiku, sikofunikira kuchita mayeso kuti mupeze kuchuluka kwa shuga. Komabe, kupewa hypoglycemia m'magawo oyamba a zovuta mankhwala okhala ndi sulfonylurea, ndikofunikira kuyang'anira kuchuluka kwa shuga m'magazi.
Kugwiritsa ntchito mankhwalawa m'magulu apadera a odwala
Mankhwalawa amatha kugwiritsidwa ntchito mosasamala zaka za wodwalayo. Odwala achikulire osaposa zaka 70 safuna kusintha kwapadera kwa mankhwala tsiku lililonse. Mwachidziwitso, zotsatira za mankhwalawa kwa odwala osakwana zaka 18 sizinakhazikitsidwe. Komabe, pofuna kupewa kupezeka kwa zovuta komanso zovuta, mankhwalawa ali osavomerezeka kwa odwala omwe ali ndi zaka 18.
Kusanthula kwa kafukufuku kumawonetsa zomwe zimachitika mthupi la munthu, mosaganizira jenda ndi mtundu. Izi zikutanthauza kuti zovuta zamankhwala zokhala liraglutide sizimayenderana ndi wodwala komanso mtundu.
Komanso, palibe zovuta pazotsatira zamatenda a liraglutide zinapezeka. Kafukufuku akuwonetsa kuti index yamasamba a thupi alibe gawo lalikulu pazotsatira za mankhwalawa.
Ndi matenda a ziwalo zamkati ndi kuchepa kwa ntchito zawo, mwachitsanzo, kulephera kwa chiwindi kapena aimpso, kuchepa kwa mphamvu yogwira ntchito ya mankhwala. Kwa odwala omwe ali ndi matenda osakhazikika, kusintha kwa mankhwalawa sikofunikira.
Odwala omwe ali ndi vuto lochepa kwambiri kwa hepatic, mphamvu ya liraglutide inachepetsedwa ndi pafupifupi 13-23%. Kulephera kwambiri kwa chiwindi, ntchito yake idatsala pang'ono kutha. Kuyerekeza kunapangidwa ndi odwala omwe ali ndi ntchito yofanana ndi chiwindi.
Pakulephera kwa impso, kutengera kuwuma kwa matendawa, mphamvu ya Viktoza idatsika ndi 14-33%. Ngati matenda a impso akuwonongeka, mwachitsanzo, ngati kulephera kwaimpso kumatha, mankhwalawa ndi osavomerezeka.
Zomwe zimatengedwa kuchokera kuzomwe zimayankhidwa ndi mankhwalawa.