Mndandanda wa mankhwala linagliptin * (linagliptin *)

5 mg mapiritsi okhala ndi mafilimu

Piritsi limodzi lili

ntchito yogwira - linagliptin 5 mg,

zokopa: mannitol, wowuma pregelatinized, wowuma chimanga, Copovidone, magnesium stearate,

Chipolopolo cha opadry®pinki (02F34337): hypromellose 2910, titanium dioxide (E 171), talc, macrogol 6000, iron (III) oxide ofiira (E 172).

Mapiritsi ozungulira okhala ndi biconvex kumtunda, okhala ndi mbali zokutidwa, yokutidwa ndi chipolopolo cha mtundu wofiirira wofiirira, wojambula ndi chizindikiro cha BI mbali imodzi ndikujambulidwa "D5" mbali inayo.

Mankhwala

Pharmacokinetics

Mutatenga linagliptin pakamwa pa 5 mg, mankhwalawa amalowetsedwa msanga, nsonga za plasma (Median Tmax) zimachitika pambuyo pa maola 1.5. Kuzama kwa plasma linagliptin kumachepera malinga ndi gawo la magawo atatu. The terminal half-life is long (maola opitilira 100), omwe amakhala makamaka chifukwa cholimba kwambiri, cholimba cha linagliptin ku DPP-4 ndipo sizitsogolera pakuphatikizika kwa mankhwalawa. Hafu yaumoyo wa kuchuluka kwa linagliptin pambuyo mobwerezabwereza makonzedwe a linagliptin pa 5 mg pafupifupi maola 12. Pambuyo pa gawo limodzi la lignagliptin pa mlingo wa 5 mg, mankhwala osasunthika a plasma amachitika pambuyo pa mlingo wachitatu, pomwe AUC (malo omwe ali munthawi yopondera) ya lignagliptin mu plasma imakwera pafupifupi 33% poyerekeza ndi mlingo woyamba. Ma coefficients amitundu yosiyanasiyana mu pharmacokinetic magawo a AUC ya linagliptin anali ochepa (12.6% ndi 28,5%).

The pharmacokinetics of lignagliptin is nonlinear, plasma yonse ya AOL ya lignagliptin imachulukitsa modzimira modalira kuposa AUC yopanda malire, ikukula molingana ndi mlingo. Ma pharmacokinetics a linagliptin mwa anthu athanzi komanso odwala omwe ali ndi mtundu wa 2 matenda a shuga.

Cholinga: mtheradi wa bioavailability wa linagliptin pafupifupi 30%. Kulandila kwa linagliptin ndi chakudya chamafuta kwambiri kumawonjezera nthawi kuti ifike ku Cmax ndi maola awiri a 2 ndipo kumapangitsa kutsika kwa Cmax ndi 15%, koma sikukukhudza maola AUC0-72. Chifukwa chake palibe kusintha kwakukuru mu Cmax ndi Tmax, motero, linagliptin ingagwiritsidwe ntchito mosasamala chakudya.

Kugawa: ambiri voliyumu yogawa mu ofanana pambuyo pa limodzi mlingo wa 5 mg kudzera m`mitsempha pafupifupi 1110 malita, kuwonetsa kugawa kwambiri mu zimakhala. Kumangidwa kwa linagliptin kupita ku mapuloteni a plasma kumadalira kuchuluka kwa mankhwalawa ndikuchepetsa kuchoka pa 99% ku 1 nmol / L mpaka 75-89% ku> 30 nmol / L, zomwe zikuwonetsa kukwezedwa kwa kumanga kwa DPP-4 ndikuwonjezereka kwa kuchuluka kwa lignagliptin. Pazowunikira kwambiri za linagliptin ndi machulukitsidwe athunthu a DPP-4, 70-80% ya linagliptin imamangiriza mapuloteni ena a plasma (osati DPP-4), ndi 20-30% mu plasma yaulere.

Matenda a metabolism ndi chimbudzi: gawo laling'ono la mankhwala lomwe limalandilidwa mthupi limapukusidwa. Njira yayikulu yotulutsira m'matumbo imakhala pafupifupi 80% ndipo 5% ya linagliptin imatuluka mkodzo.

Kuchotsa chilolezo ndi pafupifupi 70 ml / mphindi.

Magulu apadera a odwala

Odwala omwe ali ndi vuto la aimpso: odwala omwe ali ndi vuto lililonse la impso, kusintha kwa linagliptin sikofunikira. Kuchepa pang'ono kwa impso sikumakhudza pharmacokinetics ya linagliptin odwala omwe ali ndi matenda a shuga a 2.

Odwala omwe ali ndi vuto la chiwindi: Odwala omwe ali ndi vuto la chiwindi cha digiri iliyonse (makalasi A, B ndi C malinga ndi gulu la ana-Pugh), kusintha kwa mankhwalawa kwa linagliptin sikofunikira.

Mlingo woyenera malinga ndi jenda, kuchuluka kwa thupi (BMI), mtundu, ndi zaka za odwala sizofunikira.

Ana: maphunziro a pharmacokinetics a linagliptin mwa ana sanachitike.

Mankhwala

Linagliptin ndi choletsa wa enzyme DPP-4 (dipeptidyl peptidase 4, EC code 3.4.14.5), yomwe ikuphatikizidwa ndi kupangika kwa ma intretins mahomoni - glucagon-ngati peptide-1 (GLP-1) ndi glucose-insulinotropic polypeptide (GIP). Ma hormone awa amawonongeka mwachangu ndi enzyme DPP-4. Ma insretin onsewa akukhudzidwa ndi kuyendetsa thupi kwa glucose homeostasis. Mlingo woyambira wa insretin secretion masana ndi wotsika, umakwera msanga mutatha kudya. GLP-1 ndi GIP zimathandizira kukhala biosynthesis ndi secretion ya insulin ndi masamba a pancreatic beta pamlingo wambiri komanso wokwera wamagazi. Kuphatikiza apo, GLP-1 imachepetsa kubisalira kwa glucagon ndi maselo a pancreatic alpha, omwe amatsogolera kuchepa kwa kupanga kwa shuga mu chiwindi.

Linagliptin imagwira bwino komanso imasinthidwa kumanga ku DPP-4, yomwe imayambitsa kuwonjezeka kosasunthika kwa ma insretins komanso kusunga kwakanthawi ntchito yawo. Linagliptin imakulitsa katemera wa insulini kutengera kuchuluka kwa glucose ndipo amachepetsa katulutsidwe wa glucagon, kukonza glucose homeostasis.

Linagliptin amadzisankhira kusankha DPP-4, muvitro kapangidwe kake kupitilira kusankha kwa DPP-8 kapena ntchito ya DPP-9 nthawi zopitilira 10,000.

Kuchita Mwachipatala ndi Chitetezo

Kuti muwone kuyendetsa bwino ndi chitetezo, mayesero 8 azoyenda mosasamala a gawo lachitatu adachitika pogwiritsa ntchito linagliptin.

Linagliptin monotherapy: kugwiritsa ntchito linagliptin pa mlingo wa 5 mg kamodzi patsiku kunapangitsa kutsika kwakukulu kwa glycated hemoglobin A (HbA1c) ndi 0.69% poyerekeza ndi placebo, mwa odwala omwe ali ndi HbA1c yoyambira pafupifupi 8%. Linagliptin imathandizanso kuchepa kwakukulu kwa kudya kwa plasma glucose (GPN) ndi maola 2 mutatha kudya (GLP). Zomwe zimachitika mu hypoglycemia mwa odwala omwe amalandidwa linagliptin kapena placebo zinali zofanana.

Linagliptin monotherapymwa odwala omwe sayenera kulandira chithandizo cha metformin chifukwa cha tsankho lake kapena kuphwanya kwake chifukwa cha kulephera kwa impso, adawonetsa kuwonjezeka kwakukulu kwa HbA1c ndi - 0.57% poyerekeza ndi placebo, mwa odwala omwe ali ndi msana wa HbA1c pafupifupi 8.09%. Linagliptin adawonetsa kuchepa kwakukulu kwa kudya kwa plasma glucose (GPN) poyerekeza ndi placebo. Zomwe zimachitika mu hypoglycemia mwa odwala omwe amalandidwa linagliptin kapena placebo zinali zofanana.

Linagliptin monotherapy: zambiri kuchokera pakayerekezedwa ndi masabata 12 ndi placebo ndi zambiri kuchokera pakayerekezera masabata a 26 ndi cy-glucosidase inhibitor (voglibose).

Kuchita bwino ndi chitetezo cha linagliptin monotherapy ndidaphunziranso poyerekeza ndi placebo (masabata 12) komanso ndi voglibose (α-glucosidase inhibitor) kwa masabata 26. Linagliptin pa mlingo wa 5 mg unatsogolera kuwonjezeka kwakukulu kwa HbA1c poyerekeza ndi placebo (-0.87%), chiwerengero choyambirira cha HbA1c chinali 8,0%. Zinawonetsedwanso kuti kugwiritsa ntchito linagliptin pa mlingo wa 5 mg kumadziwika ndi kuwonjezeka kwakukulu pamlingo wa HbA1c, kusintha kwa -0.32% poyerekeza ndi voglibose, kukula koyamba kwa HbA1c kunali 8.0%. Kuphatikiza apo, linagliptin idayambitsa kusintha kwakukulu pakupanga shuga m'magazi (GPN) (kuchepa kwa 19.7 mg / dl / 1.1 mmol / L poyerekeza ndi placebo ndi 6.9 mg / dl / 0.4 mmol / L poyerekeza ndi voglibose), ndi mulingo wakulephera wa HbA1c (

Kufotokozera za mankhwalawa

Linagliptin * (Linagliptin *) - Wothandizira Hypoglycemic. Linagliptin ndi choletsa wa enzyme dipeptidyl peptidase-4 (DPP-4), yomwe ikuphatikizidwa ndi inactivation ya mahomoni amtundu - glucagon-ngati peptide mtundu 1 (GLP-1) ndi glucose-insulinotropic polypeptide (HIP). Ma hormone awa amawonongeka mwachangu ndi enzyme DPP-4. Zonsezi ma incretin zimathandizira kuti thupi lizisungunuka. Zoyambira zapansi pa GLP-1 ndi GUI masana ndizochepa, zimachulukirachulukira poyankha chakudya. GLP-1 ndi HIP zimathandizira insulin biosynthesis ndi katulutsidwe kake ka maselo a pancreatic beta panthawi yokhazikika kapena yokwera yamagazi. Kuphatikiza apo, GLP-1 imachepetsa kubisalira kwa glucagon ndi maselo a pancreatic alpha, omwe amatsogolera kuchepa kwa kupanga kwa shuga mu chiwindi.

Linagliptin amagwira ntchito limodzi ndi enzyme DPP-4 (chomangira chosinthika), chomwe chimayambitsa kuwonjezeka kosasunthika kwa ma insretins komanso kusunga kwakanthawi ntchito yawo. Kuchulukitsa shuga wodalira glucose ndipo kumachepetsa katulutsidwe wa glucagon, kamene kamayambitsa matenda a shuga m'magazi. Linagliptin amadzisankhira moyenera enzyme DPP-4 ndipo ali ndi mawonekedwe owerengeka okwanira 10,000 a DPP-4 poyerekeza ndi enzymes dipeptyl peptidase-8 kapena dipeptyl peptidase-9 mu vitro.

Kutulutsa mawonekedwe, kapangidwe kake ndi ma CD

Amapezeka mu mawonekedwe a piritsi mumitundu iwiri ya alogliptin - 12,5 ndi 25 mg.

Othandizira (mwachitsanzo, "Vipidia"):

• mannitol
• cellcrystalline mapadi,
• Hyprolose
• sodium croscarmellose,
• magnesium wakuba.

Mapiritsi osungunula, odzaza matuza. Mu phukusi 4 matuza a 7 zidutswa.

Zotsatira za pharmacological

Hypoglycemic wothandizira. Ndi cholepheretsa cha DPP-4, chomwe chimawononga mahomoni a insretin. Amathandizira kuwonjezera insulin yopanga ma cell a pancreatic beta, komanso amachepetsa kupanga shuga kwa chiwindi. Zotsatira zake, glycosylated hemoglobin imatsika ndipo kuchuluka kwa shuga m'magazi kumatsika, komanso pamimba yopanda kanthu, ndikatha kudya zofanana.

Pharmacokinetics

Bioavailability pafupifupi 100%. Itha kugwiritsidwa ntchito mosasamala nthawi yakudya, chifukwa izi sizikhudza kupezeka ndi kuchuluka kwa zinthu zomwe zikugwirika. Kuzindikira kwakukulu kumatheka pambuyo pa maola 1-2. Samadzikundana m'thupi. Imayatsidwa osasinthika ndi impso. Gawo limatuluka ndi matumbo. Hafu ya moyo wa thupi ndi maora 21.

Contraindication

• Hypersensitivity pamagawo ake,
• Kulephera kwakukulu kwa impso ndi kwa hepatic,
• Mtundu woyamba wa shuga
• Matenda a shuga ketoacidosis
• Mbiri yakale yokoma
• Kulephera kwa mtima
• Ana osakwana zaka 18
• Mimba komanso kuyamwa.

Gwiritsani ntchito mosamala pazochitika zotsatirazi:

• Pancreatitis
• Kulephera kwapakati kwaimpso
• Kulandila molumikizana ndi othandizira ena a hypoglycemic.

Malangizo ogwiritsira ntchito (njira ndi Mlingo)

Imatengedwa pakamwa popanda kutafuna, koma imatsukidwa ndi madzi ambiri. Malangizo onse ndi 25 mg ya alogliptin patsiku. Mlingo weniweni umayikidwa ndi adotolo pamaziko a umboni. Itha kugwiritsidwa ntchito kuphatikiza mankhwala. Pankhaniyi, mlingo umachepetsedwa kupewa hypoglycemia. Ngati mukusowa mlingo, ndikofunika kumwa mapiritsi msanga. Mlingo wachiwiri woti ugwire umaletsedwa!

Kuyanjana kwa mankhwala osokoneza bongo

Palibe zotsatira zoyanjana za alogliptin ndi zinthu zina zomwe zadziwika.

Gawo lenilenilo silikhudza zochita za mankhwala otsatirawa:

• khofi
• glibenclamide,
• warfarin
• tolbutamide
• pioglitazone
• atorvastatin,
• kulera kwamlomo
• dextromethorphan
• fexofenadine,
• midazolam
• metformin
• digoxin
• cimetidine.

Zotsatira za alogliptin sizikhudzidwa:

• gemfibrozil
• cyclosporin
• fukuchiyama
• alpha glucosidase inhibitor
• ketoconazole,
• metformin
• pioglitazone
• digoxin
• cimetidine
• atorvastatin.

Ndiye kuti, kulandirana kwawo kotetezeka. Komabe, muyenera kukumbukiridwa kuti pochiza ndi alogliptin limodzi ndi sulfonylurea, insulin, kusintha kwa mankhwalawa kumafunikira kuti muchepetse chiopsezo cha hypoglycemia.

Malangizo apadera

Ndikofunika mukamamwa mankhwala ena a hypoglycemic kuti musankhe mlingo woyenera wa mankhwalawa kuti mupewe mavuto.

Chenjezo liyenera kuchitika mukamapereka mankhwala kwa anthu omwe ali ndi vuto la kutupa kwa impso komanso aimpso.

Pali chiopsezo chokhala ndi pancreatitis pachimake. Chizindikiro chake chachikulu ndi kupweteka kwakanthawi, m'mimba. Kukayikira kulikonse kwa chitukuko kumafunikira kuchipatala komanso kulandira chithandizo choyenera.

Ngati pali zolakwika pakugwira impso kapena chiwindi pakumwa, njira ya mankhwalawa iyenera kusinthidwa ndipo mankhwalawo ayenera kusiyidwa.

Alogliptin yokha siyimakhudza kuyendetsa galimoto, komabe, kuphatikiza ndi insulin kapena sulfonylurea, chiwopsezochi chikuwoneka. Chifukwa chake, ngati kuli kotheka, muyenera kukana kuyendetsa galimoto ndikugwira ntchito ndi zida.

Imatulutsidwa kokha pamankhwala!

Gwiritsani ntchito muubwana ndi ukalamba

Palibe zambiri pakukhudzidwa kwa thupi la ana, chifukwa chake, mankhwalawa amaletsedwa kuchiza anthu osakwana zaka 18.

Palibe zotsutsana pazovomerezeka za okalamba, komabe, ndikofunikira kukumbukira kuti m'badwo uno uli pachiwopsezo cha hypoglycemia ndi ketoacidosis. Kuwunikira pafupipafupi mkhalidwe kumafunikira.

Fananizani ndi fanizo

Pali mankhwala angapo omwe ali ndi katundu wofanana. Ayenera kuganiziridwa poyerekeza.

Vipidia. Mapiritsi okhala ndi Alogliptin. Mtengo - kuchokera ku ma ruble 840 phukusi lililonse. Yopangidwa ndi Takeda GmbH, Japan. Chodziwika kwambiri chopangidwa ndi chinthu ichi pakuphatikizika.

"Januvia." Zomwe zimagwiritsidwa ntchito ndi sitagliptin. Zogulitsa pakamwa, mtengo - kuchokera 1700 rubles. Wopanga - Merck Sharp ndi Dome, USA. Zomwe zimatha mankhwalawa ndizoyandikira kwambiri pamwambapa. Pali mitundu itatu ya muyeso wa chinthu. Zotsutsana zina, kuwunika bwino.

"Yanumet." Mtengo wa phukusi la mapiritsi a 56 ndi ma ruble 2800. Kuphatikizika - metformin ndi sitagliptin palimodzi. Yopangidwa ndi Merck Sharp & Dome, USA. Amagwiritsidwa ntchito onse mu monotherapy komanso molumikizana ndi mankhwala ena, kuphatikizapo insulin. Zinthu zambiri zoyipa ndi zoletsa kuvomereza. Komabe, ndemanga zimalemba kuti zimathandizira kuchepetsa bwino, zomwe ndizofunikira kwambiri kwa anthu odwala matenda ashuga.

Galvus Met. Mtengo - kuchokera ku 1500 rubles. Wopanga - "Novartis", Switzerland. Kuphatikizikako kumaphatikizapo metformin ndi vildagliptin. Mankhwala othandiza omwe amathandizanso kuchepa thupi mukamadya. Pali zotsutsana zambiri.

"Kuchulukitsa kwa Combogliz." Muli ndi metformin ndi saxagliptin. Mtengo - ma ruble 3300 ndi pamwambapa. Amapanga kampani "Bristol-Myers squibb", USA. Mapiritsi Otulutsidwa Omasulidwa. Pali zoletsa zambiri pazovomerezeka. Gwiritsani ntchito mosamala pothandizira achikulire.

Bagomet. Mankhwala okwera mtengo kwambiri (kuchokera ku ma ruble 160), koma ofanana pazinthu zonse. Amapanga kampani "Chemistry Montpelfer", Argentina. Pamtengo wotsika, mtunduwo umakhalabe wokwanira. Ndemanga za mankhwalawa ndi zabwino. Wopangidwa ndi metformin ndi glibenclamide.

Glibomet. Mapiritsi opangidwa ndi Berlin Chemie, Germany. Mtengo - kuchokera ku ma ruble a 350. Zinthu zogwira ntchito ndi glibenclamide ndi metformin. Mankhwalawa ali ndi zoletsa zingapo zoti atenge, zimadziwika kuti sizoyenera kwa odwala matenda ashuga onse. Oyenera kuphatikiza mankhwala.

Kusankha kusinthana ndi mankhwala ena kumapangidwa ndi katswiri. Kudzipatsa nokha koletsedwa!

Ndemanga zambiri zimakhala zabwino. Anthu amadziwa zabwino mu monotherapy komanso mankhwalawa. Kuchepetsa kulimbitsa thupi kumadziwika. Zotsatira zoyipa ndizochepa.

Valentina: “Mayi anga ali ndi zaka 10 akudwala matenda ashuga. Tayesani pafupifupi mapiritsi onse, sitikufuna kukhala pa insulin. Tsopano adalembedwa Glucophage Long ndi Vipidia. Ndife okondwa ndi zotsatira zake. Kunenepa kwachepa. Amamva bwino, anayamba kugwira ntchito, miyendo yake inali yotupa komanso zowawa. Kuphatikiza apo, mulingo wa shuga unakhazikika. Ndi mankhwala abwino bwanji! ”

Denis: “Ndakhala ndikuchitiridwa ndi Vipidia kwazaka zopitilira ziwiri. Ichi ndiye mankhwala abwino kwambiri omwe ndayesapo. Shuga ndi okhazikika, monganso kulemera. Palibe mavuto. Ndipo zomwe ndimakonda - chilakolako chochepa, sindikufuna kudya. ”

Larisa: “Poyamba ndinkagwiridwa ndi matenda a Diabetes, koma sizinkandiyendera. Shuga adalumpha. Adotolo adandiwuza kuti ndisinthe ku Vipidia. Adanenanso kuti ali ndi mavuto ochepa, amagwira bwino ntchito kwa ine. Ndipo anali kunena zoona. Msuzi wokhazikika wa shuga, makamaka ngati sindiphwanya zakudya. Piritsi limodzi patsiku ndilokwanira kuti thupi lizigwira ntchito bwino. Ndipo koposa zonse - palibe mantha ngati kuti hypoglycemia imachitika. Chinthu chachikulu sikuti kuphwanya zakudya. Ndasangalala kwambiri. "

Alla: "Ndakhala akundipanga ndi Vitidia ngati mankhwala osokoneza bongo kwazaka zingapo. Timangowonjezera mankhwala ndi dotolo, monga zosowa za thupi nthawi zina zimasintha. Ali ndi pakati, adasinthira insulin, koma atapempha kuti abwezeretsedwe ku Vipidia. Ndipo kulemera kudatha, komwe adakwanitsa kupitilira nthawi yayitali, ndipo thanzi lake lidayamba kuyenda bwino. Nthawi zonse, ndimakonda mankhwalawa. ”

Igor: “Ndidagwiritsa ntchito Vipidia pachipatala. Pang'onopang'ono ndinazindikira kuti mankhwalawo sanali oyenera kwa ine. Shuga sanasinthe, kenako adakula. Adotolo adati mapiritsiwo samandikwana. Ndinasinthira kukhala ndi insulin malinga ndi zomwe ndazindikira. ”

The zikuchokera ndi Mlingo mawonekedwe a mankhwala

Mankhwala odziwika kwambiri omwe ali ndi linagliptin ndi mankhwala a dzina lomweli.

The zikuchokera mankhwala zikuphatikizira waukulu yogwira thunthu - linagliptin. Mlingo umodzi wa mankhwalawa uli ndi 5 mg yogwira ntchito.

Kuphatikiza pa chophatikizira chachikulu, mankhwalawa ali ndi zowonjezera zina.

Zothandiza pazinthu zomwe zimapangidwa ndi mankhwalawa ndi motere:

1. Mannitol
2. Wowuma pregelatinized.
3. Wowuma chimanga.
4. Colovidone.
5. Magnesium wakuba.

Mankhwalawa ndi piritsi yolumikizidwa ndi filimu yofunikira.

Mapangidwe a zipolopolo zapadera za piritsi lililonse amaphatikizapo zinthu izi:

• Opadra pinki
• hypopellose,
• titanium dioxide
• talcum ufa
• macrogol 6000,
• oxide wachitsulo ndi wofiyira.

Mankhwala amapezeka mu mawonekedwe a mapiritsi okhala ndi mawonekedwe ozungulira. Mapiritsi adalowetsa m'mphepete mwa filimu. Chipolopolo cha phale ndichopepuka. Chipolopolocho chimalembedwa ndi chizindikiro cha kampani yopanga BI pamalo amodzi ndi D5 mbali inayo.

Mapiritsi amapezeka m'matumba a masamba a zidutswa 10 chilichonse. Matumba amadzaza pabokosi lamakhadi. Phukusi lililonse lili ndi matuza atatu. Onetsetsani kuti mulinso ndi malangizo ogwiritsira ntchito mankhwalawa piritsi lililonse la mankhwalawo.

Kusungidwa kwa mankhwalawa kuyenera kuchitika m'malo amdima osachepera 25 digiri Celsius.

Malo osungira mankhwalawa sayenera kupezeka kwa ana. Alumali moyo wa mankhwala ndi zaka 3.

Pomaliza

Chida ichi chimakhala chokhazikika komanso chothandizira pakulipira matenda a shuga. Amakhala ndi ndemanga zabwino pakati pa odwala ndi madokotala. Gawani ngakhale kwa anthu omwe ali ndi vuto laimpso komanso chiwindi, omwe nthawi zambiri amafunikira insulin. Maubwino owonjezereka a mankhwalawa ndi kuthekera kwake kutsimikiziridwa kuti muchepetse thupi komanso kukonza thanzi lathunthu. Chifukwa chake chidacho chimayenera kukhala pakati pa mankhwala ena omwe amalimbikitsidwa.

Pharmacodynamics ndi pharmacokinetics a mankhwala

Pambuyo pakukonzekera pakamwa kwa thupi, Linagliptin amadzimangirira ku dipeptidyl peptidase-4.

Chomangira chovuta chomwe chimapangidwanso chimatha kusintha. Kulumikizana kwa enzyme ndi linagliptin kumabweretsa kuwonjezeka kwa kuchuluka kwa ma insretin m'thupi ndipo kumathandizira kuti azichita ntchito yawo kwakanthawi.

Zotsatira za mankhwalawa ndi kuchepa kwa kupanga kwa glucagon ndikuwonjezereka kwa insulin, komwe kumapangitsa kuti shuga azikhala mthupi la munthu.

Mukamagwiritsa ntchito Linagliptin, kuchepa kwa glucose hemoglobin komanso kuchepa kwa zomwe zili m'magazi a m'magazi kunakhazikitsidwa modalirika.

Mutatha kumwa mankhwalawa, imamwidwa mwachangu. Kuchuluka kwa mankhwalawa kwa plasma kumafikira maola 1.5 atatha kukhazikitsa.

Kutsika kwa zomwe linagliptin kumachitika pamagawo awiri. Kutha kwa theka-moyo ndikutalika ndikupanga pafupifupi maola 100. Izi ndichifukwa choti mankhwalawa amapanga khola lolimba ndi enzyme DPP-4. Chifukwa chakuti kulumikizana ndi enzyme ndikusintha kwadzakenso kwa mankhwala mthupi sikumachitika.

Pankhani yogwiritsira ntchito Linagliptin pakakhala kuchuluka kwa 5 mg patsiku, nthawi imodzi yokhazikika yokhazikika yogwira mankhwala imatheka m'thupi la wodwalayo mutatenga 3 Mlingo wa mankhwalawa.

Mtheradi bioavailability wa mankhwala pafupifupi 30%. Ngati linagliptin amatengedwa nthawi yomweyo monga chakudya chamafuta, ndiye kuti chakudya chotere sichikhudza mayamwidwe anu.

Kuchotsa mankhwala m'thupi kumachitika makamaka m'matumbo. Pafupifupi 5% imachotseredwa kudzera mu imkodzo ndi impso.

Zizindikiro ndi contraindication kugwiritsa ntchito mankhwalawa

Chizindikiro chogwiritsidwa ntchito ndi linagliptin ndiko kukhalapo kwa mtundu II shuga mellitus wodwala.

Pa monotherapy, linagliptin imagwiritsidwa ntchito kwa odwala omwe sangathe kuwongolera kuchuluka kwa glycemia m'thupi kudzera pakudya ndi zolimbitsa thupi.

Kugwiritsa ntchito mankhwalawa kumalimbikitsidwa ngati wodwala wachita tsankho kapena ngati pali zotsutsana pakugwiritsa ntchito metformin chifukwa cha kulephera kwa aimpso kwa wodwala.

Mankhwala tikulimbikitsidwa othandizira awiri othandizira kuphatikiza ndi metformin, sulfonylurea zotumphukira kapena thiazolidinedione, pochitika kuti kugwiritsa ntchito mankhwala othandizira pakudya, masewera olimbitsa thupi ndi monotherapy ndi mankhwala omwe akuwonetsedwa akupezeka kuti ndi osathandiza.

Ndizomveka kugwiritsa ntchito Linagliptin monga gawo limodzi la zinthu zitatu zomwe zimapangidwira, ngati zakudya, masewera olimbitsa thupi, monotherapy kapena mankhwala othandizira awiri sizipereka zotsatira zabwino.

N`zotheka kugwiritsa ntchito mankhwalawa limodzi ndi insulin, pochita zinthu zambiri zamankhwala othandizira odwala matenda ashuga, chifukwa pamakhala kugwiritsa ntchito mankhwala olimbitsa thupi komanso osapatsa insulin yopanda mankhwala

Milandu yofunika kwambiri yogwiritsa ntchito mankhwala ndi:

• kupezeka kwa thupi la wodwala matenda a shuga 1,
• chitukuko cha matenda ashuga ketoacidosis,
• Mimba ndi kuyamwa
• Zaka za wodwalayo ndizosakwana zaka 18,
• kukhalapo kwa hypersensitivity kuti achite pa zinthu zilizonse za mankhwala.

Linagliptin sololedwa kugwiritsa ntchito panthawi ya gestation ndi mkaka wa m`mawere. Izi ndichifukwa choti chinthu chomwe chikugwirira ntchito, chikalowa m'magazi a wodwalayo, chimatha kudutsana ndi zotchinga, komanso amatha kulowa mkaka wa m'mawere nthawi ya mkaka wa m'mawere.

Ngati kuli kofunikira kugwiritsa ntchito mankhwalawa panthawi yoyamwa, kuyamwitsa kuyenera kuyimitsidwa nthawi yomweyo.

Malangizo ogwiritsira ntchito mankhwalawa

Malangizo ogwiritsira ntchito mankhwalawa akuwonetsa kuti Linagliptin amagwiritsidwa ntchito pochiza mtundu wa 2 shuga mellitus mu mlingo wa 5 mg kamodzi patsiku, ndiye piritsi limodzi. Mankhwala amatengedwa pakamwa.

Ngati mukusowa nthawi yomwe mumamwa mankhwalawa, muyenera kumwa nthawi yomweyo wodwala akakumbukira izi. Mlingo wawiri wa mankhwalawo waletsedwa.

Mukamamwa mankhwalawa, kutengera umunthu wake, zotsatira zoyipa zimachitika.

Zotsatira zoyipa zomwe zimachitika m'thupi la wodwalayo zimakhudza:

1. Chitetezo cha mthupi.
2. Ziwalo zopumira.
3. Matumbo a m'mimba.

Kuphatikiza apo, chitukuko cha matenda opatsirana mthupi, monga nasopharyngitis, ndizotheka.

Pogwiritsa ntchito Linagliptin kuphatikiza ndi Metformin, zotsatirazi zingachitike:

• mawonekedwe a hypersensitivity,
• kupezeka kwa chifuwa
• chitukuko cha kapamba
• mawonekedwe a matenda opatsirana.

Pankhani yogwiritsa ntchito mankhwalawa limodzi ndi zomwe zimachokera ku mibadwo yamakono ya sulfonylureas, ndizotheka kukulitsa zovuta zamtundu zokhudzana ndi kugwira ntchito:

1. Chitetezo cha mthupi.
2. Njira zachikhalidwe.
3. Njira yothandizira.
4. Ziwalo zam'mimba.

Pankhani yogwiritsira ntchito Linagptin kuphatikiza ndi Pioglipazone, chitukuko cha zovuta zotsatirazi tingaone:

• mawonekedwe a hypersensitivity,
• Hyperlipidemia mu shuga
• kupezeka kwa chifuwa
• kapamba
• matenda opatsirana
• kunenepa.

Pogwiritsa ntchito Linagliptin kuphatikiza ndi insulin panthawi yamankhwala, zotsatirapo zoyipa zimatha kupezeka m'thupi la wodwalayo:

1. Kukula kwa hypersensitivity m'thupi.
2. Maonekedwe akutsokomola komanso kusokonezeka kwa njira yopumira.
3. Kuchokera mu chakudya cham'mimba, mawonekedwe a kapamba ndi kudzimbidwa ndikotheka.
4. Matenda opatsirana amatha kuchitika.

Pankhani yogwiritsidwa ntchito kwa Linagliptin wa mtundu wachiwiri wa matenda a shuga a shuga kuphatikiza ndi Metformin ndi zotumphukira zochokera ku sulfonylurea, hypersensitivity, hypoglycemia, kutsokomola, zizindikiro za kapamba komanso kulemera kwa thupi kumatha kukula m'thupi.

Kuphatikiza pazotsatira zoyipa izi, mawonekedwe ndi chitukuko cha angioedema, urticaria, pancreatitis yapakhungu, zotupa pakhungu la thupi la wodwala ndizotheka.

Ngati mankhwala osokoneza bongo agwiritsidwa ntchito, njira zomwe zimagwiritsidwa ntchito pokonzera thupi ziyenera kugwiritsidwa ntchito.

Njira zoterezi ndikuchotsa mankhwalawa mthupi komanso kuchita ngati ali ndi vuto la chidziwitso.

Kugwirizana kwa linagliptin ndi mankhwala ena

Ndi makonzedwe a Metformin 850 omwe ali ndi Linagliptin, kuchepa kwakukulu kwamlingo wa shuga m'thupi la wodwalayo kumachitika.

Ma pharmacokinetics a mankhwalawa akagwiritsidwa ntchito limodzi ndi zotumphukira za m'badwo waposachedwa sizinasinthe kwenikweni.

Mukamagwiritsa ntchito mankhwala ovuta a thiazolidinediones, palibe kusintha kwakukulu mu pharmacokinetics. Izi zikusonyeza kuti linagliptin si choletsa CYP2C8.

Kugwiritsidwa ntchito kwa ritonavir mu zovuta kuchipatala sikuti kumabweretsa kusintha kwakukulu mu pharmacodynamics ndi pharmacokinetics of linagliptin.

Kugwiritsa ntchito Linagliptin mobwerezabwereza ndi Rifampicin kumayambitsa kuchepa pang'ono kwa ntchito ya mankhwala

Linagliptin amatsutsana pa matenda a matenda a shuga 1 kapena matenda a shuga a ketoacidosis.

Pafupipafupi kukula kwa chikhalidwe cha hypoglycemia m'thupi la wodwalayo panthawi ya monotherapy kumakhala kochepa.

Kuchepa kwa hyperglycemia kumawonjezereka ngati Linagliptin amagwiritsidwa ntchito molumikizana ndi mankhwala omwe amachokera ku sulfonylureas a m'badwo waposachedwa. Pazifukwa izi, chisamaliro chapadera chimayenera kutengedwa ndi chithandizo chovuta.

Ngati ndi kotheka, mlingo wa mankhwalawa womwe umayenera kutengedwa uyenera kusinthidwa kuti mupewe kukula kwa zizindikiro za hypoglycemia.

Kugwiritsidwa ntchito kwa linagliptin sikukhudzana ndi zovuta mu ntchito ya mtima.

Linagliptin angagwiritsidwe ntchito pochiza matenda a shuga kwa odwala omwe amalephera kwambiri aimpso.

Pogwiritsa ntchito Linagliptin, kuchepa kwakukulu pazomwe zili ndi glycosylated hemoglobin ndi glucose kudya.

Ngati akukayikira kukula kwa kapamba m'thupi, kugwiritsa ntchito mankhwalawa kuyenera kuyimitsidwa nthawi yomweyo.

Ndemanga za mankhwala, mawonekedwe ake komanso mtengo wake

Mankhwalawa, omwe akuphatikiza linagliptin, ali ndi dzina lazamalonda padziko lonse lapansi la Trazhenta.

Wopanga mankhwalawa ndi Beringer Ingelheim Roxane Inc., ku United States. Kuphatikiza apo, mankhwalawa amapangidwa ndi Austria. Mankhwala amaperekedwa kuchokera ku malo ogulitsa mankhwala pamaziko a mankhwala omwe adokotala amapita.

Maganizo a odwala pamankhwala ambiri amakhala abwino. Ndemanga zoyipa nthawi zambiri zimagwirizanitsidwa ndi kugwiritsa ntchito mankhwalawa ndikuphwanya malangizo ogwiritsira ntchito, omwe amayambitsa bongo kapena mawonekedwe a zovuta zina.

Mtengo wa mankhwalawo uli ndi mtengo wosiyana kutengera wopanga, wogulitsa, komanso dera lomwe mankhwalawo amagulitsidwa ku Russia.

Linagliptin 5 mg No. 30 opangidwa ndi Beringer Ingelheim Roxane Inc., USA ku Russia ali ndi mtengo wapakati m'chigawo cha 1760 rubles.

Linagliptin m'mapiritsi 5 mg phukusi la zidutswa 30 zopangidwa ku Austria ku Russian Federation ali ndi mtengo wapakati pamtunda kuchokera 1648 mpaka 1724 rubles.

Mafanizo a Trazhenta ya mankhwala, omwe ali linagliptin, ndi Januvia, Onglisa ndi Galvus. Mankhwalawa ali ndi zosakaniza zingapo zomwe zimagwira, koma momwe zimakhudzira thupi ndizofanana ndi zomwe Trazhenta amakhala nazo mthupi.

Dziwani zambiri zamankhwala a shuga omwe ali mu vidiyoyi.