Nthawi zina zakudya zopatsa thanzi komanso kuchita masewera olimbitsa thupi sizingapereke kuchuluka kwa shuga m'thupi la odwala matenda ashuga omwe ali ndi mtundu wa 2 matenda.

Thupi lomwe limakhala ndi INN Repaglinide, malangizo omwe amamangidwa phukusi lililonse la mankhwala omwe amapezeka, amakhala ndi vuto la hypoglycemic pamene sikutheka kuwongolera kuchuluka kwa shuga m'magazi. Nkhaniyi iyankha funso la momwe mungagwiritsire ntchito mankhwalawa moyenera ndikuwonetsa kuti kugwiritsidwa ntchito kwake ndikosatheka.

Pharmacological zimatha mankhwala

Chosakaniza chogwira, Repaglinide, chimapezeka mu mawonekedwe oyera a ufa kuti mugwiritse ntchito mkati. Kupanga kwa gawo la zomwe zimapangidwazo ndikumasulidwa kwa insulin (timadzi tochepetsa shuga) m'maselo a beta omwe amapezeka m'matumbo a inshuwaransi.

Pogwiritsa ntchito repaglinide pazinthu zopangira zapadera, njira zotsalira za ATP zomwe zimapezeka m'mizimba ya maselo a beta zimatsekedwa. Njira imeneyi imakwiyitsa maselo komanso kutsegulidwa kwa njira za calcium. Zotsatira zake, kupanga insulini kumachulukitsidwa ndikuwonjezera kuchuluka kwa calcium.

Wodwalayo atatenga muyezo wa Repaglinide, thunthu limalowetsedwa m'mimba. Nthawi yomweyo, ola limodzi mutatha kudya, limadziunjikira kwambiri m'madzi a m'magazi, ndiye kuti pambuyo maola 4 mtengo wake umatsika mofulumira ndikutsika kwambiri. Kafukufuku wa mankhwalawa adawonetsa kuti palibe kusiyana kwakukulu pama mfundo a pharmacokinetic mukamagwiritsa ntchito Repaglinide musanadye kapena nthawi ya chakudya.

Thupi limagwirira kumapuloteni a plasma oposa 90%. Komanso, phindu lokwanira la bioavailability limafika pa 63%, ndipo voliyumu yake yogawa ndi malita 30. Ndi chiwindi chomwe biotransformation ya Repaglinide imachitika, chifukwa chomwe metabolites ofooka amapangika. Kwenikweni, amawachotsa ndi bile, komanso mkodzo (8%) ndi ndowe (1%).

Mphindi 30 mutatha kudya Repaglinide, kutulutsidwa kwa mahomoni kumayamba. Zotsatira zake, kuchuluka kwa shuga m'magazi kumachepetsedwa mwachangu. Pakati pa chakudya, palibe kuchuluka kwa insulin.

Odwala omwe ali ndi shuga omwe amadalira insulin omwe samatenga 0,5 mpaka 4 g wa Repaglinide, kuchepa kwa shuga kumawonedwa.

Malangizo ogwiritsira ntchito mankhwalawa

Repaglinide ndiye gawo lalikulu la NovoNorm, lomwe limapangidwa ku Denmark. Makampani opanga mankhwala a Novo Nordisk A / C amapanga mankhwala mwanjira ya mapiritsi okhala ndi mitundu yosiyanasiyana - 0,5, 1 ndi 2 mg. Chithuza chimodzi chimakhala ndi mapiritsi 15, m'thumba limodzi matuza angapo akhoza kupezeka.

Mu phukusi lirilonse la mankhwala omwe ali ndi zigawo zina repaglinide, malangizo ogwiritsira ntchito ndi omwe ayenera kuvomerezedwa. Mlingo umasankhidwa ndi katswiri aliyense payekha yemwe amawunika kuchuluka kwa shuga ndi zomwe zimagwirizanitsidwa ndi odwala. Asanagwiritse ntchito mankhwalawa, wodwalayo ayenera kuwerenga mosamala malangizo omwe aphatikizidwa.

Mlingo woyambirira ndi 0.5 mg, umatha kuwonjezeka pokhapokha sabata limodzi kapena awiri, kudutsa mayeso a labotale kwa kuchuluka kwa shuga. Mlingo umodzi waukulu kwambiri ndi 4 mg, ndipo mlingo wa tsiku ndi tsiku ndi 16 mg. Munthawi ya kusintha kwa mankhwala omwe amachepetsa shuga Repaglinide imwani 1 mg. Muyenera kugwiritsa ntchito mankhwalawa kwa mphindi 15-30 musanadye kaye.

Mankhwala a NovoNorm ayenera kusungidwa kutali ndi ana ang'ono pamtunda wa 15-25C pamalo otetezedwa ndi chinyezi.

Alumali moyo wa mankhwalawa wafika zaka 5, pambuyo pa nthawi imeneyi ndizosatheka kuzigwiritsa ntchito mulimonse.

Contraindication ndi zomwe zingavulaze

Tsoka ilo, si aliyense amene angavomereze NovoNorm. Monga mankhwala ena, ali ndi zotsutsana.

The repaglinide ya mankhwala silingatengedwe ndi:

1. mtundu wa shuga wodalira insulin
2. matenda ashuga ketoacidosis, kuphatikizapo chikomokere,
3. chiwindi chachikulu ndi / kapena kukanika kwa impso,
4. kugwiritsa ntchito mankhwala owonjezera omwe amalepheretsa CYP3A4,
5. lactose tsankho, kufupika kwa lactase ndi malisorption wa glucose-galactose,
6. kuchuluka kwa chipangizocho,
7. wosakwana zaka 18
8. Kukonzekera kapena kukhala ndi pakati,
9. yoyamwitsa.

Kafukufuku wopangidwa pa makoswe adatsimikizira kuti kugwiritsa ntchito kwa repaglinide panthawi yomwe mwana akubala mwana kumakhudza mwana wosabadwayo. Chifukwa cha kuledzera, kukula kwa malekezero akumtunda ndi otsika kwa mwana wosabadwayo kunali kovuta. Komanso, kugwiritsa ntchito chinthucho ndikuloledwa pa mkaka wa m'mawere, popeza umaperekedwa mkaka wa mayi kupita kwa mwana.

Nthawi zina kugwiritsa ntchito molakwika mankhwala kapena mankhwala osokoneza bongo, maonekedwe a zoyipa monga:

• hypoglycemia (kutuluka thukuta kwambiri, kunjenjemera, kugona tulo, tachycardia, nkhawa),
• kuwonongeka kwa zida zowonekera (poyamba, kumwa mankhwalawo, kenako ndikudutsa),
• kupukusa m'mimba (kupweteka kwam'mimba, kusanza ndi kusanza, kudzimbidwa kapena kutsegula m'mimba, kuchuluka kwa michere mu chiwindi),
• ziwengo (redness of the khungu - erythema, zidzolo, kuyabwa).

Kugwiritsa ntchito kuchuluka kwa mankhwalawa kuposa momwe dokotala ananenera pafupifupi nthawi zonse kumayambitsa hypoglycemia. Ngati munthu wodwala matenda ashuga akumva mankhwala osokoneza bongo ndipo amadziwa, ayenera kudya zakudya zopatsa mphamvu ndipo amakaonana ndi dotolo kuti amuthandize.

Mu hypoglycemia yayikulu, wodwala akakhala kuti ali ndi vuto lofooka kapena osazindikira, amapaka jekeseni wa 50% shuga pansi pa khungu ndikuwonjezeranso kulowetsedwa kwa 10% yothetsera kukhalabe ndi shuga osachepera 5.5 mmol / L.

Kuchita kwa Repaglinide ndi Mankhwala Ena

Kugwiritsa ntchito mankhwala ophatikizira nthawi zambiri kumakhudza mphamvu ya kuyambiranso kwa ndende ya glucose.

Mphamvu yake ya hypoglycemic imakonzanso pamene wodwala atenga ma MAO ndi ACE zoletsa, osagwiritsa ntchito beta-blockers, mankhwala osagwiritsa ntchito steroidal odana ndi kutupa, salicylates, anabolic steroids, okreotide, mankhwala okhala ndi ethanol.

Mankhwala otsatirawa amawononga mphamvu ya chinthu chochepetsa shuga:

• thiazide okodzeya,
• njira zakulera zothandizira pakamwa,
• danazol
• glucocorticoids,
• mahomoni a chithokomiro,
• amphanomachul.

Komanso, wodwalayo ayenera kuganizira kuti repaglinide imalumikizana ndi mankhwala omwe amachotsedwa mu ndulu. CYP3A4 inhibitors monga intraconazole, ketoconazole, fluconazole ndipo ena ena amatha kukulitsa magazi. Kugwiritsa ntchito kwa CYP3A4 inducers, makamaka rifampicin ndi phenytoin, kumatsitsa mulingo wa chinthu cham'magazi. Popeza kuti mulingo wazolowera sunatsimikizidwe, kugwiritsa ntchito Repaglinide ndi mankhwalawa ndizoletsedwa.

Repaglinide

Repaglinide
Pake wa mankhwala
IUPAC	(S) - (+) - 2-ethoxy-4-2- (3-methyl-1-2- (piperidin-1-yl) phenylbutylamino) -2-oxoethylbenzoic acid
Choyimira chokha	C27H36N2O4
Unyinji wa Molar	452.586 g / mol
Cas	135062-02-1
PubChem	65981
Drugbank	DB00912
Gulu
ATX	A10BX02
Pharmacokinetics
Bioava	56% (pakamwa)
Kumanga Mapuloteni a Plasma	>98%
Kupenda	Hepatic oxidation ndi glucuronidation (CYP3A4-mediated)
Hafu ya moyo.	Ola limodzi
Kupatula	Fecal (90%) ndi impso (8%)
Njira zoyendetsera
Pakamwa
Wikimedia Commons Media Mafayilo

Repaglinide - mankhwala osokoneza bongo, adapangidwa mu 1983. Repaglinide ndi mankhwala amkamwa omwe amagwiritsidwa ntchito kuwonjezera pa zakudya komanso masewera olimbitsa thupi kuti azilamulira shuga m'magazi a shuga a 2. Makina a Repaglinide akuwonetsa kuwonjezera kutulutsa kwa insulini kuchokera ku β-maselo a cell a kapamba, monga mankhwala ena othandizira odwala matenda ashuga, mbali yayikulu ndi hypoglycemia. Mankhwalawa amagulitsidwa ndi Novo Nordisk pansi pa dzinali Prandin ku USA Glucoorm ku Canada Surpost ku Japan Repaglinide kupita ku Egypt ndi Ifi, ndipo NovoNorm m'malo ena. Ku Japan, amapangidwa ndi Dainippon Sumitomo Pharma.

Katundu Wanzeru

Repaglinide ndi mankhwala amkamwa omwe amagwiritsidwa ntchito kuwonjezera pa zakudya komanso masewera olimbitsa thupi kuti azilamulira shuga m'magazi a shuga a 2.

Contraindication

Repaglinide imalembedwa mwa anthu ndi:

1. Matenda a shuga ketoacidosis
2. Mtundu woyamba wa shuga
3. Ntchito zogwirizana ndi gemfibrozil
4. Hypersensitivity kwa mankhwala osokoneza bongo kapena osagwira ntchito

Zotsatira zoyipa

Zotsatira zoyipazi zimapezeka:

• Matenda opumira kwambiri pamatumbo (16%)
• Sinusitis (6%)
• Rhinitis (3%)

Zotsatira zoyipazi zimaphatikizapo:

• Myocardial ischemia (2%)
• Angina pectoris (1.8%)
• Imfa chifukwa cha zochitika zamtima (0.5%)

Kwa anthu apadera

Gawo la Mimba C: Chitetezo kwa amayi apakati sichinakhazikitsidwe. Zambiri ndizochepa, ndipo pali mlandu umodzi wokha, lipotilo likuti palibe zovuta zomwe zimagwiritsidwa ntchito pakuyambiranso nthawi ya bere.

Chenjezo liyenera kuchitidwa ndi anthu omwe ali ndi matenda a chiwindi ndikuchepetsa ntchito ya impso pogwiritsa ntchito mankhwalawa.

Kuyanjana kwa mankhwala osokoneza bongo

Repaglinide ndiye gawo lalikulu la SUR3A4 ndipo siliyenera kutumikiridwa nthawi imodzi ndi gemfibrozil, clarithromycin, kapena azole antifungal mankhwala monga Itraconazole ndi Ketoconazole. Kutenga repaglinide limodzi ndi amodzi kapena angapo mwa mankhwalawa kumabweretsa kuwonjezeka kwa plasma repaglinide moyikirapo ndipo kungayambitse hypoglycemia. Kugwirizana kwa clopidogrel ndi repaglinide (ndi cyp2c8 inhibitor) kungayambitse kuchepa kwakukulu kwa shuga m'magazi chifukwa chogwiritsa ntchito mankhwala. M'malo mwake, kugwiritsa ntchito mankhwalawa pamodzi kwa tsiku limodzi kungachititse kuti mukhale ndi hypoglycemia. Repaglinide sayenera kumwedwa limodzi ndi sulfonylurea, chifukwa ali ndi magwiritsidwe ofanana.

Njira yamachitidwe

Repaglinide imatsitsa shuga m'magazi polimbikitsa kutulutsa kwa insulini kuchokera ku maselo a beta a pancreatic islet. Izi zimatheka potseka njira zotsalira za potaziyamu ya ATP mu nembanemba yama cell a beta. Izi zimanyoza maselo a beta, ndikutsegulira ma cell a calcium cell, ndipo chifukwa chake, kuchuluka kwa calcium kumapangitsa insulin kutulutsa.

Pharmacokinetics

Mafuta: Repaglinide imakhala ndi kukhudzana kwa magawo 56% mukamamwa kuchokera m'matumbo am'mimba. Bioavailability yafupika mukamadyedwa ndi chakudya, kuchuluka kwambiri kumachepetsedwa ndi 20%.

Kugawa: Kumanga mapuloteni omwe amachititsa repalglinide ku albumin ndi oposa 98%.

Metabolism: Repaglinide imapangidwa makamaka mu chiwindi, makamaka CYP450 2C8 ndi 3A4 komanso pang'ono pang'onopang'ono kudzera mu glucuronidation. Repaglinide metabolites ndi yopanda ntchito ndipo sisonyeza zotsatira zotsitsa shuga.

Chotsekera: Repaglinide ndi 90% yowonjezera mu ndowe ndi 8% mkodzo. 0.1% imachotsedwa ndi mkodzo osasinthika. Zochepera 2% zosasinthika mu ndowe.

Nkhani

Kutsogolo kwa Repaglinide anapangidwa kumapeto kwa 1983 ku Bieberrach ku Rice kumwera kwa Germany.

Katundu Wanzeru

Ku United States, kutetezedwa ndi Patent, kulembetsa kunachitika mu Marichi 1990, komwe patapita nthawi kunakhala patent ya US 5,216,167 (Juni 1993), 5,312,924 (Meyi 1994) ndi 6,143,769 (Novembara 2000). Pambuyo

Malangizo ogwiritsira ntchito

Nthawi zina, odwala ayenera kugwiritsa ntchito mankhwalawa mosamala kwambiri moyang'aniridwa ndi dokotala yemwe amapereka mankhwala ochepera. Odwala oterewa amaphatikizapo odwala omwe ali ndi matenda a chiwindi ndi / kapena impso, omwe adachitapo kanthu opaleshoni yayikulu, omwe adangokhala ndi kachilombo kapena matenda opatsirana, okalamba (kuyambira wazaka 60) omwe amatsata zakudya zama calorie otsika.

Ngati wodwala ali ndi mtundu wa hypoglycemic wofatsa kapena wowonda, amatha kuthetsedwa payokha. Kuti muchite izi, muyenera kudya zakudya zokhala ndi zopatsa mphamvu mosavuta - chidutswa cha shuga, maswiti, msuzi wokoma kapena zipatso. Mwa mawonekedwe owopsa ndi kutaya chikumbumtima, monga tanena kale, yankho la shuga limayendetsedwa kudzera m'mitsempha.

Tiyenera kudziwa kuti beta-blockers amatha kuphimba zizindikiro zomwe zikubwera za hypoglycemia. Madokotala amalimbikitsa kwambiri kupewa kumwa mowa monga Mowa umapitilira ndipo umapitiliza ndi Hypoglycemic zotsatira za Repaglinide.

Komanso, zinthu zimachepetsa chidwi cha anthu.

Chifukwa chake, oyendetsa moyang'anizana ndi maziko ogwiritsira ntchito repaglinide, ndikofunikira kukana kuyendetsa magalimoto kapena kugwira ntchito zina zoopsa panthawi yamankhwala.

Mtengo, ndemanga ndi fanizo

Repaglinide monga gawo lalikulu limagwiritsidwa ntchito mu mankhwala a NovoNorm.

Itha kugulidwa ku malo ogulitsa mankhwala kapena kuyitanitsa pa intaneti patsamba laogulitsa. Komabe, kugula kwa mankhwalawo kumatheka pokhapokha ngati wapezeka ndi udokotala.

Mtengo wamankhwala umasiyanasiyana:

• Mapiritsi 1 mg (zidutswa 30 pa paketi) - kuchokera ku 148 mpaka 167 ma ruble aku Russia,
• Mapiritsi a 2 mg (zidutswa 30 pa paketi) - kuchokera ku 184 mpaka 254 ma ruble aku Russia.

Monga mukuwonera, mitengo ndiyodalirika kwambiri kwa anthu omwe ali ndi ndalama zochepa. Kuwerenga ndemanga za anthu ambiri omwe ali ndi matenda ashuga, titha kudziwa kuti mtengo wotsika wa mankhwalawa ndiwowonjezera bwino, chifukwa chogwira ntchito. Kuphatikiza apo, zabwino za NovoNorm ndi:

• kugwiritsa ntchito bwino mapiritsi poyerekeza ndi jakisoni,
• kuthamanga kwa mankhwalawa, ola limodzi lokha,
• Kutenga nthawi yayitali kumwa mankhwalawa.

Mfundo yomalizayi ikutanthauza kuti odwala ambiri omwe amapezeka ndi matenda osokoneza bongo omwe amadalira insulin akhala akutenga NovoNorm kwa zaka 5 kapena kuposerapo. Amazindikira kuti machitidwe ake amakhalabe ofanana ndipo samazirala. Komabe, kuchuluka kwa mankhwalawa kwa mankhwalawa kumachepetsedwa mpaka zero: OSATI:

1. kutsatira zakudya zabwino (kupatula chakudya chambiri cham'mimba ndi mafuta),
2. khalani ndi moyo wokangalika (kuyenda kwa mphindi 30, zolimbitsa thupi, ndi zina),
3. Nthawi zonse muziyang'anira kuchuluka kwa shuga (pafupifupi katatu patsiku).

Mwambiri, odwala ndi madokotala amawona kuti NovoNorm ndi antipyretic wabwino kwambiri. Koma nthawi zina kugwiritsa ntchito mapiritsi kumaletsedwa, chifukwa zimabweretsa zotsatira zosayenera. Zikatero, adotolo amasankha kusintha mlingo wa mankhwalawo kapena kupereka mankhwala osiyana ndi ena onse.

Ma Synonyms ali ndi zomwe zimagwira ndipo zimangosiyana pazowonjezera zina. Mapiritsi a NovoNorm ali ndi vuto limodzi - Diagniniside (avareji ma ruble 278).

Mankhwala ofanana a NovoNorm, omwe ali osiyana m'magawo awo, koma ali ndi zofanana, ndi awa:

• Jardins (mtengo wapakatikati - ma ruble 930),
• Victoza (mtengo wapakatikati - ma ruble 930),
• Saksenda (mtengo wapakatikati - ma ruble 930),
• Forsyga (mtengo wapakatikati - ma ruble 2600),
• Attokana (mtengo wapakatikati - ma ruble 1630).

Titha kudziwa kuti mankhwalawa NovoNorm, omwe ali ndi yogwira pophika, amagwira ntchito pochiza matenda amtundu wa 2 shuga. Amachepetsa msanga shuga kukhala milingo yabwinobwino. Ngati mutsatira zakudya, kuchita masewera olimbitsa thupi komanso kuwunika pafupipafupi kuchuluka kwa shuga, mutha kuthana ndi hypoglycemia ndi zizindikiro zazikulu za matenda ashuga. Kanema yemwe ali munkhaniyi akufotokozerani momwe mungachiritsire matenda ashuga.