Repaglinide: ịta ọgwụ n'ọbara
Mgbe ụfọdụ nri nri pụrụ iche na mmega ahụ enweghị ike iwepụta ọkwa glucose nkịtị na ọrịa mamịrị nwere ụdị ọrịa abụọ.
Ihe nwere INN Repaglinide, nkuzi nke ejikọtara na ngwungwu ọgwụ ọ bụla nwere ya, nwere mmetụta hypoglycemic mgbe ọ gaghị ekwe omume ịchịkwa ịta shuga n'ọbara. Isiokwu a ga-aza ajụjụ banyere otu esi eji ọgwụ ahụ ọgwụ ọgwụ repaglinide mee ihe n'ụzọ ziri ezi ma n'ọnọdụ ya iji ọgwụ agaghị ekwe omume.
Ngwá ọgwụ ọgwụ
Ngwakọta ọrụ nọ n'ọrụ, Repaglinide, dị n'ụdị ntụ ntụ ọcha maka ojiji maka ime. Usoro nke ihe mejupụtara ya bụ mwepụta nke insulin (hormone na-ebelata shuga) site na sel beta nke dị na akwara.
Iji repaglinide na ndị na-anabata ndị pụrụ iche, a na-egbochi mkpọchi ATP nke dị na membranes nke mkpụrụ ndụ beta. Usoro a na - akpachasị nbibi nke sel yana imepe oghere nke akụrụ. N'ihi ya, a na-amụba ọgwụ insulin site na ịbawanye ụba nke calcium.
Mgbe onye ọrịa ahụ aụsịrị ọgwụ ọgwụ Repaglinide, a na-etinye ihe ahụ n'ime ngọngọ nri. N'otu oge, mgbe elekere 1 gachara nri, ọ na-agbakarị na plasma ọbara, emesia mgbe awa anọ gasịrị, uru ya ga-agbada ngwa ngwa wee belata nke ukwuu. Ihe omumu banyere ogwu a gosiputara na odighi iche di iche na ụkpụrụ nke pharmacokinetic mgbe ị na-eji Repaglinide tupu ma ọ bụ n'oge nri ahụghị.
Ihe a na - ejikọ ndị na - egbochi plasma protein karịa 90%. Na mgbakwunye, bioavailability zuru oke ruru 63%, olu nkesa ya bụ lita 30. Ọ bụ n'ime imeju ka biotransformation nke Repaglinide pụtara, n'ihi nke etolite metabolites na-adịghị arụ ọrụ. N'ụzọ bụ isi, ha na-abụkarị mmiri ara ehi, yana mmamịrị (8%) na feces (1%).
Nkeji 30 ka iri riri Repaglinide, mmiri ọgwụ hormone na-amalite. N'ihi nke a, a na-ebelata mkpụkọ glucose na ọbara ngwa ngwa. N’etiti nri, ọnụọgụ insulin adịghị aba ụba.
N'ime ndị ọrịa nwere ọrịa shuga na-enweghị insulin nke na-a fromụ site na 0,5 ruo 4 g nke Repaglinide, a na-ahụta mbelata glucose na-adabere na glucose.
Ntuziaka maka iji ọgwụ ahụ
Repaglinide bụ akụkụ bụ isi nke NovoNorm, nke a na-emepụta na Denmark. Companylọ ọrụ ọgwụ na Novo Nordisk A / C na-emepụta ọgwụ n'ụdị mbadamba ọgwụ nwere usoro dị iche iche - 0,5, 1 na 2 mg. Otu ọnya nwere 15 mbadamba, na otu ngwugwu ọtụtụ blisters nwere ike ịdị.
Na ngwungwu ọgwụ ọ bụla yana ọgwụ mejupụtara, ntuziaka maka ojiji bụ iwu. A na-ahọpụta dos site n'aka ndị ọkachamara n'otu n'otu nke na-enyocha ọkwa shuga na ọrịa ndị metụtara ya. Tupu ị theụ ọgwụ ahụ, onye ọrịa ahụ kwesịrị iji nlezianya gụọ ntuziaka agbakwunyere.
Usoro mbụ bụ 0,5 mg, enwere ike ịba ụba naanị mgbe otu izu ma ọ bụ abụọ gasịrị, na-agafe ule ụlọ nyocha maka ọkwa shuga. Usoro onunu ogwu buru ibu bu 4 mg, kwa ubochi obula bu 16 mg. N'oge mgbanwe site na ọgwụ ọzọ na-ebelata shuga Repaglinide were 1 mg. Ọ bụ ihe amamihe dị na ya iji ọgwụ ahụ ruo minit 15-30 tupu isi nri.
Ekwesịrị ịchekwa ọgwụ NovoNorm site na obere ụmụaka na ikuku ikuku nke 15-25C n'ebe a na-echebe mmiri.
Ndụ nchekwa nke ọgwụ ahụ dị afọ 5, mgbe oge a ọ gaghị ekwe omume iji ya n'ọnọdụ ọ bụla.
Ntuchi ogwu na ihe ojoo
Ọ bụ ihe nwute, ọ bụghị mmadụ niile nwere ike ịnabata NovoNorm. Dị ka ọgwụ ọjọọ ndị ọzọ, ọ nwere contraindications.
Enweghi ike iburu ihe eji eregharia ya:
- Ọrịa shuga na-akpata insulin
- ọrịa mamịrị ketoacidosis, gụnyere coma,
- umeji na / ma ọ bụ akụrụ
- ọzọ iji ọgwụ ọjọọ eme ihe ma ọ bụ na-egbochi CYP3A4,
- lactose anabataghị, ụkọ lactase na glucose-galactose malabsorption,
- nwere ike ịbawanye n'ihe ahụ,
- n'okpuru afọ 18
- emebere ma ọ bụ ịtụrụ ime,
- inye ara.
Nnyocha ndị a mere na ụmụ oke gosipụtara na iji nke repaglinide n'oge ịmụrụ nwa na-emetụta nwa ebu n'afọ n'ụzọ ọjọọ. N’ihi ịxụbiga mmanya ókè, mmepe nke akụkụ aka nwa na nke ala nwa ebu n'afọ na-emebi emebi. Ọzọkwa, a machibidoro iji ihe ahụ eme ihe n'oge a na-enye ya ara, ebe ọ bụ na -eme ya na mmiri ara nne nye nwa.
Mgbe ụfọdụ iji ọgwụ ọjọọ eme ihe ma ọ bụ ị anụbiga mmanya ókè, ọdịdị nke mmeghachi omume ọjọọ dịka:
- hypoglycemia (mmiri ọsụsọ mụbara, ịma jijiji, ụra na-adịghị mma, tachycardia, nchegbu),
- mmebi nke ngwa a na-ahụ anya (na mbụ, na-a theụ ọgwụ, wee gafee),
- nri digestive (afọ mgbu, ọgbụgbọ na ọgbụgbọ, afọ ntachi ma ọ bụ afọ ọsịsa, ụba ọrụ enzymes na imeju),
- nke ahu anataghi (akpukpo aru nke akpukpo aru - akpukpo ahu, ihe odida, itching).
Ojiji nke oke ọgwụ ahụ karịa dọkịta kwuru na ọ fọrọ nke nta ka ọ bụrụ kpatara hypoglycemia. Ọ bụrụ na onye ọrịa mamịrị na-arịa ọrịa shuga dị obere ma mara ihe, ọ ga-eri nri bara ụba nke carbohydrate, ma gakwuru dọkịta banyere ime mgbanwe iji usoro onunu ogwu.
Na nnukwu hypoglycemia, mgbe onye ọrịa nọ na nkụ ma ọ bụ na ọ maghị, a ga-eji ọgwụ glucose 50% gbanye n’ahụ ya na ntinye nke 10% iji wee nwee ọkwa shuga dịkarịa ala 5.5 mmol / L.
Mmekọrịta nke Repaglinide na ọgwụ ndị ọzọ
Ojiji nke ọgwụ oriri na-emetụta na-emetụta arụmọrụ nke repaglinide na ịta glucose.
A na-eme ka mmetụta hypoglycemic dịkwuo elu mgbe onye ọrịa na-ewere MAO na ndị na-egbochi ACE, ndị na-abụghị steroidal anti-inflammatory ọgwụ, salicylates, steroid anabolic, okreotide, ọgwụ nwere ethanol.
Ọgwụ ndị a na-emetụta ike nke ihe iji belata glucose:
- thiazide diuretics,
- ogwu mgbochi diri onu eji eme ya.
- danazol
- glucocorticoids,
- homonụ thyroid,
- nnabata ọmiko.
Ọzọkwa, onye ọrịa ahụ kwesịrị iburu n'uche na ọgwụ ezumike na-emekọ ọgwụ ọnụ nke ewepụrụ na bile. Ndị na - egbochi CYP3A4 dị ka intraconazole, ketoconazole, fluconazole na ụfọdụ ndị ọzọ nwere ike ịbawanye ọkwa ọbara ya. Ojiji ndị mmadụ ji eme ihe CYP3A4, ọkachasị na rifampicin na phenytoin, na-ebelata ọkwa nke ihe dị na plasma. N'iburu n'uche na ekwesighi ogo nke induction, a machibidoro iji ọgwụ Repaglinide na ọgwụ ndị dị otú ahụ.
Na-atụgharị
Na-atụgharị | |
---|---|
Chemical kemịkalụ | |
IUPAC | (S) - (+) - 2-ethoxy-4-2- (3-methyl-1-2- (piperidin-1-yl) phenylbutylamino) -2-oxoethylbenzoic acid |
Usoro usoro | C27H36Nd2O4 |
Oke molar | 452.586 g / mol |
Akwa | 135062-02-1 |
PubChem | 65981 |
Ogwu | DB00912 |
Nkewa | |
ATX | A10BX02 |
Mlọ ọgwụ | |
Bioa no | 56% (onu) |
Ihe Platoma Platinma | >98% |
Metabolism | Ọrịa ịba ọcha n'anya na glucuronidation (CYP3A4-onye ogbugbo) |
Nkeji ọkara ndụ. | 1 awa |
Iwepụ | Fecal (90%) na renal (8%) |
Ofzọ nlekọta | |
Ire | |
Wikimedia Commons Media |
Na-atụgharị - ọgwụ antidiabetic, mepụtara na 1983. Repaglinide bụ ọgwụ eji eme ọnụ na mgbakwunye na nri na mmega iji chịkwaa ọbara shuga n'ụdị shuga 2. Usoro nke Repaglinide na-atụ aro ịbawanye na ịhapụ insulin site na sel β-islet nke pancreas, dị ka ọgwụ ndị ọzọ antidiabetic, isi mmetụta dị na ya bụ hypoglycemia. Ndi Novo Nordisk na-ere ọgwụ ahụ n’aha Prandin na USA Glucoorm na Kanada Postlọ nyocha na Japan Na-atụgharị bịarute Ijipt site na Ifi, na NovoNorm n’ebe ozo. Na Japan, Dainippon Sumitomo Pharma na-emepụta ya.
Ngwongwo nke ọgụgụ isi
Repaglinide bụ ọgwụ eji eme ọnụ na mgbakwunye na nri na mmega iji chịkwaa ọbara shuga n'ụdị shuga 2.
Ihe ngbanwe
A na - emegharia Reaglinide n'ime ndi mmadu:
- Ọrịa mamịrị ketoacidosis
- Ọrịa shuga 1dị 1
- Ojiji ajuju a na gemfibrozil
- Akpachapụ anya na ọgwụ ma ọ bụ ihe ndị ọzọ anaghị arụ ọrụ
Nsonaazụ
Nsonaazụ ndị a na-esokarị gụnyere:
- Nnukwu akụkụ okuku ume na ọrịa ọrịa (16%)
- Sinusitis (6%)
- Rhinitis (3%)
Ọnọdụ ndị dị egwu gụnyere:
- Ischemia Myocardial (2%)
- Angina pectoris (1.8%)
- Ọnwụ n'ihi ọrịa obi (0,5%)
Maka onu ogugu ndi puru iche
Udi ime C: Edebebeghị nchekwa maka ụmụ nwanyị dị ime. Ihe data a nwere oke, na enwere otu ikpe, akụkọ ahụ kwuru na enweghị nsogbu ọ bụla gbasara iji repaglinide n'oge afọ ime ahụ.
Ekwesịrị ịkpachara anya na ndị nwere ọrịa imeju ma belata ọrụ akụrụ mgbe ị na-eji ọgwụ a.
Mkparịta ụka ọgwụ ọjọọ
Repaglinide bụ mkpụrụ nke SUR3A4 ma ekwesighi ịkọ ya n'otu oge yana gemfibrozil, clarithromycin, ma ọ bụ ọgwụ antizoungal dịka Itraconazole na Ketoconazole. Repnweta ọgwụ mgbochi na otu ma ọ bụ karịa nke ọgwụ ndị a na-eduga n'ịbawanye ụba nke plasma repaglinide ma nwee ike iduga hypoglycemia. Nchịkọta nke clopidogrel na repaglinide (yana cyp2c8 inhibitor) nwere ike ibute mbelata nke ọma na ọkwa glucose ọbara n'ihi mmekọrịta dị n'etiti ọgwụ. n'eziokwu, iji ọgwụ ndị a ọnụ ma ọ dịkarịa ala otu ụbọchị nwere ike ibute nnukwu hypoglycemia. Ekwesighi iweghachite Reaglinide na sulfonylurea, nihi na ha nwere otu usoro mmeghari.
Usoro nke ime ihe
Repaglinide na-ebelata glucose ọbara site na-akpali mwepụta nke insulin site na sel beta nke palọg ahụ. A na - emezu nke a site na imechi oghere ndị potassium na ATP na akpụkpọ ahụ nke mkpụrụ ndụ beta. Nke a na - ekpochapụ sel nke beta, na - emepe ọwa kalsel cellular, yana nke a, nnubata nke calcium na - eme ka mmiri ọgwụ insulin nwee ike.
Mlọ ọgwụ
Mbepu: Repaglinide nwere bioav adị 56% mgbe a na-etinye ya na ngụgụ eriri afọ. A na - ebelata bioavailability mgbe a na - eji nri, a na - ebelata oke ị ga - ebelata 20%.
Ihe nkesa: protein protein of repalglinide na albumin karịrị 98%.
Metabolism: Repaglinide bụ metabolized nke ukwu na imeju, ọkachasị CYP450 2C8 na 3A4 yana ruo ntakịrị karịa site na glucuronidation. Metabolites Repaglinide adịghị arụ ọrụ ma anaghị egosipụta mmetụta belata shuga.
Mgbapụta: Repaglinide bụ 90% nwere ahụ ụkwara ahụ na 8% na mmamịrị. 0.1% wepu na mmamiri agbanweghi. Erughị 2% agbanweghị na feces.
Akụkọ
E mepụtara ụzọ ndị echegharịrị na njedebe 1983 na Bieberrach na Rice n'ebe ndịda Germany.
Ngwongwo nke ọgụgụ isi
Na United States, nke Patent na-echebe, emere ka ndebanye aha ya na March 1990, nke mechara bụrụ ihe nchịkwa US 5,216,167 (June 1993), 5,312,924 (Mee 1994) na 6,143,769 (November 2000). Emechaa
Ndụmọdụ maka iji ya
N'ọnọdụ ụfọdụ, ndị ọrịa kwesịrị iji ọgwụ kpachara anya nke ukwuu n'okpuru nlekọta nke dọkịta nke depụtara obere ọgwụ ahụ. Ndị ọrịa dị otú a gụnyere ndị ọrịa na-ata ahụhụ site na ọrịa imeju na / ma ọ bụ akụrụ, bụ ndị merela ọtụtụ usoro ịwa ahụ, ndị nwere ọrịa nje na nso nso a, ndị agadi (site na 60 afọ) ndị na-agbaso nri kalori dị ala.
Ọ bụrụ na onye ọrịa nwere ọnọdụ hypoglycemic n'ụdị dị nro ma ọ bụ na-agafeghị oke, enwere ike iwepu ya n'adabereghị. Iji mee nke a, ịkwesịrị iri nri nwere carbohydrates na-adị ngwa ngwa - ntakịrị shuga, swiiti, ihe ọ juiceụ sweetụ ọma ma ọ bụ mkpụrụ osisi. N'ụdị dị ukwuu na enweghị mmụọ, dị ka anyị kwurula, a na-edozi glucose na-apụtaghị ìhè.
Okwesiri iburu n'uche na ihe mgbochi beta na - enwe ike ikpuchi ihe ngosiputa nke hypoglycemia. Ndị dọkịta kwusiri ike izere ị drinkingụ mmanya ka ethanol na-abawanye ma na-aga n'ihu na hypoglycemic mmetụta nke Repaglinide.
Ọzọkwa, ihe ahụ na-ebelata itinye uche.
Ya mere, ndị ọkwọ ụgbọala megidere ndabere nke iji repaglinide, ọ dị mkpa ịkwụsị ịkwọ ụgbọala ma ọ bụ ịrụ ọrụ ndị ọzọ dị ize ndụ n'oge ọgwụgwọ.
Efu, nyocha na analogues
A na-ejikwa Repaglinide dị ka ihe bụ isi ahụ na ọgwụ NovoNorm.
Enwere ike ịzụta ya na ahịa ọgwụ ma ọ bụ nye iwu n'ịntanetị na weebụsaịtị nke onye na-ere ere. Agbanyeghị, ịzụrụ ọgwụ ahụ ga - ekwe omume naanị mgbe ngosipụta ọgwụ dọkịta.
Ọnụ ego ọgwụ ọjọọ ahụ dịgasị:
- Mpempe mkpụrụ 1 mg (mkpụrụ 30 n'ime otu) - site na 148 ruo 167 rubles,
- Mbadamba mbadamba 2 (mkpụrụ iri atọ n'otu mkpọ) - site na 184 ruo 254 rubles Russia.
Dị ka ị pụrụ ịhụ, ịnye ọnụahịa na-akwụsi ike n'akụkụ ndị nwere obere ego. N'ịgụ nyocha nke ọtụtụ ndị ọrịa mamịrị, enwere ike iburu n'uche na ọnụ ala ọgwụ ahụ buru ibu gbakwunyere, nyere ya ike. Na mgbakwunye, uru nke NovoNorm bụ:
- Ojiji e jiri mbadamba ụrọ tụnyere inje,
- Ọsọ ọgwụ ahụ, naanị otu elekere,
- ogologo oge ị theụ ọgwụ.
Isi okwu ikpeazụ pụtara na ọtụtụ ndị ọrịa chọpụtara ọrịa shuga na-enweghị insulin na-ewere NovoNorm kemgbe afọ ise ma ọ bụ karịa. Ha na-ahụta na ihe ọ mere na-abụ otu ihe ahụ ma ọ dịghị ebelata. Agbanyeghị, mmetụta hypoglycemic nke ọgwụ ahụ na-ebelata ma ọ bụrụ na B :GH::
- rube isi na nri kwesiri ekwesi (mwepu nke carbohydrates na abụba di mfe).
- Leruo anya maka ndu ndu (ije ije ma obu opekata mpe nkeji iri atọ, ihe eji eme aru, wdg),
- na-enyocha ọkwa nke glucose mgbe niile (ọbụlagodi ugboro atọ n'ụbọchị).
Na mkpokọta, ndị ọrịa na ndị dọkịta na-ewere NovoNorm dị ka ọgwụ antipyretic dị mma. Ma mgbe ụfọdụ amachibidoro iji mbadamba ụrọ, ebe ha na-eduga na nsonaazụ na-adịghị mma. N'ọnọdụ ndị dị otú a, dọkịta kpebiri ịgbanwe ọgwụ nke ọgwụ ahụ ma ọ bụ depụta ọgwụ dị iche kpamkpam.
Mmekorita nwere otu ihe eji eme ihe aru oru ma di iche na ihe ndi ozo. Mbadamba NovoNorm nwere naanị otu synonym - Diagniniside (nkezi nke 278 rubles).
NovoNorm ọgwụ di iche, nke di iche na ihe mejuputara ha, mana ha nwere otu aru:
- Jardins (ọnụego ọnụahịa - 930 rubles),
- Victoza (nkezi ọnụahịa - 930 rubles),
- Saksenda (nkezi ọnụahịa - 930 rubles),
- Forsyga (nkezi ọnụahịa - 2600 rubles),
- Invokana (nkezi ọnụ ahịa - 1630 rubles).
Enwere ike ikwubi na ọgwụ NovoNorm, nke nwere ọgwụ na-arụ ọrụ na-agagharị agagharị, dị irè n'ịgwọ ụdị ọrịa shuga 2. Ọ na --ebelata ọkwa shuga ka ọ dị n’usoro. Ọ bụrụ n’ịgbaso usoro nri, mmega ahụ na ịlele mkpokoro glucose, ị ga - ewepu hypoglycemia na nnukwu ihe mgbaàmà shuga. Vidio dị n’isiokwu a ga-agwa gị otu esi agwọ ọrịa shuga.