Dianormet ea lithethefatsi: litaelo tsa tšebeliso
Mofumahali Dianormet (motsoako o sebetsang oa metformin -1.1 - dimethylbiguanide hydrochloride) ke moemeli oa hypoglycemic bakeng sa tsamaiso ea molomo ea sehlopha sa Biguanide. Fokotsa tsoekere e phahameng ea mali ho bakuli ba lefu la tsoekere. Setlhare sena se hlahisa litholoana tsa sona ho sa tsotelehe mesebetsi ea sekhukhu ea manyeme. Mochine oa ts'ebetso oa Dianormet o hlahisoa ke thibelo ea ho tsamaisoa ha lielektrone ka mokokotlong oa mitochondria, e lebisang ho fokotseha hoa khatello ea methapo ea methapo ea kutlo le ts'ebetso ea glycolysis ea anaerobic, ka lebaka la hore glucose e kena liseleng tse tsoang sebakeng sa kantle ho masapo le tlhahiso ea methapo ea methapo. joalo ka mala, sebete, hape le mesifa le adipose tishu.
Ketso ea Dianormet e fetela ho:
- Phekolo ea ka mpeng - e thibela ho kenngoa ha tsoekere ka mpeng, e fokotsa ho phahama ha mala le mala.
- sebete - "gluconeogeneis" le phallo ea tsoekere maling, e ntlafatsa glycolysis ea anaerobic,
- lisele tsa moea - e eketsa ho amoheloa ha tsoekere ea glucose, e bakoang ke keketseho e potlakileng ea insulin (ketso ea boemo ba insulin receptor - keketseho ea palo le tumellano ea li-receptor, hammoho le ts'ebelisano-hloko ea "lits'ebetso tse tsamaisang glucose ho lisele". Ka lebaka leo, Dianormet ha e khothalletse ho tsoa ha insulin ke lisele tsa sesebelisoa sa ispancreas, e thusa ho felisa hyperinsulinemia, e leng e 'ngoe ea lisosa tse kholo tsa ho phahama ha mathata a methapo le phaello ea boima ba mofuta oa lefu la tsoekere la II.
Ntle le moo, Dianormet e na le phello e ntle ea metabolic ho:
- lipids tsa mali - E fokotsa sekhahla sa cholesterol e felletseng ka 10-20% le likaroloana tsa eona: LDL le VLDL, e amanang le thibelo ea biosynthesis ea bona ka leboteng la mala le keketseho e kholo ka pampitšana ea mala. E eketsa HDL ka 10-20% mme e fokotsa TG ka 10-20% (le haeba boemo ba bona bo eketsehile ka 50%) ka ho thibela oxidation ea mafura acid, ho fokotsa khatello ea "insulin" le ho thibela ho kenngoa ha tsoekere maling.
- coagulation le sistimi ea fibrinolysis - e fokotsa kutloisiso ea liplatelete ho lintho tse kopanetsoeng, e hlohlelletsa mofuta o mong oa fibrinolysis ka ho eketsa ts'ebetso ea t-PA (activator ea tisy plasminogen), e theola boemo ba PAI-1 (tishu ea plasminogen activator inhibitor) le ho fokotsa boemo ba fibrinogen,
- lerako la sekepe sa mali - e thibela ho ata ha lisele tsa mesifa e boreleli.
Phello e eketsehileng ea metabolism ea lithethefatsi e lekants'a litlamorao ho tsamaiso ea potoloho, thibelo ea nts'etsopele ea lefu la tsoekere le thibelo ea mathata a kang khatello ea mali (hypertension hypertension) le lefu la pelo. Ho bakuli ba batenya haholo, ho ka fokotsa boima ba 'mele, haholo qalong ea kalafo.
Mofumahali E kenella ka har'a duodenum le mala a manyane. Bioavailability ke 50-60%. Moriana ha o kopane le liprotheine tsa mali, o hasoa ka potlako liseleng tse fapaneng, o bokellana haholo leboteng la mpa (mpa, duodenum le mala a manyane), sebete, mesifa, liphio, litšoelesa tsa lefutso. Ts'oarello e kholo ka ho fetisisa ea serum e fihlella lihora tse 2 kamora ho busa. Bophelo ba halofo ke lihora tse 1.5-6. Ho fapana le phenformin, Dianormet ha e tšeloe 'mele. Lithethefatsi ha li sa fetoloa ka har'a moroto (hoo e ka bang 90% ka nako ea lihora tse 12). Ho bakuli ba tsofetseng le ba nang le bothata ba ho sebetsa ha renal, pharmacokinetics ea metformin e fetoha haholo. Kakaretso ea tumello ea ho phekola le ho phekola bakuli ba tsofetseng e fokotsehile ka 35-40%, ho bakuli ba nang le ho hlaphoheloa ke pheko ho ho leka-lekana - ka 74-78%. Ka ts'ebetso ea renal e sa sebetseng hantle, ho sebelisoa hoa lithethefatsi hoa khoneha.
Tšebeliso ea lithethefatsi Dianormet
Kahare nakong ea lijo kapa hang ka mor'a lijo.
Dianormet 500: tekanyetso ea pele ea 500 mg ka letsatsi. Tekanyetso e lokela ho eketseha butle butle ho fumana phello e nepahetseng. Ka tloaelo nka 500 mg (pilisi e le 'ngoe) makhetlo a 2-3 ka letsatsi. Tekanyo e phahameng ea letsatsi le letsatsi ke 2500 mg.
Dianormet 850: tekanyetso ea pele ea 850 mg / ka letsatsi. Tekanyetso e lokela ho eketseha butle butle ho fumana phello e nepahetseng. Ka tloaelo nka Letlapa le le leng la makhetlo a 2-3 ka letsatsi. Tekanyo e phahameng ke 2500 mg / ka letsatsi.
Phello e phahameng ea kalafo e ka hlaha kamora matsatsi a 10-14 a kalafo, ka hona lethalamo ha lea lokela ho eketseha ka potlako haholo.
Ha o sebelisa Dianormet ka nako e le ngoe le insulin matsatsing a 4-6 a pele, lethal dose ea insulin ha le fetoloe, nakong e tlang, lethal dose la "insulin" le fokotsoa butle-butle (ke 4- IU matsatsi a 'maloa).
Contraindication mabapi le ts'ebeliso ea lithethefatsi Dianormet
Hypersensitivity ho lithethefatsi, lefu la tsoekere, metabolic acidosis, lactic acidosis, boemo ba hypoxia (ka lebaka la hypoxemia, ts'oaro, joalo-joalo), renal, ho hloleha ha sebete, ho se potolohe ha methapo hypoxia, infraction ea myocardial, ho hloleha ho phefumoloha, ho chesa haholo, ts'ebetso, mafu a tšoaetsanoang , ts'ebeliso ea li-anti-iodine tse nang le iodine e fapaneng, joala, nako ea kemolo le ho nyeka.
Litla-morao tsa lithethefatsi Dianormet
Takatso e theohileng ea letsoai, tatso ea tšepe ka hanong, ho nyekeloa, ho hlatsa, bohloko ba ka mpeng, lets'ollo. Phokotso ea botebo ba liketsahalo tsena e fumaneha ka ho sebelisa lithethefatsi ka lijo kapa ka ho qala kalafo ka tekanyetso e tlase ea letsatsi le letsatsi. Haeba dyspeptic phenomena e sa fetelle ea bona ka nako e telele, moriana o lokela ho emisoa.
Ke ka seoelo, hlooho ea hlooho le ho tsekela, ho tepella, le maemo le ho honyela ha letlalo li hlokomelehang.
Ka kalafo ea nako e telele maemong a sa tloaelehang, anemia ea megaloblastic e ka hlaha ka lebaka la malabsorption ea vithamine B12 le folic acid. Ha u sebelisa lithethefatsi, ho ka etsahala ho nts'etsapele lactic acidosis, ketsahalo ea eona e khothalletsoang ke tishu hypoxia, renal, sebete kapa ho hloleha ho phefumoloha, ho hloleha ho potoloha ha mali, hypogia ea sethoathoa, mafu a tšoaetsanoang le a oncological, hypovitaminosis, tšebeliso ea joala, anesthesia, botsofe. Maemong a joalo, hemodialysis e bontšoa. Nakong ea phekolo le Dianormet e kopantsoeng le sulfonylurea derivatives le / kapa insulin hypoglycemia e ka hlaha, maemong a joalo, tokiso ea litekanyetso tsa meriana e sebelisitsoeng e ea hlokahala.
Litaelo tse khethehileng bakeng sa ts'ebeliso ea lithethefatsi Dianormet
Nakong ea kalafo le Dianormet, litekanyetso tsa tsoekere maling le moriring li lokela ho beoa leihlo nako le nako. Haeba ho hlokahala, ts'ebetso ea ts'ebetso ea bongaka e kenelletseng, ho hlahisoa ha li-Dianormet tsa tlhahlobo ea tlhahlobo bakeng sa nakoana ho hlakotsoe. Ho nwa joala ho eketsa kotsi ea ho lactic acidosis kalafo ea Dianormet. Ka tšebeliso e kopaneng ea Dianormet e tsoang ho sulfonylurea e tsoang le insulin, e nang le phepo e lekaneng, kamora ho ikoetlisa haholo molemong oa ts'ebeliso e mpe ea joala, boemo ba hypoglycemic bo ka hlaha, bo lokelang ho tsotelloa ha ho khanna makoloi le ho sebetsa ka mekhoa e ka bang kotsi.
Pele le nakong ea kalafo le Dianormet, ho hlokahala hore nako le nako u lekole matšoao a tšebetso ea sebete le a liphio. Ka tšebeliso ea nako e telele ea lithethefatsi, tlhahlobo ea mali ea morphological e lokela ho etsoa hang ka selemo, kaha metformin e ka kenngoa liseleng tse khubelu tsa mali.
Ho sebelisana le lithethefatsi Dianormet
Dianormet e sebetsa ka mokhoa o kopaneng le sulfonylurea derivatives (glibenclamide, glipizide), insulin le acarbose. Amiloride, digoxin, quinidine, morphine, procainamide, triamteren, trimethoprim, cimetidine, ranitidine, Famotidine, calcium Channel blockers (haholo-holo nifedipine) e thibela thibelo ea tubular maling le ho ka eketsa ho teba ha Dianormet ka serum ea mali. Furosemide e eketsa khatello ea Dianormet ka serum ea mali, 'me Dianormet e fokotsa khatello ea maikutlo le halofo ea bophelo ba furosemide.
Ha e sebelisoa le lithethefatsi tse ka lebisang ho hypoglycemia (clofibrate, probenecid, propranalol, rifampicin, sulfonamides, salicylates), tekanyo ea Dianormet e fokotsehile.
Lithethefatsi tse ka bakang hyperglycemia (lithethefatsi tse thibelang pelehi ka molomo tsa estrogen, corticosteroids, diuretics, isoniazid, nicotinic acid, phenytoin, chlorpromazine, lihomone tsa qoqotho, sympathomimetics) li ka fokotsa katleho ea Dianormet. Tabeng ea tšebeliso ea eona e kopaneng le lithethefatsi tsena, litaba tsa tsoekere ea mali li lokela ho behoa leihlo mme, haeba ho hlokahala, keketseho e lekanang ea tekanyetso ea Dianormet. Tai ea Ethyl e eketsa kotsi ea lactic acidosis. Colestyramine le katara e liehisa ho amoheloa ha Dianormet, e fokotsa phello ea eona. Lichelete tsena li lokela ho sebelisoa lihora tse 'maloa ka mor'a ho nka Dianormet. Lithethefatsi li ntlafatsa phello ea li-anticoagulants tsa molomo tsa sehlopha sa coumarin.
Bongata ba lithethefatsi Dianormet, matšoao le kalafo
Le ha overdose ea bohlokoa hangata ha e lebise ho kholo ea hypoglycemia, empa ho na le ts'okelo ea lactic acidosis: ho mpefala ha bophelo bo botle, bofokoli, bohloko ba mesifa, ho nyekeloa ke pelo, ho hlatsa, lets'ollo, bohloko ba ka mpeng, ho hloleha ho hema. Phekolo ea lactic acidosis - hemodialysis.
Matšoao overdose e bonolo: ho otsela, pono e fifalitsoeng, karolo e ommeng ea mucous ea molomo. Ha matšoao ana a hlaha, mokuli o lokela ho ba tlasa tlhokomelo ea ngaka. Phekolo matšoao.
Ha e le overdose e matla, ho fokotseha kapa ho eketseha ha khatello ea mali, bana ba hlapollotsoeng, tachy kapa bradycardia, ischuria (ka lebaka la atony ea lesapo la mokokotlo), intestinal hypokinesia, hypo- kapa hyperthermia, "tendon Reflex", ho hloleha ho phefumoloha, ho sisinyeha, komisi hoa khoneha. Phekolo - Ho tlosoa hoa lithethefatsi, ho hlaka hoa mpa, hemodialysis, ho khutlisetsa mali pH, ho felisoa ha hypoxia, kalafo ea anticonvulsant, ho tsitsisa mesebetsi ea methapo ea pelo le ea ho hema.
Litaelo tsa ho sebelisa Dianormet
Metformin 500 mg, 850 mg kapa 100 mg.
Lithako tse ling: povidone, talc, stearate ea magnesium.
mofuta oa lefu la tsoekere la 2 lefu la tsoekere (le sa itšetleheng ka insulin) le phekolo ea ho se sebetse hantle, haholo ho bakuli ba nang le boima ba 'mele: kalafo ea methapo kapa motsoako hammoho le li-insulin bakeng sa kalafo ea batho ba baholo, e le monotherapy kapa motsoako oa insulin bakeng sa kalafo ea bana ho tloha ho lilemo tse 10.
Fokotsa ho teba ha mathata a lefu la tsoekere ho bakuli ba baholo ba nang le lefu la tsoekere la mofuta oa 2 le boima bo feteletseng ba sebelisang metformin e le sethethefatsi sa pele se sa sebetseng hantle kalafo ea phepo.
Mokhoa oa ho sebelisa: litekanyetso le kalafo
Ka hare, nakong kapa hang ka mor'a lijo, bakeng sa bakuli ba sa fuoeng insulin, 1 g (matlapa a 2) makhetlo a 2 ka letsatsi bakeng sa matsatsi a 3 a pele kapa 500 mg makhetlo a 3 ka letsatsi, ebe ho tloha matsatsing a mane ho isa ho a 14 - 1 g makhetlo a 3 ka letsatsi, kamora matsatsi a 15 moriana o ka fokotsoa o nahanela litaba tsa tsoekere maling le morong. Tekanyetso ea letsatsi le letsatsi - - g, g.
Matlapa a retard (850 mg) a nkuoa hoseng le mantsiboea. Sekhahla se phahameng sa letsatsi ke 3 g.
Ka tšebeliso e tšoanang ea "insulin" ka tekanyo ea li-unit tse ka tlase ho 40 / ka letsatsi, moriana oa litekanyetso tsa metformin o ts'oana, ha tekanyetso ea insulin e ka fokotsoa butle-butle (ka likarolo tsa 4-8 / letsatsi ka letsatsi le leng le le leng). Ka tekanyo ea insulin ea li-unit tse fetang 40 / ka letsatsi, ts'ebeliso ea metformin le ho fokotseha ha tekanyetso ea insulin ho hloka tlhokomelo e kholo mme e etsoa sepetlele.
Ketso ea pharmacological
Biguanide, moemeli oa hypoglycemic bakeng sa tsamaiso ea molomo. Ho bakuli ba nang le lefu la tsoekere, e fokotsa khatello ea "glucose" maling ka ho thibela gluconeogenesis ka har'a sebete, e fokotse ho monya ha tsoekere maling ho tsoa phepelong ea mpa le ho eketsa ts'ebeliso ea eona manonyeletsong. E tsitsisa kapa e theola boima ba 'mele.
Ha ho na le insulin maling, phello ea kalafo ha e bonahatsoe. Boitšoaro ba Hypoglycemic ha bo bake. E ntlafatsa thepa ea mali ea fibrinolytic ka lebaka la khatello ea inhibitor ea activator profibrinolysin (plasminogen).
Litlamorao
Ho tsoa ho tsamaiso ea tšilo ea lijo: ho nyekeloa ke pelo, ho hlatsa, tatso ea "tšepe" molomong, ho fokotse takatso ea lijo, dyspepsia, flatulence, bohloko ba ka maleng.
Ho tloha lehlakoreng la metabolism: maemong a mang - lactic acidosis (bofokoli, myalgia, mathata a ho hema, ho otsela, bohloko ba ka mpeng, hypothermia, ho fokotseha ha khatello ea mali, Reflex bradyarrhythmia), ka kalafo ea nako e telele - hypovitaminosis B12 (malabsorption).
Ho tsoa lithong tsa hemopoietic: maemong a mang - anemia ea megaloblastic.
Litla-morao:
Maemong a litla-morao, tekanyetso e lokela ho fokotsoa kapa ho hlakotsoe ka nakoana. Matšoao: lactic acidosis.
Tšebelisano
E fokotsa Cmax le T1 / 2 ea furosemide ka 31 le 42.3%, ka ho latellana.
Ha e lumellane le ethanol (lactic acidosis).
Sebelisa ka tlhokomeliso hammoho le anticoagulants le cimetidine.
Liphetho tsa sulfonylureas, insulin, acarbose, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate, cyclophosphamide le salicylates li matlafatsa phello.
Ka tšebeliso e tšoanang le GCS, lithibela-pelehi tsa li-hormone bakeng sa tsamaiso ea molomo, epinephrine, glucagon, lihormone tsa qoqotho, li-derotate tsa phenothiazine, li-thiazide diuretics, li-nicotinic acid derivatives, ho fokotseha hoa phello ea hypoglycemic ea metformin ho ka etsahala.
Furosemide e eketsa Cmax ka 22%.
Nifedipine e eketsa ho monya, Cmax, e liehisa ho tebela.
Lithethefatsi tsa Cationic (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamteren le vancomycin) tse bolokiloeng thekisong ea tlholisano ea litsamaiso tsa tsamaiso ea lefutso mme li ka eketsa Cmax ka 60% ka kalafo ea nako e telele.