Amprilan® (Amprilan)

Mukamaletsa ACE kumachepa angiotensin-2, renin ntchito imachulukitsa, zochita zimachulukana bradykininkupanga kumawonjezeka aldosterone. Hemodynamic ndi antihypertensive zotsatira za mankhwalawa zimaperekedwa pakukulitsa lumen ya chotengera, kuchepetsa OPSS. Mankhwalawa sasinthakugunda kwa mtima. Kuchiza kwa nthawi yayitali kumatha kubweretsanso kukonzanso kwa hypertrophy yamanzere, yomwe imayamba ndi ochepa matenda oopsa. Kukana kuthamanga kwa magazi olembetsa 1-2 mawola atatha kumwa mankhwalawa, antihypertensive effect imapitirira tsiku limodzi.

Odwala kulephera kwa mtima kuchepetsa chiopsezo kugunda kwa mtima, kufa mwadzidzidzi, kupitirira kwa matenda, kuchuluka kwa zipatala zadzidzidzi ndi kuchuluka kwa mavuto obwera chifukwa cha matenda. Odwala matenda ashuga pali kuchepa microalbuminuriaamachepetsa chiopsezo nephropathy. Zotsatira izi zimakula mosasamala kuchuluka kwa kuthamanga kwa magazi.

Zisonyezo Amprilana

• kulephera kwa mtima (maphunziro osachiritsika)
• matenda oopsa,
• matenda amtsempha wamagaziMitima.

Zizindikiro ntchito odwala matenda ashuga: nephropathy.

Contraindication

• Hypersensitivity ku zida zake
• kupunduka kwa mtima (mitral, aortic, kuphatikiza),
• yoyamwitsa,
• cardiomyopathy,
• aimpso dongosolo matenda,
• hyperaldosteronism,
• mimba,
• wazaka 18.

Zotsatira zoyipa

Nthawi zambiri, kugwa kwakuthwa kwamagazi kumajambulidwa,syncope, mutu wofanana ndi mutu wa migraine, chifuwa chowuma, bronchospasmzotupa pakhungu, kuchuluka gastritis ndi kapamba ndi kuwonjezeka kwa kuchuluka kwa michere, kupweteka m'malo ndi minofu.

Zochepa arrhythmiakugunda kwa mtima angina pectoriszovuta ndi myocardial infarction, Matenda a Raynaud, vasculitis, astheno-depression syndrome yokhala ndi vuto la kugona, osakhalitsa akuwukira komanso sitiroko, kusabala, aimpso dongosolo ndi kuchuluka ndende mango ndi urea mkodzo thupi lawo siligwirizanakusintha kwa magawo a labotor mu mawonekedwe a neutropenia, erythropenia.

Ndi kukula kwa zovuta zoyipa, tikulimbikitsidwa kukaonana ndi dokotala ndikusiya kumwa mankhwala Amprilan kwakanthawi.

Kutulutsa mawonekedwe ndi kapangidwe kake

Chofunikira kwambiri ku Amprilan ndi ramipril.

Zothandiza zomwe zili m'mapiritsi: croscarmellose sodium, pregelatinized starch, sodium stearyl fumarate, sodium bicarbonate, lactose monohydrate, utoto.

Mlingo womwe ukupezeka: 1.25 mg, 2.5 mg, 5 mg ndi 10 mg ya ramipril piritsi limodzi.

Amprilan amapangidwa m'mapiritsi (7 kapena 10 mapiritsi a chithuza) chowulungika ndi malo osalala ndi bevel. Mtundu wa mapiritsiwo umasiyana malinga ndi kuchuluka kwa mankhwalawa: yoyera kapena yoyera (1.25 mg ndi 10 mg iliyonse), chikasu chopepuka (2,5 mg aliyense), pinki mkati mwake (5 mg aliyense),

Zotsatira za pharmacological

Mankhwala Amprilan ndi antchito yoletsa zinthu zakale ya ACE. Kutumiza enzyme ya Angiotensin imathandizira kusintha kwa angiotensin II kuchokera ku angiotensin I, ndikufanana ndi kinase - enzyme yomwe imathandizira kuwonongeka kwa bradykinin. Zotsatira za kutsekedwa kwa ACE ndi Amprilan, kuchuluka kwa angiotensin II kumachepa, ntchito ya renin m'magazi am'magazi imachulukanso, zochita za bradykinin ndikupanga kuchuluka kwa aldosterone, zomwe zimabweretsa kuwonjezeka kwa potaziyamu m'magazi.

Amprilan ali ndi antihypertensive ndi hemodynamic zotsatira zake chifukwa cha kuchuluka kwa mitsempha yamagazi ndikuchepetsa kukana kwawo konsekonse. Poterepa, kugunda kwa mtima sasintha. Kutsika kwa kupanikizika pambuyo pa gawo limodzi la Amprilan kumawonedwa pambuyo pa maola awiri ndi awiri, pambuyo pa maola 3-6 njira yothandizira mankhwalawa ikufika pazambiri ndikupanga maola 24.

Ndi chithandizo cha nthawi yayitali ndi mankhwalawa, kumanzere kwamitsempha yamagazi kumachepa, pomwe palibe zotsatira zoyipa pa ntchito ya mtima.

Pharmacokinetics

Zinthu zomwe zimagwira zimatengedwa mwachangu kuchokera kugaya chakudya (kuthamanga sizimadalira chakudya). Ola limodzi atatha kugwiritsa ntchito, pazotheka ambiri pazogwira ntchito m'magazi zimatheka. Mpaka 73% ya ramipril omwe amamangiriza mapuloteni a plasma.

Mankhwalawa amagwera m'chiwindi, ndikupanga metabolite ramiprilat (ntchito yotsiriza ndi yokwanira 6 poyerekeza ndi ntchito ya ramipril yokha) ndi yogwira pawiri diketopiperazine. Mlingo wambiri wa ramiprilat m'magazi wapezeka patatha maola 2-4 mutatha kugwiritsa ntchito mankhwalawa, wodalirika komanso wokhazikika wochiritsira tsiku la 4 la chithandizo. Pafupifupi 56% ya ramiprilat imamangiriza mapuloteni a plasma.

Mpaka 60% ya ramipril ndi ramiprilat amathandizidwa ndi impso mu mawonekedwe a metabolites, ochepera 2% a ramipril amachotsedwa m'thupi osasinthika. Hafu ya moyo wa ramiprilat imachokera ku maola 13 mpaka 17, ramipril - maola 5.

Ndi vuto laimpso, kuwonongeka kwa ramipril ndi metabolites kumachepa. Odwala omwe ali ndi hepatic insuffuffence, kutembenuka kwa ramipril kukhala ramiprilat kumachepetsedwa, zomwe zili ndi ramipril mu seramu yamagazi zimachulukitsidwa.

Mlingo ndi makonzedwe

Mapiritsi amatengedwa pakamwa, mosasamala chakudya, osafuna kutafuna, amwe madzi ambiri.

Mlingo wa mankhwalawa amasankhidwa ndi dokotala payekhapayekha kwa wodwala aliyense, poganizira zomwe zikuwonetsa, kulolera kwa mankhwalawa, matenda oyanjana ndi msinkhu wa wodwalayo. Mukamasankha mlingo, mawonekedwe a kuthamanga kwa magazi ayenera kukumbukiridwa. Mlingo wovomerezeka wa mankhwalawa amitundu yonse ya ma pathologies ndi 10 mg patsiku. Njira ya chithandizo nthawi zambiri imakhala yotalikirapo, yokhazikitsidwa ndi adokotala.

Ndi ochepa matenda oopsa Mlingo woyambitsidwa woyamba ndi 2.5 mg kamodzi tsiku lililonse. Ngati ndi kotheka, kumwa mankhwalawa mutha kuwonjezeredwa m'masiku 7-14.

Kulephera kwa mtima kosatha muyeso woyenera wa mankhwalawa ndi 1.25 mg (umatha kubwerezedwa pambuyo pa masabata 1-2).

Ndi kulephera kwa mtima, womwe unachitika patatha masiku awiri ndi awiri kuchokera pakubadwa kwadzuwa, tikulimbikitsidwa kutenga 5 mg ya Amprilan patsiku - 2,5 mg m'mawa ndi madzulo. Ngati munthawi ya chithandizo kupanikizika kumatsika kwambiri, mlingo umadukiza (1.25 mg kawiri patsiku). Pambuyo masiku atatu, mlingo umadzukanso. Ngati mukumwa mankhwala a 2,5 mg kawiri pa tsiku komanso osavomerezeka ndi wodwala, chithandizo ndi Amprilan chitha.

Nephropathy (omwe ali ndi vuto la impso ndi matenda ashuga).Mlingo woyambira wopendekera ndi 1.25 mg patsiku. Pakadutsa masiku 14 aliwonse, mlingowo umachulukitsidwa kawiri mpaka mlingo wa 5 mg wa patsiku ufike.

Kupewa kulephera kwa mtima pambuyo poyambitsa myocardial. Pakumayambiriro kwa njira yochizira, Amprilan 2.5 mg ndi mankhwala piritsi lililonse patsiku. Pakatha sabata, mlingo umachulukitsidwa mpaka 5 mg pa tsiku, pakatha milungu iwiri - mpaka pakumwa 10 mg kamodzi patsiku.

Ndi ochepa occlusion komanso pambuyo opaleshoni yamphamvu odutsa Amprilan amatengedwa 2.5 mg kamodzi patsiku kwa masiku 7. Ndipo, kwa masabata awiri, mankhwalawa amatengedwa pa 5 mg patsiku, mlingo wake utawonjezeka kawiri - mpaka 10 mg pa tsiku.

Malangizo apadera

1. Kwa odwala omwe ali ndi vuto la impso, ntchito yoyamba ya Amprilan iyenera kukhala 1.25 mg, ndipo mlingo waukulu wa tsiku lililonse ukhale 5 mg.
2. Kwa odwala omwe ali ndi vuto la chiwindi, muyeso woyamba ndi 1.25 mg, mlingo waukulu wa tsiku ndi tsiku ndi 2,5 mg.
3. Ngati Amprilan amaperekedwa kwa odwala omwe amatenga okodzetsa, kuthetseratu kapena kuchepetsa Mlingo wa okodzetsa kumafunika. Zimafunikanso kuwunikira pafupipafupi momwe alili odwala, makamaka odwala okalamba (opitilira zaka 65).
4. Amprilan amatengedwa mosamala odwala ndi zokhudza zonse matenda a zotumphukira minofu, matenda a shuga, osakhazikika angina pectoris.
5. Mankhwala ali ndi vuto pa mwana wosabadwayo (hypoplasia ya m'mapapo ndi mafupa a chigaza, hyperkalemia, matenda opatsika aimpso) ndipo amatsutsana ndi amayi apakati. Asanataye Amprilan, ndikofunikira kuti akazi azaka zoyambira kubereka asatenge pakati.
6. Mukamamwa Amprilan pa mkaka wa m`mawere, kuyamwitsa kuyenera kuthetsedwa.

Migwirizano ndi magwiritsidwe akusungidwa

Sungani mankhwalawo pa kutentha osaposa 25 ° C, m'malo otetezedwa ndi chinyezi ndi kuwala kwa dzuwa, osavomerezeka kwa ana. Moyo wa alumali wa mapiritsi a Amprilan ndi zaka zitatu. Pambuyo pa tsiku lomwe lasonyezedwa pamaphukusi, mankhwalawa sangatengedwe.

Enquuralural analogues Amprilan (mankhwala omwe ali ndi ntchito yofananira) ndi:

Zithunzi za 3D

Mlingo ndi makonzedwe

Mkati osasamala nthawi yakudya (i.e. mapiritsi amatha kumwa onse musanadye kapena pambuyo pake), imwani madzi ambiri (chikho 1/2). Osameta kapena kuwaza mapiritsi musanatenge.

Mlingo amasankhidwa malinga ndi achire zotsatira ndi kulolera kwa wodwala mankhwala.

Kuchiza ndi Amprilan ® nthawi zambiri kumakhala kotalika, ndipo kutalika kwake kumatsimikiziridwa ndi dokotala.

Pokhapokha pofotokozedwa mwanjira ina, kenako ndi aimpso ndi chiwindi ntchito, njira zotsatirazi zikulimbikitsidwa.

Nthawi zambiri mlingo woyambira ndi 2.5 mg / tsiku m'mawa. Ngati mukumwa Amprilan ® pa mankhwalawa kwa milungu itatu kapena kupitilira apo, sizingatheke kutulutsa magazi, ndiye kuti mlingowo ungakulidwe mpaka 5 mg / tsiku. Ngati mlingo wa 5 mg sugwira ntchito mokwanira, pakatha milungu iwiri itha kupitilirabe mpaka mlingo wokwanira 10 mg.

Ngati njira ina yowonjezera mlingo mpaka 10 mg / tsiku osakwanira mphamvu ya tsiku lililonse ya 5 mg, ndizotheka kuwonjezera othandizira ena othandizira kuchipatala, makamaka okodzetsa kapena BKK.

Mlingo woyambayo ndi 1.25 mg / tsiku. Kutengera momwe wodwalayo amathandizira, mankhwalawa akhoza kuchuluka.

Ndikulimbikitsidwa kuti muwonjezere kawiri mlingo ndi masabata a 1-2. Ngati mukufuna kumwa tsiku ndi tsiku 2,5 mg kapena kuposa, angagwiritsidwe ntchito kamodzi patsiku, kapena kugawidwa pawiri.

Pazipita lililonse tsiku lililonse ndi 10 mg.

Matenda a shuga kapena odwala matenda ashuga

Mlingo woyambayo ndi 1.25 mg / tsiku. Mlingo umatha kuchuluka mpaka 5 mg / tsiku. Ndi mikhalidwe imeneyi, Mlingo woposa 5 mg / tsiku sunaphunziridwe mokwanira m'mayesero azachipatala olamulidwa.

Kuchepetsa chiopsezo chokhala ndi infracation ya myocardial, stroko, kapena mtima wamtima mwa odwala omwe ali ndi chiopsezo chamtima kwambiri.

Mlingo woyambira wothandiza ndi 2.5 mg / tsiku.

Kutengera kulolera kwa wodwala ku Amprilan ®, mlingo umatha kuwonjezeka pang'onopang'ono.

Ndikulimbikitsidwa kuti mupangitse mlingo 2 pakatha sabata limodzi, ndipo pakadutsa milungu itatu, muonjezere mpaka muyeso wa 10 mg / tsiku.

Kugwiritsa ntchito mlingo wopitilira 10 mg / tsiku pamavuto azachipatala owongoleredwa sanaphunzire bwino. Kugwiritsa ntchito mankhwalawa kwa odwala omwe ali ndi Cl creatinine ochepera 0.6 ml / sec sikumveka bwino.

Matenda amtima wamankhwala omwe amapezeka m'masiku ochepa oyambira (kuyambira masiku 2 mpaka 9) pambuyo poti wapangika kwambiri

Mlingo woyambirira woperekedwa ndi 5 mg / tsiku, logawidwa mu 2 Mlingo umodzi wa 2.5 mg (wotengedwa m'mawa ndi madzulo). Ngati wodwalayo salola mlingo woyambayo (kuchepa kwambiri kwa magazi kumawonedwa), ndiye kuti akulimbikitsidwa kumwa 1.25 mg kawiri pa tsiku kwa masiku awiri.

Kenako, kutengera zomwe wodwalayo achita, muyezo utha kuchuluka. Ndikulimbikitsidwa kuti mlingo ndi kuwonjezeka kwake kawiri ndi gawo la masiku 1-3. Kupitilira apo, muyezo wa tsiku ndi tsiku, womwe poyamba udagawidwa pawiri, utha kugwiritsidwa ntchito kamodzi.

Mlingo woyenera kwambiri ndi 10 mg.

Pakadali pano, luso la odwala omwe ali ndi vuto lalikulu la mtima (III - IV gulu lothandiza malinga ndi gulu NYHA) zomwe zidachitika nthawi yomweyo pambuyo poti infernation yokhala pachimake sikokwanira. Ngati odwala oterowo aganiza kuti akalandire chithandizo ndi Amprilan ®, ndikulimbikitsidwa kuti chithandizo chitha kuyamba ndi mlingo wotsika kwambiri - 1,25 mg / tsiku, ndipo chisamaliro chapadera chikuyenera kuthandizidwa ndikukula kulikonse.

Magulu apadera a odwala

Matenda aimpso. Ndi Cl creatinine kuyambira 50 mpaka 20 ml / mphindi / 1.73 m 2, mlingo woyambira tsiku lililonse amakhala 1.25 mg. Mulingo wovomerezeka tsiku lililonse ndi 5 mg.

Kukonzedwa kosakwanira kwamadzimadzi ndi ma electrolyte, matenda oopsa kwambiri, komanso ngati kuchepa kwambiri kwa magazi kumadzetsa chiopsezo (mwachitsanzo, ndi zotupa za atherosselotic zam'mimba ndi mitsempha ya m'magazi). Mlingo woyambirira umachepetsedwa kukhala 1.25 mg / tsiku.

M'mbuyomu okodzetsa. Ngati ndi kotheka, okodzetsa ayenera kuchotsedwa masiku awiri atatu (kutengera nthawi yomwe okonzanso amatulutsa) asanayambe chithandizo ndi Amprilan ® kapena kuchepetsa kuchuluka kwa okodzetsa omwe atengedwa. Chithandizo cha odwala chotere chiyenera kuyamba ndi mlingo wotsika kwambiri wa Amprilan ® - 1.25 mg / tsiku m'mawa. Mutamwa mlingo woyamba komanso nthawi iliyonse mutachulukitsa mlingo wa Amprilan ® ndi / kapena ma louretics, odwala ayenera kuyang'aniridwa ndi achipatala kwa maola osachepera 8 kuti apewe kusachita bwino kwa hypotensive.

Zaka zopitilira 65. Mlingo woyambirira umachepetsedwa kukhala 1.25 mg / tsiku.

Kuwonongeka kwa chiwindi. Zomwe magazi akupanga kuti atenge Amprilan ® zitha kukulira (mwakuchepetsa kuchepa kwa ramiprilat), kapena kufooka (chifukwa chakuchepetsa kutembenuka kwa ramipril osagwira ntchito kukhala ramiprilat). Chifukwa chake, kumayambiriro kwa chithandizo amafunika kuyang'aniridwa mosamala kuchipatala. Mulingo wovomerezeka tsiku lililonse ndi 2,5 mg.

Wopanga

JSC "Krka, dd, Novo mesto". Šmarješka cesta 6, 8501 Novo mesto, Slovenia.

Mukamayala ndi / kapena kumanga ku bizinesi yaku Russia, idzawonetsedwa: "KRKA-RUS" LLC. 143500, Russia, Moscow Region, Istra, ul. Moscow, 50.

Tele. ((495) 994-70-70, fakisi: (495) 994-70-78.

Oimira ofesi ya Krka, dd, Novo mesto JSC ku Russian Federation / bungwe lolandila madandaulo a ogula: 125212, Moscow, Golovinskoye sh., 5, bldg. 1, pansi 22..

Tele. ((495) 981-10-95, fakisi (495) 981-10-91.

Pharmacokinetics

Pambuyo pakukonzekera kwamlomo wa ramipril, Amprilan imatengedwa mwachangu kuchokera m'mimba (m'mimba) pamlingo wa 50-60%. Kudya nthawi yomweyo kumachepetsa mayamwidwe ake, koma sizikhudza kuchuluka kwa zomwe zalowa m'magazi. Zotsatira zamakonzedwe achilengedwe a biotransfform / activation a ramipril, makamaka m'chiwindi ndi hydrolysis, ramiprilat (yogwira metabolite, 6 nthawi yogwira kuposa ramipril pokhudzana ndi ACE inhibition) ndi diketopiperazine (metabolite yomwe ilibe zochitika za pharmacological) imapangidwa. Kupitilira apo, diketopiperazine imalumikizidwa ndi glucuronic acid, ndipo ramiprilat imapangidwa ndi glucuronated ndikuupanga kwa diketopiperazinic acid.

The bioavailability wa ramipril zimatengera pakamwa Mlingo ndipo zimasiyana 15% (2,5 mg) mpaka 28% (kwa 5 mg).The bioavailability wa ramiprilat pambuyo m`kamwa makonzedwe a 2,5 mg ndi 5 mg wa ramipril ndi

45% ya chizindikiro chotengedwa pambuyo pokonzekera kulowetsedwa kwamtundu womwewo.

Pambuyo potenga Amprilan mkati, kuchuluka kwakukulu kwa plasma kwa ramipril kumachitika pambuyo pa 1 h, ramiprilat - pambuyo pa maola 2-4. Kuchepa kwa gawo la ramiprilat mu plasma kumachitika m'magawo angapo: gawo la magawidwe ndi kuchotsa kwa T_1/2 (theka-moyo)

3 h, gawo lapakatikati ndi T_1/2

15 h ndi gawo lotsiriza lomwe lili ndi zochepa kwambiri za ramiprilat mu plasma ndi T_1/2

Masiku 4-5, zomwe ndi chifukwa cha kumasulidwa pang'onopang'ono kwa ramiprilat ku mgwirizano wolimba ndi ACE receptors. Ngakhale kutalika kwa gawo lomaliza, kutenga ramipril pakamwa 2,5 kapena kuposanso kamodzi patsiku mkati mwake kumatha kukwaniritsa kuchuluka kwa madzi a ramiprilat atatha masiku 4 atamwa mankhwalawa. Maphunziro a Amprilan ogwira T_1/2 zimatengera mlingo ndipo zimasiyana kwa maola 13 mpaka 17

Ramipril amamangirira mapuloteni a plasma pafupifupi 73%, ramiprilat - 56%.

Pambuyo pakamwa pa ramipril, yolembedwa ndi radioot isotope, mu 10 mg, mpaka 39% ya radioactivity imatulutsidwa m'matumbo, pafupifupi 60% imachotsedwa impso. Odwala a bile duct drainage chifukwa chodzitengera 5 mg ya ramipril mkati mwa impso ndi matumbo, pafupifupi zofanana ndi ramipril ndi metabolites ake amasulidwa maola 24 atangoyamba.

Pafupifupi 80-90% ya zinthu zomwe zimatengedwa mumkodzo ndi bile zimadziwika kuti ndi ramiprilat ndi metabolites. Ramipril glucuronide ndi diketopiperazine amapanga

10-20% ya okwanira mlingo, ndi unmetabolized ramipril -

M'maphunziro a nyama zanyama, zidapezeka kuti ramipril imadutsa mkaka wa m'mawere.

Odwala omwe ali ndi vuto laimpso, kulengedwa kwa creatinine chilolezo chochepera 60 ml / min kumatha ramiprilat ndi metabolites. Izi zimabweretsa kuwonjezeka kwa ndende yawo ya plasma ndi kuchepa pang'onopang'ono poyerekeza ndi odwala omwe ali ndi vuto laimpso.

Kutenga Mlingo wambiri wa ramipril (10 mg) ngati chiwindi chayamba kugwira ntchito kumayambitsa kutsika kwa mphamvu ya ramipril komanso kuchepa kwa pang'onopang'ono kwa metabolite yake yogwira.

Mwa odzipereka athanzi komanso odwala omwe ali ndi matenda oopsa, palibe kuwunika kwakukulu kwa ramipril ndi ramiprilat komwe kunachitika chifukwa cha machiritso a milungu iwiri ndi Amprilan pa 5 mg patsiku. Pambuyo pa maphunziro a masabata awiri ofanana, odwala omwe ali ndi vuto la mtima anali ndi kuchuluka kwa 1.5-1.8-ramiprilat m'magazi am'magazi komanso malo omwe ali munthawi ya ndende (AUC).

Makhalidwe a pharmacokinetic a ramipril ndi ramiprilat mu okalamba odzipereka omwe ali ndi zaka 65-75 sizisiyana kwenikweni ndi zomwe achinyamata odzipereka athanzi labwino.

Mankhwala

Mankhwala

Metabolite yogwira ya ramipril, yopangidwa ndi zochita za michere ya "chiwindi", ramiprilat ndimtundu wa ACE inhibitor wautali (ACE masinthidwe: kininase II, dipeptidyl carboxy dipeptidase I). ACE mu plasma ndi zimakhala zimathandizira kutembenuka kwa angiotensin II, yemwe ali ndi vasoconstrictor kwenikweni, ndi kuwonongeka kwa bradykinin, yomwe imapangitsa Vasodilating. Chifukwa chake, mutenga ramipril mkati, mapangidwe a angiotensin II amachepetsa ndipo bradykinin imadziunjikira, yomwe imayambitsa vasodilation ndi kuchepa kwa kuthamanga kwa magazi (BP). Kuchulukitsa kwa Ramipril komwe kumapangitsa ntchito ya kallikrein-kinin mu plasma yamagazi ndi zimakhala ndi kutsegula kwa dongosolo la prostaglandin komanso kuwonjezeka kaphatikizidwe ka prostaglandins, kamene kamapangitsa mapangidwe a nitric oxide (N0) mu endotheliocytes, amachititsa mtima wake.

Angiotensin II imathandizira kupanga aldosterone, kotero kutenga ramipril kumabweretsa kuchepa kwa secretion ya aldosterone komanso kuwonjezeka kwa potaziyamu mu seramu yamagazi.

Ndi kuchepa kwa kuchuluka kwa angiotensin II m'madzi am'magazi, mphamvu yake yoletsa kukhudzidwa kwa renin ndi mtundu wa mayankho olakwika amachotsedwa, zomwe zimapangitsa kuti ntchito ya plasma renin ipangidwe.

Amaganiziridwa kuti kukulira kwina koyipa (makamaka, chifuwa "chowuma") kumalumikizidwa ndi kuwonjezeka kwa ntchito ya bradykinin.

Odwala ochepa ochepa matenda oopsa kutenga ramipril kumabweretsa kutsika kwa magazi mu "kunama" ndi "kuyimirira" malo popanda kukakamiza kuchuluka kwa mtima (HR). Ramipril amachepetsa kwambiri zotumphukira zotupa (OPSS), popanda kuchititsa kusintha kwa magazi aimpso komanso kuchuluka kwa kusefera kwa mafuta. Mphamvu ya antihypertensive imayamba kuwonekera kwa maola 1 mpaka 2 atatha kumwa kamodzi pa mankhwalawa, mpaka imakhala yofunikira kwambiri pambuyo pa maola 3-6, ndipo imakhala kwa maola 24. Mukatenga Amprilan, mphamvu ya antihypertensive imatha kukula pang'ono, nthawi zambiri imakhala yolimbikitsidwa ndi masabata a 3-4 ogwiritsidwa ntchito pafupipafupi kenako ndikupitilira kwa nthawi yayitali. Kusiyidwa kwadzidzidzi kwa mankhwalawa sikupangitsa kuti magazi azithamanga (osowa "kusiya").

Odwala ochepa matenda oopsa, ramipril imachedwetsa kukula ndi kupitilira kwa myocardial hypertrophy ndi mtima wall.

Odwala omwe ali ndi vuto la mtima (CHF) ramipril imachepetsa OPSS (imachepetsa kutsitsa pamtima), imakulitsa mphamvu ya venous channel ndikuchepetsa kuzaza kwa lamanzere lamitsempha lamanzere (LV), kumene, kumabweretsa kutsika kwa preload pamtima. Mwa odwalawa, pamene akutenga ramipril, pali kuwonjezeka kwa kutulutsa kwamtima, kachigawo ka LV ejection (LVEF) ndikusintha kwa kulolerako zolimbitsa thupi.

Ndi matenda ashuga komanso osadwala kutenga ramipril kumachepetsa kukula kwa impso kulephera ndi kuyambika kwa gawo lotsiriza kulephera kwa impso ndipo, potero, kumachepetsa kufunika kwa hemodialysis kapena kupatsirana kwa impso. M'magawo oyamba a matenda ashuga kapena nondiabetesic nephropathy, ramipril amachepetsa vuto la albinuria.

Odwala omwe ali ndi chiopsezo chokhala ndi matenda amtima chifukwa cha zotupa zam'mitsempha. cholesterol (OXc), kuchepetsa kukhathamiritsa kwa kuchuluka-kachulukidwe lipoprotein cholesterol (HDL-C), kusuta) kuwonjezera kwa ramipril ku chithandizo chamankhwala kumachepetsa Limafotokoza za kufa kwa myocardial infarction, sitiroko, ndi kufa mtima. Kuphatikiza apo, ramipril imachepetsa chiwerengero cha anthu omwalira, komanso kufunikira kwa njira zotsitsimutsanso ndikuchepetsa kuyambika kapena kupitirira kwa kugunda kwa mtima.

Odwala omwe ali ndi vuto la mtima ndi chiwonetsero cha matenda omwe adayamba m'masiku oyamba a infarction ya pachimake (2-9 masiku), kugwiritsa ntchito ramipril, kuyambira 3 mpaka 10th tsiku lachiberekero cholowerera, kuchepetsa kufedwa (mwa 27%), chiopsezo chadzidzidzi Imfa (mwa 30%), chiwopsezo cha mtima wosalephera kupitirira pamlingo woopsa (III-IV functional class malinga ndi NYHA gulu) / chithandizo chothandizira (pofika 23%), mwayi wokhala kuchipatala chotsatira chifukwa cha kulephera kwa mtima (mwa 26%).

Mwa kuchuluka kwa odwala, komanso odwala matenda a shuga, omwe amakhala ndi matenda oopsa komanso kuthamanga kwa magazi, ramipril amachepetsa chiopsezo cha nephropathy komanso kupezeka kwa microalbuminuria.

Pharmacokinetics

Pambuyo pakukonzekera kwa pakamwa, ramipril imatengedwa mwachangu kuchokera ku m'mimba thirakiti (50-60%). Kudya kumachepetsa mayamwidwe, koma sikukhudza kuperewera kwa mayamwa.

Ramipril amakhala ndi mphamvu yayikulu yogwiritsira ntchito metabolism / activation (makamaka m'chiwindi ndi hydrolysis), zomwe zimapangitsa kuti metabolite yekha, ramiprilat, yemwe ntchito yake yokhudzana ndi kuletsa ACE ikhale pafupifupi 6 nthawi ya ramipril. Kuphatikiza apo, chifukwa cha ramipril metabolism, diketopiperazine, yomwe ilibe zochitika zamankhwala, imapangidwa, yomwe imalumikizidwa ndi glucuronic acid, ramiprilat imaphatikizidwanso glucuronated ndikupanga mankhwala a diketopiperazinic acid.

The bioavailability wa ramipril pambuyo m`kamwa makonzedwe kuyambira 15% (kwa 2,5 mg) mpaka 28% (kwa 5 mg). The bioavailability wa yogwira metabolite - ramiprilat - pambuyo mkamwa makonzedwe a 2,5 mg ndi 5 mg wa ramipril pafupifupi 45% (poyerekeza ndi bioavailability pambuyo mtsempha wamagulu Mlingo womwewo).

Pambuyo potenga ramipril mkati, plasma wozama wa ramipril ndi ramiprilat umafikiridwa pambuyo pa maola 1 ndi 2 mpaka 4, motsatana. Kuchepa kwa plasma ndende ya ramiprilat kumachitika m'magawo angapo: magawanidwe ndikugawa ndi gawo lamoyo (T1 / 2) la ramiprilat pafupifupi maola atatu, ndiye gawo lapakatikati ndi T1 / 2 ramiprilat, pafupifupi maola 15, ndipo gawo lomaliza lokhala ndi kuchepa kwambiri kwa ramiprilat mu plasma ndi T1 / 2 ramiprilat, pafupifupi masiku 4-5. Gawo lomaliza ili chifukwa chakumasulidwa kwapang'onopang'ono kwa ramiprilat kuchokera ku chomangira cholimba ndi ACE receptors. Ngakhale gawo lomaliza lomaliza lokhala ndi pakamwa limodzi la ramipril pakamwa 2,5 mg kapena kuposerapo, kuchuluka kwa madzi a ramiprilat kumachitika patatha masiku pafupifupi anayi a chithandizo. Mothandizidwa ndi mankhwala "ogwira" T1 / 2 kutengera mlingo ndi maola 13 mpaka 17.

Kuyankhulana ndi mapuloteni am'madzi am'magazi pafupifupi 73% ya ramipril, ndi 56% ya ramiprilat.

Pambuyo pamakina othandizira, kuchuluka kwa ramipril ndi ramiprilat kuli pafupifupi 90 L ndi pafupifupi 500 L, motsatana.

Pambuyo pakumeza kwa ramipril (10 mg) wolembedwa ndi isotope wailesi, 39% ya radioactivity imachotsedwa m'matumbo ndipo pafupifupi 60% ndi impso. Pambuyo pakukonzekera kwamitsempha kwa ramipril, 50-60% ya mankhwalawa imapezeka mkodzo mu mawonekedwe a ramipril ndi metabolites. Pambuyo pokonzekera kulowetsedwa kwa ramiprilat, pafupifupi 70% ya mankhwalawa imapezeka mkodzo mu mawonekedwe a ramiprilat ndi metabolites, mwanjira ina, ndi intravenous ya ramipril ndi ramiprilat, gawo lofunikira la mankhwalawa limatulutsidwa m'matumbo ndi bile, kudutsa impso (50% ndi 30%, motero). Pambuyo pakamwa makonzedwe a 5 mg a ramipril mwa odwala a kukhetsa kwa ma draina, pafupifupi kuchuluka komweko kwa ramipril ndi metabolites ake kumatsitsidwa ndi impso komanso m'matumbo mu maola 24 atangotha.

Pafupifupi 80 - 90% ya metabolites mu mkodzo ndi bile adadziwika kuti ndi ramiprilat ndi ramiprilat metabolites. Mankhwala a Ramipril glucuronide ndi ramipril diketopiperazine pafupifupi 10-20% ya kuchuluka kwathunthu, ndipo zinthu zosakhudzidwa ndi ramipril mumkodzo ndi pafupifupi 2%. Kafukufuku wazinyama awonetsa kuti ramipril imachotsedwanso mkaka wa m'mawere.

Panthawi ya kuphwanya kwa impso ndi creatinine chilolezo (CC) chochepera 60 ml / min, chimbudzi cha ramiprilat ndi ma metabolites ake ndi impso amachepetsa. Izi zimabweretsa kuwonjezeka kwa plasma ndende ya ramiprilat, yomwe imachepetsa pang'onopang'ono kuposa odwala omwe ali ndi vuto laimpso.

Mukatenga ramipril muyezo waukulu (10 mg), chiwindi chimagwira ntchito zimayendetsa pang'onopang'ono mu kagayidwe ka ramipril ndikuyamba kuchepa kwa ramiprilat. Odzipereka athanzi komanso odwala omwe ali ndi matenda oopsa oopsa, atatha kumwa kwa milungu iwiri ndi ramipril tsiku lililonse la 5 mg, palibe kuchuluka kwakukulu kwa ramipril ndi ramiprilat. Odwala omwe ali ndi vuto la mtima, pambuyo pa milungu iwiri ya chithandizo cha ramipril mu tsiku lililonse la 5 mg, kuwonjezeka kwa 1.5-1.8-plasma mozungulira kwa ramiprilat ndi dera lomwe lili pansi pa nthawi yokhazikika (AUC).

Mwa odzipereka okalamba athanzi (zaka 65-75), ma pharmacokinetics a ramipril ndi ramiprilat siosiyana kwambiri ndi omwe ali achinyamata odzipereka athanzi.

Gwiritsani ntchito pa nthawi yoyembekezera komanso nthawi yoyamwitsa

Amprilan ndi contraindicated pa mimba, monga momwe zimakhudzira mwana wosabadwayo: kusokonezeka kwa impso za mwana wosabadwayo, kuchepa magazi a mwana wosabadwayo ndi akhanda, kuphwanya kwaimpso ntchito, hyperkalemia, hypoplasia mafupa a chigaza, hypoplasia yamapapu.

Chifukwa chake, musanamwe mankhwala azimayi a msinkhu wobereka, mimba sayenera kupatula.

Ngati mayi akukonzekera kukhala ndi pakati, ndiye kuti chithandizo chokhala ndi ACE inhibitor chiyenera kusiyidwa.

Ngati muli ndi pakati pa nthawi ya chithandizo cham'mimba ndi Amprilan, muyenera kusiya kumwa mosachedwa ndikusintha wodwalayo kuti atenge mankhwala ena, ndikugwiritsa ntchito zomwe mwayi wawo kwa mwana ukhale wocheperako.

Ngati chithandizo ndi Amprilan chili chofunikira pakuyamwitsa, kuyamwitsa kuyenera kutha.

Amprilan, malangizo ogwiritsira ntchito (Njira ndi Mlingo)

Ramipril amatchulidwa mkati mwa ufulu wakudya wambiri. Mapiritsi akulimbikitsidwa kumwa madzi ambiri. Mankhwala amathandizidwa ndi dokotala yemwe amasankha mlingo wokwanira woganizira mkhalidwe wa wodwalayo ndi kulolerana kwake ndi zigawo za mankhwala. Ndikulimbikitsidwa kuti muyambe kumwa Amprilan ndi milingo yaying'ono ya 2,5 mg, kuti athe kuchuluka kwambiri - 10 mg. Kutalika kwa mankhwalawa kumatsimikiziridwa ndi dokotala kutengera madandaulo ndi deta, mbiri yakale yotsogolera mosamala.

Malangizo ogwiritsira ntchito Amprilan ND ndi NL: piritsi 1 patsiku. Kusintha kwa mankhwalawa panthawi ya mankhwala. Kutalika kwa chithandizo sikumalire.

Mlingo

Mapiritsi 1.25 mg, 2,5 mg, 5 mg ndi 10 mg

Piritsi limodzi lili

ntchito yogwira - ramipril 1.25 mg, 2,5 mg, 5 mg, 10 mg,

zokopa: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized wowuma (wowuma 1500), sodium stearyl fumarate (Mlingo wa 1.25 mg, 2.5 mg, 5 mg ndi 10 mg),

Mlingo 2,5 mg: pigment osakaniza PB22886 chikasu (lactose monohydrate, iron oxide chikasu (E 172),

Mlingo wa 5 mg: pigment osakaniza PB24899 ofiira (lactose monohydrate, red oxide red (E 172), iron oxide chikasu (E 172)

Mapiritsi okhala ndi tchuthi, kuyambira oyera mpaka oyera,

chamfered (Mlingo wa 1.25 mg ndi 10 mg)

Mapiritsi okhala ndi tchire lambiri, chikasu chopepuka, chamfriti (mulingo wa 2.5 mg)

Mapiritsi okhala ndi lathyathyathya amakhala amtundu wokulirapo, wapinki muutoto, wokongola komanso wowoneka bwino (mulingo wa 5 mg)

Bongo

Zizindikiro za mankhwala osokoneza bongo ndi bradycardia (mafupa osowa), kutsika kwakukulu kwa kuthamanga kwa magazi, dziko lodzidzimutsa ndi pachimake aimpso kulephera. Njira zadzidzidzi za bongo zimaphatikizira chapamimba ndi kugwiritsa ntchito panthawi yakeammayankhoma, komanso ndi chiwopsezo chodzidzimutsa, kuyambitsa mankhwala omwe amalimbikitsa kuthamanga kwa magazi.

Kuchita

Vasopressor amphanomachul, gulu la mankhwala omwe si a anti -idalidal anti-yotupa, mahomoni a corticosteroid amatha kuchepetsa kuopsa kwa hypotensive zotsatira raminipril. Kupititsa patsogolo mphamvu ya antipsychotic, antidepressant mankhwala. Kuphatikiza kwa Amprilan ndi mankhwala a gulu la lithiamu, golide, potaziyamu wambiri, othandizira a hypoglycemic, cytostatics, kukonzekera kwa potaziyamu, osavomerezeka.

Tulutsani mawonekedwe ndi ma CD

Mapiritsi 7 kapena 10 amayikidwa mu blister strip yokhazikitsa filimu ya laminated polyamide / aluminium / polyvinyl chloride ndi zojambulazo za aluminium.

Phukusi lodzaza lomwe lili ndi mapiritsi 7 limafotokozeredwa m'njira ziwiri, zomwe zimasiyana pakakonzedwe ka mapiritsi a phukusi.

4, 12 kapena 14 (mapiritsi 7 aliwonse) kapena 2, 3 kapena 5 (mapiritsi 10 aliwonse) chithuza chokhala ndi malangizo ogwiritsira ntchito kuchipatala komanso zilankhulo zaku Russia zimayikidwa mukatoni