Amprilan® (Amprilan)

Thaum thaiv ACE txo angiotensin-2, renin kev ua si nce, nqis tes ua nce bradykininntau lawm aldosteroneCov. Hemodynamic thiab antihypertensive zoo ntawm cov tshuaj yog muab los ntawm kev nthuav tawm lub lumen ntawm lub nkoj, txo OPSS. Cov tshuaj tsis cuam tshuam dabtsilub plawv dhiaCov. Kev kho mob ntev tuaj yeem ua rau regression ntawm laug ventricular hypertrophy, uas ua nrog leeg ntshav siabCov. Poob qis ntshav siab sau npe 1-2 teev tom qab noj cov tshuaj, cov nyhuv antihypertensive tseem muaj nyob rau ib hnub.

Hauv cov neeg mob nrog lub plawv tsis ua hauj lwm txo kev pheej hmoo plawv nres, Kev tuag tam sim, kab mob kev loj hlob, tus naj npawb ntawm tsev kho mob ceev thiab tus naj npawb ntawm tawg ua pab ua pawgCov. Hauv cov neeg mob nrog mob ntshav qab zib muaj qhov tsawg microalbuminuriatxo qhov kev pheej hmoo nephropathyCov. Cov teebmeem no txhim kho tsis hais txog ntshav siab.

Cov Kev Ntsuas Amprilana

• lub plawv tsis ua hauj lwm (mob ntev)
• ntshav siab,
• mob rau cov hlab ntshavlub siab.

Kev taw qhia rau kev siv hauv cov neeg mob nrog mob ntshav qab zib: txiv neeb.

Cov Yuav Tsum Muaj

• kev tiv thaiv tsis haum rau lub Cheebtsam
• lub plawv kho mob (txo, aortic, ua ke),
• pub niam mis,
• cardiomyopathy,
• lub kaw lus mob pathology,
• hyperaldosteronism,
• cev xeeb tub,
• hnub nyoog txog 18 xyoo.

Sab sij huam

Feem ntau, cov teev ntshav nce siab rau qhov sau,syncope, mob taub hau zoo li mob taub hau, hnoos qhuav, bronchospasmdaim tawv nqaij ua pob, ua kom tsis pom tseeb mob plab thiab pancreatitis nrog kev nce ntxiv hauv cov concentration ntawm cov enzymes, mob hauv cov pob qij txha thiab cov leeg.

Tsawg muaj arrhythmialub plawv dhia angina pectorismuaj teeb meem los ntawm myocardial infarction, Raynaud's syndrome, vasculitis, astheno-depressive syndrome nrog pw tsaug zog, hloov ischemic tawm tsam thiab mob stroke, impotence, kev ua haujlwm tsis zoo hauv lub raum nrog kev nce siab kev tsim yeej thiab urea hauv cov zis kev fab tshuaj tsis haumhloov pauv hauv chav ntsuas hauv daim ntawv ntawm neutropenia, erythropenia.

Nrog qhov kev vam meej ntawm qhov hnyav ntawm qhov tshwm sim tsis zoo, nws raug nquahu kom sab laj nrog tus kws kho mob thiab txiav txim siab tsis noj tshuaj Amprilan ib ntus.

Tso tawm daim ntawv thiab muaj pes tsawg leeg

Lub ntsiab lus tseem ceeb ntawm Amprilan yog ramipril.

Ntu cov khoom xyaw muaj nyob hauv cov ntsiav tshuaj: croscarmellose sodium, pregelatinized hmoov txhuv nplej siab, sodium stearyl fumarate, sodium bicarbonate, lactose monohydrate, dyes.

Muaj kev siv tshuaj: 1.25 mg, 2.5 mg, 5 mg thiab 10 mg ntawm ramipril hauv ib ntsiav tshuaj.

Amprilan yog tsim nyob rau hauv cov ntsiav tshuaj (7 lossis 10 ntsiav tshuaj hauv ib lub hlwv) oval nrog ib qhov chaw tiaj tiaj thiab lub ntsej muag. Cov xim ntawm cov ntsiav tshuaj txawv raws qhov ntau npaum li cas ntawm cov tshuaj: dawb lossis yuav luag dawb (1.25 mg thiab 10 mg txhua), lub teeb daj (2.5 mg txhua), paj yeeb sib xyaw (5 mg txhua),

Pharmacological kev txiav txim

Cov Tshuaj Hauv Tshuaj Amprilan yog ACE ua rau ntev. Angiotensin-hloov mus rau enzyme ua kom hloov siab ntawm kev hloov pauv ntawm angiotensin II los ntawm angiotensin I, zoo ib yam li kinase - ib qho enzyme uas ua kom nrawm tawg ntawm bradykinin. Raws li qhov tshwm sim ntawm thaiv ntawm ACE los ntawm Amprilan, cov ntsiab lus ntawm angiotensin II poob qis, kev ua si ntawm renin hauv cov ntshav plasma nce ntxiv, qhov kev ua ntawm bradykinin thiab zus tau ntawm aldosterone nce, uas ua rau muaj kev nce ntxiv hauv cov ntsiab lus potassium hauv cov ntshav.

Amprilan muaj antihypertensive thiab hemodynamic cuam tshuam vim yog nthuav cov hlab ntshav thiab txo lawv tag nrho tawm tsam. Hauv qhov no, lub plawv hloov tsis hloov. Qhov poob qis hauv lub siab tom qab siv ib zaug ntawm Amprilan yog pom tom qab 1-2 teev, tom qab 3-6 teev txoj kev kho kom zoo mus txog qhov siab thiab kav ntev li 24 teev.

Nrog rau kev kho mob ntev ntev nrog rau cov tshuaj, sab laug ventricular hypertrophy txo qis, thaum tsis muaj qhov cuam tshuam rau lub siab kev ua haujlwm.

Cov Tshuaj Pharmacokinetics

Cov tshuaj nquag muaj kev cuam tshuam sai heev los ntawm cov hnyuv (qhov ceev tsis yog nyob ntawm qhov khoom noj). Ib teev tom qab thov, qhov siab tshaj plaws ntawm cov tshuaj nquag hauv cov ntshav tau tiav. Txog li 73% ntawm ramipril khi rau cov ntshav plasma protein.

Cov tshuaj tawg rau hauv lub siab, ua rau lub zog metabolite ramiprilat (qhov kev ua haujlwm ntawm tom kawg yog 6 npaug siab dua qhov kev ua haujlwm ntawm ramipril nws tus kheej) thiab lub zog tsis sib xyaw diketopiperazine. Qhov siab tshaj plaws ntawm ramiprilat nyob rau hauv cov ntshav tau kuaj pom 2-4 teev tom qab siv tshuaj, qhov chaw ruaj khov thiab tsis tu ncua kev kho mob nyob rau 4 hnub ntawm kev kho mob. Li ntawm 56% ntawm ramiprilat khi rau ntshav cov protein.

Txog li 60% ntawm ramipril thiab ramiprilat raug tso tawm los ntawm lub raum hauv daim ntawv ntawm cov tshuaj metabolites, tsawg dua 2% ntawm ramipril raug tshem tawm ntawm lub cev tsis hloov pauv. Ib nrab-lub neej ntawm ramiprilat yog los ntawm 13 txog 17 teev, ramipril - 5 teev.

Nrog kev ua haujlwm tsis zoo hauv lub raum, tus nqi ntawm kev nthuav tawm ntawm ramipril thiab metabolites poob qis. Hauv cov neeg mob uas muaj daim siab tsis txaus, kev hloov pauv ntawm ramipril rau ramiprilat qeeb, cov ntsiab lus ntawm ramipril hauv cov ntshav cov ntshav tau nce.

Tsuas tshuaj thiab tswj hwm

Cov ntsiav tshuaj yuav noj ntawm qhov ncauj, tsis hais txog kev noj mov, tsis txhob zom, haus dej kom ntau.

Cov ntau npaum ntawm cov tshuaj yog xaiv los ntawm tus kws kho mob ib leeg zuj zus rau txhua tus neeg mob, coj mus rau hauv tus account qhov ntsuas, kev zam ntawm cov tshuaj, concomitant kab mob thiab tus neeg mob lub hnub nyoog. Thaum xaiv cov koob tshuaj, qhov ntsuas kev ntsuas ntshav siab yuav tsum raug coj los txiav txim. Qhov siab tshaj plaws tau tso cai ntau npaum li cas ntawm cov tshuaj rau txhua hom pathologies yog 10 mg rau ib hnub. Lub chav kawm ntawm kev kho yog feem ntau ntev, kuj tsim los ntawm kws kho mob.

Nrog rau cov hlab ntsha o Qhov tshuaj pom zoo thawj zaug yog 2.5 mg ib hnub ib zaug. Yog tias tsim nyog, cov koob tshuaj tuaj yeem muab ob npaug hauv 7-14 hnub.

Hauv lub plawv tsis ua haujlwm thawj zaug kev pom zoo ntawm cov tshuaj yog 1.25 mg (tuaj yeem muab ob npaug tom qab 1-2 lub lis piam).

Nrog lub plawv nres, uas tau tshwm sim 2-9 hnub tom qab mob myocardial infarction, nws raug pom zoo kom noj 5 mg ntawm Amprilan ib hnub - 2.5 mg thaum sawv ntxov thiab yav tsaus ntuj. Yog hais tias thaum lub sij hawm kho lub siab poob qis, qhov tshuaj tsuas yog halved (1.25 mg ob zaug ib hnub). Tom qab 3 hnub, cov koob tshuaj tau nce siab dua. Yog tias noj cov tshuaj hauv 2.5 koob tshuaj ob zaug ib hnub yog qhov kev mob tsis zoo rov qab los ntawm tus neeg mob, kev kho nrog Amprilan yuav tsum tau tshem tawm.

Mob nqaij hlav (nrog diffuse pathologies ntawm ob lub raum thiab ntshav qab zib).Qhov pom zoo kom pib lub koob tshuaj yog 1.25 mg rau ib hnub. Txhua 14 hnub, qhov kev muab tshuaj yog tau ob npaug txog thaum kev saib xyuas txij nkawm 5 mg ib hnub twg los txog.

Kev tiv thaiv ntawm lub plawv tsis ua haujlwm tom qab myocardial infarction. Thaum pib theem ntawm kev kho mob kom haum, Amprilan 2.5 mg yog tshuaj rau ib ntsiav tshuaj ib hnub. Tom qab ib lub lim tiam, cov koob tshuaj tau nce rau 5 mg ib hnub twg, tom qab lwm 2-3 lub lis piam - txog kev tswj hwm ntawm 10 mg ib hnub ib zaug.

Nrog arterial occlusion thiab tom qab mob caj dab bypass phais Amprilan noj 2,5 mg ib hnub ib zaug rau 7 hnub. Tom qab ntawd, rau 2-3 lub lis piam, cov tshuaj raug muab ntawm 5 mg rau ib hnub, tom qab nws cov koob tshuaj tau nce ntxiv ob zaug ntxiv - txog 10 mg rau ib hnub.

Cov lus qhia tshwj xeeb

1. Rau cov neeg mob uas ua tsis taus lub raum tsis ua haujlwm, thawj koob tshuaj Amprilan yuav tsum yog 1.25 mg, thiab qhov siab tshaj plaws niaj hnub noj yuav tsum yog 5 mg.
2. Rau cov neeg mob uas lub siab tsis ua haujlwm, qhov tshuaj tiv thaiv thawj zaug yog 1.25 mg, qhov siab tshaj plaws niaj hnub noj yog 2.5 mg.
3. Yog tias Amprilan tau sau tseg rau cov neeg mob noj cov tshuaj diuretics, tshem tawm lossis txo qhov ntau npaum ntawm kev tso tshuaj diuretics yuav tsum tau ua. Nws tseem yuav tsum tau soj ntsuam tas li ntawm cov mob ntawm cov neeg mob ntawd, tshwj xeeb cov neeg laus (laus dua 65 xyoos).
4. Amprilan tau noj nrog ceev faj hauv cov neeg mob uas muaj cov kab mob ntawm cov kab mob sib txuas, mob ntshav qab zib mellitus, tsis txaus ntseeg angina pectoris.
5. Cov tshuaj muaj qhov tsis zoo rau cov menyuam hauv plab (hypoplasia ntawm lub ntsws thiab pob txha ntawm pob txha taub hau, hyperkalemia, ua haujlwm tsis zoo hauv lub raum) thiab yog contraindicated rau cov poj niam cev xeeb tub. Ua ntej tso tawm ntawm Amprilan, nws yog ib qho tseem ceeb rau cov poj niam ntawm lub hnub nyoog yug menyuam kom tsis pub xeeb menyuam.
6. Thaum noj cov Amprilan thaum lactation, kev pub niam mis yuav tsum tau lawb tawm.

Cov lus thiab cov xwm txheej ntawm kev cia

Khaws cov tshuaj ntawm qhov kub tsis tshaj 25 ° C, hauv qhov chaw tiv thaiv los ntawm noo noo thiab tshav ntuj, nkag tsis tau rau menyuam yaus. Lub txee lub neej ntawm Amprilan ntsiav tshuaj yog 3 xyoos. Tom qab hnub uas tau teev nyob rau hauv pob, cov tshuaj tsis tuaj yeem nqa mus.

Cov qauv ntawm cov qauv ntawm Amprilan (cov tshuaj uas muaj cov tshuaj zoo ib yam) yog:

3D duab

Tsuas tshuaj thiab tswj hwm

Sab hauv tsis hais lub sijhawm noj mov (i.e. ntsiav tshuaj tuaj yeem noj ob zaug ua ntej lossis sijhawm lossis tom qab noj mov), haus dej ntau (1/2 khob). Tsis txhob zom lossis zom tej ntsiav tshuaj ua ntej noj.

Cov koob tshuaj tau xaiv nyob ntawm kev kho mob kom haum thiab ua siab ntev rau cov neeg mob rau cov tshuaj.

Kev kho nrog Amprilan usually feem ntau yog ntev, thiab lub sijhawm hauv txhua kis tau txiav txim los ntawm tus kws kho mob.

Tshwj tsis yog muaj lwm qhov sau tseg, tom qab ntawd nrog lub raum thiab cov hlab ntsws ua haujlwm, kev noj tshuaj hauv qab no raug pom zoo.

Feem ntau qhov pib noj yog 2.5 mg / hnub thaum sawv ntxov. Yog tias thaum noj Amprilan ® ntawm qhov tshuaj no 3 lub lis piam lossis ntau dua, nws tsis tuaj yeem ua kom ntshav siab li qub, ces cov koob tshuaj yuav nce ntxiv rau 5 mg / hnub. Yog tias qhov koob tshuaj 5 mg yuav siv tsis tau txaus, tom qab 2-3 lub lis piam nws tseem tuaj yeem muab ob npaug rau qhov siab tshaj qhov xav tau txhua hnub ntawm 10 mg.

Raws li lwm txoj hauv kev ntxiv cov koob tshuaj rau 10 mg / hnub nrog kev tsis txaus los tiv thaiv kev tiv thaiv kab mob ntawm ib koob tshuaj txhua hnub ntawm 5 mg, nws muaj peev xwm ntxiv lwm cov tshuaj tiv thaiv kab mob rau kev kho mob, tshwj xeeb diuretics lossis BKK.

Qhov pom zoo kom pib koob yog 1.25 mg / hnub. Nyob ntawm tus neeg mob cov lus teb rau txoj kev kho mob, cov koob tshuaj yuav nce ntxiv.

Nws raug nquahu kom txhaj koob tshuaj ob zaug nrog ib nrab sijhawm 1-2 asthiv. Yog tias koj xav noj cov tshuaj txhua hnub ntawm 2.5 mg lossis siab dua, nws tuaj yeem siv ib zaug ib hnub, lossis faib ua ob zaug.

Qhov siab tshaj plaws kev pom zoo txhua hnub koob tshuaj yog 10 mg.

Ntshav qab zib los yog tsis mob ntshav qab zib nephropathy

Qhov pom zoo kom pib koob yog 1.25 mg / hnub. Cov koob tshuaj yuav nce ntxiv txog 5 mg / hnub. Nrog rau cov xwm txheej no, cov koob tshuaj ntau dua 5 mg / hnub tseem tsis tau kawm txaus hauv kev tswj xyuas cov neeg mob.

Txo txoj kev pheej hmoo ntawm kev tsim myocardial infarction, mob hlab ntsha tawg, lossis lub plawv tuag rau cov neeg mob uas muaj kev pheej hmoo siab

Qhov pom zoo kom pib noj yog 2.5 mg / hnub.

Nyob ntawm tus neeg mob lub siab ntev rau Amprilan ®, cov koob tshuaj yuav maj mam nce ntxiv.

Nws raug nquahu kom txhaj koob tshuaj ob zaug ntxiv tom qab 1 lub lim tiam ntawm kev kho mob, thiab dhau 3 asthiv, nce nws mus rau kev tswj hwm ib txwm muaj li ntawm 10 mg / hnub.

Kev siv cov koob tshuaj ntau dua 10 mg / hnub hauv kev tswj xyuas cov chaw kho mob tsis tau kawm txaus. Kev siv cov tshuaj hauv cov neeg mob nrog Cl creatinine tsawg dua 0.6 ml / sec tsis nkag siab zoo.

Soj ntsuam lub plawv tsis ua haujlwm uas tau tsim nyob rau thawj ob peb hnub (txij li 2 txog 9 hnub) tom qab mob myocardial infarction

Qhov pom zoo kom pib koob tshuaj yog 5 mg / hnub, muab faib ua 2 koob tshuaj 2.5 mg (noj thaum sawv ntxov thiab yav tsaus ntuj). Yog tias tus neeg mob tsis zam lub koob tshuaj no thaum pib (saib ntshav siab dhau heev), ces nws raug nquahu kom noj 1.25 mg 2 zaug ib hnub rau 2 hnub.

Tom qab ntawd, nyob ntawm kev tawm tsam los ntawm tus neeg mob, cov koob tshuaj yuav raug nce ntxiv. Nws raug nquahu tias cov koob tshuaj nrog nws nce ob npaug nrog nruab nrab ntawm 1-3 hnub. Ntxiv mus, tag nrho cov koob tshuaj txhua hnub, uas tau muab faib ua 2 zaug, tuaj yeem siv tau ib zaug.

Qhov koob tshuaj ntau tshaj plaws yog 10 mg.

Tam sim no, kev paub hauv kev kho mob rau cov neeg mob lub plawv tsis ua haujlwm siab (III - IV ua haujlwm tau zoo raws li kev faib tawm) NYHA) uas tshwm sim tam sim ntawd tom qab mob myocardial infarction tsis txaus. Yog tias cov neeg mob zoo li no txiav txim siab mus kho mob nrog Amprilan ®, nws raug nquahu tias kev kho mob pib nrog kev siv qis tshaj - 1.25 mg / hnub, thiab kev saib xyuas tshwj xeeb yuav tsum tau noj nrog txhua qhov nce ntxiv.

Cov pab pawg neeg tshwj xeeb

Lub raum khiav tsis zoo. Nrog Cl creatinine los ntawm 50 txog 20 ml / min / 1.73 m 2, qhov kev pib thawj hnub feem ntau yog 1.25 mg. Qhov nyiaj pab ntau tshaj rau niaj hnub noj yog 5 mg.

Qhov ua tsis tiav kho cov kua thiab cov roj ntsha, cov ntshav khov rau lub plawv, thiab tseem yog tias qhov ntshav nce siab ntau dhau ntawm qee qhov kev pheej hmoo (piv txwv, nrog cov mob loj atherosclerotic ntawm cov hlab ntshav hlab ntshav thiab hlab hlwb). Qhov kev txhaj tshuaj thawj zaug yog txo rau 1.25 mg / hnub.

Cov tshuaj kho mob yav dhau los. Yog tias ua tau, diuretics yuav tsum tso tseg 2-3 hnub (nyob ntawm lub sijhawm ntawm kev ua ntawm kev kho mob) ua ntej pib kho nrog Amprilan ® lossis tsawg kawg txo qhov koob tshuaj diuretics noj. Kev kho mob ntawm cov neeg mob zoo li no yuav tsum tau pib nrog kev txhaj tshuaj qis tshaj plaws ntawm Amprilan / - 1.25 mg / hnub thaum sawv ntxov. Tom qab noj cov tshuaj thawj zaug thiab txhua zaus tom qab nce cov koob tshuaj Amprilan ® thiab / lossis cov diuretics, cov neeg mob yuav tsum nyob hauv kev saib xyuas mob tsawg kawg yog 8 teev kom tsis txhob muaj kev tiv thaiv kev tiv thaiv hypotensive.

Muaj hnub nyoog tshaj 65 xyoos. Qhov kev txhaj tshuaj thawj zaug yog txo rau 1.25 mg / hnub.

Lub siab ua haujlwm tsis zoo. Cov tshuaj tiv thaiv ntawm cov ntshav siab rau noj Amprilan ® tuaj yeem nce ntxiv (los ntawm kev txo qis ramiprilat excretion), lossis ua kom tsis muaj zog (vim txo qis ntawm kev hloov pauv tsis ua haujlwm mus rau ramiprilat kom nquag ua haujlwm ramiprilat). Yog li, thaum pib kho yuav tsum muaj kev saib xyuas mob nkeeg. Qhov siab tshaj plaws tau tso cai rau noj txhua hnub yog 2.5 mg.

Chaw tsim tshuaj paus

JSC “Krka, hnub, Novo mesto”. Marješka cesta 6, 8501 Novo mesto, Slovenia.

Thaum ntim khoom thiab / lossis ntim khoom ntawm Lavxias teb sab chaw ua lag luam, nws yuav tsum muaj kev sau npe: "KRKA-RUS" LLC. 143500, Russia, Moscow Cheeb Tsam, Istra, ul. Moscow, 50.

Xov Tooj: (495) 994-70-70, fev: (495) 994-70-78.

Tus sawv cev chaw ua haujlwm ntawm Krka, hnub, Novo mesto JSC hauv Lavxias Federation / koomhaum lees txais kev tsis txaus siab ntawm cov neeg siv khoom: 125212, Moscow, Golovinskoye sh., 5, bldg. 1, pem teb 22.

Xov Tooj: (495) 981-10-95, fev (495) 981-10-91.

Cov Tshuaj Pharmacokinetics

Tom qab qhov ncauj tswj hwm ntawm ramipril, Amprilan nrawm nrawm los ntawm kev mob plab (lub plab zom mov) ntawm qib 50-60%. Kev pub ib txhij nrog cov zaub mov kom txo qis nws nqus, tab sis tsis cuam tshuam rau qhov ntau ntawm cov tshuaj uas tau nkag mus rau hauv cov hlab ntshav. Raws li cov txiaj ntsig ntawm presystemic biotransformation / ua haujlwm ntawm ramipril, feem ntau yog nyob hauv daim siab los ntawm hydrolysis, ramiprilat (ib qho kev hloov pauv ntawm lub cev, 6 lub sijhawm nquag tshaj li ramipril hauv kev sib piv rau ACE inhibition) thiab diketopiperazine (ib qho metabolite uas tsis muaj pharmacological kev ua si) raug tsim. Ntxiv mus, diketopiperazine yog sib xyaw nrog glucuronic acid, thiab ramiprilat yog glucuronated thiab metabolized rau diketopiperazinic acid.

Lub bioavailability ntawm ramipril nyob ntawm qhov ncauj noj thiab nws txawv ntawm 15% (rau 2.5 mg) txog 28% (rau 5 mg).Lub bioavailability ntawm ramiprilat tom qab qhov ncauj tswj hwm ntawm 2.5 mg thiab 5 mg ntawm ramipril yog

45% ntawm qhov ntsuas no tau txais tom qab kev tso dej ntawm cov tshuaj tib.

Tom qab noj Amprilan sab hauv, qhov siab tshaj plaws plasma concentration ntawm ramipril tau mus txog tom qab 1 h, ramiprilat - tom qab 2-4 teev. Qhov kev txo qis ntawm ramiprilat hauv ntshav tau tshwm sim hauv ntau theem: theem ntawm kev faib tawm thiab kev nthuav tawm nrog T_1/2 (Ib nrab-lub neej)

3 h, theem nrab nrog T_1/2

15 h thiab theem kawg nrog cov ntsiab lus tsawg kawg ntawm ramiprilat hauv ntshav thiab T_1/2

4-5 hnub, uas yog vim qhov qeeb tawm ntawm ramiprilat los ntawm kev sib raug zoo nrog ACE receptors. Txawm hais tias lub sijhawm no nyob rau theem kawg, noj ramipril qhov ncauj 2.5 mg lossis ntau dua ib hnub ib zaug hauv ib tus tuaj yeem ua tiav qhov sib luag plasma concentration ntawm ramiprilat tom qab 4 hnub ntawm kev siv tshuaj. Thaum kawg tswj hwm ntawm Amprilan siv tau T_1/2 nyob ntawm koob tshuaj thiab txawv ntawm 13 txog 17 teev

Ramipril khi rau cov ntshav plasma ntawm thaj tsam li ntawm 73%, ramiprilat - 56%.

Tom qab qhov ncauj tswj hwm ntawm ramipril, daim ntawv lo nrog lub xov tooj cua isotope, hauv ib koob tshuaj 10 mg, nce txog 39% ntawm kev zom zaws yog tawm hauv txoj hnyuv, kwv yees li 60% yog tawm los ntawm lub raum. Hauv cov neeg mob nrog cov kua tsib cov kua dej ua rau muaj txiaj ntsig ntawm kev noj 5 mg ntawm ramipril sab hauv ob lub raum thiab dhau los ntawm cov hnyuv, yuav luag tib cov nyiaj ntawm ramipril thiab nws cov khoom siv tiv thaiv kab mob tawm thaum thawj 24 teev tom qab kev tswj hwm.

Kwv yees li 80-90% ntawm cov tshuaj tshwm sim hauv cov zis thiab cov kua tsib tau pom tias yog ramiprilat thiab nws cov khoom noj. Ramipril glucuronide thiab diketopiperazine ua tau

10-20% ntawm tag nrho cov koob tshuaj, thiab unipabolized ramipril -

Hauv kev tshawb fawb hauv cov tsiaj txhu, nws pom tias ramipril hla mus rau hauv niam cov kua mis.

Hauv cov neeg mob uas lub raum tsis ua haujlwm, creatinine tshem tawm (CC) tsawg dua 60 ml / min tshem tawm ramiprilat thiab nws cov metabolites. Qhov no ua rau muaj kev nce ntxiv hauv lawv cov ntshav plasma thiab qhov qeeb qeeb hauv kev sib piv nrog cov neeg mob uas lub raum tsis ua haujlwm.

Kev noj tshuaj siab siab ntawm ramipril (10 mg) thaum tsis pom lub siab ua haujlwm ua rau txo qis hauv presystemic metabolism ntawm ramipril thiab kev ua qeeb qeeb ntawm nws lub zog metabolite.

Hauv cov neeg tuaj yeem noj qab nyob zoo thiab hauv cov neeg mob uas mob ntshav ncig, tsis muaj qhov tseem ceeb hauv thaj chaw kho mob ntawm tus mob ramipril thiab ramiprilat tau pom los ntawm kev kho ob lub lis piam nrog Amprilan ntawm koob tshuaj 5 mg ib hnub. Tom qab kev kawm ob lub lim tiam zoo sib xws, cov neeg mob lub plawv tsis ua hauj lwm tau 1.5-1.8-nce ntxiv ntawm ramiprilat qib hauv cov ntshav plasma thiab thaj chaw hauv qab qhov nkhaus-sijhawm nkhaus (AUC).

Cov chaw muag tshuaj ntawm ramipril thiab ramiprilat hauv cov neeg laus noj qab haus huv cov neeg laus uas muaj hnub nyoog 65-75 xyoo tsis txawv tus sib txawv ntawm cov hluas pab dawb noj qab haus huv.

Cov chaw muag tshuaj

Cov Tshuaj Hauv Tshuaj

Lub zog metabolite ntawm ramipril, tsim los ntawm qhov kev nqis tes ua ntawm "daim siab" enzymes, ramiprilat yog ACE inhibitor ntev (ACE txhais: kininase II, dipeptidyl carboxy dipeptidase Kuv). ACE hauv cov ntshav thiab cov nqaij mos ua kom muaj kev hloov pauv ntawm angiotensin I mus rau angiotensin II, uas muaj vasoconstrictor effect, thiab tawg ntawm bradykinin, uas muaj cov nyhuv vasodilating. Yog li no, thaum noj cov ramipril sab hauv, qhov tsim ntawm angiotensin II poob qis thiab bradykinin ntau zuj zus, uas ua rau vasodilation thiab txo cov ntshav siab (BP). Ramipril-ntxias ua kom muaj ntau ntxiv hauv kev ua haujlwm ntawm kallikrein-kinin cov ntshav hauv ntshav thiab cov nqaij nrog kev ua haujlwm ntawm cov kab mob prostaglandin thiab qhov nce ntawm cov synthesis ntawm prostaglandins, uas txhawb kev tsim ntawm nitric oxide (N0) hauv endotheliocytes, ua rau nws cov nyhuv cardioprotective.

Angiotensin II stimulates zus ntawm aldosterone, yog li noj ramipril ua rau txo qis ntawm kev tso cai ntawm aldosterone thiab nce cov ntsiab lus ntawm potassium hauv cov ntshav dej.

Nrog rau qhov kev txo qis ntawm cov kev xav ntawm angiotensin II hauv cov ntshav ntshav, nws cov nyhuv inhibitory nyob rau kev zais ntawm renin los ntawm hom kev tawm tsam tsis zoo yog tshem tawm, uas ua rau muaj kev nce ntxiv ntawm plasma renin kev ua si.

Nws xav tias qhov kev txhim kho ntawm qee qhov tshwm sim tsis zoo (qhov tseem ceeb, "qhuav" hnoos) yog txuam nrog kev nce hauv cov kev ua ntawm bradykinin.

Hauv cov neeg mob ntshav siab noj ramipril ua rau txo qis ntshav siab hauv "dag" thiab "sawv" haujlwm yam tsis muaj kev txwv txiav rau lub plawv dhia (HR). Ramipril txo qis tag nrho peripheral vascular tsis kam (OPSS), suab tsis ua rau muaj kev hloov pauv ntawm cov ntshav raum thiab cov ntshav txhaws. Cov nyhuv antihypertensive pib tshwm 1 rau 2 teev tom qab kev noj ib zaug ntawm cov tshuaj, ncav nws cov nqi ntau tshaj plaws tom qab 3-6 teev, thiab kav ntev li 24 teev. Nrog txoj kev noj tshuaj Amprilan, cov nyhuv antihypertensive yuav maj mam nce ntxiv, feem ntau yuav ruaj khov nyob rau ntawm 3-4 lub lim tiam ntawm kev siv tas li thiab tom qab ntawd tawm tsam mus ntev. Kev txiav tawm tam sim ntawd tsis siv tshuaj tiv thaiv tsis ua rau muaj kev cuam tshuam sai thiab tseem ceeb rau cov ntshav siab (tsis muaj "tshem tawm" syndrome).

Hauv cov neeg mob uas mob ntshav tawm tsam, ramipril qeeb txoj kev txhim kho thiab kev hloov kho ntawm myocardial hypertrophy thiab leeg ntshav phab ntsa.

Hauv cov neeg mob uas muaj lub plawv tsis ua haujlwm ntev (CHF) ramipril txo OPSS (txo kev pab cuam tom qab lub siab), ua kom lub peev xwm ntawm txoj hlab xaib thiab txo qhov txhaws ntawm sab laug ventricle (LV), uas, raws li, ua rau txo qis ntawm kev thauj khoom hauv lub siab. Hauv cov neeg mob no, thaum noj cov tshuaj ramipril, muaj qhov nce hauv plawv ntau lawm, LV ejection feem (LVEF) thiab kev txhim kho qoj ib ce ua kom siab dua.

Nrog mob ntshav qab zib thiab tsis mob ntshav qab zib nephropathy noj ramipril txo qis tus nqi ntawm qhov muaj mob ntawm lub raum tsis ua haujlwm thiab qhov pib ntawm qhov kawg ntawm lub raum tsis ua haujlwm thiab, yog li, txo qhov xav tau rau kev hloov kho hemodialysis lossis lub raum. Hauv cov theem pib ntawm tus mob ntshav qab zib lossis mob ntshav qab zib nephropathy, ramipril txo qhov tshwm sim ntawm albuminuria.

Hauv cov neeg mob uas muaj kev pheej hmoo siab los ntawm kev mob plawv vim yog voos txhab (kuaj mob plawv, keeb kwm ntawm kab mob txha caj qaum, keeb kwm ntawm mob hlab ntsha tawg) lossis ntshav qab zib mellitus muaj tsawg kawg yog ib qho kev pheej hmoo ntxiv (microalbuminuria, ntshav siab, nce ntxiv ntawm qhov kev txiav txim siab ntawm tag nrho cov roj (OXc), txo qis qhov concentration ntawm cov roj lipoprotein ntau (cholesterol), HDP-C, haus luam yeeb) qhov sib ntxiv ntawm ramipril rau cov kev kho mob txo qis Nws piav qhia qhov tshwm sim ntawm myocardial infarction, mob hlab ntsha tawg, thiab lub plawv tuag. Ntxiv rau, ramipril txo tag nrho cov neeg tuag, nrog rau cov kev xav kom rov ua kom zoo li qub thiab ua rau qeeb qeeb ntawm qhov pib lossis mob zuj zus ntawm lub plawv tsis ua.

Hauv cov neeg mob lub plawv tsis ua hauj lwm nrog cov kab mob kev soj ntsuam uas tau tsim hauv thawj hnub ntawm tus mob myocardial infarction (2-9 hnub), kev siv cov ramipril, pib ntawm hnub 3 mus rau 10 hnub ntawm tus mob myocardial infarction, txo kev tuag (los ntawm 27%), txoj kev pheej hmoo sai sai kev tuag (los ntawm 30%), qhov kev pheej hmoo ntawm lub plawv dhia tsis txaus mus rau qhov tsis txaus (III-IV ua haujlwm hauv chav kawm raws li NYHA kev faib tawm) / kev kho-tiv thaiv (los ntawm 23%), qhov yuav ua rau muaj kev mus pw tom tsev kho mob vim yog kev txhim kho lub plawv tsis ua haujlwm (los ntawm 26%).

Hauv cov neeg mob dav dav, nrog rau cov neeg mob ntshav qab zib mellitus, ob qho tib si nrog kev mob ntshav siab thiab nrog cov ntshav siab, ramipril txo txoj kev pheej hmoo ntawm nephropathy thiab qhov tshwm sim ntawm microalbuminuria.

Cov Tshuaj Pharmacokinetics

Tom qab kev tswj hwm ntawm qhov ncauj, ramipril yog nqus tau sai sai ntawm txoj hnyuv (50-60%). Noj noj kom tsawg nws nqus, tab sis tsis cuam tshuam rau qhov ua tiav ntawm kev nqus.

Ramipril yauv ua rau lub cev muaj zog presystemic metabolism / ua kom zoo (feem ntau yog nyob rau hauv daim siab los ntawm hydrolysis), uas ua rau nws tsuas yog siv cov metabolite, ramiprilat, uas nws ua haujlwm nrog hwm ACE inhibition yog kwv yees li 6 npaug siab dua qhov kev ua haujlwm ntawm ramipril. Tsis tas li ntawd, raws li kev tshwm sim ntawm ramipril metabolism, diketopiperazine, uas tsis muaj pharmacological kev ua si, yog tsim, uas yog tom qab ntawd ua ke nrog glucuronic acid, ramiprilat kuj tseem glucuronated thiab metabolized rau diketopiperazinic acid.

Lub bioavailability ntawm ramipril tom qab kev tswj hwm ntawm qhov ncauj li ntawm 15% (rau ib koob tshuaj 2.5 mg) txog 28% (rau ib koob tshuaj 5 mg). Lub bioavailability ntawm lub nquag metabolite, ramiprilat, tom qab noj ntawm 2.5 mg thiab 5 mg ntawm ramipril yog kwv yees li 45% (piv nrog nws cov bioavailability tom qab kev tswj hwm hauv tib cov tshuaj).

Tom qab noj ramipril sab hauv, qhov siab tshaj plaws ntshav plasma ntawm ramipril thiab ramiprilat tau mus txog tom qab 1 thiab 2 txog 4 teev, feem. Kev poob qis hauv lub plasma concentration ntawm ramiprilat tshwm sim nyob rau hauv ntau theem: kev faib khoom thiab kev nthuav tawm theem nrog ib nrab-lub neej (T1 / 2) ntawm ramiprilat kwv yees li 3 teev, tom qab ntawd cov theem nrab nrog T1 / 2 ramiprilat, kwv yees li 15 teev, thiab theem kawg nrog qhov muaj zog tsawg ntawm ramiprilat hauv ntshav thiab T1 / 2 ramiprilat, kwv yees li 4-5 hnub. Qhov theem kawg no yog vim qhov qeeb tawm ntawm ramiprilat los ntawm kev sib raug zoo nrog ACE receptors. Txawm hais tias tau ua kom tiav lub sijhawm ntev nrog ib zaug tshuaj noj ntawm ramipril qhov ncauj ntawm qhov koob tshuaj 2.5 mg lossis ntau dua, qhov sib luag ntawm cov ntshav ntshav ntawm ramiprilat tau mus txog tom qab kwv yees li 4 hnub ntawm kev kho mob. Nrog rau chav kawm siv cov tshuaj "zoo" T1 / 2 nyob ntawm seb qhov koob tshuaj yog 13-17 teev.

Kev sib txuas lus nrog cov ntshav plasma protein yog kwv yees li 73% rau ramipril, thiab 56% rau ramiprilat.

Tom qab kev tswj hwm ntawm cov dej khov, qhov ntim ntawm ramipril thiab ramiprilat yog kwv yees li 90 L thiab kwv yees li 500 L, feem.

Tom qab kev noj cov tshuaj ramipril (10 mg) sau npe nrog lub xov tooj cua isotope, 39% ntawm lub radioactivity tau tawm ntawm txoj hnyuv thiab kwv yees li 60% los ntawm lub raum. Tom qab tso cov tshuaj ramipril, 50-60% ntawm cov koob tshuaj yog pom hauv cov zis hauv daim ntawv ntawm ramipril thiab nws cov tshuaj tiv thaiv. Tom qab kev tso cov tshuaj ramiprilat, kwv yees li 70% ntawm cov koob tshuaj tau pom nyob hauv cov zis hauv daim ntawv ntawm ramiprilat thiab nws cov metabolites, hauv lwm cov lus, nrog kev tswj hwm ntawm ramipril thiab ramiprilat, ib feem tseem ceeb ntawm cov koob tshuaj tau tawm hauv cov hnyuv nrog bile, hla lub raum (50% thiab 30%, feem). Tom qab lub qhov ncauj tswj hwm ntawm 5 mg ntawm ramipril nyob rau hauv cov neeg mob nrog cov kua tsib lub raj dej, yuav luag tus nqi ntawm ramipril thiab nws cov metabolites yog txaws los ntawm lub raum thiab dhau los ntawm txoj hnyuv hauv thawj 24 teev tom qab kev coj.

Txog 80 - 90% ntawm cov metabolites hauv cov zis thiab cov kua tsib tau pom tias yog ramiprilat thiab ramiprilat metabolites. Ramipril glucuronide thiab ramipril diketopiperazine tus account rau kwv yees li 10-20% ntawm tag nrho cov nyiaj, thiab cov ntsiab lus tsis muaj npe ntawm ramipril nyob hauv cov zis yog kwv yees li 2%. Cov kev tshawb fawb tsiaj tau pom tias ramipril ua rau tawm hauv niam cov kua mis.

Yog tias lub plab tsis zoo ua haujlwm nrog creatinine tshem tawm (CC) tsawg dua 60 ml / min, qhov kev tshem tawm ntawm ramiprilat thiab nws cov metabolites los ntawm lub raum ua rau qis dua. Qhov no ua rau muaj qhov nce ntxiv ntawm plasma concentration ntawm ramiprilat, uas ua rau qeeb qeeb qeeb dua li cov neeg mob uas lub raum tsis ua haujlwm.

Thaum noj ramipril hauv siab (10 mg), lub siab ua haujlwm tsis zoo ua rau cov qeeb qeeb hauv presystemic metabolism ntawm ramipril kom nquag ua haujlwm ramiprilat thiab qeeb qeeb ntawm ramiprilat. Hauv cov neeg tuaj yeem noj qab haus huv thiab nyob rau hauv cov neeg mob mob ntshav liab, tom qab ob lub lis piam los kho mob nrog ramipril hauv ib koob tshuaj 5 mg txhua hnub, tsis muaj qhov tseem ceeb hauv kev kho mob ntawm ramipril thiab ramiprilat. Hauv cov neeg mob lub plawv tsis ua haujlwm, tom qab ob lub lim tiam ntawm kev kho mob nrog ramipril nyob rau hauv ib koob tshuaj txhua hnub ntawm 5 mg, qhov nce 1.5-1.8-lub sij hawm nce hauv plasma cov ntsiab lus ntawm ramiprilat thiab thaj chaw hauv qab qhov nkhaus-sijhawm nkhaus (AUC) tau sau tseg.

Hauv cov neeg laus noj qab haus huv cov neeg ua haujlwm dawb (65-75 xyoo), cov chaw muag tshuaj ntawm ramipril thiab ramiprilat tsis txawv ntawm cov neeg ua haujlwm pab dawb noj qab haus huv.

Siv thaum cev xeeb tub thiab thaum pub niam mis

Amprilan yog contraindicated thaum cev xeeb tub, vim nws tuaj yeem muaj qhov tsis zoo ntawm cov menyuam hauv plab: kev txhim kho tsis zoo ntawm lub raum ntawm lub cev, txo cov ntshav siab ntawm cov menyuam hauv plab thiab cov menyuam yug tshiab, kev ua haujlwm tsis zoo rau lub raum, hyperkalemia, hypoplasia ntawm cov pob txha pob txha taub hau, hypoplasia ntawm lub ntsws.

Yog li, ua ntej siv cov tshuaj rau hauv cov poj niam ntawm lub hnub nyoog yug menyuam, cev xeeb tub yuav tsum raug cais tawm.

Yog tias tus poj niam tab tom npaj kho cev xeeb tub, tom qab ntawv kho nrog ACE inhibitor yuav tsum tsis ua ntxiv.

Thaum cev xeeb tub thaum kho mob nrog Amprilan, koj yuav tsum tsum tsis txhob noj sai li sai tau thiab hloov tus neeg mob mus rau lwm cov tshuaj, nrog kev siv uas qhov kev pheej hmoo rau tus menyuam yuav tsawg heev.

Yog tias kev kho mob nrog Amprilan tsim nyog thaum lub sijhawm pub niam mis, kev pub mis niam yuav tsum tsis ua mus ntxiv.

Amprilan, cov lus qhia rau kev siv (Txoj kev thiab ntau npaum li cas)

Ramipril yog tshuaj sab hauv kev ywj pheej ntawm kev tau txais zaub mov. Cov ntsiav tshuaj pom zoo kom haus dej kom ntau. Cov tshuaj yog kws kho mob sau los ntawm tus kws kho mob uas xaiv cov tshuaj txaus noj rau hauv tus neeg mob tus mob thiab kam rau ua rau cov tshuaj ntawm cov tshuaj. Nws raug nquahu kom pib noj Amprilan nrog kev txhaj tshuaj me me ntawm 2.5 mg, nrog kev muaj peev xwm nce ntxiv mus rau qhov siab tshaj plaws cov lej - 10 mg. Lub sijhawm ntawm cov tshuaj yog txiav txim los ntawm tus kws kho mob nyob ntawm kev yws thiab cov ntaub ntawv, keeb kwm kev kho mob ceev faj.

Cov lus qhia rau kev siv Amprilan ND thiab NL: 1 ntsiav tshuaj ib hnub. Siv tau koob tshuaj hloov kho thaum kho. Lub sijhawm tiv thaiv ntawm kev kho tsis txwv.

Dosage daim ntawv

Ntsiav tshuaj 1.25 mg, 2.5 mg, 5 mg thiab 10 mg

Ib ntsiav tshuaj muaj

cov tshuaj heev - ramipril 1.25 mg, 2.5 mg, 5 mg, 10 mg,

tus zam: sodium bicarbonate, lactose monohydrate, croscarmellose sodium, pregelatinized hmoov txhuv nplej siab (hmoov nplej 1500), sodium stearyl fumarate (rau kev noj tshuaj ntawm 1.25 mg, 2.5 mg, 5 mg thiab 10 mg),

rau qhov ntau npaum li cas 2.5 mg: cov xim sib xyaw xim PB22886 daj (lactose monohydrate, hlau oxide daj (E 172)),

rau qhov tau txais koob tshuaj 5 mg: cov xim sib xyaw xim PB24899 liab (lactose monohydrate, hlau oxide liab (E 172), hlau oxide daj (E 172))

Ca oval ntsiav tshuaj, los ntawm dawb mus rau yuav luag dawb,

chamfered (rau cov tshuaj ntawm 1.25 mg thiab 10 mg)

Tiaj kheej kheej cov ntsiav tshuaj, lub teeb daj, chamfered (rau qhov ntau npaum li 2.5 mg)

Cov ntsiav tshuaj tiaj tus ntawm cov kheej kheej, cov paj yeeb, nrog cov bevel thiab pom cov kev sib ntxiv (rau qhov ntau npaum 5 mg)

Noj ntau dhau

Cov tsos mob ntawm kev noj tshuaj ntau dhau hwv lawm bradycardia (tsis tshua muaj mem tes), txo qis hauv cov ntshav siab, poob siab lub xeev nrog mob raum tsis ua haujlwm. Cov kev ntsuas thaum maj nrawm noj rau qhov noj tshaj pais plab lavage thiab thov kom raws sijhawmenterosorbents, thiab nrog kev hem thawj ntawm kev poob siab, kev qhia ntawm cov tshuaj uas ua rau muaj ntshav siab ntxiv.

Kev sib txuam

Vasopressor sympathomimetics, ib pawg ntawm cov tshuaj tsis-tshuaj steroidal, corticosteroid cov tshuaj hormones tuaj yeem txo qhov hnyav ntawm cov nyhuv hypotensive raminiprilCov. Txhim kho cov nyhuv hypotensive ntawm cov tshuaj tiv thaiv kab mob, tshuaj tiv thaiv kev ntxhov siab. Kev sib xyaw ntawm Amprilan nrog cov tshuaj ntawm cov lithium pawg, kub, potassium-sparing diuretics, cov tshuaj tiv thaiv kab mob hypoglycemic, cytostatics, cov tshuaj poov tshuaj npaj, cov tshuaj tiv thaiv kab mob tsis pom zoo.

Daim ntawv tso tawm thiab ntim khoom

7 lossis 10 ntsiav tshuaj muab tso rau hauv blister sawb ntim ntawm zaj duab xis ntawm laminated polyamide / aluminium / polyvinyl chloride thiab aluminium ntawv ci.

Lub hlwv ntim muaj 7 ntsiav tshuaj tau nthuav tawm ua ob daim ntawv, uas txawv hauv kev npaj ntawm cov ntsiav tshuaj hauv pob.

4, 12 lossis 14 (7 ntsiav tshuaj txhua) lossis 2, 3 lossis 5 (10 ntsiav tshuaj txhua tus) hlwv cov pob nrog rau cov lus qhia rau kev kho mob hauv xeev thiab Lavxias lus muab tso rau hauv pob ntawv los qhia.