Amprilan® (Amprilan)

Mgbe igbochi ACE na-ebelata angiotensin-2Abawanye renin ọrụ, enwekwu mmetụta nke bradykininmmepụta na-abawanye aldosterone. A na-enye ọgwụ mgbochi hemodynamic na antihypertensive nke ọgwụ ahụ site n'ịgbasa lumen nke arịa ahụ, belata OPSS. Ọgwụ anaghị emetụta yaobi obi. Ọgwụgwọ ogologo oge nwere ike ibute iweghachị hypertrophy ekpe ventricular, nke malitere ọbara mgbali ike. Kpebie ọbara mgbali debara aha 1-2 awa mgbe ị theụsịrị ọgwụ ahụ, mmetụta antihypertensive na-adịgide ruo otu ụbọchị.

Na ndị ọrịa na- obi obara belata ihe egwu obi ọgụ, ọnwụ mberede, nrịba ọrịa, ọnụọgụ nke ụlọ ọgwụ mberede na ọnụọgụ nke ọdụdọ ọbara. Na ndị ọrịa na- ọrịa shuga enwere mbelata microalbuminuriabelata ihe egwu nephropathy. Mmetụta ndị a na-etolite n'agbanyeghị ogo ọbara mgbali.

Ihe ngosi Amprilana

  • obi obara (oge na-adịghị ala ala)
  • ọbara mgbali elu,
  • ọrịa akwara ọbaraobi.

Ihe ngosi maka iji na ndi oria nwere ọrịa shuga: nephropathy.

Ihe ngbanwe

  • hypersensitivity ihe ndi mejuputara
  • ntụpọ obi (mitral, aortic, jikọtara),
  • inye ara,
  • kadioyopathy,
  • Usoro gbasara akụrụ,
  • hyperaldosteronism,
  • tụụrụ ime,
  • afọ ruo afọ 18.

Nsonaazụ

Ọtụtụ mgbe, a na-edekarị ọnụọgụ ọbara dị ala,mechie, isi ọwụwa dịka isi ọwụwa, akọrọ ụkwara, bronchospasmakpukpo aru, ihe ojoo eriri afọ na pancreatitis na mmụba na ịta nke enzymes, ihe mgbu na nkwonkwo na akwara.

Naa na-ahụkarị arrhythmiankuchi obi angina pectorismgbagwoju anya site na infarction myocardial, Ọrịa Raynaud, vasculitis, ọrịa astheno-depression nke nwere nsogbu ịrahụ ụra, ọrịa ọgụ na-adịghị ala ala na ọria aru, enweghi ike, sistemụ akụrụngwa na-abawanye uru na ịba ụba ịta creatinia na urea na mmamịrị mmeghachi omume nfụkasị ahụmgbanwe na plọg nke usoro laborodị, erythropenia.

Site na ngbanwe nke ogo mmeghachi omume ọjọọ, a na-atụ aro ka ịkpọtụrụ dọkịta ma kwụsị ị Amụ ọgwụ Amprilan nwa oge.

Mwepụta wepụtara ya na ihe mejupụtara

Akụkụ bụ isi nke Amprilan bụ ramipril.

Ihe inyeaka dị n’ime mbadamba ụrọ: silium croscarmellose, stgelatinized steepụ, sodium stearyl fumarate, sodium bicarbonate, lactose monohydrate, ntutu.

Onodu ogwu: 1.25 mg, 2.5 mg, 5 mg na 10 mg nke ramipril na otu mbadamba.

A na-emepụta Amprilan na mbadamba ụrọ (mbadamba 7 ma ọ bụ 10 na ọnya) oval na ewepụghị elu na bevel. Agba nke mbadamba ihe dịgasị iche dabere n’otú ọgwụ ahụ si dị: ọcha ma ọ bụ ihe fọrọ nke nta ka ọ bụrụ ọcha (1.25 mg na 10 mg nke ọ bụla), odo edo edo (2.5 mg nke ọ bụla), pink na-agwakọta (5 mg nke ọ bụla),

Omume ọgwụ

Mlọ ọgwụ Amprilan bu onye oru ACE inhibitor nke di ogologo. Enzyme Angiotensin na-eme ka ntughari nke angiotensin nke abụọ gbanwee ihe mmụọ nke mmụọ, bụ ihe ya na kinase - enzyme nke na-eme ka agbaji bradykinin kwụsị. N'ihi mgbochi nke ACE site na Amprilan, mkpokọta nke angiotensin II na-ebelata, ọrụ nke renin na plasma ọbara na-abawanye, ihe omume bradykinin na mmepụta nke aldosterone na-abawanye, nke na-eduga n'ịba ụba ọdịnaya potassium na ọbara.

Amprilan nwere antihypertensive na mmetụta metụtara hemodynamic n'ihi mgbasawanye nke akwara ọbara ma belata ngụkọta ngụgụ onwe ha. N'okwu a, obi obi anaghị agbanwe agbanwe. A na-ahụ mbelata nrụgide mgbe otu ọgwụ Amprilan mechara 1-2 awa, mgbe awa 3-6 gasịrị, ọgwụgwọ ọgwụgwọ rutere oke ma na-adịgide 24 awa.

Site na iji ọgwụ ogologo oge na ọgwụ ahụ, ọbara mgbali ventricular hypertrophy na-ebelata, ebe enweghị mmetụta na-adịghị mma na ọrụ obi.

Mlọ ọgwụ

A na-enweta ngwa ngwa ahụ ngwa ngwa site na nri digestive (ọsọ anaghị esite na nri oriri). Otu elekere mgbe etinyechara ya n'ọrụ, a na-enweta ntinye kachasị n'ihe ndị dị na ọbara. Ihe ruru 73% nke ramipril na-egbochi protein ndị dị na plasma.

Ọgwụ ahụ na-agbaji na imeju, na-akpụ akpụ metabolite ramiprilat (ọrụ nke ikpeazụ ahụ ji okpukpu 6 karịa ọrụ ramipril n'onwe ya) yana diketopiperazine na-adịghị arụ ọrụ. A na-achọpụta ntinye uche kachasị nke ramiprilat n'ime ọbara awa 2-4 mgbe ị theụ ọgwụ ahụ, ịkwụsi ike na ọgwụgwọ oge niile n'ụbọchị nke 4 nke ọgwụgwọ. Ihe dị ka 56% nke ramiprilat na-ejikọ protein protein.

Ihe ruru 60% nke ramipril na ramiprilat na-ewepụpụta site na akụrụ n'ụdị metabolites, erughị 2% nke ramipril na-ewepụ n'ahụ ahụ adịghị agbanwe. Ọkara ọkara nke ramiprilat bụ site na awa 13 ruo 17, ramipril - 5 awa.

Site n'ịrụ ọrụ ezumike mkpirisi, ọnụego mkpachapụ nke ramipril na metabolites na-ebelata. N'ime ndị ọrịa nwere ọrịa ịba ọcha n'anya, ntụgharị nke ramipril gaa ramiprilat na-ebelata, ọdịnaya nke ramipril na ọbara ọbara na-aba ụba.

Usoro onunu ogwu na nhazi

Ana mburu mbadamba ndị ahụ ọnụ, n'agbanyeghị nri ahụ, a notụla, a ,ụ ọtụtụ mmiri.

Dọkịta a hotara ịhọrọ usoro ọgwụ ahụ n'otu n'otu maka onye ọrịa ọ bụla, na-eburu n'uche ihe ngosipụta, nnabata nke ọgwụ ahụ, ọrịa na-agbanwe agbanwe yana afọ onye ọrịa. Mgbe ị na-ahọrọ ọgwụ, ekwesịrị ịtupụta akara ngosi ọbara. Oke ike ị allowụ ọgwụ maka ụdị ọrịa niile bụ 10 mg kwa ụbọchị. Usoro ọgwụgwọ ya na-abụkarị ogologo oge, nke dọkịta mekwara ka o guzosie ike.

Site na ọbara mgbali elu Usoro ọgwụgwọ akwadoro mbụ bụ 2.5 mg otu ugboro kwa ụbọchị. Ọ bụrụ na ọ dị mkpa, enwere ike ịgbanye okpukpu abụọ na ụbọchị 7-14.

Na nkụda mmụọ obi na-adịghị ala ala na mbụ ọgwụ a tụrụ aro ya bụ ọgwụ 1.25 mg (enwere ike okpukpu abụọ ka izu 1-2 gachara).

Site na nkụchi obi, nke mere ụbọchị 2-9 mgbe ọ rịsịrị nnukwu ọrịa myocardial infarction, a na-atụ aro ka ọ were 5 mg nke Amprilan kwa ụbọchị - 2.5 mg n'ụtụtụ na mgbede. Ọ bụrụ na n’oge ọgwụgwọ nrụgide ahụ na-agbadata nke ukwu, a na -ebelata usoro a (1.25 mg ugboro abụọ n'ụbọchị). Mgbe ụbọchị atọ gasịrị, ọ̀gwụ ahụ gbagoro ọzọ. Ọ bụrụ na ị takingụ ọgwụ ahụ na ọgwụ nke 2,5 mg ugboro abụọ kwa ụbọchị onye ọrịa ahụ anabataghị ya, ọ ga-akagbu ọgwụgwọ ya na Amprilan.

Nehropathy (ya na mgbasa ọrịa nke akụrụ na ọrịa shuga).Usoro akwadoro ịmalite bụ 1.25 mg kwa ụbọchị. Kwa ụbọchị iri na anọ, a na-eji mkpụrụ ego ahụ amụba okpukpu abụọ ruo mgbe a ga-enweta ọgwụ mmezi nke 5 mg kwa ụbọchị.

Mgbochi nke nkụda obi na-esote ọrịa infịction myocardial. Na ọkwa mbụ nke usoro ọgwụgwọ, Amprilan 2.5 mg ka edobere na mbadamba ụbọchi ọ bụla. Mgbe otu izu gasịrị, usoro ịba ụba ahụ na-abawanye ruo 5 mg kwa ụbọchị, mgbe izu abụọ ọzọ gasịrị - na mmezi nke 10 mg otu ugboro n'ụbọchị.

Lusionji usoro nkwuputa anwansi na ogwugwo ogwu n’agha A na-ewere Amprilan 2.5 mg otu ugboro n'ụbọchị maka ụbọchị 7. Mgbe ahụ, maka izu 2-3, a na-a drugụ ọgwụ ahụ na 5 mg kwa ụbọchị, mgbe ị isụ ọgwụ ya mụbara ugboro abụọ ọzọ - ruo 10 mg kwa ụbọchị.

Ntụziaka pụrụ iche

  1. Maka ndị ọrịa nwere nsogbu ọrụ akụrụ, usoro izizi nke Amprilan kwesịrị ịbụ 1.25 mg, na usoro ọgwụgwọ kwa ụbọchị kwesịrị ịbụ 5 mg.
  2. Maka ndị ọrịa nwere ọrịa imeju, usoro izizi bụ 1.25 mg, ọgwụ kachasị ụbọchị bụ 2.5 mg.
  3. Ọ bụrụ na enyere ndị Amurela ọgwụ ka ndị ọrịa na - a diụ ọgwụ mkparịta ụka, achọrọ ka ọ kagbuo ma ọ bụ belata usoro onunu ogwu a. Ọ na-achọ nleba anya mgbe niile banyere ọnọdụ ndị ọrịa dị otú a, ọkachasị ndị ọrịa nwere agadi (karịa afọ 65).
  4. A na-ewere Amprilan na nlezianya na ndị ọrịa nwere ọrịa systemic nke anụ ahụ na - ejikọta, ọrịa shuga mellitus, angina pectoris na-ejighi ike.
  5. Ọgwụ nwere mmetụta dị njọ na nwa ebu n’afọ (hypoplasia nke ngụgụ na ọkpụkpụ nke okpokoro isi, hyperkalemia, ọrụ ezumike n’ọrụ) yana contraindicated na ụmụ nwanyị dị ime. Tupu ọ gbasachaa Amprilan, ọ dị mkpa ka ụmụ nwanyị toruworo ịmụ nwa ghara iwepụta afọ ime.
  6. Mgbe ị na-ewere Amprilan n'oge a na-enye nwa ara, a ga-akagbu nwa ara.

Usoro na ọnọdụ nchekwa

Chekwaa ọgwụ na okpomọkụ agaghị akarị 25 Celsius C, ebe echekwara site na mmiri ma anwụ, nke ụmụaka enweghị ike. Ndụ nchekwa nke mbadamba nkume nke Amprilan bụ afọ 3. Mgbe ụbọchị ahụ gosipụtara na ngwugwu ahụ, enweghị ike ị drugụ ọgwụ ahụ.

Ihe analogues nke Amprilan (ogwu nwere udiri ihe ndia).

Ihe onyonyo 3D

ỌgwụTaabụ 1.
ike ọrụ:
ramipril1,25 mg
2,5 mg
5 mg
10 mg
ndị na-ebu ụzọ:
mbadamba 1.25, 2,5, 5 ma ọ bụ 10 mg: sodium bicarbonate, lactose monohydrate, ssum croscarmellose, pregelatinized stachi, sodium stearyl fumarate
Mbadamba 2.5 mg: ngwakọta nke agba agba "PB 22886 odo" (lactose monohydrate, iron dye oxide edo edo (E172)
5 mg mbadamba: ngwakọta nke ntutu e ji esiji “PB 24899 pink” (lactose monohydrate, ntụ ntụ na-acha ọbara ọbara (E172), iron dye oxide odo (E172)

Usoro onunu ogwu na nhazi

N'ime n'agbanyeghị oge iri nri (ị ga - ewere mbadamba iberibe ma tupu ma n’oge ma ọ bụ mgbe erichara nri), drinkụọ nnukwu mmiri (iko 1-2). Etala ma ọ bụ ghari mbadamba tupu ị were.

A na-ahọrọ dose ahụ dabere na ọgwụgwọ ọgwụgwọ na ndidi na ndidi maka ọgwụ.

Ọgwụgwọ na Amprilan ® na-abụkarị ogologo oge, ọ bụ dọkịta kpebiri na oge ọ ga-ekpebi ihe ọ bụla.

Ọ gwụla ma akọwapụtara ya nke ọma, mgbe ahụ yana ọrụ akwara dị iche iche yana ọrụ ịwa ahụ, a na-atụ aro usoro usoro usoro ọgwụgwọ ndị a.

Ọ na - abụkarị ọgwụ mbido bụ 2.5 mg / ụbọchị n'ụtụtụ. Ọ bụrụ na mgbe ị na-ewere Amprilan ® na ọgwụ a maka izu 3 ma ọ bụ karịa, ọ gaghị ekwe omume ịme ka ọbara dị elu, mgbe ahụ, enwere ike ịbawanye dose ahụ gaa 5 mg / ụbọchị. Ọ bụrụ na dose nke 5 mg adịghị arụ ọrụ nke ọma, mgbe izu 2-3 ọ ka nwere ike okpukpu abụọ okpueze kachasị atụ aro kwa ụbọchị 10 mg.

Dika uzo ozo iji nwekwuo ogwu na 10 mg / ubochi enweghi ezigbo ogwu antihypertensive nke ubochi 5 mg, o kwere omume igbakwunye ndi ozo antihypertensive na ọgwụgwọ, karia diuretics ma obu BKK.

Usoro ọgwụgwọ akwadoro bụ 1.25 mg / ụbọchị. Dabere na nzaghachi onye ọrịa na usoro ọgwụgwọ ahụ, ọgwụ ahụ nwere ike ịba ụba.

Ọ na-atụ aro ka ị jiri okpukpu abụọ dị n’agbata 1-2 were okpukpu abụọ. Ọ bụrụ na ịchọrọ ị doseụ ọgwụ kwa ụbọchị nke 2.5 mg ma ọ bụ karịa, enwere ike iji ya otu ugboro n'ụbọchị, ma ọ bụ kewaa abụọ.

Oke kachasị tụrụ aro kwa ụbọchị bụ 10 mg.

Ọrịa mamịrị ma ọ bụ nephropathy na-arịa ọrịa mamịrị

Usoro ọgwụgwọ akwadoro bụ 1.25 mg / ụbọchị. Ọgwụ nwere ike ịrị elu ruo 5 mg / ụbọchị. Site na ọnọdụ ndị a, ọnụọgụ ọgwụ dị elu karịa 5 mg / ụbọchị agụbeghị akwụkwọ nke ọma na ule nyocha ụlọ ọgwụ.

Mbelata ihe egwu dị n'ọrịa ọgbụgba myocardial, ọrịa strok, ma ọ bụ ọnwụ obi na ndị ọrịa nwere nnukwu ọrịa obi.

Usoro akwadoro ịmalite bụ 2.5 mg / ụbọchị.

Dabere na ndidi onye ọrịa na-anabata Amprilan ®, enwere ike ịbawanye ọgwụ ahụ.

Ọ na-atụ aro ka okpukpu abụọ gwọọ ya ka ọ gachara izu 1 nke ọgwụgwọ, ma n’izu izu atọ na-abịanụ, bulie ya ka ọ bụrụ ụdị mmezi nke 10 mg / ụbọchị.

Agụbeghị ọgwụ nke gafere 10 mg / ụbọchị na ọnwụnwa nyocha ọfụma. Anaghi aghota iji ogwu ahu eme ihe na ndi ọrịa nwere Cl creatinine erughi 0.6 ml / sec nke oma.

Ọkpụkpụ nke ọrịa obi bidoro n'ime ụbọchị ole na ole mbụ (site na ụbọchị abụọ ruo ụbọchị 9) mgbe nnukwu ọrịa myocardial infarction.

Ọgwụ akwadoro ka akwadoro bụ 5 mg / ụbọchị, nke kewara 2 doses nke 2.5 mg (ewere n'ụtụtụ na mgbede). Ọ bụrụ na onye ọrịa ahụ anabataghị ọgwụ izizi a (a na-achọpụta mbelata ọbara mgbali elu), mgbe ahụ, a na-atụ aro ka ọ were 1.25 mg ugboro abụọ kwa ụbọchị maka ụbọchị 2.

Mgbe ahụ, dabere na mmeghachi omume nke onye ọrịa, enwere ike ịbawanye dose ahụ. Ọ na-atụ aro ka usoro ya na mmụba ya okpukpu abụọ na nkeji nke ụbọchị 1-3. Enwere ike iji ya gwaa ya, otu ụbọchị, nke e kewara abụọ ka usoro onunu ugboro abụọ.

Ogo kachasị akwadoro bụ 10 mg.

Ugbu a, ahụmịhe banyere ọgwụgwọ ndị ọrịa nwere nnukwu nkụchi obi (III - IV klas arụ ọrụ dị ka nhazi ọkwa NYHA) nke mere ozugbo enwere nnukwu myocardial infarction ezughi oke. Ọ bụrụ na ndị ọrịa dị otú ahụ kpebiri ịgwọ Amprilan ®, a na-atụ aro ka ọgwụgwọ malite na nke kachasị dị ala - 1.25 mg / ụbọchị, ekwesịrị ilekọta nlekọta pụrụ iche na mmụba ọ bụla.

Ndị otu ọrịa pụrụ iche

Alrụ ọrụ na-arụ ọrụ na ụlọ. Na Cl creatinine site na 50 ruo 20 ml / min / 1.73 m 2, usoro mbụ kwa ụbọchị na-abụkarị 1.25 mg. Ogo ị na-anabata kwa ụbọchị bụ 5 mg.

Ọkpụkpụ ọgbụgba na akwara na - agbadata oke, ọbara ọgbụgba dị oke egwu, yana ọ bụrụ na mbelata ọbara mgbali elu na - ebute ihe egwu ụfọdụ (dịka ọmụmaatụ, enwere nnukwu ọnya akwara akwara na akwara akwara). A na-ebelata ọgwụ mbụ ka ọ bụrụ 1.25 mg / ụbọchị.

Usoro ọgwụgwọ diuretic gara aga. Ọ bụrụ na ọ ga - ekwe omume, a ga-akagbu mkpụrụ akwụkwọ diuretic 2-3 ụbọchị (ọ dabere na oge nke ndị ọrịa ahụ) tupu ịmalite ọgwụgwọ na Amprilan ® ma ọ bụ na ọ dịkarịa ala, belata ọgwụ nke diuretics. Treatmentgwọ ndị ọrịa dị otú a kwesịrị ịmalite site na ntakịrị ọgwụ Amprilan ® - 1.25 mg / ụbọchị n'ụtụtụ. Mgbe ha takingụsịrị ọgwụ nke mbụ na oge ọ bụla mgbe ịbawanye ọgwụ Amprilan ® na / ma ọ bụ akwara diuretics, ndị ọrịa kwesịrị ịnọ n'okpuru nlekọta ahụike ma ọ dịkarịa ala 8 awa iji zere mmeghachi omume hypotensive na-achịkwa.

Afọ karịrị iri afọ isii na ise. A na-ebelata ọgwụ mbụ ka ọ bụrụ 1.25 mg / ụbọchị.

Ọrụ imeju na-arụ ọrụ. Mmeghachi omume nke ọbara mgbali na ị takingụ Amprilan ® nwere ike ịbawanye elu (site na ibelata ramiprilat excretion), ma ọ bụ mee ka ike gwụ (n'ihi na ọ na-ebelata ntụgharị nke ramipril na-adịghị arụ ọrụ na ramiprilat nọ n'ọrụ). Ya mere, na mmalite ọgwụgwọ chọrọ nlezianya nlekọta ahụike. Oke kachasị anabata ụbọchị ọ bụla bụ 2.5 mg.

Emeputa

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

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Tẹ.: (495) 981-10-95, faksị (495) 981-10-91.

Mlọ ọgwụ

Mgbe nchịkwa ọnụ nke ramipril, Amprilan na-enweta ngwa ngwa site na eriri afọ (eriri afọ) na ọkwa 50-60%. Inata oge a na nri ga-akwụsịlata ịmịkọrọ ya, mana ọ naghị emetụta ọnụọgụ nke batara n'ọbara. N'ihi nnabata biotransformation / rụọ ọrụ nke ramipril, nke kachasị na imeju site na hydrolysis, ramiprilat (metabolite na-arụ ọrụ, ugboro isii ka arụ ọrụ karịa ramipril n'ihe gbasara ACE inhibition) na diketopiperazine (metabolite nke na-enweghị ọrụ ọgwụ). Ọzọkwa, diketopiperazine nwere glucuronic acid, na ramiprilat bụ glucuronated na metabolized na diketopiperazinic acid.

Ihe bioavailability nke ramipril na-adabere na ọgwụ ọnụ ma dị iche na 15% (maka 2.5 mg) ruo 28% (maka 5 mg).Ihe bioavailability nke ramiprilat mgbe nchịkwa ọnụ nke 2.5 mg na 5 mg nke ramipril bụ

Pasent iri anọ na ise nke ihe ngosi a nwetasịrị ma nchịkwa ọgwụgwọ nke otu usoro onunu ogwu.

Mgbe imesịrị Amprilan n'ime, a na-enweta mkpo plasma kachasị nke ramipril mgbe elekere 1 gachara, ramiprilat - mgbe awa 2-4. Mbelata ọkwa nke ramiprilat na plasma na-apụta n'ọtụtụ nkebi: ọkwa nke nkesa na mwepu na T.1/2 (ọkara ndụ)

3 ele, etiti n’etiti na T1/2

15 h na ogbo ikpeazụ nke nwere ọdịnaya dị ala nke ramiprilat na plasma na T1/2

Daysbọchị 4-5, nke a bụ n’ihi nwayọ nwayọ nke ramiprilat sitere na nkekọ siri ike na ndị na-anabata ACE. Na agbanyeghị oge a, iwere ọgwụ ramipril nke 2.5 mg ma ọ bụ karịa otu ugboro kwa ụbọchị n'ime mmadụ nwere ike nweta nkwalite plasma plasma nke ramiprilat mgbe ụbọchị 4 nke ị theụ ọgwụ ahụ. N'ezie nchịkwa nke Amprilan irè T1/2 dabere na dose ma dịgasị iche site na 13 ruo 17 awa

Ramipril na - ejikọ protein protein na ihe dị ka 73%, ramiprilat - 56%.

Mgbe nchịkwa ọnụ nke ramipril, nke ejiri akara rediototo sitotototo akara, na 10 mg, ihe ruru 39% nke redioakpochasị ahụ na-apụ na eriri afọ, ihe dịka 60% akụrụ ga-ahụ ya. N'ime ndị ọrịa nwere mmeru mmiri na -akpata ihe na-akpata 5.5 mpempe nke ramipril n'ime akụrụ yana site na eriri afọ, ihe fọrọ nke nta ka ọ bụrụ otu ramipril na metabolites ya ka a na-ahapụ n'ime awa iri abụọ na anọ mbụ ka nchịkwa gasịrị.

Ihe dịka 80-90% nke ihe dị na mmamịrị na bile ka amatapụtara dị ka ramiprilat na metabolites ya. Ramipril glucuronide na diketopiperazine mejupụtara

10-20% nke ngụkọta dose, na unmipletiolized ramipril -

Na usoro ọmụmụ gbasara ụmụ anụmanụ, achọpụtara na ramipril na-abanye n’ime mmiri ara.

N'ime ndị ọrịa nwere ọrụ mgbazinye nsogbu, nhichapụ creatinine (CC) na-erughị 60 ml / min na-ewepụ ramiprilat na metabolites ya. Nke a na-ebute mmụba na mkpokọta plasma ha na mbelata nwayọ ma e jiri ya tụnyere ndị ọrịa nwere ọrụ mkpo nkịtị.

Highsesụ ọgwụ ramipril dị elu (10 mg) ma ọ bụrụ na arụ ọrụ imeju na-akpata na-eduga n'ịbelata usoro metabolism nke ramipril na nwayọ nwayọ nke metabolite na-arụ ọrụ.

N'ime ndị ọrụ afọ ofufo ahụike na ndị ọrịa nwere ọbara mgbali elu, ọ nweghị nnwale dị ukwuu nke ramipril na ramiprilat ka emere ya n'ihi ọgwụgwọ izu abụọ na Amprilan na ọgwụ nke 5 mg kwa ụbọchị. Mgbe usoro izu abụọ yiri nke ahụ gasịrị, ndị ọrịa nwere obi nwute nwere mmụba nke 1.5-1.8 na ọkwa ramiprilat na plasma ọbara na mpaghara n'okpuru usoro ịta ahụhụ (AUC).

Njirimara nke pharmacokinetic nke ramipril na ramiprilat n'ime ndị ọrụ afọ ofufo nwere ahụike dị afọ 65-75 adịghị iche na ndị ọrụ afọ ofufo na-eto eto nwere ahụ ike.

Ngwongwo ogwu

Mlọ ọgwụ

Metabolite na-arụ ọrụ nke ramipril, nke mebere enzymu nke "imeju", ramiprilat bụ ihe na - eme ACE inhibitor (njikọ nke ACE: kininase II, dipeptidyl carboxy dipeptidase I). ACE na plasma na anụ ahụ na-ejikwa ntụgharị nke angiotensin nke m ka ọ bụrụ angiotensin II, nke nwere mmetụta vasoconstrictor, yana ndakpọ nke bradykinin, nke nwere mmetụta vasodilating. Ya mere, mgbe ị na-ewere ramipril n'ime, nguzobe nke angiotensin II na-agbadata ma bradykinin na-agbakọ, nke na-eduga na vasodilation na mbelata ọbara mgbali (BP). Mmụba nke Ramipril na arụ ọrụ nke usoro kallikrein-kinin dị na plasma ọbara na anụ ahụ na-eme ka arụ ọrụ nke usoro prostaglandin na mmụba na njikọta nke prostaglandins, nke na-akpali nguzozi nke nitric oxide (N0) na endotheliocytes, na-akpata mmetụta cardioprotective.

Angiotensin II na-akpali mmepụta nke aldosterone, yabụ, iji ramipril na-eduga n'ịbelata nzuzo nke aldosterone na mmụba nke ọdịnaya potassium na ọbara.

Site na mbelata nke mkpokọta angiotensin II na plasma ọbara, a na-ewepụ mmetụta ya na nzuzo nke renin site na ụdị nzaghachi na-adịghị mma, nke na-eduga n'ịba ụba na ọrụ plasma renin.

Echere na mmepe nke ụfọdụ mmeghachi omume ọjọọ (karịchaa, ụkwara "akọrọ") metụtara mmụba nke ọrụ bradykinin.

Na ndị ọrịa nwere ọbara mgbali elu na-ewere ramipril na-eduga n'ịbelata ọbara mgbali n'ọnọdụ "ụgha" na "guzo" na-enweghị mmụba mmụba na ọnụego obi (HR). Ramipril na –ebelata mkpụkọ akwara gbasara akwara, (OPSS), na - emeghi mgbanwe na ọbara gbasara akwara na ọnụego mmụba. Mmetụta antihypertensive na-apụta ịpụta elekere 1 ruo 2 mgbe ị ofụ ọgwụ otu ọgwụ, rute uru kachasị ya mgbe awa 3-6 gasịrị, ọ ga-adịgide ruo awa 24. Mgbe ị na-ewere Amprilan, mmetụta antihypertensive nwere ike jiri nwayọọ nwayọọ na-abawanye, na-ejikarị izu site na izu 3-4 nke iji ya mgbe niile wee na-adịgide ruo ogologo oge. Contkwụsị ọgwụ ahụ na mberede anaghị ebute mmụba ọbara ngwa ngwa ma dị egwu (enweghị "nkwụsị" ọrịa).

N'ime ndị ọrịa nwere ọbara mgbali elu, ramipril na-ebelata mmepe na oganihu nke myocardial hypertrophy na mgbidi vaskụla.

N'ime ndị ọrịa nwere ọrịa obi na-adịghị ala ala (CHF) ramipril na-ebelata OPSS (belata mgbe ebuputara na obi), na-abawanye ike nke ọdụ ma na-ebelata nrụgide nke ventricle aka ekpe (LV), nke, n'ihi ya, na-eduga na mbelata preload na obi. N'ime ndị ọrịa a, mgbe ha na-ewere ramipril, enwere mmụba na nsonaazụ obi, LV ejection fraction (LVEF) na mmụba na nnagide mmega ahụ.

Na-arịa ọrịa shuga na-arịa ọrịa mamịrị na-ewere ramipril na-eji nwayọ nwayọ nwayọ na mmụba akwara na mmalite nke ọdịda akụrụngwa ọdịda, ma, site na nke a, na-ebelata mkpa ịba ama ma ọ bụ ịtụgharị akụrụ. N'ime mmalite nke ọrịa mamịrị ma ọ bụ nephropathy, ọrịa ramipril na-ebelata ọnọdụ albuminuria.

N'ime ndị ọrịa nwere nnukwu ihe ibute ọrịa obi n'ihi akwara ọnya (ọrịa obi na-arịa ọrịa akwara, akụkọ banyere ọrịa akwara ozi, ọrịa strok) ma ọ bụ ọrịa shuga nwere obere ihe ize ndụ ndị ọzọ (microalbuminuria, ọbara mgbali akwara, mmụba nke mkpokọta nke mkpokọta cholesterol (OXc), na-ebelata ịdị n'otu nke ịdị elu lipoprotein cholesterol (HDL-C), ị smokingụ sịga) mgbakwunye nke ramipril na usoro ọkọlọtọ na-ebelata Ọ na-akọwa ọghọm nke infarction myocardial, ọrịa strok, na ọnwụ obi. Na mgbakwunye, ramipril na-ebelata ọnụ ọgụgụ mmadụ na-anwụ, yana mkpa maka usoro nyochaghachi ma na-ebelata mmalite ma ọ bụ ọganihu nke nkụda obi.

N'ime ndị ọrịa nwere nkụda obi na ngosipụta nke ụlọ ọgwụ malitere na ụbọchị mbụ nke myocardial infarction (ụbọchị 2-9), ojiji nke ramipril, malitere site na ụbọchị 3- ụbọchị nke 10 nke nnukwu myocardial infarction, belata ọnwụ (site 27%), ihe egwu nke mberede ọnwụ (site na 30%), ihe egwu nke ọghọm nkụda mmụọ na-enwe ọfụma (klaasị ọrụ III-IV dị ka nhazi NYHA) / na-agwọ ọrịa (site na 23%), ohere nke ụlọ ọgwụ na-esote n'ihi mmepe nke nkụda obi (site na 26%).

N'ime ọha mmadụ n'ozuzu ya, yana ndị ọrịa nwere ọrịa mellitus, ha abụọ nwere ọbara mgbali elu na ọbara mgbali nkịtị, ramipril na-ebelata ihe ize ndụ nke nephropathy na ntinye nke microalbuminuria.

Mlọ ọgwụ

Mgbe nchịkwa ọnụ gasịrị, ramipril na-abanye ngwa ngwa site na eriri afọ (50-60%). Iri nri na - eme ka mmata gi ghara ikwusi ike, ma o nweghi otutu ovu.

Ramipril nwere usoro metabolism dị omimi / na-arụ ọrụ (nke kachasị nke imeju site na hydrolysis), na-ebute naanị metabolite na-arụ ọrụ, ramiprilat, nke ọrụ ya n'ihe gbasara ACE inhibition dị ihe dị ka ugboro isii karịa ọrụ nke ramipril. Na mgbakwunye, n'ihi metabolism ramipril, a na-emepụta diketopiperazine, nke na-enweghị ọrụ ọgwụ, nke a na-ejikọ ya na glucuronic acid, a na-agbanyekwa ramiprilat na metabolized na diketopiperazinic acid.

Bioavailability nke ramipril mgbe nchịkwa ọnụ sitere na 15% (maka ọgwụ nke 2,5 mg) ruo 28% (maka ọgwụ nke 5 mg). Ihe bioavailability nke metabolite nọ n'ọrụ, ramiprilat, mgbe ingestion nke 2.5 mg na 5 mg nke ramipril dị ihe dịka 45% (ma e jiri ya tụnyere bioavailability ya mgbe nchịkwa intravenous na otu usoro).

Mgbe iwere ramipril n'ime, pilosima kachasị nke ramipril na ramiprilat na-eru ma elekere 1 na 2 ruo 4 gachara. Mbelata na mkpokọta plasma nke ramiprilat pụtara n'ọtụtụ nkebi: nkesa na ọkara oge (T1 / 2) nke ramiprilat dị ihe dị ka awa 3, mgbe ahụ etiti na T1 / 2 ramiprilat, ihe dị ka awa iri na ise, na oge ikpeazụ nke nwere oke mkpoko nke ramiprilat na plasma na T1 / 2 ramiprilat, ihe dịka ụbọchị 4-5. Oge ikpeazu a bụ n'ihi nwayọ nke ramiprilat na nkekọ siri ike na ndị na-anabata ACE. Na agbanyeghi ogologo oge ikpeazụ were otu mkpụrụ ọgwụ ramipril nke ọnụ na-egbu elektrọnm 2.5 ma ọ bụ karịa, e mejupụtara ọkwa plasma nke ramiprilat mgbe ihe dị ka ụbọchị anọ nke ọgwụgwọ gasịrị. Site na iji ọgwụ ahụ "dị irè" T1 / 2 dabere na dose bụ 13-17 awa.

Nkwurịta okwu na protein protein plasma dị ihe dị ka 73% maka ramipril, na 56% maka ramiprilat.

Mgbe nchịkwa intraven, olu nkesa ramipril na ramiprilat dị 90 L na ihe dịka 500 L, n'otu n'otu.

Mgbe abatamiri nke ramipril (10 mg) akara akpọtototo na -akpata, 39% nke redioaktivu na-apụ na eriri afọ yana ihe dịka 60% akụrụ. Mgbe nhazi nchịkwa nke ramipril, a na-ahụ ihe dịka 50-60% nke mmamịrị na mmamịrị n'ụdị ramipril na metabolites ya. Mgbe nchịkwa intravenous nke ramiprilat, ihe dị ka pacenti 70 nke ọgwụ a na-ahụ na mmamịrị n'ụdị ramiprilat na metabolites ya, n'ụzọ ọzọ, site na nchịkwa intravenous nke ramipril na ramiprilat, akụkụ dị ukwuu nke ọgwụ ahụ ka ewepụrụ site na eriri afọ ya na agịga, na-agabiga akụrụ (50% na 30%, n'otu n'otu). Mgbe usoro nchịkwa nke 5 mg nke ramipril dị na ndị ọrịa nwere mmịpụta mmiri, ihe fọrọ nke nta ka ọ bụrụ otu ụdị ramipril na metabolites ya bụ akụrụ site na akwara ya na n'ime awa 24 mbụ ka nchịkwa gasịrị.

Achọpụtara ihe dịka 80 - 90% nke metabolites na mmamịrị na bile ka ramiprilat na ramiprilat metabolites. Ramipril glucuronide na ramipril diketopiperazine na-ewe ihe dị ka 10-20% nke ngụkọta ego, ihe ramipril na-enweghị atụ na mmamịrị bụ ihe dịka 2%. Nnyocha ụmụ anụmanụ egosila na ramipril dị na mmiri ara ara.

N'ọnọdụ arụ ọrụ ezinaụlọ nwere ikike idozi ya (CC) ihe na-erughị 60 ml / min, mpụta ahụ nke ramiprilat na metabolites ya site na akụrụ na-agbada. Nke a na-ebute mmụba na mkpokọta plasma nke ramiprilat, nke na-agbada nwayọ karịa ndị ọrịa nwere ọrụ ezumike nkịtị.

Mgbe ị na-ewere ramipril na usoro dị elu (10 mg), ọrụ imeju na-arụ ọrụ na-eduga n'ibelata usoro metabolism nke ramipril na ramiprilat na-arụ ọrụ ngwa ngwa na mkpochapu ramiprilat. N'ime ndị ọrụ afọ ofufo ahụike na ndị ọrịa nwere ọbara mgbali elu, mgbe a gwọchara ya izu abụọ na ramipril na ọgwụ kwa ụbọchị nke 5 mg, enweghị nchịkọta ọgwụ ramipril na ramiprilat. N'ime ndị ọrịa nwere nkụchi obi, mgbe izu abụọ nke ọgwụgwọ jiri ramipril na ọgwụ kwa ụbọchị nke 5 mg, mmụba nke 1.5-1.8 na plasma nke ramiprilat na mpaghara dị n'okpuru usoro ịta ahụhụ (AUC).

N'ime ndị ọrụ afọ ofufo nwere ahụike siri ike (afọ 65-75), ọgwụ ọgwụ nke ramipril na ramiprilat adịghị iche na ndị ọrụ afọ ofufo siri ike.

Jiri n’oge ime na n’oge a na-enye nwa ara

Amprilan bụ contraindicated n'oge ime, dị ka o nwere ike na-emebi mmetụta na nwa ebu n'afọ: isi ike mmepe nke akụrụ nke nwa ebu n'afọ, mbelata ọbara mgbali nke nwa ebu n'afọ na ụmụ ọhụrụ, arụ ọrụ na-arụ ọrụ nkebi, hyperkalemia, hypoplasia nke ọkpụkpụ nke okpokoro isi, hypoplasia nke ngụgụ.

N'ihi ya, tupu ị theụ ọgwụ ọjọọ n'ime ụmụ nwanyị ịmụ nwa, a ga-agụpụ afọ ime.

Ọ bụrụ na nwanyị na-eme atụmatụ ịtụrụ ime, mgbe ahụ ịkwụsị ọgwụ ya na onye na - egbochi ACE.

N'ihe banyere ime n'oge ọgwụgwọ na Amprilan, ị kwesịrị ịkwụsị ị itụ ya ngwa ngwa o kwere mee ma nyefee onye ọrịa ahụ ka ọ takingụọ ọgwụ ndị ọzọ, n'iji ihe nwute ahụ ga-adị obere.

Ọ bụrụ n’ịgwọ ọrịa na Amprilan dị mkpa n’oge a na-enye nwa ara, a ga-akwụsị ịkwụsị inye ya ara.

Amprilan, ntuziaka maka ojiji (Usoro na usoro onunu ogwu)

Edere Ramipril n'ime nnwere onwe oriri. A na-atụ aro ka ị toụọ ọtụtụ mmiri mmiri. Edere ọgwụ ahụ site na dọkịta nke na-ahọrọ ọgwụ zuru oke na-eburu n'uche ọnọdụ onye ọrịa na ndidi na akụkụ nke ọgwụ ahụ. A na-atụ aro ịmalite iwere Amprilan na obere usoro nke 2.5 mg, na enwere ike ịba ụba na ọnụ ọgụgụ kachasị elu - 10 mg. Ọ bụ dọkịta ga-ekpebi oge ọgwụ ọgwụ ahụ dabere na mkpesa na data, usoro nlekọta ahụike anakọtara.

Ntuziaka maka iji Amprilan ND na NL: 1 mbadamba kwa ụbọchị. Enwere ike ịgbanwe mmegharị ahụ n'oge ọgwụgwọ. Ogologo oge ọgwụgwọ adịghị oke.

Mpempe usoro onunu ogwu

Mbadamba 1,25 mg, 2,5 mg, 5 mg na 10 mg

Otu mbadamba ihe

ike ihe - ramipril 1.25 mg, 2,5 mg, 5 mg, 10 mg,

ndị na-ebu ụzọ: sodium bicarbonate, lactose monohydrate, ssumum croscarmellose, pregelatinized stachi (stachi 1500), sodium stearyl fumarate (maka onunu ogwu nke 1.25 mg, 2,5 mg, 5 mg na 10 mg),

maka usoro onunu ogwu 2,5 mg: agwa ngwakọta PB22886 edo edo (lactose monohydrate, iron oxide edo edo (E 172)),

maka onunu ogwu nke 5 mg: ngwakọta na agba PB24899 acha ọbara ọbara (lactose monohydrate, iron oxide red (E 172), iron oxide edo edo (E 172)

Mbadamba ola dị okirikiri, site na ọcha ruo ihe fọrọ nke nta ka ọ bụrụ ọcha,

chamfered (maka onunu ogwu nke 1.25 mg na 10 mg)

Mpempe akwụkwọ na-adịghị mma, mbadamba odo dị ọkụ, chamfered (maka usoro onunu ogwu nke 2,5 mg)

Mpempe akwụkwọ na-adịghị mma nke ụdị oval, pink, nwere bevel na nsonye anya (maka usoro nke 5 mg)

Dodoụbiga ya ókè

Ihe mgbaàmà nke oke ị ofụ ọgwụ bradycardia (ogwe ume dị ụkọ), mbelata nke ọbara mgbali elu, ujo ala ya na nnukwu gbasara akwara odida. Nzọụkwụ mberede maka ịdoụbiga mmanya ókè gụnyere gastric lavage na itinye ogeenterosorbents, na ihe iyi egwu nke ujo, iwebata ọgwụ na-eme ka ọbara mgbali elu.

Mmekorita

Vasopressor nnabata ọmiko, otu ọgwụ na - abụghị ọgwụ steroid, ọgwụ mgbochi corticosteroid nwere ike belata ogo nke mmetụta hypotensive. raminipril. Welie mmetụta hypotensive nke antipsychotics, ọgwụ antidepressant. Nchikota nke Amprilan na ogwu nke otu lithium, ọla edo, ọgwụ ndi na –eme ka ogwu di iche iche, ndi na aru mmadu, hytoglycemic, cytostatics, na akwadebe potassium, immunosuppressants ka akwadoro.

Mwepụta wepụtara na nkwakọ

A na-etinye mbadamba 7 ma ọ bụ 10 na ngwungwu na-egbuke egbuke nke ihe nkiri nke polyamide / alumini / polyvinyl chloride na foil aluminom.

A na-egosi ngwakọ ngwakọ nwere mkpụrụedemede 7 n'ụdị abụọ, dị iche na nhazi nke mbadamba na ngwugwu ahụ.

4, 12 ma ọ bụ 14 (mbadamba 7 ọ bụla) ma ọ bụ 2, 3 ma ọ bụ 5 (mbadamba 10 nke ọ bụla) ngwugwu ọnya na ntuziaka maka ojiji ahụike na steeti ahụ ma tinye asụsụ Russian n'ime otu kaadiboodu.

Ahapụ Gị Ikwu