Captopril-STI (Captopril-STI)

Captopril-STI: malangizo ogwiritsa ntchito ndi kuwunikira

Dzina lachi Latin: Captopril-STI

Code ya ATX: C09AA01

Chothandizira: Captopril (Captoprilum)

Wopanga: ВВУУУ,,, Russia (Russia)

Kusintha malongosoledwe ndi chithunzi: 07/12/2019

Captopril-STI ndi angiotensin yotembenuza enzyme (ACE) inhibitor.

Kutulutsa mawonekedwe ndi kapangidwe kake

Fomu ya Mlingo - mapiritsi: biconvex, yoyera kapena yoyera yokhala ndi kirimu wowiritsa, kuphatikiza koyipa, fungo labwino, mbali imodzi - ndi chiopsezo (mu paketi ya pulasitiki 1 pulasitiki kapena botolo lomwe lili ndi mapiritsi 60, kapena 2, 3, 4, 5 kapena 6 mapaketi a blister okhala ndi mapiritsi 10 lililonse, ndi malangizo ogwiritsira ntchito Captopril-STI).

Piritsi 1 25/50 mg:

• yogwira zinthu: Captopril - 25/50 mg,
• othandizira zigawo: talc - 1/2 mg, povidone K-17 - 1.975 / 3.95 mg, cellcrystalline cellulose - 6.97 / 13.94 mg, wowuma chimanga - 7.98 / 15.96 mg, magnesium stearate - 1 / 2 mg, lactose monohydrate - kupeza piritsi lolemera 100/20 mg.

Tulutsani mawonekedwe, ma CD ndi kapangidwe kake

Ma PC 10 - mapepala otumphukira (2) - mapaketi a makatoni.
Ma PC 10 - matumba otumphukira (3) - mapaketi a makatoni.
Ma PC 10 - mapaketi a matuza (4) - mapaketi a makatoni.
Ma PC 10 - matumba otumphuka (5) - mapaketi a makatoni.
Ma PC 10 - matumba a matuza (6) - mapaketi a makatoni.

Mankhwala

Captopril-STI ndi zoletsa za ACE zomwe zimachepetsa mapangidwe a angiotensin II kuchokera ku angiotensin I, zomwe zimatsogolera kuchepa mwachindunji kutulutsidwa kwa aldosterone. Potengera maziko awa, kutumiza ndi kukweza mtima, kuthamanga kwa magazi (BP), komanso zotumphukira zamitsempha.

Mankhwala zochita za mankhwala, chifukwa cha mphamvu ya yogwira mankhwala (capopril), akuphatikizanso:

• kukula kwa mitsempha (kwakukulu kufikira mitsempha),
• kuchuluka kwa kuphatikiza kwa prostaglandin ndi kuchepa kwa kuchepa kwa bradykinin,
• kuchuluka kwaimpso ndi magazi.
• kuchepa kwa kuwononga kwa hypertrophy ya malinga a myocardium ndi mitsempha ya mtundu wotsalira (pogwiritsa ntchito mankhwala kwa nthawi yayitali),
• kuchuluka kwa magazi kupita ku ischemic myocardium,
• kuchepa kwa maplatelet
• kuchepa kwa Na + pakumwa mtima,
• kutsitsa kuthamanga kwa magazi popanda chitukuko cha Reflex tachycardia (mosiyana ndi kuwongolera vasodilators - minoxidil, hydralazine), zomwe zimapangitsa kutsika kwa mpweya wa myocardial oxygen.

Mphamvu ya antihypertensive ya Captopril-STI sizimadalira ntchito ya plasma, ndipo kuchepa kwa kuthamanga kwa magazi motsutsana ndi kugwiritsidwa ntchito kwake kumadziwika bwino komanso kosachepera milingo ya mahomoni, zomwe zimapangitsa zotsatira za minyewa ya renin-angiotensin.

Odwala ndi mtima kulephera, kutenga angiotensin-kutembenuza enzyme zoletsa muyezo wokwanira sizimayambitsa kuthamanga kwa magazi.

Pambuyo pakukonzekera kwa pakamwa, kutsika kwakukulu kwa kuthamanga kwa magazi kumawonedwa pambuyo pa maola 1 mpaka 1.5. Kutalika kwa mphamvu ya mankhwalawa kumatengera mlingo wa Captopril-STI ndikufikira pazabwino zambiri masabata angapo.

Zotsatira za pharmacological

Antihypertensive wothandizira, ACE inhibitor. Kupanga kwa antihypertensive kanthu kumalumikizidwa ndi kupikisana kwa ntchito ya ACE, komwe kumayambitsa kuchepa kwa chiwerengero cha kutembenuka kwa angiotensin I kupita ku angiotensin II (yemwe ali ndi tanthauzo la vasoconstrictor zotsatira ndikuthandizira kubisalira kwa aldosterone mu adrenal cortex). Kuphatikiza apo, Captopril akuwoneka kuti akukhudza dongosolo la kinin-kallikrein, kupewa kupasuka kwa bradykinin. Mphamvu ya antihypertensive siyidalira ntchito ya plasma renin, kuchepa kwa magazi kumadziwonekera mwazonse komanso ngakhale kutsika kwa mahomoni, zomwe zimachitika chifukwa cha zovuta za RAAS. Kuchulukitsa kwa magazi ndi impso.

Chifukwa cha vasodilating zotsatira, amachepetsa OPSS (kutsitsa), kuthinana kwamankhwala m'matumbo am'mapapu (kutsitsa) ndi kukana m'matumbo a m'mapapo, kumawonjezera kutuluka kwa mtima ndi kulolerana zolimbitsa thupi. Kugwiritsa ntchito nthawi yayitali, kumachepetsa kuuma kwa kumanzere kwamitsempha yamagazi, kumalepheretsa kuchepa kwa mtima ndikuchepetsa kukula kwa kuchepa kwamitsempha yamanzere. Amathandizira kuchepetsa sodium odwala omwe ali ndi vuto la mtima losalephera. Imakulitsa mitsempha pamlingo wokulirapo kuposa mitsempha. Amasintha magazi kupita ku ischemic myocardium. Imachepetsa kuphatikizika kwa mapulosi.

Imachepetsa kamvekedwe ka michere ya impso, kukonza makonzedwe a hemodynamics, ndikuletsa kukula kwa matenda a shuga.

Pharmacokinetics

Pambuyo pakukonzekera pakamwa, osachepera 75% amatengedwa mwachangu kuchokera mumimba. Kudya munthawi yomweyo kumachepetsa mayamwidwe ndi 30-40%. C max m'madzi a m'magazi amafikira pambuyo pa mphindi 30-90. Kumanga mapuloteni, makamaka ndi albumin, ndi 25-30%. Wotsekedwa mkaka wa m'mawere. Zimapangidwa m'chiwindi ndikupanga kapangidwe ka Captopril disulfide dimer ndi Captopril cysteine ​​disulfide. Ma metabolabolites ndi opanga ma pharmacologic.

T 1/2 ndi ochepera maola atatu ndipo imachulukanso ndi kulephera kwa impso (maola 3,5 mpaka 32). Kuposa 95% amachotsa impso, 40-50% osasinthika, ena onse - munthawi ya metabolites.

Kulephera kwa aimpso, kumachitika.

Zizindikiro zamankhwala

Zotsatira zoyipa

Kuchokera mbali ya chapakati mantha dongosolo ndi zotumphukira mantha dongosolo: chizungulire, kupweteka kwa mutu, kutopa, asthenia, paresthesia.

Kuchokera pamtima dongosolo: orthostatic hypotension, kawirikawiri - tachycardia.

Kuchokera pamimba: kukhumudwa, kusowa kudya, kuphwanya mphamvu zam'mano, kawirikawiri - kupweteka kwam'mimba, kutsegula m'mimba kapena kudzimbidwa, kuchuluka kwa chiwindi transaminases, hyperbilirubinemia, zizindikiro za kuwonongeka kwa hepatocellular (hepatitis), nthawi zina - cholestasis, padera.

Kuchokera ku hemopoietic dongosolo: kawirikawiri - neutropenia, kuchepa magazi, thrombocytopenia, osowa kwambiri mwa odwala omwe ali ndi matenda a autoimmune - agranulocytosis.

Kuchokera kumbali ya kagayidwe: hyperkalemia, acidosis.

Kuchokera kwamikodzo dongosolo: proteinuria, mkhutu aimpso (kuchuluka kwa urea ndi creatinine m'magazi).

Kuchokera pakupuma dongosolo: chifuwa chowuma.

Zotsatira zoyipa: zotupa pakhungu, kawirikawiri - edema ya Quincke, bronchospasm, seramu matenda, lymphadenopathy, nthawi zina - mawonekedwe a antiinodar antibodies m'magazi.

Mimba komanso kuyamwa

Tiyenera kukumbukira kuti kugwiritsa ntchito Captopril mu II ndi III trimesters pamimba kungayambitse kusokonezeka kwa chitukuko ndi kufa kwa fetal. Ngati mimba yakhazikitsidwa, captopril iyenera kuchotsedwa nthawi yomweyo.

Captopril amachotseredwa mkaka wa m'mawere. Ngati ndi kotheka, ntchito pa mkaka wa m`mawere ayenera kusankha pa kuyamwitsa.

Gwiritsani ntchito ntchito yolakwika yaimpso

Chenjezo uyenera kugwiritsidwa ntchito mu mawonekedwe a kupatsirana kwa impso, kulephera kwa impso.

Ngati aimpso ntchito, tsiku lililonse mlingo uyenera kuchepetsedwa.

Kugwiritsa ntchito munthawi yomweyo mankhwala osokoneza bongo a potaziyamu komanso kukonzekera kwa potaziyamu odwala ayenera kupewedwa.

Malangizo apadera

Chenjezo liyenera kugwiritsidwa ntchito ngati pali mbiri ya angioedema odwala omwe ali ndi ACE inhibitor mankhwala, cholowa kapena idiopathic angioedema, ndi aortic stenosis, matenda a mtima komanso matenda amtima (kuphatikizira kwa kuchepa kwa magazi, matenda a mtima, kuchepa kwa mphamvu ya coronary). matenda a autoimmune a minofu yolumikizira (kuphatikiza SLE, scleroderma), ndi chopinga cha m'matumbo a hematopoiesis, odwala matenda a shuga, hyperkalemia, bilpatal renal aren stenosis, mtsempha wama impso amodzi, boma litafalikira, impso ndi / kapena kulephera kwa chiwindi, motsutsana ndi zakudya zomwe zimaletsedwa ndi sodium, mikhalidwe yotsatana ndi kuchepa kwa BCC (kuphatikiza kutsekula m'mimba, kusanza), mwa odwala okalamba.

Odwala omwe ali ndi matenda a mtima osakhazikika, mankhwalawa amagwiritsidwa ntchito moyang'aniridwa ndi achipatala.

Arterial hypotension yomwe imachitika pakuchita opareshoni pomwe mukumwa mankhwalawa amachotsedwa ndikubwezeretsanso kuchuluka kwa madzimadzi.

Kugwiritsa ntchito munthawi yomweyo mankhwala osokoneza bongo a potaziyamu komanso kukonzekera kwa potaziyamu kuyenera kupewedwa, makamaka kwa odwala omwe amalephera impso ndi matenda a shuga.

Mukamamwa mankhwalawa, zotsatira zoyipa zimawonedwa pokambirana mkodzo wa acetone.

Kugwiritsa ntchito kwa ana m'mitengo ya ana kumatheka pokhapokha ngati mankhwala ena sangathe.

Kukopa pa kuyendetsa magalimoto ndi kayendedwe kazinthu

Kusamala kumafunikira poyendetsa magalimoto kapena pochita ntchito ina yofunika kuthandizira, monga chizungulire n`kotheka, makamaka pambuyo koyamba mlingo wa captopril.

Kuyanjana kwa mankhwala osokoneza bongo

Pogwiritsa ntchito munthawi yomweyo ndi ma immunosuppressants, cytostatics, chiopsezo chokhala ndi leukopenia ukuwonjezeka.

Pogwiritsa ntchito munthawi yomweyo mankhwala osokoneza bongo a potaziyamu, kuphatikizapo spironolactone, triamteren, amiloride, kukonzekera kwa potaziyamu, mchere wothandizidwa ndi zakudya komanso zowonjezera pazakudya zomwe zili ndi potaziyamu, hyperkalemia imatha kupezeka (makamaka odwala omwe ali ndi vuto la impso), chifukwa ACE zoletsa amachepetsa zomwe zili aldosterone, zomwe zimayambitsa kuchepa kwa potaziyamu m'thupi motsutsana ndi kumbuyo kwa kuchepetsa kwa potaziyamu kapena kuchuluka kwake.

Pogwiritsa ntchito munthawi yomweyo ACE zoletsa ndi NSAIDs, chiopsezo chokhala ndi vuto la impso chimawonjezeka, Hyperkalemia sichioneka.

Pogwiritsa ntchito munthawi yomweyo "loop" diuretics kapena thiazide diuretics, kutanthauzira kwa hypotension kungatheke, makamaka mutatenga gawo loyamba la okodzetsa, mwachiwonekere chifukwa cha hypovolemia, yomwe imayambitsa kuchepa kwakanthawi mu mphamvu ya antihypertensive. Pali chiopsezo cha hypokalemia. Chiwopsezo chowonjezeka cha matenda aimpso.

Ndi munthawi yomweyo kugwiritsa ntchito mankhwala osokoneza bongo, ochepa ochepa hypotension n`zotheka.

Pogwiritsa ntchito munthawi yomweyo ndi azathioprine, kuchepa magazi m'thupi kungayambike chifukwa choletsa zinthu za erythropoietin mothandizidwa ndi ACE zoletsa ndi azathioprine. Milandu yokhudzana ndi leukopenia akufotokozedwa, omwe amatha kuphatikizidwa ndi zowonjezera zoletsa za ntchito ya m'mafupa.

Pogwiritsa ntchito munthawi yomweyo ndi allopurinol, chiopsezo chotenga matenda amtunduwu chikuwonjezeka, milandu ya chitukuko chachikulu cha zochita za hypersensitivity, kuphatikizapo Stevens-Johnson syndrome, ikufotokozedwa.

Ndi munthawi yomweyo kugwiritsa ntchito aluminium hydroxide, magnesium hydroxide, magnesium carbonate, bioavailability wa Captopril yafupika.

Acetylsalicylic acid mu Mlingo wambiri ungachepetse mphamvu ya antihypertensive. Sizinakhazikitsidwe mwatsatanetsatane ngati acetylsalicylic acid imachepetsa kuchiritsa kwa ACE zoletsa mwa odwala omwe ali ndi matenda amitsempha yamagazi ndi matenda a mtima. Zomwe matendawa amatengera zimadalira matendawa. Acetylsalicylic acid, zoletsa COX ndi syntaglandin kaphatikizidwe, zimatha kuyambitsa vasoconstriction, komwe kumayambitsa kuchepa kwa kutulutsa kwamtima komanso kuwonongeka kwa chikhalidwe cha olephera a mtima omwe alandila ACE zoletsa.

Pali malipoti akuwonjezereka kwa kuchuluka kwa digoxin m'magazi am'magazi ndi kugwiritsa ntchito pamodzi kwa Captopril ndi digoxin. Chiwopsezo cha kuyanjana ndi mankhwala chikuwonjezeka mwa odwala omwe ali ndi vuto laimpso.

Pogwiritsidwa ntchito munthawi yomweyo ndi indomethacin, ibuprofen, antihypertensive mphamvu ya capopril imatsika, mwachidziwikire chifukwa cha chopinga cha syntaglandin synthesis mothandizidwa ndi NSAIDs (omwe akukhulupirira kuti atengapo gawo pachitukuko cha zotsatira zoyipa za ACE zoletsa).

Pogwiritsa ntchito pamodzi ndi ma insulin, othandizira a hypoglycemic, zotumphukira za sulfonylurea, hypoglycemia imatha kuyamba chifukwa cha kulolerana kwa shuga.

Ndi kugwiritsa ntchito pamodzi kwa ACE zoletsa ndi ma interleukin-3, pali chiopsezo chokhala ochepa hypotension.

Ndi munthawi yomweyo kugwiritsa ntchito interferon alpha-2a kapena interferon beta, milandu ya kukula kwa granulocytopenia amafotokozedwa.

Mukasintha kuchokera ku kutenga clonidine kukhala Captopril, mphamvu yotsutsa yamapeto imayamba pang'onopang'ono. Pankhani ya kusiya kwadzidzidzi kwa clonidine mwa odwala omwe akulandiridwa ndi capopid, kuwonjezereka kwakukulu kwa kuthamanga kwa magazi ndikotheka.

Ndi munthawi yomweyo kugwiritsa ntchito lifiyamu ya carbonum, kuchuluka kwa maamuamu m'magazi a seramu kumawonjezera, limodzi ndi zizindikiro za kuledzera.

Pogwiritsa ntchito munthawi yomweyo ndi minoxidil, sodium nitroprusside, mphamvu ya antihypertensive imatheka.

Pogwiritsa ntchito nthawi yomweyo ndi orlistat, captopril imakhala yothandiza kwambiri, yomwe imatha kubweretsa kuchuluka kwa magazi, vuto la matenda oopsa, komanso chifukwa cha kukha magazi kwa ziwalo.

Pogwiritsa ntchito munthawi yomweyo ACE zoletsa zomwe zimakhala ndi perorid, kuwonjezeka kwa antihypertensive kungatheke.

Pogwiritsa ntchito munthawi yomweyo ndi phenenecid, chidziwitso cha impso chimachepa.

Pogwiritsa ntchito munthawi yomweyo ndi procainamide, chiwopsezo chokhala ndi leukopenia nchotheka.

Pogwiritsa ntchito munthawi yomweyo ndi trimethoprim, pamakhala chiopsezo chokhala ndi hyperkalemia, makamaka kwa odwala omwe ali ndi vuto laimpso.

Kugwiritsa ntchito pamodzi ndi chlorpromazine, pamakhala chiopsezo chokhala ndi orthostatic hypotension.

Pogwiritsa ntchito munthawi yomweyo ndi cyclosporine, pali malipoti a kakulidwe kaimpso kulephera, oliguria.

Amakhulupirira kuti kuchepa kwa kugwiritsa ntchito antihypertensive mankhwala pogwiritsa ntchito erythropoietins ndikotheka.

Zotsatira zoyipa

Kutheka kovuta komwe kungachitike> 10% - nthawi zambiri (> 1% ndi 0,1% ndi 0,01% ndi + mu seramu yamagazi. Ngati matenda a shuga apezeka, kulephera kwaimpso, kumwa mankhwala a potaziyamu, mankhwala okhala ndi potaziyamu kapena mankhwala omwe amachulukitsa kuchuluka kwa potaziyamu m'magazi (mwachitsanzo, heparin) kumawonjezera chiopsezo cha hyperkalemia.Nthawi imeneyi, tikulimbikitsidwa kupewa mankhwala ophatikizana ndi potaziyamu osasamala okonzekera potaziyamu.

Panthawi ya hemodialysis pa kasamalidwe ka Captopril-STI, ndikofunikira kuti muchepetse kugwiritsa ntchito michere ya dialysis yokhala ndi vuto lalikulu (mwachitsanzo, AN69), popeza muzochitika zotere zimachitika.

Pamene edema ya angioneurotic ikuwonekera, ma eniotensin osandulika otembenuza amalephera, wodwalayo amayang'aniridwa mosamala komanso amathandizidwa ndi chithandizo chamankhwala.

Tiyenera kukumbukira kuti zotsatira za kusanthula kwamkodzo kwa acetone panthawi yakutenga kwa captopril zitha kukhala zabodza.

Odwala omwe ali ndi mchere wochepa kapena wopanda mchere wopanda mchere ayenera kudya Captopril-STI mosamala, chifukwa chowonjezera chiopsezo cha ochepa hypotension.

Contraindication

Hypersensitivity (kuphatikiza kwa ACE enhibitors ena), angioedema (mbiri ya mankhwala ndi ACE zoletsa kapena cholowa), aimpso / kwa chiwindi, kuperewera, kuchepa kwa impso limodzi ndi azotemia, mkhalidwe pambuyo pa kupatsirana kwa impso, IHSS, matenda ndi mikhalidwe yovuta kutuluka kwa magazi kuchokera ku LV, kutenga pakati, kuyamwa, zaka zosakwana zaka 18 (kuchita bwino ndi chitetezo sizinakhazikitsidwe).

Momwe mungagwiritsire ntchito: Mlingo ndi njira ya chithandizo

Mkati, ola limodzi musanadye, komanso matenda oopsa, chithandizo chimayamba ndi mlingo wochepa kwambiri wa 12,5 mg kawiri pa tsiku. Ngati ndi kotheka, mlingo umakulitsidwa pang'onopang'ono pakadutsa masabata 2-4 mpaka mulingo woyenera. Ndiofatsa pang'ono kwamankhwala oopsa, kuchuluka kwa mankhwalawa nthawi zambiri kumakhala 25 mg kawiri pa tsiku, mlingo waukulu ndi 50 mg kawiri pa tsiku. Pa matenda oopsa kwambiri, magazi oyamba ndi 12,5 mg 2 kawiri pa tsiku, omwe amayamba kuwonjezeka pang'onopang'ono mpaka tsiku lililonse 150 mg (50 mg katatu tsiku).

Mu CHF, mlingo woyambira tsiku lililonse ndi 6.25 mg katatu pa tsiku, ngati kuli kotheka, onjezani mlingo ndi masabata osachepera awiri. Mlingo wapakati wokonza ndi 25 mg katatu patsiku. Mlingo wambiri watsiku ndi tsiku ndi 150 mg.

Ngati vuto la LV layimitsidwa pambuyo povutika m'mitsempha yamatumbo mwa odwala omwe ali ndi matenda okhazikika, mankhwalawa amatha kuyambika patangotha ​​masiku atatu pambuyo poti myocardial infarction. Mlingo woyambirira ndi 6.25 mg / tsiku, ndiye kuti tsiku lililonse mlingo ungathe kuchuluka mpaka 37,5-75 mg mu 2-3 Mlingo (malingana ndi kulekerera kwa mankhwalawa) mpaka mpaka 150 mg / tsiku.

Mu matenda a shuga a nephropathy, muyezo wa 75-150 mg / tsiku ndi mankhwala Mlingo wa 2-3. Mu 1 mtundu wa shuga ndi macroalbuminuria (30-300 mg / tsiku) - 50 mg kawiri pa tsiku. Ndi kwathunthu mapuloteni oposa 500 mg / tsiku - 25 mg katatu pa tsiku.

Ndi mulingo woyenera waimpso ntchito (CC osachepera 30 ml / mphindi / 1.73 sq.m) - 75-100 mg / tsiku. Ndi kuchuluka kutalika kwa aimpso (CC osakwana 30 ml / mphindi / 1.73 m), muyezo woyambira sapitirira 12,5 mg kawiri pa tsiku, ndiye, ngati kuli koyenera, mlingo wa capopril umakulitsidwa pang'onopang'ono ndi nthawi yayitali mpaka achire akwaniritse, koma tsiku lililonse ikhale yotsika kuposa masiku onse.

Mwa odwala okalamba, mlingo woyambirira ndi 6.25 mg 2 kawiri pa tsiku.

Kuchita

Mphamvu ya antihypertensive imafooka ndi indomethacin ndi ena NSAID, kuphatikiza kusankha COX-2 zoletsa (akuchedwa Na + ndi kuchepa kwa kaphatikizidwe ka Pg), makamaka motsutsana ndi maziko am'mbuyo mwa renin, komanso estrogens (akuchedwa Na +).

Kuphatikiza ndi thiazide diuretics, vasodilators (minoxidil) kumathandizira hypotensive zotsatira.

Kuphatikiza pamodzi ndi potaziyamu mosamala okodzetsa, K + kukonzekera, zowonjezera potaziyamu, mchere wam'malo (wokhala ndi zochuluka za K +) kumawonjezera chiopsezo cha hyperkalemia.

Imachepetsa kuchotseka kwa mankhwala a Li +, ndikuwonjezera kuchuluka kwake m'magazi.

Ndi kusankha kwa captopril pamene mukumwa allopurinol kapena procainamide, chiopsezo chotenga matenda a Stevens-Johnson ndi neutropenia chikuwonjezeka.

Pogwiritsa ntchito munthawi yomweyo ACE zoletsa komanso kukonzekera golide (sodium aurothiomalate), chizindikiro chafotokozedwa, kuphatikiza nkhope, kutupa, nseru, kusanza komanso kuchepa kwa kuthamanga kwa magazi.

Insulin ndi mankhwala ena amkamwa a hypoglycemic - chiopsezo cha hypoglycemia.

Kugwiritsidwa ntchito kwa Captopril odwala omwe amalandila ma immunosuppressants (kuphatikizapo azathioprine kapena cyclophosphamide) kumawonjezera chiopsezo cha zovuta za hematological.

Kutulutsa mafomu ndi kapangidwe kake

Kukonzekera ndi chinthu choyera cha khristalo, chosungunuka mosavuta mu methyl, mowa wa ethyl ndi madzi, wokhala ndi fungo losalala la sulufule. The solubility ya mankhwala mu ethyl acetate ndi chloroform ndi dongosolo la kukula kwambiri. Thupi silisungunuka mu ether.

Chogulikacho chimapezeka m'mapiritsi okhala ndi mafuta a kayendetsedwe ka kayendetsedwe ka kayendetsedwe ka kayendetsedwe ka kayendetsedwe ka zinthu.

Kuphatikiza pa chophatikizira chachikulu mu 12,5-100 mg, piritsi imakhala ndi zinthu zina zothandiza: silicon dioxide, stearic acid, MCC, wowuma, etc.

Zimagwira bwanji?

The pharmacological mphamvu ya Captopril akadali kuphunzira.

Kuponderezedwa kwa dongosolo la renin-angiotensin-aldosterone (PAA) ndi mankhwalawa kumabweretsa zotsatira zake zabwino pothandizira kulephera kwa mtima komanso kuthamanga kwa magazi.

Zochita za Captopril ndikuchepetsa kufooka kwa mtima kwaponseponse kwamitsempha yamagazi (OPSS).

Renin wopangidwa ndi impso amagwira ntchito m'magazi a plasma globulin, zomwe zimayambitsa kupangika kwa decapeptide ndi angiotensin. Kenako, mothandizidwa ndi ACE (angiotensin-kutembenuza enzyme), mankhwala a vasoconstrictor a endo native, angiotensin l amasinthidwa kukhala angiotensin ll, omwe amachititsa kaphatikizidwe ka aldosterone ndi adrenal cortex. Zotsatira zake, madzi ndi sodium amazisungira.

Zochita za Captopril ndikuchepetsa kufooka kwa mtima kwaponseponse kwamitsempha yamagazi (OPSS). Poterepa, zotsatira za mtima zimachuluka kapena sizimasinthika. Kuchuluka kwa kusefera mu impso glomeruli sikusintha.

Kuyamba kwa hypotensive mphamvu ya mankhwalawa kumachitika 60-90 patatha mphindi imodzi.

Mankhwalawa amalembedwa kwa nthawi yayitali, chifukwa kuthamanga kwa magazi m'matumbo kumachepa pang'onopang'ono mothandizidwa ndi mankhwalawa. Pogwiritsa ntchito kuphatikiza kwa Captopril ndi thiazide diuretics, kuwonjezera kwawo kumawonedwa. Chikuonetseratu kuphatikiza ndi beta-blockers sichiyambitsa kukonzekera kwa izi.

Kuthamanga kwa magazi kumafikira manambala pang'onopang'ono, osatsogolera pakupanga tachycardia ndi orthostatic hypotension. Palibe kukwera mwachangu kwa kuthamanga kwa magazi komanso kusiya mwachangu mankhwala.

Kutsika kwa kugunda kwa mtima, kuchepa kwa kuthamanga kwa magazi, kuthamanga kwa mtima, kukokana kwa mtima, kuchuluka kwa zotuluka zamtima, ndi zizindikiro za kuyeseza kochita masewera olimbitsa thupi zimawonedwa mwa odwala omwe ali ndi matenda a mtima pa nthawi ya capopril. Komanso, zotulukazi zimapezeka mwa odwala mutatha kumwa koyamba, kupitiriza chithandizo.

Chithandizocho chimasungunuka m'madzi a m'mimba ndipo amalowa m'magazi kudzera m'matumbo. Kuzindikira kwakukulu m'magazi kumafika pafupifupi ola limodzi.

Mankhwala anagwiritsidwa ntchito pochizira matenda aimpso.

Kudzera m'magazi, chinthucho chimagwira ntchito pa puloteni ya ACE m'mapapu ndi impso ndipo imalepheretsa. Mankhwala amachotseredwa woposa theka mosasintha. Mwanjira ya metabolite yogwira ntchito, imapukusidwa kudzera mu impso ndi mkodzo. 25-30% ya mankhwala imalowa mukulumikizana ndi mapuloteni amwazi. 95% ya mankhwala amuchotsa impso pambuyo pa maola 24. Maola awiri pambuyo pa kuperekera, kuchuluka kwa magazi kumachepa pafupifupi theka.

Kulephera kwamkati kwa odwala omwe amamwa mankhwalawa kumabweretsa kuchepa kwake m'thupi.

Zomwe zimathandiza

Mankhwala anagwiritsidwa ntchito pochiza:

1. Matenda oopsa: mawonekedwe a piritsi amagwiritsidwa ntchito ngati chithandizo chachikulu kwa odwala omwe ali ndi impso yosungidwa. Odwala omwe ali ndi vuto laimpso, makamaka omwe ali ndi collagenosis, sayenera kugwiritsa ntchito mankhwalawa atapezeka kale pa mankhwala ena. Chidacho chitha kugwiritsidwa ntchito ngati monotherapy kapena kuphatikiza ndi zinthu zina zamankhwala.
2. Kulephera kwa mtima kwamphamvu: Captopril therapy imagwiritsidwa ntchito limodzi ndi digitis ndi diuretics.
3. Kuphwanya kwaposachedwa kwa infurated yam'mbuyo ntchito: kuchuluka kwaopulumuka kwa odwala otere kumakulitsidwa chifukwa cha kuchepa kwa kachigawo kotulutsa mtima mpaka 40%.
4. Matenda a diabetesic nephropathy: kufunikira kwa dialysis ndi kupatsirana kwa impso kumachepetsedwa ndikuchepetsa kupitilira kwa vuto la nephrotic. Amagwiritsidwa ntchito ngati insulin yodalira matenda a shuga ndi nephropathy okhala ndi proteinuria yoposa 500 mg / tsiku.
5. Matenda oopsa.

Pazovuta za mtima, Captopril mankhwala amagwiritsidwa ntchito limodzi ndi digitis ndi diuretics.

Momwe mungatengere

Ndi kuthamanga kwa magazi, imwani pang'onopang'ono mutamwa.

Ndikofunikira kumwa mankhwalawa ola limodzi musanadye, chifukwa zomwe zili m'mimba zimatha kuchepetsa kuyamwa kwa zinthu ndi 30-40%.

Chithandizo cha nthawi yayitali chimatsatana ndikumwa mankhwala mkati. Ngati mankhwalawo amagwiritsidwa ntchito pochiritsa mwadzidzidzi ndi kuwonjezeka kwa kuthamanga kwa magazi komwe kumachitika chifukwa cha kutengeka mtima kapena thupi, umaperekedwa pansi pa lilime.

Patha mphindi 15 kuchokera pakamwa, chinthucho chimazungulira m'magazi.

Ndi sublingual makonzedwe, bioavailability ndi kuchuluka kwa mwadzidzidzi zotsatira.

Kuyamba kwa mankhwala kumayendetsedwa ndi kuperekera mankhwala omwe amagawidwa m'mankhwala amadzulo ndi m'mawa.

Kuyamba kwa mankhwala kumayendetsedwa ndi kuperekera mankhwala omwe amagawidwa m'mankhwala amadzulo ndi m'mawa.

Chithandizo cha kulephera kwa mtima chimaphatikizapo kugwiritsa ntchito mankhwala katatu patsiku. Ngati cholinga cha Captopril chokha sichitha kuchepetsa kukakamira, hydrochlorothiazide imatchulidwa ngati antihypertensive yachiwiri. Palinso mtundu wina wapadera wa mulingo womwe umaphatikizapo zinthu zonsezi (Caposide).

Chithandizo cha kupanikizika kwakukulu chimayamba ndi tsiku la 25-50 mg. Kenako, mankhwalawo amawonjezereka, monga momwe dokotala amafotokozera, pang'onopang'ono mpaka magazi atakhala abwinobwino. Komabe, siziyenera kupitirira muyeso wokwanira 150 mg.

Chithandizo cha kulephera kwa mtima zimaphatikizapo kuyambira ndikugwiritsa ntchito Mlingo umodzi wa 6.5-12,5 mg ndi kuwonjezeka kowonjezereka ngati pakufunika.

Chithandizo cha kulephera kwa mtima zimaphatikizapo kuyambira ndikugwiritsa ntchito Mlingo umodzi wa 6.5-12,5 mg ndi kuwonjezeka kowonjezereka ngati pakufunika.

Kuyamba kuvomereza kumachitika tsiku lachitatu pambuyo kuwonongeka kwa minofu yamtima. Mankhwalawa aledzera malinga ndi chiwembu:

1. 6.25 mg kawiri tsiku lililonse kwa masiku atatu oyamba.
2. Pakati pa sabata, 12,5 mg kawiri pa tsiku.
3. Masabata 2-3 - 37,5 mg, wogawidwa 3 waukulu.
4. Ngati mankhwalawa amaloledwa popanda chovuta, mlingo wa tsiku ndi tsiku umasinthidwa kukhala 75 mg, ndikuwonjezera ngati 150 mg.

Captopril imayamba tsiku lachitatu pambuyo kuwonongeka kwa minofu yamtima.

Matenda a shuga a shuga okhala ndi mkodzo wambiri mu mkodzo amafunika kugwiritsa ntchito mankhwala osokoneza bongo kawiri patsiku, ofanana ndi 50 mg. Ngati kuchuluka kwa mapuloteni kupitirira 500 mg mu mkodzo watsiku ndi tsiku - 25 mg katatu.

Ndi limodzi ndi matenda a shuga a mellitus l l nephropathy, mlingo wa 75-100 mg / tsiku umagawidwa mu Mlingo wa 2-3.

Bongo

Kumwa Mlingo wowonjezera pamiyeso yomwe imalimbikitsa kungayambitse kutsika kwa magazi. Kuphatikiza apo, pakhoza kukhala zovuta mu mawonekedwe a thromboembolism ikuluikulu yamitsempha yamagazi, mitsempha yamagazi ya mtima ndi ubongo, zomwe, zimatha kuyambitsa matenda a mtima ndi stroke.

Ndi bongo wa Captopril, hemodialysis imafunika.

Njira zotsatirazi zimatengedwa ngati njira ya chithandizo:

1. Muzimutsuka m'mimba mutachotsa kapena kuchepetsa kuchuluka kwa mankhwalawo.
2. Bwezeretsani magazi, ndikupatsa wodwalayo malo okhala ndi miyendo, ndikukweza kulowetsedwa kwa mchere, Reopoliglyukin kapena plasma.
3. Yambitsani Epinephrine kudzera m'mitsempha kapena mozungulira kuti muwonjezere magazi. Monga othandizira, gwiritsani ntchito hydrocortisone ndi antihistamines.
4. Chitani hemodialysis.

Malo opumulira a captopril kuchokera ku mankhwala

Pokhapokha malinga ndi Chinsinsi cholembedwa pa fomu yapadera mu Chilatini, mwachitsanzo:

1. Rp. Captoprili 0.025.
2. D.t.d. N 20 mu tabulettis.
3. S. 1 piritsi theka la ola musanadye m'mawa ndi madzulo.

Mtengo wa mankhwalawa umasiyana ndi ma ruble 9-159.

Ndemanga za madotolo ndi odwala za Captopril

Oksana Aleksandrovna, Pskov, dokotala wazachipatala: “Ndimagwiritsa ntchito Captopril ngati ambulansi ya mavuto. Nthawi zambiri amalephera, motero ndibwino kulabadira: kodi ndi mankhwala osokoneza bongo kapena oyambirirawo. "

Maria, wazaka 45, ku Moscow: “Ndimamwa mankhwalawo motsimikiza kwa dokotala wamtima wokonda kupanikizika. Zotsatira zake sizoyipa kuposa zomwe zinkachitika masiku onse a Moxonidine. Imagwira ntchito yake "yothandiza" mwangwiro, komanso pamtengo wabwino chotere. ”

Vitaliy Konstantinovich, Krasnodar, dokotala wamtima: “Ngati wodwala akufunika kusankha, mungakhale ndi Kapoten kapena Captopril, ndikulimbikitsa woyamba. Inde, zomwe zimagwiritsidwa ntchito m'mankhwala onsewa ndi zofanana, koma chimodzi ndi choyambirira, chachiwiri ndi kope. Odwala nthawi zambiri amadandaula za kufooka kwa mankhwalawa, ngakhale kuti amagwiritsidwa ntchito pamavuto omwe thandizo limayenera kukhala lachangu komanso labwino. Ndikupangira Kapoten kwa odwala omwe ali ndi vuto lotetemera kwambiri, chifukwa kwa ine ndekha ndikanatha kumwa mankhwalawa. Komanso, mtengo umalola. ”

Phunziro la UKPDS

Chimodzi mwa umboni woyamba wa chitetezo ndi kugwiritsa ntchito bwino kwa matenda a BB mu mtundu 2 wa matenda ashuga chinali kutsiriza kuphunzira kwa UKPDS, komwe kuyerekeza kuchepa kwa thupi ndi kufa, komanso zovuta zamatenda am'mimba (MD, DR) odwala omwe ali ndi matenda a shuga a 2 omwe ali ndi matenda oopsa Captopril pa mlingo wa 25-50 mg 2 kawiri pa tsiku (anthu 400), kapena kusankha atenolol BB pa mlingo wa 50-100 mg / tsiku (anthu 358).

Pambuyo pa nthawi yowonera (zaka 8.4) m'magulu onse awiri, gawo lomwelo la kuthamanga kwa magazi lidakwaniritsidwa: 144/83 mmHg. Art. pagulu la Captopril ndi 143/8 mm RT. Art. m'gulu la atenolol. Nthawi yomweyo, panalibe kusiyana kwakukulu pamalingaliro oyerekeza omaliza (ziwopsezo zomwe zimagwirizanitsidwa ndi matenda ashuga, kuchuluka kwa zochitika pamtima, zovuta zam'magazi) pakati pamagulu. Mwanjira ina, Captopril ndi atenolol adachititsanso chitetezo chotere motsutsana ndi zovuta zazing'ono komanso zazikulu kwambiri kwa odwala omwe ali ndi matenda a shuga a 2.

Monga ndemanga, ndikufuna kudziwa kuti kafukufuku wa UKPDS adayamba kumapeto kwa m'ma 1970, pomwe Captopril anali yekhayo woyeserera wa ACE pamsika wapadziko lonse. M'mazaka amenewo, regopen regimen ya 25-100 mg 2 kawiri pa tsiku idalandiridwa. Komabe, patapita nthawi anazindikira kuti mankhwalawa samatha kuyambitsa mphamvu antihypertensive masana, chifukwa mankhwalawa amakhala ndi nthawi yayifupi (maola 4-6).

Kuti muchepetse kuthamanga kwa magazi, makonzedwe atatu a mankhwalawa tsiku lililonse mu 150 mg umafunika. Chifukwa chake, kufananizidwa kwa wogwirizira wogwirizira kwakanthaŵi ndi atenolol wokhala ndi nthawi yayitali sikunali koyenera pamalingaliro. Komabe, onse awiriwa anali ndi chitetezo chofanana. Nditapeza zotsatira za kafukufuku wa UKPDS, zinaonekeratu kuti kugwiritsa ntchito BB posankha odwala omwe ali ndi matenda ashuga a 2 ndipo AT ndi otetezeka komanso othandiza.

Phunziro la GEMINI (Zotsatira za Glycemic in Diabetes Mellitus: Carvedilol-Metoprolol Comparison in Hypertensives)

Phunziro ili lokhala ndi khungu lamaso awiri, cholinga chinali kuyeseza mwachindunji ma BB awiri pakuchiza matenda oopsa mwa odwala omwe ali ndi matenda a shuga 2: metoprolol, B β1-yosankha, ndi carvedilol, BB yosasankha, yomwe ili ndi zinthu zowonjezera zoletsa α1-AR. Ofufuzawo anena kuti chifukwa cha blockade ya α1-AR, carvedilol idzakhala ndi mwayi wopitilira metoprolol osati chifukwa chokhazikitsidwa kale ndi vasodilator, komanso, mwina, chifukwa cha zotsatira zabwino pa magawo a metabolic (dyslipidemia, IR), kuyambira cy1-AR blockade kuchuluka kwa lipoprotein lipase komwe kumaswa TG.

Phunziroli lidaphatikizapo odwala 1235 omwe ali ndi matenda oopsa komanso matenda a shuga 2. Gulu limodzi (n = 737) limalandira metoprolol tartrate muyezo wa 50-200 mg 2 kawiri pa tsiku, lachiwiri (n = 498) limalandira carvedilol muyezo wa 6.25-25 mg 2 kawiri patsiku kwa masabata a 35. Nthawi yomweyo, odwala onse adapitilirabe kumwa mankhwala a RAS blockers (ACE inhibitors kapena ARA) m'mbuyomu. Poyerekeza chizindikiro cha glycemic control, zidapezeka kuti panthawi ya chithandizo chamagulu a carvedilol, mitengo ya HbAlc sinasinthe, pomwe gulu la metoprolol limawonjezeka ndi 0.15%, sensulinivs insulin (yotsimikiziridwa ndi index ya NOMA) ikuyenda bwino pa carvedilol, koma osati metoprolol ( mlozo unachepa ndi 9.1 ndi 2, motsatana). Chiwopsezo cha UIA chinali chotsika kwambiri pa carvedilol kuposa metoprolol (6.4 ndi 10.3%, motsatana).

Chifukwa chake, kafukufukuyu adatsimikiza kwathunthu za kuopsa kogwiritsa ntchito BB m'matenda a shuga ndipo adatsimikizira kuti carvedilol sikuti imangokulitsa kuperewera kwa metabolic mu mtundu 2 wa shuga, komanso imathandizanso kuzindikira kwa insulin. Zachidziwikire, zotsatira za kafukufukuyu sizingasamutsidwe gulu lonse la BB, popeza carvedilol ili ndi zina zowonjezera za cy1-blocker, zomwe zimafotokozera zotsatira za metabolic zomwe zapezeka. Phunziroli, carvediol (Dilatrend) adagwiritsidwa ntchito ndi Hoffman - la Roche.

BB ndi kulephera kwa mtima

Kafukufuku wothandizidwa ndi BB pakulephera kwa mtima kwakhala kuli maphunziro angapo, kuphatikizaMERIT-HF (Metoprolol CR: XL Randomized Intervention Trial in congestive Mtima Kulephera), CIBIS-II (Cardiac Insufficiency Bisoprolol Study) ndi SENIOR (Kafukufuku wa Zotsatira za Nebivolol Kuyambukira Zotsatira ndi Kupatsidwanso Mphamvu kwa Achinyamata omwe ali ndi vuto la mtima).

Cholinga cha kafukufuku wa MERIT-HF chinali kudziwa chitetezo ndi kufunikira kwa BB kwa odwala omwe ali ndi vuto la mtima. Odwala 3991 omwe ali ndi zaka zapakati pa zaka 63 adaphatikizidwa ndi HYHA grade II-IV mtima Kulephera. Pafupifupi 25% ya omwe adaphatikizidwa anali odwala omwe ali ndi matenda a shuga a mtundu wa 2. Pogwiritsa ntchito njira yosaona kawiri, odwalawo adasinthidwa m'magulu awiri: kulandira metoprolol CR (wokhala nthawi yayitali) pa mlingo wa 25 mpaka 200 mg kapena placebo. Nthawi yomweyo, odwala adapitiliza kutenga diuretics (90%), ACE inhibitors (89%) ndi digitis (63%). Phunziroli lidathetsedwa asanadutse chaka kuchokera poyambira chithandizo chifukwa chodziwikiratu cha metoprolol. Chiwerengero chonse cha anthu akufa ndi mtima chinali chotsika ndi metoprolol ndi 34 ndi 38%.

Zotsatira zofananazo zidapezeka mu kafukufuku wa CIBIS-II, yemwe adaphunzira mankhwala a popoprolol omwe ali mgulu lofananalo la odwala. Phunziroli, kuchuluka kwa odwala matenda a shuga a 2 anali 12%. Kufa kwa mtima pa bisoprolol kumatsika ndi 34%.

Posachedwa, kafukufuku wa CIBIS-III adamalizidwa, cholinga chake chinali kuwonetsa kuti kuyambitsa monotherapy ndi bisoprolol kutsatiridwa ndikusamutsidwa kwa odwala omwe ali ndi vuto la mtima kulephera kuphatikizana kwa BB bisoprolol ndi ACE inhibitors enalapril sikuti latsoka pakuyambiranso kwachikhalidwe (ACE inhibitors enalapril yotsatiridwa ndikuphatikizidwa kwa BB bisoprolol) pakuthana ndi BB bisoprolol kuchuluka kwaimfa ndi kulandira zipatala. Zotsatira za miyezi 6 ya monotherapy ndi mankhwala aliwonse, ndikutsatiridwa ndikusakanizidwa kwa mankhwalawa (miyezi 18) kwa nthawi yoyamba idatsimikizira kukokomeza kuti kusankha koyambira kochizira matenda osalephera a mtima (BB ndi bisoprolol kapena ACE inhibitors enalapril) sikukhudza mfundo yayikulu (kuchuluka kwaimfa ndi zipatala pakutha kwa kuonedwa. ) ndipo akuyenera kutengera zomwe dokotala wachita posankha wodwala aliyense.

Pakufufuza kosiyana kwa gulu la odwala omwe ali ndi matenda ashuga m'maphunziro onse awiri, zidapezeka kuti chiopsezo cha kufa kwa odwala omwe ali ndi matenda a shuga 2 omwe amalandila BD anali 46% kutsika kuposa odwala omwe ali ndi matenda ashuga omwe sanalandidwe ndi BD.

Kafukufuku wakhungu wamaso awiri, wosasinthika, wowongoleredwa ndi SENIOR umalimbana ndikuwunika kuyeserera kwa nebivolol (kusankha BB yokhala ndi vasodilator) pamankhwala osokoneza mtima. Phunziroli lidaphatikizapo odwala okalamba oposa 2000 (> azaka 70), omwe 26% awo anali ndi matenda ashuga 2. Nthawi yowonera inali pafupifupi zaka ziwiri. Zotsatira zake, nebivolol yatsimikizira kugwira ntchito kwake komanso kulolera bwino pothandizidwa ndi gululi, kuphatikizapo odwala omwe ali ndi matenda a shuga 2: Kufa kwamtima ndi zipatala zachepa kwambiri poyerekeza ndi gulu la placebo.

Chifukwa chake, maphunziro omwe adachitika amatsimikizira zabwino zogwiritsira ntchito BB kwa odwala omwe ali ndi matenda osokoneza bongo omwe ali ndi vuto la mtima.

BB mankhwalawa pambuyo infaration nthawi

Kuthekera kogwiritsa ntchito BB koyambirira pambuyo povomerezeka kunaphunziridwa m'maphunziro a MIAMI (Metoprolol In Acute Myocardial infarction), ISIS-1 (Phunziro Loyamba la International International on infarct Survival), CAPRICORN (Carvedilol Post infarct Survival Control mu LV Dysfunction).

M'maphunziro onsewa, adawonetsedwa kuti kugwiritsa ntchito BB patatha nthawi ya infarction (miyezi itatu yoyambirira pambuyo panjira ya infaration yacute) imakhala yothandiza kwambiri kwa odwala omwe ali ndi matenda ashuga kuposa odwala omwe alibe shuga.

Chifukwa chake, maphunziro onsewa amatsimikizira mwayi wosagwiritsidwa ntchito wa kugwiritsidwa ntchito kwa BB kwa odwala omwe ali ndi matenda ashuga omwe ali ndi matenda a mtima m'masiku a infarction. Kuphatikiza apo, monga taonera mu kafukufuku wa Bezafibrate infarction Prevention (B1P), kuletsa BD kwa odwala matenda a shuga omwe akudwala matenda a mtima kumawonjezera kufa.

Ngakhale pali zopezeka zenizeni zakugwiritsidwe ntchito kwa BB mu matenda ashuga, komabe, ndi 40-50% yokha ya odwala omwe ali ndi matenda ashuga omwe amalandila BB panthawi yopanda infaration. Mwinanso, izi zitha kufotokozera kuti, ndi chizolowezi chakuchepetsa kufa kwa mtima mwa anthu onse, odwala omwe ali ndi matenda osokoneza bongo m'zaka zaposachedwa, kuchuluka kwa zamatenda amtima sikunangotsika komanso kuwonjezera kuchuluka.