Lithethefatsi Aterocardium: litaelo bakeng sa tšebeliso

Aterocardium e fumaneha ka mofuta oa matlapa a koahetsoeng ka filimi: pota, biconvex, pinki (likotoana tse 10 e ngoe le e ngoe ka blister, ka lebokoseng la mekotla e le 'ngoe ea 4 kapa 4).

Letlapa la 1

ntho e sebetsang: Clopidogrel (ka sebopeho sa Clopidogrel hydrosulfate) - 75 mg,
likarolo tse thusang: "magnesium stearate", povidone, lactose monohydrate, starch ea pregelatinized, polyethylene glycol 6000, cellulose ea microcrystalline,
kobo ea lifilimi: Opadry II Pink (hypromellose, triacetin, titanium dioxide, lactose monohydrate, polyethylene glycol, indigo carmine aluminium varnish, varnish e ntle ea aluminium).

Matšoao a ho sebelisoa

Aterocardium e sebelisoa ho thibela lipontšo tsa atherothrombosis ka mekhahlelo e latelang ea bakuli ba baholo:

bakuli ba nang le lefu la ischemic (kalafo e qala matsatsi a 7 kamora ho otloa, empa eseng kamora likhoeli tse 6 kamora hore e hlahe),
bakuli ba nang le infraction ea myocardial (kalafo e qala matsatsi a 'maloa kamora ho hlaseloa ke lefu la pelo, empa kamora matsatsi a 35 kamora hore e etsahale),
bakuli ba nang le mafu a methapo ea methapo ea kutlo (vascular atherothrombosis le Tšenyo ea methapo ea methapo e tlase),
bakuli ba nang le infarction ea hlobaetsang ea myocardial le sekhahla sa ST ka nako e le ngoe le ASA (acetylsalicylic acid) (ho bakuli ba fumanang kalafo e tloaelehileng ea lithethefatsi le ba bonts'itsoeng kalafo ea thrombolytic),
bakuli ba nang le asiti ea methapo ea pelo ntle le ho phahamisa karolo ea ST (myocardial infarction ntle le Q wave kapa angina e sa tsitsang) ka nako e tšoanang le acetylsalicylic acid.

Contraindication

ho hloleha ho matla ha sebete
ho ruruha ha masapo a kenang ka mokokotlong, lesapo la peptic le maemo a mang a nang le kotsi ea ho tsoa mali haholo,
khaello ea lactase, ho se mamellane ha galactose, lefu la tsoekere la galactose,
bana le bacha ba ka tlase ho lilemo tse 18,
boimana
sefuba
eketsa kutloisiso ea motho ka mong ho Clopidogrel kapa karolo efe kapa efe ea thuso ea lithethefatsi.

Setsoalle (Aterocardium se sebelisoa ka hlokolosi):

tekano ho isa tekanyong e nyane ea hepatic,
ho hloleha ha rems
hemorrhagic diathesis (nalane),
mehato ea ho buuoa, likotsi le maemo a mang a methapo ea methapo a nang le kotsi ea ho tsoa mali,
Tšebeliso e kopanetsoeng le heparin, ASA, lithethefatsi tse seng khahlanong le ts'oaetso tsa kokoana-hloko le glycoprotein IIb / IIIa inhibitors.

Tekanyetso le tsamaiso

Matlapa a Aterocardium a nooa ka molomo, ho sa tsotelehe lijo tse ngata.

Tekanyetso e khothalletsoang ho batho ba baholo, ho kenyeletsa le bakuli ba tsofetseng, ke Letlapa le le leng hang ka letsatsi.

A a hlobaetsang le coronary syndrome ntle le karolo ea bophahamo ba ST, kalafo e qala ka lethal dose ea 300 mg hang, ebe e tsoela pele ka tekanyetso e tloaelehileng (75 mg) hang ka letsatsi hammoho le acetylsalicylic acid ka lethal dose ea letsatsi le letsatsi ea 75-325 mg. Ho nka tekanyetso e phahameng ea acetylsalicylic acid e eketsa menyetla ea ho tsoa mali, ka hona ha ho khothaletsoe ho nka ho feta 100 mg ea ASA ka letsatsi.

Nako e nepahetseng ea kalafo ha e so theoe, empa liphetho tsa lithuto li bonts'itse hore Aterocardium e lokela ho nkuoa ho isa ho likhoeli tse 12. Phello e phahameng ea kalafo e ile ea bonoa kamora likhoeli tse 3 tsa ho sebelisa moriana.

Ka infraction ea myocardial e hlobaetsang le sekhahla se phahameng sa ST, kalafo e boetse e qala ka lethalinyana le le leng la ho jarolla (300 mg) hammoho le acetylsalicylic acid, kapa lithethefatsi tse se nang thrombolytic kapa ntle le tsona. Bakuli ba kaholimo ho lilemo tse 75 ha ba fuoe lethal dose la ho laolla. Tsamaiso ea ASA e qala kapele haholo mme e nka bonyane libeke tse 4.

Litlamorao

tsamaiso ea tšilo ea lijo: khafetsa - mathata a dyspeptic, bohloko ba ka mpeng, mali a tsoang ka mpeng, lets'ollo, hangata - ho nyekeloa, ho hlatsa, lefu la mokokotlo, liso tsa ka mpeng le mokokotlo, ka seoelo - ho hlaba mali ka makhetlo a mangata, hangata - - stomatitis, colitis (ho ho kenyelletsa lymphocytic kapa ulcerative), pancreatitis, ho khutlisetsa mali le ho ruruha hoa mpa ka phello e bolaeang.
tsamaiso ea hepatobiliary: ka seoelo - hepatitis, ho hloleha ha sebete haholo, liteko tsa ts'ebetso ea sebete,
tsamaiso ea methapo ea pelo: hangata - hematoma, ka seoelo - vasculitis, lefu le matla la mokokotlo, khatello ea methapo ea mali, mali a tsoang leqebeng le sebetsang
hematopoietic system: khafetsa - leukopenia, thrombocytopenia, eosinophilia, ka seoelo - neutropenia (ho kenyeletsa le matla), ka seoelo - anemia, agranulocytosis, granulocytopenia, thrombotic thrombocytopenic purpura, pancytopenia,
Sistimi ea phefumoloho: khafetsa - nosebleeds, ka seoelo - bronchospasm, hemorrhage ea pulmonary, hemoptysis, pneumonitis ea methapo,
tsamaiso ea methapo e bohareng: khafetsa - ho tsekela, ho chesoa ke pelo, ho tsoa mali ka nako e 'ngoe (ka linako tse ling hoa bolaea), ho opeloa ke hlooho, ka seoelo - ho khathatsoa ke tatso, ho bona lipono, pherekano,
litho tsa methapo ea kutlo: khafetsa - mali, maqhutsu kapa ho tsoa mali hape, seoelo - ho tsekela ka lebaka la pathology ea tsebe le labyrinth.
Sistimi ea musculoskeletal: hangata ramatiki - ramatiki, myalgia, hemarthrosis, arthralgia,
Sisteme ea urine: khafetsa - hematuria, ka seoelo - keketseho ea plasma creatinine, glomerulonephritis,
Letlalo le letlalo la mokokotlo: hangata - - hemorrhage e sa sebetseng, hangata - ho hlohlona, lekhopho, hangata, hangata - urticaria, lichen planus, rrythematous rash, eczema, dermatitis e bolaeang, li-angioedema,
karohano e bakoang ke ho kula: ka seoelo - maikutlo a anaphylactic, bokuli ba serum,
matšoao a laboratori: khafetsa - ho lelefatsa nako ea ho tsoa mali,
ba bang: ka seoelo - feberu.

Litaelo tse khethehileng

Haeba ho tsoa mali ho belaelloa, liteko tse nepahetseng le / kapa tlhahlobo e hlakileng ea mali e lokela ho etsoa ka potlako.

Aterocardium e lokela ho hlakoloa matsatsi a 7 pele ho ts'ebetso e buelletsoeng ea ho buoa, kaha moriana o eketsa nako ea ho tsoa mali.

Bakuli ba lokela ho lemosoa hore nakong ea kalafo ka clopidogrel, ho tsoa mali ho ka ba telele le ho emisa kamora nako. Nyeoe e 'ngoe le e' ngoe ea ho tsoa mali ka mokhoa o sa tloaelehang kapa ho hlaseloa ha mali ho sebakeng sa heno ho lokela ho tlaleheloa ngaka ea hau.

Aterocardium ha e ame kapa e na le phello e fokolang lebelo la karabelo ea psychomotor le bokhoni ba ho tsepamisa mohopolo. Haeba ho tsekela ho hlaha ha o ntse o sebelisa moriana, o lokela ho tlohela ho khanna le lintho tse ling tse ka bang kotsi.

Ketso ea pharmacological

Li-inhibitors tsa liplatelete ntle le heparin. Melemo ea pharmacological. Clopidogrel ka boikhethelo e thibela ho tlangoa ha adenosine diphosphate (ADP) ho li-receptor holim'a mokokotlo oa mokokotlo le ts'ebetso e latelang ea mochini oa GPIIb / IIIa tlas'a tšusumetso ea ADP, ka hona, e thibela bongata ba mokelikeli. Clopidogrel e boetse e thibela ho kopana ha liplatelete tse hlahisoang ke agonists tse ling ka ho thibela ho eketseha ha tšebetso ea liplatelete ka ADP e lokolotsoeng le ho fetolela li-receptors tsa ADP habonolo. Liplatelete tse sebelisaneng le liphetoho tsa clopidogrel ho fihlela qetellong ea bophelo ba bona. Ts'ebetso e tloaelehileng ea liplatelete e khutlisoa ka tekanyo e lumellanang le sekhahla sa nchafatso ea liplatelete.
Ho tloha ka letsatsi la pele la ts'ebeliso ea litekanyetso tsa 75 mg tsa moriana, ho fokotseha ho hoholo hoa sekhahla sa kopanyo ea methapo ea methapo ea methapo. Ketso ena e tsoela pele le ho tsitsisa pakeng tsa matsatsi a 3 ho isa ho a supileng. Ha e tsitsitse, boemo ba bohareng ba thibelo ea motsoako tlasa ts'usumetso ea lethal dose ea letsatsi le letsatsi ea 75 mg e tsoa ho 40% ho isa ho 60%. Phatlalatso ea liplatelete le nako ea ho tsoa hoa mali li khutlela mokokotlong ka karolelano matsatsi a 5 kamora ho khaotsa kalafo.
Kamora ho tsamaisoa ha molomo ka tekanyo ea 75 mg, e kenella ka potlako ho tsoa mokokotlong. Karolelano ea tlhase ea plasma e akaretsang ea Clopidogrel e sa fetoheng (hoo e ka bang 2,2-2,5 ng / ml ka mor'a tekanyetso e le 'ngoe ea 75 mg ka molomo) e fihlelletse metsotso e ka bang 45 ka mor'a ho kenella. Ho ba le botenya ke bonyane 50%, joalo ka ha ho bontšitsoe ke lits'oants'o tsa "metaboliti" ea "clopidogrel" ka moroto. Clopidogrel le metabolite ea mantlha (e sa sebetseng) e potang maling e le vitro e khutlela morao ho protheine ea plasma ea motho (98% le 94%, ka ho latellana). Tlamo ena e lula e tletse ka vitro ka holim'a mefuta e mengata e fapaneng.
In vitro le vivo ho na le tse peli
Clopidogrel ke katoloso ea litsela tse kholo tsa metabolism ea eona: e 'ngoe e feta ka ho nka karolo ha litheko mme e lebisa ho hydrolysis ka ho theha motsoako o sa sebetseng oa carboxylic acid (e etsang 85% ea metabolites eohle e potileng ka har'a plasma), le li-enzyme tsa cytochrome P450 system li ameha ho tse ling. Taba ea pele, "Clopidogrel" e fetoha metabolite e bohareng ea 2-oxo-clopidogrel. Ka lebaka la metabolism e eketsehileng ea 2-oxo-clopidogrel, e hlahisoang ke thiol, metabolite e sebetsang, e thehiloe. Ka vitro, tsela ena ea metabolic e kenella pakeng tsa enzymes CYP3A4, CYP2C19, CYP1A2, CYP2B6. Metabolite e sebetsang ea clopidogrel, e neng e arotsoe ka vitro, e tlama ka potlako le ka mokhoa o ke keng oa fetoloa ho li-receptor tsa liplatelete, e sitisang pokello ea liplatelete.
Lihora tse 120 kamora ho kenella, hoo e batlang e le 50% ea lethal dose e nkuoeng e hlobolisoa ka har'a moroto ebe 46% e na le mantle. Kamora ho tsamaisoa ha molomo ka tekanyetso e le 'ngoe, halofo ea bophelo ba clopidogrel e ka ba lihora tse 6. Bophelo ba halofo ea metabolite ea mantlha (e sa sebetseng) e potoloha maling ke lihora tse 8 ka mor'a taolo e le 'ngoe ea meriana.
Li-enzyme tse 'maloa tsa polymorphic CYP450 li fetola clopidogrel hore e be metabolite e sebetsang, e e sebetse. CYP2C19 e ameha ho thehoeng ha metabolite ka bobeli le metabolite e mahareng ea 2-oxo-clopidogrel. Li-pharmacokinetics tsa metabolite e sebetsang le litlamorao tsa antiplatelet, ho latela tekanyo ea kopanyo ea liplatelete, li fapana ho latela mofuta oa CYP2C19. CYP2C19 * 1 allele e tsamaisana le metabolism e sebetsang ka botlalo, ha li-CYP2C19 * 2 le CYP2C19 * 3 li lumellana le metabolism e fokolang. Tsena li ikarabella bakeng sa 85% ea litlatsetso tse fokotsang ts'ebetso ho makhooa le 99% ho Maasia. Likhakanyo tse ling tse amanang le metabolism e fokolisitsoeng li kenyelletsa CYP2C19 * 4, * 5, * 6, * 7 le * 8, empa li fokola haholo ho baahi.

Tekanyetso le tsamaiso

Batho ba baholo le bakuli ba tsofetseng. Kahare, Letlapa le le leng (75 mg) hang ka letsatsi, ho sa tsotelehe lijo tse ngata.

Ho bakuli ba nang le acute coronary syndrome (ACS) ntle le karolo ea ST ST (ho sa tsitsang angina kapa myocardial infarction ntle le Q wave ho ECG), kalafo ea Aterocardium e qala ka lethal dose le le leng la 300 mg, ebe e tsoela pele ka lethal dose ea 75 mg hang ka letsatsi e kopane le acetylsalicylic acid ( ASA) ka tekanyo ea 75-325 mg ka letsatsi. Kaha tšebeliso ea litekanyetso tse phahameng tsa ASA e eketsa menyetla ea ho tsoa mali, ho khothaletsoa hore e se ke ea feta tekanyetso ea acetylsalicylic acid ea 100 mg. Nako e nepahetseng ea kalafo ha e so theoe. Liphetho tsa lithuto li bontša tšebeliso ea moriana ona ho isa ho likhoeli tse 12, 'me phello e phahameng e ile ea bonoa kamora likhoeli tse 3 tsa kalafo.

Bakeng sa bakuli ba nang le infraction ea myocardial e hlobaetsang le sekhahla se phahameng sa ST, Clopidogrel e beoa 75 mg hang ka letsatsi, ho qala ka lethalamo le le leng la 300 mg hammoho le ASA, ka lithethefatsi tsa thrombotic kapa ntle le tsona. Phekolo ea bakuli ba lilemo tse kaholimo ho 75 e qala ntle le lethal dose ea clopidogrel. Phekolo ea ho kopanya e lokela ho qaloa kapele ka mor'a ho qala ha matšoao 'me e lokela ho tsoela pele bonyane libeke tse' ne. Melemo ea ho kopantsoe ha Clopidogrel le ASA bakeng sa libeke tse fetang tse 'nè ha e so ithutoe ka lefu lena.

Pharmacogenetics. Bathong ba nang le metabolism e fokolang ea CYP2C19, karabelo e fokotsehileng ea kalafo ea clopidogrel e ile ea bonoa. Mokhoa o nepahetseng oa litekanyetso ho batho ba nang le metabolism e fokolang ha o e-so thehoe.

Ho hloleha hape Phihlelo ea ho sebelisa lithethefatsi ho bakuli ba nang le bothata ba ho phekoloa ka methapo e lekanyelitsoe. Setlhare se lokela ho sebelisoa ka hloko (sheba karolo "likarolo tsa tšebeliso").

Ho hloleha ha sebete. Phihlelo ea ho sebelisa lithethefatsi ho bakuli ba nang le mafu a sebete le monyetla oa hemorrhagic diathesis li lekanyelitsoe. Setlhare se lokela ho sebelisoa ka hloko (sheba karolo "likarolo tsa tšebeliso").

Matšoao le litekanyetso:

Thibelo ea matšoao a atherothrombotic ho batho ba baholo:

Bakeng sa bakuli ba a hlobaetsang le coronary syndrome

Batho ba nang le lefu la myocardial infarction (ho hlokahala hore ba qale kalafo kamora matsatsi a 'maloa, empa ha ho feta matsatsi a 35 ho tloha ho qala ha lefu la pelo), lefu la ischemic (ho hlokahala ho qala kalafo kamora matsatsi a 7, empa eseng ho feta likhoeli tse 6 kamora lefu la stroke), kapa bakuli ba nang le mafu a tsebahalang a methapo ea methapo ea kutlo (atherosulinosis ea lijana tsa methapo e tlase le ho senyeha ha methapo ea methapo)

Ho bakuli ba se nang karolo e phahameng ea ST ho ECG (myocardial infarction ntle le Q wave kapa angina e sa tsitsang), ho kenyelletsa le ba nang le stent e kentsoeng nakong ea percutaneous coronary angioplasty, e kopantsoeng le acetylsalicylic acid

Ho bakuli ba nang le infarction e mpe ea myocardial, ha karolo ea ST e phahama hammoho le acetylsalicylic acid (ho bakuli ba fumanang kalafo e tloaelehileng ea lithethefatsi le ba hlokang kalafo ea thrombolytic)

Batho ba baholo le bakuli ba tsofetseng ba lokela ho nka letlapa le le leng (75 mg) ka molomo hang ka letsatsi, ho sa tsotelehe lijo tse ngata.

Bakeng sa bakuli ba nang le lefu la sethoathoa se matla sa methapo ea methapo ntle le sekhahla sa ST (myocardial infarction ntle le Q wave kapa angina e sa tsitsang), lethal dose ea 300 mg e beuoe qalong ea kalafo.

Ebe tafole e le 'ngoe (75 mg) e beoa hanngoe ka letsatsi, e kopantsoe le asiti ea acetylsalicylic ka litekanyetso tsa 75-325 mg / ka letsatsi.

Nako e nepahetseng ea kalafo ha e so theoe.

Ho latela liphetho tsa lithuto, phello e phahameng e tlalehiloe kamora likhoeli tse 3 ho tloha ho qala kalafo, mme molemo oa ts'ebeliso ea lithethefatsi e ne e le likhoeli tse 12.

Ho bakuli ba nang le infarction e mpe ea myocardial, eo ho eona sekhechana sa ST se tlalehiloeng ho ECG, moriana o fuoa tekanyetso ea 75 mg hang ka letsatsi.

Hoa hlokahala ho qala ho nka Aterocardium ka lethal dose ea 300 loading hammoho le acetylsalicylic acid.

Phekolo ea bakuli ba lilemo li ka tlase ho 75 e lokela ho etsoa ntle le lethal dose. Phekolo ea ho kopanya ea Aterocardium le acetylsalicylic acid e lokela ho qala hang kamora ho qala matšoao mme e tsoelletse libeke tse 4. Melemo ea ho ja nako e telele ha e e-so fumanoe.

Ho bakuli ba nang le metabolism e liehang ea CYP 2C19, karabelo e fokotsehileng ea kalafo ka Aterocardium e tlalehiloe.

Mokhoa o nepahetseng oa litekanyetso tsa bakuli ba joalo ha o e-so thehoe.

Phihlelo le Aterocardium ho bakuli ba nang le bothata ba ho phekoloa ha a reculing e lekanyelitsoe. Fana ka litlhare ho batho ba joalo ka tlhokomeliso.

Hape, ka tlhokomeliso, Aterocardium e fuoa bakuli ba nang le mafu a sebete le batho ba kotsing e kholo ea ho ba le hemorrhagic diathesis.

Litlamorao:

Ho tsoa ho sistimi ea hematopoietic: leukopenia, thrombocytopenia, eosinophilia, neutropenia (ho kenyeletsa le ho teba), thrombotic thrombocytopenic purpura, parytopenia, anemia (ho kenyeletsa aplasiki), thrombocytopenia, granulocytopenia, agranulocytosis.

Ho tsoa ho tsamaiso ea methapo ea pelo: hematomas, hemorrhages e matla, arterial hypotension, vasculitis, ho tsoa mali ho tsoa maqeba a postoperative.

Ho tsoa ho tsamaiso ea tšilo ea lijo: lets'ollo, dyspepsia, bohloko ba ka mpeng, ho tsoa mali, ho ruruha, ho nyekeloa, seso sa ka mpeng, ho hlatsa, gastritis, lefutso. Ho sa tloaelehang ho tloaelehileng e ka ba colitis (ho kenyelletsa le lymphocytic kapa ulcerative), pancreatitis, stomatitis, ho tsoa mali le ho khutla ha mali ka phello e bolaeang.

Ho tsoa ho sebete: hepatitis, ho hloleha ka matla ha sebete, liteko tse sa sebetseng tsa sebete.

Ho tloha lehlakoreng la ts'ebetso ea methapo e bohareng: paresthesia, ho tsekela, ho opeloa ke hlooho, ho tsoa mali ka sekhahla (ka linako tse ling ho fihlela lefung), lipono, ho ferekana ha maikutlo, pherekano.

Ho tsoa lintlheng tsa kutlo: retinal, ocular, conjunctival madi, ho tsekela ho amanang le lefu la tsebe kapa labyrinth.

Ho tloha letlalong le mokokotlong oa "subcutaneous hemorrhage", hemorrhage, ho hlohlona, letlalo, lekhopho la mokokotlo, erythematous rash, angioedema, bullous dermatitis (Stevens-Johnson syndrome, erythema multiforme, chefo ea epidermal necrolysis), lichen planus, eczema, urticaria.

Ho tsoa ts'ebetsong ea ho hema: nosebleeds, ho hema ka matšoafo (pulmonary hemorrhage, hemoptysis), pneumonitis ea methapo, "bronchospasm".

Ho tsoa ho tsamaiso ea musculoskeletal: ramatiki, hemarthrosis, myalgia, arthralgia.

Ho tsoa ts'ebetsong ea moroto: hematuria, litekanyetso tse eketsehang tsa creatinine maling, glomerulonephritis.

Boitšoaro ba Hypersensitivity: liphetoho tse anaphylactic, bokuli ba serum.

Liphetoho maemong a laboratori: ho fokotseha ha liplatelete le li-neutrophil, keketseho ea nako ea ho tsoa mali.

Litla-morao tse ling: feberu, ho tsoa mali setsing sa ente.

Ho sebelisana le meriana e meng le joala:

Protein Inhibitors IIb / IIIa. Setlhare se lokela ho laeloa ka hloko ho bakuli ba kotsing e kholo ea ho tsoa mali ka lebaka la ts'ebetso ea mokokotlo, khatello ea maikutlo kapa maemo a mang a amanang le ts'oaetso a hlokang ts'ebeliso ea liprotheine tsa IIb / IIIa.

BUANG. ASA ha e ame phello ea inhibitory ea clopidogrel ho ADP-induction platelet aggregation, empa Clopidogrel e ntlafatsa phello ea ASA ho kopaneng ea liplatelese tlas'a ts'ebetso ea collagen.

Tsamaiso e ts'oanang ea 500 mg ea ASA habeli ka letsatsi bakeng sa letsatsi le le leng ha ea ka ea lebisa phetohong ea bohlokoa ea nako ea ho tsoa mali. Tšebeliso e tšoanang ea Aterocardium le ASA e hloka tlhokomeliso, hobane ho na le monyetla oa ho tsoa mali.

Li-anticoagulants tsa molomo. Ka lebaka la kotsi e kholo ea ho tsoa mali, ts'ebeliso e kopaneng ea li-anticoagulants tsa molomo le atherocardia ha e khothalletsoe.

Heparin. Boithuto bo bontša hore ts'ebeliso ea clopidogrel ha e ame phello ea heparin mme ha e hloke tokiso ea litekanyetso tsa nako e tlang. Ho amoheloa ha heparin ha hoa ka ha ama phello ea Clopidogrel. Empa ka lebaka la kotsi e kholo ea ho tsoa mali, ts'ebeliso e tšoanang ea lithethefatsi tsena ha e khothalletsoe.

Manonyeletso a matla. Tšireletseho ea tšebelisano-'moho ea Aterocardium, fibrin-itseng kapa fibrin e khethehileng ea li-thrombolytic le heparin e ithutile ho bakuli ba nang le infarction ea myocardial e mpe. Monyetla oa ho tsoa mali o ne o tšoana le ts'ebeliso e kopaneng ea li-thrombolytic agents le heparin le ASA.

NSAIDs. Tšebeliso e tšoanang ea Aterocardium le naproxen e eketsa kotsi ea ho tsoa mali ka mpeng. Ha ho na data mabapi le tšebelisano ea clopidogrel le litlhare tse ling tse seng khahlanong le ts'oaetso tsa mali.

Ho kopanya le lithethefatsi tse ling. Kaha metabolite ea Clopidogrel e sebetsang e thehiloe tlasa ts'ebetso ea CYP 2C19, ts'ebeliso ea lithethefatsi tse fokotsang ts'ebetso ea enzyme ena e lebisa ho fokotseha ha khatello ea metabolite e sebetsang, ka hona, ho fokotseha ha phello ea kliniki ea Aterocardium. Ka hona, ho hlokahala ho qoba taolo e tšoanang ea Aterocardium le lithethefatsi tse amang ts'ebetso ea CYP 2C19. Lithethefatsi tse joalo li kenyeletsa: esomeprazole, omeprazole, fluoxetine, fluvoxamine, moclobemide, voriconazole, ticlopidine, fluconazole, ciprofloxacin, carbamazepine, cimetidine, chloramphenicol le oxcarbazepine.

Proton inhibitors.

Ho pakoa hore tekanyo ea thibelo ea enzyme ea CYP 2C19 tlasa ts'ebetso ea lithethefatsi ho tsoa ho sehlopha sa proton pump inhibitors ha e tšoane. Lintlha tse teng li bontša monyetla oa tšebelisano lipakeng tsa Aterocardium le lithethefatsi leha e le life sehlopheng sena. Ha ho na bopaki bo kholisang ba hore lithethefatsi tse ling tse fokotsang tlhahiso ea hydrochloric acid (antacid, H2 blockers) li ama phello ea antiplatelet ea Aterocardium.

Ts'ebeliso e kopaneng ea Aterocardium e nang le atenolol le nifedipine ha ea ka ea fetola katleho ea tleliniki ea meriana ena. Ntle le moo, thepa ea clopidogrel ea pharmacodynamic e ile ea lula e sa fetoha ha e ntse e sebelisoa le cimetidine, digoxin, theophylline, estrogen, le phenobarbital.

Li-antacid ha li ame ho ajoa ha clopidogrel.

Boithuto bo bontša hore li-carbonyl tse tsoang ho clopidogrel li ka sitisa mosebetsi oa cytochrome P450 2C9. Ho ka etsahala, sena se ka baka keketseho ea likhathatso tsa plasma tsa NSAIDs, tolbutamide le phenytoin, metabolism ea eona e bang teng ka tšusumetso ea cytochrome P450 2C9. Empa liphetho tsa lipatlisiso li bonts'a hore tolbutamide le phenytoin li ka nkuoa ka polokeho ka atherocard.

Ha ho na ts'ebelisano e kholo ea bongaka e fumanoeng pakeng tsa Aterocardium le beta-adrenergic blockers, diuretics, calcium block blockers, ACE inhibitors, antacids, antidiabetesic, antiepileptic, antiepileptic, anti-cholesterol-lowering drug, and anticycythology activist.

Sebopeho le thepa:

Letlapa le le leng le na le:

Clopidogrel 75 mg

Likarolo tse thusang: cellcosestalline cellulose, magnesium stearate, lactose monohydrate, setlolo sa pregelatinized, polyethylene glycol 6000, povidone K 25, oxide e khubelu ea tšepe (E 172)

Motsoako o ka sehloohong oa ts'ebetso, Clopidogrel, ka mokhoa o khethang ho tlama ha ADP ho li-receptor holim'a liplatelete le ts'ebetso e latelang ea GPIIb / IIIa li thehiloe tlasa ts'usumetso ea ADP, e hlahisang thibelo ea pokello ea liplatelete.

Thibelo ea ho kopana ha liplatelete e hlahisoang ke agonists tse ling le eona e etsahala ka ho thibela ho eketseha ha mosebetsi oa liplatelete ka ADP le li-receptors tse sa fetoheng ka mokhoa o ke keng oa fetoloa.

Liplatelete tse neng li sebelisana le clopidogrel li fetola phetoho ho fihlela qetellong ea bophelo ba tsona.

Ts'ebetso ea polasetiki e khutlela boemong bo tloaelehileng kamora nako e hlokahalang bakeng sa nchafatso ea tlhaho ea lisele tsena tsa mali.

Ho tloha matsatsing a pele a tšebeliso ea makhetlo a 75 mg ea lithethefatsi, khatello ea bohlokoa ea ADP e kentsoeng liplatelete e tlalehiloe.

Phello ena e ntlafatsoa hanyane ka hanyane, e tsitsisa nako e pakeng tsa matsatsi a 3 le a 7 a kalafo.

Tekanyo e tloaelehileng ea thibelo ea ho kopanyetsoa tlasa ts'ebetso ea litekanyetso tsa 75 mg ho boemo bo tsitsitseng ke 40-60%.

Nako ea ho tsoa mali le sekhahla sa ho kopana ha liplatelete se khutlela molemong oa matsatsi a 5 kamora ho qeta kalafo.

Kamora ho tsamaisoa ha moriana oa moriana ka tekanyetso ea 75 mg, ho kenngoa ka potlako mokokotlong oa lijo ho etsahala. Litekanyetso tse phahameng tsa plasma tse akaretsang tsa Clopidogrel e sa fetoheng (ka bongata ba 2,2-2,5 ng / ml ka mora ts'ebetso e le 'ngoe ea molomo ea 75 mg ea lithethefatsi) li fihletsoe metsotso e 45 kamora ho nka Aterocardium.

Excretion ea clopidogrel ka moroto e bontša hore monko oa ntho e sebetsang ke bonyane 50%.

Litekong tsa vitro, Clopidogrel le metabolite ea eona e sa sebetseng hantleng ka plasma ea mali e khutlela hape liprotheine, khokahano ena e boloka boholo ba eona bo tebileng ka ho teba.

Metabolism ea tlhaho ea Clopidogrel e etsoa ka har'a sebete. Ho vivo le vitro ho na le mekhoa e 'meli ea metabolism.

Ea pele e feta ka ho nka karolo ha litheko, ho lebisang ho hydrolysis ha ho etsoa motsoako oa carboxylic acid o tsoang (karolo ena e etsa 85% ea metabolites eohle maling).

Tsela ea bobeli ea metabolic e etsoa ka ho nka karolo ha cytochrome P450 enzyme system.

Taba ea pele, metabolite e bohareng ea 2-oxo-clopidogrel e thehoa ho tsoa ho Clopidogrel, eo hamorao e fetohang metabolite e sebetsang (thiol derivative). Semelo se sebetsang sa metabolite se arohaneng ho vitro ka potlako le ka mokhoa o sa fetoheng se sebelisana le lisebelisoa tsa mokelikeli tsa liplatelete, tse sitisang pokello ea liplatelete.

Hoo e ka bang 50% ea lethal dose e laetsoeng e tšeloa ka har'a moroto le 46% e nang le mantle ka mor'a lihora tse 120. Bophelo ba halofo ea lethal e le 'ngoe ke lihora tse 6.

Bophelo ba halofo ea metabolite e sa sebetseng ke lihora tse 8 (ka mor'a tekanyetso e le 'ngoe le ka mor'a taolo e pheta-phetoang).

Matlapa a kopaneng 75 mg No. 10, 40.

Ka mocheso o sa feteng 25 degrees Celsius ka har'a sephutheloana sa mantlha.

Melemo ea pharmacological

Clopidogrel ka boikhethelo e thibela ho tlangoa ha adenosine diphosphate (ADP) sebakeng sa polasetiki le ts'ebetsong e latelang ea "GPIIb / IIIa tata" ka ADP, ka hona e sitisa pokello ea liplatelete. Clopidogrel e hatella hape lipokello tsa liplatelete tse hlahisoang ke agonists tse ling ka ho thibela ho eketseha ha tšebetso ea liplatelete ka ADP e lokolotsoeng le ho fetolela li-receptors tsa ADP habonolo. Liplatelete tse sebelisaneng le liphetoho tsa clopidogrel ho fihlela qetellong ea bophelo ba bona. Ts'ebetso e tloaelehileng ea liplatelete e khutlisoa ka tekanyo e tsamaellanang le sekhahla sa nchafatso ea platelet.

Ho tloha matsatsing a pele a tsamaiso ka makhetlo a 75 mg a pharalletseng, ho fokotseha ho hoholo hoa matla a kopantsoeng a ADP. Ketso ena e tsoela pele le ho tsitsisa pakeng tsa matsatsi a 3 ho isa ho a supileng. Ha e tsitsitse, boemo ba bohareng ba thibelo ea motsoako tlasa ts'usumetso ea lethal dose ea letsatsi le letsatsi ea 75 mg e tsoa ho 40% ho isa ho 60%. Phatlalatso ea liplatelete le nako ea ho tsoa mali e khutlela metheong ka kakaretso matsatsi a 5 kamora ho khaotsa kalafo.

Kamora ho tsamaisoa ha molomo ka tekanyo ea 75 mg, e kenella ka potlako ho tsoa mokokotlong.

Palo e kholo ea plasma ea clopidogrel e sa fetoheng (hoo e ka bang 2,2-2,5 ng / ml ka mor'a ho sebelisa tekanyetso e le 'ngoe ea 75 mg ka molomo) e fihlelletsoe metsotso e ka bang 45 ka mor'a kopo. Ho ba le botenya ke bonyane 50%, joalo ka ha ho bontšitsoe ke lits'oants'o tsa "metaboliti" ea "clopidogrel" ka moroto. Clopidogrel le metabolite ea mantlha (e sa sebetseng) e potang maling e le vitro e khutlela morao ho protheine ea plasma ea motho (98% le 94%, ka ho latellana).

Tlamahano ena e lula e tsitsitse ka vitro ka mefuta e mengata e fapaneng.

Clopidogrel e tšelitsoe haholo ka har'a sebete. In vitro le vivo, ho na le mekhoa e 'meli ea mantlha ea metabolism ea eona: e le' ngoe e etsahala ka ho nka karolo ha litheko mme e lebisa ho hydrolysis ka ho theha motsoako o sa sebetseng oa carboxylic acid (e etsang 85% ea metabolites eohle e potileng ka plasma ea mali), le li-enzyme tsa cytochrome P450 system li ameha ho tse ling. .

Taba ea pele, "Clopidogrel" e fetoha metabolite e bohareng ea 2-oxo-clopidogrel. Ka lebaka la metabolism e eketsehileng ea 2-oxo-clopidogrel, e hlahisoang ke thiol, metabolite e sebetsang, e thehiloe. In vitro, tsela ena ea metabolic e tsamaisoa ke enzymes CYP3A4, CYP2C19, CYP1A2, le CYP2B6. Metabolite e sebetsang ea clopidogrel, e neng e arotsoe ka vitro, e tlama ka potlako le ka mokhoa o ke keng oa fetoloa ho li-receptor tsa liplatelete, ka ho etsa joalo e sitisa pokello ea liplatelete.

Lihora tse 120 kamora ho kenella, hoo e ka bang 50% ea lethal dose e ntšoa ka har'a moroto 'me 46% e na le makhopho. Kamora ho tsamaisoa ha molomo ka tekanyetso e le 'ngoe, nako ea bophelo ba Clopidogrel e ka ba ka 6:00. Bophelo ba halofo ea metabolite ea mantlha (e sa sebetseng) e potoloha maling ke 8:00 kamora tšebeliso ea lithethefatsi e le 'ngoe hape.

Pharmacogenetics. Li-enzyme tse 'maloa tsa polymorphic CYP450 li fetola clopidogrel hore e be metabolite e sebetsang, e e sebetse. CYP2C19 e ameha ho thehoeng ha metabolite ka bobeli le metabolite e mahareng ea 2-oxo-clopidogrel. Li-pharmacokinetics tsa metabolite e sebetsang le litlamorao tsa antiplatelet, ho latela tekanyo ea kopanyo ea liplatelete, li fapana ho latela mofuta oa CYP2C19. CYP2C19 * 1 allele e tsamaisana le metabolism e sebetsang ka botlalo, ha li-CYP2C19 * 2 le CYP2C19 * 3 li lumellana le metabolism e fokolang. Li-alleles tsena li ikarabella bakeng sa 85% ea litlatsetso, li fokolisa tšebetso ho tšoeu le 99% ho Maasia. Likhakanyo tse ling tse amanang le metabolism e fokolisitsoeng li kenyelletsa CYP2C19 * 4, * 5, * 6, * 7 le * 8, empa li fokola haholo ho baahi.

Thibelo ea atherothrombosis ho batho ba baholo

ho bakuli ba nang le lefu la myocardial infarction (ho qala ha kalafo ke matsatsi a 'maloa, empa ha ho sa feta matsatsi a 35 kamora ho qala), lefu la ischemic (qalo ea kalafo ke matsatsi a 7, empa ha ho so fete likhoeli tse 6 kamora ho qala kapa ba fumanoeng ba na le lefu lena methapo ea methapo ea kutlo (Tšenyo ea methapo ea methapo ea methapo le methapo ea methapo ea lijana tse lipheletsong tse tlase),
ho bakuli ba nang le a hlobaetsang le coronary syndrome:

̶ e nang le acute coralary syndrome ntle le ST dikarolo tse phahameng tsa mokokotlo (angina e sa tsitsang kapa myocardial infarction ntle le Q wave), ho kenyelletsa le ho bakuli ba neng ba e-na le stent e kentsoeng nakong ea percutaneous coronary angioplasty, hammoho le acetylsalicylic acid (ASA)

̶ infarction ea hlobaetsang myocardial e nang le keketseho ea karolo ea ST hammoho le acetylsalicylic acid (ho bakuli ba fumanang meriana e tloaelehileng le ba bontsitsoeng kalafo ea thrombolytic).

Thibelo ea liketsahalo tsa atherothrombotic le thromboembolic ho atraya fibrillation. Clopidogrel hammoho le ASA e bonts'oa ho bakuli ba baholo ba nang le fibrillation ea atrial, ba nang le bonyane kotsi e le 'ngoe ea ho hlaha ha liketsahalo tsa vascular, moo ho nang le li-contraindication tsa kalafo ka li-antagonists tsa Vitamin (AVK) le ba nang le kotsi e tlase ea ho tsoa mali, bakeng sa thibelo ea liketsahalo tsa atherothrombotic le thromboembolic. ho kenyelletsa le stroke. Bona le karolo "Melemo ea Pharmacological".

Ho sebelisana le lithethefatsi

Ha ho kgothaletswe ho kopanya kalafo ea Aterocardium le anticoagulants ea molomo ka lebaka la ts'oso ea keketseho ea matla a tsoang mali.

Khokahano e ka khonehang ka tšebeliso e tšoanang ea Clopidogrel e nang le lintho tse ling tsa kalafo / litokisetso:

lithethefatsi tse seng khahlanong le ho ruruha (ho kenyeletsa COX-2 inhibitors), ASA, li-inhibitors tsa protheine IIb / IIIa, lithethefatsi tsa thrombolytic, heparin: ho na le monyetla oa ho tsoa mali (sebelisa clopidogrel ka tlhokomeliso ka motsoako ona),
fluconazole, fluoxetine, omeprazole, moclobemide, esomeprazole, voriconazole, carbamazepine, ticlopidine, chloramphenicol, ciprofloxacin, fluvoxamine, oxcarbazepine, cimetidine (lithethefatsi tse thibelang ts'ebetso ea metabolism ea CYP2C19: metabolism ea eona e fokotseha metabolism.
proton pump inhibitors: karabelo ea tšebelisano e ka khona, ka hona, metsoako ena ha e khothalletsoe ntle le ha e le bohlokoa,
lithethefatsi tse nang le metabolism li sebelisa cytochrome P450 2C9: hoa khonahala ho eketsa boemo ba lithethefatsi tsena ka plasma (ntle le tolbutamide le phenytoin, e bolokehileng ho e sebelisa le Aterocardium),
atenolol, nifedipine, estrogen, cimetidine, phenobarbital, theophylline, antacids, digoxin, diuretics, ACE inhibitors (angiotensin-converting enzyme), beta-blockers, calcium channel blockers, antiepileptic, hypocholesterolemic le lithethefatsi tse ling. ho eketsa likepe tsa coronary, bahanyetsi ba GPIIb / IIIa, lithethefatsi tsa phekolo ea li-hormone: ha ho na ts'ebelisano e kholo ea kliniki e ileng ea hlokomeloa.

Liratso tsa Aterocardium ke: Clopidogrel, Plavix, Aspirin Cardio, Dipyridamole.

Litla-morao

hematoma, ka seoelo

tloaelehileng - ho tšoaroa ke mali haholo, ho tsoa mali ho tsoa leqeba le sebetsang, vasculitis, hypotension ea methapo,

ho tsoa ho tšilo ea lijo: ho tloaeleha - bohloko ba ka mpeng, lets'ollo, ho bola, ho tsoa mali, ho sa tloaeleha - ho nyekeloa, ho ruruha, mpeng le lesapo la mokokotlo, gastritis, ho hlatsa, lefufuru, ka seoelo ho tloaelehile - ho tsoa mali, ho sa tloaelehang haholo - pancreatitis, colitis (ho kenyelletsa ulcerative kapa lymphocytic), ho bola ka mpeng le ho tsoa mali hape ka mokokotlo, stomatitis,

ho tsoa ho hepatobiliary system: ka seoelo - ho hloleha ha sebete haholo, hepatitis, liteko tsa ts'ebetso ea sebete,

ho tsoa ho tsamaiso ea methapo e bohareng: e sa tloaelehang - hlooho ea hlooho, paresthesia, ho tsekela, ho tsoa mali kahare (maemong a mang, ho bolaoa), ho sa tloaelehang haholo - pherekano, hallucinations, tsieleho ea tatso,

ho tsoa lithong tsa kutlo: ha e sa tloaeleha - ho tsoa mali

(conjunctival, ocular, retinal), e sa tloaelehang haholo - ho tsekela (pathology ea tsebe le labyrinth),

letlalong la letlalo le linama tse katamelaneng: tloaelo - hemorrhage e sa sebetseng - e sa tloaelehang - lekhopho la letlalo, ho hlohlona, hangata, ho sa tloaelehang haholo - angioedema, rrythematous rash, oxous dermatitis (lefutso le nang le chefo ea methapo ea methapo, lefu la Stevens-Johnson, erythema multiforme, kraemia), lichen planus

Tsamaisong ea phefumoloho: e tloaelehileng - nosebleeds, e sa tloaelehang haholo - phefumoloho ea ho hema (hemoptysis, pulmonary hemorrhage), bronchospasm, pneumonitis e ka hare ho nako,

ho tsoa ho ts'ebetso ea musculoskeletal: e sa tloaelehang haholo - hemarthrosis, ramatiki, arthralgia, myalgia,

ho tsoa ho ts'ebetso ea urine: e sa tloaelehang - hematuria, e sa tloaelehang haholo - glomerulonephritis, e leng tenginine e maling.

Boitšoaro ba Hypersensitivity bo ile ba bonoa, bo sa tloaeleha haholo - lefu la serum, karabelo ea anaphylactic,

Matšoao a laboratori: a sa tloaelehang - ho lelefatsa nako ea ho tsoa mali, ho fokotseha hoa boemo ba li-neutrophils le liplatelete,

tse ling: tse tloaelehileng - ho tsoa mali setsing sa ente, hangata ho sa tloaelehang - feberu.

Ho sebelisana le lithethefatsi tse ling le mefuta e meng ea litšebelisano

Li-anticoagulants tsa molomo. Tšebeliso e kopanetsoeng le clopidogrel ha e khothalletsoe, kaha ho na le monyetla oa ho eketseha ha mali ho eketsehileng.

Lithibelo tsa glycoprotein IIb, / IIIA. Aterocardium e lokela ho sebelisoa ka hloko ho bakuli ba nang le menyetla ea ho tsoa mali ka lebaka la khatello ea maikutlo, ho buuoa kapa maemo a mang a methapo a sebelisang glycoprotein IIb, IIAa inhibitors.

Acetylsalicylic acid (ASA). ASA ha e fetole phello ea inhibitory ea clopidogrel ho ADP-induction platelet aggregation, empa clopidogrel e ntlafatsa phello ea ASA ho kopaneng ea pollagen e kentsoeng ke collagen. Leha ho le joalo, tšebeliso e tšoanang ea 500 mg ea ASA makhetlo a 2 ka letsatsi bakeng sa letsatsi la 1 ha ea ka ea baka keketseho e kholo ea nako ea ho tsoa mali, e atolositsoeng ka lebaka la ts'ebeliso ea clopidogrel. Kaha tšebelisano lipakeng tsa clopidogrel le acetylsalicylic acid e ka etsahala ka kotsi e eketsehang ea ho tsoa mali, ts'ebeliso e tšoanang ea meriana ena e hloka tlhokomeliso. Leha ho le joalo, clopidogrel le ASA li sebelisitsoe hammoho ho fihlela selemo se le seng.

Heparin. Ho latela liphuputso, Clopidogrel e ne e sa hloke phetoho ea tekanyetso bakeng sa heparin ebile ha ea ka ea fetola phello ea heparin ho coagulation. Tšebeliso e tšoanang ea heparin ha ea ka ea fetola phello ea inhibitory ea clopidogrel ho kopaneng ea platelet. Kaha tšebelisano pakeng tsa clopidogrel le heparin e ka etsahala ka kotsi e eketsehileng ea ho tsoa mali, tšebeliso e tšoanang ka nako e le ngoe e hloka tlhokomeliso.

Manonyeletso a matla. Tšireletseho ea tšebeliso ea nako e le 'ngoe ea li-clopidogrel, fibrin-maalum kapa fibrin e khethehileng ea li-thrombolytic le heparin li fumanoe lipatlisiso ho bakuli ba nang le infarction e mpe ea myocardial. Khafetsa ho tsoa mali ka mokhoa o ikhethang ho ne ho tšoana le ha ho sebelisoa ka nako e le 'ngoe lithethefatsi tsa thrombolytic le heparin ka ASA.

Lithethefatsi tse seng khahlanong le ho ruruha (NSAIDs). Tšebeliso e tšoanang ea Clopidogrel le naproxen li ka eketsa palo ea ho tsoa mali ka mpeng. Leha ho le joalo, leha ho se na datha mabapi le tšebelisano ea lithethefatsi le li-NSAID tse ling, ha e e-so hlake kapa kotsi ea ho tsoa mali ha e sebelisoa le NSAIDs tsohle. Ka hona, ho hlokahala tlhokomeliso ha u sebelisa li-NSAIDs, haholo COX-2 inhibitors, e nang le clopidogrel.

Ho kopanya le meriana e meng.

Kaha clopidogrel e fetotsoe ho metabolite ea eona e sebetsang ka karolo e itseng ea CYP2C19, ts'ebeliso ea lithethefatsi tse fokotsang ts'ebetso ea enzyme ena e ka lebisa ho fokotseha ha khatello ea metabolite e sebetsang ea Clopidogrel ka plasma ea mali, hammoho le ho fokotseha ha ts'ebetso ea bongaka. Tšebeliso e tšoanang ea lithethefatsi tse sitisang ts'ebetso ea CYP2C19 e lokela ho qojoa.

Lithethefatsi tse thibelang ts'ebetso ea CYP2C19 li kenyelletsa omeprazole, esomeprazole, fluvoxamine, fluoxetine, moclobemide, voriconazole, fluconazole, ticlopidine, ciprofloxacin, cimetidine, carbamazepine, oxcarbazepine le chloramphenicol.

Proton inhibitors. Leha bopaki bo supa hore tekanyo ea thibelo ea ts'ebetso ea CYP2C19 tlasa ts'ebetso ea lithethefatsi tse fapaneng tsa sehlopha sa proton pump inhibitors ha e tšoane, ho na le bopaki bo bontšang monyetla oa ho sebelisana le lithethefatsi tsohle tsa sehlopha sena. Ka hona, tšebeliso e tšoanang ea li-inhibitors tsa proton pump e lokela ho qojoa, ntle le haeba ho hlile ho hlokahala. Ha ho na bopaki ba hore lithethefatsi tse ling tse fokotsang tlhahiso ea acid ka mpeng, joalo ka mohlala, li-blockers tsa H 2 (ntle le cimetidine, e leng CYP2C9 inhibitor kapa li-antacid, li ama mosebetsi oa antiplatelet oa clopidogrel.

Ka lebaka la lithuto, ha ho ts'ebelisano e kholo ea kliniki e ileng ea senoloa ka ts'ebeliso ea clopidogrel ka nako e le ngoe le atenolol, nifedipine, kapa ka lithethefatsi ka bobeli. Ntle le moo, ts'ebetso ea pharmacodynamic ea clopidogrel e lula e sa fetohe ha e ntse e sebelisoa le phenobarbital le estrogen.

Mekhoa ea li-pharmacokinetic ea digoxin kapa theophylline ha ea ka ea fetoha ha ts'ebeliso ea clopidogrel. Li-antacid ha li ame ho ajoa ha clopidogrel.

Lintlha tsa lipatlisiso li fana ka maikutlo a hore li-carboxyl metabolites tsa Clopidogrel li ka thibela ts'ebetso ea cytochrome P450 2C9. Sena se ka eketsa maemo a plasma a phenytoin, tolbutamide le NSAID, a entsoeng ka cytochrome P450 2C9. Leha ho le joalo, liphetho tsa lithuto li bontša hore phenytoin le tolbutamide li ka sebelisoa ka mokhoa o sireletsehileng ka nako e le ngoe le clopidogrel.

Ho ne ho se na ts'ebelisano e kholo ea lithethefatsi ka li-diuretics, beta-blockers, li-inhibitors tsa ACE, li-blockers tsa calcium calcium, li-agents tse fetolang likepe tsa coronary, antacids, hypoglycemic (ho kenyeletsa insulin), hypocholesterolemic, antiepileptic drug, GPIIb / IIIa antagonists, and antagonists of GPIIb / III.

Likarolo tsa ts'ebeliso

Ho tsoa mali le mathata a hematological. Ka lebaka la kotsi ea ho tsoa mali le litlamorao tsa hematological, tlhahlobo e felletseng ea mali le / kapa liteko tse ling tse nepahetseng li lokela ho etsoa hang hang haeba matšoao a ho tsoa mali a shejoa nakong ea ts'ebeliso ea lithethefatsi (bona.

Tabeng ea ts'ebetso e reriloeng ea ts'ebetso ea bongaka e hlokang ho sebelisoa, ka nakoana e hloka ts'ebeliso ea li-antiplatelet agents, kalafo e nang le clopidogrel e lokela ho khaotsa matsatsi a 7 pele ho buuoa. Bakuli ba lokela ho tsebisa ngaka (ho kenyeletsa le ngaka ea meno) hore ba sebelisa Clopidogrel, pele ho etsoa opereishene leha e le efe, kapa pele o sebelisa moriana o mocha. Clopidogrel e eketsa nako ea ho tsoa mali, ka hona e lokela ho sebelisoa ka tlhokomeliso ho bakuli ba nang le kotsi e eketsehileng ea ho tsoa mali (haholo-holo gastrointestinal le intraocular).

Bakuli ba lokela ho lemosoa hore nakong ea kalafo ka clopidogrel (a le mong kapa e kopane le ASA), ho tsoa mali ho ka emisa kamora nako e tloaelehileng, le hore ba lokela ho tsebisa ngaka ka nyeoe e 'ngoe le e' ngoe ea ho tsoa mali ka mokhoa o sa tloaelehang (sebakeng kapa nako).

Thrombotic thrombocytopenic purpura (TTP). Litaba tsa thrombotic thrombocytopenic purpura (TTP) ha li sa ka tsa bonoa haholo ka mor'a taolo ea clopidogrel, ka linako tse ling esita le ka mor'a tšebeliso ea eona ea nakoana. TTP e bonts'oa ke "anemia" ea "thrombocytopenia" le "hemangi" (hemangi). TTP ke boemo bo ka bang kotsi bo ka bolaeang, ka hona e hloka kalafo ea kapele, ho kenyeletsoa plasmapheresis.

Haemophilia e fumanehang Tlaleho ea nts'etsopele ea hemophilia e fumanoeng kamora ts'ebeliso ea Clopidogrel e tlalehiloe. Maemong a keketseho e ikhethileng ea APTT (nako e sebelisitsoeng ea karolo ea thromboplastin), e tsamaeang le kapa e sa tsamaisane le ho tsoa mali, potso ea ho fumana hemophilia e fumanoeng e lokela ho nahanoa. Bakuli ba nang le ts'oaetso e netefalitsoeng ea hemophilia e fumanoeng ba tlameha ho ba tlasa tlhokomelo ea ngaka mme ba fumane kalafo, ts'ebeliso ea clopidogrel e lokela ho emisoa.

Haufinyane tjena o ile a tšoaroa ke lefu la ischemic. Ka lebaka la data e sa lekaneng, ha ho kgothaletswe ho fana ka Clopidogrel matsatsing a 7 a pele ka mor'a ho otloa habohloko ke ischemic.

Cytochrome P450 2 C19 (CYP2C19). Pharmacogenetics Ho bakuli ba sebetsang ka liphatsa tsa lefutso ba CYP2C19, ho na le mokokotlo o tlase oa metabolite e sebetsang ea clopidogrel plasma ea mali le phello e seng e boletsoeng ea antiplatelet. Hona joale ho na le liteko tsa ho khetholla mofuta oa CYP2C19 ho mokuli.

Kaha clopidogrel e fetoha sebopeho sa eona se sebetsang sa metabolite ka tlase ho tšusumetso ea CYP2C19, ts'ebeliso ea lithethefatsi tse fokotsang ts'ebetso ea enzyme ena e kanna ea lebisa ho fokotseha ha khatello ea metabolite ea Clopidogrel e sebetsang ka plasma ea mali. Leha ho le joalo, bohlokoa ba bongaka ba tšebelisano ena ha bo hlakisoe. Ka hona, mohato ke ho kenyelletsa ts'ebeliso ea nako e le 'ngoe ea li-inhibitors tse matla le tse itekanetseng tsa CYP2C19 (bona

Phapang e khutlelang pakeng tsa thienopyridine. Nalane ea mokuli ea hypersensitivity ho thienopyridine tse ling (joalo ka ticlopidine, prasugrel) e lokela ho hlahlojoa hobane ho bile le litlaleho tsa tšebelisano lipakeng tsa thienopyridine (bona karolo ea "Karabelo e mpe"). Ts'ebeliso ea thienopyridine e ka lebisa ho tsitsipano ea maikutlo a bobebe ho tebileng ho tebileng, joalo ka ho ba le tšohanyetso, edema ea Quincke, kapa maikutlo a hematological a joalo ka thrombocytopenia le neutropenia. Bakuli ba kileng ba ba le nalane ea liphetoho tsa mmele le / kapa ho fetoha hoa hematopiki ho thienopyridine e ngoe ba ka ba le kotsi e eketsehileng ea ho ba le karabelo e tšoanang kapa e fapaneng le thienopyridine e ngoe. Ho khothaletsoa ho lekola tšebeliso ea mesebetsi e amanang le maemo

Ts'ebetso ea mokokotlo e sa sebetseng. Phihlelo ea kalafo ea ho sebelisa Clopidogrel ho bakuli ba nang le bothata ba ho phekoloa ka methapo e lekanyelitsoe, ka hona, bakuli ba joalo ba lokela ho fuoa meriana ka hloko (bona Karolo "Karolo le Tsamaiso").

Ts'ebetso ea sebete e sa sebetseng. Phihlelo ea ho sebelisa lithethefatsi ho bakuli ba nang le mafu a itekanetseng a sebete le monyetla oa hemorrhagic diathesis e lekanyelitsoe, ka hona, bakuli ba joalo ba lokela ho fuoa Clopidogrel ka tlhokomeliso (bona Karolo "Karolo le Tsamaiso").

Bahlomphehi. Aterocardium e na le lactose. Bakuli ba nang le mafu a lefutso a fumanehang ka mokhoa o sa tloaelehang a kang galactose ts'oarello, khaello ea Lappase ea lactase kapa malabsorption ea glucose-galactose e sa sebetseng ha baa lokela ho sebelisa lithethefatsi tsena.

Sebelisa nakong ea bokhachane kapa ka ho lactation

Ka lebaka la khaello ea tlhaiso-leseling ea kalafo ka tšebeliso ea Clopidogrel nakong ea kemolo, moriana ha oa lokela ho fuoa basali baimana (joalo ka boits'ireletso). Liteko tsa liphoofolo ha li hlahise phello e mpe ea Clopidogrel ho ima, bokhachane / nts'etsopele, ho tsoala le ho holisa pelehi.

Ha ho tsejoe hore na Clopidogrel e kotsiloe lebeseng la matsoele. Liphuputso tsa liphoofolo li bontšitse hore e pepesitsoe lebeseng la matsoele, ka hona, matsoele a tlameha ho emisoa nakong ea kalafo le moriana.

Melemo. Nakong ea lithuto tsa liphoofolo tsa mahaeng, ha ho litlamorao tse bohloko tsa Clopidogrel mabapi le tsoalo tse ileng tsa fumanoa.

Bongata

Matšoao: Nako e telele ea ho tsoa mali e nang le mathata a latelang.

Phekolo ke matšoao. Haeba ho hlokahala, khalemelo e potlakileng ea nako e telele ea ho tsoa mali, phello ea lithethefatsi e ka tlosoa ka ho tšeloa mali. Motsoako oa meriana ea Clopidogrel ha o tsejoe.

Boikutlo bo fapaneng

Karolong ea sistimi ea mali le tsamaiso ea methapo ea kutlo: thrombocytopenia, leukopenia, eosinophilia, neutropenia, ho kenyelletsa le ho teba ha neutropenia, thrombotic thrombocytopenica granulocytopenia, anemia.

Ka lehlakoreng la tsamaiso ea 'mele ea ho itšireletsa mafung: lefu la serum, karabelo ea anaphylactoid, sefapano sa hypersensitivity lipakeng tsa thienopyridine (joalo ka ticlopidine, prasugrel) (bona

Ho tloha lehlakoreng la ts'ebetso ea methapo: ho tsoa mali ka intracranial (maemong a mang - ho bolaoa), hlooho ea hlooho, paresthesia, kizunguoe, phetoho ea tatso ea tatso.

Ho tloha lehlakoreng la setho sa pono: ho tsoa mali sebakeng sa leihlo (conjunctiva, sebono, retinal).

Karolong ea litho tsa kutlo le tse leka-lekaneng: ho tsekela.

Ho tsoa ho tsamaiso ea methapo ea pelo: hematoma, hemorrhage e matla, ho tsoa mali ho tsoa leqebeng le ka mor'a opereishene, vasculitis, hypotension ea methapo.

Ho tsoa mokokotlong oa mokokotlo: ho tsoa mali ka mpeng, lets'ollo, bohloko ba ka mpeng, dyspepsia ea seso sa ka mpeng le mokokotlo oa duodenal, gastritis, ho hlatsa, ho nyekeloa, ho nyekeloa, ho ruruha ha methapo ea methapo, ho hema ka mpeng, ho ruruha ha litho tsa ka mpeng, lefu le bolaeang ka mpeng, lefu le bolaeang ka mpeng. (ka ho khetheha, ulcerative kapa lymphocytic), stomatitis.

Ho tsoa ho tsamaiso ea tšilo ea lijo: ho se sebetse hantle ha sebete, hepatitis, litholoana tse sa tloaelehang tsa matšoao a tšebetso ea sebete.

Karolong ea letlalo le lisele tse poteletseng: ho ruruha ha methapo ea methapo, ho ruruha, pruritus, intradermal hemorrhage (purpura), lefu le thibelang methapo ea methapo (letheba le nang le chefo), lefu la Stevens-Johnson, erythema multiforme). ka lipono tsa eosinophilia le systemic (DRESS syndrome), eczema, lichen planus.

Karolong ea sistimi ea mesifa ea masapo, mesifa e amanang le masapo: masculoskeletal hemorrhage (hemarthrosis), ramatiki, arthralgia, myalgia.

Ho tsoa liphio le tsamaiso ea moroto: hematuria glomerulonephritis, e leng tlhahiso ea "syntinine" maling.

Mathata a kelello: ho bona lipono, pherekano.

Mathata a amanang le ho hema, thoracic le mediastinal: nosebleeds, nosetso ea ho hema (hemoptysis, hemorrhage ea pulmonary), bronchospasm, pneumonitis ea methapo, "pneumonitis" ea methapo.

Mathata a tloaelehileng: feberu.

Lithuto tsa laboratori: Nako e telele ea ho tsoa mali, ho fokotseha hoa palo ea li-neutrophils le liplatelete.