Clopidogrel - litaelo tsa tšebeliso ea matlapa, matšoao, mokhoa oa ts'ebetso, litla-morao le theko

Tlhaloso e amanang le 28.01.2015

• Lebitso la Latin: Clop>

Letlapa la Clopidogrel ea lithethefatsi le kenyelletsa 75 mg ea ntho e le 'ngoe e sebetsang ka sebopeho sa hydrosulfate.

Lintho tse ling: prosalv, lactose monohydrate, colloidal silicon dioksiase, croscarmellose sodium, sodium fumarate.

Sebopeho sa Shell: pinki opadray II (hypromellose, lactose monohydrate, titanium dioxide, carmine, dae yellow iron oxide, macrogol), emicion ea silicone.

Fomu ea tokollo

Letlapa le koahetsoeng ka pinki le biconvex le sebopeho, le bosoeu bo bosehla karolong eo.

• Matlapa a 14 ka pakete e le 'ngoe, tse 2 kapa tse peli ka paketeng.
• Matlapa a 7 kapa a 10 ka pakete e le 'ngoe, tse 2, 3 kapa tse 4 ka paketeng ea pampiri.
• Ho na le matlapa a 7 kapa a 10 ka blister, 1, 2, 3 kapa 4 blacks ka har'a pakete ea pampiri.
• Matlapa a 14 kapa 28 ka botlolong ea polymer, botlolo e le 'ngoe ka har'a pakete ea pampiri.
• Ho na le matlapa a 14 kapa 28 a polanteng, a le mong ka pakete ea pampiri.

Pharmacodynamics le pharmacokinetics

Moriana ona o hatella ho kopanya liplatelete ka bongata 'me ka mokhoa o ikhethileng o fokotsa ho tlama ha adenosine diphosphate (ADP) ho li-receptor tsa liplatelete, hape o fokotsa bokhoni ba ho kenya tšebetsong li-receptor tsa glycoprotein tlasa ketso ea adenosine diphosphate. Setlhare sena se fokotsa khokahano ea liplatelete, tse bakoang ke bahanyetsi leha e le bafe, tse thibelang ts'ebetso ea bona ka ADP e lokollotsoeng. Limolek'hule tsa lithethefatsi li kopana le li-receptor tsa li-platter tsa ADP, kamora moo liplatelete li lahlehang ka ho sa feleng tsa ho hlasimoloha ha ADP.

Matla a ho thibela ho kopanya ha liplatelete ho etsahala lihora tse peli ka mor'a tekanyetso ea pele. Tekanyo ea khatello ea khatello e eketseha ka nako ea matsatsi a 4-7 hape e fihla sehlohlolong qetellong ena. Tabeng ena, ho kenella ka letsatsi letsatsi le leng le le leng e lokela ho ba 50-100 mg ka letsatsi. Haeba tšenyo ea methapo ea pelo e fumaneha, joale ho sebelisa moriana ho thibela tsoelo-pele ea lefu lena.

Kamora ho sebelisa moriana ona ka nako e khuts'oane o kenella ka mpeng ea gastrointestinal. Tekanyo ea bioavailability ea lithethefatsi ke 50%; tšebeliso ea lijo ha e ame boemo bona. Motsoako oa lithethefatsi o hlaha ka har'a sebete. Ka plasma ea mali, boleng bo phahameng bo fihlella hora e le ngoe ka mor'a ho sebelisa moriana. Ho felisoa ha halofo ea bophelo ke lihora tse robeli, li hlahisoa ke liphio le mala.

Litaelo tse khethehileng

Tšebeliso ea moriana o amahanngoa le tlhoko ea ho lekola boemo ba mokuli kamehla. Matšoao a latelang a fumaneha:

1. Ho bakuli bao lilemo tsa bona li fetang lilemo tse 75, molao oa tekanyetso ea pele e lokelang ho felisoa o lokela ho felisoa.
2. Ts'ebetsong ea kalafo, o hloka ho latela matšoao a tsamaiso ea heestatic, ho sekaseka boemo bo sebetsang ba sebete.
3. Sebelisa ka hloko ho bakuli ba nang le kotsi e eketsehileng ea ho lahleheloa ke mali ka lebaka la ho lemala kapa mabaka a mang.
4. Boteng ba maloetse a amanang le tahlehelo ea mali, ho lokela ho hopoloa hore moriana o eketsa nako ea ho tsoa mali.
5. Ha u khanna makoloi, hlokomela hore Clopidogrel e ka baka likotsi.

Nakong ea kemolo

Ho fihla joale, ha ho na lithuto tse felletseng le tlhahlobo mabapi le phello ea Clopidogrel ho ima le nts'etsopele ea lesea e sa nts'etsopele. Ka lebaka lena, sethethefatsi ha se laeloe nakong ea kemolo. Ha ho na bopaki ba khatello ea hore na moriana o fetela lebeseng la letsoele, ka hona ho nka Clopidogrel ha ho khothaletsoe nakong ea matsoele.

Matšoao a ho sebelisoa

Thibelo ea liketsahalo tsa atherothrombotic ho bakuli kamora lefu la myocardial (ho tloha matsatsing a 'maloa ho isa ho matsatsi a 35), lefu la ischemic (ho tloha matsatsing a 7 ho isa ho likhoeli tse 6) kapa ba nang le lefu le fumanehang la lefu la methapo ea methapo.

Thibelo ea liketsahalo tsa atherothrombotic (hammoho le acetylsalicylic acid) ho bakuli ba nang le lefu la methapo ea mahlo:

- ntle le ho phahamisa karolo ea ST (e sa tsitsang angina pectoris kapa infarction ea myocardial ntle le leqhubu la Q), ho kenyelletsa bakuli ba ntseng ba tsitlella ho kenella ha maikutlo,

- ka ho phahama ha sekhahla sa ST (infutate ea myocardial e mpe) ka kalafo ea lithethefatsi le monyetla oa thrombolysis.

Contraindication

- ho tsoa mali haholo (ka mohlala, ho tsoa mali ho tsoa ho peptic ulcer kapa hemorrhage ea intracranial),

- lefutso le futsanehileng la lactose le fumanehang ka seoelo, khaello ea lactase le malabsorption ea glucose-galactose,

- bana le bacha ba ka tlase ho lilemo tse 18 (polokeho le katleho ha e so theoe),

- Hypersensitivity ho clopidogrel kapa leha e le efe ea ipabolang ka lithethefatsi.

- ho hloleha ho lekaneng ha sebete, moo ho ka bang le monyetla oa ho tsoa mali (boiphihlelo bo fokolang ba tleliniki)

- ho se sebetse hantle haholo (boiphihlelo bo fokolang ba tleliniki)

- mafu ao ho nang le 'ona a tlang pele ho nts'etsopele ea mali (haholo-holo gastrointestinal kapa intraocular),

- Tsamaiso e ts'oanang ea lithethefatsi tse seng khahlanong le ts'oaetso tsa steroidal, ho kenyeletsa li-inhibitors tse khethiloeng tsa COX-2,

- tšebeliso e tšoanang ea warfarin, heparin, glycoprotein IIb / IIIa inhibitors

Mokhoa oa ho sebelisa: litekanyetso le kalafo

Batho ba baholo le bakuli ba tsofetseng ba nang le ts'ebetso e tloaelehileng ea CYP2C19 isoenzyme

Clopidogrel-SZ e lokela ho nkuoa ka molomo, ho sa tsotelehe lijo tse ngata.

Myocardial infarction, ischemic stroke, le lefu la pherekano ea methapo ea kutlo

Moriana o nooa ho 75 mg 1 nako / letsatsi.

Ho bakuli ba nang le myocardial infarction (MI), kalafo e ka qala ho tloha matsatsing a pele ho isa ho la 35 la MI, le ho bakuli ba nang le lefu la ischemic stroke (II), ho tloha matsatsing a 7 ho isa ho likhoeli tse 6 ka mor'a MI.

Acute coronary syndrome ntle le karolo ea SEHOLO (Angina e sa tsitsang, infarction ea myocardial ntle le leqhubu la Q)

Phekolo ka Clopidogrel-SZ e lokela ho qala ka tekanyetso e le 'ngoe ea lethal dose ea 300 loading, mme e ntano tsoela pele ka tekanyetso ea 75 mg 1 nako / letsatsi (hammoho le acetylsalicylic acid e le moemeli oa antiplatelet ka tekanyetso ea 75-325 mg / letsatsi). Kaha tšebeliso ea acetylsalicylic acid ho litekanyetso tse phahameng e amahanngoa le kotsi e eketsehileng ea ho tsoa mali, lethal dose le khothalletsoang la acetylsalicylic acid polelong ena ha lea lokela ho feta 100 mg. Phello e phahameng ea kalafo e bonoa ke khoeli ea boraro ea kalafo. Nako ea kalafo e ho fihlela selemo se le seng.

Acute coronary syndrome e nang le ST sehemu e phahamisa (infrection ea acute myocardial infarction le ST karolo e phahameng)

Clopidogrel e laetsoe ka tekanyo ea 75 mg 1 nako / letsatsi ka tekanyo e le 'ngoe ea pele ea lethal dose e kopantsoeng le acetylsalicylic acid e le moemeli oa antiplatelet le thrombolytics (kapa ntle le thrombolytics). Phekolo ea ho kopanya e qaloa kapele ka mor'a ho qala ha matšoao mme e tsoela pele bonyane libeke tse 4. Bakeng sa bakuli ba lilemo tse fetang 75, kalafo le Clopidogrel-SZ e lokela ho qala ntle le ho nka tekanyo ea ho jarolla.

Bakuli ba nang le ts'ebetso ea CYP2C19 ea liphatsa tsa lefutso ba sebetse hantle

Ho fokola ha metabolism ka ho sebelisa CYP2C19 isoenzyme ho ka lebisa ho fokotseha hoa phello ea antiplatelet ea clopidogrel. Mokhoa o nepahetseng oa litekanyetso tsa bakuli ba nang le metabolism e fokolang o sebelisa CYP2C19 isoenzyme ha o e-so thehoe.

Ketso ea pharmacological

Moemeli oa antiplatelet. Clopidogrel ke setlhare, e 'ngoe ea li-metabolites tse sebetsang tseo e thibelang ho kopana le liplatelete. Clopidogrel metabolite e sebetsang e thibela ho kopanya ha adenosine diphosphate (ADP) ho P2Y12 platelet receptor le tšebetso ea morao-rao ea ADP e kopantseng moferefere oa lintho tse ngata. Ka lebaka la tlamo e ke keng ea fetoloa, liplatelete li lula li se na tšusumetso ea ADP bophelo bohle ba bona (hoo e ka bang matsatsi a 7- 7), 'me ho khutlisetsoa ha ts'ebetso e tloaelehileng ea liplatelete ho etsahala ka lebelo le lekanang le sekhahla sa ntlafatso ea platelet. Phatlalatso ea liplatelete e bakoang ke li-agonists ntle le ADP le eona e thibetsoe ke thibelo ea ts'ebetso ea liplatelete e atisitsoeng ke ADP e lokollotsoeng. Hobane sebopeho sa metabolite e sebetsang se etsahala ka P450 isoenzymes, e meng e ka fapana ka polymorphism kapa e ka thibeloa ke lithethefatsi tse ling; ha se bakuli bohle ba ka bang le khatello ea methapo ea methapo e lekaneng.

Litlamorao

Ho tloha tsamaisong ea methapo e bohareng le e poteletseng: hangata - ho opeloa ke hlooho, ho tsekela le paresthesia, ka seoelo - vertigo, ka seoelo - tlolo ea maikutlo a monate.

Karolong ea methapo ea pelo le methapo: hangata haholo - vasculitis, e tšoaeang ho fokotseha ha khatello ea mali, intracranial hemorrhage, ocular hemorrhage (conjunctival, ka tiske le retina), hematoma, nosebleeds, madi a tsoang mokhoeng oa ho hema, ho tsoa mali, ho tsoa mali. sephetho, hemorrhages ka mesifa le manonyeletso, hematuria.

Ho tsoa ts'ebetsong ea ho hema: ka seoelo - bronchospasm, pneumonitis ea methapo.

Ho tsoa ho ts'ebetso ea tšilo ea lijo: hangata - - lets'ollo, bohloko ba ka mpeng, dyspepsia, hangata - seso sa ka mpeng le seso sa duodenal, gastritis, ho hlatsa, ho nyekeloa, ho ruruha, ho ruruha, hangata - pancreatitis, colitis (ho kenyeletsa ulcerative kapa lymphocytic colitis), stomatitis, ho hloleha ka matla ha sebete, hepatitis.

Ho tsoa ts'ebetsong ea moroto: ka seoelo - glomerulonephritis.

Ho tsoa tsamaisong ea mali ea mali: khafetsa - ho lelefatsa nako ea ho tsoa mali.

Ho tsoa ho sistimi ea hemopoietic: khafetsa - thrombocytopenia, leukopenia, neutropenia le eosinophilia, ka seoelo - thrombocytopenic thrombohemolytic purpura, thrombocytopenia e kholo (palo ea liplatele ka tlase ho kapa e lekanang le 30 × 109 / l), agranulocytosis, granulocytopenia.

Karolong ea letlalo le lisele tse potolohileng: khafetsa - lekhopho la letlalo le ho hlohlona, ​​hangata - - angioedema, urticaria, erythematous rash (e amanang le clopidogrel kapa acetylsalicylic acid), hangata haholo - oxous dermatitis (erythema multiforme, Stevens-Johnson syndrome, e nang le chefo le chefo. ), eczema le lichen planus.

Ho tsoa ts'ebetsong ea musculoskeletal: ka seoelo - arthralgia, ramatiki, myalgia.

Ka lehlakoreng la tsamaiso ea 'mele ea ho itšireletsa mafung: hangata ka seoelo - ketso ea anaphylactoid, bokuli ba serum.

Tšebelisano

Tsamaiso e tšoanang ka clopidogrel e ka eketsa bongata ba mali, ka hona ts'ebeliso ea motsoako ona ha e khothalletsoe.

Ts'ebeliso ea IIb / IIIa receptor blockers hammoho le clopidogrel e hloka tlhokomeliso ho bakuli ba nang le kotsi e eketsehileng ea ho tsoa mali (ka likotsi le ho kenella ha ho buuoa kapa maemo a mang a pathological).

Acetylsalicylic acid ha e fetole phello ea Clopidogrel, e thibelang ho kopantsoe ha methapo ea methapo ea methapo ea methapo ea methapo, empa clopidogrel e hlahisa phello ea acetylsalicylic acid ho li-pllagen tse kenyellelitsoeng ka liplatelete. Leha ho le joalo, ts'ebeliso e tšoanang ea acetylsalicylic acid e nang le clopidogrel e le moemeli oa antipyretic oa 500 mg makhetlo a 2 / letsatsi bakeng sa letsatsi la 1 ha ea ka ea baka keketseho e kholo ea nako ea ho tsoa mali e bakiloeng ke tsamaiso ea clopidogrel. Pakeng tsa clopidogrel le acetylsalicylic acid, ts'ebelisano ea pharmacodynamic e ka etsahala, e lebisang kotsing e kholo ea ho tsoa mali. Ka hona, ka ts'ebeliso ea bona e ts'oanang, ho lokela ho sebelisoe tlhokomeliso, leha ho le joalo lithutong tsa kliniki, bakuli ba fumane kalafo e kopaneng le clopidogrel le acetylsalicylic acid ho fihlela selemo.

Ho latela lipatlisiso tsa bongaka tse entsoeng le baithaopi ba phetseng hantle, ha ba nka clopidogrel, ho ne ho se na lebaka la ho fetola tekanyetso ea heparin mme phello ea eona ea anticoagulant ha ea fetoha. Tšebeliso e tšoanang ea heparin ha ea ka ea fetola phello ea antiplatelet ea clopidogrel. Pakeng tsa clopidogrel le heparin, ts'ebelisano ea pharmacodynamic e ka etsahala, e ka eketsang kotsi ea ho tsoa mali, ka hona ts'ebeliso e tšoanang ea meriana ena e hloka tlhokomeliso.

Litaelo tsa ho sebelisoa

Clopidogrel e sebelisoa ho bakuli ba baholo nako e le 'ngoe ka letsatsi (pele ho lijo tsa motšeare, kamora lijo tsa motšeare), ho sa tsotelehe lijo. Letlapa leo ha lea lokela ho hlafuna. Noa metsi a mangata (bonyane 70 ml). Motsoako o khothalelitsoeng oa moriana ke 75 mg ka letsatsi (tafole e le 'ngoe).

Mokhoa oa kopo ea maloetse a pelo a hlobaetsang: batho ba baholo lefapheng la lefu la pelo le laoloang ke bongaka hang hang ba fuoa 300 mg ea clopidogrel. Kamora moo, kalafo e ntse e tsoela pele ka tekanyetso ea tlhokomelo ea 75 mg, hangata e kopantsoe le asiti ea acetylsalicylic ho litekanyetso ho tloha ho040 ho isa ho 0,325 g.

Bohlokoa! Ho qoba ho tsoa mali, u se ke ua nka 100 mg ea acetylsalicylic acid.

Nako ea ho amoheloa ha e tsejoe hantle. Ho nka moriana ho tsoelapele ho fihlela boemo ba mokuli bo khutlela ho bo tloaelehileng ka khetho ea ngaka e eang.

Nako ea kalafo nakong ea methati e matla ea ho hlaseloa ke pelo: litekanyetso tsa Clopidogrel ke 75 mg ka letsatsi, ho kenyelletsa le lethal dose la pele la 300 mg hammoho le meriana ea acetylsalicylic acid le thrombolytic.

Bohlokoa! Ho bohlokoa ho bakuli kamora lilemo tse 75 ho khetholla ts'ebeliso ea ho tlatsa litekanyetso tsa moriana.

Nako ea regimen bonyane khoeli e le 'ngoe.

Maemong a sieo, ho lokela ho etsoa:

1. Haeba ho setse lihora tse fetang 12 pele u nka pilisi e latelang, noha pilisi hanghang.
2. Haeba pele u sebelisa tekanyetso e latelang ea Clopidogrel e ka tlase ho lihora tse 12 - nka moriana o latelang ka nako e nepahetseng (u se ke oa eketsa tekanyetso).

Ho thibetsoe ho ikemela le ka tšohanyetso ho emisa ts'ebeliso ea Clopidogrel, kaha boemo ba mokuli bo ka mpefala, ho khutla ha lefu le ka tlase ho ka hlaha.

Bongata

Tšebeliso e mpe ea litekanyetso tse phahameng tsa Clopidogrel e ka tsamaisana le litlamorao tse joalo:

• ho tsoa mali
• ho eketsa nako ea ho tsoa mali.

Phekolo ea overdose ke letšoao. E atlehang haholoanyane ke ho tšeloa ha lithethefatsi ho latela boima ba platelet.

Ka joala

Tabeng ea ho sebelisana le joala, menyetla ea ho teneha ka mpeng le mala e ea eketseha, ka lebaka leo ho tsoa madi ho ka ba teng. Ka hona, ho kopantsoe ha Clopidogrel le joala ha hoa lokela ho qheleloa ka thoko ka lebaka la ho tsamaisana ho tlase haholo.

Likhamphani tsa meriana li hlahisa mofuta o joalo oa Clopidogrel:

• Agrel,
• Gridoklein,
• Atherocard,
• Avix,
• Clopidogrel ea baetsi ba fapaneng - Izvarino, Tatkhimpharmpreparaty, Canon Pharma, Severnaya Zvezda (SZ), Biocom (analogues oa Russia oa Clopidogrel), Teva, Gideon Richter, Ratiopharm, Zentiva,
• Atrogrel
• Cardogrel
• Diloxol
• Sylt,
• Areplex,
• Deplatt
• Noclot,
• Clopact,
• Clorelo
• Clopix
• Clopidal
• Lodigrel,
• Orogrel
• Thabeleng,
• Placep
• Lopirel
• Plavix,
• Reodar,
• Trombix,
• Plaglir,
• Trombeks,
• Ploglil
• Pingel
• Reomax
• Trombone,
• Clopidex
• Plavigrel
• Flamogrel.

Lithethefatsi tsena kaofela ha li na phapang ea sebopeho le litekanyetso tsa ntho e sebetsang. Phapang e ho baetsi le litšenyehelo feela.

Mofumahali

Ho fufuleloa Kamora ho tsamaisoa ka molomo le ho pheta-pheta ka tekanyetso ea 75 mg ka letsatsi, clopidogrel e kenella ka potlako. Karolelano ea boholo ba plasma ea k'homphieutha ea mantlha (hoo e ka bang 2,2-2,5 ng / ml ka mor'a ho sebelisa tekanyetso e le 'ngoe ea molomo ea 75 mg) e ile ea bonoa kamora metsotso e ka bang 45 ka mor'a taolo.Ho ipapisitsoe le li-metabolites tsa "clopidogrel" tse hlahisitsoeng ka har'a moroto, ho imeloa bonyane 50%.

Tsamaiso. Clopidogrel le "metabolite" e ka sehloohong e potolohang e khutlela morao ho liprotheine tsa plasma kavitro (98 le 94%, ka ho latellana). Tlamo ena e lula e sa koaheloa. kavitro ka mefuta e mengata e fapaneng.

Metabolism. Clopidogrel e kenngoa ka potlako maling. Hovitro le kavivo clopidogrel e tšelisoa ka mekhoa e 'meli e meholo: e le ngoe e hokahanngoe le litheko mme e lebisa ho hydrolysis ho kenyelletso e sa sebetseng ea carboxylic acid (85% ea metabolites e potileng maling), e' ngoe (15%) e pakeng tsa li-cytochromes tse ngata tsa P450. Taba ea pele, clopidogrel e tšeloa metabolite ea methapo e bohareng ea 2-oxo-clopidogrel. Ho latela metabolism ea morao-rao ea metabolite e bohareng ea 2-oxo-clopidogrel ho lebisa ho thehoeng ha metabolite e sebetsang, thiol e tsoang ho clopidogrel. Hovitro tsela ena ea metabolic e kenelletsoe ke CYP3A4, CYP2C19, CYP1A2 le CYP2B6. Acth thiol metabolite e ikhethileng kavitro ka potlako le ka mokhoa o sa fetoheng, e kopana le li-receptor tsa liplatelete, ka ho etsa joalo li thibela ho kopana ha liplatelete.

Le_max metabolite e sebetsang e phahame habeli ka mor'a tekanyetso e le 'ngoe ea lethal dose ea 300 mg ea Clopidogrel ho feta kamora matsatsi a mane ea lethal dose ea 75 mg. Le_max e bonoe nakong ea metsotso e 30-60 kamora ho sebelisa moriana.

Ho felisoa. Hoo e ka bang 50% ea moriana o hloekisoa ka har'a moroto 'me o batla o le 46% ka mantle nakong ea lihora tse 120 ka mor'a taolo. Kamora tekanyetso e le 'ngoe ea molomo ea 75 mg, ho felisoa ha halofo ea bophelo ba clopidogrel ke lihora tse 6. Bophelo ba halofo ea metabolite ea potoloho e ka sehloohong ke lihora tse 8 ka mor'a taolo e le 'ngoe le e pheta-phetoang.

Pharmacogenetics. CYP2C19 e ameha ho thehoeng ha metabolite e sebetsang le metabolite e bohareng, 2-oxo-clopidogrel. Pharmacokinetics le antiplatelet litlamorao tsa metabolite e sebetsang ea Clopidogrel joalo ka ha e lekantsoe ho tlhahlobo ea pokello ea lipokelletso exvivo, 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 sa sebetse. CYP2C19 * 2 le CYP2C19 * 3 akhaonto bakeng sa boholo ba linyeoe tse nang le tšebetso e fokotsehileng ho letlalo le tšoeu (85%) le Maasia (99%) ka metabolism e sa lekanang. Linyeoe tse ling tse nang le mosebetsi o lahlehileng kapa o fokotsehileng li kenyelletsa, har'a tse ling, CYP2C19 * 4, * 5, * 6, * 7 le * 8. Bakuli ba nang le metabolism e fokotsehileng ke bakuli ba likarolo tse peli tse sa sebetseng. Ho ea ka tlhaiso-leseling e phatlalalitsoeng, khafetsa ho hlaha ha genotype ka ts'ebetso e fokolang ea metabolism ea CYP2C19 e batla e le 2% peisong ea Caucasoid, 4% peisong ea Negroid le 14% peisong ea Mongoloid.

Boholo ba lithuto tse entsoeng ha boa lekana ho bona phapang liphellong tsa bakuli ba nang le metabolism e sa lekaneng ea clopidogrel.

Ts'ebetso ea mokokotlo e sa sebetseng. Khokahano ea metabolite ea mantlha e potolohang plasma ea mali ha e nka 75 mg ea clopidogrel ka letsatsi e ne e le tlase ho bakuli ba nang le lefu le matla la liphio (clearinine clearance ho tloha ho 5 ho isa ho 15 ml / min) ha e bapisoa le bakuli bao tumello ea bona ea creatinine e leng 30-60 ml / min le batho ba phetseng hantle. Ka nako e ts'oanang, phello ea inhibitory ho motsoako oa methapo ea methapo ea methapo ea methapo ho bakuli ba nang le lefu le matla la liphio e ile ea fokotsoa (25%) ha e bapisoa le phello e ts'oanang ho batho ba phetseng hantle, nako ea ho tsoa mali e ile ea eketsoa ka mokhoa o ts'oanang le ho batho ba phetseng hantle ba amohetseng 75 mg clopidogrel ka letsatsi. Ho feta moo, mamello ea tleliniki e ne e le molemo ho bakuli bohle.

Ts'ebetso ea sebete e sa sebetseng. Bakeng sa bakuli ba nang le bothata bo matla ba ho ba le bothata ba ho ba le takatso e matla ea hepatic, ha ba nka tekanyetso ea letsatsi le letsatsi ea 75 ml ea Clopidogrel ka matsatsi a 10, khothaletso ea ADP ea khothalletso ea liplatelese e ne e tšoana le ea batho ba phetseng hantle. Keketseho e kholo ea nako ea ho tsoa mali e ne e le joalo le ka lihlopha tsena tse peli.

Peiso. Bokapele ba linyeoe tsa CYP2C19, bo bakang metabolism e mahareng le e mpe e kenyang CYP2C19, e fapana ka morabe kapa morabe. Ke lintlha tse lekanyelitsoeng ho palo ea baahi ba Asia tse fumanehang ka har'a lingoliloeng ho hlahloba bohlokoa ba bongaka ba mofuta ona oa CYP bakeng sa liphetho tsa bongaka.

Bokhachane le pelehi

Boithuto mabapi le litlamorao tsa Clopidogrel mabapi le boimana bo entsoeng liphoofolong ha bo a bonts'a phello e mpe ho ima, nts'etsopele ea "lehe", lesea le pelehi.

Ho anyesa. Ha ho tsejoe hore na Clopidogrel e fetela lebeseng la motho. Lithuto tsa liphoofolo li supile hore moriana o fetela lebese la matsoele. E le ts'ireletso, ho anyesa ho lokela ho emisoa nakong ea kalafo ka clopidogrel.

Kaha lithethefatsi tse ngata li qheletsoe ka lebese la letsoele, hape hape ka lebaka la monyetla oa ho hlahisa litla-morao tse mpe lipelong tsa masea tse anyesitsoeng, qeto ea ho khaotsa lithethefatsi kapa ho emisa ho anyesa e lokela ho etsoa, ​​ka lebaka la tlhoko ea kalafo ea clopidogrel ho mme ea anyesang.

Mosebetsi oa ho ikatisa. Lithutong tsa liphoofolo, Clopidogrel ha ea ka ea ama ts'ebetso ea ho ikatisa.

Tekanyetso le tsamaiso

Clopidogrel e etselitsoe tsamaiso ea molomo hang ka letsatsi, ho sa tsotelloe lijo tse ngata.

Lithapo

Batho ba baholo le batho ba baholo

Tekanyetso e tloaelehileng ea letsatsi le letsatsi ke 75 mg ka molomo hang ka letsatsi.

Acute coronary syndrome:

- acute coronary syndrome ntle le karolo ea bophahamoST(e sa tsitsang angina kapa myocardial infarction ntle le leinoQ.): Phekolo ea Clopidogrel e lokela ho qala ka tekanyo e le 'ngoe ea ho jarisa 300 mg, ebe e tsoela pele ka tekanyetso ea 75 mg hang ka letsatsi (le acetylsalicylic acid ka lethal dose ea 75-325 mg ka letsatsi). Ha ho kgothaletswe ho feta tekanyo ea acetylsalicylic acid ea 100 mg, hobane litekanyetso tse phahameng tsa ASA li amahanngoa le kotsi e eketsehileng ea ho tsoa mali. Nako e nepahetseng ea kalafo ha e e-so theoe ka molao. Lintlha tsa teko ea bongaka li netefatsa tšebeliso ea regimen bakeng sa likhoeli tse 12, mme phaello e phahameng e bonoa kamora likhoeli tse 3.

- infarction e mpe ea myocardial ka ho phahamisa likaroloST: clopidogrel e laetsoe hanngoe ka letsatsi ka tekanyo ea 75 mg e sebelisa tekanyetso ea pele ea ho kenya 300 mg hammoho le acetylsalicylic acid ha e kopantsoe kapa e se na thrombolytics e ngoe. Bakeng sa bakuli ba lilemo tse ka tlase ho 75, kalafo ea clopidogrel e lokela ho etsoa ntle le tšebeliso ea lethal dose. Phekolo ea ho kopanya e qaloa kapele ka mor'a ho qala ha matšoao mme e tsoela pele bonyane libeke tse 'ne. Melemo ea ho kopantsoe ha Clopidogrel le ASA kamora libeke tse 'ne ha e sa ithutoa ho sena.

Fibrillation ea methapo: 75 mg clopidogrel hang ka letsatsi. Abela ASA (75-100 mg / ka letsatsi) mme o tsoelepele ho nka hammoho le Clopidogrel.

Boemong ba ho tlola tekanyetso:

- nako e ka tlase ho lihora tse 12 kamora nako e tloaelehileng ea ho amoheloa: hoa hlokahala ho nka tekanyetso hang-hang, tekanyetso e latelang e lokela ho nkuoa ka nako e behiloeng,

- Lihora tse fetang 12 kamora nako e tloaelehileng ea ho amoheloa: tekanyetso e latelang e lokela ho nkuoa ka nako e behiloeng, ntle le ho e pheta habeli.

Bana le bacha

Ts'ireletseho le katleho ea Clopidogrel hara bana ba bana ha e so thehiloe.

Bakuli ba nang le ts'oaetso ea renal

Phihlelo ea ho phekola bakuli ba nang le ts'ebetso ea renal e fokolisitsoeng e nyane.

Bakuli ba nang le ts'ebetso ea sebete e sa sebetseng

Phihlelo ea ho phekola bakuli ba nang le mafu a itekanetseng a sebete moo ho ka khonehang hemorrhagic diathesis e nyane.

Litlhokahalo tsa polokeho

Ho tsoa mali le litla-morao tsa hematologic

Haeba matšoao a kliniki a hlaha nakong ea kalafo e bontšang nts'etsopele ea mali le litla-morao tsa hematological, tlhahlobo ea mali e lokela ho etsoa hanghang. Ka lebaka la kotsi e eketsehileng ea ho tsoa mali, tlhokomeliso e lokela ho sebelisoa ha ho sebelisana 'moho oa Clopidogrel le warfarin.

Clopidogrel e lokela ho sebelisoa ka hloko ho bakuli ba kotsing e kholo ea ho tsoa mali e amanang le ho sithabela maikutlo, ho buuoa kapa maemo a mang a methapo, hammoho le maemong a kopaneng a Clopidogrel le acetylsalicylic acid, lithethefatsi tse seng khahlanong le ts'oaetso tsa steroidal, ho kenyeletsa li-inhibitors tsa COX-2, heparin, glycoprotein inhibitors IIb / IIIa, serotonin reuptake inhibitors (SSRIs) kapa lithethefatsi tse ling tse amanang le kotsi ea ho tsoa mali. joalo ka pentoxifylline. Ho hlahlojoa ka hloko pontšo ea matšoao a ho tsoa mali, ho kenyelletsa le ho tsoa mali morao, hoa hlokahala, haholo-holo nakong ea libeke tsa pele tsa kalafo le / kapa kamora lits'ebetso tse amanang le pelo le ts'ebetso ea pelo. Ts'ebeliso e kopaneng ea clopidogrel e nang le li-anticoagulants tsa molomo ha e khothalletsoe, hobane motsoako o joalo o ka eketsa matla a tsoang mali.

Tabeng ea ts'ebetso ea ts'ebetso ea ts'ebetso ea ts'ebetso, haeba phello ea antiplatelet e sa lakatsehe, tsela ea kalafo e nang le clopidogrel e lokela ho khaotsa matsatsi a 7 pele ho buuoa. Hoa hlokahala ho tsebisa ngaka e kenang le ngaka ea meno ka ho nka moriana haeba mokuli a tlil'o etsoa opereishene kapa haeba ngaka e fa mokuli meriana e ncha.

Clopidogrel e lokela ho sebelisoa ka hloko ho bakuli ba kotsing ea ho tsoa mali (haholo-holo mala) le intraocular. Ha u nka Clopidogrel, sebelisa tlhokomeliso ha u sebelisa lithethefatsi tse ka bakang mafu a pampitšana ea gastrointestinal (mohlala, acetylsalicylic acid le NSAIDs).

U lokela ho tseba hore kaha ho emisa ho tsoa mali ha o ntse o nka clopidogrel (a le mong kapa a kopane le ASA) ho hloka nako e eketsehileng, o lokela ho tsebisa ngaka ea hau ka nyeoe e 'ngoe le e' ngoe ea ho tsoa mali ho sa tloaelehang (ho latela sebaka le / kapa nako).

Thrombotic Thrombocytopenic Purpura (TTP)

Maemo a sa tloaelehang haholo a thrombotic thrombocytopenic purpura (TTP) kamora ho ba ho tlalehiloe ha Clopidogrel ho tlalehiloe. Sena se ne se tšoaetsoa ke anemia ea hemogtophilia le microangiopathic hemolytic hammoho le matšoao a methapo, ts'ebetso ea renal e sa sebetseng hantle kapa feberu. Nts'etsopele ea TTP e ka beha bophelo kotsing mme e ka hloka ts'ebetso e potlakileng, ho kenyelletsa plasmapheresis.

Litaba tsa ho ntlafatsoa ha hemophilia e fumanoeng li tlalehiloe kamora ho nka Clopidogrel. Tabeng ea keketseho e netefalitsoeng ea nako e arotsoeng e sa sebetseng ea nako ea thromboplastin ka kapa ho sena madi, menyetla ea ho ba le hemophilia e fumanoeng e lokela ho nahanoa. Bakuli ba nang le ts'oaetso e netefalitsoeng ea hemophilia e fumanoeng ba lokela ho hlahlojoa le ho phekoloa ke litsebi, kalafo ea Clopidogrel e lokela ho khaotsa.

Ka lebaka la data e sa lekaneng, Clopidogrel ha ea lokela ho khethoa nakong ea matsatsi a 7 a pele ka mor'a ho otloa ke sethoathoa haholo.

Ho bakuli ba nang le metabolism e fokotsang ea CYP2C19, clopidogrel ka tekanyetso e khothalletsoang e fana ka palo e nyane ea metabolite ea Clopidogrel ebile e na le phello e tlase ea antiplatelet. Bakuli ba nang le metabolism e fokotsehileng ea methapo ea kutlo le ba nang le ts'oaetso ea methapo ea methapo ea kutlo le ba fumanang kalafo ea Clopidogrel ka tekanyetso e ka ba kotsing e kholo ea ho ba le mathata a pelo ho feta bakuli ba nang le ts'ebetso e tloaelehileng ea CYP2C19.

Kaha clopidogrel e tšelisoa metabolite e sebetsang ka karolo ea eona ke CYP2C19, ho lebelletsoe hore meriana e hatellang ts'ebetso ea enzyme ena e tla lebisa ho fokotseha ha maikutlo a lithethefatsi tsa metabolite e sebetsang ea Clopidogrel. Bohlokoa ba ts'ebelisano ena ha bo so ithutoe. Ts'ebeliso e tšoanang ea li-inhibitors tsa CYP2C19 tse matla kapa tse leka-lekaneng li lokela ho lahloa.

Ho hlokahala tlhokomeliso ho bakuli ba fumanang ka mokhoa o tšoanang le lithethefatsi tsa clopidogrel - karoloana ea CYP2C8 isoenzyme.

Ho ts'oaroa ke lintho tse ling

Mokuli o lokela ho ba le nalane ea hypersensitivity ho li-thienopyridine tse ling (jk. Ticlopidine, prasugrel), kaha ho na le linyeoe tsa ho ts'oaroa ha allergic le thienopyridines. Bakuli ba nang le nalane ea hypersensitivity ho thienopyridine tse ling ba lokela ho bonoa ka hloko nakong ea kalafo bakeng sa matšoao a hypersensitivity ho clopidogrel. Li-Thienopyridine li ka lebisa ho hola hoa mefuta e fapaneng ea ho satalla ha lintho tse sa utloahaleng, tse kang ho ba le tšohanyetso, edema ea Quincke, kapa maikutlo a amanang le lefutso, a kang thrombocytopenia le neutropenia. Bakuli ba kileng ba ba le nalane ea methapo le / kapa ho fetoha hoa hematopiki ho thienopyridine e ngoe ba ka ba le kotsi e kholo ea ho ba le karabelo e ts'oanang kapa e fapaneng le thienopyridine e ngoe.

Sebopeho sa moriana sena se kenyelletsa dae karmuazin (E-122), e ka bakang mathata.

Ts'ebetso ea mokokotlo e sa sebetseng

Phihlelo ea kalafo e nang le "clopidogrel" ho bakuli ba nang le ts'ebetso ea renal e fokola. Setlhare se lokela ho sebelisoa ho bakuli ba joalo ka tlhokomeliso.

Ts'ebetso ea sebete e sa sebetseng

Clopidogrel e lokela ho sebelisoa ka hloko ho bakuli ba nang le ts'ebetso ea sebete e fokolang, e ka bakang hemorrhagic diathesis.

Tšusumetso ho bokhoni ba ho khanna makoloi le mekhoa e meng e ka bang kotsi. Clopidogrel ha e ame kapa e na le phello e nyane ho bokhoni ba ho khanna makoloi le mekhoa e meng.