Peringatan Keamanan

A single dose of clopidogrel at 1500-2000mg/kg was lethal to mice and rats while 3000mg/kg was lethal to baboons.L7213 Symptoms of overdose include vomiting, breathing difficulty, gastrointestinal hemorrhage, and prostration.L7213 Clopidogrel is irreversibly bound to platelets for their lifetime, which is approximately 11 days.L7213 Overdoses of clopidogrel can be treated with platelet transfusions to restore clotting ability.L7213

Clopidogrel

DB00758

small molecule approved

Deskripsi

Clopidogrel is a prodrug of a platelet inhibitor used to reduce the risk of myocardial infarction and stroke.A180508,L7213 Clopidogrel is indicated to reduce the risk of myocardial infarction for patients with non-ST elevated acute coronary syndrome (ACS), patients with ST-elevated myocardial infarction, and in recent MI, stroke, or established peripheral arterial disease,L7213

It has been shown to be superior to aspirin in reducing cardiovascular outcomes in patients with cardiovascular disease and provides additional benefit to patients with acute coronary syndromes already taking aspirin.A180547

Clopidogrel was granted FDA approval on 17 November 1997.L7213

Struktur Molekul 2D

Berat 321.822
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) That half life of clopidogrel is approximately 6 hours following a 75mg oral dose while the half life of the active metabolite is approximately 30 minutes.[L7213]
Volume Distribusi The apparent volume of distribution of clopidogrel is 39,240±33,520L.[A180538]
Klirens (Clearance) The clearance of a 75mg oral dose was 18,960±15,890L/h and for a 300mg oral dose was 16,980±10,410L/h.[A180538]

Absorpsi

A 75mg oral dose of clopidogrel is 50% absorbed from the intestine.L7213 Clopidogrel can be taken with or without food.L7213 A meal decreases the AUC of the active metabolite by 57%.L7213 The active metabolite of clopidogrel reaches a maximum concentration after 30-60 minutes.L7213 Clopidogrel reached a Cmax of 2.04±2.0ng/mL in 1.40±1.07h.A180538 The AUC for a 300mg oral dose of clopidogrel was 45.1±16.2ng\*h/mL for poor metabolizers, 65.6±19.1ng\*h/mL for intermediate metabolizers, and 104.3±57.3ng\*h/mL for extensive metabolizers.A180541 The Cmax was 31.3±13ng/mL for poor metabolizers, 43.9±14ng/mL for intermediate metabolizers, and 60.8±34.3ng/mL for extensive metabolizers.A180541

Metabolisme

85-90% of an oral dose undergoes first pass metabolism by carboxylesterase 1 in the liver to an inactive carboxylic acid metabolite.A180535 about 2% of clopidogrel is oxidized to 2-oxoclopidogrel.A180535 This conversion is 35.8% by CYP1A2, 19.4% by CYP2B6, and 44.9% by CYP2C19A180535 though other studies suggest CYP3A4, CYP3A5, and CYP2C9 also contribute.A180508 2-oxoclopidogrel is further metabolized to the active metabolite.A180508,A180535 This conversion is 32.9% by CYP2B6, 6.79% by CYP2C9, 20.6% by CYP2C19, and 39.8% by CYP3A4.A180508,A180535

Rute Eliminasi

An oral dose of radiolabelled clopidogrel is excreted 50% in the urine and 46% in the feces over 5 days.L7213 The remainder of clopidogrel is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.A180544

Farmakogenomik

4 Varian
CYP2C9 (rs1057910)

Patients with this genotype have reduced metabolism of clopidogrel resulting in reduced plasma concentrations of its active metabolite.

CYP2C19 (rs4244285)

Patients with this genotype have reduced metabolism of clopidogrel resulting in reduced plasma concentrations of its active metabolite.

CYP2C19 (rs4986893)

The presence of this polymorphism in CYP2C19 is associated with reduced or poor metabolism of clopidogrel.

CYP2C19 (rs4244285)

Patients with this polymorphism in CYP2C19 are poor metabolizers of clopidogrel and are associated with diminished platelet response and increased risk of adverse cardiovascular events in response to clopidogrel therapy.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1203 Data
Apixaban The risk or severity of adverse effects can be increased when Clopidogrel is combined with Apixaban.
Dasatinib Dasatinib may increase the anticoagulant activities of Clopidogrel.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Clopidogrel is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Clopidogrel is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Clopidogrel.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Clopidogrel is combined with Ibritumomab tiuxetan.
Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Clopidogrel.
Obinutuzumab The risk or severity of adverse effects can be increased when Clopidogrel is combined with Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the antiplatelet activities of Clopidogrel.
Rivaroxaban Clopidogrel may increase the anticoagulant activities of Rivaroxaban.
Tipranavir Tipranavir may increase the antiplatelet activities of Clopidogrel.
Urokinase Clopidogrel may increase the anticoagulant activities of Urokinase.
Vitamin E Vitamin E may increase the antiplatelet activities of Clopidogrel.
Deferasirox The serum concentration of Clopidogrel can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Clopidogrel can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Clopidogrel can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Clopidogrel can be decreased when it is combined with Teriflunomide.
Zafirlukast The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Zafirlukast resulting in a loss in efficacy.
Ticlopidine The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Ticlopidine resulting in a loss in efficacy.
Efavirenz The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Efavirenz resulting in a loss in efficacy.
Sertraline The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Sertraline resulting in a loss in efficacy.
Abiraterone The serum concentration of Clopidogrel can be increased when it is combined with Abiraterone.
Armodafinil The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Armodafinil resulting in a loss in efficacy.
Eslicarbazepine acetate The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Eslicarbazepine acetate resulting in a loss in efficacy.
Dabrafenib The serum concentration of Clopidogrel can be decreased when it is combined with Dabrafenib.
Fluvoxamine The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Fluvoxamine resulting in a loss in efficacy.
Chloramphenicol The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Chloramphenicol resulting in a loss in efficacy.
Imipramine The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Imipramine resulting in a loss in efficacy.
Fluoxetine The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Fluoxetine resulting in a loss in efficacy.
Delavirdine The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Delavirdine resulting in a loss in efficacy.
Isoniazid The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Isoniazid resulting in a loss in efficacy.
Miconazole The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Miconazole resulting in a loss in efficacy.
Gemfibrozil The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Gemfibrozil resulting in a loss in efficacy.
Clomipramine The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Clomipramine resulting in a loss in efficacy.
Stiripentol The metabolism of Clopidogrel can be decreased when combined with Stiripentol.
Pantoprazole The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Pantoprazole resulting in a loss in efficacy.
Luliconazole The serum concentration of Clopidogrel can be increased when it is combined with Luliconazole.
Isradipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Isradipine.
Diltiazem The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Diltiazem.
Trimethadione The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Trimethadione.
Amlodipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Amlodipine.
Nimodipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nimodipine.
Nisoldipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nisoldipine.
Lercanidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Lercanidipine.
Cinnarizine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Cinnarizine.
Ethosuximide The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Ethosuximide.
Nicardipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nicardipine.
Magnesium sulfate The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Magnesium sulfate.
Verapamil The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Verapamil.
Loperamide The metabolism of Loperamide can be decreased when combined with Clopidogrel.
Zonisamide The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Zonisamide.
Felodipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Felodipine.
Nitrendipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nitrendipine.
Perhexiline The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Perhexiline.
Nifedipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nifedipine.
Carvedilol The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Carvedilol.
Bepridil The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Bepridil.
Mibefradil The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Mibefradil.
Nimesulide The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nimesulide.
Prenylamine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Prenylamine.
Cyclandelate The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Cyclandelate.
Flunarizine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Flunarizine.
Fluspirilene The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Fluspirilene.
Clevidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Clevidipine.
Methsuximide The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Methsuximide.
Seletracetam The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Seletracetam.
Nylidrin The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nylidrin.
Ziconotide The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Ziconotide.
Dotarizine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Dotarizine.
Xylometazoline The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Xylometazoline.
Nilvadipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nilvadipine.
Tranilast The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Tranilast.
Fasudil The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Fasudil.
Agmatine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Agmatine.
Fendiline The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Fendiline.
Eperisone The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Eperisone.
Trimebutine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Trimebutine.
Pinaverium The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Pinaverium.
Barnidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Barnidipine.
Aranidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Aranidipine.
Azelnidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Azelnidipine.
Benidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Benidipine.
Cilnidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Cilnidipine.
Darodipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Darodipine.
Efonidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Efonidipine.
Lacidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Lacidipine.
Manidipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Manidipine.
Niguldipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Niguldipine.
Niludipine The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Niludipine.

Target Protein

P2Y purinoceptor 12 P2RY12

Referensi & Sumber

Synthesis reference: Revital Lifshitz-Liron, "Novel crystal forms III, IV, V, and novel amorphous form of clopidogrel hydrogensulfate, processes for their preparation, processes for the preparation of form I, compositions containing the new forms and methods of administering the new forms." U.S. Patent US20030114479, issued June 19, 2003.
Artikel (PubMed)
  • PMID: 23116430
    Ganesan S, Williams C, Maslen CL, Cherala G: Clopidogrel variability: role of plasma protein binding alterations. Br J Clin Pharmacol. 2013 Jun;75(6):1468-77. doi: 10.1111/bcp.12017.
  • PMID: 29474768
    Mostafizar M, Haque P, Mazid A, Shohel M, Shazly G, Kazi M, Reza HM: CHARACTERIZATION OF BINDING SITES OF CLOPIDOGREL AND INTERFERENCE OF LINOLEIC ACID AT THE BINDING SITE ON BOVINE SERUM ALBUMIN. Acta Pol Pharm. 2017 Jan;74(1):119-125.
  • PMID: 28335443
    Zhang YJ, Li MP, Tang J, Chen XP: Pharmacokinetic and Pharmacodynamic Responses to Clopidogrel: Evidences and Perspectives. Int J Environ Res Public Health. 2017 Mar 14;14(3). pii: ijerph14030301. doi: 10.3390/ijerph14030301.
  • PMID: 25559342
    Jiang XL, Samant S, Lesko LJ, Schmidt S: Clinical pharmacokinetics and pharmacodynamics of clopidogrel. Clin Pharmacokinet. 2015 Feb;54(2):147-66. doi: 10.1007/s40262-014-0230-6.
  • PMID: 24127209
    Karazniewicz-Lada M, Danielak D, Burchardt P, Kruszyna L, Komosa A, Lesiak M, Glowka F: Clinical pharmacokinetics of clopidogrel and its metabolites in patients with cardiovascular diseases. Clin Pharmacokinet. 2014 Feb;53(2):155-64. doi: 10.1007/s40262-013-0105-2.
  • PMID: 27514617
    Umemura K, Iwaki T: The Pharmacokinetics and Pharmacodynamics of Prasugrel and Clopidogrel in Healthy Japanese Volunteers. Clin Pharmacol Drug Dev. 2016 Nov;5(6):480-487. doi: 10.1002/cpdd.259. Epub 2016 Apr 25.
  • PMID: 20736449
    Frelinger AL 3rd, Barnard MR, Fox ML, Michelson AD: The Platelet Activity After Clopidogrel Termination (PACT) study. Circ Cardiovasc Interv. 2010 Oct;3(5):442-9. doi: 10.1161/CIRCINTERVENTIONS.110.937961. Epub 2010 Aug 24.
  • PMID: 17352522
    Plosker GL, Lyseng-Williamson KA: Clopidogrel: a review of its use in the prevention of thrombosis. Drugs. 2007;67(4):613-46. doi: 10.2165/00003495-200767040-00013.

Contoh Produk & Brand

Produk: 599 • International brands: 0
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Sekuens Gen/Protein (FASTA)

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