Monograph
B01AC04 - Clopidogrel |
Propably not porphyrinogenic |
PNP |
Side effects
Common side effects are diarrhea and abdominal pain.
Rationale
Clopidogrel or its metabolites are not inducers or mechanism-based inhibitors of the quantitatively major CYP isoenzymes in the liver (i.e. CYP 3A4/5, CYP 2C9 and CYP 1A2). Clopidogrel is a mechanism-based inhibitor of CYP 2B6 and a metabolite of clopidogrel is a mechanism-based inhibitor of CYP 2C8.The amount of CYP 2C8 and 2B6 in the liver is relatively low and the de novo synthesis of these enzymes secondary to the mechanism-based inhibition is therefore limited and will not lead to a significant upregulation in the heme biosynthesis via ALAS-1.
Chemical description
Alpha amino acid ester
Therapeutic characteristics
Clopidogrel is a platelet aggregation inhibitor indicated for the prevention of atherothrombotic events (myocardial infarction, stroke and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease.
Clopidogrel has a half-life of 6 hours.
Metabolism and pharmacokinetics
Clopidogrel is a prodrug and the active metabolite is formed primarily by CYP2C19 with contributions from several other CYP enzymes, including CYP1A2, CYP2B6, CYP2C9 and CYP3A4 (Jiang 2015).
Clopidogrel is first metabolised to a 2-oxo-clopidogrel intermediate metabolite. Subsequent metabolism of the 2-oxo-clopidogrel intermediate metabolite results in formation of the active metabolite, a thiol derivative of clopidogrel (SPC).
Clopidogrel is found to be a mechanism-based inhibitor of CYP 2B6 (strong) and of CYP 2C19 (weak) (Richter 2004). The inhibition of CYP 2B6 have shown to cause clinically relevant drug-drug interactions with CYP 2B6 substrates (Turpeinen 2005).
The glucuronide metabolite clopidogrel acyl-β-D-glucuronide is a mechanism-based inhibitor of CYP 2C8 (Tornio 2014).
CYP2C8 accounts for 5% ( Pelkonen 2008) or 7% (Aquilante 2013) of the total CYP content in the liver, while the content of CYP 2B6 is reported to vary from 2% to 10% (Wang 2008) and below 5% (Pelkonen 2008).
IPNet drug reports
Uneventful use reported in 9 patients with acute porphyria.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Tornio A, Filppula AM et al Glucuronidation converts clopidogrel to a strong time-dependent inhibitor of CYP2C8: a phase II metabolite as a perpetrator of drug-drug interactions.
Clin Pharmacol Ther. 2014 Oct;96(4):498-507. |
|
| 2. | Turpeinen M, Tolonen A, Effect of clopidogrel and ticlopidine on cytochrome P450 2B6 activity as measured by bupropion hydroxylation.
Clin Pharmacol Ther. 2005 Jun;77(6):553-9. |
15961986 |
| 3. | PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 8.
Aquilante CL, Niemi M et al. Pharmacogenet Genomics. 2013 Dec;23(12):721-8. |
23962911 |
| 4. | Clinical pharmacokinetics and pharmacodynamics of clopidogrel.
Jiang XL, Samant S et al. Clin Pharmacokinet. 2015 Feb;54(2):147-66. |
|
| 5. | Mechanism-based inhibition of human cytochrome P450 2B6 by ticlopidine, clopidogrel, and the thiolactone metabolite of prasugrel.
Nishiya Y, Hagihara K, et al. Drug Metab Dispos. 2009 Mar;37(3):589-93. |
19047469 |
| 6. | Inhibition and induction of human cytochrome P450 enzymes: current status.
Pelkonen O, Turpeinen M et al. Arch Toxicol. 2008 Oct;82(10):667-715. |
18618097 |
| 7. | Potent mechanism-based inhibition of human CYP2B6 by clopidogrel and ticlopidine.
Richter T, Mürdter TE et al. J Pharmacol Exp Ther. 2004 Jan;308(1):189-97. |
|
| 8. | CYP2B6:
Wang H, Tompkins LM. new insights into a historically overlooked cytochrome P450 isozyme Curr Drug Metab. 2008 Sep;9(7):598-610. |
10665838 |
| * | Summary of Product Characteristics | |
| 9. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Plavix.
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Tradenames
This list comprises raw data collected from different countries.
In some cases, a more comprehensive list of available drug packages is included.
Consequently, very similar terms may therefore appear multiple times.
Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors.
We strive to improve it continuously.
Clopidogrel (als hydrochloride) Sandoz 75 mg, filmomhulde tabletten · Clopidogrel Accord 75 mg filmomhulde tabletten · Clopidogrel Amarox 75 mg, filmomhulde tabletten · Clopidogrel Aurobindo 75 mg, filmomhulde tabletten · Clopidogrel BGR 75 mg filmomhulde tabletten · Clopidogrel CF 75 mg, filmomhulde tabletten · Clopidogrel HCS 75 mg filmomhulde tabletten · Clopidogrel Krka 75 mg filmomhulde tabletten · Clopidogrel Krka d.d. 75 mg filmomhulde tabletten · Clopidogrel ratiopharm 75 mg filmomhulde tabletten · Clopidogrel Reddy 300 mg filmomhulde tabletten · Clopidogrel Reddy 75 mg filmomhulde tabletten · Clopidogrel TAD 75 mg filmomhulde tabletten · Clopidogrel Taw Pharma 75 mg filmomhulde tabletten · Clopidogrel Teva 75 mg filmomhulde tabletten · Clopidogrel Viatris 75 mg filmomhulde tabletten · Clopidogrel Vivanta 75 mg filmomhulde tabletten · Clopidogrel Xiromed 75 mg filmomhulde tabletten · Clopidogrel Zentiva 300 mg, filmomhulde tablet · Clopidogrel Zentiva 75 mg, filmomhulde tablet · Grepid 75 mg filmomhulde tabletten · Iscover 300 mg, filmomhulde tabletten · Iscover, filmomhulde tabletten 75 mg · Plavix 300 mg filmomhulde tabletten · Plavix, filmomhulde tabletten 75 mg · Zyllt 75 mg filmomhulde tabletten 
Clopidogrel (HCl) Sandoz 75 mg compr. pellic. · Clopidogrel AB 75 mg compr. pellic. · Clopidogrel EG 75 mg compr. pellic. · Clopidogrel Krka 75 mg compr. pellic. · Clopidogrel Krka d.d. 75 mg compr. pellic. · Clopidogrel Ratiopharm 75 mg compr. pellic. · Clopidogrel TAD 75 mg compr. pellic. · Clopidogrel Teva 75 mg compr. pellic. pot · Clopidogrel Viatris 75 mg compr. pellic. · Clopidogrel Zentiva 75 mg compr. pellic. · Grepid 75 mg compr. pellic. · Iscover 300 mg compr. pellic. · Iscover 75 mg compr. pellic. · Plavix 300 mg compr. pellic. · Plavix 75 mg compr. pellic. · Zyllt 75 mg compr. pellic. 
AGRELAN 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel · Clopidogrel Ababor 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL ALMUS 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel Apotex 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL ARISTO 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel Aurovitas 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL CINFAMED 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL CODRAMOL 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL DERMOGEN 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL ESSETI 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL FARMALID 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL FARMALIDER 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel hec Pharm 75 Comprimidos Recubiertos con Pelicula efg · Clopidogrel Krka 75 mg Comprimidos Recubiertos con Pelicula efg · Clopidogrel Krka d.d. 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL MABO 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL NORMON 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL PENSA 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel Pharma Combix 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL PLACASOD 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel ratiopharm 75 mg comprimidos recubiertos con pelicula EFG · CLOPIDOGREL SANDOZ 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL STADA 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel Stadafarma 75 mg Comprimidos Recubiertos con Pelicula efg · Clopidogrel sun 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL TAD 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL TARBIS 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel taw Pharma 75 mg Comprimidos Recubiertos con pel?Cula efg · Clopidogrel taw Pharma 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL TECNIGEN 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CLOPIDOGREL TEVA 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · Clopidogrel Teva 75 mg Comprimidos Recubiertos con Pelicula efg · CLOPIDOGREL TEVA PHARMA B.V. 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · CLOPIDOGREL UR 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel Viatris 75 mg Comprimidos Recubiertos con pel?Cula efg · CLOPIDOGREL VIR PHARMA 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Clopidogrel Vivanta 75 mg Comprimidos Recubiertos con pel?Cula efg · CLOPIDOGREL ZENTIVA 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · GREPID 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Iscover 300 mg Comprimidos Recubiertos con Pelicula · Iscover 75 mg Comprimidos Recubiertos con Pelicula · MABOCLOP 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Nastilox 75 mg Comprimidos Recubiertos con Pelicula efg · Plavix 300 mg Comprimidos Recubiertos con Pelicula · PLAVIX 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · VATOUD 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · ZYLAGREN 75 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · Zyllt 75 mg Comprimidos Recubiertos con Pelicula efg 
Averelix · Clopidogrel · Clopinovo · Flodigrel · Nogreg · Plavix · Zyllt 
CLOPIDOGREL ARENA 75 mg · CLOPIDOGREL EIPICO 75 mg · CLOPIDOGREL GEMAX PHARMA 75 mg · CLOPIDOGREL MSN 75 mg · CLOPIDOGREL TERAPIA 75 mg · PLAVIX 75mg · TROMBEX 75 mg · Zyllt 
Clopidogrel · Grepid · Plavix 
Clopidogrel Accord · Clopidogrel Actavis · Clopidogrel Amarox · Clopidogrel Juta · Clopidogrel Krka · Clopidogrel Krka d.d. · Clopidogrel Medical Valley · Clopidogrel Orion · Clopidogrel Pharmathen · Clopidogrel ratiopharm · Clopidogrel Stada · Clopidogrel TAD · Clopidogrel Teva · Clopidogrel Teva Generics B.V. · Clopidogrel Viatris · Clopidogrel Zentiva · Clopimar · Cloriocard · Grepid · Iscover · Maddogrel · Plavix · Vatoud · Zyllt 
Clopidogrel abz · Clopidogrel Accord · Clopidogrel Medical Valley · Clopidogrel Zentiva · Grepid · Plavix 
Agregex · Areplex · Clopidix · Clopidogrel Aurovitas · Clopidogrel BGR · Clopidogrel Bluefish · Clopidogrel Genoptim · Clopidogrel Krka · Clopidogrel Krka d.d. · Clopidogrel Medreg · Clopidogrel MSN · Clopidogrel Ranbaxy · Clopidogrel ratiopharm · Clopidogrel TAD · Clopidogrel Taw Pharma · Clopidogrel Teva · Clopidogrel Viatris · Clopidogrel Zentiva · Grepid · Iscover · Pegorel · Plavix · Plavocorin · Trombex · Vixam · Zyllt 
Clopidogrel · Clopidogrel (hcl) Sandoz · Clopidogrel EG · Clopidogrel ratiopharm · Clopidogrel Taw Pharma 75mg · Clopidogrel Teva-75 · Clopidogrel Viatris · Clopidogrel Zentiva · Grepid-75 · Iscover · Plavix · Zopya · Zylagren · Zyllt 
Clopidogrel Actavis · Clopidogrel Krka · Clopidogrel Krka d.d. · Clopidogrel Medical Valley · Clopidogrel ratiopharm · Clopidogrel TAD · Clopidogrel Teva · Clopidogrel Viatris · Clopidogrel Zentiva · Grepid · Iscover · Plavix · Zyllt 
Clopidogrel Krka · Clopidogrel Krka d.d. · Clopidogrel Orion · Clopidogrel Ratiopharm · Clopidogrel Stada · Clopidogrel TAD · Clopidogrel Teva · Clopidogrel Viatris · Clopidogrel Zentiva · Grepid · Iscover · Plavix · Zyllt 
Clopidogrel BGR · Clopidogrel Krka · Clopidogrel Krka d.d. · Clopidogrel Mylan · Clopidogrel ratiopharm · Clopidogrel TAD · Clopidogrel Teva · Clopidogrel Viatris · Clopidogrel Zentiva · Grepid · Iscover · Platel · Plavix · Trombex · Zyllt 
Antiagrex® · Clopicor® · Clopidix · Clopigal® · Plavix® · Zyllt®
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