Peringatan Keamanan

LD50 (rat) 1,000 - 2,000 mg/kg; LD50 (rabbit) > 1,000 mg/kg

Prasugrel

DB06209

small molecule approved

Deskripsi

Prasugrel, a thienopyridine derivative, is a platelet activation and aggregation inhibitor structurally and pharmacologically related to clopidogrel and ticlopidine. Similar to clopidogrel, prasugrel is a prodrug that requires enzymatic transformation in the liver to its active metabolite, R-138727. R-138727 irreversibly binds to P2Y12 type ADP receptors on platelets thus preventing activation of the GPIIb/IIIa receptor complex. As a result, inhibition of ADP-mediated platelet activation and aggregation occurs. Prasugrel was developed by Daiichi Sankyo Co. and is currently marketed in the United States and Canada in cooperation with Eli Lilly and Company for acute coronary syndromes planned for percutaneous coronary intervention (PCI). FDA approved in 2009.

Struktur Molekul 2D

Berat 373.441
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The active metabolite has an elimination half-life of about 7.4 hours (range 2-15 hours).
Volume Distribusi 44-68L
Klirens (Clearance) Apparent clearance = 112 - 166 L/hr

Absorpsi

79% or greater of the dose is absorbed after oral administration. Absorption and metabolism occur rapidly and peak plasma concentrations (Cmax) are reached approximately 30 minutes following oral administration. Administration with a high fat, high calorie meal did not affect the AUC of the active metabolite in healthy individuals, but the Cmax was decreased by ~49% and the Tmax was increased to 0.5 to 1.5 hours. Prasugrel may be administered with or without food.

Metabolisme

Prasugrel is not detected in plasma following oral administration. It is rapidly hydrolyzed in the intestine to thiolactone by human carboxylesterase (hCE) 2. This intermediate is further metabolized to its active metabolite, R-138727, in a single step by cytochrome P450 enzymes in the liver (primarily CYP3A4 and CYP2B6 and to a lesser extent by CYP2C9 and CYP2C19). The active metabolite is further metabolized by S-methylation or cysteine conjugation to two inactive metabolites. Unlike clopidogrel, transformation of prasugrel to its active metabolite does not appear to be affected by cytochrome P450 polymorphisms.

Rute Eliminasi

Approximately 68% of the orally administered dose is excreted in urine and 27% in the feces, as inactive metabolites. The active metabolite is not expected to be removed by dialysis.

Interaksi Makanan

2 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Take with or without food.

Interaksi Obat

1371 Data
Apixaban Apixaban may increase the anticoagulant activities of Prasugrel.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Prasugrel.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Prasugrel.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Prasugrel is combined with Deferasirox.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Prasugrel.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Prasugrel.
Rivaroxaban Prasugrel may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Prasugrel is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Prasugrel.
Urokinase Urokinase may increase the anticoagulant activities of Prasugrel.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Prasugrel.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Prasugrel is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Prasugrel is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Prasugrel.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Prasugrel is combined with Ibritumomab tiuxetan.
Obinutuzumab The risk or severity of adverse effects can be increased when Prasugrel is combined with Obinutuzumab.
Tipranavir Tipranavir may increase the antiplatelet activities of Prasugrel.
Vitamin E Vitamin E may increase the antiplatelet activities of Prasugrel.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Prasugrel.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Prasugrel.
Quinine The therapeutic efficacy of Prasugrel can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Prasugrel can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Prasugrel.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Prasugrel.
Pentoxifylline The therapeutic efficacy of Prasugrel can be increased when used in combination with Pentoxifylline.
Cangrelor Cangrelor may decrease the antiplatelet activities of Prasugrel.
Pentosan polysulfate The risk or severity of adverse effects can be increased when Pentosan polysulfate is combined with Prasugrel.
Levocarnitine The therapeutic efficacy of Prasugrel can be increased when used in combination with Levocarnitine.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Prasugrel.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Prasugrel.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Prasugrel.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Prasugrel.
Estrone sulfate Estrone sulfate may decrease the anticoagulant activities of Prasugrel.
Quinestrol Quinestrol may decrease the anticoagulant activities of Prasugrel.
Hexestrol Hexestrol may decrease the anticoagulant activities of Prasugrel.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Prasugrel.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Prasugrel.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Prasugrel.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Prasugrel.
Zeranol Zeranol may decrease the anticoagulant activities of Prasugrel.
Equol Equol may decrease the anticoagulant activities of Prasugrel.
Methallenestril Methallenestril may decrease the anticoagulant activities of Prasugrel.
Epimestrol Epimestrol may decrease the anticoagulant activities of Prasugrel.
Moxestrol Moxestrol may decrease the anticoagulant activities of Prasugrel.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Prasugrel.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Prasugrel.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Prasugrel.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Prasugrel.
Biochanin A Biochanin A may decrease the anticoagulant activities of Prasugrel.
Formononetin Formononetin may decrease the anticoagulant activities of Prasugrel.
Estriol Estriol may decrease the anticoagulant activities of Prasugrel.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Prasugrel.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Prasugrel.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Prasugrel.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Prasugrel.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Prasugrel.
Ketorolac The risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Prasugrel.
Tenoxicam The risk or severity of bleeding and hemorrhage can be increased when Tenoxicam is combined with Prasugrel.
Celecoxib The risk or severity of bleeding and hemorrhage can be increased when Celecoxib is combined with Prasugrel.
Tolmetin The risk or severity of bleeding and hemorrhage can be increased when Tolmetin is combined with Prasugrel.
Rofecoxib The risk or severity of bleeding and hemorrhage can be increased when Rofecoxib is combined with Prasugrel.
Piroxicam The risk or severity of bleeding and hemorrhage can be increased when Piroxicam is combined with Prasugrel.
Fenoprofen The risk or severity of bleeding and hemorrhage can be increased when Fenoprofen is combined with Prasugrel.
Valdecoxib The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Prasugrel.
Diclofenac The risk or severity of bleeding and hemorrhage can be increased when Diclofenac is combined with Prasugrel.
Sulindac The risk or severity of bleeding and hemorrhage can be increased when Sulindac is combined with Prasugrel.
Flurbiprofen The risk or severity of bleeding and hemorrhage can be increased when Flurbiprofen is combined with Prasugrel.
Etodolac The risk or severity of bleeding and hemorrhage can be increased when Etodolac is combined with Prasugrel.
Mefenamic acid The risk or severity of bleeding and hemorrhage can be increased when Mefenamic acid is combined with Prasugrel.
Naproxen The risk or severity of bleeding and hemorrhage can be increased when Naproxen is combined with Prasugrel.
Sulfasalazine The risk or severity of bleeding and hemorrhage can be increased when Sulfasalazine is combined with Prasugrel.
Phenylbutazone The risk or severity of bleeding and hemorrhage can be increased when Phenylbutazone is combined with Prasugrel.
Meloxicam The risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Prasugrel.
Carprofen The risk or severity of bleeding and hemorrhage can be increased when Carprofen is combined with Prasugrel.
Diflunisal The risk or severity of bleeding and hemorrhage can be increased when Diflunisal is combined with Prasugrel.
Salicylic acid The risk or severity of bleeding and hemorrhage can be increased when Salicylic acid is combined with Prasugrel.
Meclofenamic acid The risk or severity of bleeding and hemorrhage can be increased when Meclofenamic acid is combined with Prasugrel.
Oxaprozin The risk or severity of bleeding and hemorrhage can be increased when Oxaprozin is combined with Prasugrel.
Ketoprofen The risk or severity of bleeding and hemorrhage can be increased when Ketoprofen is combined with Prasugrel.
Balsalazide The risk or severity of bleeding and hemorrhage can be increased when Balsalazide is combined with Prasugrel.
Olsalazine The risk or severity of bleeding can be increased when Olsalazine is combined with Prasugrel.
Lumiracoxib The risk or severity of bleeding and hemorrhage can be increased when Lumiracoxib is combined with Prasugrel.
Magnesium salicylate The risk or severity of bleeding and hemorrhage can be increased when Magnesium salicylate is combined with Prasugrel.
Salsalate The risk or severity of bleeding and hemorrhage can be increased when Salsalate is combined with Prasugrel.
Choline magnesium trisalicylate The risk or severity of bleeding and hemorrhage can be increased when Choline magnesium trisalicylate is combined with Prasugrel.
Antrafenine The risk or severity of bleeding and hemorrhage can be increased when Antrafenine is combined with Prasugrel.
Aminophenazone The risk or severity of bleeding and hemorrhage can be increased when Aminophenazone is combined with Prasugrel.
Antipyrine The risk or severity of bleeding and hemorrhage can be increased when Antipyrine is combined with Prasugrel.
Tiaprofenic acid The risk or severity of bleeding and hemorrhage can be increased when Tiaprofenic acid is combined with Prasugrel.

Target Protein

P2Y purinoceptor 12 P2RY12

Referensi & Sumber

Synthesis reference: Teruhiko Inoue, Kazuyoshi Nakamura, Masahiko Hagihara, Hiroyuki Miyata, Yukinori Wada, Naoyuki Yokota, "Process for Producing High-Purity Prasugrel and Acid Addition Salt Thereof." U.S. Patent US20090203729, issued August 13, 2009.
Artikel (PubMed)
  • PMID: 18485086
    Dovlatova NL, Jakubowski JA, Sugidachi A, Heptinstall S: The reversible P2Y antagonist cangrelor influences the ability of the active metabolites of clopidogrel and prasugrel to produce irreversible inhibition of platelet function. J Thromb Haemost. 2008 Jul;6(7):1153-9. doi: 10.1111/j.1538-7836.2008.03020.x. Epub 2008 Jul 1.
  • PMID: 20874669
    Tagarakis GI: Ticagrelor and prasugrel: two novel, most-promising antiplatelet agents. Recent Pat Cardiovasc Drug Discov. 2010 Nov;5(3):208-11.
  • PMID: 23083110
    Angiolillo DJ: The evolution of antiplatelet therapy in the treatment of acute coronary syndromes: from aspirin to the present day. Drugs. 2012 Nov 12;72(16):2087-116. doi: 10.2165/11640880-000000000-00000.
  • PMID: 22783896
    Jeong YH, Tantry US, Gurbel PA: Importance of potent P2Y(12) receptor blockade in acute myocardial infarction: focus on prasugrel. Expert Opin Pharmacother. 2012 Aug;13(12):1771-96. doi: 10.1517/14656566.2012.704909. Epub 2012 Jul 12.

Contoh Produk & Brand

Produk: 76 • International brands: 1
Produk
  • Effient
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Effient
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
  • Effient
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Effient
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
  • Effient
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Effient
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Effient
    Tablet, coated • 5 mg/1 • Oral • US • Approved
  • Effient
    Tablet, coated • 10 mg/1 • Oral • US • Approved
Menampilkan 8 dari 76 produk.
International Brands
  • Prasita — Daiichi Sankyo Co.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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