Peringatan Keamanan

Patients experiencing an overdose may present with bleeding, nausea, vomiting, diarrhea, and ventricular pauses.L14201 Overdose can be managed through symptomatic and supportive treatment, including ECG monitoring.L14201,L14207 Dialysis is not expected to remove ticagrelor from the blood due to it being highly protein bound.L14201

Ticagrelor

DB08816

small molecule approved

Deskripsi

Ticagrelor, or AZD6140, was first described in the literature in 2003.A204170,A2903 Ticagrelor is an ADP derivative developed for its P2Y12 receptor antagonism.A2903 Unlike clopidogrel, ticagrelor is not a prodrug.A2903 It is marketed by Astra Zeneca as Brilinta in the USL14201 and Brilique or Possia in the EU,L14207.

Ticagrelor was granted EMA approval on 3 December 2010.L14207
Ticagrelor was granted FDA approval on 20 July 2011.L14201

Struktur Molekul 2D

Berat 522.568
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ticagrelor has a plasma half life of approximately 8 hours, while the active metabolite has a plasma half life of approximately 12 hours.[A17595]
Volume Distribusi The steady state volume of distribution of ticagrelor is 88 L.[L14201]
Klirens (Clearance) The renal clearance of ticagrelor is 0.00584L/h.[A17595]

Absorpsi

Ticagrelor is 36% orally bioavailable.L14201 A single 200mg oral dose of ticagrelor reaches a Cmax of 923ng/mL, with a Tmax of 1.5 hours and an AUC of 6675ng\*h/mL.A17595 The active metabolite of ticagrelor reaches a Cmax of 264ng/mL, with a Tmax of 3.0 hours and an AUC of 2538ng\*h/mL.A17595

Metabolisme

The complete structure of all ticagrelor metabolites are not well defined.A17595 Ticagrelor can be dealkylated at postition 5 of the cyclopentane ring to form the active AR-C124910XX.A17595 AR-C124910XX's cyclopentane ring can be further glucuronidated or the alkyl chain attached to the sulfur can be hydroxylated.A17595 Ticagrelor can also be glucuronidated or hydroxylated.A17595 Ticagrelor can also be N-dealkylated to form AR-C133913XX, which is further glucuronidated or hydroxylated.A17595

Rute Eliminasi

A radiolabelled dose of ticagrelor is 57.8% recovered in feces and 26.5% recovered in urine.A17595,L14201 Less than 1% of the dose is recovered as the unmetabolized parent drug.L14201 The active metabolite AC-C124910XX makes up 21.7% of the recovery in the feces.A17595 The metabolite AR-C133913XX makes up 9.2% of the recovery in the urine and 2.7% of the recovery in the feces.A17595 Other minor metabolites are predominantly recovered in the urine.A17595

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of ticagrelor, which may increase its serum concentration.
  • 2. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Herbs with antiplatelet activity may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 3. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of ticagrelor and may reduce its serum concentration.
  • 4. Take with or without food.

Interaksi Obat

1219 Data
Apixaban Apixaban may increase the anticoagulant activities of Ticagrelor.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Ticagrelor.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Ticagrelor is combined with Deferasirox.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Ticagrelor.
Rivaroxaban Ticagrelor may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Ticagrelor is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Ticagrelor.
Urokinase Urokinase may increase the anticoagulant activities of Ticagrelor.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ticagrelor.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Ticagrelor is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Ticagrelor is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Ticagrelor.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ticagrelor is combined with Ibritumomab tiuxetan.
Obinutuzumab The risk or severity of adverse effects can be increased when Ticagrelor is combined with Obinutuzumab.
Vitamin E Vitamin E may increase the antiplatelet activities of Ticagrelor.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Ticagrelor.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Ticagrelor.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Ticagrelor.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Ticagrelor.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Ticagrelor.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Ticagrelor.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Ticagrelor.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Ticagrelor.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Ticagrelor.
Silodosin The excretion of Silodosin can be decreased when combined with Ticagrelor.
Cyclosporine The serum concentration of Ticagrelor can be increased when it is combined with Cyclosporine.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Ticagrelor.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Ticagrelor.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Ticagrelor.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Ticagrelor.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Ticagrelor.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Ticagrelor.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Ticagrelor.
Fentanyl Fentanyl can cause a decrease in the absorption of Ticagrelor resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Ticagrelor.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Ticagrelor.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Ticagrelor.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Ticagrelor.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Ticagrelor.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Ticagrelor.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Ticagrelor.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Ticagrelor.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Ticagrelor.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Ticagrelor.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Ticagrelor.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Ticagrelor.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Ticagrelor.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Ticagrelor.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Ticagrelor.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Ticagrelor.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Ticagrelor.
Quinine The therapeutic efficacy of Ticagrelor can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Ticagrelor can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Ticagrelor.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Ticagrelor.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Ticagrelor.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Ticagrelor.
Acetylsalicylic acid The therapeutic efficacy of Ticagrelor can be decreased when used in combination with Acetylsalicylic acid.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Ticagrelor.
Pentoxifylline The therapeutic efficacy of Ticagrelor can be increased when used in combination with Pentoxifylline.
Dabigatran etexilate Ticagrelor may increase the anticoagulant activities of Dabigatran etexilate.
Pentosan polysulfate The risk or severity of adverse effects can be increased when Pentosan polysulfate is combined with Ticagrelor.
Levocarnitine The therapeutic efficacy of Ticagrelor can be increased when used in combination with Levocarnitine.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Ticagrelor.
Quinestrol Quinestrol may decrease the anticoagulant activities of Ticagrelor.
Hexestrol Hexestrol may decrease the anticoagulant activities of Ticagrelor.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Ticagrelor.
Zeranol Zeranol may decrease the anticoagulant activities of Ticagrelor.
Equol Equol may decrease the anticoagulant activities of Ticagrelor.
Methallenestril Methallenestril may decrease the anticoagulant activities of Ticagrelor.
Epimestrol Epimestrol may decrease the anticoagulant activities of Ticagrelor.
Moxestrol Moxestrol may decrease the anticoagulant activities of Ticagrelor.
Biochanin A Biochanin A may decrease the anticoagulant activities of Ticagrelor.
Formononetin Formononetin may decrease the anticoagulant activities of Ticagrelor.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Ticagrelor.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Ticagrelor.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Ticagrelor.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Ticagrelor.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Ticagrelor.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Ticagrelor.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Ticagrelor.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Ticagrelor.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Ticagrelor.
Estriol Estriol may decrease the anticoagulant activities of Ticagrelor.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Ticagrelor.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Ticagrelor.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Ticagrelor.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Ticagrelor.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Ticagrelor.

Target Protein

P2Y purinoceptor 12 P2RY12

Referensi & Sumber

Synthesis reference: Anil Shahaji Khile, "NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR." U.S. Patent US20130165696, issued June 27, 2013.
Artikel (PubMed)
  • PMID: 20551239
    Teng R, Oliver S, Hayes MA, Butler K: Absorption, distribution, metabolism, and excretion of ticagrelor in healthy subjects. Drug Metab Dispos. 2010 Sep;38(9):1514-21. doi: 10.1124/dmd.110.032250. Epub 2010 Jun 15.
  • PMID: 30167561
    Angheloiu GO, Gugiu GB, Ruse C, Pandey R, Dasari RR, Whatling C: Ticagrelor Removal From Human Blood. JACC Basic Transl Sci. 2017 Apr 24;2(2):135-145. doi: 10.1016/j.jacbts.2017.01.007. eCollection 2017 Apr.
  • PMID: 14755328
    Dorsam RT, Kunapuli SP: Central role of the P2Y12 receptor in platelet activation. J Clin Invest. 2004 Feb;113(3):340-5. doi: 10.1172/JCI20986.
  • PMID: 15078212
    Jacobson KA, Costanzi S, Ohno M, Joshi BV, Besada P, Xu B, Tchilibon S: Molecular recognition at purine and pyrimidine nucleotide (P2) receptors. Curr Top Med Chem. 2004;4(8):805-19. doi: 10.2174/1568026043450961.
  • PMID: 17827008
    Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG, Hunt SF, Ince F, Ingall AH, Kirk IP, Leeson PD, Leff P, Lewis RJ, Martin BP, McGinnity DF, Mortimore MP, Paine SW, Pairaudeau G, Patel A, Rigby AJ, Riley RJ, Teobald BJ, Tomlinson W, Webborn PJ, Willis PA: From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6013-8. Epub 2007 Aug 19.

Contoh Produk & Brand

Produk: 38 • International brands: 2
Produk
  • Ag-ticagrelor
    Tablet • 60 mg • Oral • Canada • Generic • Approved
  • Ag-ticagrelor
    Tablet • 90 mg • Oral • Canada • Generic • Approved
  • Apo-ticagrelor
    Tablet • 60 mg • Oral • Canada • Generic • Approved
  • Apo-ticagrelor
    Tablet • 90 mg • Oral • Canada • Generic • Approved
  • Brilinta
    Tablet • 90 mg/1 • Oral • US • Approved
  • Brilinta
    Tablet • 90 mg/1 • Oral • US • Approved
  • Brilinta
    Tablet • 60 mg/1 • Oral • US • Approved
  • Brilinta
    Tablet • 90 mg/1 • Oral • US • Approved
Menampilkan 8 dari 38 produk.
International Brands
  • Brilinta
  • Possia — AstraZeneca

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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