Peringatan Keamanan

Toxicity information regarding alteplase is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as risk of bleeding and thromboembolic events.L43125 Symptomatic and supportive measures are recommended. The carcinogenic potential of alteplase or its effect on fertility have not been evaluated. In vivo studies evaluating tumorigenicity and in vitro studies evaluating mutagenicity were negative.L43125 It has been estimated that the acute oral and dermal toxicity of alteplase is above 5,000 mg/kg.L43175

Alteplase

DB00009

biotech approved investigational

Deskripsi

Alteplase is a recombinant tissue plasminogen activator (rt-PA) used as a thrombolytic agent.L43125 It cleaves plasminogen to form plasmin, an enzyme involved in the degradation of fibrin clots. In the absence of fibrin, the alteplase-mediated conversion of plasminogen is limited, thanks to the high affinity between alteplase and fibrin.A252330,L43125 Alteplase is a purified glycoprotein of 527 amino acids expressed in Chinese hamster ovary (CHO) cells.A252345,L43125 It was first approved by the FDA in 1987 for the management of thromboembolic disease, including acute myocardial infarction (AMI).A252270 The use of alteplase to manage AMI has decreased thanks to the availability of safer treatments such as angioplasty and stenting. However, its use for the treatment of acute ischemic stroke (AIS) has increased over the years.A252340 New thrombolytic agents derived from tissue plasminogen activator, such as desmoteplase, tenecteplase and reteplase, have also been developed.A252270,A252345 Alteplase is also available as Cathflo Activase (intracatheter instillation) for the restoration of function to central venous access devices.L34864

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Alteplase has an initial half-life of less than 5 minutes in patients with acute myocardial infarction (AMI). The dominant initial plasma half-life of the 3-hour and the accelerated regimens for AMI are similar.[L43125]
Volume Distribusi The initial volume of distribution approximates plasma volume.[L43125] The average volume of distribution of the central compartment goes from 3.9 to 4.3 L, and the volume of distribution at steady state goes from 7.2 to 12 L.[A252270]
Klirens (Clearance) Alteplase has a plasma clearance between 380 and 570 mL/min.[L43125]

Absorpsi

Healthy volunteers with a baseline endogenous tissue plasminogen activator (t-PA) of 3.3 ng/ml had a 290-fold increase in baseline concentrations after receiving alteplase at an infusion rate of 0.25 mg/kg for 30 min; with an infusion rate of 0.5 mg/kg, a 550-fold increase was observed.A252270 Acute myocardial infarction patients (n=12) given 10 mg of alteplase in a 2-minute infusion reached a peak plasma concentration of 3310 ng/ml. This was followed by 50 mg of alteplase in 1 h and 30 mg in 1.5 h, resulting in steady-state plasma levels of 2210 ng/ml and 930 ng/ml, respectively.A252285

Metabolisme

Alteplase is mainly metabolized by the liver. The carbohydrate and polypeptide domains of alteplase interact with hepatic glycoprotein receptors, leading to receptor-mediated endocytosis.A252270 In vivo studies suggest that alteplase follows zero-order kinetics, meaning that its metabolism is saturable at higher plasma concentrations.A252270

Rute Eliminasi

In healthy volunteers, more than 80% of alteplase is eliminated through urine 18 hours after administration.A252270

Interaksi Makanan

1 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

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

Target Protein

Plasminogen PLG
Fibrinogen alpha chain FGA
Fibrinogen gamma chain FGG
Plasminogen activator inhibitor 1 SERPINE1

Referensi & Sumber

Synthesis reference: Goeddel, DV., et al. (1988). Human tissue plasminogen activator (U.S. Patent No. 4,766,075 A). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/a7/38/45/ec3813293b05c5/US4766075.pdf
Artikel (PubMed)
  • PMID: 22248305
    Acheampong P, Ford GA: Pharmacokinetics of alteplase in the treatment of ischaemic stroke. Expert Opin Drug Metab Toxicol. 2012 Feb;8(2):271-81. doi: 10.1517/17425255.2012.652615. Epub 2012 Jan 17.
  • PMID: 2508258
    Seifried E, Tanswell P, Ellbruck D, Haerer W, Schmidt A: Pharmacokinetics and haemostatic status during consecutive infusions of recombinant tissue-type plasminogen activator in patients with acute myocardial infarction. Thromb Haemost. 1989 Jun 30;61(3):497-501.
  • PMID: 22950491
    Dhillon S: Alteplase: a review of its use in the management of acute ischaemic stroke. CNS Drugs. 2012 Oct 1;26(10):899-926. doi: 10.2165/11209940-000000000-00000.
  • PMID: 11772304
    Doggrell SA: Alteplase: descendancy in myocardial infarction, ascendancy in stroke. Expert Opin Investig Drugs. 2001 Nov;10(11):2013-29. doi: 10.1517/13543784.10.11.2013.
  • PMID: 15102005
    Collen D, Lijnen HR: Tissue-type plasminogen activator: a historical perspective and personal account. J Thromb Haemost. 2004 Apr;2(4):541-6. doi: 10.1111/j.1538-7933.2004.00645.x.

Contoh Produk & Brand

Produk: 10 • International brands: 0
Produk
  • Activase
    Injection, powder, lyophilized, for solution; Kit • 50 mg/50mL • Intravenous • US • Approved
  • Activase
    Injection, powder, lyophilized, for solution; Kit • 100 mg/100mL • Intravenous • US • Approved
  • Activase RT-PA
    Liquid; Powder, for solution • - • Intravenous • Canada • Approved
  • Activase RT-PA
    Liquid; Powder, for solution • - • Intravenous • Canada • Approved
  • Activase RT-PA Inj
    Powder, for solution • 50 mg/50mL • Intravenous • Canada • Approved
  • Activase RT-PA Inj
    Powder, for solution • 50 mg/50mL • Intravenous • Canada • Approved
  • Activase RT-PA Inj
    Powder, for solution • 50 mg/50mL • Intravenous • Canada • Approved
  • Cathflo
    Powder, for solution • 2 mg / vial • Intravenous • Canada • Approved
Menampilkan 8 dari 10 produk.

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