Aprotinin

DB06692

biotech approved investigational withdrawn

Deskripsi

Aprotinin is a protein-based drug that is also known as bovine pancreatic trypsin inhibitor (BPTI). Since it demonstrates the capacity to slow fibrinolysis, it has been employed to reduce bleeding during complex surgery such as heart and liver surgery. For this use, it is typically administered by injection. The goal of using of aprotinin was subsequently to minimize end-organ damage resulting from hypotension due to blood loss in surgery and to reduce the necessity for blood transfusions during surgery. Nevertheless, the drug was formally withdrawn worldwide in May of 2008 after studies confirmed that its use enhanced the risk of complications or death. The substance is consequently made available only for very restricted research use.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following this distribution phase, a plasma half-life of about 150 minutes is observed. At later time points, (i.e., beyond 5 hours after dosing) there is a terminal elimination phase with a half-life of about 10 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

100% (IV)

Metabolisme

Aprotinin is slowly degraded by lysosomal enzymes.

Rute Eliminasi

Following a single IV dose of radiolabelled aprotinin, approximately 25-40% of the radioactivity is excreted in the urine over 48 hours. After a 30 minute infusion of 1 million KIU, about 2% is excreted as unchanged drug. After a larger dose of 2 million KIU infused over 30 minutes, urinary excretion of unchanged aprotinin accounts for approximately 9% of the dose.

Interaksi Obat

384 Data
Alteplase The therapeutic efficacy of Alteplase can be decreased when used in combination with Aprotinin.
Urokinase The therapeutic efficacy of Urokinase can be decreased when used in combination with Aprotinin.
Reteplase The therapeutic efficacy of Reteplase can be decreased when used in combination with Aprotinin.
Anistreplase The therapeutic efficacy of Anistreplase can be decreased when used in combination with Aprotinin.
Tenecteplase The therapeutic efficacy of Tenecteplase can be decreased when used in combination with Aprotinin.
Drotrecogin alfa The therapeutic efficacy of Drotrecogin alfa can be decreased when used in combination with Aprotinin.
Streptokinase The therapeutic efficacy of Streptokinase can be decreased when used in combination with Aprotinin.
Dicoumarol The therapeutic efficacy of Dicoumarol can be decreased when used in combination with Aprotinin.
Desmoteplase The therapeutic efficacy of Desmoteplase can be decreased when used in combination with Aprotinin.
Defibrotide The therapeutic efficacy of Defibrotide can be decreased when used in combination with Aprotinin.
Ancrod The therapeutic efficacy of Ancrod can be decreased when used in combination with Aprotinin.
Sulodexide The therapeutic efficacy of Sulodexide can be decreased when used in combination with Aprotinin.
Astaxanthin The therapeutic efficacy of Astaxanthin can be decreased when used in combination with Aprotinin.
Amediplase The therapeutic efficacy of Amediplase can be decreased when used in combination with Aprotinin.
Protein C The therapeutic efficacy of Protein C can be decreased when used in combination with Aprotinin.
Monteplase The therapeutic efficacy of Monteplase can be decreased when used in combination with Aprotinin.
Brinase The therapeutic efficacy of Brinase can be decreased when used in combination with Aprotinin.
Saruplase The therapeutic efficacy of Saruplase can be decreased when used in combination with Aprotinin.
Ramipril Aprotinin may decrease the antihypertensive activities of Ramipril.
Fosinopril Aprotinin may decrease the antihypertensive activities of Fosinopril.
Trandolapril Aprotinin may decrease the antihypertensive activities of Trandolapril.
Benazepril Aprotinin may decrease the antihypertensive activities of Benazepril.
Enalapril Aprotinin may decrease the antihypertensive activities of Enalapril.
Moexipril Aprotinin may decrease the antihypertensive activities of Moexipril.
Lisinopril Aprotinin may decrease the antihypertensive activities of Lisinopril.
Perindopril Aprotinin may decrease the antihypertensive activities of Perindopril.
Quinapril Aprotinin may decrease the antihypertensive activities of Quinapril.
Omapatrilat Aprotinin may decrease the antihypertensive activities of Omapatrilat.
Rescinnamine Aprotinin may decrease the antihypertensive activities of Rescinnamine.
Captopril Aprotinin may decrease the antihypertensive activities of Captopril.
Cilazapril Aprotinin may decrease the antihypertensive activities of Cilazapril.
Spirapril Aprotinin may decrease the antihypertensive activities of Spirapril.
Temocapril Aprotinin may decrease the antihypertensive activities of Temocapril.
Enalaprilat Aprotinin may decrease the antihypertensive activities of Enalaprilat.
Imidapril Aprotinin may decrease the antihypertensive activities of Imidapril.
Zofenopril Aprotinin may decrease the antihypertensive activities of Zofenopril.
Delapril Aprotinin may decrease the antihypertensive activities of Delapril.
Benazeprilat Aprotinin may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Aprotinin may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Aprotinin may decrease the antihypertensive activities of Ramiprilat.
Trandolaprilat Aprotinin may decrease the antihypertensive activities of Trandolaprilat.
Moexiprilat Aprotinin may decrease the antihypertensive activities of Moexiprilat.
Perindoprilat Aprotinin may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Aprotinin may decrease the antihypertensive activities of Quinaprilat.
Cilazaprilat Aprotinin may decrease the antihypertensive activities of Cilazaprilat.
Dipyridamole The therapeutic efficacy of Aprotinin can be decreased when used in combination with Dipyridamole.
Ephedrine Aprotinin may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Aprotinin may increase the neuromuscular blocking activities of Bambuterol.
Clevidipine Aprotinin may increase the neuromuscular blocking activities of Clevidipine.
Sar9, Met (O2)11-Substance P Aprotinin may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Mirabegron Aprotinin may increase the neuromuscular blocking activities of Mirabegron.
Moxisylyte Aprotinin may increase the neuromuscular blocking activities of Moxisylyte.
Propacetamol Aprotinin may increase the neuromuscular blocking activities of Propacetamol.
Procaine Aprotinin may increase the neuromuscular blocking activities of Procaine.
Cocaine Aprotinin may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Aprotinin may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Aprotinin may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Aprotinin may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Aprotinin may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Aprotinin may increase the neuromuscular blocking activities of Aclidinium.
Butyrylthiocholine Aprotinin may increase the neuromuscular blocking activities of Butyrylthiocholine.
Oxybuprocaine Aprotinin may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Aprotinin may increase the neuromuscular blocking activities of Benzonatate.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Aprotinin.
Alpha-1-proteinase inhibitor Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Aprotinin.
Menadione Menadione may increase the thrombogenic activities of Aprotinin.
Tranexamic acid Tranexamic acid may increase the thrombogenic activities of Aprotinin.
Aminocaproic acid Aminocaproic acid may increase the thrombogenic activities of Aprotinin.
Hydrogen peroxide Aprotinin may increase the thrombogenic activities of Hydrogen peroxide.
Aminomethylbenzoic acid Aprotinin may increase the thrombogenic activities of Aminomethylbenzoic acid.
Camostat Aprotinin may increase the thrombogenic activities of Camostat.
Menadione bisulfite Aprotinin may increase the thrombogenic activities of Menadione bisulfite.
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Aprotinin.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Aprotinin.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Aprotinin.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Aprotinin.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Aprotinin.
Benzatropine The therapeutic efficacy of Benzatropine can be decreased when used in combination with Aprotinin.
Ziprasidone The therapeutic efficacy of Ziprasidone can be decreased when used in combination with Aprotinin.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Aprotinin.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Aprotinin.
Pentobarbital The therapeutic efficacy of Pentobarbital can be decreased when used in combination with Aprotinin.
Amitriptyline The therapeutic efficacy of Amitriptyline can be decreased when used in combination with Aprotinin.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Aprotinin.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Aprotinin.
Olanzapine The therapeutic efficacy of Olanzapine can be decreased when used in combination with Aprotinin.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Aprotinin.
Terfenadine The therapeutic efficacy of Terfenadine can be decreased when used in combination with Aprotinin.
Buclizine The therapeutic efficacy of Buclizine can be decreased when used in combination with Aprotinin.
Clozapine The therapeutic efficacy of Clozapine can be decreased when used in combination with Aprotinin.
Doxylamine The therapeutic efficacy of Doxylamine can be decreased when used in combination with Aprotinin.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Aprotinin.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Aprotinin.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Aprotinin.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Aprotinin.
Secobarbital The therapeutic efficacy of Secobarbital can be decreased when used in combination with Aprotinin.
Promazine The therapeutic efficacy of Promazine can be decreased when used in combination with Aprotinin.
Hyoscyamine The therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Aprotinin.
Cyproheptadine The therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Aprotinin.
Imipramine The therapeutic efficacy of Imipramine can be decreased when used in combination with Aprotinin.

Target Protein

Serine protease 1 PRSS1
Chymotrypsinogen B CTRB1
Plasminogen PLG
Kallikrein-1 KLK1

Referensi & Sumber

Synthesis reference: Marion Steinbuch, Jacques Chabbat, Olivier Taby, "Process for preparation of activated protein C by immobilized aprotinin chromatography." U.S. Patent US5198534, issued February, 1985.
Artikel (PubMed)
  • PMID: 15277296
    Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Artiss
    Solution • - • Topical • Canada • Approved
  • Tisseel
    Kit • - • Topical • Canada • Approved
  • Tisseel
    Solution • - • Topical • Canada • Approved
  • Trasylol
    Solution • 1000000 1/100mL • Intravenous • US • Approved
  • Trasylol
    Solution • 2000000 1/200mL • Intravenous • US • Approved
  • Trasylol
    Solution • 10000 unit / mL • Intravenous • Canada • Approved
  • Trasylol Inj 10000 Kiu/ml
    Liquid • 100000 unit / amp • Intravenous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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