Peringatan Keamanan

Patients experiencing an overdose may present with tachycardia, arrhythmias, palpitations, angina, hypotension, or hypertension.L33160 Overdose should be treated by reducing or stopping administration of isoprenaline and monitoring blood pressure, pulse, respiration, and ECG.L33160

In rats, the LD50 is 2221 mg/kg orally, 128 mg/kg intraperitoneally, and 600 mg/kg subcutaneously.L33189 In mice, the LD50 is 1260 orally and 450 mg/kg intraperitoneally.L33189

Isoprenaline

DB01064

small molecule approved investigational

Deskripsi

Isoprenaline is a non-selective beta adrenergic receptor agonist indicated to treat heart block, Adams-Stokes attacks, bronchospasm in anesthesia, cadiac arrest, hypovolemic shocks, septic shock, hypoperfusion, congestive hear failure, and cardiogenic shock.A15638,L33160

Isoprenaline research in the 1940s found that this isopropyl analog of epinephrine dilated the bronchi, as well as raising the heart rate and cardiac output, without vasoconstriction.A233724,A233729 The US patent from 1943 states that this compound had a wider therapeutic index and a stronger action than adrenaline.L33204

Isoprenaline was granted FDA approval on 19 February 1948.L33155

Struktur Molekul 2D

Berat 211.2576
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of intravenous isoprenaline is 2.5-5 minutes.[A233584] Oral isoprenaline has a half life of 40 minutes.[A233664]
Volume Distribusi In pediatric patients, the volume of distribution was 216 ± 57 mL/kg.[A233689]
Klirens (Clearance) In pediatric patients, the clearance of isoprenaline was 42.5 ± 5.0 mL/kg/min.[A233689]

Absorpsi

Data regarding absorption kinetics of isoprenaline are not readily available.A233699,A233689

Metabolisme

Isoprenaline is predominantly metabolized to glucuronide conjugates.A233664 Isoprenaline can also be O-methylated by catechol O-methyltransferase to the metabolite 3-O-methylisoprenaline, which can also be further glucuronidated.A233664

Rute Eliminasi

Isoprenaline is 12.2-27.0% recovered in the feces and 59.1-106.8% recovered in the urine after 48 hours.A233664 The majority of the recovered dose in the urine is conjugated isoprenaline, with 6.5-16.2% free isoprenaline, and 2.6-11.4% 3-O-methylisoprenaline and conjugates.A233664

Interaksi Obat

887 Data
Valsartan Isoprenaline may decrease the antihypertensive activities of Valsartan.
Ramipril Isoprenaline may decrease the antihypertensive activities of Ramipril.
Reserpine Isoprenaline may decrease the antihypertensive activities of Reserpine.
Remikiren Isoprenaline may decrease the antihypertensive activities of Remikiren.
Isradipine Isoprenaline may decrease the antihypertensive activities of Isradipine.
Olmesartan Isoprenaline may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Isoprenaline may decrease the antihypertensive activities of Nitroprusside.
Diltiazem Isoprenaline may decrease the antihypertensive activities of Diltiazem.
Minoxidil Isoprenaline may decrease the antihypertensive activities of Minoxidil.
Treprostinil Isoprenaline may decrease the antihypertensive activities of Treprostinil.
Amlodipine Isoprenaline may decrease the antihypertensive activities of Amlodipine.
Nimodipine Isoprenaline may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Isoprenaline may decrease the antihypertensive activities of Nisoldipine.
Fosinopril Isoprenaline may decrease the antihypertensive activities of Fosinopril.
Trandolapril Isoprenaline may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Isoprenaline may decrease the antihypertensive activities of Lercanidipine.
Benazepril Isoprenaline may decrease the antihypertensive activities of Benazepril.
Bosentan Isoprenaline may decrease the antihypertensive activities of Bosentan.
Enalapril Isoprenaline may decrease the antihypertensive activities of Enalapril.
Candoxatril Isoprenaline may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Isoprenaline may decrease the antihypertensive activities of Mecamylamine.
Losartan Isoprenaline may decrease the antihypertensive activities of Losartan.
Moexipril Isoprenaline may decrease the antihypertensive activities of Moexipril.
Eplerenone Isoprenaline may decrease the antihypertensive activities of Eplerenone.
Lisinopril Isoprenaline may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Isoprenaline may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Isoprenaline may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Isoprenaline may decrease the antihypertensive activities of Cryptenamine.
Perindopril Isoprenaline may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Isoprenaline may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Isoprenaline may decrease the antihypertensive activities of Fenoldopam.
Tadalafil Isoprenaline may decrease the antihypertensive activities of Tadalafil.
Eprosartan Isoprenaline may decrease the antihypertensive activities of Eprosartan.
Quinapril Isoprenaline may decrease the antihypertensive activities of Quinapril.
Telmisartan Isoprenaline may decrease the antihypertensive activities of Telmisartan.
Methyldopa Isoprenaline may decrease the antihypertensive activities of Methyldopa.
Irbesartan Isoprenaline may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Isoprenaline may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Isoprenaline may decrease the antihypertensive activities of Deserpidine.
Pentolinium Isoprenaline may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Isoprenaline may increase the neuromuscular blocking activities of Trimethaphan.
Diazoxide Isoprenaline may decrease the antihypertensive activities of Diazoxide.
Captopril Isoprenaline may decrease the antihypertensive activities of Captopril.
Epoprostenol Isoprenaline may decrease the antihypertensive activities of Epoprostenol.
Bepridil Isoprenaline may decrease the antihypertensive activities of Bepridil.
Hydralazine Isoprenaline may decrease the antihypertensive activities of Hydralazine.
Cilazapril Isoprenaline may decrease the antihypertensive activities of Cilazapril.
Saprisartan Isoprenaline may decrease the antihypertensive activities of Saprisartan.
Spirapril Isoprenaline may decrease the antihypertensive activities of Spirapril.
Mibefradil Isoprenaline may decrease the antihypertensive activities of Mibefradil.
Tienilic acid Isoprenaline may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Isoprenaline may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Isoprenaline may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Isoprenaline may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Isoprenaline may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Isoprenaline may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Isoprenaline may decrease the antihypertensive activities of Pinacidil.
Temocapril Isoprenaline may decrease the antihypertensive activities of Temocapril.
Riociguat Isoprenaline may decrease the antihypertensive activities of Riociguat.
Macitentan Isoprenaline may decrease the antihypertensive activities of Macitentan.
Hexamethonium Isoprenaline may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Isoprenaline may decrease the antihypertensive activities of Aliskiren.
Nicorandil Isoprenaline may decrease the antihypertensive activities of Nicorandil.
Efonidipine Isoprenaline may decrease the antihypertensive activities of Efonidipine.
Lacidipine Isoprenaline may decrease the antihypertensive activities of Lacidipine.
Manidipine Isoprenaline may decrease the antihypertensive activities of Manidipine.
Rauwolfia serpentina root Isoprenaline may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Isoprenaline may decrease the antihypertensive activities of Enalaprilat.
Selexipag Isoprenaline may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Isoprenaline may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Isoprenaline may decrease the antihypertensive activities of Imidapril.
BQ-123 Isoprenaline may decrease the antihypertensive activities of BQ-123.
Tetrahydropalmatine Isoprenaline may decrease the antihypertensive activities of Tetrahydropalmatine.
Cicletanine Isoprenaline may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Isoprenaline may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Isoprenaline may decrease the antihypertensive activities of Zofenopril.
Guanoxan Isoprenaline may decrease the antihypertensive activities of Guanoxan.
Delapril Isoprenaline may decrease the antihypertensive activities of Delapril.
Vincamine Isoprenaline may decrease the antihypertensive activities of Vincamine.
Linsidomine Isoprenaline may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Isoprenaline may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Isoprenaline may decrease the antihypertensive activities of Tolonidine.
Endralazine Isoprenaline may decrease the antihypertensive activities of Endralazine.
Cadralazine Isoprenaline may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Isoprenaline may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Isoprenaline may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Isoprenaline may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Isoprenaline may decrease the antihypertensive activities of Guanoclor.
Muzolimine Isoprenaline may decrease the antihypertensive activities of Muzolimine.
Xipamide Isoprenaline may decrease the antihypertensive activities of Xipamide.
Candesartan Isoprenaline may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Isoprenaline may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Isoprenaline may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Isoprenaline may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Isoprenaline may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Isoprenaline may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Isoprenaline may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Isoprenaline may decrease the antihypertensive activities of Quinaprilat.
Felodipine Isoprenaline may decrease the antihypertensive activities of Felodipine.
Levamlodipine Isoprenaline may decrease the antihypertensive activities of Levamlodipine.

Target Protein

Beta-1 adrenergic receptor ADRB1
Interleukin-12 subunit beta IL12B
Beta-2 adrenergic receptor ADRB2
Beta-3 adrenergic receptor ADRB3
Superoxide dismutase [Cu-Zn] SOD1

Referensi & Sumber

Synthesis reference: U.S. Patent 2,308,232. U.S. Patent 2,715,141.
Artikel (PubMed)
  • PMID: 30252298
    Szymanski MW, Singh DP: Isoproterenol .
  • PMID: 20590599
    Baker JG: The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol. 2010 Jul;160(5):1048-61. doi: 10.1111/j.1476-5381.2010.00754.x.
  • PMID: 24683526
    Striessnig J, Pinggera A, Kaur G, Bock G, Tuluc P: L-type Ca(2+) channels in heart and brain. Wiley Interdiscip Rev Membr Transp Signal. 2014 Mar 1;3(2):15-38. doi: 10.1002/wmts.102.
  • PMID: 23266596
    Harvey RD, Hell JW: CaV1.2 signaling complexes in the heart. J Mol Cell Cardiol. 2013 May;58:143-52. doi: 10.1016/j.yjmcc.2012.12.006. Epub 2012 Dec 22.
  • PMID: 31643996
    Authors unspecified: Beta-2 Adrenergic Agonists .
  • PMID: 4656607
    Conolly ME, Davies DS, Dollery CT, Morgan CD, Paterson JW, Sandler M: Metabolism of isoprenaline in dog and man. Br J Pharmacol. 1972 Nov;46(3):458-72. doi: 10.1111/j.1476-5381.1972.tb08143.x.
  • PMID: 8429110
    Reyes G, Schwartz PH, Newth CJ, Eldadah MK: The pharmacokinetics of isoproterenol in critically ill pediatric patients. J Clin Pharmacol. 1993 Jan;33(1):29-34. doi: 10.1002/j.1552-4604.1993.tb03899.x.
  • PMID: 6630523
    Goldstein DS, Horwitz D, Keiser HR, Polinsky RJ, Kopin IJ: Plasma l-3Hnorepinephrine, d-14Cnorepinephrine, and d,l-3Hisoproterenol kinetics in essential hypertension. J Clin Invest. 1983 Nov;72(5):1748-58. doi: 10.1172/JCI111134.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 44 • International brands: 2
Produk
  • Duo-Medihaler
    Aerosol, metered • - • Respiratory (inhalation) • US • Approved
  • Isoproterenol
    Injection, solution • 0.2 mg/1mL • Intracardiac; Intramuscular; Intravenous; Subcutaneous • US • Generic • Approved
  • Isoproterenol
    Injection, solution • 1 mg/5mL • Intracardiac; Intramuscular; Intravenous; Subcutaneous • US • Generic • Approved
  • Isoproterenol HCl Inj 1:5000
    Liquid • .2 mg / mL • Intravenous • Canada • Approved
  • Isoproterenol Hydrochloride
    Injection, solution • 0.2 mg/1mL • Intracardiac; Intramuscular; Intravenous; Subcutaneous • US • Generic • Approved
  • Isoproterenol Hydrochloride
    Injection, solution • 0.2 mg/1mL • Intracardiac; Intramuscular; Intravenous; Subcutaneous • US • Generic • Approved
  • Isoproterenol Hydrochloride
    Injection, solution • 0.2 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Isoproterenol Hydrochloride
    Injection, solution • 0.2 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
Menampilkan 8 dari 44 produk.
International Brands
  • Proternol L — Kowa Souyaku
  • Saventrine — Pharmax

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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