Peringatan Keamanan

Patients experiencing an overdose of ephedrine will present with rapidly increasing blood pressure.L12972,L34645 Manage overdose with blood pressure monitoring, and possibly the administration of parenteral antihypertensives.L12972,L34645 The LD50 in mice after oral administration is 785mg/kg, after intraperitoneal administration if 248mg/kg, and after subcutaneous administration is 425mg/kg.L12990

Ephedrine

DB01364

small molecule approved

Deskripsi

Ephedrine was first described in western literature in 1888, as a naturally occurring component of the ephedra plant, along with pseudoephedrine.A193698 Ephedrine acts as both a direct and indirect sympathomimetic. It is an alpha- and beta-adrenergic receptor agonist; however, it also causes the indirect release of norepinephrine from sympathetic neurons, inhibiting norepinephrine reuptake and displacing more norepinephrine from storage vesicles.A193650,L12972 Ephedrine is used for its vasoconstrictive, positive chronotropic, and positive inotropic effects.L12972 Ephedrine and phenylephrine are still used to treat hypotension, but their use in other indications has decreased due to the development of more selective adrenergic agonists.A193701,A193704,L12975 Ephedrine was granted a type 7 FDA Approval on 29 April 2016.L12975

Struktur Molekul 2D

Berat 165.2322
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Oral ephedrine has a plasma elimination half life of approximately 6 hours, but there is a large degree of inter-patient variability.[A193644,L12972,L34645]
Volume Distribusi Oral ephedrine has an average volume of distribution of 215.6L.[A193644]
Klirens (Clearance) Oral ephedrine has a clearance of 23.3L/h but there is a high degree of inter-patient variability.[A193644]

Absorpsi

Oral ephedrine reaches an average Cmax of 79.5ng/mL, with a Tmax of 1.81h, and a bioavailability of 88%.A193644

Metabolisme

Ephedrine is largely unmetabolized in the body.A193641 Ephedrine can be N-demethylated to norephedrine, or demethylated and deaminized to benzoic acid conjugates and 1,2-hydroxypropylbenzene.A193641

Rute Eliminasi

Ephedrine is mainly eliminated in the urine.A193641,L12972 Approximately 60% is eliminated as the unmetabolized parent compound, 13% as benzoic acid conjugates, and 1% as 1,2-dihydroxypropylbenzene.A193641

Interaksi Obat

968 Data
Valsartan Ephedrine may decrease the antihypertensive activities of Valsartan.
Reserpine Ephedrine may decrease the antihypertensive activities of Reserpine.
Remikiren Ephedrine may decrease the antihypertensive activities of Remikiren.
Isradipine Ephedrine may decrease the antihypertensive activities of Isradipine.
Olmesartan Ephedrine may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Ephedrine may decrease the antihypertensive activities of Nitroprusside.
Diltiazem Ephedrine may decrease the antihypertensive activities of Diltiazem.
Minoxidil Ephedrine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Ephedrine may decrease the antihypertensive activities of Treprostinil.
Amlodipine Ephedrine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Ephedrine may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Ephedrine may decrease the antihypertensive activities of Nisoldipine.
Fosinopril Ephedrine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Ephedrine may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Ephedrine may decrease the antihypertensive activities of Lercanidipine.
Benazepril Ephedrine may decrease the antihypertensive activities of Benazepril.
Bosentan Ephedrine may decrease the antihypertensive activities of Bosentan.
Enalapril Ephedrine may decrease the antihypertensive activities of Enalapril.
Candoxatril Ephedrine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Ephedrine may decrease the antihypertensive activities of Mecamylamine.
Losartan Ephedrine may decrease the antihypertensive activities of Losartan.
Moexipril Ephedrine may decrease the antihypertensive activities of Moexipril.
Lisinopril Ephedrine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Ephedrine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Ephedrine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Ephedrine may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Ephedrine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Ephedrine may decrease the antihypertensive activities of Fenoldopam.
Tadalafil Ephedrine may decrease the antihypertensive activities of Tadalafil.
Eprosartan Ephedrine may decrease the antihypertensive activities of Eprosartan.
Quinapril Ephedrine may decrease the antihypertensive activities of Quinapril.
Telmisartan Ephedrine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Ephedrine may decrease the antihypertensive activities of Methyldopa.
Irbesartan Ephedrine may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Ephedrine may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Ephedrine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Ephedrine may decrease the antihypertensive activities of Pentolinium.
Captopril Ephedrine may decrease the antihypertensive activities of Captopril.
Epoprostenol Ephedrine may decrease the antihypertensive activities of Epoprostenol.
Bepridil Ephedrine may decrease the antihypertensive activities of Bepridil.
Hydralazine Ephedrine may decrease the antihypertensive activities of Hydralazine.
Cilazapril Ephedrine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Ephedrine may decrease the antihypertensive activities of Saprisartan.
Spirapril Ephedrine may decrease the antihypertensive activities of Spirapril.
Mibefradil Ephedrine may decrease the antihypertensive activities of Mibefradil.
Debrisoquine Ephedrine may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Ephedrine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Ephedrine may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Ephedrine may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Ephedrine may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Ephedrine may decrease the antihypertensive activities of Pinacidil.
Temocapril Ephedrine may decrease the antihypertensive activities of Temocapril.
Riociguat Ephedrine may decrease the antihypertensive activities of Riociguat.
Macitentan Ephedrine may decrease the antihypertensive activities of Macitentan.
Hexamethonium Ephedrine may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Ephedrine may decrease the antihypertensive activities of Aliskiren.
Nicorandil Ephedrine may decrease the antihypertensive activities of Nicorandil.
Lacidipine Ephedrine may decrease the antihypertensive activities of Lacidipine.
Manidipine Ephedrine may decrease the antihypertensive activities of Manidipine.
Rauwolfia serpentina root Ephedrine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Ephedrine may decrease the antihypertensive activities of Enalaprilat.
Selexipag Ephedrine may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Ephedrine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Ephedrine may decrease the antihypertensive activities of Imidapril.
BQ-123 Ephedrine may decrease the antihypertensive activities of BQ-123.
Tetrahydropalmatine Ephedrine may decrease the antihypertensive activities of Tetrahydropalmatine.
Dihydralazine Ephedrine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Ephedrine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Ephedrine may decrease the antihypertensive activities of Guanoxan.
Delapril Ephedrine may decrease the antihypertensive activities of Delapril.
Vincamine Ephedrine may decrease the antihypertensive activities of Vincamine.
Linsidomine Ephedrine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Ephedrine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Ephedrine may decrease the antihypertensive activities of Tolonidine.
Endralazine Ephedrine may decrease the antihypertensive activities of Endralazine.
Cadralazine Ephedrine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Ephedrine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Ephedrine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Ephedrine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Ephedrine may decrease the antihypertensive activities of Guanoclor.
Candesartan Ephedrine may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Ephedrine may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Ephedrine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Ephedrine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Ephedrine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Ephedrine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Ephedrine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Ephedrine may decrease the antihypertensive activities of Quinaprilat.
Felodipine Ephedrine may decrease the antihypertensive activities of Felodipine.
Ramipril Ephedrine may decrease the antihypertensive activities of Ramipril.
Perindopril Ephedrine may decrease the antihypertensive activities of Perindopril.
Levamlodipine Ephedrine may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil Ephedrine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Ephedrine may decrease the antihypertensive activities of Diazoxide.
Atomoxetine The risk or severity of hypertension can be increased when Atomoxetine is combined with Ephedrine.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Ephedrine.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Ephedrine.
Cyclosporine The risk or severity of hypertension can be increased when Cyclosporine is combined with Ephedrine.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Ephedrine.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Ephedrine.

Target Protein

D(2) dopamine receptor DRD2
Alpha-1A adrenergic receptor ADRA1A
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Sodium-dependent noradrenaline transporter SLC6A2

Referensi & Sumber

Synthesis reference: Thomas Moest, Uwe Loeffler, Hans Waiblinger, "Production of pellets composed of an ephedrine derivative." U.S. Patent US5453280, issued March, 1994.
Artikel (PubMed)
  • PMID: 786688
    Sever PS, Dring LG, Williams RT: The metabolism of (-)-ephedrine in man. Eur J Clin Pharmacol. 1975 Dec 19;9(2-3):193-8. doi: 10.1007/bf00614017.
  • PMID: 973934
    Pickup ME, May CS, Ssendagire R, Paterson JW: The pharmacokinetics of ephedrine after oral dosage in asthmatics receiving acute and chronic treatment. Br J Clin Pharmacol. 1976 Feb;3(1):123-34. doi: 10.1111/j.1365-2125.1976.tb00579.x.
  • PMID: 30391401
    Volpp M, Holzgrabe U: Determination of plasma protein binding for sympathomimetic drugs by means of ultrafiltration. Eur J Pharm Sci. 2019 Jan 15;127:175-184. doi: 10.1016/j.ejps.2018.10.027. Epub 2018 Oct 31.
  • PMID: 31613441
    Statler AK, Maani CV, Kohli A: Ephedrine .
  • PMID: 20315579
    Stehle RL: Ephedrine-A New (?) Sympathomimetic Drug. Can Med Assoc J. 1925 Nov;15(11):1158-60.
  • PMID: 30738019
    Wang X, Mao M, Liu S, Xu S, Yang J: A Comparative Study of Bolus Norepinephrine, Phenylephrine, and Ephedrine for the Treatment of Maternal Hypotension in Parturients with Preeclampsia During Cesarean Delivery Under Spinal Anesthesia. Med Sci Monit. 2019 Feb 9;25:1093-1101. doi: 10.12659/MSM.914143.
  • PMID: 29090733
    Kinsella SM, Carvalho B, Dyer RA, Fernando R, McDonnell N, Mercier FJ, Palanisamy A, Sia ATH, Van de Velde M, Vercueil A: International consensus statement on the management of hypotension with vasopressors during caesarean section under spinal anaesthesia. Anaesthesia. 2018 Jan;73(1):71-92. doi: 10.1111/anae.14080. Epub 2017 Nov 1.

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