Peringatan Keamanan

Ld50 mouse (intraperitoneal): 185mg/kg L2835.

Sympathomimetic drugs, such as DL-methylphedrine, can lead to an increase in catecholamines, resulting in a variety of effects A33132, L2848:

Nervous System/CNS/Psychiatric

Insomnia, Headaches, Seizure, Cerebrovascular Accident, Nervousness, Tremor or other motor disturbance, Psychosis with long-term, chronic use F100

Cardiovascular System
Hypertension, Cardiac arrhythmia, Myocardial Infarction, Hypersensitivity Myocarditis

Renal System
Nephrolithiasis

General
Predisposition to Heat Exhaustion and Heat Stroke, Hyperglycemia, Glaucoma

The Japanese Ministry of Health made a statement in July 2017 that preparations containing this drug should not be used in children younger than 12 years old (who are highly susceptible to respiratory depression. Overseas, there have been reports that the risk of serious respiratory depression, including death, is high in children younger than 12 years old) F98.

DL-Methylephedrine

DB11278

small molecule approved

Deskripsi

Methylephedrine is a sympathomimetic amine that appears in various over-the-counter cough and cold medications throughout the world L2838, L2839, L2840. The abuse of methylephedrine-containing medications has been reported in Japan. Methylephedrine is not legally available in the United States, but has been identified in cases of drug abuse L2836.

Struktur Molekul 2D

Berat 179.263
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3-6 hours (Ephedrine) [F100].
Volume Distribusi Ephedrine: 2.5-3.0 L/kg [T217]. Methylephedrine is a derivative of ephedrine [L2844] and quickly distributed throughout the body [F100].
Klirens (Clearance) -

Absorpsi

Methylephedrine is rapidly absorbed following oral administration L2836. Peak plasma concentrations of ephedrine (from which methylephedrine is derived) occur 2-3h after administration T217. Due to the fact that methylephedrine is a derivative of ephedrine L2844, peak plasma concentrations are likely similar.

Metabolisme

Methylephedrine is metabolized to give ephedrine and norephedrine F100.

Rute Eliminasi

The primary compound excreted in urine is unchanged methylephedrine (33-40% of dose), followed by the metabolite methylephedrine-N-oxide (15% of dose), and approximately 8% of the dose excreted as ephedrine after 24 hours. About 70% of the dose is excreted in the urine as metabolites over 72 hours L2836. Alkaline urine reduces elimination to 20-35% of the dose F100.

Interaksi Obat

1178 Data
Valsartan DL-Methylephedrine may decrease the antihypertensive activities of Valsartan.
Ramipril DL-Methylephedrine may decrease the antihypertensive activities of Ramipril.
Remikiren DL-Methylephedrine may decrease the antihypertensive activities of Remikiren.
Olmesartan DL-Methylephedrine may decrease the antihypertensive activities of Olmesartan.
Diltiazem DL-Methylephedrine may decrease the antihypertensive activities of Diltiazem.
Minoxidil DL-Methylephedrine may decrease the antihypertensive activities of Minoxidil.
Treprostinil DL-Methylephedrine may decrease the antihypertensive activities of Treprostinil.
Amlodipine DL-Methylephedrine may decrease the antihypertensive activities of Amlodipine.
Nimodipine DL-Methylephedrine may decrease the antihypertensive activities of Nimodipine.
Trandolapril DL-Methylephedrine may decrease the antihypertensive activities of Trandolapril.
Lercanidipine DL-Methylephedrine may decrease the antihypertensive activities of Lercanidipine.
Benazepril DL-Methylephedrine may decrease the antihypertensive activities of Benazepril.
Bosentan DL-Methylephedrine may decrease the antihypertensive activities of Bosentan.
Enalapril DL-Methylephedrine may decrease the antihypertensive activities of Enalapril.
Candoxatril DL-Methylephedrine may decrease the antihypertensive activities of Candoxatril.
Losartan DL-Methylephedrine may decrease the antihypertensive activities of Losartan.
Moexipril DL-Methylephedrine may decrease the antihypertensive activities of Moexipril.
Nitroglycerin DL-Methylephedrine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine DL-Methylephedrine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine DL-Methylephedrine may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil DL-Methylephedrine may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan DL-Methylephedrine may decrease the antihypertensive activities of Eprosartan.
Quinapril DL-Methylephedrine may decrease the antihypertensive activities of Quinapril.
Telmisartan DL-Methylephedrine may decrease the antihypertensive activities of Telmisartan.
Irbesartan DL-Methylephedrine may decrease the antihypertensive activities of Irbesartan.
Nitrendipine DL-Methylephedrine may decrease the antihypertensive activities of Nitrendipine.
Deserpidine DL-Methylephedrine may decrease the antihypertensive activities of Deserpidine.
Pentolinium DL-Methylephedrine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan DL-Methylephedrine may decrease the antihypertensive activities of Trimethaphan.
Captopril DL-Methylephedrine may decrease the antihypertensive activities of Captopril.
Bepridil DL-Methylephedrine may decrease the antihypertensive activities of Bepridil.
Cilazapril DL-Methylephedrine may decrease the antihypertensive activities of Cilazapril.
Saprisartan DL-Methylephedrine may decrease the antihypertensive activities of Saprisartan.
Spirapril DL-Methylephedrine may decrease the antihypertensive activities of Spirapril.
Mibefradil DL-Methylephedrine may decrease the antihypertensive activities of Mibefradil.
Debrisoquine DL-Methylephedrine may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan DL-Methylephedrine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan DL-Methylephedrine may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine DL-Methylephedrine may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine DL-Methylephedrine may decrease the antihypertensive activities of Nilvadipine.
Pinacidil DL-Methylephedrine may decrease the antihypertensive activities of Pinacidil.
Temocapril DL-Methylephedrine may decrease the antihypertensive activities of Temocapril.
Riociguat DL-Methylephedrine may decrease the antihypertensive activities of Riociguat.
Hexamethonium DL-Methylephedrine may decrease the antihypertensive activities of Hexamethonium.
Aliskiren DL-Methylephedrine may decrease the antihypertensive activities of Aliskiren.
Lacidipine DL-Methylephedrine may decrease the antihypertensive activities of Lacidipine.
Manidipine DL-Methylephedrine may decrease the antihypertensive activities of Manidipine.
Rauwolfia serpentina root DL-Methylephedrine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag DL-Methylephedrine may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 DL-Methylephedrine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril DL-Methylephedrine may decrease the antihypertensive activities of Imidapril.
BQ-123 DL-Methylephedrine may decrease the antihypertensive activities of BQ-123.
Tetrahydropalmatine DL-Methylephedrine may decrease the antihypertensive activities of Tetrahydropalmatine.
Dihydralazine DL-Methylephedrine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril DL-Methylephedrine may decrease the antihypertensive activities of Zofenopril.
Guanoxan DL-Methylephedrine may decrease the antihypertensive activities of Guanoxan.
Delapril DL-Methylephedrine may decrease the antihypertensive activities of Delapril.
Vincamine DL-Methylephedrine may decrease the antihypertensive activities of Vincamine.
Linsidomine DL-Methylephedrine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz DL-Methylephedrine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine DL-Methylephedrine may decrease the antihypertensive activities of Tolonidine.
Endralazine DL-Methylephedrine may decrease the antihypertensive activities of Endralazine.
Cadralazine DL-Methylephedrine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine DL-Methylephedrine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine DL-Methylephedrine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine DL-Methylephedrine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor DL-Methylephedrine may decrease the antihypertensive activities of Guanoclor.
Candesartan DL-Methylephedrine may decrease the antihypertensive activities of Candesartan.
Dexniguldipine DL-Methylephedrine may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone DL-Methylephedrine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat DL-Methylephedrine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat DL-Methylephedrine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat DL-Methylephedrine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat DL-Methylephedrine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat DL-Methylephedrine may decrease the antihypertensive activities of Quinaprilat.
Felodipine DL-Methylephedrine may decrease the antihypertensive activities of Felodipine.
Levamlodipine DL-Methylephedrine may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil DL-Methylephedrine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide DL-Methylephedrine may decrease the antihypertensive activities of Diazoxide.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with DL-Methylephedrine.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with DL-Methylephedrine.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with DL-Methylephedrine.
Bethanidine DL-Methylephedrine may decrease the antihypertensive activities of Bethanidine.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with DL-Methylephedrine.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with DL-Methylephedrine.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with DL-Methylephedrine.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with DL-Methylephedrine.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with DL-Methylephedrine.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with DL-Methylephedrine.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with DL-Methylephedrine.
Clonidine DL-Methylephedrine may decrease the antihypertensive activities of Clonidine.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with DL-Methylephedrine.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with DL-Methylephedrine.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with DL-Methylephedrine.
Guanabenz DL-Methylephedrine may decrease the antihypertensive activities of Guanabenz.
Epinephrine The risk or severity of hypertension can be increased when Epinephrine is combined with DL-Methylephedrine.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with DL-Methylephedrine.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with DL-Methylephedrine.
Tranylcypromine The risk or severity of hypertension can be increased when Tranylcypromine is combined with DL-Methylephedrine.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with DL-Methylephedrine.

Target Protein

Beta-1 adrenergic receptor ADRB1
Alpha-2A adrenergic receptor ADRA2A
Alpha adrenergic receptor ADRA1A
Beta adrenergic receptor ADRB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2327112
    Inoue T, Suzuki S: The metabolism of (+-)-methylephedrine in rat and man. Xenobiotica. 1990 Jan;20(1):99-106. doi: 10.3109/00498259009046816.
  • PMID: 17676524
    Dunnick JK, Kissling G, Gerken DK, Vallant MA, Nyska A: Cardiotoxicity of Ma Huang/caffeine or ephedrine/caffeine in a rodent model system. Toxicol Pathol. 2007 Aug;35(5):657-64. doi: 10.1080/01926230701459978.
Textbook
  • Steven B. Karch, Olaf Drummer (1996). Karch's Pathology of Drug Abuse, Third Edition. CRC Press.

Contoh Produk & Brand

Produk: 3 • International brands: 9
Produk
  • Facol Classic One
    Capsule • - • Oral • US • OTC
  • Pancold S
    Liquid • - • Oral • US • OTC
  • Whituben
    Capsule • - • Oral • US • OTC
International Brands
  • DL-Methylephedrine HCl — Fu Yuan
  • dl-Methylephedrine Hydrochloride 10% Maruishi — Maruishi Pharmaceuticals
  • dl-Methylephedrine Hydrochloride 10% Metal — Nakakita Yakuhin, Japan
  • dl-Methylephedrine Hydrochloride 10% Sankei — Sankei Seiyaku
  • dl-Methylephedrine Hydrochloride 10% Sanwa — Sanwa Kagaku
  • Methy F — Tanabe Mitsubishi Pharma
  • Methylephedrine 10% Fuso — Fuso Pharmaceutical
  • Methylhoedrin 10% — Mylan Seiyaku
  • Tabellae DL-Methyl — Ying Yuan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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