Peringatan Keamanan

Droxidopa has minimal toxic effects and an acute, oral LD50 of more than 5 g/kg in mice, rats, dogs, and monkeys. Side effects occur in in 0.78% of patients and include nausea, headache, increased blood pressure, hallucination, and anorexia.

Droxidopa

DB06262

small molecule approved investigational

Deskripsi

Droxidopa is a precursor of noradrenaline that is used in the treatment of Parkinsonism. It is approved for use in Japan and is currently in trials in the U.S. The racaemic form (dl-threo-3,4-dihydroxyphenylserine) has also been used, and has been investigated in the treatment of orthostatic hypotension. There is a deficit of noradrenaline as well as of dopamine in Parkinson's disease and it has been proposed that this underlies the sudden transient freezing seen usually in advanced disease.

Though L-DOPS has been used in Japan and Southeast Asia already for some time, it is also currently in clinical trials at the phase III point in the United States (U.S.), Canada, Australia, and throughout Europe. Provided L-DOPS successfully completes clinical trials, it could be approved for the treatment of neurogenic orthostatic hypotension (NOH) as early as 2011. Additionally, phase II clinical trials for intradialytic hypotension are also underway. Chelsea Therapeutics obtained orphan drug status (ODS) for L-DOPS in the U.S. for NOH, and that of which associated with Parkinson's disease , pure autonomic failure, and multiple system atrophy, and is the pharmaceutical company developing it in that country.

Struktur Molekul 2D

Berat 213.189
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2-3 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Oral bioavailability is 90%.

Metabolisme

Droxidopa is metabolized by aromatic L-amino acid decarboxylase.

Rute Eliminasi

Droxidopa is mainly excreted in the urine, with the main metabolite being 3-O-methyldihydroxyphenylserine.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Take consistently with regard to food.

Interaksi Obat

1344 Data
Valsartan Droxidopa may decrease the antihypertensive activities of Valsartan.
Ramipril Droxidopa may decrease the antihypertensive activities of Ramipril.
Remikiren Droxidopa may decrease the antihypertensive activities of Remikiren.
Olmesartan Droxidopa may decrease the antihypertensive activities of Olmesartan.
Diltiazem Droxidopa may decrease the antihypertensive activities of Diltiazem.
Minoxidil Droxidopa may decrease the antihypertensive activities of Minoxidil.
Treprostinil Droxidopa may decrease the antihypertensive activities of Treprostinil.
Amlodipine Droxidopa may decrease the antihypertensive activities of Amlodipine.
Nimodipine Droxidopa may decrease the antihypertensive activities of Nimodipine.
Trandolapril Droxidopa may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Droxidopa may decrease the antihypertensive activities of Lercanidipine.
Benazepril Droxidopa may decrease the antihypertensive activities of Benazepril.
Bosentan Droxidopa may decrease the antihypertensive activities of Bosentan.
Enalapril Droxidopa may decrease the antihypertensive activities of Enalapril.
Candoxatril Droxidopa may decrease the antihypertensive activities of Candoxatril.
Losartan Droxidopa may decrease the antihypertensive activities of Losartan.
Moexipril Droxidopa may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Droxidopa may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Droxidopa may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Droxidopa may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Droxidopa may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Droxidopa may decrease the antihypertensive activities of Eprosartan.
Quinapril Droxidopa may decrease the antihypertensive activities of Quinapril.
Telmisartan Droxidopa may decrease the antihypertensive activities of Telmisartan.
Irbesartan Droxidopa may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Droxidopa may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Droxidopa may decrease the antihypertensive activities of Deserpidine.
Pentolinium Droxidopa may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Droxidopa may decrease the antihypertensive activities of Trimethaphan.
Captopril Droxidopa may decrease the antihypertensive activities of Captopril.
Bepridil Droxidopa may decrease the antihypertensive activities of Bepridil.
Cilazapril Droxidopa may decrease the antihypertensive activities of Cilazapril.
Saprisartan Droxidopa may decrease the antihypertensive activities of Saprisartan.
Spirapril Droxidopa may decrease the antihypertensive activities of Spirapril.
Mibefradil Droxidopa may decrease the antihypertensive activities of Mibefradil.
Debrisoquine Droxidopa may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Droxidopa may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Droxidopa may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Droxidopa may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Droxidopa may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Droxidopa may decrease the antihypertensive activities of Pinacidil.
Temocapril Droxidopa may decrease the antihypertensive activities of Temocapril.
Riociguat Droxidopa may decrease the antihypertensive activities of Riociguat.
Hexamethonium Droxidopa may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Droxidopa may decrease the antihypertensive activities of Aliskiren.
Lacidipine Droxidopa may decrease the antihypertensive activities of Lacidipine.
Manidipine Droxidopa may decrease the antihypertensive activities of Manidipine.
Rauwolfia serpentina root Droxidopa may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag Droxidopa may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Droxidopa may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Droxidopa may decrease the antihypertensive activities of Imidapril.
BQ-123 Droxidopa may decrease the antihypertensive activities of BQ-123.
Tetrahydropalmatine Droxidopa may decrease the antihypertensive activities of Tetrahydropalmatine.
Dihydralazine Droxidopa may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Droxidopa may decrease the antihypertensive activities of Zofenopril.
Guanoxan Droxidopa may decrease the antihypertensive activities of Guanoxan.
Delapril Droxidopa may decrease the antihypertensive activities of Delapril.
Vincamine Droxidopa may decrease the antihypertensive activities of Vincamine.
Linsidomine Droxidopa may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Droxidopa may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Droxidopa may decrease the antihypertensive activities of Tolonidine.
Endralazine Droxidopa may decrease the antihypertensive activities of Endralazine.
Cadralazine Droxidopa may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Droxidopa may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Droxidopa may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Droxidopa may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Droxidopa may decrease the antihypertensive activities of Guanoclor.
Candesartan Droxidopa may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Droxidopa may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Droxidopa may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Droxidopa may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Droxidopa may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Droxidopa may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Droxidopa may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Droxidopa may decrease the antihypertensive activities of Quinaprilat.
Felodipine Droxidopa may decrease the antihypertensive activities of Felodipine.
Levamlodipine Droxidopa may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil Droxidopa may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Droxidopa may decrease the antihypertensive activities of Diazoxide.
Carbidopa The serum concentration of norepinephrine, an active metabolite of Droxidopa, can be decreased when used in combination with Carbidopa.
Benzylpenicilloyl polylysine Droxidopa may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Bethanidine Droxidopa may decrease the antihypertensive activities of Bethanidine.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Droxidopa.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Droxidopa.
Clonidine Droxidopa may decrease the antihypertensive activities of Clonidine.
Guanabenz Droxidopa may decrease the antihypertensive activities of Guanabenz.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Droxidopa.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Droxidopa.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Droxidopa.
Propofol The risk or severity of hypertension can be increased when Propofol is combined with Droxidopa.
Omapatrilat Droxidopa may decrease the antihypertensive activities of Omapatrilat.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Droxidopa.
Methoxyflurane The risk or severity of hypertension can be increased when Methoxyflurane is combined with Droxidopa.
Halothane The risk or severity of hypertension can be increased when Halothane is combined with Droxidopa.
Rescinnamine Droxidopa may decrease the antihypertensive activities of Rescinnamine.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Droxidopa.
Sevoflurane The risk or severity of hypertension can be increased when Sevoflurane is combined with Droxidopa.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Droxidopa.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Droxidopa.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Droxidopa.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Beta-3 adrenergic receptor ADRB3
Phenylalanine-4-hydroxylase PAH

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18368303
    Kaufmann H: L-dihydroxyphenylserine (Droxidopa): a new therapy for neurogenic orthostatic hypotension: the US experience. Clin Auton Res. 2008 Mar;18 Suppl 1:19-24. doi: 10.1007/s10286-007-1002-2. Epub 2008 Mar 27.
  • PMID: 18051291
    Balk SH, Yoshioka H, Yukawa H, Harayama S: Synthesis of L-threo-3,4-dihydroxyphenylserine (L-threo-DOPS) with thermostabilized low-specific L-threonine aldolase from Streptomyces coelicolor A3(2). J Microbiol Biotechnol. 2007 May;17(5):721-7.
  • PMID: 18368304
    Mathias CJ: L-dihydroxyphenylserine (Droxidopa) in the treatment of orthostatic hypotension: the European experience. Clin Auton Res. 2008 Mar;18 Suppl 1:25-9. doi: 10.1007/s10286-007-1005-z. Epub 2008 Mar 27.
  • PMID: 17214596
    Goldstein DS: L-Dihydroxyphenylserine (L-DOPS): a norepinephrine prodrug. Cardiovasc Drug Rev. 2006 Fall-Winter;24(3-4):189-203.
  • PMID: 15666063
    Goldstein DS, Holmes C, Kaufmann H, Freeman R: Clinical pharmacokinetics of the norepinephrine precursor L-threo-DOPS in primary chronic autonomic failure. Clin Auton Res. 2004 Dec;14(6):363-8.

Contoh Produk & Brand

Produk: 63 • International brands: 1
Produk
  • Droxidopa
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 300 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 300 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Droxidopa
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 63 produk.
International Brands
  • Dops

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