About: Droxidopa     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • 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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # 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. Epub 2008 Mar 27. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18368303 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18051291 # Mathias CJ: L-dihydroxyphenylserine (Droxidopa) in the treatment of orthostatic hypotension: the European experience. Clin Auton Res. 2008 Mar;18 Suppl 1:25-9. Epub 2008 Mar 27. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18368304 # Goldstein DS: L-Dihydroxyphenylserine (L-DOPS): a norepinephrine prodrug. Cardiovasc Drug Rev. 2006 Fall-Winter;24(3-4):189-203. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17214596 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15666063 # Goldstein DS: L-Dihydroxyphenylserine (L-DOPS): a norepinephrine prodrug. Cardiovasc Drug Rev. 2006 Fall-Winter;24(3-4):189-203. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17214596 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 2-3 hours. (en)
http://linked.open...ugbank/indication
  • For treatment of neurogenic orthostatic hypotension (NOH) associated with various disorders including Multiple System Atrophy, Familial Amyloid Polyneuropathy, hemodialysis induced hypotension and Parkinson's Disease. Also investigated for use/treatment in neurologic disorders, nephropathy, blood (blood forming organ disorders, unspecified), and dizzy/fainting spells. (en)
sameAs
Title
  • Droxidopa (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Droxidopa crosses the blood-brain barrier where it is converted to norepinephrine via decarboxylation by L-aromatic-amino-acid decarboxylase. Increased levels of norepinephrine in the central nervous system (CNS) may be beneficial to patients in a wide range of indications. Norephinephrine acts at alpha-adrenergic receptors as a vasoconstrictor and at beta-adrenergic receptors as a heart stimulator and artery dilator. (en)
http://linked.open...outeOfElimination
  • Droxidopa is mainly excreted in the urine, with the main metabolite being 3-O-methyldihydroxyphenylserine. (en)
http://linked.open.../drugbank/synonym
  • Dops (en)
  • L-DOPS (en)
  • L-Dihydroxyphenylserine (en)
  • L-threo-dihydroxyphenylserine (en)
http://linked.open...drugbank/toxicity
  • 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. (en)
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http://linked.open...ugbank/absorption
  • Oral bioavailability is 90%. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 23651-95-8 (en)
http://linked.open...drugbank/category
  • (en)
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