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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB06262
rdf:type
n3:Drug
n3: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.
n3:dosage
n4:271B4B48-363D-11E5-9242-09173F13E4C5 n4:271B4B46-363D-11E5-9242-09173F13E4C5 n4:271B4B47-363D-11E5-9242-09173F13E4C5
n3: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
n3:group
investigational approved
n3:halfLife
2-3 hours.
n3: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.
owl:sameAs
n11:DB06262 n14:DB06262
dcterms:title
Droxidopa
adms:identifier
n9:PA164748386 n12:Droxidopa n13:76320-100-90 n15:391994 n16:443940 n17:99443239 n18:DB06262 n19:D01277
n3: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.
n3:routeOfElimination
Droxidopa is mainly excreted in the urine, with the main metabolite being 3-O-methyldihydroxyphenylserine.
n3:synonym
L-threo-dihydroxyphenylserine Dops L-DOPS L-Dihydroxyphenylserine
n3: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.
n6:hasConcept
n7:M0023229
n3:IUPAC-Name
n5:271B4B4D-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B4B53-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B4B52-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B4B4F-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B4B50-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B4B51-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4B4B-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B4B49-363D-11E5-9242-09173F13E4C5 n5:271B4B4C-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B4B4A-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n5:271B4B59-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B4B5A-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B4B54-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B4B55-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B4B57-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B4B56-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B4B58-363D-11E5-9242-09173F13E4C5
n3:absorption
Oral bioavailability is 90%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
23651-95-8
n3:category
n3:Bioavailability
n5:271B4B5F-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B4B61-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B4B62-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B4B5E-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B4B5D-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B4B60-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B4B4E-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B4B5B-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B4B5C-363D-11E5-9242-09173F13E4C5