droxidopa indications/contra

Stem definitionDrug idCAS RN
dopamine receptor agonists, dopamine derivatives, used as antiparkinsonism/prolactin inhibitors 971 23651-95-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • northera
  • L-DOPS
  • droxidopa
  • threo-Dopaserine
  • L-threo-3,4-Dihydroxyphenylserine
A precursor of noradrenaline that is used in the treatment of parkinsonism. The racemic 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. Administration of DL-threo-3,4-dihydroxyphenylserine has been claimed to result in an improvement in this phenomenon but controlled studies have failed to demonstrate improvement. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)
  • Molecular weight: 213.19
  • Formula: C9H11NO5
  • CLOGP: -2.48
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 5
  • TPSA: 124.01
  • ALOGS: -1.14
  • ROTB: 3

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 18, 2014 FDA LUNDBECK NA LTD

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dizziness 2092.54 59.07 696 3483 75816 3305864
Blood pressure increased 1532.14 59.07 416 3763 21814 3359866
Fall 891.55 59.07 350 3829 58533 3323147
Blood pressure fluctuation 872.53 59.07 172 4007 2034 3379646
Drug ineffective 872.41 59.07 420 3759 115670 3266010
Headache 775.47 59.07 361 3818 91619 3290061
Hypertension 743.76 59.07 274 3905 38192 3343488
Death 678.64 59.07 389 3790 151935 3229745
Loss of consciousness 677.16 59.07 236 3943 27911 3353769
Fatigue 602.57 59.07 320 3859 106920 3274760
Drug dose omission 580.60 59.07 229 3950 38203 3343477
Hypotension 564.18 59.07 241 3938 49273 3332407
Blood pressure decreased 550.28 59.07 170 4009 13666 3368014
Nausea 439.13 59.07 279 3900 129366 3252314
Syncope 411.59 59.07 160 4019 25473 3356207
Asthenia 409.51 59.07 211 3968 65454 3316226
Presyncope 347.96 59.07 96 4083 5135 3376545
Feeling abnormal 328.71 59.07 139 4040 27386 3354294
Orthostatic hypotension 287.37 59.07 82 4097 4954 3376726
Confusional state 282.74 59.07 138 4041 37860 3343820
Condition aggravated 269.63 59.07 135 4044 39098 3342582
Balance disorder 243.73 59.07 90 4089 12349 3369331
Malaise 240.78 59.07 149 4030 65028 3316652
Palpitations 219.56 59.07 94 4085 18989 3362691
Tremor 208.38 59.07 102 4077 28042 3353638
Somnolence 192.50 59.07 101 4078 32103 3349577
Drug intolerance 168.95 59.07 68 4111 11730 3369950
Urinary tract infection 164.00 59.07 90 4089 31238 3350442
Hyperhidrosis 152.30 59.07 78 4101 23532 3358148
Chest pain 150.61 59.07 93 4086 40182 3341498

Pharmacologic Action:

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SourceCodeDescription
ATC C01CA27 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:50514 vasoconstrictor agent
CHEBI has role CHEBI:35674 antihypertensive agent
FDA Chemical/Ingredient N0000007715 Catecholamines
FDA PE N0000178478 Increased Blood Pressure
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Orthostatic hypotension indication 28651003
Parkinson's disease indication 49049000 DOID:14330

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.23 acidic
pKa2 9.52 acidic
pKa3 11.41 acidic
pKa4 12.37 acidic
pKa5 8.22 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG NORTHERA LUNDBECK NA LTD N203202 Feb. 18, 2014 RX CAPSULE ORAL Feb. 18, 2019 NEW CHEMICAL ENTITY
200MG NORTHERA LUNDBECK NA LTD N203202 Feb. 18, 2014 RX CAPSULE ORAL Feb. 18, 2019 NEW CHEMICAL ENTITY
300MG NORTHERA LUNDBECK NA LTD N203202 Feb. 18, 2014 RX CAPSULE ORAL Feb. 18, 2019 NEW CHEMICAL ENTITY
100MG NORTHERA LUNDBECK NA LTD N203202 Feb. 18, 2014 RX CAPSULE ORAL Feb. 18, 2021 TREATMENT OF NEUROGENIC SYMPTOMATIC ORTHOSTATIC HYPOTENSION IN PATIENTS WITH PRIMARY AUTONOMIC FAILURE, DOPAMINE-BETA-HYDROXYLASE DEFICIENCY, AND NONDIABETIC AUTONOMIC NEUROPATHY
200MG NORTHERA LUNDBECK NA LTD N203202 Feb. 18, 2014 RX CAPSULE ORAL Feb. 18, 2021 TREATMENT OF NEUROGENIC SYMPTOMATIC ORTHOSTATIC HYPOTENSION IN PATIENTS WITH PRIMARY AUTONOMIC FAILURE, DOPAMINE-BETA-HYDROXYLASE DEFICIENCY, AND NONDIABETIC AUTONOMIC NEUROPATHY
300MG NORTHERA LUNDBECK NA LTD N203202 Feb. 18, 2014 RX CAPSULE ORAL Feb. 18, 2021 TREATMENT OF NEUROGENIC SYMPTOMATIC ORTHOSTATIC HYPOTENSION IN PATIENTS WITH PRIMARY AUTONOMIC FAILURE, DOPAMINE-BETA-HYDROXYLASE DEFICIENCY, AND NONDIABETIC AUTONOMIC NEUROPATHY

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Adrenergic receptor GPCR AGONIST CHEMBL CHEMBL

External reference:

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IDSource
C3817378 UMLSCUI
7391 IUPHAR_LIGAND_ID
D01277 KEGG_DRUG
92974 PUBCHEM_CID
426390004 SNOMEDCT_US
426457000 SNOMEDCT_US
N0000170222 NDFRT
1489913 RXNORM
008194 NDDF
27016 MMSL
d07567 MMSL
4033597 VANDF
N0000190929 NDFRT
CHEBI:31524 CHEBI
DB06262 DRUGBANK_ID
CHEMBL2103827 ChEMBL_ID
J7A92W69L7 UNII
6120 INN_ID
D015103 MESH_DESCRIPTOR_UI
DB00368 DRUGBANK_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-820 CAPSULE 100 mg ORAL NDA 18 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-821 CAPSULE 200 mg ORAL NDA 18 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-822 CAPSULE 300 mg ORAL NDA 18 sections