droxidopa Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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 synthetic precursor of norepinephrine that is used in the treatment of PARKINSONIAN DISORDERS and ORTHOSTATIC HYPOTENSION.
  • Molecular weight: 213.19
  • Formula: C9H11NO5
  • CLOGP: -2.48
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 5
  • TPSA: 124.01
  • ALOGS: -1.14
  • ROTB: 3

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1 g O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Feb. 18, 2014 FDA LUNDBECK NA LTD

FDA Adverse Event Reporting System (Female)

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 774.22 31.06 634 10309 339780 46335339
Blood pressure increased 452.88 31.06 311 10632 126355 46548764
Product dose omission issue 392.58 31.06 320 10623 168200 46506919
Blood pressure decreased 291.88 31.06 176 10767 56983 46618136
Blood pressure fluctuation 284.64 31.06 140 10803 30308 46644811
Loss of consciousness 241.80 31.06 201 10742 108037 46567082
Headache 239.17 31.06 411 10532 477941 46197178
Supine hypertension 190.65 31.06 30 10913 52 46675067
Fall 166.60 31.06 285 10658 328812 46346307
Hypotension 162.90 31.06 234 10709 232355 46442764
Hypertension 162.20 31.06 214 10729 196142 46478977
Presyncope 158.40 31.06 88 10855 24366 46650753
Feeling abnormal 143.35 31.06 161 10782 124899 46550220
Death 134.70 31.06 263 10680 335285 46339834
Orthostatic hypotension 133.62 31.06 79 10864 24579 46650540
Syncope 132.34 31.06 142 10801 104661 46570458
Blood pressure orthostatic decreased 123.94 31.06 20 10923 44 46675075
Palpitations 86.49 31.06 109 10834 95150 46579969
Intentional underdose 72.18 31.06 24 10919 1874 46673245
Drug dose titration not performed 71.55 31.06 17 10926 382 46674737
Drug titration error 69.43 31.06 18 10925 584 46674535
Malaise 68.54 31.06 201 10742 331031 46344088
Migraine 68.14 31.06 83 10860 69943 46605176
Drug ineffective 67.03 31.06 324 10619 677514 45997605
Fatigue 66.79 31.06 300 10643 608397 46066722
Nausea 64.69 31.06 324 10619 687130 45987989
Adverse drug reaction 62.83 31.06 64 10879 44298 46630821
Tremor 56.59 31.06 99 10844 115540 46559579
Incorrect dose administered 52.64 31.06 59 10884 45491 46629628
Hyperhidrosis 48.35 31.06 80 10863 89228 46585891
Heart rate increased 47.38 31.06 72 10871 74719 46600400
Dizziness postural 46.69 31.06 25 10918 6421 46668698
Asthenia 45.56 31.06 168 10775 310907 46364212
Multiple system atrophy 42.96 31.06 10 10933 205 46674914
Memory impairment 38.82 31.06 67 10876 77270 46597849
Condition aggravated 38.08 31.06 135 10808 244917 46430202
Therapeutic response decreased 36.93 31.06 48 10895 43097 46632022
Incorrect dosage administered 36.31 31.06 14 10929 1677 46673442
Balance disorder 35.17 31.06 58 10885 64463 46610656
Blood pressure abnormal 34.24 31.06 26 10917 12191 46662928
Acute kidney injury 31.92 31.06 8 10935 235847 46439272

FDA Adverse Event Reporting System (Male)

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 821.30 30.66 634 10633 194275 29746936
Blood pressure increased 630.10 30.66 370 10897 71558 29869653
Death 594.03 30.66 694 10573 356589 29584622
Blood pressure fluctuation 440.11 30.66 185 11082 17318 29923893
Product dose omission issue 426.68 30.66 318 10949 91313 29849898
Fall 406.96 30.66 415 10852 181457 29759754
Blood pressure decreased 328.71 30.66 210 11057 46865 29894346
Drug ineffective 233.08 30.66 438 10829 339949 29601262
Hypertension 231.29 30.66 255 11012 121099 29820112
Loss of consciousness 221.18 30.66 205 11062 79170 29862041
Supine hypertension 189.17 30.66 38 11229 219 29940992
Orthostatic hypotension 187.25 30.66 115 11152 23864 29917347
Hypotension 160.54 30.66 277 10990 200288 29740923
Headache 115.64 30.66 228 11039 182078 29759133
Syncope 108.41 30.66 146 11121 84757 29856454
Presyncope 107.73 30.66 70 11197 15986 29925225
Multiple system atrophy 102.16 30.66 22 11245 186 29941025
Balance disorder 98.94 30.66 93 11174 36400 29904811
Blood pressure orthostatic decreased 88.04 30.66 20 11247 221 29940990
Feeling abnormal 83.92 30.66 105 11162 56651 29884560
Hallucination 82.69 30.66 97 11170 48962 29892249
Condition aggravated 63.76 30.66 152 11115 137714 29803497
Urinary tract infection 62.86 30.66 105 11162 73554 29867657
Asthenia 59.17 30.66 200 11067 221090 29720121
Confusional state 58.43 30.66 145 11122 134689 29806522
Dizziness postural 57.59 30.66 32 11235 5498 29935713
Tremor 54.64 30.66 100 11167 75263 29865948
Labile blood pressure 52.49 30.66 16 11251 581 29940630
Blood pressure abnormal 48.11 30.66 31 11236 6968 29934243
Acute kidney injury 47.34 30.66 22 11245 273820 29667391
Incorrect dose administered 45.79 30.66 58 11209 31628 29909583
Dysstasia 45.34 30.66 35 11232 10470 29930741
Anaemia 43.94 30.66 12 11255 207980 29733231
Intentional underdose 43.87 30.66 15 11252 789 29940422
Incorrect dosage administered 43.55 30.66 15 11252 807 29940404
Adverse drug reaction 41.02 30.66 47 11220 23098 29918113
Head injury 39.74 30.66 40 11227 16980 29924231
Therapeutic response decreased 39.09 30.66 47 11220 24302 29916909
Fatigue 38.95 30.66 229 11038 320444 29620767
Gait disturbance 37.27 30.66 85 11182 74692 29866519
Off label use 35.94 30.66 25 11242 249265 29691946
Drug titration error 35.61 30.66 11 11256 418 29940793
Somnolence 33.66 30.66 96 11171 96667 29844544
Drug dose titration not performed 32.26 30.66 9 11258 238 29940973
Haemoglobin decreased 32.01 30.66 3 11264 114095 29827116
Product use complaint 31.66 30.66 13 11254 1139 29940072

Pharmacologic Action:

SourceCodeDescription
ATC C01CA27 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
FDA CS M0003647 Catecholamines
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
FDA PE N0000178478 Increased Blood Pressure
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:50266 prodrugs

Drug Use (View source of the data)

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

Acid dissociation constants calculated using MoKa v3.0.0

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG NORTHERA LUNDBECK NULL 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 NULL 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 NULL 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:

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

External reference:

IDSource
D01277 KEGG_DRUG
4033597 VANDF
C0000378 UMLSCUI
CHEBI:31524 CHEBI
CHEMBL2103827 ChEMBL_ID
DB06262 DRUGBANK_ID
D015103 MESH_DESCRIPTOR_UI
92974 PUBCHEM_CID
7391 IUPHAR_LIGAND_ID
6120 INN_ID
J7A92W69L7 UNII
1489913 RXNORM
213092 MMSL
27016 MMSL
343658 MMSL
d07567 MMSL
008194 NDDF
426390004 SNOMEDCT_US
426457000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 0054-0532 CAPSULE 100 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 0054-0533 CAPSULE 200 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 0054-0534 CAPSULE 300 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 0832-0720 CAPSULE 100 mg ORAL ANDA 29 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 0832-0721 CAPSULE 200 mg ORAL ANDA 29 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 0832-0722 CAPSULE 300 mg ORAL ANDA 29 sections
Droxidopa Human Prescription Drug Label 1 27241-199 CAPSULE 100 mg ORAL ANDA 27 sections
Droxidopa Human Prescription Drug Label 1 27241-200 CAPSULE 200 mg ORAL ANDA 27 sections
Droxidopa Human Prescription Drug Label 1 27241-201 CAPSULE 300 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 31722-010 CAPSULE 300 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 50228-429 CAPSULE 100 mg ORAL ANDA 29 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 50228-430 CAPSULE 200 mg ORAL ANDA 29 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 50228-431 CAPSULE 300 mg ORAL ANDA 29 sections
Droxidopa Human Prescription Drug Label 1 59651-375 CAPSULE 100 mg ORAL ANDA 27 sections
Droxidopa Human Prescription Drug Label 1 59651-376 CAPSULE 200 mg ORAL ANDA 27 sections
Droxidopa Human Prescription Drug Label 1 59651-377 CAPSULE 300 mg ORAL ANDA 27 sections
droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 63304-086 CAPSULE 100 ug ORAL ANDA 27 sections
droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 63304-104 CAPSULE 200 ug ORAL ANDA 27 sections
droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 63304-112 CAPSULE 300 ug ORAL ANDA 27 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-820 CAPSULE 100 mg ORAL NDA 28 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-821 CAPSULE 200 mg ORAL NDA 28 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-822 CAPSULE 300 mg ORAL NDA 28 sections
Droxidopa Human Prescription Drug Label 1 67877-704 CAPSULE 100 mg ORAL ANDA 28 sections
Droxidopa Human Prescription Drug Label 1 67877-705 CAPSULE 200 mg ORAL ANDA 28 sections
Droxidopa Human Prescription Drug Label 1 67877-706 CAPSULE 300 mg ORAL ANDA 28 sections
Droxidopa Human Prescription Drug Label 1 69539-088 CAPSULE 200 mg ORAL ANDA 24 sections
Droxidopa Human Prescription Drug Label 1 69539-089 CAPSULE 300 mg ORAL ANDA 24 sections
Droxidopa Human Prescription Drug Label 1 69539-146 CAPSULE 100 mg ORAL ANDA 24 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 70710-1389 CAPSULE 100 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 70710-1390 CAPSULE 200 mg ORAL ANDA 27 sections