droxidopa 🐶 Veterinary Use | 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 749.64 33.47 610 10493 345759 50248262
Blood pressure increased 464.62 33.47 314 10789 132818 50461203
Product dose omission issue 409.91 33.47 331 10772 183507 50410514
Blood pressure decreased 311.64 33.47 178 10925 55731 50538290
Loss of consciousness 275.42 33.47 208 10895 104145 50489876
Blood pressure fluctuation 274.73 33.47 141 10962 35682 50558339
Headache 244.46 33.47 413 10690 506122 50087899
Supine hypertension 198.24 33.47 30 11073 38 50593983
Death 190.07 33.47 290 10813 325089 50268932
Fall 186.53 33.47 292 10811 334640 50259381
Hypertension 168.82 33.47 219 10884 210984 50383037
Presyncope 167.54 33.47 89 11014 24109 50569912
Hypotension 160.58 33.47 226 10877 235243 50358778
Feeling abnormal 153.45 33.47 162 10941 125330 50468691
Syncope 136.72 33.47 139 10964 102863 50491158
Blood pressure orthostatic decreased 122.91 33.47 20 11083 52 50593969
Palpitations 98.02 33.47 112 10991 94394 50499627
Malaise 79.35 33.47 205 10898 335327 50258694
Intentional underdose 77.45 33.47 24 11079 1598 50592423
Nausea 72.98 33.47 326 10777 705072 49888949
Orthostatic hypotension 71.45 33.47 56 11047 29425 50564596
Migraine 70.98 33.47 85 11018 75195 50518826
Drug titration error 70.38 33.47 18 11085 592 50593429
Drug dose titration not performed 70.12 33.47 17 11086 447 50593574
Tremor 64.65 33.47 101 11002 114802 50479219
Adverse drug reaction 54.76 33.47 64 11039 55158 50538863
Incorrect dose administered 54.62 33.47 60 11043 48354 50545667
Fatigue 53.83 33.47 300 10803 707301 49886720
Hyperhidrosis 52.22 33.47 80 11023 89346 50504675
Asthenia 51.30 33.47 170 10933 318872 50275149
Drug ineffective 50.02 33.47 328 10775 819005 49775016
Dizziness postural 49.38 33.47 25 11078 6120 50587901
Heart rate increased 49.23 33.47 72 11031 77178 50516843
Multiple system atrophy 49.07 33.47 11 11092 203 50593818
Memory impairment 40.81 33.47 67 11036 79293 50514728
Joint swelling 37.04 33.47 5 11098 245281 50348740
Incorrect dosage administered 37.02 33.47 14 11089 1700 50592321
Hallucination 36.47 33.47 48 11055 46609 50547412
Arthralgia 36.45 33.47 26 11077 438676 50155345
Therapeutic response decreased 36.01 33.47 48 11055 47183 50546838
Balance disorder 35.49 33.47 59 11044 70531 50523490

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 772.37 31.41 615 10962 189069 29373881
Death 692.98 31.41 750 10827 341334 29221616
Blood pressure increased 610.06 31.41 371 11206 73432 29489518
Fall 437.06 31.41 434 11143 176744 29386206
Blood pressure fluctuation 416.58 31.41 187 11390 19707 29543243
Product dose omission issue 411.84 31.41 323 11254 96060 29466890
Blood pressure decreased 340.13 31.41 215 11362 45262 29517688
Hypertension 238.22 31.41 259 11318 116355 29446595
Loss of consciousness 234.26 31.41 209 11368 73847 29489103
Drug ineffective 213.69 31.41 449 11128 362721 29200229
Supine hypertension 180.31 31.41 38 11539 274 29562676
Hypotension 165.39 31.41 282 11295 194072 29368878
Headache 121.61 31.41 232 11345 173775 29389175
Syncope 114.89 31.41 150 11427 81221 29481729
Orthostatic hypotension 114.06 31.41 84 11493 22545 29540405
Multiple system atrophy 109.72 31.41 23 11554 161 29562789
Presyncope 105.05 31.41 70 11507 16019 29546931
Balance disorder 96.48 31.41 93 11484 36077 29526873
Hallucination 92.08 31.41 100 11477 44612 29518338
Blood pressure orthostatic decreased 90.47 31.41 20 11557 185 29562765
Feeling abnormal 87.28 31.41 107 11470 54338 29508612
Urinary tract infection 67.86 31.41 110 11467 72244 29490706
Dizziness postural 60.03 31.41 33 11544 5334 29557616
Confusional state 58.60 31.41 144 11433 127733 29435217
Condition aggravated 58.02 31.41 156 11421 146139 29416811
Blood pressure abnormal 57.93 31.41 35 11542 6755 29556195
Asthenia 56.86 31.41 199 11378 215051 29347899
Tremor 54.79 31.41 101 11476 73437 29489513
Labile blood pressure 52.19 31.41 16 11561 569 29562381
Off label use 51.34 31.41 27 11550 300773 29262177
Intentional underdose 47.04 31.41 15 11562 608 29562342
Dysstasia 46.36 31.41 36 11541 10438 29552512
Incorrect dosage administered 45.24 31.41 16 11561 894 29562056
Incorrect dose administered 43.65 31.41 59 11518 32925 29530025
Acute kidney injury 43.51 31.41 25 11552 265242 29297708
Adverse drug reaction 43.03 31.41 50 11527 23970 29538980
Anaemia 42.45 31.41 13 11564 200938 29362012
Head injury 42.17 31.41 41 11536 16040 29546910
Product use complaint 40.93 31.41 15 11562 929 29562021
Gait disturbance 40.56 31.41 89 11488 73260 29489690
Thrombocytopenia 38.56 31.41 4 11573 134819 29428131
Fatigue 37.83 31.41 232 11345 316589 29246361
Therapeutic response decreased 37.03 31.41 47 11530 24664 29538286
Drug titration error 34.98 31.41 11 11566 426 29562524
Somnolence 34.01 31.41 97 11480 93858 29469092

FDA Adverse Event Reporting System (Geriatric)

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
Death 956.99 28.56 855 15267 481850 64000760
Dizziness 879.40 28.56 776 15346 429387 64053223
Blood pressure increased 812.29 28.56 515 15607 172037 64310573
Product dose omission issue 659.17 28.56 474 15648 194273 64288337
Blood pressure decreased 472.07 28.56 284 15838 85915 64396695
Blood pressure fluctuation 457.46 28.56 234 15888 51637 64430973
Fall 453.66 28.56 537 15585 416289 64066321
Loss of consciousness 387.65 28.56 310 15812 148055 64334555
Supine hypertension 272.37 28.56 51 16071 310 64482300
Hypertension 234.04 28.56 305 15817 258956 64223654
Hypotension 224.30 28.56 366 15756 380608 64102002
Headache 208.25 28.56 427 15695 529040 63953570
Feeling abnormal 174.50 28.56 190 15932 133412 64349198
Syncope 157.00 28.56 195 15927 157440 64325170
Presyncope 152.40 28.56 100 16022 34989 64447621
Blood pressure orthostatic decreased 137.84 28.56 28 16094 273 64482337
Multiple system atrophy 125.17 28.56 27 16095 360 64482250
Orthostatic hypotension 120.22 28.56 97 16025 46641 64435969
Hallucination 97.48 28.56 105 16017 72683 64409927
Intentional underdose 80.47 28.56 27 16095 2031 64480579
Balance disorder 78.91 28.56 101 16021 83825 64398785
Incorrect dose administered 76.72 28.56 85 16037 60680 64421930
Tremor 75.61 28.56 134 15988 148096 64334514
Drug dose titration not performed 75.45 28.56 20 16102 663 64481947
Dizziness postural 74.40 28.56 40 16082 9712 64472898
Asthenia 72.40 28.56 253 15869 427791 64054819
Blood pressure abnormal 72.22 28.56 45 16077 14390 64468220
Head injury 71.66 28.56 62 16060 32780 64449830
Drug ineffective 71.50 28.56 404 15718 839843 63642767
Off label use 66.43 28.56 38 16084 632768 63849842
Confusional state 61.26 28.56 173 15949 260971 64221639
Drug titration error 60.34 28.56 18 16104 922 64481688
Fatigue 53.33 28.56 344 15778 748386 63734224
Dysstasia 53.03 28.56 45 16077 23170 64459440
Therapeutic response decreased 50.92 28.56 64 16058 52124 64430486
Adverse drug reaction 49.61 28.56 59 16063 45405 64437205
Condition aggravated 47.17 28.56 201 15921 372225 64110385
Arthralgia 47.14 28.56 26 16096 442234 64040376
Seizure like phenomena 46.62 28.56 17 16105 1635 64480975
Labile blood pressure 46.33 28.56 18 16104 2062 64480548
Malaise 45.00 28.56 207 15915 396040 64086570
Acute kidney injury 44.25 28.56 29 16093 449211 64033399
Gait disturbance 44.24 28.56 118 16004 172037 64310573
Anaemia 43.74 28.56 20 16102 378660 64103950
Migraine 41.81 28.56 64 16058 62613 64419997
Palpitations 41.53 28.56 85 16037 104403 64378207
Memory impairment 39.25 28.56 74 16048 85608 64397002
Urinary tract infection 38.24 28.56 136 15986 231460 64251150
Thrombocytopenia 36.62 28.56 6 16116 223795 64258815
Somnolence 36.58 28.56 123 15999 203522 64279088
Hyperhidrosis 35.55 28.56 89 16033 124831 64357779
Vision blurred 35.33 28.56 73 16049 90243 64392367
Nausea 35.09 28.56 324 15798 785476 63697134
Incorrect dosage administered 31.72 28.56 14 16108 2212 64480398
Drug hypersensitivity 31.70 28.56 10 16112 237805 64244805
Pain 31.02 28.56 57 16065 553454 63929156
Heart rate increased 30.95 28.56 73 16049 98602 64384008
Hip fracture 30.94 28.56 36 16086 27063 64455547
Joint swelling 28.80 28.56 9 16113 215373 64267237

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CA27 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
FDA CS M0003647 Catecholamines
FDA EPC N0000175570 Catecholamine
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013566 Sympathomimetics
MeSH PA D014662 Vasoconstrictor Agents
FDA PE N0000178478 Increased Blood Pressure
CHEBI has role CHEBI:25512 neurotransmitters
CHEBI has role CHEBI:35524 sympathomimetic
CHEBI has role CHEBI:35569 alpha-adrenergic agonists
CHEBI has role CHEBI:75771 Mus musculus metabolites
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:50266 Prodrugs
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)

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Adrenergic receptor GPCR AGONIST CHEMBL CHEMBL
Muscarinic acetylcholine receptor M1 GPCR ANTAGONIST Ki 7.10 IUPHAR

External reference:

IDSource
D01277 KEGG_DRUG
4019859 VANDF
4033597 VANDF
C0000378 UMLSCUI
CHEBI:31524 CHEBI
CHEBI:33569 CHEBI
LT4 PDB_CHEM_ID
CHEMBL2103827 ChEMBL_ID
DB06262 DRUGBANK_ID
D015103 MESH_DESCRIPTOR_UI
92974 PUBCHEM_CID
6120 INN_ID
7391 IUPHAR_LIGAND_ID
J7A92W69L7 UNII
DB00368 DRUGBANK_ID
1489913 RXNORM
213092 MMSL
27016 MMSL
2706 MMSL
343658 MMSL
d00323 MMSL
d07567 MMSL
004718 NDDF
008194 NDDF
111130009 SNOMEDCT_US
426390004 SNOMEDCT_US
426457000 SNOMEDCT_US
45555007 SNOMEDCT_US
439260 PUBCHEM_CID
C0028351 UMLSCUI
D009638 MESH_DESCRIPTOR_UI
33 INN_ID

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 27808-199 CAPSULE 100 mg ORAL ANDA 28 sections
droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 27808-200 CAPSULE 200 mg ORAL ANDA 28 sections
droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 27808-201 CAPSULE 300 mg ORAL ANDA 28 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 31722-010 CAPSULE 300 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 31722-014 CAPSULE 100 mg ORAL ANDA 27 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 31722-015 CAPSULE 200 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 67386-820 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 67386-821 CAPSULE 200 mg ORAL NDA 28 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-822 CAPSULE 300 mg ORAL NDA 28 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-822 CAPSULE 300 mg ORAL NDA 28 sections