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
S (Water solubility) 15.30 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

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 748.57 32.19 611 10674 429314 63048423
Blood pressure increased 473.37 32.19 316 10969 161746 63315991
Product dose omission issue 406.83 32.19 334 10951 233979 63243758
Blood pressure decreased 327.03 32.19 180 11105 64842 63412895
Loss of consciousness 303.16 32.19 213 11072 117908 63359829
Blood pressure fluctuation 271.40 32.19 142 11143 46175 63431562
Headache 244.52 32.19 416 10869 632825 62844912
Death 220.76 32.19 300 10985 374081 63103656
Fall 205.41 32.19 297 10988 392037 63085700
Supine hypertension 204.56 32.19 30 11255 38 63477699
Hypotension 176.57 32.19 229 11056 272375 63205362
Presyncope 173.60 32.19 89 11196 27696 63450041
Feeling abnormal 161.08 32.19 163 11122 148229 63329508
Hypertension 159.97 32.19 221 11064 279082 63198655
Syncope 148.00 32.19 140 11145 117245 63360492
Blood pressure orthostatic decreased 122.66 32.19 20 11265 70 63477667
Palpitations 101.12 32.19 112 11173 112658 63365079
Malaise 79.80 32.19 206 11079 415748 63061989
Intentional underdose 78.91 32.19 24 11261 1858 63475879
Orthostatic hypotension 78.35 32.19 59 11226 36101 63441636
Nausea 77.03 32.19 327 10958 854144 62623593
Tremor 72.97 32.19 103 11182 132136 63345601
Drug dose titration not performed 70.96 32.19 17 11268 528 63477209
Drug titration error 68.79 32.19 18 11267 805 63476932
Migraine 65.33 32.19 86 11199 103260 63374477
Incorrect dose administered 57.94 32.19 62 11223 59906 63417831
Asthenia 55.81 32.19 172 11113 383432 63094305
Hyperhidrosis 55.08 32.19 81 11204 107755 63369982
Fatigue 52.73 32.19 302 10983 887726 62590011
Multiple system atrophy 51.38 32.19 11 11274 203 63477534
Dizziness postural 50.04 32.19 25 11260 7351 63470386
Heart rate increased 49.88 32.19 72 11213 94166 63383571
Drug ineffective 48.15 32.19 333 10952 1044432 62433305
Adverse drug reaction 46.78 32.19 64 11221 79650 63398087
Joint swelling 41.09 32.19 5 11280 327661 63150076
Arthralgia 40.17 32.19 26 11259 569684 62908053
Hallucination 38.35 32.19 48 11237 54769 63422968
Memory impairment 37.75 32.19 67 11218 104191 63373546
Incorrect dosage administered 37.37 32.19 14 11271 2049 63475688
Balance disorder 36.87 32.19 59 11226 84363 63393374
Hip fracture 34.86 32.19 34 11251 29440 63448297
Pain 34.52 32.19 49 11236 740579 62737158
Therapeutic response decreased 34.00 32.19 48 11237 61477 63416260
Blood pressure abnormal 33.35 32.19 25 11260 15173 63462564
Somnolence 32.56 32.19 87 11198 178598 63299139

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 780.48 31.63 617 11174 217904 34727236
Death 737.64 31.63 776 11015 397273 34547867
Blood pressure increased 600.30 31.63 371 11420 87731 34857409
Fall 455.08 31.63 441 11350 202444 34742696
Blood pressure fluctuation 406.76 31.63 189 11602 25060 34920080
Product dose omission issue 396.65 31.63 325 11466 119386 34825754
Blood pressure decreased 349.96 31.63 217 11574 51298 34893842
Loss of consciousness 247.38 31.63 212 11579 82455 34862685
Hypertension 239.94 31.63 261 11530 136182 34808958
Drug ineffective 192.41 31.63 452 11339 456299 34488841
Supine hypertension 186.40 31.63 39 11752 320 34944820
Hypotension 174.40 31.63 286 11505 221363 34723777
Multiple system atrophy 124.12 31.63 25 11766 166 34944974
Headache 122.66 31.63 232 11559 200403 34744737
Syncope 120.29 31.63 151 11640 91300 34853840
Orthostatic hypotension 117.32 31.63 85 11706 25834 34919306
Presyncope 103.74 31.63 70 11721 18989 34926151
Balance disorder 99.01 31.63 93 11698 40561 34904579
Hallucination 98.02 31.63 103 11688 51395 34893745
Blood pressure orthostatic decreased 90.95 31.63 21 11770 282 34944858
Feeling abnormal 87.21 31.63 107 11684 63128 34882012
Urinary tract infection 73.27 31.63 114 11677 83967 34861173
Dizziness postural 65.94 31.63 35 11756 6129 34939011
Off label use 62.45 31.63 32 11759 419492 34525648
Confusional state 62.45 31.63 145 11646 144015 34801125
Asthenia 60.77 31.63 201 11590 245050 34700090
Tremor 58.48 31.63 102 11689 82485 34862655
Blood pressure abnormal 57.01 31.63 35 11756 8071 34937069
Labile blood pressure 52.66 31.63 16 11775 643 34944497
Intentional underdose 48.21 31.63 15 11776 653 34944487
Condition aggravated 47.96 31.63 158 11633 192038 34753102
Dysstasia 46.25 31.63 36 11755 12159 34932981
Head injury 45.04 31.63 42 11749 18118 34927022
Incorrect dosage administered 42.41 31.63 16 11775 1250 34943890
Acute kidney injury 41.37 31.63 26 11765 304962 34640178
Incorrect dose administered 41.05 31.63 59 11732 40456 34904684
Adverse drug reaction 40.96 31.63 50 11741 29292 34915848
Anaemia 40.71 31.63 14 11777 233321 34711819
Gait disturbance 40.54 31.63 89 11702 85051 34860089
Product use complaint 40.50 31.63 16 11775 1416 34943724
Thrombocytopenia 38.49 31.63 4 11787 156243 34788897
Fatigue 36.95 31.63 232 11559 370421 34574719
Therapeutic response decreased 36.21 31.63 47 11744 29266 34915874
Drug titration error 35 31.63 11 11780 495 34944645
Somnolence 33.83 31.63 98 11693 111018 34834122

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 1034.36 29.10 880 15513 565634 79162361
Dizziness 878.84 29.10 778 15615 525663 79202332
Blood pressure increased 808.69 29.10 515 15878 210845 79517150
Product dose omission issue 644.72 29.10 476 15917 247061 79480934
Blood pressure decreased 491.12 29.10 286 16107 99180 79628815
Fall 480.73 29.10 543 15850 487086 79240909
Blood pressure fluctuation 449.31 29.10 236 16157 66909 79661086
Loss of consciousness 420.61 29.10 316 16077 167627 79560368
Supine hypertension 280.51 29.10 52 16341 372 79727623
Hypotension 245.30 29.10 371 16022 439946 79288049
Hypertension 225.36 29.10 307 16086 330685 79397310
Headache 206.01 29.10 429 15964 653343 79074652
Feeling abnormal 179.44 29.10 191 16202 159008 79568987
Syncope 169.02 29.10 196 16197 179253 79548742
Presyncope 155.92 29.10 100 16293 40954 79687041
Blood pressure orthostatic decreased 142.02 29.10 29 16364 360 79727635
Multiple system atrophy 141.79 29.10 29 16364 363 79727632
Orthostatic hypotension 125.51 29.10 99 16294 56065 79671930
Hallucination 103.84 29.10 107 16286 85638 79642357
Tremor 84.01 29.10 136 16257 169947 79558048
Intentional underdose 82.09 29.10 27 16366 2327 79725668
Balance disorder 81.47 29.10 101 16292 98756 79629239
Dizziness postural 78.23 29.10 41 16352 11508 79716487
Off label use 78.13 29.10 45 16348 907170 78820825
Asthenia 77.58 29.10 256 16137 511433 79216562
Incorrect dose administered 77.58 29.10 87 16306 76543 79651452
Head injury 77.34 29.10 63 16330 37306 79690689
Drug dose titration not performed 75.95 29.10 20 16373 790 79727205
Blood pressure abnormal 73.13 29.10 45 16348 17124 79710871
Drug ineffective 61.97 29.10 406 15987 1080507 78647488
Confusional state 61.09 29.10 173 16220 317824 79410171
Drug titration error 60.05 29.10 18 16375 1144 79726851
Dysstasia 53.70 29.10 45 16348 27701 79700294
Arthralgia 52.58 29.10 26 16367 571777 79156218
Fatigue 51.22 29.10 346 16047 929381 78798614
Labile blood pressure 48.35 29.10 18 16375 2235 79725760
Therapeutic response decreased 48.28 29.10 64 16329 66789 79661206
Seizure like phenomena 47.84 29.10 17 16376 1850 79726145
Gait disturbance 45.92 29.10 119 16274 207387 79520608
Malaise 44.67 29.10 209 16184 489660 79238335
Urinary tract infection 42.04 29.10 138 16255 274374 79453621
Palpitations 41.73 29.10 85 16308 126525 79601470
Adverse drug reaction 41.08 29.10 59 16334 66333 79661662
Somnolence 40.11 29.10 124 16269 238857 79489138
Anaemia 39.73 29.10 21 16372 444994 79283001
Acute kidney injury 38.87 29.10 30 16363 519374 79208621
Vision blurred 38.40 29.10 74 16319 105824 79622171
Condition aggravated 38.02 29.10 203 16190 500921 79227074
Hyperhidrosis 36.76 29.10 90 16303 151402 79576593
Memory impairment 35.62 29.10 74 16319 111660 79616335
Thrombocytopenia 35.36 29.10 6 16387 265253 79462742
Migraine 35.29 29.10 64 16329 87429 79640566
Nausea 34.85 29.10 324 16069 956872 78771123
Pain 34.82 29.10 57 16336 703745 79024250
Joint swelling 33.44 29.10 9 16384 288637 79439358
Drug hypersensitivity 33.37 29.10 10 16383 298906 79429089
Hip fracture 32.96 29.10 36 16357 30725 79697270
Incorrect dosage administered 31.27 29.10 14 16379 2785 79725210
Heart rate increased 30.65 29.10 73 16320 120651 79607344
Freezing phenomenon 29.41 29.10 12 16381 1902 79726093
Cerebrovascular accident 29.28 29.10 84 16309 155208 79572787

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 | Suggest Off label Use Form| |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
7391 IUPHAR_LIGAND_ID
6120 INN_ID
J7A92W69L7 UNII
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
C0028351 UMLSCUI
DB00368 DRUGBANK_ID
33 INN_ID
D009638 MESH_DESCRIPTOR_UI
439260 PUBCHEM_CID

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 0832-0720 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 0832-0721 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 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 51407-765 CAPSULE 100 mg ORAL ANDA 29 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 51407-766 CAPSULE 200 mg ORAL ANDA 29 sections
Droxidopa HUMAN PRESCRIPTION DRUG LABEL 1 51407-767 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