droxidopa 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHUK,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT1,FLT3,GRK2,GRK3,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K14,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM1,PIM2,PLK1,PRKCD,PRKDC,PTK2,SGK1,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 82
kinase-selectivity-class ACVR2B,AXL,BMX,BRAF,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,JAK2,MAP2K6,MAP3K14,MAPK7,MAPK8,PIK3CB,PIK3CD,PRKDC,STK33,SYK,TEK,TGFBR1 21
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 786.04 31.41 627 11048 588657 90028115
Blood pressure increased 522.39 31.41 321 11354 196896 90419876
Product dose omission issue 443.75 31.41 337 11338 291350 90325422
Blood pressure decreased 372.39 31.41 185 11490 74710 90542062
Loss of consciousness 339.71 31.41 216 11459 140022 90476750
Blood pressure fluctuation 298.07 31.41 142 11533 52271 90564501
Death 276.99 31.41 316 11359 456235 90160537
Headache 255.03 31.41 421 11254 862325 89754447
Fall 243.60 31.41 304 11371 481506 90135266
Supine hypertension 214.21 31.41 30 11645 38 90616734
Hypotension 211.90 31.41 234 11441 325163 90291609
Feeling abnormal 193.35 31.41 165 11510 167070 90449702
Presyncope 192.47 31.41 90 11585 31715 90585057
Syncope 182.84 31.41 145 11530 132518 90484254
Hypertension 137.89 31.41 226 11449 457306 90159466
Palpitations 116.91 31.41 114 11561 136614 90480158
Blood pressure orthostatic decreased 106.41 31.41 20 11655 260 90616512
Orthostatic hypotension 92.55 31.41 61 11614 41766 90575006
Nausea 91.30 31.41 331 11344 1109985 89506787
Tremor 88.90 31.41 104 11571 153069 90463703
Intentional underdose 84.53 31.41 24 11651 2025 90614747
Malaise 79.07 31.41 208 11467 585778 90030994
Drug dose titration not performed 70.51 31.41 17 11658 755 90616017
Drug titration error 67.26 31.41 18 11657 1219 90615553
Fatigue 66.12 31.41 308 11367 1153715 89463057
Incorrect dose administered 65.88 31.41 65 11610 78865 90537907
Hyperhidrosis 60.57 31.41 81 11594 136224 90480548
Heart rate increased 59.46 31.41 73 11602 112829 90503943
Drug ineffective 58.22 31.41 339 11336 1383959 89232813
Asthenia 56.79 31.41 174 11501 533577 90083195
Multiple system atrophy 55.07 31.41 11 11664 200 90616572
Dizziness postural 52.82 31.41 25 11650 9028 90607744
Migraine 47.85 31.41 87 11588 190305 90426467
Hallucination 45.42 31.41 49 11626 65910 90550862
Joint swelling 44.71 31.41 6 11669 503294 90113478
Adverse drug reaction 43.85 31.41 64 11611 116637 90500135
Balance disorder 43.58 31.41 58 11617 97022 90519750
Somnolence 43.28 31.41 88 11587 208996 90407776
Hip fracture 40.91 31.41 34 11641 33043 90583729
Arthralgia 39.43 31.41 26 11649 778496 89838276
Head injury 38.45 31.41 32 11643 31156 90585616
Incorrect dosage administered 37.30 31.41 14 11661 2846 90613926
Blood pressure abnormal 37.12 31.41 26 11649 19619 90597153
Arthropathy 36.00 31.41 3 11672 366239 90250533
Systemic lupus erythematosus 35.47 31.41 3 11672 361893 90254879
Drug hypersensitivity 31.96 31.41 10 11665 463599 90153173
Therapeutic response decreased 31.96 31.41 48 11627 89681 90527091
Freezing phenomenon 31.62 31.41 11 11664 1801 90614971

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 809.76 31.71 624 11653 248630 42360428
Death 797.33 31.71 813 11464 470372 42138686
Blood pressure increased 609.37 31.71 373 11904 101555 42507503
Fall 510.07 31.71 467 11810 234053 42375005
Blood pressure fluctuation 423.75 31.71 189 12088 26719 42582339
Product dose omission issue 369.17 31.71 325 11952 154040 42455018
Blood pressure decreased 361.77 31.71 219 12058 58113 42550945
Loss of consciousness 270.79 31.71 219 12058 92135 42516923
Hypertension 230.10 31.71 261 12016 166943 42442115
Supine hypertension 189.82 31.71 39 12238 346 42608712
Hypotension 186.95 31.71 294 11983 257337 42351721
Drug ineffective 147.74 31.71 455 11822 629742 41979316
Syncope 134.36 31.71 154 12123 99252 42509806
Orthostatic hypotension 130.61 31.71 91 12186 30479 42578579
Multiple system atrophy 130.10 31.71 25 12252 151 42608907
Headache 120.77 31.71 233 12044 239136 42369922
Hallucination 109.51 31.71 107 12170 57400 42551658
Presyncope 105.94 31.71 71 12206 22316 42586742
Balance disorder 98.93 31.71 93 12184 47552 42561506
Feeling abnormal 94.00 31.71 108 12169 69678 42539380
Blood pressure orthostatic decreased 91.42 31.71 21 12256 326 42608732
Off label use 85.26 31.71 39 12238 638296 41970762
Urinary tract infection 75.34 31.71 116 12161 99168 42509890
Confusional state 67.62 31.71 149 12128 167448 42441610
Asthenia 66.23 31.71 204 12073 280589 42328469
Dizziness postural 63.42 31.71 35 12242 7760 42601298
Blood pressure abnormal 60.39 31.71 37 12240 9961 42599097
Tremor 59.61 31.71 103 12174 96826 42512232
Labile blood pressure 53.25 31.71 16 12261 727 42608331
Intentional underdose 48.83 31.71 15 12262 735 42608323
Head injury 48.19 31.71 43 12234 20539 42588519
Dysstasia 46.69 31.71 36 12241 14050 42595008
Gait disturbance 43.91 31.71 91 12186 97909 42511149
Anaemia 42.39 31.71 14 12263 280264 42328794
Acute kidney injury 40.83 31.71 28 12249 367309 42241749
Incorrect dosage administered 40.12 31.71 16 12261 1702 42607356
Product use complaint 39.34 31.71 17 12260 2214 42606844
Fatigue 38.42 31.71 235 12042 435406 42173652
Thrombocytopenia 37.94 31.71 5 12272 190274 42418784
Adverse drug reaction 37.55 31.71 50 12227 37384 42571674
Toxicity to various agents 37.26 31.71 10 12267 229126 42379932
Condition aggravated 36.40 31.71 160 12117 260594 42348464
Incorrect dose administered 36.13 31.71 59 12218 52915 42556143
Therapeutic response decreased 33.44 31.71 47 12230 36965 42572093
Drug titration error 32.34 31.71 11 12266 747 42608311
Dyskinesia 31.97 31.71 38 12239 25352 42583706
Gait inability 31.81 31.71 36 12241 22797 42586261

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 1173.99 28.77 916 16089 697953 109874341
Dizziness 912.14 28.77 792 16213 697401 109874893
Blood pressure increased 861.30 28.77 519 16486 257854 110314440
Product dose omission issue 658.78 28.77 477 16528 321305 110250989
Blood pressure decreased 546.50 28.77 292 16713 114799 110457495
Fall 531.39 28.77 552 16453 602930 109969364
Blood pressure fluctuation 489.95 28.77 236 16769 74588 110497706
Loss of consciousness 468.18 28.77 320 16685 195986 110376308
Hypotension 292.70 28.77 380 16625 523469 110048825
Supine hypertension 292.38 28.77 52 16953 399 110571895
Feeling abnormal 209.65 28.77 193 16812 180518 110391776
Headache 207.78 28.77 433 16572 881944 109690350
Syncope 205.80 28.77 201 16804 202335 110369959
Hypertension 196.06 28.77 310 16695 509774 110062520
Presyncope 169.17 28.77 101 16904 48786 110523508
Multiple system atrophy 151.94 28.77 29 16976 340 110571954
Orthostatic hypotension 143.43 28.77 102 16903 66147 110506147
Blood pressure orthostatic decreased 137.74 28.77 29 16976 574 110571720
Hallucination 126.65 28.77 113 16892 101319 110470975
Tremor 99.08 28.77 138 16867 202094 110370200
Off label use 97.74 28.77 55 16950 1500130 109072164
Balance disorder 91.76 28.77 101 16904 116459 110455835
Head injury 87.97 28.77 64 16941 42953 110529341
Intentional underdose 87.66 28.77 27 16978 2525 110569769
Dizziness postural 80.37 28.77 41 16964 14568 110557726
Blood pressure abnormal 79.28 28.77 47 16958 22377 110549917
Incorrect dose administered 78.46 28.77 88 16917 103553 110468741
Asthenia 78.26 28.77 258 16747 688741 109883553
Drug dose titration not performed 76.28 28.77 20 16985 1045 110571249
Drug titration error 59.01 28.77 18 16987 1629 110570665
Fatigue 58.48 28.77 352 16653 1215606 109356688
Dysstasia 58.35 28.77 45 16960 32941 110539353
Urinary tract infection 55.11 28.77 141 16864 326141 110246153
Drug ineffective 54.44 28.77 409 16596 1520131 109052163
Confusional state 53.53 28.77 176 16829 468504 110103790
Arthralgia 52.89 28.77 27 16978 779605 109792689
Labile blood pressure 51.83 28.77 18 16987 2453 110569841
Toxicity to various agents 50.53 28.77 7 16998 480548 110091746
Gait disturbance 49.87 28.77 123 16882 278085 110294209
Seizure like phenomena 48.21 28.77 17 16988 2424 110569870
Somnolence 47.61 28.77 126 16879 297323 110274971
Palpitations 46.65 28.77 86 16919 159126 110413168
Malaise 46.26 28.77 215 16790 671604 109900690
Vision blurred 46.01 28.77 76 16929 128946 110443348
Therapeutic response decreased 44.46 28.77 64 16941 96435 110475859
Nausea 42.20 28.77 329 16676 1235361 109336933
Hip fracture 41.55 28.77 38 16967 35113 110537181
Hyperhidrosis 41.46 28.77 90 16915 187208 110385086
Joint swelling 40.99 28.77 9 16996 442836 110129458
Drug hypersensitivity 40.50 28.77 10 16995 454080 110118214
Cerebrovascular accident 40.00 28.77 87 16918 181197 110391097
Dyskinesia 37.75 28.77 43 16962 51403 110520891
Heart rate increased 37.57 28.77 74 16931 143760 110428534
Anaemia 35.51 28.77 20 16985 547066 110025228
Adverse drug reaction 33.43 28.77 59 16946 105500 110466794
Pain 33.36 28.77 60 16945 954895 109617399
Freezing phenomenon 32.62 28.77 13 16992 2596 110569698
Thrombocytopenia 32.46 28.77 7 16998 348878 110223416
Condition aggravated 32.18 28.77 208 16797 734628 109837666
Incorrect dosage administered 30.65 28.77 14 16991 3904 110568390
Acute kidney injury 30.12 28.77 32 16973 635398 109936896
Blood pressure immeasurable 30.04 28.77 12 16993 2411 110569883
Treatment failure 29.21 28.77 4 17001 277230 110295064

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 D000316 Adrenergic alpha-Agonists
MeSH PA D002317 Cardiovascular Agents
MeSH PA D013566 Sympathomimetics
MeSH PA D014662 Vasoconstrictor Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D018726 Anti-Dyskinesia Agents
FDA PE N0000178478 Increased Blood Pressure
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:50514 vasoconstrictor agent

Related Drugs by ATC class:

C01CA Adrenergic and dopaminergic agents 25 drugs
amezinium metilsulfatearbutaminecafedrinedimetofrinedobutaminedopaminedopexamineephedrineepinephrineetilefrinefenoldopamgepefrine show all 25 →

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
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
439260 PUBCHEM_CID
D009638 MESH_DESCRIPTOR_UI
CHEBI:18357 CHEBI
J7A92W69L7 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 0904-7392 CAPSULE 100 mg ORAL ANDA 24 sections
Droxidopa Human Prescription Drug Label 1 0904-7393 CAPSULE 200 mg ORAL ANDA 24 sections
Droxidopa Human Prescription Drug Label 1 0904-7394 CAPSULE 300 mg ORAL ANDA 24 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 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
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 27 sections
Droxidopa Human Prescription Drug Label 1 67877-705 CAPSULE 200 mg ORAL ANDA 27 sections
Droxidopa Human Prescription Drug Label 1 67877-706 CAPSULE 300 mg ORAL ANDA 27 sections