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 1799.00 53.70 595 2862 58070 2296558
Blood pressure increased 1025.78 53.70 293 3164 16693 2337935
Headache 910.90 53.70 397 3060 79782 2274846
Product dose omission 773.27 53.70 288 3169 37969 2316659
Blood pressure fluctuation 655.31 53.70 134 3323 1741 2352887
Blood pressure decreased 580.25 53.70 165 3292 9071 2345557
Fall 561.84 53.70 243 3214 46856 2307772
Drug ineffective 547.71 53.70 304 3153 101320 2253308
Fatigue 543.76 53.70 285 3172 84588 2270040
Hypertension 539.68 53.70 203 3254 27158 2327470
Hypotension 534.20 53.70 211 3246 32225 2322403
Loss of consciousness 530.94 53.70 182 3275 18585 2336043
Nausea 527.67 53.70 307 3150 111882 2242746
Feeling abnormal 396.29 53.70 156 3301 23425 2331203
Syncope 345.35 53.70 129 3328 16746 2337882
Malaise 343.23 53.70 183 3274 55402 2299226
Death 333.66 53.70 205 3252 81263 2273365
Presyncope 326.27 53.70 87 3370 3716 2350912
Asthenia 299.16 53.70 158 3299 46768 2307860
Condition aggravated 259.79 53.70 127 3330 31852 2322776
Palpitations 258.83 53.70 104 3353 16352 2338276
Orthostatic hypotension 252.21 53.70 67 3390 2812 2351816
Migraine 204.99 53.70 78 3379 10575 2344053
Tremor 194.69 53.70 91 3366 20570 2334058
Hyperhidrosis 180.32 53.70 79 3378 15343 2339285
Heart rate increased 166.82 53.70 68 3389 11037 2343591
Confusional state 165.92 53.70 86 3371 24258 2330370
Supine hypertension 160.71 53.70 22 3435 5 2354623
Chest pain 154.21 53.70 86 3371 28051 2326577
Somnolence 151.53 53.70 80 3377 23405 2331223
Adverse drug reaction 142.66 53.70 56 3401 8227 2346401
Balance disorder 130.48 53.70 55 3402 9692 2344936
Insomnia 128.23 53.70 74 3383 25713 2328915
Memory impairment 128.00 53.70 59 3398 12864 2341764
Blood pressure orthostatic decreased 126.73 53.70 19 3438 25 2354603
Incorrect dose administered 124.11 53.70 53 3404 9642 2344986
Dyspnoea 123.81 53.70 112 3345 78621 2276007
Gait disturbance 118.22 53.70 67 3390 22478 2332150
Vomiting 116.74 53.70 104 3353 71498 2283130
Urinary tract infection 115.48 53.70 73 3384 29869 2324759
Intentional underdose 111.69 53.70 24 3433 395 2354233
Therapeutic response decreased 111.17 53.70 45 3412 7150 2347478
Abdominal pain upper 108.69 53.70 63 3394 22037 2332591
Drug intolerance 103.56 53.70 52 3405 13665 2340963
Dizziness postural 96.90 53.70 25 3432 929 2353699
Drug titration error 85.70 53.70 16 3441 122 2354506
Drug dose titration not performed 82.63 53.70 15 3442 96 2354532
Vision blurred 72.52 53.70 42 3415 14626 2340002
Muscle spasms 69.38 53.70 47 3410 21519 2333109
Hip fracture 67.72 53.70 28 3429 4684 2349944
Chest discomfort 62.25 53.70 38 3419 14557 2340071
Hallucination 61.76 53.70 31 3426 8117 2346511
Blood pressure abnormal 61.62 53.70 20 3437 1685 2352943
Anxiety 60.65 53.70 49 3408 29310 2325318
Inappropriate schedule of product administration 60.45 53.70 35 3422 12169 2342459
Feeling hot 60.40 53.70 29 3428 6899 2347729
Hypoaesthesia 60.16 53.70 42 3415 20173 2334455
Multiple system atrophy 59.61 53.70 10 3447 37 2354591
Seizure 59.55 53.70 45 3412 24421 2330207
Incorrect dosage administered 58.66 53.70 14 3443 375 2354253
Dysstasia 58.12 53.70 22 3435 2917 2351711
Head injury 58.06 53.70 24 3433 4010 2350618
Abdominal discomfort 56.02 53.70 38 3419 17418 2337210
Heart rate irregular 54.70 53.70 20 3437 2407 2352221

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 1723.95 58.99 590 3292 33771 1709128
Blood pressure increased 1227.36 58.99 349 3533 10404 1732495
Death 1022.51 58.99 534 3348 86909 1655990
Fall 959.96 58.99 363 3519 26851 1716048
Blood pressure fluctuation 827.77 58.99 170 3712 1142 1741757
Drug ineffective 816.23 58.99 416 3466 63385 1679514
Product dose omission 712.14 58.99 278 3604 22162 1720737
Blood pressure decreased 652.50 58.99 199 3683 7447 1735452
Hypertension 605.63 58.99 238 3644 19210 1723689
Hypotension 527.65 58.99 244 3638 29410 1713489
Loss of consciousness 461.81 58.99 182 3700 14693 1728206
Headache 422.53 58.99 220 3662 34156 1708743
Fatigue 337.53 58.99 218 3664 50563 1692336
Orthostatic hypotension 333.41 58.99 99 3783 3332 1739567
Asthenia 322.97 58.99 185 3697 34485 1708414
Syncope 283.24 58.99 127 3755 14042 1728857
Condition aggravated 257.59 58.99 135 3747 21015 1721884
Supine hypertension 241.75 58.99 36 3846 7 1742892
Feeling abnormal 232.25 58.99 103 3779 11063 1731836
Balance disorder 229.40 58.99 85 3797 5727 1737172
Presyncope 215.45 58.99 67 3815 2631 1740268
Confusional state 214.80 58.99 120 3762 21158 1721741
Urinary tract infection 196.18 58.99 89 3793 10064 1732835
Tremor 171.47 58.99 88 3794 13043 1729856
Parkinson's disease 154.86 58.99 47 3835 1695 1741204
Malaise 152.38 58.99 109 3773 29456 1713443
Gait disturbance 134.50 58.99 74 3808 12596 1730303
Somnolence 133.10 58.99 81 3801 16658 1726241
Hallucination 124.92 58.99 61 3821 8109 1734790
Nausea 118.51 58.99 119 3763 51077 1691822
Blood pressure orthostatic decreased 104.60 58.99 18 3864 35 1742864
Dizziness postural 102.21 58.99 29 3853 821 1742078
Drug intolerance 94.83 58.99 46 3836 6016 1736883
Therapeutic response decreased 92.91 58.99 44 3838 5456 1737443
Dysstasia 89.19 58.99 31 3851 1723 1741176
Multiple system atrophy 89.11 58.99 16 3866 44 1742855
Adverse drug reaction 86.50 58.99 40 3842 4698 1738201
Head injury 86.29 58.99 35 3847 2989 1739910
Incorrect dose administered 86.10 58.99 46 3836 7363 1735536
Insomnia 85.87 58.99 61 3821 16215 1726684
Memory impairment 84.90 58.99 44 3838 6619 1736280
Dysphagia 75.07 58.99 47 3835 10121 1732778
Chest pain 70.72 58.99 59 3823 19855 1723044
Vision blurred 67.41 58.99 41 3841 8382 1734517
Labile blood pressure 66.73 58.99 15 3867 158 1742741
Gait inability 66.42 58.99 30 3852 3333 1739566
Muscular weakness 64.85 58.99 43 3839 10206 1732693
Incorrect dosage administered 64.20 58.99 15 3867 190 1742709
Peripheral swelling 61.74 58.99 38 3844 7933 1734966
Cerebrovascular accident 61.49 58.99 52 3830 17814 1725085

Pharmacologic Action:

SourceCodeDescription
ATC C01CA27 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
FDA CS M0003647 Catecholamines
FDA PE N0000178478 Increased Blood Pressure
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:50514 vasoconstrictor agent
CHEBI has role CHEBI:35674 antihypertensive agent
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

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 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:

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

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-820 CAPSULE 100 mg ORAL NDA 17 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-821 CAPSULE 200 mg ORAL NDA 17 sections
Northera HUMAN PRESCRIPTION DRUG LABEL 1 67386-822 CAPSULE 300 mg ORAL NDA 17 sections