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

Stem definition	Drug id	CAS RN
dopamine receptor agonists, dopamine derivatives, used as antiparkinsonism/prolactin inhibitors	971	23651-95-8

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
1	g	O

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
Feb. 18, 2014	FDA	LUNDBECK NA LTD

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Adrenergic receptor	GPCR	P07550 P08588 P08913 P13945 P18089 P18825 P25100 P35348 P35368	ADRB2_HUMAN ADRB1_HUMAN ADA2A_HUMAN ADRB3_HUMAN ADA2B_HUMAN ADA2C_HUMAN ADA1D_HUMAN ADA1A_HUMAN ADA1B_HUMAN	AGONIST				CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN	ANTAGONIST	Ki	7.10		IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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