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

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	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 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	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 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	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:

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
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:

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	0832-0721	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