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

Stem definition	Drug id	CAS RN
tricyclic compounds	956	1668-19-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: P-3693A doxepin doxepine doxepin hydrochloride silenor doxepin HCl	A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors. Molecular weight: 279.38 Formula: C19H21NO CLOGP: 4.09 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 12.47 ALOGS: -3.94 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

P-3693A
doxepin
doxepine
doxepin hydrochloride
silenor
doxepin HCl

A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.

Molecular weight: 279.38
Formula: C19H21NO
CLOGP: 4.09
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 12.47
ALOGS: -3.94
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O
0.10	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	17.90 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	30 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	12 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	14 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.20 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	15 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 23, 1969	FDA

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
Completed suicide	561.11	13.21	405	15616	131484	50457619
Toxicity to various agents	374.85	13.21	395	15626	212104	50376999
Respiratory depression	176.91	13.21	83	15938	11927	50577176
Cardio-respiratory arrest	155.54	13.21	132	15889	53760	50535343
Drug abuse	93.97	13.21	105	15916	59741	50529362
Respiratory arrest	83.45	13.21	72	15949	29937	50559166
Depressed level of consciousness	61.54	13.21	79	15942	51874	50537229
Cardiac arrest	58.19	13.21	99	15922	83552	50505551
Suicidal ideation	54.58	13.21	77	15944	55308	50533795
Suicide attempt	54.08	13.21	74	15947	51658	50537445
Sleep-related eating disorder	47.08	13.21	15	16006	753	50588350
Urticaria	45.79	13.21	116	15905	129445	50459658
Decreased bronchial secretion	44.96	13.21	9	16012	62	50589041
Insomnia	38.25	13.21	132	15889	174733	50414370
Joint swelling	38.11	13.21	15	16006	245271	50343832
Depression	36.28	13.21	125	15896	165298	50423805
Electrocardiogram QRS complex prolonged	36.14	13.21	22	15999	5322	50583781
Coma	35.23	13.21	64	15957	56815	50532288
Systemic lupus erythematosus	33.48	13.21	3	16018	140619	50448484
Skin plaque	32.73	13.21	22	15999	6306	50582797
Jaundice neonatal	30.59	13.21	11	16010	800	50588303
Lipohypertrophy	29.62	13.21	10	16011	603	50588500
Paranasal sinus inflammation	29.13	13.21	9	16012	408	50588695
Somnolence	28.80	13.21	111	15910	154874	50434229
Infusion related reaction	28.67	13.21	9	16012	169548	50419555
Diverticulum oesophageal	28.24	13.21	7	16014	138	50588965
Bradypnoea	27.01	13.21	15	16006	3059	50586044
Mandibular mass	26.66	13.21	7	16014	175	50588928
Sleep disorder	26.46	13.21	57	15964	57226	50531877
Intentional overdose	26.40	13.21	60	15961	62444	50526659
Rheumatoid arthritis	25.99	13.21	16	16005	202534	50386569
Exposure via ingestion	25.51	13.21	14	16007	2789	50586314
Poisoning	25.17	13.21	25	15996	12404	50576699
Migraine	25.12	13.21	66	15955	75214	50513889
Overdose	25.10	13.21	79	15942	99648	50489455
Therapeutic product effect increased	24.69	13.21	10	16011	1006	50588097
Glossodynia	23.77	13.21	4	16017	115565	50473538
Nail avulsion	23.33	13.21	6	16015	138	50588965
Maternal exposure during pregnancy	22.85	13.21	11	16010	159767	50429336
Osteosclerosis	22.75	13.21	14	16007	3453	50585650
Self esteem decreased	22.53	13.21	8	16013	561	50588542
Death	22.00	13.21	177	15844	325202	50263901
Drug withdrawal syndrome neonatal	21.90	13.21	11	16010	1830	50587273
Acute lung injury	21.66	13.21	10	16011	1383	50587720
Therapeutic product effect decreased	21.64	13.21	8	16013	136042	50453061
Blood test abnormal	21.52	13.21	22	15999	11297	50577806
Arthropathy	20.91	13.21	12	16009	157894	50431209
Ventricular arrhythmia	20.79	13.21	13	16008	3296	50585807
Restlessness	20.47	13.21	32	15989	25141	50563962
Blood glucose fluctuation	20.46	13.21	14	16007	4132	50584971
Product prescribing error	20.42	13.21	29	15992	20932	50568171
Contraindicated product administered	20.19	13.21	11	16010	148947	50440156
Defaecation disorder	19.10	13.21	7	16014	538	50588565
Dyshidrotic eczema	18.92	13.21	7	16014	552	50588551
Treatment failure	18.89	13.21	10	16011	137627	50451476
Hepatic enzyme increased	18.83	13.21	10	16011	137370	50451733
Anxiety	18.81	13.21	108	15913	177498	50411605
Eczema	18.66	13.21	29	15992	22673	50566430
Hepatic lesion	18.52	13.21	13	16008	3995	50585108
Pruritus	18.47	13.21	153	15868	283415	50305688
Sinobronchitis	18.04	13.21	5	16016	154	50588949
Stress	17.77	13.21	47	15974	53746	50535357
Drug interaction	17.74	13.21	116	15905	199505	50389598
Psoriasis	17.67	13.21	55	15966	68945	50520158
Breast adenoma	17.49	13.21	4	16017	55	50589048
Dermatitis atopic	17.44	13.21	12	16009	3574	50585529
Pyrexia	17.34	13.21	62	15959	380141	50208962
Blood pressure systolic increased	17.20	13.21	36	15985	35413	50553690
Choking	17.04	13.21	17	16004	8481	50580622
Synovitis	17.00	13.21	9	16012	123856	50465247
Restless legs syndrome	16.99	13.21	23	15998	15874	50573229
Febrile neutropenia	16.83	13.21	5	16016	97662	50491441
Allergic oedema	16.82	13.21	7	16014	755	50588348
Osteoporotic fracture	16.42	13.21	11	16010	3134	50585969
Somnambulism	16.14	13.21	13	16008	4911	50584192
Major depression	16.12	13.21	15	16006	6869	50582234
Iritis	16.06	13.21	10	16011	2518	50586585
Mastocytosis	15.75	13.21	6	16015	513	50588590
Bradycardia	15.26	13.21	50	15971	64376	50524727
Myofascial pain syndrome	15.18	13.21	9	16012	2074	50587029
Impaired work ability	14.98	13.21	20	16001	13620	50575483
Junctional ectopic tachycardia	14.77	13.21	4	16017	113	50588990
Drug hypersensitivity	14.54	13.21	132	15889	250878	50338225
Arrhythmia	14.20	13.21	32	15989	33100	50556003
Scratch	13.97	13.21	12	16009	4950	50584153
Burns second degree	13.91	13.21	6	16015	707	50588396
Gastrointestinal infection	13.90	13.21	14	16007	7060	50582043
Hypothermia	13.79	13.21	18	16003	11998	50577105
Quality of life decreased	13.40	13.21	13	16008	6270	50582833
Brain oedema	13.38	13.21	18	16003	12352	50576751
Seizure	13.34	13.21	73	15948	117801	50471302
Blood pressure diastolic increased	13.31	13.21	14	16007	7429	50581674

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
Completed suicide	377.67	18.08	249	7059	89997	29477222
Toxicity to various agents	213.54	18.08	237	7071	173424	29393795
Needle fatigue	113.72	18.08	27	7281	573	29566646
Gait spastic	109.97	18.08	27	7281	663	29566556
Drug abuse	109.81	18.08	116	7192	79767	29487452
Relapsing-remitting multiple sclerosis	108.39	18.08	27	7281	705	29566514
Hypertonic bladder	90.00	18.08	27	7281	1429	29565790
Monoparesis	82.88	18.08	27	7281	1876	29565343
Muscle spasticity	58.17	18.08	27	7281	4856	29562363
Nocturia	57.81	18.08	32	7276	8330	29558889
Memory impairment	57.31	18.08	57	7251	36413	29530806
Micturition urgency	56.68	18.08	27	7281	5146	29562073
Central nervous system lesion	54.43	18.08	27	7281	5621	29561598
Pulmonary oedema	48.13	18.08	56	7252	42679	29524540
Brugada syndrome	43.32	18.08	13	7295	688	29566531
Erectile dysfunction	41.70	18.08	35	7273	17974	29549245
Movement disorder	39.50	18.08	27	7281	10210	29557009
Multiple sclerosis relapse	39.12	18.08	28	7280	11391	29555828
Ataxia	37.66	18.08	28	7280	12075	29555144
Brain oedema	37.42	18.08	28	7280	12192	29555027
Insomnia	36.89	18.08	73	7235	88688	29478531
Pollakiuria	35.34	18.08	31	7277	16885	29550334
Soft tissue haemorrhage	30.41	18.08	7	7301	129	29567090
Hydrocholecystis	29.61	18.08	8	7300	289	29566930
Cardio-respiratory arrest	29.16	18.08	48	7260	50553	29516666
Dysarthria	29.07	18.08	37	7271	30874	29536345
Illness anxiety disorder	28.82	18.08	7	7301	164	29567055
Somatic symptom disorder	24.81	18.08	8	7300	537	29566682
Overdose	23.31	18.08	57	7251	79762	29487457
Helplessness	23.01	18.08	5	7303	70	29567149
Anxiety	22.88	18.08	59	7249	85306	29481913
Toxic cardiomyopathy	21.59	18.08	6	7302	241	29566978
Drug dependence	21.14	18.08	26	7282	20955	29546264
Soft tissue swelling	19.73	18.08	6	7302	332	29566887
Wrong patient received product	19.33	18.08	10	7298	2272	29564947
Pruritus	19.23	18.08	68	7240	116781	29450438
Hypopnoea	18.32	18.08	8	7300	1246	29565973
Measles	18.26	18.08	5	7303	190	29567029
Febrile neutropenia	18.11	18.08	3	7305	112237	29454982

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
Completed suicide	922.58	13.90	666	19148	223748	64255170
Toxicity to various agents	568.04	13.90	624	19190	362889	64116029
Drug abuse	182.80	13.90	214	19600	132160	64346758
Cardio-respiratory arrest	177.36	13.90	183	19631	98210	64380708
Respiratory depression	139.63	13.90	88	19726	23355	64455563
Needle fatigue	98.45	13.90	25	19789	563	64478355
Respiratory arrest	94.38	13.90	98	19716	52887	64426031
Gait spastic	88.13	13.90	25	19789	867	64478051
Relapsing-remitting multiple sclerosis	82.77	13.90	25	19789	1083	64477835
Insomnia	78.77	13.90	182	19632	197654	64281264
Cardiac arrest	69.47	13.90	149	19665	153915	64325003
Hypertonic bladder	68.31	13.90	29	19785	3389	64475529
Monoparesis	62.33	13.90	26	19788	2908	64476010
Overdose	55.10	13.90	139	19675	159427	64319491
Suicide attempt	49.82	13.90	83	19731	70924	64407994
Electrocardiogram QRS complex prolonged	48.37	13.90	32	19782	9212	64469706
Decreased bronchial secretion	44.98	13.90	9	19805	64	64478854
Nocturia	42.91	13.90	32	19782	11133	64467785
Anxiety	42.61	13.90	148	19666	202501	64276417
Self esteem decreased	40.97	13.90	14	19800	903	64478015
Poisoning	39.89	13.90	41	19773	21838	64457080
Death	39.86	13.90	269	19545	482436	63996482
Urticaria	39.52	13.90	117	19697	147200	64331718
Depressed level of consciousness	39.26	13.90	81	19733	81355	64397563
Erectile dysfunction	37.33	13.90	31	19783	12596	64466322
Depression	36.91	13.90	132	19682	183159	64295759
Sleep-related eating disorder	36.79	13.90	12	19802	670	64478248
Micturition urgency	36.09	13.90	28	19786	10331	64468587
Febrile neutropenia	35.95	13.90	7	19807	187650	64291268
Coma	35.23	13.90	81	19733	87534	64391384
Brugada syndrome	35.05	13.90	13	19801	1065	64477853
Intentional overdose	34.90	13.90	82	19732	89862	64389056
Illness anxiety disorder	34.02	13.90	9	19805	239	64478679
Exposure via ingestion	33.24	13.90	20	19794	4882	64474036
Memory impairment	33.12	13.90	78	19736	85604	64393314
Brain oedema	32.58	13.90	37	19777	22038	64456880
Thrombocytopenia	29.50	13.90	16	19798	223785	64255133
Skin plaque	28.64	13.90	23	19791	8917	64470001
Diverticulum oesophageal	27.68	13.90	7	19807	155	64478763
Lipohypertrophy	27.41	13.90	10	19804	782	64478136
Central nervous system lesion	26.82	13.90	25	19789	11824	64467094
Dyshidrotic eczema	26.76	13.90	9	19805	553	64478365
Hydrocholecystis	26.54	13.90	8	19806	344	64478574
Intentional product misuse	25.99	13.90	64	19750	72231	64406687
Mandibular mass	25.81	13.90	7	19807	205	64478713
Therapeutic product effect increased	25.56	13.90	11	19803	1329	64477589
Suicidal ideation	25.09	13.90	60	19754	66482	64412436
Somnolence	24.88	13.90	126	19688	203519	64275399
Muscle spasticity	24.70	13.90	28	19786	16641	64462277
Restlessness	24.61	13.90	44	19770	39741	64439177
Infusion related reaction	24.37	13.90	10	19804	164457	64314461
Pyrexia	24.35	13.90	89	19725	558555	63920363
Obsessive-compulsive personality disorder	24.11	13.90	6	19808	124	64478794
Joint swelling	23.52	13.90	19	19795	215363	64263555
Feeling guilty	23.41	13.90	9	19805	814	64478104
Helplessness	22.83	13.90	7	19807	319	64478599
Neutropenia	22.78	13.90	24	19790	239600	64239318
Blood glucose fluctuation	22.73	13.90	17	19797	5938	64472980
Somatic symptom disorder	22.06	13.90	11	19803	1857	64477061
Dermatitis atopic	21.70	13.90	14	19800	3862	64475056
Acute kidney injury	20.61	13.90	70	19744	449170	64029748
Bradypnoea	20.30	13.90	15	19799	5144	64473774
Ataxia	19.93	13.90	29	19785	22055	64456863
Maternal exposure during pregnancy	19.62	13.90	3	19811	95881	64383037
Pulmonary congestion	19.60	13.90	30	19784	23850	64455068
Pruritus	19.43	13.90	163	19651	312237	64166681
Scratch	19.32	13.90	16	19798	6473	64472445
Spinal disorder	18.97	13.90	18	19796	8704	64470214
Bradycardia	18.76	13.90	79	19735	118140	64360778
Dizziness	18.65	13.90	208	19606	429955	64048963
Soft tissue haemorrhage	18.22	13.90	6	19808	345	64478573
Stress	18.08	13.90	50	19764	60484	64418434
Toxic cardiomyopathy	18.01	13.90	6	19808	358	64478560
Interstitial lung disease	17.98	13.90	4	19810	97728	64381190
Breast adenoma	17.61	13.90	4	19810	55	64478863
Renal impairment	17.28	13.90	10	19804	135007	64343911
Allergic oedema	17.18	13.90	7	19807	737	64478181
Pulmonary oedema	16.97	13.90	58	19756	78616	64400302
Product prescribing error	16.89	13.90	35	19779	35234	64443684
Crime	16.87	13.90	4	19810	67	64478851
Alanine aminotransferase increased	16.81	13.90	11	19803	139020	64339898
Libido decreased	16.81	13.90	13	19801	4771	64474147
Rheumatoid arthritis	16.12	13.90	16	19798	164278	64314640
Disease progression	16.09	13.90	12	19802	141668	64337250
Anaemia	16.03	13.90	61	19753	378619	64100299
Somnambulism	15.99	13.90	13	19801	5128	64473790
Movement disorder	15.80	13.90	26	19788	21974	64456944
Acute lung injury	15.62	13.90	10	19804	2721	64476197
Depressed mood	15.47	13.90	37	19777	40975	64437943
Osteoporotic fracture	15.38	13.90	11	19803	3587	64475331
Malignant neoplasm progression	14.96	13.90	8	19806	112863	64366055
Dysarthria	14.80	13.90	46	19768	59360	64419558
Hepatic enzyme increased	14.76	13.90	11	19803	129932	64348986
Pollakiuria	14.76	13.90	31	19783	31499	64447419
Hepatic lesion	14.57	13.90	13	19801	5811	64473107
Arrhythmia	14.13	13.90	42	19772	52902	64426016
Pancytopenia	14.01	13.90	14	19800	143295	64335623

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	D04AX01	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Other antipruritics
ATC	N06AA12	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors
CHEBI has role	CHEBI:35469	antidepressants
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D000929	Antidepressive Agents, Tricyclic
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006993	Hypnotics and Sedatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D000068776	Sleep Aids, Pharmaceutical
FDA EPC	N0000175752	Tricyclic Antidepressant

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Atopic dermatitis	indication	24079001	DOID:3310
Depressive disorder	indication	35489007
Anxiety	indication	48694002
Lichen simplex chronicus	indication	53891004
Severe major depression with psychotic features	indication	73867007
Bipolar affective disorder, current episode depression	indication	191627008	DOID:3312
Insomnia	indication	193462001
Itching of skin	indication	418363000
Cholestatic pruritus	off-label use	707150004
Suicidal thoughts	contraindication	6471006
Alcoholism	contraindication	7200002
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Hyperthyroidism	contraindication	34486009	DOID:7998
Conduction disorder of the heart	contraindication	44808001
Hepatic failure	contraindication	59927004
Sleep apnea	contraindication	73430006	DOID:0050847
Chronic idiopathic constipation	contraindication	82934008
Open-angle glaucoma	contraindication	84494001	DOID:1067
Epilepsy	contraindication	84757009	DOID:1826
Prolonged QT interval	contraindication	111975006
Bipolar affective disorder, current episode manic	contraindication	191618007
Sleep automatism	contraindication	247962006
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Syncope	contraindication	271594007
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Breastfeeding (mother)	contraindication	413712001
Myocardial infarction in recovery phase	contraindication	418044006
Congenital long QT syndrome	contraindication	442917000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.66	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10238620	May 18, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10653662	May 18, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9486437	May 18, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9861607	May 18, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10238620	May 18, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10653662	May 18, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9486437	May 18, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9861607	May 18, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10653660	July 20, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	11110074	July 20, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9572814	July 20, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10653660	July 20, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	11110074	July 20, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9572814	July 20, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	7915307	Aug. 24, 2027	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	7915307	Aug. 24, 2027	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	11234954	Jan. 18, 2028	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	11234954	Jan. 18, 2028	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10548871	April 11, 2028	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	11096920	April 11, 2028	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	10548871	April 11, 2028	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	11096920	April 11, 2028	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9107898	May 1, 2028	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	9107898	May 1, 2028	TREATMENT OF INSOMNIA
EQ 3MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	8513299	Sept. 7, 2030	TREATMENT OF INSOMNIA
EQ 6MG BASE	SILENOR	CURRAX	N022036	March 17, 2010	RX	TABLET	ORAL	8513299	Sept. 7, 2030	TREATMENT OF INSOMNIA

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 150MG BASE	DOXEPIN HYDROCHLORIDE	EDENBRIDGE PHARMS	A213796	April 19, 2022	RX	CAPSULE	ORAL	Oct. 29, 2022	COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Kd	7.53	WOMBAT-PK	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	9.75	WOMBAT-PK	DRUG LABEL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.30	DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.58	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Kd	7.17	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.54	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		EC50	7.45	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		EC50	7.20	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		EC50	7	WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.98	CHEMBL
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN				WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.63	WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		IC50	7.21	WOMBAT-PK
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.33	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		EC50	6.50	WOMBAT-PK
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		EC50	6.79	WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	7.42	WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.80	WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	7.28	WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	7.09	WOMBAT-PK
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	7.13	WOMBAT-PK
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		IC50	7	WOMBAT-PK
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	7.37	DRUG MATRIX
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.95	CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	4.89	WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.74	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		EC50	6.50	WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	7.48	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	11	CHEMBL
Serotonin (5-HT) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT1A_RAT 5HT1B_RAT 5HT1D_RAT 5HT1F_RAT 5HT2B_RAT 5HT6R_RAT 5HT7R_RAT 5HT5A_RAT 5HT5B_RAT 5HT3A_RAT 5HT4R_RAT 5HT3B_RAT		IC50	6.70	CHEMBL

External reference:

ID	Source
4019736	VUID
N0000147828	NUI
D00814	KEGG_DRUG
1229-29-4	SECONDARY_CAS_RN
4017851	VANDF
4019736	VANDF
C0013085	UMLSCUI
CHEBI:4710	CHEBI
CHEMBL1628227	ChEMBL_ID
CHEMBL1628234	ChEMBL_ID
DB01142	DRUGBANK_ID
D004316	MESH_DESCRIPTOR_UI
667477	PUBCHEM_CID
1225	IUPHAR_LIGAND_ID
1855	INN_ID
5ASJ6HUZ7D	UNII
203179	RXNORM
172015	MMSL
239355	MMSL
27123	MMSL
278670	MMSL
3183	MMSL
4638	MMSL
d00217	MMSL
001509	NDDF
004607	NDDF
11841005	SNOMEDCT_US
372587005	SNOMEDCT_US
85037008	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Doxepin	HUMAN PRESCRIPTION DRUG LABEL	1	0228-3315	TABLET, FILM COATED	3 mg	ORAL	ANDA	31 sections
Doxepin	HUMAN PRESCRIPTION DRUG LABEL	1	0228-3316	TABLET, FILM COATED	6 mg	ORAL	ANDA	31 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1049	CAPSULE	10 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1049	CAPSULE	10 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3125	CAPSULE	25 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3125	CAPSULE	25 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4250	CAPSULE	50 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4250	CAPSULE	50 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4810	TABLET	3 mg	ORAL	NDA authorized generic	32 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4811	TABLET	6 mg	ORAL	NDA authorized generic	32 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5375	CAPSULE	75 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5375	CAPSULE	75 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5390	TABLET	3 mg	ORAL	ANDA	34 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5391	TABLET	6 mg	ORAL	ANDA	34 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6410	CAPSULE	100 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6410	CAPSULE	100 mg	ORAL	ANDA	17 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-8117	CREAM	50 mg	TOPICAL	NDA authorized generic	18 sections
Zonalon	HUMAN PRESCRIPTION DRUG LABEL	1	0378-8123	CREAM	50 mg	TOPICAL	NDA	19 sections
PRUDOXIN	HUMAN PRESCRIPTION DRUG LABEL	1	0378-8130	CREAM	50 mg	TOPICAL	NDA	18 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4062	CAPSULE	10 mg	ORAL	ANDA	15 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4063	CAPSULE	25 mg	ORAL	ANDA	15 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4064	CAPSULE	50 mg	ORAL	ANDA	15 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4065	CAPSULE	75 mg	ORAL	ANDA	15 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4066	CAPSULE	100 mg	ORAL	ANDA	15 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6970	CAPSULE	10 mg	ORAL	ANDA	16 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6971	CAPSULE	25 mg	ORAL	ANDA	16 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6972	CAPSULE	50 mg	ORAL	ANDA	16 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6973	CAPSULE	100 mg	ORAL	ANDA	16 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7052	CAPSULE	10 mg	ORAL	ANDA	16 sections
Doxepin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7053	CAPSULE	25 mg	ORAL	ANDA	16 sections