doxepin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tricyclic compounds 956 1668-19-5

Description:

MoleculeDescription

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:

DoseUnitRoute
0.10 g O
0.10 g P

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
Sept. 23, 1969 FDA

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
Completed suicide 628.13 13.12 435 17871 145238 63325478
Toxicity to various agents 408.51 13.12 425 17881 246825 63223891
Respiratory depression 220.79 13.12 98 18208 13617 63457099
Cardio-respiratory arrest 158.07 13.12 134 18172 59825 63410891
Drug abuse 95.43 13.12 111 18195 72407 63398309
Respiratory arrest 86.06 13.12 73 18233 32572 63438144
Depressed level of consciousness 79.96 13.12 94 18212 61984 63408732
Chronic spontaneous urticaria 74.71 13.12 23 18283 1134 63469582
Urticaria 65.07 13.12 146 18160 165656 63305060
Cardiac arrest 62.96 13.12 103 18203 92442 63378274
Suicidal ideation 60.46 13.12 82 18224 62339 63408377
Suicide attempt 52.99 13.12 76 18230 60842 63409874
Sleep-related eating disorder 51.09 13.12 16 18290 835 63469881
Decreased bronchial secretion 45.80 13.12 9 18297 62 63470654
Skin plaque 45.69 13.12 29 18277 8291 63462425
Systemic lupus erythematosus 45.48 13.12 4 18302 208914 63261802
Depression 45.33 13.12 142 18164 196350 63274366
Joint swelling 43.58 13.12 20 18286 327646 63143070
Pruritus 41.66 13.12 210 18096 361243 63109473
Overdose 39.28 13.12 96 18210 114982 63355734
Insomnia 38.60 13.12 143 18163 215109 63255607
Electrocardiogram QRS complex prolonged 38.47 13.12 23 18283 5915 63464801
Glossodynia 37.41 13.12 4 18302 178872 63291844
Infusion related reaction 35.85 13.12 13 18293 245508 63225208
Drug interaction 35.22 13.12 145 18161 228986 63241730
Coma 33.85 13.12 64 18242 64300 63406416
Rheumatoid arthritis 31.46 13.12 17 18289 253802 63216914
Contraindicated product administered 30.97 13.12 12 18294 217636 63253080
Dermatitis atopic 30.35 13.12 24 18282 9700 63461016
Jaundice neonatal 30.18 13.12 11 18295 914 63469802
Maternal exposure during pregnancy 29.91 13.12 13 18293 220049 63250667
Lipohypertrophy 29.74 13.12 10 18296 655 63470061
Inadequate analgesia 28.94 13.12 15 18291 2928 63467788
Synovitis 28.84 13.12 9 18297 186909 63283807
Diverticulum oesophageal 28.61 13.12 7 18299 144 63470572
Paranasal sinus inflammation 28.44 13.12 9 18297 486 63470230
Somnolence 28.17 13.12 114 18192 178571 63292145
Mandibular mass 27.31 13.12 7 18299 175 63470541
Poisoning 26.96 13.12 26 18280 13674 63457042
Therapeutic product effect decreased 26.91 13.12 11 18295 193176 63277540
Bradypnoea 26.30 13.12 15 18291 3535 63467181
Exposure via ingestion 26.25 13.12 14 18292 2895 63467821
Sleep disorder 25.67 13.12 66 18240 81500 63389216
Death 25.56 13.12 190 18116 374191 63096525
Stress 25.03 13.12 58 18248 67109 63403607
Intentional overdose 24.38 13.12 61 18245 74091 63396625
Therapeutic product effect increased 23.87 13.12 10 18296 1205 63469511
Major depression 23.34 13.12 19 18287 7999 63462717
Hepatic enzyme increased 23.02 13.12 15 18291 202313 63268403
Osteosclerosis 22.47 13.12 14 18292 3874 63466842
Migraine 22.26 13.12 73 18233 103273 63367443
Nail avulsion 22.02 13.12 6 18300 191 63470525
Self esteem decreased 21.95 13.12 8 18298 665 63470051
Drug withdrawal syndrome neonatal 21.60 13.12 11 18295 2070 63468646
Acute lung injury 21.40 13.12 10 18296 1561 63469155
Anxiety 21.32 13.12 121 18185 217420 63253296
Blood glucose fluctuation 20.39 13.12 14 18292 4562 63466154
Restlessness 20.30 13.12 33 18273 29420 63441296
Ventricular arrhythmia 20.17 13.12 13 18293 3815 63466901
Hepatic lesion 19.72 13.12 14 18292 4811 63465905
Febrile neutropenia 19.57 13.12 5 18301 118444 63352272
Dyshidrotic eczema 18.70 13.12 7 18299 627 63470089
Psychotic symptom 18.41 13.12 9 18297 1552 63469164
Sinobronchitis 18.15 13.12 5 18301 166 63470550
Choking 18.04 13.12 18 18288 9861 63460855
Somnambulism 17.99 13.12 14 18292 5529 63465187
Breast adenoma 17.86 13.12 4 18302 55 63470661
Product prescribing error 17.50 13.12 29 18277 26260 63444456
Abdominal discomfort 17.42 13.12 42 18264 320843 63149873
Blood test abnormal 17.40 13.12 22 18284 15607 63455109
Wound 17.38 13.12 13 18293 163250 63307466
Defaecation disorder 17.28 13.12 7 18299 774 63469942
Allergic oedema 16.89 13.12 7 18299 821 63469895
Blood pressure systolic increased 16.64 13.12 40 18266 47357 63423359
Seizure 16.60 13.12 79 18227 132555 63338161
Psoriasis 16.59 13.12 59 18247 86898 63383818
Microcephaly 16.03 13.12 7 18299 933 63469783
Quality of life decreased 16.00 13.12 16 18290 8787 63461929
Restless legs syndrome 15.92 13.12 23 18283 18508 63452208
Scratch 15.91 13.12 14 18292 6551 63464165
Pyrexia 15.72 13.12 76 18230 470402 63000314
Osteoporotic fracture 15.61 13.12 11 18295 3735 63466981
Eczema 15.61 13.12 31 18275 32260 63438456
Mastocytosis 15.59 13.12 6 18300 580 63470136
Papule 15.55 13.12 13 18293 5678 63465038
Blood pressure increased 15.12 13.12 89 18217 161973 63308743
Bradycardia 15.12 13.12 51 18255 73176 63397540
Myofascial pain syndrome 15.07 13.12 9 18297 2309 63468407
Junctional ectopic tachycardia 15.00 13.12 4 18302 117 63470599
Iritis 14.83 13.12 10 18296 3165 63467551
Sedation complication 14.67 13.12 19 18287 13803 63456913
Brain oedema 14.27 13.12 19 18287 14176 63456540
Impaired work ability 14.02 13.12 21 18285 17454 63453262
Suspected suicide 13.94 13.12 13 18293 6555 63464161
Anaphylactic reaction 13.61 13.12 46 18260 66054 63404662
Stomatitis 13.57 13.12 12 18294 138713 63332003
Tinnitus 13.52 13.12 31 18275 35597 63435119
Product use issue 13.49 13.12 27 18279 220493 63250223
Treatment failure 13.39 13.12 23 18283 199020 63271696
Hypothermia 13.38 13.12 18 18288 13563 63457153
Arthropathy 13.32 13.12 30 18276 234762 63235954
Angioedema 13.26 13.12 37 18269 47928 63422788
Arrhythmia 13.19 13.12 32 18274 38108 63432608

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
Completed suicide 386.14 17.26 258 8140 97910 34850623
Toxicity to various agents 207.46 17.26 247 8151 200115 34748418
Needle fatigue 154.35 17.26 37 8361 844 34947689
Relapsing-remitting multiple sclerosis 147.90 17.26 37 8361 1013 34947520
Gait spastic 146.32 17.26 37 8361 1059 34947474
Drug abuse 136.24 17.26 142 8256 98954 34849579
Hypertonic bladder 126.86 17.26 37 8361 1827 34946706
Monoparesis 118.46 17.26 37 8361 2309 34946224
Muscle spasticity 85.26 17.26 37 8361 5851 34942682
Central nervous system lesion 81.95 17.26 37 8361 6426 34942107
Micturition urgency 81.61 17.26 37 8361 6488 34942045
Nocturia 79.84 17.26 42 8356 10168 34938365
Pollakiuria 75.17 17.26 51 8347 19623 34928910
Memory impairment 68.37 17.26 67 8331 43251 34905282
Movement disorder 64.81 17.26 39 8359 12209 34936324
Multiple sclerosis relapse 59.79 17.26 38 8360 13095 34935438
Erectile dysfunction 59.31 17.26 45 8353 20592 34927941
Ataxia 57.94 17.26 38 8360 13815 34934718
Insomnia 54.56 17.26 93 8305 103814 34844719
Pulmonary oedema 44.59 17.26 56 8342 47473 34901060
Dysarthria 42.62 17.26 47 8351 34735 34913798
Brugada syndrome 41.97 17.26 13 8385 788 34947745
Anxiety 38.37 17.26 78 8320 99350 34849183
Brain oedema 35.06 17.26 28 8370 13793 34934740
Balance disorder 30.57 17.26 43 8355 40611 34907922
Reduced facial expression 30.38 17.26 11 8387 1080 34947453
Soft tissue haemorrhage 29.97 17.26 7 8391 142 34948391
Illness anxiety disorder 28.77 17.26 7 8391 170 34948363
Cardio-respiratory arrest 28.33 17.26 49 8349 55224 34893309
Somatic symptom disorder 27.11 17.26 9 8389 682 34947851
Hydrocholecystis 26.20 17.26 8 8390 462 34948071
Hypoaesthesia 25.84 17.26 50 8348 61394 34887139
Dermatitis atopic 23.16 17.26 15 8383 5332 34943201
Helplessness 23.02 17.26 5 8393 72 34948461
Dissociation 22.64 17.26 10 8388 1648 34946885
Dissociative disorder 22.02 17.26 7 8391 462 34948071
Disease prodromal stage 21.42 17.26 4 8394 25 34948508
Toxic cardiomyopathy 21.30 17.26 6 8392 261 34948272
Pruritus 20.74 17.26 78 8320 141903 34806630
Thrombocytopenia 20.60 17.26 6 8392 156241 34792292
Overdose 20.51 17.26 58 8340 91001 34857532
Drug dependence 20.29 17.26 27 8371 24190 34924343
Pancreatic disorder 18.98 17.26 9 8389 1745 34946788
Depressed mood 18.48 17.26 23 8375 19294 34929239
Acute kidney injury 18.46 17.26 28 8370 304960 34643573
Wrong patient received product 18.17 17.26 10 8388 2644 34945889
Crime 17.74 17.26 4 8394 69 34948464
Measles 17.60 17.26 5 8393 224 34948309
Bradyphrenia 17.27 17.26 12 8386 4786 34943747
Fall 17.27 17.26 95 8303 202790 34745743

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
Completed suicide 1005.52 13.79 705 21896 245062 79476725
Toxicity to various agents 590.60 13.79 658 21943 420882 79300905
Drug abuse 207.85 13.79 243 22358 162448 79559339
Cardio-respiratory arrest 180.04 13.79 186 22415 108324 79613463
Respiratory depression 155.12 13.79 97 22504 27533 79694254
Needle fatigue 137.46 13.79 35 22566 867 79720920
Gait spastic 127.64 13.79 35 22566 1162 79720625
Relapsing-remitting multiple sclerosis 119.39 13.79 35 22566 1484 79720303
Hypertonic bladder 98.30 13.79 39 22562 4162 79717625
Respiratory arrest 95.99 13.79 99 22502 57451 79664336
Monoparesis 94.21 13.79 36 22565 3475 79718312
Insomnia 92.18 13.79 210 22391 244960 79476827
Chronic spontaneous urticaria 73.83 13.79 23 22578 1201 79720586
Cardiac arrest 69.78 13.79 152 22449 171944 79549843
Overdose 66.11 13.79 155 22446 184051 79537736
Nocturia 61.97 13.79 42 22559 13639 79708148
Erectile dysfunction 57.04 13.79 41 22560 14623 79707164
Urticaria 56.04 13.79 146 22455 185055 79536732
Micturition urgency 55.35 13.79 38 22563 12603 79709184
Anxiety 54.04 13.79 174 22427 248338 79473449
Ataxia 48.99 13.79 47 22554 24992 79696795
Electrocardiogram QRS complex prolonged 48.46 13.79 33 22568 10800 79710987
Suicide attempt 47.85 13.79 85 22516 82847 79638940
Central nervous system lesion 46.63 13.79 35 22566 13333 79708454
Decreased bronchial secretion 45.70 13.79 9 22592 64 79721723
Depressed level of consciousness 44.54 13.79 90 22511 96562 79625225
Depression 43.72 13.79 148 22453 216642 79505145
Skin plaque 41.69 13.79 30 22571 10715 79711072
Self esteem decreased 40.86 13.79 14 22587 988 79720799
Poisoning 39.48 13.79 42 22559 25230 79696557
Death 39.45 13.79 285 22316 566229 79155558
Dermatitis atopic 38.84 13.79 28 22573 10028 79711759
Pollakiuria 38.28 13.79 50 22551 37267 79684520
Muscle spasticity 37.71 13.79 38 22563 21437 79700350
Suicidal ideation 37.47 13.79 73 22528 76267 79645520
Sleep-related eating disorder 37.20 13.79 12 22589 702 79721085
Febrile neutropenia 36.75 13.79 10 22591 230989 79490798
Memory impairment 35.75 13.79 90 22511 111644 79610143
Pruritus 34.99 13.79 211 22390 394437 79327350
Brugada syndrome 34.31 13.79 13 22588 1225 79720562
Illness anxiety disorder 34.29 13.79 9 22592 252 79721535
Exposure via ingestion 33.73 13.79 20 22581 5154 79716633
Thrombocytopenia 32.98 13.79 17 22584 265242 79456545
Brain oedema 32.61 13.79 38 22563 25225 79696562
Intentional overdose 32.50 13.79 84 22517 105876 79615911
Coma 32.12 13.79 81 22520 100568 79621219
Infusion related reaction 31.34 13.79 13 22588 230224 79491563
Movement disorder 30.28 13.79 38 22563 27221 79694566
Joint swelling 28.45 13.79 24 22577 288622 79433165
Diverticulum oesophageal 28.11 13.79 7 22594 158 79721629
Pyrexia 27.13 13.79 100 22501 678609 79043178
Lipohypertrophy 27.12 13.79 10 22591 874 79720913
Dyshidrotic eczema 26.85 13.79 9 22592 594 79721193
Mandibular mass 26.05 13.79 7 22594 215 79721572
Neutropenia 25.89 13.79 26 22575 287684 79434103
Bradycardia 25.09 13.79 90 22511 135467 79586320
Therapeutic product effect increased 24.73 13.79 11 22590 1560 79720227
Blood glucose fluctuation 24.43 13.79 18 22583 6664 79715123
Obsessive-compulsive personality disorder 24.37 13.79 6 22595 129 79721658
Hydrocholecystis 23.91 13.79 8 22593 525 79721262
Feeling guilty 23.64 13.79 9 22592 859 79720928
Maternal exposure during pregnancy 23.49 13.79 5 22596 136533 79585254
Restlessness 23.47 13.79 45 22556 46447 79675340
Dizziness 23.47 13.79 240 22361 526201 79195586
Multiple sclerosis relapse 23.44 13.79 45 22556 46488 79675299
Product prescribing error 23.39 13.79 44 22557 44769 79677018
Dysarthria 23.24 13.79 56 22545 67566 79654221
Acute kidney injury 23.13 13.79 73 22528 519331 79202456
Scratch 22.92 13.79 19 22582 8344 79713443
Somatic symptom disorder 22.50 13.79 12 22589 2525 79719262
Helplessness 22.48 13.79 7 22594 365 79721422
Rheumatoid arthritis 22.22 13.79 16 22585 208454 79513333
Depressed mood 22.15 13.79 45 22556 48435 79673352
Somnolence 21.93 13.79 129 22472 238852 79482935
Stress 21.28 13.79 60 22541 79552 79642235
Inadequate analgesia 20.46 13.79 14 22587 4615 79717172
Intentional product misuse 20.07 13.79 66 22535 95099 79626688
Pulmonary congestion 19.95 13.79 31 22570 27069 79694718
Disease progression 19.85 13.79 14 22587 184348 79537439
Drug interaction 19.80 13.79 192 22409 414991 79306796
Renal impairment 19.77 13.79 10 22591 157773 79564014
Panic attack 19.67 13.79 29 22572 24187 79697600
Spinal disorder 19.58 13.79 19 22582 10241 79711546
Alanine aminotransferase increased 19.35 13.79 11 22590 162559 79559228
Bradypnoea 19.25 13.79 15 22586 6037 79715750
Suspected suicide 19.09 13.79 19 22582 10557 79711230
Drug intolerance 18.40 13.79 29 22572 264090 79457697
Synovitis 18.22 13.79 10 22591 150724 79571063
Anaemia 18.12 13.79 65 22536 444950 79276837
Breast adenoma 17.93 13.79 4 22597 55 79721732
Toxic cardiomyopathy 17.70 13.79 6 22595 410 79721377
Interstitial lung disease 17.66 13.79 5 22596 112595 79609192
Soft tissue haemorrhage 17.60 13.79 6 22595 417 79721370
Allergic oedema 17.31 13.79 7 22594 784 79721003
Disease prodromal stage 17.30 13.79 4 22597 65 79721722
Mental impairment 17.22 13.79 24 22577 19012 79702775
Dissociative disorder 17.06 13.79 7 22594 814 79720973
Crime 17.03 13.79 4 22597 70 79721717
Contraindicated product administered 16.91 13.79 12 22589 157526 79564261
Libido decreased 16.52 13.79 13 22588 5308 79716479
Major depression 15.96 13.79 16 22585 8964 79712823
Platelet count decreased 15.95 13.79 19 22582 194645 79527142
Hepatic enzyme increased 15.86 13.79 17 22584 182593 79539194
Pulmonary oedema 15.82 13.79 58 22543 88196 79633591
Off label use 15.73 13.79 173 22428 907042 78814745
Somnambulism 15.69 13.79 13 22588 5708 79716079
Hepatic lesion 15.41 13.79 14 22587 6945 79714842
Acute lung injury 15.20 13.79 10 22591 3090 79718697
Dissociation 15.08 13.79 11 22590 4010 79717777
Neutrophil count decreased 15.06 13.79 4 22597 93955 79627832
Stomatitis 14.70 13.79 12 22589 146745 79575042
Papule 14.67 13.79 14 22587 7393 79714394
Feeling abnormal 14.63 13.79 86 22515 159113 79562674
Osteoporotic fracture 14.56 13.79 11 22590 4229 79717558
Therapeutic product effect decreased 14.51 13.79 15 22586 163848 79557939
Arrhythmia 14.29 13.79 44 22557 61228 79660559
Measles 14.03 13.79 5 22596 396 79721391
Psychotic symptom 13.96 13.79 9 22592 2688 79719099

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.66 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
5% DOXEPIN HYDROCHLORIDE TEVA PHARMS A215408 Feb. 17, 2023 RX CREAM TOPICAL Aug. 16, 2023 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent noradrenaline transporter Transporter INHIBITOR Kd 7.53 WOMBAT-PK CHEMBL
Histamine H1 receptor GPCR ANTAGONIST Ki 9.75 WOMBAT-PK DRUG LABEL
Alpha-2A adrenergic receptor GPCR Ki 6.30 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.58 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter INHIBITOR Kd 7.17 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 6.54 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR EC50 7.45 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR EC50 7.20 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR EC50 7 WOMBAT-PK
5-hydroxytryptamine receptor 6 GPCR Ki 6.98 CHEMBL
5-hydroxytryptamine receptor 7 GPCR WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 7.63 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR IC50 7.21 WOMBAT-PK
D(3) dopamine receptor GPCR Ki 6.33 DRUG MATRIX
D(1A) dopamine receptor GPCR EC50 6.50 WOMBAT-PK
Histamine H4 receptor GPCR EC50 6.79 WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR Ki 7.42 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 6.80 WOMBAT-PK
Muscarinic acetylcholine receptor M3 GPCR Ki 7.28 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR Ki 7.09 WOMBAT-PK
Muscarinic acetylcholine receptor M5 GPCR Ki 7.13 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR IC50 7 WOMBAT-PK
Alpha-1D adrenergic receptor GPCR Ki 7.37 DRUG MATRIX
Solute carrier family 22 member 1 Transporter IC50 4.95 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 4.89 WOMBAT-PK
Histamine H2 receptor GPCR Ki 5.74 DRUG MATRIX
D(2) dopamine receptor GPCR EC50 6.50 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 7.48 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 11 CHEMBL
Serotonin (5-HT) receptor GPCR IC50 6.70 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
doxepin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-9609 CREAM 50 mg TOPICAL ANDA 18 sections
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 0527-4062 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 0527-4063 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 0527-4064 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 0527-4065 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 0527-4066 CAPSULE 100 mg ORAL ANDA 15 sections