naloxone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists related to normorphine 1878 465-65-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • naloxone hydrochloride dihydrate
  • naloxone hydrochloride hydrate
  • naloxone hydrobromide
  • evzio
  • naloxone
  • l-naloxone
  • (-)-Naloxone
  • naloxone hydrochloride
  • naloxone HCl
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
  • Molecular weight: 327.38
  • Formula: C19H21NO4
  • CLOGP: 0.16
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 70
  • ALOGS: -1.76
  • ROTB: 2

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
75 mg O

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) 0.31 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 2 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.70 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 23 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.54 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 13, 1971 FDA ADAPT

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
Drug withdrawal syndrome 519.94 11.86 278 28385 27106 46630293
Drug dependence 292.88 11.86 171 28492 19730 46637669
Drug withdrawal syndrome neonatal 283.88 11.86 86 28577 1842 46655557
Intentional underdose 263.84 11.86 81 28582 1817 46655582
Product preparation error 239.46 11.86 91 28572 3948 46653451
General physical health deterioration 202.56 11.86 299 28364 115470 46541929
Product solubility abnormal 192.34 11.86 53 28610 799 46656600
Product use issue 175.01 11.86 251 28412 94393 46563006
Maternal exposure during pregnancy 172.37 11.86 260 28403 102289 46555110
Drug abuse 171.65 11.86 203 28460 63205 46594194
Product dosage form issue 164.95 11.86 31 28632 60 46657339
Substance abuse 164.28 11.86 70 28593 4097 46653302
Drug screen negative 155.50 11.86 38 28625 345 46657054
Product substitution issue 135.86 11.86 95 28568 14936 46642463
Withdrawal syndrome 128.60 11.86 99 28564 18035 46639364
Nausea 127.79 11.86 787 27876 686667 45970732
Exposure during pregnancy 110.27 11.86 220 28443 107992 46549407
Vomiting 108.76 11.86 556 28107 452238 46205161
Oral mucosal blistering 102.51 11.86 53 28610 4807 46652592
Foetal exposure during pregnancy 97.64 11.86 107 28556 30640 46626759
Abortion spontaneous 94.47 11.86 125 28538 43521 46613878
Wrong technique in product usage process 92.76 11.86 139 28524 54283 46603116
Tongue blistering 83.36 11.86 32 28631 1426 46655973
Inappropriate schedule of product administration 80.87 11.86 144 28519 64869 46592530
Jaundice neonatal 79.68 11.86 27 28636 836 46656563
Premature delivery 73.91 11.86 79 28584 21990 46635409
Oral administration complication 72.15 11.86 17 28646 130 46657269
Miosis 71.91 11.86 47 28616 6610 46650789
Product prescribing error 71.12 11.86 74 28589 19973 46637426
Overdose 66.68 11.86 174 28489 101805 46555594
Rheumatoid arthritis 63.82 11.86 34 28629 240181 46417218
Selective abortion 54.37 11.86 14 28649 160 46657239
Pallor 52.67 11.86 68 28595 23098 46634301
Drug ineffective 51.59 11.86 228 28435 677610 45979789
Joint swelling 46.34 11.86 22 28641 166051 46491348
Stomatitis 46.12 11.86 118 28545 68179 46589220
Respiratory depression 45.10 11.86 45 28618 11555 46645844
Exposure via breast milk 44.48 11.86 20 28643 1332 46656067
Maternal exposure during breast feeding 43.75 11.86 25 28638 2764 46654635
Drug detoxification 42.76 11.86 12 28651 194 46657205
Drug diversion 42.54 11.86 17 28646 844 46656555
Drug use disorder 41.52 11.86 24 28639 2711 46654688
Euphoric mood 40.94 11.86 28 28635 4244 46653155
Toxicity to various agents 40.48 11.86 245 28418 211521 46445878
Product formulation issue 39.23 11.86 15 28648 661 46656738
Hyperhidrosis 38.90 11.86 132 28531 89176 46568223
Retching 37.27 11.86 43 28620 13014 46644385
Product monitoring error 37.22 11.86 20 28643 1961 46655438
Fatigue 35.97 11.86 223 28440 608474 46048925
Accidental exposure to product by child 35.00 11.86 16 28647 1107 46656292
Abortion induced 34.82 11.86 37 28626 10223 46647176
Constipation 32.35 11.86 200 28463 173897 46483502
Fracture 32.31 11.86 45 28618 16426 46640973
Systemic infection 31.92 11.86 13 28650 678 46656721
Bradypnoea 31.71 11.86 21 28642 3018 46654381
Haematochezia 30.91 11.86 70 28593 37423 46619976
Sinusitis 30.73 11.86 21 28642 129747 46527652
Alopecia 30.30 11.86 33 28630 162381 46495018
Migraine 30.05 11.86 103 28560 69923 46587476
Thymus disorder 29.51 11.86 9 28654 197 46657202
Drug screen positive 29.24 11.86 22 28641 3869 46653530
Poor feeding infant 29.22 11.86 9 28654 204 46657195
Respiratory rate decreased 28.89 11.86 20 28643 3090 46654309
Somnolence 27.94 11.86 178 28485 156343 46501056
Synovitis 26.94 11.86 3 28660 61072 46596327
Rhesus incompatibility 26.80 11.86 7 28656 85 46657314
Unresponsive to stimuli 26.44 11.86 60 28603 32114 46625285
Glossitis 25.98 11.86 18 28645 2785 46654614
Arthralgia 25.61 11.86 126 28537 364477 46292922
Intentional product misuse 25.41 11.86 75 28588 47053 46610346
Insurance issue 25.40 11.86 15 28648 1763 46655636
Thyroid stimulating immunoglobulin increased 25.01 11.86 7 28656 112 46657287
Sopor 24.73 11.86 44 28619 19784 46637615
Faecaloma 24.63 11.86 27 28636 7725 46649674
Arrhythmia 24.34 11.86 61 28602 34780 46622619
Foreign body reaction 24.12 11.86 6 28657 59 46657340
Nasopharyngitis 23.85 11.86 36 28627 153962 46503437
Tongue erythema 23.82 11.86 8 28655 241 46657158
Treatment failure 23.49 11.86 14 28649 93073 46564326
Yawning 23.15 11.86 11 28652 831 46656568
Drug effect less than expected 22.96 11.86 6 28657 73 46657326
Product dose omission issue 22.77 11.86 43 28620 168477 46488922
Systemic lupus erythematosus 22.65 11.86 6 28657 65174 46592225
Alcohol abuse 22.64 11.86 15 28648 2157 46655242
Glomerulonephritis chronic 22.51 11.86 7 28656 164 46657235
Infusion related reaction 21.87 11.86 18 28645 101190 46556209
White blood cell count decreased 21.83 11.86 22 28641 112209 46545190
Musculoskeletal stiffness 21.71 11.86 17 28646 97976 46559423
Osteochondrosis 21.68 11.86 11 28652 959 46656440
Drug hypersensitivity 21.60 11.86 77 28586 243748 46413651
Cough 20.87 11.86 72 28591 230177 46427222
Spinal cord paralysis 20.80 11.86 5 28658 42 46657357
Pyometra 20.38 11.86 6 28657 116 46657283
Restlessness 20.31 11.86 47 28616 25477 46631922
Plantar fascial fibromatosis 19.15 11.86 6 28657 144 46657255
Bacterial test 19.12 11.86 11 28652 1232 46656167
Myosclerosis 18.96 11.86 6 28657 149 46657250
Lordosis 18.90 11.86 7 28656 282 46657117
Bradyphrenia 18.59 11.86 21 28642 6209 46651190
Tongue discomfort 17.87 11.86 12 28651 1765 46655634
Depressed level of consciousness 17.86 11.86 67 28596 47502 46609897
Gastrointestinal tract adenoma 17.80 11.86 7 28656 333 46657066
Asthma 17.73 11.86 18 28645 91524 46565875
Rhonchi 17.71 11.86 13 28650 2202 46655197
Oral discomfort 17.61 11.86 23 28640 7895 46649504
Herpes zoster 17.42 11.86 10 28653 67862 46589537
Apnoea 17.40 11.86 22 28641 7317 46650082
Spasmodic dysphonia 17.37 11.86 5 28658 89 46657310
Orthostatic intolerance 17.18 11.86 10 28653 1144 46656255
Delirium 17.06 11.86 56 28607 37172 46620227
Dependence 16.96 11.86 12 28651 1919 46655480
Shoplifting 16.65 11.86 3 28660 4 46657395
Infertility 16.48 11.86 8 28655 634 46656765
Rash 16.43 11.86 140 28523 356372 46301027
Multiple lentigines syndrome 16.41 11.86 6 28657 233 46657166
Neuropathy peripheral 16.36 11.86 19 28644 90874 46566525
Febrile infection 16.35 11.86 10 28653 1253 46656146
Electrolyte imbalance 16.29 11.86 34 28629 17192 46640207
Tachyphylaxis 16.20 11.86 6 28657 242 46657157
Contusion 16.06 11.86 18 28645 87469 46569930
Anaemia folate deficiency 16.03 11.86 6 28657 249 46657150
Anti-thyroid antibody positive 15.98 11.86 7 28656 438 46656961
Disturbance in attention 15.85 11.86 49 28614 31511 46625888
Platelet count decreased 15.85 11.86 23 28640 100001 46557398
Lower respiratory tract infection 15.81 11.86 7 28656 55082 46602317
Tachypnoea 15.58 11.86 30 28633 14321 46643078
Dental caries 15.55 11.86 25 28638 10354 46647045
Disease progression 15.47 11.86 20 28643 91280 46566119
Nail avulsion 15.43 11.86 4 28659 47 46657352
Withdrawal hypertension 15.37 11.86 5 28658 136 46657263
Coeliac artery compression syndrome 15.33 11.86 5 28658 137 46657262
Swollen tongue 15.26 11.86 46 28617 29186 46628213
Spinal cord infarction 15.16 11.86 6 28657 290 46657109
Pneumobilia 14.75 11.86 5 28658 155 46657244
Cardiac failure congestive 14.63 11.86 21 28642 91729 46565670
Death 14.47 11.86 134 28529 335414 46321985
Gastric antral vascular ectasia 14.18 11.86 7 28656 575 46656824
Metastatic gastric cancer 14.17 11.86 5 28658 175 46657224
Chemotherapeutic drug level increased 14.04 11.86 5 28658 180 46657219
Gamma-glutamyltransferase increased 13.88 11.86 47 28616 31693 46625706
Product substitution 13.82 11.86 3 28660 15 46657384
Reticulocyte count increased 13.54 11.86 7 28656 634 46656765
Acquired claw toe 13.54 11.86 5 28658 200 46657199
Lichenification 13.44 11.86 6 28657 393 46657006
Therapy change 13.26 11.86 16 28647 5074 46652325
Leukoplakia 13.10 11.86 4 28659 88 46657311
Acute hepatitis C 12.97 11.86 4 28659 91 46657308
Premature baby 12.95 11.86 32 28631 18080 46639319
Bradykinesia 12.93 11.86 14 28649 3952 46653447
Injection site erythema 12.92 11.86 16 28647 74411 46582988
Arthropathy 12.91 11.86 20 28643 84680 46572719
Hypocoagulable state 12.82 11.86 8 28655 1039 46656360
Oral mucosal erythema 12.71 11.86 9 28654 1441 46655958
Paranasal sinus inflammation 12.59 11.86 5 28658 244 46657155
Headache 12.52 11.86 383 28280 477969 46179430
Gravitational oedema 12.45 11.86 8 28655 1092 46656307
Gastrointestinal hypomotility 12.43 11.86 8 28655 1096 46656303
Thyroxine free increased 12.41 11.86 7 28656 755 46656644
Dystrophic calcification 12.36 11.86 4 28659 107 46657292
Allergic oedema 12.30 11.86 7 28656 768 46656631
Diabetic retinal oedema 12.25 11.86 6 28657 485 46656914
Piloerection 12.22 11.86 5 28658 264 46657135
Cystic lymphangioma 12.20 11.86 3 28660 28 46657371
Pain in extremity 12.16 11.86 101 28562 258579 46398820
Thought blocking 12.12 11.86 4 28659 114 46657285
Haematemesis 12.02 11.86 42 28621 28764 46628635
Hepatitis C 12.00 11.86 17 28646 6301 46651098
Pneumonia 11.98 11.86 161 28502 376159 46281240
Gastroenteritis radiation 11.94 11.86 6 28657 512 46656887
Oral disorder 11.94 11.86 19 28644 7803 46649596
Adverse event 11.89 11.86 47 28616 34137 46623262
Macular scar 11.89 11.86 4 28659 121 46657278

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
Drug withdrawal syndrome 793.25 12.90 363 23519 19446 29909150
Drug dependence 478.67 12.90 264 23618 21031 29907565
Intentional underdose 311.74 12.90 81 23801 723 29927873
Drug screen negative 256.96 12.90 56 23826 208 29928388
Drug abuse 223.40 12.90 300 23582 81772 29846824
Drug withdrawal syndrome neonatal 216.35 12.90 85 23797 3090 29925506
Overdose 205.09 12.90 292 23590 84045 29844551
Product use issue 202.51 12.90 215 23667 45801 29882795
Withdrawal syndrome 197.87 12.90 119 23763 11131 29917465
Product substitution issue 197.09 12.90 114 23768 9921 29918675
Product solubility abnormal 196.26 12.90 52 23830 504 29928092
Product preparation error 195.55 12.90 67 23815 1639 29926957
Substance abuse 165.48 12.90 90 23792 6950 29921646
Drug detoxification 164.24 12.90 38 23844 196 29928400
Nausea 126.78 12.90 519 23363 296438 29632158
Euphoric mood 124.04 12.90 63 23819 4227 29924369
Intentional product misuse 105.40 12.90 134 23748 34533 29894063
Inappropriate schedule of product administration 89.72 12.90 133 23749 39595 29889001
Vomiting 87.11 12.90 376 23506 219442 29709154
Maternal exposure during breast feeding 84.85 12.90 36 23846 1596 29927000
Product prescribing error 80.34 12.90 82 23800 16651 29911945
Wrong technique in product usage process 80.17 12.90 111 23771 31044 29897552
Accidental exposure to product by child 79.68 12.90 34 23848 1529 29927067
Oral administration complication 65.05 12.90 15 23867 76 29928520
Respiratory depression 60.05 12.90 59 23823 11444 29917152
Product dosage form issue 59.28 12.90 13 23869 50 29928546
Unresponsive to stimuli 57.55 12.90 87 23795 26332 29902264
Drug diversion 57.08 12.90 23 23859 893 29927703
Foetal exposure during pregnancy 56.91 12.90 104 23778 36767 29891829
Intentional product use issue 56.52 12.90 103 23779 36337 29892259
Jaundice neonatal 56.37 12.90 24 23858 1073 29927523
Drug screen positive 56.01 12.90 38 23844 4369 29924227
Toxicity to various agents 53.23 12.90 280 23602 176903 29751693
Oral mucosal blistering 51.14 12.90 26 23856 1747 29926849
Headache 50.64 12.90 282 23600 182024 29746572
General physical health deterioration 47.39 12.90 181 23701 99763 29828833
Hyperhidrosis 47.38 12.90 139 23743 66951 29861645
Miosis 46.50 12.90 43 23839 7733 29920863
Product formulation issue 45.99 12.90 17 23865 521 29928075
Tongue blistering 45.19 12.90 14 23868 246 29928350
Product colour issue 37.94 12.90 14 23868 427 29928169
Pneumomediastinum 36.89 12.90 21 23861 1770 29926826
Drug use disorder 36.57 12.90 26 23856 3222 29925374
Purpura fulminans 36.35 12.90 10 23872 113 29928483
Tremor neonatal 35.91 12.90 13 23869 375 29928221
Alcohol abuse 34.75 12.90 31 23851 5322 29923274
Product taste abnormal 34.02 12.90 17 23865 1101 29927495
Fracture 33.59 12.90 32 23850 5974 29922622
Anxiety 33.34 12.90 151 23731 89720 29838876
Product monitoring error 32.11 12.90 19 23863 1722 29926874
Cardiac failure congestive 31.38 12.90 14 23868 84393 29844203
Somnolence 31.12 12.90 156 23726 96607 29831989
Thermophobia 29.19 12.90 8 23874 89 29928507
Wound 28.66 12.90 42 23840 12360 29916236
Foreign body reaction 26.78 12.90 7 23875 64 29928532
Cerebral congestion 26.60 12.90 6 23876 27 29928569
Pneumonia 25.65 12.90 159 23723 334147 29594449
Disease progression 25.63 12.90 16 23866 79858 29848738
Therapy naive 24.57 12.90 5 23877 12 29928584
Accessory spleen 24.49 12.90 8 23874 168 29928428
Hepatitis C 23.94 12.90 40 23842 13165 29915431
Sopor 23.64 12.90 36 23846 10955 29917641
Platelet count decreased 23.57 12.90 30 23852 106099 29822497
Pain 23.37 12.90 225 23657 172416 29756180
Cerebrovascular accident 22.56 12.90 20 23862 83457 29845139
Sedation 22.54 12.90 44 23838 16329 29912267
Skull fracture 22.16 12.90 12 23870 917 29927679
Myocardial infarction 21.73 12.90 42 23840 125583 29803013
Agitation 21.66 12.90 93 23789 53980 29874616
Yawning 21.59 12.90 10 23872 547 29928049
Piloerection 20.63 12.90 7 23875 166 29928430
Retching 20.58 12.90 25 23857 6143 29922453
Counterfeit product administered 20.24 12.90 7 23875 176 29928420
Gastrointestinal haemorrhage 20.23 12.90 22 23860 83424 29845172
Feeling abnormal 20.02 12.90 94 23788 56662 29871934
Dental caries 19.97 12.90 21 23861 4410 29924186
Pulmonary fistula 19.83 12.90 5 23877 39 29928557
Prescribed overdose 19.79 12.90 29 23853 8532 29920064
Premature baby 19.60 12.90 42 23840 16649 29911947
Dependence 19.07 12.90 12 23870 1214 29927382
Hypoxic-ischaemic encephalopathy 18.99 12.90 21 23861 4666 29923930
Hepatic function abnormal 18.96 12.90 5 23877 41940 29886656
Exposure via breast milk 18.66 12.90 13 23869 1559 29927037
Rheumatoid arthritis 18.45 12.90 5 23877 41192 29887404
Acute on chronic liver failure 18.32 12.90 6 23876 127 29928469
Neutropenia 18.14 12.90 48 23834 128492 29800104
Drug effect less than expected 17.98 12.90 5 23877 59 29928537
Accidental exposure to product 17.49 12.90 30 23852 10085 29918511
Adrenocorticotropic hormone deficiency 17.40 12.90 8 23874 430 29928166
Multiple cardiac defects 17.26 12.90 5 23877 69 29928527
Hypopnoea 17.01 12.90 11 23871 1167 29927429
Stoma site haemorrhage 16.82 12.90 10 23872 914 29927682
Disturbance in attention 16.71 12.90 47 23835 22082 29906514
Alanine aminotransferase increased 16.48 12.90 21 23861 74255 29854341
Suicidal ideation 15.94 12.90 64 23818 36050 29892546
Potentiating drug interaction 15.82 12.90 19 23863 4612 29923984
Neuropathy peripheral 15.56 12.90 20 23862 70455 29858141
Restless legs syndrome 15.48 12.90 23 23859 6849 29921747
Acute kidney injury 15.37 12.90 142 23740 273700 29654896
Hypogonadism 15.15 12.90 11 23871 1408 29927188
Substance use disorder 15.09 12.90 5 23877 110 29928486
Gonadotrophin deficiency 14.81 12.90 4 23878 42 29928554
Road traffic accident 14.64 12.90 38 23844 17033 29911563
White blood cell count decreased 14.56 12.90 28 23854 83919 29844677
Bone marrow failure 14.55 12.90 3 23879 29782 29898814
Interstitial lung disease 14.44 12.90 16 23866 60181 29868415
Libido decreased 14.41 12.90 18 23864 4548 29924048
Victim of homicide 14.19 12.90 5 23877 133 29928463
Aspartate aminotransferase increased 14.00 12.90 18 23864 63404 29865192
Non-cardiogenic pulmonary oedema 13.98 12.90 8 23874 681 29927915
Therapeutic product effect prolonged 13.85 12.90 6 23876 280 29928316
Renal impairment 13.82 12.90 29 23853 84155 29844441
Lactic acidosis 13.58 12.90 4 23878 31209 29897387
Hypercapnia 13.58 12.90 16 23866 3808 29924788
Selective eating disorder 13.48 12.90 11 23871 1673 29926923
Breech presentation 13.38 12.90 5 23877 158 29928438
Diarrhoea 13.35 12.90 187 23695 333916 29594680
Low birth weight baby 13.21 12.90 20 23862 6056 29922540
Sepsis 13.15 12.90 66 23816 146329 29782267

Pharmacologic Action:

SourceCodeDescription
ATC A06AH04 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Peripheral opioid receptor antagonists
ATC N02AA53 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Natural opium alkaloids
ATC N02AA55 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Natural opium alkaloids
ATC V03AB15 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes
FDA MoA N0000000154 Opioid Antagonists
FDA EPC N0000175691 Opioid Antagonist
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009292 Narcotic Antagonists
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35488 cns depressants
CHEBI has role CHEBI:50137 mu-opioid receptor antagonists
CHEBI has role CHEBI:90755 antidote to opioid overdose

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000
Opioid dependence indication 75544000 DOID:2559
Poisoning by opiate analgesic drug indication 241749009
Prevention of opioid abuse indication 426928008
Opiate-Induced Respiratory Depression indication
Suicidal thoughts contraindication 6471006
Dependent drug abuse contraindication 6525002
Alcohol withdrawal delirium contraindication 8635005
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Asthenia contraindication 13791008
Constipation contraindication 14760008 DOID:2089
Chronic disease of respiratory system contraindication 17097001
Mood swings contraindication 18963009
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Orthostatic hypotension contraindication 28651003
Hypercapnia contraindication 29596007
Torsades de pointes contraindication 31722008
Dehydration contraindication 34095006
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Paralytic ileus contraindication 55525008 DOID:8442
Chronic type B viral hepatitis contraindication 61977001
Ulcerative colitis contraindication 64766004 DOID:8577
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Cor pulmonale contraindication 83291003 DOID:8515
Opioid withdrawal contraindication 87132004
Pulmonary emphysema contraindication 87433001
Kidney disease contraindication 90708001 DOID:557
Disorder of biliary tract contraindication 105997008 DOID:9741
Prolonged QT interval contraindication 111975006
Acute abdominal pain contraindication 116290004
Neoplasm of brain contraindication 126952004 DOID:1319
Chronic hepatitis C contraindication 128302006
Seizure disorder contraindication 128613002
Liver function tests abnormal contraindication 166603001
Drug-induced psychosis contraindication 191483003 DOID:1742
Disease of liver contraindication 235856003 DOID:409
Morbid obesity contraindication 238136002 DOID:11981
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Exacerbation of asthma contraindication 281239006
Lesion of brain contraindication 301766008
Coma contraindication 371632003
Primary adrenocortical insufficiency contraindication 373662000
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Operation on gastrointestinal tract contraindication 386621005
Hypoxia contraindication 389086002
Respiratory insufficiency contraindication 409623005
Central nervous system depression contraindication 418072004
Dysfunction of sphincter of Oddi contraindication 430887001
Congenital long QT syndrome contraindication 442917000
Kyphoscoliosis with Respiratory Compromise contraindication
Pain in Opioid Naive Patients contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.31 acidic
pKa2 7.47 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR ANTAGONIST Ki 8.81 WOMBAT-PK CHEMBL
Kappa-type opioid receptor GPCR ANTAGONIST Ki 8.50 WOMBAT-PK
Cytochrome P450 2D6 Enzyme IC50 5.70 DRUG MATRIX
Adenosine receptor A3 GPCR IC50 8.80 CHEMBL
Delta-type opioid receptor GPCR ANTAGONIST Ki 7.27 WOMBAT-PK
C-C chemokine receptor type 5 GPCR Kd 7.98 CHEMBL
Kappa-type opioid receptor GPCR Ki 8.50 CHEMBL
Delta-type opioid receptor GPCR Kd 7.30 CHEMBL
Mu-type opioid receptor GPCR Ki 9.17 CHEMBL
Opioid receptor GPCR Kd 9 CHEMBL
Kappa-type opioid receptor GPCR Kd 9 CHEMBL
Delta-type opioid receptor GPCR Kd 7.74 CHEMBL
Mu-type opioid receptor GPCR IC50 8.30 CHEMBL
Mu-type opioid receptor GPCR Kd 9.40 CHEMBL
Kappa-type opioid receptor GPCR ANTAGONIST IC50 8.30 IUPHAR
Mu-type opioid receptor GPCR ANTAGONIST Ki 9 IUPHAR

External reference:

IDSource
D01340 KEGG_DRUG
357-08-4 SECONDARY_CAS_RN
4018057 VANDF
4019852 VANDF
C0027358 UMLSCUI
CHEBI:7459 CHEBI
5284596 PUBCHEM_CID
CHEMBL1718 ChEMBL_ID
CHEMBL80 ChEMBL_ID
D009270 MESH_DESCRIPTOR_UI
DB01183 DRUGBANK_ID
1638 IUPHAR_LIGAND_ID
1526 INN_ID
36B82AMQ7N UNII
1010598 RXNORM
2074 MMSL
221948 MMSL
27364 MMSL
5150 MMSL
71995 MMSL
d00311 MMSL
001614 NDDF
004661 NDDF
21518006 SNOMEDCT_US
371000220109 SNOMEDCT_US
372890007 SNOMEDCT_US
89018006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0188 TABLET 0.50 mg SUBLINGUAL ANDA 32 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0189 TABLET 2 mg SUBLINGUAL ANDA 32 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3154 TABLET 0.50 mg SUBLINGUAL ANDA 32 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3155 TABLET 2 mg SUBLINGUAL ANDA 32 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8765 FILM 0.50 mg SUBLINGUAL ANDA 34 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8766 FILM 1 mg SUBLINGUAL ANDA 34 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8767 FILM 2 mg SUBLINGUAL ANDA 34 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8768 FILM 3 mg SUBLINGUAL ANDA 34 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8005 TABLET 0.50 mg SUBLINGUAL ANDA 30 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8020 TABLET 2 mg SUBLINGUAL ANDA 30 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1212 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 21 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1215 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 21 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1219 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 21 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1782 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
Pentazocine and naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0591-0395 TABLET 0.50 mg ORAL ANDA 28 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0641-6132 INJECTION 0.40 mg INTRAMUSCULAR ANDA 23 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0904-7009 TABLET 0.50 mg SUBLINGUAL ANDA 32 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0904-7010 TABLET 2 mg SUBLINGUAL ANDA 32 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1202 FILM, SOLUBLE 0.50 mg SUBLINGUAL NDA 31 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1204 FILM, SOLUBLE 1 mg SUBLINGUAL NDA 31 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1208 FILM, SOLUBLE 2 mg SUBLINGUAL NDA 31 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1212 FILM, SOLUBLE 3 mg SUBLINGUAL NDA 31 sections
PENTAZOCINE HCL AND NULLLOXONE HCL HUMAN PRESCRIPTION DRUG LABEL 2 16590-556 TABLET 0.50 mg ORAL ANDA 13 sections
BUPRENORPHINE HYDROCHLORIDE and NULLLOXONE HYDROCHLORIDE DIHYDRATE HUMAN PRESCRIPTION DRUG LABEL 2 16729-549 TABLET 0.50 mg SUBLINGUAL ANDA 33 sections
BUPRENORPHINE HYDROCHLORIDE and NULLLOXONE HYDROCHLORIDE DIHYDRATE HUMAN PRESCRIPTION DRUG LABEL 2 16729-550 TABLET 2 mg SUBLINGUAL ANDA 33 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-041 INJECTION, SOLUTION 0.40 mg INTRAVENOUS ANDA 23 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-042 INJECTION, SOLUTION 0.40 mg INTRAVENOUS ANDA 23 sections
naloxone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 36000-308 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 21 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 42858-601 TABLET 0.50 mg SUBLINGUAL ANDA 31 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 42858-602 TABLET 2 mg SUBLINGUAL ANDA 31 sections