naloxone ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 ยตM/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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.482 Moderate 0.76
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.941 Moderate 0.76
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 20.845 10^-6 cm/s Moderate 0.76
dh-clint Dog hepatocyte intrinsic clearance 27.733 uL/min/10^6 cells Moderate 0.76
dppb Dog plasma protein binding (% unbound) 56.810 % Moderate 0.76
fcs-ppb Fetal calf serum protein binding (% unbound) 78.210 % Moderate 0.76
herg hERG pIC50 4.834 pIC50 Moderate 0.76
hh-clint Human hepatocyte intrinsic clearance 21.135 uL/min/10^6 cells Moderate 0.76
hlm-clint Human liver microsomal intrinsic clearance 13.614 uL/min/mg protein Moderate 0.76
hppb Human plasma protein binding (% unbound) 60.220 % Moderate 0.76
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,KDR,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 38
kinase-selectivity-class EIF2AK3,GRK2,MAP2K6,MAP3K14,TEK 5
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 3.673 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.018 Moderate 0.76
mh-clint Mouse hepatocyte intrinsic clearance 169.044 Moderate 0.76
mppb Mouse plasma protein binding (% unbound) 61.700 Moderate 0.76
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 11.912 Moderate 0.76
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
pppb Pig plasma protein binding (% unbound) 73.990 % Moderate 0.76
rat-kpuu-brain Rat brain Kpuu 0.066 % High 1
rh-clint Rat hepatocyte intrinsic clearance 177.011 uL/min/10^6 cells Moderate 0.76
rh-fuinc Rat hepatocyte fraction unbound in incubation 85.770 % Moderate 0.76
rppb Rat plasma protein binding (% unbound) 50.120 % Moderate 0.76
solubility-dd Solubility at pH 7.4 in DMSO 948.418 uM Moderate 0.76

Approvals:

DateAgencyCompanyOrphan
April 13, 1971 FDA ADAPT
Nov. 9, 2017 EMA Mundipharma Corporation (Ireland) Limited

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
Toxicity to various agents 297.81 14.07 298 14719 287548 90325882
Exposure during pregnancy 171.32 14.07 204 14813 238206 90375224
Respiratory depression 167.07 14.07 71 14946 15504 90597926
Drug withdrawal syndrome 136.73 14.07 75 14942 28648 90584782
Overdose 124.94 14.07 142 14875 157567 90455863
Abortion spontaneous 122.24 14.07 88 14929 53968 90559462
Drug withdrawal syndrome neonatal 105.52 14.07 31 14986 2288 90611142
Unresponsive to stimuli 83.75 14.07 61 14956 38060 90575370
Miosis 81.49 14.07 37 14980 9447 90603983
Selective abortion 73.20 14.07 14 15003 153 90613277
Cardiac arrest 67.43 14.07 85 14932 104850 90508580
Depressed level of consciousness 67.04 14.07 71 14946 72713 90540717
Premature delivery 61.16 14.07 51 14966 38711 90574719
Coma 60.17 14.07 67 14950 72565 90540865
Bradypnoea 59.28 14.07 24 14993 4634 90608796
Electrocardiogram QT prolonged 58.58 14.07 66 14951 72390 90541040
Mental status changes 51.07 14.07 49 14968 44630 90568800
Suicide attempt 49.90 14.07 62 14955 75337 90538093
Somnolence 49.62 14.07 108 14909 208976 90404454
Sinus tachycardia 45.98 14.07 38 14979 28475 90584955
Arthropathy 45.92 14.07 4 15013 366238 90247192
Infusion related reaction 43.94 14.07 8 15009 416772 90196658
Apnoea 43.18 14.07 24 14993 9390 90604040
Abortion induced 43.07 14.07 26 14991 11862 90601568
Intestinal infarction 43.05 14.07 13 15004 1054 90612376
Hypotension 43.04 14.07 135 14882 325262 90288168
Thymus disorder 42.15 14.07 10 15007 320 90613110
Renal infarct 41.68 14.07 14 15003 1601 90611829
Respiratory rate decreased 38.90 14.07 17 15000 3966 90609464
Seizure 38.68 14.07 81 14936 152548 90460882
Drug interaction 37.75 14.07 116 14901 276337 90337093
Sepsis 36.13 14.07 87 14930 179727 90433703
Systemic lupus erythematosus 35.94 14.07 8 15009 361888 90251542
Encephalopathy 35.32 14.07 41 14976 46403 90567027
Respiratory alkalosis 34.60 14.07 15 15002 3433 90609997
Coccydynia 34.48 14.07 13 15004 2078 90611352
Pelvic haematoma 34.25 14.07 10 15007 722 90612708
Intentional overdose 33.97 14.07 58 14959 93776 90519654
Treatment failure 33.88 14.07 5 15012 303923 90309507
Joint swelling 33.57 14.07 21 14996 503279 90110151
Non-cardiogenic pulmonary oedema 33.13 14.07 11 15006 1213 90612217
Alopecia 32.54 14.07 21 14996 495050 90118380
Respiratory failure 31.35 14.07 64 14953 118354 90495076
Drug abuse 31.26 14.07 52 14965 82295 90531135
Generalised anxiety disorder 31.04 14.07 13 15004 2734 90610696
Bradycardia 30.57 14.07 52 14965 83795 90529635
Respiratory acidosis 30.04 14.07 18 14999 8101 90605329
Acute respiratory failure 29.53 14.07 36 14981 42882 90570548
Drug intolerance 29.39 14.07 19 14998 447572 90165858
Hypersensitivity 28.92 14.07 20 14997 454657 90158773
Pulmonary oedema 28.83 14.07 43 14974 62037 90551393
Abdominal discomfort 27.79 14.07 23 14994 477305 90136125
Impaired insulin secretion 27.66 14.07 5 15012 39 90613391
Discomfort 27.36 14.07 6 15011 274329 90339101
Glossodynia 26.64 14.07 10 15007 321769 90291661
Metabolic acidosis 26.48 14.07 39 14978 55637 90557793
Withdrawal syndrome 26.29 14.07 25 14992 22499 90590931
Sinusitis 26.25 14.07 12 15005 343076 90270354
Tachypnoea 25.54 14.07 24 14993 21285 90592145
Aplastic anaemia 24.18 14.07 19 14998 13250 90600180
Therapeutic product effect decreased 24.05 14.07 8 15009 277563 90335867
Congestive cardiomyopathy 23.88 14.07 15 15002 7339 90606091
Contraindicated product administered 23.27 14.07 12 15005 320127 90293303
Rhabdomyolysis 23.08 14.07 35 14982 51221 90562209
Rhesus incompatibility 22.74 14.07 5 15012 113 90613317
Substance abuse 22.68 14.07 13 15004 5393 90608037
Blood albumin decreased 22.23 14.07 20 14997 16783 90596647
Insulin resistance 22.04 14.07 8 15009 1150 90612280
Tachyphylaxis 21.84 14.07 6 15011 347 90613083
Impaired healing 21.64 14.07 6 15011 234193 90379237
Wound 21.08 14.07 12 15005 302968 90310462
Rash 21.06 14.07 65 14952 796035 89817395
Appetite disorder 20.93 14.07 15 15002 9118 90604312
Hypoaesthesia teeth 20.89 14.07 4 15013 44 90613386
Dyspepsia 20.44 14.07 4 15013 198156 90415274
Metastatic gastric cancer 20.24 14.07 5 15012 190 90613240
Hypoxia 20.19 14.07 40 14977 72359 90541071
Ventricular hypokinesia 20.17 14.07 12 15005 5329 90608101
Retroperitoneal haematoma 19.42 14.07 10 15007 3358 90610072
Drug diversion 19.06 14.07 7 15010 1040 90612390
Foetal exposure during pregnancy 18.86 14.07 29 14988 42946 90570484
Premature baby 18.83 14.07 22 14995 25055 90588375
Mobility decreased 18.82 14.07 9 15008 250725 90362705
Hepatic necrosis 18.11 14.07 12 15005 6426 90607004
Psoriatic arthropathy 17.43 14.07 8 15009 228327 90385103
Accidental exposure to product by child 17.42 14.07 7 15010 1326 90612104
Type 2 diabetes mellitus 17.35 14.07 6 15011 203238 90410192
Retroperitoneal haemorrhage 17.34 14.07 9 15008 3071 90610359
Metastases to bone 16.90 14.07 21 14996 25484 90587946
Gastrointestinal disorder 16.69 14.07 11 15006 256676 90356754
Death 16.68 14.07 131 14886 456420 90157010
Odynophagia 16.59 14.07 13 15004 9030 90604400
Vomiting 16.42 14.07 201 14816 788092 89825338
Drug dependence 16.09 14.07 22 14995 29305 90584125
Rheumatoid arthritis 16.03 14.07 22 14995 362592 90250838
Cardiogenic shock 15.98 14.07 20 14997 24448 90588982
Stress cardiomyopathy 15.93 14.07 15 15002 13340 90600090
Hepatic enzyme increased 15.83 14.07 22 14995 360714 90252716
Maternal exposure during pregnancy 15.83 14.07 108 14909 359955 90253475
Wheezing 15.75 14.07 10 15007 238070 90375360
Irritability 15.56 14.07 24 14993 35638 90577792
Lethargy 15.39 14.07 33 14984 63106 90550324
Malaise 15.36 14.07 48 14969 585938 90027492
Upper gastrointestinal haemorrhage 15.36 14.07 19 14998 22957 90590473
Therapy naive 15.28 14.07 3 15014 38 90613392
Blister 15.18 14.07 12 15005 254986 90358444
Pruritus 15.17 14.07 43 14974 541482 90071948
Leukocytosis 15.15 14.07 22 14995 30968 90582462
Haematemesis 15.14 14.07 23 14994 33703 90579727
Brain death 15.10 14.07 9 15008 4012 90609418
Cachexia 15.08 14.07 11 15006 6867 90606563
Hepatotoxicity 14.85 14.07 27 14990 45815 90567615
Irritable bowel syndrome 14.73 14.07 8 15009 207440 90405990
Liver injury 14.62 14.07 5 15012 170562 90442868
Pulmonary congestion 14.51 14.07 17 15000 19416 90594014
Intentional product use issue 14.50 14.07 9 15008 216883 90396547
Acne pustular 14.42 14.07 4 15013 240 90613190
Ventricular tachycardia 14.27 14.07 19 14998 24689 90588741
Constipation 14.09 14.07 87 14930 280308 90333122

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
Toxicity to various agents 479.85 15.02 443 11596 228693 42380603
Overdose 348.94 15.02 266 11773 104998 42504298
Drug withdrawal syndrome 183.56 15.02 99 11940 21450 42587846
Unresponsive to stimuli 139.44 15.02 95 11944 31308 42577988
Drug withdrawal syndrome neonatal 131.73 15.02 49 11990 4412 42604884
Drug abuse 115.58 15.02 145 11894 104626 42504670
Miosis 109.52 15.02 60 11979 13386 42595910
Respiratory depression 98.07 15.02 63 11976 18805 42590491
Non-cardiogenic pulmonary oedema 93.62 15.02 26 12013 909 42608387
Drug dependence 75.71 15.02 64 11975 29030 42580266
Neurodegenerative disorder 72.32 15.02 18 12021 407 42608889
Pulmonary oedema 63.92 15.02 77 11962 53195 42556101
Substance dependence 55.39 15.02 16 12023 646 42608650
Antemortem blood drug level abnormal 45.61 15.02 9 12030 65 42609231
Agitation 42.70 15.02 70 11969 64244 42545052
Substance abuse 42.02 15.02 28 12011 8877 42600419
Depressed level of consciousness 41.44 15.02 59 11980 47911 42561385
Hypercapnia 41.11 15.02 23 12016 5338 42603958
Cardiac arrest 40.58 15.02 93 11946 109227 42500069
Maternal exposure during breast feeding 38.41 15.02 15 12024 1540 42607756
Coma 37.88 15.02 60 11979 53494 42555802
Poisoning 35.51 15.02 31 12008 14668 42594628
Postmortem blood drug level abnormal 35.35 15.02 10 12029 374 42608922
Respiratory acidosis 35.02 15.02 22 12017 6309 42602987
Blood ethanol 32.20 15.02 7 12032 85 42609211
Bradypnoea 31.40 15.02 18 12021 4375 42604921
Accidental exposure to product by child 31.39 15.02 13 12026 1554 42607742
Hypoxic-ischaemic encephalopathy 31.12 15.02 19 12020 5183 42604113
Rhesus incompatibility 29.65 15.02 6 12033 50 42609246
Somnolence 28.38 15.02 96 11943 141009 42468287
Postmortem blood drug level 27.88 15.02 7 12032 164 42609132
Respiratory failure 27.39 15.02 89 11950 128043 42481253
Dementia 26.92 15.02 28 12011 16452 42592844
Foetal exposure during pregnancy 26.79 15.02 48 11991 47263 42562033
Amphetamines positive 26.59 15.02 7 12032 199 42609097
Lethargy 25.82 15.02 47 11992 46843 42562453
Cerebral congestion 25.78 15.02 6 12033 101 42609195
Pneumomediastinum 25.62 15.02 14 12025 3102 42606194
Glabellar reflex abnormal 25.35 15.02 5 12034 36 42609260
Drug ineffective 24.82 15.02 279 11760 629918 41979378
Therapy naive 24.78 15.02 5 12034 41 42609255
Counterfeit product administered 24.13 15.02 7 12032 287 42609009
Opiates positive 23.73 15.02 8 12031 539 42608757
Hypoxia 22.24 15.02 56 11983 69730 42539566
Delusion 22.23 15.02 24 12015 14710 42594586
Breech presentation 22.17 15.02 6 12033 190 42609106
Delirium 22.08 15.02 47 11992 52472 42556824
Brain oedema 21.89 15.02 25 12014 16302 42592994
Paranoia 21.43 15.02 23 12016 14003 42595293
Arteriosclerosis coronary artery 20.76 15.02 26 12013 18651 42590645
Accidental poisoning 20.19 15.02 9 12030 1287 42608009
Brief psychotic disorder with marked stressors 20.18 15.02 6 12033 268 42609028
Apnoea 19.94 15.02 17 12022 7786 42601510
Therapeutic product effect prolonged 19.30 15.02 6 12033 312 42608984
Genitourinary symptom 19.30 15.02 4 12035 38 42609258
Mental status changes 19.23 15.02 39 12000 42076 42567220
Stress cardiomyopathy 18.81 15.02 11 12028 2774 42606522
Withdrawal syndrome 18.76 15.02 22 12017 14753 42594543
Jaundice neonatal 18.50 15.02 10 12029 2169 42607127
Intentional product misuse 18.00 15.02 48 11991 61852 42547444
Hypopnoea 17.79 15.02 16 12023 7866 42601430
Death 17.75 15.02 207 11832 470978 42138318
Restrictive cardiomyopathy 17.70 15.02 7 12032 743 42608553
Axillary pain 17.50 15.02 6 12033 426 42608870
Hallucination 17.13 15.02 45 11994 57462 42551834
Compartment syndrome 17.12 15.02 11 12028 3278 42606018
Serotonin syndrome 16.96 15.02 28 12011 25817 42583479
Pancreatic disorder 16.30 15.02 9 12030 2036 42607260
Respiratory arrest 16.29 15.02 29 12010 28395 42580901
Accidental exposure to product 16.02 15.02 24 12015 20369 42588927
Disease progression 15.26 15.02 11 12028 143645 42465651

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
Toxicity to various agents 760.06 13.42 688 21810 479867 110086934
Overdose 416.37 13.42 359 22139 233435 110333366
Drug withdrawal syndrome 259.02 13.42 135 22363 37919 110528882
Respiratory depression 254.16 13.42 126 22372 31875 110534926
Miosis 196.92 13.42 94 22404 21889 110544912
Unresponsive to stimuli 196.84 13.42 136 22362 63654 110503147
Drug abuse 139.39 13.42 176 22322 177235 110389566
Non-cardiogenic pulmonary oedema 126.10 13.42 36 22462 1948 110564853
Pulmonary oedema 121.84 13.42 125 22373 100534 110466267
Cardiac arrest 107.66 13.42 164 22334 196589 110370212
Coma 103.95 13.42 124 22374 117745 110449056
Depressed level of consciousness 98.81 13.42 118 22380 112160 110454641
Bradypnoea 93.05 13.42 42 22456 8607 110558194
Somnolence 79.25 13.42 182 22316 297267 110269534
Neurodegenerative disorder 76.72 13.42 20 22478 767 110566034
Mental status changes 70.26 13.42 82 22416 76040 110490761
Substance dependence 68.63 13.42 18 22480 707 110566094
Respiratory failure 66.67 13.42 140 22358 215192 110351609
Respiratory acidosis 66.39 13.42 39 22459 13787 110553014
Drug dependence 60.28 13.42 62 22436 49958 110516843
Drug ineffective 59.90 13.42 519 21979 1520021 109046780
Apnoea 56.52 13.42 35 22463 13604 110553197
Accidental exposure to product by child 52.62 13.42 21 22477 3177 110563624
Respiratory rate decreased 50.72 13.42 25 22473 6233 110560568
Agitation 50.51 13.42 86 22412 112965 110453836
Sinus tachycardia 48.01 13.42 52 22446 44441 110522360
Antemortem blood drug level abnormal 47.97 13.42 9 22489 70 110566731
Hypotension 47.79 13.42 222 22276 523627 110043174
Death 46.36 13.42 271 22227 698598 109868203
Lethargy 45.57 13.42 74 22424 93502 110473299
Substance abuse 44.22 13.42 29 22469 12434 110554367
Synovitis 44.06 13.42 3 22495 274089 110292712
Suicide attempt 44.02 13.42 77 22421 103317 110463484
Hypoxic-ischaemic encephalopathy 42.59 13.42 25 22473 8822 110557979
Joint swelling 41.63 13.42 19 22479 442826 110123975
Hypoxia 40.98 13.42 85 22413 129430 110437371
Acute respiratory failure 40.07 13.42 62 22436 75198 110491603
Intentional overdose 38.51 13.42 84 22414 132417 110434384
Hypercapnia 37.26 13.42 25 22473 11134 110555667
Intestinal infarction 36.69 13.42 13 22485 1417 110565384
Drug intolerance 35.85 13.42 19 22479 406493 110160308
Bradycardia 34.76 13.42 89 22409 155428 110411373
Generalised anxiety disorder 34.75 13.42 15 22483 2764 110564037
Brain oedema 34.70 13.42 37 22461 31061 110535740
Thymus disorder 34.42 13.42 10 22488 576 110566225
Hypersensitivity 34.01 13.42 20 22478 403978 110162823
Postmortem blood drug level abnormal 33.55 13.42 10 22488 630 110566171
Infusion related reaction 33.33 13.42 18 22480 381144 110185657
Therapeutic product effect decreased 33.26 13.42 5 22493 244311 110322490
Systemic lupus erythematosus 32.86 13.42 6 22492 254332 110312469
Withdrawal syndrome 32.67 13.42 36 22462 31344 110535457
Blood ethanol 32.46 13.42 7 22491 116 110566685
Stress cardiomyopathy 31.57 13.42 26 22472 15780 110551021
Lower respiratory tract infection 30.84 13.42 6 22492 243100 110323701
Glossodynia 29.20 13.42 5 22493 221999 110344802
Renal infarct 28.82 13.42 14 22484 3381 110563420
Pelvic haematoma 28.69 13.42 10 22488 1039 110565762
Electrocardiogram QT prolonged 28.22 13.42 66 22432 108894 110457907
Cerebral congestion 28.04 13.42 7 22491 225 110566576
Accidental overdose 28.01 13.42 43 22455 51791 110515010
Treatment failure 27.47 13.42 11 22487 277223 110289578
Malaise 27.41 13.42 60 22438 671759 109895042
Glabellar reflex abnormal 26.87 13.42 5 22493 37 110566764
Psoriatic arthropathy 26.84 13.42 4 22494 196757 110370044
Encephalopathy 26.58 13.42 54 22444 81001 110485800
Seizure 26.54 13.42 102 22396 221083 110345718
Accidental poisoning 26.50 13.42 12 22486 2475 110564326
Serotonin syndrome 26.41 13.42 45 22453 59108 110507693
Rheumatoid arthritis 26.41 13.42 14 22484 299599 110267202
Pneumomediastinum 26.29 13.42 15 22483 5021 110561780
Amphetamines positive 26.19 13.42 7 22491 296 110566505
Postmortem blood drug level 25.81 13.42 7 22491 313 110566488
Dementia 25.74 13.42 32 22466 31641 110535160
Alopecia 25.52 13.42 22 22476 364731 110202070
Aplastic anaemia 25.50 13.42 28 22470 24280 110542521
Blood cholesterol increased 24.66 13.42 4 22494 184781 110382020
Poisoning 24.61 13.42 30 22468 29075 110537726
Respiratory alkalosis 24.51 13.42 15 22483 5706 110561095
Impaired insulin secretion 24.39 13.42 5 22493 64 110566737
Respiratory arrest 24.27 13.42 43 22455 58256 110508545
Rhabdomyolysis 23.95 13.42 66 22432 120335 110446466
Nasopharyngitis 23.89 13.42 27 22471 394334 110172467
Urticaria 23.84 13.42 18 22480 318839 110247962
Pruritus 23.66 13.42 52 22446 581508 109985293
Product use issue 22.79 13.42 18 22480 311677 110255124
Abdominal discomfort 22.75 13.42 28 22470 393830 110172971
Fibromyalgia 22.14 13.42 4 22494 170905 110395896
Opiates positive 22.07 13.42 8 22490 931 110565870
Delirium 22.06 13.42 69 22429 134956 110431845
Rash 21.50 13.42 90 22408 820874 109745927
Intentional product use issue 21.24 13.42 12 22486 247894 110318907
Sepsis 21.02 13.42 126 22372 327220 110239581
Accidental exposure to product 20.96 13.42 37 22461 49971 110516830
Sinusitis 20.62 13.42 18 22480 296670 110270131
Tachycardia 20.57 13.42 96 22402 226549 110340252
Brief psychotic disorder with marked stressors 20.51 13.42 6 22492 354 110566447
Tachypnoea 20.33 13.42 32 22466 39363 110527438
Therapeutic product effect prolonged 20.23 13.42 7 22491 711 110566090
Brain death 20.22 13.42 14 22484 6559 110560242
Drug interaction 20.15 13.42 172 22326 500011 110066790
Hypoaesthesia teeth 19.83 13.42 4 22494 47 110566754
Drug hypersensitivity 19.81 13.42 39 22459 454051 110112750
Type 2 diabetes mellitus 19.32 13.42 6 22492 177226 110389575
Abortion spontaneous 19.31 13.42 29 22469 34253 110532548
Impaired healing 19.16 13.42 8 22490 196709 110370092
Compartment syndrome 19.16 13.42 13 22485 5897 110560904
Discomfort 18.96 13.42 10 22488 214697 110352104
Gastrointestinal disorder 18.94 13.42 13 22485 241939 110324862
Pulmonary congestion 18.60 13.42 27 22471 30939 110535862
Necrotising fasciitis 18.41 13.42 14 22484 7577 110559224
Delayed recovery from anaesthesia 18.40 13.42 9 22489 2206 110564595
Arteriosclerosis coronary artery 18.24 13.42 24 22474 25094 110541707
Dyspepsia 18.23 13.42 8 22490 190957 110375844
Lung disorder 18.06 13.42 7 22491 180040 110386761
Delusion 17.72 13.42 23 22475 23732 110543069
Anion gap increased 17.62 13.42 11 22487 4333 110562468
Restrictive cardiomyopathy 17.57 13.42 7 22491 1054 110565747
Counterfeit product administered 17.49 13.42 5 22493 272 110566529
Insulin resistance 17.33 13.42 8 22490 1726 110565075
Appetite disorder 17.31 13.42 15 22483 9754 110557047
Metabolic acidosis 17.25 13.42 52 22446 99692 110467109
Paranoia 17.22 13.42 22 22476 22352 110544449
Drug ineffective for unapproved indication 17.21 13.42 53 22445 102785 110464016
Inflammation 17.06 13.42 9 22489 193229 110373572
Respiratory distress 17.05 13.42 41 22457 68833 110497968
Mobility decreased 16.99 13.42 14 22484 237408 110329393
C-reactive protein increased 16.67 13.42 12 22486 217907 110348894
Product counterfeit 16.67 13.42 5 22493 322 110566479
Leukocytosis 16.63 13.42 35 22463 53793 110513008
Retroperitoneal haematoma 16.42 13.42 12 22486 6119 110560682
Contraindicated product administered 16.14 13.42 16 22482 248251 110318550
Musculoskeletal stiffness 16.04 13.42 20 22478 279802 110286999
Hospice care 16.00 13.42 16 22482 12457 110554344
Wheezing 15.97 13.42 17 22481 255213 110311588
Sickle cell anaemia with crisis 15.60 13.42 14 22484 9531 110557270
Muscle twitching 15.01 13.42 24 22474 29911 110536890
Loss of consciousness 14.86 13.42 79 22419 196227 110370574
Axillary pain 14.30 13.42 8 22490 2578 110564223
Wound 14.24 13.42 16 22482 234421 110332380
Streptococcal infection 14.03 13.42 14 22484 10876 110555925
Arthralgia 14.00 13.42 97 22401 779535 109787266
Idiopathic pulmonary fibrosis 13.87 13.42 10 22488 4994 110561807
Exposure during pregnancy 13.80 13.42 69 22429 167355 110399446
Night sweats 13.79 13.42 5 22493 133978 110432823
Pupil fixed 13.78 13.42 9 22489 3829 110562972
Selective abortion 13.68 13.42 3 22495 54 110566747
Hypertensive urgency 13.67 13.42 6 22492 1151 110565650
Blood albumin decreased 13.63 13.42 22 22476 27630 110539171
Hepatic enzyme increased 13.61 13.42 28 22470 320864 110245937
Pancreatic disorder 13.58 13.42 9 22489 3925 110562876
Deafness neurosensory 13.58 13.42 13 22485 9606 110557195
Hyporesponsive to stimuli 13.55 13.42 8 22490 2852 110563949
Hypopnoea 13.51 13.42 14 22484 11366 110555435
Liver disorder 13.51 13.42 6 22492 142237 110424564

FDA Adverse Event Reporting System (Pediatric)

None

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 N02AD51 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Benzomorphan derivatives
ATC N02AX51 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Other opioids
ATC V03AB15 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes
FDA MoA N0000000154 Opioid Antagonists
MeSH PA D009292 Narcotic Antagonists
MeSH PA D018689 Sensory System Agents
FDA EPC N0000175691 Opioid Antagonist
CHEBI has role CHEBI:35488 central nervous system depressant
CHEBI has role CHEBI:50137 ฮผ-opioid receptor antagonist
CHEBI has role CHEBI:90755 antidote to opioid poisoning

Related Drugs by ATC class:

A06AH Peripheral opioid receptor antagonists 4 drugs
alvimopanmethylnaltrexonenaldemedinenaloxegol
N02AA Natural opium alkaloids 8 drugs
codeinedihydrocodeinehydromorphonemorphinenaltrexonenicomorphineoxycodoneoxymorphone
N02AD Benzomorphan derivatives 2 drugs
pentazocinephenazocine
N02AX Other opioids 6 drugs
dezocinemeptazinololiceridinetapentadoltilidinetramadol
V03AB Antidotes 28 drugs
4-dimethylaminophenolacetylcysteineamyl nitriteandexanet alfaatropinecopper sulfatedimercaprolethanolflumazenilfomepizoleglutathionehydroxocobalamin show all 28 →

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

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000
Opioid dependence indication 75544000 DOID:2559
Poisoning by opiate analgesic drug indication 241749009
Overdose of opiate indication 242253008
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




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 9.31 acidic
pKa2 7.47 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9724471 May 23, 2027 METHOD FOR CONFIRMING DOSE DELIVERY
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9724471 May 23, 2027 METHOD FOR CONFIRMING DOSE DELIVERY
EQ 2.1MG BASE;EQ 0.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 DISCN FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 2.1MG BASE;EQ 0.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 DISCN FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 4.2MG BASE;EQ 0.7MG BASE BUNAVAIL BDSI N205637 June 6, 2014 DISCN FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 4.2MG BASE;EQ 0.7MG BASE BUNAVAIL BDSI N205637 June 6, 2014 DISCN FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 6.3MG BASE;EQ 1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 DISCN FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 6.3MG BASE;EQ 1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 DISCN FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 0.7MG BASE;EQ 0.18MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 1.4MG BASE;EQ 0.36MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 11.4MG BASE;EQ 2.9MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 2.9MG BASE;EQ 0.71MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 June 4, 2015 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 5.7MG BASE;EQ 1.4MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 8.6MG BASE;EQ 2.1MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 12MG BASE;EQ 3MG BASE SUBOXONE INDIVIOR N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 11135216 Aug. 7, 2029 TREATING OPIOID USE DISORDER
EQ 12MG BASE;EQ 3MG BASE SUBOXONE INDIVIOR N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 2MG BASE;EQ 0.5MG BASE SUBOXONE INDIVIOR N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 11135216 Aug. 7, 2029 TREATING OPIOID USE DISORDER
EQ 2MG BASE;EQ 0.5MG BASE SUBOXONE INDIVIOR N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 4MG BASE;EQ 1MG BASE SUBOXONE INDIVIOR N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 11135216 Aug. 7, 2029 TREATING OPIOID USE DISORDER
EQ 4MG BASE;EQ 1MG BASE SUBOXONE INDIVIOR N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 8MG BASE;EQ 2MG BASE SUBOXONE INDIVIOR N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 11135216 Aug. 7, 2029 TREATING OPIOID USE DISORDER
EQ 8MG BASE;EQ 2MG BASE SUBOXONE INDIVIOR N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 12MG BASE;EQ 3MG BASE SUBOXONE INDIVIOR N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 2MG BASE;EQ 0.5MG BASE SUBOXONE INDIVIOR N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 4MG BASE;EQ 1MG BASE SUBOXONE INDIVIOR N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 8MG BASE;EQ 2MG BASE SUBOXONE INDIVIOR N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 0.7MG BASE;EQ 0.18MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 1.4MG BASE;EQ 0.36MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 11.4MG BASE;EQ 2.9MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 2.9MG BASE;EQ 0.71MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 June 4, 2015 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 5.7MG BASE;EQ 1.4MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 8.6MG BASE;EQ 2.1MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10322239 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9474869 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10322239 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9474869 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
10MG/0.4ML (10MG/0.4ML) NALOXONE HYDROCHLORIDE (AUTOINJECTOR) KALEO INC N215457 Feb. 28, 2022 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10322239 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
10MG/0.4ML (10MG/0.4ML) NALOXONE HYDROCHLORIDE (AUTOINJECTOR) KALEO INC N215457 Feb. 28, 2022 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9474869 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10143972 May 24, 2031 USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10143792 May 24, 2031 USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
10MG/0.4ML (10MG/0.4ML) NALOXONE HYDROCHLORIDE (AUTOINJECTOR) KALEO INC N215457 Feb. 28, 2022 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10143792 May 24, 2031 USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
3MG/SPRAY RIVIVE HARM REDUCTION THERP N217722 July 28, 2023 OTC SPRAY, METERED NASAL 11020343 May 11, 2032 USE OF INTRANASAL NALOXONE FOR THE TREATMENT OF OPIOID OVERDOSE
3MG/SPRAY RIVIVE HARM REDUCTION THERP N217722 July 28, 2023 OTC SPRAY, METERED NASAL 12458591 May 11, 2032 USE OF INTRANASAL NALOXONE FOR THE TREATMENT OF OPIOID OVERDOSE
EQ 0.7MG BASE;EQ 0.18MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL 11020388 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 1.4MG BASE;EQ 0.36MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 11020388 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 1.4MG BASE;EQ 0.36MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 11433066 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 11.4MG BASE;EQ 2.9MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 11020387 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 11.4MG BASE;EQ 2.9MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 11020388 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 11.4MG BASE;EQ 2.9MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 11433066 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 2.9MG BASE;EQ 0.71MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 June 4, 2015 RX TABLET SUBLINGUAL 11020387 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 2.9MG BASE;EQ 0.71MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 June 4, 2015 RX TABLET SUBLINGUAL 11020388 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 2.9MG BASE;EQ 0.71MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 June 4, 2015 RX TABLET SUBLINGUAL 11433066 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 5.7MG BASE;EQ 1.4MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 11020387 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 5.7MG BASE;EQ 1.4MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 11020388 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 5.7MG BASE;EQ 1.4MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 July 3, 2013 RX TABLET SUBLINGUAL 11433066 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 8.6MG BASE;EQ 2.1MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 11020387 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 8.6MG BASE;EQ 2.1MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 11020388 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
EQ 8.6MG BASE;EQ 2.1MG BASE ZUBSOLV EDENBRIDGE PHARMS N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 11433066 Sept. 18, 2032 USE OF ZUBSOLV FOR TREATMENT OF OPIOID DEPENDENCE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9517307 July 18, 2034 USE OF AN AUTO INJECTOR TO ADMINISTER NALOXONE HCL
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9517307 July 18, 2034 USE OF AN AUTO INJECTOR TO ADMINISTER NALOXONE HCL
8MG/SPRAY KLOXXADO HIKMA N212045 April 29, 2021 RX SPRAY NASAL 10722510 Aug. 26, 2034 USE OF NALOXONE FOR THE EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION, FOR ADULT AND PEDIATRIC PATIENTS
8MG/SPRAY KLOXXADO HIKMA N212045 April 29, 2021 RX SPRAY NASAL 10973814 Aug. 26, 2034 USE OF NALOXONE FOR THE EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION, FOR ADULT AND PEDIATRIC PATIENTS
8MG/SPRAY KLOXXADO HIKMA N212045 April 29, 2021 RX SPRAY NASAL 11617713 Aug. 26, 2034 USE OF NALOXONE FOR THE EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION, FOR ADULT AND PEDIATRIC PATIENTS
8MG/SPRAY KLOXXADO HIKMA N212045 April 29, 2021 RX SPRAY NASAL 11628139 Aug. 26, 2034 USE OF NALOXONE FOR THE EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION, FOR ADULT AND PEDIATRIC PATIENTS
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10220158 March 20, 2035 USE OF A DELIVERY DEVICE TO DELIVER A BIOEQUIVALENT DOSE OF A NALOXONE COMPOSITION VIA A NEEDLE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10220158 March 20, 2035 USE OF A DELIVERY DEVICE TO DELIVER A BIOEQUIVALENT DOSE OF A NALOXONE COMPOSITION VIA A NEEDLE
10MG/SPRAY REZENOPY SCIENTURE N215487 April 19, 2024 RX SPRAY NASAL 12514854 Feb. 5, 2041 TREATMENT OF OPIOID OVERDOSE
5MG/0.5ML (5MG/0.5ML) ZIMHI ZMI PHARMA N212854 Oct. 15, 2021 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 11571518 June 14, 2041 A METHOD FOR ADMINISTERING A THERAPEUTIC DOSE OF AN OPIOID ANTAGONIST COMPRISING AN EMERGENCY SYRINGE DEVICE
5MG/0.5ML (5MG/0.5ML) ZIMHI ZMI PHARMA N212854 Oct. 15, 2021 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 11571518 June 14, 2041 A METHOD FOR ADMINISTERING A THERAPEUTIC DOSE OF AN OPIOID ANTAGONIST COMPRISING AN EMERGENCY SYRINGE DEVICE INCLUDING A NEEDLE GUARD
5MG/0.5ML (5MG/0.5ML) ZIMHI ZMI PHARMA N212854 Oct. 15, 2021 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 11571518 June 14, 2041 A METHOD FOR ADMINISTERING A THERAPEUTIC DOSE OF AN OPIOID ANTAGONIST COMPRISING AN EMERGENCY SYRINGE DEVICE INCLUDING A WINDOW CONFIGURED TO ALLOW THE USER TO VIEW THE OPIOID ANTAGONIST IN THE SYRINGE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
4MG/SPRAY REXTOVY AMPHASTAR PHARMS INC N208969 March 7, 2023 OTC SPRAY, METERED NASAL March 7, 2026 NEW PRODUCT
10MG/SPRAY REZENOPY SCIENTURE N215487 April 19, 2024 RX SPRAY NASAL April 19, 2027 NEW PRODUCT

Bioactivity Summary:

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

External reference:

IDSource
D01340 KEGG_DRUG
51481-60-8 SECONDARY_CAS_RN
357-08-4 SECONDARY_CAS_RN
4018057 VANDF
4019852 VANDF
C0027358 UMLSCUI
CHEBI:7459 CHEBI
CHEMBL80 ChEMBL_ID
CHEMBL5315056 ChEMBL_ID
CHEMBL1718 ChEMBL_ID
DB01183 DRUGBANK_ID
D009270 MESH_DESCRIPTOR_UI
5284596 PUBCHEM_CID
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
A1APV PDB_CHEM_ID
36B82AMQ7N INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0188 TABLET 0.50 mg SUBLINGUAL ANDA 33 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0188 TABLET 0.50 mg SUBLINGUAL ANDA 33 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0189 TABLET 2 mg SUBLINGUAL ANDA 33 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0189 TABLET 2 mg SUBLINGUAL ANDA 33 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0121-1018 TABLET 0.50 mg SUBLINGUAL ANDA 31 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0121-2036 TABLET 2 mg SUBLINGUAL ANDA 31 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3154 TABLET 0.50 mg SUBLINGUAL ANDA 33 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3155 TABLET 2 mg SUBLINGUAL ANDA 33 sections
Naloxone Hydrochloride HUMAN OTC DRUG LABEL 1 0363-2140 SPRAY 4 mg NASAL ANDA 11 sections
Naloxone Hydrochloride HUMAN OTC DRUG LABEL 1 0363-2140 SPRAY 4 mg NASAL ANDA 11 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
NALOXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0404-9773 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0404-9920 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 14 sections
NALOXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0404-9922 INJECTION 1 mg PARENTERAL ANDA 14 sections
NALOXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0404-9922 INJECTION 1 mg PARENTERAL ANDA 14 sections
NALOXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0404-9923 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 14 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8005 TABLET 0.50 mg SUBLINGUAL ANDA 37 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8020 TABLET 2 mg SUBLINGUAL ANDA 37 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
Naloxone Hydrochloride HUMAN OTC DRUG LABEL 1 0480-3478 SPRAY, METERED 4 mg NASAL ANDA 10 sections
Pentazocine and naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0591-0395 TABLET 0.50 mg ORAL ANDA 28 sections
Naloxone Hydrochloride HUMAN OTC DRUG LABEL 1 0591-3871 SPRAY, METERED 4 mg NASAL ANDA 10 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0641-6132 INJECTION 0.40 mg INTRAMUSCULAR ANDA 23 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0641-6193 INJECTION 0.40 mg INTRAMUSCULAR ANDA 24 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0641-6205 INJECTION 1 mg INTRAMUSCULAR ANDA 24 sections