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

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists related to normorphine 1765 16590-41-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • naltrexone
  • cyclopropylmethylnoroxymorphone
  • naltrel
  • naltrexone hydrochloride
  • naltrexone hydrochloride dihydrate
  • naltrexone HCl
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
  • Molecular weight: 341.41
  • Formula: C20H23NO4
  • CLOGP: 0.36
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 70
  • ALOGS: -2.05
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 100 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.44 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 22 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 7.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 57 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.79 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 20, 1984 FDA TEVA WOMENS

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
Injection site reaction 3530.66 22.54 1135 18565 48897 50536527
Injection site mass 2614.09 22.54 695 19005 14985 50570439
Injection site pain 1351.79 22.54 717 18983 110307 50475117
Injection site induration 971.32 22.54 280 19420 8117 50577307
Therapeutic response shortened 474.43 22.54 157 19543 7232 50578192
Product administered at inappropriate site 302.53 22.54 86 19614 2357 50583067
Feeling abnormal 253.84 22.54 277 19423 125215 50460209
Injection site swelling 252.94 22.54 173 19527 41600 50543824
Withdrawal syndrome 248.17 22.54 126 19574 17464 50567960
Injection site abscess 215.15 22.54 55 19645 994 50584430
Inadequate analgesia 146.87 22.54 50 19650 2508 50582916
Inappropriate schedule of product administration 142.27 22.54 157 19543 71674 50513750
Injection site warmth 141.22 22.54 80 19620 13786 50571638
Product dose omission issue 136.35 22.54 251 19449 183587 50401837
Injection site nodule 130.08 22.54 49 19651 3299 50582125
Needle issue 129.18 22.54 61 19639 7214 50578210
Alcohol use 122.44 22.54 41 19659 1954 50583470
Anxiety 122.35 22.54 235 19465 177371 50408053
Drug screen positive 118.57 22.54 46 19654 3356 50582068
Insomnia 112.69 22.54 225 19475 174640 50410784
Substance abuse 103.33 22.54 44 19656 4080 50581344
Depression 101.98 22.54 209 19491 165214 50420210
Body tinea 100.58 22.54 32 19668 1295 50584129
Lack of injection site rotation 98.87 22.54 23 19677 274 50585150
Product administration error 92.56 22.54 70 19630 19629 50565795
Inhibitory drug interaction 91.56 22.54 34 19666 2199 50583225
Alcohol poisoning 91.01 22.54 32 19668 1768 50583656
Injection site erythema 90.71 22.54 128 19572 74808 50510616
Injection site pruritus 86.36 22.54 92 19608 40319 50545105
Infection susceptibility increased 79.75 22.54 32 19668 2552 50582872
Lack of administration site rotation 77.36 22.54 12 19688 6 50585418
Injection site discomfort 74.18 22.54 34 19666 3756 50581668
Injection site cellulitis 71.52 22.54 24 19676 1151 50584273
Dependence 67.64 22.54 26 19674 1849 50583575
Tremor 67.01 22.54 142 19558 114761 50470663
Necrosis ischaemic 63.59 22.54 20 19680 779 50584645
Injection site cyst 63.13 22.54 12 19688 47 50585377
Acute kidney injury 61.69 22.54 8 19692 228050 50357374
Glucose tolerance impaired 61.65 22.54 33 19667 5085 50580339
Euphoric mood 59.94 22.54 30 19670 4025 50581399
Poor quality sleep 58.69 22.54 50 19650 16596 50568828
Hospitalisation 56.94 22.54 98 19602 67839 50517585
Alcohol abuse 56.79 22.54 23 19677 1878 50583546
Impaired quality of life 56.47 22.54 33 19667 6023 50579401
Injection site infection 56.06 22.54 22 19678 1654 50583770
Irritability 54.26 22.54 61 19639 28365 50557059
Anaemia 53.41 22.54 16 19684 252440 50332984
Alcoholism 53.26 22.54 21 19679 1599 50583825
Nausea 52.80 22.54 460 19240 704938 49880486
Imprisonment 52.68 22.54 13 19687 202 50585222
Pneumonia 51.64 22.54 43 19657 378358 50207066
Surgery 51.24 22.54 61 19639 30144 50555280
Pregnancy 50.62 22.54 60 19640 29517 50555907
Impaired work ability 50.20 22.54 42 19658 13598 50571826
Pneumonia streptococcal 49.64 22.54 20 19680 1611 50583813
Feeling drunk 48.11 22.54 25 19675 3628 50581796
Injection site bruising 47.74 22.54 65 19635 36703 50548721
Injection site necrosis 47.73 22.54 18 19682 1215 50584209
Dyspnoea 47.72 22.54 88 19612 547520 50037904
Beta haemolytic streptococcal infection 47.42 22.54 20 19680 1810 50583614
Magnesium deficiency 46.06 22.54 14 19686 486 50584938
Headache 44.61 22.54 343 19357 506192 50079232
Malaise 44.60 22.54 252 19448 335280 50250144
Alcohol withdrawal syndrome 44.52 22.54 15 19685 728 50584696
Hypotension 42.90 22.54 19 19681 235450 50349974
Apathy 42.66 22.54 30 19670 7518 50577906
Wrong technique in product usage process 42.53 22.54 77 19623 55433 50529991
Condition aggravated 41.43 22.54 33 19667 297025 50288399
Crying 41.00 22.54 45 19655 20371 50565053
General physical health deterioration 41.00 22.54 4 19696 142430 50442994
Drug dependence 40.46 22.54 44 19656 19715 50565709
Neutropenia 40.45 22.54 5 19695 147960 50437464
Purpura 39.58 22.54 32 19668 9879 50575545
Malabsorption from injection site 38.78 22.54 7 19693 19 50585405
Fatigue 38.49 22.54 432 19268 707169 49878255
Hyperammonaemia 36.96 22.54 23 19677 4701 50580723
Bone density decreased 36.47 22.54 32 19668 11043 50574381
Drug intolerance 36.40 22.54 20 19680 219084 50366340
Detoxification 35.62 22.54 6 19694 9 50585415
Oral herpes 35.39 22.54 42 19658 20683 50564741
Treatment failure 34.50 22.54 6 19694 137631 50447793
Mood altered 34.45 22.54 33 19667 12740 50572684
Rheumatoid arthritis 32.90 22.54 19 19681 202531 50382893
Panic attack 32.70 22.54 39 19661 19303 50566121
Toothache 31.80 22.54 36 19664 16858 50568566
Decreased appetite 31.47 22.54 158 19542 200765 50384659
Injection site irritation 31.08 22.54 20 19680 4330 50581094
Intentional overdose 30.50 22.54 72 19628 62432 50522992
Mass 30.15 22.54 30 19670 12127 50573297
Restless legs syndrome 30.13 22.54 34 19666 15863 50569561
Coronavirus infection 30.08 22.54 17 19683 2912 50582512
Feeling of despair 30.03 22.54 15 19685 2003 50583421
Road traffic accident 30.02 22.54 42 19658 24310 50561114
Injection site haematoma 29.49 22.54 22 19678 6038 50579386
Somnolence 29.48 22.54 129 19571 154856 50430568
Hypersomnia 29.45 22.54 33 19667 15281 50570143
Hyperlipidaemia 29.13 22.54 35 19665 17455 50567969
Skin disorder 28.97 22.54 41 19659 23989 50561435
Food craving 28.44 22.54 13 19687 1426 50583998
Drug screen false positive 28.27 22.54 11 19689 808 50584616
Death of relative 28.24 22.54 8 19692 216 50585208
Cold sweat 27.76 22.54 27 19673 10617 50574807
Caffeine consumption 27.41 22.54 4 19696 0 50585424
Infusion related reaction 27.40 22.54 16 19684 169541 50415883
Product use issue 27.30 22.54 12 19688 149463 50435961
Rash 27.13 22.54 84 19616 437387 50148037
Haemoglobin decreased 26.98 22.54 8 19692 127208 50458216
Illness 26.86 22.54 40 19660 24500 50560924
Arthropathy 26.82 22.54 14 19686 157892 50427532
Disease progression 26.79 22.54 3 19697 95863 50489561
Pyrexia 26.51 22.54 69 19631 380134 50205290
Adiposis dolorosa 26.51 22.54 8 19692 271 50585153
Pulmonary embolism 26.46 22.54 4 19696 101700 50483724
Anger 26.34 22.54 27 19673 11306 50574118
Product preparation error 26.16 22.54 18 19682 4354 50581070
Suicidal ideation 26.16 22.54 63 19637 55322 50530102
Restlessness 26.08 22.54 40 19660 25133 50560291
Drug hypersensitivity 25.87 22.54 36 19664 250974 50334450
Pain 25.52 22.54 340 19360 578563 50006861
Oedema peripheral 25.38 22.54 15 19685 157946 50427478
White blood cell count decreased 25.38 22.54 7 19693 116715 50468709
Sepsis 25.35 22.54 10 19690 132915 50452509
Snoring 25.27 22.54 16 19684 3368 50582056
Dental operation 25.21 22.54 11 19689 1082 50584342
Abnormal dreams 24.86 22.54 24 19676 9353 50576071
Stomatitis 24.15 22.54 5 19695 101339 50484085
Contraindicated product administered 24.14 22.54 14 19686 148944 50436480
Alanine aminotransferase increased 24.10 22.54 3 19697 88356 50497068
Wound 23.66 22.54 6 19694 105788 50479636
Injection site inflammation 23.55 22.54 15 19685 3190 50582234
Cough 23.49 22.54 36 19664 241228 50344196
Depressed mood 23.31 22.54 45 19655 33978 50551446
Product preparation issue 23.25 22.54 9 19691 652 50584772
Urinary tract infection 23.20 22.54 32 19668 223988 50361436

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
Injection site reaction 5139.42 29.40 1234 18129 9954 29545210
Injection site pain 2812.54 29.40 978 18385 31468 29523696
Injection site mass 1410.17 29.40 382 18981 5073 29550091
Feeling abnormal 648.02 29.40 417 18946 54028 29501136
Therapeutic response shortened 610.27 29.40 194 19169 4597 29550567
Injection site induration 607.42 29.40 168 19195 2408 29552756
Product administered at inappropriate site 409.22 29.40 113 19250 1607 29553557
Injection site swelling 384.17 29.40 165 19198 9252 29545912
Withdrawal syndrome 359.68 29.40 165 19198 10827 29544337
Product dose omission issue 327.02 29.40 357 19006 96026 29459138
Needle issue 305.21 29.40 115 19248 4568 29550596
Insomnia 285.79 29.40 320 19043 88441 29466723
Lack of injection site rotation 198.91 29.40 39 19324 95 29555069
Alcohol use 193.54 29.40 74 19289 3058 29552106
Inappropriate schedule of product administration 188.68 29.40 186 19177 44286 29510878
Injection site discomfort 187.05 29.40 58 19305 1259 29553905
Depression 172.90 29.40 244 19119 84903 29470261
Pain 166.39 29.40 354 19009 171078 29384086
Drug screen positive 152.94 29.40 66 19297 3735 29551429
Anxiety 147.81 29.40 227 19136 85138 29470026
Acute kidney injury 135.83 29.40 10 19353 265257 29289907
Headache 126.57 29.40 321 19042 173686 29381478
Product administration error 123.15 29.40 90 19273 14220 29540944
Malaise 120.82 29.40 299 19064 159303 29395861
Substance abuse 116.62 29.40 66 19297 6721 29548443
Alcohol poisoning 115.69 29.40 51 19312 3038 29552126
Anaemia 114.02 29.40 4 19359 200947 29354217
Injection site abscess 112.48 29.40 34 19329 675 29554489
Nausea 110.20 29.40 426 18937 288829 29266335
Euphoric mood 108.24 29.40 56 19307 4769 29550395
Dependence 103.77 29.40 35 19328 1000 29554164
Imprisonment 101.96 29.40 29 19334 461 29554703
Drug withdrawal syndrome 98.92 29.40 87 19276 17897 29537267
Apathy 95.34 29.40 56 19307 6115 29549049
Irritability 94.48 29.40 93 19270 22059 29533105
Pneumonia 91.55 29.40 48 19315 320124 29235040
Inadequate analgesia 84.10 29.40 39 19324 2615 29552549
Feeling drunk 84.10 29.40 34 19329 1630 29553534
Injection site erythema 81.76 29.40 70 19293 13886 29541278
Yawning 79.89 29.40 24 19339 466 29554698
Decreased appetite 75.87 29.40 238 19125 145104 29410060
Injection site bruising 72.84 29.40 51 19312 7529 29547635
Tremor 71.17 29.40 152 19211 73386 29481778
Injection site nerve damage 70.48 29.40 12 19351 7 29555157
Fatigue 70.41 29.40 399 18964 316422 29238742
Road traffic accident 67.59 29.40 66 19297 15495 29539669
Injection site warmth 67.58 29.40 30 19333 1816 29553348
Lack of administration site rotation 67.00 29.40 11 19352 3 29555161
Alcoholism 65.83 29.40 33 19330 2628 29552536
Sepsis 61.25 29.40 10 19353 142672 29412492
Thrombocytopenia 61.23 29.40 8 19355 134815 29420349
Injection site nodule 60.69 29.40 26 19337 1444 29553720
Emotional poverty 59.69 29.40 19 19344 450 29554714
Alcohol withdrawal syndrome 59.05 29.40 25 19338 1348 29553816
Feeling of despair 57.72 29.40 22 19341 900 29554264
Toxicity to various agents 57.45 29.40 21 19342 173640 29381524
Atrial fibrillation 56.87 29.40 3 19360 105643 29449521
Condition aggravated 55.03 29.40 14 19349 146281 29408883
Renal failure 53.93 29.40 7 19356 118592 29436572
Depressed mood 53.89 29.40 60 19303 16388 29538776
Dyspnoea 53.74 29.40 82 19281 326650 29228514
Platelet count decreased 53.28 29.40 4 19359 104668 29450496
Gait disturbance 50.69 29.40 133 19230 73216 29481948
Pyrexia 50.41 29.40 69 19294 287553 29267611
Hospitalisation 50.27 29.40 100 19263 45888 29509276
Drug use disorder 50.10 29.40 30 19333 3392 29551772
Hypotension 49.94 29.40 33 19330 194321 29360843
Drug dependence 49.84 29.40 65 19298 20916 29534248
Neutropenia 48.78 29.40 13 19350 131698 29423466
Restlessness 48.60 29.40 66 19297 22079 29533085
Injection site pruritus 46.30 29.40 35 19328 5814 29549350
Mood altered 46.11 29.40 40 19323 8071 29547093
Respiratory failure 45.97 29.40 5 19358 97126 29458038
Haemoglobin decreased 45.60 29.40 8 19355 108367 29446797
Anger 45.07 29.40 45 19318 10845 29544319
Oedema peripheral 45.00 29.40 7 19356 103550 29451614
Overdose 44.61 29.40 134 19229 79685 29475479
Hypersomnia 43.70 29.40 44 19319 10710 29544454
Injection site cellulitis 42.59 29.40 15 19348 489 29554675
Blood creatinine increased 41.25 29.40 4 19359 85098 29470066
Toothache 40.85 29.40 32 19331 5600 29549564
Cardiac failure 40.42 29.40 3 19360 79284 29475880
General physical health deterioration 40.32 29.40 9 19354 102848 29452316
Pancytopenia 40.07 29.40 4 19359 83164 29472000
Abdominal pain upper 39.51 29.40 108 19255 60885 29494279
Substance use 39.00 29.40 14 19349 483 29554681
Alcohol abuse 38.96 29.40 28 19335 4305 29550859
Wrong technique in product usage process 38.83 29.40 72 19291 31356 29523808
Cardiac failure congestive 38.75 29.40 3 19360 76578 29478586
Coronavirus infection 38.47 29.40 25 19338 3263 29551901
Substance use disorder 38.45 29.40 12 19351 266 29554898
Injection site inflammation 38.10 29.40 15 19348 670 29554494
Mood swings 37.71 29.40 34 19329 7217 29547947
White blood cell count decreased 37.69 29.40 5 19358 83357 29471807
Sciatic nerve injury 36.73 29.40 9 19354 77 29555087
Product preparation error 36.44 29.40 19 19344 1643 29553521
Death of relative 35.71 29.40 7 19356 17 29555147
Muscle spasms 35.17 29.40 108 19255 64974 29490190
Injection site scar 34.62 29.40 11 19352 259 29554905
Panic attack 33.71 29.40 34 19329 8292 29546872
Energy increased 33.29 29.40 16 19347 1162 29554002
Abnormal dreams 33.17 29.40 31 19332 6889 29548275
Procedural pain 32.71 29.40 25 19338 4219 29550945
Chromaturia 32.50 29.40 41 19322 12761 29542403
Libido decreased 32.43 29.40 25 19338 4273 29550891
Somnolence 31.98 29.40 134 19229 93821 29461343
Injection site infection 30.93 29.40 14 19349 887 29554277
Myocardial infarction 30.70 29.40 17 19346 110279 29444885
Mobility decreased 30.52 29.40 58 19305 25722 29529442
Alanine aminotransferase increased 30.35 29.40 5 19358 70939 29484225
Surgery 30.34 29.40 38 19325 11741 29543423
Migraine 30.28 29.40 39 19324 12391 29542773
Thinking abnormal 30.12 29.40 26 19337 5210 29549954
Bradycardia 29.51 29.40 4 19359 65625 29489539

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
Injection site reaction 7421.83 22.35 2120 31825 44544 64420243
Injection site pain 3601.16 22.35 1545 32400 109863 64354924
Injection site mass 3568.85 22.35 967 32978 16303 64448484
Injection site induration 1483.12 22.35 422 33523 8510 64456277
Therapeutic response shortened 814.72 22.35 275 33670 9895 64454892
Feeling abnormal 760.86 22.35 600 33345 133002 64331785
Product administered at inappropriate site 626.03 22.35 171 33774 2939 64461848
Injection site swelling 549.82 22.35 315 33630 41038 64423749
Withdrawal syndrome 526.96 22.35 254 33691 23238 64441549
Needle issue 389.72 22.35 156 33789 9116 64455671
Product dose omission issue 381.38 22.35 490 33455 194257 64270530
Insomnia 365.95 22.35 484 33461 197352 64267435
Inappropriate schedule of product administration 334.86 22.35 321 33624 91965 64372822
Injection site abscess 291.25 22.35 79 33866 1319 64463468
Alcohol use 278.35 22.35 101 33844 4501 64460286
Drug screen positive 249.81 22.35 99 33846 5630 64459157
Depression 248.36 22.35 387 33558 182904 64281883
Lack of injection site rotation 237.05 22.35 51 33894 292 64464495
Anxiety 226.12 22.35 392 33553 202257 64262530
Injection site discomfort 219.45 22.35 83 33862 4158 64460629
Injection site nodule 195.75 22.35 71 33874 3159 64461628
Inadequate analgesia 191.99 22.35 74 33871 3904 64460883
Product administration error 189.50 22.35 139 33806 27504 64437283
Injection site warmth 185.31 22.35 105 33840 13357 64451430
Acute kidney injury 172.78 22.35 18 33927 449222 64015565
Alcohol poisoning 152.87 22.35 64 33881 4191 64460596
Injection site erythema 150.64 22.35 186 33759 70614 64394173
Euphoric mood 149.90 22.35 72 33873 6519 64458268
Irritability 148.81 22.35 136 33809 36610 64428177
Anaemia 148.62 22.35 14 33931 378666 64086121
Lack of administration site rotation 141.30 22.35 22 33923 3 64464784
Imprisonment 138.73 22.35 36 33909 502 64464285
Substance abuse 134.73 22.35 75 33870 9217 64455570
Headache 125.92 22.35 581 33364 528886 63935901
Nausea 123.45 22.35 769 33176 785031 63679756
Pneumonia 121.81 22.35 72 33873 559504 63905283
Dependence 121.80 22.35 45 33900 2110 64462677
Apathy 113.96 22.35 72 33873 11160 64453627
Malaise 111.79 22.35 458 33487 395789 64068998
Injection site pruritus 110.26 22.35 117 33828 37709 64427078
Pain 109.19 22.35 576 33369 552935 63911852
Feeling drunk 108.56 22.35 50 33895 4117 64460670
Tremor 108.11 22.35 240 33705 147990 64316797
Injection site cellulitis 105.66 22.35 37 33908 1484 64463303
Fatigue 105.38 22.35 713 33232 748017 63716770
Drug withdrawal syndrome 104.25 22.35 104 33841 31187 64433600
Decreased appetite 103.29 22.35 354 33591 280935 64183852
Condition aggravated 96.03 22.35 38 33907 372388 64092399
Dyspnoea 93.10 22.35 147 33798 718527 63746260
Body tinea 88.08 22.35 31 33914 1262 64463525
Hypotension 87.14 22.35 46 33899 380928 64083859
Injection site bruising 86.23 22.35 101 33844 36272 64428515
Thrombocytopenia 85.81 22.35 9 33936 223792 64240995
Injection site infection 84.00 22.35 33 33912 1832 64462955
Anger 83.49 22.35 68 33877 15673 64449114
Yawning 82.25 22.35 29 33916 1187 64463600
Alcohol withdrawal syndrome 81.55 22.35 32 33913 1771 64463016
Wrong technique in product usage process 80.63 22.35 132 33813 64842 64399945
Emotional poverty 80.50 22.35 25 33920 684 64464103
Atrial fibrillation 76.95 22.35 3 33942 171086 64293701
General physical health deterioration 76.40 22.35 9 33936 204416 64260371
Mood altered 76.38 22.35 65 33880 15914 64448873
Alcohol abuse 75.40 22.35 41 33904 4811 64459976
Neutropenia 75.22 22.35 17 33928 239607 64225180
Sepsis 75.05 22.35 15 33930 230326 64234461
Road traffic accident 73.92 22.35 86 33859 30659 64434128
Feeling of despair 73.81 22.35 33 33912 2535 64462252
Inhibitory drug interaction 71.66 22.35 36 33909 3591 64461196
Alcoholism 70.71 22.35 35 33910 3382 64461405
Injection site nerve damage 70.67 22.35 14 33931 49 64464738
Hypersomnia 70.26 22.35 68 33877 19649 64445138
Injection site cyst 68.62 22.35 14 33931 59 64464728
Oedema peripheral 67.88 22.35 14 33931 210303 64254484
Platelet count decreased 66.23 22.35 6 33939 167705 64297082
Infection susceptibility increased 65.71 22.35 31 33914 2695 64462092
Toothache 65.60 22.35 62 33883 17397 64447390
Panic attack 64.96 22.35 67 33878 20886 64443901
Drug dependence 63.65 22.35 83 33862 33229 64431558
Pyrexia 63.39 22.35 124 33821 558520 63906267
Pancytopenia 62.83 22.35 3 33942 143306 64321481
Disease progression 62.00 22.35 3 33942 141677 64323110
Poor quality sleep 61.30 22.35 62 33883 18889 64445898
Restlessness 60.79 22.35 89 33856 39696 64425091
Abnormal dreams 59.74 22.35 47 33898 10309 64454478
Somnolence 58.51 22.35 237 33708 203408 64261379
Malabsorption from injection site 57.63 22.35 10 33935 12 64464775
Product preparation error 57.16 22.35 32 33913 3973 64460814
Haemoglobin decreased 57.03 22.35 16 33929 195047 64269740
Blood creatinine increased 56.00 22.35 4 33941 135778 64329009
Depressed mood 55.92 22.35 87 33858 40925 64423862
Urinary tract infection 55.85 22.35 26 33919 231570 64233217
Gait disturbance 55.67 22.35 208 33737 171947 64292840
Restless legs syndrome 55.37 22.35 56 33889 17060 64447727
Injection site irritation 54.89 22.35 29 33916 3211 64461576
Renal failure 54.82 22.35 14 33931 181674 64283113
Cardiac failure 54.30 22.35 4 33941 132369 64332418
Necrosis ischaemic 53.62 22.35 20 33925 963 64463824
Renal impairment 52.85 22.35 5 33940 135012 64329775
Hospitalisation 52.77 22.35 120 33825 75087 64389700
Injection site haematoma 52.27 22.35 30 33915 3906 64460881
Drug use disorder 52.08 22.35 35 33910 6019 64458768
White blood cell count decreased 51.98 22.35 10 33935 157827 64306960
Impaired work ability 51.45 22.35 51 33894 15168 64449619
Pulmonary embolism 50.98 22.35 8 33937 146348 64318439
Gastrointestinal haemorrhage 48.99 22.35 6 33939 132306 64332481
Death of relative 48.91 22.35 13 33932 200 64464587
Pleural effusion 48.72 22.35 5 33940 126554 64338233
Alanine aminotransferase increased 47.53 22.35 8 33937 139023 64325764
Chromaturia 47.39 22.35 59 33886 22552 64442235
Crying 46.30 22.35 55 33890 20035 64444752
Muscle spasms 44.42 22.35 169 33776 140854 64323933
Libido decreased 44.40 22.35 29 33916 4755 64460032
Mood swings 43.90 22.35 50 33895 17418 64447369
Infusion related reaction 43.62 22.35 16 33929 164451 64300336
Glucose tolerance impaired 43.23 22.35 32 33913 6411 64458376
Impaired quality of life 43.11 22.35 32 33913 6439 64458348
Stomatitis 43.05 22.35 4 33941 109601 64355186
Sciatic nerve injury 43.02 22.35 14 33931 447 64464340
Cold sweat 42.88 22.35 48 33897 16407 64448380
Drug screen false positive 42.41 22.35 17 33928 995 64463792
Suicidal ideation 42.13 22.35 102 33843 66440 64398347
Injection site inflammation 41.31 22.35 24 33921 3197 64461590
Beta haemolytic streptococcal infection 40.98 22.35 20 33925 1874 64462913
Hyponatraemia 40.07 22.35 14 33931 148325 64316462
Incorrect route of product administration 39.84 22.35 55 33890 23243 64441544
Toxicity to various agents 39.18 22.35 83 33862 363430 64101357
Multiple organ dysfunction syndrome 39.05 22.35 4 33941 101409 64363378
Rheumatoid arthritis 38.74 22.35 19 33926 164275 64300512
Aspartate aminotransferase increased 38.57 22.35 8 33937 119780 64345007
Substance use 38.52 22.35 14 33931 626 64464161
Fall 37.95 22.35 104 33841 416722 64048065
Substance use disorder 37.75 22.35 12 33933 355 64464432
Respiratory failure 37.47 22.35 19 33926 161164 64303623
Surgery 37.28 22.35 59 33886 28154 64436633
Cerebrovascular accident 37.14 22.35 13 33932 137570 64327217
Drug interaction 37.10 22.35 85 33860 361998 64102789
Drug intolerance 36.95 22.35 27 33918 187965 64276822
Pneumonia streptococcal 36.68 22.35 20 33925 2358 64462429
Detoxification 36.64 22.35 9 33936 99 64464688
Magnesium deficiency 36.46 22.35 13 33932 550 64464237
Dizziness 36.01 22.35 365 33580 429798 64034989
C-reactive protein increased 35.88 22.35 4 33941 94905 64369882
Bradycardia 35.86 22.35 9 33936 118210 64346577
Influenza like illness 35.29 22.35 91 33854 61611 64403176
Pregnancy 35.29 22.35 49 33896 20816 64443971
Treatment failure 35.23 22.35 9 33936 116807 64347980
Cardio-respiratory arrest 35.13 22.35 5 33940 98388 64366399
Cough 35.11 22.35 66 33879 302082 64162705
Myocardial infarction 35.02 22.35 22 33923 165799 64298988
Musculoskeletal discomfort 34.96 22.35 43 33902 16234 64448553
Cardiac arrest 34.57 22.35 19 33926 154045 64310742
Oedema 34.44 22.35 4 33941 91931 64372856
Maternal exposure during pregnancy 33.93 22.35 5 33940 95879 64368908
Energy increased 33.92 22.35 20 33925 2738 64462049
Injection site scar 33.41 22.35 13 33932 703 64464084
Migraine 33.37 22.35 90 33855 62587 64402200
Product preparation issue 32.93 22.35 13 33932 731 64464056
Product administered by wrong person 32.75 22.35 5 33940 0 64464787
Hyperhidrosis 32.41 22.35 141 33804 124779 64340008
Product use issue 32.21 22.35 20 33925 151695 64313092
Hangover 32.16 22.35 17 33928 1884 64462903
Deep vein thrombosis 31.91 22.35 8 33937 105174 64359613
Injection site necrosis 31.73 22.35 15 33930 1310 64463477
Food craving 30.70 22.35 15 33930 1409 64463378
Abdominal pain 30.66 22.35 75 33870 312300 64152487
Syringe issue 30.37 22.35 22 33923 4264 64460523
Decreased interest 30.29 22.35 20 33925 3340 64461447
Procedural pain 30.18 22.35 39 33906 15469 64449318
Abdominal pain upper 30.17 22.35 176 33769 174854 64289933
Product physical consistency issue 29.87 22.35 11 33934 511 64464276
Rash 29.86 22.35 132 33813 458417 64006370
Emotional disorder 29.85 22.35 35 33910 12572 64452215
Dental operation 29.83 22.35 13 33932 939 64463848
Neutrophil count decreased 29.83 22.35 3 33942 77193 64387594
Oral surgery 29.66 22.35 13 33932 952 64463835
Bone density decreased 29.37 22.35 31 33914 9921 64454866
Therapeutic product effect incomplete 29.29 22.35 9 33936 103473 64361314
Product use in unapproved indication 29.08 22.35 30 33915 176588 64288199
Thinking abnormal 28.90 22.35 33 33912 11523 64453264
Drug hypersensitivity 28.46 22.35 51 33894 237764 64227023
Feeling jittery 27.67 22.35 31 33914 10604 64454183
Injection site injury 27.44 22.35 11 33934 644 64464143
Stress 27.42 22.35 82 33863 60452 64404335
Rehabilitation therapy 27.07 22.35 14 33931 1484 64463303
Hepatitis C 26.78 22.35 31 33914 10984 64453803
Wheezing 26.74 22.35 5 33940 80574 64384213
Acute myocardial infarction 26.20 22.35 3 33942 69715 64395072
Acne 26.09 22.35 45 33900 23036 64441751
Mass 26.02 22.35 36 33909 15240 64449547
Infection 25.56 22.35 36 33909 184844 64279943
Tachycardia 25.09 22.35 25 33920 149554 64315233
Leukopenia 24.95 22.35 11 33934 101231 64363556
Pruritus 24.78 22.35 83 33862 312317 64152470
Liquid product physical issue 24.77 22.35 11 33934 831 64463956
Hypokalaemia 24.61 22.35 17 33928 121886 64342901
Heat stroke 24.58 22.35 13 33932 1442 64463345
Tooth disorder 24.44 22.35 43 33902 22359 64442428
Arthropathy 24.25 22.35 17 33928 120950 64343837
Neuropathy peripheral 24.25 22.35 16 33929 117509 64347278
Adiposis dolorosa 24.13 22.35 8 33937 271 64464516
Tachyphrenia 24.12 22.35 14 33931 1862 64462925
Caffeine consumption 23.96 22.35 4 33941 3 64464784
Injection site indentation 23.77 22.35 7 33938 159 64464628
Exposure during pregnancy 23.38 22.35 6 33939 77669 64387118
Nervousness 22.80 22.35 49 33896 29507 64435280
Hypoxia 22.65 22.35 9 33936 88140 64376647
Alcoholic hangover 22.54 22.35 4 33941 6 64464781

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A08AA62 ALIMENTARY TRACT AND METABOLISM
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
Centrally acting antiobesity products
ATC N02AA56 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Natural opium alkaloids
ATC N07BB04 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in alcohol dependence
FDA MoA N0000000154 Opioid Antagonists
MeSH PA D000427 Alcohol Deterrents
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 central nervous system depressants
CHEBI has role CHEBI:35703 Xenobiotic
CHEBI has role CHEBI:50137 mu-opioid receptor antagonists
CHEBI has role CHEBI:78298 environmental contaminants
CHEBI has role CHEBI:90755 antidote to opioid overdose
FDA EPC N0000175691 Opioid Antagonist

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

DiseaseRelationSNOMED_IDDOID
Alcoholism indication 7200002
Severe pain indication 76948002
Chronic pain indication 82423001
Obesity indication 414916001 DOID:9970
Prevention of opioid abuse indication 426928008
Therapeutic opioid induced constipation indication 136801000119102
Severe Pain with Opioid Tolerance indication
Chronic Pain with Opioid Tolerance indication
Neuropathic pain off-label use 247398009
Suicidal thoughts contraindication 6471006
Alcohol withdrawal delirium contraindication 8635005
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Chronic disease of respiratory system contraindication 17097001
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Hypercapnia contraindication 29596007
Depressive disorder contraindication 35489007
Acute hepatitis contraindication 37871000
Disorder of gallbladder contraindication 39621005 DOID:0060262
Gastrointestinal ulcer contraindication 40845000
Hypothyroidism contraindication 40930008 DOID:1459
Low blood pressure contraindication 45007003
Gastrointestinal perforation contraindication 51875005
Paralytic ileus contraindication 55525008 DOID:8442
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Opioid dependence contraindication 75544000 DOID:2559
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Cor pulmonale contraindication 83291003 DOID:8515
Opioid withdrawal contraindication 87132004
Disorder of biliary tract contraindication 105997008 DOID:9741
Gastrointestinal obstruction contraindication 126765001
Seizure disorder contraindication 128613002
Drug-induced psychosis contraindication 191483003 DOID:1742
Acute hepatic failure contraindication 197270009
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Chronic diarrhea contraindication 236071009
Benign prostatic hyperplasia contraindication 266569009
Primary malignant neoplasm of gastrointestinal tract contraindication 363745004
Macrocolon contraindication 367495003
Eosinophilic asthma contraindication 367542003 DOID:9498
Primary adrenocortical insufficiency contraindication 373662000
Severe diarrhea contraindication 409587002
Central nervous system depression contraindication 418072004
Acute exacerbation of asthma contraindication 708038006
Increased Creatine Phosphokinase contraindication
Pain in Opioid Naive Patients contraindication
Opioid Use Within Last 4 Hours in Narcotic-Dependent Patient contraindication




🐶 Veterinary Drug Use

SpeciesUseRelation
Cervidae Antagonist to carfentanil citrate immobilization Indication

🐶 Veterinary products

ProductApplicantIngredients
Trexonil Wildlife Laboratories Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.31 acidic
pKa2 7.66 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 11278544 April 21, 2024 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 7462626 July 20, 2024 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 8815889 July 20, 2024 FOR EFFECT ON BLOOD GLUCOSE PARAMETERS IN PATIENTS WITH INSULIN RESISTANCE
100MG;4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
20MG;0.8MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
30MG;1.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
50MG;2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
60MG;2.4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
80MG;3.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
1.2MG;10MG TROXYCA ER PFIZER N207621 Aug. 19, 2016 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
2.4MG;20MG TROXYCA ER PFIZER N207621 Aug. 19, 2016 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
3.6MG;30MG TROXYCA ER PFIZER N207621 Aug. 19, 2016 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
4.8MG;40MG TROXYCA ER PFIZER N207621 Aug. 19, 2016 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
7.2MG;60MG TROXYCA ER PFIZER N207621 Aug. 19, 2016 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
9.6MG;80MG TROXYCA ER PFIZER N207621 Aug. 19, 2016 DISCN CAPSULE, EXTENDED RELEASE ORAL 8685443 July 3, 2025 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 9107837 June 4, 2027 USE OF NALTREXONE AND BUPROPION IN EXTENDED-RELEASE FORM FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
100MG;4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 7682633 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
100MG;4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8158156 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
20MG;0.8MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 7682633 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
20MG;0.8MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8158156 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
30MG;1.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 7682633 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
30MG;1.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8158156 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
50MG;2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 7682633 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
50MG;2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8158156 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
60MG;2.4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 7682633 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
60MG;2.4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8158156 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
80MG;3.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 7682633 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
80MG;3.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8158156 June 19, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 10307376 Nov. 8, 2027 USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 8318788 Nov. 8, 2027 USE OF NALTREXONE AND BUPROPION IN A LAYERED FORMULATION FOR CHRONIC WEIGHT MANAGEMENT FOR AFFECTING WEIGHT LOSS
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 8722085 Nov. 8, 2027 USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 9125868 Nov. 8, 2027 USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 11324741 May 29, 2029 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
380MG/VIAL VIVITROL ALKERMES N021897 April 13, 2006 RX FOR SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 7919499 Oct. 15, 2029 PREVENTION OF RELAPSE TO OPIOID DEPENDENCE, FOLLOWING OPIOID DETOXIFICATION
380MG/VIAL VIVITROL ALKERMES N021897 April 13, 2006 RX FOR SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 7919499 Oct. 15, 2029 TREATMENT OF ALCOHOL DEPENDENCE
100MG;4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8623418 Nov. 7, 2029 TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
20MG;0.8MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8623418 Nov. 7, 2029 TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
30MG;1.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8623418 Nov. 7, 2029 TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
50MG;2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8623418 Nov. 7, 2029 TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
60MG;2.4MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8623418 Nov. 7, 2029 TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
80MG;3.2MG EMBEDA ALPHARMA PHARMS N022321 Aug. 13, 2009 DISCN CAPSULE, EXTENDED RELEASE ORAL 8623418 Nov. 7, 2029 TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 8916195 Feb. 2, 2030 USE OF NALTREXONE AND BUPROPION IN EXTENDED-RELEASE FORM FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 11033543 Jan. 10, 2031 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 9248123 Jan. 13, 2032 USE OF NALTREXONE AND BUPROPION FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY IN PATIENTS WITH MAJOR DEPRESSIVE DISORDER
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 10403170 June 5, 2033 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 11139056 June 5, 2033 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 9633575 June 25, 2033 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 10231964 July 2, 2034 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 10828294 July 2, 2034 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG CONTRAVE NALPROPION N200063 Sept. 10, 2014 RX TABLET, EXTENDED RELEASE ORAL 10835527 July 2, 2034 FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Delta-type opioid receptor GPCR ANTAGONIST Ki 7.99 WOMBAT-PK CHEMBL
Kappa-type opioid receptor GPCR ANTAGONIST Ki 8.93 WOMBAT-PK CHEMBL
Mu-type opioid receptor GPCR ANTAGONIST Ki 9.38 WOMBAT-PK CHEMBL
Cytochrome P450 2D6 Enzyme IC50 6 DRUG MATRIX
Neuronal acetylcholine receptor subunit alpha-7 Ion channel IC50 4.60 CHEMBL
Mu-type opioid receptor GPCR Ki 9.34 CHEMBL
Mu-type opioid receptor GPCR Ki 9.58 CHEMBL
Mu-type opioid receptor GPCR Ki 9.77 CHEMBL
Delta-type opioid receptor GPCR Ki 7.91 CHEMBL
Delta-type opioid receptor GPCR Ki 8.32 CHEMBL
Kappa-type opioid receptor GPCR Ki 9.51 CHEMBL
Neuronal acetylcholine receptor subunit alpha-4 Ion channel IC50 4.51 CHEMBL
Kappa-type opioid receptor GPCR Ki 8.97 CHEMBL
Kappa-type opioid receptor GPCR Ki 8.84 CHEMBL
Opioid receptor GPCR Ki 9.26 CHEMBL
Opioid receptors; mu and delta GPCR Ki 9.06 CHEMBL

External reference:

IDSource
4019853 VUID
N0000147939 NUI
D02095 KEGG_DRUG
16676-29-2 SECONDARY_CAS_RN
4018545 VANDF
4019853 VANDF
C0027360 UMLSCUI
CHEBI:7465 CHEBI
CHEMBL19019 ChEMBL_ID
CHEMBL1201149 ChEMBL_ID
D009271 MESH_DESCRIPTOR_UI
DB00704 DRUGBANK_ID
1639 IUPHAR_LIGAND_ID
3368 INN_ID
850808-02-5 SECONDARY_CAS_RN
5S6W795CQM UNII
5360515 PUBCHEM_CID
105069 RXNORM
11621 MMSL
20600 MMSL
5151 MMSL
d01406 MMSL
001615 NDDF
004662 NDDF
373546002 SNOMEDCT_US
64191009 SNOMEDCT_US
87617007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NALTREXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0406-1170 TABLET, FILM COATED 50 mg ORAL ANDA 15 sections
NALTREXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0904-7036 TABLET, FILM COATED 50 mg ORAL ANDA 22 sections
EMBEDA HUMAN PRESCRIPTION DRUG LABEL 2 16590-897 CAPSULE, EXTENDED RELEASE 0.80 mg ORAL NDA 14 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 16729-081 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-632 TABLET, FILM COATED 50 mg ORAL ANDA 25 sections
ContraveExtended-Release HUMAN PRESCRIPTION DRUG LABEL 2 43063-772 TABLET, EXTENDED RELEASE 8 mg ORAL NDA 31 sections
ContraveExtended-Release HUMAN PRESCRIPTION DRUG LABEL 2 43063-772 TABLET, EXTENDED RELEASE 8 mg ORAL NDA 31 sections
NALTREXONE HYDROCHLORIDE Human Prescription Drug Label 1 47335-326 TABLET, FILM COATED 50 mg ORAL ANDA 22 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-2866 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
ContraveExtended-Release HUMAN PRESCRIPTION DRUG LABEL 2 50090-2945 TABLET, EXTENDED RELEASE 8 mg ORAL NDA 30 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-3076 TABLET, FILM COATED 50 mg ORAL ANDA 28 sections
NALTREXONE HYDROCHLORIDE Human Prescription Drug Label 1 50090-3929 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-4925 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 51224-206 TABLET, FILM COATED 50 mg ORAL ANDA 28 sections
ContraveExtended-Release HUMAN PRESCRIPTION DRUG LABEL 2 51267-890 TABLET, EXTENDED RELEASE 8 mg ORAL NDA 31 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 53217-261 TABLET, FILM COATED 50 mg ORAL ANDA 25 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-5574 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Addex-1000 HUMAN PRESCRIPTION DRUG LABEL 1 57377-010 PELLET, IMPLANTABLE 1000 mg SUBCUTANEOUS Export only 4 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 62135-242 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63629-1046 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63629-1046 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63629-1047 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63629-1047 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-2721 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
NALTREXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 68084-291 TABLET, FILM COATED 50 mg ORAL ANDA 16 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68094-853 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Naltrexone HUMAN PRESCRIPTION DRUG LABEL 2 69364-3143 IMPLANT 200 mg SUBCUTANEOUS Unapproved drug other 25 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70518-1146 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
NALTREXONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 70518-2718 TABLET, FILM COATED 50 mg ORAL ANDA 22 sections
Naltrexone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71335-0014 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections