naltrexone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists related to normorphine | 1765 | 16590-41-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 20, 1984 | FDA | TEVA WOMENS |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Injection site reaction | 3314.27 | 19.26 | 1126 | 22638 | 50040 | 53275262 |
| Alcoholism | 2573.05 | 19.26 | 493 | 23271 | 1738 | 53323564 |
| Injection site mass | 2473.19 | 19.26 | 690 | 23074 | 15524 | 53309778 |
| Injection site pain | 1239.75 | 19.26 | 715 | 23049 | 112676 | 53212626 |
| Injection site induration | 916.68 | 19.26 | 278 | 23486 | 8380 | 53316922 |
| Drug dependence | 537.65 | 19.26 | 238 | 23526 | 21234 | 53304068 |
| Therapeutic response shortened | 445.42 | 19.26 | 153 | 23611 | 6886 | 53318416 |
| Feeling abnormal | 361.91 | 19.26 | 369 | 23395 | 134932 | 53190370 |
| Product administered at inappropriate site | 280.75 | 19.26 | 85 | 23679 | 2537 | 53322765 |
| Withdrawal syndrome | 254.01 | 19.26 | 138 | 23626 | 19163 | 53306139 |
| Injection site swelling | 222.11 | 19.26 | 170 | 23594 | 42458 | 53282844 |
| Injection site abscess | 201.41 | 19.26 | 54 | 23710 | 1027 | 53324275 |
| Inappropriate schedule of product administration | 195.78 | 19.26 | 202 | 23562 | 74676 | 53250626 |
| Nausea | 179.59 | 19.26 | 736 | 23028 | 755355 | 52569947 |
| Anxiety | 138.41 | 19.26 | 284 | 23480 | 196420 | 53128882 |
| Inadequate analgesia | 137.90 | 19.26 | 51 | 23713 | 2844 | 53322458 |
| Drug use disorder | 136.21 | 19.26 | 52 | 23712 | 3167 | 53322135 |
| Insomnia | 129.12 | 19.26 | 268 | 23496 | 186804 | 53138498 |
| Injection site warmth | 127.27 | 19.26 | 79 | 23685 | 14049 | 53311253 |
| Product dose omission issue | 123.55 | 19.26 | 267 | 23497 | 191353 | 53133949 |
| Needle issue | 120.52 | 19.26 | 60 | 23704 | 6952 | 53318350 |
| Alcohol use | 115.77 | 19.26 | 41 | 23723 | 2017 | 53323285 |
| Drug screen positive | 113.42 | 19.26 | 48 | 23716 | 3824 | 53321478 |
| Injection site nodule | 111.84 | 19.26 | 46 | 23718 | 3411 | 53321891 |
| Lack of injection site rotation | 95.94 | 19.26 | 23 | 23741 | 272 | 53325030 |
| Substance abuse | 94.01 | 19.26 | 44 | 23720 | 4450 | 53320852 |
| Tremor | 88.83 | 19.26 | 182 | 23582 | 125554 | 53199748 |
| Alcohol poisoning | 85.62 | 19.26 | 32 | 23732 | 1837 | 53323465 |
| Headache | 85.14 | 19.26 | 466 | 23298 | 536355 | 52788947 |
| Rheumatoid arthritis | 83.45 | 19.26 | 19 | 23745 | 314512 | 53010790 |
| Product administration error | 80.80 | 19.26 | 71 | 23693 | 21460 | 53303842 |
| Depression | 80.30 | 19.26 | 220 | 23544 | 182832 | 53142470 |
| Body tinea | 79.43 | 19.26 | 27 | 23737 | 1174 | 53324128 |
| Lack of administration site rotation | 77.93 | 19.26 | 12 | 23752 | 3 | 53325299 |
| Pneumonia | 76.88 | 19.26 | 43 | 23721 | 407126 | 52918176 |
| Injection site pruritus | 74.08 | 19.26 | 92 | 23672 | 41497 | 53283805 |
| Euphoric mood | 72.68 | 19.26 | 37 | 23727 | 4492 | 53320810 |
| Acute kidney injury | 72.17 | 19.26 | 13 | 23751 | 253855 | 53071447 |
| Injection site erythema | 70.83 | 19.26 | 125 | 23639 | 77124 | 53248178 |
| Inhibitory drug interaction | 69.11 | 19.26 | 29 | 23735 | 2261 | 53323041 |
| Injection site discomfort | 66.66 | 19.26 | 33 | 23731 | 3775 | 53321527 |
| Dependence | 64.24 | 19.26 | 27 | 23737 | 2114 | 53323188 |
| Dizziness | 64.19 | 19.26 | 331 | 23433 | 371928 | 52953374 |
| Anaemia | 63.57 | 19.26 | 22 | 23742 | 276696 | 53048606 |
| Injection site cellulitis | 63.28 | 19.26 | 23 | 23741 | 1220 | 53324082 |
| Injection site cyst | 62.36 | 19.26 | 12 | 23752 | 43 | 53325259 |
| Drug titration error | 60.42 | 19.26 | 19 | 23745 | 644 | 53324658 |
| Infection susceptibility increased | 59.83 | 19.26 | 27 | 23737 | 2510 | 53322792 |
| Necrosis ischaemic | 59.52 | 19.26 | 20 | 23744 | 839 | 53324463 |
| Irritability | 57.58 | 19.26 | 70 | 23694 | 30883 | 53294419 |
| Injection site infection | 52.73 | 19.26 | 22 | 23742 | 1691 | 53323611 |
| Alcohol abuse | 51.98 | 19.26 | 23 | 23741 | 2041 | 53323261 |
| Feeling drunk | 50.61 | 19.26 | 28 | 23736 | 4021 | 53321281 |
| Hypotension | 50.59 | 19.26 | 25 | 23739 | 254051 | 53071251 |
| Imprisonment | 49.90 | 19.26 | 13 | 23751 | 220 | 53325082 |
| Impaired work ability | 47.99 | 19.26 | 44 | 23720 | 14046 | 53311256 |
| Food craving | 47.73 | 19.26 | 20 | 23744 | 1554 | 53323748 |
| Poor quality sleep | 47.49 | 19.26 | 48 | 23716 | 17275 | 53308027 |
| Dyspnoea | 46.70 | 19.26 | 122 | 23642 | 586110 | 52739192 |
| Glucose tolerance impaired | 46.02 | 19.26 | 29 | 23735 | 5291 | 53320011 |
| Pneumonia streptococcal | 45.54 | 19.26 | 20 | 23744 | 1743 | 53323559 |
| Neutropenia | 45.54 | 19.26 | 8 | 23756 | 159177 | 53166125 |
| Injection site bruising | 45.43 | 19.26 | 69 | 23695 | 37577 | 53287725 |
| Hospitalisation | 44.54 | 19.26 | 98 | 23666 | 70914 | 53254388 |
| Thrombocytopenia | 44.29 | 19.26 | 5 | 23759 | 138722 | 53186580 |
| Magnesium deficiency | 43.79 | 19.26 | 14 | 23750 | 501 | 53324801 |
| Feeling jittery | 43.64 | 19.26 | 39 | 23725 | 12044 | 53313258 |
| Impaired quality of life | 43.26 | 19.26 | 27 | 23737 | 4844 | 53320458 |
| General physical health deterioration | 42.88 | 19.26 | 7 | 23757 | 146935 | 53178367 |
| Beta haemolytic streptococcal infection | 42.87 | 19.26 | 20 | 23744 | 2007 | 53323295 |
| Drug intolerance | 42.77 | 19.26 | 19 | 23745 | 205474 | 53119828 |
| Systemic lupus erythematosus | 41.38 | 19.26 | 4 | 23760 | 125410 | 53199892 |
| Pregnancy | 41.35 | 19.26 | 60 | 23704 | 31381 | 53293921 |
| Crying | 40.84 | 19.26 | 50 | 23714 | 22212 | 53303090 |
| Alcohol withdrawal syndrome | 40.80 | 19.26 | 15 | 23749 | 822 | 53324480 |
| Panic attack | 40.75 | 19.26 | 49 | 23715 | 21369 | 53303933 |
| Surgery | 40.59 | 19.26 | 60 | 23704 | 31904 | 53293398 |
| Treatment failure | 40.07 | 19.26 | 5 | 23759 | 128398 | 53196904 |
| Injection site necrosis | 39.99 | 19.26 | 17 | 23747 | 1369 | 53323933 |
| Pyrexia | 39.34 | 19.26 | 75 | 23689 | 403118 | 52922184 |
| Illness | 39.00 | 19.26 | 49 | 23715 | 22347 | 53302955 |
| Wrong technique in product usage process | 38.96 | 19.26 | 84 | 23680 | 59948 | 53265354 |
| Suicidal ideation | 37.37 | 19.26 | 83 | 23681 | 60428 | 53264874 |
| Haemoglobin decreased | 36.95 | 19.26 | 8 | 23756 | 137299 | 53188003 |
| Platelet count decreased | 36.87 | 19.26 | 3 | 23761 | 108096 | 53217206 |
| Condition aggravated | 36.85 | 19.26 | 47 | 23717 | 297087 | 53028215 |
| Malabsorption from injection site | 36.84 | 19.26 | 7 | 23757 | 23 | 53325279 |
| Oedema peripheral | 36.80 | 19.26 | 15 | 23749 | 170772 | 53154530 |
| Somnolence | 36.71 | 19.26 | 160 | 23604 | 167574 | 53157728 |
| Apathy | 36.48 | 19.26 | 30 | 23734 | 8282 | 53317020 |
| Malaise | 35.28 | 19.26 | 276 | 23488 | 357341 | 52967961 |
| Detoxification | 34.81 | 19.26 | 6 | 23758 | 9 | 53325293 |
| Drug withdrawal syndrome | 33.30 | 19.26 | 51 | 23713 | 27971 | 53297331 |
| Atrial fibrillation | 33.29 | 19.26 | 5 | 23759 | 111647 | 53213655 |
| Infusion related reaction | 33.11 | 19.26 | 14 | 23750 | 155943 | 53169359 |
| Sepsis | 32.97 | 19.26 | 12 | 23752 | 146417 | 53178885 |
| Cough | 32.51 | 19.26 | 40 | 23724 | 256853 | 53068449 |
| Toothache | 32.48 | 19.26 | 40 | 23724 | 17874 | 53307428 |
| Fatigue | 32.11 | 19.26 | 479 | 23285 | 730027 | 52595275 |
| Abnormal dreams | 32.07 | 19.26 | 31 | 23733 | 10570 | 53314732 |
| Cold sweat | 31.39 | 19.26 | 32 | 23732 | 11630 | 53313672 |
| Feeling of despair | 30.77 | 19.26 | 16 | 23748 | 2029 | 53323273 |
| Death | 30.19 | 19.26 | 72 | 23692 | 357160 | 52968142 |
| Mood altered | 30.11 | 19.26 | 34 | 23730 | 13867 | 53311435 |
| Disease progression | 29.40 | 19.26 | 5 | 23759 | 101915 | 53223387 |
| Restless legs syndrome | 28.90 | 19.26 | 37 | 23727 | 17186 | 53308116 |
| Cardiac arrest | 28.37 | 19.26 | 4 | 23760 | 93663 | 53231639 |
| White blood cell count decreased | 28.36 | 19.26 | 10 | 23754 | 124465 | 53200837 |
| Pulmonary embolism | 28.20 | 19.26 | 8 | 23756 | 114434 | 53210868 |
| Restlessness | 27.74 | 19.26 | 47 | 23717 | 28040 | 53297262 |
| Hypersomnia | 27.23 | 19.26 | 35 | 23729 | 16320 | 53308982 |
| Aspartate aminotransferase increased | 26.88 | 19.26 | 3 | 23761 | 84026 | 53241276 |
| Caffeine consumption | 26.87 | 19.26 | 4 | 23760 | 0 | 53325302 |
| Exposure during pregnancy | 26.83 | 19.26 | 11 | 23753 | 124849 | 53200453 |
| Alanine aminotransferase increased | 26.71 | 19.26 | 5 | 23759 | 95090 | 53230212 |
| Fall | 26.66 | 19.26 | 77 | 23687 | 358363 | 52966939 |
| Nervousness | 26.56 | 19.26 | 48 | 23716 | 30130 | 53295172 |
| Death of relative | 26.28 | 19.26 | 8 | 23756 | 243 | 53325059 |
| Renal failure | 26.17 | 19.26 | 10 | 23754 | 118442 | 53206860 |
| Migraine | 26.08 | 19.26 | 87 | 23677 | 80330 | 53244972 |
| Product use issue | 25.90 | 19.26 | 15 | 23749 | 139569 | 53185733 |
| Mass | 25.78 | 19.26 | 30 | 23734 | 12639 | 53312663 |
| Drug screen false positive | 25.68 | 19.26 | 11 | 23753 | 902 | 53324400 |
| Hyperammonaemia | 25.61 | 19.26 | 20 | 23744 | 5129 | 53320173 |
| Bone density decreased | 25.58 | 19.26 | 28 | 23736 | 11036 | 53314266 |
| Adiposis dolorosa | 25.47 | 19.26 | 8 | 23756 | 270 | 53325032 |
| Anger | 24.64 | 19.26 | 29 | 23735 | 12361 | 53312941 |
| Purpura | 24.29 | 19.26 | 27 | 23737 | 10826 | 53314476 |
| Hyponatraemia | 24.28 | 19.26 | 9 | 23755 | 108598 | 53216704 |
| Road traffic accident | 24.14 | 19.26 | 42 | 23722 | 25589 | 53299713 |
| Blood creatinine increased | 23.97 | 19.26 | 4 | 23760 | 82658 | 53242644 |
| Arthropathy | 23.78 | 19.26 | 17 | 23747 | 141436 | 53183866 |
| Injection site irritation | 23.62 | 19.26 | 18 | 23746 | 4454 | 53320848 |
| Oral herpes | 23.01 | 19.26 | 37 | 23727 | 21142 | 53304160 |
| Rash | 22.67 | 19.26 | 112 | 23652 | 446079 | 52879223 |
| Dental operation | 22.34 | 19.26 | 11 | 23753 | 1243 | 53324059 |
| Urinary tract infection | 22.17 | 19.26 | 46 | 23718 | 239857 | 53085445 |
| Depressed mood | 22.03 | 19.26 | 50 | 23714 | 36914 | 53288388 |
| Snoring | 21.67 | 19.26 | 16 | 23748 | 3776 | 53321526 |
| Hyperhidrosis | 21.66 | 19.26 | 93 | 23671 | 96700 | 53228602 |
| Wound | 21.47 | 19.26 | 7 | 23757 | 91550 | 53233752 |
| Product preparation error | 21.44 | 19.26 | 17 | 23747 | 4458 | 53320844 |
| Yawning | 21.18 | 19.26 | 10 | 23754 | 1031 | 53324271 |
| Intentional overdose | 21.16 | 19.26 | 72 | 23692 | 67133 | 53258169 |
| Gastrointestinal haemorrhage | 20.96 | 19.26 | 5 | 23759 | 80325 | 53244977 |
| Renal impairment | 20.20 | 19.26 | 6 | 23758 | 83312 | 53241990 |
| Injection site haematoma | 20.19 | 19.26 | 19 | 23745 | 6266 | 53319036 |
| Decreased appetite | 20.10 | 19.26 | 164 | 23600 | 214810 | 53110492 |
| Joint swelling | 20.03 | 19.26 | 47 | 23717 | 234591 | 53090711 |
| Product preparation issue | 19.99 | 19.26 | 8 | 23756 | 552 | 53324750 |
| Patient dissatisfaction with treatment | 19.95 | 19.26 | 5 | 23759 | 72 | 53325230 |
| Disturbance in attention | 19.93 | 19.26 | 46 | 23718 | 34337 | 53290965 |
| Diaphragmatic paralysis | 19.70 | 19.26 | 8 | 23756 | 574 | 53324728 |
| Coronavirus infection | 19.65 | 19.26 | 14 | 23750 | 3126 | 53322176 |
| Mood swings | 19.62 | 19.26 | 31 | 23733 | 17455 | 53307847 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Injection site reaction | 5057.27 | 27.73 | 1226 | 19997 | 10343 | 32481960 |
| Alcoholism | 2903.55 | 27.73 | 629 | 20594 | 2943 | 32489360 |
| Injection site pain | 2768.40 | 27.73 | 971 | 20252 | 32087 | 32460216 |
| Injection site mass | 1398.44 | 27.73 | 380 | 20843 | 5121 | 32487182 |
| Drug dependence | 923.53 | 27.73 | 400 | 20823 | 23084 | 32469219 |
| Feeling abnormal | 652.40 | 27.73 | 435 | 20788 | 59988 | 32432315 |
| Therapeutic response shortened | 609.46 | 27.73 | 193 | 21030 | 4527 | 32487776 |
| Injection site induration | 587.34 | 27.73 | 165 | 21058 | 2519 | 32489784 |
| Product administered at inappropriate site | 395.38 | 27.73 | 111 | 21112 | 1688 | 32490615 |
| Injection site swelling | 371.99 | 27.73 | 162 | 21061 | 9422 | 32482881 |
| Withdrawal syndrome | 350.78 | 27.73 | 167 | 21056 | 11955 | 32480348 |
| Needle issue | 312.28 | 27.73 | 115 | 21108 | 4294 | 32488009 |
| Product dose omission issue | 309.47 | 27.73 | 357 | 20866 | 102218 | 32390085 |
| Insomnia | 264.28 | 27.73 | 326 | 20897 | 100022 | 32392281 |
| Drug use disorder | 251.09 | 27.73 | 93 | 21130 | 3528 | 32488775 |
| Alcohol use | 195.27 | 27.73 | 76 | 21147 | 3307 | 32488996 |
| Inappropriate schedule of product administration | 193.64 | 27.73 | 191 | 21032 | 45634 | 32446669 |
| Injection site discomfort | 193.28 | 27.73 | 59 | 21164 | 1217 | 32491086 |
| Lack of injection site rotation | 191.88 | 27.73 | 37 | 21186 | 80 | 32492223 |
| Depression | 160.13 | 27.73 | 252 | 20971 | 96808 | 32395495 |
| Pain | 159.76 | 27.73 | 367 | 20856 | 187189 | 32305114 |
| Drug screen positive | 155.77 | 27.73 | 69 | 21154 | 4172 | 32488131 |
| Acute kidney injury | 141.68 | 27.73 | 14 | 21209 | 293454 | 32198849 |
| Anxiety | 136.33 | 27.73 | 233 | 20990 | 95772 | 32396531 |
| Substance abuse | 119.31 | 27.73 | 68 | 21155 | 7039 | 32485264 |
| Product administration error | 116.33 | 27.73 | 90 | 21133 | 15535 | 32476768 |
| Headache | 114.28 | 27.73 | 333 | 20890 | 195864 | 32296439 |
| Alcohol poisoning | 112.76 | 27.73 | 51 | 21172 | 3238 | 32489065 |
| Nausea | 112.08 | 27.73 | 459 | 20764 | 320390 | 32171913 |
| Injection site abscess | 110.03 | 27.73 | 34 | 21189 | 731 | 32491572 |
| Euphoric mood | 109.81 | 27.73 | 58 | 21165 | 5169 | 32487134 |
| Malaise | 107.31 | 27.73 | 305 | 20918 | 176833 | 32315470 |
| Pneumonia | 101.42 | 27.73 | 53 | 21170 | 355199 | 32137104 |
| Dependence | 101.09 | 27.73 | 36 | 21187 | 1217 | 32491086 |
| Imprisonment | 100.73 | 27.73 | 29 | 21194 | 484 | 32491819 |
| Drug withdrawal syndrome | 99.94 | 27.73 | 92 | 21131 | 20139 | 32472164 |
| Anaemia | 99.56 | 27.73 | 14 | 21209 | 223610 | 32268693 |
| Apathy | 91.11 | 27.73 | 56 | 21167 | 6659 | 32485644 |
| Irritability | 89.91 | 27.73 | 95 | 21128 | 24559 | 32467744 |
| Inadequate analgesia | 81.39 | 27.73 | 39 | 21184 | 2824 | 32489479 |
| Feeling drunk | 79.79 | 27.73 | 34 | 21189 | 1869 | 32490434 |
| Yawning | 75.65 | 27.73 | 24 | 21199 | 564 | 32491739 |
| Injection site erythema | 74.96 | 27.73 | 68 | 21155 | 14600 | 32477703 |
| Injection site bruising | 73.86 | 27.73 | 52 | 21171 | 7768 | 32484535 |
| Injection site nerve damage | 70.51 | 27.73 | 12 | 21211 | 7 | 32492296 |
| Lack of administration site rotation | 67.04 | 27.73 | 11 | 21212 | 3 | 32492300 |
| Injection site warmth | 66.52 | 27.73 | 30 | 21193 | 1891 | 32490412 |
| Decreased appetite | 64.71 | 27.73 | 241 | 20982 | 160572 | 32331731 |
| Road traffic accident | 61.63 | 27.73 | 66 | 21157 | 17315 | 32474988 |
| Renal failure | 60.77 | 27.73 | 8 | 21215 | 134470 | 32357833 |
| Tremor | 60.22 | 27.73 | 151 | 21072 | 81126 | 32411177 |
| Injection site nodule | 59.39 | 27.73 | 26 | 21197 | 1527 | 32490776 |
| Emotional poverty | 59.28 | 27.73 | 19 | 21204 | 462 | 32491841 |
| Fatigue | 58.06 | 27.73 | 409 | 20814 | 350292 | 32142011 |
| Sepsis | 57.96 | 27.73 | 16 | 21207 | 158818 | 32333485 |
| Toxicity to various agents | 57.81 | 27.73 | 22 | 21201 | 178019 | 32314284 |
| Hypotension | 57.55 | 27.73 | 35 | 21188 | 216075 | 32276228 |
| Thrombocytopenia | 55.89 | 27.73 | 14 | 21209 | 148285 | 32344018 |
| Feeling of despair | 55.63 | 27.73 | 22 | 21201 | 998 | 32491305 |
| Dyspnoea | 55.22 | 27.73 | 95 | 21128 | 361950 | 32130353 |
| Atrial fibrillation | 55.05 | 27.73 | 6 | 21217 | 116698 | 32375605 |
| Alcohol withdrawal syndrome | 53.91 | 27.73 | 24 | 21199 | 1467 | 32490836 |
| Pyrexia | 53.45 | 27.73 | 79 | 21144 | 319889 | 32172414 |
| Depressed mood | 52.11 | 27.73 | 62 | 21161 | 18238 | 32474065 |
| Platelet count decreased | 51.33 | 27.73 | 7 | 21216 | 114584 | 32377719 |
| Neutropenia | 50.61 | 27.73 | 15 | 21208 | 142160 | 32350143 |
| Haemoglobin decreased | 49.78 | 27.73 | 9 | 21214 | 119662 | 32372641 |
| Respiratory failure | 46.94 | 27.73 | 7 | 21216 | 107175 | 32385128 |
| Condition aggravated | 46.10 | 27.73 | 22 | 21201 | 155639 | 32336664 |
| Anger | 45.40 | 27.73 | 47 | 21176 | 11857 | 32480446 |
| Injection site pruritus | 45.13 | 27.73 | 35 | 21188 | 6055 | 32486248 |
| Disease progression | 44.95 | 27.73 | 3 | 21220 | 86859 | 32405444 |
| Pancytopenia | 44.82 | 27.73 | 4 | 21219 | 91231 | 32401072 |
| Mood altered | 43.00 | 27.73 | 40 | 21183 | 8864 | 32483439 |
| Blood creatinine increased | 42.74 | 27.73 | 6 | 21217 | 96126 | 32396177 |
| Oedema peripheral | 42.53 | 27.73 | 11 | 21212 | 114080 | 32378223 |
| Injection site cellulitis | 42.09 | 27.73 | 15 | 21208 | 508 | 32491795 |
| Gait disturbance | 41.45 | 27.73 | 131 | 21092 | 80277 | 32412026 |
| Restlessness | 41.44 | 27.73 | 65 | 21158 | 24816 | 32467487 |
| Substance use disorder | 41.15 | 27.73 | 12 | 21211 | 210 | 32492093 |
| Cardiac failure congestive | 40.94 | 27.73 | 4 | 21219 | 84848 | 32407455 |
| Hospitalisation | 40.54 | 27.73 | 95 | 21128 | 48876 | 32443427 |
| Overdose | 40.52 | 27.73 | 137 | 21086 | 86940 | 32405363 |
| Toothache | 40.31 | 27.73 | 33 | 21190 | 6168 | 32486135 |
| Cardiac failure | 40.11 | 27.73 | 6 | 21217 | 91667 | 32400636 |
| Hypersomnia | 39.92 | 27.73 | 44 | 21179 | 11917 | 32480386 |
| General physical health deterioration | 39.50 | 27.73 | 13 | 21210 | 115246 | 32377057 |
| Alcohol abuse | 38.24 | 27.73 | 28 | 21195 | 4444 | 32487859 |
| Substance use | 37.78 | 27.73 | 14 | 21209 | 531 | 32491772 |
| Hangover | 37.54 | 27.73 | 17 | 21206 | 1082 | 32491221 |
| Injection site inflammation | 37.08 | 27.73 | 15 | 21208 | 722 | 32491581 |
| Abdominal pain upper | 36.82 | 27.73 | 112 | 21111 | 67226 | 32425077 |
| Coronavirus infection | 35.78 | 27.73 | 25 | 21198 | 3687 | 32488616 |
| White blood cell count decreased | 35.54 | 27.73 | 8 | 21215 | 91190 | 32401113 |
| Myocardial infarction | 35.34 | 27.73 | 19 | 21204 | 125657 | 32366646 |
| Sciatic nerve injury | 35.05 | 27.73 | 9 | 21214 | 95 | 32492208 |
| Death of relative | 34.91 | 27.73 | 7 | 21216 | 20 | 32492283 |
| Wrong technique in product usage process | 34.62 | 27.73 | 73 | 21150 | 34986 | 32457317 |
| Mood swings | 34.35 | 27.73 | 34 | 21189 | 8131 | 32484172 |
| Product preparation error | 34.20 | 27.73 | 19 | 21204 | 1871 | 32490432 |
| Panic attack | 32.53 | 27.73 | 35 | 21188 | 9226 | 32483077 |
| Energy increased | 31.44 | 27.73 | 16 | 21207 | 1319 | 32490984 |
| Hyperhidrosis | 31.37 | 27.73 | 110 | 21113 | 71058 | 32421245 |
| Urinary tract infection | 31.24 | 27.73 | 7 | 21216 | 80064 | 32412239 |
| Thinking abnormal | 30.51 | 27.73 | 27 | 21196 | 5608 | 32486695 |
| Injection site infection | 30.50 | 27.73 | 14 | 21209 | 919 | 32491384 |
| Libido decreased | 30.44 | 27.73 | 25 | 21198 | 4693 | 32487610 |
| Muscle spasms | 30.32 | 27.73 | 108 | 21115 | 70310 | 32421993 |
| Feeling jittery | 29.67 | 27.73 | 23 | 21200 | 3976 | 32488327 |
| Product use in unapproved indication | 29.58 | 27.73 | 10 | 21213 | 87194 | 32405109 |
| Emotional disorder | 29.32 | 27.73 | 26 | 21197 | 5415 | 32486888 |
| Mobility decreased | 29.04 | 27.73 | 60 | 21163 | 28349 | 32463954 |
| Chromaturia | 28.64 | 27.73 | 41 | 21182 | 14437 | 32477866 |
| Bradycardia | 28.44 | 27.73 | 6 | 21217 | 71556 | 32420747 |
| Suicidal ideation | 28.42 | 27.73 | 71 | 21152 | 38012 | 32454291 |
| Surgery | 28.41 | 27.73 | 38 | 21185 | 12561 | 32479742 |
| Migraine | 28.25 | 27.73 | 40 | 21183 | 13945 | 32478358 |
| Drug interaction | 28.18 | 27.73 | 63 | 21160 | 218122 | 32274181 |
| Alcoholic hangover | 27.74 | 27.73 | 5 | 21218 | 6 | 32492297 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | CNS 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 (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.31 | acidic |
| pKa2 | 7.66 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 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 |
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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 |
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |
| 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 | 63629-1047 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 27 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 |
| NALTREXONE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-1480 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 15 sections |
| NALTREXONE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76519-1160 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 13 sections |