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

Stem definitionDrug idCAS RN
1728 76-99-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • metadone
  • methadone
  • methadone hydrochloride
  • methadone HCl
A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)
  • Molecular weight: 309.45
  • Formula: C21H27NO
  • CLOGP: 4.17
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 20.31
  • ALOGS: -4.72
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
25 mg O
25 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 120 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 24 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.62 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 92 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 4.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.21 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 31 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 13, 1947 FDA ROXANE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug abuse 2181.03 12.26 998 31215 62410 46591439
Toxicity to various agents 1591.91 12.26 1247 30966 210519 46443330
Respiratory arrest 770.76 12.26 403 31810 33413 46620436
Completed suicide 697.97 12.26 666 31547 145254 46508595
Cardiac arrest 546.20 12.26 471 31742 89928 46563921
Exposure during pregnancy 505.46 12.26 488 31725 107724 46546125
Cardio-respiratory arrest 504.12 12.26 379 31834 59490 46594359
Poisoning 342.10 12.26 175 32038 13819 46640030
Premature delivery 307.78 12.26 191 32022 21878 46631971
Death 304.97 12.26 696 31517 334852 46318997
Overdose 302.63 12.26 362 31851 101617 46552232
Torsade de pointes 285.54 12.26 148 32065 12006 46641843
Intentional product misuse 233.67 12.26 220 31993 46908 46606941
Premature labour 227.07 12.26 124 32089 11175 46642674
Drug dependence 220.27 12.26 149 32064 19752 46634097
Drug withdrawal syndrome 203.16 12.26 161 32052 27223 46626626
Accidental overdose 202.66 12.26 142 32071 19924 46633925
Drug withdrawal syndrome neonatal 196.99 12.26 67 32146 1861 46651988
Respiratory depression 191.69 12.26 112 32101 11488 46642361
Maternal exposure during pregnancy 164.30 12.26 271 31942 102278 46551571
Electrocardiogram QT prolonged 161.61 12.26 188 32025 51137 46602712
Drug diversion 108.28 12.26 35 32178 826 46653023
Unresponsive to stimuli 103.15 12.26 119 32094 32055 46621794
Rheumatoid arthritis 97.64 12.26 23 32190 240192 46413657
Hyperaesthesia 89.72 12.26 60 32153 7796 46646053
Miosis 81.25 12.26 53 32160 6604 46647245
Exposure via ingestion 80.77 12.26 42 32171 3425 46650424
Drug interaction 80.75 12.26 315 31898 202779 46451070
Withdrawal syndrome 79.16 12.26 79 32134 18055 46635794
Somnolence 72.42 12.26 255 31958 156266 46497583
Delirium 70.04 12.26 106 32107 37122 46616727
Coma 66.33 12.26 133 32080 58216 46595633
Accidental death 63.09 12.26 29 32184 1806 46652043
Drug screen positive 62.77 12.26 37 32176 3854 46649995
Substance abuse 60.42 12.26 37 32176 4130 46649719
Sedation 59.20 12.26 76 32137 22834 46631015
Accidental exposure to product by child 55.77 12.26 23 32190 1100 46652749
Diarrhoea 55.76 12.26 199 32014 559403 46094446
Mental status changes 50.88 12.26 93 32120 37995 46615854
Drug ineffective 49.42 12.26 271 31942 677567 45976282
Drug use disorder 49.42 12.26 28 32185 2707 46651142
Leukoencephalopathy 49.16 12.26 32 32181 3972 46649877
Toxic leukoencephalopathy 47.93 12.26 17 32196 536 46653313
Drug abuser 47.63 12.26 29 32184 3204 46650645
Accidental poisoning 46.44 12.26 17 32196 588 46653261
Foetal exposure during pregnancy 46.13 12.26 79 32134 30668 46623181
Rash 45.36 12.26 113 32100 356399 46297450
Bradypnoea 41.56 12.26 26 32187 3013 46650836
Inadequate analgesia 40.75 12.26 25 32188 2799 46651050
Cough 39.63 12.26 61 32152 230188 46423661
Drug tolerance 37.76 12.26 25 32188 3193 46650656
Suspected counterfeit product 35.99 12.26 12 32201 313 46653536
Congenital nystagmus 35.25 12.26 6 32207 3 46653846
Depressed level of consciousness 34.67 12.26 91 32122 47478 46606371
Atrial fibrillation 33.11 12.26 15 32198 103575 46550274
Affective disorder 32.90 12.26 27 32186 4788 46649061
Nasopharyngitis 31.37 12.26 36 32177 153962 46499887
Intentional overdose 31.00 12.26 107 32106 64837 46589012
Urticaria 30.63 12.26 22 32191 117870 46535979
Pulmonary oedema 30.58 12.26 91 32122 51014 46602835
Hypoxic-ischaemic encephalopathy 30.29 12.26 24 32189 4049 46649800
Ventricular tachycardia 30.05 12.26 47 32166 16920 46636929
Erythema 29.51 12.26 33 32180 142787 46511062
Cyanosis 29.35 12.26 45 32168 15926 46637923
Off label use 28.02 12.26 151 32062 379690 46274159
Drug intolerance 27.20 12.26 37 32176 147012 46506837
Neurological examination abnormal 27.13 12.26 9 32204 231 46653618
Joint swelling 26.68 12.26 46 32167 166027 46487822
Asphyxia 26.62 12.26 25 32188 5301 46648548
Ventricular fibrillation 26.40 12.26 36 32177 11460 46642389
Crying 26.20 12.26 50 32163 21091 46632758
Pruritus 26.19 12.26 83 32130 242269 46411580
Neonatal complications of substance abuse 25.91 12.26 5 32208 10 46653839
Substance use disorder 25.62 12.26 6 32207 39 46653810
Infection 25.33 12.26 33 32180 133559 46520290
Poisoning deliberate 24.86 12.26 29 32184 7897 46645952
Alopecia 24.29 12.26 47 32166 162367 46491482
Loss of consciousness 24.00 12.26 142 32071 108096 46545753
Basal ganglia infarction 23.78 12.26 9 32204 342 46653507
Arthralgia 23.65 12.26 151 32062 364452 46289397
Sinusitis 23.65 12.26 33 32180 129735 46524114
Infusion related reaction 23.64 12.26 21 32192 101187 46552662
Agitation 23.63 12.26 88 32125 55327 46598522
Cardio-respiratory distress 23.49 12.26 7 32206 125 46653724
Anaemia 23.38 12.26 94 32119 255685 46398164
Systemic lupus erythematosus 23.18 12.26 8 32205 65172 46588677
Suicidal ideation 22.77 12.26 88 32125 56294 46597555
Brain oedema 22.71 12.26 35 32178 12443 46641406
Abdominal discomfort 22.38 12.26 44 32169 151121 46502728
Hypersensitivity 22.05 12.26 44 32169 150277 46503572
Febrile neutropenia 21.66 12.26 20 32193 94607 46559242
Confusional state 21.57 12.26 186 32027 159706 46494143
Seizure 21.49 12.26 152 32061 122902 46530947
Treatment failure 20.93 12.26 20 32193 93067 46560782
Post-anoxic myoclonus 20.78 12.26 5 32208 37 46653812
Cardiac failure 20.66 12.26 15 32198 79933 46573916
Hyponatraemia 20.29 12.26 24 32189 101308 46552541
Peripheral swelling 20.13 12.26 50 32163 158021 46495828
Neutropenia 20.08 12.26 43 32170 143161 46510688
Hepatitis C 19.62 12.26 23 32190 6295 46647554
Exposure via breast milk 19.59 12.26 12 32201 1340 46652509
Pulmonary congestion 19.58 12.26 36 32177 14763 46639086
Contraindicated product administered 19.38 12.26 16 32197 79931 46573918
Fatigue 19.28 12.26 300 31913 608397 46045452
Tachyphylaxis 19.15 12.26 7 32206 241 46653608
Glossodynia 18.49 12.26 4 32209 44369 46609480
Respiratory acidosis 18.46 12.26 22 32191 6126 46647723
Long QT syndrome 18.43 12.26 16 32197 3064 46650785
Arthritis 18.10 12.26 16 32197 77300 46576549
Swelling 17.78 12.26 37 32176 124474 46529375
Palpitations 17.58 12.26 24 32189 95235 46558614
Pyrexia 17.15 12.26 156 32057 348646 46305203
Brain hypoxia 17.04 12.26 8 32205 523 46653326
Injection site reaction 16.80 12.26 6 32207 47843 46606006
Pneumonia aspiration 16.79 12.26 54 32159 31551 46622298
Chest discomfort 16.40 12.26 23 32190 90246 46563603
Synovitis 16.38 12.26 11 32202 61064 46592785
Respiratory rate decreased 16.32 12.26 15 32198 3095 46650754
Hodgkin's disease 16.19 12.26 9 32204 839 46653010
Injection site pain 16.02 12.26 31 32182 107121 46546728
Herpes zoster 15.94 12.26 14 32199 67858 46585991
Sudden infant death syndrome 15.85 12.26 6 32207 228 46653621
Housebound 15.76 12.26 6 32207 232 46653617
Low birth weight baby 15.59 12.26 19 32194 5415 46648434
Epistaxis 15.43 12.26 13 32200 64292 46589557
Pleural adhesion 15.43 12.26 5 32208 119 46653730
Product dose omission issue 15.34 12.26 62 32151 168458 46485391
Injection site bruising 15.29 12.26 3 32210 35633 46618216
Narcotic bowel syndrome 15.12 12.26 5 32208 127 46653722
Arthropathy 14.97 12.26 22 32191 84678 46569171
Faeces hard 14.94 12.26 10 32203 1301 46652548
Thyroxine decreased 14.83 12.26 7 32206 463 46653386
Radiation associated pain 14.82 12.26 4 32209 49 46653800
Dizziness 14.73 12.26 157 32056 340257 46313592
Hand deformity 14.64 12.26 3 32210 34571 46619278
Respiratory paralysis 14.45 12.26 3 32210 10 46653839
Spleen congestion 14.21 12.26 5 32208 154 46653695
Drug level increased 14.17 12.26 36 32177 18405 46635444
Acute kidney injury 14.10 12.26 100 32113 235755 46418094
Aggression 14.08 12.26 41 32172 22703 46631146
Pseudohyperkalaemia 14.02 12.26 3 32210 12 46653837
Restlessness 13.91 12.26 44 32169 25480 46628369
Catatonia 13.91 12.26 15 32198 3747 46650102
Genital herpes simplex 13.91 12.26 5 32208 164 46653685
Hypercapnic coma 13.82 12.26 5 32208 167 46653682
Allodynia 13.72 12.26 7 32206 548 46653301
Breakthrough pain 13.64 12.26 9 32204 1143 46652706
Retroperitoneal fibrosis 13.63 12.26 6 32207 337 46653512
Secondary adrenocortical insufficiency 13.28 12.26 8 32205 867 46652982
Lethargy 13.23 12.26 70 32143 51101 46602748
Myoclonus 13.16 12.26 30 32183 14322 46639527
Therapeutic product effect decreased 13.14 12.26 23 32190 82578 46571271
Accidental exposure to product 13.05 12.26 38 32175 21043 46632806
General physical health deterioration 12.94 12.26 39 32174 115730 46538119
Leukopenia 12.83 12.26 17 32196 68326 46585523
Suicide attempt 12.70 12.26 73 32140 54963 46598886
Substance dependence 12.50 12.26 5 32208 221 46653628
Emotional distress 12.45 12.26 48 32165 30659 46623190
Ventricular extrasystoles 12.30 12.26 25 32188 11038 46642811

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug abuse 3363.09 13.03 1779 37318 80293 29833088
Toxicity to various agents 2782.67 13.03 2088 37009 175095 29738286
Respiratory arrest 963.96 13.03 552 38545 28706 29884675
Overdose 630.62 13.03 657 38440 83680 29829701
Respiratory depression 566.88 13.03 284 38813 11219 29902162
Poisoning 534.50 13.03 272 38825 11110 29902271
Cardiac arrest 531.30 13.03 629 38468 92221 29821160
Cardio-respiratory arrest 487.34 13.03 479 38618 56827 29856554
Completed suicide 463.36 13.03 608 38489 98884 29814497
Intentional product misuse 451.97 13.03 369 38728 34298 29879083
Electrocardiogram QT prolonged 435.05 13.03 366 38731 35469 29877912
Drug dependence 393.07 13.03 279 38818 21016 29892365
Torsade de pointes 385.29 13.03 188 38909 7002 29906379
Coma 352.72 13.03 343 38754 40106 29873275
Accidental overdose 317.88 13.03 231 38866 18044 29895337
Substance abuse 283.94 13.03 152 38945 6888 29906493
Death 266.37 13.03 1042 38055 356241 29557140
Miosis 258.99 13.03 148 38949 7628 29905753
Drug withdrawal syndrome 229.27 13.03 197 38900 19612 29893769
Drug interaction 227.52 13.03 672 38425 198896 29714485
Withdrawal syndrome 199.65 13.03 144 38953 11106 29902275
Drug withdrawal syndrome neonatal 191.27 13.03 90 39007 3085 29910296
Serotonin syndrome 171.50 13.03 160 38937 17731 29895650
Unresponsive to stimuli 160.55 13.03 185 38912 26234 29887147
Somnolence 146.19 13.03 362 38735 96401 29816980
Asphyxia 145.98 13.03 90 39007 5335 29908046
Bradypnoea 139.44 13.03 62 39035 1859 29911522
Drug diversion 126.78 13.03 47 39050 869 29912512
Prescription drug used without a prescription 125.75 13.03 51 39046 1211 29912170
Drug screen positive 123.40 13.03 75 39022 4332 29909049
Diarrhoea 112.67 13.03 164 38933 333939 29579442
Depressed level of consciousness 107.57 13.03 185 38912 38037 29875344
Brain oedema 96.58 13.03 99 38998 12299 29901082
Hepatic fibrosis 92.79 13.03 58 39039 3522 29909859
Exposure via ingestion 85.05 13.03 49 39048 2562 29910819
Pulmonary oedema 81.04 13.03 178 38919 43797 29869584
Pyrexia 77.12 13.03 169 38928 294320 29619061
Brain injury 74.15 13.03 60 39037 5488 29907893
Drug abuser 68.33 13.03 52 39045 4349 29909032
Sedation 66.68 13.03 94 39003 16279 29897102
Hyperaesthesia 66.27 13.03 47 39050 3526 29909855
Drug use disorder 65.56 13.03 45 39052 3203 29910178
Delirium 65.48 13.03 156 38941 40475 29872906
Drug tolerance 63.64 13.03 38 39059 2124 29911257
Hypoxic-ischaemic encephalopathy 59.09 13.03 49 39048 4638 29908743
Febrile neutropenia 58.90 13.03 33 39064 106660 29806721
Self-medication 56.53 13.03 36 39061 2258 29911123
Cough 55.98 13.03 49 39048 125593 29787788
Ventricular tachyarrhythmia 55.09 13.03 19 39078 282 29913099
Off label use 55.08 13.03 156 38941 249134 29664247
Housebound 54.18 13.03 17 39080 184 29913197
Brachial plexopathy 53.54 13.03 13 39084 47 29913334
Loss of consciousness 53.28 13.03 225 38872 79150 29834231
Respiratory acidosis 53.12 13.03 44 39053 4158 29909223
Interstitial lung disease 52.36 13.03 8 39089 60189 29853192
Atrial fibrillation 52.11 13.03 39 39058 108085 29805296
Toxicologic test abnormal 51.71 13.03 22 39075 591 29912790
Rhabdomyolysis 50.51 13.03 190 38907 63390 29849991
Accidental death 49.68 13.03 32 39065 2047 29911334
Cardiopulmonary failure 49.54 13.03 41 39056 3870 29909511
Postmortem blood drug level abnormal 48.12 13.03 16 39081 211 29913170
Poisoning deliberate 47.53 13.03 48 39049 5856 29907525
Cardiac failure 47.19 13.03 25 39072 83393 29829988
Neutropenia 46.23 13.03 60 39037 128480 29784901
Drug-induced liver injury 46.03 13.03 92 39005 21182 29892199
Agitation 45.81 13.03 165 38932 53908 29859473
Cardiac failure congestive 45.30 13.03 27 39070 84380 29829001
Accidental exposure to product by child 44.78 13.03 27 39070 1536 29911845
Mental status changes 43.03 13.03 126 38971 36953 29876428
Substance dependence 42.09 13.03 17 39080 399 29912982
Acute kidney injury 41.05 13.03 201 38896 273641 29639740
Myocardial infarction 39.89 13.03 64 39033 125561 29787820
Hepatitis C 39.88 13.03 66 39031 13139 29900242
Sepsis 39.87 13.03 82 39015 146313 29767068
Dyspnoea 39.56 13.03 264 38833 333031 29580350
Compartment syndrome 39.54 13.03 30 39067 2497 29910884
Intentional overdose 38.96 13.03 131 38966 41350 29872031
Asthenia 38.86 13.03 153 38944 221137 29692244
Visceral congestion 37.70 13.03 17 39080 527 29912854
Platelet count decreased 36.67 13.03 51 39046 106078 29807303
Rash 36.07 13.03 129 38968 191760 29721621
Myocardial fibrosis 36.06 13.03 18 39079 703 29912678
Pleural effusion 35.30 13.03 27 39070 74039 29839342
Biliary dilatation 35.12 13.03 18 39079 744 29912637
Foetal growth restriction 34.21 13.03 32 39065 3553 29909828
Pulmonary congestion 33.91 13.03 59 39038 12228 29901153
Aspiration 33.58 13.03 54 39043 10497 29902884
Fatigue 33.20 13.03 264 38833 320409 29592972
Leukoencephalopathy 33.06 13.03 33 39064 3969 29909412
General physical health deterioration 32.59 13.03 50 39047 99894 29813487
Hypercapnia 32.46 13.03 32 39065 3792 29909589
Pneumonia 32.45 13.03 280 38817 334026 29579355
Incorrect route of product administration 32.10 13.03 55 39042 11260 29902121
Foetal exposure during pregnancy 31.63 13.03 113 38984 36758 29876623
Pneumoconiosis 30.14 13.03 12 39085 271 29913110
Pneumonia aspiration 30.06 13.03 113 38984 37667 29875714
Drug ineffective 30.04 13.03 292 38805 340095 29573286
Condition aggravated 29.84 13.03 87 39010 137779 29775602
Ventricular tachycardia 29.53 13.03 83 39014 23779 29889602
Cerebrovascular accident 28.94 13.03 40 39057 83437 29829944
Gastrointestinal haemorrhage 28.91 13.03 40 39057 83406 29829975
Withdrawal arrhythmia 28.27 13.03 7 39090 28 29913353
Renal failure 28.18 13.03 81 39016 128885 29784496
Decreased appetite 28.00 13.03 101 38996 149809 29763572
Haematuria 27.54 13.03 12 39085 44822 29868559
Laryngomalacia 27.12 13.03 11 39086 261 29913120
Rheumatoid arthritis 26.98 13.03 10 39087 41187 29872194
Victim of child abuse 26.44 13.03 11 39086 279 29913102
IVth nerve disorder 25.56 13.03 6 39091 18 29913363
Dizziness 25.31 13.03 150 38947 194759 29718622
Coronary artery disease 25.15 13.03 17 39080 49695 29863686
Respiratory rate decreased 25.04 13.03 20 39077 1795 29911586
Arthralgia 25.01 13.03 92 39005 135699 29777682
Electrocardiogram QT shortened 24.76 13.03 9 39088 157 29913224
Hyponatraemia 24.52 13.03 31 39066 67171 29846210
Ectopic kidney 24.42 13.03 7 39090 54 29913327
Hypersensitivity 24.12 13.03 21 39076 54007 29859374
Apnoea 24.11 13.03 35 39062 6223 29907158
Brachial plexus injury 23.96 13.03 8 39089 107 29913274
Renal impairment 23.88 13.03 46 39051 84138 29829243
Suicide attempt 23.80 13.03 103 38994 36594 29876787
Disease progression 23.22 13.03 43 39054 79831 29833550
Epistaxis 23.16 13.03 21 39076 52960 29860421
Postoperative ileus 22.66 13.03 13 39084 674 29912707
Dependence 22.44 13.03 16 39081 1210 29912171
Sudden cardiac death 22.31 13.03 26 39071 3726 29909655
Sopor 21.96 13.03 46 39051 10945 29902436
Sudden death 21.28 13.03 56 39041 15436 29897945
Pruritus 21.17 13.03 81 39016 118123 29795258
Sinus bradycardia 21.13 13.03 47 39050 11648 29901733
Thrombocytopenia 20.81 13.03 100 38997 136944 29776437
Pupil fixed 20.73 13.03 18 39079 1814 29911567
Anaemia 20.66 13.03 173 38924 207819 29705562
Accidental poisoning 20.64 13.03 11 39086 493 29912888
Haemoglobin decreased 20.55 13.03 78 39019 114020 29799361
Lethargy 20.54 13.03 104 38993 39415 29873966
White blood cell count decreased 20.39 13.03 50 39047 83897 29829484
Myoclonus 20.24 13.03 50 39047 13262 29900119
Angioedema 19.88 13.03 10 39087 34374 29879007
Encephalopathy 19.82 13.03 89 39008 32116 29881265
Product dose omission issue 19.68 13.03 58 39039 91573 29821808
International normalised ratio increased 19.61 13.03 20 39077 47719 29865662
Psoriasis 19.61 13.03 16 39081 42490 29870891
Central nervous system necrosis 19.53 13.03 7 39090 117 29913264
Cyanosis 19.40 13.03 46 39051 11889 29901492
Product administered to patient of inappropriate age 19.24 13.03 20 39077 2523 29910858
Confusional state 19.14 13.03 264 38833 134570 29778811
Urticaria 19.08 13.03 26 39071 54580 29858801
Chronic kidney disease 19.06 13.03 13 39084 37825 29875556
Joint swelling 18.91 13.03 20 39077 46926 29866455
Blood creatinine increased 18.79 13.03 59 39038 91316 29822065
Accidental exposure to product 18.67 13.03 41 39056 10074 29903307
Peripheral swelling 18.54 13.03 32 39065 61042 29852339
Intentional misuse of drug delivery system 18.53 13.03 4 39093 7 29913374
Transient ischaemic attack 18.48 13.03 5 39092 25195 29888186
Contraindication to medical treatment 18.23 13.03 10 39087 475 29912906
Erythema 18.14 13.03 47 39050 77404 29835977
Oedema peripheral 18.00 13.03 74 39023 105758 29807623
Hyperhidrosis 17.81 13.03 149 38948 66941 29846440
Muscle mass 17.48 13.03 8 39089 257 29913124
Asthma 17.47 13.03 13 39084 36161 29877220
Hyperreflexia 17.43 13.03 20 39077 2819 29910562
Pulse absent 17.40 13.03 28 39069 5445 29907936
Anoxia 17.34 13.03 6 39091 90 29913291
Blood lactate dehydrogenase increased 17.32 13.03 3 39094 20598 29892783
Mononeuropathy 17.16 13.03 6 39091 93 29913288
Chloasma 16.80 13.03 4 39093 13 29913368
Drug resistance 16.78 13.03 3 39094 20130 29893251
Deafness neurosensory 16.65 13.03 18 39079 2375 29911006
Ventricular arrhythmia 16.54 13.03 24 39073 4264 29909117
Cluster headache 16.54 13.03 10 39087 572 29912809
Euphoric mood 16.53 13.03 24 39073 4266 29909115
Anaphylactic reaction 16.39 13.03 8 39089 27974 29885407
Dysarthria 16.38 13.03 81 39016 30409 29882972
Colitis 16.32 13.03 10 39087 30810 29882571
Product use in unapproved indication 16.29 13.03 46 39051 73647 29839734
Synostosis 16.23 13.03 6 39091 110 29913271
Neutrophil count decreased 16.09 13.03 19 39078 42435 29870946
Treatment failure 16.06 13.03 13 39084 34666 29878715
Blood urine 16.06 13.03 9 39088 446 29912935
Cardiac disorder 16.06 13.03 17 39080 39876 29873505
Dehydration 16.05 13.03 95 39002 123444 29789937
Premature baby 15.92 13.03 53 39044 16638 29896743
Acute myocardial infarction 15.83 13.03 28 39069 52911 29860470
Treatment noncompliance 15.70 13.03 70 39027 25183 29888198
Anticholinergic syndrome 15.65 13.03 11 39086 813 29912568
Haematochezia 15.64 13.03 13 39084 34209 29879172
Child abuse 15.61 13.03 7 39090 214 29913167
Hospitalisation 15.59 13.03 21 39076 44298 29869083
Fall 15.56 13.03 157 38940 181715 29731666
Dyspnoea exertional 15.53 13.03 14 39083 35416 29877965
Blood glucose increased 15.45 13.03 36 39061 61494 29851887
Prostate cancer 15.37 13.03 6 39091 23951 29889430
Leukopenia 14.80 13.03 32 39065 56127 29857254
Abdominal distension 14.76 13.03 23 39074 45686 29867695
Elbow synostosis 14.68 13.03 4 39093 25 29913356
Mucosal inflammation 14.67 13.03 11 39086 30483 29882898
Perforated ulcer 14.65 13.03 6 39091 146 29913235
Neuromuscular blockade 14.50 13.03 6 39091 150 29913231
Maternal exposure during breast feeding 14.49 13.03 14 39083 1618 29911763
Nasopharyngitis 14.33 13.03 35 39062 58814 29854567
Infection 14.29 13.03 53 39044 78021 29835360
Toxic epidermal necrolysis 14.26 13.03 3 39094 17937 29895444
Neuropathy peripheral 14.14 13.03 46 39051 70429 29842952
Gastric bypass 14.03 13.03 7 39090 273 29913108
Melaena 14.00 13.03 13 39084 32424 29880957
Liver disorder 13.94 13.03 11 39086 29711 29883670
Local anaesthetic systemic toxicity 13.91 13.03 6 39091 167 29913214
Medication error 13.70 13.03 59 39038 20913 29892468
Subdural haematoma 13.48 13.03 4 39093 18968 29894413
Cerebral infarction 13.36 13.03 9 39088 26364 29887017
Bronchitis 13.30 13.03 19 39078 39106 29874275
Hygroma colli 13.12 13.03 4 39093 39 29913342
Inhibitory drug interaction 13.08 13.03 13 39084 1555 29911826
Cardiogenic shock 13.04 13.03 3 39094 16858 29896523

Pharmacologic Action:

SourceCodeDescription
ATC N02AC52 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Diphenylpropylamine derivatives
ATC N07BC02 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in opioid dependence
FDA MoA N0000175684 Full Opioid Agonists
FDA EPC N0000175690 Opioid Agonist
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D000996 Antitussive Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35482 narcotic analgesics
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:50949 serotonin reuptake inhibitor
CHEBI has role CHEBI:55322 mu opioid agonist
CHEBI has role CHEBI:60643 n-methyl-d-aspartate receptor antagonists
CHEBI has role CHEBI:78298 environmental contaminants

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Severe pain indication 76948002
Opioid withdrawal indication 87132004
Chronic disease of respiratory system contraindication 17097001
Mood swings contraindication 18963009
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Hypercapnia contraindication 29596007
Torsades de pointes contraindication 31722008
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Paralytic ileus contraindication 55525008 DOID:8442
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Epilepsy contraindication 84757009 DOID:1826
Kidney disease contraindication 90708001 DOID:557
Prolonged QT interval contraindication 111975006
Acute abdominal pain contraindication 116290004
Procedure on urinary system contraindication 118677009
Disease of liver contraindication 235856003 DOID:409
Benign prostatic hyperplasia contraindication 266569009
Pseudomembranous enterocolitis contraindication 397683000
Congenital long QT syndrome contraindication 442917000
Acute exacerbation of asthma contraindication 708038006

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.55 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST Ki 8.78 WOMBAT-PK CHEMBL
Delta-type opioid receptor GPCR IC50 5.96 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.01 CHEMBL
Kappa-type opioid receptor GPCR IC50 6.29 CHEMBL
Neuronal acetylcholine receptor subunit alpha-10 Ion channel WOMBAT-PK
Glutamate receptor ionotropic, NMDA 3A Ion channel WOMBAT-PK
Opioid receptor GPCR IC50 7.29 CHEMBL

External reference:

IDSource
4019820 VUID
N0000147909 NUI
D02102 KEGG_DRUG
1095-90-5 SECONDARY_CAS_RN
4017431 VANDF
4019820 VANDF
C0025605 UMLSCUI
CHEBI:6807 CHEBI
CHEMBL651 ChEMBL_ID
CHEMBL1200825 ChEMBL_ID
D008691 MESH_DESCRIPTOR_UI
DB00333 DRUGBANK_ID
5458 IUPHAR_LIGAND_ID
788 INN_ID
UC6VBE7V1Z UNII
4095 PUBCHEM_CID
218337 RXNORM
1981 MMSL
5065 MMSL
d00050 MMSL
001566 NDDF
004628 NDDF
23883005 SNOMEDCT_US
387286002 SNOMEDCT_US
51758009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0391 CONCENTRATE 10 mg ORAL ANDA 28 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0391 CONCENTRATE 10 mg ORAL ANDA 28 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0392 CONCENTRATE 10 mg ORAL ANDA 28 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0392 CONCENTRATE 10 mg ORAL ANDA 28 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0054-0709 TABLET 5 mg ORAL ANDA 32 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0054-0710 TABLET 10 mg ORAL ANDA 32 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-3553 CONCENTRATE 10 mg ORAL ANDA 31 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-3555 SOLUTION 5 mg ORAL ANDA 30 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-3556 SOLUTION 10 mg ORAL ANDA 30 sections
DOLOPHINE HUMAN PRESCRIPTION DRUG LABEL 1 0054-4218 TABLET 5 mg ORAL NDA 32 sections
DOLOPHINE HUMAN PRESCRIPTION DRUG LABEL 1 0054-4219 TABLET 10 mg ORAL NDA 32 sections
DISKETS HUMAN PRESCRIPTION DRUG LABEL 1 0054-4538 TABLET 40 mg ORAL NDA 31 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0054-4570 TABLET 5 mg ORAL NDA 32 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0054-4571 TABLET 10 mg ORAL NDA 32 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0054-8553 TABLET 5 mg ORAL NDA 32 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0054-8554 TABLET 10 mg ORAL NDA 32 sections
METHADOSE HUMAN PRESCRIPTION DRUG LABEL 1 0406-0527 CONCENTRATE 10 mg ORAL NDA 16 sections
METHADOSE DISPERSIBLE HUMAN PRESCRIPTION DRUG LABEL 1 0406-0540 TABLET 40 mg ORAL ANDA 31 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0406-2540 TABLET 40 mg ORAL ANDA 31 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0406-5755 TABLET 5 mg ORAL ANDA 29 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0406-5771 TABLET 10 mg ORAL ANDA 29 sections
METHADOSESUGAR-FREE HUMAN PRESCRIPTION DRUG LABEL 1 0406-8725 CONCENTRATE 10 mg ORAL NDA 16 sections
Methadone Hydrocloride HUMAN PRESCRIPTION DRUG LABEL 1 0527-1926 CONCENTRATE 10 mg ORAL ANDA 16 sections
Methadone Hydrocloridedye-free, sugar-free, unflavored HUMAN PRESCRIPTION DRUG LABEL 1 0527-1927 CONCENTRATE 10 mg ORAL ANDA 16 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-6530 TABLET 10 mg ORAL ANDA 31 sections
Methadone Hydrochloride Human Prescription Drug Label 1 13107-088 TABLET 5 mg ORAL ANDA 32 sections
Methadone Hydrochloride Human Prescription Drug Label 1 13107-089 TABLET 10 mg ORAL ANDA 32 sections
METHADONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 16590-689 TABLET 5 mg ORAL NDA 14 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-380 INJECTION, SOLUTION 10 mg INTRAMUSCULAR ANDA 25 sections
Methadone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17856-0392 CONCENTRATE 10 mg ORAL ANDA 26 sections