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

Stem definitionDrug idCAS RN
1599 53179-11-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • loperamide
  • loperamide hydrochloride
  • imodium
  • loperamide HCl
One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.
  • Molecular weight: 477.05
  • Formula: C29H33ClN2O2
  • CLOGP: 4.66
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 43.78
  • ALOGS: -5.74
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1.40 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.48 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 40 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 28, 1976 FDA MCNEIL CONS

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
Diarrhoea 1551.34 10.43 3088 77185 622458 52646335
Dehydration 289.80 10.43 723 79550 167687 53101106
Rheumatoid arthritis 205.05 10.43 109 80164 314422 52954371
Pneumonia viral 183.25 10.43 121 80152 6991 53261802
Maternal exposure during pregnancy 165.27 10.43 20 80253 155619 53113174
Drug ineffective 151.16 10.43 676 79597 816569 52452224
Vomiting 144.05 10.43 1255 79018 495884 52772909
Pneumonia aspiration 132.28 10.43 207 80066 34094 53234699
Drug abuse 131.56 10.43 299 79974 65227 53203566
Systemic lupus erythematosus 126.27 10.43 19 80254 125395 53143398
Torsade de pointes 122.74 10.43 123 80150 12882 53255911
Hypokalaemia 121.57 10.43 370 79903 96147 53172646
Soft tissue disorder 115.43 10.43 75 80198 4215 53264578
Ventricular tachycardia 113.71 10.43 137 80136 17625 53251168
Decreased appetite 112.69 10.43 628 79645 214346 53054447
Coma 102.61 10.43 262 80011 61521 53207272
Pain 98.88 10.43 503 79770 587895 52680898
Hypomagnesaemia 97.42 10.43 151 80122 24660 53244133
Electrocardiogram QT prolonged 96.60 10.43 242 80031 56161 53212632
Gastrooesophageal reflux disease 95.87 10.43 308 79965 82355 53186438
Colitis 95.20 10.43 200 80073 41352 53227441
Oral pain 91.27 10.43 153 80120 26684 53242109
Abdominal pain 89.48 10.43 675 79598 255228 53013565
Hypomania 88.48 10.43 67 80206 4815 53263978
Contraindicated product administered 85.32 10.43 49 80224 135580 53133213
Jaundice cholestatic 85.26 10.43 69 80204 5465 53263328
Nausea 85.00 10.43 1601 78672 754490 52514303
Glossodynia 84.74 10.43 23 80250 100268 53168525
Gastrointestinal stoma complication 79.14 10.43 42 80231 1614 53267179
Small intestinal obstruction 78.27 10.43 112 80161 17035 53251758
Pericarditis 69.01 10.43 8 80265 64398 53204395
Intestinal obstruction 68.95 10.43 141 80132 28600 53240193
Completed suicide 65.19 10.43 67 80206 138134 53130659
Drug hypersensitivity 63.98 10.43 196 80077 265046 53003747
Neuropathy peripheral 63.27 10.43 315 79958 102872 53165921
Exposure during pregnancy 63.00 10.43 57 80216 124803 53143990
Drug intolerance 61.69 10.43 136 80137 205357 53063436
Arthropathy 59.73 10.43 75 80198 141378 53127415
Blood magnesium increased 59.59 10.43 44 80229 3043 53265750
Schizophrenia 58.90 10.43 75 80198 10204 53258589
Presbyacusis 58.55 10.43 43 80230 2949 53265844
Infusion related reaction 58.54 10.43 90 80183 155867 53112926
Pleural thickening 55.93 10.43 40 80233 2632 53266161
Mucosal inflammation 54.74 10.43 165 80108 42619 53226174
Neutropenic sepsis 54.52 10.43 87 80186 14562 53254231
Colitis microscopic 54.28 10.43 60 80213 7034 53261759
Discomfort 53.87 10.43 39 80234 95433 53173360
Somnolence 52.77 10.43 432 79841 167302 53101491
Deafness neurosensory 52.24 10.43 49 80224 4729 53264064
Weight decreased 51.85 10.43 561 79712 234387 53034406
Intentional overdose 51.44 10.43 219 80054 66986 53201807
Pleural fibrosis 51.43 10.43 43 80230 3565 53265228
Blood magnesium decreased 49.34 10.43 74 80199 11740 53257053
Lethargy 49 10.43 185 80088 53575 53215218
Constipation 48.61 10.43 484 79789 197928 53070865
Therapeutic product effect decreased 47.64 10.43 72 80201 125583 53143210
Brain stem glioma 46.59 10.43 15 80258 152 53268641
Wound 45.93 10.43 42 80231 91515 53177278
Febrile neutropenia 44.92 10.43 291 79982 104645 53164148
Psoriatic arthropathy 44.76 10.43 9 80264 48181 53220612
Segmental diverticular colitis 43.74 10.43 14 80259 139 53268654
Respiration abnormal 42.79 10.43 47 80226 5471 53263322
Pedal pulse abnormal 42.79 10.43 14 80259 150 53268643
Swelling 42.72 10.43 146 80127 190959 53077834
Calcium ionised decreased 42.67 10.43 16 80257 263 53268530
Injection site pain 42 10.43 66 80207 113325 53155468
Injection site erythema 41.73 10.43 33 80240 77216 53191577
Malignant neoplasm progression 41.45 10.43 215 80058 71326 53197467
Psoriasis 41.30 10.43 42 80231 87047 53181746
Flatulence 40.74 10.43 122 80151 31395 53237398
Injection site pruritus 40.26 10.43 7 80266 41582 53227211
Electrocardiogram QRS complex prolonged 39.57 10.43 46 80227 5696 53263097
Nail dystrophy 39.53 10.43 20 80253 695 53268098
Helicobacter infection 39.11 10.43 6 80267 39063 53229730
Knee arthroplasty 39.05 10.43 3 80270 33566 53235227
Arthralgia 38.88 10.43 449 79824 439334 52829459
Headache 38.00 10.43 574 79699 536247 52732546
Clostridium difficile infection 37.99 10.43 110 80163 27783 53241010
Epigastric discomfort 36.89 10.43 46 80227 6127 53262666
Accidental overdose 36.59 10.43 92 80181 21387 53247406
Long QT syndrome 36.42 10.43 34 80239 3262 53265531
Device related infection 36.13 10.43 95 80178 22691 53246102
Treatment failure 36.07 10.43 88 80185 128315 53140478
Total lung capacity increased 35.48 10.43 20 80253 867 53267926
Herpes zoster 35.26 10.43 211 80062 73808 53194985
Pouchitis 34.65 10.43 16 80257 453 53268340
Blood potassium decreased 34.23 10.43 136 80137 40324 53228469
Sinusitis 34.22 10.43 134 80139 168430 53100363
Device expulsion 33.76 10.43 3 80270 29810 53238983
Appetite disorder 33.24 10.43 45 80228 6498 53262295
Pneumonia 33.14 10.43 824 79449 406345 52862448
Brugada syndrome 33.08 10.43 14 80259 320 53268473
Blood bilirubin increased 32.59 10.43 123 80150 35607 53233186
Gallbladder polyp 32.47 10.43 18 80255 755 53268038
Drug interaction 31.49 10.43 197 80076 219132 53049661
Red blood cell sedimentation rate increased 31.29 10.43 3 80270 28054 53240739
Cholelithiasis 30.96 10.43 133 80140 40831 53227962
Arteriovenous fistula occlusion 30.89 10.43 14 80259 379 53268414
Disease progression 30.69 10.43 260 80013 101660 53167133
Joint swelling 30.55 10.43 217 80056 234421 53034372
Frequent bowel movements 30.28 10.43 67 80206 14345 53254448
Injection site reaction 30.05 10.43 20 80253 51146 53217647
Blue toe syndrome 29.91 10.43 14 80259 409 53268384
Post procedural diarrhoea 29.78 10.43 11 80262 173 53268620
Stoma complication 29.76 10.43 13 80260 322 53268471
Hypersensitivity 29.33 10.43 191 80082 210474 53058319
Injection site bruising 29.32 10.43 10 80263 37636 53231157
Syncope 28.76 10.43 276 79997 111717 53157076
Hip arthroplasty 28.53 10.43 4 80269 27858 53240935
Wrong technique in product usage process 28.40 10.43 29 80244 60003 53208790
Dry skin 28.24 10.43 140 80133 45620 53223173
Intentional self-injury 28.19 10.43 93 80180 25191 53243602
Impaired healing 28.19 10.43 33 80240 64172 53204621
Ventricular arrhythmia 28.08 10.43 31 80242 3629 53265164
Conduction disorder 27.95 10.43 21 80252 1491 53267302
Drug use disorder 27.75 10.43 29 80244 3190 53265603
Rhinorrhoea 27.64 10.43 156 80117 53422 53215371
Liver function test abnormal 27.52 10.43 144 80129 47927 53220866
Therapeutic response decreased 27.39 10.43 19 80254 47550 53221243
Gastroenteritis radiation 27.27 10.43 14 80259 502 53268291
Heart sounds 26.79 10.43 14 80259 521 53268272
Feeding intolerance 26.64 10.43 14 80259 527 53268266
Brain injury 26.57 10.43 40 80233 6365 53262428
No adverse event 26.41 10.43 13 80260 39252 53229541
Weight increased 26.23 10.43 190 80083 204377 53064416
Premature delivery 26.15 10.43 4 80269 26100 53242693
Therapeutic reaction time decreased 25.55 10.43 19 80254 1328 53267465
Folliculitis 25.44 10.43 8 80265 31701 53237092
Bile acid malabsorption 25.14 10.43 10 80263 194 53268599
Urticaria 25.11 10.43 112 80161 135773 53133020
Clostridium difficile colitis 25.06 10.43 76 80197 19689 53249104
Anal abscess 24.65 10.43 30 80243 3898 53264895
Gastrointestinal stoma output increased 24.64 10.43 10 80263 205 53268588
Pulmonary embolism 24.61 10.43 272 80001 114170 53154623
Mydriasis 24.19 10.43 53 80220 11273 53257520
Thymus disorder 24.11 10.43 10 80263 217 53268576
Foetal exposure during pregnancy 24.11 10.43 11 80262 34704 53234089
Unresponsive to stimuli 24.09 10.43 107 80166 33319 53235474
Fatigue 24.01 10.43 1335 78938 729171 52539622
Product quality issue 23.80 10.43 13 80260 37010 53231783
Crohn's disease 23.63 10.43 39 80234 6711 53262082
Overdose 23.59 10.43 257 80016 107479 53161314
Skin fissures 23.50 10.43 45 80228 8700 53260093
Stomatitis 23.30 10.43 238 80035 97920 53170873
Injection site swelling 23.28 10.43 18 80255 42610 53226183
Ill-defined disorder 23.26 10.43 24 80249 49420 53219373
Multiple sclerosis relapse 23.18 10.43 20 80253 44833 53223960
Pneumonitis 23.12 10.43 100 80173 30788 53238005
Hypophagia 22.82 10.43 100 80173 30962 53237831
Anaemia 22.76 10.43 561 79712 276157 52992636
Off label use 22.51 10.43 540 79733 471672 52797121
Leukopenia 22.42 10.43 188 80085 73275 53195518
Pulmonary thrombosis 22.38 10.43 42 80231 7999 53260794
Pyrexia 22.12 10.43 777 79496 402416 52866377
Prolonged expiration 21.95 10.43 13 80260 619 53268174
Vascular device infection 21.84 10.43 30 80243 4391 53264402
Ear infection 21.75 10.43 6 80267 25894 53242899
Musculoskeletal stiffness 21.42 10.43 104 80169 123264 53145529
Abdominal discomfort 21.35 10.43 221 80052 220841 53047952
Sedation 21.24 10.43 9 80264 29666 53239127
Coronary artery disease 21.12 10.43 12 80261 33425 53235368
Blood creatinine increased 20.86 10.43 203 80070 82459 53186334
Loss of personal independence in daily activities 20.27 10.43 47 80226 69768 53199025
Palmar-plantar erythrodysaesthesia syndrome 20.22 10.43 75 80198 21531 53247262
Cardiotoxicity 20.16 10.43 38 80235 7261 53261532
Dermatitis acneiform 20.11 10.43 29 80244 4441 53264352
Short-bowel syndrome 20.07 10.43 11 80262 451 53268342
Femur fracture 20.03 10.43 18 80255 39567 53229226
Rash 19.97 10.43 515 79758 445676 52823117
Large intestine polyp 19.74 10.43 40 80233 8057 53260736
Enteritis 19.62 10.43 38 80235 7408 53261385
Therapeutic product effect incomplete 19.24 10.43 72 80201 91712 53177081
Hepatotoxicity 19.16 10.43 88 80185 27792 53241001
Type 2 diabetes mellitus 19.11 10.43 12 80261 31658 53237135
Paronychia 19.09 10.43 30 80243 4954 53263839
Food interaction 19.01 10.43 12 80261 641 53268152
Bone hypertrophy 18.99 10.43 10 80263 378 53268415
Product dose omission issue 18.73 10.43 191 80082 191429 53077364
Enterocolitis 18.59 10.43 36 80237 7016 53261777
Gastroenteritis 18.46 10.43 82 80191 25534 53243259
Dyspepsia 18.34 10.43 188 80085 77412 53191381
Tenderness 18.05 10.43 68 80205 19662 53249131
Dry eye 18.04 10.43 99 80174 33545 53235248
Drug resistance 17.98 10.43 4 80269 19958 53248835
Neutropenia 17.65 10.43 337 79936 158848 53109945
Pancreatitis chronic 17.64 10.43 20 80253 2410 53266383
Congenital knee deformity 17.54 10.43 5 80268 32 53268761
Pregnancy 17.52 10.43 13 80260 31428 53237365
Intestinal fibrosis 17.40 10.43 7 80266 140 53268653
Anal incontinence 17.34 10.43 50 80223 12597 53256196
Ileal stenosis 17.27 10.43 16 80257 1520 53267273
Reflux gastritis 17.25 10.43 13 80260 927 53267866
Accidental exposure to product 17.24 10.43 7 80266 23667 53245126
Alopecia 17.15 10.43 249 80024 234334 53034459
Autoimmune nephritis 17.15 10.43 9 80264 338 53268455
Hypovolaemia 17.14 10.43 44 80229 10358 53258435
Peripheral pulse decreased 17.04 10.43 5 80268 36 53268757
Proctitis 17.02 10.43 18 80255 2007 53266786
Ejection fraction decreased 17.01 10.43 67 80206 19781 53249012
Urinary tract infection 17.00 10.43 477 79796 239426 53029367
Sinus arrest 16.59 10.43 17 80256 1827 53266966
Long QT syndrome congenital 16.58 10.43 5 80268 40 53268753
Sepsis 16.57 10.43 311 79962 146118 53122675
Hypermagnesaemia 16.48 10.43 13 80260 992 53267801
Inflammatory bowel disease 16.28 10.43 24 80249 3749 53265044
Cor pulmonale acute 16.27 10.43 9 80264 376 53268417
Plantar erythema 16.19 10.43 8 80265 264 53268529
Hypocalcaemia 16.18 10.43 87 80186 29250 53239543
Bone cyst 16.10 10.43 18 80255 2136 53266657
Synovitis 15.94 10.43 96 80177 107797 53160996
Fracture pain 15.91 10.43 9 80264 393 53268400
Drug eruption 15.86 10.43 9 80264 25085 53243708
Stoma site ulcer 15.84 10.43 8 80265 277 53268516
Condition aggravated 15.77 10.43 334 79939 296800 52971993
Cyst 15.77 10.43 49 80224 12862 53255931
Gastrointestinal sounds abnormal 15.75 10.43 24 80249 3860 53264933
Abortion spontaneous 15.56 10.43 29 80244 46606 53222187
Enterocutaneous fistula 15.47 10.43 14 80259 1290 53267503
Asthenia 15.46 10.43 648 79625 342942 52925851
Rectal abscess 15.41 10.43 13 80260 1091 53267702
Dysgeusia 15.37 10.43 114 80159 42817 53225976
Influenza like illness 15.34 10.43 44 80229 60815 53207978
Intestinal anastomosis 15.33 10.43 8 80265 297 53268496
Failure to thrive 15.25 10.43 33 80240 6959 53261834
Paralysis recurrent laryngeal nerve 15.24 10.43 5 80268 54 53268739
Malnutrition 15.08 10.43 53 80220 14818 53253975
Food refusal 14.92 10.43 8 80265 314 53268479
Tachycardia 14.83 10.43 237 80036 107975 53160818
Ileostomy 14.82 10.43 13 80260 1150 53267643
Biliary sepsis 14.81 10.43 12 80261 952 53267841
Electrolyte imbalance 14.80 10.43 62 80211 18822 53249971
Peritoneal perforation 14.74 10.43 6 80267 124 53268669
Palmar erythema 14.66 10.43 15 80258 1609 53267184
Nail disorder 14.65 10.43 40 80233 9765 53259028
Intestinal perforation 14.65 10.43 44 80229 11336 53257457
Arthritis 14.64 10.43 198 80075 87100 53181693
Pruritus 14.53 10.43 334 79939 293498 52975295
Amoebic colitis 14.43 10.43 3 80270 3 53268790
Catheter site bruise 14.40 10.43 8 80265 337 53268456
Small intestine ulcer 14.21 10.43 8 80265 346 53268447
Hepatic lesion 14.19 10.43 24 80249 4213 53264580
Unmasking of previously unidentified disease 14.12 10.43 11 80262 824 53267969
Ileus 14.06 10.43 52 80221 14903 53253890
Onychalgia 13.83 10.43 11 80262 850 53267943
Blood potassium increased 13.53 10.43 58 80215 17783 53251010
Hepatic enzyme increased 13.50 10.43 123 80150 126072 53142721
Gluten sensitivity 13.40 10.43 9 80264 535 53268258
Amputation 13.32 10.43 6 80267 160 53268633
Peritoneal disorder 13.26 10.43 9 80264 544 53268249
Rectal haemorrhage 13.10 10.43 107 80166 41374 53227419
Product use in unapproved indication 13.10 10.43 107 80166 112182 53156611
Tumour inflammation 13.05 10.43 4 80269 34 53268759
Pleural effusion 12.89 10.43 196 80077 88383 53180410
Periventricular leukomalacia 12.87 10.43 5 80268 91 53268702
Acute kidney injury 12.85 10.43 485 79788 253383 53015410
Nail bed tenderness 12.84 10.43 7 80266 284 53268509
Ataxia 12.83 10.43 50 80223 14687 53254106
Ureteric obstruction 12.81 10.43 15 80258 1871 53266922
Hyperchlorhydria 12.73 10.43 14 80259 1632 53267161
Osteopenia 12.66 10.43 58 80215 18297 53250496
Eye irritation 12.57 10.43 6 80267 18443 53250350
Psychotic disorder 12.57 10.43 71 80202 24314 53244479
Road traffic accident 12.56 10.43 12 80261 25619 53243174
Cerebral haemorrhage 12.55 10.43 16 80257 29980 53238813
Accidental exposure to product by child 12.47 10.43 12 80261 1196 53267597
Adverse event 12.44 10.43 27 80246 41034 53227759
Autonomic neuropathy 12.31 10.43 11 80262 997 53267796
Megacolon 12.31 10.43 15 80258 1951 53266842
Foetal arrhythmia 12.29 10.43 6 80267 193 53268600
Anaemia of malignant disease 12.26 10.43 8 80265 453 53268340
Defaecation urgency 12.22 10.43 19 80254 3109 53265684
Device issue 12.01 10.43 9 80264 21649 53247144
Blood cholesterol increased 11.87 10.43 127 80146 52862 53215931
Cardiorenal syndrome 11.84 10.43 9 80264 650 53268143
Piloerection 11.79 10.43 7 80266 335 53268458
Autoimmune colitis 11.72 10.43 8 80265 488 53268305
Suicidal ideation 11.70 10.43 49 80224 60462 53208331
Pharyngo-oesophageal diverticulum 11.69 10.43 3 80270 12 53268781
Platelet count decreased 11.68 10.43 228 80045 107871 53160922
Ventricular fibrillation 11.67 10.43 42 80231 11883 53256910
Anxiety 11.66 10.43 217 80056 196487 53072306
Accidental poisoning 11.63 10.43 9 80264 668 53268125
Motion sickness 11.61 10.43 10 80263 863 53267930
Alveolar bone resorption 11.60 10.43 4 80269 51 53268742
Renal pain 11.53 10.43 27 80246 6000 53262793
Fibromyalgia 11.49 10.43 109 80164 43966 53224827
Abdominal mass 11.39 10.43 17 80256 2685 53266108
Joint effusion 11.39 10.43 3 80270 13349 53255444
Moraxella infection 11.33 10.43 7 80266 360 53268433
Hypophosphataemia 11.30 10.43 34 80239 8771 53260022
Large intestine perforation 11.29 10.43 32 80241 7982 53260811
Hip fracture 11.25 10.43 77 80196 28180 53240613
Gastroenteropancreatic neuroendocrine tumour disease 11.19 10.43 4 80269 57 53268736
Glaucoma 11.19 10.43 53 80220 16950 53251843
Neutrophil count decreased 11.15 10.43 118 80155 48980 53219813
Blood sodium decreased 11.07 10.43 66 80207 23050 53245743
Lip erosion 11.00 10.43 10 80263 927 53267866
Intentional product use issue 10.97 10.43 64 80209 72430 53196363
Osteosclerosis 10.92 10.43 20 80253 3738 53265055
Miosis 10.90 10.43 29 80244 6973 53261820
Soft tissue swelling 10.80 10.43 10 80263 949 53267844
Abdominal pain upper 10.77 10.43 327 79946 165964 53102829
Abdominal distension 10.64 10.43 174 80099 79616 53189177
Cardiac arrest 10.61 10.43 199 80074 93468 53175325
Obesity 10.49 10.43 6 80267 16656 53252137

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
Diarrhoea 1102.01 11.19 2026 49903 362776 32098821
Drug abuse 277.91 11.19 476 51453 79767 32381830
Torsade de pointes 222.75 11.19 142 51787 7273 32454324
Dehydration 198.32 11.19 551 51378 128407 32333190
Electrocardiogram QRS complex prolonged 187.61 11.19 107 51822 4467 32457130
Electrocardiogram QT prolonged 179.53 11.19 266 51663 39375 32422222
Intentional overdose 154.74 11.19 255 51674 41346 32420251
Colitis 130.15 11.19 211 51718 33740 32427857
Ventricular tachycardia 107.85 11.19 166 51763 25390 32436207
Abdominal pain 94.46 11.19 480 51449 149049 32312548
Drug ineffective 70.15 11.19 345 51584 383132 32078465
Small intestinal obstruction 65.27 11.19 96 51833 14100 32447497
Intestinal obstruction 63.60 11.19 117 51812 20681 32440916
Intentional self-injury 62.47 11.19 93 51836 13807 32447790
Brugada syndrome 62.36 11.19 28 51901 697 32460900
Vomiting 59.62 11.19 606 51323 234951 32226646
Blood mercury abnormal 58.31 11.19 19 51910 188 32461409
Conduction disorder 57.01 11.19 37 51892 1953 32459644
5-hydroxyindolacetic acid in urine increased 56.18 11.19 19 51910 213 32461384
Decreased appetite 53.48 11.19 439 51490 160374 32301223
Drug use disorder 51.08 11.19 44 51885 3577 32458020
Completed suicide 50.57 11.19 44 51885 92473 32369124
Overdose 48.36 11.19 270 51659 86807 32374790
Rheumatoid arthritis 47.95 11.19 7 51922 44537 32417060
Foetal exposure during pregnancy 43.30 11.19 7 51922 41294 32420303
Pouchitis 39.16 11.19 20 51909 667 32460930
Nausea 39.09 11.19 724 51205 320125 32141472
Electrolyte imbalance 37.96 11.19 70 51859 12392 32449205
Abscess intestinal 36.29 11.19 25 51904 1458 32460139
Respiratory depression 36.28 11.19 71 51858 13140 32448457
Alveolar lung disease 35.35 11.19 16 51913 406 32461191
Fatigue 34.00 11.19 765 51164 349936 32111661
Ileus 33.76 11.19 78 51851 16187 32445410
Product use in unapproved indication 30.53 11.19 58 51871 87146 32374451
Pulmonary interstitial emphysema syndrome 29.97 11.19 15 51914 479 32461118
Myocardial infarction 29.77 11.19 102 51827 125574 32336023
Abdominal distension 29.76 11.19 161 51768 51134 32410463
Hypomagnesaemia 29.42 11.19 81 51848 18724 32442873
Drug hypersensitivity 29.19 11.19 45 51884 73355 32388242
Weight decreased 29.12 11.19 396 51533 164422 32297175
Low density lipoprotein decreased 28.75 11.19 19 51910 1034 32460563
Psoriasis 27.62 11.19 20 51909 46103 32415494
Hepatic neoplasm 26.81 11.19 24 51905 2054 32459543
Gastrointestinal stoma complication 26.68 11.19 20 51909 1332 32460265
Cardiotoxicity 26.59 11.19 36 51893 4896 32456701
Cardiac arrest 26.33 11.19 253 51676 96523 32365074
Enteritis 26.28 11.19 44 51885 7217 32454380
Treatment failure 26.15 11.19 15 51914 39148 32422449
Ventricular arrhythmia 25.77 11.19 36 51893 5043 32456554
Crohn's disease 25.40 11.19 33 51896 4312 32457285
Asthma 25.24 11.19 20 51909 44045 32417552
Accidental overdose 25.17 11.19 78 51851 19261 32442336
Intentional product misuse 25.01 11.19 119 51810 35932 32425665
Clostridium difficile colitis 24.71 11.19 64 51865 14267 32447330
Enterocolitis 24.62 11.19 43 51886 7297 32454300
Colitis microscopic 24.30 11.19 22 51907 1910 32459687
Stomatitis 23.83 11.19 127 51802 40102 32421495
Blood potassium decreased 23.56 11.19 71 51858 17267 32444330
Enterocolonic fistula 23.09 11.19 8 51921 97 32461500
Expired product administered 22.25 11.19 26 51903 3049 32458548
Palmar-plantar erythrodysaesthesia syndrome 21.88 11.19 65 51864 15684 32445913
Colitis ulcerative 21.47 11.19 68 51861 16983 32444614
Wrong technique in product usage process 21.25 11.19 15 51914 35044 32426553
Gastrointestinal obstruction 21.12 11.19 14 51915 766 32460831
Frequent bowel movements 20.36 11.19 46 51883 9406 32452191
Mucosal inflammation 20.10 11.19 106 51823 33328 32428269
Abdominal abscess 20.06 11.19 29 51900 4192 32457405
Miosis 19.47 11.19 43 51886 8661 32452936
Proctalgia 19.39 11.19 30 51899 4604 32456993
Immune-mediated enterocolitis 18.99 11.19 18 51911 1657 32459940
Dysgeusia 18.97 11.19 86 51843 25445 32436152
Hepatic haematoma 18.80 11.19 11 51918 482 32461115
Anal fissure 18.44 11.19 23 51906 2886 32458711
Atrioventricular block first degree 18.18 11.19 33 51896 5770 32455827
Intestinal stenosis 18.12 11.19 19 51910 1976 32459621
Therapeutic product effect decreased 17.86 11.19 14 51915 31003 32430594
Brain herniation 17.53 11.19 26 51903 3845 32457752
Pneumonitis 17.07 11.19 94 51835 30040 32431557
Anal fistula infection 17.06 11.19 4 51925 9 32461588
Angioedema 16.69 11.19 20 51909 36269 32425328
Electrocardiogram PR prolongation 16.65 11.19 12 51917 752 32460845
Right ventricular dilatation 16.64 11.19 11 51918 599 32460998
Colorectal cancer metastatic 16.63 11.19 14 51915 1103 32460494
Interstitial lung disease 16.59 11.19 51 51878 64950 32396647
Lethargy 16.13 11.19 117 51812 41111 32420486
Autoimmune colitis 16.04 11.19 13 51916 971 32460626
Gastrointestinal sounds abnormal 15.99 11.19 18 51911 2027 32459570
Peripheral embolism 15.96 11.19 13 51916 978 32460619
Gastroenteritis 15.80 11.19 54 51875 14027 32447570
Coronary artery disease 15.74 11.19 35 51894 49671 32411926
Intestinal perforation 15.68 11.19 40 51889 8835 32452762
Product dose omission issue 15.51 11.19 98 51831 102477 32359120
Gastrointestinal inflammation 15.31 11.19 22 51907 3162 32458435
Wheezing 15.24 11.19 22 51907 36852 32424745
Basosquamous carcinoma 15.00 11.19 6 51923 111 32461486
Flatulence 14.99 11.19 66 51863 19289 32442308
Intestinal fistula 14.97 11.19 12 51917 882 32460715
Subileus 14.87 11.19 22 51907 3246 32458351
Bacterial diarrhoea 14.79 11.19 5 51924 56 32461541
Musculoskeletal stiffness 14.73 11.19 25 51904 39239 32422358
Nephroangiosclerosis 14.73 11.19 7 51922 199 32461398
Malignant neoplasm progression 14.40 11.19 190 51739 78306 32383291
Off label use 14.38 11.19 376 51553 305944 32155653
Vascular device infection 14.28 11.19 19 51910 2541 32459056
Post procedural diarrhoea 14.26 11.19 5 51924 63 32461534
Drug delivery device placement 14.13 11.19 6 51923 130 32461467
Sedation 14.02 11.19 6 51923 18520 32443077
Diffuse alveolar damage 13.83 11.19 17 51912 2102 32459495
Drug reaction with eosinophilia and systemic symptoms 13.81 11.19 19 51910 32466 32429131
Proctitis 13.81 11.19 18 51911 2360 32459237
Neoplasm 13.75 11.19 25 51904 4376 32457221
Drug resistance 13.69 11.19 10 51919 22955 32438642
Hypophosphataemia 13.65 11.19 38 51891 8837 32452760
Cardiac failure 13.65 11.19 88 51841 91585 32370012
Joint swelling 13.63 11.19 40 51889 51695 32409902
Immune-mediated hepatitis 13.45 11.19 14 51915 1443 32460154
Drug level above therapeutic 13.41 11.19 21 51908 3257 32458340
Dyschromatopsia 13.36 11.19 8 51921 366 32461231
Pyomyositis 13.34 11.19 6 51923 150 32461447
Blood magnesium decreased 13.31 11.19 29 51900 5788 32455809
Eye infection fungal 13.28 11.19 8 51921 370 32461227
Generalised oedema 13.25 11.19 47 51882 12436 32449161
Retinal ischaemia 13.22 11.19 8 51921 373 32461224
Medication error 13.19 11.19 10 51919 22525 32439072
Gastrointestinal stoma output increased 13.14 11.19 4 51925 31 32461566
Aggression 13.08 11.19 27 51902 39362 32422235
Device related infection 13.02 11.19 60 51869 17873 32443724
Short-bowel syndrome 13.01 11.19 7 51922 260 32461337
Gastrointestinal stenosis 12.94 11.19 5 51924 84 32461513
Gastroenteritis staphylococcal 12.89 11.19 7 51922 265 32461332
Cardiac failure congestive 12.86 11.19 81 51848 84771 32376826
Necrotising ulcerative gingivostomatitis 12.68 11.19 5 51924 89 32461508
CSF white blood cell count decreased 12.61 11.19 4 51925 36 32461561
Blood creatine phosphokinase increased 12.09 11.19 35 51894 45441 32416156
Splenic vein thrombosis 12.08 11.19 8 51921 437 32461160
Intracranial mass 12.04 11.19 12 51917 1175 32460422
Seizure 12.00 11.19 107 51822 103747 32357850
Biopsy intestine abnormal 11.94 11.19 3 51926 10 32461587
Feeling abnormal 11.76 11.19 53 51876 60370 32401227
Mixed dementia 11.73 11.19 7 51922 318 32461279
Hypokalaemia 11.67 11.19 137 51792 54957 32406640
No adverse event 11.61 11.19 9 51920 20044 32441553
Injection site pain 11.55 11.19 22 51907 33036 32428561
Sleep apnoea syndrome 11.47 11.19 8 51921 18806 32442791
Drug withdrawal syndrome 11.39 11.19 63 51866 20168 32441429
Product prescribing error 11.22 11.19 9 51920 19708 32441889
Faecaloma 11.21 11.19 24 51905 4732 32456865

Pharmacologic Action:

SourceCodeDescription
ATC A07DA03 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
ANTIPROPULSIVES
Antipropulsives
ATC A07DA53 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
ANTIPROPULSIVES
Antipropulsives
FDA MoA N0000000174 Opioid Agonists
MeSH PA D000930 Antidiarrheals
MeSH PA D005765 Gastrointestinal Agents
CHEBI has role CHEBI:55322 mu opioid agonist
CHEBI has role CHEBI:55323 antiperistaltics
CHEBI has role CHEBI:149553 anti-coronaviral agents
FDA EPC N0000175690 Opioid Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Traveler's diarrhea indication 11840006
Diarrhea indication 62315008
Diarrhea Secondary to Inflammatory Bowel Disease indication
Chemotherapy-Induced Diarrhea off-label use
Infectious diarrheal disease contraindication 19213003 DOID:13250
Paralytic ileus contraindication 55525008 DOID:8442
Hemorrhagic diarrhea contraindication 95545007
Disease of liver contraindication 235856003 DOID:409

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.78 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
2MG LOPERAMIDE HYDROCHLORIDE STRIDES PHARMA A213070 Aug. 11, 2021 OTC CAPSULE ORAL April 20, 2022 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST Ki 8.82 WOMBAT-PK CHEMBL
Sodium channel protein type 5 subunit alpha Ion channel IC50 6.62 CHEMBL
Glutamate receptor ionotropic, NMDA 2A Ion channel WOMBAT-PK
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.58 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 5.93 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 5.58 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.34 DRUG MATRIX
Histamine H1 receptor GPCR IC50 5.70 WOMBAT-PK
Histamine H2 receptor GPCR Ki 5.52 DRUG MATRIX
Aldehyde oxidase Enzyme IC50 5 WOMBAT-PK
Voltage-dependent P/Q-type calcium channel subunit alpha-1A Ion channel WOMBAT-PK
Cytochrome P450 2D6 Enzyme IC50 5.70 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 5.60 DRUG MATRIX
Kappa-type opioid receptor GPCR Ki 6.81 WOMBAT-PK
Calmodulin Cytosolic other WOMBAT-PK
Delta-type opioid receptor GPCR Ki 6.91 WOMBAT-PK
Somatostatin receptor type 5 GPCR Ki 5.35 WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2B Ion channel WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2C Ion channel WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2D Ion channel WOMBAT-PK
Angiopoietin-1 receptor Kinase Kd 5.23 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.63 CHEMBL
Cocaine esterase Enzyme IC50 5.39 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 6.57 CHEMBL
Menin Unclassified IC50 4.16 CHEMBL
Beta-2 adrenergic receptor GPCR Ki 5.69 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 6.27 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 6.07 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 5.21 CHEMBL
Mu-type opioid receptor GPCR Ki 9.80 CHEMBL
Delta-type opioid receptor GPCR Ki 7.30 CHEMBL
Calmodulin Cytosolic other Kd 5.46 CHEMBL

External reference:

IDSource
4019804 VUID
N0000147893 NUI
D00729 KEGG_DRUG
34552-83-5 SECONDARY_CAS_RN
4019178 VANDF
4019804 VANDF
C0023992 UMLSCUI
CHEBI:6532 CHEBI
CHEMBL841 ChEMBL_ID
CHEMBL1707 ChEMBL_ID
D008139 MESH_DESCRIPTOR_UI
DB00836 DRUGBANK_ID
7215 IUPHAR_LIGAND_ID
3098 INN_ID
6X9OC3H4II UNII
3955 PUBCHEM_CID
151889 RXNORM
2069 MMSL
2336 MMSL
4992 MMSL
d01025 MMSL
001154 NDDF
004545 NDDF
116726003 SNOMEDCT_US
387040009 SNOMEDCT_US
57574005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Loperamide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0311 CAPSULE 2 mg ORAL ANDA 26 sections
good sense anti diarrheal anti gas HUMAN OTC DRUG LABEL 2 0113-0087 TABLET 2 mg ORAL ANDA 16 sections
Good Sense anti diarrheal HUMAN OTC DRUG LABEL 1 0113-0224 TABLET, FILM COATED 2 mg ORAL ANDA 16 sections
Good Sense Anti Diarrheal Anti Gas HUMAN OTC DRUG LABEL 2 0113-1087 TABLET 2 mg ORAL ANDA 16 sections
Good Sense antidiarrheal HUMAN OTC DRUG LABEL 1 0113-1645 SOLUTION 1 mg ORAL ANDA 16 sections
anti diarrheal HUMAN OTC DRUG LABEL 1 0113-2224 TABLET, FILM COATED 2 mg ORAL ANDA 16 sections
basic care loperamide hydrochloride and simethicone HUMAN OTC DRUG LABEL 2 0113-7119 TABLET 2 mg ORAL ANDA 16 sections
Basic Care loperamide hydrochloride HUMAN OTC DRUG LABEL 1 0113-7224 TABLET, FILM COATED 2 mg ORAL ANDA 16 sections
Anti-Diarrheal HUMAN OTC DRUG LABEL 1 0363-0375 TABLET 2 mg ORAL ANDA 16 sections
loperamide hydrochloride HUMAN OTC DRUG LABEL 1 0363-0645 SUSPENSION 1 mg ORAL ANDA 16 sections
anti diarrheal HUMAN OTC DRUG LABEL 1 0363-1010 TABLET, FILM COATED 2 mg ORAL ANDA 16 sections
Anti-Diarrheal HUMAN OTC DRUG LABEL 1 0363-1176 CAPSULE, LIQUID FILLED 2 mg ORAL NDA 16 sections
anti diarrheal and anti gas HUMAN OTC DRUG LABEL 2 0363-1830 TABLET 2 mg ORAL ANDA 16 sections
Loperamide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-2100 CAPSULE 2 mg ORAL ANDA 29 sections
Antidiarrheal Relief HUMAN OTC DRUG LABEL 1 0498-1071 TABLET 2 mg ORAL ANDA 16 sections
Loperamide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-0362 CAPSULE 2 mg ORAL ANDA 25 sections
Loperamide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8087 CAPSULE 2 mg ORAL ANDA 29 sections
loperamide hydrochloride HUMAN OTC DRUG LABEL 1 0904-6836 SOLUTION 1 mg ORAL ANDA 16 sections
anti diarrheal HUMAN OTC DRUG LABEL 1 0904-7725 TABLET, FILM COATED 2 mg ORAL ANDA 16 sections
Anti-Diarrheal HUMAN OTC DRUG LABEL 1 11673-177 CAPSULE, LIQUID FILLED 2 mg ORAL NDA 17 sections
Up and Up anti diarrheal HUMAN OTC DRUG LABEL 1 11673-224 TABLET, FILM COATED 2 mg ORAL ANDA 16 sections
up and up anti diarrheal anti gas HUMAN OTC DRUG LABEL 2 11673-646 TABLET 2 mg ORAL ANDA 16 sections
Up and Up anti diarrheal HUMAN OTC DRUG LABEL 1 11673-900 SUSPENSION 1 mg ORAL ANDA 16 sections
Anti-Diarrheal HUMAN OTC DRUG LABEL 1 11822-0375 TABLET 2 mg ORAL ANDA 16 sections
anti diarrheal anti gas HUMAN OTC DRUG LABEL 2 11822-1003 TABLET 2 mg ORAL ANDA 16 sections
loperamide hydrochloride HUMAN OTC DRUG LABEL 1 11822-1645 SUSPENSION 1 mg ORAL ANDA 16 sections
loperamide hydrochloride HUMAN OTC DRUG LABEL 1 11822-5519 SOLUTION 1 mg ORAL ANDA 16 sections
Anti-Diarrheal HUMAN OTC DRUG LABEL 1 11822-7834 CAPSULE, LIQUID FILLED 2 mg ORAL NDA 17 sections
Loperamide Hydrochloride HUMAN OTC DRUG LABEL 1 15127-338 TABLET 2 mg ORAL ANDA 16 sections
LOPERAMIDE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 16590-423 CAPSULE 2 mg ORAL ANDA 25 sections