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 1283.11 10.37 2732 70059 556870 46056401
Dehydration 263.04 10.37 689 72102 158851 46454420
Pneumonia viral 182.28 10.37 119 72672 6505 46606766
Rheumatoid arthritis 137.78 10.37 104 72687 240111 46373160
Vomiting 129.04 10.37 1171 71620 451623 46161648
Torsade de pointes 115.00 10.37 117 72674 12037 46601234
Drug ineffective 112.44 10.37 611 72180 677227 45936044
Drug abuse 110.58 10.37 280 72511 63128 46550143
Soft tissue disorder 109.82 10.37 73 72718 4113 46609158
Pneumonia aspiration 107.82 10.37 184 72607 31421 46581850
Ventricular tachycardia 98.76 10.37 127 72664 16840 46596431
Maternal exposure during pregnancy 98.45 10.37 20 72771 102529 46510742
Decreased appetite 96.94 10.37 574 72217 193262 46420009
Hypomagnesaemia 88.88 10.37 139 72652 22071 46591200
Hypokalaemia 87.53 10.37 319 72472 87705 46525566
Electrocardiogram QT prolonged 86.73 10.37 224 72567 51101 46562170
Coma 85.89 10.37 242 72549 58107 46555164
Oral pain 85.41 10.37 145 72646 24652 46588619
Completed suicide 83.80 10.37 63 72728 145857 46467414
Colitis 82.61 10.37 181 72610 37166 46576105
Gastrointestinal stoma complication 80.07 10.37 42 72749 1519 46611752
Gastrooesophageal reflux disease 74.38 10.37 270 72521 74074 46539197
Hypomania 72.83 10.37 58 72733 4330 46608941
Abdominal pain 72.53 10.37 609 72182 229422 46383849
Jaundice cholestatic 69.96 10.37 60 72731 4969 46608302
Small intestinal obstruction 67.21 10.37 103 72688 16069 46597202
Drug hypersensitivity 65.12 10.37 181 72610 243644 46369627
Nausea 61.93 10.37 1453 71338 686001 45927270
Pain 59.91 10.37 467 72324 476481 46136790
Presbyacusis 57.17 10.37 42 72749 2780 46610491
Blood magnesium increased 56.74 10.37 43 72748 2984 46610287
Exposure during pregnancy 55.61 10.37 52 72739 108160 46505111
Intestinal obstruction 54.98 10.37 124 72667 25951 46587320
Systemic lupus erythematosus 54.28 10.37 17 72774 65163 46548108
Pleural thickening 53.42 10.37 39 72752 2556 46610715
Neutropenic sepsis 53.35 10.37 80 72711 12244 46601027
Deafness neurosensory 51.39 10.37 48 72743 4446 46608825
Schizophrenia 49.65 10.37 64 72727 8504 46604767
Pleural fibrosis 48.47 10.37 42 72749 3527 46609744
Stomatitis 47.67 10.37 222 72569 68075 46545196
Blood magnesium decreased 47.08 10.37 71 72720 10921 46602350
Injection site erythema 46.88 10.37 29 72762 74398 46538873
Colitis microscopic 46.12 10.37 54 72737 6502 46606769
Lethargy 44.69 10.37 178 72613 50993 46562278
Injection site pain 44.69 10.37 61 72730 107091 46506180
Injection site pruritus 44.40 10.37 5 72786 39738 46573533
Intentional overdose 43.79 10.37 209 72582 64735 46548536
Psoriasis 42.51 10.37 36 72755 78568 46534703
Mucosal inflammation 41.05 10.37 144 72647 38832 46574439
Segmental diverticular colitis 40.08 10.37 13 72778 130 46613141
Calcium ionised decreased 39.97 10.37 15 72776 238 46613033
Somnolence 39.90 10.37 396 72395 156125 46457146
Pedal pulse abnormal 39.13 10.37 13 72778 141 46613130
Therapeutic response decreased 38.23 10.37 10 72781 43135 46570136
Total lung capacity increased 37.37 10.37 20 72771 754 46612517
Long QT syndrome 37.36 10.37 34 72757 3046 46610225
Brugada syndrome 37.08 10.37 14 72777 226 46613045
Epigastric discomfort 36.99 10.37 45 72746 5639 46607632
Electrocardiogram QRS complex prolonged 36.87 10.37 44 72747 5405 46607866
Headache 36.84 10.37 525 72266 477827 46135444
Malignant neoplasm progression 36.13 10.37 198 72593 64728 46548543
Weight decreased 36.12 10.37 494 72297 210355 46402916
Pouchitis 34.84 10.37 16 72775 431 46612840
Accidental overdose 34.32 10.37 88 72703 19978 46593293
Nail dystrophy 34.23 10.37 16 72775 449 46612822
Flatulence 34.21 10.37 111 72680 28767 46584504
Constipation 33.62 10.37 417 72374 173680 46439591
Drug interaction 33.44 10.37 183 72608 202911 46410360
Herpes zoster 33.19 10.37 200 72591 67672 46545599
Psoriatic arthropathy 33.07 10.37 8 72783 36371 46576900
Frequent bowel movements 32.32 10.37 65 72726 12567 46600704
Neuropathy peripheral 32.02 10.37 247 72544 90646 46522625
Device expulsion 31.97 10.37 3 72788 27539 46585732
Gallbladder polyp 31.96 10.37 18 72773 751 46612520
Contraindicated product administered 31.85 10.37 47 72744 79900 46533371
Off label use 31.69 10.37 410 72381 379431 46233840
Injection site reaction 31.03 10.37 18 72773 47831 46565440
Blood potassium decreased 29.77 10.37 128 72663 37935 46575336
Respiration abnormal 29.76 10.37 36 72755 4485 46608786
Gastroenteritis radiation 29.63 10.37 15 72776 503 46612768
Drug use disorder 28.96 10.37 28 72763 2707 46610564
Conduction disorder 28.75 10.37 21 72770 1377 46611894
Fatigue 28.69 10.37 1190 71601 607507 46005764
Drug intolerance 28.52 10.37 125 72666 146924 46466347
Gastrointestinal stoma output increased 28.45 10.37 11 72780 190 46613081
Pneumonia 27.93 10.37 776 72015 375544 46237727
Febrile neutropenia 27.89 10.37 247 72544 94380 46518891
Clostridium difficile infection 27.52 10.37 94 72697 25009 46588262
Stoma complication 26.97 10.37 11 72780 220 46613051
Wrong technique in product usage process 26.96 10.37 27 72764 54395 46558876
Injection site bruising 26.76 10.37 11 72780 35625 46577646
Knee arthroplasty 26.38 10.37 3 72788 23662 46589609
Arteriovenous fistula occlusion 26.34 10.37 12 72779 317 46612954
Intentional self-injury 26.06 10.37 90 72701 24076 46589195
Liver function test abnormal 26.01 10.37 142 72649 46345 46566926
Multiple sclerosis relapse 25.72 10.37 17 72774 42108 46571163
Infusion related reaction 25.60 10.37 77 72714 101131 46512140
Blue toe syndrome 25.47 10.37 12 72779 343 46612928
Ventricular arrhythmia 25.44 10.37 29 72762 3392 46609879
Red blood cell sedimentation rate increased 25.27 10.37 3 72788 22886 46590385
Injection site swelling 24.99 10.37 16 72775 40311 46572960
Arthralgia 24.66 10.37 410 72381 364193 46249078
Mydriasis 24.30 10.37 52 72739 10501 46602770
Feeding intolerance 24.12 10.37 13 72778 497 46612774
Post procedural diarrhoea 24.07 10.37 10 72781 210 46613061
Pulmonary thrombosis 23.80 10.37 42 72749 7360 46605911
Blood bilirubin increased 23.75 10.37 111 72680 34073 46579198
Product quality issue 23.71 10.37 13 72778 35635 46577636
Leukopenia 23.66 10.37 185 72606 68158 46545113
Urticaria 23.60 10.37 99 72692 117793 46495478
Dry skin 23.43 10.37 126 72665 40890 46572381
Glossodynia 23.16 10.37 21 72770 44352 46568919
Coronary artery disease 22.90 10.37 12 72779 33740 46579531
Syncope 22.85 10.37 257 72534 104546 46508725
Anal abscess 22.79 10.37 28 72763 3544 46609727
Crohn's disease 22.53 10.37 39 72752 6732 46606539
No adverse event 22.02 10.37 13 72778 34218 46579053
Therapeutic reaction time decreased 21.87 10.37 16 72775 1052 46612219
Premature delivery 21.81 10.37 4 72787 22065 46591206
Thymus disorder 21.32 10.37 9 72782 197 46613074
Ear infection 21.03 10.37 5 72786 23008 46590263
Foetal exposure during pregnancy 20.76 10.37 11 72780 30736 46582535
Product dose omission issue 20.59 10.37 166 72625 168354 46444917
Brain stem glioma 20.59 10.37 7 72784 82 46613189
Pyrexia 20.45 10.37 699 72092 348103 46265168
Skin fissures 20.22 10.37 40 72751 7640 46605631
Cholelithiasis 20.21 10.37 116 72675 38565 46574706
Food interaction 19.89 10.37 12 72779 570 46612701
Pneumonitis 19.54 10.37 92 72699 28328 46584943
Paronychia 18.85 10.37 29 72762 4537 46608734
Loss of personal independence in daily activities 18.77 10.37 38 72753 57145 46556126
Femur fracture 18.73 10.37 18 72773 36979 46576292
Bone hypertrophy 18.68 10.37 10 72781 377 46612894
Sinusitis 18.66 10.37 122 72669 129646 46483625
Hip arthroplasty 18.52 10.37 3 72788 18109 46595162
Dermatitis acneiform 18.45 10.37 27 72764 4043 46609228
Blood cholesterol increased 18.35 10.37 116 72675 39897 46573374
Congenital knee deformity 18.24 10.37 5 72786 26 46613245
Device related infection 18.21 10.37 73 72718 20968 46592303
Therapeutic product effect decreased 18.03 10.37 67 72724 82534 46530737
Short-bowel syndrome 17.92 10.37 10 72781 410 46612861
Blood creatinine increased 17.86 10.37 190 72601 76213 46537058
Gastroenteritis 17.83 10.37 80 72711 24139 46589132
Unresponsive to stimuli 17.81 10.37 98 72693 32076 46581195
Palmar-plantar erythrodysaesthesia syndrome 17.73 10.37 71 72720 20380 46592891
Proctitis 17.63 10.37 17 72774 1638 46611633
Hypovolaemia 17.57 10.37 44 72747 9844 46603427
Fibromyalgia 17.53 10.37 107 72684 36356 46576915
Anal incontinence 17.46 10.37 49 72742 11729 46601542
Tenderness 17.45 10.37 62 72729 16819 46596452
Suicidal ideation 17.23 10.37 39 72752 56343 46556928
Ileal stenosis 17.21 10.37 16 72775 1473 46611798
Hypermagnesaemia 17.07 10.37 13 72778 909 46612362
Overdose 17.04 10.37 238 72553 101741 46511530
Intestinal fibrosis 17.03 10.37 7 72784 143 46613128
Pericarditis 16.99 10.37 8 72783 23919 46589352
Sinus arrest 16.99 10.37 17 72774 1714 46611557
Peripheral pulse decreased 16.86 10.37 5 72786 36 46613235
Dyspepsia 16.82 10.37 172 72619 68300 46544971
Ileostomy 16.65 10.37 14 72777 1128 46612143
Influenza like illness 16.65 10.37 41 72750 57529 46555742
Clostridium difficile colitis 16.56 10.37 65 72726 18488 46594783
Cardiotoxicity 16.50 10.37 34 72757 6688 46606583
Pulmonary embolism 16.40 10.37 249 72542 108336 46504935
Brain injury 16.16 10.37 32 72759 6118 46607153
Plantar erythema 16.15 10.37 8 72783 256 46613015
Arthritis 16.13 10.37 188 72603 77128 46536143
Abortion spontaneous 16.10 10.37 27 72764 43619 46569652
Cor pulmonale acute 16.08 10.37 9 72782 371 46612900
Hypophagia 16.04 10.37 89 72702 29217 46584054
Onychalgia 15.96 10.37 11 72780 658 46612613
Rhinorrhoea 15.93 10.37 128 72663 47537 46565734
Anaemia 15.84 10.37 516 72275 255263 46358008
Fracture pain 15.82 10.37 9 72782 383 46612888
Arthropathy 15.81 10.37 73 72718 84627 46528644
Treatment failure 15.78 10.37 83 72708 93004 46520267
Failure to thrive 15.53 10.37 33 72758 6631 46606640
Drug resistance 15.43 10.37 4 72787 17364 46595907
Food refusal 15.41 10.37 8 72783 283 46612988
Dysgeusia 15.36 10.37 112 72679 40379 46572892
Gastrointestinal disorder 15.28 10.37 151 72640 59425 46553846
Anxiety 15.27 10.37 196 72595 181761 46431510
Intestinal anastomosis 15.23 10.37 8 72783 290 46612981
Enteritis 15.22 10.37 33 72758 6722 46606549
Paralysis recurrent laryngeal nerve 15.15 10.37 5 72786 53 46613218
Hepatotoxicity 15.08 10.37 78 72713 24931 46588340
Tumour inflammation 15.07 10.37 4 72787 18 46613253
Large intestine polyp 15.05 10.37 36 72755 7825 46605446
Accidental exposure to product 15.05 10.37 7 72784 21074 46592197
Catheter site bruise 14.82 10.37 8 72783 307 46612964
Cyst 14.77 10.37 47 72744 12053 46601218
Bone cyst 14.60 10.37 17 72774 2034 46611237
Autoimmune nephritis 14.56 10.37 8 72783 318 46612953
Peritoneal perforation 14.53 10.37 6 72785 124 46613147
Condition aggravated 14.50 10.37 282 72509 244770 46368501
Tachycardia 14.49 10.37 227 72564 99395 46513876
Hypocalcaemia 14.43 10.37 81 72710 26704 46586567
Amoebic colitis 14.32 10.37 3 72788 3 46613268
Sedation 14.32 10.37 9 72782 22901 46590370
Electrolyte imbalance 14.30 10.37 59 72732 17167 46596104
Therapeutic product effect incomplete 14.21 10.37 68 72723 78085 46535186
Perforation 14.19 10.37 12 72779 975 46612296
Musculoskeletal stiffness 14.15 10.37 92 72699 97901 46515370
Gastrointestinal sounds abnormal 14.10 10.37 22 72769 3484 46609787
Neutropenia 14.08 10.37 307 72484 142897 46470374
Asthenia 14.07 10.37 606 72185 310469 46302802
Palmar erythema 14.04 10.37 14 72777 1406 46611865
Ileus 13.98 10.37 51 72740 14013 46599258
Enterocutaneous fistula 13.98 10.37 13 72778 1197 46612074
Pregnancy 13.98 10.37 13 72778 27124 46586147
Dry eye 13.96 10.37 88 72703 30234 46583037
Drug eruption 13.86 10.37 8 72783 21321 46591950
Weight increased 13.86 10.37 177 72614 164296 46448975
Urinary tract infection 13.80 10.37 445 72346 219821 46393450
Gluten sensitivity 13.76 10.37 9 72782 493 46612778
Appetite disorder 13.40 10.37 27 72764 5227 46608044
Peritoneal disorder 13.23 10.37 9 72782 527 46612744
Amputation 13.22 10.37 6 72785 157 46613114
Blood potassium increased 13.22 10.37 57 72734 16910 46596361
Piloerection 13.12 10.37 7 72784 262 46613009
Foetal arrhythmia 13.12 10.37 6 72785 160 46613111
Intestinal perforation 13.11 10.37 42 72749 10809 46602462
Soft tissue swelling 13.08 10.37 11 72780 887 46612384
Cerebral haemorrhage 13.02 10.37 15 72776 28356 46584915
Anaemia of malignant disease 12.96 10.37 8 72783 396 46612875
Product use in unapproved indication 12.90 10.37 85 72706 90188 46523083
Myocardial infarction 12.87 10.37 94 72697 97434 46515837
Accidental exposure to product by child 12.85 10.37 12 72779 1111 46612160
Ureteric obstruction 12.72 10.37 15 72776 1819 46611452
Periventricular leukomalacia 12.69 10.37 5 72786 91 46613180
Enterocolitis 12.63 10.37 29 72762 6139 46607132
Abdominal pain upper 12.58 10.37 306 72485 144999 46468272
Ventricular fibrillation 12.56 10.37 43 72748 11453 46601818
Defaecation urgency 12.53 10.37 18 72773 2649 46610622
Malnutrition 12.45 10.37 49 72742 13954 46599317
Hepatic lesion 12.39 10.37 22 72769 3875 46609396
Surgery 12.38 10.37 16 72775 28769 46584502
Ejection fraction decreased 12.28 10.37 58 72733 17879 46595392
Bile acid malabsorption 12.26 10.37 5 72786 100 46613171
Frustration tolerance decreased 12.21 10.37 26 72765 5231 46608040
Cardiorenal syndrome 12.05 10.37 9 72782 611 46612660
Autoimmune colitis 12.04 10.37 8 72783 450 46612821
Megacolon 12.01 10.37 14 72777 1677 46611594
Muscle twitching 11.90 10.37 4 72787 14668 46598603
Motion sickness 11.80 10.37 10 72781 815 46612456
Injection site rash 11.68 10.37 5 72786 15808 46597463
Sepsis 11.64 10.37 286 72505 135728 46477543
Alveolar bone resorption 11.46 10.37 4 72787 51 46613220
Road traffic accident 11.45 10.37 12 72779 23679 46589592
Peripheral swelling 11.41 10.37 325 72466 157746 46455525
Inflammatory bowel disease 11.37 10.37 19 72772 3186 46610085
Miosis 11.18 10.37 29 72762 6628 46606643
Moraxella infection 11.17 10.37 7 72784 356 46612915
Eye irritation 11.13 10.37 6 72785 16608 46596663
Gastroenteropancreatic neuroendocrine tumour disease 11.05 10.37 4 72787 57 46613214
Pharyngo-oesophageal diverticulum 11.04 10.37 3 72788 15 46613256
Bone disorder 11.04 10.37 9 72782 20024 46593247
Device issue 10.98 10.37 9 72782 19971 46593300
Portal tract inflammation 10.88 10.37 3 72788 16 46613255
Obstruction 10.81 10.37 13 72778 1609 46611662
Joint space narrowing 10.81 10.37 5 72786 137 46613134
Abdominal mass 10.78 10.37 16 72775 2426 46610845
Injury 10.77 10.37 34 72757 43993 46569278
Heart sounds 10.73 10.37 6 72785 247 46613024
Stoma site extravasation 10.65 10.37 7 72784 387 46612884
Immobilisation syndrome 10.61 10.37 5 72786 143 46613128
Pleural effusion 10.58 10.37 185 72606 82767 46530504
Injection site haemorrhage 10.57 10.37 10 72781 20699 46592572
Gait disturbance 10.57 10.37 161 72630 145102 46468169
Cardiac failure congestive 10.46 10.37 92 72699 91658 46521613
Forced expiratory volume decreased 10.45 10.37 24 72767 5080 46608191
Renal pain 10.44 10.37 25 72766 5436 46607835
Vulvovaginal inflammation 10.44 10.37 8 72783 564 46612707
Emotional distress 10.42 10.37 20 72771 30687 46582584

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 1019.21 10.88 1870 46266 332233 29572109
Drug abuse 252.70 10.88 464 47672 81608 29822734
Torsade de pointes 206.11 10.88 134 48002 7056 29897286
Dehydration 194.06 10.88 534 47602 123005 29781337
Electrocardiogram QRS complex prolonged 190.97 10.88 106 48030 4171 29900171
Electrocardiogram QT prolonged 170.61 10.88 247 47889 35588 29868754
Intentional overdose 151.46 10.88 253 47883 41228 29863114
Colitis 128.91 10.88 200 47936 30620 29873722
Ventricular tachycardia 102.79 10.88 157 47979 23705 29880637
Abdominal pain 94.69 10.88 450 47686 135204 29769138
Small intestinal obstruction 67.66 10.88 96 48040 13563 29890779
Intentional self-injury 63.94 10.88 93 48043 13439 29890903
Completed suicide 61.89 10.88 42 48094 99450 29804892
Drug ineffective 60.99 10.88 311 47825 340076 29564266
Conduction disorder 57.47 10.88 37 48099 1914 29902428
Vomiting 57.43 10.88 572 47564 219246 29685096
Intestinal obstruction 56.92 10.88 107 48029 19105 29885237
Drug use disorder 55.03 10.88 44 48092 3204 29901138
Brugada syndrome 53.81 10.88 24 48112 584 29903758
Blood mercury abnormal 52.09 10.88 17 48119 168 29904174
5-hydroxyindolacetic acid in urine increased 49.97 10.88 17 48119 193 29904149
Decreased appetite 46.05 10.88 404 47732 149506 29754836
Overdose 45.07 10.88 260 47876 84077 29820265
Rheumatoid arthritis 43.52 10.88 7 48129 41190 29863152
Respiratory depression 43.06 10.88 71 48065 11432 29892910
Electrolyte imbalance 39.09 10.88 68 48068 11432 29892910
Foetal exposure during pregnancy 37.33 10.88 7 48129 36864 29867478
Abscess intestinal 37.05 10.88 25 48111 1400 29902942
Nausea 36.67 10.88 675 47461 296282 29608060
Abdominal distension 34.27 10.88 155 47981 45554 29858788
Pouchitis 34.11 10.88 18 48118 639 29903703
Myocardial infarction 33.90 10.88 97 48039 125528 29778814
Alveolar lung disease 33.11 10.88 15 48121 379 29903963
Treatment failure 32.23 10.88 8 48128 34671 29869671
Ventricular arrhythmia 30.42 10.88 36 48100 4252 29900090
Pulmonary interstitial emphysema syndrome 29.61 10.88 14 48122 391 29903951
Hypomagnesaemia 29.23 10.88 75 48061 16523 29887819
Ileus 29.19 10.88 72 48064 15483 29888859
Fatigue 28.54 10.88 695 47441 319978 29584364
Product use in unapproved indication 28.05 10.88 47 48089 73646 29830696
Crohn's disease 25.20 10.88 33 48103 4319 29900023
Low density lipoprotein decreased 25.01 10.88 17 48119 964 29903378
Hepatic neoplasm 24.92 10.88 22 48114 1837 29902505
Drug hypersensitivity 24.89 10.88 45 48091 68474 29835868
Enteritis 24.85 10.88 41 48095 6604 29897738
Cardiotoxicity 24.83 10.88 33 48103 4381 29899961
Accidental overdose 24.71 10.88 75 48061 18200 29886142
Enterocolonic fistula 24.52 10.88 8 48128 79 29904263
Weight decreased 24.07 10.88 358 47778 150563 29753779
Blood potassium decreased 24.06 10.88 70 48066 16592 29887750
Gastrointestinal stoma complication 22.96 10.88 18 48118 1274 29903068
Intentional product misuse 22.66 10.88 113 48023 34554 29869788
Miosis 22.64 10.88 43 48093 7733 29896609
Psoriasis 22.56 10.88 21 48115 42485 29861857
Gastrointestinal obstruction 21.80 10.88 14 48122 721 29903621
Clostridium difficile colitis 21.77 10.88 57 48079 12711 29891631
Inferior vena cava dilatation 21.40 10.88 9 48127 189 29904153
Abdominal abscess 21.10 10.88 29 48107 3975 29900367
Wrong technique in product usage process 20.94 10.88 12 48124 31143 29873199
Proctalgia 20.58 10.88 30 48106 4342 29900000
Colitis microscopic 20.56 10.88 19 48117 1684 29902658
Expired product administered 20.21 10.88 24 48112 2845 29901497
Palmar-plantar erythrodysaesthesia syndrome 20.08 10.88 61 48075 14809 29889533
Basosquamous carcinoma 19.29 10.88 8 48128 162 29904180
Cardiac arrest 19.24 10.88 231 47905 92619 29811723
Hepatic haematoma 18.84 10.88 11 48125 477 29903865
Intestinal stenosis 18.75 10.88 19 48117 1886 29902456
Coronary artery disease 18.64 10.88 32 48104 49680 29854662
Dysgeusia 18.50 10.88 84 48052 24717 29879625
Right ventricular dilatation 18.41 10.88 11 48125 498 29903844
Colitis ulcerative 18.36 10.88 58 48078 14376 29889966
Enterocolitis 18.28 10.88 36 48100 6651 29897691
Mucosal inflammation 18.26 10.88 97 48039 30397 29873945
Interstitial lung disease 18.11 10.88 44 48092 60153 29844189
Brain herniation 18.09 10.88 26 48110 3714 29900628
Stomatitis 18.01 10.88 112 48024 37167 29867175
Colorectal cancer metastatic 17.89 10.88 14 48122 988 29903354
Peripheral embolism 17.32 10.88 13 48123 862 29903480
Atrioventricular block first degree 17.24 10.88 32 48104 5656 29898686
Joint swelling 16.89 10.88 31 48105 46915 29857427
Lethargy 16.82 10.88 115 48021 39404 29864938
Asthma 16.81 10.88 20 48116 36154 29868188
Angioedema 15.99 10.88 19 48117 34365 29869977
Subileus 15.73 10.88 22 48114 3065 29901277
Intestinal perforation 15.52 10.88 39 48097 8480 29895862
Anal fissure 15.21 10.88 19 48117 2372 29901970
Gastrointestinal inflammation 15.17 10.88 21 48115 2898 29901444
Cardiac failure congestive 15.08 10.88 77 48059 84330 29820012
Dyschromatopsia 15.03 10.88 8 48128 289 29904053
Frequent bowel movements 14.82 10.88 38 48098 8367 29895975
Gastroenteritis 14.81 10.88 51 48085 13215 29891127
Flatulence 14.73 10.88 63 48073 18066 29886276
Therapeutic product effect decreased 14.69 10.88 15 48121 29061 29875281
Nephroangiosclerosis 14.69 10.88 7 48129 199 29904143
Gastrointestinal sounds abnormal 14.55 10.88 17 48119 1981 29902361
Electrocardiogram PR prolongation 14.52 10.88 11 48125 740 29903602
Mixed dementia 14.41 10.88 7 48129 208 29904134
Post procedural diarrhoea 14.30 10.88 5 48131 62 29904280
Eye infection fungal 14.24 10.88 8 48128 322 29904020
Anal fistula infection 14.23 10.88 3 48133 3 29904339
Drug delivery device placement 14.05 10.88 6 48130 131 29904211
Intestinal fistula 13.91 10.88 11 48125 788 29903554
Ascites 13.81 10.88 102 48034 35819 29868523
Autoimmune colitis 13.77 10.88 11 48125 800 29903542
Pneumonitis 13.59 10.88 83 48053 27371 29876971
Pyomyositis 13.53 10.88 6 48130 144 29904198
Retinal ischaemia 13.35 10.88 8 48128 364 29903978
Malignant neoplasm progression 13.32 10.88 176 47960 72111 29832231
Hypophosphataemia 13.24 10.88 36 48100 8209 29896133
Gastrointestinal stenosis 13.20 10.88 5 48131 79 29904263
Drug resistance 13.18 10.88 8 48128 20125 29884217
Diffuse alveolar damage 13.18 10.88 16 48120 1940 29902402
Electrocardiogram abnormal 12.93 10.88 29 48107 5863 29898479
Hypokalaemia 12.73 10.88 130 48006 50062 29854280
Necrotising ulcerative gingivostomatitis 12.65 10.88 5 48131 89 29904253
Immune-mediated hepatitis 12.60 10.88 12 48124 1104 29903238
Product dose omission issue 12.49 10.88 91 48045 91540 29812802
Faecaloma 12.38 10.88 24 48112 4381 29899961
Neoplasm 12.36 10.88 23 48113 4073 29900269
Proctitis 12.07 10.88 16 48120 2118 29902224
Blood magnesium decreased 12.05 10.88 27 48109 5456 29898886
Intracranial mass 12.03 10.88 12 48124 1169 29903173
Sepsis 11.97 10.88 314 47822 146081 29758261
Seizure 11.93 10.88 101 48035 98374 29805968
Biopsy intestine abnormal 11.92 10.88 3 48133 10 29904332
Megacolon 11.90 10.88 14 48122 1643 29902699
Feeling abnormal 11.78 10.88 49 48087 56707 29847635
Musculoskeletal stiffness 11.78 10.88 25 48111 35856 29868486
Blood creatine phosphokinase increased 11.70 10.88 34 48102 43814 29860528
Medication error 11.56 10.88 10 48126 20962 29883380
Splenic vein thrombosis 11.55 10.88 7 48129 325 29904017
Device related infection 11.50 10.88 56 48080 16959 29887383
Sedation 11.45 10.88 6 48130 16367 29887975
Dermatitis acneiform 11.38 10.88 27 48109 5662 29898680
Anal abscess 11.18 10.88 25 48111 5044 29899298
Aggression 11.08 10.88 27 48109 36880 29867462
Angina pectoris 11.06 10.88 19 48117 29499 29874843
Generalised oedema 11.00 10.88 43 48093 11842 29892500
Drug reaction with eosinophilia and systemic symptoms 10.99 10.88 18 48118 28470 29875872
Transcription medication error 10.98 10.88 5 48131 128 29904214
Enzyme inhibition 10.95 10.88 3 48133 15 29904327
Creatinine renal clearance abnormal 10.95 10.88 6 48130 230 29904112
Injection site pain 10.92 10.88 20 48116 30290 29874052

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
FDA EPC N0000175690 Opioid Agonist
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

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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST Ki 8.82 WOMBAT-PK CHEMBL
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 H2 receptor GPCR Ki 5.52 DRUG MATRIX
Cytochrome P450 2D6 Enzyme IC50 5.70 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 5.60 DRUG MATRIX
Glutamate receptor ionotropic, NMDA 2D Ion channel WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2C Ion channel WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2B Ion channel WOMBAT-PK
Somatostatin receptor type 5 GPCR Ki 5.34 WOMBAT-PK
Delta-type opioid receptor GPCR Ki 6.91 WOMBAT-PK
Calmodulin Cytosolic other WOMBAT-PK
Kappa-type opioid receptor GPCR Ki 6.81 WOMBAT-PK
Voltage-dependent P/Q-type calcium channel subunit alpha-1A Ion channel WOMBAT-PK
Aldehyde oxidase Enzyme IC50 5 WOMBAT-PK
Histamine H1 receptor GPCR IC50 5.70 WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2A Ion channel WOMBAT-PK
Solute carrier family 22 member 1 Transporter IC50 4.63 CHEMBL
Angiopoietin-1 receptor Kinase Kd 5.23 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 6.57 CHEMBL
Beta-2 adrenergic receptor GPCR Ki 5.68 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
Delta-type opioid receptor GPCR Ki 7.30 CHEMBL
Mu-type opioid receptor GPCR Ki 9.80 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 5.21 CHEMBL

External reference:

IDSource
4019804 VUID
N0000147893 NUI
D00729 KEGG_DRUG
34552-83-5 SECONDARY_CAS_RN
4019178 VANDF
4019804 VANDF
C0591635 UMLSCUI
CHEBI:6533 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 0363-1176 CAPSULE, LIQUID FILLED 2 mg ORAL NDA 16 sections
loperamide hydrochloride HUMAN OTC DRUG LABEL 1 0363-1645 SOLUTION 1 mg ORAL ANDA 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 0615-8012 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
Loperamide HCl HUMAN OTC DRUG LABEL 1 11673-520 CAPSULE, LIQUID FILLED 2 mg ORAL NDA 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