| Stem definition | Drug id | CAS RN |
|---|---|---|
| acetylcholinesterase inhibitors | 2330 | 155-97-5 |
| Dose | Unit | Route |
|---|---|---|
| 0.18 | g | O |
| 10 | mg | P |
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 52 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 85 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 76.59 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 7.60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 1 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.50 hours | Lombardo F, Berellini G, Obach RS |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 6, 1955 | FDA | VALEANT PHARMS LLC |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Myasthenia gravis | 577.22 | 17.25 | 128 | 7146 | 4453 | 63477295 |
| Myasthenia gravis crisis | 356.13 | 17.25 | 60 | 7214 | 452 | 63481296 |
| Diplopia | 86.96 | 17.25 | 46 | 7228 | 23682 | 63458066 |
| Eyelid ptosis | 74.85 | 17.25 | 29 | 7245 | 7238 | 63474510 |
| Thymoma | 68.65 | 17.25 | 13 | 7261 | 200 | 63481548 |
| Off label use | 49.36 | 17.25 | 179 | 7095 | 674283 | 62807465 |
| Dysphagia | 44.88 | 17.25 | 53 | 7221 | 88532 | 63393216 |
| Muscular weakness | 44.36 | 17.25 | 62 | 7212 | 122291 | 63359457 |
| Adiposis dolorosa | 40.77 | 17.25 | 9 | 7265 | 304 | 63481444 |
| Nocardiosis | 39.89 | 17.25 | 13 | 7261 | 1963 | 63479785 |
| Glucose tolerance impaired | 36.75 | 17.25 | 17 | 7257 | 6560 | 63475188 |
| Speech disorder | 36.34 | 17.25 | 33 | 7241 | 40596 | 63441152 |
| Oromandibular dystonia | 36.11 | 17.25 | 9 | 7265 | 518 | 63481230 |
| Diaphragmatic paralysis | 34.60 | 17.25 | 9 | 7265 | 615 | 63481133 |
| Cholinergic syndrome | 31.29 | 17.25 | 8 | 7266 | 510 | 63481238 |
| Myasthenic syndrome | 31.25 | 17.25 | 7 | 7267 | 253 | 63481495 |
| Bradycardia | 29.38 | 17.25 | 39 | 7235 | 73188 | 63408560 |
| Postural orthostatic tachycardia syndrome | 28.14 | 17.25 | 9 | 7265 | 1280 | 63480468 |
| Arteriospasm coronary | 27.74 | 17.25 | 12 | 7262 | 3956 | 63477792 |
| Product residue present | 27.71 | 17.25 | 12 | 7262 | 3967 | 63477781 |
| Product substitution issue | 27.29 | 17.25 | 19 | 7255 | 15977 | 63465771 |
| Borderline leprosy | 27.01 | 17.25 | 4 | 7270 | 11 | 63481737 |
| Acute on chronic liver failure | 27 | 17.25 | 6 | 7268 | 209 | 63481539 |
| Meningitis aseptic | 25.50 | 17.25 | 12 | 7262 | 4811 | 63476937 |
| Blood pressure increased | 23.39 | 17.25 | 55 | 7219 | 162007 | 63319741 |
| Sinoatrial block | 22.72 | 17.25 | 7 | 7267 | 881 | 63480867 |
| Gastric infection | 22.61 | 17.25 | 10 | 7264 | 3477 | 63478271 |
| Suspected COVID-19 | 22.11 | 17.25 | 9 | 7265 | 2553 | 63479195 |
| Respiratory distress | 21.79 | 17.25 | 23 | 7251 | 33928 | 63447820 |
| Symptom recurrence | 21.43 | 17.25 | 8 | 7266 | 1802 | 63479946 |
| Supine hypertension | 20.97 | 17.25 | 4 | 7270 | 64 | 63481684 |
| Torticollis | 20.86 | 17.25 | 8 | 7266 | 1941 | 63479807 |
| Salivary hypersecretion | 20.26 | 17.25 | 12 | 7262 | 7654 | 63474094 |
| Transfusion-related circulatory overload | 20.13 | 17.25 | 4 | 7270 | 80 | 63481668 |
| Pulmonary nocardiosis | 19.07 | 17.25 | 5 | 7269 | 352 | 63481396 |
| Headache | 18.60 | 17.25 | 130 | 7144 | 633111 | 62848637 |
| Respiratory failure | 18.58 | 17.25 | 38 | 7236 | 101820 | 63379928 |
| COVID-19 | 18.09 | 17.25 | 40 | 7234 | 113063 | 63368685 |
| Cerebral toxoplasmosis | 18.00 | 17.25 | 6 | 7268 | 972 | 63480776 |
| Asthenia | 17.89 | 17.25 | 89 | 7185 | 383515 | 63098233 |
| Dysarthria | 17.51 | 17.25 | 23 | 7251 | 42688 | 63439060 |
| Thermal burn | 17.40 | 17.25 | 10 | 7264 | 6036 | 63475712 |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Myasthenia gravis | 251.87 | 17.40 | 75 | 4861 | 6865 | 34945130 |
| Myasthenia gravis crisis | 235.69 | 17.40 | 45 | 4891 | 582 | 34951413 |
| Eyelid ptosis | 148.73 | 17.40 | 48 | 4888 | 5718 | 34946277 |
| Diplopia | 92.84 | 17.40 | 46 | 4890 | 16797 | 34935198 |
| Glucose tolerance impaired | 48.25 | 17.40 | 18 | 4918 | 3286 | 34948709 |
| Respiratory failure | 44.48 | 17.40 | 65 | 4871 | 108507 | 34843488 |
| Off label use | 42.99 | 17.40 | 143 | 4793 | 419381 | 34532614 |
| Myasthenic syndrome | 39.02 | 17.40 | 10 | 4926 | 521 | 34951474 |
| Product residue present | 36.62 | 17.40 | 14 | 4922 | 2732 | 34949263 |
| Muscular weakness | 33.29 | 17.40 | 46 | 4890 | 72851 | 34879144 |
| Ocular myasthenia | 30.47 | 17.40 | 7 | 4929 | 229 | 34951766 |
| Eye luxation | 26.75 | 17.40 | 4 | 4932 | 9 | 34951986 |
| Thymoma | 25.73 | 17.40 | 5 | 4931 | 71 | 34951924 |
| Meningitis aseptic | 24.50 | 17.40 | 11 | 4925 | 3213 | 34948782 |
| Cerebral toxoplasmosis | 23.76 | 17.40 | 9 | 4927 | 1712 | 34950283 |
| Ophthalmoplegia | 23.17 | 17.40 | 9 | 4927 | 1831 | 34950164 |
| Myiasis | 22.46 | 17.40 | 4 | 4932 | 34 | 34951961 |
| Myopathy | 22.18 | 17.40 | 16 | 4920 | 11538 | 34940457 |
| Lip swelling | 21.56 | 17.40 | 18 | 4918 | 16062 | 34935933 |
| Faecal vomiting | 21.46 | 17.40 | 6 | 4930 | 436 | 34951559 |
| Histoplasmosis | 21.18 | 17.40 | 8 | 4928 | 1510 | 34950485 |
| Lichenoid keratosis | 20.48 | 17.40 | 9 | 4927 | 2499 | 34949496 |
| Osteopenia | 20.24 | 17.40 | 11 | 4925 | 4838 | 34947157 |
| Cholinergic syndrome | 19.78 | 17.40 | 6 | 4930 | 581 | 34951414 |
| Throat tightness | 19.39 | 17.40 | 13 | 4923 | 8345 | 34943650 |
| Osteoporosis | 18.70 | 17.40 | 15 | 4921 | 12653 | 34939342 |
| Skin hyperpigmentation | 18.22 | 17.40 | 9 | 4927 | 3255 | 34948740 |
| Rash scarlatiniform | 17.91 | 17.40 | 4 | 4932 | 115 | 34951880 |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Myasthenia gravis | 623.49 | 14.26 | 164 | 10335 | 10235 | 79723654 |
| Myasthenia gravis crisis | 501.40 | 14.26 | 92 | 10407 | 1019 | 79732870 |
| Eyelid ptosis | 199.00 | 14.26 | 69 | 10430 | 10975 | 79722914 |
| Diplopia | 130.98 | 14.26 | 71 | 10428 | 33395 | 79700494 |
| Thymoma | 87.08 | 14.26 | 17 | 10482 | 267 | 79733622 |
| Glucose tolerance impaired | 84.89 | 14.26 | 34 | 10465 | 8050 | 79725839 |
| Off label use | 82.74 | 14.26 | 284 | 10215 | 906931 | 78826958 |
| Myasthenic syndrome | 63.68 | 14.26 | 16 | 10483 | 826 | 79733063 |
| Muscular weakness | 61.68 | 14.26 | 90 | 10409 | 160639 | 79573250 |
| Respiratory failure | 52.34 | 14.26 | 89 | 10410 | 180822 | 79553067 |
| Cholinergic syndrome | 50.32 | 14.26 | 14 | 10485 | 1073 | 79732816 |
| Dysphagia | 47.71 | 14.26 | 69 | 10430 | 122067 | 79611822 |
| Cerebral toxoplasmosis | 43.46 | 14.26 | 15 | 10484 | 2347 | 79731542 |
| Meningitis aseptic | 42.68 | 14.26 | 20 | 10479 | 6908 | 79726981 |
| Adiposis dolorosa | 39.52 | 14.26 | 9 | 10490 | 304 | 79733585 |
| Ocular myasthenia | 37.62 | 14.26 | 9 | 10490 | 378 | 79733511 |
| Product residue present | 34.13 | 14.26 | 14 | 10485 | 3522 | 79730367 |
| Speech disorder | 30.94 | 14.26 | 37 | 10462 | 54408 | 79679481 |
| Nocardiosis | 30.74 | 14.26 | 15 | 10484 | 5664 | 79728225 |
| Ophthalmoplegia | 29.71 | 14.26 | 12 | 10487 | 2900 | 79730989 |
| Salivary hypersecretion | 29.26 | 14.26 | 20 | 10479 | 14204 | 79719685 |
| Suspected COVID-19 | 28.86 | 14.26 | 12 | 10487 | 3121 | 79730768 |
| Oromandibular dystonia | 28.66 | 14.26 | 9 | 10490 | 1049 | 79732840 |
| Diaphragmatic paralysis | 28.22 | 14.26 | 9 | 10490 | 1103 | 79732786 |
| Osteopenia | 26.83 | 14.26 | 21 | 10478 | 18343 | 79715546 |
| Pulmonary nocardiosis | 26.76 | 14.26 | 9 | 10490 | 1302 | 79732587 |
| Eye luxation | 26.20 | 14.26 | 4 | 10495 | 12 | 79733877 |
| Acute on chronic liver failure | 23.78 | 14.26 | 6 | 10493 | 315 | 79733574 |
| Bradycardia | 23.70 | 14.26 | 54 | 10445 | 135503 | 79598386 |
| Borderline leprosy | 23.69 | 14.26 | 4 | 10495 | 26 | 79733863 |
| Gastric infection | 23.63 | 14.26 | 11 | 10488 | 3742 | 79730147 |
| Dysarthria | 23.24 | 14.26 | 36 | 10463 | 67586 | 79666303 |
| Respiratory distress | 22.82 | 14.26 | 33 | 10466 | 58306 | 79675583 |
| Blood pressure increased | 22.49 | 14.26 | 70 | 10429 | 211290 | 79522599 |
| Myiasis | 22.44 | 14.26 | 4 | 10495 | 37 | 79733852 |
| Symptom recurrence | 21.78 | 14.26 | 9 | 10490 | 2305 | 79731584 |
| COVID-19 | 19.40 | 14.26 | 55 | 10444 | 157619 | 79576270 |
| Product substitution issue | 19.05 | 14.26 | 18 | 10481 | 20238 | 79713651 |
| Respiratory acidosis | 18.99 | 14.26 | 14 | 10485 | 11186 | 79722703 |
| Sinoatrial block | 18.89 | 14.26 | 7 | 10492 | 1344 | 79732545 |
| Torticollis | 18.21 | 14.26 | 8 | 10491 | 2379 | 79731510 |
| Asthenia | 17.96 | 14.26 | 122 | 10377 | 511567 | 79222322 |
| Lymphopenia | 17.74 | 14.26 | 21 | 10478 | 30536 | 79703353 |
| Postural orthostatic tachycardia syndrome | 17.41 | 14.26 | 6 | 10493 | 934 | 79732955 |
| Sensory disturbance | 17.33 | 14.26 | 15 | 10484 | 15062 | 79718827 |
| Thermal burn | 16.97 | 14.26 | 11 | 10488 | 7149 | 79726740 |
| Lichenoid keratosis | 16.96 | 14.26 | 9 | 10490 | 4048 | 79729841 |
| Faecal vomiting | 16.36 | 14.26 | 6 | 10493 | 1118 | 79732771 |
| Menopause | 15.89 | 14.26 | 7 | 10492 | 2095 | 79731794 |
| Drug ineffective for unapproved indication | 15.84 | 14.26 | 26 | 10473 | 51212 | 79682677 |
| Myopathy | 15.14 | 14.26 | 16 | 10483 | 20547 | 79713342 |
| Histoplasmosis | 15.10 | 14.26 | 7 | 10492 | 2358 | 79731531 |
| Bulbar palsy | 14.87 | 14.26 | 4 | 10495 | 270 | 79733619 |
| Muscle contractions involuntary | 14.75 | 14.26 | 8 | 10491 | 3757 | 79730132 |
| Diabetes mellitus | 14.55 | 14.26 | 32 | 10467 | 78358 | 79655531 |
| Arthritis bacterial | 14.52 | 14.26 | 11 | 10488 | 9155 | 79724734 |
| Cartilage injury | 14.52 | 14.26 | 6 | 10493 | 1537 | 79732352 |
| Restrictive pulmonary disease | 14.48 | 14.26 | 7 | 10492 | 2588 | 79731301 |
| Rebound effect | 14.48 | 14.26 | 10 | 10489 | 7216 | 79726673 |
| Skin hyperpigmentation | 14.38 | 14.26 | 10 | 10489 | 7293 | 79726596 |
None
| Source | Code | Description |
|---|---|---|
| ATC | N07AA02 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases |
| FDA MoA | N0000000177 | Cholinesterase Inhibitors |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D002800 | Cholinesterase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| FDA EPC | N0000175723 | Cholinesterase Inhibitor |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Myasthenia gravis | indication | 91637004 | DOID:437 |
| Neuromuscular Block due to Nondepolarizing Drug | indication | ||
| Prevention of Nerve Agent Poisoning | indication | ||
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
None
None
None
None
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase | Enzyme | INHIBITOR | IC50 | 6.44 | CHEMBL | CHEMBL | |||
| Cholinesterase | Enzyme | Ki | 5.46 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 7.09 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | Ki | 4.71 | CHEMBL |
| ID | Source |
|---|---|
| 4019921 | VUID |
| N0000148006 | NUI |
| D00487 | KEGG_DRUG |
| 101-26-8 | SECONDARY_CAS_RN |
| 4017783 | VANDF |
| 4019921 | VANDF |
| C0034261 | UMLSCUI |
| CHEBI:8665 | CHEBI |
| CHEMBL1115 | ChEMBL_ID |
| DB00545 | DRUGBANK_ID |
| CHEMBL812 | ChEMBL_ID |
| D011729 | MESH_DESCRIPTOR_UI |
| 4991 | PUBCHEM_CID |
| 8994 | IUPHAR_LIGAND_ID |
| 4685-03-4 | SECONDARY_CAS_RN |
| 19QM69HH21 | UNII |
| 9000 | RXNORM |
| 46043 | MMSL |
| 5392 | MMSL |
| d00363 | MMSL |
| 001707 | NDDF |
| 004687 | NDDF |
| 34915005 | SNOMEDCT_US |
| 373344003 | SNOMEDCT_US |
| 59953007 | SNOMEDCT_US |
| 278 | INN_ID |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-1404 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-2134 | TABLET | 30 mg | ORAL | ANDA | 11 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-3511 | TABLET | 60 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-3511 | TABLET | 60 mg | ORAL | ANDA | 12 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3010 | TABLET | 60 mg | ORAL | NDA | 15 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3010 | TABLET | 60 mg | ORAL | NDA | 15 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3012 | SOLUTION | 60 mg | ORAL | NDA | 15 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3012 | SOLUTION | 60 mg | ORAL | NDA | 15 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3013 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | NDA | 15 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3013 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | NDA | 15 sections |
| Regonol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-3040 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 19 sections |
| Regonol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-3040 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 19 sections |
| pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6622 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
| Pryidostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16571-833 | SOLUTION | 60 mg | ORAL | ANDA | 11 sections |
| PRYIDOSTIGMINE BROMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24689-104 | SOLUTION | 60 mg | ORAL | ANDA | 14 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-335 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-335 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58657-810 | TABLET | 30 mg | ORAL | ANDA | 13 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58657-810 | TABLET | 30 mg | ORAL | ANDA | 13 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-502 | TABLET | 60 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-502 | TABLET | 60 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | Human Prescription Drug Label | 1 | 63739-969 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
| Pyridostigmine Bromide | Human Prescription Drug Label | 1 | 64980-220 | TABLET | 180 mg | ORAL | ANDA | 9 sections |
| Pyridostigmine Bromide | Human Prescription Drug Label | 1 | 64980-220 | TABLET | 180 mg | ORAL | ANDA | 9 sections |
| pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65841-819 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
| pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65841-819 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66689-406 | SOLUTION | 60 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66689-406 | SOLUTION | 60 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68071-5032 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | ANDA | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-494 | TABLET | 60 mg | ORAL | ANDA | 15 sections |