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) | 100 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
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 | 445.22 | 16.81 | 98 | 5438 | 3454 | 50596134 |
Myasthenia gravis crisis | 289.73 | 16.81 | 48 | 5488 | 340 | 50599248 |
Diplopia | 68.39 | 16.81 | 36 | 5500 | 19224 | 50580364 |
Eyelid ptosis | 62.37 | 16.81 | 24 | 5512 | 6163 | 50593425 |
Muscular weakness | 43.90 | 16.81 | 53 | 5483 | 94960 | 50504628 |
Dysphagia | 42.10 | 16.81 | 47 | 5489 | 77471 | 50522117 |
Adiposis dolorosa | 36.59 | 16.81 | 8 | 5528 | 271 | 50599317 |
Cholinergic syndrome | 34.08 | 16.81 | 8 | 5528 | 374 | 50599214 |
Myasthenic syndrome | 33.33 | 16.81 | 7 | 5529 | 195 | 50599393 |
Thymoma | 33.12 | 16.81 | 6 | 5530 | 75 | 50599513 |
Diaphragmatic paralysis | 30.97 | 16.81 | 8 | 5528 | 557 | 50599031 |
Product residue present | 29.18 | 16.81 | 12 | 5524 | 3660 | 50595928 |
Acute on chronic liver failure | 27.98 | 16.81 | 6 | 5530 | 185 | 50599403 |
Blood pressure increased | 27.60 | 16.81 | 51 | 5485 | 133081 | 50466507 |
Intentional product use issue | 24.81 | 16.81 | 36 | 5500 | 76882 | 50522706 |
Meningitis aseptic | 24.52 | 16.81 | 11 | 5525 | 4141 | 50595447 |
Sinoatrial block | 23.98 | 16.81 | 7 | 5529 | 768 | 50598820 |
Headache | 22.52 | 16.81 | 112 | 5424 | 506423 | 50093165 |
Salivary hypersecretion | 22.48 | 16.81 | 12 | 5524 | 6579 | 50593009 |
Speech disorder | 21.80 | 16.81 | 23 | 5513 | 35525 | 50564063 |
Gastric infection | 21.16 | 16.81 | 9 | 5527 | 2983 | 50596605 |
Supine hypertension | 21.16 | 16.81 | 4 | 5532 | 64 | 50599524 |
Transfusion-related circulatory overload | 20.99 | 16.81 | 4 | 5532 | 67 | 50599521 |
COVID-19 | 19.86 | 16.81 | 25 | 5511 | 46637 | 50552951 |
Cartilage injury | 18.82 | 16.81 | 7 | 5529 | 1635 | 50597953 |
Product substitution issue | 18.47 | 16.81 | 14 | 5522 | 14043 | 50585545 |
Asthenia | 17.42 | 16.81 | 75 | 5461 | 318967 | 50280621 |
Respiratory distress | 17.42 | 16.81 | 19 | 5517 | 30470 | 50569118 |
Off label use | 17.04 | 16.81 | 99 | 5437 | 474327 | 50125261 |
Thermal burn | 17.03 | 16.81 | 9 | 5527 | 4832 | 50594756 |
Drooling | 16.96 | 16.81 | 8 | 5528 | 3376 | 50596212 |
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 | 246.77 | 17.50 | 62 | 3996 | 3089 | 29567380 |
Myasthenia gravis crisis | 202.98 | 17.50 | 38 | 4020 | 453 | 29570016 |
Eyelid ptosis | 90.62 | 17.50 | 32 | 4026 | 5154 | 29565315 |
Diplopia | 75.75 | 17.50 | 37 | 4021 | 13481 | 29556988 |
Respiratory failure | 40.87 | 17.50 | 58 | 4000 | 97073 | 29473396 |
Product residue present | 38.08 | 17.50 | 14 | 4044 | 2525 | 29567944 |
Myasthenic syndrome | 31.78 | 17.50 | 8 | 4050 | 399 | 29570070 |
Ocular myasthenia | 30.97 | 17.50 | 7 | 4051 | 219 | 29570250 |
Off label use | 29.31 | 17.50 | 99 | 3959 | 300701 | 29269768 |
Eye luxation | 27.53 | 17.50 | 4 | 4054 | 7 | 29570462 |
Thymoma | 27.14 | 17.50 | 5 | 4053 | 54 | 29570415 |
Cerebral toxoplasmosis | 25.72 | 17.50 | 9 | 4049 | 1407 | 29569062 |
Myiasis | 24.09 | 17.50 | 4 | 4054 | 22 | 29570447 |
Histoplasmosis | 22.28 | 17.50 | 8 | 4050 | 1348 | 29569121 |
Faecal vomiting | 22.26 | 17.50 | 6 | 4052 | 392 | 29570077 |
Lichenoid keratosis | 21.99 | 17.50 | 9 | 4049 | 2161 | 29568308 |
Lip swelling | 21.57 | 17.50 | 16 | 4042 | 12394 | 29558075 |
Myopathy | 21.56 | 17.50 | 15 | 4043 | 10518 | 29559951 |
Meningitis aseptic | 21.20 | 17.50 | 9 | 4049 | 2367 | 29568102 |
Cholinergic syndrome | 21.07 | 17.50 | 6 | 4052 | 480 | 29569989 |
Ophthalmoplegia | 20.60 | 17.50 | 8 | 4050 | 1674 | 29568795 |
Muscular weakness | 20.30 | 17.50 | 33 | 4025 | 62019 | 29508450 |
Skin hyperpigmentation | 19.58 | 17.50 | 9 | 4049 | 2855 | 29567614 |
Rebound effect | 19.14 | 17.50 | 8 | 4050 | 2023 | 29568446 |
Throat tightness | 19.14 | 17.50 | 12 | 4046 | 7079 | 29563390 |
Rash scarlatiniform | 18.06 | 17.50 | 4 | 4054 | 114 | 29570355 |
Intestinal perforation | 17.70 | 17.50 | 12 | 4046 | 8074 | 29562395 |
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 | 538.68 | 15.79 | 129 | 8177 | 5609 | 64484817 |
Myasthenia gravis crisis | 412.24 | 15.79 | 75 | 8231 | 809 | 64489617 |
Eyelid ptosis | 136.76 | 15.79 | 50 | 8256 | 9475 | 64480951 |
Diplopia | 100.95 | 15.79 | 55 | 8251 | 26710 | 64463716 |
Myasthenic syndrome | 57.88 | 15.79 | 14 | 8292 | 631 | 64489795 |
Cholinergic syndrome | 54.15 | 15.79 | 14 | 8292 | 829 | 64489597 |
Thymoma | 52.32 | 15.79 | 10 | 8296 | 143 | 64490283 |
Muscular weakness | 51.11 | 15.79 | 72 | 8234 | 127266 | 64363160 |
Respiratory failure | 47.55 | 15.79 | 79 | 8227 | 161104 | 64329322 |
Cerebral toxoplasmosis | 43.46 | 15.79 | 14 | 8292 | 1812 | 64488614 |
Dysphagia | 42.26 | 15.79 | 60 | 8246 | 106752 | 64383674 |
Off label use | 39.24 | 15.79 | 173 | 8133 | 632633 | 63857793 |
Ocular myasthenia | 38.08 | 15.79 | 9 | 8297 | 367 | 64490059 |
Meningitis aseptic | 37.09 | 15.79 | 17 | 8289 | 5713 | 64484713 |
Product residue present | 35.60 | 15.79 | 14 | 8292 | 3228 | 64487198 |
Adiposis dolorosa | 35.29 | 15.79 | 8 | 8298 | 271 | 64490155 |
Salivary hypersecretion | 32.60 | 15.79 | 20 | 8286 | 12093 | 64478333 |
Ophthalmoplegia | 27.34 | 15.79 | 11 | 8295 | 2691 | 64487735 |
Eye luxation | 26.82 | 15.79 | 4 | 8302 | 10 | 64490416 |
Diaphragmatic paralysis | 24.90 | 15.79 | 8 | 8298 | 1026 | 64489400 |
Acute on chronic liver failure | 24.50 | 15.79 | 6 | 8300 | 285 | 64490141 |
Myiasis | 23.91 | 15.79 | 4 | 8302 | 25 | 64490401 |
Gastric infection | 22.17 | 15.79 | 10 | 8296 | 3238 | 64487188 |
Blood pressure increased | 21.91 | 15.79 | 60 | 8246 | 172492 | 64317934 |
Dysarthria | 21.48 | 15.79 | 32 | 8274 | 59374 | 64431052 |
Sinoatrial block | 20.05 | 15.79 | 7 | 8299 | 1159 | 64489267 |
COVID-19 | 19.27 | 15.79 | 32 | 8274 | 65108 | 64425318 |
Lichenoid keratosis | 18.82 | 15.79 | 9 | 8297 | 3325 | 64487101 |
Respiratory distress | 18.65 | 15.79 | 28 | 8278 | 52303 | 64438123 |
Toxicity to various agents | 18.55 | 15.79 | 12 | 8294 | 363501 | 64126925 |
Asthenia | 17.94 | 15.79 | 105 | 8201 | 427939 | 64062487 |
Myopathy | 17.49 | 15.79 | 16 | 8290 | 17664 | 64472762 |
Speech disorder | 17.38 | 15.79 | 26 | 8280 | 48415 | 64442011 |
Sensory disturbance | 17.22 | 15.79 | 14 | 8292 | 13194 | 64477232 |
Faecal vomiting | 17.03 | 15.79 | 6 | 8300 | 1019 | 64489407 |
Thermal burn | 16.53 | 15.79 | 10 | 8296 | 5896 | 64484530 |
Histoplasmosis | 16.30 | 15.79 | 7 | 8299 | 2015 | 64488411 |
Respiratory acidosis | 16.24 | 15.79 | 12 | 8294 | 9843 | 64480583 |
Restrictive pulmonary disease | 15.82 | 15.79 | 7 | 8299 | 2165 | 64488261 |
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 | 0115-3511 | 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 | 0187-3012 | SOLUTION | 60 mg | ORAL | NDA | 15 sections |
Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3013 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | NDA | 15 sections |
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 | 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 | 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 | 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 | 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 | 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 |
pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68382-659 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-301 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | NDA authorized generic | 12 sections |
Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-302 | TABLET | 60 mg | ORAL | NDA authorized generic | 12 sections |
pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-307 | SOLUTION | 60 mg | ORAL | NDA authorized generic | 15 sections |
Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1731 | SOLUTION | 60 mg | ORAL | ANDA | 11 sections |
Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69784-130 | SOLUTION | 60 mg | ORAL | ANDA | 14 sections |
Pyridostigmine | Human Prescription Drug Label | 1 | 70954-148 | SOLUTION | 60 mg | ORAL | ANDA | 13 sections |
Pyridostigmine Bromide | Human Prescription Drug Label | 1 | 71930-028 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72458-128 | TABLET | 30 mg | ORAL | NDA | 33 sections |
Pryidostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73152-028 | SOLUTION | 60 mg | ORAL | ANDA | 11 sections |