pyridostigmine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| acetylcholinesterase inhibitors | 2330 | 155-97-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.18 | g | O |
| 10 | mg | P |
ADMET properties:
| 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 µM/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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 6, 1955 | FDA | VALEANT PHARMS LLC |
FDA Adverse Event Reporting System (Female)
| 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 | 89.71 | 58.63 | 13 | 126 | 609 | 2357337 |
| Myasthenia gravis crisis | 67.78 | 58.63 | 8 | 131 | 70 | 2357876 |
FDA Adverse Event Reporting System (Male)
| 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 | 117.68 | 49.44 | 17 | 96 | 594 | 1746074 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07AA02 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases |
| FDA EPC | N0000175723 | Cholinesterase Inhibitor |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D002800 | Cholinesterase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use (View source of the data)
| 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 |
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| 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 | Ki | 4.71 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 7.09 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019921 | VUID |
| N0000148006 | NUI |
| C0034261 | UMLSCUI |
| D00487 | KEGG_DRUG |
| 59953007 | SNOMEDCT_US |
| 4019921 | VANDF |
| 9000 | RXNORM |
| 373344003 | SNOMEDCT_US |
| d00363 | MMSL |
| 004687 | NDDF |
| 4991 | PUBCHEM_CID |
| CHEBI:8665 | CHEBI |
| CHEMBL812 | ChEMBL_ID |
| CHEMBL1115 | ChEMBL_ID |
| DB00545 | DRUGBANK_ID |
| KVI301NA53 | UNII |
| 278 | INN_ID |
| 101-26-8 | SECONDARY_CAS_RN |
| D011729 | MESH_DESCRIPTOR_UI |
| 8994 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| 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 | 12 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3012 | SOLUTION | 60 mg | ORAL | NDA | 12 sections |
| Mestinon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-3013 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | NDA | 12 sections |
| Regonol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-3040 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 13 sections |
| pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6622 | TABLET | 60 mg | ORAL | ANDA | 11 sections |
| Pryidostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13811-716 | SOLUTION | 60 mg | ORAL | ANDA | 11 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-335 | TABLET, EXTENDED RELEASE | 180 mg | ORAL | ANDA | 10 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-638 | TABLET | 60 mg | ORAL | NDA authorized generic | 11 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58657-810 | TABLET | 30 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 | 65084-999 | 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 | 11 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 | 12 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 | 11 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-302 | TABLET | 60 mg | ORAL | NDA authorized generic | 11 sections |
| pyridostigmine bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-307 | SOLUTION | 60 mg | ORAL | NDA authorized generic | 12 sections |
| Pyridostigmine Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1731 | SOLUTION | 60 mg | ORAL | ANDA | 11 sections |
| Pyridostigmine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70954-148 | SOLUTION | 60 mg | ORAL | ANDA | 11 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 | 19 sections |