physostigmine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| acetylcholinesterase inhibitors | 2159 | 57-47-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | ml | None |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.06 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 10 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.90 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 72 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.64 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.99 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1875 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Anticholinergic syndrome | 80.72 | 74.60 | 13 | 206 | 3598 | 79740571 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | S01EB05 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Parasympathomimetics |
| ATC | V03AB19 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D002800 | Cholinesterase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D008916 | Miotics |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| CHEBI has role | CHEBI:37733 | EC 3.1.1.8 inhibitor |
| CHEBI has role | CHEBI:51068 | Miotico |
| CHEBI has role | CHEBI:74530 | curare poisoning antidote |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Anticholinergic Toxicity | indication | ||
| Secondary glaucoma | off-label use | 95717004 | |
| Angle-closure glaucoma | off-label use | 392291006 | DOID:13550 |
| Hereditary Ataxias | off-label use | ||
| Keratitis | contraindication | 5888003 | DOID:4677 |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Parkinsonism | contraindication | 32798002 | |
| Gangrene | contraindication | 36024000 | |
| Retinal detachment | contraindication | 42059000 | DOID:5327 |
| Bradycardia | contraindication | 48867003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Neuromuscular block, function | contraindication | 55394004 | |
| Iritis | contraindication | 65074000 | DOID:1406 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Anterior uveitis | contraindication | 410692006 | DOID:1407 |
| Pupillary Block Glaucoma | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.89 | acidic |
| pKa2 | 8.15 | Basic |
| pKa3 | 2.09 | Basic |
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 | 9.37 | CHEMBL | IUPHAR | |||
| Cholinesterase | Enzyme | Ki | 5.30 | CHEMBL | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.70 | DRUG MATRIX | |||||
| Acetylcholinesterase | Enzyme | IC50 | 7.96 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 9.17 | CHEMBL | |||||
| Butyrylcholinesterase; Protein Bche | Enzyme | IC50 | 8.12 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 9.17 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | Ki | 7.47 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 7.52 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | IC50 | 4.43 | CHEMBL | |||||
| Cholinesterase | Enzyme | IC50 | 6.55 | CHEMBL | |||||
| Butyrylcholinesterase | Enzyme | IC50 | 7.80 | CHEMBL | |||||
| Cholinesterase | Enzyme | Ki | 7.39 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 7.70 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019894 | VUID |
| N0000147979 | NUI |
| D00196 | KEGG_DRUG |
| 57-64-7 | SECONDARY_CAS_RN |
| 4018587 | VANDF |
| 4019894 | VANDF |
| C0031849 | UMLSCUI |
| CHEBI:27953 | CHEBI |
| CHEMBL94 | ChEMBL_ID |
| DB00981 | DRUGBANK_ID |
| CHEMBL338975 | ChEMBL_ID |
| D010830 | MESH_DESCRIPTOR_UI |
| 5983 | PUBCHEM_CID |
| 6598 | IUPHAR_LIGAND_ID |
| C026718 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9U1VM840SP | UNII |
| 33656 | RXNORM |
| 1415 | MMSL |
| 5296 | MMSL |
| d00342 | MMSL |
| 001700 | NDDF |
| 001701 | NDDF |
| 373347005 | SNOMEDCT_US |
| 69050006 | SNOMEDCT_US |
| 85429009 | SNOMEDCT_US |
| CHEMBL2105891 | ChEMBL_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PHYSOSTIGMINE SALICYLATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9934 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 14 sections |
| PHYSOSTIGMINE SALICYLATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9934 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 14 sections |
| Physostigmine Salicylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-510 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |
| Physostigmine Salicylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-510 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |
| Physostigmine Salicylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-510 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |
| Physostigmine Salicylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-4406 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |
| PHYSOSTIGMINE SALICYLATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1439 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |
| PHYSOSTIGMINE SALICYLATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1439 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |
| PHYSOSTIGMINE SALICYLATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-510 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 14 sections |
| Physostigmine Salicylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7074 | INJECTION | 1 mg | INTRAVENOUS | unapproved drug other | 13 sections |