neostigmine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| acetylcholinesterase inhibitors | 1897 | 59-99-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 60 | mg | O |
| 2 | mg | P |
| 0.40 | ml | None |
| 40 | mg | ointment |
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) | 67 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.12 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 2 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.74 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.30 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 31, 2013 | FDA | ECLAT 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 |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 66.39 | 28.47 | 27 | 1783 | 24686 | 50578628 |
| Neuromuscular block prolonged | 65.90 | 28.47 | 12 | 1798 | 499 | 50602815 |
| Atrioventricular dissociation | 47.21 | 28.47 | 8 | 1802 | 218 | 50603096 |
| Subileus | 45.75 | 28.47 | 12 | 1798 | 2747 | 50600567 |
| Procedural hypertension | 45.52 | 28.47 | 8 | 1802 | 271 | 50603043 |
| Anaphylactic reaction | 43.66 | 28.47 | 26 | 1784 | 54029 | 50549285 |
| Vascular encephalopathy | 42.85 | 28.47 | 8 | 1802 | 382 | 50602932 |
| Apnoea | 42.70 | 28.47 | 14 | 1796 | 6952 | 50596362 |
| Dystonia | 42.49 | 28.47 | 16 | 1794 | 11910 | 50591404 |
| Pulmonary oedema | 35.55 | 28.47 | 22 | 1788 | 48916 | 50554398 |
| Myopia | 32.04 | 28.47 | 8 | 1802 | 1505 | 50601809 |
| Delayed recovery from anaesthesia | 32 | 28.47 | 7 | 1803 | 742 | 50602572 |
| Ileus | 30.59 | 28.47 | 13 | 1797 | 13216 | 50590098 |
| Generalised tonic-clonic seizure | 30.34 | 28.47 | 16 | 1794 | 26294 | 50577020 |
| Presbyopia | 29.33 | 28.47 | 6 | 1804 | 461 | 50602853 |
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 |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 126.88 | 35.66 | 40 | 1038 | 17472 | 29555977 |
| Bradycardia | 84.40 | 35.66 | 43 | 1035 | 65586 | 29507863 |
| Cardiac arrest | 58.17 | 35.66 | 37 | 1041 | 85554 | 29487895 |
| Metabolic acidosis | 58.14 | 35.66 | 28 | 1050 | 37634 | 29535815 |
| Pseudomonal sepsis | 54.40 | 35.66 | 14 | 1064 | 2928 | 29570521 |
| Drug interaction | 47.25 | 35.66 | 46 | 1032 | 197339 | 29376110 |
| Appendicitis perforated | 40.93 | 35.66 | 10 | 1068 | 1693 | 29571756 |
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 |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 135.51 | 25.95 | 55 | 2892 | 39227 | 64456558 |
| Bradycardia | 87.95 | 25.95 | 59 | 2888 | 118160 | 64377625 |
| Neuromuscular block prolonged | 66.55 | 25.95 | 14 | 2933 | 963 | 64494822 |
| Cardiac arrest | 65.50 | 25.95 | 55 | 2892 | 154009 | 64341776 |
| Pulmonary oedema | 65.09 | 25.95 | 42 | 2905 | 78632 | 64417153 |
| Apnoea | 51.58 | 25.95 | 19 | 2928 | 10403 | 64485382 |
| Tachycardia | 46.89 | 25.95 | 45 | 2902 | 149534 | 64346251 |
| Drug interaction | 45.12 | 25.95 | 68 | 2879 | 362015 | 64133770 |
| Delayed recovery from anaesthesia | 44.75 | 25.95 | 11 | 2936 | 1517 | 64494268 |
| Laryngospasm | 44.57 | 25.95 | 13 | 2934 | 3432 | 64492353 |
| Procedural hypertension | 43.22 | 25.95 | 8 | 2939 | 283 | 64495502 |
| Atrioventricular dissociation | 42.34 | 25.95 | 8 | 2939 | 317 | 64495468 |
| Dystonia | 40.69 | 25.95 | 19 | 2928 | 18846 | 64476939 |
| Anaphylactic reaction | 38.75 | 25.95 | 29 | 2918 | 68635 | 64427150 |
| Vascular encephalopathy | 37.83 | 25.95 | 8 | 2939 | 564 | 64495221 |
| Subileus | 35.84 | 25.95 | 12 | 2935 | 4965 | 64490820 |
| Pseudomonal sepsis | 35.39 | 25.95 | 12 | 2935 | 5160 | 64490625 |
| Cholinergic syndrome | 34.74 | 25.95 | 8 | 2939 | 835 | 64494950 |
| Appendicitis perforated | 33.66 | 25.95 | 10 | 2937 | 2810 | 64492975 |
| Atrioventricular block second degree | 32.79 | 25.95 | 12 | 2935 | 6442 | 64489343 |
| Metabolic acidosis | 31.46 | 25.95 | 26 | 2921 | 70932 | 64424853 |
| Ileus | 31.44 | 25.95 | 17 | 2930 | 22949 | 64472836 |
| Hyperthermia malignant | 30.58 | 25.95 | 9 | 2938 | 2450 | 64493335 |
| Post procedural complication | 29.77 | 25.95 | 16 | 2931 | 21337 | 64474448 |
| Myopia | 28.90 | 25.95 | 8 | 2939 | 1750 | 64494035 |
| White blood cell count increased | 28.87 | 25.95 | 24 | 2923 | 65990 | 64429795 |
| Neuromuscular blockade | 27.29 | 25.95 | 6 | 2941 | 508 | 64495277 |
| Presbyopia | 26.67 | 25.95 | 6 | 2941 | 564 | 64495221 |
| Non-cardiogenic pulmonary oedema | 26.41 | 25.95 | 7 | 2940 | 1301 | 64494484 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07AA01 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases |
| ATC | N07AA51 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases |
| ATC | S01EB06 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Parasympathomimetics |
| 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 |
| MeSH PA | D010277 | Parasympathomimetics |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| CHEBI has role | CHEBI:38462 | acetylcholinesterase inhibitors |
| CHEBI has role | CHEBI:74530 | curare poisoning antidote |
| CHEBI has role | CHEBI:37733 | EC 3.1.1.8 inhibitor |
| FDA EPC | N0000175723 | Cholinesterase Inhibitor |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Myasthenia gravis | indication | 91637004 | DOID:437 |
| Reversal of neuromuscular blockade | indication | 241703000 | |
| Retention of urine | indication | 267064002 | |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Increased gastric tonus | contraindication | 18644006 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Peritonitis | contraindication | 48661000 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Coronary occlusion | contraindication | 63739005 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Seizure disorder | contraindication | 128613002 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Macrocolon | contraindication | 367495003 | |
| Gastrointestinal hypomotility | contraindication | 421807004 | |
| Increased Bronchial Secretions | contraindication | ||
| Colonic Necrosis | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cattle | Rumen atony | Indication |
| Cattle | Initiating peristalsis which causes evacuation of the bowel | Indication |
| Cattle | Emptying the urinary bladder | Indication |
| Cattle | Stimulating skeletal muscle contractions | Indication |
| Cattle | Antagonizes the effect of curare | Indication |
| Horses | Rumen atony | Indication |
| Horses | Initiating peristalsis which causes evacuation of the bowel | Indication |
| Horses | Emptying the urinary bladder | Indication |
| Horses | Stimulating skeletal muscle contractions | Indication |
| Horses | Antagonizes the effect of curare | Indication |
| Sheep | Rumen atony | Indication |
| Sheep | Initiating peristalsis which causes evacuation of the bowel | Indication |
| Sheep | Emptying the urinary bladder | Indication |
| Sheep | Stimulating skeletal muscle contractions | Indication |
| Sheep | Antagonizes the effect of curare | Indication |
| Swine | Rumen atony | Indication |
| Swine | Initiating peristalsis which causes evacuation of the bowel | Indication |
| Swine | Emptying the urinary bladder | Indication |
| Swine | Stimulating skeletal muscle contractions | Indication |
| Swine | Antagonizes the effect of curare | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Stiglyn 1:500 | Intervet Inc. | 1 |
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 | 7.59 | WOMBAT-PK | CHEMBL | |||
| Cholinesterase | Enzyme | IC50 | 7.22 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 8.34 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 7.46 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | Ki | 6 | CHEMBL | |||||
| Cholinesterase | Enzyme | IC50 | 7.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019856 | VUID |
| N0000147942 | NUI |
| D00995 | KEGG_DRUG |
| 51-60-5 | SECONDARY_CAS_RN |
| 114-80-7 | SECONDARY_CAS_RN |
| 4017784 | VANDF |
| 4017785 | VANDF |
| 4019856 | VANDF |
| C0027679 | UMLSCUI |
| CHEBI:7514 | CHEBI |
| CHEMBL54126 | ChEMBL_ID |
| CHEMBL278020 | ChEMBL_ID |
| DB01400 | DRUGBANK_ID |
| CHEMBL211471 | ChEMBL_ID |
| D009388 | MESH_DESCRIPTOR_UI |
| 4456 | PUBCHEM_CID |
| 8993 | IUPHAR_LIGAND_ID |
| 3982TWQ96G | UNII |
| 262500 | RXNORM |
| 3968 | MMSL |
| 5165 | MMSL |
| 5166 | MMSL |
| 72417 | MMSL |
| 9863 | MMSL |
| d00313 | MMSL |
| 001703 | NDDF |
| 001704 | NDDF |
| 001705 | NDDF |
| 373346001 | SNOMEDCT_US |
| 387294009 | SNOMEDCT_US |
| 80024007 | SNOMEDCT_US |
| 87151005 | SNOMEDCT_US |
| 401 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9925 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 15 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-1133 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 24 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-1134 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0548-9601 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 16 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0548-9602 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6149 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6150 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 24 sections |
| NEOSTIGMINE METHYLSULFATE | Human Prescription Drug Label | 1 | 14445-413 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 24 sections |
| NEOSTIGMINE METHYLSULFATE | Human Prescription Drug Label | 1 | 14445-414 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-610 | INJECTION, SOLUTION | 0.50 mg | INTRAVENOUS | ANDA | 28 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-611 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 28 sections |
| neostigmine methylsulfate | Human Prescription Drug Label | 1 | 31722-994 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 24 sections |
| neostigmine methylsulfate | Human Prescription Drug Label | 1 | 31722-995 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-188 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 23 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-189 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 23 sections |
| Neostigmine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-528 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 24 sections |
| Neostigmine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-529 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-4532 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 17 sections |
| Neostigmine methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-5197 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 25 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1557 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 16 sections |
| Bloxiverz | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51754-1210 | INJECTION | 0.50 mg | INTRAVENOUS | NDA | 25 sections |
| Bloxiverz | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51754-1220 | INJECTION | 1 mg | INTRAVENOUS | NDA | 25 sections |
| Bloxiverz | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51754-1240 | INJECTION | 1 mg | INTRAVENOUS | NDA | 26 sections |
| Bloxiverz | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51754-1240 | INJECTION | 1 mg | INTRAVENOUS | NDA | 26 sections |
| NEOSTIGMINE METHYLSULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-057 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 15 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-413 | INJECTION, SOLUTION | 0.50 mg | INTRAVENOUS | NDA | 24 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-413 | INJECTION, SOLUTION | 0.50 mg | INTRAVENOUS | NDA | 24 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-415 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | NDA | 24 sections |
| Neostigmine Methylsulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-415 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | NDA | 24 sections |
| Neostigmine Methylsulfate | Human Prescription Drug Label | 1 | 65145-111 | INJECTION | 0.50 mg | INTRAVENOUS | ANDA | 20 sections |