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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
Molfile Inchi Smiles Synonyms: neostigmine eustigmin eustigmine prostigmin prostigmine vagostigmine neostigmine methylsulfate neostigmine bromide	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. Molecular weight: 223.30 Formula: C12H19N2O2 CLOGP: -2.81 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 29.54 ALOGS: -3.58 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

neostigmine
eustigmin
eustigmine
prostigmin
prostigmine
vagostigmine
neostigmine methylsulfate
neostigmine bromide

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.

Molecular weight: 223.30
Formula: C12H19N2O2
CLOGP: -2.81
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 29.54
ALOGS: -3.58
ROTB: 3

Status: OFP

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:

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Property	Value	Reference
CL (Clearance)	9.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	67 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	2 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	100 mg/mL	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.30 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	1 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
Vd (Volume of distribution)	0.74 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.12 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
May 31, 2013	FDA	ECLAT PHARMS LLC

FDA Adverse Event Reporting System (Female)

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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	73.73	28.84	29	1899	28653	63458441
Neuromuscular block prolonged	67.16	28.84	12	1916	530	63486564
Atrioventricular dissociation	48.51	28.84	8	1920	218	63486876
Anaphylactic reaction	47.98	28.84	28	1900	66072	63421022
Apnoea	47.10	28.84	15	1913	8007	63479087
Subileus	46.01	28.84	12	1916	3167	63483927
Procedural hypertension	45.63	28.84	8	1920	316	63486778
Vascular encephalopathy	43.17	28.84	8	1920	433	63486661
Dystonia	42.74	28.84	16	1912	13803	63473291
Pulmonary oedema	39.16	28.84	23	1905	54850	63432244

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FDA Adverse Event Reporting System (Male)

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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	123.94	37.63	40	1164	19893	34935834
Bradycardia	113.57	37.63	54	1150	75364	34880363
Cardiac arrest	89.96	37.63	50	1154	96109	34859618
Drug interaction	69.41	37.63	59	1145	225887	34729840
Metabolic acidosis	55.66	37.63	28	1176	43652	34912075
Pseudomonal sepsis	52.58	37.63	14	1190	3533	34952194
Appendicitis perforated	40.36	37.63	10	1194	1898	34953829
Acute pulmonary oedema	38.54	37.63	13	1191	7330	34948397

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FDA Adverse Event Reporting System (Geriatric)

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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	142.02	24.83	57	3143	44970	79696218
Bradycardia	114.93	24.83	70	3130	135487	79605701
Cardiac arrest	102.01	24.83	71	3129	172025	79569163
Pulmonary oedema	68.14	24.83	43	3157	88211	79652977
Neuromuscular block prolonged	67.62	24.83	14	3186	1016	79740172
Drug interaction	64.41	24.83	81	3119	415102	79326086
Apnoea	51.83	24.83	19	3181	11685	79729503
Tachycardia	50.90	24.83	48	3152	177720	79563468
Laryngospasm	48.76	24.83	14	3186	3983	79737205
Delayed recovery from anaesthesia	45.17	24.83	11	3189	1662	79739526

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
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
FDA MoA	N0000000177	Cholinesterase Inhibitors
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D002800	Cholinesterase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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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

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🐶 Veterinary Drug Use

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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

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🐶 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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
3MG/3ML (1MG/ML)	NEOSTIGMINE METHYLSULFATE	DR REDDYS	A216291	July 6, 2022	RX	SOLUTION	INTRAVENOUS	Jan. 21, 2023	COMPETITIVE GENERIC THERAPY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN	INHIBITOR	IC50	7.59	WOMBAT-PK	CHEMBL
Cholinesterase	Enzyme	P06276	CHLE_HUMAN		IC50	7.22	CHEMBL
Acetylcholinesterase	Enzyme		ACES_TORCA		IC50	8.34	CHEMBL
Acetylcholinesterase	Enzyme		ACES_RAT		IC50	7.46	CHEMBL
Acetylcholinesterase	Enzyme		ACES_ELEEL		Ki	6	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		IC50	7.15	CHEMBL

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External reference:

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ID	Source
001703	NDDF
001704	NDDF
001705	NDDF
114-80-7	SECONDARY_CAS_RN
262500	RXNORM
373346001	SNOMEDCT_US
387294009	SNOMEDCT_US
3968	MMSL
3982TWQ96G	UNII
401	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	0404-9925	INJECTION	1 mg	INTRAVENOUS	ANDA	15 sections
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	0548-9601	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	0548-9602	INJECTION	1 mg	INTRAVENOUS	ANDA	16 sections

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