pyridostigmine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
acetylcholinesterase inhibitors	2330	155-97-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pyridostigmine pyridostigmine bromide pyridostigmine iodide	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. Molecular weight: 181.21 Formula: C9H13N2O2 CLOGP: -4.26 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 33.42 ALOGS: -2.32 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pyridostigmine
pyridostigmine bromide
pyridostigmine iodide

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.

Molecular weight: 181.21
Formula: C9H13N2O2
CLOGP: -4.26
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 33.42
ALOGS: -2.32
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.18	g	O
10	mg	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
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
S (Water solubility)	52 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.50 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.10 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	1 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
April 6, 1955	FDA	VALEANT 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
Myasthenia gravis	577.22	17.25	128	7146	4453	63477295
Myasthenia gravis crisis	356.13	17.25	60	7214	452	63481296
Diplopia	86.96	17.25	46	7228	23682	63458066
Eyelid ptosis	74.85	17.25	29	7245	7238	63474510
Thymoma	68.65	17.25	13	7261	200	63481548
Off label use	49.36	17.25	179	7095	674283	62807465
Dysphagia	44.88	17.25	53	7221	88532	63393216
Muscular weakness	44.36	17.25	62	7212	122291	63359457
Adiposis dolorosa	40.77	17.25	9	7265	304	63481444
Nocardiosis	39.89	17.25	13	7261	1963	63479785

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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
Myasthenia gravis	251.87	17.40	75	4861	6865	34945130
Myasthenia gravis crisis	235.69	17.40	45	4891	582	34951413
Eyelid ptosis	148.73	17.40	48	4888	5718	34946277
Diplopia	92.84	17.40	46	4890	16797	34935198
Glucose tolerance impaired	48.25	17.40	18	4918	3286	34948709
Respiratory failure	44.48	17.40	65	4871	108507	34843488
Off label use	42.99	17.40	143	4793	419381	34532614
Myasthenic syndrome	39.02	17.40	10	4926	521	34951474
Product residue present	36.62	17.40	14	4922	2732	34949263
Muscular weakness	33.29	17.40	46	4890	72851	34879144

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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
Myasthenia gravis	623.49	14.26	164	10335	10235	79723654
Myasthenia gravis crisis	501.40	14.26	92	10407	1019	79732870
Eyelid ptosis	199.00	14.26	69	10430	10975	79722914
Diplopia	130.98	14.26	71	10428	33395	79700494
Thymoma	87.08	14.26	17	10482	267	79733622
Glucose tolerance impaired	84.89	14.26	34	10465	8050	79725839
Off label use	82.74	14.26	284	10215	906931	78826958
Myasthenic syndrome	63.68	14.26	16	10483	826	79733063
Muscular weakness	61.68	14.26	90	10409	160639	79573250
Respiratory failure	52.34	14.26	89	10410	180822	79553067

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N07AA02	NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases
FDA EPC	N0000175723	Cholinesterase Inhibitor
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

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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
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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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:

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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	6.44	CHEMBL	CHEMBL
Cholinesterase	Enzyme	P06276	CHLE_HUMAN		Ki	5.46	CHEMBL
Acetylcholinesterase	Enzyme		ACES_TORCA		IC50	7.09	CHEMBL
Acetylcholinesterase	Enzyme		ACES_BOVIN		Ki	4.71	CHEMBL

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External reference:

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ID	Source
001707	NDDF
004687	NDDF
101-26-8	SECONDARY_CAS_RN
19QM69HH21	UNII
278	INN_ID
34915005	SNOMEDCT_US
373344003	SNOMEDCT_US
4017783	VANDF
4019921	VUID
4019921	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Mestinon	HUMAN PRESCRIPTION DRUG LABEL	1	0187-3010	TABLET	60 mg	ORAL	NDA	15 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	0187-3012	SOLUTION	60 mg	ORAL	NDA	15 sections
Mestinon	HUMAN PRESCRIPTION DRUG LABEL	1	0187-3013	TABLET, EXTENDED RELEASE	180 mg	ORAL	NDA	15 sections
Mestinon	HUMAN PRESCRIPTION DRUG LABEL	1	0187-3013	TABLET, EXTENDED RELEASE	180 mg	ORAL	NDA	15 sections
Pryidostigmine Bromide	HUMAN PRESCRIPTION DRUG LABEL	1	16571-833	SOLUTION	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	0115-1404	TABLET, EXTENDED RELEASE	180 mg	ORAL	ANDA	12 sections
Pyridostigmine Bromide	HUMAN PRESCRIPTION DRUG LABEL	1	0115-2134	TABLET	30 mg	ORAL	ANDA	11 sections

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