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

Stem definition	Drug id	CAS RN
	2699	26171-23-3

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tolmetin sodium anhydrous
tolmetin
tolmetine
tolmetin sodium
tolmetin sodium salt
tolmetin sodium salt dihydrate

A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.

Molecular weight: 257.29
Formula: C15H15NO3
CLOGP: 2.21
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 59.30
ALOGS: -3.29
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.70	g	O
0.70	g	R

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.22 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	7 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	116.60 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	95 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
March 24, 1976	FDA

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
Drug hypersensitivity	108.07	51.49	29	39	310658	63178296

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
Drug hypersensitivity	113.51	62.86	27	27	298889	79445445

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M01AB03	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Acetic acid derivatives and related substances
ATC	M02AA21	MUSCULO-SKELETAL SYSTEM TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN Antiinflammatory preparations, non-steroids for topical use
FDA CS	M0001335	Anti-Inflammatory Agents, Non-Steroidal
FDA MoA	N0000000160	Cyclooxygenase Inhibitors
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:35544	cyclooxygenase inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D000894	Anti-Inflammatory Agents, Non-Steroidal
MeSH PA	D018501	Antirheumatic Agents
MeSH PA	D016861	Cyclooxygenase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
FDA EPC	N0000175722	Nonsteroidal Anti-inflammatory Drug

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

Disease	Relation	SNOMED_ID	DOID
Rheumatoid arthritis	indication	69896004	DOID:7148
Osteoarthritis	indication	396275006
Juvenile rheumatoid arthritis	indication	410795001
Ankylosing spondylitis	off-label use	9631008	DOID:7147
Peptic ulcer	contraindication	13200003	DOID:750
Myocardial infarction	contraindication	22298006	DOID:5844
Hypertensive disorder	contraindication	38341003	DOID:10763
Gastrointestinal ulcer	contraindication	40845000
Chronic heart failure	contraindication	48447003
Disorder of cardiovascular system	contraindication	49601007	DOID:1287
Hepatic failure	contraindication	59927004
Blood coagulation disorder	contraindication	64779008	DOID:1247
Gastrointestinal hemorrhage	contraindication	74474003
Kidney disease	contraindication	90708001	DOID:557
Coronary artery bypass graft	contraindication	232717009
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Cardiovascular event risk	contraindication	395112001
Smokes tobacco daily	contraindication	449868002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.6	acidic

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
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	6.84		WOMBAT-PK	CHEMBL
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	6.27		WOMBAT-PK	CHEMBL
Aldose reductase	Enzyme	P15121	ALDR_HUMAN		IC50	5.62		CHEMBL
Lactoylglutathione lyase	Enzyme	Q04760	LGUL_HUMAN		Ki	4.06		CHEMBL
Interleukin-8	Cytokine	P10145	IL8_HUMAN		IC50	7.05		CHEMBL
Aldose reductase	Enzyme		ALDR_RAT		IC50	5.67		DRUG MATRIX

External reference:

ID	Source
4019952	VUID
N0000148037	NUI
D00158	KEGG_DRUG
35711-34-3	SECONDARY_CAS_RN
64490-92-2	SECONDARY_CAS_RN
4018480	VANDF
4019952	VANDF
C0040377	UMLSCUI
CHEBI:71941	CHEBI
TLT	PDB_CHEM_ID
CHEMBL1020	ChEMBL_ID
CHEMBL1200613	ChEMBL_ID
DB00500	DRUGBANK_ID
D014046	MESH_DESCRIPTOR_UI
5509	PUBCHEM_CID
7311	IUPHAR_LIGAND_ID
2861	INN_ID
D8K2JPN18B	UNII
10636	RXNORM
1146	MMSL
5598	MMSL
d00054	MMSL
002379	NDDF
004811	NDDF
372748008	SNOMEDCT_US
45680002	SNOMEDCT_US
60988002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
TOLMETIN SODIUM	Human Prescription Drug Label	1	16571-825	TABLET, FILM COATED	600 mg	ORAL	ANDA	25 sections
Tolmetin Sodium	Human Prescription Drug Label	1	16571-826	CAPSULE	400 mg	ORAL	ANDA	24 sections
TOLMETIN SODIUM	HUMAN PRESCRIPTION DRUG LABEL	1	16590-987	TABLET, FILM COATED	600 mg	ORAL	ANDA	22 sections