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

Stem definition	Drug id	CAS RN
	2663	51931-66-9

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tilidine hydrochloride hemihydrate
tilidine
tilidate
tilidine hydrochloride
tilidine HCl

An opioid analgesic used similarly to MORPHINE in the control of moderate to severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1097)

Molecular weight: 273.38
Formula: C17H23NO2
CLOGP: 3.76
LIPINSKI: 0
HAC: 3
HDO: 0
TPSA: 29.54
ALOGS: -3.18
ROTB: 5

Drug dosage:

Dose	Unit	Route
0.20	g	O
0.20	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	9.19 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	4 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	16 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.21 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1970	YEAR INTRODUCED

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
Ecthyma	43.41	31.68	7	1110	291	63487614
Escherichia infection	40.07	31.68	13	1104	12741	63475164

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
Brain oedema	148.53	41.01	43	1258	13778	34941852
Toxicity to various agents	95.75	41.01	70	1231	200292	34755338
Pulmonary oedema	93.43	41.01	42	1259	47487	34908143
Hepatitis E antibody positive	66.16	41.01	11	1290	256	34955374
Hepatitis E virus test positive	64.92	41.01	11	1290	288	34955342
Suspected transmission of an infectious agent via product	53.47	41.01	11	1290	837	34954793
Prescription drug used without a prescription	43.26	41.01	11	1290	2143	34953487
VACTERL syndrome	41.81	41.01	6	1295	50	34955580

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
Brain oedema	133.06	31.83	42	2064	25221	79717061
Pulmonary oedema	73.53	31.83	39	2067	88215	79654067
Hepatitis E antibody positive	69.87	31.83	11	2095	257	79742025
Toxicity to various agents	68.81	31.83	69	2037	421471	79320811
Hepatitis E virus test positive	68.74	31.83	11	2095	286	79741996
Suspected transmission of an infectious agent via product	59.45	31.83	12	2094	1174	79741108
General physical health deterioration	54.13	31.83	50	2056	275188	79467094
Respiratory depression	40.50	31.83	18	2088	27612	79714670
Hydrocholecystis	36.49	31.83	7	2099	526	79741756
Social anxiety disorder	36.01	31.83	7	2099	564	79741718
Prescription drug used without a prescription	35.42	31.83	10	2096	4075	79738207
Product prescribing error	35.00	31.83	19	2087	44794	79697488
Ecthyma	34.05	31.83	7	2099	749	79741533

FDA Adverse Event Reporting System (Pediatric)

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
Reflexes abnormal	19.82	12.64	3	6	15	89768

Pharmacologic Action:

Source	Code	Description
ATC	N02AX01	NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids
ATC	N02AX51	NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D009294	Narcotics
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
CHEBI has role	CHEBI:35482	narcotic analgesic
CHEBI has role	CHEBI:50266	Prodrugs

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

Disease	Relation	SNOMED_ID	DOID
Pain	indication	22253000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.95	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
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	EC50	5.10		WOMBAT-PK	SCIENTIFIC LITERATURE

External reference:

ID	Source
N0000166666	NUI
D06147	KEGG_DRUG
255733-17-6	SECONDARY_CAS_RN
C0040219	UMLSCUI
CHEBI:77823	CHEBI
CHEMBL2220384	ChEMBL_ID
DB13787	DRUGBANK_ID
D013993	MESH_DESCRIPTOR_UI
30131	PUBCHEM_CID
2510	INN_ID
27107-79-5	SECONDARY_CAS_RN
GY33N31E9Y	UNII
10597	RXNORM
006735	NDDF
006736	NDDF
373562008	SNOMEDCT_US
96185000	SNOMEDCT_US
96186004	SNOMEDCT_US
CHEMBL2218854	ChEMBL_ID

Pharmaceutical products:

None