tilidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
2663 51931-66-9

Description:

MoleculeDescription

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:

DoseUnitRoute
0.20 g O
0.20 g P

ADMET properties:

PropertyValueReference
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) 7.60 % 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.058 Moderate 0.65
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.793 Moderate 0.65
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 37.068 10^-6 cm/s Moderate 0.65
dh-clint Dog hepatocyte intrinsic clearance 49.317 uL/min/10^6 cells Moderate 0.65
dppb Dog plasma protein binding (% unbound) 59.270 % Moderate 0.65
fcs-ppb Fetal calf serum protein binding (% unbound) 50.860 % Moderate 0.65
herg hERG pIC50 4.624 pIC50 Moderate 0.65
hh-clint Human hepatocyte intrinsic clearance 18.113 uL/min/10^6 cells Moderate 0.65
hlm-clint Human liver microsomal intrinsic clearance 94.624 uL/min/mg protein Moderate 0.65
hppb Human plasma protein binding (% unbound) 55.450 % Moderate 0.65
kinase-safety-class ACVR2A,ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK7,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1 35
kinase-selectivity-class AXL,EIF2AK3,GRK2,PDK4 4
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.735 Moderate 0.65
mh-clint Mouse hepatocyte intrinsic clearance 90.365 Moderate 0.65
mppb Mouse plasma protein binding (% unbound) 50.630 Moderate 0.65
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.349 Moderate 0.65
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 64.850 % Moderate 0.65
rh-clint Rat hepatocyte intrinsic clearance 155.597 uL/min/10^6 cells Moderate 0.65
rh-fuinc Rat hepatocyte fraction unbound in incubation 83.040 % Moderate 0.65
rppb Rat plasma protein binding (% unbound) 59.660 % Moderate 0.65
solubility-dd Solubility at pH 7.4 in DMSO 654.636 uM Moderate 0.65

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1970 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Ecthyma 40.76 24.91 7 1666 407 90626367
Femoral neck fracture 38.05 24.91 12 1661 10221 90616553
Escherichia infection 36.63 24.91 13 1660 15882 90610892
Hypoaesthesia teeth 29.67 24.91 4 1669 44 90626730
Upper gastrointestinal haemorrhage 28.58 24.91 12 1661 22964 90603810
Electrocardiogram QT prolonged 25.11 24.91 16 1657 72440 90554334

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Brain oedema 230.17 33.38 65 1796 16262 42603212
Pulmonary oedema 151.50 33.38 64 1797 53208 42566266
Toxicity to various agents 128.52 33.38 94 1767 229042 42390432
Respiratory depression 68.23 33.38 27 1834 18841 42600633
Hepatitis E antibody positive 64.39 33.38 11 1850 256 42619218
Hepatitis E virus test positive 62.82 33.38 11 1850 297 42619177
Suspected transmission of an infectious agent via product 50.41 33.38 11 1850 943 42618531
Psychiatric decompensation 46.86 33.38 14 1847 4208 42615266
Poisoning 42.73 33.38 18 1843 14681 42604793
VACTERL syndrome 40.53 33.38 6 1855 53 42619421
Respiratory arrest 39.75 33.38 21 1840 28403 42591071
Prescription drug used without a prescription 38.92 33.38 11 1850 2719 42616755
Substance abuse 36.61 33.38 14 1847 8891 42610583
Neuromuscular blockade 35.90 33.38 7 1854 344 42619130
Hemivertebra 35.06 33.38 6 1855 141 42619333
Kidney congestion 33.81 33.38 7 1854 466 42619008
General physical health deterioration 33.62 33.38 37 1824 151209 42468265

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Brain oedema 216.82 27.99 64 2832 31034 110555369
Pulmonary oedema 133.87 27.99 61 2835 100598 110485805
Toxicity to various agents 112.87 27.99 96 2800 480459 110105944
Respiratory depression 81.93 27.99 31 2865 31970 110554433
Hepatitis E antibody positive 69.92 27.99 11 2885 258 110586145
Hepatitis E virus test positive 68.43 27.99 11 2885 297 110586106
Suspected transmission of an infectious agent via product 57.55 27.99 12 2884 1388 110585015
Psychiatric decompensation 49.60 27.99 14 2882 5751 110580652
Poisoning 42.92 27.99 19 2877 29086 110557317
General physical health deterioration 41.12 27.99 53 2843 425242 110161161
Substance abuse 38.98 27.99 14 2882 12449 110573954
Kidney congestion 36.60 27.99 7 2889 522 110585881
Hydrocholecystis 35.75 27.99 7 2889 590 110585813
Respiratory arrest 35.64 27.99 21 2875 58278 110528125
Neuromuscular blockade 34.22 27.99 7 2889 737 110585666
Product prescribing error 32.72 27.99 19 2877 51312 110535091
Prescription drug used without a prescription 32.57 27.99 10 2886 5486 110580917
Social anxiety disorder 32.40 27.99 7 2889 959 110585444
Ecthyma 31.89 27.99 7 2889 1032 110585371
Hepatomegaly 31.64 27.99 14 2882 21400 110565003
Lung hyperinflation 31.43 27.99 8 2888 2221 110584182
Mental impairment 30.89 27.99 14 2882 22625 110563778
Brain hypoxia 30.42 27.99 7 2889 1275 110585128
Encephalomalacia 29.32 27.99 7 2889 1495 110584908
Suicide attempt 28.99 27.99 23 2873 103371 110483032
Pancreatic enzymes increased 28.34 27.99 7 2889 1722 110584681
Hypoaesthesia teeth 28.02 27.99 4 2892 47 110586356

FDA Adverse Event Reporting System (Pediatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Reflexes abnormal 20.53 13.11 3 6 15 113929

Pharmacologic Action:

SourceCodeDescription
ATC N02AX01 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Other opioids
ATC N02AX51 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Other opioids
MeSH PA D009294 Narcotics
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35482 opioid analgesic
CHEBI has role CHEBI:50266 prodrug

Related Drugs by ATC class:

N02AX Other opioids 6 drugs
dezocinemeptazinolnaloxoneoliceridinetapentadoltramadol

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

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.95 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST EC50 5.10 WOMBAT-PK SCIENTIFIC LITERATURE

External reference:

IDSource
N0000166666 NUI
D06147 KEGG_DRUG
255733-17-6 SECONDARY_CAS_RN
C0040219 UMLSCUI
CHEBI:77823 CHEBI
CHEMBL2220384 ChEMBL_ID
DB13787 DRUGBANK_ID
CHEMBL2218854 ChEMBL_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

Pharmaceutical products:

None