- Molecular NameKetorolac
- SynonymKetoralac; Ketorolac Tromethamine; Ketorolaco [Spanish]; Ketorolacum [Latin]
- Weight255.273
- Drugbank_IDDB00465
- ACS_NO74103-06-3
- Show 2D model
- LogP (experiment)2.32
- LogP (predicted, AB/LogP v2.0)2.66
- pka3.49
- LogD (pH=7, predicted)-0.52
- Solubility (experiment)0.025 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-0.45
- LogSw (predicted, AB/LogsW2.0)0.47
- Sw (mg/ml) (predicted, ACD/Labs)0.24
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds3
- TPSA59.3
- StatusFDA approved
- AdministrationN/A
- PharmacologyA non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives, often used as an analgesic, antipyretic (fever reducer), and anti-inflammatory.
- Absorption_value95.0
- Absorption (description)Ketorolac trometamol is more hydrophilic than ketorolac and is rapidly absorbed after both oral and intramuscular administration. Peak plasma concentrations are reached between 30 and 60 min.
- Caco_2N/A
- Bioavailability100.0
- Protein binding99.2
- Volume of distribution (VD)0.21 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt is metabolised via conjugation and hydroxylation but does not undergo a significant degree of presystemic metabolism. The major metabolites are the acyl glucuronide and p-hydroxyketorolac which represent 77% and 12%, respectively, of an oral dose as urinary excretion products. However, the glucuronic acid conjugates are not detected in plasma. p-Hydroxyketorolac has about 20% of the anti-inflammatory activity and 1% of the analgesic activity of ketorolac. A small amount is distributed in breast milk. It does not readily penetrate the blood–brain barrier but crosses the placenta.
- Half life2.5 hours for the S-enantiomer compared with 5 hours for the R-enantiomer
- ExcretionRenal:91.4% (mean), Biliary:6.1% (mean)
- Urinary Excretion5~10
- Clerance0.50 ml/min/kg
- ToxicityAdverse effects include nausea, rash oedema, headache and hypertension, occurring at ketorolac plasma concentration above 5 mg/L.
- LD50 (rat)LD50=189 mg/kg
- LD50 (mouse)N/A