- Molecular NameCetirizine
- SynonymCetirizina [Spanish]; Cetirizinum [Latin]; Cetrizine Hcl
- Weight388.895
- Drugbank_IDDB00341
- ACS_NO83881-51-0
- Show 3D model
- LogP (experiment)1.7
- LogP (predicted, AB/LogP v2.0)2.39
- pkaN/A
- LogD (pH=7, predicted)-0.26
- Solubility (experiment)0.101 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-2.17
- LogSw (predicted, AB/LogsW2.0)0.44
- Sw (mg/ml) (predicted, ACD/Labs)1.04
- No.of HBond Donors1
- No.of HBond Acceptors5
- No.of Rotatable Bonds8
- TPSA53.01
- StatusFDA approved
- AdministrationN/A
- PharmacologyA major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
- Absorption_value100.0
- Absorption (description)Cetirizine is rapidly absorbed after oral administration
- Caco_2N/A
- Bioavailability90.0
- Protein binding98.8
- Volume of distribution (VD)0.58 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCYP3A4. Undergoes metabolism in the liver, to a very limited extent by O-dealkylation. The metabolite produced has negligible antihistaminic activity.
- Half life9.42 h
- ExcretionCetirizine is primarily excreted in urine (70%) and in faeces (10%), as the unchanged drug. It is secreted in breast milk.
- Urinary Excretion70.9
- Clerance0.74 ml/min/kg
- ToxicityTwo cases of overdose have been reported: an adult took a 150 mg dose of cetirizine and was admitted to hospital with somnolence but no other clinical signs or blood chemistry/haematology. An 18-month-old child overdosed on 180 mg and became restless, irritable and drowsy. Multiple dose toxicity targets the liver and single dose the central nervous system.
- LD50 (rat)N/A
- LD50 (mouse)N/A