- Molecular NamePromethazine
- SynonymIsopromethazine; Lilly 1516; Proazaimine; Proazamine; Promazinamide; Prometazine; Promethazin; Promethazine Hcl; Promethiazine; Promezathine; Prothazin; Prothazine
- Weight284.427
- Drugbank_IDDB01069
- ACS_NO60-87-7
- Show 3D model
- LogP (experiment)4.81
- LogP (predicted, AB/LogP v2.0)4.59
- pka9.1
- LogD (pH=7, predicted)2.8
- Solubility (experiment)0.0156 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-2.92
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors0
- No.of HBond Acceptors2
- No.of Rotatable Bonds3
- TPSA31.78
- StatusFDA approved
- AdministrationOral, rectal, IV, IM, topical
- PharmacologyA first-generation H1 receptor antagonist used medically as an antihistamine and antiemetic. It can also have strong sedative effects and in some countries is prescribed for insomnia when benzodiazepines are contraindicated.
- Absorption_value88.0
- Absorption (description)On average, 88% of a promethazine dose is absorbed after oral administration; however, the absolute bioavailability is only 25% because of first-pass clearance.
- Caco_2N/A
- Bioavailability25.0
- Protein binding85.0
- Volume of distribution (VD)14 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic glucuronidation and sulfoxidation
- Half life10~15 h
- ExcretionRenal and biliary
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySymptoms of overdose include mild depression of the central nervous system and cardiovascular system to profound hypotension, respiratory depression, unconsciousness, and sudden death. Other reported reactions include hyperreflexia, hypertonia, ataxia, athetosis, and extensor-plantar reflexes (Babinski reflex). LD50=55mg/kg (I.V. in mice)
- LD50 (rat)N/A
- LD50 (mouse)LD50=55mg/kg (IV)