- Molecular NameLorcainide
- SynonymNA
- Weight370.924
- Drugbank_IDN/A
- ACS_NO59729-31-6
- Show 2D model
- LogP (experiment)4.85
- LogP (predicted, AB/LogP v2.0)4.73
- pkaN/A
- LogD (pH=7, predicted)2.08
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.21
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.03
- No.of HBond Donors0
- No.of HBond Acceptors3
- No.of Rotatable Bonds5
- TPSA23.55
- StatusN/A
- AdministrationN/A
- PharmacologyA class 1c antiarrhythmic agent.
- Absorption_valueN/A
- Absorption (description)Well absorbed after oral administration
- Caco_2N/A
- Bioavailability30.0
- Protein binding85.0
- Volume of distribution (VD)8 L/kg but there is considerable intersubject variation.
- Blood/Plasma Partitioning ratio (D_blood)Plasma : whole blood ratio, about 1.3.
- MetabollsmExtensive, saturable, first-pass metabolism. The principal active metabolite, norlorcainide, is found in high concentrations in plasma during chronic oral dosing. Other major metabolites include a 4-hydroxyphenyl derivative and a 4-hydroxy-3-methoxyphenyl compound.
- Half lifelorcainide 3~15 h (mean 8), increased in subjects with cirrhosis of the liver and during chronic oral dosing; norlorcainide 20~40 h (mean 27)
- ExcretionAfter intravenous administration, less than 2% of a dose is excreted in the urine as unchanged drug in 48 h; a total of about 60% of a dose is excreted in the urine as metabolites in 4 days and 35% is eliminated in the faeces.
- Urinary ExcretionN/A
- Clerance10~25 ml/min/kg
- ToxicityA 15-year-old girl died 3 h after ingesting at least 2.5 g of lorcainide; the lorcainide concentration in a blood sample taken 30 to 60 min post ingestion was 1.82 mg/L [J. Evers and U. Buttner-Belz,J. Toxicol. Clin. Toxicol.,1995, 33, 157–159].
- LD50 (rat)N/A
- LD50 (mouse)N/A