- Molecular NameBretylium
- SynonymBretylate; Bretylium p-toluenesulfonate; Bretylium tolsylate; Bretylium tosylate; Bretylum
- Weight243.168
- Drugbank_IDDB01158
- ACS_NO59-41-6
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)-1.39
- pkaN/A
- LogD (pH=7, predicted)-1.39
- Solubility (experiment)Soluble
- LogS (predicted, ACD/Labs)(ph=7)-0.12
- LogSw (predicted, AB/LogsW2.0)78.49
- Sw (mg/ml) (predicted, ACD/Labs)182.54
- No.of HBond Donors0
- No.of HBond Acceptors1
- No.of Rotatable Bonds3
- TPSA0.0
- StatusFDA approved
- AdministrationIV, IM
- PharmacologyAn antiarrhythmic agent. It blocks the release of noradrenaline from the peripheral sympathetic nervous system.
- Absorption_value23.0
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability23.0
- Protein binding4.0
- Volume of distribution (VD)8 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmNone
- Half life7~10 h, increased in renal impairment
- ExcretionRenal, Excretion rate of the compound administered intramuscularly in urine during first 24 hour; 72- 81%
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityOral, mouse: LD50 = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Bretylium serum levels were 8000 ng/mL.
- LD50 (rat)N/A
- LD50 (mouse)N/A