• Molecular NameAlprenolol
  • SynonymAlfeprol [Russian]; Alpheprol; Alprenololum [INN-Latin]
  • Weight249.354
  • Drugbank_IDDB00866
  • ACS_NO13655-52-2
  • Show 3D model
  • LogP (experiment)3.144
  • LogP (predicted, AB/LogP v2.0)2.61
  • pka9.5
  • LogD (pH=7, predicted)0.21
  • Solubility (experiment)0.547 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)0.4
  • LogSw (predicted, AB/LogsW2.0)6.43
  • Sw (mg/ml) (predicted, ACD/Labs)2.43
  • No.of HBond Donors2
  • No.of HBond Acceptors3
  • No.of Rotatable Bonds8
  • TPSA41.49
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA non-selective beta blocker as well as 5-HT1A receptor antagonist, used in the treatment of angina pectoris.
  • Absorption_value93.0
  • Absorption (description)Alprenolol is rapidly and almost completely absorbed after oral administration but undergoes extensive first-pass metabolism.
  • Caco_2-4.62
  • Bioavailability8.0
  • Protein binding85.0
  • Volume of distribution (VD)3 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)Plasma:whole blood ratio, about 1.6.
  • MetabollsmN/A
  • Half life2-3 h (4-OH-alprenolol)
  • ExcretionAbout 90% of an oral dose is excreted in the urine in 24 h with about 40% as the glucuronide conjugate of the active metabolite 4-hydroxyalprenolol, 5% as free 4-hydroxyalprenolol, 20 to 30% as alprenolol glucuronide, 1% as desisopropylalprenolol, and less than 1% as unchanged drug; unknown metabolites account for the remainder of the dose.
  • Urinary ExcretionN/A
  • ClerancePlasma clearance, about 15 mL/min/kg.
  • ToxicityIn 2 fatalities due to the ingestion of about 4 g and 20 g, respectively, the following postmortem tissue-alprenolol concentrations were reported: blood 40 and 43 mg/L, liver 72 and 91 μg/g. [S. J. Dickson et al.,J. Anal. Toxicol.,1978, 2, 242–244].
  • LD50 (rat)N/A
  • LD50 (mouse)N/A