- Molecular NameAcebutolol
- SynonymAcebutolol HCL; Acebutolol Hydrochloride; Acebutololo; Acetobutolol; dl-Acebutolol
- Weight336.432
- Drugbank_IDDB01193
- ACS_NO37517-30-9
- Show 2D model
- LogP (experiment)1.77
- LogP (predicted, AB/LogP v2.0)1.5
- pka9.4
- LogD (pH=7, predicted)-0.9
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-0.05
- LogSw (predicted, AB/LogsW2.0)4.61
- Sw (mg/ml) (predicted, ACD/Labs)1.3
- No.of HBond Donors3
- No.of HBond Acceptors6
- No.of Rotatable Bonds10
- TPSA87.66
- StatusFDA approved
- Administrationoral, iv
- PharmacologyA beta blocker for the treatment of hypertension and arrhythmias.
- Absorption_value85.0
- Absorption (description)N/A
- Caco_2-5.83
- Bioavailability37.0
- Protein binding26.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)Plasma:whole blood ratio, about 0.8.
- MetabollsmAcarbose is metabolized exclusively within the gastrointestinal tract, principally by intestinal bacteria. A fraction of these metabolites (approximately 34% of the dose) was absorbed and subsequently excreted in the urine. At least 13 metabolites have been separated chromato-graphically from urine specimens. The major metabolites have been identified as 4-methylpyrogallol derivatives (i. e., sulfate, methyl, and glucuronide conjugates). One metabolite (formed by cleavage of a glucose molecule from acarbose) also has alpha-glucosidase inhibitory activity. but also by digestive enzymes. A fraction of these metabolites (approximately 34% of the dose) was from urine specimens. This metabolite, together with the parent compound, recovered from the urine, accounts for less than 2% of the total administered dose.
- Half life3-4 hours (parent drug) 8-13 hours (active metabolite)
- ExcretionAfter an oral dose, about 20 to 40% of the dose is excreted in the urine in 24 h, about 9 to 12% of the dose as unchanged drug and about 12 to 24% as diacetalol. Up to about 60% of the dose is eliminated in the faeces as unchanged drug and diacetalol. After an intravenous dose, relatively more is excreted in the urine than in the faeces, and the proportion of unchanged drug in the urine is greater than after an oral dose.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityA fatal case of self-poisoning with acebutolol was reported with a blood concentration of 34.7 μg/mL. [A. Tracqui et al.,J. Anal. Toxicol.,1992, 16(6), 398–400].
- LD50 (rat)N/A
- LD50 (mouse)N/A