- Molecular NameDirithromycin
- SynonymNA
- Weight835.086
- Drugbank_IDDB00954
- ACS_NO62013-04-1
- Show 3D model
- LogP (experiment)2.833
- LogP (predicted, AB/LogP v2.0)3.86
- pkaN/A
- LogD (pH=7, predicted)1.02
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)0.08
- LogSw (predicted, AB/LogsW2.0)0.82
- Sw (mg/ml) (predicted, ACD/Labs)101.39
- No.of HBond Donors5
- No.of HBond Acceptors16
- No.of Rotatable Bonds12
- TPSA196.33
- StatusFDA approved
- AdministrationN/A
- PharmacologyA macrolide glycopeptide antibiotic.
- Absorption_valueN/A
- Absorption (description)Oral dirithromycin is rapidly absorbed, with an absolute bioavailability of approximately 10%. Dietary fat has little or no effect on the bioavailability of dirithromycin.
- Caco_2N/A
- Bioavailability10.0
- Protein binding19.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmDirithromycin is converted by nonenzymatic hydrolysis during absorption to the active compound, erythromycylamine. Sixty to 90% of a dose is hydrolyzed to erythromycylamine within 35 minutes after dosing, and conversion is nearly complete after 1.5 hours. Erythromycylamine undergoes little or no hepatic biotransformation. No other metabolites of dirithromycin have been detected in the serum.
- Half lifeThe mean plasma half-life of erythromycylamine was estimated to be about 8 h (2 to 36 h), with a mean urinary terminal elimination half-life of about 44 h (16 to 65 h) in patients with normal renal function.
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityThe toxic symptoms following an overdose of a macrolide antibiotic may include nausea, vomiting, epigastric distress, and diarrhea.
- LD50 (rat)N/A
- LD50 (mouse)N/A