- Molecular NameGuanfacine
- SynonymGuanfacina [INN-Spanish]; guanfacine; Guanfacine HCl; Guanfacine Hydrochloride; Guanfacinum [INN-Latin]; SPD 503
- Weight246.097
- Drugbank_IDDB01018
- ACS_NO29110-47-2
- Show 2D model
- LogP (experiment)1.33
- LogP (predicted, AB/LogP v2.0)1.41
- pkaN/A
- LogD (pH=7, predicted)1.4
- Solubility (experiment)1.892 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-2.98
- LogSw (predicted, AB/LogsW2.0)0.02
- Sw (mg/ml) (predicted, ACD/Labs)0.25
- No.of HBond Donors4
- No.of HBond Acceptors4
- No.of Rotatable Bonds3
- TPSA81.47
- StatusFDA approved
- Administrationoral, intravenous
- PharmacologyAn agonist of the α2A subtype of norepinephrine receptors.
- Absorption_value100.0
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability81.0
- Protein binding70.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmThe principal metabolite was the 3-hydroxy-derivative of guanfacine conjugated as either O-glucuronide or O-sulphate. The key-intermediate is an epoxide, the existence of which has been postulated based on product analysis. Indeed, the dihydrodiol and its glucuronide have both been isolated with, in addition, the oxidized pre-mercapturic acid derivative and the mercapturic acid derivatives
- Half life14.8~18.3 h
- Excretionrenal
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySymptoms of overdose include drowsiness, lethargy, bradycardia and hypotension.
- LD50 (rat)N/A
- LD50 (mouse)LD50=165mg/kg