- Molecular NameLofexidine
- Synonym2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole; 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline; Lofexidina [inn-spanish]; lofexidine; Lofexidine hydrochloride; Lofexidinum [inn-latin]
- Weight259.136
- Drugbank_IDDB04948
- ACS_NO31036-80-3
- Show 2D model
- LogP (experiment)3.23
- LogP (predicted, AB/LogP v2.0)2.91
- pkaN/A
- LogD (pH=7, predicted)0.61
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.22
- LogSw (predicted, AB/LogsW2.0)0.14
- Sw (mg/ml) (predicted, ACD/Labs)0.03
- No.of HBond Donors1
- No.of HBond Acceptors3
- No.of Rotatable Bonds3
- TPSA33.62
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn alpha2-adrenergic receptor agonist, historically used as a short-acting anti-hypertensive, but more commonly used to alleviate physical symptoms of heroin and opiate withdrawal.
- Absorption_valueN/A
- Absorption (description)Lofexidine is rapidly absorbed after administration
- Caco_2N/A
- Bioavailability90.0
- Protein binding40.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmExtensively biotransformed and excreted mainly in urine (87%) and faeces (5%). The principal metabolite is 2,6-dichlorophenol, and minor metabolites have been detected including glucuronic acid conjugates.
- Half lifeLofexidine undergoes biphasic elimination with half-lives 1.3 to 3.7 h and 9.0 to 18.3 h; also reported as 11 h.
- ExcretionRenal excretion is rapid and is the most important route of elimination. 73 to 94.4% (mean 85%) of the drug is excreted in urine and 0.4 to 4.2% (mean 1.5%) in faeces. Peak plasma concentration occurs 2 to 5 h after administration. The rate of bioavailability is rapid and subject dependent.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityOverdosage may cause hypotension, bradycardia and sedation.
- LD50 (rat)N/A
- LD50 (mouse)N/A