Lofexidine 是一种选择性α2 受体激动剂,常用于缓解海洛因和其他阿片类戒断的躯体症状。
产品描述
Lofexidine is a selective α2-receptor agonist, Lofexidine reduces narcotic withdrawal symptoms.
体内活性
Lofexidine significantly decreased SOWS scores compared to placebo and demonstrated better retention rates in participants undergoing opioid withdrawal. Lofexidine potentially offers a useful non-opioid alternative to treat opioid withdrawal symptoms[1].
动物实验
8-day, randomized, double-blind, placebo-controlled, parallel-group study in 264 patients dependent on short-acting opioids evaluated the efficacy of lofexidine hydrochloride in reducing withdrawal symptoms in patients undergoing opioid withdrawal.?The primary efficacy measures were SOWS-Gossop on Day 3 and time-to-dropout.?Secondary endpoints included the proportion of participants who were completers;?area under the 5-day SOWS-Gossop - time curve (i.e., AUC1-5), and daily mean SOWS-Gossop, OOWS-Handelsman, MCGI (subject and rater), and VAS-E scores.?Participants received lofexidine HCl 3.2mg daily in four divided doses or matching placebo on Days 1-5, followed by 2days of placebo[1].
Cas No.
31036-80-3
分子式
C11H12Cl2N2O
分子量
259.13
别名
Lofexidine
储存和溶解度
DMSO:62.5 mg/mL (241.19 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years