Drug intelligence / Profile preview

lofexidine + methadone

Development stage
Unknown
Lead developer
US WorldMeds
Modality
Small Molecules
Administration
Oral
01

Overview

**lofexidine + methadone** is a combination therapy used in opioid dependence treatment, especially for opioid detoxification and maintenance. Methadone is an opioid agonist used for maintenance therapy in opioid dependence, while lofexidine is an alpha-2 adrenergic agonist indicated primarily for managing opioid withdrawal symptoms. Both drugs can cause cardiovascular effects, such as bradycardia and hypotension, and each prolongs the QT interval, which can potentially increase cardiac arrhythmia risk[1][2][3]. Clinical monitoring (particularly ECG) is recommended when both drugs are co-administered due to the additive risk for QTc prolongation and other cardiac conduction changes[1][2][3]. The combination is sometimes used to assist in transitioning patients from methadone maintenance to other therapies or for relapse prevention during methadone maintenance[1]. Lofexidine does not alter methadone pharmacokinetics, but the combination can result in clinically significant cardiovascular effects, particularly in susceptible individuals[1][2][3].

02

Targets

HTR7 (5-hydroxytryptamine receptor 7)HTR1D (5-hydroxytryptamine receptor 1D)ADRA1A (α1A)HTR2C (5-hydroxytryptamine 2C receptor)ADRA2A (α2A)MOR (Mu opioid receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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