Products
Lofexidine was approved in the United States in 2018 in film-coated tablet form (Lucemyra). In the United Kingdom, the agent was approved for the treatment of opioid withdrawal back in the early 1990s (UK: BritLofex).
Structure and properties
Lofexidine (C11H12Cl2N2O, Mr = 259.1 g/mol) is present in the drug as lofexidine hydrochloride, a white crystalline powder that is highly soluble in water. It is structurally related to clonidine and it is an imidazoline derivative.
Effects
Lofexidine (ATC N07BC04) is a central agonist at alpha2-adrenoceptors. This reduces the release of norepinephrine and reduces sympathetic tone. The half-life is in the range of 12 hours.
Indications
For the attenuation of withdrawal symptoms during abrupt discontinuation of opioids in adults.
Dosage
According to the prescribing information. Tablets are taken four times daily, 5 to 6 hours apart. Discontinuation should be gradual. Therapy may be continued for up to two weeks.
Contraindications
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effects include orthostatic hypotension, bradycardia, dizziness, somnolence, drowsiness, and dry mouth. Lofexidine may prolong the QT interval.
