Lofexidine

Generic Name: Lofexidine

Brand Names: Lucemyra

Drug Type: Small Molecule

Chemical Formula: C_₁₁H_₁₂Cl_₂N_₂O

CAS Number: 31036-80-3

Unique Ingredient Identifier: UI82K0T627

Background: Lofexidine is a non-opioid centrally acting alpha2-adrenergic receptor agonist that was first approved for the treatment of opioid withdrawal in the United Kingdom in 1992. It was first studied for use as an antihypertensive in 1980, but its researched was stopped as it was found less effective for the treatment of hypertension than clonidine. Lofexidine was then repurposed for the treatment of opioid withdrawal, as it was seen to be more economical and have fewer side effects than clonidine. Lofexidine was developed by US Woldmeds LLC and it was approved by the FDA on May 16, 2018.

Indication: Lofexidine is indicated for mitigation of symptoms associated with acute withdrawal from opioids and for facilitation of the completion of opioid discontinuation treatment. It is the first non-opioid medication for the symptomatic management of opioid discontinuation.

Opioid withdrawal syndrome is a debilitating manifestation of opioid dependence. This condition is extremely unpleasant lasting several days with some of the main features being abdominal pain, nausea, diarrhea, mydriasis, lacrimation, and piloerection. These symptoms are often observed after abrupt reductions in the opioid dose and can be resolved by re-administration of the opioid.

Associated Conditions: Abrupt opioid withdrawal

Clinical Trials

Lofexidine for Inpatient Opiate Detox

Phase 3

Completed

Conditions: Opiate Addiction

Interventions: Drug: Placebo
Drug: Lofexidine

First Posted Date: 2005-10-10

Last Posted Date: 2009-03-20

Lead Sponsor: US Department of Veterans Affairs

Target Recruit Count: 264

Registration Number: NCT00235729

Locations: 🇺🇸
CNS, Cerritos, Cerritos, California, United States
🇺🇸
CNS Psychiatric Institute of Washington, Washington, District of Columbia, United States
🇺🇸
Atlanta Center for Medical Research, Atlanta, Georgia, United States

and more 13 locations

Effectiveness of Naltrexone and Lofexidine in Treating Detoxified Heroin Addicts - 1

Phase 1

Completed

Conditions: Heroin Dependence

First Posted Date: 2005-09-22

Last Posted Date: 2017-01-12

Lead Sponsor: National Institute on Drug Abuse (NIDA)

Registration Number: NCT00218530

Locations: 🇺🇸
Substance Abuse Treatment Unit, New Haven, Connecticut, United States

Effectiveness of Lofexidine to Prevent Stress-Related Opiate Relapse During Naltrexone Treatment - 1

Phase 2

Completed

Conditions: Opioid-Related Disorders

Interventions: Drug: Placebo
Drug: Lofexidine

First Posted Date: 2005-09-02

Last Posted Date: 2015-07-30

Lead Sponsor: Yale University

Target Recruit Count: 86

Registration Number: NCT00142909

Locations: 🇺🇸
Yale University, Psychiatry, New Haven, Connecticut, United States

Lofexidine for Opiate Withdrawal - 1

Phase 3

Completed

Conditions: Opioid-Related Disorders

First Posted Date: 2002-04-08

Last Posted Date: 2017-01-12

Lead Sponsor: National Institute on Drug Abuse (NIDA)

Target Recruit Count: 66

Registration Number: NCT00032942

Locations: 🇺🇸
Philadelphia Veterans Medical Center, Philadelphia, Pennsylvania, United States
🇺🇸
UCLA Medical Center, Los Angeles, California, United States
🇺🇸
Columbia University, New York, New York, United States