IUPAC_name = 2- [1-(2,6-dichlorophenoxy)ethyl] -4,5-dihydro-1"H"-imidazole

width = 181
CAS_number = 31036-80-3
ATC_prefix = N07
ATC_suffix = BC04
PubChem = 30667
DrugBank =
C = 11 | H = 12 | Cl = 2 | N = 2 | O = 1
molecular_weight = 259.131 g/mol
bioavailability = >90%
protein_bound = 80–90%
metabolism = Hepatic glucuronidation
elimination_half-life = 11 hours
excretion = Renal
pregnancy_AU =
pregnancy_US =
pregnancy_category =
legal_AU =
legal_CA =
legal_UK = POM
legal_US =
legal_status =
routes_of_administration = Oral

Lofexidine is an 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.


In the United Kingdom, the hydrochloride form, lofexidine HCl, has been licensed and sold since 1992 for opiate withdrawal relief in tablet form as BritLofex by Britannia Pharmacuetical. BritLofex is only available by prescription. Lofexidine is also commonly used in conjunction with the opioid receptor agonist naltrexone in rapid detoxification cases. When these two drugs are paired, naltrexone is administered to relieve craving of the opioid, while lofexidine is given to relive physical withdrawal symptoms including chills, sweating, stomach cramps, muscle pain, and runny nose.As opiate withdrawal relief, lofexidine works to restore natural levels of norepinephrine and endorphins to pre-opiate addiction levels [ [http://www.lofexidine.co.uk/how.htm BritLofex tablets for opiate detox ] ] .

Clinical Similarities to Methadone

While clinically equivalent to methadone, lofexidine is not an opiate, as methadone is, and therefore does not have the addictive and dependent qualities of methadone. Fact|date=June 2008 Indeed, one suggested use for lofexidine is to ease withdrawal symptoms of methadone dependence. Additionally, a significantly smaller dose is required, as the maximum recommended dose of BritLofex is 2.4 mg/day (0.2 mg/tablet) while a minimum effective methadone administration is about 40 mg/dose, and can increase to ~120 mg/dose. While abstaining from opiates and taking lofexidine, effective detoxification can succeed in as little as 3 days G. Gerra, et al, Lofexidine versus clonidine in rapid opiate detoxification, Journal of Substance Abuse TreatmentVolume 21, Issue 1, , July 2001, Pages 11-17.] , although the standard duration of detoxification using lofexidine is 10 days [ J. Bearn, M. Gossop, J. Strang, Drug Alcohol Depend. 43, 87 (1996)] . The LD50 of lofexidine is 77 mg/kg. Lofexidine is not currently available in the United States. Britannia Pharmaceuticals has licensed lofexidine to be sold by US World Meds for sale in North America [ [http://www.britannia-pharm.co.uk/ Britannia Pharmaceuticals Limited ] ] , and clinical trials are currently underway to secure approval for sale in the United States by the FDA [ [http://www.usworldmeds.com/lofexidine.htm US WorldMeds | +1 502 893 3235 ] ] . An additional benefit of lofexidine treatment is that it is given as part of an outpatient, or ambulatory regimen, and can be completed without a hospital stay. This reduces costs for both healthcare provider and patient, and keeps specialist hospital beds free for particularly difficult withdrawal cases.

tructural Similarities to Clonidine

Lofexidine is structurally analogous to clonidine, another alpha2-adrenergic receptor agonist used for treatment of opioid withdrawal symptoms. A comparison of the two structures is shown at right. Both contain an imidazole ring and a 2,6-dichlorinated phenyl ring. The differences in structure are shown in red, while the similarities are in black. In addition to the structural differences, administration of lofexidine in heroin addicts has been shown to be more effective for a longer duration, with fewer withdrawal symptoms than clonidine even after one day. However, Clonidine is often preferred as it is substantially cheaper than Lofexidine when purchased with a private (non-NHS) prescription. This factor is exacerbated by the considerable number of and quantities of medications prescribed to alleviate the constellation of withdrawal signs and symptoms. Additionally, clonidine has been shown to significantly lower blood pressure. Therefore, although similar to lofexidine, clonidine is most frequently prescribed to treat high-blood pressure.

Other Clinical Uses

The possibility of using lofexidine to treat alcohol addiction withdrawal symptoms has been investigated, and has not yet been shown to be an effective treatment [ Keaney F, Strang J, Gossop M, Marshall EJ, Farrell M, Welch S, Hahn B, Gonzalez A. A double-blind randomized placebo-controlled trial of lofexidine in alcohol withdrawal: lofexidine is not a useful adjunct to chlordiazepoxide. Alcohol Alcohol (2001) 36:426–30.] .

Additionally, the possibility of lofexidine to treat ADHD symptoms in children has been investigated Niederhofer H, Staffen W, Mair A: A placebo-controlled study of lofexidine in the treatment of children with tic disorders and attention deficit hyperactivity disorder. J Psychopharmacol 2003, 17:113-119.] . Although this subject has only a small body of research, when a small dose of lofexidine is given (0.4 mg, 3x daily), ADHD severity significantly decreased. Similar studies have shown reduction of tics in children with the small dosage.

Adverse Side Effects [http://www.lofexidine.co.uk/leaflets/bfl-pil-v4_07-2006.pdf]

*Dry mouth
*Dry Nose


ee also


External links

* [http://www.lofexidine.co.uk BritLofex Official Website]

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