Lofexidine, an α2-receptor agonist for opioid detoxification

Annals of Pharmacotherapy

Volumn 44, Issue 2, 2010, Pages 343-351

  Gish, Emily C ^a   Miller, Jamie L ^a   Honey, Brooke L ^a   Johnson, Peter N ^a  

^a UNIVERSITY OF OKLAHOMA   (United States)

Author keywords

Lofexidine; Opioid withdrawal

Indexed keywords

ALCOHOL; BACLOFEN; BARBITURIC ACID DERIVATIVE; BENZODIAZEPINE; BUPRENORPHINE; CHLORDIAZEPOXIDE; CHLORPROMAZINE; CLONIDINE; DIAMORPHINE; DIAZEPAM; GLUCURONIDE; KETOPROFEN; LOFEXIDINE; METHADONE; MORPHINE; NALOXONE; NALTREXONE; OPIATE; OXAZEPAM; PLACEBO; SCOPOLAMINE; TRICYCLIC ANTIDEPRESSANT AGENT;

AGITATION; ANTIHYPERTENSIVE ACTIVITY; ASTHENIA; ATAXIA; CENTRAL NERVOUS SYSTEM DEPRESSION; CLINICAL ASSESSMENT; CLINICAL TRIAL; CONVULSION; DIAPHORESIS; DIZZINESS; DRUG ABSORPTION; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG DETOXIFICATION; DRUG DOSE REGIMEN; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG PROTEIN BINDING; EXOPHTHALMOS; FOLLOW UP; GERIATRIC PATIENT; HEROIN DEPENDENCE; HIGH RISK PATIENT; HOSPITAL PATIENT; HUMAN; HYPERTENSION; HYPOTENSION; INFORMATION RETRIEVAL; INGESTION; INSOMNIA; LENGTH OF STAY; LETHAL DOSE; LETHARGY; LIVER FUNCTION TEST; MEDLINE; MONOTHERAPY; MUCOSAL DRYNESS; NAUSEA AND VOMITING; NEUROTRANSMISSION; ORTHOSTATIC HYPOTENSION; PREGNANCY; PRIORITY JOURNAL; REVIEW; RISK BENEFIT ANALYSIS; SEDATION; SIDE EFFECT; TABLET; TACHYCARDIA; TREATMENT DURATION; UNITED KINGDOM; URINARY EXCRETION; WITHDRAWAL SYNDROME;

ADRENERGIC ALPHA-AGONISTS; ANIMALS; CLINICAL TRIALS AS TOPIC; CLONIDINE; HUMANS; NARCOTIC ANTAGONISTS; OPIOID-RELATED DISORDERS; RECEPTORS, ADRENERGIC, ALPHA-2; SUBSTANCE WITHDRAWAL SYNDROME;

EID: 76249118694     PISSN: 10600280     EISSN: None     Source Type: Journal    
DOI: 10.1345/aph.1M347     Document Type: Review

References (27)

1. Substance Abuse and Mental Health Services Administration, Office of Applied Studies. Results from the 2007 National Survey on Drug Use and Health: National Findings (NSDUH Series H-34, DHHS Publication No. SMA 08- 4343). Rockville, MD 2008. http://www.oas.samhsa.gov/NSDUH/2k7NSDUH/2k7results.cfm (accessed 2009 Jul 10).
2. Kosten TR, O'Connor PG. Management of drug and alcohol withdrawal. N Engl J Med 2003;348:1786-95.
3. Gowing L, Farrell M, Ali R, White J. Alpha-2 adrenergic agonists for the management opioid withdrawal (review). Cochrane Database Syst Rev 2009;(2):CD002024.
4. Marjamaki A, Luomala K, Ala-Uotila S, Scheinen M. Use of recombinant human alpha 2-adrenoreceptors to characterize subtype selectively of antagonist binding. Eur J Pharmacol 1993;246:219-26.
5. Kahn A, Mumford JP, Rogers A, Beckford H. Double-blind study of lofexidine and clonidine in the detoxification of opiate addicts in hospital. Drug Alcohol Depend 1997;44:57-61.
6. Bearn J, Gossop M, Strang J. Randomized double-blind comparison of lofexidine and methadone in the in-patient treatment of opiate withdrawal. Drug Alcohol Depend 1996;43:87-91.
7. Howells C, Allen S, Gupta J, Stillwell G, Marsden J, Farrell M. Prison based detoxification for opioid dependence: a randomized double blind controlled trial of lofexidine and methadone. Drug Alcohol Depend 2002;67:169-76.
8. Bearn J, Gossop M, Strang J. Accelerated lofexidine treatment regimen compared with conventional lofexidine and methadone treatment for in patient opiate detoxification. Drug Alcohol Depend 1998;50:227-32.
9. Raistrick D, West D, Finnegan O, Thistlethwaite G, Brearley R, Branbery J. A comparison of buprenorphine and lofexidine for community opiate detoxification: results from a randomized controlled trial. Addiction 2005;100:1860-7.
10. Lin SK, Strang J, Su LW, Tsai CJ, Hu WH. Double-blind randomized controlled trial of lofexidine versus clonidine in the treatment of heroin withdrawal. Drug Alcohol Depend 1997;48:127-33.
11. Carnwath T, Hardman J. Randomised double-blind comparison of lofexidine and clonidine in the out-patient treatment of opiate withdrawal. Drug Alcohol Depend 1998;50:251- 4.
12. Gerra G, Zaimovic A, Giusti F, et.al. Lofexidine versus clonidine in rapid opiate detoxification. J Subst Abuse Treat 2001;21:11-7.
13. Yu E, Miotto K, Akerele E, et al. A phase 3 placebo-controlled, double-blind, multi-site trial of the alpha-2-adrenergic agonist, lofexidine, for opioid withdrawal. Drug Alcohol Depend 2008;97:158-68.
14. Summary of product characteristics. BritLofex (lofexidine). Redhill, Surrey RH1 6YS, United Kingdom. Britannia Pharmaceuticals Limited, July 2006. http://www.lofexidine.co.uk/leaflets/bfl-spc-v3-07-2006.pdf (accessed 2009 Jun 16).
15. Cox S, Alcorn R. Lofexidine and opioid withdrawal. Lancet 1995;345: 1385-6.
16. Gold MS, Redmond DE Jr, Kleber HD. Clonidine blocks acute opiate-withdrawal symptoms. Lancet 1978;2:599-602.
17. Cook CCH, Scannell TD, Lipsedge MS. Another trial that failed. Lancet 1988;1:524-5.
18. Tsai TH, Beitman RE, Gibson JP, Larson EJ, Friehe H, Fontaine R. Acute, subacute and chronic toxicity/carcinogenicity of lofexidine. Arzneimittelforschung 1982;32:955-62.
19. Midgley I, Chasseaud LF, Taylor T, Darragh A. The absorption and excretion of 14C-lofexidine hydrochloride in man. Arzneimittelforschung 1982;32:972-5.
20. Midgely I, Fowkes AG, Chasseaud LF, Hawkins DR, Girkin R. Biotransformation of lofexidine in humans. Xenobiotica 1983;13:87-95.
21. Al-Ghananeem AM. Pharmacokinetics of lofexidine hydrochloride in healthy volunteers. J Pharm Sci 2009;98:319-26.
22. Yu E, Miotto K, Akerele E, et al. Clinical pharmacokinetics of lofexidine, the alpha2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis. Am J Drug Alcohol Abuse 2009;34:611-6.
23. Al-Ghananeem AM, Herman BH, Abbassi M, et al. Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients. Am J Drug Alcohol Abuse. Epub 27 July 2009.
24. Buntwal N, Bearn J, Gossop M, Strang J. Naltrexone and lofexidine combination treatment compared with conventional lofexidine treatment for in-patient opiate detoxification. Drug Alcohol Depend 2000;59:183-8.
25. McCambridge J, Gossop M, Beswick T, et al. In-patient detoxification procedures, treatment retention, and post-treatment opiate use: comparison of lofexidine + naloxone, lofexidine + placebo, and methadone. Drug Alcohol Depend 2007;88:91-5.
26. Schmittner J, Schroeder JR, Epstein DH, Preston KL. QT interval increased after single dose of lofexidine. BMJ 2004;329:1075.
27. Schmittner J, Schroeder JR, Epstein DH, Krantz MJ, Eid NC, Preston KL. Electrocardiographic effects of lofexidine and methadone coadministration: secondary findings from a safety study. Pharmacotherapy 2009; 29:459-502.