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Lofexidine


Lofexidine
Systematic (IUPAC) name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Identifiers
CAS number	?
ATC code	N07BC04
PubChem	?
Chemical data
Formula	C₁₁H₁₂Cl₂N₂O
Mol. mass	259.131 g/mol
Pharmacokinetic data
Bioavailability	>90%
Protein binding	80–90%
Metabolism	Hepatic glucuronidation
Half life	11 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	?
Legal status	POM(UK)
Routes	Oral

Lofexidine is an alpha₂-adrenergic receptor agonist, can be used as a short acting (short half life) anti-hypertensive, but mostly used to help with relief from symptoms of heroin or opiate withdrawal in opiate dependency. Used primarily in the United Kingdom [1]. See also clonidine.

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v • d • e Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents (including alpha)	centrally acting/antiadrenergics (Clonidine, Guanfacine, Methyldopa, Moxonidine, Rescinnamine, Reserpine, Rilmenidine) • ganglion-blocking/nicotinic antagonist (Mecamylamine, Trimethaphan) • peripherally acting/antiadrenergics (Prazosin, Guanethidine, Indoramin, Doxazosin)
Vasodilators	Diazoxide • Hydralazine • Minoxidil • Nitroprusside • Phentolamine
Other antihypertensives	serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan)
Low ceiling diuretics	Thiazide (Bendroflumethiazide, Chlorothiazide, Hydrochlorothiazide) • Chlortalidone • Indapamide • Quinethazone • Mersalyl • Metolazone • Theobromine • Cicletanine
High ceiling diuretics	Loop diuretic (Bumetanide, Furosemide, Torasemide)
Potassium-sparing diuretics	ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)

v • d • e Drugs used in addictive disorders (N07B)
Nicotine dependence	Nicotine - Bupropion - Varenicline - Mecamylamine - Clonidine
Alcohol dependence	Disulfiram - Calcium carbimide - Acamprosate - Naltrexone - Nalmefene - Topiramate - Clonidine
Opioid dependence	Buprenorphine - Methadone - Levacetylmethadol - Heroin - Fentanyl - Dihydrocodeine - Dihydroetorphine - Clonidine - Lofexidine - Naltrexone - Ibogaine - 18-Methoxycoronaridine - Morphine - MS-Contin
Stimulant dependence	Dexamphetamine - Bupropion - Vanoxerine - Nocaine
Benzodiazepine dependence	Clonidine - Diazepam - Phenytoin - Phenobarbital
Cocaine dependence	Bupropion - Vanoxerine - Nocaine - Baclofen