BritLofex
BritLofex - General Information
BritLofex is an alpha2-adrenergic receptor agonist. It can be used as a short acting anti-hypertensive, but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. It is approved in the United Kingdom, but is still undergoing clinical trials in the United States.
Pharmacology of BritLofex
BritLofex is an orally active imidazoline adrenergic alpha-2-receptor agonist; and is believed to have a high affinity for 2A receptor subtypes resulting in less anti-hypertensive activity than clonidine, a non-selective alpha-2-receptor agonist. Hypotension may occur in susceptible subjects, accompanied by a decrease in heart rate. Abrupt discontinuation of lofexidine has been, in some cases, associated with a transient increase in blood pressure to higher than pre-treatment levels.
Additional information about BritLofex
BritLofex Indication: Investigated for use/treatment in addictions and substance abuse.
Mechanism Of Action: BritLofex is an alpha2-adrenergic receptor agonist.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Lofexidine
Synonyms: Lofexidina [inn-spanish]; Lofexidinum [inn-latin]; 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline; 2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole; Lofexidine hydrochloride
Drug Category: Adrenergic alpha-Agonists; Antihypertensive Agents; Narcotic Antagonists
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Lofexidine: BritLofex;
Absorption: Lofexidine is extensively absorbed and achieves peak plasma concentration at
3 hours after administration of a single dose. Bioavailability is over 90% following oral administration.
Toxicity (Overdose): Lofexidine was tolerated at high dosage in singe dose toxicity studies in animals, the LD50 being >77 mg/kg. With repeat dosing in mice, rats and dogs symptoms related to the pharmacology of the drug (ataxia, sedation, tremor, unkempt appearance and exhaustion) appeared. Overdosage may cause hypotension, bradycardia and sedation.
Protein Binding: 80–90%
Biotransformation: Lofexidine undergoes extensive metabolism in the liver and excretion is mainly by the kidney.
Half Life: 11 hours
Dosage Forms of BritLofex: Tablet, film coated Oral
Chemical IUPAC Name: 2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Chemical Formula: C11H12Cl2N2O
Lofexidine on Wikipedia: https://en.wikipedia.org/wiki/Lofexidine
Organisms Affected: Humans and other mammals