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Lofexidine

产品号 DB04948 公司名称 DrugBank
CAS号 31036-80-3 公司网站 http://www.ualberta.ca/
分子式 C11H12Cl2N2O 电 话 (780) 492-3111
分子量 259.13178 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 4402

产品价格信息

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产品别名

标题
Lofexidine
IUPAC标准名
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
IUPAC传统名
lofexidine
商标名
BritLofex
别名
Lofexidina [inn-spanish]
Lofexidine hydrochloride
2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline
Lofexidinum [inn-latin]
2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole
lofexidine

产品登记号

PubChem CID 30668
CAS号 31036-80-3
PubChem SID 46508453

产品性质

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved; investigational
Description Lofexidine 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.
Indication Investigated for use/treatment in addictions and substance abuse.
Pharmacology Lofexidine 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. It selectively stimulates receptors in the brain that monitor catecholamine levels in the blood. These receptors close a negative feedback loop that begins with descending sympathetic nerves from the brain that control the production of catecholamines (epinephrine, also known as adrenaline, and norepinephrine) in the adrenal medulla. By fooling the brain into believing that catecholamine levels are higher than they really are, lofexidine causes the brain to reduce its signals to the adrenal medulla, which in turn lowers catecholamine production and blood levels. The result is a lowered heart rate and blood pressure. This central action is responsible for the suppression of opiate withdrawal symptoms.
Toxicity 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.

Affected Organisms
Humans and other mammals
Biotransformation Lofexidine undergoes extensive metabolism in the liver and excretion is mainly by the kidney.
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.
Half Life 11 hours
Protein Binding 80 to 90%
References
Walsh SL, Strain EC, Bigelow GE: Evaluation of the effects of lofexidine and clonidine on naloxone-precipitated withdrawal in opioid-dependent humans. Addiction. 2003 Apr;98(4):427-39. [Pubmed]
Manufacturer Website [Link]
External Links
Wikipedia

参考文献

  • Walsh SL, Strain EC, Bigelow GE: Evaluation of the effects of lofexidine and clonidine on naloxone-precipitated withdrawal in opioid-dependent humans. Addiction. 2003 Apr;98(4):427-39. Pubmed
  • Manufacturer Website Link