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Lofexidine hydrochloride

Lofexidine hydrochloride structure

CAS No:
21498-08-8
Formula:
C11H12Cl2N2O.ClH
Chemical Name:
Lofexidine hydrochloride
Synonyms:
1H-Imidazole,2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-,hydrochloride (1:1);2-Imidazoline,2-[1-(2,6-dichlorophenoxy)ethyl]-,monohydrochloride;1H-Imidazole,2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-,monohydrochloride;Lofexidine hydrochloride;Britlofex;Loxacor;Lofetensin;MDL 14042;Baq 168;2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole hydrochloride;73372-54-0
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Lofexidine hydrochloride is an α2A-adrenergic receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.

Lofexidine hydrochloride Basic Attributes

Molecular Weight：

295.59

Exact Mass：

294.009338

NSC Number：

759654

DSSTox ID：

DTXSID0020781

HScode：

2933290090

Characteristics

PSA：

33.6

XLogP3：

3.32880

Appearance：

white to beige

Melting Point：

221-223 °C

Boiling Point：

421.5ºC at 760 mmHg

Flash Point：

208.7ºC

Water Solubility：

H2O: soluble 20mg/mL, clear

Storage Conditions：

-20°C Freezer

Vapor Pressure：

6.35E-07mmHg at 25°C

Toxicity：

LD50 in mice, rats, dogs (mg/kg): between 74-147 orally (all species); between 8-18 i.v. (all species) (Tsai)

Safety Information

Hazard category：

6.1

Transport codes：

UN 2811 6.1 / PGIII

wgk germany：

hazard class code：

safety instructions：

Marks：

Precautionary statement(s)：

P301 + P310

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 39 companies from 1 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. (See all compounds classified as Adrenergic alpha-2 Receptor Agonists.)|Agents inhibiting the effect of narcotics on the central nervous system. (See all compounds classified as Narcotic Antagonists.)

MeSH Entry Terms：

2-(alpha-(2,6-dichlorophenoxy)ethyl) delta-2-imidazoline

Lofexidine hydrochloride Use and Manufacturing

Uses

Lofexidine is an α2-adrenergic receptor agonist (Kd = 7.6 nM for rat cerebral cortex membranes) that has transient antihypertensive effects. It is used in managing opioid withdrawal symptoms during detoxification from heroin and methadone.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:295.6
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:3
Exact Mass:294.009346
Monoisotopic Mass:294.009346
Topological Polar Surface Area:33.6
Heavy Atom Count:17
Complexity:263
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is an imidazoline derivative, which selectively stimulates central α-2 receptors, reduces peripheral sympathetic nerve activity, inhibits norepinephrine release, relaxes vascular smooth muscle, and produces a blood pressure lowering effect; it can counteract the hyperactivity of norepinephrine neurons during opioid withdrawal, and reduce the intensity and duration of heroin withdrawal syndrome; it is non-addictive.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Lofexidine Hydrochloride Tablets
Ingredients	Lofexidine hydrochloride.
Indication	Because this product is a α2 receptor agonist, it cannot be used simultaneously with α2 receptor blockers to avoid pharmacological antagonism.
Specifications	0.2mg
Manufacturer	Hunan Mingrui Pharmaceutical Co., Ltd.

Lofexidine hydrochloride
Manufacturer	Hunan Mingrui Pharmaceutical Co., Ltd.

Lofexidine hydrochloride

See More Related Drugs

Registered Holders

MSN LABORATORIES PRIVATE LTD

United States
Active
PROCOS S.P.A.

Italy
Active
Sichuan Chenlong Pharmaceutical Co., Ltd.

China
Active

See More Registered Holders

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