Lofexidine: Difference between revisions

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{{Drugbox
{{DrugProjectFormSinglePage
|authorTag=
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|drugClass=Acetylcholine release inhibitor, Adrenergic receptor agonist
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* Dosing Information
 
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* Developed by: (Organisation)
 
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* Strength of Evidence: (Category A/B/C) (Link)
 
* Dosing Information/Recommendation
 
:* (Dosage)
 
=====Condition 2=====
 
* Developed by: (Organisation)
 
* Class of Recommendation: (Class) (Link)
 
* Strength of Evidence: (Category A/B/C) (Link)
 
* Dosing Information/Recommendation
 
:* (Dosage)
|offLabelPedNoGuideSupport======Condition 1=====
 
* Dosing Information
 
:* (Dosage)
 
=====Condition 2=====
 
* Dosing Information
 
:* (Dosage)
 
=====Condition 3=====
 
* Dosing Information
 
:* (Dosage)
|contraindications=CONTRAINDICATIONS
|warnings======Conidition 1=====
 
(Description)
 
=====Conidition 2=====
 
(Description)
 
=====Conidition 3=====
 
(Description)
|clinicalTrials=======Central Nervous System======
 
: (list/description of adverse reactions)
 
======Cardiovascular======
 
: (list/description of adverse reactions)
 
======Respiratory======
 
: (list/description of adverse reactions)
 
======Gastrointestinal======
 
: (list/description of adverse reactions)
 
======Hypersensitive Reactions======
 
: (list/description of adverse reactions)
 
======Miscellaneous======
 
: (list/description of adverse reactions)
 
=====Condition 2=====
 
======Central Nervous System======
 
: (list/description of adverse reactions)
 
======Cardiovascular======
 
: (list/description of adverse reactions)
 
======Respiratory======
 
: (list/description of adverse reactions)
 
======Gastrointestinal======
 
: (list/description of adverse reactions)
 
======Hypersensitive Reactions======
 
: (list/description of adverse reactions)
 
======Miscellaneous======
 
: (list/description of adverse reactions)
|postmarketing=(Description)
|drugInteractions=* Drug 1
* Drug 2
* Drug 3
* Drug 4
* Drug 5
 
=====Drug 1=====
 
(Description)
 
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(Description)
 
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(Description)
|useInPregnancyFDA=(Description)
|useInLaborDelivery=(Description)
|useInNursing=(Description)g
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|useInGeri=(Description)
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|useInRace=(Description)
|useInRenalImpair=(Description)
|useInHepaticImpair=(Description)
|useInReproPotential=(Description)
|useInImmunocomp=(Description)
|othersTitle=Others
|useInOthers=(Description)
|administration=(Oral/Intravenous/etc)
|monitoring======Condition 1=====
 
(Description regarding monitoring, from ''Warnings'' section)
 
=====Condition 2=====
 
(Description regarding monitoring, from ''Warnings'' section)
 
=====Condition 3=====
 
(Description regarding monitoring, from ''Warnings'' section)
 
|overdose====Acute Overdose===
 
====Signs and Symptoms====
 
(Description)
 
====Management====
 
(Description)
 
===Chronic Overdose===
 
====Signs and Symptoms====
 
(Description)
 
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|drugBox={{Drugbox2
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| StdInChI = 1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)
| StdInChI = 1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = KSMAGQUYOIHWFS-UHFFFAOYSA-N
| StdInChIKey = KSMAGQUYOIHWFS-UHFFFAOYSA-N}}
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|mechAction=(Description)
__Notoc__
|structure=(Description with picture)
{{SI}}
|PD=(Description)
{{CMG}}
|PK=(Description)
==Overview==
|nonClinToxic=(Description)
|clinicalStudies======Condition 1=====


'''Lofexidine''' (sold under the brand names: '''Britlofex''' and '''Kai Er Ding''') is an [[alpha-2A adrenergic receptor|α<sub>2A</sub>-adrenergic receptor]] agonist, historically used as an [[anti-hypertensive]], but more commonly used to alleviate the physical symptoms of [[heroin]] and other types of [[opioid]] withdrawal.<ref name = BNF/>
(Description)


==Indication==
=====Condition 2=====
In the [[United Kingdom]], the [[hydrochloride]] form, lofexidine HCl, has been licensed and sold since 1992 for opiate withdrawal relief in tablet form as Britlofex by Britannia Pharmaceuticals.<ref name = BNF/> Britlofex is only available by [[medical prescription|prescription]]. Lofexidine is also commonly used in conjunction with the opioid receptor antagonist [[naltrexone]] in rapid detoxification cases.  When these two drugs are paired, naltrexone is administered to induce an opioid-receptor blockade sending the subject into immediate withdrawal and accelerating the [[Drug detoxification|detoxification]] process, while lofexidine is given to relieve the symptoms associated with the withdrawal including chills, sweating, stomach cramps, muscle pain, and runny nose.


Lofexidine inhibits the release of [[norepinephrine]] in the central and peripheral nervous system, thereby reducing some of the withdrawal symptoms, but it has no documented effect on drug [[craving]] and [[endogenous opioid]] levels.<ref name = BNF>{{cite isbn|9780857110848|page=330}}</ref>
(Description)


==Use in opioid detoxification==
=====Condition 3=====
Lofexidine is not an opioid, whereas methadone is. Some opioid detox programs use methadone in decreasing amounts in their detox protocol, whereas other detox programs use lofexidine. The drugs are completely chemically unrelated, and their physiological effects are completely unrelated, although both are used as part of an opioid detoxification protocol. Whereas lofexidine cannot stop opioid withdrawal and merely eases some symptoms of withdrawal, methadone—being an opioid itself—will completely ameliorate all withdrawal symptoms in a sufficient dose. Indeed, one suggested use for lofexidine is to ease withdrawal symptoms of methadone dependence. While abstaining from opiates and taking lofexidine, effective detoxification can succeed in as little as 3 days<ref name=gerra>G. Gerra, et al., Lofexidine versus clonidine in rapid opiate detoxification, Journal of Substance Abuse TreatmentVolume 21, Issue 1, , July 2001, Pages 11-17.</ref>
, although the standard duration of detoxification using lofexidine is 10 days.<ref>J. Bearn, M. Gossop, J. Strang, Drug Alcohol Depend. 43, 87 (1996)</ref>  The {{LD50}} of lofexidine is 77&nbsp;mg/kg. 
Lofexidine is not currently available in the [[United States]].  Britannia Pharmaceuticals has licensed lofexidine to be sold by US World Meds for sale in North America,<ref>[http://www.britannia-pharm.co.uk/ Britannia Pharmaceuticals Limited<!-- Bot generated title -->]</ref> and clinical trials are currently underway to secure approval for sale in the United States by the [[Food and Drug Administration (United States)|U.S. Food and Drug Administration]] (FDA).<ref>[http://www.usworldmeds.com/lofexidine.htm US WorldMeds | +1 502 893 3235<!-- Bot generated title -->]</ref>
An additional benefit of lofexidine treatment is that it is given as part of an [[outpatient]], or ambulatory regimen, and can be completed without a hospital stay.  This reduces costs for both healthcare provider and patient, and keeps specialist hospital beds free for particularly difficult withdrawal cases.


==Structural similarities to clonidine==
(Description)
[[Image:LofexidineClonidine.png|thumb|350px|right|Structure of Lofexidine and Clonidine]]
|howSupplied=(Description)
Lofexidine is structurally analogous to [[clonidine]], another alpha2-adrenergic receptor agonist used for treatment of opioid withdrawal symptoms.  A comparison of the two structures is shown at right.  Both contain an [[imidazole]] ring and a 2,6-dichlorinated [[phenyl]] ring.  The differences in structure are shown in red, while the similarities are in black.  In addition to the structural differences, administration of lofexidine in heroin addicts has been shown to be more effective for a longer duration, with fewer withdrawal symptoms than clonidine even after one day.<ref name=gerra/> However, Clonidine is often preferred as it is substantially cheaper than Lofexidine when purchased with a private (non-NHS) prescription. This factor is exacerbated by the considerable number of and quantities of medications prescribed to alleviate the constellation of withdrawal signs and symptoms.
|storage=(Description)
Additionally, clonidine has been shown to significantly lower blood pressure.  Therefore, although similar to lofexidine, clonidine is most frequently prescribed to treat [[hypertension|high-blood pressure]].
|packLabel=
|fdaPatientInfo=(Patient Counseling Information)
|nlmPatientInfo=(Link to patient information page)
|lookAlike=* (Paired Confused Name 1a) — (Paired Confused Name 1b)
* (Paired Confused Name 2a) — (Paired Confused Name 2b)
* (Paired Confused Name 3a) — (Paired Confused Name 3b)
|brandNames=
|drugShortage=Drug Shortage


==Other clinical uses==
}}
The possibility of using lofexidine to treat alcohol addiction withdrawal symptoms has been investigated, and has not yet been shown to be an effective treatment.<ref>Keaney F, Strang J, Gossop M, Marshall EJ, Farrell M, Welch S, Hahn B, Gonzalez A. A double-blind randomized placebo-controlled trial of lofexidine in alcohol withdrawal: lofexidine is not a useful adjunct to chlordiazepoxide. Alcohol Alcohol (2001) 36:426–30.</ref>
 
==Adverse side effects==
*Drowsiness
*Dry mouth
*Dry Nose
*[[Hypotension]]
*Dizziness<ref>http://www.lofexidine.co.uk/leaflets/bfl-pil-v4_07-2006.pdf</ref>
 
==See also==
*[[Methadone]]
*[[Naltrexone]]
*[[Clonidine]]
 
==References==
{{reflist|2}}
 
==External links==
* [http://www.lofexidine.co.uk BritLofex Official Website]
 
 
{{Antihypertensives and diuretics}}
 
 
[[Category:Drug]]
[[Category:Antihypertensive agents]]
[[Category:Imidazolines]]
[[Category:Phenol ethers]]
[[Category:Organochlorides]]

Revision as of 19:02, 16 July 2018

Lofexidine
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

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Black Box Warning

Warning Title
See full prescribing information for complete Boxed Warning.
Condition Name: (Content)

Overview

Lofexidine is a Acetylcholine release inhibitor, Adrenergic receptor agonist that is FDA approved for the (type of indication of drug) of a list of indications, separated by commas.. There is a Black Box Warning for this drug as shown here. Common adverse reactions include a list of adverse reactions, separated by commas..

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition 1
  • Dosing Information
  • (Dosage)
Condition 2
  • Dosing Information
  • (Dosage)

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition 1
  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
  • Dosing Information/Recommendation
  • (Dosage)
Condition 2
  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
  • Dosing Information/Recommendation
  • (Dosage)

Non–Guideline-Supported Use

Condition 1
  • Dosing Information
  • (Dosage)
Condition 2
  • Dosing Information
  • (Dosage)
Condition 3
  • Dosing Information
  • (Dosage)

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition 1
  • Dosing Information
  • (Dosage)
Condition 2
  • Dosing Information
  • (Dosage)

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition 1
  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
  • Dosing Information/Recommendation
  • (Dosage)
Condition 2
  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
  • Dosing Information/Recommendation
  • (Dosage)

Non–Guideline-Supported Use

Condition 1
  • Dosing Information
  • (Dosage)
Condition 2
  • Dosing Information
  • (Dosage)
Condition 3
  • Dosing Information
  • (Dosage)

Contraindications

CONTRAINDICATIONS

Warnings

Warning Title
See full prescribing information for complete Boxed Warning.
Condition Name: (Content)
Conidition 1

(Description)

Conidition 2

(Description)

Conidition 3

(Description)

Adverse Reactions

Clinical Trials Experience

Central Nervous System
(list/description of adverse reactions)
Cardiovascular
(list/description of adverse reactions)
Respiratory
(list/description of adverse reactions)
Gastrointestinal
(list/description of adverse reactions)
Hypersensitive Reactions
(list/description of adverse reactions)
Miscellaneous
(list/description of adverse reactions)
Condition 2
Central Nervous System
(list/description of adverse reactions)
Cardiovascular
(list/description of adverse reactions)
Respiratory
(list/description of adverse reactions)
Gastrointestinal
(list/description of adverse reactions)
Hypersensitive Reactions
(list/description of adverse reactions)
Miscellaneous
(list/description of adverse reactions)

Postmarketing Experience

(Description)

Drug Interactions

  • Drug 1
  • Drug 2
  • Drug 3
  • Drug 4
  • Drug 5
Drug 1

(Description)

Drug 2

(Description)

Drug 3

(Description)

Drug 4

(Description)

Drug 5

(Description)

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): (Description)
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lofexidine in women who are pregnant.

Labor and Delivery

(Description)

Nursing Mothers

(Description)g

Pediatric Use

(Description)

Geriatic Use

(Description)

Gender

(Description)

Race

(Description)

Renal Impairment

(Description)

Hepatic Impairment

(Description)

Females of Reproductive Potential and Males

(Description)

Immunocompromised Patients

(Description)

Others

(Description)

Administration and Monitoring

Administration

(Oral/Intravenous/etc)

Monitoring

Condition 1

(Description regarding monitoring, from Warnings section)

Condition 2

(Description regarding monitoring, from Warnings section)

Condition 3

(Description regarding monitoring, from Warnings section)

IV Compatibility

There is limited information regarding the compatibility of Lofexidine and IV administrations.

Overdosage

Acute Overdose

Signs and Symptoms

(Description)

Management

(Description)

Chronic Overdose

Signs and Symptoms

(Description)

Management

(Description)

Pharmacology

Template:Px
1 : 1 mixture (racemate)Lofexidine
Systematic (IUPAC) name
(RS)-2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Identifiers
CAS number 31036-80-3
ATC code N07BC04
PubChem 30668
DrugBank DB04948
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 259.131 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability >90%
Protein binding 80–90%
Metabolism Hepatic glucuronidation
Half life 11 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

?

Legal status

Prescription Only (S4)(AU) POM(UK)

Routes Oral

Mechanism of Action

(Description)

Structure

(Description with picture)

Pharmacodynamics

(Description)

Pharmacokinetics

(Description)

Nonclinical Toxicology

(Description)

Clinical Studies

Condition 1

(Description)

Condition 2

(Description)

Condition 3

(Description)

How Supplied

(Description)

Storage

(Description)

Images

Drug Images

{{#ask: Page Name::Lofexidine |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Lofexidine |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

(Patient Counseling Information)

Precautions with Alcohol

Alcohol-Lofexidine interaction has not been established. Talk to your doctor regarding the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Lofexidine Brand Names in the drug label.

Look-Alike Drug Names

  • (Paired Confused Name 1a) — (Paired Confused Name 1b)
  • (Paired Confused Name 2a) — (Paired Confused Name 2b)
  • (Paired Confused Name 3a) — (Paired Confused Name 3b)

Drug Shortage Status

Drug Shortage

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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