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lofexidine

Structure via PubChem · Public domain (PubChem)

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lofexidine

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Also known as 2-(alpha-(2,6-dichlorophenoxy)ethyl)2-imidazoline

Lofexidine, sold as a generic by Indoco, MSN, Novitium, Ani Pharma, Regcon, etc; and under the brand name Lucemyra; is a medication historically used to treat high blood pressure; today, it is more commonly used to help with the physical symptoms of opioid withdrawal. It is taken by mouth. It is an α2A-adrenergic receptor agonist. It was initially approved for use by the Food and Drug Administration in the United States in 2018, considering it to be a first-in-class medication. Subsequent generic approvals by the FDA started August 21, 2024 with Indoco Remedies with Competitive Generic Therapy

Chemical data

Formula
C11H12Cl2N2O
Molecular weight
259.13 g/mol
IUPAC name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
SMILES
CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl
InChIKey
KSMAGQUYOIHWFS-UHFFFAOYSA-N
XLogP
2.6
Polar surface area
33.6 Ų
H-bond donors
1
H-bond acceptors
2
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
2018
Admin. routes
oral
Indications
cocaine dependence, drug dependence, heroin dependence, opioid dependence

via ChEMBL · EBI

Wikidata facts

Mass
258.032668
Has use
medication
Show 6 more facts
chemical formula
C₁₁H₁₂Cl₂N₂O
World Health Organisation international non-proprietary name
lofexidine
canonical SMILES
CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl
defined daily dose
1.4
subject has role
opioid antagonist
Commons category
Lofexidine
Sources (3)

via Wikidata · CC0

~9 min read

Encyclopedic overview

17 sections
Contents
  • Medical uses
  • Opioid withdrawal
  • Other clinical uses
  • Special populations
  • Adverse effects
  • Overdose
  • Interactions
  • QT prolongation
  • CNS depression
  • Hypotension
  • Pharmacology
  • Pharmacokinetics
  • Chemistry
  • Comparison to clonidine
  • Society and culture
  • See also
  • References

Lofexidine, sold as a generic by Indoco, MSN, Novitium, Ani Pharma, Regcon, etc; and under the brand name Lucemyra; is a medication historically used to treat high blood pressure; today, it is more commonly used to help with the physical symptoms of opioid withdrawal. It is taken by mouth. It is an α2A-adrenergic receptor agonist. It was initially approved for use by the Food and Drug Administration in the United States in 2018, considering it to be a first-in-class medication. Subsequent generic approvals by the FDA started August 21, 2024 with Indoco Remedies with Competitive Generic Therapy (CGT) designation (ANDA #218613), which provided Indoco with a 180-day exclusivity period from the date of the product’s first commercial launch in the United States. Following this exclusivity period multiple generics were approved by other manufacturers: MSN February 24, 2025 (ANDA #218699), NOVITIUM PHARMA October 22, 2025 (ANDA #219917), Regcon Holdings (ANDA #218613). The FDA approval of multiple generic sources of Lofexidine has resulted in the widespread availability of FDA approved cheaper alternative to the branded medication with significant cost savings to patients. The normal out-of-pocket price of Lucemyra is $1,144.96 per 36, 0.18mg tablets. As of the 12th of December 2025 at one representative pharmacy, a branded Lucemyra 3 day supply costs $756, whereas the generic versions costs $142, an 81% discount. Due to widespread inter-generic competition the price/unit of generic lofexidine itself is under steady downward pressure and this is an example of the rapid erosion of the branded drug (Lucemyra) purchase and value in the face of generic competition; alongside the continued decreases in generic costs.

==Medical uses== In the United States, lofexidine is approved for the "mitigation of withdrawal symptoms to facilitate abrupt discontinuation of opioids in adults," for a treatment duration of 14 days. In the United Kingdom, lofexidine is 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 detoxification process, while lofexidine is given to relieve the symptoms associated with the withdrawal including chills, sweating, stomach cramps, muscle pain, and runny nose.

Excerpted from Wikipedia’s “lofexidine” article, available under the CC BY-SA 4.0 licence.

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