Lofexidine

Lofexidine
Clinical data
Trade namesBritlofex, Lucemyra, others
AHFS/Drugs.comMonograph
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability>90%
Protein binding80–90%
MetabolismLiver (glucuronidation)
Elimination half-life11 hours
ExcretionKidney
Identifiers
IUPAC name
  • (RS)-2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC11H12Cl2N2O
Molar mass259.13 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
SMILES
  • Clc2c(OC(C/1=N/CCN\1)C)c(Cl)ccc2
InChI
  • InChI=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) Y
  • Key:KSMAGQUYOIHWFS-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

Lofexidine, sold under the brand name Lucemyra among others,[1] 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.[2] It is taken by mouth.[3] It is an α2A-adrenergic receptor agonist.[3] It was approved for use by the Food and Drug Administration in the United States in 2018,[3] considering it to be a first-in-class medication.[4]

  1. ^ Cite error: The named reference FDA Approval was invoked but never defined (see the help page).
  2. ^ Cite error: The named reference BNF was invoked but never defined (see the help page).
  3. ^ a b c "FDA approves the first non-opioid treatment for management of opioid withdrawal symptoms in adults". U.S. Food and Drug Administration (FDA) (Press release). Archived from the original on September 2, 2019. Retrieved 18 May 2018.
  4. ^ New Drug Therapy Approvals 2018. U.S. Food and Drug Administration (FDA) (Report). January 2019. Archived from the original (PDF) on August 26, 2019. Retrieved 16 September 2020.