II. Indications

  1. Opioid Withdrawal in adults age >=18 years

III. Mechanism

  1. Released in 2018
  2. Central Alpha-2 Adrenergic Agonist
    1. Similar to Clonidine
    2. Lofexidine is more specific to Alpha-2a receptor (less hypotensive effect)
    3. Decreases Norepinephrine release
    4. Decreases sympathetic tone
  3. Decreases symptoms associated with Opioid Withdrawal
    1. Diarrhea
    2. Vomiting
    3. Abdominal Cramping
    4. Myalgias and muscle spasms
    5. Malaise
    6. Anxiety
    7. Palpitations
    8. Insomnia

IV. Dosing

  1. Start
    1. Three 0.18 mg tablets four times daily
    2. Titrate dose to symptoms
  2. Maximum
    1. Daily Maximum: 2.88 mg/day
    2. Dose Maximum: 0.72 mg (four 0.18 mg tablets)
    3. Duration up to 7-14 days
  3. Decreased dose indications
    1. Hepatic insufficiency
    2. Renal Insufficiency

V. Adverse Effects

  1. Somnolence (42%)
  2. Dizziness (29%)
  3. Hypotension (18%)
  4. Bradycardia (3%)
  5. Rebound Hypertension
    1. Titrate off over 2-4 days
  6. Serious adverse effects (2.3%)
    1. Syncope
    2. QT Prolongation

VI. Cost

  1. Daily cost: $330/day (compare with Clonidine is at most, $1/day)

VII. References

  1. (2018) Presc Lett 25(9): 54
  2. Johns and Lovecchio (2018) Crit Dec Emerg Med 32(10): 24
  3. Bryce (2019) Am Fam Physician 99(6): 393-4 [PubMed]
  4. Doughty (2019) Ann Pharmacother 53(7):746-53 +PMID:30724094 [PubMed]

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Ontology: lofexidine (C0065152)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C025655
SnomedCT 349934008, 395989000
English 1H-imidazole, 2-(1-(2,6-dichlorophenoxy)ethyl)-4,5-dihydro-, 2-(alpha-(2,6-dichlorophenoxy)ethyl) delta-2-imidazoline, lofexidine, LOFEXIDINE, lofexidine [Chemical/Ingredient], 2-(1-(2,6-Dichlorophenoxy)Ethyl)-2-Imidazoline, 1H-Imidazole, 2-(1-(2,6-Dichlorophenoxy)Ethyl)-4,5-Dihydro-, Lofexidine, Lofexidine (product), Lofexidine (substance)
Spanish lofexidina (producto), lofexidina (sustancia), lofexidina