Lofexidine

Lofexidine Brand Name– LUCEMYRA

What is Lofexidine

Lofexidine is an oral, selective alpha 2-adrenergic receptor agonist indicated for the mitigation of withdrawal symptoms to facilitate abrupt discontinuation of opioids in adults.

Lofexidine represents the first non-opioid medication to receive FDA approval for opioid agonist withdrawal.

Central alpha-2 agonists are particularly beneficial in treating opiate withdrawal symptoms related to autonomic hyperactivity such as tachycardia, increased blood pressure, anxiety, chills, and sweating.

Because lofexidine is associated with QT prolongation, ECG monitoring is recommended in patient populations receiving the drug who are at increased risk for developing QT prolongation.

Due to the central alpha-2 agonist properties of lofexidine, hypotension, orthostasis, and syncope can occur. Patients receiving lofexidine on an outpatient basis should be instructed on recognizing and managing the symptoms of orthostasis.

Available data indicate that lofexidine is associated with less significant hypotension than clonidine, another central alpha-2 agonist used for the treatment of opioid agonist withdrawal.

Lofexidine is not a treatment for opioid use disorder (OUD), but can be used as part of a broader, long-term treatment plan for managing OUD.

Lofexidine was FDA-approved in May 2018.

Indications

  • opiate agonist withdrawal

For the treatment of opiate agonist withdrawal symptoms to facilitate abrupt opiate discontinuation

Side Effects

  1. bradycardia
  2. dizziness
  3. drowsiness
  4. hypotension
  5. insomnia
  6. orthostatic hypotension
  7. QT prolongation
  8. syncope
  9. tinnitus
  10. torsade de pointes
  11. withdrawal
  12. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • abrupt discontinuation
  • acute myocardial infarction
  • apheresis
  • AV block
  • bradycardia
  • breast-feeding
  • cardiomyopathy
  • celiac disease
  • cerebrovascular disease
  • children
  • coadministration with other CNS depressants
  • dehydration
  • dialysis
  • driving or operating machinery
  • electrolyte imbalance
  • ethanol ingestion
  • females
  • fever
  • geriatric
  • heart failure
  • hepatic disease
  • human immunodeficiency virus (HIV) infection
  • hyperparathyroidism
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypotension
  • hypothermia
  • hypothyroidism
  • infants
  • infertility
  • long QT syndrome
  • myocardial infarction
  • orthostatic hypotension
  • overdose
  • pheochromocytoma
  • poor metabolizers
  • pregnancy
  • QT prolongation
  • renal failure
  • renal impairment
  • rheumatoid arthritis
  • sickle cell disease
  • sleep deprivation
  • stroke
  • syncope
  • systemic lupus erythematosus (SLE)

Interactions

  • Acebutolol
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Pentazocine
  • Acetaminophen; Tramadol
  • Aclidinium; Formoterol
  • Albuterol
  • Albuterol; Ipratropium
  • Alfentanil
  • Alfuzosin
  • Alpha-blockers
  • Alprazolam
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amlodipine; Celecoxib
  • Amobarbital
  • Amoxapine
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Anxiolytics; Sedatives; and Hypnotics
  • Apomorphine
  • Arformoterol
  • Aripiprazole
  • Arsenic Trioxide
  • Artemether; Lumefantrine
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atenolol
  • Atenolol; Chlorthalidone
  • Atomoxetine
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  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
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  • Atropine; Diphenoxylate
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  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Dextromethorphan; Phenylephrine
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
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  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
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  • Dimenhydrinate
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  • Diphenhydramine; Hydrocodone; Phenylephrine
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  • Fluoxetine; Olanzapine
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  • Fluvoxamine
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  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guanabenz
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  • Halogenated Anesthetics
  • Haloperidol
  • Halothane
  • Histrelin
  • Homatropine; Hydrocodone
  • Hydralazine
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxychloroquine
  • Hydroxyzine
  • Ibuprofen; Oxycodone
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