Lofexidine

Lofexidine is a prescription medication used for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults.

• Lofexidine is available under the following different brand names: Lucemyra

Common side effects of Lofexidine include:

• dizziness on standing
• slow heart rate
• low blood pressure (hypotension)
• dizziness
• drowsiness
• sleepiness
• dry mouth

Serious side effects of Lofexidine include:

• low blood pressure (hypotension)
• slow heart rate (bradycardia)
• lightheadedness 
• feeling fainting at rest or when standing up
• dizziness

Rare side effects of Lofexidine include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 0.18 mg

Opioid withdrawal

Adult dosage

• Starting dose: Three 0.18-mg tablets (0.54 mg) orally four times a day (5 to 6 hours between doses) during the period of peak withdrawal symptoms (generally the first 5 to 7 days after the last opioid use)
• Not to exceed a total daily dose of 2.88 mg (16 tablets)
• No single dose should exceed 0.72 mg (4 tablets)
• Treatment may be continued for up to 14 days with dosing guided by symptoms
• Dose should be reduced, held, or discontinued for individuals who demonstrate a greater sensitivity
• Lower doses may be appropriate as opioid withdrawal symptoms wane
• Discontinue by gradually reducing the dose over a 2-to 4-day period to mitigate lofexidine withdrawal symptoms (e.g., reducing by 1 tablet per dose every 1 to 2 days)

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Lofexidine has severe interactions with no other drugs
• Lofexidine has serious interactions with at least 136 other drugs
• Lofexidine has moderate interactions with at least 222 other drugs
• Lofexidine has minor interactions with the following drugs:
  • eucalyptus
  • sage

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Lofexidine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Lofexidine?”

Cautions

• May cause hypotension, bradycardia, and syncope; monitor vital signs before dosing and symptoms related to bradycardia and orthostasis; avoid use in patients with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, chronic renal failure, and in patients with marked bradycardia
• Increased risk of QT prolongation; monitor ECG in congestive heart failure, bradyarrhythmias, hepatic impairment, renal impairment, or patients taking medications that lead to QT prolongation (e.g., methadone); correct any electrolyte abnormalities (e.g., hypokalemia, hypomagnesemia) before initiating treatment
• Patients administering therapy in an outpatient setting should be capable of and instructed on self-monitoring for hypotension, orthostasis, bradycardia, and associated symptoms; instruct outpatients to withhold doses when experiencing symptoms of hypotension or bradycardia and to contact health care providers for guidance on how to adjust dosing; if clinically significant or symptomatic hypotension and/or bradycardia occur, next dose should be reduced in amount, delayed, or skipped
• Inform patients that therapy may cause hypotension and that patients moving from a supine to an upright position may be at increased risk for hypotension and orthostatic effects
• Instruct patients to stay hydrated, on how to recognize symptoms of low blood pressure, and how to reduce the risk of serious consequences should hypotension occur (e.g., sit or lie down, carefully rise from a sitting or lying position)
• Advise patients in an outpatient setting that, until they learn how they respond to therapy, they should be careful or avoid doing activities such as driving or operating heavy machinery
• Increased risk of opioid overdose after opioid discontinuation
• Not a treatment for opioid use disorder
  • Patients who complete opioid discontinuation are likely to have a reduced tolerance to opioids and are at increased risk of fatal overdose should they resume opioid use
  • Use lofexidine in patients with opioid use disorder only in conjunction with a comprehensive management program for the treatment of opioid use disorder and inform patients and caregivers of this increased risk of overdose
• Sudden discontinuation of treatment
  • Stopping abruptly can cause a marked rise in blood pressure; symptoms including diarrhea, insomnia, anxiety, chills, hyperhidrosis, and extremity pain have been observed with discontinuation
  • Instruct patients not to discontinue therapy without consulting their healthcare provider
  • When discontinuing therapy with tablets, gradually reduce the dose 
  • Manage symptoms related to discontinuation by administering the previous dose and subsequent taper
• Drug interaction overview
  • Avoid use in combination with medications that decrease pulse or blood pressure to avoid the risk of excessive bradycardia and hypotension
  • Methadone and lofexidine both prolong the QT interval; monitor ECG when used concomitantly
  • Coadministration with naltrexone may reduce the efficacy of oral naltrexone
• Coadministration with CYP2D6 inhibitors
  • Concomitant use of paroxetine resulted in increased plasma levels of lofexidine; monitor for symptoms of orthostasis and bradycardia with concomitant use of a CYP2D6 inhibitor
• Coadministration with CNS depressants
  • Lofexidine potentiates CNS depressive effects of benzodiazepines and is expected to potentiate CNS depressive effects of alcohol, barbiturates, and other sedating drugs
  • Advise patients to inform healthcare providers of other medications they are taking, including alcohol
  • In an outpatient setting, advise patients to be careful or to avoid doing activities such as driving or operating heavy machinery

Pregnancy and Lactation

• There are no available data regarding use in pregnant women
• Lactation
  • No information is available regarding the presence of lofexidine or its metabolites in human milk, the effects on the breastfed infant, or milk production
  • Caution if administered to breastfeeding women
  • The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child or from the underlying maternal condition