Lucemyra: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on Feb 13, 2024.

1. How it works

• Lucemyra is a brand (trade) name for lofexidine which may be used to help ease opioid withdrawal symptoms when opioids need to be stopped suddenly.
• Lucemyra works by binding to alpha-2 receptors in the brain which reduces the release of norepinephrine and decreases sympathetic tone (this means it calms down an overactive nervous system). This allows muscles to relax, blood vessels to dilate, and blood pressure to decrease.
• Lucemyra belongs to the group of medicines known as centrally-acting antiadrenergic agents. It may also be called an alpha-2 adrenergic agonist.

2. Upsides

• May be used to mitigate withdrawal symptoms to allow the abrupt discontinuation of opioids in adults.
• Usually started at a higher dose (0.54mg 4 times a day) during peak withdrawal symptoms which are typically the first 5 to 7 days following the last dose of the opioid.
• May be administered for up to 14 days.
• Dosing is guided by symptoms and tolerance to Lucemyra (reduce dosage if side effects are intolerable).
• May be taken with or without food.
• There are no contraindications listed by the manufacturer to Lucemyra; however, it should be used with caution in people with certain comorbid conditions (see downsides below).
• Helps to keep the nervous system from becoming overactive, which typically occurs during opioid withdrawal. Can help relieve symptoms such as feeling sick, stomach cramps, muscle spasms, twitching, feeling cold, a pounding heart, muscle tension, aches and pains, yawning, runny eyes, and sleep problems.
• Taken orally (by mouth).

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Sleeplessness, low blood pressure, a slow heart rate, dizziness, drowsiness, and a dry mouth are the most common side effects reported.
• Dizziness or drowsiness that may affect your ability to drive or operate machinery, particularly during the first few days of dosing, when going from lying down to a standing position, during hot weather, or after activity. Do not drive or operate machinery until you know how Lucemyra affects you.
• Fainting and tinnitus have also been reported at higher dosages.
• Do not administer more than 0.72mg (4 tablets of 0.18mg) per dose and no more than 2.88mg (16 tablets) in a single 24-hour period. Do not administer more frequently than every 5 to 6 hours.
• Can cause withdrawal symptoms so needs to be withdrawn slowly over a 2 to 4-day period (reduce by 1 tablet per dose every 1 to 2 days). High blood pressure on withdrawal has been reported, this usually peaks on day 2. Other withdrawal symptoms include diarrhea, insomnia, anxiety, chills, and increased sweating.
• Some individuals are sensitive to the side effects of Lucemyra and a lower dosage may be needed.
• The dosage needs to be reduced in people with liver disease. The maximum dosage per day in people with mild hepatic impairment is 2.16 mg/day; moderate hepatic impairment is 1.44 mg/day; and severe hepatic impairment is 0.72 mg/day.
• The dosage needs to be reduced in those with kidney disease. the maximum dosage in those with moderate renal impairment (30-90 mL/min/1.73m²) is 1.44 mg/day and in those with severe renal impairment, ESRD, or on dialysis (< 30 mL/min/1.73m²) is 0.72 mg/day.
• May not be suitable for people with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, chronic renal failure, congenital QT syndrome, or marked bradycardia.
• Prolongs the QT interval. Perform ECG monitoring in people at risk of QT prolongation, such as those with bradyarrhythmias, congestive heart failure, liver or kidney disease, or taking other medicines that prolong the QT interval. Correct any electrolyte abnormalities first (such as low potassium or low magnesium levels) before administering Lucemyra.
• Females are more likely to experience a serious cardiovascular adverse event while taking Lucemyra. 31% of females required a dose-hold or discontinuation of Lucemyra 2.88 mg/day as a result of adverse events compared to 18% of males.
• May interact with many drugs, including those that also lower blood pressure, prolong the QT interval, or cause sedation.
• The absorption and effects of Lucemyra may be increased in people who are poor CYP2D6 metabolizers. Monitor for side effects.
• Not for use in children under the age of 18 years.
• Safety in pregnancy has not been established but animal studies show an increased risk of fetal resorption, reduced birth weights, and miscarriages. There is no information about using Lucemyra during breastfeeding but caution should be administered. May affect female fertility, but the effect on male fertility is unknown.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

• Lucemyra may be used to ease the symptoms caused by abruptly stopping opioids in people who are addicted to them. It is given four times a day for up to 14 days but must be slowly discontinued. The main side effects are sleeplessness, low blood pressure, a slow heartbeat, and dizziness.

5. Tips

• Lucemyra is usually given four times a day. The dosage you are prescribed depends on your kidney or liver function and other comorbid conditions or medications.
• Withdrawing from opioids is not easy. Lucemyra will help relieve some of the symptoms associated with opioid withdrawal such as feeling sick, aches and pains, sweating, and a pounding heart but should be used in addition to a comprehensive treatment program for opioid use disorder. Make sure you follow all aspects of this program.
• Lucemyra can drop your blood pressure and slow your heartbeat which may make you feel dizzy or pass out. If you are feeling like you might faint all the time, either skip, reduce, or delay the next dose of Lucemryra and talk to your doctor. Be careful when moving from lying down to sitting up or standing position. Keep hydrated. If you feel yourself beginning to faint or feeling dizzy or lightheaded while on Lucemyra, lie down until the feeling passes.
• Do not drink alcohol or drive or operate machinery while you are taking Lucemyra.
• Do not allow yourself to become dehydrated or overheated while taking Lucemyra because it may make the side effects worse.
• Lucemyra does not treat opioid use disorder, it just helps ease the symptoms of withdrawal. Be aware that you have a reduced tolerance to opioids once you have gone through opioid discontinuation and are at an increased risk for fatal overdose if you resume opioid use.
• Do not stop taking Lucemyra suddenly. This may cause a marked increase in blood pressure and symptoms may include diarrhea, insomnia, anxiety, chills, increased sweating, and pain in your fingers and toes. Lucemyra needs to be slowly tapered off and you should talk to your doctor about this.
• Lucemyra may interact with several other medications that also lower blood pressure, cause sedation, or slow your heart rate. Tell your doctor about all the medications you take before starting Lucemyra.
• Tell your doctor if you are breastfeeding or pregnant because Lucemyra may not be suitable for you.

6. Response and effectiveness

• Well absorbed. Blood levels of Lucemyra reach a peak within three to five hours after a single dose.
• Accumulation of Lucemyra occurs with repeat dosing.
• 41% of Lucemyra 2.16mg and 40% of Lucemyra 2.16mg patients completed 7 days of treatment, compared to only 28% of patients given a placebo (an inactive medication).
• The Short Opiate Withdrawal Scale (SOWS)-Gossop is a 10-item questionnaire developed to evaluate opioid withdrawal symptom severity, and measures symptoms such as anxiety, yawning, and perspiration. People taking Lucemyra 2.16 mg/day or 2.88 mg/day reported a significantly lower score in the SOWS-Gossop than people taking a placebo.

7. Interactions

Medicines that interact with Lucemyra may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with doxazosin. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Lucemyra interacts with over 519 medications, most of these interactions are considered moderate or major. Common medications that may interact with Lucemyra include:

• amisulpride
• antiarrhythmic medications such as disopyramide
• antibiotics such as norfloxacin
• antidepressants such as escitalopram
• antinausea medications such as dolasetron
• antipsychotics such as clozapine, haloperidol, or ziprasidone
• any medication that causes sedation, such as sedating antihistamines or barbiturates
• benzodiazepines such as clonazepam, diazepam, or lorazepam
• bisacodyl
• bromocriptine
• bupropion
• buspirone
• cannabis
• erectile dysfunction medications (eg, alprostadil, sildenafil, tadalafil, or vardenafil)
• HIV medications such as efavirenz or saquinavir
• hydroxychloroquine
• lithium
• methadone (also prolongs the QT interval)
• mifepristone
• monamine oxidase inhibitor antidepressants, such as phenelzine or tranylcypromine
• multiple sclerosis medications such as fingolimod or siponimod
• other heart medications that may also lower blood pressure, such as atenolol, carvedilol, clonidine, diltiazem, labetalol, metoprolol, nadolol, propranolol, sotalol, trandolapril, or verapamil
• paroxetine (inhibits CYP2D6 and may cause a 28% increase in the absorption of Lucemyra)
• papaverine
• quinidine
• QT-prolonging medicines such as buprenorphine, amiodarone, or cisapride
• sedating antihistamines such as diphenhydramine or azelastine
• tamoxifen
• targeted treatments such as ceritinib or cabozantinib
• valerian
• valproic acid.

Avoid drinking alcohol while taking Lucemyra.

May reduce the efficacy of oral naltrexone if used together. Administer naltrexone by other routes.

Avoid using Lucemyra with any other medications that decrease pulse or blood pressure to avoid the risk of excessive bradycardia and low blood pressure.

Avoid other medications that also cause CNS depression or sedation.

Note that this list is not all-inclusive and includes only common medications that may interact with Lucemyra. You should refer to the prescribing information for Lucemyra for a complete list of interactions.

References

• Lucemyra (lofexidine hydrochloride). Updated 10/2023. USWM, LLC https://www.drugs.com/pro/lucemyra.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Lucemyra only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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