Lofexidine Patient Tips

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on May 29, 2025.

1. How it works

• Lofexidine (brand name: Lucemyra) works by binding to alpha-2 receptors in the brain and reduces the release of the chemical norepinephrine. It causes your muscles to relax, blood vessels to widen, and blood pressure to reduce to help lower an overactive nervous system.
• It is used in adults to help ease opioid (narcotic) withdrawal symptoms when opioids need to be stopped right away. These symptoms can include: insomnia, chills, feeling sick to your stomach, runny eyes, yawning, muscles spasms or stomach cramps. Lofexidine does not treat opioid addiction (opioid use disorder).
• Belongs to the group of medicines known as centrally acting antiadrenergic agents (also called alpha-2 adrenergic agonists).

2. Upsides

• May be used in adults to reduce withdrawal symptoms so that opioids can be quickly discontinued. It is not an opioid (narcotic) and is not addictive.
• Taken orally (by mouth) with or without food. May be administered for up to 14 days. Dosing is guided by symptoms and side effects that may occur.
• There are no contraindications to lofexidine (reasons why you could not receive this treatment) listed by the manufacturer; however, it should be used with caution in people with certain medical conditions, especially certain heart or kidney problems (see below in downsides).
• Slows down nervous system activity which typically occurs during opioid withdrawal. Helps relieve (but not completely eliminate) symptoms such as nausea, stomach cramps, muscle spasms, twitching, feeling cold, a pounding heart, muscle tension, aches and pains, yawning, runny eyes, and sleep problems (insomnia) due to opioid withdrawal.

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, low blood pressure upon standing (which may lead to fainting or injury), a slow heart rate, dizziness, drowsiness, sedation and a dry mouth. This may affect your ability to drive or operate machinery, particularly during the first few days of dosing, during hot weather, or after activity. Do not drink alcohol, drive, operate machinery or perfrorm hazardous activities until you know how lofexidine affects you.
• Fainting and tinnitus (ringing in the ears) have also been reported at higher dosages.
• Can cause withdrawal symptoms so needs to be withdrawn slowly over a 2 to 4-day period (for example: reduce by 1 tablet per dose every 1 to 2 days). High blood pressure on withdrawal has been reported and peaked on day two after discontinuation. Other withdrawal symptoms include diarrhea, insomnia, anxiety, chills, extremity pain and increased sweating.
• The dosage may need to be reduced in people with liver or kidney disease. Lofexidine may also cause abnormal heart rhythms (prolonging the QT interval). Monitoring and correction of electrolyte abnormalities (such as low potassium or magnesium) may be needed before starting lofexidone.
• This medicine may not be suitable for people with certain heart or kidney disorders. Females (compared to men) are more likely to experience a serious cardiovascular (heart / blood vessel) side effect while taking lofexidine, including low blood pressure upon standing and low heart rate. This has led to more females being intructed to temporarily or permanently stop treatment. Do not stop treatment unless you have spoken with your doctor.
• May not be suitable for people with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, chronic renal failure, congenital QT syndrome, or marked bradycardia.
• May interact with many drugs, including those that also lower blood pressure, prolong the QT interval, or cause sedation.
• Especially tell your healthcare provider if you take benzodiazepines, barbiturates, tranquilizers, or sleeping pills, as these medicines can cause serious side effects. Tell them if you take any medications for the individual symptoms of opioid withdrawal (such as pain relievers or medications for upset stomach). Tell your doctor if you take methadone, oral naltrexone, or paroxetine. Ask your healthcare provider or pharmacist if you are not sure if you are taking any of these medicines.
• Safety in pregnancy has not been established but animal studies show a possible risk. There is no information about using lofexidine during breastfeeding but caution should be used. Talk to your doctor about use in pregnancy / breastfeeding.
• Animal studies show use may affect female fertility endpoints, 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

Lofexidine is used to ease the symptoms due to abruptly stopping opioids in people with opioid addiction (opioid use disorder). It is given for up to 14 days, with dosing based on symptoms and peak withdrawal, but must be slowly discontinued. Peak withdrawal typically occurs the first 5 to 7 days following last use of opioid. The main side effects are low blood pressure, a slow heartbeat (bradycardia), sleepiness, sedation, dizziness, and dry mouth. Do not drink alcohol, drive, operate machinery or perfrorm hazardous activities until you know how lofexidine affects you.

5. Tips

• Lofexidine is not a treatment for opioid use disorder (OUD), but it helps to ease the symptoms of opioid withdrawal. You will have a reduced tolerance to opioids once you have gone through opioid discontinuation. You will be at an increased risk for a fatal overdose if you resume opioid use.
• It is initially given four times a day. Doses may decrease as your withdrawal symptoms improve. The dosage you are prescribed depends on your kidney or liver function and other additional medical conditions or medications you take.
• Tell your doctor if you have: low blood pressure, a slow heart rate, any heart problems, had a heart attack, if you have abnormal heart rhythms, or kidney or liver problems. Tell them if you drink alcohol.
• Do not drink alcohol, drive, operate machinery or perform potentially hazardous activities until you know how lofexidine affects you.
• Withdrawing from the effects of opioids is not easy. Lofexidine 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 recommendations from your healthcare provider.
• This medicine can drop your blood pressure and slow your heartbeat which may make you feel dizzy or pass out. Be careful when moving from lying down to sitting up or standing position. If you feel yourself beginning to faint or feeling dizzy or lightheaded while on lofexidine, lie or sit down until the feeling passes and call your doctor right away. Carefully rise from sitting or lying positions. If you are feeling like you are dizzy, lightheaded or might faint all the time, do not take your next dose of lofexidine until you have talked to your doctor.
• Keep hydrated by drinking plenty of water. Do not allow yourself to become dehydrated or overheated while taking lofexidine because it may make the side effects (like low blood pressure or fainting) worse.
• Do not stop taking lofexidine suddenly unless instructed by your doctor. This may cause a marked increase in blood pressure and symptoms may include diarrhea, insomnia (trouble sleeping), anxiety, chills, increased sweating, and pain in your fingers and toes. Lofexidine needs to be slowly stopped over time and you should talk to your doctor about this.
• This medicine may interact with other medications that also lower blood pressure, cause sleepiness, or slow your heart rate. Tell your doctor and pharmacist about all the medications you take before starting lofexidine treatment.
• Tell your doctor if you are breastfeeding, pregnant, or plan to become pregnant because lofexidine may not be suitable for you.

6. Response and effectiveness

• Blood levels of lofexidine reach a peak within 3 to 5 hours after a single dose. Accumulation of lofexidine occurs with repeat dosing.
• About 40% of patients using lofexidine completed 7 days of treatment, compared to only 28% of patients given a placebo (an inactive medication), a significant difference. Patients in the placebo group were more likely to drop out of studies early due to lack of effectiveness compared to those taking lofexidine.
• The Short Opiate Withdrawal Scale (SOWS)-Gossop is a 10-item questionnaire developed to evaluate opioid withdrawal symptom severity. It measures symptoms such as anxiety, yawning, and perspiration. People taking lofexidine reported a significantly lower score in the SOWS-Gossop than people taking a placebo.

7. Interactions

Medicines that interact with lofexidine may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect. 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 and pharmacist about how drug interactions should be managed.

Tell your healthcare provider about all of the medicines you take, including prescription and over-the-counter medicines, vitamins, herbal supplements, and any medications you may take for the individual symptoms of opioid withdrawal (such as pain relievers or medications for upset stomach).

Lofexidine interacts with over 500 medications, and most of these interactions are considered moderate or major. Common medications or substances that may interact with lofexidine include:

• alcohol (ethanol)
• 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 (e.g., diphenhydramine or azelastin) or barbiturates
• benzodiazepines such as clonazepam, diazepam, or lorazepam
• bisacodyl
• bromocriptine
• bupropion
• buspirone
• cannabis (marijuana)
• 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
• monoamine 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 lofexidine)
• papaverine
• quinidine
• QT-prolonging medicines such as buprenorphine, amiodarone, or cisapride
• tamoxifen
• targeted treatments such as ceritinib or cabozantinib
• valerian
• valproic acid

Avoid drinking alcohol while taking lofexidine, as it may increase your risk for dizziness, drowsiness, confusion, and difficulty concentrating. Tell your doctor if you drink alcohol before you start treatment.

Avoid other medications that also cause nervous system (CNS) depression or sedation. Especially tell your healthcare provider if you take benzodiazepines, barbiturates, tranquilizers, sleeping pills or drink alcohol. Taking lofexidine with these medicines can cause serious side effects.

Lofexidine may reduce the efficacy of oral naltrexone. Administer naltrexone by other routes than by mouth.

Avoid using lofexidine with any other medications that decrease pulse or blood pressure to avoid the risk of excessively slowed heart rate, low blood pressure and possible fainting. Monitor for orthostatic low blood pressure and low heart rate when an inhibitor of CYP2D6 is used concomitantly with this medicine.

ECG monitoring (a test that measures the electrical activity of the heart) is recommended in patients receiving methadone and lofexidine at the same time.

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

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Frequently asked questions

• Is Lucemyra (lofexidine) a controlled drug?
• How long does lofexidine typically take to work?
• How do you get Lucemyra (lofexidine)?

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use lofexidine 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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