Lofexidine
Substance Withdrawal Syndrome
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Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
NA
Controlled Drug Substance
No
Lofexidine
Summary
Lofexidine is used to manage symptoms of opioid withdrawal in adults. It helps in abruptly discontinuing the use of opioids.
Lofexidine works by binding to alpha2 adrenergic receptors in the body. This reduces the release of a substance called norepinephrine, which in turn decreases the body's sympathetic tone. This action helps relax blood vessels and reduce heart rate, alleviating symptoms of opioid withdrawal.
The usual starting dose for adults is three 0.18 mg tablets taken four times daily. The maximum daily dose is 2.88 mg. Lofexidine can be taken with or without food.
Common side effects of Lofexidine include insomnia, orthostatic hypotension (a drop in blood pressure when standing up), bradycardia (slow heart rate), and dizziness. More serious adverse effects include hypotension (low blood pressure), bradycardia, and syncope (fainting).
Lofexidine can cause hypotension, bradycardia, and syncope. It should be used cautiously in patients with heart conditions and those taking medications that affect heart rate or blood pressure. Abrupt discontinuation can cause withdrawal symptoms. It is also not recommended for children and its safety during pregnancy has not been established.
Indications and Purpose
How does Lofexidine work?
Lofexidine is a central alpha-2 adrenergic agonist that binds to receptors on adrenergic neurons. This action reduces the release of norepinephrine, decreasing sympathetic tone and relaxing blood vessels. As a result, it helps alleviate symptoms associated with opioid withdrawal, such as nausea, muscle spasms, and insomnia.
Is Lofexidine effective?
Lofexidine's effectiveness is supported by clinical trials, including two randomized, double-blind, placebo-controlled studies. These studies demonstrated that Lofexidine significantly reduced opioid withdrawal symptoms compared to placebo. Patients treated with Lofexidine were more likely to complete the treatment period and reported lower scores on the Short Opiate Withdrawal Scale, indicating reduced withdrawal symptom severity.
What is Lofexidine?
Lofexidine is a medication used to manage opioid withdrawal symptoms in adults. It works by relaxing blood vessels, allowing blood to flow more easily, and reducing the release of norepinephrine, which decreases sympathetic tone. This helps alleviate symptoms such as nausea, muscle spasms, and insomnia that occur when opioid use is abruptly stopped.
Directions for Use
For how long do I take Lofexidine?
Lofexidine is typically used for up to 14 days to manage opioid withdrawal symptoms. The duration of use depends on the severity of withdrawal symptoms and the individual's response to the medication. It is important to follow the doctor's instructions and not to stop taking Lofexidine abruptly without medical guidance.
How do I take Lofexidine?
Lofexidine should be taken orally, with or without food, four times a day, with 5 to 6 hours between each dose. There are no specific food restrictions while taking Lofexidine, but it is important to follow the prescribed dosage and schedule. Patients should consult their healthcare provider for any additional dietary recommendations.
How should I store Lofexidine?
Lofexidine should be stored in its original container at room temperature, between 68°F to 77°F (20°C to 25°C). It should be kept away from excess heat and moisture, and the desiccant packs should not be removed until all tablets are used. Ensure the container is tightly closed and out of reach of children to prevent accidental ingestion.
What is the usual dose of Lofexidine?
The usual starting dose for adults is three 0.18 mg tablets taken orally four times daily, with 5 to 6 hours between each dose. The total daily dosage should not exceed 2.88 mg (16 tablets), and no single dose should exceed 0.72 mg (4 tablets). Lofexidine is not recommended for use in children as its safety and effectiveness have not been established in pediatric patients.
Warnings and Precautions
Can I take Lofexidine with other prescription drugs?
Lofexidine can interact with medications that prolong the QT interval, such as methadone, increasing the risk of heart rhythm problems. It also potentiates the CNS depressive effects of benzodiazepines, alcohol, and other sedating drugs, increasing the risk of drowsiness and dizziness. Patients should inform their healthcare provider of all medications they are taking to avoid potential interactions.
Can Lofexidine be taken safely while breastfeeding?
There is no information on the presence of Lofexidine in human milk or its effects on the breastfed infant. Caution should be exercised when administering Lofexidine to nursing women. The benefits of breastfeeding should be weighed against the mother's need for Lofexidine and any potential adverse effects on the infant. Consultation with a healthcare provider is recommended.
Can Lofexidine be taken safely while pregnant?
The safety of Lofexidine in pregnant women has not been established. Animal studies have shown potential risks such as reduced fetal weights and increased fetal resorptions at exposures below human levels. There is no strong evidence from human studies on fetal harm, but caution is advised. Pregnant women should discuss the potential risks and benefits with their healthcare provider before using Lofexidine.
Is it safe to drink alcohol while taking Lofexidine?
Drinking alcohol while taking Lofexidine can increase the risk of side effects such as drowsiness, dizziness, and fainting. Alcohol can potentiate the central nervous system depressive effects of Lofexidine, making these side effects more pronounced. It is advisable to avoid alcohol consumption while taking this medication to ensure safety.
Is it safe to exercise while taking Lofexidine?
Lofexidine may cause dizziness, lightheadedness, and fainting, which could limit the ability to exercise safely. It is important to be cautious when engaging in physical activities and to avoid becoming dehydrated or overheated. If you experience any symptoms that affect your ability to exercise, consult your healthcare provider for guidance.
Is Lofexidine safe for the elderly?
Caution should be exercised when administering Lofexidine to patients over 65 years of age, as no specific studies have been performed to establish its safety and effectiveness in this population. Dosing adjustments similar to those recommended for patients with renal impairment should be considered. Elderly patients should be monitored closely for side effects such as hypotension and bradycardia.
Who should avoid taking Lofexidine?
Important warnings for Lofexidine include the risk of hypotension, bradycardia, and syncope. Patients should be monitored for these symptoms, especially when moving from a lying to an upright position. Lofexidine can also prolong the QT interval, so it should be used cautiously in patients with heart conditions. Avoid using Lofexidine with other medications that lower blood pressure or pulse. Discontinuation should be gradual to prevent withdrawal symptoms.
