Leborexine indications, efficacy and effects, dosage, efficacy, side effects, precautions, price

Drug Ingredients

1. Active ingredient: leborexan.

2. Inactive ingredients: hydroxypropylcellulose, lactose monohydrate, low-substituted hydroxypropylcellulose and magnesium stearate. The film coating contains inactive ingredients such as hypromellose 2910, polyethylene glycol 8000, talc, and titanium dioxide.

Dosage forms and specifications

1. 5mg tablet: light yellow, round, biconvex film-coated tablet, with "5" debossed on one side and "L M" on the other side.

2. 10mg tablet: orange, round, biconvex film-coated tablet, with "10" debossed on one side and "L M" on the other side.

Indications

It is an orexin receptor antagonist suitable for the treatment of adult insomnia patients characterized by difficulty falling asleep or maintaining sleep.

Efficacy and role

Lemborexant is a reversible, competitive and orally active orexin OX1 and OX2 receptor antagonist. It inhibits orexin by competitively binding to two subtypes of orexin receptors, thereby treating insomnia.

1. The recommended dose of leborexan is 5mg, taken no more than once a night, before going to bed. The dose may be increased to 10 mg based on clinical response and tolerability, with the maximum recommended dose being 10 mg once daily.

2. Liver damage:

(1) Moderate liver damage: The initial and maximum recommended dose is 5 mg, no more than once per night.

(2) Severe liver damage: Not recommended.

In a clinical study, the efficacy of leboresen and zolpidem extended-release, suvorexan, doxepin, ramelteon, zolpidem immediate-release, eszopiclone, zaleplon and other drugs in the treatment of insomnia were compared.

Compared with placebo, leborexan has an NNT value of up to 3, demonstrating that leborexan has a clinically relevant therapeutic effect. Compared with placebo, leborexan had an NNH value of ≥ 10, indicating that leborexan was relatively tolerable.

Leborexen generally has more robust NNT values ​​than zolpidem ER with respect to polysomnography and sleep diary results. In indirect comparisons, NNT data for other hypnotics showed similar effect sizes to Lebraxanthin.

Leborexan 5mg and 10mg demonstrated statistically significant superiority in the primary efficacy indicator LPS compared with placebo, and compared with placebo, Leborexan 5mg and 10mg showed statistically significant improvements in SEF and WASO.

Side effects and treatment measures

The most common side effect is drowsiness.

1. Adjust the drug dosage: It is recommended to adjust the dosage of Leborexen under the guidance of a doctor. If the symptoms are mild, you can try to reduce the dosage or temporarily stop taking the drug for a few days to observe whether the symptoms improve.

2. Avoid driving and other activities that require mental alertness: If you feel drowsy during medication, it is recommended to avoid driving or other activities that require complete mental alertness the next day to avoid danger.

3. Adjust the medication time: If you still feel sleepy after taking medication at night, you can adjust the medication time to 2-3 hours before going to bed to better control the effects of the medication.

4. Avoid using it with other sedative drugs at the same time: If you need to use other sedative drugs at the same time, it is recommended to consult your doctor whether it can be used at the same time to avoid aggravating drowsiness symptoms.

Contraindications

Leborexen is contraindicated in patients with narcolepsy.

Precautions

1. CNS depressant effects and daytime impairment: Coadministration with other CNS depressants, such as benzodiazepines and opioids, increases the risk of CNS depression and can lead to daytime impairment. Due to the potential for additive effects, dosage adjustments of leborexan and CNS depressants may be necessary when administered concurrently. It is not recommended to use Leborexen in combination with other drugs to treat insomnia, and do not drink alcohol and take Leborexen at the same time.

2. Sleep paralysis, hypnotic/hypnotic hallucinations and cataplexy-like symptoms: may include periods of leg weakness lasting from seconds to minutes and may occur at night or during the day.

3. Complex sleep behaviors: such as sleepwalking, sleepwalking driving, and engaging in other activities when not fully awake. If the patient has complex sleep behaviors, Lebrasen should be stopped immediately and do not drive a vehicle or engage in other dangerous activities.

4. Worsening depression or suicidal ideation: Protective measures may be needed.

Price

1. Japan’s Eisai Laibo Leisheng

1. Lebrasin tablets 10mg: The current reference price is about US$165 per box.

2. デエビゴ tablets 5mg: The current reference price is about US$117 per box.

3. デエビゴ tablets 2.5mg: The current reference price is about US$77 per box.

2. Hong Kong version of Laibo Leisheng

The current reference price of 5mg*28 capsules is about US$105 per box.

Storage

Store at room temperature of 68℉-77℉ (20℃-25℃), and keep Lebrasin out of the reach of children.

Usage in Special Populations

1. Pregnancy: There are currently no available data on the use of Lebraxant in pregnant women to evaluate the drug-related risks of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

2. Lactation: There is currently no data on the effects of lemborexant on breastfed infants or on milk production. The developmental and health benefits of breastfeeding should be considered, as well as the mother's clinical need for lemborexant.

3. Pediatric medication: The safety and effectiveness of lemborexant in pediatric patients has not yet been determined.

4. Medication for elderly patients: The elderly have a higher risk of falling after taking medication. Patients aged ≥65 years should be cautious when using doses exceeding 5 mg.

5. Renal impairment: Patients with mild, moderate or severe renal impairment do not need to adjust the dose. Patients with severe renal impairment may have an increased risk of drowsiness and it is recommended to reduce the dose.

Drug Abuse and Dependence

1. Abuse: Because individuals with a history of alcohol or other drug abuse or addiction may be at increased risk for Leborexant abuse and addiction, such patients should be followed closely.

2. Dependence: Long-term administration of Leborexen will not produce withdrawal signs or symptoms after stopping the drug, so Leborexen will not cause physical dependence.

References:

Citrome L, Juday T, Frech F, Atkins N Jr. Lemborexant for the Treatment of Insomnia: Direct and Indirect Comparisons With Other Hypnotics Using Number Needed to Treat, Number Needed to Harm, and Likelihood to Be Helped or Harmed. J Clin Psychiatry. 2021 Jun 1;82:20m13795. doi: 10.4088/JCP.20m13795. PMID: 34077032.

Related hot article recommendations: