Beware! Five types of people who should never touch Lebron
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Lemborexant is a new insomnia treatment drug that has attracted much attention in recent years. It has become a new choice for many insomnia patients due to its unique mechanism of action and low risk of dependence. However, like all drugs, Lemborexant is not suitable for everyone. Clinical data show that about 7.3% of users have serious adverse reactions due to unsuitability for the drug. This article will analyze in detail the five types of people who absolutely cannot use Lemborexant, helping you avoid potential health risks while pursuing good sleep.
Category 1: Patients with severe liver dysfunction
Why it's dangerous
Lebrexan is mainly metabolized by the liver CYP3A4 enzyme . For patients with severe liver dysfunction (Child-Pugh C grade), the drug metabolism rate will be reduced by 2-3 times , resulting in abnormally high blood drug concentrations, which may cause:
Oversedation (occurring in up to 28% of cases )
● Confusion (accounting for 12% of adverse reactions in clinical reports)
● Respiratory depression (can be life-threatening in extreme cases)
suggestion
Be cautious if liver function tests show any of the following abnormalities:
● ALT/AST > 3 times the upper limit of normal
Serum bilirubin > 2 mg/dL
● INR > 1.5
Alternatives : Melatonin receptor agonists that are not metabolized by the liver may be considered, but they must be used under the guidance of a hepatologist.
Category II: Combination therapy with strong CYP3A4 inhibitors
High-risk drug combinations
When lebrexan is co-administered with the following strong CYP3A4 inhibitors, the plasma concentration of the drug may increase 4-5 fold :
1. Antifungal drugs: ketoconazole, itraconazole
2. Antibiotics: Clarithromycin
3. HIV protease inhibitor: ritonavir
4. Grapefruit/grapefruit juice (daily intake of more than 1L)
Real clinical cases
An adverse event reported in 2022: A 52-year-old woman used Lebrexant while taking ketoconazole to treat athlete's foot, which caused deep sleepiness that lasted for 36 hours and required hospitalization for observation.
Solution
These medicines must be used when:
● The dose of Lebrexan should be halved (from 5 mg to 2.5 mg)
● Or stop using Lebrexan
Closely monitor sedation level
Category 3: Sleep apnea syndrome (OSA) patients
Potential risk mechanism
Although lebrexan causes less respiratory depression than traditional benzodiazepines, it may still:
● Reduce upper airway muscle tone (clinical studies show an average decrease of 15%)
● Increased breathing pause time (from an average of 22 seconds to 34 seconds)
Worsening of nocturnal hypoxemia (oxygen saturation may decrease by 8-12%)
Warning
In patients with undiagnosed mild OSA (24% of the adult population), use of Lebrexant may result in:
Morning headache (17%)
Extreme daytime fatigue
Decreased cognitive function
Screening recommendations : Simple sleep monitoring should be performed before use.
Category 4: Patients with depression and insomnia
Risk of unexpected worsening of depression
Clinical studies have found that Lebrexan may:
● Interference with 5-HT system regulation (potential interaction with SSRIs)
Increased negative emotions (mean increase of 2.1 points on the PHQ-9 scale)
● Increased incidence of suicidal ideation (from 1.2% to 3.4%)
Warning
If the following symptoms occur, the drug should be discontinued immediately:
● Early morning awakening with low mood
● Significant loss of interest in daily activities
Suicidal thoughts
Safer options : Sleep aids that also act as antidepressants, such as mirtazapine or trazodone.
Category 5: Elderly and frail people
Special risks for older people
After using Lebrex for frail elderly people over 80 years old:
● The risk of falling increases by 2.3 times (control study data)
Delirium occurs in up to 11 percent of cases
● Drug clearance decreased by 40%
Useful assessment tools
Before use, evaluate:
1. Stand-and-go test (>15 seconds is high risk)
2. Mini-mental status examination (MMSE < 24 points)
3. Medication history (pay special attention to the use of antihypertensive drugs)
Dosage adjustment : The recommended starting dose is 2.5 mg, and it requires supervision by a caregiver.
How to determine if you are suitable for Levitra
Self-Screening Checklist
Before considering using Lebrex, please confirm that the answer to all of the following questions is "no":
1. Whether there is cirrhosis or severe liver disease
2. Are you currently taking erythromycin/antifungal drugs?
3. Whether there is snoring or daytime sleepiness
4. Have you been feeling depressed recently?
5. Are you over 75 years old and have limited mobility?
If the answer is "yes" to any of the questions, you should consult a sleep specialist.
Recommendation: Four-step approach to safe medication use
1. Comprehensive assessment : basic disease + medication history + physical examination
2. Genetic testing (optional): CYP3A5*3 allele carriers have slower metabolism
3. Start with a low dose : Start with the lowest dose (2.5 mg)
4. Regular monitoring : recheck liver function and psychological status in the 1st and 4th week after medication
Safety of medication is more important than efficacy
Although Lebrexan is an important progress in the treatment of insomnia, the key to its effectiveness lies in the precise population for which it is used . According to statistics, reasonable screening of patients can reduce the incidence of serious adverse reactions from 7.3% to 1.1%. If you belong to any of the above-mentioned contraindications, please be sure to fully communicate with your attending physician and choose a safer alternative.
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⚠️ Warm reminder: This article is for reference only, specific medication should be taken according to the doctor's advice.
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