Drug intelligence / Profile preview

Silexan

Development stage
Phase 4
Lead developer
Schwabe
Modality
Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Silexan is a standardized lavender oil preparation that has been extensively studied for its anxiolytic (anti-anxiety) properties. It's derived from Lavandula angustifolia flowers through steam distillation and contains specific percentages of active constituents, primarily linalool (36.8%) and linalyl acetate (34.2%)[8]. ## Pharmacological Properties Silexan works through several mechanisms that contribute to its anxiolytic effects: 1. **Calcium Channel Inhibition**: Silexan is a potent inhibitor of voltage-dependent calcium channels (VOCCs) in synaptosomes, primary hippocampal neurons, and stably overexpressing cell lines[5][7]. This inhibition is comparable to pregabalin but occurs through a different binding site[7]. 2. **Serotonergic Effects**: It has serotonin-1A agonist properties, similar to buspirone and vortioxetine[4]. 3. **Additional Mechanisms**: Silexan also exhibits GABA-ergic effects (like benzodiazepines) and NMDA antagonist properties (like ketamine)[4]. The pharmacokinetics of Silexan have been studied in rats, showing that its main constituents (linalool and linalyl acetate) are distributed to various tissues including the brain, with linalyl acetate rapidly metabolizing into linalool[6]. ## Clinical Efficacy Clinical trials have demonstrated Silexan's effectiveness for: - **Generalized Anxiety Disorder (GAD)**: In a large randomized controlled trial (n=539), Silexan at doses of 80mg and 160mg daily was compared to paroxetine 20mg daily and placebo. Both Silexan doses showed significant superiority to placebo and were comparable or superior to paroxetine[7]. - **Subthreshold Anxiety**: Anxiolytic effects become evident after approximately 2 weeks of treatment[1]. - **Sleep Improvement**: Silexan has been shown to improve sleep quality as a result of its anxiolytic effects[3]. ## Safety Profile Silexan has a favorable safety profile: - **No Abuse Potential**: Studies have confirmed that Silexan does not exhibit abuse potential and is unlikely to be recreationally abused[5]. - **No Withdrawal Symptoms**: Unlike benzodiazepines, Silexan can be discontinued without tapering and without causing withdrawal symptoms[7]. - **Non-Sedating**: Despite its anxiolytic properties, Silexan does not cause sedation[5]. - **Side Effects**: The most common adverse effects are mild gastrointestinal symptoms and occasional allergic skin reactions[5]. Some users report "lavender burps" (taste of lavender)[9]. ## Availability Silexan is available as: - A prescription medication for anxiety in 14 countries[2]. - An over-the-counter supplement in the United States, marketed under brand names like Lavela WS 1265 (by Integrative Therapeutics) and CalmAid[9]. - In Europe, it's available as Lasea® in 80mg soft gelatin capsules[6][10]. The recommended dosage is typically one 80mg capsule daily[10], though some studies have also evaluated a 160mg daily dose[7].

Brand names
Lavela WS 1265CalmAidLasea
Other names
lavender oilSilexan
02

Targets

VDCC (Voltage-dependent calcium channel)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))GABAA (Gamma-aminobutyric acid receptor)NMDAR (Glutamate receptor ionotropic, NMDA)

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