Pharmacology of Suvorexant (Belsomra) ; Mechanism of action, Pharmacokinetics, Uses, Effects

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Suvorexant, marketed under the brand name Belsomra, is an orexin receptor antagonist used to treat insomnia. Here's an overview of its pharmacology:

Mechanism of Action
Orexin Receptor Antagonism: Suvorexant works by selectively antagonizing orexin receptors OX1R and OX2R. Orexins are neuropeptides that promote wakefulness and arousal. By inhibiting the binding of orexin A and B to their receptors, suvorexant reduces wakefulness and promotes sleep.

Indications
Insomnia: Suvorexant is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.

Dosage and Administration
Initial Dose: The recommended starting dose is 10 mg, taken orally within 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening.

Maximum Dose: If the 10 mg dose is well-tolerated but not effective, the dose can be increased, not to exceed 20 mg once daily.

Adverse Effects
Common Side Effects: Include somnolence, dizziness, and headache.

Serious Side Effects: Include complex sleep behaviors (e.g., sleep-walking, sleep-driving), which may result in serious injuries, including death.

Pharmacokinetics
Absorption: Suvorexant is well absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 2 hours.

Metabolism: It is extensively metabolized in the liver by the cytochrome P450 enzyme CYP3A4.

Excretion: The metabolites are primarily excreted in the feces (66%) and urine (23%).

Half-Life: The elimination half-life of suvorexant is approximately 12 hours

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