Suvorexant

Indications

Suvorexant is indicated for the treatment of insomnia, characterized by difculties with sleep onset and/or sleep maintenance.

Pharmacology

Suvorexant is a highly selective antagonist for orexin receptors OX1R and OX2R. The mechanism by which Suvorexant exerts its therapeutic efect in insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.

Dosage & Administration

Recommended dose is 10 mg, no more than once per night taken before 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening. If the 10 mg dose is well-tolerated but not effective, the dose can be increased, not to exceed 20 mg once daily. Lowest dose effective should be used for the patient. Time to effect may be delayed if taken with or soon after a meal.

Interaction

CNS-Active Drugs: An additive effect on psychomotor performance was observed when a single dose of 40 mg of Suvorexant was co-administered with a single dose of 0.7 g/kg alcohol. Suvorexant does not afect alcohol concentrations and alcohol does not afect Suvorexant concentrations.

effect s of Other Drugs on Suvorexant: Strong (e.g., ketoconazole or itraconazole) and moderate (e.g., diltiazem) CYP3A inhibitors signifcantly increased Suvorexant exposure. Strong CYP3A inducers (e.g., rifampin) substantially decreases Suvorexant exposure.

effect s of Suvorexant on Other Drugs: Suvorexant is unlikely to cause clinically signifcant inhibition of human CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19 or CYP2D6. Chronic administration of Suvorexant is unlikely to induce the metabolism of drugs metabolized by major CYP isoforms.

Contraindications

Do not use in patients with narcolepsy.

Side Effects

Common side effects are Sleepiness during the day, Not thinking clearly, Act strangely, confused, or upset, Sleep-walking

Pregnancy & Lactation

Pregnancy Category C. There is no adequate and well-controlled studies in pregnant women. Suvorexant should be used during pregnancy only if the potential beneft justifes the potential risk to the fetus.

Precautions & Warnings

Daytime somnolence: Risk of impaired alertness and motor coordination, including impaired driving; risk increases with dose; caution patients taking 20 mg against next-day driving and other activities requiring complete mental alertness.

Need to evaluate for co-morbid diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment.

Therapeutic Class

Miscellaneous sedatives & hypnotics

Storage Conditions

Store in dry and cool place, protect from light & keep away from children.