Suvorexant (Belsomra)

A sleeping agent that blocks the action of neurotransmitters, orexins, that regulate wakefulness and sleep.

Has the potential to cause next-day sleepiness and impaired driving, so that no more than one pill should be taken per night and the dose should not exceed 20 milligrams.

Associated with impaired driving in patients who take 20 milligrams and patients are cautioned against next-day driving or activities requiring full mental alertness.

Drug available in 5, 10, 15 and 20 milligram doses.

A Schedule IV controlled substance because it can be addictive and has the potential to be abused.

Proposed that non-elderly adults start on 20 milligrams and increase to 40 if needed.

Recommended that elderly patients start by taking 15 milligrams and increase to 30 if necessary.

Little evidence that the drug is more effective at higher doses and it is less safe.

Trade names Belsomra

Oral agent.

Schedule IV drug.

Bioavailability at 82%.

Protein binding >99%

Metabolism-hepatic, CYP3A, CYP2C19

Biological half-life approximately 12 hours.

Excretion feces (66%) and urine (23%).

A medication for the treatment of insomnia.

A selective, dual orexin receptor antagonist.

May lead to limited physical dependence or psychological dependence relative to the drugs or other substances in schedule III.

The potential for psychological dependence is similar to that of zolpidem

Used for the treatment of insomnia, characterized by difficulties with sleep onset and/or sleep maintenance.

Most common complaint from users is it did not help them to sleep.

Some patients report sleep disturbance such as a nightmare, sleep t2242or, or abnormal dream.

In some cases the drug caused them to be more awake, have sleepiness the next day and issues with driving, or suicide.

Reports of people performing complex tasks with little recollection of the events.

Not recommended in people with liver impairment.

Suvorexant pregnancy category is currently classified as Category C.

Contraindicated in people diagnosed with narcolepsy.

Not recommended if people are also taking medications that strongly inhibit the liver enzyme CYP3A like itraconazole, lopinavir/ritonavir, clarithromycin, ritonavir, ketoconazole, indinavir/ritonavir, or conivaptan.

If used with a medication that moderately inhibits the liver enzyme CYP3A, like verapamil, erythromycin, diltiazem, or dronedarone, it is recommended that the dose be adjusted.

Exerts its therapeutic effect in insomnia through antagonism of orexin receptors, and 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 orexin receptor type 1 (OX1) and orexin receptor type 2 (OX2) is thought to suppress wake drive.

Highly protein-bound.

Taken with food delays the time to max concentration.

Extensively metabolized by the liver.

Designated a schedule IV controlled substance in the U.S. under the Controlled Substances Act.

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