Tasimelteon

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Information about Tasimelteon

Tasimelteon is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

Liver safety of Tasimelteon

Tasimelteon therapy is associated with a low rate of serum enzyme elevations, but has not been implicated in cases of clinically apparent liver injury.

Mechanism of action of Tasimelteon

Tasimelteon (tas" i mel' tee on) is a synthetic melatonin receptor agonist with affinity for both the melatonin type 1 and type 2 receptors (MT1 and MT2). These receptors are believed to be involved in the maintenance of the circadian rhythm that regulates the normal sleep-wake cycle. Melatonin itself has been proposed as therapy of sleep disturbances including insomnia and jet lag, but systematic reviews and metaanalyses of controlled trials of various melatonin formulations have failed to demonstrate consistent efficacy. In contrast, melatonin receptor agonists such as ramelteon and tasimelteon were found to have effects on the circadian rhythm and sleep patterns.

FDA approval information for Tasimelteon

Tasimelteon was approved for use in “non-24 hour sleep-wake disorder” in the United States in 2014, the second melatonin receptor antagonist approved for use in sleep disorders. Whereas ramelteon has been approved for insomnia, tasimelteon is used more for shifting of sleep-wake patterns and may take weeks to have its full effect. Tasimelteon is available in 20 mg capsules under the brand name Hetlioz.

Dosage and administration for Tasimelteon

The recommended dose is 20 mg taken orally before bedtime at the same time every night.

Side effects of Tasimelteon

Side effects are few, but may include daytime somnolence, fatigue, dizziness, headache and vivid or abnormal dreams.

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