Hetlioz

Hetlioz Uses, Dosage, Side Effects, Food Interaction and all others data.

Hetlioz is a selective dual melatonin receptor agonist indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (N24HSWD). Occurring commonly in blind individuals without light perception, this condition is often characterized by periods of night-time insomnia and day-time sleepiness. In blind individuals, a lack of light stimulation causes an extension of the 24-hour circadian cycle and can lead to progressively delayed sleep onset. By activating melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, tasimelteon has been shown to improve sleep by resynchronizing the circadian rhythm through its "non-photic" mechanism. Hetlioz is currently the only drug available for the treatment of N24HSWD and was granted orphan drug status by the FDA in 2010.

Trade Name Hetlioz
Availability Prescription only
Generic Tasimelteon
Tasimelteon Other Names Tasimeltéon, Tasimelteon, Tasimelteón, Tasimelteonum
Related Drugs Hetlioz, Hetlioz LQ
Weight 20mg,
Type Oral capsule
Formula C15H19NO2
Weight Average: 245.322
Monoisotopic: 245.141578856
Protein binding

At therapeutic concentrations, tasimelteon is about 90% bound to proteins.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country United States,
Last Updated: September 19, 2023 at 7:00 am
Hetlioz
Hetlioz

Uses

Hetlioz is a melatonin receptor agonist used to treat Non- 24-Hour Sleep-Wake Disorder.

Hetlioz is indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (N24HSWD).

Hetlioz is also used to associated treatment for these conditions: Non-24-Hour Sleep-Wake Disorder

How Hetlioz works

Hetlioz is a selective dual agonist of the melatonin receptors MT1 and MT2.

Toxicity

The most common adverse reactions are headache, increased alanine aminotransferase, nightmares or unusual dreams, and upper respiratory or urinary tract infections. There are currently no adequate or well-controlled studies that suggest that tasimelteon is safe to use during pregnancy. In animal studies, administration of tasimelteon during pregnancy resulted in developmental toxicity (embryofetal mortality, neurobehavioral impairment, and decreased growth and development in offspring) at doses greater than those used clinically. During clinical trials, rats did not self-administer tasimelteon, suggesting that the drug does not have a potential for abuse.

Food Interaction

  • Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of tasimelteon, which may increase its serum concentration. Alternatively, the dose of tasimelteon may need to be modified.
  • Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of tasimelteon and may reduce its serum concentration. Alternatively, the dose of tasimelteon may need to be modified.
  • Take on an empty stomach. The Cmax of tasimelteon is reduced when taken with food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of tasimelteon.

Use in combination may result in additive central nervous system depression and
ADJUST DOSING INTERVAL: Food may delay the absorption and onset of action of tasimelteon.

According to the product labeling, administration of tasimelteon with a high-fat meal decreased peak plasma concentration (Cmax) by 44% and delayed the median time to reach Cmax by approximately 1.75 hours compared to administration in the fasted state.

MONITOR: Smoking induces CYP450 1A2 and may reduce the plasma concentrations of tasimelteon, which is metabolized by the isoenzyme.

According to the product labeling, tasimelteon systemic exposure was approximately 40% lower in smokers than in nonsmokers.

MANAGEMENT: Patients receiving tasimelteon should be advised to avoid or limit consumption of alcohol.

Hetlioz should be taken without food.

Patients who smoke may have a reduced therapeutic response to tasimelteon.

Volume of Distribution

The apparent oral volume of distribution of tasimelteon at steady state in young healthy subjects is approximately 56 - 126 L.

Half Life

The observed mean elimination half-life for tasimelteon is 1.3 ± 0.4 hours.

Elimination Route

Following oral administration of radiolabeled tasimelteon, 80% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 84%. Less than 1% of the dose was excreted in urine as the parent compound.

Innovators Monograph

You find simplified version here Hetlioz

*** Taking medicines without doctor's advice can cause long-term problems.
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