Tasimelteon

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

Tasimelteon 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. Tasimelteon is currently the only drug available for the treatment of N24HSWD and was granted orphan drug status by the FDA in 2010.

Tasimelteon
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Tasimelteon
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

Uses

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

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

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

How Tasimelteon works

Tasimelteon 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.

Tasimelteon should be taken without food.

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

Tasimelteon Drug Interaction

Major: acetaminophen / oxycodone, acetaminophen / codeineModerate: suvorexant, gabapentin enacarbil, propranolol, desvenlafaxine, alprazolamUnknown: amphetamine / dextroamphetamine, fexofenadine, aspirin, liothyronine, galcanezumab, acetaminophen, levothyroxine, dimethyl fumarate, cholecalciferol, lisdexamfetamine, pitolisant, bupropion, ondansetron

Tasimelteon Disease Interaction

Major: depression, severe renal impairmentModerate: glaucoma, liver disease

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.