Tasimelteon

What is Tasimelteon?

• Tasimelteon (HETLIOZ) is a melatonin receptor agonist used for the treatment of Non-24-Hour sleep-wake disorder (Non-24) in adults, nighttime sleep disturbances in Smith-Magenis Syndrome (SMS) in patients 16 years of age and older.

What are the uses of this medicine?

This medicine is used: HETLIOZ capsules are indicated for the treatment of:

• Non-24-Hour Sleep-Wake Disorder (Non-24) in adults
• Nighttime sleep disturbances in Smith-Magenis Syndrome (SMS) in patients 16 years of age and older

HETLIOZ LQ oral suspension is indicated for the treatment of:

• Nighttime sleep disturbances in SMS in pediatric patients 3 years to 15 years of age

How does this medicine work?

• 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.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid use of HETLIOZ in combination with fluvoxamine or other strong CYP1A2 inhibitors.
• Avoid use of HETLIOZ in combination with rifampin or other CYP3A4 inducers.
• Nighttime administration of beta-adrenergic receptor antagonists may reduce the efficacy of HETLIOZ.

Is this medicine FDA approved?

• It was approved for use in the United States in 2014.

How should this medicine be used?

Recommended Dosage: Adults

• The recommended dosage of HETLIOZ capsules in adults is 20 mg one hour before bedtime, at the same time every night.

Patients 16 years of Age and Older

• The recommended dosage of HETLIOZ capsules in patients 16 years and older is 20 mg one hour before bedtime, at the same time every night.

Pediatric Patients 3 Years to 15 Years of Age

• The recommended dosage of HETLIOZ LQ oral suspension in pediatric patients 3 years to 15 years of age is based on body weight.

Administration

• Administer HETLIOZ capsules and HETLIOZ LQ oral suspension without food.
• If a patient is unable to take HETLIOZ at approximately the same time on a given night, they should skip that dose and take the next dose as scheduled.
• Shake HETLIOZ LQ oral suspension well for at least 30 seconds before every administration.
• Remove seal and insert press-in bottle adapter (included in the package) into the neck of the bottle until a tight seal is made.
• Turn the bottle upside down and withdraw the prescribed amount of HETLIOZ LQ oral suspension from the bottle.
• Leave the press-in bottle adapter in place on bottle neck and replace cap on bottle.
• Store refrigerated.
• After opening, discard after 5 weeks (for the 48 mL bottle) and after 8 weeks (for the 158 mL bottle).

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 20 mg
• Oral Suspension: 4 mg/mL

This medicine is available in fallowing brand namesː

• HETLIOZ

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• increased alanine aminotransferase
• nightmares or unusual dreams
• upper respiratory or urinary tract infection

What special precautions should I follow?

• After taking HETLIOZ, patients should limit their activity to preparing for going to bed.
• HETLIOZ can potentially impair the performance of activities requiring complete mental alertness.

What to do in case of emergency/overdose?

• There is limited data avaialable for overdosage of HETLIOZ.

Management of overdosage:

• As with the management of any overdose, general symptomatic and supportive measures should be used, along with immediate gastric lavage where appropriate. Intravenous fluids should be administered as needed.
• Respiration, pulse, blood pressure, and other appropriate vital signs should be monitored, and general supportive measures employed.
• While hemodialysis was effective at clearing HETLIOZ and the majority of its major metabolites in patients with renal impairment, it is not known if hemodialysis will effectively reduce exposure in the case of overdose.

Can this medicine be used in pregnancy?

• Based on animal data showing adverse renal effects, FARXIGA is not recommended during the second and third trimesters of pregnancy.
• Limited data with FARXIGA in pregnant women are not sufficient to determine drug-associated risk for major birth defects or miscarriage.

Can this medicine be used in children?

• Available postmarketing case reports with HETLIOZ use in pregnant women are not sufficient to evaluate drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.

What are the active and inactive ingredients in this medicine?

• Active ingredient: tasimelteon
• Inactive ingredients: ascorbic acid, cherry flavor, mannitol, microcrystalline cellulose/carboxymethylcellulose sodium, polysorbate 80, sodium benzoate, sodium chloride, sucrose, sucralose, and water.

Who manufactures and distributes this medicine?

Distributed by: Vanda Pharmaceuticals Inc. Washington, D.C. 20037 USA

What should I know about storage and disposal of this medication?

• Store HETLIOZ LQ in a refrigerator at 36°F to 46°F (2°C to 8°C).
• Keep HETLIOZ LQ and all medicines out of the reach of children.

Disposal of HETLIOZ LQ Suspension

• Once opened, the 48 mL bottle can be stored for 5 weeks and the 158 mL bottle can be stored for 8 weeks, both at refrigerated temperature. Safely throw away any unused HETLIOZ LQ suspension after these time points.
• Ask your pharmacist how to properly throw away (dispose of) medicines you no longer use.

• Dailymed label info on Tasimelteon
• FDA Tasimelteon