tasimelteon

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: melatonin receptor agonists

Indications ⬆ ⬇

REMS

Non-24-hour sleep-wake disorder (a circadian rhythm disorder more common in totally blind patients).
Nighttime sleep disturbances in Smith-Magenis Syndrome.

Action ⬆ ⬇

Acts as an agonist at melatonin MT₁ and MT₂ receptor sites, which are involved in regulation or circadian rhythm.

Therapeutic effects:

Improved circadian rhythm with improved sleep/wake patterns.

Pharmacokinetics ⬆ ⬇

Absorption: 38% absorbed following oral administration, plasma concentrations ↑ in female patients.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP1A2 and CYP3A4 isoenzymes. Primarily excreted in urine as metabolites.

Half-Life: 1.3 hr.

Time/Action Profile ⬆ ⬇

(establishment of circadian rhythm/sleep cycle)

ROUTE	ONSET	PEAK	DURATION
PO	wks–mos	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Severe hepatic impairment.

Use Cautiously in:

OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults have ↑ risk of adverse reactions.

Adv. Reactions/Side Effects ⬆ ⬇

GI: ↑liver enzymes

Neuro: headache, nightmares/unusual dreams

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of strong CYP1A2 inhibitors, including fluvoxamine, may ↑ levels and risk of toxicity.
Concurrent use of strong CYP1A2 inducers, including rifampin and cigarette smoke , may ↓ levels and effectiveness.
Strong CYP3A4 inhibitors, including ketoconazole, may ↑ levels and risk of toxicity.
Alcohol may ↑ CNS depression.

Route/Dosage ⬆ ⬇

Capsules are not interchangeable with the oral suspension.

Non-24-Hour Sleep-Wake Disorder

PO (Adults ): Capsules: 20 mg one hr before bedtime, taken at the same time every night.

Nighttime Sleep Disturbances in Smith-Magenis Syndrome

PO (Adults and Children ≥16 yr): Capsules: 20 mg one hr before bedtime, taken at the same time every night.
PO (Children 3–15 yr and >28 kg): Oral suspension: 20 mg one hr before bedtime, taken at the same time every night.
PO (Children 3–15 yr and ≤28 kg): Oral suspension: 0.7 mg/kg one hr before bedtime, taken at the same time every night.

Availability ⬆ ⬇

(Generic available)

Capsules (Hetlioz): 20 mg
Oral suspension (Hetlioz LQ) cherry flavor: 4 mg/mL

Assessment ⬆ ⬇

Assess mental status, sleep patterns, and frequency of daytime naps prior and periodically during therapy.

Lab Test Considerations:

May cause ↑ transaminases.

Implementation ⬆ ⬇

PO: Administer without food before bedtime at the same time each night. DNC: Swallow capsule whole; do not open, dissolve, crush, or chew.
- Shake oral suspension for ≥30 sec before administering. Store suspension in refrigerator. Discard refrigerated suspension after 5 wk (for 48 mL bottle) and after 8 wk (for 158 mL bottle).
- Oral capsules and suspension are not interchangeable.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take tasimelteon as directed at the same time each day. If unable to take at approximately the same time on a given night, skip dose and resume following night. After taking, advise patient to limit activity to preparing to go to bed.
Pedi: Teach parents or caregivers to calculate and measure doses accurately. Reinforce importance of using measuring device supplied by pharmacy or with product, not household items.
Caution patient tasimelteon can impair performance of activities requiring complete mental alertness. Advise patient to avoid driving and other activities requiring alertness after taking tasimelteon.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes ⬆ ⬇

Improved circadian rhythm with improved sleep/wake patterns. Due to differences in circadian rhythms, may require daily use for several wk or mo before benefit from tasimelteon is noticeable.

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Pronunciation ⬇

Classifications ⬆ ⬇