tasimelteon

tasimelteon

(tas-i-mel-tee-on),

Hetlioz

(trade name)

Classification

Therapeutic: sedative hypnotics
Pharmacologic: melatonin receptor agonists
Pregnancy Category: C

Indications

Treatment of non-24–Hour Sleep-Wake Disorder (a circadian rhythm disorder more common in totally blind patients).

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: Systemic absorption follows oral administration, blood levels are ↑ in female patients.
Distribution: Unknown.
Metabolism and Excretion: Extensively metabolized mostly by CYP1A2 and also CYP3A4, metabolited do not contribute significantly to pharmacological effect. Metabolites are primarily excreted in urine, less than 1% as unchanged drug), 4% excreted in feces.
Half-life: 1.3 hr.

Time/action profile (establishment of circadian rhythm/sleep cycle)

ROUTEONSETPEAKDURATION
POwks-mosunknownunknown

Contraindications/Precautions

Contraindicated in: Severe hepatic impairment.
Use Cautiously in: Concurrent use of strong inducers/inhibitors of CYP1A2 (may alter drug effects); Geriatric: ↑ risk of adverse reactions in patients > 65 yr (↑ blood levels); Obstetric: May cause fetal harm, use only if potential benefit justifies potential fetal risk; Lactation: use cautiously if breastfeeding;Safe and effective use in children has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • headache
  • nightmares/unusual dreams

Gastrointestinal

  • ↑ liver enzymes

Interactions

Drug-Drug interaction

Concurrent use of strong inhibitors of CYP1A2 including fluvoxamine may ↑ drug effects).Concurrent use of strong inducersof CYP1A2 including rifampin and cigarette smoke may ↓ drug effects.Strong inhibitors of CYP3A4, including ketoconazole may ↑ blood levels and effects.Alcohol may ↑ CNS depression.

Route/Dosage

Oral (Adults) 20 mg at bedtime, taken at the same time every day.

Availability

Capsules: 20 mg

Nursing implications

Nursing assessment

  • Assess mental status, sleep patterns, and frequency of daytime naps prior and periodically during therapy.
  • Lab Test Considerations: May cause ↑ transaminases.

Potential Nursing Diagnoses

Readiness for enhanced sleep (Indications)

Implementation

  • Oral: Administer without food before bedtime at the same time each night. Swallow capsule whole; do not open, dissolve, crush, or chew.

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.
  • 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.
  • Advise female patient 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 wks or mo before benefit from tasimelteon is noticeable.
References in periodicals archive ?
Tasimelteon was shown to improve sleep initiation and maintenance in individuals with no light perception in the human trials named Safety and Efficacy of Tasimelteon (SET) and Randomized Withdrawal Study of the Efficacy and Safety of Tasimelteon (RESET) (Johnsa & Neville, 2014; Lankford, 2011).
The approval was based on data from the Hetlioz clinical development program, which included two pivotal Phase III clinical trials, Safety and Efficacy of Tasimelteon (SET) and Randomised-withdrawal study of the Efficacy and Safety of Tasimelteon to treat Non-24 (RESET).
Suvorexant (Belsomra) and tasimelteon (Hetlioz) are oral drugs given for treatment of insomnia and the treatment of non-24-hour sleep-wake disorder, respectively.
Suvorexant (Belsomra) and tasimelteon (Hetlioz) are oral drugs given for the treatment of insomnia and the treatment of non-24-hour sleep-wake disorder, respectively.
An exception is two melatonin antagonists, approved by the Food and Drug Administration, Rozerem and Tasimelteon, strictly used for insomnia (23, 24, 25).
Food and Drug Administration has approved tasimelteon (Hetlioz) for sleep disturbances in the blind.
Tasimelteon, also a selective MT1 and MT2 agonist, is undergoing phase III trials for insomnia (36) and agomelatine, an MT1/MT2 agonist and 5HT2c antagonist, is being evaluated as an antidepressant/anxiolytic drug (37).
Two company-funded studies found people who went to bed five hours earlier than normal fell asleep faster and spent less time tossing and turning when given tasimelteon rather than a placebo.
Experts from Harvard Medical School in the US and Monash University in Australia have found that the drug tasimelteon made it easier for volunteers to get to sleep, and helped them stay asleep for longer, after their sleeping pattern was disrupted to mimic long distance travel.
This steady growth is primarily attributed to the expected launch of pipeline products in 2014 (such as Intermezzo, tasimelteon and MK-4305 in the G7 countries, the launch of SEP-190 (eszopiclone) in Japan and the launch of ramelteon in Europe).
The clinical development programme included two pivotal Phase 3 clinical trials, SET (Safety and Efficacy of Tasimelteon) and RESET (Randomized-withdrawal study of the Efficacy and Safety of Tasimelteon to treat Non-24).
To reduce the risk of decreased mental alertness, patients should take tasimelteon at the same time every night before bedtime and limit activities after taking the drug, according to the agency.