tasimelteon

(redirected from Hetlioz)

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 ?
HETLIOZ is currently approved in the US and Europe for the treatment of Non-24-hour sleep-wake disorder, a rare and chronic circadian rhythm sleep disorder.
An FDA spokesman, responding to an information request from Pharmaceutical Processing, said that the agency "would be open to reviewing braille labeling on a drug product if a sponsor were to submit for review," pointing to the drug Hetlioz that was "previously approved by the FDA with braille labeling for brand name and strength.
In January 2014, the US Food and Drug Administration (FDA) approved Hetlioz (tasimelteon), a melatonin receptor agonist, for the treatment of non-24.
M2 PHARMA-July 9, 2015-Vanda Pharmaceuticals receives approval for Hetlioz from The European Commission
M2 EQUITYBITES-July 9, 2015-Vanda Pharmaceuticals receives approval for Hetlioz from The European Commission
Vanda expects to report 2017 total net product sales from HETLIOZ and Fanapt of approximately $165 million, consistent with Vanda's prior guidance of between $163 million and $169 million.
M2 EQUITYBITES-July 8, 2015-Vanda Pharmaceuticals awarded approval for first and only HETLIOZ for Non-24 in totally blind adults in the EU
M2 PHARMA-July 8, 2015-Vanda Pharmaceuticals awarded approval for first and only HETLIOZ for Non-24 in totally blind adults in the EU
M2 EQUITYBITES-July 3, 2015-Vanda lists new HETLIOZ patent ('995 patent) in the US FDA Orange Book
M2 PHARMA-June 5, 2014-Vanda Pharmaceuticals receives approval to evaluate Marketing Authorisation Application for oral HETLIOZ
Food and Drug Administration today approved Hetlioz (tasimelteon), a melatonin receptor agonist, to treat non-24- hour sleep-wake disorder ( non-24 ) in totally blind individuals.