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 ?
Food and Drug Administration (FDA) as part of its ongoing review of Vanda's supplemental New Drug Application (sNDA) for HETLIOZ (tasimelteon) for the treatment of Jet Lag Disorder (JLD).
Vanda Pharmaceuticals FDA Update for HETLIOZ in the Treatment of Jet Lag Disorder
Vanda Pharmaceuticals Inc (Nasdaq:VNDA) said on Thursday that it has submitted its Supplemental New Drug Application for HETLIOZ (tasimelteon) with the US Food and Drug Administration (FDA) for the treatment of jet lag disorder.
Vanda Pharmaceuticals Inc announces US FDA's action target date for HETLIOZ
BALTIMORE -- Tasimelteon, a drug approved for non-24-hour sleep-wake disorder, has been shown to increase sleep times in travelers with jet lag, according to results from a phase 3 trial.
Phase 3 trial: Tasimelteon effective for jet lag disorder
(Vanda) announced results from the JET Study (VP-VEC-162-2102), a 3-night transatlantic travel study of the effects of tasimelteon on Jet Lag Disorder.
United Kingdom : HETLIOZ (tasimelteon) Effective in Treating Jet Lag during Transatlantic Travel
In January 2014, the US Food and Drug Administration (FDA) approved Hetlioz (tasimelteon), a melatonin receptor agonist, for the treatment of non-24.
Another drug that we don't need and can't afford
"Melatonin receptor agonists" (analogues of melatonin designed to bind to melatonin receptors with a greater potency than melatonin itself), such as the drug tasimelteon, have been investigated in the treatment of circadian rhythm disorders.
Retinal disorders and sleep disorders: are they genetically related?
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.
Commentary: New drugs in 2014 and pregnancy, lactation data
Suvorexant (Belsomra) and tasimelteon (Hetlioz) are oral drugs given for treatment of insomnia and the treatment of non-24-hour sleep-wake disorder, respectively.
Year in review: drug use in pregnant and breastfeeding women
An exception is two melatonin antagonists, approved by the Food and Drug Administration, Rozerem and Tasimelteon, strictly used for insomnia (23, 24, 25).
Chronobiology perspectives in psychiatry/Perspective ale cronobiologiei in psihiatrie
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).
Perioperative melatonin use
'Tasimelteon' works by shifting the natural ebb and flow of the body's sleep hormone melatonin and resetting the body's natural sleep rhythms.
Body matters
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.
Jet setters and shift workers worldwide may benefit from an experimental pill developed by Vanda Pharmaceuticals Inc (Rockville MD) that may reset the body's internal clock and improve sleep quality
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