tasimelteon
tasimelteon
(tas-i-mel-tee-on),Hetlioz
(trade name)Classification
Therapeutic: sedative hypnoticsPharmacologic: melatonin receptor agonists
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)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | wks-mos | unknown | unknown |
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.
Drug Guide, © 2015 Farlex and Partners