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tasimelteon

General

Pronunciation:
tas-i-mel-tee-on


Trade Name(s)

  • Hetlioz

Ther. Class.
sedative/hypnotics

Pharm. Class.
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 Effect(s):

Improved circadian rhythm with improved sleep/wake patterns.

Pharmacokinetics

Absorption: 38% absorbed following 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

Contraindication/Precautions

Contraindicated in:

  • Severe hepatic impairment.

Use Cautiously in:

  • Concurrent use of strong CYP1A2 inducers/inhibitors (may alter drug effects)
  • Geri: ↑ risk of adverse reactions due to ↑ blood levels;
  • OB: May cause fetal harm, use only if potential benefit justifies potential fetal risk;
  • Lactation:Use cautiously if breastfeeding;
  • Pedi: Safety and effectiveness not established.

Adverse Reactions/Side Effects

CNS: headache, nightmares/unusual dreams

GI: ↑ liver enzymes

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

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

Route/Dosage

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

Availability

Capsules: 20 mg

Assessment

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

Lab Test Considerations:

May cause ↑ transaminases.

Potential Diagnoses

Implementation

  • PO: 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.

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Citation

Quiring, Courtney, et al. "Tasimelteon." Davis's Drug Guide, 16th ed., F.A. Davis Company, 2019. Emergency Central, emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110106/all/tasimelteon.
Quiring C, Sanoski CA, Vallerand AH. Tasimelteon. Davis's Drug Guide. 16th ed. F.A. Davis Company; 2019. https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110106/all/tasimelteon. Accessed April 21, 2019.
Quiring, C., Sanoski, C. A., & Vallerand, A. H. (2019). Tasimelteon. In Davis's Drug Guide. Available from https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110106/all/tasimelteon
Quiring C, Sanoski CA, Vallerand AH. Tasimelteon [Internet]. In: Davis's Drug Guide. F.A. Davis Company; 2019. [cited 2019 April 21]. Available from: https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110106/all/tasimelteon.
* Article titles in AMA citation format should be in sentence-case
TY - ELEC T1 - tasimelteon ID - 110106 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110106/all/tasimelteon PB - F.A. Davis Company ET - 16 DB - Emergency Central DP - Unbound Medicine ER -