tasimelteon

REMS

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

Contraind./Precautions

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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.

Adv. Reactions/Side Effects

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CNS: headache, nightmares/unusual dreams

GI: ↑liver enzymes

Interactions

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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.

Availability

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Route/Dosage

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

US Brand Names

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Action

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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.

Classifications

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Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: melatonin receptor agonists

Pharmacokinetics

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Absorption: 38% absorbed following oral administration, blood levels are ↑ in female patients.

Distribution: Unknown.

Metabolism/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

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(establishment of circadian rhythm/sleep cycle)

ROUTE	ONSET	PEAK	DURATION
PO	wks-mos	unknown	unknown

Patient/Family Teaching

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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

Pronunciation

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Code

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NDC Code

43068- Vanda Pharmaceuticals Inc.
- 43068-220- Hetlioz
  - 43068-220-01- 30 CAPSULE in 1 BOTTLE (43068-220-01)

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Classifications ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

Code ⬆

Indications