tasimelteon (Rx)

Brand and Other Names:Hetlioz
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 20mg (Hetlioz)

Non-24-Hour Disorder

Indicated for the treatment of non-24-hour sleep-wake disorder in totally blind

20 mg PO per day taken before bedtime, at the same time every night

Smith-Magenis Syndrome

Indicated for nighttime sleep disturbances in Smith-Magenis syndrome (SMS)

Capsule: 20 mg PO 1 hr before bedtime, at same time qPM

Dosage Modifications

Renal impairment

  • All severities: No dosage adjustment necessary

Hepatic impairment

  • Mild-to-moderate (Child-Pugh Class A to B): No dosage adjustment necessary
  • Severe (Child-Pugh Class C): Not studied

Dosing Considerations

Capsules and oral suspension are not interchangeable

Non-24-Hour disorder

  • Owing to individual differences in circadian rhythms, drug effect may not occur for weeks or months

Dosage Forms & Strengths

capsule

  • 20mg (Hetlioz)

oral suspension

  • 4mg/mL (Hetlioz Lq)

Smith-Magenis Syndrome

Capsule

  • Indicated for nighttime sleep disturbances in Smith-Magenis syndrome (SMS) in patients aged ≥16 years
  • 20 mg PO 1 hr before bedtime, at same time qPM

Oral suspension

  • Indicated for nighttime sleep disturbances in SMS in pediatric patients aged 3-15 years
  • <3 years: No data available
  • 3-15 years
    • ≤28 kg: 0.7 mg/kg PO 1 hr before bedtime
    • >28 kg: 20 mg PO 1 hr before bedtime

Dosage Modifications

Renal impairment

  • All severities: No dosage adjustment necessary

Hepatic impairment

  • Mild-to-moderate (Child-Pugh Class A to B): No dosage adjustment necessary
  • Severe (Child-Pugh Class C): Not studied

Dosing Considerations

Capsules and oral suspension are not interchangeable

In patients >65 years, tasimelteon exposure increased by ~2-fold compared with younger adults

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Interactions

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            Adverse Effects

            >10%

            Headache (17%)

            1-10%

            Increased ALT (10%)

            Nightmares/abnormal dreams (10%)

            Upper respiratory infections (7%)

            Urinary tract infections (7%)

            Postmarketing Reports

            Nighttime Sleep Disturbances in Smith-Magenis Syndrome (SMS)

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            Warnings

            Contraindications

            None

            Cautions

            After administration, advise patients to limit activity to prepare for going to bed

            May potentially impair performance of activities requiring complete mental alertness

            Drug interaction overview

            • Tasimelteon is a CYP3A4 and CYP1A2 substrate
            • Smokers
              • Smoking is a moderate CYP1A2 inducer
              • Tasimelteon exposure decreased by ~40% in smokers compared with nonsmokers
            • Strong CYP1A2 Inhibitors
              • Avoid coadministration
              • Fluvoxamine or other strong CYP1A2 inhibitors may potentially increase tasimelteon exposure and increase risk of adverse reactions
            • Strong CYP3A4 inducers
              • Avoid coadministration
              • Rifampin or other CYP3A4 inducers may potentially decrease tasimelteon exposure and reduced efficacy
            • Beta-adrenergic receptor antagonists
              • Beta-adrenergic receptor antagonists have been shown to reduce production of melatonin via specific inhibition of beta-1 adrenergic receptors
              • Nighttime administration of beta-adrenergic receptor antagonists may reduce tasimelteon efficacy
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            Pregnancy & Lactation

            Pregnancy

            Available postmarketing case reports use in pregnant females are not sufficient to evaluate drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes

            Animal data

            • In pregnant rats, no embryofetal developmental toxicity was observed at exposures of 50 mg/kg/day, or up to 24x higher than the human exposure at the maximum recommended human dose

            Lactation

            No data available on drug presence or its metabolites in human or animal milk, effects on breastfed infants, effects on milk production

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Melatonin receptor agonist with high affinity for MT1 and MT2 receptors in the suprachiasmatic nucleus of the brain; MT1 and MT2 are thought to synchronize the body's melatonin and cortisol circadian rhythms with the day-night cycle in patients with non-24-hour disorder

            Absorption

            Peak plasma concentration: 0.5-3 hr (fasting)

            When administered with a high-fat meal, peak plasma concentration was 44% lower than when given in a fasted state, and the median peak concentration was delayed by approximately 1.75 hr

            Oral bioavailability: 38.3%

            Distribution

            Protein bound: 96%

            Vd: 59-126 L

            Metabolism

            Extensively metabolized primarily by oxidation at multiple sites and oxidative dealkylation resulting in opening of the dihydrofuran ring followed by further oxidation to give a carboxylic acid

            CYP1A2 and CYP3A4 are the major isozymes involved

            Phenolic glucuronidation is the major phase II metabolic route

            Major metabolites had 13-fold or less activity at melatonin receptors compared to tasimelteon

            Elimination

            Half-life: 1.3 hr; 1.3-3.7 hr (metabolites)

            Excretion: 80% urine (<1% as parent compound); 4% feces

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            Administration

            Oral Administration

            All formulations

            • Administer without food
            • If unable to take dose at approximately the same time on a given night, skip that dose and take next dose as scheduled

            Capsules

            • Swallow capsules whole

            Oral suspension

            • Shake well for at least 30 seconds before administration
            • Remove seal and insert press-in bottle adapter (included in packaging) until tightly sealed
            • Turn upside down and withdraw prescribed dose with oral syringe

            Storage

            Capsules

            • Store at room temperature, 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)
            • Protect from exposure to light and moisture

            Oral suspension

            • Unopened bottle: Refrigerate at 5ºC (41ºF), excursions permitted to 2-8ºC (36-46ºF)
            Opened bottle
            • Refrigerate at 5ºC (41ºF), excursions permitted to 2-8ºC (36-46ºF)
            • After opening, discard after 5 weeks (for 48-mL bottle) and after 8 weeks (for 158-mL bottle)
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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.