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tasimelteon (Rx)Brand and Other Names:Hetlioz

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 20mg
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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

Dosage Modifications

Renal impairment (all stages): No dosage adjustment necessary

Hepatic impairment

  • Mild or moderate: No dosage adjustment necessary
  • Severe (Child-Pugh C): Not studied; use not recommended

Dosing Considerations

Because of individual differences in circadian rhythms, drug effect may not occur for weeks or months

Administration

Take on empty stomach without food

Limit activity to preparing for going to bed following administration

Safety and efficacy not established

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Interactions

Interaction Checker

tasimelteon and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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%)

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            Warnings

            Contraindications

            None

            Cautions

            Somnolence; can impair performance of activities requiring complete mental alertness

            Tasimelteon is a CYP1A2 substrate; avoid coadministration with strong CYP1A2 inhibitors because of a potentially large increase in tasimelteon exposure and greater risk of adverse reactions

            Smoking causes induction of CYP1A2 levels; tasimelteon exposure in smokers was lower (~40%) than in nonsmokers and therefore the efficacy may be reduced

            Tasimelteon is a CYP3A4 substrate: avoid coadministration with CYP3A4 inducers because of a potentially large decrease in tasimelteon exposure with reduced efficacy

            Risk of adverse reactions may be greater in elderly (>65 years) patients than younger patients because exposure to tasimelteon is increased by approximately 2-fold

            In clinical trials, coadministration with alcohol showed a trend toward additive sedation

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Unknown if distributed in human breast milk

            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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            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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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