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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              Serious - Use Alternative (23)

              • abametapir

                abametapir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

                abametapir will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP1A2 substrates. If not feasible, avoid use of abametapir.

              • amobarbital

                amobarbital will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • apalutamide

                apalutamide will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

              • benzhydrocodone/acetaminophen

                benzhydrocodone/acetaminophen, tasimelteon. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • fentanyl

                fentanyl, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.

              • fentanyl intranasal

                fentanyl intranasal, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.

              • fentanyl transdermal

                fentanyl transdermal, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.

              • fentanyl transmucosal

                fentanyl transmucosal, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.

              • fexinidazole

                fexinidazole will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

              • givosiran

                givosiran will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP1A2 substrates with givosiran. If unavoidable, decrease the CYP1A2 substrate dosage in accordance with approved product labeling.

              • hydrocodone

                hydrocodone, tasimelteon. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • idelalisib

                idelalisib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

              • ivosidenib

                ivosidenib will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

              • lemborexant

                lemborexant, tasimelteon. Either increases effects of the other by sedation. Avoid or Use Alternate Drug. Use of lemborexant with other drugs to treat insomnia is not recommended.

              • lonafarnib

                lonafarnib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

              • metoclopramide intranasal

                tasimelteon, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

              • oxycodone

                tasimelteon and oxycodone both increase sedation. Avoid or Use Alternate Drug. Additive CNS depression may lead to hypotension, profound sedation, respiratory depression, or coma

              • secobarbital

                secobarbital will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • selinexor

                selinexor, tasimelteon. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.

              • sufentanil SL

                sufentanil SL, tasimelteon. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may result in hypotension, profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • tucatinib

                tucatinib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

              • valerian

                valerian and tasimelteon both increase sedation. Avoid or Use Alternate Drug.

              • voxelotor

                voxelotor will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

              Monitor Closely (75)

              • atazanavir

                atazanavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • bosentan

                bosentan will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • brexanolone

                brexanolone, tasimelteon. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buprenorphine, long-acting injection

                tasimelteon increases toxicity of buprenorphine, long-acting injection by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of buprenorphine and benzodiazepines or other CNS depressants increases risk of adverse reactions including overdose, respiratory depression, and death. Cessation of benzodiazepines or other CNS depressants is preferred in most cases. In some cases, monitoring at a higher level of care for tapering CNS depressants may be appropriate. In others, gradually tapering a patient off of a prescribed benzodiazepine or other CNS depressant or decreasing to the lowest effective dose may be appropriate.

              • cannabidiol

                cannabidiol, tasimelteon. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Owing to the potential for both CYP1A2 induction and inhibition with the coadministration of CYP1A2 substrates and cannabidiol, consider reducing dosage adjustment of CYP1A2 substrates as clinically appropriate.

              • carbamazepine

                carbamazepine will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • cenobamate

                cenobamate will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

                cenobamate, tasimelteon. Either increases effects of the other by sedation. Use Caution/Monitor.

              • chloramphenicol

                chloramphenicol will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • cigarette smoking

                cigarette smoking will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Tasimelteon exposure in smokers was lower (~40%) than in nonsmokers

              • ciprofloxacin

                ciprofloxacin will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Avoid coadministration; potentially large increase in tasimelteon exposure and greater risk of adverse reactions with strong CYP1A2 inhibitors

              • clarithromycin

                clarithromycin will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • conivaptan

                conivaptan will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • dabrafenib

                dabrafenib will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • darunavir

                darunavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • deutetrabenazine

                tasimelteon and deutetrabenazine both increase sedation. Use Caution/Monitor.

              • dexamethasone

                dexamethasone will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • diazepam intranasal

                diazepam intranasal, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may potentiate the CNS-depressant effects of each drug.

              • efavirenz

                efavirenz will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • elagolix

                elagolix decreases levels of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

              • elvitegravir/cobicistat/emtricitabine/tenofovir DF

                elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • encorafenib

                encorafenib, tasimelteon. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

              • enzalutamide

                enzalutamide will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • esketamine intranasal

                esketamine intranasal, tasimelteon. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.

              • eslicarbazepine acetate

                eslicarbazepine acetate will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • ethanol

                ethanol and tasimelteon both increase sedation. Use Caution/Monitor.

              • etravirine

                etravirine will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • fedratinib

                fedratinib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

              • fexinidazole

                fexinidazole will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              • flibanserin

                tasimelteon and flibanserin both increase sedation. Modify Therapy/Monitor Closely. Risk for sedation increased if flibanserin is coadministration with other CNS depressants.

              • fluvoxamine

                fluvoxamine will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. May increase adverse effects

              • fosamprenavir

                fosamprenavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • gabapentin

                gabapentin, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • gabapentin enacarbil

                gabapentin enacarbil, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • imatinib

                imatinib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • indinavir

                indinavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • isoniazid

                isoniazid will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • istradefylline

                istradefylline will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

              • itraconazole

                itraconazole will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ketoconazole

                ketoconazole will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • lasmiditan

                lasmiditan, tasimelteon. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.

              • lopinavir

                lopinavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • lorlatinib

                lorlatinib will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • methoxsalen

                methoxsalen will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Avoid coadministration; potentially large increase in tasimelteon exposure and greater risk of adverse reactions with strong CYP1A2 inhibitors

              • mexiletine

                mexiletine will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Avoid coadministration; potentially large increase in tasimelteon exposure and greater risk of adverse reactions with strong CYP1A2 inhibitors

              • midazolam intranasal

                midazolam intranasal, tasimelteon. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.

              • mifepristone

                mifepristone will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • mitotane

                mitotane will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • nefazodone

                nefazodone will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nelfinavir

                nelfinavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nevirapine

                nevirapine will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • nicardipine

                nicardipine will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ofloxacin

                ofloxacin will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Avoid coadministration; potentially large increase in tasimelteon exposure and greater risk of adverse reactions with strong CYP1A2 inhibitors

              • oliceridine

                oliceridine, tasimelteon. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • oxcarbazepine

                oxcarbazepine will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • pentobarbital

                pentobarbital will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • phenobarbital

                phenobarbital will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • phenytoin

                phenytoin will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • posaconazole

                posaconazole will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • pregabalin

                pregabalin, tasimelteon. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • primaquine

                primaquine will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Avoid coadministration; potentially large increase in tasimelteon exposure and greater risk of adverse reactions with strong CYP1A2 inhibitors

              • primidone

                primidone will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • quinidine

                quinidine will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • remimazolam

                remimazolam, tasimelteon. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.

              • rifabutin

                rifabutin will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • rifampin

                rifampin will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • rifapentine

                rifapentine will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid coadministration of tasimelteon with strong CYP3A4 inducers

              • ritonavir

                ritonavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • rucaparib

                rucaparib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • saquinavir

                saquinavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • stiripentol

                stiripentol, tasimelteon. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP1A2 inhibitor and inducer. Monitor CYP1A2 substrates coadministered with stiripentol for increased or decreased effects. CYP1A2 substrates may require dosage adjustment.

                stiripentol, tasimelteon. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

                stiripentol, tasimelteon. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.

              • tazemetostat

                tazemetostat will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • tecovirimat

                tecovirimat will decrease the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

              • tipranavir

                tipranavir will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • voriconazole

                voriconazole will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              Minor (1)

              • ribociclib

                ribociclib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

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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

              No images available for this drug.
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              Patient Handout

              Patient Education
              tasimelteon oral

              TASIMELTEON - ORAL

              (TAS-i-MEL-tee-on)

              COMMON BRAND NAME(S): Hetlioz

              USES: Tasimelteon is used to treat certain sleep disorders (non-24-hour sleep-wake disorder, sleep disturbances in Smith-Magenis Syndrome). It works like a natural substance called melatonin that your body produces. It helps to control your sleep-wake cycle (circadian rhythm). Tasimelteon may improve your ability to sleep at night and to be more active during the day.

              HOW TO USE: Take this medication by mouth on an empty stomach as directed by your doctor, usually one hour before bedtime, at the same time every night. The dosage is based on your medical condition and response to treatment. Children's dose is also based on weight. If you are using the capsule form, swallow the capsules whole.If you are using the liquid form of this medication, read the Instructions for Use Leaflet if available from your pharmacist before you start using tasimelteon suspension and each time you get a refill. Shake the bottle well for at least 30 seconds before each dose. Carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose. If you have any questions, ask your doctor or pharmacist.It is very important to take this medication at the same time each night so that you can form a normal sleep-wake cycle. See also Missed Dose section.It may take up to several months before you get the full benefit of this drug.Tell your doctor if your condition does not get better or if it gets worse.

              SIDE EFFECTS: Headache, nightmares, or strange dreams may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. Tasimelteon may also make you drowsy during the day. Talk to your doctor or pharmacist if you have daytime drowsiness.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking tasimelteon, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease.This drug may make you drowsy. Alcohol or marijuana (cannabis) can make you more drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Liquid products may contain sugar and/or aspartame. Caution is advised if you have diabetes, phenylketonuria (PKU), or any other condition that requires you to limit/avoid these substances in your diet. Ask your doctor or pharmacist about using this product safely.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Other medications can affect the removal of tasimelteon from your body, which may affect how tasimelteon works. Examples include ciprofloxacin, fluvoxamine, rifamycins (such as rifabutin), St. John's wort, drugs used to treat seizures (such as carbamazepine, phenytoin), viloxazine, among others.Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), other drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.Cigarette smoking decreases blood levels of this medication. Tell your doctor if you smoke or if you have recently stopped smoking.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Do not share this medication with others.

              MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store the capsules at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Store the liquid form of this medication in a refrigerator. After opening, discard after 5 weeks (for the 48 milliliter bottle) or after 8 weeks (for the 158 milliliter bottle).Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

              To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

              Adding plans allows you to:

              • View the formulary and any restrictions for each plan.
              • Manage and view all your plans together – even plans in different states.
              • Compare formulary status to other drugs in the same class.
              • Access your plan list on any device – mobile or desktop.

              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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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.