Peringatan Keamanan

The most common adverse reactions are headache, increased alanine aminotransferase, nightmares or unusual dreams, and upper respiratory or urinary tract infections. There are currently no adequate or well-controlled studies that suggest that tasimelteon is safe to use during pregnancy. In animal studies, administration of tasimelteon during pregnancy resulted in developmental toxicity (embryofetal mortality, neurobehavioral impairment, and decreased growth and development in offspring) at doses greater than those used clinically. During clinical trials, rats did not self-administer tasimelteon, suggesting that the drug does not have a potential for abuse.

Tasimelteon

DB09071

small molecule approved investigational

Deskripsi

Tasimelteon is a selective dual melatonin receptor agonist indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (N24HSWD). Occurring commonly in blind individuals without light perception, this condition is often characterized by periods of night-time insomnia and day-time sleepiness. In blind individuals, a lack of light stimulation causes an extension of the 24-hour circadian cycle and can lead to progressively delayed sleep onset. By activating melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, tasimelteon has been shown to improve sleep by resynchronizing the circadian rhythm through its "non-photic" mechanism. Tasimelteon is currently the only drug available for the treatment of N24HSWD and was granted orphan drug status by the FDA in 2010.

Struktur Molekul 2D

Berat 245.322
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The observed mean elimination half-life for tasimelteon is 1.3 ± 0.4 hours.
Volume Distribusi The apparent oral volume of distribution of tasimelteon at steady state in young healthy subjects is approximately 56 - 126 L.
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Tasimelteon is extensively metabolized. Metabolism of tasimelteon consists primarily of 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 in the metabolism of tasimelteon. Phenolic glucuronidation is the major phase II metabolic route.

Rute Eliminasi

Following oral administration of radiolabeled tasimelteon, 80% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 84%. Less than 1% of the dose was excreted in urine as the parent compound.

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of tasimelteon, which may increase its serum concentration. Alternatively, the dose of tasimelteon may need to be modified.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of tasimelteon and may reduce its serum concentration. Alternatively, the dose of tasimelteon may need to be modified.
  • 3. Take on an empty stomach. The Cmax of tasimelteon is reduced when taken with food.

Interaksi Obat

1762 Data
Phenytoin The metabolism of Tasimelteon can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Tasimelteon can be increased when combined with Fosphenytoin.
Deferasirox The serum concentration of Tasimelteon can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Tasimelteon can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Tasimelteon can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Tasimelteon can be decreased when it is combined with Teriflunomide.
Buprenorphine Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Hydrocodone Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Magnesium sulfate The therapeutic efficacy of Tasimelteon can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Tasimelteon may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Mirtazapine Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Orphenadrine Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Pramipexole Tasimelteon may increase the sedative activities of Pramipexole.
Ropinirole Tasimelteon may increase the sedative activities of Ropinirole.
Rotigotine Tasimelteon may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Tasimelteon.
Suvorexant Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Thalidomide Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Tasimelteon.
Sodium oxybate Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Cyproterone acetate The metabolism of Tasimelteon can be increased when combined with Cyproterone acetate.
Ethanol Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Tasimelteon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Citalopram The risk or severity of adverse effects can be increased when Tasimelteon is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Tasimelteon is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Tasimelteon is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Tasimelteon is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Tasimelteon is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Seproxetine.
Levomilnacipran Levomilnacipran may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Indalpine The risk or severity of adverse effects can be increased when Tasimelteon is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Tasimelteon is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Tasimelteon is combined with Alaproclate.
Benzatropine Benzatropine may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Tasimelteon.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Tasimelteon.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Tasimelteon.
Propantheline Propantheline may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Tasimelteon.
Tolterodine Tolterodine may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Flavoxate Flavoxate may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Tiotropium Tiotropium may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Tasimelteon.
Fesoterodine Fesoterodine may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Aclidinium Aclidinium may decrease the excretion rate of Tasimelteon which could result in a higher serum level.
Trimebutine Tasimelteon may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Dosulepin The risk or severity of CNS depression can be increased when Tasimelteon is combined with Dosulepin.
Imidafenacin Tasimelteon may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Tasimelteon may decrease the excretion rate of Propiverine which could result in a higher serum level.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Tasimelteon.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Tasimelteon.
Imipramine The metabolism of Tasimelteon can be decreased when combined with Imipramine.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Tasimelteon.
Clozapine The metabolism of Tasimelteon can be decreased when combined with Clozapine.
Zopiclone The risk or severity of adverse effects can be increased when Tasimelteon is combined with Zopiclone.
Bexarotene The metabolism of Tasimelteon can be increased when combined with Bexarotene.
Bosentan The metabolism of Tasimelteon can be increased when combined with Bosentan.
Nafcillin The metabolism of Tasimelteon can be increased when combined with Nafcillin.
Modafinil The metabolism of Tasimelteon can be increased when combined with Modafinil.
Etravirine The metabolism of Tasimelteon can be increased when combined with Etravirine.
Avasimibe The metabolism of Tasimelteon can be increased when combined with Avasimibe.
Echinacea The metabolism of Tasimelteon can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Tasimelteon can be increased when combined with Dexamethasone acetate.
Albendazole The metabolism of Tasimelteon can be increased when combined with Albendazole.
Caffeine The metabolism of Tasimelteon can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Tasimelteon can be decreased when combined with Moxifloxacin.
Lidocaine The metabolism of Tasimelteon can be decreased when combined with Lidocaine.
Mexiletine The metabolism of Tasimelteon can be decreased when combined with Mexiletine.
Alosetron The metabolism of Tasimelteon can be decreased when combined with Alosetron.
Gatifloxacin The metabolism of Tasimelteon can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Tasimelteon can be decreased when combined with Simeprevir.
Lobeglitazone The metabolism of Tasimelteon can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Tasimelteon can be decreased when combined with Pazufloxacin.
Osilodrostat The metabolism of Tasimelteon can be decreased when combined with Osilodrostat.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Tasimelteon.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Tasimelteon.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Tasimelteon.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Tasimelteon.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Tasimelteon.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Tasimelteon.

Target Protein

Melatonin receptor type 1A MTNR1A
Melatonin receptor type 1B MTNR1B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25534555
    Lavedan C, Forsberg M, Gentile AJ: Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology. 2015 Apr;91:142-7. doi: 10.1016/j.neuropharm.2014.12.004. Epub 2014 Dec 19.
  • PMID: 25685859
    Neubauer DN: Tasimelteon for the treatment of non-24-hour sleep-wake disorder. Drugs Today (Barc). 2015 Jan;51(1):29-35. doi: 10.1358/dot.2015.51.1.2258364.
  • PMID: 25422900
    Stahl SM: Mechanism of action of tasimelteon in non-24 sleep-wake syndrome: treatment for a circadian rhythm disorder in blind patients. CNS Spectr. 2014 Dec;19(6):475-8. doi: 10.1017/S1092852914000637.
  • PMID: 12661062
    Vachharajani NN, Yeleswaram K, Boulton DW: Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist. J Pharm Sci. 2003 Apr;92(4):760-72.

Contoh Produk & Brand

Produk: 6 • International brands: 1
Produk
  • Hetlioz
    Capsule • 20 mg/1 • Oral • US • Approved
  • Hetlioz
    Capsule • 20 mg • Oral • EU • Approved
  • Hetlioz LQ
    Suspension • 4 mg/1mL • Oral • US • Approved
  • Tasimelteon
    Capsule, gelatin coated • 20 mg/1 • Oral • US • Generic • Approved
  • Tasimelteon
    Capsule • 20 mg/1 • Oral • US • Generic • Approved
  • Tasimelteon
    Capsule • 20 mg/1 • Oral • US • Generic • Approved
International Brands
  • Hetlioz

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