Dosing & Uses
Dosage Forms & Strengths
capsule
- 20mg
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
Smith-Magenis Syndrome (Orphan)
Orphan designation to improve sleep in patients with Smith-Magenis syndrome (SMS)
Orphan sponsor
- Vanda Pharmaceuticals Inc
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Headache (17%)
1-10%
Increased ALT (10%)
Nightmares/abnormal dreams (10%)
Upper respiratory infections (7%)
Urinary tract infections (7%)
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
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.
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
Administration
Oral Administration
Take on empty stomach without food
Limit activity to preparing for going to bed following administration
Images
Patient Handout
Formulary
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