Tasimelteon
HETLIOZ
Pronunciation: tas-i-MEL-tee-on
“Tassel melty on Heater”
for non-24-hour sleep-wake disorder
What it isMT1 and MT2 melatonin receptor agonist; non-24-hour sleep-wake disorder in blind patients.
Why this oneIt entrains the circadian clock in people with no light perception, which nothing else does.
What limits itEntrainment takes weeks to months. CYP1A2 and CYP3A4 dependent; avoid with fluvoxamine.
FDA-approved for
- non-24-hour sleep-wake disorder (2014)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Non-24-hour sleep-wake disorder | Adults (capsules) | 20 mg QHS | 20 mg QHS | 20 mg QHS |
| Nighttime sleep disturbances in Smith-Magenis syndrome | ≥16 yr (capsules) | 20 mg QHS | 20 mg QHS | 20 mg QHS |
| Nighttime sleep disturbances in Smith-Magenis syndrome, ≤28 kg | Pediatric 3-15 yr (oral suspension) | 0.7 mg/kg QHS | 0.7 mg/kg QHS | 0.7 mg/kg QHS |
| Nighttime sleep disturbances in Smith-Magenis syndrome, >28 kg | Pediatric 3-15 yr (oral suspension) | 20 mg QHS | 20 mg QHS | 20 mg QHS |
Renal Undefined
Hepatic Severe: not studied, not recommended
Instructions
- Take one hour before bedtime, at the same time every night
- Take without food
- Capsules and LQ oral suspension are not substitutable
- If unable to take at about the same time, skip that dose and take next as scheduled
- Non-24: drug effect may take weeks to months
Available strengths
- cap 20 mg
- susp 4 mg/mL
Cautions
- Somnolence — after dosing, limit activity to preparing for bed; impairs mental-alertness tasks
Adverse reactions
- Headache
- Increased ALT
- Nightmares/unusual dreams
- Upper respiratory tract infection
- Urinary tract infection
Pregnancy Insufficient human data; no embryofetal toxicity in rats at tested exposures
Lactation No human or animal milk data
Cost
| Strength | #/mo | generic $ | CostPlus | |
|---|---|---|---|---|
| 20 mg | cap | 30 qd | $6,847.44/mo | offered |
| 4 mg/mL | susp | per unit | not offered |
Generic entry2022
NO BOXED WARNINGS
Principal riskEntrainment takes weeks to months
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySomnolence, headache and hepatic enzyme elevations; acute toxicity is generally limited.
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