Hetlioz
(tasimelteon)Dosage & Administration
| Indicated Population | Dosage Form | Body Weight | Recommended Dosage |
| Non-24 | |||
| Adults | Capsules | Not applicable | 20 mg one hour prior to bedtime |
| Nighttime sleep disturbances in SMS | |||
| Patients 16 years of age and older | Capsules | Not applicable | 20 mg one hour prior to bedtime |
| Pediatric Patients 3 to 15 years of age | Oral Suspension | ≤ 28 kg | 0.7 mg/kg one hour before bedtime |
| ≥ 28 kg | 20 mg one hour prior to bedtime | ||
By using PrescriberAI, you agree to the AI Terms of Use.
Hetlioz Prescribing Information
Non-24-Hour Sleep-Wake Disorder (Non-24)
- HETLIOZ capsules are indicated for the treatment of Non-24 in adults.
Nighttime Sleep Disturbances in Smith-Magenis Syndrome (SMS)
- HETLIOZ capsules are indicated for the treatment of nighttime sleep disturbances in SMS in patients 16 years of age and older.
- HETLIOZ LQ oral suspension is indicated for the treatment of nighttime sleep disturbances in SMS in pediatric patients 3 to 15 years of age.
Non-Interchangeability between HETLIOZ Capsules and HETLIOZ LQ Oral Suspension
HETLIOZ capsules and HETLIOZ LQ oral suspension are not substitutable [see Clinical Pharmacology ].
Recommended Dosage for HETLIOZ Capsules for Non-24
Adults
The recommended dosage of HETLIOZ capsules in adults is 20 mg one hour before bedtime, at the same time every night.
Because of individual differences in circadian rhythms, drug effect may not occur for weeks or months.
Recommended Dosage for HETLIOZ Capsules and HETLIOZ LQ Oral Suspension for Nighttime Sleep Disturbances in SMS
Patients 16 years of Age and Older
The recommended dosage of HETLIOZ capsules in patients 16 years and older is 20 mg one hour before bedtime, at the same time every night.
Pediatric Patients 3 Years to 15 Years of Age
The recommended dosage of HETLIOZ LQ oral suspension in pediatric patients 3 years to 15 years of age is based on body weight . Administer HETLIOZ one hour before bedtime, at the same time every night.
| Body Weight | Daily Dose (oral suspension) |
| ≤28 kg | 0.7 mg/kg one hour before bedtime |
| >28 kg | 20 mg one hour before bedtime |
Important Administration Information
Administer HETLIOZ capsules and HETLIOZ LQ oral suspension without food [see Clinical Pharmacology ].
If a patient is unable to take HETLIOZ at approximately the same time on a given night, they should skip that dose and take the next dose as scheduled.
HETLIOZ LQ Oral Suspension
See " Instructions for Use" for complete administration instructions.
Shake HETLIOZ LQ oral suspension well for at least 30 seconds before every administration. Remove seal and insert press-in bottle adapter (included in the package) into the neck of the bottle until a tight seal is made. Turn the bottle upside down and withdraw the prescribed amount of HETLIOZ LQ oral suspension from the bottle. Leave the press-in bottle adapter in place on bottle neck and replace cap on bottle. Store refrigerated. After opening, discard after 5 weeks (for the 48 mL bottle) and after 8 weeks (for the 158 mL bottle).
Capsules: 20 mg size 1 dark blue opaque, hard gelatin capsules printed with “VANDA 20 mg” in white.
Oral suspension: 4 mg/mL white to slightly yellow opaque suspension in 48 mL or 158 mL bottles.
Pregnancy
Risk Summary
Available postmarketing case reports with HETLIOZ use in pregnant women are not sufficient to evaluate drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In pregnant rats, no embryofetal developmental toxicity was observed at exposures of 50 mg/kg/day, or up to 24 times higher than the human exposure at the maximum recommended human dose (MRHD) (see Data).
The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Data
Animal Data
In pregnant rats administered tasimelteon at oral doses of 5, 50, or 500 mg/kg/day during the period of organogenesis, there were no effects on embryofetal development. The highest dose tested is approximately 240 times the MRHD of 20 mg/day, based on mg/m2 body surface area.
In pregnant rabbits administered tasimelteon at oral doses of 5, 30, or 200 mg/kg/day during the period of organogenesis, embryolethality and embryofetal toxicity (reduced fetal body weight and delayed ossification) were observed at the highest dose tested. The highest dose is approximately 200 times the MRHD.
Oral administration of tasimelteon at 50, 150, or 450 mg/kg/day to rats throughout organogenesis resulted in persistent reductions in body weight, delayed sexual maturation, and physical development, and neurobehavioral impairment in offspring at the highest dose tested which is approximately 220 times the MRHD based on mg/m2 body surface area. Reduced body weight in offspring was also observed at the mid-dose. The no effect dose (NOEL), (50 mg/kg/day) is approximately 25 times the MRHD based on mg/m2 body surface area.
Lactation
Risk Summary
There are no data on the presence of tasimelteon or its metabolites in human or animal milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for HETLIOZ and any potential adverse effects on the breastfed infant from HETLIOZ or from the underlying maternal condition.
Pediatric Use
Safety and effectiveness of HETLIOZ for the treatment of Non-24 in pediatric patients have not been established.
Safety and effectiveness of HETLIOZ LQ oral suspension for the treatment of nighttime sleep disturbances in Smith-Magenis Syndrome (SMS) have been established in pediatric patients 3 years and older. Use is based on a placebo-controlled crossover study of pediatric and adult patients [see Clinical Studies ].
Safety and effectiveness of HETLIOZ for the treatment of nighttime sleep disturbances in SMS have not been established in patients younger than 3 years old.
Juvenile Animal Toxicity Data
Juvenile rats received oral doses of tasimelteon at 50, 150, or 450 mg/kg from weaning (day 21) through adulthood (day 90). These doses are approximately 12 to 108 times the maximum recommended human dose (MRHD) of 20 mg based on a mg/m2 body surface area. Toxicity was observed mainly at the highest dose and included mortality (females only), tremors, unsteady gait, decrease in growth and development compared to controls. The former reflected as decreases in bone growth, bone mineral content, bone ossification, and a delay in attainment of sexual maturation. Tasimelteon had no effect on fertility, reproduction, or learning and memory. The No Observed Adverse Effect Level (NOAEL) is 150 mg/kg/day, which is approximately 178 times the MRHD based on AUC.
Geriatric Use
The 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 compared with younger patients.
Hepatic Impairment
Dose adjustment is not necessary in patients with mild or moderate hepatic impairment. HETLIOZ has not been studied in patients with severe hepatic impairment (Child-Pugh Class C). Therefore, HETLIOZ is not recommended for use in patients with severe hepatic impairment [see Clinical Pharmacology ].
Smokers
Smoking causes induction of CYP1A2 levels. The exposure of tasimelteon in smokers was lower than in non-smokers and therefore the efficacy of HETLIOZ may be reduced in smokers [see Clinical pharmacology ].
None.
Somnolence
After taking HETLIOZ, patients should limit their activity to preparing for going to bed. HETLIOZ can potentially impair the performance of activities requiring complete mental alertness.