What is Hetlioz (tasimelteon)?
Hetlioz is indicated for the
treatment of Non-24-Hour Sleep-Wake Disorder (Non-24).
The precise mechanism by which tasimelteon exerts its therapeutic effect in patients with Non24 is not known. Tasimelteon is an agonist at melatonin MT1 and MT2 receptors. These receptors are thought to be involved in the control of circadian rhythms.
What are the side effects of Hetlioz?
Clinical Trials Experience
Because clinical trials are
conducted under widely varying conditions, adverse reaction rates observed in
the clinical trials of a drug cannot be directly compared to rates in the
clinical trials of another drug and may not reflect the rates observed in clinical
practice.
A total of 1346 subjects were
treated with at least one dose of Hetlioz, of which 139 were treated for >
26 weeks and 93 were treated for > 1 year.
A 26-week, parallel-arm placebo-controlled study (Study
1) evaluated Hetlioz (n=42) compared to placebo (n=42) in patients with Non-24.
A randomized-withdrawal, placebo-controlled study of 8 weeks duration (Study 2)
also evaluated Hetlioz (n=10), compared to placebo (n=10), in patients with
Non-24.
In placebo-controlled studies, 6% of patients exposed to
Hetlioz discontinued treatment due to an adverse event, compared with 4% of
patients who received placebo.
Table 1 shows the incidence of adverse reactions from
Study 1.
Table 1: Adverse Reactions in Study 1
Hetlioz N=42
Placebo N=42
Headache
17 %
7 %
Alanine aminotransferase increased
10 %
5 %
Nightmare/abnormal dreams
10 %
0 %
Upper respiratory tract infection
7 %
0 %
Urinary tract infection
7 %
2 %
*Adverse reactions with an
incidence > 5% and at least twice as high on Hetlioz than on placebo are
displayed.
Can you get addicted to Hetlioz?
Controlled Substance
Tasimelteon is not a controlled substance under the
Controlled Substances Act.
Abuse
Tasimelteon did not produce any abuse-related signals in
animal behavioral studies. Rats did not self-administer tasimelteon, suggesting
that the drug does not have rewarding properties. There were also no signs or
symptoms indicative of abuse potential in clinical studies with Hetlioz.
Dependence
Discontinuation of Hetlioz in humans following chronic
administration did not produce withdrawal signs. Hetlioz does not appear to
produce physical dependence.
What is the dosage for Hetlioz?
The recommended dosage of
Hetlioz is 20 mg per day taken before bedtime, at the same time every night.
Because of individual
differences in circadian rhythms, drug effect may not occur for weeks or
months.
Hetlioz should be taken without
food.
Dosage Forms And Strengths
Capsules: 20 mg size 1 dark
blue opaque, hard gelatin capsules printed with “Vanda 20 mg” in white.
What drugs interact with Hetlioz?
Strong CYP1A2 Inhibitors (e.g.,
fluvoxamine)
Avoid use of Hetlioz in
combination with fluvoxamine or other strong CYP1A2 inhibitors because of a
potentially large increase in tasimelteon exposure and greater risk of adverse
reactions.
Strong CYP3A4 Inducers (e.g.,
rifampin)
Avoid use of Hetlioz in
combination with rifampin or other CYP3A4 inducers because of a potentially
large decrease in tasimelteon exposure with reduced efficacy.
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.
Is Hetlioz safe to take while pregnant or breastfeeding?
There are no adequate and
well-controlled studies of Hetlioz in pregnant women. 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. Hetlioz should be used during pregnancy only if the potential
benefit justifies the potential risks.
It is not known whether this drug is excreted in human
milk. Because many drugs are excreted in human milk, caution should be
exercised when Hetlioz is administered to a nursing woman.