Tasimelteon is a medication that has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of Non-24-Hour Sleep-Wake Disorder in blind individuals.
Non-24-Hour Sleep-Wake Disorder (Non-24) is a rare condition that affects the sleep-wake cycle of individuals who are totally blind, causing them to have difficulty falling asleep and waking up at the same time each day. Tasimelteon is a melatonin receptor agonist that helps regulate the body’s internal clock and improve sleep quality in individuals with Non-24.
In addition to its use in Non-24-Hour Sleep-Wake Disorder, Tasimelteon has also been studied for its potential effectiveness in treating Smith-Magenis Syndrome (SMS), a rare genetic disorder that affects multiple organ systems and is characterized by sleep disturbances. SMS is caused by a deletion or mutation in the RAI1 gene, which regulates the production of melatonin. Tasimelteon has been shown to improve sleep quality and reduce disruptive behaviors in individuals with SMS.
As a melatonin receptor agonist, Tasimelteon works by binding to the MT1 and MT2 receptors in the brain, which are involved in regulating the sleep-wake cycle. By activating these receptors, Tasimelteon helps promote the onset of sleep and regulate the timing of the sleep-wake cycle. Overall, Tasimelteon has shown promise as a treatment option for individuals with Non-24 and SMS, and further research is ongoing to explore its potential uses in other sleep disorders.
Clinical Overview of Tasimelteon
Mechanism of Action
Tasimelteon is a melatonin receptor agonist that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN) of the brain. This interaction helps to regulate the circadian rhythm, which is responsible for regulating the sleep-wake cycle. Tasimelteon works by resetting the body’s internal clock, making it a useful treatment for sleep disorders related to circadian rhythm, such as Non-24 Sleep-Wake Disorder.
Uses and Indications
Tasimelteon, marketed under the brand name Hetlioz, is indicated for the treatment of Non-24 Sleep-Wake Disorder in individuals who are totally blind. It is available in capsule and oral suspension formulations, and is only available with a prescription. Tasimelteon should be taken at bedtime, and medical advice should be sought before use.
Dosage and Administration
The recommended dosage of Tasimelteon is dependent on the formulation. The capsule formulation is available in 20mg strength and should be taken orally at bedtime without food. The oral suspension formulation, Hetlioz LQ, is available in 20mg/mL strength and should be taken orally at bedtime with food. The dosage should be individualized based on the patient’s needs and response to treatment.
Pharmacokinetics
Tasimelteon has a high oral bioavailability and a short half-life of approximately 1-2 hours. It is extensively distributed throughout the body and is metabolized by the CYP1A2 and CYP3A4 enzymes. Tasimelteon is primarily eliminated through the liver, with approximately 80% of the dose excreted in the feces and 20% in the urine.
In summary, Tasimelteon is a melatonin receptor agonist that selectively binds to the MT1 and MT2 receptors in the SCN of the brain. It is indicated for the treatment of Non-24 Sleep-Wake Disorder in individuals who are totally blind. Tasimelteon is available in capsule and oral suspension formulations, and the dosage should be individualized based on the patient’s needs and response to treatment. It is important to seek medical advice before using Tasimelteon and to take it at bedtime as directed.
Safety and Side Effects
Common Adverse Reactions
Tasimelteon is generally well-tolerated, but some patients may experience adverse reactions. The most common adverse reactions include headache, drowsiness, and nightmares/strange dreams. If these symptoms persist or worsen, healthcare providers should be informed.
Contraindications and Precautions
Tasimelteon is contraindicated in patients with a known hypersensitivity to the drug. It should also be used with caution in patients with liver disease, as it is primarily metabolized in the liver. Pregnant and breastfeeding women should consult their healthcare provider before using Tasimelteon.
Drug Interactions
Tasimelteon may interact with other drugs, such as fluvoxamine and rifampin, and herbal products. Patients should inform their healthcare provider of all medications, herbal products, and vitamins they are taking before using Tasimelteon.
Overdose and Emergency
In the event of an overdose, patients should seek immediate medical attention or contact the Poison Help Line. Symptoms of overdose may include excessive drowsiness and sedation.
Patients should also be advised to inform their healthcare provider of any allergies, swelling of the face, tongue, or throat, and any other symptoms that may indicate an allergic reaction.
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