TASIMELTEON
THERAPEUTICS
brands
Class
- Melatonin 1 and 2 receptor agonist
TASIMELTEON commonly prescribed for
(Bold for FDA approved)
How TASIMELTEON works
• Binds selectively to melatonin 1 and melatonin 2 receptors as a full agonist, with greater affinity for melatonin 2 receptors than for melatonin 1 receptors
How long until TASIMELTEON works
• Because of individual differences in circadian rhythms, daily use for several weeks or months may be necessary before efficacy is observed
SIDE EFFECTS
Notable Side Effects
• Headache, nightmares, or unusual dreams
• Increased alanine aminotransferase
• Upper respiratory infection, urinary infection
Life Threatening Side Effects
• None reported
weight gain

unusual
sedation

common
What to do about TASIMELTEON side effects
• Wait
• To avoid problems with memory, take tasimelteon only if planning to have a full night’s sleep
• Switch to a different hypnotic
DOSING AND USE
usual dosage range
• 20 mg at bedtime
Dosage Forms
• Capsule 20 mg
long term use
• Not restricted to short-term use
• Continued use is necessary to maintain circadian entrainment
• Has been studied and found safe in a small number of patients for up to 1 year
habit forming
• No
SPECIAL POPULATIONS
Renal Impairment
• Dose adjustment not necessary
Hepatic Impairment
• Dose adjustment not necessary for mild to moderate impairment
• Not recommended for patients with severe impairment
Cardiac Impairment
• Not studied
Elderly
• Exposure to tasimelteon is increased by approximately 2-fold
Children and Adolescents
• Safety and efficacy have not been established
Pregnancy
• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001
• Controlled studies have not been conducted in pregnant women
• In animal studies, administration of tasimelteon during pregnancy resulted in developmental toxicity (embryofetal mortality, neurobehavioral impairment, decreased growth and development in offspring)
Breast Feeding
• Unknown if tasimelteon is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk
• Use caution if patient is breast feeding
Based on data Published online by Cambridge University Press
Compiled by Dr. Jash Ajmera