TASIMELTEON

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

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

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

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