LEMBOREXANT

brands

Class

• Dual orexin receptor antagonist (DORA); hypnotic

LEMBOREXANT commonly prescribed for

(Bold for FDA approved)

How LEMBOREXANT works

• Orexin serves to stabilize and promote wakefulness; lemborexant binds to orexin 1 and orexin 2 receptors, blocking orexin from binding there and thus preventing it from promoting wakefulness

How long until LEMBOREXANT works

• Generally takes effect in less than an hour

Notable Side Effects

• Sedation, headache, abnormal dreams

Life Threatening Side Effects

• Sleep paralysis, hypnagogic/hypnopompic hallucinations, and cataplexy-like symptoms (rare)

weight gain

unusual

sedation

common

What to do about LEMBOREXANT side effects

• Wait

• To avoid problems with memory, take lemborexant only if planning to have a full night’s sleep

• Lower the dose

• Switch to a different hypnotic

usual dosage range

• 5 mg/night

Dosage Forms

• Tablet 5 mg, 10 mg

long term use

• Has been evaluated and found effective in trials up to 1 year

habit forming

• Schedule IV drug

• No evidence of physiological dependence or withdrawal symptoms in clinical trials

Renal Impairment

• Dose adjustment not necessary

• Somnolence may be increased in patients with severe renal impairment

Hepatic Impairment

• Dose adjustment not necessary for mild hepatic impairment

• Initial and maximum recommended dose 5 mg/night for moderate hepatic impairment

• Not recommended for patients with severe hepatic impairment

Cardiac Impairment

• Not studied in patients with cardiac impairment

Elderly

• Some patients may tolerate lower doses better

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Controlled studies have not been conducted in pregnant women

• When administered during organogenesis, the no observed adverse effect levels (NOAELs) for fetal toxicity are approximately >100 and 23 times the maximum recommended human dose (MRHD) based on AUC in rats and rabbits, respectively

• When administered during pregnancy and lactation, the NOAEL for toxicity is 93 times the MRHD based on AUC in rats

Breast Feeding

• Unknown if lemborexant is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or formula feed