Lemborexant:Pharmacodynamics,Mechanism,Side Effects

Lemborexant is used to treat insomnia (difficulty falling asleep or staying asleep).Lemborexant belongs to a class of medications called hypnotics. It works by slowing activity in the brain to allow sleep.

Pharmacodynamics

Lemborexant is a dual antagonist of the orexin OX1 and OX2 receptors.It associates and dissociates from the orexin receptors more rapidly than certain other orexin receptor antagonists, such as suvorexant, and this may cause it to have a shorter duration of action.

Mechanism

The orexin neuropeptide signaling system is involved in many physiologic functions, including sleep/wake control. Orexin-A and orexin-B activate post-synaptic G-protein coupled orexin-1 receptors (OX1R) and orexin-2 receptors (OX2R), which are found on neurons in the hypothalamus that project to numerous wake-controlling nuclei. Each receptor carries slightly different activity - activation of OX1R appears to suppress the onset of rapid eye movement (REM) sleep, whereas activation of OX2R appears to suppress non-REM sleep.

Lemborexant is an competitive antagonist of OX1R and OX2R. By blocking the binding of wake-promoting orexin-A and -B at these receptors, lemborexant suppresses the wake-drive, thereby promoting sleep.

The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Side Effects

Nightmares, unusual dreams, or tiredness may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Lemborexantmay make you sleepy during the day. Tell your doctor if you have aytime drowsiness. Your dose may need to be adjusted.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as depression, hallucinations, thoughts of suicide), temporary weakness in your legs.

This medication may cause sleep paralysis, which is a temporary inability to move or talk (for up to several minutes) while you are going to sleep or waking up.

Rarely,after taking this drug, people have gotten out of bed and driven vehicles while not fully awake ("sleep-driving"). People have also sleepwalked, prepared/eaten food, made phone calls, or had sex while not fully awake. Often, these people do not remember these events. This problem can be dangerous to you or to others. If you find out that you have done any of these activities after taking this medication, tell your doctor right away.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

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