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Suvorexant; Uses, Dosage, Side Effects, Interactions

Suvorexant is an Orexin Receptor Antagonist. The mechanism of action of suvorexant is as an Orexin Receptor Antagonist, and P-Glycoprotein Inhibitor, and Cytochrome P450 3A Inhibitor.

Suvorexant is an orexin receptor antagonist used for the treatment of insomnia and sleep disorders. Suvorexant therapy is associated with rare occurrence of transient serum enzyme elevations but has not been implicated in cases of clinically apparent liver injury.

Suvorexant is an aromatic amide obtained by formal condensation of the carboxy group of with the secondary amino group of. An orexin receptor antagonist used for the management of insomnia. It has a role as a central nervous system depressant and an orexin receptor antagonist. It is a member of 1,3-benzoxazoles, a member of triazoles, a diazepine, an aromatic amide, and an organochlorine compound.

Mechanism of Action of Suvorexant

Suvorexant is a dual antagonist of orexin receptors OX1R and OX2R. It exerts its pharmacological effect by inhibiting binding of neuropeptides orexin A and B, also known as hypocretin 1 and 2, that are produced by neurons in the lateral hypothalamus. These neurons control the wake-promoting centers of the brain and are active during wakefulness, especially during motor activities, and stop firing during sleep. By inhibiting the reinforcement of arousal systems, suvorexant use causes a decrease in arousal and wakefulness, rather than having a direct sleep-promoting effect.

Indications of Suvorexant

Suvorexant is an orexin receptor antagonist used for the treatment of insomnia and sleep disorders. Suvorexant therapy is associated with the rare occurrence of transient serum enzyme elevations but has not been implicated in cases of clinically apparent liver injury.

Suvorexant is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.
Insomnia

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Contraindications of Suvorexant

Hyper sense. to drug/class/compon.
Narcolepsy
Hardening of the Liver
liver problems
Mild to Moderate Kidney Impairment
Alcohol use
Caution if concurrent CNS depressant use
Caution in obese female pts
Caution if impaired respiratory
Caution if depression
Caution if alcohol or drug abuse
Lung Tissue Problems
Risk of angle-closure glaucoma due to narrow-angle of the anterior chamber of the eye
Chronic kidney disease stage 3A (moderate)
Chronic kidney disease stage 3B (moderate)
Chronic kidney disease stage 4 (severe)
Chronic kidney disease stage 5 (failure)

Dosage of Suvorexant

Strengths: 15 mg; 20 mg; 5 mg; 10 mg

Insomnia

10 mg orally once a day at bedtime
Maximum dose: 20 mg once a day
Take within 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening.
If 10 mg is well-tolerated but not effective, the dose can be increased.
Time to effect may be delayed if taken with or soon after a meal.

Side Effects of Suvorexant

The most common

Common

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Rare

Anxiety
change in vision
chest pain or tightness
confusion
cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
hallucinations
headache
irritability
lightheadedness
cold and clammy skin
fast and shallow breathing
swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
fast or abnormal heart rate or palpitations
loss of appetite
lower back, side, or stomach pain
mental depression
muscle pain or cramps
Swelling of your feet or ankles
Shortness of breath
Nausea, fever, dark urine, loss of appetite
Depression
Ataxia
Somnolence (difficulty staying awake)
Mental confusion
Hypotension
Respiratory arrest
Vasomotor collapse

Drug Interactions of Suvorexan

Suvorexan may interact with following drugs, supplements, & may change the efficacy of the drugs

Antacids
antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
aripiprazole
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
baclofen
barbiturates (e.g., butalbital, phenobarbital)
benzodiazepines (e.g.diazepam, lorazepam)
calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
carbamazepine
estradiol (birth control pills)
gabapentin
macrolide antibiotics (e.g., clarithromycin, erythromycin)
mirtazapine
Oral contraceptives (birth control pills)
muscle relaxants
phenytoin
proton pump inhibitors (e.g., lansoprazole, omeprazole)
quinolone antibiotics (e.g., ciprofloxacin, ofloxacin)
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
tapentadol
theophylline
tramadol
tricyclic antidepressasnts (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

Alcohol may increase your risk of experiencing some of the side effects of suvorexan

Pregnancy & Lactation of Suvorexan

FDA pregnancy category C

Pregnancy

US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

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