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
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
- Confusion
- Irritability and aggression
- Anxiety
- Drowsiness
- Dry mouth
- Abdominal or stomach pain
- cold or flu symptoms such as stuffy nose, sore throat, fever;
- Constipation
- dizziness or lightheadedness
- blurred vision
- hiccups
- coughing
- pain, redness, or hardening of the skin at the injection site
- Nausea ,vomiting,
- painful or swollen gums
- numbness or heavy feeling in the jaw
- stomach pain,
- headache,
- reversible hair loss or thinning, and
- fever
Common
- chills or fever
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- excessive sweating
- sudden drowsiness or need to sleep
- coughing up blood
- liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite,
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.
References
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