Belsomra (Suvorexant) is a dual orexin receptor antagonist (DORA) that is used to treat patients with insomnia. Insomnia is defined as either difficulty with the onset of sleep or in the maintenance of sleep.
Belsomra (Suvorexant) dose in Adults
Belsomra (Suvorexant) dose in the treatment of Insomnia:
Note: Use the lowest effective dose for the patient.
- Usual dose:
- A dose of 10 mg once a day within 30 minutes of bedtime.
- It may be increased to a maximum dose of 20 mg once a day if the 10 mg dose is tolerated well but not effective.
- The maximum daily dose of 20 mg
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Dosage adjustment in concomitant therapy:
- Moderate CYP3A inhibitors which include crepitant, atazanavir, amprenavir, aprepitant, diltiazem, ciprofloxacin, erythromycin, grapefruit juice, fluconazole, fosamprenavir, imatinib, and verapamil.
- The usual dose of 5 mg once daily;
- A maximum daily dose of 10 mg once daily
- Strong CYP3A inhibitors which include itraconazole, ketoconazole, clarithromycin, posaconazole, ritonavir, nefazodone, saquinavir, nelfinavir, indinavir, boceprevir, telaprevir, conivaptan, telithromycin.
- Suvorexant use is not recommended.
- Moderate CYP3A inhibitors which include crepitant, atazanavir, amprenavir, aprepitant, diltiazem, ciprofloxacin, erythromycin, grapefruit juice, fluconazole, fosamprenavir, imatinib, and verapamil.
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CNS depressants:
- It is necessary to adjust the dose of suvorexant or other CNS depressants.
Belsomra (Suvorexant) dose in Childrens
Not recommended for use in children.
Belsomra (Suvorexant) Pregnancy Risk Factor C
- Some studies on animal reproduction have shown adverse effects.
Use of suvorexant while breastfeeding
- It is unknown if breast milk contains suvorexant.
- If the product is being administered to a nursing mother, it is recommended that caution be taken.
Belsomra (Suvorexant) dose in Kidnet Disease:
No dosage adjustment necessary.
Belsomra (Suvorexant) dose in Liver Disease:
- In Liver disease, Belsomra (Suvorexant), dose:
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Mild to moderate impairment
- There is no need to adjust the dosage.
-
Severe impairment
- It is not recommended and has not been tested.
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Common Side Effects of Belsomra (Suvorexant) Include:
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Central nervous system:
- Drowsiness
Less Common Side Effects of Belsomra (Suvorexant) Include:
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Central nervous system:
- Headache
- Dizziness
- Abnormal Dreams
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Gastrointestinal:
- Diarrhea
- Xerostomia
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Respiratory:
- Cough
- Upper Respiratory Tract Infection
Rare side effects of Belsomra (Suvorexant)
-
Central Nervous System:
- Abnormal Behavior
- Abnormality In Thinking
- Amnesia
- Behavioral Changes
- Cataplexy (Mild; With Or Without Triggering Event)
- Central Nervous System Depression
- Daytime Sedation
- Exacerbation Of Depression
- Hallucination (Including Hypnagogic And Hypnopompic)
- Sleep Driving
- Sleep Paralysis
- Suicidal Ideation
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Endocrine & Metabolic:
- Increased Serum Cholesterol
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Neuromuscular & Skeletal:
- Lower Extremity Weakness (Cataplexy-Like Symptoms
Contraindication to Belsomra (Suvorexant) Include:
Narcolepsy
Warnings and precautions
- Abnormal thinking/behavioral changes
- Hypnotics are often associated with abnormal thinking or behavior changes (eg anxiety, amnesia and hallucinations).
- Depression in the CNS:
- Patients should be cautious about performing tasks that could cause CNS depression, which can impair physical and mental abilities.
- Suvorexant should be administered only to patients who are able to remain in bed for at least seven hours before becoming active again.
- Patients who drive should discontinue or decrease their dose if somnolence is present during the day.
- REM Sleep Effects:
- Definitions of sleep paralysis include inability to speak or move for several minutes during sleep-wake transitions.
- Cataplexy and hypnagogic/hypnopompic hallucinations can also occur.
- Cataplexy symptoms can include a weakness in the leg for a period of time that lasts from a few seconds up to a couple of minutes.
- They can also occur at night or day and are not usually associated with any trigger event (eg laughter, surprise).
- Activities that are sleep-related:
- There is an increased chance of dangerous sleep-related activities like driving, cooking, eating, and making phone calls while you sleep.
- Patients who have experienced any sleep-related episode should discontinue treatment.
- Depression
- Patients with depression or worsening depression should exercise caution.
- The use of hypnotics has been linked to suicide or suicidal thoughts.
- Intentional overdose is a serious problem in this population.
- It is best to use the minimum amount that will effectively treat each patient.
- Use of drugs:
- Patients with a history or drug dependence should exercise caution.
- Suvorexant prolonged use can increase the risk of abuse in patients who have a history or use other drugs together.
- Hepatic impairment
- Patients with severe hepatic impairment should not use it (has not been tested).
- Respiratory disease
- Patients with COPD, respiratory compromise, and sleep apnea should be cautious.
Suvorexant: Drug Interaction
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Alizapride |
May enhance the CNS depressant effect of CNS Depressants. |
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Bosentan |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Brimonidine (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
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Bromopride |
May enhance the CNS depressant effect of CNS Depressants. |
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Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
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Cannabis |
May enhance the CNS depressant effect of CNS Depressants. |
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Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of CNS Depressants. |
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Clofazimine |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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CYP3A4 Inducers (Moderate) |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Deferasirox |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Dimethindene (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
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Dronabinol |
May enhance the CNS depressant effect of CNS Depressants. |
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Erdafitinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Erdafitinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Fosaprepitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Ivosidenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Kava Kava |
May enhance the adverse/toxic effect of CNS Depressants. |
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Larotrectinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Lofexidine |
May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Magnesium Sulfate |
May enhance the CNS depressant effect of CNS Depressants. |
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Melatonin |
May enhance the sedative effect of Hypnotics (Nonbenzodiazepine). |
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MetyroSINE |
CNS Depressants may enhance the sedative effect of MetyroSINE. |
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Minocycline |
May enhance the CNS depressant effect of CNS Depressants. |
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Nabilone |
May enhance the CNS depressant effect of CNS Depressants. |
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Palbociclib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Piribedil |
CNS Depressants may enhance the CNS depressant effect of Piribedil. |
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Pramipexole |
CNS Depressants may enhance the sedative effect of Pramipexole. |
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ROPINIRole |
CNS Depressants may enhance the sedative effect of ROPINIRole. |
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Rotigotine |
CNS Depressants may enhance the sedative effect of Rotigotine. |
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Rufinamide |
May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
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Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Selective Serotonin Reuptake Inhibitors |
CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
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Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Simeprevir |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Tetrahydrocannabinol |
May enhance the CNS depressant effect of CNS Depressants. |
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Tetrahydrocannabinol and Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
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Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Risk Factor D (Consider therapy modification) |
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Blonanserin |
CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
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Buprenorphine |
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Chlormethiazole |
May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. |
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CNS Depressants |
May enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. |
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CYP3A4 Inducers (Strong) |
May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
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CYP3A4 Inhibitors (Moderate) |
May increase the serum concentration of Suvorexant. Management: The recommended dose of suvorexant is 5 mg daily in patients receiving a moderate CYP3A4 inhibitor. The dose can be increased to 10 mg daily (maximum dose) if necessary for efficacy. |
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Dabrafenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). |
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Droperidol |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Enzalutamide |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. |
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Flunitrazepam |
CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
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HYDROcodone |
CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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Lorlatinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
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Methotrimeprazine |
CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. |
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Mitotane |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. |
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OxyCODONE |
CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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Perampanel |
May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
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St John's Wort |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
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Stiripentol |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
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Tapentadol |
May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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Zolpidem |
CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. |
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Risk Factor X (Avoid combination) |
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Alcohol (Ethyl) |
May enhance the CNS depressant effect of Suvorexant. |
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Azelastine (Nasal) |
CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
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Bromperidol |
May enhance the CNS depressant effect of CNS Depressants. |
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Conivaptan |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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CYP3A4 Inhibitors (Strong) |
May increase the serum concentration of Suvorexant. |
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Fusidic Acid (Systemic) |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Idelalisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Orphenadrine |
CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
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Oxomemazine |
May enhance the CNS depressant effect of CNS Depressants. |
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Paraldehyde |
CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
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Sodium Oxybate |
Hypnotics (Nonbenzodiazepine) may enhance the CNS depressant effect of Sodium Oxybate. |
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Thalidomide |
CNS Depressants may enhance the CNS depressant effect of Thalidomide. |
Monitoring Parameters while using Belsomra (Suvorexant):
- Daytime alertness
- respiratory rate
- behavior profile
- tolerance
- abuse
- dependence
How to administer Belsomra (Suvorexant)?
Orally administer within 30 minutes of your bedtime, with at least 7 hours before the time you are to wake up. Food delays the onset of action. Do not give orders with or right after meals.
Mechanism of action of Suvorexant (Belsomra):
- Suvorexant, which suppresses wake-promoting neuropeptides OrexinA/Orexin B, blocks their binding to OX1R or OX2R.
- Potentially adverse effects, such as cataplexy/narcolepsy, can also be caused by antagonism to orexin receptors.
The beginning of actionIt takes 30 minutes AbsorptionHigher doses cause a decrease in the effectiveness of this drug. DistributionIs49 L Protein bindingIs >99% Metabolism CYP3A is the predominant hepatic metabolite, with a small contribution from CYP2C19. The hydroxy suvorexant metabolite however is an inactive metabolite. BioavailabilityIs 82% Eliminating half-lifeIt takes 12 hours Terminal with half-lifeIs15 hours (In healthy subjects, range is between 10 and 22 hours). (In moderate hepatic diseases, range is between 11 to 49 hours.
Time to reach peak2 hours (range: 30-60 minutes to 6 hours); Delayed 1.5 hour if administered with a meal
ExcretionThe average urine content is 23%, while the average in feces is 66%
International Brands of Suvorexant:
- Belsomra
- Insoma
- Silubra
- Somarant
- Suvorex
- Xantosuvan
Belsomra (Suvorexant) Brands in Pakistan:
Belsomra (Suvorexant) is not available in Pakistan.
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