suvorexant

medtigo

suvorexant

Brand Name :

Belsomra

Synonyms :

suvorexant

Class :

Orexin Antagonists,Hypnotics/Sedatives

Action and Spectrum

Actions and Spectrum:

Mechanism of Action:

Orexin system modulation: suvorexant works by selectively blocking the action of orexin receptors in the brain. Orexins, or hypocretins, are neuropeptides that regulate wakefulness and sleep-wake cycles. By blocking orexin receptors, suvorexant inhibits the wake-promoting effects of orexins, promoting sleep initiation and maintenance.

Sleep-wake regulation: Orexins are produced by a group of neurons in the hypothalamus known as the lateral hypothalamic area. They project throughout the brain, including areas involved in sleep-wake regulation, such as the arousal centers in the brainstem and the hypothalamic areas involved in controlling the sleep-wake cycle. suvorexant’s mechanism of action in blocking orexin receptors helps to promote sleep by reducing wakefulness-promoting signals.

Spectrum of Activity:

suvorexant is primarily indicated for treating insomnia, characterized by difficulty falling or staying asleep. It has been shown to reduce sleep latency and increase total sleep time. The spectrum of activity of suvorexant includes:

Sleep onset insomnia: suvorexant can effectively reduce the time it takes to fall asleep, helping individuals with sleep onset insomnia to initiate sleep more quickly.

Sleep maintenance insomnia: suvorexant can also benefit individuals with difficulty staying asleep throughout the night. Promoting sleep maintenance can help individuals with sleep maintenance insomnia experience uninterrupted and restful sleep.

Overall sleep quality improvement: suvorexant has been shown to improve subjective sleep quality and patient-reported outcomes, leading to a more restful and satisfying sleep experience.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined

1-10%

Somnolence (7%)

Somnolence, males (3%)

Abnormal dreams (2%)

Diarrhea (2%)

Upper respiratory tract infection (2%)

Headache (7%)

Dizziness (3%)

Cough (2%)

Dry mouth (2%)

Somnolence, females (8%)

Post-marketing reports

Tachycardia

Psychomotor hyperactivity

Palpitations

Pruritis

Anxiety

Vomiting

Nausea

Black Box Warning

Contraindication / Caution

Contraindications/caution:

Contraindications:

Hypersensitivity: suvorexant should not be used in individuals with known hypersensitivity or allergy to suvorexant or its components. Allergic reactions can range from mild to severe and may require immediate medical attention.

Severe hepatic impairment: suvorexant is primarily metabolized in the liver. Therefore, individuals with severe liver impairment should not use suvorexant, as it may affect the metabolism and clearance of the drug.

CYP3A4 inhibitors: suvorexant is primarily metabolized by the enzyme CYP3A4. Concomitant use of potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, clarithromycin, and nefazodone, can significantly increase suvorexant plasma concentrations. This can lead to an increased risk of adverse effects and may require dose adjustments or alternative treatment options.

Caution:

CNS Depressant Effects: suvorexant may cause central nervous system (CNS) depressant effects, such as drowsiness, impaired coordination, and cognitive impairment. Caution should be exercised when driving, operating machinery, or engaging in activities that require mental alertness until the individual’s response to suvorexant is known.

Drug Interactions: suvorexant may interact with other medications, including those that also have CNS depressant effects or affect the activity of CYP3A4 enzymes.

Respiratory Depression: suvorexant, like other CNS depressants, can potentially cause respiratory depression, especially in individuals with underlying respiratory disorders. It should be used with caution in individuals with compromised respiratory function.

Substance Use: suvorexant may have additive effects when used with alcohol or other substances that have CNS depressant effects. Combining suvorexant with these substances can increase the risk of excessive sedation, impaired coordination, and other adverse effects. It is advisable to avoid alcohol and discuss the use of other substances with your healthcare provider while taking suvorexant.

Elderly Population: Elderly individuals may be more sensitive to the effects of suvorexant due to age-related changes in drug metabolism and clearance. Lower doses or close monitoring may be required in this population.

Pregnancy and Breastfeeding: The safety of suvorexant in pregnancy and breastfeeding has not been established. It is generally recommended to avoid using suvorexant during pregnancy and breastfeeding unless the potential benefits outweigh the potential risks.

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

<b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

Drug Interactions: suvorexant is metabolized by CYP3A4, so concomitant use of potent CYP3A4 inhibitors, such as ketoconazole or clarithromycin, can increase suvorexant plasma concentrations. Conversely, inducers of CYP3A4, such as rifampin or St. John’s wort, may decrease suvorexant levels. It is essential to consider potential drug interactions when prescribing or using suvorexant.

Dose-Dependent Effects: suvorexant exhibits dose-dependent effects on sleep. Lower doses of suvorexant primarily target the OX2R receptors and promote sleep onset. In comparison, higher doses additionally block OX1R receptors and promote sleep maintenance. Individual responses to suvorexant may vary, and finding the optimal dose for an individual may require titration.

Safety and Tolerability: suvorexant has been generally well-tolerated in clinical trials. The most common side effects include drowsiness, headache, dizziness, and dry mouth. Rarely, more severe adverse effects, such as angioedema or anaphylaxis, may occu

suvorexant

No data available for drug.

DRUG INTERACTION

suvorexant

&

suvorexant +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

suvorexant

No data available for drug.

DRUG INTERACTION

suvorexant

&

suvorexant +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

suvorexant

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology