Suvorexant
Suvorexant Uses, Dosage, Side Effects, Food Interaction and all others data.
Suvorexant is a highly selective antagonist for orexin receptors OX1R and OX2R. The mechanism by which Suvorexant exerts its therapeutic efect in insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.
| Trade Name | Suvorexant |
| Availability | Prescription only |
| Generic | Suvorexant |
| Suvorexant Other Names | Suvorexant |
| Related Drugs | amitriptyline, lorazepam, melatonin, zolpidem, diphenhydramine, Ativan |
| Weight | 10mg, 15mg, 20mg, 5mg |
| Type | Oral tablet |
| Formula | C23H23ClN6O2 |
| Weight | Average: 450.93 Monoisotopic: 450.1571017 |
| Protein binding | Suvorexant is extensively bound (>99%) to human plasma proteins and does not preferentially distribute into red blood cells. It binds to both human serum albumin and alpha1-acid glycoprotein. |
| Groups | Approved, Investigational |
| Therapeutic Class | Miscellaneous sedatives & hypnotics |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Suvorexant is used for the treatment of insomnia, characterized by difculties with sleep onset and/or sleep maintenance.
Suvorexant is also used to associated treatment for these conditions: Insomnia
How Suvorexant works
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.
Dosage
Suvorexant dosage
Recommended dose is 10 mg, no more than once per night taken before 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening. If the 10 mg dose is well-tolerated but not effective, the dose can be increased, not to exceed 20 mg once daily. Lowest dose effective should be used for the patient. Time to effect may be delayed if taken with or soon after a meal.
Side Effects
Common side effects are Sleepiness during the day, Not thinking clearly, Act strangely, confused, or upset, Sleep-walking
Toxicity
Dose-related somnolence and CNS depression are the most common adverse effects associated with the use of suvorexant. It has also been shown to impair driving skills and may increase the risk of falling asleep while driving. Next-day impairments are found to be highest if suvorexant is taken with less than a full night of sleep remaining, with higher doses, or if co-administered with other CNS depressants or CYP3A inhibitors. Complex behaviours such as sleep driving, preparing and eating food, and making phone calls have been reported in association with the use of hypnotics such as suvorexant. A dose-dependant increase in suicidal ideation has been observed, especially in patients with a previous diagnosis of depression. Sleep paralysis, hypnagogic/hypnopompic hallucinations including vivid and disturbing perceptions, and mild cataplexy have also been reported. There are no adequate studies in pregnant women to ensure its safety during pregnancy or breast feeding.
Precaution
Daytime somnolence: Risk of impaired alertness and motor coordination, including impaired driving; risk increases with dose; caution patients taking 20 mg against next-day driving and other activities requiring complete mental alertness.
Need to evaluate for co-morbid diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment.
Interaction
CNS-Active Drugs: An additive effect on psychomotor performance was observed when a single dose of 40 mg of Suvorexant was co-administered with a single dose of 0.7 g/kg alcohol. Suvorexant does not afect alcohol concentrations and alcohol does not afect Suvorexant concentrations.
effect s of Other Drugs on Suvorexant: Strong (e.g., ketoconazole or itraconazole) and moderate (e.g., diltiazem) CYP3A inhibitors signifcantly increased Suvorexant exposure. Strong CYP3A inducers (e.g., rifampin) substantially decreases Suvorexant exposure.
effect s of Suvorexant on Other Drugs: Suvorexant is unlikely to cause clinically signifcant inhibition of human CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19 or CYP2D6. Chronic administration of Suvorexant is unlikely to induce the metabolism of drugs metabolized by major CYP isoforms.
Food Interaction
- Avoid grapefruit products.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of suvorexant.
Use in combination may result in additive central nervous system depression and In addition, alcohol may increase the risk of cognitive and complex behavioral changes associated with the use of hypnotics including suvorexant, such as amnesia, anxiety, hallucinations, sleep-driving, and other neuropsychiatric symptoms. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. According to the product labeling, administration of suvorexant with a high-fat meal resulted in no meaningful change in peak plasma concentration (Cmax) or systemic exposure (AUC), but a delay in Tmax of approximately 1.5 hours. Patients should be advised not to use suvorexant if they had alcohol that evening or before bed. Grapefruit juice should preferably be avoided; otherwise, the recommended dose of suvorexant is 5 mg when used with grapefruit juice and should not exceed 10 mg. Suvorexant may be taken with or without food; however, for faster sleep onset, suvorexant should not be administered with or soon after a meal.
ADJUST DOSE: Grapefruit juice may significantly increase the plasma concentrations of suvorexant.
ADJUST DOSING INTERVAL: Administration with or soon after a meal may delay the gastrointestinal absorption of suvorexant.
MANAGEMENT: Concomitant use of suvorexant with alcohol should be avoided.
Suvorexant Drug Interaction
Moderate: aripiprazole, zolpidem, lorazepam, duloxetine, clonazepam, lamotrigine, pregabalin, desvenlafaxine, ramelteon, quetiapineUnknown: amphetamine / dextroamphetamine, sucralfate, loratadine, ubiquinone, acetaminophen, cyanocobalamin, cholecalciferol, lisdexamfetamine, bupropion, ondansetron
Suvorexant Disease Interaction
Major: depression, severe renal impairment, impaired respiratory function, narcolepsyModerate: glaucoma, liver disease
Volume of Distribution
Mean volume of distribution is approximately 49 litres.
Elimination Route
Peak concentrations occur at a median Tmax of 2 hours under fasted conditions. Ingestion of suvorexant with a high-fat meal has no effect on AUC or Cmax, but may delay Tmax by approximately 1.5 hours. Mean absolute bioavailability of 10 mg is 82%.
Half Life
Mean half life is approximately 12 hours.
Elimination Route
Approximately 66% is eliminated in feces and 23% is eliminated in urine.
Pregnancy & Breastfeeding use
Pregnancy Category C. There is no adequate and well-controlled studies in pregnant women. Suvorexant should be used during pregnancy only if the potential beneft justifes the potential risk to the fetus.
Contraindication
Do not use in patients with narcolepsy.
Storage Condition
Store in dry and cool place, protect from light & keep away from children.
Innovators Monograph
You find simplified version here Suvorexant
Suvorexant contains Suvorexant see full prescribing information from innovator Suvorexant Monograph, Suvorexant MSDS, Suvorexant FDA label
FAQ
What is Suvorexant used for?
Suvorexant is used treat insomnia (difficulty falling asleep or staying asleep).
How safe is Suvorexant?
Suvorexant was generally safe and well tolerated over 1 year of nightly treatment in patients with insomnia, with efficacy noted for subjective measures of sleep onset and maintenance.
How does Suvorexant work?
Suvorexant works by blocking the action of a certain natural substance in the brain that causes wakefulness.
What are the common side effects of Suvorexant?
Common side effects of Suvorexant are include:
Is Suvorexant safe during pregnancy?
Suvorexant should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby. 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.
Is Suvorexant safe during breastfeeding?
Caution is recommended.The effects in the nursing infant are unknown.Suvorexant and a hydroxyl-suvorexant metabolite were excreted in rat milk at levels higher than that in maternal plasma.
Can I drink alcohol with Suvorexant?
Avoid drinking alcohol. Do not take Suvorexant if you have consumed alcohol within a few hours before getting ready for sleep.
How long does Suvorexant take to work?
Your sleep problems should improve within 7 to 10 days after you start taking Suvorexant.
When is the best time to take Suvorexant?
Take Suvorexant only once per night, 30 minutes before bedtime. You may take Suvorexant with or without food. Avoid taking the medicine shortly after eating a meal, or the medicine may take longer to work.
Is Suvorexant addictive?
Suvorexant may be habit-forming. Misuse can cause addiction, overdose, or death. Keep the medication in a place where others cannot get to it.
How long does Suvorexant stay in my system?
Suvorexant has a long elimination half-life of 12 hours and reaches steady state by the 3rd day with regular use. It should only be taken when the patient will be able to stay in bed for at least 7 hours before arising and resuming activities, including driving.
How long does Suvorexant take to work?
Your sleep problems should improve within 7 to 10 days after you start taking Suvorexant.
Can I overdose on Suvorexant?
Never use Suvorexant in larger amounts, or for longer than prescribed. Tell your doctor if you feel an increased urge to use more of this medicine. Suvorexant may be habit-forming. Misuse can cause addiction, overdose, or death.
Why is Suvorexant a controlled substance?
Suvorexant is a federally controlled substance (C-IV) because it can be abused or cause dependence. Keep Suvorexant in a safe place to prevent misuse and abuse.
Does Suvorexant make me sleep?
Suvorexant may make you sleepy during the day. Tell your doctor if you have daytime drowsiness.
How to use Suvorexant?
Take Suvorexant by mouth as directed by your doctor, usually 30 minutes before you get into bed. This medication can be taken with or without food, but it may take longer to work if you take it with or right after a meal.
What happens if I miss a dose?
Since Suvorexant is taken only at bedtime if needed, you are not likely to miss a dose. Never take this medicine if you do not have 7 hours to sleep before being active again.
Is Suvorexant a narcotic?
No,Suvorexant is not a narcotic, but it is a controlled substance. This means that your use of Suvorexant will be tracked to prevent potential prescription abuse.
