suvorexant

Contraindicated in:

Narcolepsy;
Severe hepatic impairment.

Use Cautiously in:

History of substance abuse or drug dependence;
Obese patients (↑ levels, especially in women; dose ↓ may be warranted);
History of or concurrent psychiatric diagnoses;
Underlying pulmonary disease;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of falls in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Adverse reactions, especially related to CNS depression are dose-related, especially at the 20-mg dose.

Neuro: drowsiness, cataplexy, complex sleep behaviors (including sleep driving, sleep walking, or engaging in other activities while sleeping), daytime drowsiness, hallucinations (during sleep), sleep paralysis, worsening of depression/suicidal ideation

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inhibitors, including clarithromycin, conivaptan, itraconazole, ketoconazole, nefazodone, nelfinavir, posaconazole, and ritonavir, may ↑ risk of excessive sedation; avoid concurrent use.
Moderate CYP3A inhibitors, including aprepitant, atazanavir, ciprofloxacin, diltiazem, erythromycin, fluconazole, fosamprenavir, imatinib, and verapamil, may result in ↑ sedation; ↓ suvorexant dose.
Risk of CNS depression, next-day impairment, sleep-driving, and other complex behaviors while not fully awake ↑ with other CNS depressants, including alcohol, some antihistamines, opioids, other sedative/hypnotics (including benzodiazepines), and tricyclic antidepressants; dose adjustments may be necessary.
CYP3A inducers, including carbamazepine, phenytoin, and rifampin, may ↓ levels and effectiveness.
May alter digoxin levels; closely monitor serum digoxin concentrations.

Drug-Food:

Grapefruit juice may ↑ levels and excess sedation; ↓ suvorexant dose.

Availability ⬆ ⬇

Tablets: 5 mg; 10 mg; 15 mg; 20 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 10 mg within 30 min of going to bed; if well tolerated but not optimally effective, may ↑ dose the following night; not to exceed 20 mg (dose may not be repeated on a single night and should be when ≥7 hr of sleep time is anticipated before planned awakening). Concurrent use of moderate CYP3A inhibitors: 5 mg initially; may ↑ dose to 10 mg if lower dose is tolerated but not optimally effective. Lowest effective dose should be used.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Antagonizes the effects of orexins A and B, naturally occurring neuropeptides that promote wakefulness, by binding to their receptors.

Therapeutic effects:

Improved sleep.

Classifications ⬆ ⬇

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: orexin receptor antagonists

Pharmacokinetics ⬆ ⬇

Absorption: 82% absorbed following oral administration; a high-fat meal will delay absorption and sleep onset. ↑ absorption in obese women.

Distribution: Well distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Extensively metabolized by the liver via the CYP3A isoenzyme and to a lesser extent by the CYP2C19 isoenzyme to inactive metabolites. 66% excreted in feces; 23% in urine, mostly as metabolites.

Half-Life: 12 hr (↑ in hepatic impairment).

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

( sleep)

ROUTE	ONSET	PEAK	DURATION
PO	30 min (delayed by food)	unknown	7 hr‡

‡Excess sedation may persist for several days after discontinuation.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed. Advise patient not to take suvorexant unless able to stay in bed for ≥7 hr before being active again. Do not take more than the amount prescribed because of the habit-forming potential. Not recommended for use >7–10 days.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications. Caution patient to avoid concurrent use of alcohol or other CNS depressants, including opioids.
Because of rapid onset, advise patient to go to bed immediately after taking suvorexant.
May cause daytime drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness for ≥8 hr after dosing until response to this medication is known.
Caution patient that complex sleep-related behaviors (sleep-driving) may occur while asleep. Inform caregivers of these behaviors and advise to notify health care provider if any occur.
Advise patient to notify health care provider if depression worsens or suicidal thoughts occur.
Advise patient to notify health care provider immediately if signs of anaphylaxis (swelling of the tongue or throat, trouble breathing, nausea, vomiting) occur.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇