zaleplon

Contraindicated in:

Hypersensitivity;
History of experiencing complex sleep behaviors with zaleplon;
Severe hepatic impairment;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Mild or moderate hepatic impairment or weight ≤50 kg (initiate therapy at lowest dose);
Impaired respiratory function;
History of suicide attempt;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. ↑ risk of cognitive impairment, delirium, falls, fractures, and motor vehicle accidents in older adults. Avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema

Derm: photosensitivity

EENT: abnormal vision, altered sense of smell, ear pain, epistaxis, hearing sensitivity, ocular pain

GI: abdominal pain, anorexia, colitis, dyspepsia, nausea

GU: dysmenorrhea

Neuro: abnormal thinking, amnesia, anxiety, behavior changes, COMPLEX SLEEP BEHAVIORS (INCLUDING SLEEP DRIVING, SLEEP WALKING, OR ENGAGING IN OTHER ACTIVITIES WHILE SLEEPING), depersonalization, dizziness, drowsiness, hallucinations, headache, hyperesthesia, impaired memory (briefly following dose), impaired psychomotor function (briefly following dose), malaise, nightmares, paresthesia, tremor, vertigo, weakness

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Cimetidine may ↑ levels and the risk of toxicity; initiate therapy at a lower dose.
Additive CNS depression with other CNS depressants, including alcohol, antihistamines, opioid analgesics, other sedative/hypnotics, phenothiazines, and tricyclic antidepressants.
CYP3A4 inducers, including rifampin, phenytoin, carbamazepine, and phenobarbital, may ↓ levels and effectiveness.

Drug-Natural Products:

Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.

Drug-Food:

Concurrent ingestion of a high-fat meal slows the rate of absorption.

Availability ⬆ ⬇

(Generic available)

Capsules: 5 mg; 10 mg

Route/Dosage ⬆ ⬇

PO (Adults <65 yr): 10 mg (range 5–20 mg) at bedtime.

Hepatic Impairment

PO (Adults ): Initiate therapy at 5 mg at bedtime (not to exceed 10 mg at bedtime).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Produces CNS depression by binding to GABA receptors in the CNS.
Has no analgesic properties.

Therapeutic effects:

Induction of sleep.

Classifications ⬆ ⬇

Therapeutic Classification: sedative/hypnotics

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly absorbed following oral administration.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Extensively metabolized in the liver (mostly by aldehyde oxidase and some by the CYP3A4 isoenzyme).

Half-Life: 1 hr.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	within min	unknown	3–4 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take zaleplon as directed. Do not take more than the amount prescribed because of the habit-forming potential. Not recommended for use longer than 7–10 days. Rebound insomnia (1–2 nights) may occur when stopped. If used for 2 wk or longer, abrupt withdrawal may result in dysphoria, insomnia, abdominal or muscle cramps, vomiting, sweating, tremors, and seizures.
Because of rapid onset, advise patient to go to bed immediately after taking zaleplon.
May cause daytime drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to this medication is known.
Inform patient that amnesia may occur, but can be avoided if zaleplon is only taken when patient is able to get >4 hr sleep.
Caution patient that complex sleep-related behaviors (sleep-driving, making phone calls, preparing and eating food, having sex, sleep walking) may occur while asleep. Inform patient to notify health care professional if sleep-related behaviors (may include sleep-driving—driving while not fully awake after ingestion of a sedative-hypnotic product, with no memory of the event) occur.
Caution patient to avoid concurrent use of alcohol or other CNS depressants, including opioids.
Rep: May cause fetal harm. Use is not recommended during pregnancy or breastfeeding. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

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Indications ⬇

Contraind./Precautions ⬆ ⬇