This medication is a Schedule IV drug.
For the short-term treatment of insomnia: The recommended initial dose is 10 mg. Low-weight patients may find a 5 mg dose to be sufficient. In patients where the 10 mg dose is not effective, a 20 mg dose is indicated. Doses above 20 mg are not recommended. A 5 mg dose is indicated in elderly patients, in patients with hepatic insufficiency, and in patients taking prescription or nonprescription cimetidine. Take immediately before bedtime or after the patient has already gone to bed and has experienced problems falling asleep.
Pharmacology/Pharmacokinetics:
Although the chemical structure of zaleplon is unrelated to benzodiazepines, it facilitates the inhibitory neurotransmitter action of gamma-aminobutyric acid (GABA) by interacting with the GABA-BZ receptor complex. This interaction mediates both pre- and post-synaptic inhibition in all regions of the CNS. Zaleplon is rapidly absorbed after an oral dose with a time to peak plasma levels of 1 hour. Terminal elimination half-life is also 1 hour. Plasma protein binding is 60%. Metabolism occurs via aldehyde oxidase and to a lesser extent CYP3A4. Food delays absorption up to 2 hours.
Drug Interactions:
Cimetidine and grapefruit juice may increase plasma levels. Alcohol may potentiate CNS depression. Use with other CNS depressants may produce additive effects. Rifampin may decrease effectiveness.
Contraindications/Precautions:
Contraindicated in patients who have previously experienced an episode of complex sleep behavior with eszopiclone, zaleplon, or zolpidem. RARE BUT SERIOUS INJURIES HAVE OCCURRED DUE TO ABNORMAL SLEEP BEHAVIORS INCLUDING SLEEP WALKING, SLEEP DRIVING, AND ENGAGING IN OTHER ACTIVITIES WHEN NOT FULLY AWAKE. Insomnia lasting more than 7-10 days may be a manifestation of a physical and/or psychiatric disorder. Sedatives/hypnotics may stimulate abnormal thinking and any change in behavior requires careful attention. Resulting drowsiness will pose a hazard to activities requiring mental alertness and concentration. Lower the normal dose and use caution in elderly patients and in patients with hepatic impairments. Use with caution in depressed patients due to the risk of suicide. Pregnancy Category C.
Adverse Effects:
The most common adverse effects in frequency of incidence are headache, myalgia, dizziness, nausea, asthenia, abdominal pain, dyspepsia, and eye pain. Less common adverse effects include amnesia, fever, dysmenorrhea, somnolence, paresthesia, tremor, and hyperacusis.
Contact a physician if the above side effects are severe or persistent.
This medication is rapid in its onset. Therefore, patients should take it immediately before bed.
Patients should have at least 4 hours of sleep to avoid psychomotor impairment.
Because of induced drowsiness, do not operate machinery or engage in activities when mental alertness is required.
Avoid alcohol while taking this medication.
WARNING: This medication may be habit-forming.
Store in a cool, dry place away from sunlight and children.
