Zaleplon (zaleplon)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Zaleplon, a pyrazolopyrimidine derivative, is a sedative and hypnotic agent structurally unrelated to the benzodiazepines and other sedative-hypnotic agents.
Zaleplon, a pyrazolopyrimidine derivative, is a sedative and hypnotic agent structurally unrelated to the benzodiazepines and other sedative-hypnotic agents. Pharmacologically and pharmacokinetically, zaleplon is similar to zolpidem; both are hypnotic agents with short half-lives, and both have been shown to interact with the CNS gamma-aminobutyric acid (GABAA)-receptor-chloride ionophore complex at benzodiazepine (BZ) omega-1 (BZ1, omega1) receptors. In contrast, some benzodiazepines nonselectively activate central BZ1 (omega1) and BZ2 (omega2) receptors as well as peripheral BZ3 (omega3) receptors, resulting in nonspecific pharmacologic actions.
Zaleplon is extensively metabolized, principally by aldehyde oxidase, and to a lesser extent by the cytochrome P-450 (CYP) isoenzyme 3A4. Zaleplon generally appears to be absorbed and eliminated more rapidly than zolpidem.
USES: This medication is used for a short time to treat people who have trouble falling asleep. If you have other sleep problems such as not being able to sleep through the night, this medication may not be right for you. Zaleplon is known as a hypnotic.
It works on certain centers in the brain to relax you and help you fall asleep faster.
Generic name: zaleplon
Pronunciation: (ZAL-e-plon)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Zaleplon
Indications
The following indications are listed for Zaleplon:
- Sleep-Onset Insomnia
Also known as: Insomnia Due To Delayed Sleep Onset, Insomnia Due To Increased Sleep Latency.
Dosing
Dosage of zaleplon should be individualized. The lowest effective dosage of the drug should be used in all patient populations.
The recommended initial dosage of zaleplon for the management of insomnia in most adults <65 years of age is 10 mg immediately before bedtime or after unsuccessfully attempting to sleep. Although the risk of certain adverse effects appears to be dose dependent, 20-mg doses have been shown to be adequately tolerated and may be considered in most adults who do not respond adequately to lower doses. Doses >20 mg have not been adequately studied and are not recommended by the manufacturer.
Zaleplon is administered orally without regard to meals, although administration with a high-fat meal should be avoided because of a potential decreased rate of drug absorption. Such delay in GI absorption could result in decreased efficacy on sleep latency.
Because of its rapid onset of action, zaleplon should be taken immediately before retiring when the patient is ready to go to sleep or after the patient has already gone to bed but has experienced difficulty falling asleep. Patients should be advised that zaleplon should only be used in circumstances where they are able to get a full night's sleep.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Zaleplon is metabolized principally by aldehyde oxidase, and to a lesser extent by CYP3A4; all metabolites of the drug are inactive.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Hypersensitivity to zaleplon or any ingredient in the formulation.
*History of a complex sleep behavior while taking eszopiclone, zaleplon, or zolpidem.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in >=5% of patients receiving zaleplon include headache, asthenia, dizziness, nausea, abdominal pain, and somnolence.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy not established in pediatric patients <18 years of age.
There are no studies of zaleplon in pregnant women to date. The manufacturer does not recommend use in this population, and there is no established use of the drug in labor and delivery.
Zaleplon is distributed into milk. Since the effects of zaleplon on nursing infants are not known but even small amounts might be potentially important, the manufacturer does not recommend use in nursing women.
Patients >=65 years of age may be more sensitive to pharmacologic and adverse effects of sedative-hypnotic agents; initial and maximum dose reduction recommended.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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