Zaleplon

Mechanism-of-action classes: GABA A Agonists; GABA A Receptor Interactions.

• Zaleplon capsules are indicated for the short-term treatment of insomnia. Zaleplon capsules have been shown to decrease the time to sleep onset for up to 30 days in controlled clinical studies (see Clinical Trials under CLINICAL PHARMACOLOGY ).ICD-10: G47.00

• Zaleplon is contraindicated in patients: who have experienced complex sleep behaviors after taking zaleplon (see WARNINGS ) with hypersensitivity to zaleplon or any excipients in the formulation (see PRECAUTIONS )contraindicated

The dose of zaleplon capsules should be individualized. The recommended dose of zaleplon capsules for most nonelderly adults is 10 mg. For certain low weight individuals, 5 mg may be a sufficient dose. Although the risk of certain adverse events associated with the use of zaleplon capsules appears to be dose dependent, the 20 mg dose has been shown to be adequately tolerated and may be considered for the occasional patient who does not benefit from a trial of a lower dose. Doses above 20 mg have not been adequately evaluated and are not recommended. Zaleplon capsules should be taken immediately before bedtime or after the patient has gone to bed and has experienced difficulty falling asleep (see PRECAUTIONS ). Taking zaleplon capsules with or immediately after a heavy, high-fat meal results in slower absorption and would be expected to reduce the effect of zaleplon capsules on sleep latency (see Pharmacokinetics under CLINICAL PHARMACOLOGY ). Special Populations Elderly patients and debilitated patients appear to be more sensitive to the effects of hypnotics, and respond to 5 mg of zaleplon capsules. The recommended dose for these patients is therefore 5 mg. Doses over 10 mg are not recommended. Hepatic insufficiency: Patients with mild to moderate hepatic impairment should be treated with zaleplon capsules 5 mg because clearance is reduced in this population. Zaleplon capsules are not recommended for use in patients with severe hepatic impairment. Renal insufficiency: No dose adjustment is necessary in patients with mild to moderate renal impairment.

Complex Sleep Behaviors Complex sleep behaviors including sleep-walking, sleep-driving, and engaging in other activities while not fully awake may occur following the first or any subsequent use of zaleplon. Patients can be seriously injured or injure others during complex sleep behaviors. Such injuries may result in a fatal outcome. a. Other complex sleep behaviors (e.g., preparing and eating food, making phone calls, or having sex) have also been reported. Patients usually do not remember these events. Post-marketing reports have shown that complex sleep behaviors may occur with zaleplon alone at recommended dosages, with or without the concomitant use of alcohol or other central nervous system (CNS) depressants. CNS-Depressant Effects and Next-Day Impairment Zaleplon, like other hypnotics, has CNS-depressant effects. Because of the rapid onset of action, zaleplon should only be ingested immediately prior to going to bed or after the patient has gone to bed and has experienced difficulty falling asleep . Coadministration with other CNS depressants (e.g., benzodiazepines, opioids, tricyclic antidepressants, alcohol) increases the risk of CNS depression. Dosage adjustments of zaleplon and of other concomitant CNS depressants may be necessary when zaleplon is administered with such agents because of the potentially additive effects. The use of zaleplon with other sedative-hypnotics at bedtime or the middle of the night is not recommended (see DOSAGE AND ADMINISTRATION ).

The premarketing development program for zaleplon included zaleplon exposures in patients and/or normal subjects from 2 different groups of studies: approximately 900 normal subjects in clinical pharmacology/pharmacokinetic studies; and approximately 2,900 exposures from patients in placebo-controlled clinical effectiveness studies, corresponding to approximately 450 patient exposure years. The conditions and duration of treatment with zaleplon varied greatly and included (in overlapping categories) open-label and double-blind phases of studies, inpatients and outpatients, and short-term or longer-term exposure. Adverse reactions were assessed by collecting adverse events, results of physical examinations, vital signs, weights, laboratory analyses, and ECGs. Adverse events during exposure were obtained primarily by general inquiry and recorded by clinical investigators using terminology of their own choosing. Consequently, it is not possible to provide a meaningful estimate of the proportion of individuals experiencing adverse events without first grouping similar types of events into a smaller number of standardized event categories. In the tables and tabulations that follow, COSTART terminology has been used to classify reported adverse events. The stated frequencies of adverse events represent the proportion of individuals who experienced, at least once, a treatment-emergent adverse event of the type listed. An event was considered treatment-emergent if it occurred for the first time or worsened while receiving therapy following baseline evaluation.

Metabolism

The pharmacokinetics of zaleplon have been investigated in more than 500 healthy subjects (young and elderly), nursing mothers, and patients with hepatic disease or renal disease. In healthy subjects, the pharmacokinetic profile has been examined after single doses of up to 60 mg and once-daily administration at 15 mg and 30 mg for 10 days.

Signs and Symptoms Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing. Overdose is usually manifested by degrees of central nervous system depression ranging from drowsiness to coma. In mild cases, symptoms include drowsiness, mental confusion, and lethargy; in more serious cases, symptoms may include ataxia, hypotonia, hypotension, respiratory depression, rarely coma, and very rarely death. Loss of consciousness, in addition to signs and symptoms consistent with CNS depressants as described above, have been reported following zaleplon overdose. Individuals have fully recovered from zaleplon overdoses of greater than 200 mg (10 times the maximum recommended dose of zaleplon). Rare instances of fatal outcomes following overdose with zaleplon, most often associated with overdose of additional CNS depressants, have been reported. Recommended Treatment General symptomatic and supportive measures should be used along with immediate gastric lavage where appropriate. Intravenous fluids should be administered as needed.

• Jun 6, 2008ANDAANDA078829Aurobindo Pharma
• Jun 6, 2008ANDAANDA078989Unichem
• Jun 6, 2008ANDAANDA077237Hikma
• Sep 17, 2009ANDAANDA090374Orbion Pharms

1. 1Drug Ineffective1409.0%
2. 2Nausea1127.2%
3. 3Completed Suicide885.6%
4. 4Insomnia805.1%
5. 5Fall795.1%
6. 6Headache795.1%
7. 7Anxiety774.9%
8. 8Fatigue724.6%
9. 9Pain724.6%
10. 10Dizziness603.8%
11. 11Diarrhoea583.7%
12. 12Depression513.3%
13. 13Malaise513.3%
14. 14Off Label Use503.2%
15. 15Vomiting493.1%

The 10 most recently updated of 39 ClinicalTrials.gov registrations naming Zaleplon as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Self-administered ONe-of-a Kind Approach to Epilepsy Therapy Through a Web-based Music Application
  Recruiting · Interventional · 24 enrolled · Dartmouth-Hitchcock Medical Center
  NCT06425029updated 2026-05-20
• A Study to Evaluate the Efficacy and Safety of Sotagliflozin in Symptomatic Obstructive and Non-obstructive Hypertrophic Cardiomyopathy
  Recruiting · Phase 3 · Interventional · 500 enrolled · Lexicon Pharmaceuticals
  NCT06481891updated 2026-05-18
• Effect of Music on Surgical Performance During Artificial Intelligence-Based Simulation Training
  Completed · Interventional · 97 enrolled · McGill University
  NCT07111481updated 2026-05-06
• The Study in Outpatient Medicine Using Nudges to Improve Sleep
  Enrolling by invitation · Interventional · 444 enrolled · University of Southern California
  NCT06640023updated 2026-04-27
• A Pilot Randomized Controlled Trial of a Social Network Intervention
  Recruiting · Interventional · 70 enrolled · University of Rochester
  NCT07393529updated 2026-04-15
• A Single Arm Pilot Trial of a Social Network Intervention
  Recruiting · Interventional · 330 enrolled · University of Rochester
  NCT05745038updated 2026-03-31
• Effect of Music on Pain, Anxiety, and Behavior in Anxious Children During Molar Restorations
  Completed · Interventional · 45 enrolled · Mersin University
  NCT07144579updated 2025-08-27
• The Effects of Different Time Reminder On Surgical Hand Scrubing
  Active not recruiting · Interventional · 66 enrolled · Saglik Bilimleri Universitesi Gulhane Tip Fakultesi
  NCT07005635updated 2025-06-05
• Investigation of the Effect of muSic on the Stress of Preterm neONates Through innovATive Applications (SONATA)
  Recruiting · Interventional · 70 enrolled · University of West Attica
  NCT06650189updated 2025-04-01
• The Effect of Classical Music on Dental Students' Stress and Anxiety During the COVID-19 Pandemic
  Completed · Interventional · 46 enrolled · Karabuk University
  NCT06787833updated 2025-01-22

Frequently asked questions

How does Zaleplon work?

Mechanism-of-action classes: GABA A Agonists; GABA A Receptor Interactions.

What is Zaleplon used for?

According to FDA labeling, Zaleplon carries indications including: Zaleplon capsules are indicated for the short-term treatment of insomnia. Zaleplon capsules have been shown to decrease the time to sleep onset for up to 30 days in controlled clinical studies (see Clinical Trials under CLINICAL PHARMACOLOGY ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Zaleplon?

Zaleplon is classified as Benzodiazepine related drugs, gamma-Aminobutyric Acid A Receptor Agonist, GABA A Agonists, GABA A Receptor Interactions, Central Nervous System Depression, Gamma Amino Butyric Acid (GABA) Activity Alteration.

What are the contraindications for Zaleplon?

Zaleplon labeling lists contraindications including: Zaleplon is contraindicated in patients: who have experienced complex sleep behaviors after taking zaleplon (see WARNINGS ) with hypersensitivity to zaleplon or any excipients in the formulation (see PRECAUTIONS ). Always consult the full prescribing information and a clinician.