Eplon

Approved:

• Short-term treatment of insomnia characterized by difficulty with sleep initiation.

Clinically Accepted Off-label:

• Middle-of-the-night awakenings (due to rapid onset and ultra-short half-life).
• Used in controlled settings for pre-scheduled rest periods (e.g., pre-flight naps for shift workers or military use).

রেজিস্টার্ড চিকিৎসকের নির্দেশনা অনুযায়ী ঔষধ সেবন করুন।

Adults (≤ 65 years):

• Initial dose: 10 mg orally at bedtime or when unable to fall asleep.
• Dose range: 5–20 mg once nightly.
• Take only when a full night (at least 4 hours) of sleep is possible.

Geriatric/Debilitated Patients:

• Start with 5 mg once nightly.
• Increased sensitivity to hypnotic effects—avoid higher doses unless necessary.

Pediatric Use (< 18 years):

• Not recommended or contraindicated.

Hepatic Impairment:

• Mild to moderate: Use with caution at 5 mg.
• Severe impairment: Contraindicated.

Renal Impairment:

• No adjustment needed in mild to moderate impairment.
• Use with caution in severe impairment due to limited data.

Drug Interactions:

• With cimetidine: Reduce zaleplon dose to 5 mg.

Administration Notes:

• Take immediately before bedtime.
• Do not take after a high-fat meal (may delay absorption).
• Avoid taking unless at least 4 hours of sleep time remain.

রেজিস্টার্ড চিকিৎসকের নির্দেশনা অনুযায়ী ঔষধ সেবন করুন।

Zaleplon is a non-benzodiazepine hypnotic of the pyrazolopyrimidine class. It binds selectively to the benzodiazepine site on the GABA-A receptor complex, with high affinity for receptors containing the α1 subunit. This enhances GABA-mediated neuronal inhibition, leading to rapid sleep induction. Unlike benzodiazepines, it has minimal effects on sleep architecture and is specific to sleep initiation rather than maintenance.

• Absorption: Rapid; peak plasma concentration within 1 hour.
• Distribution: Volume of distribution ~1.4 L/kg; 60% protein-bound.
• Metabolism: Extensively metabolized in the liver by aldehyde oxidase and, to a lesser extent, CYP3A4.
• Elimination: Half-life ~1 hour; metabolites are inactive and excreted primarily via urine.
• Special Populations: Exposure increased significantly in hepatic impairment; minor changes in renal impairment.

• Pregnancy: Insufficient human data. Animal studies show no major teratogenicity. Use only if benefits outweigh risks.
• Lactation: Excreted in low amounts in breast milk. Due to potential CNS depression in the infant, use is not recommended while breastfeeding. Caution advised if used.

• Primary: Sedative-Hypnotic.
• Subclass: Non-benzodiazepine GABA-A receptor modulator ("Z-drug").

• Hypersensitivity to zaleplon or any of its components
• Severe hepatic impairment
• History of complex sleep behaviors (e.g., sleep-driving) after previous sedative-hypnotic use
• Severe respiratory insufficiency
• Obstructive sleep apnea
• Myasthenia gravis
• Pediatric patients (<18 years)

• Complex Sleep Behaviors: Sleepwalking, driving, eating while not fully awake—may occur without memory. Discontinue immediately if these occur.
• CNS Depression: Additive sedation with alcohol, opioids, or other depressants.
• Next-Day Impairment: Possible if insufficient sleep time follows dose, or if taken with CNS depressants.
• Dependence and Abuse Potential: Especially in those with a history of substance abuse.
• Depression/Suicidality: May worsen symptoms—use caution in psychiatric illness.
• Hepatic Impairment: Increased drug exposure—dose adjustment or avoidance necessary.
• Angioedema/Anaphylaxis: Rare but potentially life-threatening allergic reactions.

Common:

• Headache
• Dizziness
• Drowsiness
• Lightheadedness

Less Common / Serious:

• Memory disturbance (anterograde amnesia)
• Sleep-related behaviors (driving, cooking, talking in sleep)
• Hallucinations
• Coordination problems
• Allergic reactions (rash, angioedema)
• Respiratory depression (especially with CNS depressants)
• Rebound insomnia or withdrawal symptoms with abrupt discontinuation

• CNS Depressants (e.g., alcohol, opioids): Additive sedation and respiratory depression risk.
• Cimetidine: Inhibits metabolism; increases zaleplon levels—reduce zaleplon dose to 5 mg.
• CYP3A4 inhibitors (e.g., ketoconazole): May increase zaleplon exposure.
• CYP3A4 inducers (e.g., rifampin): May reduce efficacy.
• No significant interaction: With digoxin, warfarin, or ibuprofen.

• Regulatory agencies emphasize boxed warnings on complex sleep behaviors for all Z-drugs, including zaleplon.
• Current insomnia guidelines recommend cognitive behavioral therapy as first-line treatment, with short-term use of agents like zaleplon as secondary options.
• Updated guidelines discourage chronic use and emphasize patient education on risks.

• Store at 20–25°C (68–77°F).
• Allowable range: 15–30°C (59–86°F).
• Protect from light and moisture.
• Do not freeze.
• No reconstitution or refrigeration required.