Introduction
Eplon Capsule 5 mg is a sedative/hypnotic, mainly used for insomnia. It is known as a nonbenzodiazepine hypnotic. Eplon Capsule 5 mg interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Eplon Capsule 5 mg is a schedule IV drug in the United States.
Uses
Eplon Capsule 5 mg is a sedative used for short term treatment of insomnia in adults.
For the treatment of short-term treatment of insomnia in adults.
Associated Conditions
Pharmacodynamics
Eplon Capsule 5 mg is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Eplon Capsule 5 mg is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Eplon Capsule 5 mg also binds selectively to the CNS GABAA-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors.
Mechanism of Action
Eplon Capsule 5 mg exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Eplon Capsule 5 mg also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding.
Absorption
Absorption Eplon Capsule 5 mg is rapidly and almost completely absorbed following oral administration.
Volume of Distribution
- 1.4 L/kg
Protein Binding
Approximately 60% (in vitro plasma protein binding).
Route of Elimination
Eplon Capsule 5 mg is metabolized primarily by the liver and undergoes significant presystemic metabolism. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Renal excretion of unchanged zaleplon accounts for less than 1% of the administered dose.
Half Life
Approximately 1 hour
Clearance
- 1 L/h/kg
Toxicity
Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness
Food Interactions
- Avoid alcohol. Ingesting alcohol may increase the CNS depressant effects of zaleplon.
- Do not take with or immediately after a high-fat meal. The effects of zaleplon are reduced when taken with a high-fat meal.
Dosage
Eplon Capsule 5 mg should be taken immediately before bedtime. Taking Eplon Capsule 5 mg with or immediately after a heavy, high fat meal results in slower absorption and would be expected to reduce the effect of Eplon Capsule 5 mg on sleep latency. Elderly patients and debilitated patients appear to be more sensitive to the effects of hypnotic, and respond to 5 mg of Eplon Capsule 5 mg. The recommended dose for these patients is therefore 5 mg, doses over 10 mg are not recommended.
For patients with mild to moderate renal impairment, no dose adjustment is necessary.
An initial dose of 5 mg should be given to patients concomitantly taking Cimetidine because Eplon Capsule 5 mg clearance is reduced in this population.
Pediatric use: The safety and effectiveness of Eplon Capsule 5 mg in pediatric patients have not been established.
