Short acting sleep drug, useful in patients that awaken during the night and have difficulty falling back asleep.
Zaleplon
Pregnancy category C (Risk not ruled out)
Routes of administration oral.
US: Schedule IV
Pharmacokinetic data
Bioavailability 30%.
Metabolism, hepatic.
Biological half-life 1–1.5 h.
Excretion renal.
Marketed under the brand names Sonata.
A sedative-hypnotic, almost entirely used for the management/treatment of insomnia.
It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class.
Slightly effective in the management/treatment of insomnia, primarily characterized by difficulty falling asleep.
Because of its ultrashort elimination half-life, may not be effective in reducing premature awakenings.
It may result in an impaired ability to drive the next day, though it has proven promising when compared to other sedative/hypnotics and next-day residual sedation.
Has fewer adverse effects than benzodiazepines.
Should not be combined with alcohol, as both modulate GABAA receptor sites, in a synergistic manner increase the chances of fatal respiratory depression and asphyxiation from vomiting.
Not recommended for chronic use in the elderly.
The elderly are more sensitive to the adverse effects of zaleplon such as cognitive side effects.
May increase the risk of injury among the elderly.
It should not be used while in pregnancy or lactation, and in patients with a history of alcohol or drug abuse, psychotic illness or depression.
Nonbenzodiazepines such as zaleplon appear to offer few significant advantages in efficacy or tolerability among elderly individuals.
Long-term use of sedative/hypnotics for insomnia: because of potential adverse drug effects as cognitive impairment, amnesia, sedation, musculoskeletal impairment, and subsequently an increased risk of falling and accidents.
Does not to cause an increase in traffic accidents, as compared to other hypnotics currently.
Recommended doses are typically 5–20 mg before bed.
Withdrawal syndrome, following abrupt discontinuation ranges from mild dysphoria and insomnia to more serious cases that include abdominal and muscle cramps, vomiting, sweating, tremors, convulsions, and the seizure threshold is further lowered, wherein coma and death are possible outcomes if untreated.
Exhibits far fewer rebound effects when compared with other nonbenzodiazepines.
Like zolpidem, zopiclone, or eszopiclone, it is a specific agonist at the benzodiazepine GABAA α1 sub-receptor site, and also modulates the GABAA sub-sites, α2 and α3, to a lesser degree. It
It is not an anticonvulsant
The ultrashort half-life provides advantage over other hypnotics.
Lacks next-day residual effects on driving and other performance-related skills.
Appears to induce sleep without disrupting the natural sleep pattern.
Associated, with an increased in slow wave deep sleep with rapid onset of hypnotic action.
The elimination half-life is about 1–1.5 hours.
Absorption rate is rapid and the onset of therapeutic effects is typically within 5–15 minutes following ingestion.
An ultrashort-acting sedative-hypnotic drug for the treatment of insomnia.
Zaleplon is primarily metabolized by aldehyde oxidase, and its half-life can be affected by substances which inhibit or induce aldehyde oxidase.
Reaches full concentration in about one hour.
It is extensively metabolised with less than 1% of it excreted intact in urine.
Has the potential to be a drug of abuse, and has been found to have an abuse potential similar to benzodiazepine and benzodiazepine-like hypnotics.
A common effect of abuse is the occurrence of hallucinations.
Anterograde amnesia can occur.
In combination with alcohol can result in fatal respiratory depression.