Zaleplon



Zaleplon
Systematic (IUPAC) name
N-[3-(7-cyano-1,5,9-triazabicyclo[4.3.0]nona-
2,4,6,8-tetraen-2-yl)phenyl]-N-ethyl-acetamide
Identifiers
CAS number 151319-34-5
ATC code N05CF03
PubChem 5719
DrugBank APRD00411
Chemical data
O 
Mol. mass 305.34
Pharmacokinetic data
Bioavailability 30% (oral)
Metabolism Hepatic
Half life 1 hour
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status

Schedule IV(US)

Routes Oral

Zaleplon (marketed under the brand names Sonata and Starnoc) is a sedative/pyrazolopyrimidine class.

Chemistry

Pure zaleplon in its solid state is a white to off-white powder that has very low pH range is between 1 and 7.

Pharmacology

Taken orally, zaleplon reaches full concentration in approximately one hour. It is extensively metabolised, into 5-oxo-zaleplon and 5-oxo-desethylzaleplon (the latter via desethylzaleplon), with less than 1% of it excreted intact in urine.

Zaleplon interacts with the benzodiazepine, zaleplon can cause similar effects: anterograde amnesia (forgetting the period during the effects) as the most common.

Zaleplon is primarily metabolised by aldehyde oxidase, and its half-life can be affected by substances which inhibit or induce aldehyde oxidase.

A meta-analysis of randomised controlled clinical trials which compared benzodiazepines against Zaleplon or other Z Drugs such as benzodiazepines in terms of sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia and daytime alertness.[1]

Zaleplon has a pharmacological profile similar to benzodiazepines, that is characterized by an increase in SWDS with rapid onset of hypnotic action. Zaleplon is a selective full agonist for the EEG power density in the delta frequency band and a decrease in the energy of the theta frequency band. In tests on rabbits zaelplon shows drowsy pattern of spontaneous EEG characterized by high-voltage slow waves and desynchronization of hippocampal theta waves and an increase in the energy of the delta frequency band on the spectral analysis of the electroencephalogram.[2]

Side-effects

Zaleplon may cause hallucinations, abnormal behavior, severe confusion, day-time drowsiness, dizziness or lightheadedness, unsteadiness and/or falls, double vision or other vision problems, agitation, headache, nausea, vomiting, diarrhea or abdominal pain, depression, muscle weakness, tremor, vivid or abnormal dreams and memory difficulties or amnesia.

Zaleplon is habit-forming, meaning addiction may occur. Stopping this medication suddenly after prolonged or frequent use may cause withdrawal effects such as mood changes, anxiety, and restlessness.

Recreational use

Zaleplon (Sonata) has a relatively high potential to be abused. Often this use involves a different delivery method (insufflation) to induce effects faster.  

The side effects of zaleplon are greatly increased when taken improperly, especially retrograde amnesia - the inability to remember the time during which one was under the influence of the drug. Zaleplon is a benzodiazepine drugs, but that they still carried a risk higher than first believed. The study specifically mentions persons with prior substance abuse problems as individuals with a high risk for addiction to nonbenzodiazepine type drugs. [3]

References

  1. ^ Dündar, Y; Dodd S, Strobl J, Boland A, Dickson R, Walley T. (Jul 2004). "Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis.". Hum Psychopharmacol. 19 (5): 305-22. PMID 15252823.
  2. ^ Noguchi H; Kitazumi K, Mori M, Shiba T. (Mar 2004). "Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats." (pdf). J Pharmacol Sci. 94 (3): 246-51. PMID 15037809.
  3. ^ http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14519173&dopt=Abstract
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Zaleplon". A list of authors is available in Wikipedia.