Description
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Zaleplon is primarily metabolized by aldehyde oxidase. Zaleplon is rapidly and almost completely absorbed following oral administration. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Zaleplon is primarily metabolized by aldehyde oxidase to form 5-oxo-zaleplon. Zaleplon is metabolized to a lesser extent by cytochrome P450 (CYP) 3A4 to form desethylzaleplon, which is quickly converted, presumably by aldehyde oxidase, to 5-oxo-desethylzaleplon. These oxidative metabolites are then converted to glucuronides and eliminated in urine. All of zaleplon's metabolites are pharmacologically inactive (RxList, A308). Route of Elimination: Zaleplon 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
- Uses/Sources: For the treatment of short-term treatment of insomnia in adults (A308).
- Health Effects: Angina pectoris, bundle branch block, hypertension, hypotension, palpitation, syncope, melena, mouth ulceration, rectal hemorrhage, stomatitis, dysphagia, enteritis, gum hemorrhage, diabetes mellitus, goiter, hypothyroidism, arthrosis, bursitis, hyperesthesia, hyperkinesia, hypotonia, incoordination, insomnia, libido decreased, neuralgia, nystagmus, dry skin, eczema, maculopapular rash, skin hypertrophy, dysuria, hematuria, impotence, kidney calculus, kidney pain, urinary retention, and vaginal hemorrhage (RxList, A308). They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.
- Symptoms: Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness
- Treatment: General symptomatic and supportive measures should be used along with immediate gastric lavage where appropriate. Intravenous fluids should be administered as needed. As in all cases of drug overdose, respiration, pulse, blood pressure, and other appropriate signs should be monitored and general supportive measures employed. Hypotension and CNS depression should be monitored and treated by appropriate medical intervention. (L1712)
- Route of Exposure: Ingestion (RxList, A308); inhalation (RxList, A308); dermal (RxList, A308); eye contact (RxList, A308). Absorption Zaleplon is rapidly and almost completely absorbed following oral administration.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Gamma-aminobutyric acid receptor subunit alpha-1 Translocator protein |
Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex.Zaleplon binds selectively to the brain alomega-1 receptor situated on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding. |
17016423 17139284 |
Zaleplon Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Hepatic Encephalopathy | 14.71 |
|
Autism | 11.4 |
|
Ataxia | 8.12 |
|
Generalized Epilepsy With Febrile Seizures Plus, Type 3 | 7.09 |
|
Generalized Epilepsy With Febrile Seizures Plus, Type 1 | 6.39 |
|
Myoclonic Epilepsy, Juvenile | 5.82 |
|
Febrile seizures | 5.7 |
|
Essential tremor | 5.43 |
|
Epilepsy, Absence | 5.2 |
|
Epilepsies, Myoclonic | 5.18 |
|
Ovarian Cysts | 5.13 |
|
Amyotrophic lateral sclerosis 1 | 5.02 |
|
Alcohol dependence | 4.94 |
|
Respiratory Distress Syndrome, Adult | 4.9 |
|
Amphetamine-Related Disorders | 4.62 | |
Schizophrenia | 4.34 |
|
Cocaine dependence | 4.07 |
|
Prostatic Neoplasms | 3.87 |
|