Pharmacological action of Zaleplon

Hypnotic pyrazolo-pyrimidine-type chemical structure differs from other benzodiazepines and sleeping pills. Exhibits high selectivity and low affinity for the benzodiazepine receptor type 1. Also has sedative, anxiolytic, muscle relaxant, anticonvulsant effect.

Pharmacokinetics

After oral administration, absorption is approximately 71%. Plasma concentration is directly proportional to dose. Cmax in the plasma levels achieved after 1 h. As a result, first-pass metabolism the absolute bioavailability of approximately 30%. Binding to plasma proteins - about 60%. Excreted in breast milk. Metabolized to form several inactive metabolites. At a daily dose of 30 mg of cumulation is not observed. T1 / 2 of zaleplon - about 1 hour Excreted as metabolites in the urine and 71% in the faeces - 17%.

Statement

Severe sleep disturbances with difficulty falling asleep.

Dosage and administration

Is the inside just before bedtime, if the patient feels that he can not sleep. We do not recommend readmission for one night. Single dose - 10 mg. The maximum dose - 10 mg / day. Due to a more pronounced sensitivity to hypnotic drugs for the elderly dose of 5 mg / day. Duration of use - no more than 2 weeks.

Side effects

Central nervous system: common - headache, weakness, drowsiness, dizziness, and possible anterograde amnesia (especially when taken in high doses), accompanied by behavioral disorders, symptoms of latent depression, physical and psychological dependence, drug abuse, mainly in the elderly - paradoxical reactions (anxiety, restlessness, irritability, aggression, hallucinations, impaired perception, anger, nightmares, behavioral disorders).

Contraindications

Severe hepatic insufficiency, sleep apnea syndrome, severe respiratory failure, severe myasthenia gravis, lactation, childhood and adolescence to 18 years, hypersensitivity to zaleplon.

Pregnancy and lactation

Safe and well-controlled safety studies in pregnancy zaleplon has been done, so not recommended.
Women of childbearing age applying zaleplon should inform your doctor about planned or unwanted pregnancy.
If necessary, use of zaleplon in the III trimester of pregnancy or the use of high doses during labor should bear in mind the possibility of neonatal hypothermia, hypotonia, moderate respiratory distress.

Zaleplon is excreted in breast milk, so use during lactation is contraindicated.

Cautions

With extreme caution in patients with chronic respiratory failure, in the presence of alcohol and drug dependence.
Zaleplon is not recommended for use as the primary drug for psychosis.
Zaleplon is not intended to treat depression and related conditions increased anxiety, as able to provoke a suicide attempt. If necessary, use in patients with depression zaleplon should be used in the lowest effective dose to avoid deliberate overdose.
If, after a brief application of zaleplon is normal sleep or sleep disorder progresses, the diagnosis should be reconsidered.
The necessity of zaleplon than 2 weeks are determined individually after clinical examination of the patient.
In renal insufficiency, mild to moderate severity dosage adjustment is required. The data on the safety of zaleplon in renal failure, severe missing.
After several weeks of treatment may develop addiction and reducing the effectiveness of zaleplon.
Perhaps the development of physical and psychological dependence, the probability of which is associated with taking high doses of zaleplon, long-term use and availability of alcohol and drug dependence.
With physical dependence formed abrupt withdrawal of the drug leads to the development of withdrawal symptoms: headache, myalgia, pronounced anxiety, increased tension, anxiety, irritability, confusion. In severe cases, can autoaggression, depersonalization, hearing loss, paresthesias in the extremities, increased reaction to light, sound and physical stimuli, hallucinations, seizures.
After cessation of treatment may be transient manifestations of insomnia, but in a more pronounced form. It is possible the development of associated symptoms such as mood disorder, a sense of heightened anxiety and concern.
After a few hours after taking zaleplon may develop anterograde amnesia and psychomotor disturbances. In order to avoid the development of these symptoms should be taken zaleplon only if the patient has a chance of uninterrupted sleep, at least in the first 4 h after administration of zaleplon.
Treatment should be discontinued zaleplon in the case of high anxiety, agitation, irritability, aggression, disorders of perception, fits of anger, nightmares, hallucinations, and especially behavior problems. Elderly patients most likely to develop such symptoms.
Zaleplon can be used in elderly patients, including 75 years of age.

Effects on ability to drive and control mechanisms

Negative impact on ability to drive vehicles. During the period of treatment should exercise extreme caution when engaging in potentially hazardous activities that require concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of antipsychotics, hypnotics, anxiolytics, antidepressants, antiepileptic drugs, anesthetics, histamine H1-blocker receptors with sedative effect of opioid analgesics, ethanol is increased sedation zaleplon.
With simultaneous use of zaleplon, and opioid analgesics may cause euphoria, which leads to dependence.
Cimetidine, which is a nonspecific inhibitor of liver enzymes (aldehyde oxidase and CYP3A4), increases the concentration of zaleplon in the blood plasma by 85% (combination use with caution).
Selective blockers of CYP3A4 (including ketoconazole, erythromycin) increase the concentration of zaleplon in the blood plasma, with the possible strengthening of zaleplon sedation (dose adjustment is required).
Strong inducers of CYP3A4, such as rifampicin, carbamazepine, phenobarbital, derivatives can reduce by 25% the concentration of zaleplon in the blood plasma and its effect.

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