Index of drugs

Short-term treatment of insomnia manifested by difficulty in falling asleep. The drug is recommended only in patients with severe disorders, preventing a normal lifestyle or causing severe discomfort.

1 capsule contains 5 mg or 10 mg of zaleplon.

A sleeping pill from the pyrazolopyrimidine group. It binds to the benzodiazepine GABA receptor_AND, found in neural structures o.u.n. Selectively binds to the omega-1 receptor of the GABA complex_AND, located on the alpha receptor subunit. The GABA receptor acts as a chloride ion channel, and the binding of zaleplon to the t-butylobicycloophosphophate (TBPS) site on the receptor causes an influx of Cl ions.^- with hyperpolarization of the cell membrane, leading to the inhibition of neuronal conduction, and subsequent to hypnotic, sedative, anxiolytic, anticonvulsive and amnesty effects. Following oral administration, zaleplon is absorbed quickly and almost completely (at least 71%). The maximum concentration in the blood reaches within 0.5-1 h. Zaleplon is metabolized in the liver (the so-called first-pass effect), and its bioavailability is about 30%. It binds to plasma proteins in 45-65%. It is metabolized primarily in the liver, where it is converted to 5-oxy-zaleplon as a result of the action of an aldehyde oxidase enzyme. To a lesser extent, it breaks down the 3A4 cytochrome P-450 isoenzyme to deethyl zaleplon, which undergoes rapid conversion, presumably thanks to the aldehyde oxidase to 5-oxy-deethyl zaleplon. Then, both metabolites - 5-oxy-zaleplon and 5-oxy-deetylozaleplon - are converted to glucuronides and are excreted in the urine (32% of the dose), while 17% of the drug is excreted in the faeces - mainly in the form of 5-oxy-zaleplon. Less than 1% of zaleplon is excreted unchanged. The half-life of zaleplon is relatively short and is about 1 hour. Food, especially high-fat, affects the absorption of the drug, prolonging t_max up to 2 h and reducing the maximum concentration by 35%; however, it does not affect AUC and half-life.

Hypersensitivity to zaleplon or other components of the preparation. Severe hepatic failure. Sleep apnea syndrome. Severe respiratory failure. Myasthenia gravis. Children (under the age of 18).

Alternative therapy should be considered when waking up early in the morning (short half-life of zaleplon). Caution use with drugs that affect CYP3A4. The drug should not be used in people with symptoms of depression. Exercise caution in people who abuse alcohol or medication. Special care should be taken in people with chronic respiratory failure. Do not use the drug as a basic psychosis treatment. Use with caution in patients with mild or moderate hepatic impairment and in the elderly (dose modification) and in patients with impaired renal function.

You should not use zaleplon in pregnant women. The use of zaleplon in high doses during the last period of pregnancy or during delivery may cause neonatal hypothermia, hypotension or moderate respiratory depression. The drug in a small amount penetrates into the milk of lactating women - do not use the drug in women who are breastfeeding.

Common: amnesia, paresthesia, drowsiness, ataxia, confusion; painful menstruation. Uncommon: anorexia, asthenia, decreased sensation of touch, malaise, hypersensitivity to light; impaired concentration, apathy, depersonalization, depression, dizziness, hallucinations, hyperaesthesia, olfactory hallucinations, diplopia, blurred speech, visual field disorders, psychic and paradoxical reactions (most commonly in children and the elderly); nausea. Very rare: anaphylactic and anaphylactoid reactions. The use of benzodiazepine derivatives can lead to mental and physical addiction. Discontinuation of therapy may cause symptoms of abstinence syndrome or rebound insomnia.

Treatment should last as short as possible, maximum 2 weeks.
Orally.Adults: the recommended daily dose is 10 mg. The drug should be taken immediately before going to bed, at least 4 hours before waking up. Do not use a daily dose of more than 10 mg. Do not give your second dose the same night. In patients with mild or moderate hepatic impairment and in the elderly, a 5 mg dose is recommended.
Do not use the drug during or after a meal.