Zolsana (Tablets) Instructions for Use

ATC Code

N05CF02 (Zolpidem)

Active Substance

Zolpidem (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Hypnotic drug

Pharmacotherapeutic Group

Hypnotic agent

Pharmacological Action

A hypnotic agent from the imidazopyridine group, a specific agonist of central nervous system ω₁-receptors. It shortens the time to fall asleep, reduces the number of nocturnal awakenings, increases the duration of sleep, and improves its quality. It prolongs sleep stage II and deep sleep stages (III and IV), without affecting the duration of the REM sleep phase.

Central muscle relaxant and anticonvulsant effects are also characteristic.

Pharmacokinetics

After oral administration, C_max in plasma is observed within 0.5-3 hours. The bioavailability is about 70%.

Plasma protein binding is 92%. There is a linear relationship between the dose and the plasma concentration of the active substance. V_d is 0.54±0.02 L/kg.

Zolpidem is metabolized in the liver and excreted in the urine (56%) and feces (37%) as inactive metabolites. It does not induce hepatic microsomal enzymes.

T_1/2 ranges from 0.7 hours to 3.5 hours (average 2.4 hours).

In elderly individuals, a decrease in the plasma clearance of zolpidem is possible, while T_1/2 increases slightly (on average up to 3 hours), C_max increases by 50%, and V_d decreases to 0.34±0.05 L/kg.

In patients with severe renal impairment, the clearance of zolpidem decreases slightly; other pharmacokinetic parameters do not change.

In patients with severe hepatic impairment, the bioavailability of zolpidem increases, clearance decreases somewhat, and T_1/2 increases to 10 hours.

Indications

Episodic, transient, and chronic insomnia.

ICD codes

Dosage Regimen

Administer Zolsana tablets orally. Take the tablet immediately before bedtime, ensuring you have at least 7-8 hours dedicated to sleep.

For adults under 65 years, the standard single dose is 10 mg. Do not exceed this dose without medical reevaluation.

For patients over 65 years of age, initiate therapy at a reduced single dose of 5 mg.

For patients with concomitant hepatic impairment, also initiate therapy at a reduced single dose of 5 mg.

The maximum daily dose for adults under 65 is 10 mg. The maximum dose for elderly or hepatically impaired patients is 5 mg.

Limit the total duration of treatment. The typical course ranges from a few days to 4 weeks, including any gradual dose reduction period.

Do not exceed the prescribed dose. Monitor for efficacy and adverse reactions, particularly in elderly patients.

When discontinuing treatment, reduce the dose gradually to minimize the risk of withdrawal symptoms and rebound insomnia.

Avoid consumption of alcoholic beverages during therapy. Use with extreme caution with other central nervous system depressants.

Adverse Reactions

From the digestive system in some cases – abdominal pain, nausea, vomiting, diarrhea.

From the central and peripheral nervous system depending on the dose and individual sensitivity (especially in elderly patients) – dizziness, imbalance, ataxia, headache, daytime sleepiness, impaired attention, muscle weakness, diplopia, anterograde amnesia, paradoxical or psychopathological reactions; when used in high doses or during long-term treatment, rebound insomnia is possible.

Allergic reactions skin rash, itching.

Other rarely – disorders of libido; development of tolerance, formation of mental and physical dependence (when used for several weeks).

Contraindications

Severe respiratory failure, sleep apnea, severe hepatic failure, childhood and adolescence under 15 years, first trimester of pregnancy, lactation (breastfeeding), hypersensitivity to zolpidem.

Use in Pregnancy and Lactation

Zolpidem is contraindicated for use during pregnancy and during lactation (breastfeeding).

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency. In cases of hepatic impairment, a dose reduction of the drug may be necessary.

Pediatric Use

Contraindicated in children and adolescents under 15 years of age.

Special Precautions

Use is not recommended in myasthenia gravis.

Use with caution in patients with respiratory failure. In cases of hepatic impairment, a dose reduction may be necessary.

When discontinuing therapy, the dose should be reduced gradually. The likelihood of developing tolerance increases with long-term use of zolpidem.

During treatment, alcohol consumption should be avoided while on therapy.

Effect on ability to drive vehicles and operate machinery

During the treatment period, one should refrain from potentially hazardous activities that require concentration and high speed of psychomotor reactions.

Drug Interactions

With simultaneous use with opioid analgesics, antitussives, barbiturates, antidepressants, sedatives, antihistamines, benzodiazepines, clonidine, neuroleptics, ethanol, the development of symptoms of central nervous system and respiratory center depression is possible.

With simultaneous use with rifampicin, the plasma concentration of zolpidem decreases, which is accompanied by a reduction in its hypnotic effect. The interaction is due to the induction of the CYP3A4 isoenzyme.

With simultaneous use with inducers of the CYP3A4 isoenzyme (including carbamazepine, phenytoin), a possibility of decreased plasma concentration of zolpidem is assumed.

With simultaneous use with clozapine, the risk of collapse, circulatory arrest, and respiratory arrest increases.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.