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Zaleplon - instructions for use, reviews, analogs and forms of release (capsules or tablets 5 mg and 10 mg) of the drug for the treatment of sleep disorders or insomnia in adults, children and pregnancy. Composition and alcohol

Zaleplon - instructions for use, reviews, analogs and forms of release (capsules or tablets 5 mg and 10 mg) of the drug for the treatment of sleep disorders or insomnia in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Zaleplon. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Zaleplon in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Zaleplon in the presence of existing structural analogues. Use for the treatment of sleep disorders or insomnia in adults, children, as well as during pregnancy and lactation. The composition of the drug and its interaction with alcohol.

 

Zaleplon - a hypnotic pyrazolo-pyrimidine type, differs in chemical structure from benzodiazepines and other hypnotics. Selectively binds to type 1 benzodiazepine receptors (omega-1).

 

Significantly reduces the latent time of falling asleep, prolongs the time of sleep (in the first half of the night), does not cause changes in the ratio of different phases of sleep. When used in a dose of 5 mg and 10 mg for 2-4 weeks does not cause pharmacological tolerance. In addition, it has a sedative, slightly expressed anxiolytic, anticonvulsant and central muscle relaxant effect.

 

Excites benzodiazepine receptors (omega) receptor complexes GABA (gamma-aminobutyric acid) type A. Interaction with the omega receptors leads to the discovery of neuronal ionoform channels for chlorine ions, the development of hyperpolarization and the enhancement of inhibition processes in the central nervous system (CNS).

 

Composition

 

Zaleplon + auxiliary substances.

 

Pharmacokinetics

 

After oral administration Zaleplon quickly and almost completely (about 71%) is absorbed from the gastrointestinal tract (GIT). The plasma concentration is directly proportional to the dose.Taking the drug immediately after a meal can delay for 2 hours the time to reach its maximum concentration in the blood, without affecting the absorption of the drug. Binding to plasma proteins is about 60% (the probability of interaction with other drugs is very small). Excreted in breast milk. It is excreted as inactive metabolites, mainly with urine (71%) and feces (17%). Pharmacokinetics in elderly patients (including those older than 75 years) does not differ significantly from those in younger patients. Pharmacokinetics Zaleplona in patients with renal insufficiency does not differ significantly from that of healthy ones, although the level of inactive metabolites is higher.

 

Indications

  • insomnia or severe forms of sleep disturbance (difficulty falling asleep), leading to excessive fatigue, hampering daily activity and impairing performance.

 

Forms of release

 

Capsules 5 mg and 10 mg (sometimes mistakenly called pills).

 

Instructions for use and dosing regimen

 

The duration of therapy should not exceed 2 weeks.

 

The drug should be taken orally immediately before going to bed, 2 hours after eating or after the patient feels that he can not fall asleep.

 

The recommended adult dose is 10 mg.The maximum daily dose of 10 mg (the patient must be warned about the dangers of taking a second dose for one night).

 

With hepatic insufficiency of mild and moderate severity, the daily dose is 5 mg (because of delayed excretion from the body).

 

With renal failure of mild to moderate severity, dose adjustment is not required. Data on the safety of the drug in patients with severe renal failure are not available.

 

Side effect

  • abdominal pain;
  • nausea, vomiting;
  • diarrhea;
  • headache, dizziness;
  • weakness, increased drowsiness;
  • anterograde amnesia (impaired memory of events after the onset of the disease), accompanied by a violation of behavior;
  • depression;
  • paradoxical and psychic reactions (more often in elderly patients): anxiety, increased excitability, aggressiveness, paresthesia, fits of attacks, nightmares, hallucinations, psychosis, behavioral disorders;
  • the development of physical dependence with symptoms of withdrawal even when used in therapeutic doses (the appearance of initial symptoms of sleep disturbance in a more severe form, as well as mood changes, anxiety, anxiety);
  • withdrawal syndrome (headache, myalgia - muscle pain, increased irritability, confusion);
  • development of mental dependence leading to drug abuse;
  • ataxia (partial or complete loss of coordination of voluntary muscle movements);
  • tremor (fast, rhythmic movements of limbs or trunk);
  • increased irritability;
  • impaired perception;
  • autoaggression, depersonalization;
  • hearing loss, increased reaction to light, sound and physical stimuli;
  • epileptic seizures;
  • allergic reactions: skin rash, itching.

 

Contraindications

  • severe hepatic impairment;
  • syndrome of nocturnal apnea (respiratory arrest in sleep);
  • severe pulmonary insufficiency;
  • severe myasthenia gravis (an autoimmune neuromuscular disease characterized by pathologically fast fatigue of the striated muscles);
  • pregnancy;
  • lactation period (breastfeeding);
  • children and adolescents under 18;
  • hypersensitivity to the components of the drug.

 

Application in pregnancy and lactation

 

The drug Zaleplon is contraindicated in pregnancy and lactation.

 

When prescribing a drug for women of childbearing age, patients should be warned about the need to seek immediate medical attention in the case of conception or when planning a pregnancy.

 

In the case of using zaleplon in the third trimester of pregnancy, or when the drug is used in high doses of the drug during labor in a newborn, it is possible to develop hypothermia, muscle hypotension, and moderate respiratory insufficiency as a result of the pharmacological action of the drug. In newborns, whose mothers regularly took benzodiazepine or benzodiazepine-like medication in the last weeks of pregnancy, physical dependence and withdrawal symptoms may develop.

 

Use in children

 

Zaleplon is contraindicated in children and adolescents under 18 years of age, since the safety of the drug is not established.

 

Application in elderly patients

 

For elderly patients, the drug is prescribed in a dose of 5 mg (because of greater sensitivity to sleeping pills).

 

special instructions

 

The patient should be warned that the drug is not intended for long-term therapy and the possibility of developing a withdrawal syndrome after the completion of the drug Zaleplon.The course of taking the drug should be short and in no case should not exceed 2 weeks. Extend treatment only after a thorough clinical examination of the patient.

 

The drug can be prescribed for elderly patients (including those older than 75 years).

 

Sleep disorders can be the result of diseases (including mental illness). If, after a short-term use of Zaleplon, sleep does not return to normal or if sleep disturbance progresses, the clinical situation should be reassessed.

 

If the patient wakes up soon after midnight (due to the short half-life of Zaleplon), another drug with a longer half-life may be required. It should be warned patients about the need to use no more than 1 capsule per night.

 

The use of benzodiazepines and benzodiazepine-like short-acting drugs for several weeks can be accompanied by a decrease in the hypnotic effect.

 

The use of benzodiazepines and benzodiazepine-like drugs may lead to the development of physical and mental dependence, the likelihood of which increases when used in high doses, with prolonged therapy, chronic alcoholism and drug dependence in a patient's history.

 

With the resulting physical dependence, abrupt withdrawal of the drug leads to the development of withdrawal symptoms: headache, myalgia, severe anxiety, increased tension and irritability, psychomotor agitation, confusion. In severe cases, autoaggression, depersonalization, hearing loss, paresthesia in the extremities, an increased response to light, sound and physical stimuli, hallucinations and epileptic seizures are possible.

 

After the termination of Zaleplon application, the appearance of transient and more pronounced symptoms of insomnia (withdrawal syndrome) than at the beginning of treatment is possible. It is possible to develop other related phenomena (changes in mood, anxiety, sleep disturbance, anxiety).

 

Benzodiazepines and benzodiazepine-like drugs can cause the development of anterograde amnesia and impaired psychomotor functions. To avoid the development of these symptoms, the drug should be taken only if the patient has the possibility of continuous sleep, at least 4 hours after taking the drug.

 

Treatment zaleplon should be discontinued in the event of increased excitability, irritability, aggressiveness, impaired perception, nightmarish dreams, hallucinations, psychotic disorders and especially behavioral disorders. Elderly patients are most likely to develop such symptoms.

 

The drug is not intended to treat depression and / or anxiety, as it can be used to implement suicidal intentions, often accompanying depressive disorders. Patients with depression, the drug can be administered in a minimal dose to avoid a conscious overdose.

 

It is not recommended to prescribe the drug to patients with severe hepatic insufficiency because of the danger of encephalopathy.

 

When lactose intolerance, it should be noted that the capsule containing 5 mg zaleplon contains 67 mg lactose, 10 mg - 134 mg.

 

Impact on the ability to drive vehicles and manage mechanisms

 

During the period of application of the drug it is necessary to refrain from driving motor vehicles and taking classes that require an increased concentration of attention and speed of psychomotor reactions, since sedation, amnesia,a decrease in the concentration of attention and muscle strength adversely affect the ability for such activities.

 

Drug Interactions

 

Simultaneous reception of ethanol (alcohol) or ethanol-containing medicines increases the sedative effect of zaleplon.

 

Simultaneous use of antipsychotics (neuroleptics), other hypnotics, anxiolytic, sedative, antidepressant, anti-epileptic, antihistamines, anesthetics, opioid analgesics leads to an increase in sedation Zaleplona.

 

With simultaneous use with opioid analgesics, a manifestation of the euphoric effect of the latter, leading to the development of drug dependence, is possible.

 

With the simultaneous use of cimetidine (inhibitor aldehyde oxidase and CYP3A4) increases the concentration of zaleplon in plasma by 85%.

 

With the simultaneous use of selective inhibitors of CYP3A4 (ketoconazole, erythromycin) increase the concentration of zaleplon in the plasma and increase its sedative effect (when using this combination, it may sometimes be necessary to correct the zaleplon dose).

 

With the simultaneous use of inducers CYP3A4 (rifampicin, carbamazepine, Phenobarbital derivatives) can reduce the efficacy of zaleplon by 25%.

 

With simultaneous application Zaleplon does not affect the pharmacodynamics and pharmacokinetics of Digoxin and Warfarin (dose adjustment of these drugs is not required).

 

Interactions Ibuprofen with zaleplon is not revealed.

 

Analogues of the drug Zaleplon

 

Structural analogs for the active substance:

  • Andante.

 

Analogues of the drug Zaleplon on the pharmacological group (hypnotics):

  • Andante;
  • Apo-Flurazepam;
  • Belsomra;
  • Berlidorm;
  • Bromizoval;
  • Valocordin;
  • Heminearrin;
  • Hypnogen;
  • Diphenhydramine;
  • Doxylamine;
  • Donormil;
  • Dormikum;
  • Zolpidem;
  • Zopiclone;
  • Iwadal;
  • Imovan;
  • Coxpal Neo;
  • Melaxen;
  • Melarena;
  • Melatonin;
  • Nitrazadone;
  • Nitrazepam;
  • Nitram;
  • Nitrust;
  • Nitrosan;
  • Onyria;
  • Piklodorm;
  • Radedorm;
  • Reladorm;
  • Relaxon;
  • The Raslip;
  • Rohypnol;
  • Sanvall;
  • Signopam;
  • Snovitel;
  • Somnol;
  • Sonnivan;
  • Thorson;
  • Phenobarbital;
  • Flormidal;
  • Circadian;
  • Estazolam;
  • Eunotin.

 

Review of the neurologist's doctor

 

The drug Zaleplon is a good hypnotic.Patients with sleep disorders, whom I appoint, note that they fall asleep much faster and do not wake up at night. But almost all complain that the day they are concerned about dizziness, weakness, sometimes nausea. Therefore, until a week, none of my patients took it. Most likely, therefore, I did not have any of them to observe the formation of dependence or the development of withdrawal symptoms. Observing such frequent side effects during Zaleplon therapy, I try to use for the treatment of insomnia other drugs with a similar effect.

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