ANDANTE
Active material: zaleplon
When ATH: N05CF03
CCF: Sleeping pills
ICD-10 codes (testimony): F51.2
When CSF: 02.07.01.05
Manufacturer: GEDEON RICHTER Ltd. (Hungary)
DOSAGE FORM, STRUCTURE AND PACKAGING
Capsules hard gelatin, size №4, with blue opaque cap and a light blue opaque body; contents of capsules – Powder is light blue with a grayish tinge.
| 1 caps. | |
| zaleplon | 5 mg |
Excipients: starlak (mixture of lactose and corn starch), microcrystalline cellulose, magnesium stearate, indigokarmin, Titanium dioxide, sodium lauryl, colloidal silicon dioxide.
Ingredients of the capsule shell: indigokarmin, Titanium dioxide, gelatin.
7 PC. – blisters (1) – packs cardboard.
7 PC. – blisters (2) – packs cardboard.
Capsules hard gelatin, size №2, with blue opaque cap and blue opaque body; contents of capsules – Powder is light blue with a grayish tinge.
| 1 caps. | |
| zaleplon | 10 mg |
Excipients: starlak (mixture of lactose and corn starch), microcrystalline cellulose, magnesium stearate, indigokarmin, Titanium dioxide, sodium lauryl, colloidal silicon dioxide.
Ingredients of the capsule shell: indigokarmin, Titanium dioxide, gelatin.
7 PC. – blisters (1) – packs cardboard.
7 PC. – blisters (2) – packs cardboard.
Pharmacological action
Hypnotics pyrazolo-pyrimidine type, in chemical structure different from benzodiazepines and other hypnotics. It binds selectively to the benzodiazepine receptors 1 type (m-1).
Significantly reduces the latency time to fall asleep, prolong sleep time (in the first half of the night), no change in the ratio of the different phases of sleep. When applied in a dose of 5 mg 10 mg for 2-4 weeks does not cause pharmacological tolerance. Besides, has a sedative, slightly pronounced anxiolytic, anticonvulsant and central muscle relaxant effect.
Excited benzodiazepine receptors (oh) GABA receptor complexes of type A. Interaction with ω-receptors leads to neuronal ionoformnyh opening channels for chlorine ions, Development hyperpolarization and increased inhibition in the CNS.
Pharmacokinetics
Absorption
Once inside quickly and almost completely (about 71%) absorbed from the gastrointestinal tract, Cmax Blood thus achieved through 1 no. The absolute bioavailability is a result of first pass metabolism 30%. Plasma concentration is directly proportional to the dose. The drug immediately after meals may for 2 h delay the time to reach Cmax, without affecting the absorption of the drug.
Distribution
It is a fat-soluble compound. Vd after i / v injection of 1.4 ± 0.3 l / kg. Plasma protein binding is approximately 60% (probability of interaction with other drugs is very low). Provided with breast milk.
Metabolism
The primary metabolism play of aldehyde oxidase and leads to the formation of 5-oksozaleplona. CYP3A4 is also involved in the metabolism of zaleplon to form dezetil-zaleplon, which in turn, using the aldehyde is converted into 5-oxo-zaleplon dezetil. Subsequently oxidation products undergo conjugation with glucuronic acid. All metabolites are inactive. When used in doses up to 30 mg / day accumulation is not observed. T1/2 zaleplon – about 1 no.
Deduction
It is displayed in the form of inactive metabolites, mainly in the urine (71%) and feces (17%). To 57% of the dose is found in the urine as 5-oksozaleplona or its metabolites, 9% dose – as a 5-oxo-dezetil zaleplon or its metabolites, the remainder of the dose – a less significant metabolites. Among the metabolites, outputted through the intestines, 5-dominated oksozaleplona. Rapidly eliminated from the body.
Pharmacokinetics in special clinical situations
Pharmacokinetics in elderly patients (incl. senior 75 years) It is not significantly different from that in younger persons.
The pharmacokinetics of zaleplon in patients with renal failure patients is not significantly different from that of healthy, although the level of inactive metabolites have higher.
Testimony
- severe sleep disturbances (difficulty zasыpaniya), leading to excessive fatigue, impede daily activities and reduce efficiency.
Dosage regimen
Duration of therapy should not exceed 2 Sun.
The drug, taken orally immediately before bedtime, through 2 hours after a meal or after, the patient will feel, that he could not sleep.
The recommended dose for Adult – 10 mg. The maximum daily dose 10 mg (must notify the patient about the dangers receiving booster dose for one night). Individuals Seniors the drug is prescribed in a dose 5 mg (due to greater sensitivity to sleeping pills).
At hepatic insufficiency mild to moderate daily dose of gravity 5 mg (due to the slow elimination from the body).
At renal failure mild and moderate severity dose adjustment is required. Data on the safety of the drug in renal failure severe absent.
The safety of the drug in children aged 18 years not installed, therefore, patients in this age group do not prescribe zaleplon.
Side effect
From the digestive system: abdominal pain, nausea, vomiting, diarrhea.
From the central and peripheral nervous system: common – headache, weakness, hypersomnia, dizziness, anterogradnaya amnesia (accompanied by a breach of conduct), depression; paradoxical and mental reactions (more frequently in elderly patients): anxiety, hypererethism, aggressiveness, paresthesia, fits of rage, nightmares, hallucinations, psychosis, behavioral disturbances; development of physical dependence with withdrawal symptoms, even when used in therapeutic doses (the appearance of initial symptoms of sleep disorders more severe, as well as mood changes, alarm, anxiety); withdrawal (headache, myalgia, irritability, confusion); development of psychological dependence, leading to drug abuse; ataxia, tremor, irritability, perceptual disorders. In severe cases,: autoagressiâ, depersonalization, hearing loss, increased reaction to light, auditory and physical stimuli, seizures.
Allergic reactions: skin rash, itch.
Contraindications
- Severe hepatic impairment;
- Sleep apnea syndrome;
- severe pulmonary insufficiency;
- Myasthenia gravis;
- Pregnancy;
- Lactation;
- Children's age (to 18 years);
- Hypersensitivity to any component of the drug.
FROM caution is prescribed for chronic obstructive pulmonary disease, hepatic and / or renal failure, alcoholism, Drug Dependence (incl. history), depression.
Pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breast-feeding).
In appointing the drug women of childbearing age patients should be warned about the need for immediate treatment to the doctor in case of conception or when planning a pregnancy.
In the case of zaleplon in the III trimester of pregnancy or use of the drug in high doses during labor in the newborn may develop hypothermia, hypotonia, moderate respiratory failure as a result of the pharmacological action of the drug. Newborns, mothers regularly took benzodiazepines or benzodiazepinopodobnyh drug in the last weeks of pregnancy, may develop physical dependence, and the risk of developing withdrawal symptoms.
Cautions
Patients should be warned about, that the drug is not intended for long-term therapy and the possibility of withdrawal at the end of the use of the drug Andante®. The course of the drug must be short, and in any case not exceed 2 of the week. Extend treatment is possible only after careful clinical examination of the patient.
The drug can be given to elderly patients (incl. senior 75 years).
Sleep disorders can be the result of disease (incl. mental). If the short-term use of the drug Andante® normalizes sleep or sleep disturbance progresses, should re-evaluate clinical situation.
If the patient wakes up shortly after midnight (because of the short T1/2 zaleplon), It may require the appointment of another drug with a longer T1/2. It should warn patients about the need for no more than 1 tab. overnight.
Benzodiazepines and short-acting drugs benzodiazepinopodobnyh for several weeks may be accompanied by a decrease in somnolent effect.
Benzodiazepinopodobnyh benzodiazepines and drugs can lead to physical and mental dependence, probability of which increases when used in high doses, long-term therapy, chronic alcoholism and drug addiction in a patient's anamnesis.
When formed of physical dependence abrupt withdrawal of the drug leads to the development of withdrawal symptoms: headache, mialgii, pronounced anxiety, increased tension and irritability, psychomotor agitation, confusion. In severe cases, possible autoaggression, depersonalization, hearing loss, paresthesias in extremities, increased reaction to light, auditory and physical stimuli, hallucinations and epileptic seizures.
After discontinuation of benzodiazepines and drugs benzodiazepinopodobnyh transient and may cause more pronounced, than at the beginning of treatment, symptoms of insomnia (withdrawal). With the possible development of other related phenomena (mood changes, alarm, sleep disorders or anxiety).
Benzodiazepinopodobnyh benzodiazepines and drugs can cause the development of anterograde amnesia and impaired psychomotor functions. In order to avoid the development of these symptoms the drug should be taken only in case of, when the patient has the possibility of uninterrupted sleep, at least, during 4 hours after dosing.
zaleplon treatment should be discontinued in case of hyperexcitability, irritability, aggressiveness, disorders of perception, nightmares, gallyutsinatsii, psychotic disorders, particularly behavioral disorders. Children and elderly patients are more likely to develop these symptoms.
The drug is not intended for the treatment of depression and / or anxiety state, tk. It can be used for the implementation of suicidal intentions, often accompanied by depressive disorders. Patients with depression medication can be prescribed the minimum dose to avoid deliberate overdose.
It is not recommended to prescribe a drug to patients with severe hepatic impairment because of the risk of encephalopathy.
If lactose intolerance should be considered, that the composition of the tablet, contains 5 mg zaleplona, included 67 Lactose mg, 10 mg -134 mg.
Effects on ability to drive vehicles and management mechanisms
During the period of the drug should refrain from driving motor vehicles and sports activities, require high concentration and speed of psychomotor reactions, tk. sedation, amnesia, reduced concentration and muscle strength may adversely affect the ability to engage in such activities.
Overdose
Information on acute overdose bit. The concentration in the blood zaleplon overdose not measured.
Like other benzodiazepines and benzodiazepinopodobnyh overdosing does not cause life-threatening conditions, zaleplon if not taken in combination with other drugs, CNS depressants (incl. ethanol). In case of overdose should never forget about the possibility of combined poisoning.
Symptoms: signs of CNS depression, manifested in sleepiness until coma. In case of overdose mild – drowsiness, confusion, lethargy; In more severe cases, – ataxia, decrease in blood pressure, respiratory failure, cut coma (in very rare cases with a fatal outcome).
Treatment: According to preclinical studies flumazenil is an antagonist of zaleplon, although clinical studies have confirmed the effectiveness of flumazenil in overdose Andante®. Flumazenil may be used as an antidote. If the patient is conscious, in the first hour after ingestion, induce vomiting. If the patient is unconscious, the conduct gastric lavage, activated charcoal. Monitoring of cardiac and respiratory activity is carried out in an intensive care unit.
Drug Interactions
Simultaneous reception of ethanol or ethanol-containing drugs enhances sedation zaleplona.
The simultaneous use of antipsychotics (neuroleptics), other hypnotics, anccioliticakih, sedativnyh, antidepressant, antiepileptic, antihistamines, tools for anesthesia, opioid analgesics leads to increased sedative action of zaleplon.
While the use of opioid analgesics may be a manifestation of euphoric effect of the latter, leading to the development of drug dependence.
With simultaneous application of cimetidine (an inhibitor of aldehyde oxidase and CYP3A4) increases the concentration of zaleplon plasma on 85%.
With simultaneous use of selective inhibitors of CYP3A4 (ketoconazole, Erythromycin) increase the concentration of zaleplon plasma and enhance its sedative effect (when using such a combination can sometimes require dosage adjustment zaleplona).
With simultaneous use of CYP3A4 inducers (rifampicin, Carbamazepine, phenobarbital derivatives) may reduce the effectiveness of zaleplon to 25%.
With simultaneous use of zaleplon did not affect the pharmacodynamics and pharmacokinetics of digoxin and warfarin (correction doses of these drugs are not required).
Interactions of ibuprofen with zaleplon is not revealed.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The preparation should be stored in their original packaging in reach of children at a temperature of from 15 ° to 30 ° C.. Shelf life – 2 year.
