Zopiclone

Chemical name

6-(5-Хлор-2-пиридинил)-6,7- дигидро-7-оксо-5H-пирро��о[3,4-b]пиразин-5-иловый ether 4 -метил-1-пиперазинкарб оновой acid

Gross

C17-H17-Cl-N6-O3

Characteristics

Red means nebenzodiazepinova structure (ziklopirrolona derivative).

Of drugs

Drugs, the pills, sedative. Is benzodiazapine adrenergic receptors. Interacts with the central receptor (proved omega_1 and omega_2 benzodiazapine receptors) macromolekulyarnogo ГАМК-бензодиазепин-хл орионофорного complex and does not interact with perifericescimi benzodiazepinovmi receptor. Increases sensitivity to Gamk-retseptorov mediatoru (GABA), which leads to an increase in the frequency of opening zitoplazmaticescoy neuronal membrane channels for incoming currents chlorine ions. As a result, increasing braking power GABA and braking mezhneironna transfer in the various divisions Zns.bystro drawn from the blood. C_max achieved through 1-1.5 hrs Linking blood plasma proteins is about 45%. Easily passes through gistogematicalkie barriers, including GEB, and relate to the organs and tissues, including brain. Passes through the placental barrier, enters the breast milk (in breast milk in concentrations 11 times lower than in the blood plasma). Metabolised in the liver to education N-oksida with little pharmacological activity, and two inactive metabolites. T_1/2 - 3,5-6 hours, and expressed insufficient liver function increases up to 11 hours Report the news is in the form of metabolites (80%), as well as through the intestine (16%). There is evidence for the withdrawal of small quantities slunnami disorders. Not кумулирует.Укорачива��т Sleep period, it reduces the amount of night probujdeni, improves the quality of sleep, does not alter the phase of sleep. Effective in the situational insomnia related to psychoemotional voltage change in the normal life (eg, hospitalization), desinhronozom, incl. in the change of time zones shift work. Song occurs within 20 to 30 minutes after administration and lasts for 6-8 C.u patients with heart manifestations of asthma in combination with drugs metilxantinovogo stimulants (theofillin) urejaet asthma attacks in the early pre-dawn hours, reduces the severity and duration.

Indications

Violations of sleep (sleep difficulty, frequent night and / or early morning awakening), incl. seetuatinaya, short-term, chronic insomnia; secondary sleep disturbance is free.

Restrictions on the use of

Movements during sleep, infants expressed liver failure.

Pregnancy and lactation

Contraindicated in pregnancy (especially in the I and III trimester). In applying zopiclone woman in the third trimester of pregnancy, newborn possible violations of the nervous system, the emergence of the syndrome. If a woman doctor's prescription has zopiclon immediately prior to the labor and delivery need continuous medical monitoring of the newborn. At the time of treatment should stop breast-feeding (zopiclon enters breast milk).

Contraindications

Hypersensitivity expressed respiratory distress, pregnancy (especially I and III Plus), breast-feeding, age and 18 years of age.

Side-Effects

From the nervous system and sensory organs : drowsiness, weakness, fatigue, headache, dizziness, irritability, sputannosti consciousness (being older), mood depression, muscle weakness, coordination of movements, diplopia, the deterioration of memory paradoxical reaction (increased insomnia, nightmares, restlessness, agitation aggressiveness, deep anger, hallucinations). Other : bitter or metallic taste in the mouth, dry mouth, nausea, vomiting, skin allergies, the change drive, anterogradnaya Amnesia.vozmojna addiction, drug dependency, the syndrome, including ricochetnaya insomnia (see "Precautions").

Patient interaction

In joint application zopiclone with other means, oppressive central nervous system (including neiroleptiki other hypnotics funds противоэпилептически е PP, some antihistamines PP, alcohol) may reinforce one another Effectov.zopiclon decreases the trimipramina plasma.

Overdosing

Symptoms : oppression CNS varying degrees of symptoms (from itching to the point of unconsciousness). Treatment : washing stomach reception activated carbon; If necessary, symptomatic therapy. As a specific antidote used BZ antagonist flumazenil receptors (in the hospital). Haemodialysis ineffective.

Precautions

Application for a long period of time may be designated by a doctor in exceptional circumstances (for the opportunity of Drug Dependence). If insomnia persists for a period of four weeks, it should be to inform the attending physician. The likelihood of addiction, physical or psychological dependence increases if there is a violation of the prescribed dosage or duration of treatment more than 4 Ned.otmenu should be implemented in a gradual manner, as with a sharp cut treatment possible resumption of insomnia, frequent awakening, headache, muscle pain, anxiety, agitation withdrawn, раздражительность.Па��адоксальные reaction can be observed in patients older. In the event of a paradoxical reactions zopiclon should Otmeniti.na next day after taking zopiclone should avoid driving and Occupation potentially hazardous activities that require greater attention and speed of reaction. During treatment zopiclonom should refrain from alcohol or drugs containing alcohol.

Dosing and Administration

Inside. Dose and duration of treatment is determined by a physician on a case-by-case. The average dose is 7.5 mg once on the night with a maximum dose of 15 mg. For patients over 65, patients with liver disease or chronic respiratory distress polovinne recommended dose (3.75 mg). The course of treatment : from a few days to four weeks.

Literature

1. Avedisov A.S. Gipnotiki : modern психофармакологии//Пс ихиатрия and psihofarmakoterapia .- 2002 .- V. 4-N 5.2. Babak SL, Chuchalin AG Nightlife asthma / / RMJ .- 1998 .- T. 6-N-17 C. 1108-1114.3. Wayne A. years experience with imovana in patients with insomnia / / / RMJ .- 1998 .- T. 1-N 3.4. Levin E94, E94 Wayne Modern somnology and some aspects of the use of sleeping pills / / Kremlin. Medicine-1998 (additional number).

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