Zolsana - instructions for use, doses, side effects, contraindications

Fill white with Y-1-7000 (this is a ready-made coating agent: 62.5% of hypromellose 2910 (E464), 31.25% titanium dioxide (E171) and 6.25% macrogol 400).

Description:

Tablets 5 mg: oval biconvex tablets covered with a white film shell, engraved on one side of the "ZIM" tablet, on the other side of the "5".

Tablets 10 mg: oval biconvex tablets covered with a white film membrane, with a risk on both sides with an engraving on one side of the "ZIM" and "10" tablets.

Pharmacotherapeutic group:Sleeping Pills

ATX: & nbsp

N.05.C.F.02 Zolpidem

Pharmacodynamics:

The drug belongs to the list of 1 potent substances of the Standing Committee on Drug Control M3 RF.

Zolpidem - a hypnotic from the group of imidazopyridines. Has a pronounced hypnotic, sedative, and also slightly expressed anxiolytic, central miorelaxing and anticonvulsant action. The mechanism of action is a selective effect on the benzodiazepine omega-1 and omega-2 receptors of the central nervous system, in the alpha subunit of GABA receptor complexes located in the region of the IV plate of the sensory-motor cortical zones, the reticular sections of the black substance, the visual tubercles of the ventral thalamic complex, bridge, pale ball, etc. This leads to the discovery of neural ionoform channels for chlorine Zolpidem acts predominantly on the ω1-subtype of benzodiazepine receptors.

Shortens the time of falling asleep, reduces the number of nocturnal awakenings, increases the duration of sleep. Lengthens the II stage of sleep and the stage of deep sleep (III-IV).

Pharmacokinetics:

After oral administration zolpidem quickly absorbed from the gastrointestinal tract (GIT). Bioavailability is about 70%.In the range of therapeutic doses, the kinetics of the preparation is linear. The therapeutic range of plasma concentrations is from 80 to 200 ng / ml. The maximum concentration in plasma (TS_max) is noted 0.5-3 hours after ingestion and is 120 ng / ml. The volume of distribution (Vd) in adults is 0.54 l / kg and decreases in the elderly to 0.34 l / kg. Binding to plasma proteins - up to 92%. 35% of the drug is exposed to the effect of "first passage" through the liver. The half-life (T_½) is, on average, 2.4 hours, with a duration of up to 6 hours. All metabolites are pharmacologically inactive and excreted in the urine (56%) and through the intestine (37%). Do not cumulate. Zolpidem is not excreted from the body during hemodialysis.

Special patient groups

In patients with renal insufficiency, there is a moderate decrease in clearance. In the elderly and patients with hepatic insufficiency, the bioavailability of zolpidem increases, its clearance decreases and increases (up to 10 hours). In patients with cirrhosis, a 5-fold increase in the area under the concentration-time curve (AUC) and a 3-fold increase in T_½.

Indications:

Short-term therapy of sleep disorders: difficulty falling asleep, early and night awakenings.

Contraindications:

Hypersensitivity to zolpidem or other components of the drug;
Severe hepatic impairment;
Sleep apnea syndrome;
Myasthenia gravis;
Severe respiratory failure;
Age to 18 years;
Pregnancy and lactation;
Acute alcohol intoxication.

Carefully:

Chronic obstructive pulmonary disease (COPD) (acute), respiratory failure, myasthenia gravis, hepatic / renal failure, alcoholism, drug abuse (drug abuse) or history of drug dependence, depression, advanced age, as well as hereditary galactose intolerance, lactase deficiency Lappa or impaired absorption of glucose-galactose (see section "Special instructions").

Pregnancy and lactation:

Zolpidem is not prescribed for pregnancy, especially in the first trimester. If the drug is prescribed to a woman of reproductive age, she should be warned about immediate contact with a doctor at the first sign of pregnancy in order to cancel the drug. If, for urgent medical reasons, the drug is prescribed late in pregnancy or during labor, a newborn can expect the development of such effects,as hypothermia, hypotension, moderate respiratory depression, which are a consequence of the pharmacological action of the drug. In newborns, whose mothers in the late stages of pregnancy took benzodiazepines for a long time or benzodiazepine-like drugs, symptoms of "cancellation" as a result of the formation of physical dependence may develop in the postnatal period. Zolpidem in minimal quantities it absorbs into the mother's milk. The drug can not be administered during breastfeeding, because its effect in infants is not studied.

Dosing and Administration:

Inside, squeezed with enough liquid. The drug should be taken immediately before bed. Use of the drug is not recommended if the estimated duration of the upcoming sleep is less than 8 hours.

Adults under 65 years of age receive a single dose of 10 mg. For patients over 65 years of age or with concomitant hepatic failure: the initial starting dose is 5 mg. An increase of up to 10 mg is possible only in the case of insufficient therapeutic effect and good drug tolerance. The maximum daily dose is 10 mg.The duration of therapy, as a rule, is short. Usually its duration varies from a few days to 2 weeks at the most, and taking into account the period of "cancellation" - up to 4 weeks. A gradual dose reduction is recommended, the treatment cancellation regimen is individual. The need for longer-term therapy is assessed when a doctor is consulted again.

Side effects:

The likelihood of undesirable side effects increases with individual hypersensitivity and within the first hour after taking the drug, if the patient does not immediately go to sleep.

Common (> 1/100, <1/10):

From the side of the central nervous system (more often in elderly patients): severe headache, dizziness, decreased attention, memory impairment, anxiety, nightmares, hallucinations, confusion, daytime drowsiness, impaired coordination of movements, muscle weakness, diplopia, anterograde amnesia;

From the digestive system: diarrhea, nausea, vomiting, abdominal pain;

Allergic reactions: skin rash, itching.

Other: drug dependence (with prolonged use).

Undistributed (1 / 100-1 / 1000):

From the central and peripheral nervous system: muscle weakness, ataxia.

Other: general weakness.

Rare (<1/1000):

From the genitourinary system: possibly a decrease in libido.

Overdose:

Symptoms: impaired consciousness (from a semi-conscious state to a mild coma), cardiovascular and respiratory disorders.

Treatment: gastric lavage, as an antidote is recommended flumazenil. Even with severe excitation, sedative drugs are not acceptable. Dialysis is ineffective. If necessary, symptomatic therapy in a hospital.

Interaction:

Opioid analgesics, antitussives, barbiturates, antidepressants, sedatives and antihistamines, benzodiazepines, clonidine, antipsychotics (antipsychotics) and ethanol increase the risk of developing symptoms of central nervous system depression.

Flumazenil weakens or eliminates the hypnotic effect.

Benzodiazepine anxiolytic drugs (tranquilizers) increase the risk of drug dependence.

Strengthens the action of imipramine and chlorpromazine, prolongs the half-life (T1) of chlorpromazine (chlorpromazine increases drowsiness and incidence of anterograde amnesia), reduces the maximum concentration (C_max) of imipramine in blood plasma.

In case of analgesia with narcotic analgesics, a state of euphoria can also develop, which will lead to the formation of psychic dependence.

Zolpidem is metabolized in the liver by cytochrome P₄₅₀. The main one is CYP3A4. therefore rifampicin enhances the metabolism of zolpidem, leading to an increase in its concentration in the plasma and increased activity. However, with the simultaneous use of zolpidem and itraconazole (CYP3A4 inhibitor), the pharmacokinetics and pharmacodynamics of zolpidem significantly remain unchanged. The clinical significance of these effects is not established.

Special instructions:

In each case, if possible, it is necessary to establish the cause of insomnia. If after 7-14 days of therapy insomnia persists, you should suspect a psychiatric or mental disorder that requires diagnosis.

With prolonged use (within a few weeks), the risk of addiction increases (it is possible to reduce the hypnotic effect).Also, with prolonged use (more than 4 weeks), the drug should be discontinued gradually.

Elderly persons and patients with hepatic insufficiency are prescribed smaller doses of the drug.

In case of violations of the liver function, a dose reduction is indicated.

It is necessary to observe special care when prescribing the drug for severe depressions with high suicide risk.

Zolsana contains lactose, so the drug is not recommended for patients with hereditary intolerance to galactose, deficiency of lactase Lappa, or impaired absorption of glucose-galactose.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions, as well as the use of alcohol.

Form release / dosage:

Tablets, film-coated, 5 mg and 10 mg.

Packaging:10 tablets in a blister pack. For 1, 2, 3, 5, 6, 9, 10 or 12 blisters in a pack of cardboard along with instructions for use.

Storage conditions:

The drug belongs to the list of 1 potent substances of the Standing Committee on Drug Control M3 RF.

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000553/09

Date of registration:29.01.2009

Expiration Date:Unlimited

Date of cancellation:2016-03-22

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, dd, Novo mesto, AO Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp17.10.2017

Illustrated instructions

Instructions

Zolsana (Zolsana)