Золомакс®

General characteristics. Structure:

Active ingredient: 0,25 mg or 1 mg of an alprazola.

Excipients of 0,25 mg: sodium докусат, Natrium benzoicum, starch prezhelatinizirovanny, microcrystallic cellulose, lactoses monohydrate, magnesium stearate, silicon dioxide colloid,

Excipients of 1 mg: sodium докусат, Natrium benzoicum, starch prezhelatinizirovanny, microcrystallic cellulose, lactoses monohydrate, magnesium stearate, silicon dioxide colloid, indigo carmine (E132).

Tranquilizer. The drug removing alarm, fear, a depression.

Pharmacological properties:

Pharmacodynamics. Золомакс (alprazola) is derivative benzodiazepine of which existence of the expressed anxiolytic effect is characteristic. It kazyvat also sedative, somnolent, anticonvulsant, muscular weakening action. The identical tranquilizing effect can be reached when using by 10 times smaller, in comparison with diazepam, Zolomaks's doses. Золомакс has antidepressive effect.

In the central nervous system (CNS) of Zolomaks interacts with specific benzodiazepine receptors which are functionally closely tied with receptors of the main brake mediator of TsNS – γ-aminobutyric acid of acid (GAMK) therefore effect of drug is resulted by strengthening of the braking influence of GAMK in TsNS.

Pharmacokinetics. Alprazolam is quickly and completely absorbed in digestive tract. Its bioavailability – not less than 80%. The maximum concentration in blood after administration of drug is inside observed in 1-2 hours. It fluctuates, depending on a dose, ranging from 7 to 40 ng/ml after a single dose of 0,5-3 mg. After multiple dose of 1,5-10 mg of drug its average equilibrium concentration in a blood plasma makes 18-100 ng/ml. At regular reception equilibrium concentration of drug in a blood plasma is reached within 3 days.

Alprazolam is medicine with an average elimination half-life (12-15 h after a single dose). Alprazolam is exposed to biotransformation in a liver by oxidation. The main active metabolite – to α-gidroksialprazola, however, its concentration in a blood plasma quite low and therefore it has no clinical value. Other metabolites of a maloaktivna or are absolutely inactive. The elimination half-life of not changed drug and its metabolites is approximately identical. Alprazolam in not changed look (about 20%) and in the form of metabolites is allocated with urine.

Indications to use:

— states of which the alarm, tension, concern, concern, sleep disorders, excitement, a depression, the somatic complaints caused by a superactivity of an autonomous nervous system is characteristic;

— panic state, including at patients with an agoraphobia.

Route of administration and doses:

Drug is appointed inside. The initial single dose makes 250-500 mkg, a daily therapeutic dose - 1 mg, the maximum daily dose - 10 mg. A course dose - 60-80 mg at a course of treatment of 8-12 weeks.

Doses and duration of treatment choose for each patient individually, using the minimum doses which eliminate symptoms of excessive alarm, but do not exert the oppressing impact on TsNS. Золомакс, as well as other tranquilizers, it is desirable to use in the form of short courses of treatment.

At treatment of alarm an initial dose for adults – on 250-500 mkg 3 In case of need the dose is increased by 250 mkg by each 3-4 days depending on weight of symptoms of a disease and reaction of the patient to treatment. Increase in a dose is recommended to be begun with an evening dose. At the expressed alarm symptoms treatment can be begun with higher doses. The maximum daily dose – 4 mg.

To the elderly and weakened patients in an initiation of treatment appoint 2-3 on 125-250 mkg

At the first purpose of tranquilizers the therapeutic effect is usually reached after use of low doses, and to patients who take alcoholic drinks or earlier is long were treated by tranquilizers, higher doses of drug are necessary.

At alarm the course of treatment, including time necessary for gradual drug withdrawal, usually should not exceed 8-12 weeks. Expediency of more long course of treatment should be estimated seriously.

At treatment of panic states use higher doses. The recommended initial dose – 500 mkg of 3 days. In case of need it is raised, but no more than on 1 mg each 3-4 days. The doses are higher, the more gradually it is necessary to increase them the therapeutic effect of drug managed to develop completely. Usually therapeutic effect is reached at use of a dose of 5-6 mg/days, and in hard cases - to 10 mg/days (the maximum daily dose).

Duration of treatment of each patient is determined individually. When the therapeutic effect is reached and symptoms of a disease are eliminated, Zolomaks's dose can be reduced, but not quicker than on 500 mkg each 3 days. If the phenomenon of cancellation or abstinence signs develops, the dose of drug can be increased again, and further to carry out cancellation more gradually.

Features of use:

If patients accept Zolomaks is long or in high doses, physical or psychological dependence on drug can sometimes develop. At a bystry dose decline or the termination of reception of medicine the abstinence syndrome of which the following symptoms are characteristic develops: a headache, a dysphoria, concern, a shiver, sleeplessness, confusion, and in hard cases – vomiting, pristupoobrazny abdominal pains and muscles, paresthesia, hypersensitivity to tactile, sound and light irritants, hallucinations, a delirium, attacks of spasms. The risk of development of dependence is higher at patients with existence in the anamnesis of alcoholism or toxicomania. Perhaps also development of a withdrawal. It means that at the sudden termination of administration of drug disease symptoms concerning which drug was used (alarm, concern, sleeplessness, changes of mood) renew, sometimes even in more expressed form, than prior to treatment.

To prevent a possibility of development of an abstinence syndrome or a withdrawal, drug should be used whenever possible quickly, and to carry out its cancellation by a gradual dose decline. Patients should be informed that without the permission of the doctor it is impossible to stop suddenly administration of drug, to increase its dose or duration of use.

Золомакс it is not intended for treatment of the alarm resulting from a physiological or daily stress. Drug is also not recommended to be used for treatment of schizophrenia, psychoses, changes of the personality and obsessivno-compulsive states. It is necessary to be careful at Zolomaks's appointment to patients with a heavy depression and probable tendency to suicide.

At repeated use of drug development of tolerance to sedative effect of drug is possible.

Efficiency and safety of use of Zolomaks for children is not found out.

At the elderly and weakened patients, and also in the presence of organic lesion of a brain the oppressing Zolomaks's influence on TsNS (an ataxy, sedation, hypotension) is expressed stronger and therefore in these cases it is necessary to apply the minimum doses of drug, raising them in case of need with care.

Золомакс patients should appoint with care with chronic obstructive diseases of lungs or respiratory insufficiency since derivatives of benzodiazepine can oppress a respiratory center.

Patients with abnormal liver functions or kidneys are also recommended to appoint the minimum doses of Zolomaks as in these cases removal of drug can be reduced that, in turn, can cause strengthening of its action. At prolonged treatment by Zolomaks it is desirable to control periodically functions of a liver and a picture of blood.

Influence on ability to driving of motor transport and to control of mechanisms

Золомакс can cause drowsiness and reduce ability to concentration and coordination of movements. The probability of development of these symptoms is higher in an initiation of treatment and also when the patient does not get enough sleep.

The patient should be warned that during treatment by Zolomaks it is necessary to avoid work for which performance bystry reaction is necessary (work with technical devices, control of vehicles).

Safety of use of drug at pregnancy is not studied, however, results of separate researches demonstrate that use of some tranquilizers from group of benzodiazepines (chlordiazepoxide, diazepam, meprobamate) in the I trimester of pregnancy increases risk of emergence of inborn pathology. Regular use of benzodiazepines at pregnancy can lead to oppression of TsNS or development of an abstinence syndrome in newborns (concern, a tremor, increase in a muscle tone).

Women of childbearing age should be warned that at pregnancy it is not necessary to begin treatment with drug of Zolomaks, and at its use before pregnancy it is necessary to consult to the doctor about expediency of further use of drug at suspicion on pregnancy or its planning.

Alprazolam is allocated with breast milk and can cause drowsiness and decrease in body weight in newborns therefore, in case of need Zolomaks's uses feeding by a breast should be stopped.

Side effects:

From TsNS: drowsiness, dizziness, an incoordination of movements (these side effects are usually observed in an initiation of treatment by drug, do not happen heavy and at continuation of treatment or a dose decline disappear); seldom - a headache, disturbance of clearness of sight, a shiver, disturbance of the speech, confusion, euphoria or a depression; sometimes - an ecmnesia, most often in several hours after administration of drug in high doses; in some cases - a hypomania or a mania at patients with a depression.

Reception of benzodiazepines sometimes, is more often at children and elderly patients, leads to development of paradoxical reactions (concern, excitement, hostility, hallucinations, nonsense, a behavior disorder).

From the alimentary system: seldom - nausea, vomiting, dryness in a mouth, diarrhea or a lock; sometimes - increase in level of liver enzymes (ShchF, ALT, nuclear heating plant) and bilirubin in a blood plasma.

From cardiovascular system: palpitation, arterial hypotension.

From a musculoskeletal system: spasms or weakness of skeletal muscles.

From system of a hemopoiesis: sometimes - a leukopenia, decrease in a hematocrit and hemoglobin.

Allergic reactions: skin rash, skin itch.

Others: change of appetite and body weight, urine incontience, decrease in sexual desire, increase or decrease in content of glucose in blood.

Interaction with other medicines:

The combined use of Zolomaks with the ethanol and other medicines having the oppressing effect on TsNS (anesthetics, opioid analgetics, antidepressants, tranquilizers, somnolent, antiepileptic, antipsychotic, antihistaminic means) can lead to strengthening of oppression of TsNS.

At combined use of Zolomaks and opioid analgetics the probability of emergence of euphoria increases that can promote dependence development.

Combined use of Zolomaks with antifungal means of group of azoles is not recommended (кетоконазол, итраконазол). The combined use with the medicines oppressing activity of enzymes of P450 cytochrome in a liver (Cimetidinum, peroral contraceptives, antibiotics from group of macroleads, fluoxetine, флувоксамин, нефаксодон, the propoxyhair dryer), can slow down metabolism and elimination of an alprazolam. Therefore in case of need uses of combinations of these drugs it is necessary to be careful.

Carbamazepine can accelerate metabolism and removal of an alprazolam from an organism.

It is established that at combined use of Zolomaks and tricyclic antidepressants of Imipraminum and desipramine equilibrium concentration of the last in a blood plasma increases, however, clinical value of this fact remains not clear.

Contraindications:

— acute glaucoma;

— myasthenia gravis;

— heavy respiratory insufficiency;

— an apnoea in a dream;

— heavy abnormal liver functions;

— chronic psychosis;

— age up to 18 years;

— hypersensitivity to an alprazolam or other benzodiazepines in the anamnesis.

Overdose:

Overdose - reception of 500-600 mg of drug.

At treatment of patients with overdose by benzodiazepine derivatives, it is always necessary to mean probability that the overdose is caused by the simultaneous use of alcoholic drinks or a combination of medicines.

Symptoms: the expressed drowsiness, muscular weakness, an ataxy, a dysarthtia, sometimes, especially at children, excitement. In hard cases confusion, oppression of reflexes, a lump can develop.

Treatment: it is necessary to cause vomiting, and in case of unconsciousness of the patient to make a gastric lavage. It is necessary to control breath, pulse and the ABP. Overdose treatment symptomatic: provide to the victim adequate breath and cordial activity, enter infusion solutions, in case of need apply vasoconstrictors to elimination of hypotension.

It is possible to apply to decrease in oppression of TsNS the specific antagonist of benzodiazepine receptors – flumazenit. Efficiency of dialysis for acceleration of removal of an alprazolam is low.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature not above 25 °C

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from PVC and aluminum. On 3 planimetric packagings in a cardboard pack.