Zolomax® (Zolomaks®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAlprazolamAlprazolam
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    • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: alprazolam 0.25 mg or 1.0 mg;

    Excipients: docusate sodium, sodium benzoate, pregelatinized starch, microcrystalline cellulose; lactose, monohydrate, magnesium stearate, silicon dioxide colloid; dye (only in 1 mg tablets) - indigocarmine (EEC E132).

    Description:

    Tablets 0.25 mg: oval white tablets, on one side - risk, on the other side the inscription "APZM 0.25 ", with a bevel.

    Tablets 1 mg: oval blue tablets, on one side - risk, on the other side of the inscription "APZM 1 ", with a bevel.

    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer). List III of the List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation
    ATX: & nbsp

    N.05.B.A   Benzodiazepine derivatives

    N.05.B.A.12   Alprazolam

    Pharmacodynamics:

    Alprazolam has an anxiolytic, central muscle relaxant anticonvulsant, sedative-hypnotic and antipanic action.Has a depressing effect on the central nervous system (CNS), which is realized mainly in the thalamus, hypothalamus and limbic system. Increases the inhibitory effect of gamma-aminobutyric acid (GABA) which is one of the main mediators of pre- and postsynaptic inhibition of the transmission of nerve impulses in the central nervous system.

    The mechanism of action of alprazolam is determined by stimulation benzodiazepine receptors of supramolecular GABA-benzodiazepine-chloronophore receptor complex, leading to activation of the GABA receptor, which causes a decrease in the excitability of the subcortical structures of the brain, inhibition of polysynaptic spinal reflexes.

    Anxiolytic effect is manifested in the reduction of emotional tension, alleviation of symptoms of anxiety, fear. The pronounced anxiolytic activity is combined with a mild hypnotic effect; shortens the period of falling asleep, prolongs the duration of sleep, reduces the number of nocturnal awakenings. The mechanism of hypnotic action is the inhibition of cells of the reticular formation of the brain stem.Reduces the impact of emotional, vegetative and motor stimuli, which break the mechanism of falling asleep.

    Virtually no effect on the cardiovascular and respiratory system.

    Pharmacokinetics:

    When taken orally, the maximum concentration in the plasma is reached after about 1-2 hours. After a single oral dose of 0.5 mg, the average maximum concentration is 7.1 ng / ml. There is a linear relationship between the dose of alprazolam and its concentration in the plasma. At oral intake about 80% of the dose is absorbed.

    About 80% of the drug binds to plasma proteins.

    It can pass through the placenta, the blood-brain barrier (GEB), penetrate into breast milk. The equilibrium concentration in plasma is usually achieved within a few (2 - 3) days.

    Alprazolam is actively metabolized in the liver, the main metabolite is the alpha-hydroxyl metabolite, which has biological activity. In the metabolism of the drug, isozymes participate CYP3A4, CYP3A5 and CYP3A7. Removal of the drug from the body occurs mainly through the kidneys in the form of compounds with glucuronic acid. Half-life (T1/2) is 11 - 16 hours. Accumulation with a reappointment is minimal (refers to benzodiazepines with a short or medium half-life), withdrawal after cessation of treatment is rapid.

    Indications:

    Treatment of neurotic and neurosis-like disorders with anxiety, including those associated with depression.

    Panic disorders.

    Contraindications:

    Hypersensitivity to alprazolam or other benzodiazepines.

    Coma, shock, zakratougolnaya glaucoma, myasthenia gravis, acute alcohol poisoning, narcotic, hypnotics and psychotropic drugs, severe course of chronic obstructive pulmonary diseases, severe depression (suicidal attempts), sleep apnea syndrome, marked violations of kidney and liver function; pregnancy (especially I trimester - see "Special instructions"), the period of breastfeeding.

    Due to the presence of lactose, patients with rare hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption, should not take the drug.

    The safety of alprazolam in children and adolescents (under 18 years) has not been established.

    Carefully:Cerebral and spinal ataxia, drug dependence in history, propensity to abuse psychotropic drugs, hyperkinesis, organic brain diseases, psychosis (possible paradoxical reactions), hypoproteinemia, hepatic insufficiency, chronic renal failure, elderly age.
    Pregnancy and lactation:

    During pregnancy are used only in exceptional cases and only for life indications. Has a toxic effect on the fetus and increases the risk of developing congenital malformations when used in the first trimester of pregnancy. Taking therapeutic doses at a later time of pregnancy can cause depression of the newborn's central nervous system. Continuous use during pregnancy can lead to physical dependence with the development of the "cancellation" syndrome in a newborn.

    The use directly before childbirth or during labor can cause a respiratory depression in the newborn, a decrease in muscle tone, hypotension, hypothermia, and a weak act of sucking (the so-called "sluggish child syndrome").

    Dosing and Administration:

    Inside, 2 - 3 times a day, regardless of food intake.

    The dose of ZOLOMAX® is selected individually and adjusted during treatment, depending on the effect and individual tolerability. The use of minimum effective doses is recommended.

    In case of anxiety, the initial dose is 0.25 mg - 0.5 mg three times a day. If necessary, this dose can be increased to 4 mg / day (divided into several receptions).

    In panic disorders - 0.5 mg 3 times a day, the daily dose can reach 3-6 mg, the highest daily dose of -10 mg.

    In anxiety conditions associated with depression, the initial dose is 0.5 mg three times a day. If necessary, the dose is increased to 4.5 mg / day. The initial dose can be administered before bedtime to minimize daytime sleepiness. Duration of treatment - 4 - 12 weeks.

    Stopping the use of ZOLOMAX® should be done with great care. Gradual withdrawal of the drug should take an extended period of time, i.e. if the patient takes 0.5 mg in the morning, 0.5 mg in the afternoon and 1 mg in the evening, then he should reduce the daily dose by no more than 0.25 mg every 3 days.

    For most patients, a sufficient dose is 4-6 mg / day for 4-12 weeks. In some cases, if necessary, the dose can be increased to 10 mg / day (but not more than 1 mg every 3-4 days), and the duration of treatment - up to 8 months.

    In the treatment of elderly and weakened patients, smaller doses should be used: the initial dose is 0.25 mg 2 to 3 times a day, if necessary and tolerated, it is gradually increased to 0.5-0.75 mg / day.

    Side effects:

    Side effects usually occur at the beginning of the treatment and gradually disappear as the drug is used or the dose is lowered.

    From the central nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, impaired concentration, disorientation, slowing of mental and motor reactions; rarely - headache, euphoria, decreased mood, tremor, memory loss, confusion, impaired coordination of movements, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), myasthenia gravis, dysarthria; extremely rarely - paradoxical reactions (aggressive outbursts, confusion, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, irritability, anxiety, insomnia).

    From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia.

    From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, anorexia, constipation, diarrhea; violations of liver function, increased activity of "liver" transaminases and alkaline phosphatase (APF), jaundice.

    From the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.

    Allergic reactions: skin rash, itching.

    Influence on the fetus: teratogenicity (especially I trimester), central nervous system depression, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

    Other: addiction, drug dependence; lowering of blood pressure (BP); rarely - visual impairment (diplopia), weight loss, tachycardia. With a sharp decrease in dose or withdrawal of the syndrome, "withdrawal" syndrome (increased irritability, sleep disturbance, dysphoria, spasm of the smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, incl.hyperaemia, paresthesia, photophobia; tachycardia, convulsions, rarely - acute psychosis).

    Overdose:

    Overdose - taking 500 - 600 mg of the drug.

    Symptoms: drowsiness, confusion, decreased reflexes, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, lowering of blood pressure, coma.

    Treatment: gastric lavage, reception of activated charcoal; symptomatic therapy (maintenance of respiration and blood pressure), administration of flumazenil (in a hospital setting).

    Hemodialysis is ineffective.

    Interaction:

    Alprazolam enhances the effect of other psychotropic drugs, anticonvulsant and antihistamines, ethanol and drugs that exert a depressing effect on the central nervous system.

    Inhibitors of microsomal oxidation - increase the risk of toxic effects. Inductors of microsomal liver enzymes - reduce efficacy. Hypotensive drugs can increase the severity of blood pressure lowering.

    Clozapine - may increase respiratory depression. Reduces the effectiveness of levodopa in patients with Parkinsonism. It is possible to increase the toxicity of zidovudine.

    Alprazolam in a dose of 4 mg / day increases the plasma concentrations of imipramine and desipramine while concomitantly taking.The metabolic clearance of alprazolam decreases with the simultaneous administration of conventional therapeutic doses of cimetidine and antibiotics from the macrolide group. Simultaneous use with cimetidine, macrolides, nefazodone, fluvoxamine, fluoxetine, dextropropoxyphene, sertraline, diltiazem, digoxin and oral contraceptives can reduce the metabolism of alprazolam in the liver and enhance its effect.

    Special instructions:

    In the process of treatment with alprazolam, patients are strictly prohibited from drinking alcohol (ethanol).

    With renal / hepatic insufficiency and long-term treatment, control over the picture of peripheral blood and "hepatic" enzymes is necessary.

    Patients who did not previously take psychotropic drugs "respond" to the drug at lower doses, compared with patients who previously took antidepressants, anxiolytics or who suffer from alcoholism.

    With endogenous depression alprazolam can be used in combination with antidepressants. With the use of alprazolam, patients with depression have reported cases of hypomanic and manic state development.

    Patients with depressive disorders should be monitored, especially at the beginning of treatment, because of the increased risk of suicidal attempts.

    Like other benzodiazepines, alprazolam has the ability to cause drug dependence with long-term admission in large doses (more than 4 mg / day).

    When patients develop such unusual reactions as increased aggressiveness, acute excitement, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficult sleep, superficial sleep, treatment should be discontinued.

    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 that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:Tablets of 0.25 mg and 1 mg.
    Packaging:

    For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil.

    3 or 5 contour cell packs, together with the instructions for the use of the medicinal product for medical use, are placed in a pack of cardboard with the control of the first opening ina self-adhesive transparent sticker of light green color.

    Storage conditions:

    List III The list of narcotic drugs, psychotropic substances and their precursors, subject to control in Russian Federation.

    Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001893/10
    Date of registration:12.03.2010 / 03.02.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:GRINDEX, JSC GRINDEX, JSC Latvia
    Manufacturer: & nbsp
    Representation: & nbspGrindeks Rus, Open CompanyGrindeks Rus, Open CompanyRussia
    Information update date: & nbsp15.10.2017
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