Alzolam (Alzolam)

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:

    Active substance:

    Alprazolam 0.25 mg or 0.5 mg

    Excipients: lactose, starch, microcrystalline cellulose, silicon dioxide colloidal anhydrous, magnesium stearate, dye diamond blue, dye quinoline yellow, dye crimson (Ponso 4R).

    Description:

    Alzolam 0.25 mg.

    Round, flat cylindrical with a chamfer of a green tablet, marked "ALZOLAM" on the one hand and risk on the other.

    Alzolam 0.5 mg.

    Round, flat-cylindrical with a bevel of a tablet of pink color, having marks "ALZOLAM" on the one hand and risk on the other.

    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer)
    ATX: & nbsp

    N.05.B.A   Benzodiazepine derivatives

    N.05.B.A.12   Alprazolam

    Pharmacodynamics:

    Alzolam has an anxiolytic, central muscle relaxant, anticonvulsant, sedative-hypnotic and antipanic effect. Has a depressing effect on the central nervous system (CNS), which is realized mainly in the thalamus, hypothalamus and limbic system.Enhances 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. It also has anxiolytic, sedative, miorelaxing and anticonvulsant action.

    The mechanism of action of Alzolam is determined by the stimulation of the benzodiazepine receptors of supramolecular GABA-benzodiazepine-chloro-formof the formulation 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 mean maximum concentration was 7.1 ng / ml. There is a linear relationship between the dose of alzolam and the 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. A stable concentration in the plasma is usually achieved within a few (2-3) days. Alzolam is actively metabolized in the liver, the main metabolite is the alpha-hydroxyl metabolite, which has biological activity. Removal of the drug from the body occurs mainly through the kidneys in the form of compounds with glucuronic acid. The half-life is about 11-16 hours. Accumulation with a repeated appointment is minimal (refers to benzodiazepines with a short or medium T1/2), withdrawal after cessation of treatment is rapid.

    Indications:

    Treatment of neurotic and neurosis-like disorders with anxiety, incl. related to 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 the first trimester), see "Special instructions", the period of breastfeeding.

    Carefully:

    Cerebral and spinal ataxia, drug dependence in history, propensity to abuse psychotropic drugs, hyperkinesis, organic brain diseases, psychosis (possible paradoxical reactions), hypoproteinemia, elderly age.

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

    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.

    Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.

    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 the drug is selected individually and corrected during the 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 the elderly, the initial dose is 0.25 mg 2 to 3 times a day.

    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 drug should be done with great care. The dose should be reduced gradually and slowly, no more than 0.5 mg - 1 mg at bedtime or 0.5 mg three times a day. 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 eight months.

    In the treatment of elderly and weakened patients, smaller doses should be used: the initial dose is 0.25 mg 2-3 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 side of the central nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, impaired concentration, ataxia, disorientation, slowing of mental and motor reactions; rarely - headache, euphoria, decreased mood, tremor, memory loss, movement coordination disorder, confusion, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), muscle weakness, blurred speech; extremely rarely - paradoxical reactions (aggressive outbursts, confusion, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, insomnia).

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

    From the digestive system: dry mouth or drooling, 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 the I trimester), central nervous system depression, respiratory failure and suppression of sucking reflex in infants whose mothers used the drug.

    Other: addiction, drug dependence; lowering blood pressure (hereinafter referred to as "blood pressure"); rarely - visual impairment (diplopia), weight loss, tachycardia. With a sharp decrease in dose or discontinuation of reception - withdrawal syndrome (increased irritability, sleep disturbance, dysphoria, spasm of smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, decreased mood, nausea, vomiting, tremor, perceptual disorders, h. Hyperacusia, paresthesia, photophobia, tachycardia, convulsions, rarely - acute psychosis).

    Overdose:

    Overdose of the drug (taking 500-600 mg).

    Symptoms: drowsiness, confusion, decreased reflexes, movement, tremors, bradycardia, dyspnea and wheezing, decrease in blood pressure (BP), coma. Treatment: gastric lavage, reception of activated charcoal. Symptomatic therapy (respiration and blood pressure maintenance), administration of flumazenil (in a hospital). Hemodialysis is ineffective.

    Interaction:

    Alzolam 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. Alzolam in a dose of 4 mg / day increases plasma concentrations of imipramine and desipramine (by 31% and 20% % respectively) with simultaneous admission. The metabolic clearance of alzolam decreases with the simultaneous administration of conventional therapeutic doses of cimetidine and antibiotics from the macrolide group. Caution should be exercised and thought should be given to reducing doses of alzolam when taken with cimetidine, macrolides, nefazodone, fluvoxamine, fluoxetine, propoxyphene, sertraline, diltiazem, digoxin and oral contraceptives.

    Special instructions:

    In the process of Alzolam treatment, 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, Alzolam can be used in combination with antidepressants. When Alzolam was used, patients with depression experienced cases of hypomanic and manic state development.

    Like other benzodiazepines, Alzolam has the ability to induce drug dependence in 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.

    Form release / dosage:Tablets 0.25 mg, 0.5 mg.
    Packaging:

    10 tablets per blister, made of PVC and aluminum foil.For 5 or 10 blisters together with the instructions for use are placed in a cardboard box. A transparent film of polyolefin (sticker) with a printed logo is applied to the cardboard pack on both sides to ensure control of the first opening.

    Storage conditions:

    It refers to the list of the III list of narcotic drugs, psychotropic substances and their precursors, which are subject to control in the Russian Federation. Store in a dry, dark place at a temperature of not more than + 30 ° C. Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012954 / 01
    Date of registration:13.08.2008 / 09.10.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India
    Information update date: & nbsp06.07.2017
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