Alprazolam (Alprazolam)

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 1 mg.

    Excipients: potato starch, magnesium stearate (magnesium stearate), milk sugar (lactose), low molecular weight polyvinylpyrrolidone (povidone).

    Description:

    Tablets white or white with a weak yellowish hue.

    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 miorelaxing, anticonvulsant, sedative-hypnotic and antipanic effect. Has a depressing effect on the central nervous system, which is realized mainly in the thalamus, hypothalamus and limbic system. Enhances the inhibitory effect of gamma-aminobutyric acid, which is one of the main mediators of pre- and postsynaptic inhibition of nerve impulse transmission in the central nervous system.

    The mechanism of action of alprazolam is determined by the stimulation of the benzodiazepine receptors of supramolecular gamma-aminobutyric acid-benzodiazepine-chloro-nophoric compound, leading to activation of the gamma-aminobutyric acid 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.

    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 mg / ml.There is a linear relationship between the dose of alprazolam 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. Alprazolam actively metabolizes 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. Half-life (T1/2 - 11-16 hours Accumulation at repeated appointment - minimal (refers to benzodiazepines with an average 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, angle-closure glaucoma, myasthenia gravis, acute alcohol poisoning, narcotic,sleeping pills and psychotropic drugs; the severe course of chronic obstructive pulmonary diseases, severe depression (suicidal attempts), sleep apnea syndrome, severe renal and hepatic impairment, 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 alprazolam in children and adolescents (under 18 years) has not been established.

    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 0.25-0.5 mg three times a day. If necessary, this dose can be increased to 4 mg / day (divided into several methods).

    In the elderly, the initial dose is 0.25 mg 2-3 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 is 4-12 weeks. Stopping the drug should be done with great care. The dose should be reduced gradually and slowly, no more than 0.5-1 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, tremors, memory loss, impaired coordination of movements, confusion, dystonic extrapyramidal reactions (uncontrolled movements, including eye), muscle weakness, slurring of speech, very rarely - paradoxical reaction (aggressive flashes, confusion, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, insomnia).

    From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, unusual tiredness or weakness), anemia, and thrombocytopenia.

    From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, anorexia, constipation, diarrhea; impaired 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), CNS depression, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

    Other: addiction, drug dependence; lowering blood pressure (BP), 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, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, lowering blood pressure, coma.

    Treatment: gastric lavage, reception of activated carbon. Symptomatic therapy (maintenance of respiration and blood pressure), administration of flumazenil (in hospital settings). 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 the effectiveness of alprazolam.

    Hypotensive drugs can increase the severity of blood pressure lowering.

    With simultaneous administration with clozapine, an increase in respiratory depression is possible.

    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 plasma concentrations of imipramine and desipramine (by 31% and 20%, respectively) with simultaneous administration. The metabolic clearance of alprazolam decreases with the simultaneous administration of conventional therapeutic doses of cimetidine and antibiotics from the macrolide group. Caution should be exercised and thought about reducing the dosage of alprazolam when taken with cimetidine, macrolides, nefazodone, fluvoxamine, fluoxetine, propoxyphene, sertraline, daltiazem, digoxin, and oral contraceptives.

    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 taking antidepressants, anxiolytics or suffering 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.

    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.

    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.

    Direct use before birth or during labor can cause neonatal­respiratory depression, decreased muscle tone, hypotension, hypothermia, and a weak act of sucking (the so-called "sluggish child syndrome").

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

    For 50 tablets in a jar of dark glass.

    10 tablets per contour cell pack. Each jar or 5 contour mesh packages are placed in a pack of cardboard together with instructions for use.

    Storage conditions:

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

    Store in a dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002581
    Date of registration:29.07.2011 / 13.10.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.07.2017
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