Clinical and pharmacological group: & nbsp

Anxiolytics

Included in the formulation
  • Nozepam
    pills inwards 
    ORGANICS, JSC     Russia
  • Tazepam
    pills inwards 
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.05.B.A   Benzodiazepine derivatives

    N.05.B.A.04   Oxazepam

    Pharmacodynamics:

    The drug is a benzodiazepine derivative, has an anxiolytic and sedative effect, central muscle relaxant activity and anticonvulsant properties. Has a calming and hypnotic effect on CNS. Removes emotional tension, reduces anxiety, fear, anxiety, promotes the onset of sleep. It alleviates the symptoms of acute alcohol withdrawal.

    The mechanism is realized due to the potentiation of GABAergic processes in the cerebral cortex, hippocampus, cerebellum, thalamus and hypothalamus.

    The mechanism of action is associated with the stimulation of benzodiazepine (ω) receptors whose agonist oxazepam are. There are 3 subtypes of ω-receptors - ω1, ω2, ω3. The hypnotic effect of the drug is due to the preferential binding to ω1-receptors. Stimulation of benzodiazepine receptors located on the γ-subunit of the GABAA receptor is accompanied by an increase in the affinity (sensitivity) of GABA receptors to GABA and an increase in the efficacy of this mediator.At the same time, GABA activity does not increase, which causes the absence of narcotic effect in benzodiazepines. When the sensitivity of GABA receptors to GABA increases under the influence of oxazepam, the frequency of opening of the chloride channels increases, as a result, a greater number of negatively charged chlorine ions enter the neuron, which leads to hyperpolarization of the neuronal membrane and the development of inhibitory processes.

    Pharmacokinetics:

    Absorption after oral administration is rapid (2 h) and complete. The maximum concentration after ingestion is 1-4 hours. It binds to plasma proteins by 97%, biotransformation in the liver by direct conjugation with glucuronic acid to inactive metabolites, the elimination half-life is 5-15 hours. Excreted by the kidneys and gastrointestinal tract.

    The drug passes through the blood-brain barrier, placental barrier and penetrates into breast milk.

    Indications:
    • Reactive depressions.
    • Neuroses.
    • Neuro-like and psychopathic conditions, accompanied by fear, anxiety, increased irritability, sleep disorders and others.
    • Psycho-vegetative disorders.
    • Anxiety associated with depression (as part of complex therapy).
    • Sesto-hypochondriacal disorders and obtrusiveness (especially with poor tolerability of other anxiolytics).
    • Alcohol abstinence syndrome (accompanied by acute arousal, tremor, threatening or acute delirium, hallucinations).
    • Vegetative disorders in women associated with menopause or menstrual cycle disorders.
    • Pronounced premenstrual syndrome.
    • Sleep disorders.

    V.F10-F19.F10.2   Mental and behavioral disorders caused by alcohol use - addiction syndrome

    V.F30-F39.F31   Bipolar affective disorder

    V.F30-F39.F32   Depressive episode

    V.F30-F39.F33   Recurrent depressive disorder

    V.F40-F48.F40   Phobic anxiety disorders

    V.F40-F48.F41   Other anxiety disorders

    V.F40-F48.F41.2   Mixed anxiety and depressive disorder

    V.F40-F48.F43   Reaction to severe stress and adaptation disorders

    V.F40-F48.F45.3   Somatoform dysfunction of the autonomic nervous system

    V.F40-F48.F48   Other neurotic disorders

    V.F40-F48.F48.0   Neurasthenia

    V.F50-F59.F51.2   Sleep and wakefulness disorder inorganic etiology

    VI.G40-G47.G47.0   Disturbances of falling asleep and maintaining sleep [insomnia]

    XVIII.R40-R46.R45.1   Anxiety and Excitement

    XVIII.R40-R46.R45.7   Condition of emotional shock and stress, unspecified

    XIV.N80-N98.N94.3   Premenstrual tension syndrome

    XIV.N80-N98.N95.1   Menopause and menopause in women

    Contraindications:
    • Acute alcohol intoxication.
    • Coma.
    • Shock.
    • Intoxication with medications that depress the central nervous system (narcotic analgesics, hypnotics and psychotropic drugs).
    • Myasthenia gravis.
    • Closed-angle glaucoma.
    • Severe depression.
    • Age before 6 years.
    • Hypersensitivity.
    • Pregnancy (especially I trimester).
    • Lactation.
    • Heavy depression.
    • Acute respiratory failure.
    • Chronic obstructive pulmonary disease.
    Carefully:

    Arterial hypertension, old age, hyperkinesis, psychosis, organic brain diseases, drug dependence in history, hypoproteinemia, liver, kidney, nighttime apnea, abuse of psychotropic drugs, spinal, cerebral ataxia.

    Pregnancy and lactation:

    Category FDA not determined, is contraindicated in pregnancy and lactation.

    Regular use during pregnancy can lead to a withdrawal syndrome in a newborn, use in the last weeks of pregnancy and during childbirth leads to CNS depression, lethargy,hypothermia, respiratory and feeding disorders in a newborn. It is advisable to avoid use during pregnancy, carefully correlate potential risks and benefits and exclude pregnancy before therapy begins.

    Dosing and Administration:

    Orally, regardless of food intake.

    Adults: 10-20 mg 2-3 times a day.

    Elderly patients: 10-20 mg twice a day.

    Children: 10-30 mg per day for 2-3 hours.

    The maximum daily dose for inpatient treatment is 120 mg

    Side effects:

    From the nervous system and sensory organs: sleepiness (usually in the first days of treatment), lethargy, dizziness, fatigue, fatigue, headache, memory impairment, muscle weakness, ataxia, tremor, lubricated speech, weakness, paradoxical reactions in mentally ill, including psychomotor agitation, anxiety, ataxia.

    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, decreased appetite, constipation, or diarrhea; a violation of liver function, increased activity of "liver" transaminases and alkaline phosphatase, jaundice.

    From the genitourinary system: urinary incontinence, urinary retention, impaired renal function, weakened libido, dysmenorrhea.

    Allergic reactions: skin rash, itching.

    Influence on the fetus: teratogenicity, CNS depression, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

    Other: addiction, drug dependence, reduction of blood pressure; rarely - depression of the respiratory center, impaired vision (diplopia), bulimia, weight loss, tachycardia, anterograde amnesia.

    With a sharp reduction in dose or discontinuation arises withdrawal syndrome: irritability, headache, anxiety, excitement, agitation, a sense of fear, nervousness, sleep disturbance, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perceptual disorders, including hyperacusis , paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - acute psychosis).

    Overdose:

    Symptoms: oppression CNS various degrees of expression - drowsiness, confusion, lethargy; in more severe cases (especially against the background of receiving other drugs, depressing CNS or alcohol) - ataxia, depression HELL, hypnotic state, coma.

    Treatment: induction of vomiting, gastric lavage, symptomatic therapy, monitoring of vital functions. With severe hypotension - the administration of norepinephrine. A specific antidote, a benzodiazepine receptor antagonist flumazenil (introduction only in a hospital). Hemodialysis is ineffective.

    Interaction:

    Strengthens the effect of means that depress CNS, including hypnotic, antiepileptic, neuroleptics, opioid analgesics, indirect muscle relaxants, means for general anesthesia, alcohol. The drug may alter the effect of indirect anticoagulants.

    Medicines that block calcium secretion can increase the effect of oxazepam.

    Reduces the effectiveness of levodopa in patients with Parkinsonism.

    Inhibitors of microsomal oxidation prolong the half-life, increase the risk of toxic effects.

    Inducers of microsomal liver enzymes reduce the effectiveness of oxazepam.

    The narcotic analgesics intensify euphoria, leading to an increase in mental dependence.

    Cimetidine, disulfiram, estrogen-containing oral contraceptives and erythromycin increase the concentration and lengthen the action of the drug (due to inhibition of hepatic metabolism), to a lesser extent affect oxazepam, which binds to glucuronic acid.

    Hypotensive drugs can increase the severity of blood pressure lowering.

    Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.

    Oxazepam may increase the toxicity of zidovudine.

    Inhibitors of monoamine oxidase, strychnine, corazole and large doses of caffeine weaken the action of oxazepam.

    Special instructions:

    The drug should be phased out gradually.

    Oxazepam should not be used for a long time (for several months) due to the possibility of developing drug dependence. With prolonged treatment, it is necessary to monitor liver function and the state of peripheral blood.

    They are used with caution for predisposition to arterial hypotension, especially in elderly patients (due to the possibility of cardiac dysfunction), an increased risk of drug dependence.

    It is recommended in the treatment of anxiety, stress, agitation, irritability in weakened patients, people of senile age, as well as patients with residual traumatic or infectious lesions CNS.

    It should be borne in mind that anxiety or stress associated with everyday stress usually do not require treatment with anxiolytics.

    During the treatment period, vehicles should not be driven and other potentially hazardous activities that require increased attention; do not drink alcohol.

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