Medazepam (Medazepamum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Anxiolytics

Included in the formulation
  • Mezapam
    pills inwards 
    ORGANICS, JSC     Russia
    • АТХ:

    N.05.B.A.03   Medazepam

    Pharmacodynamics:

    The benzodiazepine receptor agonist, which is closely related to GABAAreceptors. When benzodiazepine receptors are activated, the sensitivity of GABA increasesAreceptors to the mediator, which leads to an increase in the frequency of opening channels for chloride ions. There is hyperpolarization of the postsynaptic membrane of the neuron and suppression of neuronal activity, inhibition of interneuronal transmission in the central nervous system occurs.

    Has a pronounced anxiolytic effect. Eliminates anxiety, fear, psychoneurotic tension, motor anxiety, excessive fussiness. Restores critical assessment of one's own state. Sedation, hypnotics, central miorelaxing and anticonvulsant effects are less evident. Stabilizes the autonomic functions. It alleviates the symptoms of acute alcohol withdrawal.

    The soothing effect is combined with some activating properties; practically does not affect the daily performance. It is recommended for the therapy of weakened patients and elderly patients (due to the absence of pronounced myorelaxing and sedative properties). Assign for a short time, becauseat long reception, especially in high doses, development of mental (less often physical) drug dependence is possible. In children's practice appoint strictly according to the indications (reduces the ability to memorize).

    Pharmacokinetics:When ingested quickly absorbed from the gastrointestinal tract, bioavailability - 50-75%. Maximum concentration in blood is reached in 1-2 hours. Almost completely binds to plasma proteins (more than 99%). Metabolised in the liver by hydroxylation, N-demethylation and oxidation with the formation of active metabolites: desmethylmedazepam, diazepam, desmethyldiazepam (nordiazepam) and oxazepam. Metabolites have large half-lives, so after the end of the medazepam intake for another 3-14 days determine their significant concentrations in the blood plasma. Half-life of the medazepam from the plasma is 2 hours, and its half-life with allowance for metabolites is 20-176 hours. Active metabolites pass through the placental barrier and enter the breast milk. It is excreted as metabolites (mainly glucuronides) by the kidneys (63-85%) and through the intestine (15-37%).
    Indications:

    Neuroses, psychopathies, neurosis-like and psychopathic conditions, accompanied by increased excitability, irritability, emotional lability, decreased mood, tension, anxiety, fear; psycho-vegetative and psychosomatic disorders, incl. vegeto-vascular dystonia, sleep disorders, functional disorders of the cardiovascular system and gastrointestinal tract, migraine (prevention of attacks), menopausal syndrome.

    In pediatric practice: mental lability and excessive excitability in children, "school" neuroses.

    In narcology: alcohol withdrawal syndrome (uncomplicated), complex therapy of delayed neurotic disorders in the remission of alcoholism and drug addiction.

    ICD-10

    XXI.Z80-Z99.Z81.1   In a family history, alcohol dependence

    V.F10-F19.F10.3   Mental and behavioral disorders caused by alcohol use - withdrawal symptoms

    V.F40-F48.F40.2   Specific (isolated) phobias

    V.F40-F48.F41.9   Anxiety disorder, unspecified

    V.F40-F48.F43.2   Disorder of adaptive reactions

    V.F40-F48.F48   Other neurotic disorders

    V.F60-F69.F60   Specific personality disorders

    V.F60-F69.F60.3   Emotionally unstable personality disorder

    VI.G40-G47.G43   Migraine

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

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

    XVIII.R40-R46.R45.0   Nervousness

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

    XVIII.R40-R46.R45.4   Irritability and anger

    Contraindications:Hypersensitivity(including other benzodiazepine derivatives), closed-angle glaucoma, sleep apnea syndrome, acute liver and kidney disease, severe hepatic and / or renal insufficiency, severe myasthenia gravis, alcohol and drug dependence, pregnancy (I trimester), breast-feeding, children under 10 years.
    Carefully:Hepatic and / or renal failure, spinal and cerebellar ataxia, increased intraocular pressure, organic lesions of the central nervous system, circulatory and respiratory failure, children's age (prescribed for children strictly according to indications), elderly, weakened patients, pregnancy (II and III trimester) .
    Pregnancy and lactation:

    Contraindicated in the first trimester of pregnancy and lactation. Application in the II and III trimesters of pregnancy is possible only on strict indications.

    The FDA action category is not defined.

    For the duration of treatment, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside. The dosage regimen is set individually depending on the indications, course of the disease, tolerability, etc. Treatment should be started with a minimally effective dose, the daily dose is divided into 2-3 doses, if necessary, the daily dose is increased by increasing the evening dose. Average doses for adults: one-time - 10-20 mg, the average daily - 20-30 mg, the highest daily - 60-70 mg. At the beginning of treatment appoint 5 mg 2-3 times a day, then gradually increase the dose to 30-40 mg per day. In outpatient settings, taking 5 mg in the morning and in the afternoon and 10 mg in the evening is recommended. Elderly patients, adolescents, as well as in cases of impaired renal function - 5-10 mg 1-2 times a day or 10 mg per night. Children are given a dose depending on their age and body weight. Duration of treatment: approximately 2 weeks and not more than 2 months (including a period of gradual dose reduction). Before the second course, take a break of at least 3 weeks.

    At treatment of an alcoholism appoint 30 mg a day within 1-2 weeks.

    Side effects:

    From the nervous system and sensory organs: drowsiness, headache (usually at the beginning of treatment, disappears after dose reduction), dizziness, lethargy, weakness, fatigue, depressed mood (including in patients with a previous depressive illness), stuniness, confusion consciousness, anterograde amnesia, dysarthria, accommodation paromy, diplopia, eyeball twitching, chest pain, ataxia (in elderly patients and weakened patients); paradoxical reactions (strong arousal, a sense of fear, suicidal thoughts - more often in elderly patients and children, sleep disturbances, increased aggressiveness, seizures of different muscle groups).

    From the cardiovascular system: lowering blood pressure, tachycardia, bradycardia.

    On the part of the respiratory system: depression of the respiratory center (with airway obstruction or brain damage), alveolar hypoventilation (in patients with chronic obstructive pulmonary disease with high doses), dyspnea, laryngospasm.

    On the part of the gastrointestinal tract: dry mouth, nausea, vomiting, pain in the epigastric region, constipation, increased activity of hepatic transaminases, jaundice.

    Other: urinary retention, weakness of skeletal muscles, skin-allergic reactions (redness, itching, rash, exanthema), decreased libido, dysmenorrhea, chest pain; with prolonged use - development of addiction, dependence (physical and mental), withdrawal syndrome.

    Overdose:

    Symptoms: prolonged confusion, drowsiness, fatigue, ataxia, tachycardia, arterial hypotension, decreased muscle tone; in severe cases - coma, convulsions, respiratory depression, until the complete cessation of breathing and cardiac activity.

    Treatment: gastric lavage; reception of activated carbon and laxatives; control and correction of breathing, heart rate, blood pressure, body temperature and blood circulation; symptomatic therapy. Forced diuresis and hemodialysis are ineffective. If necessary, introduce a specific antagonist of benzodiazepines flumazenil.

    Interaction:Strengthens the effect of drugs that depress the central nervous system (including hypnotics, neuroleptics, antihistamines with a sedative, narcosis drugs, narcotic analgesics, ethanol and ethanol-containing drugs), muscle relaxants. When combined with alcohol, in addition to increasing the oppressive effect on central nervous system, it is possible to develop a paradoxical reaction. Theophylline in small doses eliminates the sedative effect of medazepam. Cimetidine, omeprazole, disulfiram, estrogen-containingOral contraceptives increase and prolong the action of medazepam. Nicotine accelerates the excretion of medazepam from the body.
    Special instructions:

    Medazepam should be used as short a course as possible. with prolonged use, especially in high doses, there is a risk of drug dependence. To prevent the development of withdrawal symptoms, the drug should be withdrawn, gradually reducing the dose.

    Reduces the ability to learn and memorize.

    During the treatment, alcoholic drinks are not allowed.

    Children medazepam apply according to strict indications.

    During the period of application of medazepam, it is not recommended to engage in potentially dangerous activities requiring fast psychomotor reactions, for example driving a car.

    Instructions
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