Mezapam: indications for use

Composition and features

The drug belongs to the pharmacological group of anxiolytics. The main active ingredient of the drug is medazepam. Available in the form of tablets, granules and a substance for oral administration with different concentrations of the active component.

Mezapam is considered a “daytime” tranquilizer, as it does not cause drowsiness or decreased performance.

The tablets contain 10 mg of medazepam and are intended for the treatment of psycho-emotional disorders in adults. Granules and solution are usually prescribed to children in individual dosages.

The cost of the drug is about 1000 rubles, it is available in pharmacies with a prescription, and the shelf life at room temperature is 3 years.

Publications in the media

(Medazepamum) INN Synonyms. Mezapam, Rudotel. Composition and release form. Medazepam tablets 0.01 g.

Indications. Neuroses, psychopathy, neurosis-like and psychopath-like states in schizophrenia; somatic diseases accompanied by signs of emotional stress, anxiety, fear, increased irritability, senesto-hypochondriacal, obsessive and phobic disorders. Pharmachologic effect. Medazepam is considered among benzodiazepine derivatives as a “daytime” tranquilizer, since it, having a pronounced anxiolytic effect, does not have a sedative-hypnotic effect. The mechanism of action of the drug - see diazepam . Pharmacokinetics. When taken orally, the drug is absorbed from the gastrointestinal tract into the blood by 49-75%; The peak concentration of the drug in the blood serum is observed after 1-2 hours. It is almost completely (99.8%) bound to blood plasma proteins. Metabolized in the liver by hydroxylation, oxidation and N-demethylation. Metabolites in the form of compounds with glucuronic acid are excreted by the kidneys (63-85%) and through the intestines. T1/2 is 20-176 hours. Metabolites of the drug (oxazepam, desmethylmedazepam, diazepam, desmethyldiazepam) have a longer T1/2, so they can be detected in the blood for another 3-14 days after finishing taking medazepam. Side effects. Feeling of slight fatigue, headache, irritability, nervousness, ataxia, loss of libido, impotence, menstrual irregularities, hypoventilation. Contraindications. Myasthenia; severe chronic obstructive pulmonary diseases; hypersensitivity to benzodiazepines. Adverse reactions when interacting with other drugs. See diazepam .

Information for the patient. Medazepam is usually prescribed 0.005 g in the morning and at lunch after meals, and in the evening - 0.01 g; drink with enough water. It is recommended to prescribe the drug only for a short time due to the risk of drug dependence. Missed dose: take as soon as you remember the missed dose, but no later than 1 hour after the missed dose; if more time has passed, then the missed dose is not taken at all; do not take double doses. During treatment with medazepam, you should refrain from drinking alcoholic beverages and driving vehicles.

Therapeutic effect

Medazepam belongs to the anxiolytic substances of the benzodiazepine series. It has a relaxing, psychotropic and anticonvulsant effect. The sedative and hypnotic effect is weak, so it can be taken during the daytime without the risk of adverse reactions in the form of increased drowsiness, fatigue and decreased performance.

The active substance Mezapam relieves the most common manifestations of psycho-emotional disorders - anxiety, mood swings, excessive excitement, fear.

The drug has a weak thymoleptic effect, that is, it increases emotional activity and improves mood.

The maximum effect from taking Mezapam is achieved after a week, since its components have a cumulative effect.

After oral administration, medazepam is rapidly absorbed from the gastrointestinal tract, metabolized and bound to plasma proteins. One of the metabolites of the substance, nordiazepam, has a cumulative effect, due to which its concentration in the blood remains high for 3-14 days after taking the drug. The remaining components are excreted by the kidneys and intestines.

Pharmacological properties of the drug Medazepam

Daytime tranquilizer of the group of benzodiazepine derivatives. It has an anxiolytic, muscle relaxant, sedative and anticonvulsant effect. Medazepam has moderate affinity for benzodiazepine receptors in the central nervous system; pharmacological effects are mainly due to competitive stimulation of GABA receptors by active metabolites. It has a pronounced anxiolytic and weak, practically no effect on self-control, sedative effect. Eliminates anxiety, fear, mental stress, general motor restlessness, and fussiness. Stabilizes physical activity. Does not have antidepressant or antipsychotic effects. With long-term use, especially in high doses, there is a risk of developing drug dependence. However, tolerance and physical and mental dependence rarely develop. When taken orally, 49–75% of medazepam is absorbed. The maximum concentration in blood plasma is achieved 1–2 hours after oral administration. Medazepam is almost completely (99.8%) bound to plasma proteins. Metabolized in the liver. The half-life of medazepam is 20–176 hours; its pharmacologically active metabolites also have long half-lives (after discontinuation of medazepam, significant concentrations of its metabolites are determined in the blood plasma for 3–14 days).

Indications for treatment

Indications for the use of Mezapam include the following psycho-emotional disorders:

• neuroses of various etiologies and forms;
• psychopathy, accompanied by nervous excitement, emotional lability, constant tension;
• cardiopsychoneurosis;
• withdrawal syndrome in chronic alcoholism and its treatment;
• disturbances in the emotional state of women associated with the onset of menopause.

Mazepam is prescribed to children for “school” neuroses, hyperactivity, and increased excitability. The drug can be used to prevent migraine attacks in patients who are prone to this pathology. It can be used both for the treatment of situational neuroses (associated with moving to another place of residence, changing jobs, etc.) and for the treatment of chronic disorders of the psycho-emotional state.

Mode of application

Tablets and granules are taken orally, best before meals. The starting dosage is 5 mg 2-3 times a day, after which it can be gradually increased to 30 mg daily, but not more than 40 mg. For outpatient treatment, the standard therapeutic regimen is as follows: 5 mg of the active substance in the morning and 10 mg in the evening.

Adult patients treated as inpatients are allowed to increase the maximum dosage of the active component to 60-70 mg per day.

The dosage and treatment regimen may differ from those recommended if the doctor selects them individually.

Elderly people and children over 10 years of age are prescribed 10-20 mg; when treating patients under ten years of age, the dosage is prescribed individually. The standard dose for the treatment of chronic alcoholism is 30 mg daily. The course of treatment lasts no more than 2 months, after which a break is taken for at least 3 weeks, and a repeat course is prescribed if necessary.

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Medazepam overdose, symptoms and treatment

Manifested by fatigue, lethargy, ataxia, tachycardia, decreased blood pressure, muscle hypotension; in severe cases - coma, convulsions, respiratory depression. As a result of the long half-life of pharmacologically active metabolites, overdose symptoms may persist for quite a long time. Treatment: gastric lavage, taking activated carbon and sodium sulfate; monitoring and correction of the functions of the cardiovascular and respiratory systems, and, if necessary, symptomatic treatment. Forced diuresis and hemodialysis are usually ineffective or ineffective.

List of pharmacies where you can buy Medazepam:

• Moscow
• Saint Petersburg

Side effects

Like all “daytime” tranquilizers, Mezapam rarely causes side effects, but sometimes the following reactions may develop:

• drowsiness, chronic fatigue, weakness;
• headaches and dizziness;
• confusion;
• sexual dysfunctions and menstrual cycle disorders in women;
• respiratory dysfunction, pulmonary hypoventilation;
• heart rhythm disturbances, arterial hypotension;

• dryness of the mucous membranes of the mouth, diarrhea;
• urinary retention;
• allergic reactions, manifested by itching, hives, rash;
• pain in the sternum area.

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Most often, adverse reactions during treatment are mild or moderate. They usually develop after the first dose and disappear after a few days or after reducing the dosage. If the condition worsens, it is better to stop taking it and consult a doctor.

T.S. Illarionova Department of General and Clinical Pharmacology, RUDN University, Moscow

An old friend is better than two new ones.

According to statistics, 10-12% of the total population uses benzodiazepine tranquilizers. Global consumption of psychopharmacological drugs has increased more than 5 times over the past 20 years. This increase in consumption is explained by the widespread use of psychotropic drugs not only in psychiatric but also in general practice. Moreover, if until 1970 the largest share in the structure of the Russian market of drugs with psychopharmacological action fell on the group of psychostimulants (36%), then subsequently negligible numbers of them were registered, and the structure of the market changed due to the rapid expansion of the range of tranquilizers and antidepressants. Data on the consumption of benzodiazepine tranquilizers (BDTs) indicate that these drugs remain the most common psychotropic drugs to date. Indications for their use in relation to mental disorders cover both subclinical and complete psychopathological conditions. The term “tranquilizers” (from the Latin tranquillo - calmness, serenity) entered the medical literature in 1957 to designate psychotropic drugs used mainly for neuroses, states of mental tension and fear. Unlike neuroleptic substances, most tranquilizers do not have a pronounced antipsychotic effect. Benzodiazepine tranquilizers (BT) have been widely used in medicine since the 1960s, when the high tranquilizing activity of benzodiazepine derivatives - the drugs chlordiazepoxide and diazepam - was discovered (1962). These two drugs marked the beginning of widespread study of benzodiazepines and the creation of a number of highly active tranquilizers. Radicals in the benzodiazepine molecule are easily replaced at various positions, which has led to the synthesis of about 3000 compounds, of which more than 40 are used today as drugs. Currently, medazepam (Rudotel), nitrazepam, bromazepam, alprazolam, etc. are widely used. The characteristics of the psychotropic effect of each tranquilizer of the benzodiazepine structure are determined by the ratio of pharmacological properties in the spectrum of action of the individual drug. As is known, the main manifestations of action characteristic of all benzodiazepines are the following: anxiolytic, anticonvulsant, hypnotic, sedative, muscle relaxant. In addition, many drugs in this group have antihypoxic, vegetotropic, antiarrhythmic, hypotensive effects, and alprazolam has antidepressant and antipanic effects. The combination of various effects of each drug determines the uniqueness of the pharmacological spectrum and indications for its use. Benzodiazepines are the most widely used drugs among psychotropic drugs, not only in psychiatric practice, but also in other areas of medicine (neurology, surgery, dermatology, pediatrics, oncology, obstetrics, gynecology, etc.). In psychiatric practice, BDT is effective for various neurotic, neurosis-like psychopathic and psychopathic conditions, accompanied by anxiety, fear, increased irritability, and emotional lability. BT are effective for obsessions, phobias, and hypochondriacal syndromes. Some of these drugs are indicated for psychogenic psychoses and panic reactions. BTs are also used to relieve alcohol withdrawal, are prescribed as anticonvulsants and hypnotics, and are used for premedication in preparation for surgical operations.

“Daytime” tranquilizers For use in general medical practice, a group of “daytime” tranquilizers (medazepam, tofizepam, alprazolam) is distinguished - drugs with a pronounced anxiolytic effect, but do not cause some sedative effects in therapeutic doses - muscle relaxation, impaired coordination of movements and operant activity, drowsiness and etc. Medazepam (Rudotel) has all the main types of action of BDT. However, the lower severity of sedative and muscle relaxant effects determines fewer side effects of the drug, especially in relation to mental and physical performance during the day. In addition, medazepam has a normalizing effect on disorders of the autonomic nervous system. Back in the 1970s. As a result of clinical studies of the drug Rudotel® (medazepam), manufactured by AWD, it was concluded that the drug can be successfully used as a “daytime” tranquilizer for the treatment of working patients, without affecting their professional activities, as well as for the treatment of people experiencing strong psycho-emotional stress, and really helps to improve working and living conditions for such patients. Medazepam is metabolized in the liver by hydroxylation, N-demethylation and oxidation. The main pharmacologically active metabolites of medazepam are oxazepam (7.1% of the dose), desmethylmedazepam, diazepam and desmethyldiazepam (nordiazepam). Nordiazepam has a long T1/2 (80 hours, but with fluctuations ranging from 30 to 200 hours), accumulates in the body and probably has a pronounced sedative effect. The ability of the drug to be metabolized to form nordiazepam ensures the implementation of anxiolytic activity. The principle of action of medazepam, like other benzodiazepines, is the binding of the drug molecule to the “benzodiazepine” receptor (alpha 1 and gamma 2 subtypes), as a result of which the affinity for the GABA-A receptor increases, GABA is released, which interacts with two beta receptor subtypes - the frequency of opening of chlorine channels increases; the flow of chlorine into the neuron increases - hyperpolarization of the membrane occurs and the process of inhibition develops (suppression of neuronal activity). Like other benzodiazepine tranquilizers, medazepam has a sedative, anxiolytic, muscle relaxant, and anticonvulsant effect, but the muscle relaxant and general depressant effect is relatively less pronounced. The calming effect of medazepam is combined with some activating effect. In this regard, it is considered as a “daytime” tranquilizer, which is less disruptive to performance during the day. The drug potentiates the effect of sleeping pills, narcotics, and analgesics. Medazepam is prescribed to patients with neuroses, psychopathy and other neuropsychic disorders with neurosis-like and psycho-like disorders, accompanied by increased excitability, irritability, tension, anxiety, fear, emotional lability, as well as with withdrawal syndrome. The absence of pronounced muscle relaxant and hypnotic properties allows mezapam to be prescribed to debilitated patients, the elderly and children. Medazepam is taken orally (regardless of food intake).

Treatment of primary nocturnal enuresis in children and medazepam (Rudotel) Enuresis is persistent involuntary urination that occurs in an individual at different times of the day (night, day, combined) due to various etiological reasons. In turn, primary nocturnal enuresis is urinary incontinence at night, which was not preceded by at least a 6-month period of bladder control in a child aged 5 years or more. Medazepam (Rudotel) is one of the drugs used in the treatment of primary nocturnal enuresis in children and adolescents. Taking into account the development of resistance to therapy with the first-choice drug desmopressin, the relevance of the use of anxiolytics in this pathology increases. Rudotel is dosed at the rate of 2 mg/kg/day and is prescribed in two doses.

Premenstrual syndrome and medazepam (Rudotel) Premenstrual syndrome (PMS) is a complex pathological symptom complex that occurs during the premenstrual days and is manifested by neuropsychic, vegetative-vascular and metabolic-endocrine disorders. Symptoms of PMS occur 2-10 days before the start of menstruation and disappear in the first days or immediately after the end. In addition to the most characteristic symptoms (increased fatigue, engorgement and tenderness of the mammary glands, bloating, nausea, sometimes vomiting, sleep and coordination disturbances, swelling of the extremities of varying severity, pain in the back and pelvic area, weight gain, itching of the skin, pain in the heart, tachycardia), with PMS, irritability, tearfulness, depression, aggressiveness, indecision, forgetfulness, hypochondriacal thoughts, suspiciousness, increased demands on others, isolation, unmotivated fear of “expected misfortune”, a feeling of loneliness, bad mood or its rapid change are often observed. etc. In 5-10% of women, PMS symptoms are pronounced. Depending on the type of PMS, along with specific therapy (hormones - Norkolut, Duphaston, Regulon; antihistamines, magnesium supplements, vitamins, etc.), it is recommended to prescribe Rudotel for emotional lability from the 10th day of the menstrual cycle.

Benzodiazepines and somatic diseases: compatibility with somatotropic drugs When treating mental disorders in patients with somatic diseases, there are indications for the simultaneous prescription of various types of psychotropic drugs and drugs used in the clinic of internal diseases. In this case, it is necessary to take into account the somatotropic effects of psychopharmacotherapy, as well as drug interactions of psycho- and somatotropic medications. Accordingly, the problem of choosing psychotropic drugs comes to the fore. The results of a number of studies indicate that such drugs may primarily include tranquilizers, as well as some antidepressants and antipsychotics, which have a minimal effect on somatic functions and a low likelihood of adverse interaction with somatotropic drugs.

Safety of benzodiazepine tranquilizers in somatic diseases The safety of the use of anxiolytics is associated with the absence of adverse effects on a number of functional systems of the body, as well as interactions with somatotropic drugs. According to M.Yu. Drobizheva (2000), the only fairly common undesirable effect of tranquilizers (15.4% of all those treated) is “behavioral toxicity” (daytime drowsiness, muscle relaxation, impaired attention and motor coordination). Here, a very limited effect of tranquilizers on the functions of internal organs is noted. Tranquilizers do not have a significant effect on respiratory rate, pumping function of the heart, blood pressure levels, cardiomyocyte conductivity, appetite and fat metabolism, and do not help slow down the passage of food through the intestines or the development of hematological complications. These results almost completely coincide with the data of a number of publications. In the literature, there are only isolated references to the possibility of reversible and non-fatal depression of the respiratory center with intravenous administration of high doses of diazepam, especially in patients suffering from chronic obstructive pulmonary diseases. Moreover, this effect is not found in other benzodiazepine derivatives. Similarly, there are only anecdotal reports in the literature that some anxiolytics (diazepam administered intravenously and lorazepam administered orally) may slightly reduce myocardial contractility and, as a result, slightly reduce cardiac output. It is indicated that most tranquilizers have virtually no effect on blood pressure, and only with their overdose is unexpressed arterial hypotension possible. The likelihood of an inhibitory effect of anxiolytics on bone marrow hematopoiesis is minimal. Thus, when taking benzodiazepine derivatives, hematological complications (leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia) occur extremely rarely and are reversible. Tranquilizers do not have clinically significant effects on the endocrine system. The exception is extremely rare cases of mild hyperprolactinemia, hyperglycemia and glycosuria. Concluding the enumeration of the somatotropic effects of tranquilizers, it should be emphasized that the drugs in question also have a number of therapeutically desirable effects. Monotherapy with benzodiazepines is effective for so-called functional heart rhythm disorders (sinus tachycardia, atrial and ventricular arrhythmia, paroxysmal atrial fibrillation). Thus, in a joint study (Department for the Study of Borderline Mental Pathology and Psychosomatic Disorders of the National Center for Mental Health of the Russian Academy of Medical Sciences and the Department of Clinical Pharmacology of the I.M. Sechenov Moscow Medical Academy) it was shown that in more than a third of 200 patients with the considered heart rhythm disturbances, the prescription of benzodiazepine anxiolytics (medazepam) , chlordiazepoxide, oxazepam, diazepam, bromazepam, tofisopam) is accompanied by a complete reduction of painful manifestations. Some publications indicate that tranquilizers have an independent coronary effect. It is even recommended to use benzodiazepine anxiolytics in resuscitation practice to “postpone” the increase in oxygen demand in seriously ill patients, especially those with combined respiratory and cardiovascular failure, who need to undergo certain manipulations. Most tranquilizers (benzodiazepine derivatives) reduce gastric secretion and reduce the content of pepsin and hydrochloric acid in gastric juice as a result of both direct anticholinergic and central sedative and vegetostabilizing effects. Such effects of the psychotropic drugs in question are used in the combined treatment of peptic ulcer. The possibility of using tranquilizers in gastroenterology is associated with their antiemetic effect, which extends even to dyspeptic symptoms caused by taking chemotherapy drugs or radiation therapy, as well as to “nausea and vomiting of anticipation” that occurs in cancer patients before starting the next course of chemotherapy.

Interaction of tranquilizers with somatotropic drugs According to the literature, even if tranquilizers enter into unfavorable interactions with somatotropic drugs, the effects of such interaction are not so pronounced. In particular, the combined use of non-selective beta-blockers (propranolol) and tranquilizers may contribute to some increase in the behavioral toxicity of psychotropic drugs. Much less often, similar effects occur when tranquilizers are combined with central α2-adrenergic agonists (clonidine) and calcium channel blockers. When tranquilizers and diuretics are used together, a slight increase in arterial hypotension may be observed. The results of the interaction of a combination of methylxanthine derivatives (aminophylline, theophylline) with anxiolytics are equally moderate. Thus, when methylxanthine derivatives and benzodiazepines are co-administered, a slight increase in blood pressure may occur. Gel-structured antacids (Almagel, Maalox) impair the absorption of benzodiazepine tranquilizers. However, despite this, the completeness of absorption is not affected and, accordingly, the clinical effects of the anxiolytics in question occur later. The H2 receptor blocker cimetidine, due to inhibition of hepatic metabolism, reduces clearance and slightly increases the blood content of a number of benzodiazepine derivatives (medazepam, diazepam, chlordiazepoxide, alprazolam), which is easily corrected by slightly reducing the doses of psychotropic drugs. An increase in the prothrombin index was noted when benzodiazepines were combined with warfarin. Finally, it is mentioned that when antidiabetic drugs are combined with benzodiazepine derivatives, a slight increase in the hypoglycemic effect is observed.

Benzodiazepines during pregnancy The safety of drugs in this series for the human fetus has not been proven. Given the ability of benzodiazepines to cross the placental barrier and the likelihood of developing cardiac arrhythmias in the fetus, their use should be avoided in early pregnancy. At the same time, according to the Hungarian Case-Control Surveillance of Congenital Abnormalities (HCCSCA) study, conducted by the National Center of Epidemiology in Budapest, the purpose of which was to identify a cause-and-effect relationship between the birth of children with congenital pathologies (CP) and therapy including benzodiazepine anxiolytics : medazepam, nitrazepam, tofisopam, alprazolam and clonazepam, which were not discontinued during pregnancy, 38,151 children were born between 1980 and 1996 without any anomalies, 75 (0.20%) women took one during pregnancy of the five benzodiazepines studied. In 22,865 cases of births of children with congenital anomalies, only 57 (0.25%) were treated with benzodiazepine drugs. Moreover, the use of these drugs in the period between the second and third months of pregnancy - the most critical period for the development of most CAP - did not lead to significant differences in comparison with the control. Thus, in this study, E. Eros et al. (2002) failed to identify an association between the use of medazepam and other benzodiazepines and an increase in teratogenic risk in humans. It should be noted that the study included only cases of births of children with congenital anomalies, which could limit the informativeness of these results.

Recommended literature 1. Dorofeeva V., Belyakova O., Sinaiskaya O. Market of psychopharmacological drugs: baggage of the 20th century // Russian pharmacies. 2003. No. 1-2. 2. Drobizhev M.Yu. Psychopharmacotherapy in the general somatic network (somatotropic effects, compatibility with somatotropic drugs) // Psychiatry and psychopharmacotherapy. 2000. T. 2. No. 2. 3. Lawrence D.R., Bennett P.N., Brown M.J. Clinical pharmacology / trans. from English 2nd ed. M.: “Medicine”, 2002. 680 p. 4. Mezhevitinova A.E. Premenstrual syndrome (to help the practitioner) // Gynecology. 2002. T. 4. No. 3. 5. Studenikin V.M. Treatment of primary nocturnal enuresis in children // Pediatrics. 2004. T. 6. No. 2. 6. Shelkovsky V.I., Studenikin V.M., Maslova O.I. Nocturnal enuresis in children // Issues of modern pediatrics. 2002. No. 1 (1). pp. 75-82. 7. Eros E., Czeizel AE, Rockenbauer M., Sorensen HT, Olsen J. A population-based case-control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy // Eur. J. Obstet. Gynecol. Reprod. Biol. 2002; 101(2):147-54. 8. Program on substance abuse. Rational use of benzodiazepines. WHO. 1996.

Contraindications for use

The following diseases and pathological conditions are contraindications for use:

• individual intolerance to the components of the drug;

• myasthenia gravis;
• acute renal and hepatic dysfunction;
• apnea attacks;
• drug addiction;
• first trimester of pregnancy, lactation period.

Medazepam is prescribed with caution in case of kidney and liver failure, pregnancy, ataxia, increased intraocular pressure, and organic lesions of the central nervous system. In case of disorders of the respiratory system and an increased tendency to allergic reactions, therapy is best carried out under the supervision of a doctor in a hospital. Treatment of elderly patients requires monitoring of vital signs.

Side effects of the drug Medazepam

When you first take medazepam, you may feel slightly tired and have a headache, which can be corrected by reducing the dose. In elderly patients and children, disorientation, impaired inhibition processes, aggressiveness, and increased fatigue are possible; in elderly patients and patients with mental retardation - ataxia, correctable by dose reduction. From the reproductive system: decreased libido, impotence, menstrual irregularities. From the respiratory system: rarely - hypoventilation in patients with COPD when taking high doses.

special instructions

Medazepam is recommended for short-term use, since long-term treatment may lead to drug addiction and withdrawal symptoms. Physical dependence on the drug is rare, but with increasing recommended doses, unpleasant consequences may develop. To prevent withdrawal symptoms, withdrawal of the drug must be carried out gradually.

In children (up to 10 years), medazepam is used only in case of emergency under strict medical supervision. During treatment, learning and memory processes may slow down and cognitive functions may decline. If there are no sufficient grounds for using the drug in a child, it is better to replace it with safer means.

The active ingredient Mezapam can cause drowsiness and decreased psychomotor reactions, therefore, during therapy it is recommended to avoid potentially hazardous activities. Drinking alcoholic beverages during therapy is strictly prohibited. In people with chronic alcoholism, the drug should be used with caution.

MESAPAM

Dosage form:

granules for the preparation of suspension for oral administration [for children], tablets

Pharmachologic effect:

A “daytime” anxiolytic drug (tranquilizer) from the group of benzodiazepines, it has anxiolytic, muscle relaxant and antiepileptic effects, and has a slightly pronounced thymoleptic effect. Interacts with benzodiazepine receptors of the limbic system and the ascending activating formation of the brain stem, promotes the opening of Cl channels, which leads to an increase in the inhibitory effects of GABA in the central nervous system. Eliminates anxiety, fear, psychoneurotic tension, general motor agitation, excessive fussiness, restores emotional behavior and has a stabilizing effect on the autonomic nervous system. Restores a critical assessment of one’s own illness. Antiepileptic, central muscle relaxant, sedative and hypnotic effects are less pronounced than those of typical benzodiazepine anxiolytic drugs (tranquilizers).

Indications:

Neuroses, psychopathy with anxiety, agitation, nervous tension, irritability, migraine (prevention of attacks), menopausal syndrome, alcoholism (withdrawal syndrome). Children have “school” neuroses, mental lability, and excessive excitability.

Contraindications:

Hypersensitivity, myasthenia gravis, acute liver and kidney diseases, sleep apnea, alcohol and drug addiction, pregnancy (first trimester), lactation period, children (up to 10 years). With caution. Hepatic and/or renal failure, pregnancy, spinal and cerebellar ataxia, intraocular hypertension, organic lesions of the central nervous system, respiratory failure, old age, general severity of the condition.

Side effects:

From the nervous system: drowsiness, headache (the first reaction to administration, disappearing after reducing the dose), weakness, dizziness, stunnedness, anterograde amnesia, depression, confusion, dysarthria, ataxia (in elderly patients and patients with mental retardation), paresis accommodation; in elderly patients and children - loss of orientation, disinhibition, aggressiveness. From the cardiovascular system: tachycardia, decreased blood pressure. From the digestive system: dry mouth, dyspepsia, increased activity of “liver” transaminases. From the respiratory system: depression of the respiratory center (with airway obstruction or brain damage), alveolar hypoventilation (in patients with COPD when taken in high doses). Other: decreased potency and/or libido, dysmenorrhea, urinary retention, spasm of the vocal cords, chest pain, withdrawal syndrome, paradoxical reactions, drug dependence (especially with long-term use), allergic reactions. Overdose. Symptoms: feeling of fatigue, catalepsy, ataxia, tachycardia, decreased blood pressure, muscle hypotension; in severe cases - coma, convulsions, respiratory depression. Treatment: gastric lavage, taking activated charcoal and laxatives, intravenous fluid infusion, monitoring respiratory rate, heart rate, blood pressure and body temperature, general measures aimed at maintaining the basic vital functions of the body, and preparing all the conditions necessary for emergency care with the possible development of airway obstruction. Forced diuresis and hemodialysis are ineffective.

Directions for use and dosage:

Orally, before meals, starting with 5 mg 2-3 times a day, gradually increasing the dose to 30 mg/day (if necessary, up to 40 mg/day). In outpatient settings, it is recommended to take 5 mg in the morning and at noon and 10 mg in the evening. The maximum daily dose for adults is 40 mg (in outpatient settings) and 60-70 mg (in hospital settings). Duration of the course - no more than 2 months, repeated course - after a break (at least 3 weeks). Elderly people and adolescents are prescribed 10-20 mg/day, children a single (daily) dose: at the age of 1-2 years - 1 mg (2-3 mg), 3-6 years - 1-2 mg (3-6 mg), 7-10 years - 4-8 mg (6-24 mg) and over 10 years - 6-10 mg (20-60 mg). When treating alcoholism, 30 mg/day is prescribed for 1-2 weeks.

Special instructions:

During the treatment period, it may cause difficulty remembering and learning; you should refrain from drinking ethanol. When treating and preventing the development of withdrawal syndrome, withdrawal is carried out gradually. Prescribed for a short time, with long-term use - the formation of drug dependence (if the dose is excessively exceeded - the development of tolerance and mental dependence). 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.

Interaction:

When administered together, there is a mutual enhancement of the effects of ethanol, narcotic analgesics, drugs for general anesthesia, centrally acting muscle relaxants, barbiturates, sleeping pills, and antidepressants. When taking centrally acting antihypertensive drugs, beta-blockers or anticoagulants simultaneously, the result of the interaction is unpredictable. Inhibitors of microsomal oxidation (cimetidine) enhance and prolong the effect, inducers (barbiturates and phenytoin) weaken it. Oral contraceptives may delay the metabolism of medazepam, resulting in an increase in the intensity and duration of its action. Reduces the effect of levodopa, enhances phenytoin (inhibition of the metabolism of the latter).

Drug interactions

It is not recommended to use Mezapam simultaneously with antihypertensive drugs, cardiac drugs and anticoagulants, as the results of the interaction can lead to unpleasant consequences. When taking opioid analgesics, anesthetics and muscle relaxants, serious depression of central nervous system functions is possible. Oral contraceptives inhibit the metabolism of the active substance, which can lead to an increase in the therapeutic effect and unwanted reactions of the body.

Reviews and opinions of patients

Reviews from patients who took Mezapam to eliminate symptoms of psycho-emotional disorders are generally positive. The drug is highly effective and mild, as well as the absence of adverse reactions. However, some patients said that taking it causes mild lethargy and the return of symptoms even after completing the full course of treatment.

Analogues and substitutes

There are no exact analogues of Mezapam, since only this drug is made on the basis of medazepam. The list of the closest drug substitutes includes benzodiazepine tranquilizers, which have a similar mechanism of action. This is a whole group of drugs that include drugs based on diazepam, lorazepam and other substances.

Benzodiazepine derivatives have a similar mechanism of action and indications for use, but may differ in the characteristics of their effects. Before replacing one drug with another, you should consult your doctor, and during therapy strictly follow the instructions and medical recommendations. This is especially true for the elderly, children and patients with concomitant disorders.

When is Mezapam necessary?

Mezapam is a tranquilizer with an anxiolytic effect that has a rapid and long-lasting effect. It helps against neuroses and psycho-emotional disorders, accompanied by increased excitability, panic attacks, anxiety and other symptoms.

The drug is considered a safe drug, has a small list of contraindications and side effects, but if taken uncontrolled, it can cause dependence and withdrawal symptoms. Treatment with Mezapam quickly normalizes the activity of the nervous system, but requires extreme caution and compliance with medical recommendations.