International Name

Disulfiram (Disulfiram)

Group Affiliation

Alcoholism Treatment Treatment

Dosage form

Tablets, Implant Tablets

pharmachologic effect

Inhibits acetal dehydhydrogenase, participating in ethanol metabolism; Increases the concentration of acetaldehyde, which is ethanol metabolite and causing a number of unpleasant sensations after its use ("tides" of the blood to the skin of the face, nausea, vomiting, a sense of ailment, tachycardia, a decrease in blood pressure). As a result, a conditionally reflex reaction of disgust to taste and the smell of ethanol occurs.

The duration of the oral tablets is 48 hours.

Application in the form of implants creates a constant concentration of the drug in the body. Reactions "Disulfiram-ethanol" may occur within 5-9 months after implantation. In the case of ethanol, lipid mobilization occurs, the vessels are expanding and the blood flow in the place of implantation increases, resulting in the flow of disulfirama into the blood.

Indications

Tablets: Chronic alcoholism (prevention of relapses during treatment). Pills for implantation: chronic alcoholism (treatment); Chronic nickel poisoning (disintellation).

Contraindications

Hypersensitivity, thyrotoxicosis, CSS disease in decompensation stage (incl. Sharply pronounced cardiosclerosis, atherosclerosis of the brain vessels, pre- and post-infarction states, aortic aneurysm, coronary failure, arterial hypertension II-III Art., HSN), pulmonary tuberculosis with hemoprod , bronchial asthma, COPD, expressed emphysema of the lungs, erosive lesions of the mucous membrane of the gastrointestinal tract, ulcerative illness of the stomach and 12-rosewood (in the aggravation stage), bleeding from the gastrointestinal tract, kidney disease, liver failure, diabetes, epilepsy, neuropsychiatric diseases, infectious diseases CNS, polyneuropathy, neuritis auditory and eye nerves, glaucoma, malignant tumors, pregnancy, lactation period. Caution. Age of 60 years old, ulcerative ulcer of the stomach and 12-rosewind (in the remission stage), endarteritic, residual phenomena of brain circulation disorders, psychosis against the background of receiving a disulfirama in an anamnesis.

Side effects

Tablets: "Metal" taste in the mouth, an unpleasant smell (caused by the survo-carbon) in patients with a colostite, hepatitis, polyneuropathy lower extremities, neuropsychiatric disorders, reducing memory, disorientation in time and space, asthenia, headache, skin allergic reactions.

Pills for implantation: suppuration (as a result of friction belt, premature seam removal), the phenomenon of rejection (when the tablets were implanted too close to the cut), allergic dermatitis.

Side effects caused by Association Disulfiram-ethanol: Collapse, arrhythmia, angina, myocardial infarction, brain swelling, hemorrhagic stroke.

Application and dosage

Tablets: Inside, in the morning, an empty stomach, in front of breakfast, at the beginning of treatment, the average dose - 500 mg / day, subsequently, it is gradually reduced to 250-125 mg / day.

P / C and V / M (implantation). After careful disinfection and local anesthesia make a small incision (approximately 6 mm) in the left iliac region, low enough to avoid friction belt. The subcutaneous tissue is pushing and with a trocar are introduced 2 tablets for implantation (100 mg) to a depth of 4 cm. This procedure is repeated 4 times, entering the tablet cruciform around the place of the cut, parallel to the skin surface. The total dose is 800 mg (8 tablets). On the incision impose a seam with a subsequent sterile bandage.

special instructions

Before implantation, a step of gradual oscillating of the patient from ethanol should be conducted.

Polynevropathy arising from the use of the drug disappears when the group's vitamins are prescribed to or remove the implanted tablets.

In the place of implantation, a small tubercle due to fibrosis of the skin and subcutaneous fatty fiber is often formed.

In the case of simultaneous purposes with oral anticoagulants, it is necessary to carry out more frequent control of the protester maintenance and correction of the doses of anticoagulants, which is associated with an increased risk of bleeding.

Interaction

Effects (including neurotoxic) enhance tricyclic antidepressants (amitriptyline), metronidazole, isoniazide; Reduces ascorbic acid (reaction to ethanol).

Increases the concentration in the plasma LS, metabolizing in the liver, due to the inhibition of microsomal oxidation.

Enhances the toxic effects of antiprin, phenytoin, chlordiazepoxide and diazepama by inhibiting their metabolism.

Isoniazide increases the risk of violations of behavior and coordination of movements.

Phenytoin increases the risk of side effects, metronidazole - the risk of developing psyche disorders, the occurrence of nonsense.

Enhances the effect of indirect anticoagulants and increases the risk of bleeding.

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Structure

Active substance: Disulfiram - 500 mg.

Excipients: Polyvidone to 30, sodium carmellosis, magnesium stearate, microcrystalline cellulose, purified water.

Indications for use Esperal

Treatment and prevention of recurrence of chronic alcoholism.
Additionally, the drug is used as a disinfectant with chronic poisoning with nickel.

Contraindications for use Esparl

Heavy liver failure.
- Diabetes.
- Epilepsy and convulsive syndrome of any genesis.
- mental illness.
- Pregnancy.
- Lactation period.
- Increased individual sensitivity to the drug.

Carefully:
- Renal failure.
- hypothyroidism.

Treatment is appointed after a careful examination of the patient and warning about the consequences and complications.

The drug is taken inside 0.5 g 1 time per day in the morning while eating according to an individual scheme, gradually reducing the dose to 1/2 or 1/4 tablets per day.

The dose can be changed in the direction of increasing or decreasing depending on the patient's reaction.

After 7-10 days, a teturamalcoholic sample is carried out (20-30 ml of 40% ethanol (vodka) after receiving 0.5 g of the drug), with a weak reaction, the dose of alcohol is increased by 10-20 ml (maximum dose of vodka 100-120 ml).

The sample is repeated after 1-2 days in the hospital and after 3-5 days outpatient, with the correction of alcohol and / or the drug as needed.

In the future, you can use the maintenance dose of 0.15-0.2 g per day for 1-3 years.

Application Esperal for pregnancy and breastfeeding

Application is contraindicated in pregnancy and breastfeeding.

pharmachologic effect

The disulfirama action is based on the blockade of acetal dehydrogenase, which participates in metabolism ethyl alcohol.

This leads to an increase in the concentration of ethyl alcohol metabolite - acetaldehyde, causing negative sensations (blood stuff to face, nausea, vomiting, tachycardia, decrease arterial pressure etc.), which make an extremely unpleasant use of alcohol after receiving the drug.

This leads to a conditional reflector disgust to taste and smell of alcoholic beverages.

The maximum therapeutic effect is achieved 12 hours after oral administration and can continue within 10-14 days after the cessation of treatment.

Side effects Esperal

Side effects due to disulfram:
- metal taste in the mouth;
- an unpleasant smell (caused by the servo-carbon) in patients with a functioning colostrict;
- rarely - hepatitis (marked both in patients with chronic alcoholism, and in some patients treated for eczema on nickel);
- polyneurite lower extremities;
- neuropsychiatric disorders, reducing memory, disorientation in time and space, asthenia;
- headache;
- skin allergic reactions;

Side effects caused by Association Disulfiram-ethanol:
- collapse, heart rate disorders, angina attacks, myocardial infarction;
- brain swelling, brain hemorrhage.

special instructions

In the case of simultaneous purposes with warfarin or other oral anticoagulants, it is necessary to carry out more frequent control of the protecrin level and correction of the doses of anticoagulants, which is associated with an increased risk of bleeding.

Overdose

The combination of disulfiram - ethanol causes the oppression of consciousness, up to coma, cardiovascular collapse, neurological complications.

Treatment is symptomatic.

Medicinal interaction

Contraindicated combinations:

Alcohol: reaction of intolerance (blood rings, erythema, vomiting, tachycardia). Avoid receiving alcoholic beverages and medicinescontaining alcohol. Unwanted combinations.

Isoniazid: violation of behavior and coordination.

Nitro-5-imidazole (metronidazole, ornidazole, secretion, tinidazole): delicious disorders, confusion of consciousness.

Phenytoin: a significant and rapid rise of phenytoin concentration in blood plasma with toxic symptoms (suppressing its metabolism).

If combinations cannot be avoided, clinical observation and control of the concentrations of the drug in plasma during and after disulfram treatment are carried out.

Combinations requiring caution:

Warfarin (and other oral anticoagulants): an increased effect of oral anticoagulants and the danger of bleeding (decrease in warfarin metabolism in the liver). It is recommended to better control the level of prothrombin in the blood and adjusting the dose of anticoagulants within 8 days after the abolition of the disulfiram.

Teophylline: Disulfiram inhibits theophylline metabolism. As a result of this, the dose of theophylline must be adjusted (reduced dosage), depending on the clinical symptoms and the concentration of the drug in the plasma.

Benzodiazepines: Disulfiram can enhance the sedative effect of benzodiazepines by inhibiting their oxidative metabolism (especially chloridiazepoxide and diazepama). The dosage of benzodiazepine should be adjusted in accordance with clinical manifestations.

Tricyclic antidepressants: Strengthening the reaction of alcohol intolerance (if patients receiving disulfiram, take alcoholic beverages).

Storage conditions

In the place protected from light at a temperature not higher than + 25 ° C. Shelf life - 3 years.

Drug for the treatment of alcohol dependence

Active substance

Disulfiram (Disulfiram)

Release form, composition and packaging

Pills White with cream colors, round, with engraving "Esperal" on one side and cruciform risk to another.

Auxiliary substances: Polyvidone K30, sodium carmellosis, magnesium stearate, microcrystalline cellulose.

20 pcs. - Polypropylene bottles, clamping with a plug with moisture absorber and the control of the first opening (1) - packs cardboard.

pharmachologic effect

Preparation for the treatment of alcoholism. The disulfirama action is based on the blockade of acetal dehydrogenase, which is involved in ethanol metabolism. This leads to an increase in the concentration of ethanol metabolite - acetaldehyde, causing negative sensations (including blood tides to face, nausea, vomiting, tachycardia, decreased blood pressure), which make an extremely unpleasant alcohol consumption after taking the drug. This leads to a conditional reflector disgust to taste and smell of alcoholic beverages.

The maximum therapeutic effect is achieved 12 hours after taking the drug inside and can continue within 10-14 days after the cessation of treatment.

Pharmacokinetics

After oral administration, the absorption of disulfirama from the GTS is from 70 to 90%. It is rapidly metabolized, restoring to a dithiocarbamate, which itself is derived as a glucuron conjugate or converted to diethylamine and carbon sulfide, part of which (4-53%) is excreted through the lungs.

Indications

- Treatment and prevention of recurrence of chronic alcoholism.

Additionally, the drug is used as a disinfectant with chronic poisoning with nickel.

Contraindications

Absolute:

- diabetes;

- epilepsy and convulsive syndrome of any genesis;

- mental illness;

- pregnancy;

- lactation period;

- Increased sensitivity to the components of the drug.

Relative:

- renal failure;

- hypothyroidism.

Dosage

Before starting treatment, the patient should be carefully examined and prevented about the consequences and complications.

The drug is prescribed inside 500 mg 1 time / day in the morning during food according to an individual scheme, gradually reducing the dose to 250 mg (1/2 tablets) or 125 mg (1/4 tablets) in the day. Depending on the patient's reaction, the dose treatment can be increased or decreased.

After 7-10 days, a tetura-alcoholic trial is carried out: 20-30 ml of 40% ethanol (vodka) after taking the drug at a dose of 500 mg; With a weak reaction, the dose of alcohol is increased by 10-20 ml (the maximum dose of vodka is 100-120 ml). The sample is repeated after 1-2 days in the hospital and after 3-5 days outpatient, with the correction of alcohol and / or drug doses, as needed. In the future, the drug can be applied in a supporting dose of 150-200 mg / day for 1-3 years.

Side effects

Conditioned by disulfiram properties:metal taste in the mouth, an unpleasant smell in patients with colostomy (associated with carbon sulfide); Rarely - hepatitis, sometimes occurring in nickel eczema patients who do not suffer from alcoholism, polyneurite the lower extremities, neurrites the optic nerve, reduced memory, confusion of consciousness, asthenia, headaches, skin allergic reactions.

Associated with a combination of disulfiram-ethanol:cases of respiratory failure, collapse, rhythm disorders or acute angina, sometimes myocardial infarction, as well as neurological disorders, brain swelling is described.

Complications with long-term reception:psychoses resembling alcohol, hepatitis, gastritis; In patients with cardiovascular diseases, thrombosis of the vessels of the brain is possible, so with complaints of paresthesia in limbs and face, the drug should be immediately canceled; The aggravation of Polynevrit.

When taking alcohol doses over 50-80 ml (in terms of 40% ethanol) on the background of drug intake, severe violations of cardiovascular and respiratory systems, swelling, convulsions. In this case, it is urgently carried out disinfecting therapy, anagetti is introduced, symptomatic treatment is carried out.

Overdose

Symptoms: The combination of disulfiram-ethanol causes the oppression of consciousness up to coma, cardiovascular collapse, neurological complications.

Treatment:conducting symptomatic therapy.

Medicinal interaction

Combinations are contraindicated

With the simultaneous admission of the drug, espoperal and ethanol develops the reaction of intolerance (blood tales, erythema, vomiting, tachycardia).

With simultaneous use with isoniazid - violation of behavior and coordination.

With simultaneous use with 5-nitroimidazole derivatives (, ornidazole, generidases, tinidazole) develop delicious disorders, confusion of consciousness.

With simultaneous use with phenytio, there is a significant and rapid increase in the concentration of phenytoin in the blood with the development of toxic symptoms (due to the oppression of phenytoin metabolism). If the combinations cannot be avoided, then clinical observation and control of the plasma concentration in the plasma should be carried out during and after treatment with disulfiram.

Combinations requiring caution

With simultaneous use with (and other oral anticoagulants), its effect increases and the risk of bleeding is increased (due to the oppression of warfarin metabolism in the liver). With this combination, more frequent control of the level of prothrombin in the blood is recommended and the dose correction for 8 days after the discontinuation of the disulfiram.

The site provides reference information Exceptionally for familiarization. Diagnosis and treatment of diseases must be under the supervision of a specialist. All drugs have contraindications. Consultation of a specialist is obligatory!

Esperal represents drug Treatmenttreatment alcoholism. EXPERIAL ACTION Based on a violation of the ethyl alcohol nehylic processes in the body, as a result of which the use of alcoholic beverages against the background of the drug causes a person extremely unpleasant sensations (heartbeat, a sharp drop in blood pressure, pain in the heart, redness of the face, etc.). As a result of the appearance under the action of the espache of the negative reaction of the body on alcohol, development occurs negative conditional reflex And there is a disgust for alcohol, thanks to which alcoholism is heal.

Composition, form of issue and name

Currently, only one dosage form Esperal is officially registered on the territory of Russia and entered into the register of drugs - this is pills.

Gel, capsules, injections, suspension, spray and other dosage forms Esperal None in official pharmaceutical reference books of the Russian Federation.

The composition of the Tablets espache as an active substance includes disulfiers in a dosage of 500 mg. The following substances include auxiliary components in tablets:

• Polyvidon K30;
• Sodium carmellosis;
• Microcrystalline cellulose;
• Magnesium stearate.

Esperal tablets have a round shape, painted in white with a cream tint color and equipped with a cross-shaped risk on one side, and engraving "Esperal" - on the other. Produced in packs of 20 pieces.

Therapeutic effect Esperal

Esperal is used to treat alcoholism only if other methods (psychotherapy, etc.) turned out to be ineffective, since the effect of the drug is based on the development of negative conventional reflex in response to the consumption of alcoholic beverages. Negative conventional reflex or alcohol disgust is produced due to the fact that the espache is violates the process of disposal and disposal of ethyl alcohol in the body, causing the accumulation of toxic acetaldehyde, which, in turn, provokes extremely unpleasant, painful symptoms of poisoning, similar to a very strong hangover.

Thus, the essence of the therapeutic effect of any dosage form Esperal is that against the background of the drug the use of alcohol causes extremely unpleasant sensations: redness of the skin, heat in the upper part of the body and in the face of the face, chest compression, breathing, heartbeat, chill , reduction of blood pressure, nausea, vomiting, fear.

The unpleasant sensations arising in response to the use of alcoholic beverages against the background of the use of Esparl are due to the fact that the drug disrupts the neloralization and elimination of ethyl alcohol from the body, causing the accumulation of toxic acetaldehyde. Acetaldehyde is a high-oxidic substance, and therefore its appearance in the body causes disorders of the respiratory, cardiovascular and central nervous system.

The fact is that the ethyl alcohol who fell into the body undergoes a chain of metabolic transformations before fully depends and output. At the same time, the ethyl alcohol turns into acetaldehyde, and then acetaldehyde in acetic acid. Acetic acid itself is a finite product of ethyl alcohol processing and, in turn, turns into acetyl coenzyme-A, spent in a cycle of tricarboxylic acids for energy generation.

And Esperally blocks the work of the enzyme acetaldehydehydrogenase, which is necessary for the conversion of acetaldehyde (acetic aldehyde) into acetic acid. Accordingly, when using the espache, the chain of biochemical reactions to neutoral alcohol neloitizing is disturbed, as a result of which acetaldehyde accumulates in the body, causing extremely unpleasant sensations in a person when drinking alcohol.

When taking inside in the form of tablets Disulfiram is rapidly absorbed into the blood flow from the intestine and the stomach in the amount of 70 - 90% of the entire dosage dosage. After that, the Esparl penetrates the fatty tissue and creates a depot ("stock"), from which slowly and gradually releases, creating a constant concentration of the drug in the blood and, accordingly, a long effect. The first significant clinical effect Esperal appears after 3 to 4 hours after taking the first tablet of the drug, but the maximum severity of the therapeutic effect occurs only after 12 hours. Full tablets Esparl continue to act within 2 days after the reception. But a distinctive feature of the drug is that, due to the deposition in adipose tissue, it blocks the work of acetaldehydehydehydrogenase for about 7 to 14 days after the cessation of taking tablets. This means that after receiving the last dosage, the esteral of its usual action is necessarily maintained for a minimum for 2 days, and for another 1 to 2 weeks there remains a relatively weak therapeutic effect, but is sufficient to create a state of alcohol intolerance.

The concentration of the active component of the espache in the blood does not change with moderately and weakly pronounced diseases of the liver. And in cirrhosis of the liver, on the contrary, the concentration of the drug is higher than in the absence of liver diseases, as a result of which the severity of the therapeutic effects in this category of people is also enhanced.

Esperal is derived from the body, mainly with urine and partly with exhaled air and cartoons.

Disulfiram (existing substance Esparl) and other means for the treatment of alcoholism - video

Indications for use

Tablets for receiving inside with a dosage of 500 mg are shown to use for the treatment of chronic alcoholism, as well as for the prevention of disruptions (swallowing) in the process of alcohol dependence of other methods.

Esperal - instructions for use

Receive Tablets Esperal

Tablets should be taken during meals, drinking enough water (not less than half of the glass). Optimally take tablets in the morning, during breakfast, but if there is no such possibility for some reason, you can drink a medicine at any time in the first half of the day (before lunch). Tablets Esparl can be divided into halves and quarters at risks to take the necessary prescribed dose. All daily dosage should be taken at once in the morning.

Treatment of chronic alcoholism with the help of reception of tablets Esparl is carried out in three stages:

• In the first 7 - 10 days A person takes one tablet espearl (500 mg) one time a day. At this stage, the drug is carried out in order for disulfers to accumulate in fatty depots and it turned out to be in a sufficiently high concentration that can cause reaction to intolerance in response to alcohol use.
• In the second stagewhich usually continues from 7 to 21 days, the espache dosage is reduced to 250 mg (1/2 tablets) per day, and alcohol samples are carried out (the so-called "provocations"). Alcoholic trial is the intentional consumption of a small amount of alcohol against the background of the espache, produced by the doctor's control. The data "provocations" is carried out after 1 - 2 days, if a person lies in the hospital, and after 3 - 5 days, if the patient is at home and comes to the clinic for alcohol samples. A total of 2 - 4 alcohol samples are carried out, the purpose of which is that a person under the control of the doctor felt the course of the reaction of intolerance caused in response to the use of alcohol against the background of the espache. Due to the extremely unpleasant sensations of intolerance reaction in humans, a negative conditional reflex is produced on alcohol consumption or even disgust for alcohol.
• In the third stage Alcoholic samples stop and reduce the dosage of espache to supporting - 125 mg (1/4 tablets) 1 time per day. In this maintenance dosage, the drug is taken up to the moment when a person feel that it completely got rid of alcohol addiction. Taking espache in the maintenance dosage can be continued to 3 years without breaks.

Thus, schematically, the use of Tablets Esperal is as follows - first for 7 to 10 days the drug is taken in the maximum dosage (500 mg per day) for its accumulation in fatty depot and creating a high concentration in the blood. After that, the dosage is reduced half (250 mg per day), and several alcohol samples are carried out, during which disgusts to alcoholic beverages are produced due to the emerging unpleasant sensations (heartbeat, reduction of pressure, leaning of skin, tides, sweating, nausea, vomiting, Fear, etc.). Further, a person is transferred to the reception espache in a supporting dosage - 125 mg (1/4 tablets) one time per day.

In principle, the main therapeutic effect is the second stage - alcoholic samples, during which a person has a disgust to alcohol. After all, the alcoholic test is, in fact, the intentional challenge of unpleasant sensations, the provocation so that a person felt bad after the consumption of alcohol, as a result of which the desire to drink he would have reduced or completely disappeared.

At each stage, the Esparl is accepted in various dosages. So, in the first stage, within 7 - 10 days, the drug takes 500 mg (1 tablet) one time per day. At the second stage, during the period of alcohol samples, the espache is taken 250 mg (1/2 tablets) one time per day. And in the third, final stage, the Esparl is taken in the maintenance dosage - 125 mg (1/4 tablets) for one time per day.

After completion of the first stage, transfers alcohol samples. To do this, on the appointed day of the sample, the person is last adopted 500 mg Esperal (1 tablet), after which after 30 minutes it is given to drink 20 - 30 ml of 40% vodka. Instead of vodka, you can give another alcoholic beverage, but in such a quantity so that the alcohol content in it is the same as in 20-30 ml of vodka. After 30 - 40 minutes after the use of alcohol, the person will develop the reaction of intolerance, and it will feel the whole range of unpleasant sensations (reinforced heartbeat, reduced pressure, redness of the skin, tides, nausea, vomiting, fear, etc.). It is these unpleasant sensations that should develop intolerance and disgust for alcohol. If the reaction to alcohol consumption was weak, then the amount of vodka by 10-20 ml increases to each next sample. However, the amount of vodka for alcohol sample should not exceed 100 - 120 ml.

If a person is in the hospital, then the samples are carried out after 1 - 2 days, and if the patient lives at home and goes to the clinic on "provocations", they produce them after 3 to 4 days. In total, there are usually 2 - 4 "provocations", during which a person experiences the whole range of unpleasant sensations after consuming alcohol and which is enough to develop disgust to alcohol.

After the first alcoholic sample, Esparl begin to take 250 mg (1/2 tablets) for one time per day. In such a dose, the drug is accepted to the last alcohol sample. When all alcoholic samples are spent, the Esparrel begin to take 125 mg (1/4 tablets) for one time per day for the required period of time (maximum 3 years).

Alcoholic samples should be carried out exclusively under the control of the doctor, since it is impossible to predict the severity and severity of the reaction of alcohol intolerance for each particular person. In some cases, the reaction of intolerance takes place very hard and specialized medical care is required, so the person must be under the supervision of the doctor.

If, when conducting an alcoholic sample, a person has a headache with dripping and ripples, the difficulty of breathing, excitement and convulsions, or unpleasant sensations last longer than 1.5 hours, then it is necessary to provide medical care and stop the symptoms of drugs.

In such situations, 15-20 ml of 1% solution of methylene blue, subcutaneously - cordiamine and camphor, and intramuscularly - cytion (or lobeline), ephedrine, strikhin, and additionally inhalation of oxygen is additionally carried out additionally. With a strong headache, an ascorbic acid solution with glucose is additionally introduced, with pills in the heart - the validol, Corvalol or Nitroglycerin tablets are given, with an excessively low arterial pressure (below 70/50) - Mesafant or ephedrine is administered, in the oppression of cardiac activity - stroophantin ( 0.5 ml of 0.05% solution is bred in a physiological solution), during convulsions - 10 ml of 25% magnesia or sybazone, with strong nausea and vomiting - 10 ml of 10% calcium chloride solution and 0.5 ml 0.1% atropine . If, when conducting an alcoholic sample, the person is strongly excited, then 1- 2 ml of 2.5% of the aminezine solution is introduced intramuscularly.

In addition to the described three-step method of use, the espache can also be used by other, simpler methods. So, tablets can be taken without alcohol samples, but only in cases where a person himself wants to get rid of harmful habit. In such situations, the espral is taken within 7 - 10 days at 500 mg (1 tablet) 1 time per day, then for the following 7 - 10 days - 250 mg (1/2 tablets) 1 time per day, and yet 7 - 10 days The drug is drinking 125 mg (1/4 tablets) 1 time per day. The total duration of treatment is 21 - 30 days, during which the attraction is reduced to alcohol, so for a person who independently decided to throw a drink alcohol, this method is optimal. Such a course of treatment can be carried out as needed when a person will feel that the attraction to alcohol appeared again.

Before the start of treatment, Esperal must tell a person about what kind of discomfort he will have when drinking alcohol against the background of taking tablets. It should also be warned to prevent that consumption of more than 150 ml of vodka or other alcoholic beverage in an amount containing equivalent to 150 ml of vodka volume of alcohol will lead to poisoning.

Attention! Since the Esperal causes an unpleasant sensation when drinking alcohol, and also can provoke acute ethyl alcohol poisoning, treatment with this drug can be carried out only with the consent of the patient with alcoholism.

special instructions

Esperal should be used only under the supervision of the doctor and with the consent of the patient himself, as a person should be aware of the possible negative consequences of alcohol consumption against the background of the drug.

Before starting reception, the espearl should not consume alcoholic beverages within 3 - 4 days. If a person was in the feed for a long time, then before the start of use, the Esparl should carry out detoxification, for example, droppers with vitamins, intake of the medigorel, etc.

Since the Esperal can cause damage to the liver (fullentant hepatitis, necrosis, etc.), which are capable of leading liver failure, a coma or even a deadly outcome, then before the use of the drug, liver samples should be made (bilirubin, asat, alosa). Next, it should be regularly determined (once a month) to determine the concentration of bilirubin and transaminase activity (AsaT, Alat). If at least a three-time increase in the activity of Asat and Alat is revealed, then immediately stop the taking espache and observe the doctor until the full normalization of the hepatic samples.

If the Esperal is accepted simultaneously with indirect anticoagulants (warfarin, dicumarine, etc.), then it is necessary in the first 3 to 4 weeks after the start of taking espache and within 2 weeks after its application is completed; at least 1 time per week control MNO and other blood clotting indicators And, in accordance with them, change the dosage of anticoagulants.

With the appearance of a parestheusium (feeling of tingling or running "goosebumps") in the limbs should immediately cancel the taking espache.

If the following symptoms appear, immediately stop taking espache and consult a doctor:

• Nausea;
• Vomiting;
• Stomach pain;
• Jaundice (yellow coloring of the skin and mucous membranes);
• Darkening of urine;

If a person has any of the above symptoms, it is necessary to conduct a survey and find out the liver state, since these features may indicate damage to the authority.

A person should be warmed that if he consumes alcohol against the background of the espache, he will develop intolerance (tides, redness of the face, a rapid heartbeat, a decrease in blood pressure, nausea, vomiting, ailment, fear, etc.). On average, this reaction of intolerance can continue from half an hour to 3 days. If against the background of the taking espache, a person will drink more than 50 - 80 ml of vodka or other alcoholic beverage in an amount equivalent to 50-80 ml of vodka, then he can develop severe disorders of cardiovascular and respiratory systems, swelling and convulsions. Therefore, when using any alcoholic beverages in quantities equivalent to 50-80 ml of vodka or more, a person should be urgently hospitalized into the conditions of the resuscitation compartment for symptomatic therapy.

Reactions of intolerance to alcohol can occur not only when using alcohol, but also when taking medicines or products (for example, kvass, kefir, etc.) containing ethyl alcohol. In addition, the poorly pronounced reaction of intolerance may occur even when using alcohol-containing cosmetics, such as shave lotions, eau de Toilette, perfume, etc. Therefore, a person should warn that at the time of treatment, Esperal will have to refuse not only from the use of alcoholic beverages, but also from the use of any alcohol-containing products, including for outdoor use.

Reactions of intolerance may occur for another two weeks after stopping the espache, which is due to a long period of removal of the drug from fatty depot.

Overdose

Overdose is possible when taking inside the high doses of tablets, and manifests the functioning of the nervous system, such as:

• confusion of consciousness;
• coma;
• convulsions;
• collapse;
• extrapyramidal symptoms (motion disorders - involuntary twitching of various parts of the body, black-shaped manifest movements with fingers, turns of the head and body to the sides, swallowing thrust movements of the limbs, tremor, spasm of half of the face, neck and tongue, etc.).

With the development of symptoms of overdose by Esperal, it is necessary to urgently hospitalize a person to the hospital and conduct symptomatic therapy aimed at maintaining the normal work of vital organs and systems.

Impact on the ability to manage mechanisms

During the entire period of use, the espache, and especially at the initial stages, drowsiness may occur, so the drug negatively affects the ability to manage mechanisms. As a result, on the background of treatment with Esperal, it is recommended to abandon any activities that require high speed reactions and concentrations of attention (for example, driving a car, work behind machines, etc.).

Interaction with other medicines

Esperal cannot be used simultaneously with any medications or cosmetic products containing alcohol, since the entry of ethyl alcohol in the body against the background of the drug is caused by the reaction of intolerance, manifested by blood tides, redness of the skin, headache, nausea, vomiting, rapid heartbeat, flowering blood pressure, confusion Consciousness. The reaction of the intolerance of alcohol Against the background of esperial intake weakened by the reception of diazepam, ascorbic acid and antihistamine preparations (for example, suprastine, telfast, erotic, claritine, zetrin, cetirizin, etc.). Accordingly, these drugs can be taken to reduce the severity of unpleasant sensations arising from the use of alcohol against the background of the espache.

Unwanted combination Esperal with the following medicines:

• Isoniazid. High risk Violations of coordination of movements and behavior (depression), as well as the appearance of dizziness.
• Imidazole derivatives (metronidazole, ornidazole, secretion, tinidazole). The high risk of confusion of the consciousness, the development of psychosis or delirium ("white hot").
• Phenitoin. With simultaneous use with espache, the concentration of phenytoin in the blood is sharply increased, which leads to the development of the toxic effects of the latter. Therefore, if necessary, the combined application of these drugs should control the concentration of phenytoin in the blood, adjusting it to the dosage.
• Hepatotoxic preparations (for example, azatioprine, azithromycin, aztreon, almopurinol, amiodorone, amphotylin, amoxiclav, ampicillin, amphotericin, aspirin, androgens, bikefen, bispetol, valproic acid, verapamil, vincristine, galotan, glucocorticoid, griseofullvin, josamamicin, diazepam, diltiazem , diclofenac, doxycycline, doxirubicin, Zidovudine, Ibuprofen, Isoniazid, captopril, carbamazepine, ketoconazole, ketoprofen, Clarithromycin, Clindamycin, Levofloxacin, lincomycin, Losartan, Chloramphenicol, methyldopa, methotrexate, methacycline, Metronidazole, Moxifloxacin, naproxen, Nicotinic acid, Nifedipine, nonsteroidal antiinflammatory drugs (NSAIDs), Oxacillin, omeprazole, oral contraceptives, penicillin antibiotics, paracetamol, pefloxacin, Ranitidine, Rifampin, Roxithromycin, salicylates, sulfonamides, terbinafine, tetracycline, tricyclic antidepressants, Fluconazole, ftivazid, quinidine, Chlorpromazine, Cefazolin, Cefoperazone, Cefotaxim, ceftazidim, ceftriaxone, cefuroxime, cyclosporine, cyclophosphamide, cimetidine, enalapril, erythromycin, estrogens, etc.). The combination of espache with hepatotoxic drugs sharply increases the risk of damage to the liver with the development of hepatitis.

Esperal in combination with the following drugs can be taken only in compliance with caution and, if necessary:

• Indirect anticoagulants (warfarin, dicumarine, etc.). Esparl enhances the therapeutic effect of anticoagulants, so when they are combined, the risk of bleeding increases, as a result of which the need arises to control blood clotting and adjust the dosage of anticoagulants.
• Teophylline. Esperal Reduces the impact rate of theophylline from the body, as a result of which its concentration in the blood is sharply increasing. Therefore, the combined application of these drugs requires regular determination of the concentration of theophylline in the blood and reduce its dosage.
• Benzodiazepines (phenazepam, diazepam, etc.). Esparl enhances the sedative effect of benzodiazepines (dizziness appears, inhibition), as a result of which, with their combined application, it is necessary to reduce the dosage of the latter in accordance with clinical manifestations. Sometimes benzodiazepines reduce the severity of the reaction of the intolerance to alcohol caused by an espass.
• Tricyclic antidepressants (amitriptyline, imipramine, etc.). With the simultaneous use of espache and antidepressants, the severity of the reaction of intolerance to alcohol occurs. As a result, the use of alcohol causes extremely unpleasant sensations lasting.
• Tricyclic antidepressants, phenytoin and Mao inhibitors (IProniazide, SELEGILIN, etc.). When combining these drugs with espral, the risk of developing side effects of all accepted drugs increases.
• Rifampicin, caffeine, fenasone, chloro-massazone. Esperal slows down the derivation of these drugs, as a result, it may be necessary to reduce their dosage.
• Timazide. Combined use leads to an increase in the severity of organic brain syndrome.
• Chlorpromazine. When combined with espearn increases the risk of a sharp decrease in blood pressure.

Esperal validity period

Tablets for receiving inside Esperal Start across an hour after reception, but the maximum effect develops after 12 hours. After taking the last tablet, the Esparrel continues 1 more than 1 week, after which the effect of intolerance to alcohol completely disappears.

After how many days after the use of alcohol, you can take an espache?

Esparrel can be started to take a minimum of 24 hours (one day) after the latest dose of alcohol. However, it is optimal to start taking an espache after three days after the use of the last dose of alcoholic beverages.

Take a drug earlier than 24 hours after consumption of alcohol - it is impossible, because during this period of time, alcohol that fell into the body is neutralized and is displayed. If during this period, start taking an espache, then the drug will cause an unpleasant feeling, as if the person drank after the use of tablets.

Antidote Esperal

Unfortunately, the antidote capable of neutralizing the action or remove the espache from the body does not exist. A variety of drugs (ascorbic acid, iron preparations, etc.), which are trying to apply to the accelerated output or neutralization of the espache, are actually ineffective. The drug will act all the required time, that is, within 1 - 2 weeks after receiving the last dose. It will not be possible to remove the espache from the body before, as the drug accumulates in the subcutaneous fat layer, from where small doses enters the bloodstream.

It is common to consider the narcologist for the "decoding" so that it makes the injection, neutralizing the effect of the drug, is no more than the myth. Doctors, narcologists do not speak to suffering alcoholism, that the antidote does not exist, since a person who wants to drink is very aggressive and often does not want to objectively perceive the information, but simply requires that he can be given. In such a situation, narcologists are introduced vitamins under the guise of "antidote".

The only substance that can be considered as a conditional antidote Esparl is 1% Methylene Blue solution. This drug allows you to eliminate the unpleasant sensations arising from the use of alcohol against the background of the treatment of Espar. That is, if the period of validity of the drug has not yet ended, and the person drank and feels very bad, then the intravenous introduction of a 1% solution of methylene blue will help to save this condition and relieve unpleasant sensations. However, methylene blue only stops symptoms of alcohol poisoning, but does not remove the espache from the body and does not reduce its validity.

In addition, the severity of the unpleasant sensations arising from the use of alcohol against the background of the expiral term can be reduced by adopting ascorbic acid, diazepams or any antihistamine drug (for example,

As well as additional ingredients: polyvidon K30. , magnesium Stearat , carmellosis sodium , microcrystalline cellulose .

Form release

The drug is produced by B. tabletswhich have a round shape, white color with a cream tint. On one side of the tablet - cruciform risk, on the other - engraving " Esperal.". Tablets are packed in polypropylene bottles with a plug of 20 pieces. The bottle is packed in a cardboard pack.

Also medicine Esperal is produced in the form of a special gelwhich is used to carry out implantation under the skin.

pharmachologic effect

Pills and gel Esperal Used for treatment alcoholism . Active substance disoulphyram. It acts, providing blockade of acetal dehydrogenase, participating in ethanol metabolism. As a result, concentration increases in the body acetaldehyde , ethanol metabolite. It provokes a manifestation of negative sensations (, reduced pressure, nausea , vomot and etc.). Consequently, the intake of alcohol becomes a source of extremely negative sensations. As a result, the conditionally reflex disgust for the smell and taste of alcohol is produced.

The greatest therapeutic effect is marked 12 hours after the use of tablets. The effect of the drug can persist for 10-14 days after the treatment has been discontinued.

Esperal Implanta makes it possible to maintain a permanent level in the human body disulfiram . It is important to comply with the following condition: Before implantation, a person should not take alcoholic beverages for several days.

Pharmacodynamics and pharmacokinetics

The effect of disulfirama is based on the blockade of acetaldehydehydehydrogenase, participating in ethyl alcohol metabolism.

After receiving orally, from 70 to 90% of the disulfiram is absorbed. Next, the rapid process of metabolism is noted, the substance is restored to dithiocarbamata which is either excreted from the body in the form glucuron conjugate or turns into diethylamine and carbon sulfide. The latter is partially excreted through the lungs of a person (from 4 to 53%).

Indications for use

The drug applies according to the following testimony:

• prevention and therapy of the recurrence of chronic ;
• as an additional disinfectant poisoning nickel which has chronic character.

Contraindications

• heavy form liver failure ;
• and causes any origin;
• mental diseases ;
• pregnancy and lactation;
• pronounced sensitivity to the constituent drug.

Relative contraindications are:

• renal failure .

Side effects

Before starting treatment with this drug, a person must clearly realize what it is, and what side effects can manifest in the treatment process.

Side effectsthat manifest themselves due to properties disulfiram : Feelings of the metal taste in the mouth, manifestation of unpleasant odor in people with colthomy . In rare cases can develop neurry optic nerve , hepatitis , polyneurite lower extremities , worsening memory, manifestation, headaches, asthenia , Allergies on the skin.

Side effects that manifest themselves due to the combination of disulfirama with ethanol: manifestation of respiratory failure, collapse, neurological disorders, heart rhythm disorders, motor's swelling .

With prolonged treatment, the means may be marked: psychosians similar to alcohol, hepatitis Exacerbation polynevrit. . In people who suffer from cardiovascular diseases can develop brain vessel thrombosis . With paresthesia in the face and limbs, you need to immediately cancel the tool.

If a dose of alcohol has been adopted on the background of the drug, exceeding 50-80 ml (recalculating with 40% ethanol), manifestation heavy violations in the functions of respiratory and cardiovascular systems, cramps, swelling. In this case, immediate disinfect treatment is carried out.

Instructions for the use of esperial (method and dosage)

Before the therapy begin, the patient must pass a thorough examination. In addition, it should clearly understand how the drug acts, and what consequences and complications can manifest itself in the process of its reception.

The instruction on the espache is as follows: Tablets are accepted inside 500 mg. Reception is carried out once, in the morning, during meals. Instructions for use Esperal Provides a gradual decrease in the dose of the drug to 250 mg or up to 125 mg per day. How to take a tool and adjust the dose, the doctor will tell more in more detail.

After the start of treatment, an alcoholic trial is carried out after 7-10 days: 20-30 ml of 40% ethanol is taken after the use of 500 mg espache. If the reaction is weak, then the dose of alcohol increases. In this case, the maximum dose can be 100-120 ml of 40% alcohol. Next, one more sample is carried out in the hospital after 1-2 days and outpatiently after 3-5 days. Later, the drug is used in the daily supporting dose of 150-200 mg for 1-3 years.

Stitching implants it is carried out into the tissue of the muscles for four centimeters deep into. As a rule, the stitch is carried out in top Buttocks or in the left iliac area. It is initially carried out disinfection and anesthesia, then an incision is made of approximately 6 mm. The subcutaneous fiber is moved by a special tool, after which the drug is injected. Total patient introduces 0.8 g of drug. After the implantation is completed, seams and bandage is superimposed. After launching, Esparl can act from six months to five years. Coding continues depending on the dose that was applied.

Overdose

In overdose (combination disulfiram-ethanol ) possibly depression of consciousness , cardiovascular Collapse , complications of a neurological nature. In this case, symptomatic treatment is carried out.

Interaction

Reception of means with alcohol is contraindicated, since in this case the reaction of intolerance occurs.

It is undesirable to combine Espar C, as it is possible to violate behavior and coordination.

With the simultaneous use of funds with 5-nitro-imidazoles probably development deliosis disorders .

With simultaneous reception with Phenytio A rapid increase in plasma concentration in plasma, toxic symptoms can be noted.

With caution with the preparation apply the following drugs:

• Teophylline Since disulfiram inhibits its metabolism. Therefore, the dose of theophylline needs to be corrected.
• and a number of other oral anticoagulants. There is a danger of bleeding, since the effectiveness of oral anticoagulants increases. It should be regularly monitored by the level of prolromine in the blood and adjust the dosage of anticoagulants for eight days after the abolition of the disulfiram.
• Benzodiazepines Since disulfiram increases the level of sedative effects of benzodiazepines, inhibiting their oxidative metabolism.
• Tricyclic antidepressants In the treatment of disulfiram, the intolerance to alcohol significantly increases.

Terms of sale

Recommended by a doctor's prescription.

Storage conditions

The remedy needs to be protected from the access of children, stored in dry places. The air temperature should not be above 25 ° C.

Shelf life

Store Esparl can be 3 years old.

special instructions

During the time, while a person takes an espache tablets, you can not take alcoholic beverages, as well as take any LS, which contains alcohol.

If the patient uses the gel espearl, tablets from alcoholism, the reaction of its body to simultaneously receiving alcohol can be both fast and stopped. In the latter case, development is possible toxic hepatitis At which kidneys, liver, pancreas are affected.

Analogs of Esperal

Coincidences on the ATX 4 level code:

Analogs of the drug for the main operating component are drugs Torpedo , , Disoulphyram. , Tetlong-250. . It is advisable to apply analogs, it is necessary to recognize the doctor.

What is better: Esperal or Esperal Gel?

What form of the drug it is advisable to choose, depends on the preferences of the patient. If the tablets need to be used according to the scheme, the gel stuff provides a persistent effect without the need for further reception of the means. Nevertheless, it should be noted that the subcutaneous esperial injection provides a constant high concentration of disulfiram in the body. Therefore, inxication is possible when drinking alcohol.

To eliminate the drug from the body, neutralization should be carried out, for this purpose, antidote is used.

Children

Not used for the treatment of children.

With alcohol

If simultaneously take espache and alcohol, the consequences can be very serious. There is a pronounced reaction of intolerance with parallel reception of alcohol. Alcohol should be completely eliminated, as well as drugs containing alcohol.

During pregnancy

Contraindicated with esperial treatment during pregnancy and breast feeding.