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If a person is thin, where does disulfiram accumulate. Disulfiram: analogues and special instructions. Pharmacological group of the substance Disulfiram

Disulfiram is used to treat alcohol addiction. This radical method allows you to develop persistent disgust to strong drinks and erects an insurmountable barrier between the drinker and the alcoholic. The patient, receiving a break from addiction, has time to change his life guidelines and return to normal life.

The principle of action of disulfiram

pharmachologic effect The drug disulfiram is based on the suppression of the enzyme acetaldehyde dehydrogenase, produced in the liver to slow down the metabolism of acetaldehyde. This process stops the breakdown of alcohol and removes it in the form of carbon dioxide and water. If you drink an intoxicating drink, acetaldehyde with the participation of disulfiram will accumulate in the body. As a result there will be acute poisoning which will be accompanied by nausea, vomiting, tachycardia, fear of death, swelling of the face, headache, feeling of heat, throbbing in the temples, shortness of breath. This state is called the disulfiram-ethanol reaction.

The alcoholic experiences painful condition that there is a conditioned reflex development of not only an aversion to intoxicating drinks, but even the smell of alcohol becomes painfully unbearable. To consolidate the effect, the patient is given to drink a small amount of alcohol.

Drug coding for alcoholism is effect based.

Methods of introducing disulfiram into the patient's body

Disulfiram therapy is divided according to the method of drug administration.

Pills

T oral tablets are prescribed for the treatment of alcoholism and relapse of drunkenness. The drug is usually taken on an empty stomach in the morning. The initial portion of 500 mg / day, over time there is a significant dose reduction.

Implantation tablets

Implantation tablets are used to code alcohol dependence and nickel intoxication.

When implanting with disulfiram, all precautions accompanying the operation must be observed. Produced local anesthesia. An incision is made in the left iliac region and the tissue is pulled apart. Implantation tablets are administered in portions of 2 pieces, and the procedure is repeated 4 times. Then the incision with the tablets is sutured and a bandage is applied. After using implantation tablets, disulfiram penetrates into the blood. The drug is metabolized and transformed.

Intravenous disulfiram injections

An injection of the drug disulfiram intravenously will quickly deliver medicinal substance into the blood, but the maximum inhibitory effect on acetaldehyde dehydrogenase becomes noticeable only after a few days. Therapeutic effect The drug persists for about 14 days after cessation of therapy.

An intravenous injection of the drug disulfiram promotes the dissolution of the drug in lipids and its distribution in the body, followed by concentration in adipose tissue. When injected intravenously, the metabolism does not undergo significant changes with moderate liver damage, but with liver cirrhosis, the number of metabolites in the blood increases. The breakdown products of the drug are excreted through urine and air. The unchanged portion of disulfiram is eliminated by the intestines. The pharmacological effect of the drug administered intravenously is similar to the effect of disulfiram, which enters the body by other means.

Disulfiram injections intramuscularly

Disulfiram gel - form medicinal substance retarding action for intramuscular use. Disulfiram is administered by syringe and does not require special conditions for its implementation. As a result of injection, an infiltrate of a substance consisting of microcrystals enters the body, which promotes slow absorption active substance drug. When drinking alcoholic beverages, a disulfiram-ethanol reaction occurs. Vomiting, nausea occurs, blood pressure drops, and other reactions occur that are difficult for the body to tolerate. With this type of therapy, all substances, both medicinal and food containing alcohol, are prohibited. If alcohol enters the body by mistake, induce vomiting and seek medical help.

Contraindications

Contraindications for disulfiram are: long list diseases, which include:

  • hypersensitivity to the active substance of the drug;
  • pathology of cardio-vascular system during the period of exacerbation, when the body is no longer able to cope with the disease on its own;
  • pathologies of the hearing organs in severe form;
  • pathologies of the visual organs in severe cases;
  • diabetes,
  • lung pathologies in the form of hemoptysis or asthma;
  • ulcerative pathologies of the gastrointestinal tract;
  • renal and liver failure;
  • pathologies of a neuropsychic nature;
  • epilepsy and convulsions.

Also, contraindications to the drug disulfiram include pregnancy and lactation.

You should be especially careful with the drug disulfiram if the patient is over 60 years old or has uncontrolled psychosis while taking the drug.

Disulfiram analogues form a large group medicines. It includes the following drugs: abrifid, aversan, antabuse, antiethane, disethyl, crotenal, lidevin, radotera, refusal, teturam, exorran, esperal and others.

Side effects

During therapy with the drug disulfiram, there are side effects. Patients undergoing therapy note the appearance of a metallic taste, sometimes bad smell, associated with carbon sulfide. While taking the drug disulfiram, chronic diseases may worsen and psychosis resembling alcoholism may occur. During implantation, side effects may occur in the form of suture dehiscence or pill rejection.

If alarming symptoms appear, you should immediately contact ambulance, since in acute cases the side effects will greatly upset your health, even leading to coma.

Neutralization of disulfiram

Disulfiram is administered to induce a persistent aversion to alcohol for a long period of time. If the patient decides to interrupt the alcohol-free period, he comes to medical institution to interrupt encoding. Most often this happens if the alcoholic began treatment under the influence of his family or employer.

In this case, the patient is given a neutralizing antidote, which reduces the therapy to zero. Repeated treatment disulfiram will occur with reduced efficacy.

It is worth noting that the antidote of the drug disulfiram does not lead to a complete return of the patient to the original state. The patient continues to experience the effect of the encoding. A hangover is exceptionally difficult and painful.

An antidote is also injected into emergency situations, when the patient could not tolerate alcoholic abstinence and, despite the therapeutic prohibition, drank alcohol. It is possible that alcohol enters the body by mistake, for example, with medical preparations. In this case, you need to contact a narcologist, who will be forced to administer the antidote of the drug disulfiram to relieve the body’s violent reaction to alcohol.

In order to avoid having to use an antidote, it is advisable to support treatment with disulfiram by undergoing a psychotherapeutic program. Mild forms of addiction can be overcome with the help of a psychologist or herbal therapy.

The problem of alcoholism has long acquired global proportions. According to Rospotrebnadzor, only in our country for 2016 chronic alcoholics More than 5 million people are recognized (6% of them are teenagers). The Ministry of Health publishes mortality data annually. According to these statistics, every year in Russia about 500,000 people die due to prolonged drunkenness.

Such sad figures are growing. The fight against alcoholism is being carried out in all directions and is bearing fruit. Many addicts recognize the problem and begin treatment. IN complex therapy For alcohol addiction, the drug Disulfiram is successfully used, the instructions for use of which confirm the purpose of the drug. So how exactly does it work and how does it help?

Disulfiram - known remedy, used to treat alcohol addiction

Main active substance, which is part of the product, is disulfiram. This substance, when it enters the body of a person suffering from alcohol addiction, begins to actively destroy ethanol. Simultaneously provoking the development of an acute reaction toxic type in response to subsequent alcohol intake.

An alcoholic develops a stable reflex - an aversion to any type of alcoholic beverages. A person hardly begins to endure their smell and even appearance.

Disulfiram is available as an oily solution and tablets. The composition of the pills varies and depends on the method of further use of the drug.

Symptoms that occur during treatment with Disulfiram and simultaneous drinking of alcohol resemble poisoning

For implantation:

  • disulfiram: 0.1 g;
  • auxiliary ingredients: PEG-600, lures and sodium chloride.

For oral (internal) use:

  • disulfiram: 250 mg or 500 mg;
  • additional components: MCC, calcium diphosphate, polyoxyl 40 sterate, stearic acid, hydroxypropylcellulose, sodium starch.

How the drug works

To understand what Disulfiram is, you should study in detail how exactly it works. So, as soon as the agent enters the interior, the following reactions are noted:

  1. The drug begins to inhibit (reduce the rate of chemical reactions) one of the liver enzymes (acetaldehyde dehydrogenase). This enzyme is produced by the liver large quantities for oxidation and neutralization of decomposition products ethyl alcohol.
  2. Due to inhibition of the production of this enzyme, the processing of ethanol into acetaldehyde, which begins to accumulate in the body, also stops.
  3. Large accumulations of this compound provoke the development of toxic poisoning.

What does a person feel

The clinical picture after using Disulfiram manifests itself in a number of unpleasant symptoms. All sensations experienced by a person are similar to those that occur during deep poisoning of the body:

  • dizziness;
  • general weakness;
  • severe nausea;
  • a sharp drop in pressure;
  • development of the gag reflex.

Disulfiram is absorbed quite quickly and completely (75-90%) from the gastrointestinal tract. There, the drug, after intensive metabolism, is excreted from the body through the urinary system. Some of the residue (converted to carbon disulfide) leaves the body through the lungs (by breathing).

Alcoholism is a global problem

Indications for use

This tool has been successfully used for complex treatment alcohol addiction at any stage and prevention of relapse of chronic alcohol addiction. The medicine is also used to treat chronic nickel poisoning.

Disulfiram: instructions for use, reviews, price

Treatment with this remedy is carried out only after a complete examination of the person. The patient also receives a warning about possible consequences after taking the drug and complications.

Disulfiram is used in therapy in two ways: orally (in pill form) and by transplantation (intramuscular and subcutaneous).

The dose of the drug for the use of tablet form of medication is calculated individually. On average, it is 0.25-0.5 g daily. By implantation, 8-10 pills are sewn into the patient. The drug has its own characteristics of its use. These are the following details:

  • re-implantation of the drug is carried out only after 8 months from the first transplantation;
  • At the site of injection of the product under the skin, a small infiltrate (small compaction) may form, this normal reaction organism.

Side effects

If you decide to use the drug Disulfiram, the side effects that may follow after coding should not scare you. All not entirely pleasant sensations are associated with the action of disulfiram. They are as follows:

Often:

  1. Sensation of metallic taste in the mouth.
  2. In the presence of a colostomy, the patient may develop an unpleasant odor. This is due to the formation of carbon disulfide during the disintegration of disulfiram.

Sometimes:

  1. Confusion.
  2. Short-term memory loss.
  3. General weakness and exhaustion (anemia).
  4. Allergies in the form of itching and skin rashes.
  5. Neuritis nerve endings visual organ(inflammation of fibers optic nerve).
  6. Polyneuritis (nerve damage) lower limbs. In this case, the person experiences certain difficulties with movement.

Side effects during long-term use:

  1. Development of gastritis.
  2. The appearance of hepatitis.
  3. Exacerbation of polyneuritis.
  4. In the presence of heart disease, thrombosis is possible cerebral vessels.
  5. In rare cases, the appearance of psychosis (similar to alcoholism) is noted.

Consequences of drinking alcohol during treatment

If, despite all the doctor’s warnings, a patient undergoing therapy with Disulfiram nevertheless takes a risk and continues to drink alcohol, he will have to face a lot of unpleasant consequences. These may be the following reactions:

  • convulsions;
  • cerebral edema;
  • angina pectoris;
  • development of coma;
  • heart collapse;
  • loss of consciousness;
  • heart attack conditions;
  • respiratory failure;
  • neurological disorders;
  • violations heart rate(arrhythmia, tachycardia).

If the dosage of the drug is exceeded, the patient may experience life-threatening neurological disorders, coma and collapse. In these cases, the drug is discontinued, and the person is placed in a hospital, where he undergoes treatment aimed at complete detoxification of the body.

Disulfiram successfully helps in the treatment of alcoholism of all types

Patient reviews

If you carefully study all the opinions received during the therapy process, you will notice a tendency towards questions related to the secret use of the drug. Usually the relatives and friends of a person suffering from alcoholism are interested in this. This drug is actually popular and has already helped many people get rid of deadly addiction.

As for “secret” use, doctors categorically do not recommend self-medication. After all, the patient, not warned about the appearance dangerous consequences Due to further consumption of alcohol, it can aggravate its situation and sharply worsen the situation.

According to narcologists, treatment with Disulfiram should be carried out only after a conversation with the patient and warning him about possible complications.

Encoding with the drug Disulfiram can bring real benefit only after a certain psychological mood of the patient. And this therapy should always be carried out meaningfully and consciously.

Where to buy the remedy

Disulfiram is sold in most major pharmacy points. But to purchase it you must have a doctor's prescription. This drug is not intended for free sale. The price of the product depends on the manufacturer. On average, it is:

  1. For oral administration(inside): 150–1,000 rubles.
  2. Implantation varieties of the drug: 550–2,500 rubles.

When should disulfiram not be used?

Like every drug this medicine has a lot of its own contraindications. This list is quite long and includes the following:

  • oncology;
  • epilepsy;
  • polyneuritis;
  • kidney pathologies;
  • emphysema;
  • diabetes;
  • bronchial asthma;
  • ulcers in the acute stage;
  • convulsive syndromes;
  • pathology of the hearing organs;
  • mental disorders;
  • liver failure;
  • tuberculosis in the stage of hemoptysis;
  • eye diseases (glaucoma, neuritis);
  • diseases of the hematopoietic organs;
  • pregnancy and lactation period;
  • hypersensitivity to disulfiram;
  • thyrotoxicosis ( pathological condition, formed against the background of excessive production of hormones by the thyroid gland);
  • diseases of the cardiovascular system (cardiosclerosis, aortic aneurysm, arterial hypertension, atherosclerosis, infarction conditions, coronary insufficiency, heart failure).

Particular care should be taken when treating with Disulfiram for ulcerative pathologies in the remission stage, cardiovascular problems in the compensation phase. Also, doctors may not prescribe Disulfiram if the patient has already had psychosis, endarteritis and problems with cerebral circulation. The age of the person also influences – in persons over 60 years old this type therapy may not be carried out.

Interaction with other drugs

Disulfiram is a rather aggressive drug. When treating with this drug, the person's condition should be carefully monitored. You should also know that this substance does not interact with a number of other medications. What medications should not be taken during treatment are described in the following table:

Drug + Disulfiram Consequences of interaction
Anticoagulants (Warfarin) internal bleeding, increased effect of the drug
Buspirone the appearance of manic states
Amitriptyline, Isoniazid, Clozapine toxic damage to the nervous system
Chlordiazepoxide severe dizziness
Mzoniazid confusion, development of depression
Metronidazole, Omeprazole, Buspirone, Perphenazine, Fluoxetine, Sertraline, Guanfacine acute psychosis and various disorders in the work of the central nervous system
Caffeine overexcitement
Omeaprazole loss of consciousness
Chlorpromazine arterial hypotension (pressure drop)
ascorbic acid, diazepam decrease in the action of disulfiram
sedatives, sleeping pills, barbiturates severe lethargy
Rifampicin, Caffeine, Imipramine, Desipramine, Chlorzoxazone a significant decrease in the excretion of these drug residues from the body
Temazepam, Phenytoin increased drug toxicity
Cephalosporins disulfiram-like reaction (symptoms of acute toxic poisoning)
Etinamat a significant increase in activity and action this tool which can create a life-threatening situation
Chlorpromazine severe pressure drop

Disulfiram should be stored at temperature conditions up to +25⁰ C in places inaccessible to animals and children. The shelf life of the drug is 5 years (for tablet form) and 2 years for oil solutions and products intended for implantation.

There is no medicine called Disulfiram depot. In pharmacology, the substance disulfiram is used, which is part of several medications produced under different trade names. All of them are used for treatment chronic alcoholism. Including the drug of the same name Disulfiram.

Disulfiram-based drugs are available in different forms:

  • Tablets for oral administration.
  • The tablets are soluble.
  • Tablets for implantation.
  • Powder.

Various shapes suggest different ways taking medication. In this sense, the word “depot” indicates the introduction into the body of a certain amount of disulfiram, which will gradually diffuse into the blood and exert its effect regardless of the desire and will of the person.

Disulfiram is deposited or stored in the body. Used for depositing special tablets for implantation Disulfiram produced by the Polish pharmaceutical company Warsaw Pharmaceutical Works Polfa.

Pharmacological action of the drug

The pharmacological action of disulfiram is based on slowing down the metabolism of ethyl alcohol. Sometimes this slowdown is conventionally called a stop, which is not entirely factually true, however, due to the fact that the rate of breakdown of alcohol at one of its stages drops significantly, the result of the slowdown for the body is almost equal to its complete stop.

In the normal state, alcohol entering the body causes a pleasant state of intoxication, which slowly turns into unpleasant condition hangover. The degree of pleasantness and unpleasantness for each person is individual, both in dynamics and duration, and is determined by the activity of special enzymes.

Realizing that the body is horrible toxic substance– ethyl alcohol, the protective system triggers the splitting mechanism at its disposal. A reaction occurs as a result of which alcohol turns into acetaldehyde, which is also a poison, but, unlike alcohol, does not bring any pleasure.

To destroy acetaldehyde, the protective system triggers a corresponding chemical reaction. However, this reaction is natural conditions goes much slower than the first. As a result, acetaldehyde accumulates, the toxic effect of which is felt by a person as a “hangover”. Moreover, the more you drink, the more aldehyde accumulates, the stronger the hangover symptoms.

Disulfiram deposited in the body slows down the second reaction, which leads to an explosive increase in the level of acetaldehyde. Anyone who drinks 10-40 ml of vodka receives a complex of unpleasant symptoms:

  • Tremor, weakness, redness of the skin.
  • Headache, throbbing in the head, dizziness.
  • Decreased blood pressure, arrhythmia.
  • Shortness of breath, nausea, vomiting.

So in a simple way An alcoholic develops a conditioned reflexive negative reaction to the taste, smell and intoxicating effect of alcohol.

The effect of disulfiram is absolute: it cannot be reduced or changed. Over time, the alcoholic develops an aversion to alcohol and a fear of dying from drinking it.

Indications and contraindications for use

Disulfiram is indicated for the treatment of chronic alcoholism and relapse prevention.

Implantation of Disulfiram is contraindicated in a significant number of cases, namely:

  • Individual oversensitivity to disulfiram.
  • Disorders of the thyroid gland.
  • Cardiovascular diseases.
  • Neurological diseases.
  • Diabetes.
  • Diseases respiratory systems s.
  • Peptic ulcer disease.
  • Liver and kidney failure.
  • Diseases of the hematopoietic organs.
  • Cancerous tumors.
  • Mental illnesses, epilepsy.
  • Convulsive syndrome.
  • Pregnancy and lactation period.

Dosage

The amount of deposited disulfiram should be selected by the doctor individually. This requires disulfiram-alcohol testing.

The manufacturer indicates the average dosages:

  • For intramuscular implantation – 5 tablets per 1 year of deposit, 10 tablets per 2 years.
  • For subcutaneous implantation – 8-10 tablets. Subcutaneous implantation requires repeating after 8 months.

Implantation should be carried out only in a sterile hospital environment. The method of spatial placement of the tablets inside is important: only a qualified doctor can do it correctly.

Side effects

Disulfiram causes a metallic taste in the mouth. Other side effects are associated with individual response, as well as the duration of therapy. It could be:

  • Low pressure.
  • Increased thrombus formation.
  • Headache.
  • Hepatitis, gastritis.
  • Neurological disorders: neuritis, polyneuritis.
  • Confusion, asthenia, psychosis.
  • Skin allergic reactions.

Caution when using the drug

The radical and uncontested reaction that is caused by disulfiram when taking alcohol requires that the patient be informed about the consequences of even small doses of alcohol.

Acetaldehyde is an aggressive substance. Even small amounts of it cause poisoning. The amount of acetaldehyde that is formed in the body when taking more than 50 ml of vodka causes serious somatic disorders of all body systems, including:

  • Arrhythmia, tachycardia, angina pectoris.
  • Respiratory failure.
  • Neurological disorders.
  • Depression and loss of consciousness.

Please note that medications and food products containing ethyl alcohol will also cause the symptoms described above. In its extreme manifestations, acetaldehyde poisoning can lead to such serious disorders as:

  • Heart attack.
  • Swelling of various parts of the body and organs, including the brain.
  • Cramps.
  • Coma.

Alcohol consumption by a person with chronic diseases may be fatal.

Deposited disulfiram is effective for a long time. Depending on the method and amount of implanted dose, the alcohol intolerance reaction can last up to two to three years. Once the deposited disulfiram is used up, there is a possibility of relapse into alcoholism. The probability begins to increase rapidly over time.

At its core, disulfiram therapy is an external limiting factor that allows you to keep your drinking habit under control. But alcohol addiction has a psychological cause.

Therefore, when implanting disulfiram, psychotherapeutic influence is required in order to change the motivation system of the dependent person. These may be individual visits to a psychotherapist or group sessions.

Consequences of overdose

An overdose of disulfiram can lead to:

  • Falling into a comatose state.
  • collapse critical systems organism.
  • The appearance of neurological disorders.

The consequences of an overdose are treated according to the symptoms manifested.

Interaction with other drugs

Disulfiram interacts with other drugs. The following are prescribed and used with caution:

  • Isoniazid: may impair motor function and behavior.
  • Imidazoles: may cause delirium and clouding of consciousness.
  • Phenytoin: a sharp rise in phenytoin levels, accompanied by symptoms of poisoning.
  • Anticoagulants: the anticoagulation effect increases, a significant deterioration in blood clotting - the risk of bleeding.
  • Theophylline and benzodiazepines: Metabolism slows down, which requires a reduction in the dose of drugs.
  • Tricyclic antidepressants: increase alcohol intolerance.

A person with a disulfiram implant should make doctors aware of this fact when seeking medical help.


Gross formula

C 10 H 20 N 2 S 4

Pharmacological group of the substance Disulfiram

Nosological classification (ICD-10)

CAS code

97-77-8

Characteristics of the substance Disulfiram

White crystalline powder with a faint yellowish-greenish tint. Slightly soluble in alcohol, practically insoluble in water, acids and alkalis. Molecular weight 296.54.

Pharmacology

pharmachologic effect- anti-alcohol.

Inhibits acetaldehyde dehydrogenase and delays the enzymatic biotransformation of alcohol at the acetaldehyde stage. The accumulation of the latter in the body causes intoxication, which (since consciousness is preserved) is accompanied by severe sensations.

After oral administration, it is quickly and completely (70-90%) absorbed into the gastrointestinal tract. It is metabolized quite intensively, being reduced to diethyldithiocarbonate, excreted by the kidneys in the form of a glucuronide, or decomposes to form diethylamine and carbon disulfide, part of which (4-53%) is excreted through the lungs.

Use of the substance Disulfiram

Treatment and prevention of relapse of chronic alcoholism; chronic nickel intoxication.

Contraindications

Hypersensitivity, thyrotoxicosis, diseases of the cardiovascular system in the stage of decompensation (including pronounced cardiosclerosis, atherosclerosis of cerebral vessels, pre- and post-infarction conditions, aortic aneurysm, coronary insufficiency, arterial hypertension II-III, chronic heart failure) , serious illnesses hearing organs (neuritis auditory nerve) and eyes (glaucoma, optic neuritis); diabetes mellitus, pulmonary tuberculosis with hemoptysis, bronchial asthma, severe emphysema, exacerbation of peptic ulcer, severe liver failure, kidney disease, malignant tumors, diseases hematopoietic organs, mental illness, epilepsy and convulsive syndrome of any origin, polyneuritis, pregnancy, breastfeeding.

Restrictions on use

Cardiovascular diseases in the compensation stage, peptic ulcer stomach and duodenum(in remission) residual effects after violation cerebral circulation, endarteritis, previous psychosis while taking disulfiram, age over 60 years.

Use during pregnancy and breastfeeding

Side effects of the substance Disulfiram

Due to the properties of disulfiram: metallic taste in the mouth, unpleasant odor in patients with colostomy (associated with carbon sulfide), rare cases hepatitis (similar to those sometimes observed in patients with nickel eczema who do not suffer from alcoholism), polyneuritis of the lower extremities, optic neuritis, memory loss, confusion, asthenia, headache, skin allergic manifestations.

Related to the disulfiram-ethyl alcohol combination: cases are described respiratory failure, cardiovascular collapse, heart rhythm disturbances; angina pectoris, sometimes myocardial infarction, as well as neurological disorders; cerebral edema, depression of consciousness, up to coma.

When drinking alcohol in quantities exceeding 50-80 ml of vodka, while taking disulfiram, severe disorders of the cardiovascular and respiratory systems, edema, and convulsions may develop (detoxification therapy, administration of analeptics, and symptomatic therapy are necessary).

Complications with long-term use: rarely - psychoses resembling alcoholism; hepatitis, gastritis; in persons suffering from cardiovascular diseases, thrombosis of cerebral vessels is possible, therefore, if you complain of paresthesia in the limbs and facial area, you should immediately discontinue the drug; exacerbation of polyneuritis.

Interaction

The reaction to ethanol is reduced by ascorbic acid.

Contraindicated combinations

Alcohol: intolerance reaction (flushes, erythema, vomiting, tachycardia). Should be avoided simultaneous administration alcoholic beverages and drugs containing alcohol.

Undesirable combinations

Isoniazid: disturbance of behavior and coordination.

Nitro-5-imidazoles (metronidazole, ornidazole, secnidazole, tinidazole): delirium, confusion.

Phenytoin: Significant and rapid rise in plasma levels of phenytoin with toxic symptoms(suppression of his metabolism). If the combination cannot be avoided, clinical observation and monitoring plasma drug concentrations during and after treatment with disulfiram.

Combinations requiring caution

Warfarin (and other oral anticoagulants): increased effect of oral anticoagulants and risk of bleeding (decreased metabolism of warfarin in the liver). More frequent monitoring of warfarin concentrations and adjustment of the dose of anticoagulants is recommended during the administration of disulfiram and for 8 days after its discontinuation.

Theophylline: Disulfiram inhibits the metabolism of theophylline, so the theophylline dose should be adjusted (reduced dosage) depending on clinical symptoms and plasma drug concentrations.

Benzodiazepines: Disulfiram may potentiate the sedative effects of benzodiazepines by inhibiting their oxidative metabolism (especially chlordiazepoxide and diazepam). The dosage of benzodiazepine should be adjusted according to clinical manifestations.

Tricyclic antidepressants: possible increased alcohol intolerance reaction (disulfiram - ethyl alcohol reaction).

Overdose

Symptoms: coma, collapse, various neurological phenomena.

Treatment: symptomatic.

Routes of administration

Inside, intramuscularly And PC.

Precautions for the substance Disulfiram

Patients should be warned about the danger of alcohol intolerance reactions. In case of concurrent appointment with oral anticoagulants it is necessary to carry out more frequent monitoring of prothrombin levels and adjustment of doses of anticoagulants, which is associated with increased risk development of bleeding.

Should be used with caution in patients with renal failure or hypothyroidism, especially with the risk of a possible combination with alcohol.

In the article we will talk about how long Disulfiram stays in the human body after injection intramuscularly, in the form of tablets and an implant.

This drug is actively used in the treatment of alcohol dependence. It prevents the formation of an enzyme that breaks down ethyl alcohol into carbon dioxide and water. Disulfiram freezes this process when alcohol turns into poison - acetaldehyde.

If a patient drinks alcohol, severe poisoning occurs in the body, accompanied by nausea, increased heart rate and pain. This reaction causes a person to have a physical aversion to alcohol. In some cases, death is possible.

Release forms

There are a huge number of medications based on Disulfiram. They differ in the mass of the active substance in the composition and the period of elimination.

Release forms:

  1. Implantation tablets. The syringe container is sewn into the patient intramuscularly through a small incision in the skin. The medicine remains effective depending on the dosage, usually from 6 to 9 months. At this time, the body contains a small concentration of Disulfiram. However, after drinking alcohol, blood vessels dilate and, due to blood flow to the implant site, the content of the active substance in the body increases. Similar phenomenon can cause severe poisoning and even death.
  2. Tablets for oral administration. As a rule, you need to take one tablet per day; in subsequent stages, the dose may be reduced. Drinking alcohol-containing drinks during therapy is contraindicated.
  3. Solution for intravenous or intramuscular injection . The drug is injected into the buttock or into a vein within a minute. After which it “settles” in muscle tissue at the injection site. During blood circulation, its concentration is constantly maintained throughout the body.

How long does it take to leave the body?


The timing of disulfiram elimination depends on the concentration and form of release:

  1. Oral. When taking the tablets orally, the effect of the medicine lasts another 48 hours. However, the instructions indicate that this effect lasts about two weeks even after stopping treatment.
  2. Implants. The drug sewn under the skin stays in the body for 5 to 9 months, the maximum elimination period is 1 year. A small proportion of Disulfiram is deposited in fat deposits and is eliminated gradually. This method of treatment for alcoholism is considered the most convenient: the likelihood of a breakdown is reduced to zero. If the ampoule is removed from the body earlier, the drug remaining in the body is effective for up to 2 months.
  3. Intravenously and intramuscularly. Withdrawal dates liquid injection Disulfiram - from 6 to 9 months. According to the instructions, the product can retain its properties for up to 1 year.

Duration of action of drugs against alcohol and drug addiction Only the attending physician can determine. This period is individual for each patient.

Antidote

Often, drugs containing disulfiram are administered to the patient under pressure. And then the person begins to look for an antidote. However, it doesn't exist. Remove disulfiram from the body completely ahead of schedule impossible.

In case of a strong reaction to alcohol, multi-stage intoxication is carried out during treatment with the drug. It's long and difficult process, including the administration of the following drugs:

  • Ascorbic acid;
  • Ephedrine;
  • H1 blockers.

The procedure may take from 12 to 48 hours. However, it will only reduce the poisoning of the body.

Note: It is contraindicated to carry out such activities on your own. Only a specialist can prescribe the appropriate medications and calculate the dosage.

In addition, removing the drug using such methods is very dangerous. High doses ascorbic acid may cause irreversible physiological damage:

  • stomach ulcer;
  • liver cirrhosis;
  • impotence;
  • cancer.

Side effects from treatment

The drug itself is practically harmless, dangerous reaction occurs after drinking alcohol. The patient should be careful with food: a reaction may occur to kvass, syrups and other products containing the slightest dose of alcohol.

Extensive research on Disulfiram has revealed the following negative effects:

  • chronic fatigue, migraines;
  • mild memory loss;
  • unpleasant taste in the mouth;
  • intoxication of the liver and kidneys;
  • darkening of urine and yellowing of the skin.

Similar reactions occur with small and medium doses of alcohol. Drinking more than 500 ml of alcohol leads to serious consequences. The patient has pale skin and tachycardia.

Later, seizures, convulsions and convulsions may occur. In this case, the patient must be given a laxative and call an ambulance.

Sometimes patients undergoing treatment with Disulfiram begin to drink alcohol in small doses. In such cases, the drug reaction resembles normal alcohol intoxication, and the patient continues to drink alcohol 50-80 ml. Ultimately, this leads to serious disorders of the cardiovascular system and liver diseases.

Contraindications

Before prescribing the drug Disulfiram, the doctor must refer the patient for a detailed study. Patients who have taken alcohol 48 hours before contacting a specialist are not allowed to undergo treatment.

The drug is absolutely contraindicated for people suffering from the following diseases:

  • liver and respiratory failure;
  • diseases of the cardiovascular system;
  • mental disorders;
  • severe gastrointestinal diseases (stomach ulcer, erosion, etc.)
  • pregnant and lactating women.