Flushing and feeling of heat in the face, etc.). As a result of the unpleasant sensations that arise, a person develops an aversion to alcohol and, accordingly, alcoholism is cured.
Names, composition and forms of release of drugs with disulfiram
Disulfiram is the name of the active substance of a number of drugs intended for the treatment of alcoholism. The commercial names of drugs containing disulfiram are different, but they all have the same effect on the human body. And since there is no officially registered drug with the commercial name "Disulfiram" in Russia, we will consider the indications, contraindications, side effects and rules for using the active substance disulfiram. Moreover, it must be understood that all the characteristics of the active substance "disulfiram" apply to any drugs with different names containing disulfiram.Currently, disulfiram is commonly referred to by the names "disulfira" And "disulfir", which are just a corruption of the correct name. Therefore, when you hear the names "disulfir" or "disulfir", you must understand that we are talking about disulfiram.
Today in the CIS countries on the pharmaceutical market there are drugs containing disulfiram as an active ingredient, with the following commercial names:
- Antabuse effervescent tablets;
- Lidevin tablets;
- Teturam tablets;
- Esperal tablets.
Disulfiram preparations in tablet form contain the active substance in dosages of 100 mg, 150 mg, 200 mg, 250 mg, 400 mg and 500 mg. As excipients, various preparations with disulfiram contain different components. This means that before use, you need to carefully read the package leaflet with instructions that comes with each specific drug.
Tablets of various manufacturers with disulfiram are available in packs of 20, 30 or 50 pieces. As a rule, tablets with disulfiram are colored white with a cream or greenish-yellow tint, and are provided with a score and an engraving with a commercial name.
Disulfiram - action
Preparations containing disulfiram as an active ingredient are used to treat alcoholism only when other, milder methods of therapy have been ineffective. This approach is due to the fact that the action of disulfiram is based on the development of a negative conditioned reflex in response to alcohol consumption. A negative conditioned reflex is developed as a result of a deliberate call for extremely unpleasant sensations from drinking alcohol. Unpleasant sensations are caused by drinking a small amount of vodka under the supervision of a doctor while taking disulfiram. And since disulfiram violates the neutralization of alcohol in the body, the ingestion of alcohol into the body while taking drugs causes an intolerance reaction, manifested by extremely unpleasant sensations of poisoning, similar to a severe hangover. When a person experiences the unpleasant sensations of drinking alcohol several times, he develops a conditioned reflex of aversion to alcohol. And it is on this that the effect of the treatment of alcoholism with disulfiram preparations is based. That is, the essence of the therapeutic effect of disulfiram preparations is due to the fact that against the background of the action of the drug, alcohol consumption causes extremely unpleasant sensations, such as:
- redness of the skin;
- heat in the upper body and face;
- chest tightness;
- difficulty breathing;
- heartbeat;
- lowering blood pressure;
- fear.
All the discomfort that occurs in response to drinking alcohol while taking disulfiram preparations is due to the fact that the drugs interrupt the chain of biochemical reactions (block acetaldehyde dehydrogenase), during which the neutralization of ethyl alcohol occurs, at the stage of formation acetaldehyde. And this means that under the influence of disulfiram in the body of a person who has drunk alcohol, acetaldehyde accumulates - a toxic substance that causes disruption of the respiratory, cardiovascular and central nervous systems.
When taken orally in the form of tablets, disulfiram is rapidly absorbed into the bloodstream through the mucous membrane of the intestines and stomach in the amount of 70-90% of the entire dosage drunk. Then disulfiram penetrates into the adipose tissue, where its depot ("reserve") is created, from which the drug is slowly and gradually released, creating and maintaining a constant concentration of the active substance in the blood and, accordingly, a long-term effect. The first significant clinical effect appears already 3-4 hours after taking the first tablet of disulfiram, but the maximum severity of the therapeutic effect occurs only after 12 hours.
After the last intake of tablets with disulfiram, their full therapeutic effect persists for about two days. However, the residual effect of disulfiram persists for approximately 1 to 2 weeks after the last dose of the drug. Thus, within two days after taking the last dosage of disulfiram, the effect of the appearance of extremely unpleasant sensations in response to alcohol consumption is fully preserved. And within 1 - 2 weeks after taking the last dosage of the drug, a weak effect of the appearance of unpleasant sensations in response to alcohol consumption remains. This means that after taking the last tablet of disulfiram, you need to wait at least 2 weeks, and only after they have passed, you can start consuming alcoholic beverages.
Assistance in carrying out alcohol tests, if necessary, consists in the use of various medications. So, 15 - 20 ml of a 1% solution of methylene blue is necessarily injected intravenously, Cordiamin and Camphor are administered subcutaneously, and Cititon (or Lobelin), Ephedrine, Strychnine are administered intramuscularly, and oxygen is additionally inhaled. With a severe headache, they additionally make a "dropper" with a solution of ascorbic acid with glucose, with pain in the heart they give Validol, Corvalol or Nitroglycerin tablets, with low blood pressure (below 70/50), Mezaton or Ephedrine is administered, with oppression of cardiac activity Strofantin is administered ( 0.5 ml of a 0.05% solution is diluted in saline), with convulsions, 10 ml of 25% magnesia or Sibazon is administered, with severe nausea and vomiting, 10 ml of a 10% solution of calcium chloride and 0.5 ml of 0.1% Atropine. If during the alcohol test a strong psychomotor agitation develops, then 1-2 ml of a 2.5% solution of Aminazine is injected intramuscularly.
Described above three-stage method the use of disulfiram preparations is a classic method. However, it is rather inconvenient, therefore, instead of a three-stage regimen, disulfiram preparations are often used in another, simpler way. The easy way consists in taking disulfiram tablets without conducting alcohol tests. In this scheme, disulfiram preparations for the first 7-10 days are taken 500 mg once a day, then for the next 7-10 days - 200-250 mg once a day, and for another 7-10 days they drink the drug 125 - 150 mg once a day. The total duration of therapy with this simplified method is 21 - 30 days, during which the use of disulfiram reduces the craving for alcohol. Therefore, for a person who has independently decided to stop drinking and has normal willpower, such a simplified method of taking disulfiram preparations is optimal. A course of therapy using a simplified scheme can be carried out as needed, when there is a feeling that the craving for alcohol has reappeared.
Before starting the use of any disulfiram preparation, it is necessary to tell the person that he will experience discomfort when drinking alcohol while taking the pills. You should also tell what kind of discomfort it will be. In addition, it is imperative to warn that the consumption of more than 150 ml of vodka or other alcoholic beverage in an amount containing the equivalent volume of alcohol to 150 ml of vodka will lead to severe poisoning, which will end in death if the person is not quickly hospitalized in intensive care.
Since all disulfiram preparations cause discomfort when drinking alcohol, and when drinking more than 150 ml of vodka they cause severe poisoning, treatment can only be started with the consent of the patient with alcoholism.
Disulfiram implant (disulfiram under the shoulder blade)
The disulfiram implant is commonly called "filing", "torpedo" or "sewing under the shoulder blade". The essence of the procedure is that several disulfiram tablets are sewn into the subcutaneous fat or muscle layer at once, which first dissolve and are quickly absorbed into the blood, after which the entire total dosage is deposited in adipose tissue. Further, disulfiram is constantly released from adipose tissue in small doses, maintaining its constant concentration in the blood for a long period of time (5-9 months). As a result, after the introduction of the disulfiram implant, a person will experience discomfort in response to alcohol consumption for 5 to 9 months. In a way, "fixing" is a simple and reliable way to treat alcoholism, since the dosage of disulfiram is immediately administered, which will work and therefore ensure alcohol intolerance for the next 5 to 9 months.
For "filing" use disulfiram tablets with a dosage of 100 mg (these are Teturam tablets). "Filing" allows you to achieve alcohol intolerance in one procedure, it is convenient because a person does not need to first take disulfiram tablets for several days, keeping himself from drinking alcohol, and then undergo painful alcohol tests.
Also, the advantage of "filing" with disulfiram is that after implantation, the effect of the drug persists for 5-9 months, and after the pills are canceled, the effect of alcohol intolerance lasts only 1-2 weeks, after which a person can start drinking alcohol again without experiencing discomfort. And this means that while taking disulfiram tablets, it is much easier for a person to “break loose”, interrupt treatment and start drinking again, and after “filing” it is much more difficult to go into a binge, because the effect that causes discomfort in response to alcohol lasts at least 5 months. That is why "filing" is a very widespread way of using disulfiram preparations for the treatment of alcoholism in people of any age and gender.
In order to carry out "suturing" it is necessary to obtain the consent of the patient without fail, since in this case the drug is administered immediately in high concentration, as a result of which he will have to refrain from drinking alcohol for at least 5 months.
The method of performing "filing" is quite simple. First, under local anesthesia, a cruciform incision is made on the skin, the skin is pulled back, and 8 tablets of 100 mg each are immediately placed in the wound (the total dosage of the "filing" is 800 mg). Then the incision is sutured, the wound is treated with antiseptics and an adhesive plaster or bandage is applied, which is not removed or changed for two days. In 1-2 days after the insertion of the implant, the tablets completely dissolve and disulfiram is deposited in adipose tissue, from where it will enter the bloodstream for 5-9 months, maintaining the effect of intolerance on alcohol consumption.
An incision for disulfiram implantation is made under the shoulder blade on the back, in the buttocks, or in other places that the alcoholic cannot reach with his hands to remove the "filing". A small painless tubercle remains on the skin in the area of \u200b\u200bthe filing, which is not dangerous and is only a cosmetic defect. The tubercle is a consequence of fibrosis of the skin and subcutaneous fat.
Unfortunately, due to the simultaneous administration of a large dosage, the "filing" of disulfiram can provoke polyneuropathy. Therefore, when performing a "filing", vitamins of group B are necessarily prescribed (for example, combined preparations Milgamma, Neuromultivit, etc.) to prevent neuropathy. However, if, despite the intake of B vitamins, polyneuropathy has developed, then the tablets implanted under the skin are removed.
Disulfiram intravenously (shot, injection)
Disulfiram preparations intended for injection are not officially registered in Russia. Therefore, it is not possible to provide any objective information about such dosage forms.special instructions
Any disulfiram preparations should be used only under the supervision of a physician and with the consent of the patient himself, since a person should be aware of the possible negative consequences of drinking alcohol while taking medications (discomfort or severe poisoning).Before you start taking disulfiram preparations, it is recommended to refrain from drinking alcohol for 3 to 4 days. If before starting treatment with disulfiram preparations a person was on a binge, then before drinking the pills, he needs to detoxify in order to remove all the remnants of alcohol from the body. Detoxification is carried out by any available means, for example, by placing a "dropper" with vitamins, taking Medichronal, etc.
Since disulfiram preparations can cause liver damage (fulminant hepatitis, necrosis, etc.), which can lead to liver failure, coma, or even death, liver tests (bilirubin, AsAT, AlAT) must be done before starting the use of drugs. During the entire course of therapy, it is necessary to regularly (once a month) determine the concentration of bilirubin and the activity of transaminases (AsAT, AlAT). If at least a threefold increase in the activity of AST and ALT is detected, then you should immediately stop using disulfiram preparations and be under the supervision of a doctor until the liver tests are completely normalized.
If disulfiram preparations are used in combination with indirect anticoagulants (Warfarin, Dicoumarin, etc.), then it is necessary to control INR and other indicators in the first 3-4 weeks after the start of taking disulfiram and within 2 weeks after completion of the course of therapy at least once a week blood clotting and, if necessary, change the dosage of anticoagulants.
If the following symptoms appear, you should immediately consult a doctor and stop using the drug disulfiram:
- Paresthesia (tingling, numbness, or crawling sensation)
- Nausea;
- Vomit;
- Pain in the stomach;
- Jaundice (yellow coloration of the skin and mucous membranes);
- dark urine;
It is imperative to warn a person suffering from alcoholism that if he consumes alcohol while taking disulfiram preparations, he will develop an intolerance reaction, manifested by hot flashes, reddening of the skin of the face, palpitations, lowering blood pressure, nausea, vomiting, malaise, fear, etc. d. On average, such an intolerance reaction can last from half an hour to 3 days. An intolerance reaction develops if a person drinks less than 50-80 ml of vodka or other alcoholic beverage containing the same amount of alcohol as 50-80 ml of vodka. If a person drinks more than 80 ml of vodka, then he may develop poisoning with severe disorders of the cardiovascular and respiratory systems, swelling and convulsions. Therefore, when drinking any alcoholic beverages in amounts equivalent to 50-80 ml of vodka or more, a person should be urgently hospitalized in an intensive care unit for intensive care.
Alcohol intolerance reactions can occur not only when drinking alcohol, but also when taking medicines or products (for example, kvass, kefir, etc.) containing ethyl alcohol. In addition, a mild intolerance reaction can occur even when using alcohol-containing cosmetics (for example, aftershave lotions, colognes, eau de toilette, perfumes). Therefore, a person should be warned that during the use of disulfiram preparations, not only the use of alcoholic beverages should be abandoned, but also the use of any alcohol-containing products and cosmetics.
Intolerance reactions may occur as early as two weeks after the last dose of disulfiram, due to the long period of elimination of the drug from fat depots.
Overdose
An overdose is possible when ingesting high doses of tablets, and is manifested by a disorder of the central nervous system: confusion, encephalopathy, coma, convulsions, collapse, extrapyramidal symptoms (disturbances of movement - involuntary twitching of various parts of the body, worm-like wriggling finger movements, turning the head and torso to the sides, sweeping tossing movements of the limbs, tremor, spasm of half of the face, neck and tongue, etc.). With the development of symptoms of an overdose of disulfiram, a person should be urgently hospitalized in a hospital and symptomatic therapy should be carried out aimed at maintaining the normal functioning of vital organs and systems.Influence on the ability to control mechanisms
Since disulfiram can cause depression of consciousness (primarily drowsiness, especially in the initial stages of treatment), the ability to control mechanisms deteriorates during the entire period of its use. Therefore, it is desirable for the duration of treatment with disulfiram to refuse to perform any kind of work related to the need to have a high reaction rate and concentration. But if for some reason a person needs to engage in any kind of activity, including those requiring a high speed of reactions and concentration of attention, then this can be done only if there are no signs of oppression of consciousness.Interaction with other drugs
Any preparations of disulfiram should not be used simultaneously with drugs or cosmetics containing alcohol, since the ingestion of ethyl alcohol into the body will lead to the development of an intolerance reaction, manifested by flushing, reddening of the skin, headache, nausea, vomiting, rapid heartbeat, drop in blood pressure, confusion . The reaction of alcohol intolerance while taking disulfiram can be weakened by taking Diazepam, ascorbic acid or antihistamines (for example, Suprastin, Telfast, Erius, Claritin, Cetrin, Cetirizine, etc.).It is undesirable to combine any disulfiram preparations with the following drugs:
- Isoniazid. Risk of impaired coordination of movements and behavior (depression), as well as the appearance of dizziness.
- Imidazole derivatives (Metronidazole, Ornidazole, Seknidazole, Tinidazole). High risk of confusion, psychosis or delirium ("delirious tremens").
- Phenytoin. When used with disulfiram, the concentration of phenytoin in the blood increases sharply, which leads to the development of the toxic effects of the latter. Therefore, when these drugs are used together, the concentration of phenytoin in the blood should be monitored, if necessary, adjusting its dosage.
- Hepatotoxic drugs (eg, Azathioprine, Azithromycin, Aztreonam, Allopurinol, Amiodarone, Amitriptyline, Amoxiclav, Ampicillin, Amphotericin B, Aspirin, androgens, Baclofen, Biseptol, Valproic acid, Verapamil, Vincristine, Halothane, glucocorticoids, Griseofulvin, Josamycin, Diazempamycin , 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 anti-inflammatory drugs (NSAIDs), Oxacillin, Omeprazole, oral contraceptives, penicillin antibiotics, Paracetamol, Pefloxacin, Ranitidine, Rifampicin, Roxithromycin, salicylates, sulfonamides, Terbinafine, Tetracycline, tricyclic antidepressants, Fluconazole, Ftivazid, Quinidine, Chlorpromazine, Cefazoline, Cefazoline azone, Cefotaxime, Ceftazidime, Ceftriaxone, Cefuroxime, Cyclosporine, Cyclophosphamide, Cimetidine, Enalapril, Erythromycin, estrogens, etc.). The combination of disulfiram with hepatotoxic drugs dramatically increases the risk of liver damage.
- Indirect anticoagulants (Warfarin, Dicoumarin, etc.). Disulfiram enhances the effect of anticoagulants, so their combination increases the risk of bleeding. Therefore, when taking anticoagulants with disulfiram, it is necessary to control blood clotting and adjust the dosage of anticoagulants.
- Theophylline. Disulfiram reduces the rate of excretion of Theophylline from the body, resulting in a sharp increase in its concentration in the blood. Therefore, the combination of drugs requires regular determination of theophylline concentration in the blood and a decrease in its dose.
- Benzodiazepines (Phenazepam, Diazepam, etc.). Disulfiram enhances the sedative effect of benzodiazepines, resulting in dizziness and lethargy. Therefore, with their combined use, it is necessary to reduce the dosage of benzodiazepines in accordance with clinical manifestations.
- Tricyclic antidepressants (Amitriptyline, Imipramine, etc.). With the combination of these drugs, the severity of the alcohol intolerance reaction increases.
- Tricyclic antidepressants, Phenytoin and MAO inhibitors (Iproniazid, Selegiline, etc.). The combination of these drugs with disulfiram increases the risk of side effects of all drugs taken.
- Rifampicin, caffeine, Phenazone, Chlorzoxazone. Disulfiram slows down the elimination of these drugs, as a result of which a reduction in their dosage may be required.
- Thymoside. The combination with disulfiram leads to an increase in the severity of the organic brain syndrome.
- Chlorpromazine. The combination with disulfiram increases the risk of a sharp decrease in blood pressure.
Duration of action (how long does disulfiram last in the body)
Disulfiram in the form of tablets and injections begins to act one hour after ingestion, and the maximum effect is achieved after 12 hours. After taking the last dose of disulfiram, the effect of alcohol intolerance persists for another 1 to 2 weeks. That is why drugs with disulfiram can be taken at least 24 hours after drinking alcohol, since ethyl alcohol is completely eliminated from the body only during the day. If you start taking disulfiram earlier than 24 hours after drinking alcohol, then a person will develop an intolerance reaction, since there is still ethyl alcohol in the body that has not been completely excreted.
It is optimal to start taking drugs with disulfiram 2 to 3 days after the last episode of alcohol consumption.
Antidote to the drug (how to remove disulfiram?)
Unfortunately, there is no antidote or substance that can remove disulfiram preparations from the body. And various drugs (for example, ascorbic acid, iron preparations, etc.), which in practice they try to use to remove disulfiram from the body or neutralize its effect, are in fact completely useless. The drug will work for the specified period of time, that is, within 1 to 2 weeks after taking the last tablet with disulfiram. The inability to neutralize or remove it from the body is due to the fact that the substance accumulates in the subcutaneous fat layer, from where it enters the bloodstream in small doses, maintaining a constant concentration in the blood.The conventional wisdom that you can neutralize the effect of disulfiram by contacting a narcologist for "decoding" is wrong. And narcologists who supposedly perform the decoding procedure simply do not tell a person that this is impossible, since an alcoholic who wants to drink is very aggressive and does not perceive reality objectively. Therefore, narcologists simply perform certain actions, imitating the process of "decoding". In such situations, vitamins are usually administered to an alcoholic under the guise of an "antidote".
As conditional antidotes for disulfiram, only 1% methylene blue solution, ascorbic acid and antihistamines (Suprastin, Diazolin, Erius, Parlazin, etc.), which can partially stop the discomfort of an intolerance reaction. Thus, after drinking alcohol while taking disulfiram, you can stop the intolerance reaction with an injection of 1% methylene blue, taking ascorbic acid, or any antihistamine. However, all these drugs eliminate only the symptoms of an intolerance reaction, but do not remove disulfiram from the body.
disulfiram and alcohol
Alcohol is incompatible with disulfiram preparations, since the use of even a small amount of ethyl alcohol while taking disulfiram causes an intolerance reaction. An intolerance reaction is manifested by the development of extremely unpleasant sensations, such as arrhythmia, palpitations, a sharp drop in blood pressure, nausea, vomiting, flushing, a feeling of heat and redness of the skin of the face, neck and upper body, general poor health. The reaction of intolerance lasts for several hours, during which a person feels the whole range of unpleasant sensations. Drinking alcohol in an amount equivalent to 150 ml of vodka or more can cause not just an intolerance reaction, but the development of severe cardiovascular or respiratory failure, edema and convulsions with a fatal outcome. In such a situation, the victim should be immediately hospitalized in the intensive care unit for intensive care.
Therefore, it is clear that alcohol is categorically incompatible with preparations containing disulfiram. As a result, it is obvious that it is impossible to drink alcoholic beverages while taking drugs with disulfiram.
Moreover, during the entire period of taking disulfiram, one should be very careful about the alcohol content in any means used, including medicines, colognes, etc. After all, taking a drug containing ethyl alcohol will cause the same intolerance reaction as the use of any alcoholic beverage. In addition, some people report that even the use of aftershave cologne containing alcohol while taking disulfiram causes a mild alcohol intolerance reaction.
It should be remembered that the effect of disulfiram preparations persists for another 1 to 2 weeks after taking the last pill. Therefore, it is impossible to drink alcohol immediately after the end of the use of the drug, it is necessary to wait 1-2 weeks for it to be completely eliminated from the body.
Side effects
Any drugs containing disulfiram as an active substance can cause various side effects, which are divided into three groups, depending on which factor is the leading cause of side effects:
1.
Side effects of the drugs themselves with disulfiram, due to the properties of the active substance (disulfiram):
- Metallic taste in the mouth;
- Bad breath (halitosis);
- Bad body odor in people with a colostomy;
- Hepatitis (may develop only in people suffering from nickel eczema and not having alcohol addiction);
- Jaundice;
- Liver failure (occurs only in very rare cases as a complication of hepatitis);
- Polyneuritis of the legs;
- Optic neuritis;
- Loss or deterioration of memory;
- confusion;
- Disorientation in space and time;
- Drowsiness (usually observed at the beginning of treatment, then disappears);
- Increased fatigue (observed at the beginning of treatment, then disappears);
- convulsions;
- encephalopathy;
- Asthenia;
- Headaches;
- Skin allergic reactions (rash, itching, etc.);
- Nausea and vomiting;
- Pain in the stomach;
- Increased activity of hepatic transaminases (AST and ALT).
- respiratory failure;
- Cardiovascular collapse;
- Arrhythmia;
- angina;
- Neurological disorders (encephalopathy, blackout of consciousness, convulsions);
- Hemorrhage in the membranes of the brain;
- Flushing of the face and sensation of heat;
- Redness of the skin, especially the upper body, neck and face;
- Nausea and vomiting;
- fast heartbeat (tachycardia);
- A sharp decrease in blood pressure;
- General malaise.
- Psychosis similar in clinical course to alcohol;
- Hepatitis;
- Thrombosis of cerebral vessels in people suffering from various cardiovascular diseases;
- Exacerbation of polyneuritis;
- When taking alcoholic beverages in an amount equivalent to more than 50 - 80 ml of 40% vodka, severe disorders of the cardiovascular and respiratory systems develop, edema and convulsions appear. With the development of such disorders, the person should be immediately transported to the hospital, where it is necessary to carry out symptomatic treatment with simultaneous detoxification therapy.
Contraindications for use
Contraindications to the use of any drugs containing disulfiram as an active substance are divided into relative and absolute. Absolute contraindications include contraindications, in the presence of which it is impossible to use drugs with disulfiram in any case. Contraindications are relative, in which the use of drugs with disulfiram is undesirable, but, if necessary, it is possible with caution and under the supervision of a physician.
Absolute contraindications to the use of drugs containing disulfiram as an active substance include the following diseases or conditions:
- Individual hypersensitivity, allergic reactions or intolerance to any components of the drug;
- The period of pregnancy and breastfeeding;
- Polyneuritis;
- Infectious diseases of the central nervous system (for example, tick-borne encephalitis, spleen);
- Radoter effervescent tablets (may not be available in pharmacies due to the re-registration procedure);
- Teturam tablets;
- Esperal tablets.
Currently, the pharmaceutical market of the CIS countries has the following disulfiram analogues:
- Vivitrol powder for suspension for intramuscular injection;
- Zorex capsules;
- Colme drops for oral administration;
- Litonite solution for injection;
- Metadoxil tablets for oral administration and solution for intravenous and intramuscular injections;
- Sodium thiosulfate solution for injection and powder for solution for injection or oral administration;
- Selincro tablets;
- Tempozil tablets;
- Cyamide tablets.
Disulfiram, Coprinol, Alco Barrier, Extra Blocker and other drugs for the treatment of alcoholism, their effectiveness and safety (doctor's opinion) - video
Medicines for the treatment of alcoholism: disulfiram preparations (Teturam, Antabuse), Naltrexone, Medichronal, etc. (doctor's opinion) - video
Disulfiram - reviews of doctors
Narcologists working with drugs containing disulfiram as an active ingredient consider them to be quite effective drugs for the treatment of alcohol dependence in people of any age and gender. However, as narcologists emphasize, the use of drugs containing disulfiram requires compliance with two basic conditions - this is, firstly, the desire of the person himself to get rid of alcoholism, and secondly, an understanding of the destructiveness of the existing disease. If a person does not want to recover from alcoholism and does not understand the perniciousness of the disease, then drugs with disulfiram will be ineffective, since not a single drug can keep a person from drinking alcohol if he so desires.
Also, narcologists warn that it is impossible to cure alcoholism forever by taking drugs with disulfiram alone. The pills have an effect that lasts for a certain period of time, during which the person will refrain from drinking alcohol. But for a complete cure, a set of measures is needed that will relieve cravings for alcohol forever, and not for a while. That is, taking drugs with disulfiram provides a "light period" during which a person does not drink, but in the absence of complex treatment, after the expiration of disulfiram, a binge will follow again. Therefore, the use of only drugs with disulfiram will ensure the alternation of cycles of "light intervals" with hard drinking. However, this effect suits many, since it allows you to give up alcohol for a certain period of time, then drink again, and then, if necessary, give up alcohol again, taking disulfiram preparations.
In addition, narcologists warn that with a weak willpower in an alcoholic, drugs with disulfiram in tablets are often ineffective, therefore, in such situations, it is recommended to immediately make a "file" that ensures the refusal of alcohol for a certain period of time.
Disulfiram - reviews of alcoholics
On average, 70 - 80% of the reviews of people who took drugs containing disulfiram are positive, due to a noticeable decrease in cravings for alcohol under the influence of drugs. The reviews note that preparations with disulfiram significantly reduce the craving for alcohol, and in some cases even cause disgust not only for the taste, but even for the smell of alcoholic beverages. Also, the reviews indicate that Esperal is softer than the domestic Teturam, but the effectiveness of both drugs is the same. If a person, while taking drugs with disulfiram, refrains from drinking alcoholic beverages, then side effects almost never appear. However, some note that against the background of taking drugs with disulfiram, there are pains in the stomach and right hypochondrium, as well as some absent-mindedness. At the same time, these side effects are easily tolerated, and therefore are considered quite tolerable by alcoholics themselves.
A large number of positive reviews about drugs with disulfiram were left by relatives of alcoholics who, despite the recommendations, gave drugs to a person without his knowledge. In this case, the development of an intolerance reaction to alcohol could be represented as the fact that the body no longer takes alcohol, as a result of which alcoholics actually stopped drinking.
Summarizing the reviews, we can say that a positive opinion about drugs with disulfiram was formed by people who consciously decided to fight the disease and had a firm intention to stop drinking.
There are few negative reviews about drugs containing disulfiram, and they are mainly due to a severe intolerance reaction that occurs in response to drinking alcohol while taking the medication. Such reviews indicate that even a bottle of beer caused extremely unpleasant sensations that lasted a very long period of time. During the development of an alcohol intolerance reaction, a person experienced strong fear, depression, a feeling of helplessness, which caused a negative opinion about the drugs. That is, in general, we can say that negative reviews are left by people who do not like and do not like the radical effect of drugs with disulfiram, against the background of which you cannot drink even a little alcohol.
In addition, there are a number of negative reviews about drugs with disulfiram, which are left by people who hoped for some kind of "miracle". In other words, they lived with the hope that taking the drug would magically rid them of alcoholism, and they themselves would not have to make any effort to do this, but it would be enough just to take the pills on time. Naturally, such an idea is not true, and to get rid of alcoholism, you need to make efforts yourself, since any drug can only help, but not do all the work on yourself instead of a person. Accordingly, with the mood for a "miraculous cure", disappointment arose, which resulted in negative reviews.
Price
Currently, the cost of various drugs containing disulfiram as an active substance varies in pharmacies in Russian cities from 105 to 1500 rubles per pack of tablets or ampoules. Domestic drugs (eg Teturam) are the cheapest, while imported drugs (eg Esperal) are the most expensive.Torpedoing from alcoholism: action, preparation, effectiveness, decoding (doctor's opinion) - video
Sewing in an ampule from alcoholism: the pros and cons, the procedure, the consequences - video
Treatment of alcoholism without the knowledge of the patient. Preparations Proproten-100 and Colme (doctor's recommendations) - video
Compulsory treatment of alcoholism in private and public clinics - video
Hangover drugs: Polysorb, Zorex, Alka-Seltzer, Antipohmelin, Aspirin - video
Binge: duration, consequences, types, treatment at home (diet, drinking regimen) and in the clinic - video
Before use, you should consult with a specialist.Disulfiram is a drug that is actively used in the treatment of alcoholism. The drug causes an adverse reaction in which the combined use of the drug with alcohol becomes impossible.
Composition and principle of action
The drug is available in two dosage forms: tablets for implantation and oral administration. Tablets for implantation contain 100 mg. disulfiram. This substance slows down the breakdown of acetaldehyde, a component resulting from the breakdown of ethanol (the main substance found in alcoholic beverages). This leads to the fact that acetaldehyde does not turn into acetic acid, as under normal conditions, but accumulates. As a result, there are side effects of the combined use of Disulfiram in conjunction with alcoholic beverages:
- Severe nausea;
- Formation of vomit, which in most cases damage the esophagus;
- Redness of the skin and severe burning of the upper body (including the face);
- Suffocation, increased anxiety and fear of death;
- Increased sweat separation;
- Unstable blood pressure;
- Coma states.
If an addicted person "took on the chest" during the course of treatment, he will experience the effects listed above. The more alcohol you drink, the more pronounced the side effects will be. In the most severe cases, drinking alcohol can even lead to the death of a sick person.
Such side effects provoke an aversion to alcoholic beverages, due to which a person decides not to drink alcohol anymore. Over time, the effect is fixed, and the person is cured of alcohol addiction.
Indications for use
Disulfiram is prescribed for the treatment of patients who suffer from chronic alcoholism. The main purpose of the drug is to prevent relapse. Implants are prescribed to cleanse the body in case of nickel poisoning.
The drug has a number of contraindications for use:
- Hypersensitivity to active and auxiliary components, as well as structural analogues (drugs with a similar active substance);
- Diabetes;
- Epilepsy is a neurological disease, the main symptom of which is sudden convulsions;
- Emphysema of the lungs is a pathological expansion of the alveoli, as a result of which the supply of oxygen and the removal of carbon dioxide are disturbed;
- Thyrotoxicosis - increased production of thyroid hormones caused by malfunctions of the thyroid gland;
- Bronchial asthma is a pathology of the respiratory tract, in which there is a narrowing of the bronchi;
- The presence of diseases of the nervous system and psyche;
- Severe liver failure;
- The combined use of metronidazole, isoniazid, finitoin and other drugs in which there is even a small percentage of alcohol;
- Various pathologies in which the process of blood production is disrupted;
- Tuberculosis of the lungs - an infectious lesion of the lungs caused by the bacterium tuberculosis;
- Acoustic neuritis is a nerve lesion that occurs as a result of a complication of the inflammatory process in the ear;
- Ulceration of the gastrointestinal tract - the process of formation of ulcers on the gastric mucosa and other areas related to the gastrointestinal tract;
- Severe cardiac pathology - diseases associated with disruption of the heart;
- The presence of malignant (cancerous) tumors;
- Damage to the optic nerve;
- Bleeding that occurs in any of the areas of the gastrointestinal tract;
- Glaucoma is a visual pathology caused by a violation of intraocular pressure.
Also, the drug is contraindicated in women who are carrying or feeding a child.
In what cases is disulfiram prescribed to patients with caution
Before starting treatment, you need to consult a doctor and undergo a complete medical examination. Do not self-medicate in the following situations:
- When reaching old age (from 60 years and older);
- Renal failure and severe disorders in the liver;
- Ulcerative lesions of the gastrointestinal tract at the stage of remission;
- Diseases of the bronchi and lungs with respiratory failure;
- Endarteritis is a lesion of the arteries located mainly in the lower extremities.
If you have previously taken Disulfiram and experienced psychosis during treatment, the use of the drug should also be taken with caution.
How to take Disulfiram
Before starting treatment, the patient must undergo a complete medical examination, be aware of the consequences of taking alcohol together with disulfiram, and be notified of the start of treatment. Therapy should be started after the alcohol has been completely eliminated by the body - when using small doses, it takes at least 12 hours. Secretly mixing the drug into food and drinks is an unacceptable measure that can lead to dangerous and sometimes irreversible consequences.
The initial dose of the drug is 400-800 mg. drug for several days. Maintenance dose - 100-200 mg. or 400-800 mg. Two times per week. The scheme and duration of the therapeutic course is determined by the narcologist on an individual basis. If necessary, the drug is prescribed during the holidays or the patient's vacation.
Before starting treatment, the doctor concludes an antabuse agreement with the patient, according to which the patient undertakes to take the drug for six months. Without control, the use of the drug can become irregular, because of which the person does not achieve the expected effect. For this reason, it is important to take the remedy under the supervision of a specialist, spouse or close relative.
Another way to use Disulfiram is to administer an implant tablet. Intramuscular or subcutaneous implantation of the agent is carried out exclusively by a medical specialist according to the following algorithm:
- The doctor disinfects the injection site with antiseptics.
- Next, local anesthesia is performed - the doctor injects the patient with drugs that provide a pronounced analgesic effect.
- Before inserting the implant tablet, the doctor carefully cuts the skin in the designated area. The size of the incision usually does not exceed 6 mm.
- Using a trocar, the narcologist gently inserts the drug, making it parallel to the skin surface. At this stage, the first 2 tablets are inserted.
- At the next stage, the doctor injects the remaining 6 tablets in such a way that their location is cruciform relative to the incision area.
- At the final stage, the doctor sews up the incision site, forming a neat seam, and then applies a sterile bandage to the treated area. In this place, a small tubercle often forms, which is not a deviation from the norm.
800 mg is introduced into the body. disulfiram, which are gradually released over the next 8 months. At first glance, such a dosage form may seem effective, since the drug will act constantly, while you can forget about taking the pill or not take the drug intentionally. However, experienced doctors note that in this case, very little drug is absorbed into the body, due to which the therapeutic effect is weak.
How and how long does Disulfiram work
The drug begins to act 2 hours after implantation. 3-4 days after the start of treatment, the effect becomes most pronounced. After completion of the intake, the therapeutic effect persists for another 1-2 weeks. The time of the pharmacological (therapeutic effect) depends on the size of the dose taken, as well as the individual characteristics of the patient's body. The drug accumulates in the body, due to which it acts even in cases where the patient breaks down and deliberately skips taking the drug.
If an alcohol-dependent person takes the drug by mouth, the therapeutic effect manifests itself even faster - within 5-10 minutes. The body does not get used to the active substance, so the drug can be used for several years. Over time, the side effects are more easily tolerated, and the craving for alcohol noticeably weakens.
Side effects
In addition to the main action, the drug causes a number of side effects in patients:
- Violation of orientation in space;
- The appearance of a metallic taste and bad breath;
- Allergic reactions in the form of itching and various rashes on the skin;
- Hepatitis - inflammatory diseases of the liver caused by viruses;
- Disorders of the psyche and nervous system;
- Multiple lesions of the nerves of the lower extremities;
- Headaches;
- Decreased attention and memory;
- Discharge in the presence of a colostomy (artificial hole) and the appearance of unpleasant odors on the skin;
- Damage to the optic nerve;
- Anaphylactic shock.
The last side effect on the list above is a severe allergic reaction that requires immediate medical attention. A person feels a sharp pain, his face and other parts of the body swell strongly, itching spreads throughout the skin, and blood pressure drops. Anaphylactic shock develops very quickly and in the most severe cases can lead to death within minutes.
If a person undergoing treatment with Disulfiram has taken alcohol, you should immediately call an ambulance, conduct detoxification and symptomatic therapy.
Overdose
If the allowable doses are exceeded, the patient may fall into a coma, undergo sudden cardiovascular failure or neurological disorders. To improve the patient's condition, detoxification and symptomatic therapy is carried out.
Interaction of the drug with other drugs
If the patient is being treated with other drugs, he should pay attention to the compatibility of Disulfiram with other drugs. In the table below, we will look at what the combination of a drug with various substances and medicines leads to.
| Drug or category of drugs | Effect resulting from combined use with Disulfiram |
| Preparations with a minimum or high content of ethanol. | Hyperemia (flushing of the face), fever and chills, increased heart rate, severe disturbances in the work of the heart and blood vessels, fainting, nausea, vomiting, suffocation. |
| Drugs that prevent the formation of blood clots. | The occurrence of spontaneous bleeding. |
| Clozapine. | Depression of the central nervous system. |
| Vitamin C (ascorbic acid). | Decreased effectiveness as a result of a weakened and almost imperceptible reaction to the use of alcoholic beverages. |
| Barbiturates. | pathological retardation. |
| Guanfacine. | The appearance of depressive conditions, deterioration of mood, apathy. |
| Tricyclic antidepressants. | Strengthening of existing adverse reactions. |
| Chlorpromazine. | Decreased blood pressure to extreme values. |
| Perphenazine. | The onset of psychotic symptoms. |
| Chloroxazone. | Increased plasma concentration of chlorzoxazone. |
| Caffeine. | Reducing the rate of absorption, processing and excretion of coffee from the body of an alcoholic. |
| fluoxetine. | Strengthening depression. |
| Omeprazole. | Impaired consciousness, refusal to speak, increased agitation or stupor. |
| Etinamat. | Increased side effects of etinamate. The combination of Disulfiram with this drug threatens the life of the patient. |
| diazepam. | Decreased effectiveness of disulfiram. |
| Cephalosporins. | Severe intoxication that threatens health and life. |
| Temazepam. | Strengthening the toxic effect of Temazepam. |
| Phenytoin | Strengthening the toxic effect that phenytoin has. |
| Amitripillin. | Producing a toxic effect on neurons. |
| Sedative (calming) drugs | severe lethargy |
| Imipramine, Desipramine. | Decreased absorption and excretion of these drugs. |
| Sleeping drugs. | Strong sedative effect, lethargy, apathy. |
| Buspirone. | The emergence and development of manic states. |
| Rifampicin. | Reducing the rate of decay, processing and excretion of Rifampicin from the patient's body. |
| Metronidazole. | The appearance of psychosis and adverse reactions similar to those that are formed in the process of taking alcohol. |
| Sertraline | Deterioration of the emotional state in depression. |
| Isoniazid. | Increased toxic effect on neurons, worsening gait, depression. |
| Preparations for the removal and prevention of epilepsy. | Marked retardation. |
If you are taking any of the above medicines, tell your doctor before starting treatment.
Clinico-pharmacological group:Included in medications
ATH:N.07.B.B.01 Disulfiram
Pharmacodynamics:It has an anti-alcohol effect.
Inhibits acetaldehyde dehydrogenase and delays the enzymatic biotransformation of alcohol at the stage of acetaldehyde. The accumulation of the latter in the body causes intoxication, which (since consciousness is preserved) is accompanied by severe sensations.
Pharmacokinetics:After oral administration, it is quickly and completely (70-90%) absorbed in the gastrointestinal tract. It is metabolized quite intensively, recovering to diethyldithiocarbamate, excreted by the kidneys in the form of glucuronide, or decomposes to form diethylamine and carbon disulfide, part of which (4-53%) is excreted through the lungs. Indications: Treatment and prevention of recurrence of chronic alcoholism; chronic nickel intoxication.XXI.Z70-Z76.Z71.4 Alcoholism counseling and supervision
XX.Y90-Y98.Y91.2 Severe alcohol intoxication
XX.Y90-Y98.Y91.1 Alcoholic intoxication of moderate degree
XX.Y90-Y98.Y91.0 Mild alcohol intoxication
Contraindications:Hypersensitivity, thyrotoxicosis, diseases of the cardiovascular system in the stage of decompensation (including pronounced cardiosclerosis, cerebral atherosclerosis, pre- and post-infarction conditions, aortic aneurysm, coronary insufficiency, arterial hypertension II-III degree, chronic heart failure), severe diseases hearing organs (neuritis of the auditory nerve) and eyes (glaucoma, optic neuritis), diabetes mellitus, pulmonary tuberculosis with hemoptysis, bronchial asthma, severe pulmonary emphysema, exacerbation of peptic ulcer, severe liver failure, kidney disease, malignant tumors, diseases of the hematopoietic organs, mental illness, epilepsy and convulsive syndrome of any origin, polyneuritis, pregnancy, breastfeeding. Carefully:Cardiovascular diseases in the stage of compensation, peptic ulcer of the stomach and duodenum (in remission), residual effects after cerebrovascular accident, endarteritis, previous psychosis while taking disulfiram, age over 60 years. Pregnancy and lactation:Category of action on the fetus according to the FDA - C. Contraindications for use in pregnant and lactating women. Dosage and administration:Inside, intramuscularly and subcutaneously. Inside the dose is selected individually and is usually 0.25-0.5 g per day; treatment begins after a thorough examination of the patient and a warning about the consequences and complications. 8-10 tablets are implanted subcutaneously and intramuscularly. Side effects:Caused by the properties of disulfiram: metallic taste in the mouth, unpleasant odor in patients with colostomy (associated with carbon sulfide), rare cases of 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.
Associated with the combination of disulfiram-ethyl alcohol: cases of respiratory failure, cardiovascular collapse, cardiac arrhythmias, angina pectoris, sometimes myocardial infarction, as well as neurological disorders, cerebral edema, depression of consciousness, up to coma, have been described.
When taking alcohol in an amount exceeding 50-80 ml of vodka, while taking disulfiram, severe disorders of the cardiovascular and respiratory systems, edema, convulsions may develop (detoxification therapy, the introduction of analeptics, and symptomatic therapy are necessary).
Complications with long-term use: rarely - psychosis, reminiscent of alcohol; hepatitis, gastritis; in persons suffering from cardiovascular diseases, cerebral vascular thrombosis is possible, therefore, if there are complaints of paresthesia in the limbs and the face, the drug should be immediately discontinued; exacerbation of polyneuritis.
Overdose:Symptoms: coma, collapse, various neurological phenomena.
Treatment: symptomatic.
Interaction:Contraindicated combinations
Alcohol: intolerance reaction (flushing, erythema, vomiting, tachycardia). Avoid concomitant use of alcoholic beverages and medicines containing alcohol.
Unwanted Combinations
Isoniazid: impaired behavior and coordination.
Phenytoin: significant and rapid rise in plasma levels of phenytoin with toxic symptoms (suppression of its metabolism). If the combination cannot be avoided, clinical monitoring and monitoring of plasma concentrations of the drug during and after treatment with disulfiram should be carried out.
- Instructions for use Disulfiram
- Ingredients of Disulfiram
- Indications for Disulfiram
- Storage conditions of the drug Disulfiram
- Shelf life of the drug Disulfiram
ATC code: Nervous system (N) > Other drugs for the treatment of diseases of the nervous system (N07) > Drugs used for psychological or physiological dependence on various substances (N07B) > Drugs used for alcohol dependence (N07BB) > Disulfiram (N07BB01)
Release form, composition and packaging
tab. for implantation 100 mg: 10 pcs.Reg. No: 884/95/2000/05/10/15 dated 02.11.2015 - Valid
Tablets for implantation white or almost white with a yellowish-greenish tint, round, flat on both sides, with bevelled edges.
Excipients: sodium chloride, mannitol, macrogol 6000.
10 pieces. - colorless glass bottles (1) - packs of cardboard.
Description of the medicinal product DISULFIRAM was created in 2010 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Belarus. Date of update: 06/09/2011
Disulfiram is an inhibitor of aldehyde dehydrogenase, an enzyme that converts acetaldehyde (the main metabolite of ethyl alcohol) into acetic acid. In the case of simultaneous administration of the drug and the consumption of ethyl alcohol, a significant increase in the concentration of acetaldehyde in the body occurs and symptoms of intoxication with this compound occur. These include:
- nausea, vomiting, tachycardia (feeling of rapid heartbeat), hypotension, dizziness, sudden flushing of the face and feeling hot. The intensity of these symptoms depends on the amount of ethanol taken;
- they usually last 30-60 minutes, and sometimes even several hours. In severe cases, when the concentration of alcohol in the blood exceeds 125-150 mg / 100 ml, respiratory failure, arrhythmia, myocardial infarction, heart failure, loss of consciousness, convulsions, and in rare cases, in the absence of medical care - death. Usually, after alcohol intolerance, the patient becomes drowsy and can sleep for more than ten hours.
The described reaction is the basis for the use of disulfiram in the treatment of alcoholism. When using disulfiram, other forms of therapy also play an important role (for example, behavioral techniques). The effectiveness of treatment in such cases is higher than in persons treated only pharmacologically. The patient's and medical staff's confidence in treatment with disulfiram also plays a significant role. Emphasizing this type of treatment, being reminded of the dangers associated with alcohol use when using disulfiram, signing a statement informing about the consequences of alcohol use, and regular follow-up examinations increase the effectiveness of treatment.
After implantation, disulfiram penetrates into the blood. The minimum content of disulfiram in the blood is about 20 ng / ml. After implantation of 1-1.6 g, the content of diethyldithiocarbamate and carbon disulfide in the blood reaches 0.14 μg / ml after implantation of 1-1.6 g of disulfiram. However, despite these very low levels, disulfiram-ethyl alcohol reactions can occur up to 5-9 months after implantation. It is assumed that when alcohol is consumed, lipids are mobilized, blood vessels dilate and blood flow increases at the implantation site, as a result of which the flow of disulfiram into the blood increases.
Quite intensively metabolized in the liver, recovering to diethyldigiocarbamate, excreted by the kidneys in the form of glucuronide, or decomposed to form diethylamine and carbon disulfide, the proportion of which varies from 4 to 53% (excreted through the lungs). About 20% of the dose taken is excreted unchanged in the feces.
Auxiliary drug in the treatment of alcohol dependence. The drug is intended for selected and cooperating patients, with the use of appropriate ancillary treatment.
Tablets intended for implantation must be sterile, without damage and impurities, and be in their original packaging.
Implantation:
- after thorough disinfection and local anesthesia, a small incision (approximately 6 mm) is made in the left iliac region, low enough to avoid friction with the belt. The subcutaneous tissue is parted and, using a trocar, 2 implantation tablets (100 mg each) are injected subfascially (subcutaneously) to a depth of 4 cm. This procedure is repeated 4 times, placing the tablets in a star-shaped fashion around the incision site, parallel to the skin surface. The total dose is 800-1000 mg (8-10 tablets). The incision is closed with a suture followed by a sterile dressing. The procedure can be repeated after 8-9 months.
When the tablets are implanted too close to the incision, a rejection phenomenon may occur. As a result of friction with the belt or premature removal of sutures, suppuration may occur at the implant site.
Due to the properties of disulfiram: drowsiness, nausea, vomiting, metallic taste or taste of garlic in the mouth, malodor in patients with colostomy (associated with carbon sulfide), damage to hepagocytes, rare cases of tenatitis (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, transient impotence, fatigue, allergic dermatitis. In rare cases, psychotic reactions have been noted, including depressive, paranoid states, schizophrenia, mania.
Associated with disulfiram-ethyl alcohol combination: cases of respiratory failure, cardiovascular collapse, heart rhythm disturbances are described;
Hypersensitivity to disulfiram and thiocarbaminates.
The state of alcoholic intoxication, the consumption of drinks containing ethyl alcohol 12 hours before the procedure.
Established heart failure, coronary heart disease, arterial hypertension, previously transferred peripheral circulatory failure.
Mental disorders, psychosis (not counting previous acute alcoholic psychoses), history of suicide attempts. Lactation.
Preparations containing disulfiram should not be used without the conscious consent of the patient.
Use during pregnancy and lactation
When recommending disulfiram to pregnant patients, consideration should be given to the benefit of treatment to the mother versus the potential risk to the fetus, taking into account the adverse effects of alcoholism. Rare cases of congenital malformations have been noted in infants whose mothers used disulfiram in combination with other drugs.
It is not recommended to use disulfiram while breastfeeding. There is no data on the penetration of disulfiram into the milk of a woman; however, the use of the drug during breastfeeding should be excluded, especially in the case when there is a possibility of interaction with drugs taken by the child.
Before implantation, a course of gradual weaning of the patient from ethanol should be carried out. When treating with disulfiram, a strict ban on the use of alcoholic beverages is imposed. Drinking alcohol while taking disulfiram can cause life-threatening symptoms. Therefore, the drug can only be used with the consent of the patient and provided that he is informed about the dangers associated with the use of alcohol when using the drug. The remedy can be used after a very detailed history and consideration of all the advantages and disadvantages of such treatment for alcoholism.
Signs of alcohol intolerance may also occur after the use of liquids containing alcohol (for example, mouthwashes, sauces, vinegar, cough syrup, warmers, aftershave lotions, and other cosmetics containing alcohol).
When using disulfiram, care must be taken in patients with renal or hepatic insufficiency, diseases of the respiratory or cardiovascular system, diabetes mellitus, epilepsy. The disulfiram reaction can lead to a deepening of these diseases.
Polyneuropathy, which may occur with the use of the drug, disappears when the vitamins of the group. B are prescribed or the implanted tablets are removed. A small tubercle often forms at the site of implantation due to fibrosis of the skin and subcutaneous fat. In the case of simultaneous administration with oral anticoagulants, it is necessary to more frequently monitor the content of prothrombin and adjust the doses of anticoagulants, which is associated with an increased risk of bleeding.
There is no data on the effect of the drug on the ability to drive a car and maintain moving mechanical devices.
Disulfiram has low toxicity. In case of accidental ingestion of a large number of tablets, gastric lavage is recommended (if no more than an hour has passed since the ingestion) and observation of the patient.
Disulfiram enhances the action of antithrombotic drugs, antipyrine, phenytoin, chlordiazepoxide and diazepam, by inhibiting their metabolism.
Animal experiments indicate a similar effect on the metabolism of peptidine, morphine and amphetamine.
- Amitriptyline and chlorpromazine can increase, and diazepam - weaken the symptoms of the so-called. disulfiram reaction.
- Disulfiram inhibits oxidation reactions and the excretion of rifampicin by the kidneys.
- The simultaneous use of isoniazid and disulfiram can affect the functioning of the central nervous system and cause dizziness, impaired coordination of movements, irritability, insomnia.
- Metronidazole and disulfiram, used simultaneously, can cause confusion and psychotic states. It is not recommended to use these drugs at the same time.
- Contact with organic solvents containing alcohol, acetaldehyde or paraldehyde during treatment with disulfiram may lead to a disulfiram reaction.
- Disulfiram may prolong the duration of action of alfentanil.
- This is an active substance that is part of many drugs used to treat alcohol dependence.
The use of Disulfiram is justified in cases where a person cannot consciously refuse alcohol. This substance disrupts the process of neutralization of ethyl alcohol in the body, because of which a person experiences very unpleasant sensations:
- feels heat and flushes to the face and head,
- strong and rapid heartbeat,
- pain in the sternum.
However, it is these manifestations that make a person averse to alcohol. Patients begin to perceive alcohol negatively, realize the complexity of the situation and make every effort to return to normal life.
Doctors prescribe Disulfiram to patients only when other, weaker drugs do not help. Under the supervision of a doctor, the patient takes the drug Disulfiram, and then drinks a certain amount of alcohol.
Pharmacological action of disulfiram based on the interruption in the human body of a chain of biochemical reactions.
- Disulfiram blocks the enzyme acetaldehyde dehydrogenase, which is produced in the liver.
- As a result, the human body does not detoxify alcohol, which naturally proceeds with the formation of acetaldehyde.
- When taking Disulfiram, the corresponding process blocks the excretion of alcohol in the form of water and carbon dioxide.
When a person under the supervision of a doctor drinks another portion of alcohol, a large amount of acetaldehyde appears in the body. Poisoning occurs, severe intoxication occurs, accompanied by a host of unpleasant symptoms:
- nausea,
- vomiting,
- heart palpitations
- difficult breathing, etc.
A person in such a serious condition has a fear of death. This state is called disulfiram-ethanol reaction.
Experiencing a very unpleasant and painful condition, a person suffering from alcoholism begins to experience an aversion to alcoholic beverages. He has a conditioned reflex, an intolerance reaction is formed.
Release form
The commercial names of preparations containing the substance disulfiram are different. The drug Disulfiram is produced in various forms:
- there are pills with the same name,
- solution for intravenous and intramuscular administration,
- drops,
- gel.
Also used to combat alcoholism and implantation pills.
Tablets
Disulfiram tablets have different dosages. They are used to treat chronic alcoholism, in the event of binges during therapy.
In the form of tablets, the drug is taken in the morning, before meals. Start taking with a serving of 500 mg. per day, but gradually reduce the dosage of Disulfiram.
The drug is rapidly absorbed and enters the bloodstream. Further, the supply of the active substance is created in adipose tissue. The drug is excreted from it very slowly, which ensures its long-term effect.
Tablets for implantation
For the implantation of tablets, an operation is performed, during which precautions must be observed. Since surgery is the most difficult way to administer the drug, it is performed in extreme cases, if necessary, during patient coding, as well as in case of nickel intoxication.
- Implantation is performed under local anesthesia.
- The doctor makes a small cruciform incision in the iliac region, which is located between the lower ribs and pelvic bones, under the shoulder blade, or in the buttocks.
- During the operation, 2 implant tablets are inserted into the body.
- And this procedure must be repeated four times. That is, in total in the patient's body is eight tablets of disulfiram.
- After closing the wound and applying a dressing, the patient is under the influence of Disulfiram, which now does not need to be taken.
Disulfiram quickly appears in the blood. Despite the fact that the concentration of this substance in the blood is not very high, the drug works very well. And its activity is observed even after 8-9 months. This is due to the fact that Disulfiram is deposited in adipose tissue and is slowly excreted from it.
In the event that a patient who has received an implant takes a dose of alcohol, the blood flow is greatly accelerated, the flow of the substance into the blood increases.
In the area where the pills were sewn under the skin, the person will have a small painless skin tubercle.
Ampoules for intravenous injections
Intravenous administration of disulfiram is the fastest way to deliver a substance into the bloodstream. Immediately after the injection of the drug, the patient will not feel anything: the effect appears after about 3-4 days, and the accumulated effect lasts another two weeks after stopping treatment.
After the injection of Disulfiram, its main substance accumulates all the same in adipose tissue. This method of introducing the drug into the body does not actually affect the human metabolism in any way. But if the patient who is being injected has cirrhosis of the liver, the number of metabolites in the blood will increase.
Excretion of the drug is carried out by the kidneys and lungs: the substances of its decay are eliminated with urine and exhaled air. A separate part of Disulfiram is excreted through the intestines.
Intramuscular injections of disulfiram
An intramuscular injection of the drug is not very painful, Disulfiram is administered with a syringe. The infiltrate of the substance, entering the body, is slowly absorbed. And when drinking alcohol, a disulfiram-ethanol reaction occurs.
As already mentioned, a person begins to experience a terrible condition, accompanied by very unpleasant symptoms.
Of course, the effect of the drug Disulfiram is similar, regardless of the form in which it enters the body. It is important to pay special attention to the fact that during the treatment with Disulfiram, the patient is forbidden to use any drugs and alcohol-based tinctures.
Contraindications
It's a pretty strong drug. It is prescribed strictly by a doctor for certain indications. Disulfiram has many contraindications and side effects. We list only the most basic ones:
- sensitivity to the drug and its active substance;
- diseases of the cardiovascular system;
- diseases of the organs of vision and hearing in a very severe form;
- diabetes mellitus type I and II;
- asthma, various pathologies of the lungs;
- diseases of the liver and kidneys;
- malignant tumors;
- serious diseases of the nervous system;
- mental disorders;
- epilepsy and seizures.
Disulfiram is strictly contraindicated in pregnant and lactating women.
With great care, the drug is used if the patient is in old age or old age, if the patient has mental disorders.
Of course, if there are contraindications, the narcologist will help the patient choose a drug that is an analogue of Disulfiram. In general, there are many analogues of this drug, they make up a whole group of medicines.
Side effects
- Treatment with Disulfiram may be accompanied by unpleasant symptoms, as the drug has a number of side effects.
- So, when taking Disulfiram, patients may experience a metallic taste in the mouth. Also, the drug can contribute to the exacerbation of various chronic diseases, the emergence and progression of psychosis.
- A complex implantation procedure is also fraught with complications: patients may experience allergic reactions, suture divergence, etc.
Since Disulfiram is a serious and potent drug, if any of the described side effects appear, as well as other negative reactions of the body, it is necessary to urgently seek medical help in order to avoid exacerbation and the onset of coma.
Disulfiram Neutralization Process
The drug Disulfiram causes a long-term rejection of alcohol in the patient. There are times when a person who becomes addicted to alcohol and is being treated with a drug suddenly decides to stop this treatment.
Of course, such a decision looks unreasonable, since the already begun therapy should not be interrupted, it is better to bring it to the end. Nevertheless, often alcoholics begin to be treated at the coercion of relatives, at the request of relatives.
But it happens that a person simply does not tolerate the drug. Sometimes the patient cannot stand abstinence and, despite all the prohibitions, consumes alcohol. Sometimes alcohol-containing substances enter the body by accident, by mistake. And now the person understands that he is not able to survive the subsequent reaction of the body. In this case, he makes an appropriate request to the hospital or clinic.
Patient a neutralizing antidote is administered, which reduces therapy to zero. Re-treatment with disulfiram after such administration of an antidote will be much less effective.
The antidote of Disulfiram does not allow a person to return to the original state in which he was before taking the drug. The weak effect of the encoding still continues, and the patient does not cease to experience fever and all the symptoms characteristic of a hangover.
200 to 1000 rubles. Implants and oil solution of Disulfiram cost from 600 to 2400 rubles.
