Antabuse

Tetlong-250 is a substance used in the case of additive disorders (alcohol dependence).

The mechanism of the anti-alcohol effect of drugs is associated with its effect on the metabolism of alcohol inside the body by blocking the activity of enzyme systems that are involved in the transformation of alcohol. At the same time, it also blocks the action of 5-hydroxyindolocetic acid with adrenaline, causing cumulation of acetaldehyde inside the blood, which leads to the appearance of somatovegetative disorders in humans (potentiation of the heartbeat, decrease in blood pressure, tightness in the sternum, chills, horror, etc.).

Indications Tetlonga-250

It is used for therapy in persons with chronic alcoholism (any types and phases of the disease).

Release form

The release of the drug substance is realized in the form of injection fluid, inside ampoules having a volume of 1 ml. Inside the box - 10 ampoules.

Pharmacokinetics

When disulfiram is injected into the muscle tissue at a very high speed, it crystallizes, followed by the formation of a large number of small crystals, and then gradually passes into the blood. High levels of lipid solubility allow disulfiram to be widely distributed inside the body and accumulate inside the fatty tissues.

Disulfiram quite quickly undergoes metabolic processes with the formation of the element of DDC; part of the substance is excreted in the form of carbon disulfide along with the air that the patient exhales, and the other part is involved in intrahepatic metabolism with the formation of methyl-DDC, which is transformed into a component of methyl-DTC with therapeutic activity.

The term half-life of methyl-DTC is approximately 10 hours, and its inhibitory effect on the aldehyde dehydrogenase has a much longer duration. But, although the metabolic elements have a low concentration, manifestations of the type of disulfiram-ethanol can develop over the course of 20 days from the moment of administration of the drug.

In the case of mild or moderate disruption of the liver, metabolic processes are not impaired. In the case of hepatic cirrhosis, there is an increase in blood indicators of metabolites.

Excretion of metabolic elements is mainly implemented with the urine. A certain amount is excreted with the air that a person exhales (in the form of carbon disulfide). Another 20% in the form of permanent disulfiram is excreted with feces.

Dosing and administration

Before the start of therapy, it is imperative to perform a full examination of the patient. You also need to have a conversation with him, in which you should convey that he is strictly forbidden to take drugs or alcohol during therapy. After that, it is necessary to obtain his written consent and receipt that he was warned about the risks of taking drugs and alcohol, as well as about the obligatory observance of the conditions of a long therapeutic and rehabilitation course.

Also, before starting treatment, withdrawal symptoms should be completely eliminated and a general fortifying, detoxifying and symptomatic treatment should be performed. Along with this, it is recommended to perform rational psychotherapy procedures. In addition, for 1-3 days before using the drug should completely abandon the use of tranquilizers, sleeping pills, antipsychotics and antidepressants. Before starting therapy, the patient should be registered with the clinical manifestations of the post-abstinence syndrome: a strong psychological craving for drugs and alcohol, bad mood, severe irritability, sleep disorders, anxiety, loss of appetite and fear.

Intramuscular administration of the drug is performed in the clinic or in the hospital. The medicine in a portion of 1 ml (0.25 g) at low speed (for 0.5-1 minutes) is deeply inserted into the muscle tissue of the buttock (its outer upper quadrant). At this point, the patient must constantly report their subjective feelings that arise during the injection.

For 1-well injection, you can enter a maximum of 0.25 g of the substance. With the treatment of alcoholism is often administered 1 injection per month. In the case of an opioid type of dependence, the number of injection procedures can vary from 1-4 per month.

Given the severity of alcoholism (also one that is combined with drug addiction), the frequency of relapse and the patient’s characterological parameters, the annual treatment cycle can be up to 10 injections.

The occurrence of pathological craving for alcohol during remission is the main criterion for an urgent re-injection of Tetlong-250 - in order to retain long-term therapeutic remission.

[1]

Use Tetlonga-250 during pregnancy

It is forbidden to appoint Tetlong-250 during pregnancy. Before starting therapy, it is necessary to completely eliminate the probability of pregnancy in the patient, and to use reliable contraceptives during the course.

Breastfeeding should be abandoned for the period of treatment.

Contraindications

The main contraindications:

• severe intolerance associated with disulfiram;
• severe stages of diseases affecting the cardiovascular system: atherosclerosis in the vascular region of the brain, severe cardiosclerosis, aortic aneurysm, pre-or postinfarction state, elevated blood pressure values (2–3rd degrees), insufficiency of the coronary type, decompensated pathologies of the cardiovascular system and severe cerebral vascular diseases;
• severe stages of liver function failure;
• endocrine diseases, including hyperthyroidism and diabetes (severe or moderate form);
• epileptiform syndromes and epilepsy (excluding alcohol-related epilepsy);
• pathological neuropsychiatric character in a chronic degree (among them psychosis of manic-depressive type and schizophrenia);
• ulcers in the gastrointestinal tract during the acute stage or with the appearance of bleeding;
• diseases affecting the hematopoietic system;
• neuritis, as well as polyneuritis, affecting the visual or auditory nerve;
• glaucoma;
• combination with isoniazid, phenytoin or metronidazole;
• tuberculosis (also diagnosed for the first time; accompanied by infiltration and hemoptysis);
• having severe or moderate BA severity;
• malignant neoplasms;
• leukopenia or anemia;
• pulmonary emphysema and respiratory failure in severe;
• having obliterating nature of endarteritis;
• cerebral infections of an infectious nature and residual symptoms after a stroke or infection;
• persons over the age of 60;
• eating food or drinks, as well as medicines or cosmetic substances that contain alcohol (within 24 hours from the moment of the introduction of disulfiram);
• a history of psychosis;
• traumatic pathology.

Side effects Tetlonga-250

Among the side effects:

• Disorders in the work of the National Assembly: mono- or polyneuropathy, optic neuritis often observed, and polyneuritis affecting the legs, drowsiness, disorientation, memory impairment, headaches, and neuropsychiatric disorders. Sometimes epileptiform seizures develop;
• problems with digestive function: taste of metal. Sometimes there is a loss of appetite, diarrhea, vomiting, hepatitis or jaundice;
• allergy symptoms: itching or epidermal rash;
• sexual dysfunction: a single weakening of potency;
• manifestations associated with the compound disulfiram-ethanol: heart rhythm disorders, myocardial infarction, collapse, cerebral edema, and angina pectoris attacks. In addition, there may develop coronary insufficiency with a decrease in cardiac function, arrhythmic shallow breathing (or its complete stop), as well as cyanosis in the area of the nails or lips;
• others: sore throat or dry-type cough, severe fatigue, fear, a sharp medicinal breath, and severe pain in the injection area with the development of radiation in the leg, as well as warmth in the throat. Sometimes there may be an increase in temperature to 37-38 ^o C, darkening of the color of urine and anuria of a reflex nature;
• change of indications of analyzes: indications of hepatic tests can change.

Overdose

In case of intoxication, potentiation of adverse symptoms occurs, encephalopathy or extrapyramidal signs develop; there is also confused consciousness. In case of severe disorders, there is an insufficiency of the CAS function and a coma.

Symptomatic actions are carried out. In case of severe disorder, the patient is placed horizontally, with a heater in the legs, and they also give off ammonia and inject C-vitamin and glucose into / in the method.

If cardiac function is impaired, corazol, cordiamine, caffeine or camphor are used.

In the case of a fall in blood pressure levels, ephedrine, strychnine, adrenaline, as well as methazone and prednisone are used. P / k method is used lobelin or cititon; also need to inhale carbogen.

During epileptiform seizures, a 25% magnesia sulfate liquid (5 ml), diluted in 40% glucose (20-40 ml), and 2-4 ml of seduxen is injected. Perform another enema with hydrochloride.

Interactions with other drugs

Combining medication with coumarin anticoagulants (among them warfarin) leads to potentiation of anticoagulant activity and increases the likelihood of bleeding.

Disulfiram inhibits the effect of hepatic enzymes, which is why using together with substances whose metabolic processes take place inside the liver can disrupt their metabolism.

The combination of the drug and derivatives of phenothiazine, tricyclics, as well as the MAOI causes the likelihood of the appearance of negative symptoms associated with drug interactions.

Introduction together with buspirone in theory can trigger the development of mental disorders (such as mania).

Use with disulfiram reduces the clearance values of imipramine with desipramine.

The combination of Tetlong-250 and amitriptyline can potentiate the drug activity of disulfiram, but this can also increase the toxic effect of amitriptyline on the central nervous system.

Introduction in combination with chloridasepoxide and diazepam increases their plasma values, which sometimes leads to dizziness. Exposure to diazepam may reduce the severity of the effect of disulfiram-alcohol. There is a possibility of potentiation of the toxic properties of temazepam.

Administration with isoniazid can cause depression and dizziness; caffeine - causes a decrease in the rate of excretion of this element from the body; use with metronidazole leads to confusion and the development of psychosis in the active phase; use with omeprazole can cause catatonia and disorders of consciousness.

When combining drugs with perphenazine, there is a likelihood of development of psychotic manifestations.

Use simultaneously with rifampicin causes a slowdown of its metabolic processes and excretion.

The combination of medication and phenazone prolongs the term half-life of the latter.

Use with phenytoin and other benzodiazepine derivatives, and in addition with morphine, barbiturates and pentidine, potentiates the side effects and therapeutic effects of these drugs (due to an increase in their plasma values); also signs of intoxication appear.

The combination with chlorzoxazone increases its plasma values.

Administration with chlorpromazine may potentiate a decrease in blood pressure.

There is information about the emergence of drug interactions with substances such as amphetamines and bupropiron with methylphenidate.

[2], [3]

Storage conditions

Tetlong-250 is required to be stored in a dark place, closed to children. It is forbidden to freeze the liquid. Temperature indicators - a maximum of 25 ° C.

Shelf life

Tetlong 250 can be used for a 36-month period from the date of manufacture of the pharmaceutical substance.

[4]

Application for children

It is forbidden to use the medicine in pediatrics.

Analogs

Analogues of the drugs are the agents Antakson, Naltrexin, Lidevin with Biotredin, Teturam and Vivitrol with Medichronal and Disulfiram, and in addition Esperal, Colme and Naltrex.