Esperal

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

The mechanism of the anti-alcoholic effect of drugs is associated with its effect on the metabolism of alcohol within 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-hydroxyindolocytic acid with adrenaline, which causes the accumulation of acetaldehyde inside the blood, which leads to the appearance of somatovegetative disorders in a person (potentiation of the heartbeat, a decrease in blood pressure, tightness in the sternum, chills, a feeling of horror, etc.). [1]

Indications Tetlong-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 an injection liquid, inside ampoules with a volume of 1 ml. There are 10 ampoules inside the box.

Pharmacokinetics

Disulfiram, introduced into the muscle tissue, crystallizes at a very high speed, followed by the formation of a large number of small crystals, and then gradually passes into the blood. High rates of lipid solubility allow disulfiram to be widely distributed inside the body and accumulate inside adipose tissues. [2]

Disulfiram quickly enough undergoes metabolic processes with the formation of the DDC element; part of the substance is excreted in the form of carbon disulfide together with the air exhaled by the patient, and the other part is involved in intrahepatic metabolism with the formation of methyl-DDC, which is transformed into the component methyl-DTC with therapeutic activity. [3]

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

In the case of mild or moderate disturbances in the liver, metabolic processes are not weakened. Moreover, in the case of hepatic cirrhosis, an increase in the blood parameters of metabolites occurs.

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

Dosing and administration

Before starting therapy, it is imperative to complete a full examination of the patient. Also, you need to have a conversation with him, in which you should convey that he is strictly prohibited from taking drugs or alcohol during the period of therapy. After that, it is necessary to obtain his written consent and a receipt that he was warned about the risks of taking drugs and alcohol, as well as about the obligation to comply with the conditions of a long therapeutic and rehabilitation course.

Also, before starting treatment, it is necessary to completely eliminate the withdrawal symptoms and perform a course of general strengthening, detoxification and symptomatic treatment. At the same time, it is recommended to perform rational psychotherapy procedures. In addition, 1-3 days before using drugs, you must completely abandon the use of tranquilizers, hypnotics, antipsychotics and antidepressants. Before starting therapy, the patient should be registered with the clinical manifestations of post-withdrawal syndrome: strong psychological craving for drugs and alcohol, bad mood, severe irritability, sleep disorders, anxiety, loss of appetite and fear.

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

For 1 injection, a maximum of 0.25 g of the substance can be administered. In the treatment of alcoholism, 1 injection is often administered per month. In the case of opioid addiction, the number of injection procedures can vary from 1 to 4 per month.

Taking into account the severity of alcoholism (also one that is combined with drug addiction), the frequency of relapses and the patient's characterological parameters, the annual treatment cycle can be up to 10 injections.

The emergence of a pathological craving for alcohol during remission is the main criterion for an urgent repeated injection of Tetlong-250 - in order to maintain a long-term therapeutic remission.

• Application for children

It is forbidden to use the medicine in pediatrics.

Use Tetlong-250 during pregnancy

It is forbidden to prescribe Tetlong-250 during pregnancy. Before starting therapy, it is required to completely exclude the possibility of pregnancy in the patient, and during the course to use reliable contraceptives.

For the period of treatment, you need to stop breastfeeding.

Contraindications

The main contraindications:

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

Side effects Tetlong-250

Among the side signs:

• disorders in the work of the NS: often there is mono- or polyneuropathy, neuritis in the optic nerve, polyneuritis affecting the legs, drowsiness, disorientation, memory impairment, headaches and disorders of a neuropsychic nature. Epileptiform seizures sometimes develop;
• digestive problems: metal taste. Sometimes there is loss of appetite, diarrhea, vomiting, hepatitis, or jaundice;
• allergy symptoms: itching or epidermal rash;
• sexual dysfunction: a single weakening of potency occurs;
• manifestations associated with the compound disulfiram-ethanol: heart rhythm disorders, myocardial infarction, collapse, cerebral edema and angina attacks. In addition, insufficiency of coronary activity may develop 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 cough, severe fatigue, fear, sharp medicinal odor from the mouth and severe pain in the injection area with the development of irradiation in the leg, as well as warmth in the throat. Sometimes there may be an increase in temperature up to 37-38 ° C, darkening of the color of urine and anuria of a reflex nature;
• change in test readings: liver test readings may change.

Overdose

With intoxication, there is a potentiation of side symptoms, the development of encephalopathy or extrapyramidal signs; confusion is also observed. In severe disorders, there is a failure of the CVS function and a coma.

Symptomatic actions are performed. In case of severe disorder, the patient is laid horizontally, with a heating pad in his legs, and is also allowed to smell the ammonia and inject C-vitamin and glucose intravenously.

If cardiac function is weakened, corazole, cordiamine, caffeine, or camphor are used.

In case of a drop in blood pressure, ephedrine, strychnine, adrenaline, as well as metasone and prednisolone are used. Lobelin or cititon is used in the s / c method; you also need to inhale carbogen.

During epileptiform seizures, 25% liquid magnesium sulfate (5 ml), diluted in 40% glucose (20-40 ml), as well as 2-4 ml of seduxen are injected. An enema with hydrochloride is also performed.

Interactions with other drugs

The combination of drugs with coumarin anticoagulants (including warfarin) leads to potentiation of anticoagulant activity and increases the likelihood of bleeding.

Disulfiram inhibits the effect of liver enzymes, which is why the use together with substances whose metabolic processes are carried out inside the liver can lead to a violation of their metabolism.

The combination of a drug and derivatives of phenothiazine, tricyclics, and MAOIs causes the likelihood of negative signs associated with drug interactions.

The introduction together with buspirone in theory can provoke the development of mental disorders (such as mania).

The use together 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 the toxic effect of amitriptyline on the central nervous system can also increase.

Administration in combination with chlorideasepoxide and diazepam increases their plasma values, which sometimes leads to dizziness. Exposure to diazepam can weaken the severity of the effect of disulfiram alcohol. There is a possibility of potentiating the toxic properties of temazepam.

Administration together with isoniazid can provoke depression and dizziness; with 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 impaired consciousness.

When combining drugs with perphenazine, there is a possibility of developing psychotic manifestations.

Simultaneous use with rifampicin slows down its metabolic processes and excretion.

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

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

The combination with chlorzoxazone increases its plasma values.

Administration with chlorpromazine can potentiate a decrease in blood pressure.

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

Storage conditions

Tetlong-250 must be kept in a dark place out of the reach of children. It is forbidden to freeze liquid. Temperature readings - maximum 25 ° С.

Shelf life

Tetlong-250 can be used within 36 months from the date of manufacture of the pharmaceutical substance.

Analogs

Analogs of the drug are Antaxon, Naltrexin, Lidevin with Biotredin, Teturam and Vivitrol with Medichronal and Disulfiram, and besides Esperal, Kolme and Naltrex.