Esperal tablets 500mg #20

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Instruction for Esperal

Composition

The composition contains disulfiram, as well as additional ingredients: polyvidone K30, magnesium stearate, carmellose sodium, microcrystalline cellulose.

Form of issue

The drug is available in tablets that have a round shape, white color with a cream tint. On one side of the tablet is a cruciform risk, on the other side - the engraving "ESPERAL". Tablets are packed in polypropylene bottles with a stopper of 20 pieces. The bottle is packed in a cardboard box.
Also, Esperal is available as a special gel, which is used for implantation under the skin.

pharmachologic effect

Tablets and gel Esperal are used for the treatment of alcoholism. The active substance disulfiram acts by providing an acetal dehydrogenase blockade that takes part in the metabolism of ethanol. As a consequence, the body raises the concentration of acetaldehyde, the metabolite of ethanol. This provokes a manifestation of negative feelings in a person (tachycardia, depression of pressure, nausea, vomiting, etc.). Consequently, the reception of alcohol becomes for him a source of extremely negative feelings. As a result, conditioned-reflex aversion to the smell and taste of alcohol is developed.
The greatest therapeutic effect is observed 12 hours after the use of tablets. The effect of the drug may persist for 10-14 days after the treatment was discontinued.
Esperal implant provides an opportunity to maintain a constant level of disulfiram in the human body. It is important to observe the following condition: before an implantation is performed, a person should not take alcoholic beverages for several days.

Pharmacodynamics and pharmacokinetics

The effect of disulfiram is based on the blockade of acetaldehyde dehydrogenase involved in the metabolism of ethyl alcohol.
After taking orally from the gastrointestinal tract, 70 to 90% of disulfiram is absorbed. Then there is a rapid process of metabolism, the substance is reduced to dithiocarbamate, which is either excreted from the body in the form of a glucuron-conjugate, or converted to diethylamine and carbon sulphide. The latter is partially excreted through the human lungs (from 4 to 53%).

Indications for use

The drug is used for the following indications:
    prevention and therapy of recurrences of chronic alcoholism;
    as an additional detoxification agent for nickel poisoning, which is chronic.

Contraindications

The following diseases and conditions are the categorical contraindication to taking the drug:
    severe form of liver failure;
    diabetes;
    epilepsy and cramps of any origin;
    mental illness;
    pregnancy and lactation;
    marked sensitivity to the components of the drug.

Relative contraindications are:

    hypothyroidism;
    renal insufficiency.

Side effects

Before starting treatment with this drug, a person should clearly understand what it is and what side effects may appear during the treatment.
Side effects that occur due to the properties of disulfiram: the sensation of metallic taste in the mouth, the appearance of an unpleasant smell in people with colostomy. In rare cases, optic neuritis, hepatitis, lower extremity polyneuritis, memory impairment, confusion, headaches, asthenia, skin allergies can develop.
Side effects that result from the combination of disulfiram and ethanol: the manifestation of respiratory failure, collapse, neurological disorders, heart rhythm disturbances, angina pectoris, cerebral edema.
With prolonged treatment, the remedy can be noted: psychoses similar to alcoholic, gastritis, hepatitis, exacerbation of polyneuritis. People suffering from cardiovascular diseases can develop a thrombosis of the vessels of the brain. When paresthesia in the face and limbs, you must immediately cancel the remedy.
If a dose of alcohol exceeding 50-80 ml (counting up to 40% ethanol) was taken against the background of taking the drug, serious violations in the functions of the respiratory and cardiovascular systems, convulsions, edema may occur. In this case, an immediate detoxification treatment is performed.

Instructions for use Esperl (Method and dosage)

Before the therapy begins, the patient must undergo a thorough examination. In addition, he must clearly understand how the drug works, and what consequences and complications may occur during its administration.
The instruction for Esperal is as follows: tablets are taken orally for 500 mg. Reception is carried out once, in the morning, during meals. Instructions for use Esperal provides for a gradual reduction in the dose of the drug to 250 mg or 125 mg per day. How to take the remedy and adjust the dose, the doctor will explain in more detail.
After starting treatment after 7-10 days, an alcohol test is performed: 20-30 ml of 40% ethanol is taken after consuming 500 mg of Esperal. If the reaction is weak, the dose of alcohol increases. The maximum dose can be 100-120 ml of 40% alcohol. Then another sample is taken in the hospital 1-2 days later and outpatiently after 3-5 days. Later the drug is used in a daily maintenance dose of 150-200 mg for 1-3 years.
Sewing implants is carried out in the muscle tissue four centimeters deep. As a rule, the filing is carried out in the upper part of the buttocks or in the left iliac region. Initially, disinfection and anesthesia are carried out, then an incision of approximately 6 mm is made. Subcutaneous fat is spread apart with a special tool, after which the drug is injected. A total of 0.8 g of the drug is administered to the patient. After the implantation is completed, a seam and bandage is applied. After sewing Esperal can operate from six months to five years. Coding continues depending on the dose that was applied.

Overdose

In case of an overdose (combining disulfiram-ethanol) it is possible to suppress consciousness, coma, cardiovascular collapse, complications of neurological nature. In this case, symptomatic treatment is performed.

Interaction

Contraindicated taking the drug with alcohol, since in this case there is a reaction of intolerance.
It is undesirable to combine Esperal with isoniazid, since behavioral and coordination disorders are possible.
With the simultaneous use of the drug with 5-nitro-imidazoles, the development of confusion, delirious disorders is likely.
With simultaneous administration with phenytoin, a rapid increase in the concentration of phenytoin in the plasma, toxic symptoms, can be noted.

The following medicines are used with caution:

    Theophylline, since disulfiram inhibits its metabolism. Therefore, the dose of theophylline should be adjusted.
    Warfarin and a number of other oral anticoagulants. There is a danger of bleeding, as the effectiveness of oral anticoagulants is increased. It is necessary to regularly monitor the level of prothrombin in the blood and adjust the dosage of anticoagulants for eight days after disulfiram cancellation.
    Benzodiazepines, since disulfiram increases the level of sedative effects of benzodiazepines, inhibiting their oxidative metabolism.
    Tricyclic antidepressants in the treatment of disulfiram significantly increase alcohol intolerance.

Storage conditions

The product should be protected from access by children, stored in dry places and the temperature should not be above 25 ° C.

Shelf life

You can store Esperal for 3 years.

special instructions

During the time when a person takes Esperal tablets, you can not take alcohol, and take any drugs that contain alcohol.
If the patient uses Esperal gel, tablets against alcoholism, the reaction of his body to simultaneous reception of alcohol can be either fast or detached. In the latter case, the development of toxic hepatitis, which affects the kidneys, liver, pancreas.

Children

Not used to treat children.

With alcohol

If you take Esperal and alcohol at the same time, the consequences can be very serious. There is a marked reaction of intolerance with parallel intake of alcohol. It is necessary to completely exclude alcohol, as well as drugs containing alcohol.

In pregnancy

Contraindicated Esperal treatment in pregnancy and breastfeeding.

Reviews about Esperal

Reviews of the Esperal tablets indicate that patients who used them were able to give up alcohol for the period of treatment, and often stick to a sober way of life after the end. Nevertheless, it should be taken into account that both the gel and the drug in the form of tablets actually cause a very strong negative reaction when taking alcohol, as evidenced by the reviews. People who have been stitched or injected have noted a display of metal taste in the mouth, periodic headaches, allergic reactions and other side effects. It is noted that even with the use of small doses of alcohol, side effects can be very serious.