Antakson

General characteristics. Structure:

Active ingredient: 50 mg of naltrexone of a hydrochloride.

Excipients: lactoses monohydrate, magnesium stearate.

Structure of the capsule: titanium dioxide, gelatin, indigo carmine.

Pharmacological properties:

Naltrexone is a specific antagonist of opioid receptors. Competitively contacts opioid receptors of all types and warns or eliminates effect of both endogenous opioids, and exogenous opioid drugs - narcotic analgetics and their substitutes. It is possible to weaken or eliminate with administration of opioids in the increased doses action of this antagonist.

Pharmacodynamics. Naltrexone has no significant own pharmacological properties, except for some narrowing of a pupil. In a dose of 50 mg naltrexone within 24 hours blocks the pharmacological effects caused by intravenous administration of 25 mg of heroin. At a doubling of a dose of naltrexone this his action is extended till 48 o'clock, and when tripling - till 72 o'clock.

Drug does not cause accustoming and medicinal dependence.

Pharmacokinetics. Naltrexone is well soaked up after intake and for 95% is metabolized in a liver with formation pharmacological of active metabolites. The main metabolite - 6 - beta naltrexone - also has properties of the competitive opioid antagonist. Except it it is formed 2 - hydroxy - 3 - метокси - 6 - beta naltrexone. The maximum concentration of naltrexone and 6 - beta naltrexone in a blood plasma is observed in 1 hour after administration of drug. Drug well gets through gistogematichesky barriers - the volume of distribution makes 1350 l.

Semi-removal time in a blood plasma for naltrexone - 4 hours, for his metabolite 6 - beta naltrexone - 13 hours that explains his ability to cumulation. Naltrexone and his metabolites are exposed to intra hepatic recirculation. Drug is removed through kidneys in not changed look (about 1%) and in the form of metabolites (38% in the form of free and connected 6 - beta naltrexone).

Indications to use:

Complex therapy of opioid drug addiction (dependence) for the purpose of maintenance at a sick state at which opioids will not be able to have characteristic effect. Drug is appointed only after stopping of an abstinence syndrome. Use of AHTAKCOHA is begun in specialized departments on treatment of drug addiction in 7-10 days after the last reception of opioid drug. Further during out-patient treatment of the patient has to be under medical control. The patient has to have a positive installation on treatment of drug addiction. Complex therapy of alcoholism, including at a maintenance therapy, in the same dosages, as at heroin drug addiction against the background of psychotherapy.

Route of administration and doses:

Treatment of heroin drug addiction. Phase of introduction to a course of therapy by Antakson. Treatment by Antakson can be begun not earlier than in 7-10 days after the last reception of opioid drug and on condition of lack of symptoms of an abstinence syndrome. Abstention from drug taking is determined by results of the analysis of urine on the content of opioids. Treatment is not begun until provocative test with intravenous administration of 0,5 mg of Naloxonum does not become negative. Naloksonovy test is not carried out by the patient with symptoms of an abstinence syndrome or at detection of opioids in urine. Repeatedly naloksonovy test can be carried out in 24 hours. The first dose of Antakson usually makes 20 mg of solution for intake. At absence within an hour of signs of a withdrawal the patient is given the rest (30 mg) of a day dose of drug. The doctor should control the act of a proglatyvaniye of solution of drug.

Maintenance therapy Antakson. After the termination of an introduction phase appoint 50 mg of Antakson each 24 hours (this dose enough for the prevention of action of 25 mg of intravenously entered heroin).

It is possible to use also other schemes of treatment:

1. 50 mg of Antakson are appointed daily during the first five days of the week and 100 mg in to the 6th day;
2. 100 mg of Antakson appoint each 2 days or to 150 mg there are each three days;
3. 100 mg of drug appoint in 1 day (e.g. Monday), 100 mg in the 2nd day (e.g. Tuesday) and 150 mg to the 5th day (on Friday). This scheme is convenient for patients with installation on long deprivation of opioids. The minimum course - of 3 months, the recommended course - of 6 months.

Treatment of alcoholism. Daily reception of 50 mg of Antakson, the minimum course - 3 months.

Features of use:

Antakson it is necessary to cancel not less than for 48 h to surgical intervention at which purpose of opioid analgetics is required. The patient has to have at himself a card of purposes of AHTAKCOHA for information of other medics in case of need of rendering acute management. In need of overcoming blocking of opioid receptors (the general anesthesia, anesthesia in urgent cases) it is necessary to use the increased doses of short-range opioid analgetics for reduction of risk of respiratory depression and blood circulation.

Influence on ability to driving of motor transport and to control of mechanisms. In the recommended doses drug does not influence the work demanding bystry reaction and control of vehicles.

Side effects:

In therapeutic doses AHTAKCOH usually does not cause serious side effects in patients whose organism does not contain opioids.

With a frequency more than 10% both prior to treatment of AHTAKCOHOM, and against the background of its use for patients were noted: sleep disorders, alarm, acrimony, abdominal pains, nausea and vomiting, weakness, headaches, muscle and joints pains. With a frequency less than 10%: loss of appetite, lock or diarrhea, psychomotor excitement, dizziness, skin rashes, feeling of a fever, decrease in a sexual potentiality, delay of an ejaculation.

In isolated cases increased fatigue, confusion of consciousness, a depression, hallucinations and nightmares, a photophobia, cough are noted. At laboratory diagnosis increase in activity of transaminases in blood, a lymphocytosis is possible.

As noted symptoms met identical frequency both prior to treatment, and against the background of use of AHTAKCOHA, them, apparently, it is impossible to consider manifestations of side effect of drug.

One case of an idiopathic Werlhof's disease at the patient who, perhaps, was сенсибилизирован to ANTAKSONU during the previous treatment is described; recovery happened after drug withdrawal and carrying out a course of corticosteroid therapy.

Interaction with other medicines:

Some drugs containing opioids (antibechic, antidiarrheal means, narcotic analgetics) can not cause desirable effect in the persons accepting AHTAKCOH. In these cases it is necessary to use the alternative drugs which are not containing opioids. Gepatotoksichny drugs increase risk of damage of a liver. Cases of incompatibility with other drugs are not described.

Contraindications:

Use of narcotic analgetics or the positive analysis on the content in urine of opioids. Positive test for availability of opiates in urine. Opioid abstinence syndrome. Lack of data on conducting provocative test with Naloxonum (see the Route of administration and doses).

Hypersensitivity to drugs of naltrexone in the anamnesis of patients. Acute hepatitis or liver failure. Safety of use of AHTAKCOHA for patients more young is not established than 18 years, at pregnancy and in the period of a lactation.

With care: Abnormal liver functions and/or kidneys.

Overdose:

There are no sufficient clinical data about a possibility of overdose of drug now. At suspicion of intoxication it is necessary to appoint a symptomatic treatment.

Storage conditions:

Period of validity - 3 years. Not to use after the date specified on packaging. To store at a temperature not above +30 °C in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules of 50 mg: on 10 capsules in blisters; on 1 blister together with the instruction on a medical use in a cardboard pack.