Antakson - instructions for use, dose, side effects, contraindications

Hard gelatin capsules with a white opaque casing and blue lid, size 4, containing a white powder; The capsule is marked with the company's trademark, there is an inscription on the cap of the capsule "Antaxone® 50".

Pharmacotherapeutic group:Opioid receptor antagonist

ATX: & nbsp

N.07.B.B.04 Naltrexone

Pharmacodynamics:

Naltrexone is a specific antagonist of opioid receptors. Competitively binds to opioid receptors of all types and prevents or eliminates the effect of both endogenous opioids and exogenous opioids - narcotic analgesics and their surrogates.The introduction of opioids in increased doses can weaken or eliminate the effect of this antagonist.

HAltrexone does not have significant pharmacological properties of its own, except for a narrowed pupil. In a dose of 50 mg naltrexone within 24 hours blocks the pharmacological effects caused by intravenous administration of 25 mg of heroin. When doubling the dose of naltrexone, this action is prolonged to 48 hours, and when it is tripled, it lasts up to 72 hours.

The drug does not cause addiction and drug dependence.

Pharmacokinetics:

Naltrexone is well absorbed after ingestion and is metabolized 95% in the liver with the formation of pharmacologically active metabolites. The main metabolite, 6-beta-naltrexone, also has the properties of a competitive opioid antagonist. In addition, 2-hydroxy-3-methoxy-6-beta-naltrexone is formed. The maximum concentration of naltrexone and 6-beta-naltrexone in the blood plasma is observed 1 hour after taking the drug. The drug penetrates well through the histogematic barriers - the volume of distribution is 1350 liters. The half-life in blood plasma for naltrexone is 4 hours, for its metabolite 6-beta-naltrexone - 13 hours,which explains his ability to cumulate. Naltrexone and its metabolites undergo intrahepatic recirculation. The drug is excreted through the kidneys in unchanged form (about 1%) and in the form of metabolites (38% in the form of free and bound 6-beta-naltrexone).

Indications:

Complex therapy of opioid addiction (addiction) in order to maintain the patient's condition, in which opioids can not provide of a characteristic action. The drug is prescribed only after relief of the withdrawal syndrome. The use of ANTACSON is started in specialized drug treatment departments 7-10 days after the last intake of the opioid drug. Further During out-patient treatment the patient should be under medical supervision. The patient should have a positive attitude towards the treatment of drug addiction.

Complex therapy of alcoholism, including with maintenance therapy, in the same dosages as with heroin addiction against the background of psychotherapy.

Contraindications:

The use of narcotic analgesics or a positive analysis for the urinary content of opioids. Positive test for the presence of opiates in urine.

Opioid withdrawal syndrome.

The lack of data on the conduct of the provocative test with naloxone (cf. Method of administration and dose).

Hypersensitivity to naltrexone drugs in a history of patients.

Acute hepatitis or liver failure.

The safety of ANTACSON has not been established in patients under the age of 18, during pregnancy and during lactation.

Carefully:Impaired liver and / or kidney function.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Treatment of heroin addiction.

The phase of introduction to the course of ANTASCON therapy.

Treatment with ANTACSON can be started no earlier than 7-10 days after the last reception of the opioid drug and provided there are no signs of withdrawal symptoms. Abstinence from taking drugs is determined by the results of a urine test for the content of opioids. Treatment does not begin until a provocative trial with an intravenous injection of 0.5 mg of Naloxone becomes negative. Naloxone test is not performed for patients with signs of withdrawal symptoms or when opioids are detected in urine. The naloxone test can be repeated after 24 hours.

The first dose of ANTACSON is usually 20 mg of the oral solution.If there are no signs of withdrawal within an hour, the patient is given a residue (30 mg) of the daily dose of the drug. The doctor should monitor the act of swallowing the drug solution.

Supportive therapy with ANTACSON.

After the end of the introductory phase, 50 mg of ANTACSON is prescribed every 24 hours (this dose is sufficient to prevent the action of 25 mg of intravenously injected heroin).

You can use other treatment regimens:

1. 50 mg of ANTACSON is administered daily for the first five days of the week and 100 mg per day for 6 day;

2. 100 mg of ANTACSON is administered every 2 days or 150 mg every three days;

3. 100 mg of the drug is administered in 1 day (e.g. Monday), 100 mg in 2 day (e.g. Tuesday) and 150 mg on Day 5 (Friday). This scheme is convenient for patients with a long-term disinfection of opioids.

The minimum course is from 3 months, the recommended course is from 6 months.

Treatment of alcoholism.

Daily intake of 50 mg of ANTACSON, minimum course - 3 months.

Side effects:

In therapeutic doses in patients who do not contain opioids, ANTAXON usually does not cause serious side effects.

With a frequency of more than 10% as before the start of treatment, ANTACSONOM, and against the background its nChanges in patients were noted: sleep disorders, anxiety, increased irritability, abdominal pain, nausea and vomiting, weakness, headaches, muscle pains and joints.

Less than frequency 10%: decreased appetite, constipation or diarrhea, psychomotor agitation, dizziness, skin rashes, feeling chills, decreased sexual potency, deceleration of ejaculation.

In isolated cases, increased fatigue, confusion, depression, hallucinations and nightmares, photophobia, cough.

At laboratory diagnostics it is possible to increase the activity of transaminases in the blood, lymphocytosis.

Since these symptoms were observed with equal frequency both before the start of treatment and against the background of ANTACSON, they, apparently, can not be considered as side effects of the drug.

One case of idiopathic thrombocytopenic purpura has been described in a patient who may have been sensitized to ANTACSON during the previous treatment; recovery occurred after the drug was discontinued and a course of corticosteroid therapy was administered.

Overdose:Sufficient clinical data on the possibility of drug overdose is currently not available.If suspected of intoxication, symptomatic treatment should be prescribed.

Interaction:

Some drugs containing opioids (antitussives, antiparasitics, narcotic analgesics) may not produce the desired effect in persons taking ANTAXON. In these cases, alternative drugs that do not contain opioids should be used. Hepatotoxic drugs increase the risk of liver damage. Cases of incompatibility with other drugs are not described.

Special instructions:

Antakson should be discontinued no less than 48 hours prior to surgery, which requires the appointment of opioid analgesics. The patient should carry an ANTACSON appointment card for the information of other health workers in case of emergency. If it is necessary to overcome the blocking of opioid receptors (general anesthesia, anesthesia in urgent cases), use increased doses of short-acting opioid analgesics to reduce the risk of respiratory and circulatory depression.

Effect on the ability to drive transp. cf. and fur:

In recommended doses, the drug does not affect the work requiring quick response and vehicle management.

Form release / dosage:

Capsules 50 mg.

Packaging:10 capsules in blisters; 1 blister together with instructions for medical use in a cardboard box.

Storage conditions:

Store at temperatures below + 30 ° C out of the reach of children.

Shelf life:3 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N010204

Date of registration:31.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:Zambon SpAZambon SpA Italy

Manufacturer: & nbsp

ZAMBON, S.p.A. Italy

Representation: & nbspZAMBON SpA ZAMBON SpA Italy

Information update date: & nbsp05.09.2017

Illustrated instructions

Instructions

Antakson (Antaxone)