2010/09/21

Antaxone

Composition, structure and packing

Hard gelatin capsules with white opaque body and blue cap, with the image of the trademark company in case the capsule and the inscription "Antaxone 50" - on the lid, the contents of capsules - a white powder.

1 capsule. naltrexone hydrochloride 50 mg.

Excipients: lactose monohydrate, magnesium stearate. The composition of the shell capsules: gelatin, titanium dioxide, indigo.

Clinico-pharmacological group: Competitive antagonist of opioid receptors.

Pharmacological action

The specific antagonist of opioid receptors. Competitive binds to opioid receptors of all types and prevents or eliminates the effect of both endogenous opioids and exogenous opioid drugs - opioid analgesics and their surrogates. The introduction of increased doses of opioids can reduce or eliminate the effect of the antagonist. Antakson not have its own significant pharmacological properties, except for a narrowing of the pupil. Antakson not cause addiction and drug dependence.

At a dose of 50 mg.

Antakson for 24 h blocked the pharmacological effects caused by in / administration of 25 mg of heroin. With increasing doses Antaksona 2 times blocking effect is prolonged to 48 h, and 3 times - up to 72 h. Pharmacokinetics

Absorption and distribution

After oral naltrexone is well absorbed from the gastrointestinal tract, Cmax of naltrexone and its active metabolite 6-beta-naltreksola achieved in 1 h. The drug was well penetrates through tissue barriers, Vd is 1350 liters. Metabolism 95% of the dose naltrexone biotransformiruetsya in the liver with the formation of pharmacologically active metabolites, the chief of which - 6-beta-naltreksol as an antagonist opioids. The second metabolite - 2-hydroxy-3-methoxy-6-beta-naltreksol. Naltrexone and its metabolites are intrahepatic recycling.

Withdrawal

Naltrexone and its metabolites are derived primarily by the kidneys. Less than 1% of the dose of naltrexone is excreted in the urine in unchanged form, the remainder appears in the form of metabolites (including 38% - in the form of free and bound 6-beta-naltreksola). The average T1 / 2 of naltrexone - 4 h, 6-beta-naltreksola - 13 h, which explains his ability to cumulation.

Statement
in the complex therapy of opioid addiction (dependence) in order to maintain the patient condition in which opioids would not be able to provide the characteristic action; drug prescribed only after cupping withdrawal syndrome.

Application Antaksona begin in specialized departments of drug treatment in 7-10 days after receiving opioid drugs. Later, the patient should be under strict medical supervision, the patient should be a positive setting for treatment of drug addiction;
in the complex therapy of chronic alcoholism (including for maintenance therapy) in the same doses as with heroin addiction, on a background of psychotherapy.

Dosage regimen

Treatment of heroin addiction

Phase induction therapy Antaksonom

Treatment

Antaksonom can be started no earlier than 7-10 days after the last reception of drugs and in the absence of signs of withdrawal syndrome. Abstention from the use of drugs is determined by results of urine analysis for the maintenance of opioids.

Treatment

Antaksonom not start up until the provocative test with a / in the introduction of 500 mcg of naloxone does not become negative. Naloksonovaya test is not conducted in patients with signs of withdrawal symptoms or detection of opioids in the urine. Re naloksonovuyu test can be carried out within 24 hours Recommended first Antaksona single dose is 20 mg by mouth (as a solution).

In the absence of symptoms within 1 h of withdrawal symptoms the patient can be given the remainder of the daily dose (30 mg). The physician should monitor drug ingestion by the patient.

Supportive therapy Antaksonom

After the introduction phase Antakson prescribe a dose of 50 mg every 24 h (this dose is enough to block the action of 25 mg of heroin introduced in the present). You can use the other treatment regimens. 1. 50 mg Antaksona prescribed daily during the first 5 days of the week and 100 mg on Day 6. 2. 100 mg. Antaksona appointed every 2 days or 150 mg every 3 days. 3. 100 mg.Antaksona administered in 1 day (eg Monday), 100 mg in 2 day (Tuesday) and 150 mg on Day 5 (Friday). This scheme is suitable for patients with the installation of a long deprivation of opioids. Minimum course of treatment - 3 months; recommended - from 6 months.

Treatment of chronic alcoholism

The drug is prescribed daily dose of 50 mg 1 time / day. Minimum course of treatment - 3 months.

Treatment does not begin until until done naloksonovaya test to exclude the presence of opioids in the body.

Side effect

When applying for Antaksona testimony in therapeutic doses in patients in an organism which does not contain opioids, the development of serious side effects are usually not observed. With a frequency of more than 10% (as before treatment Antaksonom, and on the background of its use) in patients were observed: sleep disturbance, anxiety, irritability, weakness, headache, abdominal pain, nausea, vomiting, pain in muscles and joints .

With a frequency of less than 10%: loss of appetite, constipation, diarrhea, psychomotor agitation, dizziness, skin rashes, fever, reduced sexual potency, slowing down ejaculation. In individual cases, marked fatigue, confusion, depression, hallucinations, nightmares, photophobia, cough.

In laboratory studies may increase the activity of transaminases, lymphocytosis. All marked symptoms occurred both before treatment and on the background of reception Antaksona, and, apparently, can not be unequivocally regarded as a manifestation of side effects of the drug. Described one case of idiopathic thrombocytopenic purpura in a patient who may have been sensitized to Antaksonu during the previous treatment (recovery occurred after discontinuation of therapy and GCS).

Contraindications
use of narcotic analgesics;
positive urine test for the presence of opioids or opiates;
lack of data for a provocative test with naloxone;
opioid withdrawal syndrome;
acute hepatitis;
hepatic impairment;
sensitivity to naltrexone.

Unknown Antaksona safety of patients younger than 18 years, during pregnancy and lactation (breastfeeding).

Be wary prescribers disorders of liver function and / or kidneys.

Pregnancy and lactation

Health and Safety Antaksona during pregnancy and lactation (breastfeeding) is not installed.

Application for violations of liver function

Contraindicated in severe hepatic insufficiency. Be wary prescribers disorders of liver function.

Application for violations of renal function

Be wary prescribers disorders of kidney function.

Cautions

Antakson must cancel at least 48 hours before surgery, which requires the appointment of opioid analgesics. The patient must have a card appointments Antaksona to inform other medical personnel in case of need emergency care.

If you need to overcome the blockade of opioid receptors (introductory anesthesia, analgesia in emergency situations) should be used short-opioid analgesics in high doses, which reduces the risk of respiratory depression and vascular collapse.

Use in Pediatrics

Health & Safety Antaksona in children and adolescents under the age of 18 is not installed.

Effects on ability to drive vehicles and management mechanisms

When used in recommended doses of the drug does not affect the ability to engage in potentially hazardous activities that require attention.

Overdose

At present there is insufficient clinical data on the possibility of overdose.

Treatment: for suspected intoxication should be symptomatic therapy.

Drug Interactions

At simultaneous application with Antaksonom reduced effectiveness of preparations containing in its composition opioids (antitussives, opioid analgesics, antidiarrhoeal agents).

When the joint application of hepatotoxicity means increasing the risk of liver damage. Incompatibilities with other drugs have not been described.

Terms and Conditions of storage

The drug should be stored at temperatures not above 25 ° C. Special precautions for storage is not required. Shelf life - 3 years.Composition, structure and packing

Hard gelatin capsules with white opaque body and blue cap, with the image of the trademark company in case the capsule and the inscription "Antaxone 50" - on the lid, the contents of capsules - a white powder.

1 capsule. naltrexone hydrochloride 50 mg.

Excipients: lactose monohydrate, magnesium stearate. The composition of the shell capsules: gelatin, titanium dioxide, indigo.

Clinico-pharmacological group: Competitive antagonist of opioid receptors.

Pharmacological action

The specific antagonist of opioid receptors. Competitive binds to opioid receptors of all types and prevents or eliminates the effect of both endogenous opioids and exogenous opioid drugs - opioid analgesics and their surrogates. The introduction of increased doses of opioids can reduce or eliminate the effect of the antagonist. Antakson not have its own significant pharmacological properties, except for a narrowing of the pupil. Antakson not cause addiction and drug dependence.

At a dose of 50 mg.

Antakson for 24 h blocked the pharmacological effects caused by in / administration of 25 mg of heroin. With increasing doses Antaksona 2 times blocking effect is prolonged to 48 h, and 3 times - up to 72 h. Pharmacokinetics

Absorption and distribution

After oral naltrexone is well absorbed from the gastrointestinal tract, Cmax of naltrexone and its active metabolite 6-beta-naltreksola achieved in 1 h. The drug was well penetrates through tissue barriers, Vd is 1350 liters. Metabolism 95% of the dose naltrexone biotransformiruetsya in the liver with the formation of pharmacologically active metabolites, the chief of which - 6-beta-naltreksol as an antagonist opioids. The second metabolite - 2-hydroxy-3-methoxy-6-beta-naltreksol. Naltrexone and its metabolites are intrahepatic recycling.

Withdrawal

Naltrexone and its metabolites are derived primarily by the kidneys. Less than 1% of the dose of naltrexone is excreted in the urine in unchanged form, the remainder appears in the form of metabolites (including 38% - in the form of free and bound 6-beta-naltreksola). The average T1 / 2 of naltrexone - 4 h, 6-beta-naltreksola - 13 h, which explains his ability to cumulation.

Statement
in the complex therapy of opioid addiction (dependence) in order to maintain the patient condition in which opioids would not be able to provide the characteristic action; drug prescribed only after cupping withdrawal syndrome.

Application Antaksona begin in specialized departments of drug treatment in 7-10 days after receiving opioid drugs. Later, the patient should be under strict medical supervision, the patient should be a positive setting for treatment of drug addiction;
in the complex therapy of chronic alcoholism (including for maintenance therapy) in the same doses as with heroin addiction, on a background of psychotherapy.

Dosage regimen

Treatment of heroin addiction

Phase induction therapy Antaksonom

Treatment

Antaksonom can be started no earlier than 7-10 days after the last reception of drugs and in the absence of signs of withdrawal syndrome. Abstention from the use of drugs is determined by results of urine analysis for the maintenance of opioids.

Treatment

Antaksonom not start up until the provocative test with a / in the introduction of 500 mcg of naloxone does not become negative. Naloksonovaya test is not conducted in patients with signs of withdrawal symptoms or detection of opioids in the urine. Re naloksonovuyu test can be carried out within 24 hours Recommended first Antaksona single dose is 20 mg by mouth (as a solution).

In the absence of symptoms within 1 h of withdrawal symptoms the patient can be given the remainder of the daily dose (30 mg). The physician should monitor drug ingestion by the patient.

Supportive therapy Antaksonom

After the introduction phase Antakson prescribe a dose of 50 mg every 24 h (this dose is enough to block the action of 25 mg of heroin introduced in the present). You can use the other treatment regimens. 1. 50 mg Antaksona prescribed daily during the first 5 days of the week and 100 mg on Day 6. 2. 100 mg. Antaksona appointed every 2 days or 150 mg every 3 days. 3. 100 mg.Antaksona administered in 1 day (eg Monday), 100 mg in 2 day (Tuesday) and 150 mg on Day 5 (Friday). This scheme is suitable for patients with the installation of a long deprivation of opioids. Minimum course of treatment - 3 months; recommended - from 6 months.

Treatment of chronic alcoholism

The drug is prescribed daily dose of 50 mg 1 time / day. Minimum course of treatment - 3 months.

Treatment does not begin until until done naloksonovaya test to exclude the presence of opioids in the body.

Side effect

When applying for Antaksona testimony in therapeutic doses in patients in an organism which does not contain opioids, the development of serious side effects are usually not observed. With a frequency of more than 10% (as before treatment Antaksonom, and on the background of its use) in patients were observed: sleep disturbance, anxiety, irritability, weakness, headache, abdominal pain, nausea, vomiting, pain in muscles and joints .

With a frequency of less than 10%: loss of appetite, constipation, diarrhea, psychomotor agitation, dizziness, skin rashes, fever, reduced sexual potency, slowing down ejaculation. In individual cases, marked fatigue, confusion, depression, hallucinations, nightmares, photophobia, cough.

In laboratory studies may increase the activity of transaminases, lymphocytosis. All marked symptoms occurred both before treatment and on the background of reception Antaksona, and, apparently, can not be unequivocally regarded as a manifestation of side effects of the drug. Described one case of idiopathic thrombocytopenic purpura in a patient who may have been sensitized to Antaksonu during the previous treatment (recovery occurred after discontinuation of therapy and GCS).

Contraindications
use of narcotic analgesics;
positive urine test for the presence of opioids or opiates;
lack of data for a provocative test with naloxone;
opioid withdrawal syndrome;
acute hepatitis;
hepatic impairment;
sensitivity to naltrexone.

Unknown Antaksona safety of patients younger than 18 years, during pregnancy and lactation (breastfeeding).

Be wary prescribers disorders of liver function and / or kidneys.

Pregnancy and lactation

Health and Safety Antaksona during pregnancy and lactation (breastfeeding) is not installed.

Application for violations of liver function

Contraindicated in severe hepatic insufficiency. Be wary prescribers disorders of liver function.

Application for violations of renal function

Be wary prescribers disorders of kidney function.

Cautions

Antakson must cancel at least 48 hours before surgery, which requires the appointment of opioid analgesics. The patient must have a card appointments Antaksona to inform other medical personnel in case of need emergency care.

If you need to overcome the blockade of opioid receptors (introductory anesthesia, analgesia in emergency situations) should be used short-opioid analgesics in high doses, which reduces the risk of respiratory depression and vascular collapse.

Use in Pediatrics

Health & Safety Antaksona in children and adolescents under the age of 18 is not installed.

Effects on ability to drive vehicles and management mechanisms

When used in recommended doses of the drug does not affect the ability to engage in potentially hazardous activities that require attention.

Overdose

At present there is insufficient clinical data on the possibility of overdose.

Treatment: for suspected intoxication should be symptomatic therapy.

Drug Interactions

At simultaneous application with Antaksonom reduced effectiveness of preparations containing in its composition opioids (antitussives, opioid analgesics, antidiarrhoeal agents).

When the joint application of hepatotoxicity means increasing the risk of liver damage. Incompatibilities with other drugs have not been described.

Terms and Conditions of storage

The drug should be stored at temperatures not above 25 ° C. Special precautions for storage is not required. Shelf life - 3 years.