Antaxon
Antakson: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Antaxone
ATX code: N07BB04
Active ingredient: naltrexone (naltrexone)
Manufacturer: Zambon S.p. A. (Zambon SpA) (Italy)
Description and photo update: 2019-19-08
Antaxon is a drug for the treatment of drug and alcohol addiction.
Release form and composition
Release form - capsules: hard gelatinous, opaque, body - white, cap - blue, size No. 4; inside capsules - white powder (10 pcs. in blisters, 1 blister in a cardboard box).
The main active ingredient of the drug: naltrexone hydrochloride - 50 mg.
Auxiliary components: magnesium stearate - 4 mg, lactose monohydrate - 96 mg.
The composition of the capsule: body - titanium dioxide, gelatin; cap - titanium dioxide, indigo carmine blue, gelatin.
Pharmacological properties
Pharmacodynamics
The active substance of the Antaxon drug - naltrexone, is a specific antagonist of opioid receptors. Its mechanism of action is based on competitive binding with opioid receptors of all types, as a result of which the prevention or elimination of the effect of both exogenous opioid drugs and endogenous opioids, including opioid analgesics and their surrogates, occurs. The effect of this antagonist can be reduced or eliminated by the administration of increased doses of opioids.
Naltrexone does not possess significant pharmacological properties of its own, with the exception of some constriction of the pupil.
Drug dependence and addiction do not occur as a result of therapy.
When Antakson 50 mg is taken for 24 hours, the pharmacological effects caused by the intravenous injection of heroin at a dose of 25 mg are blocked. If the dose of naltrexone is doubled, the blocking effect is lengthened up to 48 hours, 3 times - up to 72 hours.
Pharmacokinetics
After oral administration, naltrexone is well absorbed from the gastrointestinal tract, the time to reach C max (maximum plasma concentration) of naltrexone and 6-beta-naltrexol (its active metabolite) is 1 hour.
The substance penetrates well through tissue barriers, V d (volume of distribution) - 1350 liters.
Most of the dose (95%) is biotransformed in the liver with the subsequent formation of pharmacologically active metabolites. The main metabolite, 6-beta-naltrexol, is an opioid antagonist. The second metabolite is 2-hydroxy-3-methoxy-6-beta-naltrexol. The substance and its metabolites undergo intrahepatic recirculation.
The main route of elimination of naltrexone and its metabolites is by the kidneys. Less than 1% of the dose is excreted unchanged in the urine; the remainder is excreted as metabolites (including 38% as free and bound 6-beta-naltrexol). The average T 1/2 (half-life) of naltrexone and 6-beta-naltrexol is 4 and 13 hours, respectively, which explains its ability to cumulate.
Indications for use
According to the instructions, Antakson is included in the complex therapy of opioid drug dependence to maintain a state in which the opioids taken by the patient do not have their usual effect. In addition, the drug is used in the complex treatment of alcoholism (in combination with psychotherapy).
Contraindications
- a positive urine test for opioid content;
- the use of narcotic analgesics;
- lack of data on the test performed with naloxone;
- opioid withdrawal syndrome;
- liver failure;
- acute hepatitis;
- hypersensitivity to the components of the drug;
- age under 18;
- pregnancy in any trimester;
- breast-feeding.
Antaxon is taken with caution in case of impaired renal and liver function.
Instructions for the use of Antaxon: method and dosage
The course of treatment begins in a hospital setting no earlier than 7-10 days after the last drug intake. The use of Antaxon is most effective in patients with a positive attitude towards drug addiction treatment.
For heroin addiction, a urine test for opioid content is done before starting therapy to confirm that the patient is abstaining from drugs. Do not start treatment until a negative sample is obtained with intravenous administration of 0.5 mg naloxone.
The standard daily dosage of Antaxon is 50 mg. In the first dose, the patient is prescribed 20 mg of the drug in the form of a solution. If withdrawal symptoms do not occur within an hour, the remaining 30 mg should be taken.
There are the following therapy regimens:
- every three days, the patient takes 150 mg of the drug or 100 mg every two days;
- take 50 mg daily for five weekdays and 100 mg on Saturday;
- on Monday and Tuesday, take 100 mg of the drug and another 150 mg on Friday.
The latter scheme is most effective for those who intend not to take opioids for a long time.
Antaxon should be taken from 3 months to six months.
For the treatment of alcoholism, the patient is prescribed to take 50 mg of the drug daily for 3 months.
Side effects
In some cases, the use of Antaxon can cause anxiety, weakness, abdominal pain, vomiting, headache, irritability, muscle and joint pain, sleep disturbances, diarrhea, agitation, loss of appetite, rash, impaired potency, dizziness, confusion, cough, hallucinations, depression, photophobia.
Overdose
Sufficient clinical data on the possibility of overdose are not presented.
In case of suspicion of intoxication, symptomatic therapy is indicated.
special instructions
If an operation is planned that requires the appointment of an opioid analgesic, the drug must be canceled two days before the surgery.
The patient should notify health care providers that he is taking Antaxon. It is advisable to always have a card with the prescription of the drug with you - for cases of emergency medical care.
The medicinal product does not affect the ability to drive vehicles and engage in activities requiring increased concentration.
Application during pregnancy and lactation
Antaxon is not prescribed during pregnancy / lactation (no experience of use).
Pediatric use
Antaxon therapy is contraindicated in patients under 18 years of age (no experience of use).
With impaired renal function
Caution should be exercised when prescribing Antaxon to patients with impaired renal function.
For violations of liver function
- severe hepatic impairment: therapy is contraindicated;
- liver dysfunction: Antaxon should be used with caution.
Drug interactions
Drugs taken for diarrhea, antitussives and narcotic analgesics, as well as other drugs containing opioids, can reduce the desired effect of taking Antaxon. If you need to take these funds, you should select alternative drugs that will not contain opioids.
Medicines with hepatotoxic effects increase the risk of liver damage.
There is no information about the incompatibility of Antaxon with other drugs.
Analogs
Structural analogs of Antakson are drugs Naltrexone and Vivitrol.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Antaxon
According to reviews, Antakson is effective when used to reduce drug and alcohol addiction. Therapy usually begins after the end of the detoxification course, relief of withdrawal symptoms, as well as mental and somatic disorders. Usually the drug is prescribed for a course of 5-6 months. Improvement of the condition is most often noted after a month of treatment.
It is noted that Antaxon, even with prolonged use, is not addictive. To increase the effectiveness, experts recommend combining the intake of the drug with other drugs.
The price of Antaxon in pharmacies
The approximate price for Antaxon (10 capsules of 50 mg) is 995-1325 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
