Naltrexone

Naltrexone – the medicine applied to treatment of opioid drug addiction.

Form of release and structure

Naltrexone is produced in the form of tablets (in blister strip packagings on 7 pieces, on 4 packagings in a cardboard pack; in blister strip packagings on 10 pieces, on 1, 2 or 5 packagings in a cardboard pack).

Active ingredient is a part of 1 tablet: a hydrochloride of naltrexone – 50 mg.

Indications to use

• Opioid drug addiction (as additional drug after cancellation of opioid analgetics);
• Alcohol addiction (as a part of complex treatment).

Contraindications

• Abstinence syndrome;
• Hepatitis (acute current);
• Liver failure;
• Simultaneous use with opiates;
• Positive take of the test for existence in urine of opioids;
• Pregnancy and period of breastfeeding;
• Age up to 18 years;
• Hypersensitivity to drug components.

Route of administration and dosage

Naltrexone it is necessary to accept inside.

Drug can be used only after stopping of an abstinence syndrome and preliminary holding actions for desintoxication of an organism.

Therapy needs to be begun in the departments specializing in treatment of drug addiction, thus after the last reception of opioid drug there have to pass not less than 7-10 days. At further out-patient treatment of the patient it is necessary to control strictly. Efficiency of performing therapy in many respects is defined by existence at the patient of positive installation on recovery.

For treatment of alcoholism Naltrexone as a part of complex therapy appoint 50 mg (1 tablet), frequency rate of reception – once a day. In the presence of the consent of the patient, administration of drug for 3 months prevents emergence of a recurrence within half a year.

Treatment of opioid drug addiction can be begun after 7-10 days of abstention from the use of opioids that it is necessary to confirm with the provocative test (the negative response to intravenous administration of 0,5 mg of Naloxonum) and the analysis of urine for their contents. The patient has to have no signs of a withdrawal and abstinence. The first dose makes 25 mg after which reception the patient within 1 hour has to be under control of the doctor. Further Naltrexone appoint 50 mg once a day (the dose blocks intravenous administration of 25 mg of heroin). Also drug can be used according to alternative schemes (frequency rate of reception – once a day):

• Three days a week: on 100 mg on Monday and Wednesday, 150 mg on Friday;
• Six days a week: on 50 mg daily for 5 days (on weekdays), 100 mg on Saturday;
• On 100 mg in 1 day or on 150 mg in 2 days.

At the choice of the mode of dosing it is necessary to consider that alternative schemes of therapy increase risk of development of a hepatotoxic.

The doctor determines duration of a medical course individually.

Side effects

• Cardiovascular system: seldom – nonspecific changes of an ECG, a stethalgia;
• Nervous system and sense bodys: more often – extraordinary fatigue; seldom – a photophobia, hallucinations, an illegibility of visual perception, confusion of consciousness, oppression of the central nervous system, a ring and feeling of a congestion in ears, pain and burning sensation in eyes, irritability, drowsiness, a disorientation in space and time;
• Alimentary system: seldom – aggravation of symptoms of hemorrhoids, increase in appetite, dryness in a mouth, a meteorism, an abdominal pain, increase in activity of liver enzymes, digestive tract erosive cankers;
• Urinogenital system: increase of an urination, discomfort at an urination;
• Respiratory system: seldom – dryness in a throat, the raised department of a mucous phlegm, hoarseness of a voice, a hyperemia of vessels of a nasal cavity (a nose congestion), sneezing, short wind, sinusitis;
• Allergic reactions: less often – skin rash; seldom – a hyperthermia, a skin itch, increase in secretion of sebaceous glands;
• Withdrawal of opioids: spasms in epigastriums, the general weakness, "goose-pimples", an arthralgia, abdominal pain, concern, fatigue, nervousness, a tremor, irritability, tachycardia, diarrhea, a hyperthermia, a rhinorrhea, sneezing, yawning, perspiration, a mialgiya, anorexia, vomiting and/or nausea;
• Others: seldom – thirst, a hyperadenosis, pain in inguinal area, decrease or increase in body weight, a lymphocytosis. There are data on development of an idiopathic Werlhof's disease against the background of presensitization to a hydrochloride of naltrexone.

Special instructions

Before performing therapy it is necessary to exclude existence of a subclinical liver failure.

During use of Naltrexone it is necessary to control the level of transaminases periodically.

Contraindicated combined use with medicines with hepatotoxic properties.

To avoid developing of an acute abstinence syndrome by the patient it is necessary to stop reception of opioids and the drugs containing them at least in 7-10 days prior to therapy. The abstinence syndrome at non-compliance with this condition can develop in 5 minutes after reception of Naltrexone, its average duration – 48 hours.

When performing the emergency anesthesia for overcoming antagonism with care appoint the raised doses of opiates, at the same time respiratory depression can be deeper and long.

In cases of need of use of opioid analgetics before carrying out surgical intervention Naltrexone it is necessary to cancel not less than in 48 hours.

The persistent loss of appetite and the progressing reduction of weight demand the therapy termination.

At treatment of not opioid and cocaine medicinal addiction Naltrexone is inefficient.

In cases of need of the request for medical care patients have to inform the health worker on administration of drug.

It is necessary to interrupt therapy and to see behind consultation a doctor at development of such symptoms as darkening of urine, an abdominal pain, yellowing of scleras.

The use of heroin and other drugs during use of Naltrexone to effect does not bring in small doses, increase in doses of drugs can cause an apnoea from the death.

Medicinal interaction

At joint purpose of Naltrexone with some drugs development of the following effects is possible:

• Hepatotoxic medicines: increase in probability of damage of a liver;
• Drugs with the content of opioids (antibechic medicines, analgetics): decrease in their efficiency;
• Thioridazine: increase in drowsiness, emergence of a lethargical sleep.

Terms and storage conditions

To store in dry, protected from light, the place, unavailable to children, at a temperature up to 25 °C.

Period of validity – 3 years.