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Naltrexone is an opioid antagonist with the highest affinity for opioid mu receptors. In addition to antagonism of opioid receptors, the drug does not possess or has a very slight degree of intrinsic activity. The use of the drug for unknown reasons may cause constriction of the pupil. The use of Vivitrol is not accompanied by the development of tolerance or mental and physiological dependence. In patients with physical opioid dependence, administration of the drug causes withdrawal symptoms. Naltrexone blocks the action of opioids by competitively binding to opioid receptors in the brain. The neurobiological mechanisms responsible for reducing alcohol consumption observed in patients with alcohol dependence on naltrexone are not fully understood, but it is assumed that the mechanism of action affects the endogenous opioid system. The blockade can be overcome by increasing doses of opioids, which is manifested by such symptoms as an increase in histamine secretion. Vivitrol is not a means of aversive therapy and does not cause disulfiram-like reaction when taking opiates or alcohol.
Naltrexone is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
|Naltrexone||Moscow Endocrine Plant||Russia||capsules|
|Vivitrol||Johnson and johnson||USA||bottle|
|Naltrexone FV||Moscow Pharmaceutical Factory||Russia||capsules|
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Dosage and Administration
The drug is prescribed only after relief of withdrawal syndrome and after previously performed detoxification.
Naltrexone is started in specialized drug treatment units 7-10 days after the last opioid drug intake. In the future, the patient must be under strict medical supervision, a positive attitude to the treatment of drug addiction in the patient is necessary.
Treatment of alcoholism: Inside 50 mg 1 time per day, a 12-week course of treatment prevents relapses within 6 months (the success of treatment depends on the patient’s consent).
Treatment of drug addiction: Begin only after 7-10 days of abstinence from the use of opioids, confirmed by a provocative test and analysis of urine for the content of opioids. The patient must be absent "cancellation" syndrome and signs of abstinence. Treatment is not started until the provocative test with intravenous administration of 0.5 mg of naloxone becomes negative. The initial dose of 25 mg, for 1 hour, the patient’s condition should be monitored; in the absence of withdrawal syndrome, 50 mg should be administered 1 time per day, this dose blocks 25 mg of heroin administered intravenously. Alternative treatment regimens:
1. 50 mg every weekday and 100 mg on Saturday.
2. 100 mg every other day.
3. 150 mg in 2 days.
4. 100 mg (Monday), 100 mg (Wednesday) and 150 mg (Friday). It should be borne in mind that the use of these treatment regimens increases the risk of hepatotoxicity. The course of treatment is determined individually.
On the part of the digestive system: Rarely - increased appetite, dry mouth, flatulence, worsening symptoms of hemorrhoids, erosive and ulcerative lesions of the gastrointestinal tract, abdominal pain, increased activity of "liver enzymes."
On the part of the nervous system: and sensory organs. More often - extraordinary fatigue. Rarely - blurred visual perception, confusion, hallucinations, depression of the central nervous system, ringing and a feeling of congestion in the ears, pain and burning sensation in the eyes, photophobia, irritability, drowsiness, disorientation in time and space.
On the part of the respiratory system: Rarely - hoarseness, nasal congestion (hyperemia of the vessels of the nasal cavity), sneezing, shortness of breath, dry throat, increased separation of mucous sputum, sinusitis.
Since the cardiovascular system: Rarely - chest pain, non-specific ECG changes.
On the part of the genitourinary system: Discomfort during urination, increased urination.
Allergic reactions: Less often - a skin rash. Rarely - hyperthermia, pruritus, increased secretion of the sebaceous glands.
Other: Rarely - thirst, increase or loss of body weight, pain in the groin area, swollen lymph nodes, lymphocytosis. In one case, the development of idiopathic thrombocytopenic purpura on the background of preliminary sensitization to the drug is described.
The syndrome of "cancellation" of opioids: Abdominal pain, cramping epigastric pain, anxiety, nervousness, fatigue, irritability, diarrhea, tachycardia, hyperthermia, rhinorrhea, sneezing, "goose bumps", sweating, yawning, arthralgia, myalgia, anorexia, nausea, and / or vomiting, tremor, general weakness.
- Hypersensitivity (including naloxone).
- Acceptance of opiates.
- Positive test for the presence of opioids in the urine.
- Abstinence syndrome.
- Acute hepatitis.
- Liver failure .
- Breastfeeding (at the time of treatment is excluded).
- Children's and youthful age (till 18 years).
Increases (mutually) the risk of liver damage when combined with hepatotoxic drugs.
There may be lethargy or increased drowsiness when combined with thioridazine.
Reduces the effectiveness of drugs containing opioids (antitussive drugs, analgesics).
Accelerates the appearance of the symptoms of "withdrawal syndrome" on the background of drug dependence (symptoms may appear within 5 minutes after the administration of the drug, last for 48 hours, are characterized by persistence and difficulty to eliminate them).
Pregnancy and Lactation
Before use, it is necessary to exclude subclinical hepatic insufficiency, during treatment it is necessary to periodically monitor the level of transaminases, can not be combined with drugs with hepatotoxic properties.
To prevent the development of acute withdrawal symptoms, patients should stop taking opioids and drugs containing them at least in 7-10 days, it is necessary to determine opioids in the urine and conduct a provocative test with naloxone; if these requirements are not observed, withdrawal symptoms may appear 5 minutes after taking the drug and continue for 48 hours.
Naltrexone must be discontinued at least 48 hours before surgery, which will require the use of opioid analgesics.
If it is necessary to conduct an emergency analgesia, opiates should be prescribed in high dosage (to overcome the antagonism), since respiratory depression will be more profound and prolonged.
Persistent loss of appetite and progressive weight loss require discontinuation of therapy.
Ineffective in the treatment of cocaine and non-opioid drug dependence.
Patients should be warned that:
When seeking medical care, they are obliged to inform health workers about treatment with naltrexone.
In case of pain in the abdomen, dark urine, yellowing of the sclera, stop taking and consult a doctor.
With the independent use of heroin and other drugs in small doses, the effect of their use will not be, and a further increase in the dose of narcotic drugs will lead to death (respiratory arrest).
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