Naltrexone capsules 50mg №10

Dosage form

capsules

Composition

1 capsule contains: Naltrexone hydrochloride - 50 mg

Excipients: Lactose, Magnesium stearate, No. 4 hard gelatin capsules (gelatin, indigo carmine, titanium dioxide)

Packing

In the blister 10 capsules. in a carton 1 blister.

Mechanism of action

Naltrexone PV is a specific opioid receptor antagonist.

Competitively binds to opioid receptors of all types and prevents or eliminates the action of both endogenous opioids and exogenous opioids - narcotic analgesics and their surrogates. By administering opioids in increased doses, the effect of this antagonist can be reduced or eliminated.

In addition to the blocking properties of opioids, Naltrexone PV does not have significant intrinsic pharmacological properties, with the exception of some constriction of the pupil.

At a dose of 50 mg Naltrexone, PV for 24 hours blocks the pharmacological effects caused by the intravenous administration of 25 mg of heroin, at a dose of 100 mg - its effect is extended to 48 hours, and at a dose of 150 mg to 72 hours.

The drug is not addictive and drug addiction.

Indications and usage

Comprehensive treatment:
- Opioid addiction (addiction) in order to maintain the patient's condition in which the opioids can not have a characteristic action.
- Alcoholism.

Contraindications

- The use of narcotic analgesics.
- Positive urine test for opioids.
- Lack of data on the conduct of a provocative test with naloxone.
- Hypersensitivity to naltrexone drugs in history.
- Acute hepatitis or liver failure.
- Age up to 18 years.
- Pregnancy.
- The period of breastfeeding.

- Impaired liver and / or kidney function.

Pregnancy and Breastfeeding

Contraindicated in pregnancy and lactation.

Dosage and administration

Inside

Treatment of heroin addiction: Treatment with Naltrexone EF can be started no earlier than 7-10 days after the last opioid drug intake and if there is no abstinence syndrome. Abstinence from taking drugs is determined by the results of the analysis of urine for the content of opioids. Treatment is not started until the provocation test with intravenous administration of 0.5 mg of naloxone becomes negative, the naloxone test is not performed in patients with signs of withdrawal symptoms or when opioids are detected in the urine. Re-naloxone test can be carried out after 24 hours. Supportive therapy with Naltrexone FV, after the end of the introductory phase, 50 mg of Naltrexone FV is prescribed every 24 hours (this dose is sufficient to prevent the effect of 25 mg of intravenous heroin). You can use other treatment regimens:
one.Naltrexone 50 mg is prescribed daily for the first 5 days of the week and 100 mg on Saturday.
2. 100 mg of naltrexone is prescribed 1 time in 2 days or 150 mg 1 time in 3 days.
3. 100 mg of the drug is prescribed on Monday and Tuesday, and 150 mg on Friday. This scheme is convenient for patients with the installation of long-term opioid deprivation. The minimum rate of 3 months, the standard course - 6 months.

Treatment of alcoholism: Daily intake of 50 mg of Naltrexone EF, the minimum course is 3 months. Treatment is not started until a naloxone test is performed to exclude opioids in the body.

Adverse reactions

At therapeutic doses in patients who do not contain opioids, Naltrexone usually does not cause serious side effects. At doses in excess of 200 mg per day, naltrexone may have a hepatotoxic effect.

On the part of the digestive system: More often - nausea and / or vomiting, abdominal pain. Rarely - decrease or increase in appetite, anorexia, diarrhea or constipation, dry mouth, flatulence, aggravation of hemorrhoid symptoms, erosive and ulcerative lesions of the gastrointestinal tract, pain in the abdomen, increased activity of "liver" enzymes.

On the part of the nervous system: and sensory organs. More often - anxiety, nervousness, extreme tiredness, general weakness, restless sleep, "nightmarish" dreams, headache. Rarely - dizziness, blurred vision, confusion, hallucinations, CNS depression, 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 - cough, hoarseness, nasal congestion (vascular hyperemia of the nasal cavity), rhinorrhea, sneezing, broncho-obstruction, difficulty breathing, shortness of breath, nasal bleeding, dry throat, increased sputum, sinusitis.

Cardiovascular: Rarely - chest pain, high blood pressure, tachycardia, palpitations, non-specific ECG changes, phlebitis.

From the urinary system: Discomfort during urination, increased urination, edema syndrome (swelling of the face, fingers, feet, legs), sexual disorders in men (delayed ejaculation, reduced potency).

Allergic reactions: Less often - skin rash, flushing of the skin (including facial flushing). Rarely - hyperthermia, pruritus. Rarely - increased secretion of the sebaceous glands, chills.

Other: More often - arthralgia, myalgia. Rarely - thirst, increase or loss of body weight, pain in the groin area, acne, alopecia, swollen lymph nodes, lymphocytosis, in one case the development of idiopathic thrombocytopenic purpura was described against the background of prior sensitization to the drug.

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.

The drug is prescribed only after relief of withdrawal syndrome.

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. The patient should have a positive setting for the treatment of drug addiction.

The patient should have with him a card of appointments of Naltrexone FV for the information of other health workers in case of emergency care.

If it is necessary to overcome blocking of opioid receptors (anesthesia, pain relief in necessary cases), an increase in short-acting opioid analgesics should be used to reduce the risk of respiratory depression and blood circulation.

The competitive blockade of opioid receptors can be overcome by administering a higher dose of narcotic analgesic. Before use, it is necessary to exclude subclinical liver failure; during treatment, the activity of liver transaminases should be periodically monitored.

Naltrexone PV should be discontinued at least 48 hours before surgery, which will require the use of opioid analgesics. If necessary, emergency analgesia is carried out with caution, opiates are prescribed in high dosage (to overcome the antagonism), since respiratory depression will be more profound and prolonged.

To prevent the development of acute withdrawal symptoms, patients should at least 7-10 days stop taking opioid preparations containing them, it is necessary to determine the opioids in the urine and conduct a provocative test with naloxone; if these requirements are not observed, the withdrawal syndrome may appear 5 minutes after the administration and continue for 48 hours.

In the case of pain in the abdomen, dark urine, yellowing of the sclera, you must stop taking and consult a doctor. Persistent loss of appetite and progressive weight loss require cessation of therapy. Ineffective in the treatment of cocaine and non-opioid drug addiction.

Drug interactions

Some drugs containing opioids (antitussive, anti-inflammatory drugs, narcotic analgesics) may not cause the desired effect in taking naltrexone. In these cases, alternative opioid-free drugs should be used.

Hepatotoxic drugs increase (mutually) the risk of liver damage.

Possible lethargy or increased sleepiness in combination with thioridazine.

Accelerates the appearance of the symptoms of "withdrawal syndrome" on the background of drug addiction (symptoms may appear within 5 minutes after the introduction of the drug, last for 48 hours, are characterized by persistence and difficulty to eliminate them).

Symptoms: increased side effects.
Treatment: symptomatic.

Store in a dry place protected from light, at a temperature not exceeding 25 ° C.

3 years.