Last Updated on July 1, 2018 by Dr.Derek Fhisher
Most popular brand: Revia
Active ingredient: Naltrexone
Available dosage forms: 50 mg
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Naltrexone general information
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Description of the active substance naltrexone / Naltrexone.
Formula: C20H23NO4, chemical name: (5a) – 17 – (cyclopropylmethyl) – 4,5 – epoxy – 3.14 – digidroksimorfinan – 6 – he (and as hydrochloride)
Pharmacological group: different means / tools for correcting violations in alcoholism, toxic – and addiction
Mode of action:. blocks the opiate receptors.
Naltrexone displace agonists with opioid receptors competitively or blocks their binding to opiate receptors. It removes or reduces the symptoms, which is caused by the intravenous administration of opiates. Naltrexone has the highest affinity for the kappa – and mu – receptors. When administered naltrexone is absorbed by 96%. 95% is converted in the liver to pharmacologically active metabolites, including 6 – β – naltrexol. The half-life of naltrexone is 3.9 hours, 6 – β – naltrexol is 12.9 hours. The average half-life is dose dependent and is increased with continued use of the drug. Naltrexone with its metabolites are excreted in the kidneys and faeces. Naltrexone total clearance is 1.5 l / min. The drug takes effect within 1-2 hours. When coupled with continued use prevents the development of physical dependence to heroin, morphine and other opiates. 50 mg of naltrexone to block the pharmacological effects throughout the day intravenously administered 25 mg of heroin, 100 mg – for 2 days and 150 mg – 3 days. Prolonged use of naltrexone does not cause addiction and tolerance. Joint reception of Naltrexone with high doses of opioids leads to an increased release of histamine, which is characterized by the appropriate clinical picture (rash, itching, redness of the face). Naltrexone is an attack of withdrawal in opioid-dependent patients. Naltrexone in alcoholism binding to opioid receptors, blocks the effects of endorphin. Reduce alcohol consumption and prevents recurrence for six months at 12 – week course of treatment (treatment success depends on the consent of the patient and his interaction with the attending physician).
Alcoholism; opioid addiction (as an additional tool, after the abolition of opioid analgesics).
How to use naltrexone and the dose
Naltrexone taken orally (regardless of the meal). Treatment for alcoholism: within 1 week 12 times a day at 50 mg. Treatment of drug addiction begin only after 7-10 – day abstinence from opioids, confirmed by urine analysis and provocative test; an initial dose of 25 mg, followed by 1 hour observe the state of the patient and the absence of withdrawal symptoms is administered daily dose of rest; administered naltrexone 50 mg per day (a dose sufficient to prevent the action of intravenously administered 25 mg of heroin). Alternative regimens:
1. 100 mg on Monday, 100 mg on Wednesday and 150 mg Friday;
2. 150 mg every 2 days;
3. 100 mg every other day;
4. 50 mg every weekday and 100 mg on Saturday.
it should be borne in mind that the use of these regimens increase the risk of hepatotoxicity. Minimum course of treatment is 3 months recommended -.
Six months Naltrexone is administered intramuscularly in the buttock, alternating buttocks. The drug should be administered by qualified medical personnel only using the available components in the package. packaging components can not be replaced. The recommended dose – intramuscularly 1 time in 4 weeks, 380 mg. It is impossible to naltrexone administered intravenously! If you missed the regular administration of the dose, the next injection should be done as quickly as possible
Before treatment is necessary to exclude subclinical hepatic failure, the therapy should periodically monitor the content of liver transaminases.; naltrexone can not be combined with drugs which have hepatotoxicity. For the prevention of acute withdrawal syndrome patients are at least 7-10 days should stop using opioids, and drugs that contain them, it is necessary to confirm the provocative test and analysis for the presence of opioids in the urine; If these requirements are not met, the withdrawal symptoms may develop within 5 minutes after the administration of naltrexone and last for 2 days. It should warn patients that:
– the appearance of abdominal pain, yellowing of the sclera, dark urine you want to cancel receiving naltrexone and seek medical advice;
– they are obliged to inform health care providers about naltrexone treatment when applying for medical assistance;
– with self-administration of small doses of heroin and other drugs effects, will not be on their reception, and a further increase in the dose of heroin and other drugs will result in death (cessation of breathing).
Hypersensitivity (including to naloxone), hepatic failure, acute hepatitis, a positive test for the presence of opioids in the urine, a condition of withdrawal of opioid dependence.
Restrictions on the use
Violation of the functional state of the kidneys or liver, pregnancy, breast-feeding, age and 18 years of age.
Pregnancy and breastfeeding
The use of naltrexone in pregnancy is possible only if the expected benefit to the mother above the possible risk to the fetus. Naltrexone with its metabolites into breast milk. Because – because of possible carcinogenicity, and the likelihood of infants serious adverse reactions to decide on the abolition of drug treatment during breastfeeding or termination of lactation during treatment with naltrexone, depending on the degree of importance of the treatment to the mother.
Side effects of naltrexone
The nervous system and sensory organs: anxiety, fatigue, nervousness, fatigue, nightmares, trouble sleeping, headache, blurred vision, dizziness, confusion, fainting, hallucinations, depression of the central nervous system, irritability, drowsiness, anxiety , disorientation, a feeling of fullness and tinnitus, photophobia, burning sensation and pain in the eyes; blood and circulatory system: chest pain, palpitations, hypertension, tachycardia, nonspecific ECG changes, lymphocytosis, phlebitis; Digestive system: abdominal pain, nausea and / or vomiting, constipation or diarrhea, frequent bowel movements, bloating, gastro – intestinal disorder, dry mouth, increased / decreased appetite, anorexia, dysgeusia, worsening of the symptoms of hemorrhoids, erosive – ulcerative lesions, increased activity of liver enzymes; respiratory system: hoarseness, cough, nasal congestion, runny nose, bronchial obstruction, sneezing, breathing difficulties, nosebleeds, shortness of breath, dry throat, sinusitis, pharyngitis, increased separation of mucous expectoration, nasopharyngitis; support system and movement: arthritis, pain and stiffness in the joints, pain in the back, in the extremities, muscle spasm, muscle pain, stiffness in muscles, muscle twitching; urogenital system: frequent urination, discomfort when urinating, edema syndrome (swelling of the fingers, face, legs, feet), sexual dysfunction in men (lower potency, delayed ejaculation); Allergic reactions: itching, skin rash, flushing of the skin (including the face); Other: pyrexia, chills, decreased or increased body mass, lymphadenopathy (including cervical adenitis), increased sweating; reactions at the injection site: seal, soreness, swelling.
naltrexone Interaction with other substances
Naltrexone in combination with hepatotoxic drugs mutually increases the risk of liver injury. There may be an increased drowsiness or lethargy when co-administered with naltrexone thioridazine. When combined with naltrexone opioid receptor agonists (antitussives, analgesics) reduces the effectiveness of the latter.
These naltrexone overdose is very limited. Perhaps the development of dizziness and drowsiness, abdominal pain, nausea, injection site reactions. It should be symptomatic and supportive treatment.
Trading names of drugs with working substance naltrexone
Antakson Vivitrol Naltrexone