Active substanceNaltrexoneNaltrexone
Similar drugsTo uncover
  • Antakson
    capsules inwards 
    Zambon SpA     Italy
  • Vivitrol
    powder w / m 
  • Naltrexone
    capsules inwards 
  • Naltrexone
    pills inwards 
  • Naltrexone
    pills inwards 
  • Naltrexone FV
    capsules inwards 
  • Dosage form: & nbspcapsules
    Composition:

    For one capsule.

    Active substance:

    Naltrexone (Naltrexone hydrochloride) - 50 mg

    Excipients:

    Lactose Monohydrate - 96mg

    Magnesium stearate (Magnesium stearic acid, Introductory) - 4 mg

    Weight of capsule contents - 150 mg

    Hard gelatin capsules number 4

    Capsule shell composition:

    Capsule body: titanium dioxide (E 171) - 2%; gelatin - up to 100 %; cap of the capsule: indigotine (E 132) - 0.1333%; titanium dioxide - 1%; gelatin - up to 100%.

    Description:Hard gelatin capsules No. 4 with a white opaque case and a blue cap. The contents of capsules are white or almost white powder.
    Pharmacotherapeutic group:Opioid receptor antagonist
    ATX: & nbsp

    N.07.B.B.04   Naltrexone

    Pharmacodynamics:

    Naltrexone is a pure antagonist of opioid receptors. Competitively binds to opioid receptors of all types and prevents or eliminates the effect of both endogene opioids, and exogenous opioids - opioid analgesics and their surrogates. The greatest affinity for μ- and kreceptors. Reduces the effect of opioid analgesics (analgesic, antidiarrheal, antitussive); eliminates the side effects of opioids (including endogenous), except for the symptoms caused by the histamine reaction. In comparison with naloxone acts more strongly and for a long time. May cause miosis (mechanism unknown). The combination with opioids in large doses leads to an increase in the release of histamine with a characteristic clinical picture (facial hyperemia, pruritus, rash). In patients with opioid dependence causes an attack of abstinence.

    Naltrexone does not cause disulfiram-like reactions, as a result of the use of opioids and ethanol. When alcoholism is associated with opioid receptors and blocks the effects of endorphins. Reduces the need for alcohol and prevents relapses within 6 months after the 12-week course of therapy (the success of treatment depends on the patient's consent). Long-term appointment does not cause tolerance and dependence.

    With simultaneous long-term administration, it prevents the development of physical dependence on morphine, heroin and other opioids.In a dose of 50 mg blocks the pharmacological effects of 25 mg intravenously injected heroin for 24 hours, a double dose (100 mg) for 48 hours, and 150 mg for 3 days. The competitive blockade of opioid receptors can be overcome by the administration of a higher dose of opioid analgesic.
    Pharmacokinetics:

    Suction: Absorption after ingestion - fast and almost complete (96%), undergoes intestinal-hepatic circulation. The maximum concentration (cmax), the elimination half-life and the total amount of renal excretion for both ialtrexone and 6-beta-naltrexol increase in proportion to the increase in the prescribed dose of ialrexone from 50 to 200 mg. The beginning of action - in 1-2 hours. TSmax ialtrexone and its active metabolite 6-beta-naltrexol in plasma - 1 hour, after a single dose of 50 mg Cmax Ialtrexone-8.6 ng / ml. Stach - 6-beta-naltrexol - 99.3 mg / ml;

    - distribution: The connection with plasma proteins is low (21%). It penetrates well through histogehematic barriers. The volume of distribution is 1350 liters. Bioavailability of 5-40%;

    With prolonged use in a dose of 100 mg / sug. naltrexone does not accumulate (the concentration of 6-beta-naltrexol in plasma reaches 40%).

    - metabolism: Metabolated in the liver by 98% with the formation of pharmacologically active metabolites, the main of which is 6-beta-naltrexol is also an opioid antagonist. Other metabolites are - 2-hydroxy-3-methoxy-6-beta-naltrexol and 2-hydroxy-3-methoxy-naltrexone. Enzymes of the cytochrome P450 system do not participate in the metabolism of naltrexone. Naltrexone and its metabolites form conjugates with piocoronidin;

    - excretion: T1/2 naltrexone - 4 hours, 6-beta-naltrexol - 13 hours .. which explains its ability to cumulate. Naltrexone and its metabolites are excreted mainly (53-79%) by the kidneys (naltrexone - less than 2%. 6-beta-naltrexol, including in conjugated form -43%) and through the intestine (in small amounts). The total ground clearance is 1.5 l / min. Liver failure. Pharmacokinetics of the drug naltrexone does not change in patients with mild or moderate liver function disorder (Child-Pyo classes A and B), such patients do not need correction.

    Renal insufficiency. Light renal failure (CI creatine 50 - 80 ml / min.) Almost does not affect the pharmacokinetics of the drug naltrexone and there is no need to adjust the dose of the drug. Due to naltrexone and its primary metabolite are excreted from the body mainly by urine, naltrexone Care should be taken in patients with moderate to severe renal insufficiency.

    Indications:

    Treatment of alcohol dependence and blockade of the effects of exogenously introduced opioids. Complex therapy of opioid dependence in order to maintain the patient's state in which oiioids can not have a characteristic effect. The drug is indicated to prevent the recurrence of opioid dependence after opioid detoxification. Complex therapy of alcoholism, including with maintenance therapy, in the same dosages as with heroin dependence on the background of psychotherapy.

    Contraindications:Naltrexone is contraindicated in patients who are dependent on opioids, including those treated with opioid agonists or partial agonists. Positive naloxone test. The use of opioid analgesics or a positive test for the presence of opioids in the urine. Abstinence status against the background of opioid dependence.

    Hypersensitivity to the components of the drug, including in the anamnesis.

    Acute hepatitis or liver failure. Deficiency of lactase, lactose intolerance. Glucose - galactose malabsorption.

    Naltrexone is not safe in patients under the age of 18, during pregnancy and during breastfeeding.

    Carefully:Impaired liver and / or kidney function.
    Pregnancy and lactation:

    In experiments on rats (intake in doses 30 times higher than recommended for people immediately before pregnancy and during pregnancy) and in rabbits (taking in doses 60 times higher than recommended for humans), a teratogenic effect was established. The use of the drug during pregnancy is possible only if the potential benefit from its use exceeds the potential risk to the fetus.

    When naltrexone was orally taken, naltrexone and 6-beta-naltrexol were isolated from breast milk. Due to the potential carcinogenicity and the likelihood of serious side effects in infants, a decision should be made to discontinue therapy with the drug during breastfeeding or stop breastfeeding during treatment, depending on the importance of therapy for the mother.

    Dosing and Administration:

    Inside.

    Treatment of oiioid addiction.

    The phase of introduction to the course of therapy with naltrexone.

    Treatment with naltrexone is prescribed after the patient refrains from taking opioids for 7-10 days (in the absence of manifestations of withdrawal syndrome). Abstinence from the use of opioids is identified by the indicators of laboratory urine tests for the content of opioids. Treatment begins with a negative provocative test with 0.5 g of naloxone.

    Description of the naloxone test: the patient needs to administer 0.2-0.4 mg of naloxone intravenously for 5 minutes. or in the form of injection subcutaneously or intramuscularly. If there is no reactionfor the administration of naloxone for 15-30 minutes, a second dose of 0.4 mg intravenously or 0.4-0.8 mg is administered subcutaneously, and the reaction is observed. The sample is considered positive with pronounced mydriasis, a change in affect from complacently drowsy to dysphoric, behavioral disorders, and the appearance of signs of opium withdrawal.

    A naloxone sample is not given to patients with symptoms of withdrawal and when opioids are detected in the urine. The naloxone sample can be repeated after 24 hours. Treatment with naltrexone begins with caution, gradually increasing the dose.The contents of the capsule are dissolved in 50 ml of water. Initially, 25 mg of naltrexone is administered orally to 25 ml of the stock solution). The doctor should monitor the act of swallowing the device.

    Supportive therapy with naltrexone.

    The next day after the initial dose of nal, the ghexone is administered but 50 mg every 24 hours (naltrexone is at a given dose sufficient to block the effects of opioids administered parenterally, for example, 25 mg of heroin administered intravenously).

    Naltrexone 100 mg is given every 2 days or 150 mg every 3 days.

    Treatment of alcoholism

    In the combination therapy.

    Daily intake of 50 mg of naltrexone, the minimum course is 3 months.

    Treatment should be part of the appropriate program to eliminate alcohol dependence. During the course of treatment, it is necessary to monitor adherence to all components of alcohol treatment that affect the favorable outcome. Drug treatment is recommended to accompany the course of psychotherapy.

    The criteria for selecting patients for the treatment of alcoholism are:

    1) a positive attitude towards treatment;

    2) readiness to stop using alcohol (psychoactive substances);

    3) participation in rehabilitation programs;

    4) the beginning of a healthy lifestyle after the end of the course of treatment.

    Side effects:

    Side effect

    Classification of WHO adverse adverse reactions according to the frequency of development:

    Often - > 1/10; often - from 1/100 to 1/10: infrequently - from 1/1000 to 1/100; rarely - from 1/10000 to 1/1000; rarely - <1/10000. including individual messages.

    In therapeutic doses in patients with no opioids in their bodies. Naltrexup usually does not cause serious side effects.

    From the digestive system: very often - nausea and / or vomiting, abdominal pain; often - abdominal pain, decreased or increased appetite, anorexia, diarrhea or constipation, dryness of the oral mucosa, flatulence, increased activity of "liver" enzymes; rarely - aggravation of hemorrhoid symptoms, erosive and ulcerative lesions of the gastrointestinal tract.

    From the nervous system and sense organs: very often - anxiety, nervousness, unusual fatigue, general weakness, restless soybean, "nightmarish" dreams, headache; often - dizziness, blurred vision, confusion, hallucinations, depression of the central nervous system; rarely - depression, delirium,ringing and feeling of stuffiness in the ears, pain and burning sensation in the eyes, photophobia, irritability, drowsiness, disorientation in time and space, migraine, fainting, asthenia, lethargy, lethargy, anxiety.

    From the respiratory system: infrequent - cough, hoarseness, nasal congestion (hyperemia of the vessels of the nasal cavity), rheorrhea, sneezing, bronchial obstruction, difficulty breathing, shortness of breath, epistaxis, dryness in the throat, increased mucous sputum, upper respiratory tract infections, sinusitis, laryngitis, pharyngitis including streptococcal), nasopharyngitis, and sinusitis.

    From the side of the cardiovascular system: infrequently - chest pain, increased blood pressure, tachycardia, palpitations, nonspecific changes in the electrocardiogram, phlebitis.

    From the side of the organs of sight: rarely - konjukuwit.

    From the genitourinary system: often - sexual disorders in men delay ejaculation, decreased potency), increased or decreased libido, infrequently - discomfort with urination, increased urination, edematous syndrome (swelling of the face, fingers, feet, shins).

    Allergic reactions: often - skin rash, skin hyperemia (including facial hyperemia); hyperthermia, skin itching, increased secretion of sebaceous glands, oznoo.

    From the side of the musculoskeletal system: very often - pain in the back, joint stiffness, pain in the extremities, spasm, twitching or stiffness of the muscles; often - arthralgia, myalgia; arthritis, is often unknown - rhabdomyolysis.

    From the skin: papular rash, sweating, acne, alopecia.

    Other: dry mouth or thirst, sore throat, increased or loss of body weight, pain in the groin, lymphadenopathy, lymphocytosis; oral herpes, foot mycosis; in one case, the development of idiopathic thrombocytopenic purpura is described against a background of preliminary sensation to the drug.

    Syndrome of "lifting" opioids: abdominal pain, epigastric spasm, anxiety, nervousness, fatigue, irritability, diarrhea, tachycardia, hyperthermia, rhinorrhea, sneezing, goosebump, sweating, yawning, arthralgia, myalgia, anorexia, nausea and / or vomiting, tremor , general weakness.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

    Post-registration application experience

    According to the literature, a single case of idiopathic thrombocytopenic purpura is described in a patient who may have been sensitized to naltrexone during the previous treatment. Recovery occurred after the drug was discontinued and a course of corticosteroid therapy was administered.

    Overdose:

    Naltrexone is a moderately safe drug. According to studies, even large doses do not cause serious symptoms. There is evidence of a clinical trial during which patients took 800 mg per day of naltrexone for a week without signs of intoxication. If suspected of intoxication, symptomatic treatment should be prescribed.

    At the stage of the preclinical study with repeated administration of naltrexone at a dose of 100 mg / kg, exceeding the maximum daily dose for human treatment, I try on 35 times, there were no significant changes in hematological and biochemicalblood counts, as well as in the structure of internal organs. Local irritant effect naltrexone also does not render.
    Interaction:

    Reduces the effectiveness of medicines containing opioids (antitussive, anti-inflammatory, antidiarrheal drugs, opioid analgesics).In these cases, alternative drugs that do not contain opioids should be used.

    Hepatotoxic drugs increase (mutually) the risk of liver damage. Disulfiram inhibits microsomal oxidation in the liver, which can cause an increase in the concentration of drugs in the blood plasma metabolized in the liver (naltrexone), which increases the risk of intoxication.

    Possible lethargy or increased drowsiness when combined with thioridazine.

    Accelerates the appearance of the symptoms of the "cancellation" syndrome against the background of opioid dependent ones that are characterized by persistence and difficulty of their elimination.

    In the treatment of adverse forms of alcoholism and alcohol dependence comorbid with mental illness, in some cases, complete (to achieve lasting remission) or partial (decrease in alcohol consumption) effect can be achieved with the help of combination therapy in patients with concomitant administration of naltrexone and acamprosate. Thus, careful monitoring of liver function laboratory in regard to the possible effects summation hepatotoxic therapeutic schemes used in medicaments.

    There are no data on interactions with other drugs (in addition to opioids).

    Care should be taken when concomitant administration with barbiturates, benzodiazepines, tranquilizers, hypnotics, antidepressants and antihistamines (with sedative effect), neuroleptics.

    Special instructions:

    Naltrexone is effective only as a part of complex dependence therapy.

    Before application it is necessary to exclude subclinical hepatic insufficiency, during the treatment should periodically monitor the transient increase in the activity of microsomal liver enzymes.

    Naltrexone has a hepatotoxic effect. Therefore, for the first six months, it is necessary to monitor liver function on a monthly basis, then the frequency of laboratory studies is established in accordance with the objective clinical evaluation of the patient.

    Naltrexone is prescribed only after relief of the withdrawal syndrome.

    The drug begins to take only in specialized institutions under the supervision of a doctor. It should be closely monitored for the appearance of signs of depression or suicidal thoughts in patients with alcohol and / or alcohol.Opioid dependence, including patients receiving naltrexone treatment. Family members and caregivers should be warned about the need to closely monitor the occurrence of symptoms of depression or suicidal behavior and immediately report the occurrence of such symptoms to the treating physician. To ensure the effectiveness of treatment, it is necessary to conduct complex therapy, including psychological support.

    Naltrexone blocks the effects of opioids. Blockade can be overcome by increasing the dose of opioids.

    A patient who receives naltrexone treatment should be warned that an uncontrolled intake of opioids during this period can lead to a severe withdrawal syndrome up to the development of a coma. There is a risk of death.

    Naltrexone should be discontinued no less than 48 hours before surgery, requiring the use of opioid analgesics.

    If an emergency analgesia is required, caution should be given to using opioids at a higher dose (to overcome antagonism), since oppression of breathing will be deeper and more prolonged.

    To prevent the development of an acute withdrawal syndrome, patients should at least 7-10 days later stop taking opioids and drugs containing them, be sure to determine opioids in the urine and conduct a provocative test with naloxone; Abstinence syndrome may occur if these requirements are not met.

    A persistent decrease in appetite and progressive weight loss require discontinuation of therapy. Ineffective in the treatment of cocaine, as well as non-opioid drug dependence. Perhaps the development of eosinophilic pneumonia, resistant to antibiotic therapy; with the development of progressive dyspnoea and hypoxia, you should immediately consult a doctor.

    Patients should be warned that:

    When seeking medical help, patients are required to inform health professionals about treatment with naltrexone

    in case of abdominal pain, darkening of the urine, yellowing of the sclera, it is necessary to stop taking the device and consult a doctor;

    the use of naltrexone does not eliminate or weaken symptoms of alcohol withdrawal; with the independent use of heroin and other opioids in small doses, the effect of their use will not be,and a further increase in the dose of the described drugs will lead to a lethal outcome (respiratory arrest).

    Drug addiction

    Naltrexone is a complete opioid antagonist: does not cause tolerance, physical or mental dependence.

    Effect on the ability to drive transp. cf. and fur:

    The drug can cause dizziness and other undesirable phenomena that can affect the management of vehicles and engage in other potentially hazardous activities that require increased concentration of attention, speed of psychomotor reactions.

    Form release / dosage:

    Capsules 50 mg.

    Packaging:10 capsules in a contour cell box made of polyvinylchloride film and aluminum foil. One or two contour mesh packages together with the instruction for use are placed in a pack of cardboard.
    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N000388 / 01
    Date of registration:17.01.2008 / 19.02.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSCOW PHARMACEUTICAL FACTORY, CJSC MOSCOW PHARMACEUTICAL FACTORY, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.05.2018
    Illustrated instructions
      Instructions
      Up