Active substanceNaltrexoneNaltrexone
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  • Dosage form: & nbspcoated tablets
    Composition:

    1 tablet:

    Active substance:

    Naltrexone hydrochloride - 50 mg;

    Excipients:

    lactose monohydrate 123,155 mg, cellulose 17,593 mg, microcrystalline cellulose 48.084 mg, silicon dioxide colloidal anhydrous 3,084 mg, crospovidone 4,334 mg, magnesium stearate 3,750 mg.

    Shell:

    Lactose monohydrate - 3,600 mg, hypromellose 15 cps - 2,800 mg, titanium dioxide (E 171) - 2,561 mg, macrogol 4000-1,000 mg, iron oxide black (E 172) 0.003 mg, iron oxide red (E 172) 0.001 mg , iron oxide yellow (E 172) - 0.035 mg.

    Description:

    Tablets are white with cream-colored capsule-shaped color, coated with a film sheath, with a separation notch on both sides.

    Pharmacotherapeutic group:Opioid receptor antagonist
    ATX: & nbsp

    N.07.B.B.04   Naltrexone

    Pharmacodynamics:

    Naltrexone is a specific antagonist of opioid receptors.Competitively binds to opioid receptors of all types and prevents or eliminates the effect of both endogenous opioids and exogenous opioids - narcotic analgesics and their surrogates. The introduction of opioids in increased doses can weaken or eliminate the effect of this antagonist.

    Naltrexone competitively blocks opioid receptors, and can also cause some narrowing of the pupil. In a dose of 50 mg naltrexone in 24 hours blocks the pharmacological effects caused by the intravenous administration of 25 mg of heroin. When the dose of naltrexone is doubled, this effect extends to 48 hours, and when it is tripled, it lasts up to 72 hours.

    The drug does not cause addiction and drug dependence.

    Pharmacokinetics:

    Naltrexone is well absorbed after ingestion and is metabolized 95% in the liver with the formation of pharmacologically active metabolites. The main metabolite, 6-beta-naltrexol, also has the properties of a competitive opioid antagonist. In addition, 2-hydroxy-3-methoxy-6-beta-naltrexol and 2-hydroxy-3-methyl-naltrexone are formed. The maximum concentration of naltrexone and 6-beta-naltrexol in the blood plasma is observed 1 hour after taking the drug. Well penetrates through the histogematic barriers - the volume of distribution is 1350 liters.

    The half-life in blood plasma for naltrexone is 4 hours, for its metabolite 6-beta-naltrexol - 13 hours, which explains its ability to cumulate. Naltrexone and its metabolites undergo intrahepatic recirculation. Naltrexone is excreted through the kidneys unchanged (about 1%) and in the form of metabolites (43% in the form of free and bound 6-beta-naltrexol).

    Indications:

    Opioid addiction (as an auxiliary drug after the abolition of opioid analgesics), alcoholism.

    Contraindications:

    The use of narcotic analgesics. Positive test for the presence of opioids in the urine. Abstinence condition against opioid dependence. The lack of data on the conduct of the provocative test with naloxone (cf. Method of administration and dose). Hypersensitivity to the components of the drug, including in the anamnesis. Acute hepatitis or liver failure. Deficiency of lactase, lactose intolerance, glucosogalactose malabsorption.

    The safety of Naltrexone has not been established in patients under the age of 18, during pregnancy and during lactation.

    Carefully:Impaired liver and / or kidney function.
    Dosing and Administration:

    Inside.

    Treatment of opioid addiction.

    The phase of introduction to the course of therapy Naltrexone.

    Treatment with naltrexone can be started no earlier than 7-10 days after the last reception of the opioid. drug and under condition of absence of signs of opioid withdrawal syndrome. Abstinence from taking drugs is determined by results of urine analysis for the content of opioids. Treatment does not begin until provocative. a sample with an intravenous injection of 0.5 mg of Naloxone will not become negative. Naloxone test is not performed for patients with signs of opioid withdrawal syndrome or when opioids are detected in urine. Repeated naloxone The sample can be taken after 24 hours.

    The first dose of Naltrexone is usually 25 mg (half a tablet). If there are no signs of the "cancellation" syndrome within an hour, the patient is given a remainder (25 mg) of the daily dose of the drug.

    The doctor should monitor the act of swallowing the drug.

    Supportive therapy Naltrexone

    After the end of the introductory phase, 50 mg of Naltrexone is administered every 24 hours (this dose enough to prevent the effects of 25 mg intravenously injected heroin).

    You can use other treatment regimens:

    1. 50 mg Naltrexone is prescribed daily for the first five days of the week and 100 mg for the 6th day

    2. 100 mg Naltrexone is administered every 2 days or 150 mg every 3 days;

    3. 100 mg of the drug is prescribed on day 1 (eg Monday), <100 mg on day 2 (eg, Tuesday), and 150 mg on day 5 (Friday). This scheme is convenient for patients with long-term treatment of opioid addiction.

    The minimum course is from 3 months, the recommended course is from 6 months.

    Treatment of alcoholism.

    Inside to 50 mg once a day; the minimum course is 3 months.

    Complex therapy of alcoholism, including with maintenance therapy, in the same dosages as with opioid addiction in the background of psychotherapy.

    Treatment should be performed under strict medical supervision in a specialized department.

    The criteria for selecting patients for the treatment of alcoholism are: 1) a positive setting on. treatment; 2) the readiness to stop using alcohol (psychoactive substances); 3) participation in rehabilitation programs; 4) the beginning of a healthy lifestyle after the termination of the course of treatment.

    Side effects:

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

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

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

    From the respiratory system: cough, hoarseness, nasal congestion (hyperemia of the vessels of the nose), rhinorrhea, sneezing, bronchial obstruction, difficulty breathing, shortness of breath, epistaxis, dryness in the throat, increased mucous sputum, upper respiratory tract infections, sinusitis, laryngitis, pharyngitis (v. h.streptococcal), nasopharyngitis.

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

    From the genitourinary system: discomfort with urination, increased frequency of urination, edematous syndrome (swelling of the face, fingers, feet, shins), sexual disorders in men (delayed ejaculation, decreased potency).

    Allergic reactions: skin rash, skin hyperemia (including hyperemia of the face); hyperthermia, skin itching, increased secretion of sebaceous glands, chills.

    From the side of the musculoskeletal system: arthralgia, myalgia; arthritis, joint stiffness, back pain, pain in the extremities, spasm, twitching or stiffness of the muscles. From the skin. integument: papular rash, sweating, acne, alopecia.

    Other: thirst, increase or loss of body weight, pain in the groin, enlarged lymph nodes, lymphocytosis; the development of idiopathic thrombocytopenic purpura on the background of preliminary sensitization to the drug (recovery occurred after discontinuation of the drug and the course of glucocorticosteroid therapy).

    Opioid withdrawal syndrome: abdominal pain, spasm in the epigastric region, anxiety, nervousness, fatigue, irritability, diarrhea, tachycardia, hyperthermia, rhinorrhea, sneezing, goosebumpiness, sweating, yawning, arthralgia, myalgia, anorexia, nausea and / or vomiting, tremor, total weakness.

    Post-marketing experience:

    From the digestive system: perversion of taste, gastroesophageal reflux disease, hemorrhoids, colitis, gastrointestinal bleeding, paralytic, intestinal obstruction, pararectal abscess, gastroenteritis, tooth abscess, cholelithiasis, acute cholecystitis.

    From the central nervous system: violation of concentration, convulsions, ischemic stroke, aneurysm of the cerebral arteries, irritability, alcohol withdrawal syndrome, agitation, euphoria, delirium.

    From the side of the musculoskeletal system: pain in the extremities.

    From the skin: inflammation of the subcutaneous tissue.

    From the sense organs: conjunctivitis.

    From the respiratory system: sore throat, shortness of breath, chronic obstructive pulmonary disease, influenza, bronchitis, pneumonia.

    Co cardiovascular system: "hot flashes", deep vein thrombosis, pulmonary embolism, fibrillation, atrial, myocardial infarction, angina, incl. unstable, chronic heart failure, coronary artery atherosclerosis.

    Other: heat stroke, dehydration, hypercholesterolemia, leukocytosis. Allergic reactions: angioedema, urticaria.

    From the urinary system: urinary tract infections.

    On the part of the reproductive system: spontaneous abortion, decreased libido.

    Overdose:

    Sufficient clinical data on the possibility of drug overdose is currently not available. If suspected of intoxication, symptomatic treatment should be prescribed.

    Interaction:

    Some drugs containing opioids (antitussives, antidiarrhoeals, narcotic analgesics) may not produce the desired effect in persons taking Naltrexone. In these cases, alternative drugs that do not contain opioids should be used. Hepatotoxic drugs increase the risk of liver damage.

    Cases of incompatibility with other drugs are not described.

    Special instructions:

    The competitive blockade of opioid receptors can be overcome by the introduction of a higher dose of narcotic analgesic.

    Before the beginning of treatment it is necessary to exclude the presence of liver failure and during the period of treatment periodically monitor the activity of transaminases; Do not combine with drugs that have hepatotoxic properties. Naltrexone should be discontinued no less than 48 hours before surgery, which requires the use of opioid analgesics. If necessary overcoming the blocking of opioid receptors (general anesthesia, anesthesia in urgent cases), increased doses of short-acting opioid analgesics to reduce the risk of respiratory depression and circulation.

    To prevent the development of acute withdrawal symptoms, patients should. a minimum of 7-10 days to stop taking opioids and drugs containing them, be sure to identify opioids in the urine and conduct a provocative test with naloxone; if these requirements are not met, withdrawal symptoms may appear 5 minutes after the administration and continue for 48 hours.

    When seeking medical help, patients are required to inform medical workers about treatment with Naltrexone.

    In case of pain in the abdomen, darkening of the urine, yellowing of the sclera is necessary stop taking and see a doctor. Naltrexone is ineffective in the treatment of cocaine, as well as non-opioid medicinal dependencies.

    Drug dependence.

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

    Form release / dosage:

    The coated tablets are 50 mg.

    Packaging:For 7 tablets in a blister of PVC (with a layer of PVDC) / aluminum foil. For 4 blisters together with instructions for use in a pack of cardboard.
    Storage conditions:

    At a temperature of no higher than 25 ° C, in a dry, dark place.

    Keep out of the reach of children.

    Shelf life:3 years.Do not use after the date shown on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-000989
    Date of registration:09.12.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Roushan Pharma Co., Ltd.Roushan Pharma Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspRoushan Pharma Co., Ltd.Roushan Pharma Co., Ltd.
    Information update date: & nbsp27.05.2018
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