Naltrexone + Triamcinolone (Naltrexonum + Triamcinolonum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Opioids, their analogs and antagonists

Means for correcting disorders in alcoholism, toxic and drug addiction

Included in the formulation
  • Prodetoxone®
    pills д / импл. 
       
    • АТХ:

    V.03.A.B   Antidotes

    Pharmacodynamics:

    Naltrexone: a competitive antagonist of opioid receptors. It blocks μ-, δ- and κ-receptors, therefore eliminates both the analgesic effect of narcotic analgesics, and the euphoria caused by them, respiratory depression and other effects.

    The mechanism of action of triamcinolone (glucocorticoid): interaction with intracellular glucocorticoid receptors - the formation of dimers of the glucocorticoid-glucocorticoid receptor complex (release of the receptor from the bonds with heat shock proteins 70 and 90 and immunophilin). Penetration of the activated receptor into the nucleus, binding to glucocorticoid-sensitive regulatory elements of DNA - a specific effect on gene expression (activation and suppression). Interaction with other protein transcription factors, including NFκB and AP-1, regulating the expression of many proteins of the immune system, which leads to suppression of the expression of genes encoding some cytokines, collagenase and stromelysins.

    Pharmacokinetics:

    Connectivity naltrexone with plasma proteins is weak. Passes through the placenta and the blood-brain barrier. Biotransformation in the liver. Elimination by the kidneys (70% for 72 hours). Half-life 64 min.

    The association with plasma proteins of thiamcinolone (4 mg) is high. Biotransformation in the liver, kidneys, tissues to inactive metabolites. The half-life (4 mg) in plasma is 2-5 hours, in tissues 18-36 hours, with inhalation-88 minutes, with intranasal administration 4 hours (1-7 hours). Elimination by the kidneys (inactive metabolites), inhalation forms - by the kidneys and with feces.

    Indications:

    Treatment of opioid dependence outside the withdrawal syndrome; rehabilitation and prevention of relapse of opioid dependence.

    ICD-10

    V.F10-F19.F11.9   Mental and behavioral disorders caused by the use of opioids - mental disorder and behavioral disorder, unspecified

    V.F10-F19.F11.8   Mental and behavioral disorders caused by the use of opioids - other mental disorders and behavioral disorders

    V.F10-F19.F11.7   Mental and behavioral disorders caused by the use of opioids - residual and delayed psychotic disorders

    V.F10-F19.F11.6   Mental and behavioral disorders caused by the use of opioids - amnestic syndrome

    V.F10-F19.F11.5   Mental and behavioral disorders caused by the use of opioids are a psychotic disorder

    V.F10-F19.F11.3   Mental and behavioral disorders caused by the use of opioids - withdrawal symptoms

    V.F10-F19.F11.2   Mental and behavioral disorders caused by the use of opioids - a syndrome of dependence

    V.F10-F19.F11.1   Mental and behavioral disorders caused by the use of opioids - harmful use

    V.F10-F19.F11.0   Mental and behavioral disorders caused by the use of opioids - acute intoxication

    V.F10-F19.F11   Mental and behavioral disorders caused by the use of opioids

    XXI.Z40-Z54.Z50.3   Rehabilitation of people with addiction

    Contraindications:

    Hypersensitivity to opioid receptor blockers (naloxone and naltrexone preparations) in the anamnesis and other components of the drug, in particular triamcinolone; opioid withdrawal syndrome; lack of data on the conduct of the provocative test with naloxone, indicating the withdrawal from the withdrawal syndrome; positive test for the presence of opioids in urine; acute hepatitis; liver failure; the Itenko-Cushing syndrome; systemic fungal infections; glaucoma; osteoporosis; pregnancy; the period of breastfeeding; children's age till 6 years.

    Carefully:

    Renal failure, heart failure, elderly age, children under 18 years.

    Pregnancy and lactation:

    Category FDA - C.

    The use is contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Subcutaneous implantation.

    Treatment of opioid dependence should begin after 7-10 days of abstinence from the use of opioids and preparations containing them, or after another method of opioid detoxification with the presence of confirmation of withdrawal from the withdrawal syndrome: the absence of opioids in the urine and a negative provocative test with naloxone.

    Subcutaneous implantation is preferably performed in the subcutaneous fat of the anterior abdominal wall. After infiltration anesthesia with observance of the rules of aseptic and antiseptic in the place where the implant is supposed to be placed, a skin cut about 1.5 cm long is made. In a blunt way (using the "Bilroth" clamp), a channel is created to insert an implant about 5 cm long. The syringe container is inserted into the canal until it reaches its distal end. With the aid of the piston, the implant is pushed out of the container and placed in the subcutaneous fat tissue, after which 1-2 dermal seams are inserted from the non-absorbable material.The seam is treated with an antiseptic solution, a sterile sticker is applied.

    In the future, the change of the label is made every other day with the treatment of the joint site with antiseptic solutions. Sutures are removed 7-8 days after implantation.

    If necessary, repeated implantation is possible. The duration of treatment and the number of repeated implantations are determined by the attending physician.

    Side effects:

    From the digestive system: decreased appetite, nausea, vomiting, diarrhea or constipation, abdominal pain, impaired liver function.

    From the cardiovascular system: tachycardia, increased blood pressure, phlebitis.

    From the side of the central nervous system: headache, weakness, sleep disorder, anxiety, dizziness, decreased mood, dysphoric reactions.

    From the respiratory system: nasal congestion, cough, difficulty breathing.

    On the part of the reproductive system: perhaps - slowing of ejaculation, decreased potency; rarely - increase or decrease of libido.

    Dermatological reactions: redness of the skin, acne, itching, local aseptic inflammation.

    Others: chills, tremors, joint pains, enlarged lymph nodes, exacerbation of hemorrhoids.

    Overdose:

    Not described.

    Interaction:

    With simultaneous use with naltrexone, the effectiveness of opioid receptor agonists (antitussives, analgesics) decreases. Combination with hepatotoxic drugs increases the risk of liver damage. Possible increased drowsiness with simultaneous use with thioridazine.

    Special instructions:

    The drug should be used in specialized medical institutions under the supervision of a doctor.

    Before use, liver failure should be ruled out, and the level of transaminases should be monitored periodically during treatment.

    During treatment, if necessary, anesthesia for medical reasons (surgery, trauma) is preferably using non-opioid analgesics. In case of emergency analgesia, opioid analgesics should be cautious and prescribe opioids at a higher dose to overcome antagonism.

    Patients should be warned that:

    when seeking medical help, it is necessary to inform medical workers about the treatment with the drug;

    when there are pains in the abdomen, darkening of the urine, yellowing of the sclera should consult a doctor;

    when using heroin and other opioid drugs in small doses, the effect of their use will not be, and further increase in the dose of narcotic drugs can lead to a fatal outcome as a result of stopping breathing.

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