Nalbuphine (Nalbuphinum)

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

Opioid non-narcotic analgesics and opioid antagonists

Included in the formulation
  • Nalbuphine
    solution w / m in / in 
    MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC     Russia
  • Nalbuphine
    solution for injections 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Nalbuphine Serb
    solution for injections 
    Serb S.A.     France
  • Nalbuphine hydrochloride
    solution for injections 
    Roushan Pharma Co., Ltd.     India
    • АТХ:

    N.02.A.F.02   Nalbuphine

    Pharmacodynamics:

    Opioid κ-receptor agonist, a competitive antagonist of opioid μ-receptors. Has the following pharmacological effects: analgesic (the onset of action: intravenously 2-3 minutes, intramuscularly - 15 minutes, subcutaneously - 15 minutes, maximum effect: intravenously for 30 minutes, intramuscularly - 60 minutes, duration of action: intravenously 2-3 hours , intramuscularly 3-4 hours, subcutaneously 3-6 hours, subcutaneously 3-6 hours), suppression of the respiratory and emetic centers, inhibition of conditioned reflexes, dysphoria and psychotomimetic effect in high doses, increased tone of the sphincter of the urine and biliary tract, smooth muscles of the gastrointestinal tract, bronchi, a decrease in secretion Elez gastrointestinal (activation GH secretion pancreatic D-cells), development of tolerance and addiction.

    Pharmacokinetics:Penetrates through the placenta and the blood-brain barrier. Relationship with plasma proteins 50%. Biotransformation in the liver. The half-life is 3-6 hours.Creatinine clearance 29.7 ± 3.27 ml per min × kg) increase in children. Elimination mainly by the kidneys (4 ± 2% unchanged) and partly with feces.
    Indications:

    Pain syndrome of moderate and severe intensity with myocardial infarction, in preparation for surgery (prevention) and in the postoperative period; as an additional means of analgesia in general anesthesia.

    ICD-10

    XVIII.R50-R69.R52.9   Pain, unspecified

    XVIII.R50-R69.R52.2   Another constant pain

    XVIII.R50-R69.R52.0   Acute pain

    XVIII.R50-R69.R52   Pain, not elsewhere classified

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    XXI.Z40-Z54.Z41   Procedures performed not with curative purposes

    XX.Y60-Y69.Y60.8   When performing another therapeutic or surgical procedure

    Contraindications:

    Hypersensitivity; marked respiratory depression and central nervous system; diarrhea against pseudomembranous colitis caused by cephalosporins, lincosamides, penicillins, toxic dyspepsia (delayed elimination of toxins and related exacerbation and prolongation of diarrhea); with epidural and spinal anesthesia - a violation of blood clotting (including anticoagulant therapy), infection (the risk of infection in the central nervous system).

    Carefully:

    Epileptic syndrome, intracranial hypertension; head trauma, acute alcoholic conditions, alcoholic psychosis; acute surgical diseases of the abdominal cavity (before diagnosis); operative interventions on the hepatobiliary system (possible spasm of the sphincter of Oddi); cholelithiasis, severe inflammatory bowel diseases, bronchial asthma, arrhythmia, hepatic and / or renal failure, respiratory failure (including chronic obstructive pulmonary disease, uremia), arterial hypertension, hypothyroidism, hyperplasia of the prostate, stenosis of the urethra, suicidal tendencies, emotional lability, drug dependence on morphine-like drugs (morphine, trimeridine, fentanyl), seriously ill, weakened patients, cachexia, premature birth and presumed immaturity of the fetus, breast-feeding, pregnancy, age under 18, old age.

    Pregnancy and lactation:

    Category FDA FROM.

    The risk of dependence in the fetus and the development of withdrawal syndrome in a newborn (irritability, convulsions, excessive tearfulness,tremor, lively reflexes, fever, nausea, diarrhea, sneezing and yawning). Qualitative and well-controlled studies on humans have not been conducted. Animals did not cause a teratogenic effect in large doses. There is no information on the penetration into breast milk. The application is possible if the benefit exceeds the risk of side effects.

    Dosing and Administration:

    Individual. Enter intravenously, intramuscularly and subcutaneously. For adults, the single dose varies from 100 μg / kg to 1 mg / kg. For children, the initial single dose is 300 μg / kg. The frequency of administration depends on the indications and the clinical situation. Duration of application - no more than 3 days.

    Side effects:

    From the side of the central nervous system and peripheral nervous system: often - drowsiness, retardation; Possible - dizziness, imbalance, headache; rarely - nervousness, depression, confusion, dysphoria; in some cases - difficulty speech, blurred vision.

    From the digestive system: nausea, vomiting, dry mouth.

    From the side of the cardiovascular system: in some cases - arterial hypertension or hypotension, bradycardia, tachycardia.

    Allergic reactions: in some cases - hives.

    Others: sweating is possible.

    Overdose:

    Symptoms of acute and chronic overdose: cold sticky sweat, confusion, dizziness, drowsiness, decreased blood pressure, nervousness, fatigue, miosis, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, dry mouth, delirious psychosis, intracranial hypertension before the violation of cerebral circulation), hallucinations, muscle rigidity, convulsions, in severe cases - loss of consciousness, respiratory arrest, coma.

    Treatment: gastric lavage, recovery of respiration and maintenance of cardiac activity and blood pressure; intravenous administration of a specific antagonist opioid analgesics - naloxone in a single dose of 0.2-0.4 mg with repeated administration 2-3 minutes before the total dose of 10 mg; the initial dose of naloxone for children is 0.01 mg / kg.

    Interaction:

    When used simultaneously with anesthetics, sleeping pills, sedatives, anxiolytics (tranquilizers), antipsychotic drugs (antipsychotics), antidepressants, antihistamines with sedative effect,ethanol intensifies the inhibitory effect on the central nervous system.

    Special instructions:

    Under careful supervision and in reduced doses should be used nalboufine against the background of drugs for narcosis, hypnotics, anxiolytics, antidepressants and antipsychotics (antipsychotics) in order to avoid excessive CNS suppression and inhibition of respiratory center activity.

    They are used with caution in outpatient settings in patients engaging in potentially hazardous activities requiring increased attention and high speed of psychomotor reactions.

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