Nalbuphine (Nalbuphine)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceNalbuphineNalbuphine
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  • 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
    • Dosage form: & nbspinjection
    Composition:

    1 ml of the solution contains:

    Active substance:

    nalbuphine hydrochloride - 10.00 mg, in terms of anhydrous.

    Excipients:

    sodium chloride - 1,00 mg, sodium disulfite - 1,00 mg, (sodium metabisulfite) sodium citrate dihydrate - 7.74 mg equivalent to 9.40 mg sodium citrate pentasecvhydrate, citric acid - 12.60 mg, monohydrate (or citric acid acid in terms of citric acid monohydrate),

    water for injection - up to 1 ml

    1 ml of the solution contains:

    Active substance: nalbuphine hydrochloride 20.00 mg, based on anhydrous

    Excipients:

    sodium chloride - 1,00 mg, sodium disulfite - 1,00 mg, (sodium metabisulfite) sodium citrate dihydrate - 7.74 mg, equivalent to 9.40 mg sodium citrate pentasecvhydrate, citric acid-12.60 mg, monohydrate (or citric acid acid in terms of citric acid monohydrate),

    water for injection - up to 1 ml.

    Description:Transparent colorless or slightly colored liquid.
    Pharmacotherapeutic group:An analgesic opioid: an opioid receptor agonist-antagonist. Psychotropic substance listed in List III of the "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation"
    ATX: & nbsp

    N.02.A.F.02   Nalbuphine

    Pharmacodynamics:Nalbuphine has the properties of agonist-antagonizing opioid receptors (agonist kappa and antagonist mu-opioid receptors). Activates endogenous antinociceptive system through kappa-opiate receptors, disrupts interneuronal transmission of pain impulses at various levels of the central nervous system. Influencing the higher parts of the brain, changes the emotional color of pain. It inhibits conditioned reflexes, has a sedative effect, causes dysphoria, miosis, excites the vomiting center, to a lesser extent than morphine oppresses the respiratory center and affects the motility of the gastrointestinal tract. Does not affect hemodynamic parameters. The risk of developing addiction and opioid dependence in controlled use is low. It begins to act 2-3 minutes after intravenous injection and 10-15 minutes after intramuscular injection.
    Pharmacokinetics:

    The maximum concentration in the blood plasma after intramuscular injection is observed after 30-60 minutes. The duration of action is 3-6 hours, the half-life is 2.5-3 hours. TCmax when administered intramuscularly - 1 hour, with intravenous administration - 30 minutes.

    Metabolised in the liver. It is excreted as metabolites, mainly with bile and in small amounts with urine. Penetrates through the placental barrier, excreted in the mother's milk (less than 1% of the administered dose).

    Indications:

    - Severe pain syndrome of various origin (postoperative period, myocardial infarction, gynecological interventions, trauma, malignant neoplasms);

    - as an additional tool for general anesthesia.

    Contraindications:Hypersensitivity; marked inhibition of respiration and central nervous system; epileptic syndrome, intracranial hypertension; head trauma, acute alcohol poisoning, alcoholic psychosis; acute surgical diseases of the abdominal cavity (before diagnosis); operative interventions on the hepatobiliary system (possible spasm of the sphincter of Oddi); drug dependence on morphine-like drugs (morphine, promedol, fentanyl) - the possibility of developing withdrawal syndrome; diarrhea on the background of pseudomembranous colitis caused by cephalosporins, lincosamides, peicillins, toxic dyspepsia (delay in elimination of toxins and associated exacerbation and prolongation of diarrhea).
    Carefully:Elderly age, cachexia, hepatic and / or renal insufficiency, respiratory failure (including chronic obstructive pulmonary diseases, uremia), premature birth and presumed immaturity of the fetus, lactation period, pregnancy, children and adolescence (up to 18 years). Gallstone disease, severe inflammatory bowel disease, bronchial asthma, arrhythmia, arterial hypertension, hypothyroidism, prostatic hyperplasia, urethral stenosis, suicidal tendencies, emotional lability, seriously ill patients, weakened patients.
    Dosing and Administration:

    Intravenous, intramuscular or subcutaneous. With intravenous administration, the drug is diluted with 10-15 ml of isotonic sodium chloride solution.

    Pain syndrome: 0,15-0,3 mg / kg of body weight. If necessary, you can re-enter every 4-6 hours. The maximum daily dose is 2.4 mg / kg.Duration of treatment is no more than 3 days. When suspected of myocardial infarction - 10-20 mg intravenously slowly. If necessary, the dose can be increased to 30 mg. In the absence of a distinct positive dynamics of the pain syndrome, 20 mg of the drug is given again after 30 minutes.

    For premedication - 100-200 mkg / kg, for introductory anesthesia - 0.3-1 mg / kg for 10-15 minutes, to maintain anesthesia - 250-500 mcg / kg every 30 minutes.

    Side effects:

    From the nervous system and sensory organs: less often - fatigue, general weakness; rarely (less than 1%) - nervousness, discomfort, blurred vision, diplopia, restless sleep, nightmares, unusual dreams, in children - paradoxical agitation; frequency unknown - ringing in the ears, convulsions, rigidity of the muscles (especially respiratory), tremor, involuntary muscle twitching. Lethargy, drowsiness, confusion, dizziness, headache, agitation, euphoria or depression, hallucinations.

    From the cardiovascular system: decrease or increase in blood pressure, hahi or bradycardia.

    From the digestive system: anorexia, (6%); rarely - irritation of the gastrointestinal tract, spasm of the bile duct,with inflammatory bowel diseases - paralytic intestinal obstruction and toxic megacolon (constipation, flatulence, nausea, gastralgia, vomiting); frequency unknown - constipation, hepatotoxicity (dark urine, pale stool, icteric sclera and skin). Dry mouth, indigestion, spastic pain.

    From the side of the urinary system: rarely (less than 1%) - decreased diuresis, spasm of ureters (difficulty and pain when urinating, frequent urge to urinate).

    Allergic reactions: less often - swelling of the face; rarely (less than 1%) - angioedema; local reactions: hyperemia, edema, burning at the injection site. Hives, anaphylactic shock, bronchospasm, laryngeal edema, itching, sneezing.

    From the respiratory system: pulmonary edema; decrease in the minute volume of respiration.

    Other: increased sweating, tenderness at the injection site, drug dependence, withdrawal syndrome (spastic abdominal pain, nausea, vomiting, rhinorrhea, lacrimation, weakness, anxiety, fever).

    Overdose:

    Symptoms: hypoventilation of the lungs, alteration of consciousness (up to coma), periodic respiration of Cheyne-Stokes,pallor of the skin, hypothermia, miosis, lowering of arterial pressure, cardiovascular insufficiency, paralysis of the respiratory center.

    Treatment: with respiratory depression - intravenously naloxone or nalorphine. Maintenance of adequate pulmonary ventilation and indices of central hemodynamics.

    Interaction:

    Strengthens the oppressive effect on the central nervous system of funds for general anesthesia, hypnotics, antihistamines, anxiolytic, antipsychotic, antidepressant drugs. Ethanol enhances the inhibitory effect of nalbuphine on the central nervous system. It should not be combined with other narcotic analgesics because of the danger of weakening analgesia and the possibility of provoking a withdrawal syndrome in patients with drug dependence. In combination with derivatives of phenothiazine and penicillin can enhance nausea and vomiting. It is pharmaceutically compatible with 0.9% sodium chloride solution, 5% dextrose solution and Hartmann solution in glass, polyvinyl chloride, polyethylene containers.

    Strengthens the depressing effect on the central nervous system and respiration of muscle relaxants.

    Medicines with anticholipergic activity, antidiarrhoeal drugs (including loperamide) increase the risk of constipation up to intestinal obstruction, urinary retention and central nervous system depression.

    Strengthens the hypotensive effect of drugs that reduce blood pressure (including ganglioblocators, diuretics).

    Buprenorphine (including previous therapy) reduces the effect of other opioid analgesics; against the background of the use of low doses of agonists of mu or kappa-opioid receptors can enhance respiratory depression.

    Reduces the effect of metoclopramide.

    With caution should be used simultaneously with monoamine oxidase inhibitors because of possible overexcitation or inhibition with the emergence of hyper- or hypotensive crises (first, to evaluate the interaction effect, the dose should be reduced to% of the recommended dose).

    Naloxone reduces the effect of opioid analgesics, as well as the respiratory and central nervous system caused by them; may require large doses to level the effects of butorphanol, nalbuphine and pentazocine,which were prescribed to eliminate the undesirable effects of other opioids; can accelerate the appearance of symptoms of the syndrome of "withdrawal" against the background of drug dependence. Naltrexone accelerates the appearance of symptoms of the "cancellation" syndrome against the background of drug dependence (symptoms can appear only 5 minutes after drug administration, continue for 48 hours, are characterized by persistence and difficulty of their elimination); reduces the effect of opioid analgesics (analgesic, antidiarrheal, antitussive); does not affect the symptoms caused by the histamine reaction.

    It does not prevent or alleviate the symptoms of the withdrawal syndrome with drug dependence (including fentanyl).

    Special instructions:Do not use more than 3 days and exceed the dosage because of the possibility of developing physical dependence.
    Effect on the ability to drive transp. cf. and fur:Ambulatory patients during the treatment period should refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Solution for injection 10 mg / ml or 20 mg / ml in ampoules of 1 ml.
    Packaging:

    5 ampoules in the outline of the cell.

    1 or 2 contour squares with instructions for use and a scarifier or a knife ampoule in a pack of cardboard.

    For 20, 50 or 100 contour mesh packages together with an equal number of instructions for use, respectively, in a box of cardboard or a box of corrugated cardboard (for inpatient).

    When packing ampoules with rings or break points, scarifiers or ampoule knives do not.

    Storage conditions:

    In accordance with the rules for storage of psychotropic substances listed in List III of the "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation".

    In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:3 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000074
    Date of registration:23.05.2007 / 02.08.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp28.05.2018
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