Nalbuphine hydrochloride (Nalbuphine hydrochloride)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceNalbuphineNalbuphine
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  • Nalbuphine hydrochloride
    solution for injections 
    Roushan Pharma Co., Ltd.     India
    • Dosage form: & nbspinjection for 10 mg / ml; 20 mg / ml
    Composition:

    For 1 ml of solution for injection 10 mg (20 mg):

    Active substance:

    Nalbuphine hydrochloride dihydrate (in terms of anhydrous) - 10 mg (20 mg)

    Excipients: sodium disulfite 1.00 mg / ml, sodium citrate dihydrate 9.4 mg / ml, citric acid anhydrous 12.6 mg / ml, sodium chloride 1.00 mg / ml, hydrochloric acid (0.1 M solution ) - until the pH is adjusted, water for injection - up to 1 ml.

    Description:A clear, colorless or almost colorless solution.
    Pharmacotherapeutic group:An analgesic opioid: an opioid receptor agonist-antagonist
    ATX: & nbsp

    N.02.A.F.02   Nalbuphine

    Pharmacodynamics:Nalbuphine has the properties of an agonist-antagonist 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 significantly lower than for opioid antagonists.
    Pharmacokinetics:

    Nalbuphine begins to act 2-3 minutes after intravenous administration and 10-15 minutes after intramuscular or subcutaneous injection.

    The maximum concentration in the blood plasma after intramuscular injection is observed after 60 minutes, after intravenous administration - after 30 minutes.

    The duration of action is 3-6 hours, the half-life is 2.93 +/- 0.795 hours. It is metabolized in the liver with the formation of inactive metabolites. The level of binding to plasma proteins is approximately 50%.

    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:

    For short-term treatment of pain syndrome of strong and medium intensity (including in the pre- and postoperative period).

    As an additional tool for general anesthesia.

    Contraindications:

    - Hypersensitivity to the main or auxiliary components of the drug;

    - marked depression 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);

    - severe hepatic and / or renal insufficiency;

    - surgical 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 against pseudomembranous colitis caused by cephalosporins, lincosamides or penicillins, toxic dyspepsia (delay in elimination of toxins and related exacerbation and prolongation of diarrhea).

    Carefully:Elderly age, cachexia, hepatic and / or renal insufficiency, respiratory insufficiency (incl.chronic obstructive pulmonary disease, uremia), premature birth and presumed immaturity of the fetus, lactation period, pregnancy, age under 18, cholelithiasis, severe inflammatory bowel disease, bronchial asthma, cardiac arrhythmia, hypertension, hypothyroidism, prostatic hyperplasia, stenosis urethra, suicidal tendencies, emotional lability, weakened patients.
    Pregnancy and lactation:

    Pregnancy

    Data on medical use are not sufficient to assess potential teratogenic risk. Nalbuphine penetrates the placental barrier. It is allowed to apply during pregnancy, if the benefits for the mother clearly exceed the risk to the fetus. With prolonged use during pregnancy, the development of withdrawal syndrome in newborns has been reported. Newborns whose mothers were injected with narcotic analgesics during labor should be monitored for respiratory depression (bradycardia, apnea, cardiac arrhythmia), and opioid receptor antagonists if necessary (this effect can be prevented by using a pregnant woman during naloxone delivery).

    Breast-feeding

    Nalbuphine penetrates into breast milk, its concentration in it exceeds the plasma concentration in the mother. Since a clinically significant concentration can be achieved in newborns, breastfeeding is not recommended.

    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 3-6 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.

    As an additional tool for general anesthesia - 100-200 μg / kg, for introductory anesthesia - 0.3-1 mg / kg for 10-15 minutes, to maintain anesthesia - 250-500 μg / kg every 30 minutes.

    Side effects:

    The frequency of potential adverse reactions is classified as follows: very often (≥ 1/10), often (≥ 1/100 to <1/10), infrequently (≥ 1/1000 to <1/100), rarely (≥ 1/10000 to <1/1000), very rarely (<1/10000), the frequency is not set (it is impossible to estimate based on available data).

    From the nervous system:

    Very often: sedation.

    Often: sweating, drowsiness, dizziness, dry mouth, headache.

    Rarely: numbness or sensation of tingling of the head, nervousness, tremor, symptoms of the "withdrawal" syndrome, paresthesia.

    Very rarely: euphoria.

    From the side of the psyche:

    Often: dysphoria.

    Very rarely: hallucinations, confusion, personality disorders.

    From the respiratory system, chest and mediastinum:

    Rarely: difficulty breathing.

    From the cardiovascular system:

    Very rarely: hypotension, hypertension, pulmonary edema.

    From the side of the organ of vision:

    Very rarely: lacrimation, blurred vision.

    From the immune system:

    Very rarely: allergic reactions.

    From the skin and subcutaneous fat:

    Rarely: pain at the injection site, hives.

    From the gastrointestinal tract:

    Often: nausea, vomiting.

    Pregnancy, postpartum and perinatal conditions:

    Very rarely: respiratory depression in newborns, oppression of blood circulation in newborns.

    Nalbuphine can cause withdrawal symptoms in patients with opioid dependence.

    Application during childbirth nalbuphine, solution for injection, can cause respiratory depression and / or blood flow in infants with serious consequences. In such cases, naloxone hydrochloride is used as an antidote.

    Overdose:

    Symptoms: hypoventilation, alteration of consciousness (up to coma), periodic Cheyne-Stokes respiration, pallor, hypothermia, miosis, lowering blood pressure, heart failure, rhabdomyolysis, paralysis of the respiratory center.

    Treatment: with respiratory depression - intravenously naloxone. Maintenance of adequate pulmonary ventilation and central hemodynamics, symptomatic and supportive therapy.

    Interaction:

    Dampening effect on the central nervous system and breathing medicines for general anesthesia, hypnotics, antihistamines, anxiolytic, antipsychotic drugs, antidepressants, muscle relaxants.

    Alcohol enhances the inhibitory effect of nalbuphine on the central nervous system.

    Partially reduces the analgesic effect and respiratory depression of other opioid analgesics (should not be combined with othernarcotic 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.

    Medicines with anticholinergic activity, antidiarrhoeal agents (incl. 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 ganglion blockers, diuretics).

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

    Reduces the effect of metoclopramide.

    With caution should be used simultaneously with MAO inhibitors because of possible overexcitation or inhibition with the emergence of hyper- or hypotensive crises (first, to assess the effect of interaction, the dose should be reduced to 1/4 of the recommended).

    Naloxone reduces the effect of opioid analgesics,as well as the respiratory depression and central nervous system caused by them; higher doses may be required to level the effects of butorphanol, nalbuphine and pentazocine, which have been 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 "cancel" 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).

    Pharmaceutically compatible with a 0.9% solution of NaCI, 5% dextrose solution, Hartmann solution and in glass, polyvinyl chloride, polyethylene containers.

    Special instructions:

    Do not use more than 3 days and exceed the dosage because of the possibility of developing physical dependence.

    In patients with drug dependence, the drug can cause an acute attack of abstinence.

    There is a slight risk of drug overdose due to the significant antagonistic properties of nalbuphine. A sudden cessation of prolonged use can cause a withdrawal syndrome.

    It is not recommended to apply nalboufine in outpatient settings due to the risk of daytime sleepiness.

    With prolonged use nalboufine can cause respiratory depression, which can trigger the development of respiratory failure.

    Since the metabolism of the drug occurs in the liver, and the excretion of the drug is carried out by the kidneys, it is recommended to lower the dose of the drug for hepatic or renal insufficiency.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, one should refrain from driving or working with other mechanisms.
    Form release / dosage:Solution for injection 10 mg / ml, 20 mg / ml.
    Packaging:

    Ampoules 10 mg / ml. 1 ml per ampoule of clear glass. For 10 ampoules in a plastic pallet along with instructions for use in a pack of cardboard.

    Ampoules 20 mg / ml. 1 ml per ampoule of clear glass.For 5 ampoules in a plastic pallet along with instructions for use in a pack of cardboard.

    Filled syringe 10 mg / ml. 1 ml in a transparent PVC syringe. For 1 syringe in a plastic pallet along with instructions for use in a pack of cardboard.

    Filled syringe 20 mg / ml. 1 ml in a transparent PVC syringe. For 1 syringe in a plastic pallet along with instructions for use in a pack of cardboard.

    Filled syringe tube 10mg / ml. 1 ml in a transparent PVC syringe tube. 1 syringe tube into a plastic container together with instructions for use in a cardboard pack.

    Filled syringe tube 20 mg / ml. 1 ml in a transparent PVC syringe tube. 1 syringe tube into a plastic container together with instructions for use in a cardboard pack.

    Storage conditions:

    In accordance with the rules for the storage of psychotropic substances listed in List 111 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 5 ° C to 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:PL-000437
    Date of registration:28.02.2011 / 04.07.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Roushan Pharma Co., Ltd.Roushan Pharma Co., Ltd. India
    Manufacturer: & nbsp
    Information update date: & nbsp28.05.2018
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