Pharmacological properties of the drug Nalbuphine
A synthetic agonist-antagonist of opioid receptors (agonist of κ- and antagonist of μ-opioid receptors) of the phenanthrene series, structurally close to both naloxone and oxymorphone. Activates the endogenous antinociceptive system through κ-opiate receptors, disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system. By influencing the higher parts of the brain, it changes the emotional coloring of pain. Inhibits conditioned reflexes, has a sedative effect, causes dysphoria, miosis, and stimulates the vomiting center. To a lesser extent than morphine, promedol, fentanyl, depress the respiratory center and affect the motility of the digestive tract. Does not affect hemodynamics. The risk of developing addiction and opioid dependence with controlled use is significantly lower than for opioid agonists. With intravenous administration, the effect develops within a few minutes, with intramuscular administration - after 10–15 minutes. The maximum effect occurs after 30–60 minutes, duration of action is 3–6 hours. When administered orally, it is 4–5 times less active than when administered intramuscularly. The time to reach maximum concentration with intramuscular administration is 0.5–1 hour. Metabolized in the liver. It is excreted in the form of metabolites with bile and excreted in small quantities by the kidneys. Penetrates the placental barrier and can cause respiratory depression in the newborn during the postpartum period. Less than 1% is excreted in breast milk. The half-life is 2.5–3 hours.
Nalbuphine injection solution for injection 10 mg/ml 1 ml No. 10
Compound
active ingredient: nalbuphine hydrochloride;
1 ml of nalbuphine hydrochloride dihydrate in terms of nalbuphine hydrochloride anhydrous 10 mg or 20 mg
excipients: sodium metabisulfite (E 223), sodium, sodium chloride, citric acid, diluted hydrochloric acid, water for injection (10 mg/ml) sodium metabisulfite (E 223), sodium, citric acid, diluted hydrochloric acid, water for injection (20 mg/ml).
Dosage form
Injection.
Basic physical and chemical properties: transparent, colorless or almost colorless solution.
Pharmacological group
Analgesics. Opioids. Morfinan derivatives. ATX code N02A F02.
Pharmacological properties
Pharmacodynamics.
Nalbuphine is an opioid analgesic of the opioid receptor agonist-antagonist group (it is a kappa receptor agonist and a mu receptor antagonist). It disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system, affecting the higher parts of the brain. Inhibits conditioned reflexes, has a sedative effect, causes dysphoria, miosis, and stimulates the vomiting center. To a lesser extent than morphine, promedol, fentanyl disrupts the respiratory center and affects the motility of the gastrointestinal tract. Does not affect hemodynamics. The risk of developing addiction and opioid dependence with controlled use is significantly lower than for opioid antagonists. When administered intravenously, the effect develops within a few minutes; when administered intravenously, the effect develops within 10-15 minutes. The maximum effect is after 30-60 minutes, duration of action is 3-6 hours.
Pharmacokinetics.
The drug has a rapid analgesic effect. The time to reach the maximum concentration of the drug in the blood upon administration is 0.5-1 hour. Metabolized in the liver. It is excreted in the form of metabolites in bile and in small amounts in urine. Passes through the placental barrier and during childbirth can cause respiratory depression in the newborn. Passes into breast milk. The half-life is 2.5 - 3:00.
Indications
Pain syndrome of strong and moderate intensity; as an additional means during anesthesia, to reduce pain in the pre- and postoperative period, pain relief during childbirth.
Contraindications
Hypersensitivity to nalbuphine hydrochloride or to any of the ingredients of the drug. The drug should not be used in cases of respiratory depression or severe depression of the central nervous system, increased intracranial pressure, head trauma, acute alcohol intoxication, or alcoholic psychosis. Epileptic syndrome acute surgical diseases of the abdominal organs (before diagnosis) surgical interventions on the hepatobiliary system (spasm of the sphincter of Oddi is possible) drug dependence on morphine-like drugs (morphine, promedol, fentanyl) - the possibility of developing withdrawal syndrome; diarrhea due to pseudomembrane colitis caused by cephalosporins, lincosamines, penicillins; toxic dyspepsia.
With caution: old age, cachexia, liver and kidney failure, respiratory failure (including chronic obstructive pulmonary diseases, uremia), premature birth and possibly fetal immaturity, cholelithiasis, severe inflammatory bowel disease, bronchial asthma, arrhythmia, arterial hypertension, hypothyroidism, prostatic hyperplasia, urethral stenosis, suicidal tendencies, emotional lability; weakened patients. It is not recommended to use the drug without appropriate diagnostics for surgical abdominal syndrome, since nalbuphine can mask its manifestations.
Special security measures.
Nalbuphine should only be used as an adjuvant for general anesthesia by a specially trained specialist. Safety precautions regarding the possible occurrence of respiratory depression, namely naloxone, intubation and mechanical ventilation equipment, must be kept on guard.
Interaction with other drugs and other types of interactions.
Under close supervision and in reduced doses, the drug should be used against the background of the action of anesthesia, hypnotics, anxiolytics, antidepressants and antipsychotics to prevent excessive depression of the central nervous system and suppression of the activity of the respiratory center. Alcohol also enhances the inhibitory effect of nalbuphine on the central nervous system. The drug should not be used together with other narcotic analgesics due to the risk of weakening the analgesic effect and the possibility of provoking withdrawal syndrome in patients with addiction to opioids.
Concomitant use of nalbuphine with phenothiazine derivatives and penicillin preparations may increase nausea and vomiting.
Medicines with anticholinergic activity, antidiarrheals, incl. loperamide, increase the risk of developing constipation to intestinal obstruction, urinary retention and depression of the central nervous system. Strengthens the hypotensive effect of drugs that lower blood pressure, incl. ganglion blockers, diuretics. Reduces the effectiveness of metoclopramide. Caution should be used together with MAO inhibitors due to possible overexcitation or inhibition with the development of hyper- or hypotensive crises (initially, to assess the effect of interaction, the dose should be reduced to ¼ of the recommended).
Features of application
The drug should be used with caution in emotionally unstable patients. In patients with drug addiction, the drug can cause an acute withdrawal attack. When used simultaneously with other morphine derivatives, physical and mental dependence is possible during prolonged use. Sudden cessation of nalbuphine use may cause withdrawal symptoms with prolonged use. It is not recommended to use this drug in an outpatient setting due to the risk of daytime sleepiness.
For dosing Nalbuphine Injection 10 mg, solution for injection 10 mg/ml, sodium content
2.84 mg/ml in each ampoule; for dosing Nalbuphine Injection 20 mg, solution for injection 20 mg/ml, sodium content is 2.447 mg/ml in each ampoule. This should be taken into account when used in patients on a strict low sodium diet.
Nalbuphine has a moderate ability to cause respiratory depression, so its use may provoke the development of respiratory failure.
Due to the fact that the drug is metabolized in the liver and excreted by the kidneys, the need to use nalbuphine in patients with hepatic and/or renal insufficiency should be carefully considered, and if necessary, reduce the dose and carefully monitor the patient’s condition.
When using nalbuphine in patients who are planning surgical intervention for surgical pathology of the digestive system, one should keep in mind the high risk of developing spasm of the sphincter of Oddi.
In morphine-dependent individuals or patients who have undergone morphine therapy, a withdrawal syndrome may occur due to the antagonistic properties of nalbuphine hydrochloride. Nalbuphine may interfere with enzymatic laboratory tests used to determine drug dependence.
It is not recommended to use the drug without appropriate diagnostics for surgical abdominal syndrome, since nalbuphine hydrochloride can mask its manifestations.
Use during pregnancy or breastfeeding.
Due to the lack of research, the drug should not be prescribed during pregnancy and breastfeeding.
The drug should only be used during childbirth for pain relief. After using the drug, the mother should constantly monitor the following indicators in newborns: respiratory depression, apnea, bradycardia, arrhythmia. These effects can be prevented by giving the pregnant woman naloxone during labor.
The ability to influence the reaction rate when driving vehicles or other mechanisms.
During treatment with nalbuphine, you should refrain from driving vehicles and operating machinery.
Directions for use and doses
Use the drug intravenously and intramuscularly.
The dosage should correspond to the intensity of pain, the physical condition of the patient and take into account the interaction with other concomitantly used drugs. The dose of the drug and the frequency of administration should be carefully calculated to avoid drug dependence. For pain relief, the usual recommended dose is 0.15-0.3 mg per 1 kg of body weight; if necessary, administration can be repeated every 4-6 hours.
Patients with opiate dependence may develop withdrawal symptoms (withdrawal) when taking nalbuphine. In this case, it is necessary to prescribe morphine intravenously slowly with a gradual increase in dose until the pain disappears. If the patient was receiving morphine, meperidine, codeine or another opioid analgesic with a similar duration of activity before prescribing nalbuphine, it is necessary to first prescribe nalbuphine at a dose of 25% of the patient's required dose and monitor for the possible occurrence of withdrawal symptoms (abdominal cramps, nausea, vomiting, lacrimation, rhinorrhea , anxiety, excitability, hyperthermia or piloerection). If withdrawal symptoms do not occur, the dose of nalbuphine should be gradually increased at the recommended intervals until the required level of pain relief is achieved.
The maximum single dose for adults is 0.3 mg per 1 kg of body weight, the maximum daily dose is 2.4 mg per 1 kg of body weight. The duration of use of nalbuphine depends on the patient's condition and should be as short as possible to avoid mental or physical dependence.
For myocardial infarction, 20 mg of the drug is injected slowly into a vein is often sufficient, but the dose may need to be increased to 30 mg. In the absence of clear positive dynamics of the pain syndrome - 20 mg again after 30 minutes.
When using nalbuphine as an adjuvant for anesthesia, higher doses are required than for pain relief. For premedication - 100-200 mcg/kg body weight. When conducting intravenous anesthesia: for induction of anesthesia - 0.3-1 mg / kg for 10-15 minutes, for maintaining anesthesia 250-500 mcg / kg slowly, every 30 minutes.
For pain relief during childbirth, the drug should be used in a dose of 20 mg intramuscularly.
Prescribe the drug with caution to elderly patients, with general exhaustion or poor respiratory function. In this case, use should be started with the minimum effective doses due to the more frequent occurrence of adverse reactions.
Children
Do not use the drug for children.
Overdose
In case of overdose, respiratory depression and periodic Cheyne-Stokes breathing occur; drowsiness, dysphoria, changes in consciousness up to coma; pale skin, hypothermia, miosis; decreased blood pressure, cardiovascular failure.
The specific antidote is naloxone hydrochloride. In case of intoxication, carry out symptomatic therapy.
Adverse reactions
When using the drug, adverse reactions may occur.
From the nervous system: dizziness, general weakness, headache, sedation, diplopia, nervousness, depression, agitation, tearfulness, euphoria, hostility, drowsiness, nightmares, hallucinations, tinnitus, confusion, dysphoria, paresthesia, feeling of unreality, speech impairment, mood changes; cramps, muscle rigidity, tremors, involuntary muscle contractions.
From the cardiovascular system: increased or decreased blood pressure, bradycardia, tachycardia.
From the digestive tract: dry mouth, colic, constipation, dyspepsia, bitter taste, anorexia; symptoms of gastrointestinal irritation; spasm of the biliary tract, in inflammatory bowel diseases - paralytic intestinal obstruction and toxic megacolon (constipation, flatulence, nausea, gastralgia, vomiting).
From the respiratory system: respiratory depression, decreased minute volume of breathing, shortness of breath, asthmatic attacks.
Skin: increased skin moisture, itching, urticaria, feeling of heat; icterus of the sclera and yellowness of the skin; changes at the injection site, including pain.
Allergic reactions: shock, respiratory distress syndrome, angioedema, facial swelling, sneezing, bronchospasm, pulmonary edema, skin rashes, increased sweating.
Others: hot flashes, blurred vision; decreased diuresis, frequent urge to urinate, spasm of the urinary tract, hepatotoxicity (dark urine, white feces), drug dependence, withdrawal syndrome (cramping abdominal pain, nausea, vomiting, rhinorrhea, lacrimation, weakness, anxiety, increased body temperature).
Best before date
3 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children. Do not freeze.
Incompatibility
Do not mix in the same syringe with other injection solutions.
Nalbuphine is compatible with 0.9% sodium chloride solution, 5% Hartmann solution.
Package
1 ml of solution (10 mg/ml) in ampoules No. 10 in a cardboard box.
1 ml of solution (20 mg/ml) in ampoules No. 5, in a cardboard box.
Vacation category
On prescription.
Manufacturer
Rusan Pharma Ltd.
Manufacturer's location and address of place of business
Khasra No.122, MI, Central Hopetown, Selakui, Dehradun - 248197, Uttarakhand, India.
Use of the drug Nalbuphine
S/c, i/m, i/v. For pain - IV or IM 0.15–0.3 mg/kg. Can be administered repeatedly, if necessary, every 4–6 hours. The maximum single dose is 0.3 mg/kg, the maximum daily dose is 2.4 mg/kg. The duration of the appointment is no more than 3 days. If myocardial infarction is suspected, 10–20 mg IV slowly. If necessary, the dose can be increased to 30 mg. In the absence of clear positive dynamics of the pain syndrome - 20 mg again after 30 minutes. For premedication - 100–200 mcg/kg. For induction of anesthesia - 0.3-1 mg/kg over a period of 10-15 minutes, for maintenance of anesthesia - 250-500 mcg/kg every 30 minutes. The initial single dose for children is 300 mcg/kg IV, IM, SC. You can re-enter if necessary.
Side effects of the drug Nalbuphine
Lethargy, drowsiness, confusion, dizziness, headache, agitation, euphoria or depression, hallucinations; lability of blood pressure and heart rate; nausea, vomiting, dry mouth, dyspepsia, cramping pain; urticaria, anaphylactic or anaphylactoid shock, bronchospasm, laryngeal edema, itching, sneezing; pulmonary edema; decrease in minute volume of breathing; increased sweating, pain at the injection site, drug dependence, drug withdrawal syndrome (cramping abdominal pain, nausea, vomiting, rhinorrhea, lacrimation, general weakness, anxiety, fever).
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DOSAGE FORMS injection solution 10 mg/ml
MANUFACTURERS Serb SA (France)
GROUP Opiate antagonists
COMPOSITION Active ingredient: Nalbuphine.
INTERNATIONAL NON-PROPENTED NAME Nalbuphine
SYNONYMS Nalbufin Serb, Nubain
PHARMACOLOGICAL ACTION Analgesic (narcotic). It has properties as an agonist-antagonist of opiate receptors. Depresses the central nervous system, has an analgesic, hypnotic, and antitussive effect. Well absorbed by any route of parenteral administration. The half-life is 3-6 hours. It undergoes biotransformation in the liver, metabolites are excreted with bile into the intestines, and then removed from the body with feces. Excreted in urine in small quantities.
INDICATIONS FOR USE Pain syndrome of moderate and severe intensity during myocardial infarction, in preparation for surgery (prevention) and in the postoperative period; as an additional means of pain relief during general anesthesia.
CONTRAINDICATIONS Hypersensitivity.
SIDE EFFECTS From the nervous system and sensory organs: drowsiness, depression of the respiratory center, headache, euphoria or depression, dysphoria, hallucinations. From the cardiovascular system and blood (hematopoiesis, hemostasis): hypertension/hypotension, bradycardia/tachycardia, pulmonary edema. From the gastrointestinal tract: dry mouth, nausea, vomiting, dyspepsia, cramping pain. Allergic reactions: anaphylactic or anaphylactoid shock, bronchospasm, urticaria, laryngeal edema, itching, sneezing. Other: increased sweating, pain at the site of intramuscular injection.
INTERACTION General anesthetics, tranquilizers, sedatives and hypnotics, alcohol enhance the effect, incl. side effects (with combination therapy, it is necessary to reduce the dose of nalbuphine and/or these drugs).
OVERDOSE Symptoms: increased side effects, loss of consciousness, coma, periodic breathing of the Cheyne-Stokes type, pallor and decreased skin temperature, decreased body temperature, miosis; death (paralysis of the respiratory center). Treatment: gastric lavage, intravenous administration of specific antidotes - naloxone or nalorphine, oxygen therapy, maintenance of vital functions.
SPECIAL INSTRUCTIONS It is not recommended to use more than 3 days and exceed the dosage, because physical dependence is possible. Sudden cessation of use after prolonged use may cause withdrawal symptoms (cramping abdominal pain, nausea, vomiting, rhinorrhea, lacrimation, weakness, anxiety, increased body temperature). Prescribe with caution in case of emotional instability, drug addiction (high probability of developing an acute attack of withdrawal). Due to the sedative and hypnotic effects, it should not be used on an outpatient basis by vehicle drivers and people whose profession requires a quick mental and motor reaction. The finished dosage form contains sodium disulfite as a preservative, which can cause asthma attacks, anaphylactic or anaphylactoid shock in patients with bronchial asthma (with hypersensitivity to sulfite).
STORAGE CONDITIONS Protected from light, at room temperature.
Drug interactions Nalbuphine
Strengthens the inhibitory effect on the central nervous system of drugs for general anesthesia, hypnotics, antihistamines, anxiolytics, antipsychotics, antidepressants. Ethanol enhances the inhibitory effect on the central nervous system. It should not be combined with other narcotic analgesics due to the risk of weakening analgesia and the possibility of provoking drug withdrawal syndrome in patients with drug addiction. In combination with phenothiazine and penicillin derivatives, it may increase nausea and vomiting. Pharmaceutically compatible with 0.9% sodium chloride solution, 5% dextrose solution and Hartmann solution in glass, polyvinyl chloride, polyethylene containers.
Overdose of the drug Nalbuphine, symptoms and treatment
Manifested by hypoventilation of the lungs, loss of consciousness, periodic Cheyne-Stokes breathing, pallor of the skin, hypothermia, miosis, decreased blood pressure, cardiovascular failure, stupor, coma, depression of the respiratory center. Control and maintenance of adequate pulmonary ventilation, systemic hemodynamics and body temperature, and oxygen therapy are indicated. For respiratory depression - IV naloxone or nalorphine.
List of pharmacies where you can buy Nalbuphine:
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Nalbuphine
From the nervous system and sensory organs: more often - drowsiness (36%), headache (3%); less often - dizziness, fatigue, general weakness, lethargy; rarely (less than 1%) - nervousness, euphoria, discomfort, blurred visual perception, diplopia, restless sleep, nightmares, unusual dreams, depression, confusion (hallucinations, depersonalization), in children - paradoxical arousal, anxiety; frequency unknown - ringing in the ears, convulsions, muscle rigidity (especially respiratory), tremors, involuntary muscle twitching.
From the cardiovascular system: less often - decrease in blood pressure; rarely (less than 1%) - arrhythmias (tachycardia/bradycardia), increased blood pressure.
From the respiratory system: rarely (less than 1%) - respiratory depression (decreased minute volume of breathing).
From the digestive system: less often - dry mouth (4%), anorexia, nausea and/or vomiting (6%); rarely - irritation of the gastrointestinal tract, spasm of the biliary tract, in inflammatory bowel diseases - paralytic intestinal obstruction and toxic megacolon (constipation, flatulence, nausea, stomach cramps, gastralgia, vomiting); frequency unknown - constipation, hepatotoxicity (dark urine, pale stools, icterus of the sclera and skin).
From the urinary system: rarely (less than 1%) - decreased diuresis, spasm of the ureters (difficulty and pain when urinating, frequent urge to urinate).
Allergic reactions: less often - urticaria, skin rash, itching, swelling of the face; rarely (less than 1%) - bronchospasm, angioedema, laryngospasm; in extreme cases - anaphylactic or anaphylactoid shock.
Local reactions: hyperemia, swelling, burning at the injection site, pain at the injection site.
Other: less often - increased sweating; frequency unknown - drug dependence, withdrawal syndrome (spastic abdominal pain, nausea, vomiting, rhinorrhea, lacrimation, weakness, anxiety, increased body temperature).
Overdose. Symptoms of acute and chronic overdose: cold sticky sweat, pale skin, miosis, hypothermia, confusion, dizziness, drowsiness, decreased blood pressure, cardiovascular failure, nervousness, fatigue, bradycardia, severe weakness, periodic Cheyne-Stokes breathing, hypoventilation of the lungs , hypothermia, anxiety, miosis, convulsions, in severe cases - loss of consciousness, paralysis of the respiratory center, respiratory arrest, stupor, coma.
Treatment: maintaining adequate pulmonary ventilation, systemic hemodynamics and body temperature, oxygen therapy; for respiratory depression - intravenous administration of a specific antagonist of opioid analgesics, naloxone or nalorphine.
