Nalbuphine

Nalbuphine is a narcotic pain reliever. It belongs to the class of drugs called agonist-antagonists, which act on opiate receptors.

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Indications Nalbuphine

It is indicated for the treatment of severe pain syndromes (this also includes pain during childbirth and postoperative pain). In addition, the drug is used as an auxiliary in performing anesthesia.

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Release form

It is produced as an injection solution in 1 ml glass ampoules. The package with the medicine Nalbuphine 10 contains 10 such ampoules, and the pack of Nalbuphine 20 contains 5 ampoules with the solution.

Nalbuphine Serb has a depressant effect on the central nervous system, and also has hypnotic, analgesic, and antitussive properties. The drug is capable of exerting an excitatory effect on μ-receptors, as well as blocking ҡ-receptors.

Nalbuphine-Pharmex is considered a powerful opioid painkiller. It effectively eliminates severe pain - in its effect, the drug is very similar to the properties of morphine and its derivatives on the human body. But at the same time, unlike this drug, Nalbuphine-Pharmex does not provoke the development of irreversible changes in the brain. The development of addiction (psychological and physical) is possible only in cases where the drug is combined with other morphine derivatives.

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Pharmacodynamics

Nalbuphine hydrochloride is a µ-ending antagonist and a ҡ-ending agonist. The drug disrupts the transmission of pain signals between neurons at various levels of the central nervous system, affecting the higher parts of the brain. The solution slows down conditioned reflexes, and also has powerful sedative properties, activates the vomiting center, and provokes dysphoria with miosis.

The active ingredient affects (less strongly than fentanyl with morphine and promedol) the motility of the gastrointestinal tract, as well as the respiratory center.

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Pharmacokinetics

After intramuscular administration, the drug effect begins after 10-15 minutes. The drug achieves its analgesic effect half an hour after administration. The duration of the drug effect is 3-6 hours (a more accurate figure depends on the characteristics of the patient's body).

When administered intravenously, the peak levels of the active substance in the plasma are observed after 0.5-1 hour.

The drug is metabolized in the liver, resulting in the formation of pharmacologically inactive decay products.

Excretion also occurs mainly in the liver, and only a small portion of the substance is excreted through the kidneys. The half-life of the drug is approximately 2.5-3 hours.

Nalbuphine hydrochloride is able to cross the hematoplacental barrier and can be found in breast milk.

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Dosing and administration

The drug can be administered both intramuscularly and intravenously. The dose is selected individually for each patient, taking into account their tolerance to the drug, as well as the intensity of pain and the characteristics of the patient's body.

The adult dose is often 0.15-0.3 mg/kg. The interval between procedures should be at least 4 hours. The maximum single recommended dose is 0.3 mg/kg. No more than 2.4 mg/kg of the medicinal solution can be administered per day. It is prohibited to use the medicine for more than 3 days in a row.

In case of myocardial infarction, 20 mg of nalbuphine hydrochloride is usually administered (single intravenous administration). The rate of administration of the solution should be slow. If necessary, it is allowed to increase the single dose to 30 mg. If there is no positive result (pain relief) within half an hour after the administration of the drug, a repeat procedure must be performed - 20 mg of Nalbuphine must be administered.

During preoperative preparation of the patient, 100-200 mcg/kg of the drug is usually administered.

In case of intravenous anesthesia, nalbuphine is used in a dose of 0.3-1 mg/kg to induce anesthesia, and then the drug should be administered in a dose of 250-500 mcg/kg every subsequent half hour to maintain anesthesia.

It is also necessary to take into account that people suffering from opiate dependence are at risk of developing withdrawal syndrome when using Nalbuphine (morphine can relieve them). People who received codeine or morphine and other opioid painkillers before starting to use nalbuphine should be prescribed the latter in the amount of 25% of the usual dose.

The solution should be administered by an experienced doctor. He or she should have at hand all the means necessary to eliminate a possible overdose (including naloxone, as well as equipment for performing artificial pulmonary ventilation, as well as intubation).

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Use Nalbuphine during pregnancy

The drug should not be used during pregnancy. During labor, the drug may cause apnea, bradycardia, as well as respiratory depression and cyanosis in the newborn.

Careful monitoring of neonates whose mothers were administered Nalbuphine during labor is required.

Contraindications

Among the contraindications:

• the patient has hypersensitivity to the active substance of the drug;
• use in children;
• It is prohibited to use the medicinal solution in people with TBI, acute alcohol intoxication, high intracranial pressure, and also in cases of respiratory and central nervous system function suppression, as well as in cases of alcoholic psychosis and severe renal (hepatic) pathologies;
• Prescribing medication to emotionally unstable patients (and also to people with a history of drug addiction) is permitted only after a balanced assessment of the possible benefits and risks to the patient.

The drug should be prescribed with caution to people who suffer from liver or kidney dysfunction, in conditions accompanied by vomiting with nausea and myocardial infarction, and in addition to this, to people who are about to undergo surgery in the hepatobiliary system (since there is a risk of spasm in the sphincter of Oddi). In addition, caution is required when prescribing to elderly or weakened patients.

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Side effects Nalbuphine

The following side effects may develop when using the solution:

• cardiovascular system organs: changes in heart rate and blood pressure;
• gastrointestinal tract: vomiting, epigastric pain, nausea, bitter taste in the mouth or dry mouth, as well as intestinal spasms and indigestion;
• PNS and CNS organs: dizziness or headaches, development of a feeling of nervousness, excitement, severe anxiety and euphoria, as well as sedation, emotional instability and depression. Along with this, a feeling of fatigue, speech or sleep disorders may appear, and in addition, paresthesia and a feeling of unreality of the situation arise;
• manifestations of allergy: itching, hyperhidrosis, urticaria, bronchospasm, angioedema, sensation of heat and development of respiratory distress syndrome;
• other: development of an asthma attack, shortness of breath, hot flashes and suppression of the respiratory system functions, as well as deterioration of visual acuity and increased urge to urinate. Along with this, the drug can affect the results of enzymatic tests that help to identify the presence of drug addiction.

In case of sudden cessation of drug use after a long course of treatment, the patient may develop so-called withdrawal syndrome.

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Overdose

The use of drugs in high doses can suppress the function of the central nervous system - patients experience dysphoria and a feeling of drowsiness, as well as suppression of the respiratory system.

In case of overdose, symptomatic treatment will be required, and in case of severe poisoning with the drug, the patient should be given naloxone hydrochloride (a specific antidote to Nalbuphine).

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Interactions with other drugs

Combining the drug with neuroleptics, anxiolytics, as well as sleeping pills, antidepressants and general anesthetics is possible only under the supervision of a doctor. If such combinations of drugs are used, the doses of Nalbuphine should be adjusted.

Combination of the drug with ethanol and other narcotic analgesics is prohibited.

In case of combined use of Nalbuphine and phenothiazine derivatives, as well as penicillins, the likelihood of developing vomiting with nausea increases.

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Storage conditions

The solution should be stored at a temperature of no more than 25 ^o C. Freezing the medicine is prohibited.

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Shelf life

Nalbuphine can be used for a period of 3 years from the date of manufacture of the medicinal solution.

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