Nalbuphine

Nalbuphine is a narcotic analgesic. Included in the category of drugs agonist-antagonists, acting on opiate receptors.

[1], [2], [3], [4], [5], [6], [7], [8]

Indications of the nalbuphine

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

[9], [10], [11], [12]

Release form

Produced in the form of an injection solution in ampoules of glass volume of 1 ml. At the same time, there are 10 such ampoules in the package containing the drug Nalbuphin 10, and 20 to 5 ampoules with a solution in the Nalbuphin pack.

Nalbuphine Serb has an overwhelming effect on the central nervous system, but also has sleeping pills, analgesics, and antitussive properties. The drug can exert an exciting effect on the μ-receptors, as well as block ҡ-receptors.

Nalbuphin-Farmex  is considered a powerful opioid analgesic. It effectively eliminates pains of a serious nature - the effect of the drug is very similar to the properties that are provided to the human body by morphine, as well as its derivatives. But at the same time, unlike the given medicine, Nalbufin-Farmex does not provoke the development of irreparable changes in the brain. The development of addiction (psychological as well as physical) is possible only in cases when the drug is combined with other derivatives of morphine.

[13], [14], [15], [16]

Pharmacodynamics

Nalbuphine hydrochloride is a μ-terminal antagonist, as well as an ҡ-terminal agonist. The drug disrupts the transmission of pain signals between the neurons at various levels of the central nervous system, affecting the higher cerebral spinal cord. The solution slows down the conditioned reflexes, and besides it has powerful soothing properties, activates the vomiting center, provokes dysphoria with miosis.

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

[17], [18], [19], [20], [21], [22]

Pharmacokinetics

After the / m administration of medication begins after 10-15 minutes. In this case, the pain medication achieves an analgesic effect in half an hour after administration. The duration of drug exposure is 3-6 hours (a more accurate figure depends on the characteristics of the patient's body).

With IV injection, the peak of the indices of the active substance inside the plasma is observed after 0.5-1 hour.

The metabolism of the drug is carried out in the liver, resulting in the formation of inactive pharmacologically degradable products.

Excretion also occurs mainly in the liver, and only a small part 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 pass through the hematoplacental barrier, and can be found inside the mother's milk.

[23], [24], [25], [26]

Dosing and administration

The drug can be administered both in / m and / in the way. The size of the dose is selected separately for each patient, taking into account the tolerability of the drug, and in addition to this intensity of pain and the characteristics of the patient's body.

The adult dose is often 0.15-0.3 mg / kg. In this case, the interval between the procedures should be at least 4 hours. The maximum of a single recommended dose is 0.3 mg / kg. For a day it is allowed to inject no more than 2.4 mg / kg of a drug solution. It is forbidden to use the medicine for more than 3 days in a row.

In the case of myocardial infarction, 20 mg of nalbuphine hydrochloride is usually administered (one-time IV administration). The rate of solution should be slow. If there is a need, it is allowed to increase a single dose to 30 mg. If the positive result (pain relief) is absent in half an hour after drug administration, it is required to repeat the procedure - to enter 20 mg of Nalbuphin.

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

If an anesthesia is used to inject a person into anesthesia, nalbuphin is used at a rate of 0.3-1 mg / kg, and then, in order to maintain anesthesia, a drug of 250-500 μg / kg should be injected every subsequent half-hour.

It is also necessary to take into account that people suffering from opiate addiction have a risk of developing withdrawal syndrome when using Nalbuphine (morphine can stop them). Persons receiving codeine or morphine and other opioid analgesic drugs before starting the use of nalbuphine are required to prescribe the latter at a rate of 25% of the usual dose.

The solution must be administered by an experienced doctor. At the same time he must have at hand all the means necessary to eliminate a possible overdose (among them naloxone, as well as the availability of equipment for performing artificial pulmonary ventilation, as well as intubation).

[36], [37], [38], [39]

Use of the nalbuphine during pregnancy

Do not use the medicine during pregnancy. During childbirth, the drug can cause apnea in the newborn, bradycardia, as well as suppression of respiratory function and cyanosis.

It is necessary to carefully monitor the state of the newborns, whose mothers were given Nalbuphine during labor.

Contraindications

Among the contraindications:

• presence of a hypersensitivity to the active substance of the medicine;
• use in children;
• It is forbidden to use medicinal solution in persons with CCI, acute form of alcohol intoxication, high index of intracranial pressure, and in addition, with the suppression of respiratory function and function of the central nervous system, as well as in alcoholic psychosis and renal (hepatic) pathologies in severe form;
• the prescription of the drug is emotionally unstable for the patient (and, in addition, people who have a history of addiction) are allowed only after a balanced assessment of the possible benefit and risk to the patient.

Precautions are required to prescribe medication for people who suffer from disorders of hepatic or renal function, in conditions accompanied by vomiting with nausea and myocardial infarction, and in addition to those who soon have to undergo surgery in the hepatobiliary system (since there is a possibility of spasm in the area sphincter of Oddi). In addition, care should be taken when prescribing to elderly or weakened patients.

[27]

Side effects of the nalbuphine

When using the solution, the following side effects may develop:

• CAS organs: changes in the rhythm of heart rate and blood pressure;
• Gastrointestinal organs: vomiting, epigastric pain, nausea, bitter taste in the oral cavity or dryness of the oral mucosa, and besides intestinal spasm and digestive upset;
• organs of the PNS and CNS: the appearance of dizziness or headaches, the development of feelings of nervousness, excitement, severe anxiety and euphoria, and besides sedation, emotional instability and depression. Along with this, there may be a feeling of fatigue, a disorder of speech or sleep, and in addition there is paresthesia and a feeling of unreality in the situation;
• manifestations of allergy: itching, hyperhidrosis, urticaria, bronchial spasm, angioedema, fever and development of respiratory distress syndrome; 
• Other: development of an attack of bronchial asthma, dyspnea, hot flashes and suppression of respiratory system functions, and in addition deterioration of visual acuity and an increase in urge to urinate. Along with this, the drug can affect the indications of enzyme assays that help to identify the presence of drug addiction.

In the case of a sharp halt in the use of drugs after a prolonged course of treatment, the patient may develop a so-called withdrawal syndrome.

[28], [29], [30], [31], [32], [33], [34], [35]

Overdose

The use of drugs in large doses can suppress the function of the central nervous system - in patients there is a dysphoria and sensation of drowsiness, as well as suppression of the respiratory system.

In case of an overdose, symptomatic treatment will be required, and with severe drug poisoning, it is necessary to administer naloxone hydrochloride (Nalbuphin's specific antidote) to the patient.

[40], [41], [42], [43], [44]

Interactions with other drugs

Combine the drug with neuroleptics, anxiolytics, as well as sleeping pills and antidepressants and general anesthetics can be exclusively under the supervision of a doctor. If such combinations of drugs are used, Nalbuphin dosage dosage should be adjusted.

It is forbidden to combine the drug with ethanol, as well as other narcotic analgesics.

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

[45], [46], [47], [48], [49], [50], [51]

Storage conditions

The solution should be kept in conditions of temperature not greater than 25 ^on C. Freeze medicament prohibited.

[52], [53], [54]

Shelf life

Nalbuphine can be used in the period of 3 years from the date of manufacture of the drug solution.

[55], [56], [57], [58]