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Nalbuphine

Pharmacological action

Opioid analgesic, opioid receptor antagonist. It activates the endogenous antinociceptive system primarily through opioid receptors and thus disrupts the interneuronal transmission of pain impulses at various levels of the CNS, as well as changing the emotional coloration of pain by affecting the higher parts of the brain.


It has analgesic effect comparable to morphine, has sedative effect, stimulates the vomiting center, causes myosis, inhibits conditioned reflexes. To a lesser extent than opioid μ-receptor agonists (morphine, peridol, fentanyl) depresses the respiratory centre. Does not have a significant effect on hemodynamics and gastrointestinal tract motility.


Analgesic effect develops rapidly: at w / i - in a few minutes, at w / m - after 10-15 minutes. Maximum effect is achieved in 1-2 hours, duration of action is 3-6 hours.


Pharmacokinetics Nalbuphine .

Metabolized in the liver.


T1/2 is 2.5-3 hours. Unchanged nalbufin is mainly excreted in the urine (about 70%), in the form of metabolites - mainly bile.


Readings at .

Expressed pain syndrome of various genesis (including in the postoperative period, myocardial infarction, gynecological interventions, malignant tumors); premedication before inhalation, as a component of anaesthesia.

Dosing mode

Individual. Input in/in, in/m and p/k. For adults, a single dose varies from 100 µg/kg to 1 mg/kg. For children the initial single dose is 300 µg/kg. The frequency of administration depends on indications and the clinical situation. The duration of administration is not more than 3 days.

Side effect

CNS and peripheral nervous system: often - drowsiness, retardation; possible - dizziness, balance disorders, headache; rarely - nervousness, depression, mental confusion, dysphoria; in some cases - speech difficulties, blurred vision.


From the digestive system: possible nausea, vomiting, dry mouth.

Nalbuphine Dosage

The cardiovascular system: in some cases - arterial hypertension or hypotension, bradycardia, tachycardia.


Allergic reactions: in some cases - hives.


Others: sweating may be increased.


Nalbuphine Contraindications to use: in some cases - hives, bradycardia, tachycardia, etc.

Nalbufine hypersensitivity.

Application during pregnancy and lactation

Use during pregnancy is possible only on strict indications.


Caution is exercised during premature birth and presumed immaturity of the fetus (because nalbufin penetrates the placental barrier and can cause respiratory depression in the newborn).


It is used with caution during lactation (breastfeeding).


Nalbufine is excreted with mother's milk in very small, clinically insignificant amounts (less than 1% of the injected dose).


Use in disorders of liver function

In the event of liver failure, nalbufin should be dosed carefully and provision should be made for rapid cessation of administration.

Use in renal function disorders

In case of renal failure, nalbufin should be dosed carefully and provision should be made for rapid cessation of administration.

Use in elderly patients

Caution should be exercised in elderly persons.

Specific instructions

Caution should be exercised in respiratory disorders (including obstructive pulmonary diseases, emphysema), because nalbufin can cause a 20-25% reduction in the minute volume of breathing (when administered in a dose of 20 mg by 70 kg of body weight), in uremia, in elderly people, with severe exhaustion.
https://reference.medscape.com/drug/nalbuphine-343329



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