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Description of the medicine: Nalbuphine

NALBUFHINE *. 17- (Cyclobutylmethyl) -4, 5a-epoxymorphinan-3, 6a, 14-triol.

Synonyms: Nubain, Nubain.

Produced in the form of hydrochloride.

On the chemical structure, nalbuphine is close to morphine, but the presence of a methylcyclobutyl radical instead of the methyl group (-CH3) at the nitrogen atom is also a characteristic feature of the nalbuphin molecule (see also the formula of butorphanol).

Pharmacologically, nalbuphine is an opiate receptor antagonist agonist. The analgesic effect is mainly due to the agonist effect on c-receptors, but at the same time the drug is an antagonist of m-receptors, and therefore does not have a pronounced euphoric effect. The general nature of the action of nalbuphine is close to pentazocine, but it has a stronger analgesic effect with less side effects and less ability to develop tolerance and physical dependence.

With intramuscular injection, nalbuphine is not inferior to morphine by analgesic activity and is 2.5-5 times more active than pentazocine. When administered orally, nalbuphine is 4 to 5 times less active than when injected into the muscles.

The peak concentration in plasma is observed after 30 min - 1 h after intramuscular injection; Half-life - 3 - 6 hours Metabolised in the liver; Metabolites are excreted with bile in the intestine. It is excreted in small quantities in urine.

Apply nalbuphin for moderate to severe pain after surgery, with myocardial infarction. The possibility of using nalbuphine for pain of other origin is being studied.

Introduce adults intravenously or intramuscularly at the rate of 0.15-0.3 mg (0.00015 - 0.0003 g) per 1 kg of body weight. If necessary, repeat the injection every 3 to 4 hours. The maximum single dose is 0.3 mg / kg, the maximum daily dose is 2, 4 mg / kg (which is respectively at a body weight of 70 kg 20 and 160 mg). Children are administered at a rate of 0.1-0.25 mg / kg. The maximum single dose of 0.25 mg / kg, the maximum daily dose - 2 mg / kg.

Nalbuphine is a relatively new drug; The field of its application and its possible side effects continue to be studied. It is recommended not to apply the drug for more than 3 days. Relatively strongly expressed sedative effect of the drug. The inhibitory effect on respiration is similar to that of morphine. Relatively rare are headache, increased sweating, dry mouth, nausea, vomiting. The drug has little effect on the activity of the cardiovascular system, on the motility of the gastrointestinal tract.

Caution is required when prescribing nalbuphine to patients with respiratory depression, impaired liver and kidney function, with increased intracranial pressure.

The drug passes through the placental barrier and, if used during labor, can cause respiratory depression in newborns. Caution is needed when the drug is used in pregnant women.

With intramuscular injection, pain at the injection site is possible.