Nalbufin

By its chemical structure, nalbuphine is close to morphine , however, a characteristic feature of the nalbuphine molecule (see also the butorphanol formula) is the presence of a methylcyclobutyl radical instead of a methyl group (—CH ₃ ) at the nitrogen atom.

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

When administered intramuscularly, nalbuphine is not inferior to morphine in analgesic activity and is 2.5-3 times more active than pentazocine . When injected, nalbuphine is 4-5 times less active than when introduced into the muscles.

The peak concentration in plasma is observed after 30 min - 1 h after intramuscular injection; elimination half-life - 3-6 hours. It is metabolized in the liver; metabolites excreted with bile in the intestines. With urine excreted in small quantities.

Nalbuphine is used for pain of moderate and severe severity after operations, with myocardial infarction. The possibility of using nalbuphine for pain of a different origin is being studied.

Adults are administered 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 injections every 3-4 hours. The maximum single dose is 0.3 mg / kg, the maximum daily dose is 2.4 mg / kg (which, respectively, with a body weight of 70 kg, 20 and 160 mg). Children are administered at the rate of 0.1-0.25 mg / kg. The maximum single dose is 0.25 mg / kg, the maximum daily dose is 2 mg / kg.

Nalbuphine is a relatively new drug; its scope and its possible side effects continue to be studied. It is recommended to use the drug for no more than 3 days. The sedative effect of the drug is relatively pronounced. The inhibitory effect on respiration is similar to that of morphine. Relatively rarely, headache, increased sweating, dry mouth, nausea, and vomiting are observed. 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 childbirth, can cause respiratory depression in newborns. Caution is needed when using the drug in pregnant women.

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

It should be noted that in the finished dosage form, nalbuphine (nubain) contains sodium disulfite as a preservative, which can cause asthma in patients with bronchial asthma (with increased sensitivity to sulfite).

In addicts, the use of nalbuphine can cause an acute episode of withdrawal.

Decree of the Government of the Russian Federation of April 23, 2012 No. 359 “On Amending Certain Acts of the Government of the Russian Federation in Connection with Improving Control of the Traffic in Psychotropic Substances” Nalbufin is included in list III of the list of narcotic drugs, psychotropic substances and their precursors to be controlled in the Russian Federation Federation. The decision entered into force on August 6, 2012.

Included in the kit of a medical doctor’s kit, like an analgesic.

Storage: subject to storage rules for narcotic analgesics.

• Forth, Henschler, Rummel, Förstermann, Starke (Hrsg.): Allgemeine und spezielle Pharmakologie und Toxikologie . 8. Auflage. Urban & Fischer Verlag München, Jena, Berlin Mai 2001, ISBN 3-437-42520-X , S. 254, 255, 260, 261.
• The Ministry of Health of the Republic of Ukraine on delivery to the warehouse of the first-aid kit first-rate to NATO standards