Nalbuphine

Nalbuphine is a pain reliever that belongs to the group of opioids. It is used for a short time to calm moderate to acute pain and is primarily administered as a solution with varying levels of active ingredient. The substance is also used in anesthesia.

What is nalbuphine?

Nalbuphine is a medicinal substance from the group of painkillers. The substance is assigned to the opioids and has both agonistic and antagonistic effects. In addition to the name nalbuphine, the synonyms are also used Nalbuphini hydrochloridum, Nubain and Nalbuphine hydrochloride used. In chemistry, the empirical formula C21-H27-N-O4 is used. This corresponds to a moral mass of 357.44 g / mol.

Although from a pharmacological point of view, nalbuphine belongs to the group of opioids to which u. a. Even the drug heroin counts, nalbuphine is not subject to the Narcotics Act. Under the trade name Nalpain®, the active ingredient is normally available on prescription as an injection solution.

The analgesic potency of nalbuphine is between the analgesic potency of morphine and codeine. It is therefore given as a pain reliever to relieve moderate to acute pain. It is administered subcutaneously (i.e. as an injection under the skin), intramuscularly (i.e. as an injection into a muscle) or intravenously (i.e. as a solution directly into a vein), as the case may be.

Pharmacological effect

Nalbuphine has pain relieving effects. The substance acts agonistically on a person's kappa receptors. At the same time, it is also antagonistically active on the My receptors. Due to this combined agonistic and antagonistic mode of action, nalbuphine succeeds in counteracting the respiratory depression that is otherwise typical for opioids. Such can e.g. B. occur after an operation in which fentanyl was used for anesthesia. With nalbuphine, respiratory depression can be relieved and pain therapy can be continued at the same time.

The usual dose for an adult with an average body weight (70 kg) is between 10 and 20 mg. This corresponds to 0.1 to 0.3 mg nalbuphine per body weight. It can be administered every three to six hours, with the maximum daily dose for an adult being 20 mg. The duration of action of a dose is three to six hours (depending on the pain intensity).

The onset of the effect depends on the type of award. After intravenous administration, which is common in Europe, the onset of action is recorded after two to three minutes. Intramuscular or subcutaneous injections only cause a noticeable effect on the body after 15 minutes.

Medical application & use

Nalbuphine is a pain reliever. It is one of the opioids.Nevertheless, in Germany it is not subject to the Narcotics Act, but is available as a solution for injection with a prescription.

Preparations with nalbuphine are used to treat moderate to severe pain. However, the treatment is only given for a short time. Nalbuphine is not suitable for long-term use.

The administration of nalbuphine can be intravenous, subcutaneous or intramuscular depending on the individual case. When a noticeable effect occurs depends on the type of award.

In addition to pain therapy, preparations containing the substance nalbuphine are also used in anesthesia. In this context, nalbuphine is used to artificially induce a comatose state of numbness. This is used to carry out operations or diagnostic measures without disturbance and pain.

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Risks & side effects

Nalbuphine must not be administered if the patient is hypersensitive or insensitive. In these cases there is a contraindication (contraindication). In addition, interactions can occur with agonists that act on the µ-opioid receptor. This is the case with preparations that contain morphine or fentanyl. Their main effect is almost completely neutralized by the antagonistic effect of nalbuphine. Particular caution should also be used if preparations that are active in the central nervous system are taken at the same time.

So far, the following undesirable side effects have occurred when administering nalbuphine: dizziness, profuse sweating, sedation (state of extreme calm down to complete immobilization or objectively existing numbness) and the development of somnolence (quantitative disturbance of consciousness that results in limited wakefulness goes along).

In addition, nalbuphine can cause vomiting, dry mouth, headaches and irregular heartbeat. It is also possible that hyper- or hypotension may occur.