Nalbuphine is an analgesic agent that belongs to the opioid group. It is used for short periods to relieve moderate to acute pain and is primarily administered as a solution with varying levels of active ingredient. In addition, the substance is also used in anesthesia.
What is nalbuphine?
Nalbuphine is a medicinal substance belonging to the group of painkillers. The substance is classified as an opioid and has both agonistic and antagonistic effects. In addition to the name nalbuphine, the synonyms nalbuphini hydrochloridum, nubain and nalbuphine hydrochloride are also used. In chemistry, the molecular 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, which also includes the drug heroin, nalbuphine is not subject to the Narcotics Act. Under the trade name nalpain, the active ingredient is available by regular prescription as a solution for injection. The analgesic potency of nalbuphine is between the analgesic potency of morphine and codeine. As an analgesic, it is therefore administered to relieve pain in the moderate to acute range. 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), depending on the individual case.
Pharmacologic action
Nalbuphine has analgesic effects. The substance acts agonistically at the kappa receptors of a human. At the same time, it is also antagonistically active at My receptors. Because of this combined agonistic and antagonistic mode of action, nalbuphine succeeds in counteracting respiratory depression otherwise typical of opioids. Such a depression can occur, for example, after an operation in which fentanyl was used for anesthesia. Nalbuphine can thus be used to reverse respiratory depression while continuing pain therapy. Typically, the dose for an adult of average body weight (70 kg) is between 10 and 20 mg. This is equivalent to 0.1 to 0.3 mg of nalbuphine per body weight. Administration may occur 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 pain intensity). Onset of action depends on the route of administration. Following intravenous administration, which is common in Europe, onset of action is two to three minutes. Intramuscular or subcutaneous injections cause a noticeable effect on the body only after 15 minutes.
Medical application and use
Nalbuphine is an analgesic. It belongs to the opioids. Nevertheless, it is not subject to the Narcotics Act in Germany, but is available by prescription as an injection solution. Preparations containing nalbuphine are used to treat moderate to severe pain. However, the treatment is only short-term. Nalbuphine is not suitable for long-term use. Depending on the individual case, nalbuphine can be administered intravenously, subcutaneously or intramuscularly. When a noticeable effect sets in depends on the form of administration. 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 insensibility. This is used to perform surgery or diagnostic procedures without disturbance or pain.
Risks and side effects
Nalbuphine should not be administered if hypersensitivity or insensitivity exists. In these cases, a contraindication (contraindication) exists. In addition, interactions may occur with agonists acting at the µ-opioid receptor. This is the case with preparations containing morphine or fentanyl. Indeed, their main effect is almost completely cancelled out by the antagonistic effect of nalbuphine. Special caution should also be applied if preparations active on the central nervous system are taken at the same time.To date, the following adverse reactions have occurred with the administration of nalbuphine: Dizziness, profuse sweating, sedation (a state of severe sedation to complete immobilization or objective insensibility), and the development of somnolence (quantitative disturbance of consciousness associated with impaired alertness). In addition, nalbuphine may cause vomiting, induce dry mouth, lead to headache, and cause cardiac arrhythmias. Furthermore, it is possible that hyper- or hypotension may occur.
