Nalbuphin

Products

Nalbuphine is commercially available as a solution for injection (Nalbuphine OrPha). It has been approved in many countries since 2004.

Structure and properties

Nalbuphine (C21H27NO4, Mr = 357.4 g/mol) is a morphine derivative structurally related to naloxone and oxymorphone. It is present in drugs as nalbuphine hydrochloride.

Effects

Nalbuphine (ATC N02AF02) has analgesic properties. The effects are due to agonism at κ-receptors and partial antagonism at µ-receptors. Nalbuphine is approximately equipotent to morphine.

Indications

For the treatment of moderate to severe pain of various causes. The drug is also used in anesthesia.

Dosage

According to the SmPC. The solution for injection is administered intravenously, intramuscularly, or subcutaneously.

Contraindications

  • Hypersensitivity
  • Severe kidney damage
  • Liver damage
  • Concurrent treatment with μ-agonist opioids, such as morphine or fentanyl.

For complete precautions, see the drug label.

Interactions

Drug-drug interactions have been described with central depressant drugs and alcohol, phenothiazines, and penicillins. Nalbuphine has opioid antagonistic properties and therefore may reverse the effects of other opioids, resulting in withdrawal symptoms.

Adverse effects

The most common possible adverse effects include administration site reactions, drowsiness, dizziness, headache, hallucination, upset, cold sweats, nausea, vomiting, and dry mouth. Unlike other opioids, nalbuphine is reported to have a low abuse potential.