Products
Buprenorphine is commercially available as sublingual tablets, transdermal patch and injection solution, and depot injection solution (e.g., Temgesic, Transtec, Subutex, generics). It has been approved in many countries since 1979.
Structure and properties
Buprenorphine (C29H41NO4, Mr = 467.6 g/mol) is present in drugs as buprenorphine hydrochloride, a white crystalline powder that is sparingly soluble in water. Patches contain the base, which is very sparingly soluble in water.
Effects
Buprenorphine (ATC N02AE01) has analgesic properties. The effects are due to partial agonism at μ- and antagonism at κ-opioid receptors. The effects in withdrawal are attributed to prolonged binding to μ-receptors, which reduces the urge for the drug over time.
Indications
- For the treatment of moderate to severe acute and persistent pain.
- For the treatment of opioid dependence (alone or in fixed combination with naloxone).
Dosage
According to the SmPC. The drugs are administered parenterally, sublingually or transdermally.
Contraindications
- Hypersensitivity
- Increased intracranial pressure
- Severe respiratory failure
- Severe hepatic insufficiency
Full precautions can be found in the drug label.
Interactions
Buprenorphine is metabolized and glucuronidated by CYP3A4. Drug-drug interactions have been described with benzodiazepines, central depressant drugs, alcohol, MAO inhibitors, CYP inhibitors, and CYP inducers.
Adverse effects
The most common possible adverse effects include dullness, somnolence, low blood pressure, respiratory depression, headache, small pupils, dizziness, sweating, nausea, and vomiting.
