Oxycodone + Naloxone
- OralOxycodone + NaloxoneTarginIncludes a reversal agent, to reduce adverse effects (particularly constipation)
Mechanism of Action
- Oxcodone is an opioid, which acts on opioid receptors (δ, κ and μ) and nociceptin orphanin FQ (NOF) receptors on neuronal cell membranes within the thalamus, diencephalon, midbrain and medulla, resulting in reduced neurotransmitter release.Naloxone is a competitive antagonist of μ, κ, and δ opioid receptors, reversing the action of exogenous opioids.
Pharmacology
- Less histamine release (flushing, itching, rash) and less constipating than natural opioids.
Clinical Use
Indications
- Acute and chronic pain
- Adverse Effects
- Less than with other opioidsNausea / vomiting
- Constipation
- Sedation
- Respiratory depression
- Diaphoresis
- Delirium
- Hypersensitivity - bronchospasm, urticaria
- Bradycardia
- Tolerance
- Dependence
- Hypogonadism