In these experiments, the Ki (nM) for morphine was 1.2 and for oxycodone 47.4. Chen et al. (1991) also studied thebaine, from which oxycodone is derived, which had a Ki value of 636.2 nM. Generally, however, depending on the assay, the affinity of oxycodone for the μ-opioid receptor is between 5 to 40 times lower when compared with morphine (Chen et al., 1991; Lalovic et al., 2006; Olkkola et al., 2013). Studies comparing the receptor binding of oxycodone to other opioid receptors have demonstrated μ-opioid receptor specificity with lower Ki values for the δ-opioid receptor (958 ± 499) and κ-opioid receptor (677 ± 326); the Ki (nM) of oxycodone was 18 ± 4 (Monory et al., 1999).
Nursing Considerations for Oxycodone Overdose Management
Allodynia is a condition where things that do not usually cause you pain, such as wearing glasses or brushing your hair, cause you pain. Call your health care provider if you are having more pain, pain from things that would normally not cause you pain, or pain in other parts of your body. In light of the growing opioid epidemic in the U.S., healthcare providers have become more wary when prescribing oxycodone. They’ll make sure pain can’t be managed by other means, and work with patients to make sure they don’t develop drug dependency.
H. Biased G Protein-Based Mu Opioid Receptor Agonist TRV130
If you are taking the extended-release tablets (Oxycontin®), swallow the tablets one at a time with plenty of water. Do not presoak, wet, or lick the tablets before you put them in your mouth. Oxycodone is also available in combination with acetaminophen (Oxycet®, Percocet®, others) and aspirin (Percodan®).
Employ other supportive measures (including oxygen, vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life support measures. The safety and efficacy of OXYCONTIN have been established in pediatric patients ages 11 to 16 years. Use of OXYCONTIN is supported by evidence from adequate and well-controlled trials with OXYCONTIN in adults as well as an open-label study in pediatric patients ages 6 to 16 years.
Blackwood et al. (2019a) also studied neurobiological consequences of withdrawal from oxycodone under escalated (9-hour) and nonescalated (3-hour) oxycodone self-administration conditions. After 20 days of self-administration, both groups were withdrawn from oxycodone and over a 31-day period were tested for cue-induced reinstatement. One of the main findings of this study was that the long-assess group could be further differentiated into rats with high levels of oxycodone intake and rats that responded for lower amounts of oxycodone. Rats responding for higher amounts of oxycodone showed an increase in the expression of hippocampal μ and κ receptors, whereas there were no changes with δ receptor expression in any of the short- or long-access animals. The authors speculated that large doses of oxycodone may produce changes in hippocampal-dependent learning and memory processes that could also trigger psychiatric disorders in individuals addicted to opioids.
Core Treatment
- Carcinogenic potential of oxycodone was evaluated in a 2-year oral gavage study in Sprague-Dawley rats.
- While both morphine and fentanyl are effective alternatives to oxycodone, their use requires careful monitoring due to their potency and potential for misuse.
- In comparison, morphine has been reported to bind to the μ-opioid receptor with an affinity of 1.8 nM, with an affinity of 90 nM for the δ site and 317 nM for the κ site (Robson et al., 1983).
This monograph only includes information about the use of oxycodone alone. If you are taking an oxycodone combination product, be sure to read information about all the ingredients in the product you are taking and ask your doctor or pharmacist for more information. If you cannot swallow oxycodone extended-release capsules, you can open the capsule and sprinkle the medicine onto soft food (applesauce, pudding, ice cream, or jam) or into a cup of water. While less common, the most serious side effects of oxycodone are described below, along with what to do if they happen.
In case of emergency/overdose
Get emergency medical help if you have signs of an allergic reaction to oxycodone, including hives, difficulty breathing, or swelling of your face, lips, tongue, or throat. The most effective approach matches the medication to the type of pain. Inflammatory pain needs anti-inflammatories, neuropathic pain needs specialized medications, and mechanical pain often responds well to OTC combinations. Because opioids usually work better in combination with other analgesics, both oxycodone and hydrocodone are available formulated with other ingredients such as acetaminophen or ibuprofen. Neuropathic pain results from damaged or malfunctioning nerves and responds poorly to traditional pain medications, requiring specialized treatments that target nerve signaling pathways.
Pharmacogenetic testing of these patients prior to surgery allowed for the collection of information on pain and pain management following surgery. Genetic variants were found in a number of patients that influenced drug metabolism. It was concluded that when patient’s pharmacogenetics are identified and medications customized to their genetic profile, pain scores and opioid use are greatly reduced for 10 days following surgery.
Overall, the effects of opioids appear to be modestly immunosuppressive. Oxycodone produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in CO2 tension and electrical stimulation. In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed.
Cannabinoids and opioids have several common pharmacological properties, suggesting there may be synergistic interactions with μ-opioid receptor agonists such as oxycodone. Abrams et al. (2011) examined the interaction of inhaled vaporized cannabis with sustained-release formulations of oxycodone or morphine in 21 individuals (11 men and 10 women) with chronic pain. The types of pain included musculoskeletal, posttraumatic, peripheral neuropathy, cancer, and arthritic.
- Oxycodone may cause a serious type of allergic reaction called anaphylaxis, which can be life-threatening and requires immediate medical attention.
- Oxycodone carries boxed warnings, the most serious type of safety-related warning the Food and Drug Administration (FDA) gives a medication.
- Your healthcare provider may ask you to keep a medicine called naloxone on hand.
- The bacterial changes were correlated with metabolic pathway alterations that could affect drug action throughout the lifespan.
In summary, not all μ-opioid receptor agonists show potency oxycodone: uses, side effects, dosages, precautions or sensitivity differences between male and female rats, nor do these sex differences necessarily apply to other opioid receptor drugs acting at κ- or δ-opioid receptors (Craft, 2003). There still seems to be a number of inconsistencies and ambiguities in the literature with regard to sex differences in pain and analgesia that warrant further study. Although the sex-specific data with morphine in rodents appears relatively clear with regard to morphine, as Peckham and Traynor (2006) point out, not all opioid analgesics are the same. Bartok and Craft (1997) made the point that methodological differences make contribute to the variability in findings and emphasize the importance of time- and dose-effect relationships when investigating the contribution of sex, particularly in studies of nociception.