While this pathway may be blocked by a variety of drugs such as certain cardiovascular drugs (e.g., quinidine) and antidepressants (e.g., fluoxetine), such blockade has not been shown to be of clinical significance with OXYCONTIN see DRUG INTERACTIONS. The plasma concentrations of oxycodone are only nominally affected by age, being 15% greater in elderly as compared to young subjects (age 21-45). Oxycodone is extensively metabolized by multiple metabolic pathways to produce noroxycodone, oxymorphone and noroxymorphone, which are subsequently glucuronidated. CYP3A mediated N-demethylation to noroxycodone is the primary metabolic pathway of oxycodone with a lower contribution from CYP2D6 mediated O-demethylation to oxymorphone.
Choosing an OTC Pain Reliever: What to Consider
While taking oxycodone, you should talk to your doctor about having a rescue medication called naloxone readily available (e.g., home, office). Naloxone is used to reverse the life-threatening effects of an opioid overdose. Naloxone works by blocking the effects of opiates to relieve dangerous symptoms caused by high levels of opiates in your blood. Your doctor may also prescribe you naloxone if you are living in a household where there are small children or someone who has abused street or prescription drugs. You should make sure that you and your family members, caregivers, or the people who spend time with you know how to recognize an opioid overdose, how to use naloxone, and what to do until emergency medical help arrives. Your doctor or pharmacist will show you and your family members how to use naloxone.
- The potency of oxycodone was approximately twofold greater in female that in male rats with ED50 values of 0.63 and 1.46 mg/kg, respectively.
- Finally, it’s absolutely essential that you dispose of any leftover medicine safely.
- Oxycodone should only be used for an extended time if the pain remains severe enough to require an opioid analgesic and other treatment options continue to be inadequate.
- About 60% to 87% of an oral dose of oxycodone reaches the central compartment in comparison to a parenteral dose.
More About Drugs and Medications
However, there were differences in the number of trials with morphine (six) compared with oxycodone (one) and transdermal fentanyl (four). The conclusions are also limited because the studies included cancer pain with different etiologies and of different types, making it rather difficult to draw definitive conclusions about the relative efficacy of these compounds for cancer pain. The authors concluded that there is no concrete evidence for the effectiveness and safety of opioids in chronic cancer patients. However, when focusing on a more homogeneous population, a randomized controlled study comparing controlled-release forms of oral morphine (30mg/d) or oxycodone (20 mg/d) in pancreatic cancer pain found no difference between these drugs in terms of efficacy or in the occurrence of adverse effects (Mercadante et al. 2010). Individually titrate OXYCONTIN to a dosage that provides adequate analgesia and minimizes adverse reactions. Continually reevaluate patients receiving OXYCONTIN to assess the maintenance of pain control, signs and symptoms of opioid withdrawal, and other adverse reactions, as well as to reassess for the development of addiction, abuse and misuse see WARNINGS AND PRECAUTIONS.
Role in Pain Management Protocols
- Vaccination reduced the proportion of rats acquiring oxycodone self-administration and also significantly reduced the number of infusions and total intake of oxycodone.
- The sequence of steps ended with a period whereby the post-prandial feature was discontinued but oxycodone remained available by responding under a fixed ratio four-response schedule of lever pressing.
- The μ-opioid receptor is expressed throughout the brainstem where μ-opioid receptor agonists reduce respiratory drive and the responsiveness of the respiratory centers to increased carbon dioxide (CO2), such that minute ventilation increases that would normally be triggered by hypercapnia are depressed.
- These investigators also studied cocaine self-administration in the two groups of mice and found no differences in responding, suggesting that the effects observed with morphine are specific to opioids and that the NK1 receptor may be necessary for the development of opioid addiction but not other abused drugs.
- When oxycodone was administered daily, tolerance did not develop to the analgesic effects, although tolerance did develop to some of the participant’s ratings of positive subjective effects.
Withdrawal symptoms can occur in breast-fed infants when maternal administration of an opioid analgesic is stopped, or when breast-feeding is stopped. Inform patients that OXYCONTIN could cause adrenal insufficiency, a potentially life-threatening condition. Adrenal insufficiency may present with non-specific symptoms and signs such as nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure. Advise patients to seek medical attention if they experience a constellation of these symptoms see WARNINGS AND PRECAUTIONS.
Oxycodone may cause side effects. Tell your doctor if any of these symptoms, are severe or do not go away:
A number of studies have examined gene expression in animals following periods of exposure to oxycodone to develop a better understanding of the neurobiological mechanisms underlying oxycodone, particularly under conditions when it is self-administered. Zhang et al. (2014) provided access to intravenous oxycodone in male C57BL/6J mice using a nose-poking response for 14 days in daily extended (4-hour) or shortened (1-hour) experimental sessions and assessed the effects on striatal neurotransmitter receptor gene expression. In contrast to these changes, mice in the 1-hour condition did not escalate intake of oxycodone, nor did this group show changes in the expression of neurotransmitter genes. This study also incorporated a “yoked control” group that received saline, not oxycodone; this group did not show sustained responding throughout the 14-day period. It would be interesting to determine the effects of a “true” yoked control where the yoked animals received the same frequency of oxycodone deliveries but did not have to respond for oxycodone as was the case with the active oxycodone subjects. Oxycodone, a μ-opioid receptor agonist, was synthesized in 1916 and introduced into clinical use in Germany in 1917.
A. Cancer Pain
The clinical relevance of a difference of this magnitude is low for a drug intended for chronic usage at individualized dosages, and there was no male/female difference detected for efficacy or adverse events in clinical trials. Use of opioids for an extended period of time may cause reduced fertility in females and males of reproductive potential. It is not known whether these effects on fertility are reversible see ADVERSE REACTIONS, CLINICAL PHARMACOLOGY and Nonclinical Toxicology. In a study of reproductive performance, rats were administered a once daily gavage dose of the vehicle or oxycodone hydrochloride (0.5, 2, and 8 mg/kg/day). Male rats were dosed for 28 days before cohabitation with females, during the cohabitation and until necropsy (2-3 weeks post-cohabitation). Females were dosed for 14 days before cohabitation with males, during cohabitation and up to Gestation Day 6.
Drug Interaction Studies
The leading cause of death related to opioid overdose is hypoxia caused by opioid-induced respiratory depression (White and Irvine, 1999). The μ-opioid receptor is expressed throughout the brainstem where μ-opioid receptor agonists reduce respiratory drive and the responsiveness of the respiratory centers to oxycodone: uses, side effects, dosages, precautions increased carbon dioxide (CO2), such that minute ventilation increases that would normally be triggered by hypercapnia are depressed. Webster et al. (2020) point out that there is no standard definition of respiratory depression and that, generally, it refers to a failure to maintain normal pulmonary exchange of CO2 and oxygen (O2).
Possible Interactions with Other Medications
Today it is prescribed for moderate to severe pain and is sold under various brand names, including OxyContin, Percolone, and Oxyfast. A widely prescribed drug known as Percocet contains oxycodone in combination with acetaminophen. However, the goal of identifying a nonaddicting opioid analgesic is an imperative objective. At the present time, it appears to be ever increasingly more achievable and should include comparable efforts to continue to identify potential medications to enhance the ability to treat OUDs.
Monitor for respiratory depression, especially during initiation of OXYCONTIN or following a dose increase. Instruct patients to swallow OXYCONTIN tablets whole; crushing, chewing, or dissolving OXYCONTIN tablets can cause rapid release and absorption of a potentially fatal dose of oxycodone see WARNINGS AND PRECAUTIONS. OxyContin (oxycodone hydrochloride) is an opioid drug used for the management of moderate to severe pain, usually for an extended time period. A healthcare provider will prescribe this medication when other pain medications don’t work well enough.
GLP-1 is expressed in several brain regions, including the arcuate nucleus and other hypothalamic regions, as well as in the shell of the Nac where it is expressed on dopamine D1 and D2 expressing medium spiny neurons (Merchenthaler et al., 1999). There have been suggestions for a role of GLP-1 in drugs of abuse with studies that have focused primarily on alcohol, cocaine, and nicotine (Brunchmann et al., 2019) including one study in humans with cocaine use disorder (Angarita et al., 2021). The suggestion that GLP-1 could play a potential role in OUDs is based on a study with male Sprague-Dawley rats by Zhang et al. (2020) who evaluated the effects of GLP-1 on oxycodone self-administration, reinstatement, and nociception using exendin-4. Excendin-4 also attenuated cue-induced reinstatement but had no effect on operant responding maintained by sucrose, although food consumption was transiently decreased 1 and 3 hours post-experimental session.
