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Journal of Pain and Symptom Management Feb 1993Oxycodone (14-hydroxy-7,8-dihydrocodeinone) is a strong opioid agonist that is available alone or in combination with mild analgesics. It is suitable for oral... (Review)
Review
Oxycodone (14-hydroxy-7,8-dihydrocodeinone) is a strong opioid agonist that is available alone or in combination with mild analgesics. It is suitable for oral administration due to high bioavailability (60%), and may also be given intramuscularly, intravenously, subcutaneously, and rectally; it is not recommended for spinal administration. In analgesic potency, oxycodone is comparable to morphine. With the exception of hallucinations, which may occur more rarely after oxycodone than after morphine, the side effects of these drugs are closely related. The abuse potential of oxycodone is equivalent to that of morphine. The usual indications for oxycodone are severe acute postoperative or posttraumatic pain and cancer pain. When oxycodone is administered, the same precautions should be taken as with morphine or other agonist opioids.
Topics: Biological Availability; Humans; Oxycodone; Therapeutic Equivalency
PubMed: 8492004
DOI: 10.1016/0885-3924(93)90101-z -
Scandinavian Journal of Urology and... 2006To evaluate whether combined oral intake of paracetamol (4 x 1 g) + oxycodone hydrochloride (2x10 mg) is adequate and equivalent to epidural anaesthesia (EDA) with... (Comparative Study)
Comparative Study Randomized Controlled Trial
OBJECTIVE
To evaluate whether combined oral intake of paracetamol (4 x 1 g) + oxycodone hydrochloride (2x10 mg) is adequate and equivalent to epidural anaesthesia (EDA) with respect to postoperative pain control and postoperative mobilization after radical retropubic prostatectomy (RRP).
MATERIAL AND METHODS
Forty consecutive patients scheduled for RRP were randomized to either: EDA with ropivacaine + paracetamol (4 x 1 g tablet) + injected or oral morphine on demand (EDA group); or infiltration of 25-40 ml of 0.25% bupivacaine into the wound + oxycodone hydrochloride (2 x 10 mg tablet) + paracetamol (4x1 g tablet) + injected or oral morphine on demand (OXY group). The groups were compared with respect to pain control determined by means of a visual analogue scale (VAS), time to free mobilization, hospital stay, complications, operation time and bleeding.
RESULTS
Both analgesic regimens provided satisfactory analgesia, i.e. VAS scores remained significantly below 4 (p<0.0001). The EDA group experienced slightly less pain than the OXY group on the operation day but this was not significant: median VAS scores of 0.7 and 1.8, respectively (p=0.27). Median VAS scores during hospital stay were 1.7 in both treatment groups. VAS scores ranged from 0.1 to 3.3 and from 0.2 to 3.5 in the EDA and OXY groups, respectively. There was no significant difference in postoperative mobilization between the groups (p=0.06). The median duration of hospital stay was 3 nights in both groups.
CONCLUSION
Postoperative pain control after RRP with oral oxycodone hydrochloride, paracetamol and extra morphine on demand is preferable to EDA when pain control as well as mobilization and costs are taken into account.
Topics: Acetaminophen; Administration, Oral; Aged; Amides; Analgesia, Patient-Controlled; Analgesics, Non-Narcotic; Analgesics, Opioid; Anesthesia, Epidural; Anesthetics, Local; Bupivacaine; Drug Therapy, Combination; Early Ambulation; Humans; Male; Middle Aged; Morphine; Oxycodone; Pain Measurement; Pain, Postoperative; Prostatectomy; Ropivacaine; Sufentanil
PubMed: 16809258
DOI: 10.1080/00365590600589583 -
Chemico-biological Interactions Sep 2022Cancer patients experience pain during medical treatment. Therefore, anticancer drugs and painkillers are often prescribed together. This study aims to determine the...
PURPOSE
Cancer patients experience pain during medical treatment. Therefore, anticancer drugs and painkillers are often prescribed together. This study aims to determine the interaction between anlotinib and oxycodone and reveal the underlying mechanism.
METHODS
UPLC-MS/MS, an efficient and sensitive method, was used for the simultaneous determination of oxycodone and oxycodone metabolites. Sprague-Dawley rats were given oxycodone with or without anlotinib. Then, UPLC-MS/MS was used to determine the blood concentration of oxycodone. To study the interaction mechanism, rat and human liver microsomes (HLMs) were used for determining enzyme kinetics.
RESULTS
Long-term administration of oxycodone combined with anlotinib resulted in significantly increased pharmacokinetic parameters AUC, AUC, and C for oxycodone, indicating that anlotinib inhibited oxycodone. In vitro kinetic measurements indicated that anlotinib inhibited the metabolism of oxycodone through a mixed mechanism. Further studies indicated that in HLMs, anlotinib strongly inhibited the metabolism of oxycodone.
CONCLUSION
This study showed that anlotinib inhibited the metabolism of oxycodone both in vitro and in vivo. It is recommended that the dose of oxycodone should be reconsidered when oxycodone is combined with anlotinib in clinical practice.
Topics: Animals; Chromatography, Liquid; Humans; Indoles; Oxycodone; Quinolines; Rats; Rats, Sprague-Dawley; Tandem Mass Spectrometry
PubMed: 35853539
DOI: 10.1016/j.cbi.2022.110044 -
Japanese Journal of Clinical Oncology Jun 2018Hydromorphone is a standard opioid analgesic for cancer pain that, prior to this study, was not approved in Japan, where options for opioid switching are limited. We... (Randomized Controlled Trial)
Randomized Controlled Trial
A randomized, double-blind, non-inferiority study of hydromorphone hydrochloride immediate-release tablets versus oxycodone hydrochloride immediate-release powder for cancer pain: efficacy and safety in Japanese cancer patients.
BACKGROUND
Hydromorphone is a standard opioid analgesic for cancer pain that, prior to this study, was not approved in Japan, where options for opioid switching are limited. We aimed to investigate the efficacy and safety of hydromorphone (DS-7113b) immediate-release tablets in opioid-naïve cancer patients with moderate to severe cancer pain.
METHODS
Multicenter, active-controlled, randomized, double-blind, parallel-group, non-inferiority study of 183 cancer patients over 20 years of age at 50 clinical sites in Japan. Hydromorphone tablets or oxycodone hydrochloride powder was orally administered four times daily for 5 days. The initial doses of hydromorphone and oxycodone hydrochloride were 4 mg/day and 10 mg/day, respectively, and adjusted as necessary. Efficacy was evaluated as the intergroup difference (95% confidence interval [CI]) of the least squares mean by analysis of covariance, using the baseline visual analog scale (VAS) as a covariate for change in VAS score at treatment completion/discontinuation in the full analysis set.
RESULTS
Non-inferiority of hydromorphone versus oxycodone was confirmed, with an intergroup difference (95% CI) in the least squares mean of -3.4 mm (-9.8 to 3.1 mm) for change in VAS scores, which was below the upper limit of the 95% CI at 10 mm, the non-inferiority limit determined during study planning. Adverse events occurred in 83.0% (73/88) of patients in the hydromorphone group and 77.4% (65/84) in the oxycodone group. The most frequently observed adverse events were somnolence, constipation, vomiting and nausea.
CONCLUSIONS
The efficacy and safety of hydromorphone tablets are equivalent to those of oxycodone immediate-release powder.
Topics: Aged; Analgesics, Opioid; Asian People; Cancer Pain; Delayed-Action Preparations; Demography; Depression; Double-Blind Method; Female; Humans; Hydromorphone; Japan; Male; Neoplasms; Oxycodone; Pain Measurement; Powders; Tablets; Treatment Outcome
PubMed: 29659913
DOI: 10.1093/jjco/hyy038 -
Molecular Pharmacology May 2018Oxycodone is a semisynthetic opioid compound that is widely prescribed, used, and abused today, and has a well-established role in shaping the current opioid epidemic....
Oxycodone is a semisynthetic opioid compound that is widely prescribed, used, and abused today, and has a well-established role in shaping the current opioid epidemic. Previously, we have shown that tolerance develops to the antinociceptive and respiratory depressive effects of oxycodone in mice, and that a moderate dose of acute ethanol or a protein kinase C (PKC) inhibitor reversed that tolerance. To investigate further if tolerance was occurring through neuronal mechanisms, our aims for this study were to assess the effects of acute and prolonged oxycodone in isolated dorsal root ganglia (DRG) neurons and to determine if this tolerance was reversed by either ethanol or a PKC inhibitor. We found that an acute exposure to 3 M oxycodone reduced neuronal excitability, as measured by increased threshold potentials and reduced action potential amplitude, without eliciting measurable changes in resting membrane potential. Exposure to 10 M oxycodone for 18-24 hours prevented oxycodone's effect on neuronal excitability, indicative of tolerance development. The development of opioid tolerance was mitigated in DRG neurons from -arrestin 2 knockout mice. Oxycodone tolerance was reversed in isolated DRG neurons by the acute application of either ethanol (20 mM) or the PKC inhibitor, bisindolylmaleimide XI hydrochloride (Bis XI), when a challenge of 3 M oxycodone significantly reduced neuronal excitability following prolonged exposure. Through these studies, we concluded that oxycodone acutely reduced neuronal excitability, tolerance developed to this effect, and reversal of that tolerance occurred at the level of a single neuron, suggesting that reversal of oxycodone tolerance by either ethanol or Bis XI involves cellular mechanisms.
Topics: Action Potentials; Analgesics, Opioid; Animals; Cells, Cultured; Drug Tolerance; Ethanol; Ganglia, Spinal; Indoles; Male; Maleimides; Membrane Potentials; Mice, Inbred C57BL; Mice, Knockout; Neurons; Oxycodone; Protein Kinase C; Protein Kinase Inhibitors; beta-Arrestin 2
PubMed: 29467238
DOI: 10.1124/mol.117.110775 -
The Medical Letter on Drugs and... Sep 2001
Topics: Administration, Oral; Delayed-Action Preparations; Humans; Morphine Dependence; Neoplasms; Opioid-Related Disorders; Oxycodone; Pain; Parenteral Nutrition, Total
PubMed: 11581580
DOI: No ID Found -
Advances in Therapy Nov 2020Buprenorphine is a partial μ-opioid receptor agonist that, unlike full μ-opioid receptor agonists, has been shown to have a ceiling effect on respiratory depression.... (Randomized Controlled Trial)
Randomized Controlled Trial
INTRODUCTION
Buprenorphine is a partial μ-opioid receptor agonist that, unlike full μ-opioid receptor agonists, has been shown to have a ceiling effect on respiratory depression. Buprenorphine buccal film (BBF) is approved by the US Food and Drug Administration for use in patients with chronic pain severe enough to require daily, around-the-clock, long-term opioid treatment and for whom alternative treatment options are inadequate. This study was conducted to compare the effects of BBF and immediate-release oral oxycodone hydrochloride administration on respiratory drive, as measured by the ventilatory response to hypercapnia (VRH) after drug administration.
METHODS
Subjects (N = 19) were men and women, ages 27-41 years, self-identifying as recreational opioid users who were not physically dependent on opioids as determined via a Naloxone Challenge Test. Respiratory drive was evaluated by measuring VRH through the assessment of the maximum decrease in minute ventilation (E) after administration of each treatment. The treatments utilized in this study included 300, 600, and 900 μg BBF; 30 and 60 mg orally administered oxycodone; and placebo (each separated by a 7-day washout period). Effects on respiratory drive were assessed using a double-blind, double-dummy, six-treatment, six-period, placebo-controlled, randomized crossover design. Statistical analyses were performed using a linear mixed-effects model.
RESULTS
The least squares mean differences in minute volume E (L/min, versus placebo) were as follows: 300 μg BBF (+ 1.24, P = 0.529), 600 μg BBF (+ 0.23, P = 0.908), 900 μg BBF (+ 0.93, P = 0.637), 30 mg oxycodone (- 0.79, P = 0.687), and 60 mg oxycodone (- 5.23, P = 0.010).
CONCLUSIONS
BBF did not significantly reduce respiratory drive at any dose compared with placebo, including at the maximum available prescription dose of 900 μg. Administration of oxycodone resulted in a significant dose-dependent decrease in respiratory drive. These data suggest that BBF may be a safer treatment option than full μ-opioid receptor agonists for patients with chronic pain.
TRIAL REGISTRATION
ClinicalTrials.gov identifier, NCT03996694.
Topics: Administration, Oral; Adult; Analgesics, Opioid; Buprenorphine; Double-Blind Method; Female; Humans; Male; Naloxone; Oxycodone
PubMed: 32978722
DOI: 10.1007/s12325-020-01481-0 -
Postgraduate Medicine Mar 2009OxyContin (controlled-release oxycodone hydrochloride) (Purdue Pharma, Stamford, CT) was approved in 1995 by the US Food and Drug Administration (FDA) for... (Review)
Review
BACKGROUND
OxyContin (controlled-release oxycodone hydrochloride) (Purdue Pharma, Stamford, CT) was approved in 1995 by the US Food and Drug Administration (FDA) for moderate-to-severe chronic pain. Crushing and snorting the delayed-release tablets results in a rapid release of the drug, increased absorption, and high peak serum concentrations. The propensity for addiction to OxyContin and the trend of increased prescription drug abuse have made it imperative for physicians and health care providers to recognize the clinical presentation of overdose and know how to manage associated complications.
OBJECTIVES
In this review of OxyContin, we discuss current trends in its abuse and the clinical presentation of overdose. We review the specific effects of the drug on body systems and the recognition of symptomatology, differential diagnosis, and management.
DISCUSSION
Many of the clinical findings in acute opioid overdoses are nonspecific, making diagnosis difficult. OxyContin overdose presents with a typical opiate toxidrome, including decreased respirations, miosis, hypothermia, bradycardia, hypotension, and altered mental status. The presence of coingestants can cloud the clinical picture. If OxyContin overdose is suspected, early ventilation and oxygenation should be administered, which is generally sufficient to prevent death. Even in the absence of a confirmation, cautious administration of naloxone--the opiate receptor antagonist and antidote for opioid overdoses--may have both diagnostic and therapeutic effects.
SUMMARY
With increasing rates of prescription drug abuse, OxyContin will continue to present challenges to physicians and health care providers. Physicians should be aware of potential patients who are seeking OxyContin for recreational use.
Topics: Analgesics, Opioid; Delayed-Action Preparations; Diagnosis, Differential; Drug Overdose; Humans; Opioid-Related Disorders; Oxycodone
PubMed: 19332974
DOI: 10.3810/pgm.2009.03.1988 -
Scientific Reports Aug 2023Oxycodone is one of the most widely prescribed and misused opioid painkillers in the United States. Evidence suggests that biological sex and hormonal status can impact...
Oxycodone is one of the most widely prescribed and misused opioid painkillers in the United States. Evidence suggests that biological sex and hormonal status can impact drug reward in humans and rodents, but the extent to which these factors can influence the rewarding effects of oxycodone is unclear. The purpose of this study was to utilize place conditioning to determine the effects of sex and female hormonal status on the expression of oxycodone conditioned reward in rats. Gonadally intact adult Sprague-Dawley male and female rats were used to test: (1) whether both sexes express conditioned reward to oxycodone at similar doses, (2) the impact of conditioning session length on oxycodone conditioned reward expression in both sexes, and (3) the influence of female estrous cycle stage on oxycodone conditioned reward expression. Both sexes expressed conditioned reward at the same doses of oxycodone. Increasing the length of conditioning sessions did not reveal an effect of sex and resulted in lower magnitude conditioned reward expression. Importantly however, female stage of estrous cycle significantly influenced oxycodone conditioned reward expression. These results suggest that female hormonal status can impact the rewarding effects of opioids and thus have important implications for prescription opioid treatment practices.
Topics: Adult; Humans; Rats; Female; Male; Animals; Rats, Sprague-Dawley; Oxycodone; Analgesics, Opioid; Estrous Cycle; Reward
PubMed: 37626154
DOI: 10.1038/s41598-023-40971-3 -
Pain Medicine (Malden, Mass.) Feb 2016
Topics: Analgesics, Opioid; Chronic Pain; Humans; Oxycodone; Pain Management
PubMed: 26803845
DOI: 10.1093/pm/pnv106