Normal-release and controlled-release oxycodone: pharmacokinetics, pharmacodynamics, and controversy

Davis, Mellar P.; Varga, James; Dickerson, Duke; Walsh, Declan; LeGrand, Susan B.; Lagman, Ruth

doi:10.1007/s00520-002-0385-9

Cited by 107 publications

(45 citation statements)

References 61 publications

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“…36,37 In prior pharmacokinetics studies, a 30% change in AUC was thought to be clinically significant. 38 Therefore, we set the target size at 25% to ensure that we would be able to capture a clinically significant change in AUC 12. We enrolled at least 10 participants in each of the two (morphine and oxycodone) groups.…”

Section: Discussionmentioning

confidence: 99%

Cannabinoid–Opioid Interaction in Chronic Pain

Abrams

Couey

Shade

et al. 2011

Clin Pharmacol Ther

285

232

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Cannabinoids and opioids share several pharmacologic properties and may act synergistically. The potential pharmacokinetics and the safety of the combination in humans are unknown. We therefore undertook a study to answer these questions. Twenty-one individuals with chronic pain, on a regimen of twice-daily doses of sustained-release morphine or oxycodone were enrolled in the study and admitted for a 5-day inpatient stay. Participants were asked to inhale vaporized cannabis in the evening of day 1, three times a day on days 2-4, and in the morning of day 5. Blood sampling was performed at 12-h intervals on days 1 and 5. The extent of chronic pain was also assessed daily. Pharmacokinetic investigations revealed no significant change in the area under the plasma concentration-time curves for either morphine or oxycodone after exposure to cannabis. Pain was significantly decreased (average 27%, 95% confidence interval (CI) 9, 46) after the addition of vaporized cannabis. We therefore concluded that vaporized cannabis augments the analgesic effects of opioids without significantly altering plasma opioid levels. The combination may allow for opioid treatment at lower doses with fewer side effects.

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Section: Discussionmentioning

confidence: 99%

Cannabinoid–Opioid Interaction in Chronic Pain

Abrams

Couey

Shade

et al. 2011

Clin Pharmacol Ther

285

232

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“…Davis et al (2003) note that because it was a sustained release formulation, OxyContin ® contained higher doses of oxycodone than previous preparations, and when crushed and injected, it was extremely rewarding and addictive. In the General Accounting Office Report about OxyContin ® abuse released in 2003, investigators concluded:

While OxyContin’s potency and controlled release feature may have made the drug beneficial for relief of moderate-to-severe pain over an extended period of time, the DEA has stated that those attributes of its formulation have also made it an attractive target for abuse and diversion.

…”

Section: Pharmaceutical Technologies Of Whitenessmentioning

confidence: 99%

White opioids: Pharmaceutical race and the war on drugs that wasn’t

2017

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The US ‘War on Drugs’ has had a profound role in reinforcing racial hierarchies. Although Black Americans are no more likely than Whites to use illicit drugs, they are 6–10 times more likely to be incarcerated for drug offenses. Meanwhile, a very different system for responding to the drug use of Whites has emerged. This article uses the recent history of White opioids – the synthetic opiates such as OxyContin® that gained notoriety starting in the 1990s in connection with epidemic prescription medication abuse among White, suburban and rural Americans and Suboxone® that came on the market as an addiction treatment in the 2000s – to show how American drug policy is racialized, using the lesser known lens of decriminalized White drugs. Examining four ‘technologies of whiteness’ (neuroscience, pharmaceutical technology, legislative innovation and marketing), we trace a separate system for categorizing and disciplining drug use among Whites. This less examined ‘White drug war’ has carved out a less punitive, clinical realm for Whites where their drug use is decriminalized, treated primarily as a biomedical disease, and where their whiteness is preserved, leaving intact more punitive systems that govern the drug use of people of color.

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“…Approximately 11% of an oxycodone dose is O-demethylated by CYP2D6 to the minor metabolite oxymorphone, which has a 40-fold higher affinity and eightfold higher potency for µ-opioid receptors as compared with the parent drug. 10,26 As compared with extensive metabolizers, poor metabolizers have been shown to have lower peak concentrations of oxymorphone after a dose of oxycodone. 27,28 However, prospective clinical studies have produced conflicting data pertaining to the associations between CYP2D6 metabolizer phenotype and the analgesic effect and toxicity of oxycodone.…”

Section: Codeine Backgroundmentioning

confidence: 99%

Clinical Pharmacogenetics Implementation Consortium (CPIC) Guidelines for Codeine Therapy in the Context of Cytochrome P450 2D6 (CYP2D6) Genotype

Crews

Gaedigk

Dunnenberger

et al. 2011

Clin Pharmacol Ther

339

275

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Codeine is bioactivated to morphine, a strong opioid agonist, by the hepatic cytochrome P450 2D6 (CYP2D6); hence, the efficacy and safety of codeine as an analgesic are governed by CYP2D6 polymorphisms. Codeine has little therapeutic effect in patients who are CYP2D6 poor metabolizers, whereas the risk of morphine toxicity is higher in ultrarapid metabolizers. The purpose of this guideline (periodically updated at http://www.pharmgkb.org) is to provide information relating to the interpretation of CYP2D6 genotype test results to guide the dosing of codeine.

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Normal-release and controlled-release oxycodone: pharmacokinetics, pharmacodynamics, and controversy

Cited by 107 publications

References 61 publications

Cannabinoid–Opioid Interaction in Chronic Pain

Cannabinoid–Opioid Interaction in Chronic Pain

White opioids: Pharmaceutical race and the war on drugs that wasn’t

Clinical Pharmacogenetics Implementation Consortium (CPIC) Guidelines for Codeine Therapy in the Context of Cytochrome P450 2D6 (CYP2D6) Genotype

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