What is Xtampza ER (oxycodone extended-release)?

From the Guidelines

Xtampza ER is a prescription opioid pain medication containing oxycodone in an extended-release formulation, designed to provide long-lasting pain relief for patients with severe pain requiring around-the-clock opioid treatment when other pain treatments are inadequate. According to the CDC clinical practice guideline for prescribing opioids for pain - United States, 2022 1, Xtampza ER is an example of an extended-release/long-acting (ER/LA) opioid, which should be reserved for management of pain severe enough to require daily, around-the-clock, long-term opioid treatment when alternative treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain.

The medication works by binding to opioid receptors in the brain and spinal cord to reduce pain perception. Xtampza ER is taken orally every 12 hours and should be taken with food to ensure consistent absorption. Unlike some other opioid formulations, Xtampza ER has abuse-deterrent properties, as its microsphere technology makes it difficult to crush, chew, or manipulate for misuse. Common side effects include constipation, nausea, headache, and drowsiness. As with all opioids, Xtampza ER carries risks of dependence, addiction, and respiratory depression, especially at higher doses or when combined with other central nervous system depressants.

Some key points to consider when prescribing Xtampza ER include:

• Clinicians should not treat acute pain with ER/LA opioids or initiate opioid treatment for subacute or chronic pain with ER/LA opioids 1
• ER/LA opioids should be reserved for severe, continuous pain and should be considered only for patients who have received certain dosages of immediate-release opioids daily for at least 1 week 1
• Patients should store it securely away from others, particularly children, and dispose of unused medication properly to prevent misuse
• Clinicians should use additional caution with ER/LA opioids and consider a longer dosing interval when prescribing to patients with renal or hepatic dysfunction 1

It's also important to note that the FDA has modified the labeling for ER/LA opioid pain medications, noting serious risks and recommending that ER/LA opioids be reserved for management of pain severe enough to require daily, around-the-clock, long-term opioid treatment when alternative treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain 1.

From the Research

Overview of Xtampza ER

• Xtampza ER (oxycodone extended-release) is an abuse-deterrent formulation of oxycodone, approved in the USA for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate 2.
• The microsphere-in-capsule DETERx drug delivery platform allows administration via sprinkle-dosing or enteral tubes, making it a useful treatment option for patients with severe, chronic pain, particularly when comorbid dysphagia or difficulty swallowing is a concern 2, 3.

Efficacy and Tolerability

• The efficacy of oxycodone DETERx ER in the management of moderate to severe, chronic pain was demonstrated in a well-designed, phase III trial, in which it was more effective than placebo at reducing pain intensity 2, 4.
• The formulation was generally well tolerated in this trial; the most common treatment-emergent adverse events were nausea and constipation 2, 4.
• Xtampza ER resulted in clinically and statistically significant efficacy in patients with chronic low back pain, with a statistically significant difference in average pain intensity from randomization baseline to treatment week 12 between the Xtampza ER and placebo groups 4.

Abuse-Deterrent Properties

• The physicochemical properties of the formulation make it difficult to manipulate, and its ER pharmacokinetic profile is retained after crushing or chewing 2, 5.
• Clinical abuse-potential studies suggest that these properties may translate to reduced intranasal abuse, with implications for abuse via the oral route less certain 2, 3.
• Human abuse-potential studies conducted in a population of recreational opioid users demonstrated lower drug-liking scores for oxycodone DETERx administered intranasally and orally when compared with IR oxycodone 3.

Pharmacokinetics

• The evaluation of dosing patterns indicates that this ER oxycodone capsule formulation has durability of effect over the entire 12-hour dosing interval 6.
• Across five studies, manipulated (crushed or chewed) Xtampza ER retained an ER PK profile similar to that of intact Xtampza ER, with respect to maximum plasma concentration (Cmax) and time to Cmax 5.
• Bioequivalence was established between manipulated and intact Xtampza ER, based on Cmax and area under the concentration-time curve values in healthy volunteers and nondependent recreational opioid users 5.