XTAMPZA ER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XTAMPZA ER (XTAMPZA ER).
Oxycodone is a full mu-opioid receptor agonist, producing analgesia, euphoria, and sedation. Xtampza ER utilizes DETERx technology to provide extended-release properties and resist tampering.
| Metabolism | Primarily hepatic via CYP3A4 and CYP2D6 to active and inactive metabolites. |
| Excretion | Primarily renal (70-90% as morphine-3-glucuronide, morphine-6-glucuronide, and free morphine); biliary/fecal (10-20%) |
| Half-life | 3-4 hours for immediate-release morphine; 8-12 hours for extended-release formulation (XTAMPZA ER), allowing twice-daily dosing |
| Protein binding | 20-35% bound to albumin |
| Volume of Distribution | 1-4 L/kg; high Vd indicates extensive tissue distribution (muscle, kidney, liver, lungs) |
| Bioavailability | Oral: 30-40% (first-pass metabolism reduces systemic availability; XTAMPZA ER uses Cydot technology to enhance absorption and reduce food effect) |
| Onset of Action | Oral: 30-60 minutes (immediate-release component); 2-4 hours (extended-release peak effect) |
| Duration of Action | 8-12 hours (consistent with twice-daily dosing); clinical duration may be reduced in opioid-tolerant patients |
Initial: 9 mg orally every 12 hours with food; titrate by 9 mg every 3-7 days as needed; maximum dose: 36 mg every 12 hours.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 25% and titrate cautiously; GFR <30 mL/min: contraindicated or avoid use due to accumulation of naltrexone metabolite. |
| Liver impairment | Child-Pugh Class A or B: no adjustment recommended; Child-Pugh Class C: avoid use (no studies). |
| Pediatric use | Not approved for patients <18 years of age. |
| Geriatric use | Start at low end of dosing range (9 mg every 12 hours); titrate slowly due to increased sensitivity and potential for respiratory depression. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XTAMPZA ER (XTAMPZA ER).
| Breastfeeding | Excreted in human milk; M/P ratio not reported. Monitor infant for respiratory depression, sedation, and withdrawal symptoms. Use caution, especially with high maternal doses or prolonged use. Breastfeeding generally not recommended due to risk of infant toxicity. |
| Teratogenic Risk | Pregnancy category C. First trimester: Potential for neural tube defects and other major malformations, though data limited. Second and third trimesters: Prolonged use may lead to neonatal opioid withdrawal syndrome (NOWS) and respiratory depression at birth. Risk of preterm labor, low birth weight, and fetal growth restriction with chronic use. |
■ FDA Black Box Warning
Addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants; opioid risk evaluation and mitigation strategy (REMS).
| Serious Effects |
["Significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus","Hypersensitivity to oxycodone or any component of the formulation"]
| Precautions | ["Addiction, abuse, and misuse","Life-threatening respiratory depression","Accidental ingestion","Neonatal opioid withdrawal syndrome","Risks from concomitant use with benzodiazepines or other CNS depressants","Opioid-induced hyperalgesia","Gastrointestinal effects (e.g., constipation, ileus)","Adrenal insufficiency","Severe hypotension","Seizures","Use in patients with increased intracranial pressure or head injury"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal vital signs, pain scores, and signs of opioid toxicity. Fetal monitoring includes ultrasound for growth restriction, nonstress test (NST), and biophysical profile (BPP) if chronic use. Neonatal monitoring for NOWS (irritability, poor feeding, respiratory distress) for at least 48 hours postpartum. |
| Fertility Effects | Opioids may impair fertility in females via disruption of hypothalamic-pituitary-gonadal axis, leading to menstrual irregularities and anovulation. In males, may reduce libido and cause erectile dysfunction. Effects are reversible upon dose reduction or discontinuation. |