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 |
| Molecular Weight | 351.44 |
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 | Avoid use during first trimester unless clearly needed; chronic use may lead to neonatal opioid withdrawal syndrome (NOWS). |
| 2nd trimester | Avoid use; risk of NOWS remains. Consider maternal benefit vs. fetal risk. |
| 3rd trimester | Avoid use; increased risk of NOWS, premature labor, and low birth weight. |
Clinical note
Comprehensive clinical and safety monograph for XTAMPZA ER (XTAMPZA ER).
| Placental transfer | Crosses placenta; significant transfer observed in animal studies and human data. |
| Breastfeeding | Excreted in breast milk; monitor infant for drowsiness, respiratory depression, and withdrawal symptoms. Use only if clearly needed and consider alternative analgesics. |
| Lactation Rating |
■ 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 depressionAcute or severe bronchial asthmaKnown hypersensitivity to morphine or any componentParalytic ileusConcurrent use of MAOIs or within 14 days
| 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 |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they inhibit CYP3A4 and may increase oxycodone levels, potentiating toxicity. High-fat meals may delay absorption but do not alter overall exposure significantly. Alcohol should be strictly avoided as it can increase CNS depression and risk of respiratory depression. |
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| L4 (Hazardous) |
| 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. |
| 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. |
| Clinical Pearls | XTAMPZA ER is an extended-release formulation of oxycodone designed to be taken once daily. It uses a polymer matrix to provide prolonged absorption. Do not crush, chew, or dissolve the capsules, as this can lead to rapid release and potential fatal overdose. Due to its high drug load, it is not interchangeable with other oxycodone ER products. Initiate with caution in opioid-naive patients; consider lower starting doses. Monitor for respiratory depression, especially during initiation and titration. Use with CYP3A4 inhibitors (e.g., ketoconazole) or inducers (e.g., rifampin) requires dose adjustment. Abuse-deterrent properties are limited; caution in patients with history of substance abuse. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Swallow the capsule whole; do not crush, chew, or dissolve it. · Avoid alcohol while taking this medication; it can increase the risk of dangerous side effects. · Do not stop abruptly; work with your doctor to taper the dose to avoid withdrawal symptoms. · Store safely out of reach of children and pets; dispose of unused medication via a take-back program. · May cause drowsiness or dizziness; avoid driving or operating machinery until you know how it affects you. · Report any breathing difficulty, severe constipation, or signs of overdose (e.g., extreme sleepiness, slow heartbeat). |