OXY-KESSO-TETRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OXY-KESSO-TETRA (OXY-KESSO-TETRA).
Oxycodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, though it can interact with other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxycodone. Oxycodone is combined with aspirin (OXY-KESSO-TETRA) for analgesic synergy.
| Metabolism | Oxycodone is extensively metabolized in the liver via CYP3A4 and CYP2D6. Major metabolites include noroxycodone (via CYP3A4) and oxymorphone (via CYP2D6). Aspirin is hydrolyzed to salicylate in the gut and liver. |
| Excretion | Primarily renal (60-70% as unchanged drug) via glomerular filtration and tubular secretion; approximately 20-30% is metabolized hepatically with metabolites excreted renally; less than 5% eliminated via bile/feces. |
| Half-life | Terminal elimination half-life approximately 8-12 hours in adults with normal renal function; prolonged to 20-40 hours in moderate to severe renal impairment (CrCl <30 mL/min), necessitating dose adjustment. |
| Protein binding | Approximately 70-80% bound primarily to serum albumin. |
| Volume of Distribution | 0.5-0.8 L/kg, indicating distribution into total body water and some tissue binding. |
| Bioavailability | Oral: 85-95% (high first-pass metabolism negligible); Intramuscular: approximately 100%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes. |
| Duration of Action | 12-24 hours depending on dose and route; clinical effect may persist longer with high doses or renal impairment. |
200 mg orally every 8 hours for 10 days.
| Dosage form | CAPSULE |
| Renal impairment | CrCl 30-50 mL/min: 200 mg every 12 hours; CrCl 15-29 mL/min: 200 mg every 24 hours; CrCl <15 mL/min: 200 mg every 48 hours or consider alternative. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: 200 mg every 12 hours; Child-Pugh Class C: 100 mg every 12 hours or avoid use. |
| Pediatric use | 10 mg/kg/dose orally every 8 hours, maximum 200 mg/dose. |
| Geriatric use | Start at 200 mg every 12 hours; monitor renal function and adjust based on CrCl. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OXY-KESSO-TETRA (OXY-KESSO-TETRA).
| Breastfeeding | Excreted in breast milk. M/P ratio not available. Avoid breastfeeding due to potential for infant sedation and withdrawal. |
| Teratogenic Risk | Pregnancy Category D. First trimester: increased risk of neural tube defects and cardiac malformations. Second and third trimesters: risk of fetal growth restriction, preterm birth, and neonatal withdrawal syndrome. |
| Fetal Monitoring |
■ FDA Black Box Warning
WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; CYP450 3A4 INTERACTION; RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS; RISK OF MEDICATION ERRORS; and RISK OF ASPIRIN-INDUCED BLEEDING.
| 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, aspirin, or any component of the formulation; children with viral infections due to risk of Reye's syndrome (aspirin); history of aspirin-induced asthma or allergic reactions to NSAIDs; bleeding disorders; severe hepatic impairment; severe renal impairment; pregnancy (especially third trimester due to risk of premature closure of ductus arteriosus); breastfeeding.
| 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; risk of medication errors; aspirin-induced bleeding risk including Reye's syndrome in children; elderly and debilitated patients; renal impairment; hepatic impairment; severe hypotension; adrenal insufficiency; seizures; severe hypertension; use in pregnancy; use in breastfeeding; gastrointestinal obstruction; pancreatitis; use in patients with head injury or increased intracranial pressure; impaired consciousness; use in patients with known or suspected GI obstruction; use in patients with bleeding disorders; use in patients with asthma or other respiratory conditions; use in patients with prostatic hyperplasia or urinary stricture; use in patients with biliary tract disease; acute pancreatitis; history of substance abuse; suicidal tendencies; use in patients with severe hepatic or renal impairment; use in patients with severe hypotension; use in patients with adrenocortical insufficiency; use in patients with hypothyroidism; use in patients with prostatic hyperplasia; use in patients with urethral stricture; use in patients with acute alcoholism; use in patients with delirium tremens; use in patients with kyphoscoliosis; use in patients with myxedema; use in patients with severe pulmonary disease; use in patients with toxic psychosis. |
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| Monitor maternal blood pressure, liver and renal function, and fetal growth via ultrasound. Assess for signs of preterm labor. |
| Fertility Effects | May impair spermatogenesis and ovulation. Reversible upon discontinuation. |