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. |
| Molecular Weight | 444.43 Da |
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 | Contraindicated due to teratogenicity (tetracycline-related malformations). |
| 2nd trimester | Contraindicated; causes permanent tooth discoloration and bone growth inhibition. |
| 3rd trimester | Contraindicated; same risks as t2. |
Clinical note
Comprehensive clinical and safety monograph for OXY-KESSO-TETRA (OXY-KESSO-TETRA).
| Placental transfer | Crosses placenta readily; achieves fetal serum levels 50-75% of maternal levels. |
| Breastfeeding | Excreted in breast milk; risk of dental staining and bone growth suppression in nursing infants. Avoid breastfeeding. |
| Lactation Rating | L5 (Contraindicated) |
■ 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 |
PregnancyBreastfeedingHypersensitivity to tetracyclinesSevere hepatic impairmentSystemic lupus erythematosus
| 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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| 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 | 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. |
| Food/Dietary | Avoid alcohol. Grapefruit and grapefruit juice may potentiate oxycodone effects and should be avoided. High-fat meals may delay oxycodone absorption but not overall extent. Take with food or milk if GI upset occurs, but avoid high-fat meals with rapid-release formulations. Ketorolac may increase risk of GI irritation; avoid spicy or acidic foods if sensitive. |
| Clinical Pearls | OXY-KESSO-TETRA is a fixed-dose combination of oxycodone and ketorolac. Oxycodone is a mu-opioid agonist; ketorolac is an NSAID with COX-1/COX-2 inhibition. This combination provides potent analgesia but increases risks of opioid-related respiratory depression and NSAID-related GI bleeding/renal impairment. Use lowest effective dose for shortest duration. Contraindicated in active peptic ulcer disease, severe renal impairment (CrCl <30 mL/min), or patients on anticoagulants. Monitor for signs of sedation, constipation, and urine output. Naloxone should be available for reversal of opioid overdose. |
| Patient Advice | Take this medication exactly as prescribed; do not increase dose or frequency without consulting your doctor. · This combination contains both a narcotic pain reliever (oxycodone) and a nonsteroidal anti-inflammatory drug (ketorolac). · Avoid alcohol, benzodiazepines, or other CNS depressants as they may increase risk of severe drowsiness, respiratory depression, and death. · Do not drive or operate heavy machinery until you know how this medication affects you. · Ketorolac increases risk of stomach bleeding; report black/bloody stools, bloody vomit, or abdominal pain immediately. · Drink plenty of fluids to reduce risk of kidney problems; report decreased urination or swelling. · Do not take other NSAIDs (e.g., ibuprofen, naproxen) or aspirin while on this drug. · This drug may cause constipation; increase fiber intake and hydration, and consider stool softeners if needed. · Do not stop abruptly; taper under medical supervision to avoid withdrawal symptoms. · Store in a secure place out of reach of children and away from pets; dispose of unused medication properly. |