OXAYDO

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OXAYDO (OXAYDO).

How it works

Oxycodone is a full opioid agonist with relative selectivity for mu-opioid receptors, although it can bind to kappa-opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect to analgesia for oxycodone.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4 and CYP2D6; major metabolites include noroxycodone (via CYP3A4) and oxymorphone (via CYP2D6). Conjugated with glucuronic acid.
Excretion	Primarily renal as unchanged drug and metabolites; ~90% excreted in urine (approx 10% unchanged oxycodone, rest as noroxycodone and oxymorphone conjugates) and <10% in feces via biliary elimination.
Half-life	Terminal elimination half-life is 3.5-5.5 hours for immediate-release oxycodone; clinically dose every 4-6 hours for sustained analgesia.
Protein binding	~45% bound to plasma proteins, primarily albumin.
Volume of Distribution	2.6 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral bioavailability is 60-87% due to first-pass metabolism.
Onset of Action	Oral: 10-15 minutes for pain relief; peak effect at 30-60 minutes.
Duration of Action	3-6 hours for immediate-release formulations; duration varies with dose and patient tolerance.

Classification & Brands

Dosing & administration

Oral, 5-10 mg every 4-6 hours as needed for pain; maximum 60 mg per day.

Dosage form	TABLET
Renal impairment	CrCl <30 mL/min: reduce dose by 50% and extend dosing interval to every 6 hours; avoid use in CrCl <15 mL/min.
Liver impairment	Child-Pugh class A: no adjustment; Child-Pugh class B: reduce dose by 50%; Child-Pugh class C: avoid use.
Pediatric use	Children (≥11 years): 5-10 mg every 4-6 hours as needed; maximum 60 mg/day. Children <11 years: not recommended due to high concentration.
Geriatric use	Initiate at 3 mg every 6 hours; titrate cautiously due to increased sensitivity and risk of respiratory depression.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OXAYDO (OXAYDO).

Breastfeeding	Enters breast milk; no specific M/P ratio reported. Use caution due to risk of infant sedation and respiratory depression. Monitor for signs of toxicity; alternative analgesics preferred.
Teratogenic Risk	Pregnancy Category C. First trimester: Limited human data; animal studies show increased risk of neural tube defects at high doses. Second and third trimesters: Prolonged use may cause neonatal opioid withdrawal syndrome and respiratory depression. No specific teratogenicity pattern identified in humans.

Warnings & precautions

■ FDA Black Box Warning

WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS. See full prescribing information for complete boxed warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to oxycodone or any component of the formulation","Significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus"]

Clinical Precautions

Precautions

["Addiction, abuse, and misuse","Life-threatening respiratory depression","Accidental ingestion (especially in children)","Neonatal opioid withdrawal syndrome","Risks from concomitant use with benzodiazepines or other CNS depressants","Adrenal insufficiency","Severe hypotension","Gastrointestinal effects (constipation, ileus)","Seizures in patients with seizure disorders","Serotonin syndrome with concomitant serotonergic drugs"]

Clinical Tips & Counseling

Drug interactions

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OXAYDO

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OXAYDO (OXAYDO).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP3A4 and CYP2D6; major metabolites include noroxycodone (via CYP3A4) and oxymorphone (via CYP2D6). Conjugated with glucuronic acid.
Excretion	Primarily renal as unchanged drug and metabolites; ~90% excreted in urine (approx 10% unchanged oxycodone, rest as noroxycodone and oxymorphone conjugates) and <10% in feces via biliary elimination.
Half-life	Terminal elimination half-life is 3.5-5.5 hours for immediate-release oxycodone; clinically dose every 4-6 hours for sustained analgesia.
Protein binding	~45% bound to plasma proteins, primarily albumin.
Volume of Distribution	2.6 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral bioavailability is 60-87% due to first-pass metabolism.
Onset of Action	Oral: 10-15 minutes for pain relief; peak effect at 30-60 minutes.
Duration of Action	3-6 hours for immediate-release formulations; duration varies with dose and patient tolerance.

Classification & Brands

Dosing & administration

Oral, 5-10 mg every 4-6 hours as needed for pain; maximum 60 mg per day.

Dosage form	TABLET
Renal impairment	CrCl <30 mL/min: reduce dose by 50% and extend dosing interval to every 6 hours; avoid use in CrCl <15 mL/min.
Liver impairment	Child-Pugh class A: no adjustment; Child-Pugh class B: reduce dose by 50%; Child-Pugh class C: avoid use.
Pediatric use	Children (≥11 years): 5-10 mg every 4-6 hours as needed; maximum 60 mg/day. Children <11 years: not recommended due to high concentration.
Geriatric use	Initiate at 3 mg every 6 hours; titrate cautiously due to increased sensitivity and risk of respiratory depression.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OXAYDO (OXAYDO).

Breastfeeding	Enters breast milk; no specific M/P ratio reported. Use caution due to risk of infant sedation and respiratory depression. Monitor for signs of toxicity; alternative analgesics preferred.
Teratogenic Risk	Pregnancy Category C. First trimester: Limited human data; animal studies show increased risk of neural tube defects at high doses. Second and third trimesters: Prolonged use may cause neonatal opioid withdrawal syndrome and respiratory depression. No specific teratogenicity pattern identified in humans.