Oxycodone
OxyContin · Roxicodone · Percocet (with acetaminophen)
Semisynthetic oral μ-opioid agonist
μ-opioid agonist, ~1.5× the potency of oral morphine. Oral bioavailability far higher than morphine.
Indications
- •Moderate–severe postop pain (oral)
- •Multimodal oral step-down / discharge analgesia
Dosing
| Context | Adult | Pediatric |
|---|---|---|
| Immediate-release | 5–10 mg PO q4–6h | — |
| Extended-release | Individualized (not for opioid-naïve acute pain) | — |
Pharmacokinetics
Onset 10–15 min PO, duration 3–4 h (IR).
Respiratory effects
Dose-dependent depression.
Side effects
- !Constipation
- !N/V
- !Sedation
- !Dependence/misuse potential
Contraindications
- ×Ileus / bowel obstruction
- ×MAOI within 14 days (relative)
Reversal / antidote
Naloxone
Clinical pearls
- ★Common oral discharge opioid — pair with scheduled acetaminophen ± NSAID (multimodal).
- ★Percocet contains acetaminophen — respect the APAP daily maximum.
Other drugs in Narcotics & Analgesics
- Fentanyl
μ-opioid receptor agonist. ~100× potency of morphine.
- Remifentanil
μ-opioid agonist. Ester linkage hydrolyzed by nonspecific tissue + plasma esterases — no organ-dependent clearance.
- Morphine
μ-opioid receptor agonist. Active metabolite morphine-6-glucuronide (M6G) is analgesic and renally cleared — accumulates in renal failure → prolonged sedation/respiratory depression. Causes histamine release.
- Hydromorphone
μ-opioid agonist ~5–7× more potent than morphine. No clinically significant active metabolites → safer than morphine in renal failure. Less histamine release.
- Sufentanil
Most potent opioid in common clinical use — ~1000× morphine, ~10× fentanyl. High lipid solubility.
- Alfentanil
μ-opioid agonist ~1/5–1/10 the potency of fentanyl but FASTEST onset of the family — low pKa means a high non-ionized fraction at physiologic pH.
- Meperidine
μ-opioid agonist ~1/10 morphine, plus κ-agonism (anti-shivering). Active metabolite normeperidine is renally cleared, proconvulsant, and neurotoxic.
- Methadone
μ-opioid agonist with NMDA-receptor antagonism (blunts tolerance + opioid-induced hyperalgesia) and monoamine reuptake inhibition. Very long, variable half-life.
Browse all classes: /reference/drugs
Suggested reading
- •Stoelting & Hines, Pharmacology & Physiology in Anesthetic Practice, 6e
- •Miller's Anesthesia, 9e
- •FDA package insert
