Clinical beta

FMBM is currently in clinical beta. Content is for professional review/testing and must not replace local protocols, senior clinical judgment, or official prescribing references.

Drug Monograph

Oxycodone

USE IF: Moderate-severe pain, cancer pain, post-op pain, opioid rotation

AVOID IF: Opioid-naive (ER), severe respiratory depression, MAOI use

Oxycodone

Strong opioid (mu-opioid receptor agonist)

OpioidCYP3A4ER/IRPCAHigh-risk interactions

Indication

Moderate-severe pain, cancer pain, post-op pain, opioid rotation

At a glance

INDICATION -> Strong opioid alternative to morphine

ADULT DOSE -> 5–15 mg PO q4–6h (IR)

MAX DOSE -> No ceiling (titrate); opioid-naive start <=60 mg/day

CONTRA -> ER in opioid-naive, severe respiratory depression, MAOI use

ANTIDOTE -> Naloxone (prolonged infusion for ER overdose)

Quick facts

Onset

10–30 min (PO IR); 1–5 min (IV)

Duration

Peak 0.5–1.5 h (IR), 3–4 h (ER); duration 4–6 h (IR), 8–12 h (ER). Half-life 3–5 h (IR), up to ~14 h in severe hepatic impairment.

Routes

PO, IV, SC

Pregnancy

Short-term acceptable

Renal

Reduce dose

Hepatic

Reduce dose significantly

Do not miss

Time to action: 10β€”30 min (PO), 1β€”5 min (IV)

Max dose

  • No ceiling (titrate); opioid-naive <=60 mg/day initially.

Critical risks

  • Respiratory depression.
  • ER dose-dumping (crushing/chewing can be fatal).
  • CYP3A4-related toxicity.

Antidote

  • Naloxone (repeat dosing often required).
  • Prolonged naloxone infusion may be required for ER toxicity.

High-risk scenarios

  • Fluconazole/azole use.
  • Elderly.
  • Hepatic failure.

Key interactions

  • CYP3A4 inhibitors.
  • Benzodiazepines.
  • MAOI.

Indications

Primary

  • Moderate-severe pain
  • Cancer pain

Secondary

  • Post-op pain
  • Trauma
  • PCA analgesia

Other

  • Dyspnea (palliative)
  • Opioid rotation

Dosing

Standard: 5β€”15 mg PO q4β€”6h

Max daily dose

  • No fixed ceiling in monitored settings; titrate to effect and toxicity.
  • Opioid-naive initial total dose <=60 mg/day.

Adult - PO

  • IR: 5–15 mg q4–6h PRN.
  • ER: 10 mg q12h (opioid-tolerant only).

Adult - IV

  • Opioid-naive: 1–2 mg IV slow.
  • Opioid-tolerant: 2–4 mg IV titrated.
  • PCA: 1 mg demand q6–8 min.

Pediatric

  • >=11 years: 0.05–0.15 mg/kg q4–6h.

Renal adjustment

  • GFR 10–50: start at ~50% dose.
  • GFR <10: avoid if possible.

Hepatic adjustment

  • Moderate-severe impairment: start at 30–50% of usual dose.

Warnings

Clinical warnings

  • Respiratory depression (black box).
  • CYP3A4 interaction risk (black box context).
  • Addiction/misuse risk.
  • ER dose-dumping risk (crushing can be fatal).
  • Neonatal withdrawal.
  • Hyperalgesia (dose-dependent).
  • Constipation (class effect).

Adverse effects

  • Common: sedation, nausea, constipation, pruritus.
  • Serious: respiratory depression, severe sedation, misuse/dependence.

Contraindications / caution

Do not use

  • Severe respiratory depression.
  • Paralytic ileus.
  • MAOI use.
  • ER formulation in opioid-naive patients = absolute contraindication.

Use caution / avoid high doses

  • Hepatic failure.
  • Renal impairment.
  • Elderly.
  • OSA/COPD.
  • CYP3A4 inhibitors.

Drug interactions

  • CYP3A4 inhibitors (fluconazole, clarithromycin) -> increased toxicity.
  • CYP3A4 inducers -> reduced analgesia.
  • Benzodiazepines -> respiratory depression/death.
  • MAOI -> contraindicated.
  • Alcohol -> potentially fatal CNS/respiratory depression.

Special populations

Pediatrics

Use specialist protocols; >=11 years dosing only.

Pregnancy

Short-term use acceptable; monitor for NOWS risk.

Breastfeeding

Avoid if possible (morphine often preferred).

Elderly

Start at ~50% dose (e.g., 2.5–5 mg IR).

Liver disease

Reduce dose 30–50%; prolonged half-life expected.

Renal impairment

Reduce dose; avoid severe renal impairment if alternatives available.

Administration

  • PO preferred route.
  • ER tablets/capsules must NEVER be crushed or chewed.
  • Targin/Targinact: observe local maximum naloxone component limits (e.g., 40 mg/day in some protocols).

Infusion / dilution

  • IV dilute to ~1 mg/mL.
  • Slow IV push over 3–5 minutes.

Monitoring

  • Renal function.
  • LFTs.
  • Respiratory rate.
  • RR <8–10/min or excessive sedation -> HOLD opioid and initiate urgent intervention.
  • Sedation score.
  • Pain score.
  • Bowel function.
  • Signs of opioid-induced hyperalgesia.

Overdose / toxicity

IF SUSPECTED OXYCODONE OVERDOSE: ABC first.

Recognition

  • Toxic dose is variable; ER ingestion carries higher prolonged-risk profile.
  • Miosis + respiratory depression + coma.

Immediate actions

  • Naloxone with repeat dosing based on response.
  • Escalate naloxone up to 2 mg IV and repeat as needed in ER/long-acting opioid toxicity.
  • Airway and ventilatory support.
  • Activated charcoal <=1 h when appropriate and airway protected.

Antidote

  • Naloxone (repeat dosing often required).

Decontamination

  • Activated charcoal <=1 h when indicated.

Escalation

  • Naloxone infusion for 12–24 h may be required in ER overdose.

Clinical pearls

Common mistakes, resistance logic, and bedside traps

Morphine comparison

  • Not equipotent with morphine: oral oxycodone is ~1.5x stronger.

ER safety

  • ER is NEVER for opioid-naive patients.

Fluconazole risk

  • Fluconazole interaction is a major potential fatal risk.

Oral absorption

  • Better oral bioavailability than morphine.

Targin effect

  • Targin can reduce constipation burden in selected patients.

Hyperalgesia

  • If hyperalgesia emerges, reduce/switch opioid rather than escalating dose.

PCA role

  • IV oxycodone PCA is used in many post-op protocols.

Renal choice

  • Can be safer than morphine in CKD, but fentanyl is often preferred when feasible.

Pharmacokinetics

  • Oral bioavailability ~60–87%.
  • Hepatic metabolism (CYP3A4 major pathway).
  • Renal excretion.
  • Approximate oral:IV potency ratio ~2:1.
  • Oral oxycodone is about 1.5x stronger than oral morphine.

Mechanism of action

  • Full mu-opioid receptor agonist.
  • Parent drug is active (not a prodrug).
  • CYP3A4 metabolism to noroxycodone.
  • Minor CYP2D6 pathway to oxymorphone.

Common brand names

Saudi Arabia

OxyContin Β· OxyNorm Β· Targin / Targinact

Global

Roxicodone Β· Percocet Β· Xtampza ER Β· Oxaydo

Common trade names are curated examples only β€” formulations and availability vary. Verify the exact product name with your local pharmacy and national regulator before prescribing or dispensing.

Country practice notes

  • Widely available across Gulf (OxyContin, OxyNorm, Targin).
  • Strict narcotic regulation with SFDA-controlled prescribing.
  • Increasing use in oncology and palliative care.
  • IV oxycodone is used in some Middle East hospitals (including PCA protocols).
  • Access varies by country and institution.

Saudi Arabia β€” confirm with local formulary.