oxycodone hydrochloride.txt

CLINICAL USE

Opioid analgesic for moderate to severe pain

DOSE IN NORMAL RENAL FUNCTION

Oral: 5 mg 4–6 hourly; usual maximum dose 400 mg dailyM/R: 10 mg 12 hourly; usual maximum dose 200 mg 12 hourlyIV: 1–10 mg every 4 hours SC: initially 5 mg every 4 hours SC infusion: initially 7.5 mg over 24 hours

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :351.8

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :45

%Excreted unchanged in urine &nbsp &nbsp :

<10 &nbsp &nbsp &nbsp &nbsp &nbsp :

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1.2–6.31

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :2–4 (4.5, M/R)/3–5 (5.5 M/R)

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start with small doses.

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anti-arrhythmics: delayed absorption of mexiletine

Antidepressants: CNS excitation or depression with MAOIs – avoid concomitant use; possible CNS excitation or depression with moclobemide; increased sedative effects with tricyclics

Antivirals: concentration possibly increased by ritonavirSodium oxybate: enhanced effect of sodium oxybate – avoid concomitant use

ADMINISTRATION

Reconstition

–

Route

Oral, IV, IM, SC

Rate of Administration

Infusion over 24 hours

Comments

Dilute to a concentration of 1 mg/mL with glucose 5% or sodium chloride 0.9%

OTHER INFORMATION

Has been used in CKD 5 patients; start with lowest dose and gradually increase dose according to responseLimited accumulation of metabolites in renal failure compared with morphineIncreased volume of distribution in renal failure(Kirvela M, Lindgren L, Seppala T, et al. The pharmacokinetics of oxycodone in uremic patients undergoing renal transplantation. Journal of Clinical Anaesthesia. 1996; 8: 13–18.)2 mg of oral oxycodone is approximately equivalent to 1 mg of parenteral oxycodone

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