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  Oxycodone (28:08.08) - 382132 
 

Oxycodone

AHFS Class: Opiate Agonists (28:08.08)

VA Class: CN101

Dihydrohydroxycodeinone

14-Hydroxydihydrocodeinone

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View the associated Essentials monograph.

Introduction

Oxycodone is a synthetic phenanthrene-derivative opiate agonist.

See Uses in the associated General Statement for more information.

Uses

Pain

Conventional preparations of oxycodone hydrochloride or hydrochloride and terephthalate salts are used orally for the management of moderate to moderately severe pain,154 155 156 such as that associated with bursitis, injuries, dislocations, simple fractures, and neuralgia. Conventional preparations also are used in the treatment of postoperative, postextractional, and postpartum pain.

Extended-release preparations of oxycodone hydrochloride are used orally for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time;166 uses include the treatment of cancer pain and nonmalignant pain, such as back pain, osteoarthritis-related pain, and pain during rehabilitation following total knee arthroplasty. 160 The manufacturers state that oxycodone hydrochloride extended-release tablets are not indicated for preoperative (preemptive) analgesia, or for the relief of pain in the immediate (initial 12–24 hours) postoperative period in patients not already receiving the drug or in those whose pain is mild or not expected to persist for an extended period of time. 166 Oxycodone extended-release tablets are indicated for postoperative use only in patients receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and to persist for an extended period of time.166 The extended-release preparation is not intended for use on an as-needed (“prn”) basis.166

Misuse and Abuse

Oxycodone has emerged as one of the most problematic abused opiate agonists in the US; therefore, patients should be advised about the risk of theft, and clinicians should be informed about abuse and diversion issues. (See Cautions.)

See Dosage and Administration in the associated General Statement for more information.

Dosage and Administration

Administration

Oxycodone is administered orally as the hydrochloride salt or as the hydrochloride and terephthalate salts, most often in combination with acetaminophen or aspirin.

Oxycodone hydrochloride extended-release tablets should be swallowed whole and should not be broken, chewed, or crushed since such physical alteration of the tablets could result in rapid release of the drug and absorption of a potentially toxic dose.166 The manufacturer states that oxycodone hydrochloride extended-release tablets should not be administered rectally because of increased bioavailability and peak plasma concentrations compared with oral administration.166 (See Pharmacokinetics.) Although food does not substantially affect the extent of oral absorption of oxycodone extended-release tablets, patients whose dosage is initially titrated to the 160-mg tablets (currently not commercially available in the US) should be cautioned about dietary intake to prevent increases in peak plasma concentrations resulting from administration with high-fat meals. (See Pharmacokinetics.) 166 Patients should be advised that the matrix core of the tablets does not completely dissolve and may be passed in the stool.166

Dosage

Oxycodone should be given in the smallest effective dose and as infrequently as possible to minimize the development of tolerance and physical dependence. Reduced dosage is indicated in debilitated patients, in very young or very old patients, and in patients receiving other CNS depressants.

The manufacturers recommend that initial dosages of 33–50% of the usual dosage be employed when therapy with oxycodone hydrochloride extended-release tablets is initiated in patients receiving other CNS depressants.166

In patients with severe pain, dosage of oxycodone should be adjusted according to the severity of the pain and the response and tolerance of the patient. In patients with extremely severe pain or in those who have become tolerant to the analgesic effect of opiate agonists, it may be necessary to exceed the usual dosage.

Conventional (Immediate-release) Preparations

The usual adult dosage of conventional oxycodone hydrochloride preparations is 5–15 mg every 4–6 hours.156 The usual adult dosage of conventional oxycodone preparations as the combined salts is 4.88 mg every 6 hours. Children 12 years of age or older may receive 1.22 mg of the combined salts every 6 hours. Children 6–12 years of age may receive 0.61 mg of the combined salts every 6 hours.

Extended-release Preparations

For the management of moderate to severe pain when an extended duration of continuous, around-the-clock opiate analgesia is anticipated, a suggested initial oral dosage of oxycodone hydrochloride extended-release tablets in patients 18 years of age or older who are receiving nonopiate analgesics is 10 mg every 12 hours. For patients previously receiving nonopiate analgesics, these drugs may be continued as oxycodone hydrochloride extended-release tablets are titrated to a dosage that provides adequate analgesia.166 For patients receiving conventional oxycodone preparations, the total daily dosage of the drug should be calculated and given as oxycodone hydrochloride extended-release tablets in 2 divided doses at 12-hour intervals.166

The manufacturers suggest that for patients receiving conventional formulations of another opiate, the equivalent total daily dosage of oral oxycodone should be calculated based on standard conversion factors suggested by the manufacturer and administered as oxycodone hydrochloride extended-release tablets in 2 divided doses at 12-hour intervals.166 Calculated doses that do not correspond to an available tablet strength should be rounded down to the nearest whole tablet.166

Patients receiving fentanyl transdermal systems may receive oxycodone hydrochloride extended-release tablets beginning 18 hours after removal of the transdermal system.166 The manufacturers state that an initial oxycodone hydrochloride dosage of approximately 10 mg every 12 hours as extended-release tablets can be substituted for each 25-mcg/hour increment in fentanyl transdermal system dosage; however, clinical experience with this dosage conversion ratio is limited.166

Although supplemental analgesia may be necessary during therapy with oxycodone hydrochloride extended-release tablets, the manufacturers state that all opiate analgesics given around-the-clock should be discontinued when oxycodone therapy is initiated. In addition, when patients are switched from therapy with oxycodone hydrochloride extended-release tablets to a parenteral opiate, conservative dose conversion ratios should be used to avoid toxicity.166

The 80-mg formulation should only be used in opiate tolerant patients whose opiate requirement is equivalent to a daily oxycodone hydrochloride dosage of 160 mg or more.166 The manufacturer’s labeling should be consulted for additional information on dosing the extended-release tablets.

Dosage should be adjusted according to patient tolerance and response, and supplemental analgesia in the form of conventional preparations or another suitable short-acting analgesic should be made available for breakthrough pain or to prevent pain that occurs predictably (e.g., incident pain associated with certain activities).

When therapy with oxycodone hydrochloride extended-release tablets is discontinued, it should be done so gradually to avoid precipitation of withdrawal symptoms.166 175

Dosage in Renal and Hepatic Impairment

In patients with impaired hepatic function, the manufacturers recommend that therapy with oxycodone hydrochloride extended-release tablets be initiated at 33–50% of the usual dosage and titrated carefully.166

In patients with impaired renal function (creatinine clearance less than 60 mL/minute), the initial dosage of oxycodone hydrochloride extended-release tablets should be reduced and adjusted according to the clinical situation.166

See Cautions in the associated General Statement for more information.

Cautions

Although adverse effects are milder than those of morphine, addiction liability of oxycodone is about the same as that of morphine, and the usual precautions of opiate agonist therapy should be observed. (See Cautions in the Opiate Agonists General Statement 28:08.08.) Oxycodone has been intentionally abused by crushing extended-release preparations and “snorting” the powder or dissolving the contents in water and injecting the solution IV. 166 157 158 159 160 Abuse by chewing extended-release preparations also has been reported. 166 157 158 159 Breaking, chewing, or crushing of extended-release oxycodone preparations results in immediate release of the opiate and the risk of a potentially fatal overdose.166 157 158 159 160 The risk of toxicity is increased when used concomitantly with alcohol or other CNS depressants, including other opiates.166

The manufacturers state that oxycodone extended-release tablets are subject to diversion and abuse.166 175 Patients should be instructed to keep oxycodone extended-release tablets in a secure place to prevent theft.175 Health-care professionals should contact the professional licensing board, or controlled substance authority in their states for information about prevention and detection of abuse or diversion of oxycodone hydrochloride extended-release tablets.166

When preparations containing oxycodone in combination with other drugs are administered, the cautions applicable to each ingredient must be considered.

Some commercially available formulations of oxycodone hydrochloride contain sodium metabisulfite, a sulfite that may cause allergic-type reactions, including anaphylaxis and life-threatening or less severe asthmatic episodes, in certain susceptible individuals. The overall prevalence of sulfite sensitivity in the general population is unknown but probably low; such sensitivity appears to occur more frequently in asthmatic than in nonasthmatic individuals.

Oxycodone hydrochloride extended-release tablets are contraindicated in patients with known or suspected paralytic ileus.166

Oxycodone is distributed into milk in low concentrations.166 Because of the possibility of sedation or respiratory depression in breast-fed infants, the manufacturer recommends that use of oxycodone hydrochloride extended-release tablets generally be avoided in nursing women.166

See Drug Interactions in the associated General Statement for more information.

See Acute Toxicity in the associated General Statement for more information.

See Pharmacology in the associated General Statement for more information.

See Pharmacokinetics in the associated General Statement for more information.

Pharmacokinetics

Following oral administration of conventional preparations of oxycodone, the analgesic effect occurs within 10–15 minutes, reaches its maximum in 30–60 minutes, and persists for 3–6 hours. Following oral administration of oxycodone as an extended-release tablet, the onset of analgesia occurred within 1 hour in most patients.166 Oxycodone is extensively metabolized to noroxycodone and oxymorphone and their glucuronide conjugates, with the formation of oxymorphone mediated by cytochrome P-450 (CYP) isoenzyme 2D6; oxycodone and its metabolites are excreted principally in urine. 166

The relative oral bioavailability of extended-release tablets of oxycodone hydrochloride compared with conventional oral preparations is 100%. The extended-release tablets are formulated to provide controlled delivery of oxycodone over 12 hours. In healthy individuals, the absorption half-life is 0.4 hours for conventional preparations versus 2 apparent absorption half-lives of 0.6 and 6.9 hours (corresponding to initial and prolonged release) for extended-release tablets. Release of the drug from the extended-release tablets is pH independent. In healthy adults who received a single dose of oxycodone as one 160-mg extended-release tablet after a high-fat (500–600 fat calories) breakfast, the peak plasma concentration was increased by 25% compared with administration in the fasting state.166 153 Following rectal administration of oxycodone hydrochloride extended-release tablets in healthy adults, the area under the plasma concentration-time curve (AUC) and peak plasma concentration were increased by 39 and 9%, respectively, compared with oral administration. 166 With multiple oral dosing, steady-state plasma concentrations usually are achieved within 24–36 hours in healthy individuals receiving an extended-release preparation of oxycodone. The apparent elimination half-life following oral administration of extended-release or conventional preparations is 4.5 or 3.2 hours, respectively.

Following oral administration of oxycodone hydrochloride extended-release tablets in patients with renal impairment (creatinine clearance less than 60 mL/minute), peak plasma concentrations of the drug and its noroxycodone metabolite were 50 and 20% higher, respectively, and AUCs of oxycodone, noroxycodone, and oxymorphone were 60, 50, and 40% higher, respectively, than values in individuals with normal renal function.166 The elimination half-life of oxycodone was increased by 1 hour in patients with renal impairment compared with individuals with normal renal function.166 Administration of oxycodone hydrochloride extended-release tablets to patients with mild to moderate hepatic impairment resulted in increases in peak plasma concentrations and AUCs of oxycodone (50 and 95%, respectively) and noroxycodone (20 and 65%, respectively) but decreases in peak plasma concentrations and AUC of oxymorphone (30 and 40%, respectively).166 The elimination half-life of oxycodone was increased by 2.3 hours in patients with mild to moderate hepatic impairment compared with individuals with normal hepatic function.166

See Chemistry and Stability in the associated General Statement for more information.

Chemistry and Stability

Chemistry

Oxycodone is a synthetic phenanthrene-derivative opiate agonist. The drug differs structurally from hydrocodone only in the attachment of a hydroxyl group to carbon 14 on the phenanthrene nucleus. Oxycodone occurs as long rods or as tautomeric, strongly refringent scales and is insoluble in water and soluble in alcohol. Oxycodone is commercially available as the hydrochloride salt or in combination preparations as the hydrochloride and the terephthalate salts; both salts are freely soluble in water and slightly soluble in alcohol. Oxycodone hydrochloride oral solution has a pH of 1.4–4.

Stability

Oxycodone hydrochloride preparations should be stored in tight containers and generally should be protected from light and stored at 15–30°C.

For further information on chemistry, pharmacology, pharmacokinetics, uses, cautions, chronic toxicity, acute toxicity, drug interactions, and dosage and administration of oxycodone, see the Opiate Agonists General Statement 28:08.08.

Preparations

Oxycodone preparations are subject to control under the Federal Controlled Substances Act of 1970 as schedule II (C-II) drugs. Because of concerns about the possibility of illicit use of tablets of such high strength, the manufacturer recently announced that oxycodone hydrochloride 160-mg extended-release tablets were withdrawn from the US market effective May 2001.152 158 160 This is a voluntary withdrawal and is not being mandated by the US Food and Drug Administration (FDA).152

Oxycodone Hydrochloride
RoutesFormsStrengthsBrand NamesManufacturer
Oral

Capsules

5 mg*

Oxycodone Hydrochloride Capsules (C-II)

Ethex, Mallinckrodt

OxyIR® (C-II)

Purdue Pharma

Solution

5 mg/5 mL*

Oxycodone Hydrochloride Oral Solution (C-II)

Mallinckrodt

Roxicodone® (C-II; with alcohol )

Xanodyne

20 mg/mL*

Oxycodone Hydrochloride Oral Concentrate Solution (C-II)

Mallinckrodt

Oxydose® (C-II; with propylene glycol)

Ethex

OxyFast® (C-II)

Purdue Pharma

Roxicodone® (C-II)

Xanodyne

Tablets

5 mg*

Endocodone® (C-II; scored)

Endo

Oxycodone Hydrochloride Tablets (C-II)

Amide, Ethex, Mallinckrodt, Watson

Percolone® (C-II; scored)

Endo

Roxicodone® (C-II; scored)

Xanodyne

15 mg

Roxicodone® (C-II; scored)

Xanodyne

30 mg

Roxicodone® (C-II)

Xanodyne

Tablets, extended-release

10 mg*

OxyContin® (C-II; with povidone)

Purdue Pharma

20 mg*

OxyContin® (C-II; with povidone)

Purdue Pharma

40 mg*

OxyContin® (C-II; with povidone)

Purdue Pharma

80 mg*

OxyContin® (C-II; with povidone)

Purdue Pharma

* available by nonproprietary name

Oxycodone and Acetaminophen
RoutesFormsStrengthsBrand NamesManufacturer
Oral

Capsules

5 mg Oxycodone Hydrochloride and Acetaminophen 500 mg*

Tylox® (C-II; with sodium metabisulfite)

Ortho-McNeil

Solution

5 mg/5 mL Oxycodone Hydrochloride and Acetaminophen 325 mg/5 mL

Roxicet® (C-II; with alcohol 0.4%)

Roxane

Tablets

2.5 mg Oxycodone Hydrochloride and Acetaminophen 325 mg

Percocet® (C-II; with povidone)

Endo

5 mg Oxycodone Hydrochloride and Acetaminophen 325 mg*

Endocet® (C-II; with povidone, scored)

Endo

Oxycodone Hydrochloride and Acetaminophen Tablets (C-II)

Amide, Barr, Mallinckrodt, Watson

Percocet® (C-II; with povidone, scored)

Endo

Roxicet® (C-II; scored)

Roxane

5 mg Oxycodone Hydrochloride and Acetaminophen 500 mg

Roxicet® Caplets (C-II; scored)

Roxane

7.5 mg Oxycodone Hydrochloride and Acetaminophen 325 mg*

Percocet® (C-II; with povidone)

Endo

7.5 mg Oxycodone Hydrochloride and Acetaminophen 500 mg*

Endocet® (C-II)

Endo

Oxycodone Hydrochloride and Acetaminophen Tablets (C-II)

Mallinckrodt, Watson

Percocet® (C-II; with povidone)

Endo

10 mg Oxycodone Hydrochloride and Acetaminophen 325 mg*

Percocet® (C-II; with povidone)

Endo

10 mg Oxycodone Hydrochloride and Acetaminophen 650 mg*

Endocet® (C-II)

Endo

Oxycodone Hydrochloride and Acetaminophen Tablets (C-II)

Mallinckrodt, Watson

Percocet® (C-II; with povidone)

Endo

* available by nonproprietary name

Oxycodone and Aspirin
RoutesFormsStrengthsBrand NamesManufacturer
Oral

Tablets

4.5 mg Oxycodone Hydrochloride, Oxycodone Terephthalate 0.38 mg, and Aspirin 325 mg*

Endodan® (C-II; scored)

Endo

Oxycodone Hydrochloride and Aspirin Tablets (C-II)

Watson

Percodan® (C-II; scored)

Endo

Roxiprin® (C-II)

Roxane

* available by nonproprietary name

Other Oxycodone Combinations
RoutesFormsStrengthsBrand NamesManufacturer
Oral

Tablets, film-coated

5 mg with Ibuprofen 400 mg

Combunox® (C-II; with povidone)

Forest

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit www.drugstore.com.

Combunox 5-400MG Tablets (FOREST): 20/$39.51 or 30/$59.27

Endocet 10-325MG Tablets (ENDO PHARMACEUTICALS): 20/$33.33 or 30/$49.99

Endocet 10-650MG Tablets (ENDO PHARMACEUTICALS): 20/$26.66 or 30/$39.99

Endocet 5-325MG Tablets (ENDO PHARMACEUTICALS): 30/$17.99 or 90/$52.97

Endocet 5-325MG Tablets (ENDO PHARMACEUTICALS): 30/$17.99 or 90/$53.97

Endocet 7.5-325MG Tablets (ENDO PHARMACEUTICALS): 20/$26.66 or 30/$39.99

Oxycodone HCl 10MG 12-hour Tablets (TEVA PHARMACEUTICALS USA): 20/$31.99 or 30/$43.99

Oxycodone HCl 15MG Tablets (MALLINCKRODT PHARM): 20/$17.99 or 30/$26.99

Oxycodone HCl 20MG/ML CONC (MALLINCKRODT PHARM): 20/$22.66 or 30/$33.99

Oxycodone HCl 30MG Tablets (MALLINCKRODT PHARM): 20/$24.66 or 30/$36.99

Oxycodone HCl 40MG 12-hour Tablets (TEVA PHARMACEUTICALS USA): 20/$93.33 or 30/$139.99

Oxycodone HCl 5MG Capsules (ETHEX): 20/$11.99 or 30/$13.99

Oxycodone HCl 5MG Tablets (MALLINCKRODT PHARM): 20/$16.66 or 30/$24.99

Oxycodone-Acetaminophen 10-325MG Tablets (WATSON LABS): 20/$40.66 or 30/$60.99

Oxycodone-Acetaminophen 10-650MG Tablets (WATSON LABS): 20/$33.33 or 30/$49.99

Oxycodone-Acetaminophen 5-325MG Tablets (MALLINCKRODT PHARM): 20/$11.99 or 30/$16.99

Oxycodone-Acetaminophen 5-500MG Capsules (MALLINCKRODT PHARM): 20/$15.99 or 30/$23.99

Oxycodone-Acetaminophen 5-500MG Capsules (ROXANE): 30/$21 or 90/$63

Oxycodone-Acetaminophen 7.5-325MG Tablets (MALLINCKRODT PHARM): 20/$31.99 or 30/$47.99

Oxycodone-Aspirin 4.5-0.38-325MG Tablets (WATSON LABS): 20/$26.66 or 30/$39.99

Oxycodone-Ibuprofen 5-400MG Tablets (WATSON LABS): 20/$33.33 or 30/$49.99

Oxyfast 20MG/ML CONC (PURDUE PHARMA L.P.): 30/$46.25 or 90/$138.75

OxyIR 5MG Capsules (PURDUE PHARMA L.P.): 20/$16.66 or 30/$24.99

Percocet 10-325MG Tablets (ENDO PHARMACEUTICALS): 20/$87.91 or 30/$131.87

Percocet 10-650MG Tablets (ENDO PHARMACEUTICALS): 20/$95.24 or 30/$142.86

Percocet 2.5-325MG Tablets (ENDO PHARMACEUTICALS): 30/$65.93 or 90/$186.8

Percocet 5-325MG Tablets (ENDO PHARMACEUTICALS): 20/$63 or 30/$94.51

Percocet 7.5-325MG Tablets (ENDO PHARMACEUTICALS): 20/$65.93 or 30/$98.9

Percocet 7.5-500MG Tablets (ENDO PHARMACEUTICALS): 20/$73.26 or 30/$109.89

Percodan 4.5-0.38-325MG Tablets (ENDO PHARMACEUTICALS): 20/$35.99 or 30/$47.97

Roxicet 5-325MG/5ML Solution (ROXANE): 470/$43.43 or 1340/$123.82

Roxicet 5-325MG Tablets (ROXANE): 20/$9.99 or 30/$14.99

Roxicodone 15MG Tablets (XANODYNE PHARMACAL, INC): 20/$29.39 or 30/$44.09

Roxicodone 30MG Tablets (XANODYNE PHARMACAL, INC): 20/$46.99 or 30/$66.99

Roxicodone 5MG/5ML Solution (XANODYNE PHARMACAL, INC): 430/$39.99 or 1210/$112.53

Selected Revisions March 2008, © Copyright, January 1973, American Society of Health-System Pharmacists, Inc. 7272 Wisconsin Avenue, Bethesda, MD 20814.

ASHP