Oxycodone controlled release

Oxycodone Controlled-release (CR) oxycodone is an opioid agonist and a schedule II controlled substance with an abuse liability similar to morphine. 

Not indicated for pain in the immediate postoperative period (the first 12 to 24 hours following surgery), or if the pain is mild or not expected to persist for an extended period of time. Oxycodone controlled-release tablets are only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Individualize treatment, moving from parenteral to oral analgesics as appropriate. 

Gabrail NY, Dvergsten C, Ahdieh H. Establishing the dosage equivalency of oxymorphone extended release and oxycodone controlled release in patients with cancer pain a randomized controlled study. CurrMed Res Opin. 2004 20 911-918. 

Afilalo M, Etropolski MS, Kuperwasser B, Kelly K, Okamoto A, Van Hove I, Steup A, Lange B, Rauschkolb C, Haeussler J. Efficacy and safety of tapen-tadol extended release compared with oxycodone controlled release for the management of moderate to severe chronic pain related to osteoarthritis of the knee a randomized, double-blind, placebo-and active-controlled phase III study. Clin Drug Investig 2010 30(8) 489-505. 

OxyContin (oxycodone hydrochloride controlled-release, Oxycodone CR) is an extended-duration oral opioid analgesic. It is formulated as a tablet with an outer more rapidly acting component and slower-release inner matrix that provides up to 12 hours of pain relief. Oxycodone CR offer prolonged and uniform analgesia avoiding trough effects observed with immediate-release oxycodone. Controlled-release oxycodone has abuse and diversion liability since the tablet can be easily crushed, and the entire 12 h dose administered nasally, leading to excessive acute effects and potential overdose [1]. 

Values represent numbers of patients reporting an event and percentages of patients evaluated. From Lange C, Lange R, Kuperwasser B, et al. Long-term safety of controlled, adjustable doses of tapentadol extended release and oxycodone controlled release results of a randomized, open-label, phases, 1-year trial In patients with chronic low back or osteoarthritis pain.Tenth Annual EULAR Congress, Poster number SAT-0481, June 2009, Copenhagen, Denmark. 

OxyContin is a controlled-released form of oxycodone and indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time OxyContin is not intended for use as a PRN analgesic The patient may experience fewer adverse reactions with oxycodone tlian morphine, and the drug is effective and safe for the elderly. The tablets are to be swallowed whole and are not to be broken, chewed, or crushed. 

Oxycodone, a controlled-release dosage form, is sometimes crushed by abusers to get the full 12-hour effect almost immediately. Snorting or injecting the crushed tablet can lead to overdose and death. 

Among the compounds that fall within this class are hydrocodone (e.g., Vicodin), oxycodone (e.g., OxyContin—an oral, controlled-release form of the drug), morphine, fentanyl, codeine, and related medications. Morphine and fentanyl are often used to alleviate severe pain, while codeine is used for milder pain. Other examples of opioids prescribed to relieve pain include propoxyphene (Darvon) hydromorphone (Dilaudid) and meperidine (Demerol), which is used less often because of its side effects. In addition to their effective pain-relieving properties, some of these medications can be used to relieve severe diarrhea (for example, Lomotil, also known as diphenoxylate) or severe coughs (codeine). 

Dosages and routes of administration Oxycodone is given by mouth in single doses of 5-10 mg or as controlled release preparations with doses of 40 mg (Cairns, 2001). Rectal administration is also possible. Oral formulations often contain combinations with paracetamol or acetylsalicylic acid. 

Kaiko, R.F., Benziger, D.P., Fitzmartin, R.D., Burke, B.E., Reder, R.F., Goldenheim, P.D. Pharmacokinetic-pharmacodynamic relationships of controlled-release oxycodone, Clin. Pharmacol. Ther. 1996, 59, 52-61. 

Davis, M.P., J. Varga, D. Dickerson, D. Walsh, et al., Normal-release and controlled-release oxycodone pharmacokinetics, pharmacodynamics, and controversy, Support. Care Cancer, 11(2), 84-92, 2003. 

Oral preparations of oxycodone include immediate-release pills, controlled-release pills, and a liquid solution. The immediate-release pills, as their name implies, get the drug into the bloodstream faster than other formulations. Within about 15 minutes of taking immediate-release oxycodone, the drug s analgesic effects take hold. Pain is lessened and the user experiences a feeling of drowsiness and/or well-being. 

The controlled-release formulations, on the other hand, prolong the release of oxycodone from the tablet for several hours. These pills have a special protective outer coating that makes them harder to digest, so that the oxycodone inside can be released slowly over a period of about 12 hours. That means the pills are capable of providing relief that lasts twice as long, allowing users to obtain the same effect they would get from taking an immediate-release tablet once every six hours. 

Watson, C. P., Moulin, D., Watt-Watson,J., Gordon, A., and Eisenhoffer,J. (2003). Controlled-release oxycodone relieves neuropathic pain A randomized controlled trial in painful diabetic neuropathy. Pain 105, 71-78. 

Roth SH, Fleischmann RM, Burch FX, Dietz F, Bockow B, Rapoport RJ, Rutstein J, Lacouture PG. Around-the-clock, controlled-release oxycodone therapy for osteoarthritis-related pain placebo-controlled trial and long-term evaluation. Arch Intern Med 2000 160(6) 853-60. 

Hale ME, Fleischmann R, Salzman R, Wild J, Iwan T, Swanton RE, Kaiko RF, Lacouture PG. Efficacy and safety of controlled-release versus immediate-release oxycodone randomized, double-blind evaluation in patients with chronic back pain. Clin J Pain 1999 15(3) 179-83. 

Kaplan R, Parris WC, Citron ML, Zhukovsky D, Reder RF, Buckley BJ, Kaiko RF. Comparison of controlled-release and immediate-release oxycodone tablets in patients with cancer pain. J CUn Oncol 1998 16(10) 3230-7. 

Bruera E, Belzile M, Pituskin E, Fainsinger R, Darke A, Harsanyi Z, Babul N, Ford I. Randomized, double-blind, cross-over trial comparing safety and efficacy of oral controlled-release oxycodone with controlled-release morphine in patients with cancer pain. J Chn Oncol 1998 16(10) 3222-9. 

Rischitelli DG, Karbowicz SH. Safety and efficacy of controlled-release oxycodone a systematic literature review. Pharmacotherapy 2002 22(7) 898-904. 

Oxycodone PO 5-10 mg q 3-5 h Controlled release, 10-20 mg q 12 h Use in moderate/severe pain Most effective when used with NSAIDs or aspirin or acetaminophen Use immediate-release product with controlled-release product to control "breakthrough" pain in cancer patients... 

Mandema, J., Kaiko, R.F., Oshlack, B., Reder, R.F., and Stanski, D.R. Characterization and validation of a pharmacokinetic model for controlled-release oxycodone. British Journal of Clinical Pharmacology 1996 42 747-756. 

Food can delay the absorption of dextropropoxyphene (propoxyphene), but the total amount absorbed may be slightly increased. Food increases the bioavailability of oral morphine solution and produces a sustained serum level, however, the absorption of some controlled-release preparations of morphine may be delayed by food. Food may also increase the bioavailability of oxycodone solution, but sustained-release preparations of oxycodone and tramadol and immediate-release hydromorphone appear not to be affected by food. 

A study in 22 healthy subjects found that the bioavailability of oxycodone as an immediate-release solution was significantly altered by consumption of a high-fat meal the AUC was increased by 20% and the maximum plasma level was decreased by 18%, when compared with the fasted state. However, there was no significant effect of food on the bioavailability of oxycodone given as a controlled-release tablet. ... 

Kampe S, Wolter K, Warm M, Dagtekin O, Shaheen S, Landwehr S. Clinical equivalence of controlled-release oxycodone 20 mg and controlled-release tramadol 200 mg after surgery for breast cancer. Pharmacology 2009 84 276-81. 

Oxycodone CR (controlled release) is indicated for patients whose pain requires control around the clock on a longer term or chronic basis as in cancer, osteoarthritis, or during rehabilitation following major orthopedic surgery (refer to Chapter 21). Oxycodone CR and IR have equal analgesic efficacy... 

Although parenteral preparations of oxycodone exist, in the USA oral formulations only are available. Controlled-release forms must be swallowed whole so as not to interfere with the controlled-release mechanism chewing or cutting may lead to an overdose. Available oxycodone preparations are listed in Table 19.1. 

Initial doses of oxycodone IR (all oxycodone is IR unless in the controlled-release formulation) are 5 to... 

Generic Name oxycodone hydrochloride controlled-release tablets... 

Chronic non-surgical pain OxyContin tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, round-the-dock analgesic is needed for an extended period of time. 

Somatic pain treatment with OxyContin for patients with osteoarthritis, back pain and pre- and post-operative pain is well documented. Round-the-clock controlled-release oxycodone therapy seems to provide effective analgesia for patients with chronic, moderate to severe, osteoarthritis-related pain. 

Portenoy RK, Farrar JT, Backonja MM, Cleeland CS, Yang K, Friedman M, Coined SV, Richards P. Long-term use of controlled-release oxycodone for noncancer pain results of a 3-year registry study. Clin JPain 2007 23(4) 287-299. 

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