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Oxycodone ER

Ernest A Kopecky, Alison B Fleming, Naama Levy-Cooperman, Melinda O'Connor, Edward Sellers
Oxycodone DETERx(®) (Collegium Pharmaceutical Inc, Canton, MA) is an extended-release, microsphere-in-capsule, abuse-deterrent formulation designed to retain its extended-release properties after tampering (eg, chewing/crushing). This randomized, double-blind, placebo-controlled, triple-dummy study evaluated the oral abuse potential of intact and chewed oxycodone DETERx capsules compared with crushed immediate-release oxycodone. Subjects with a history of recreational opioid use who were nondependent/nontolerant to opioids were enrolled...
September 27, 2016: Journal of Clinical Pharmacology
Bill H McCarberg, Ernest A Kopecky, Melinda O'Connor, Ann Marseilles, Ravi K Varanasi, Christy Thompson, Alison B Fleming
BACKGROUND: Patients with chronic pain may experience difficulty swallowing, in part due to worsening disease, comorbid conditions, iatrogenic etiology, or age. Patients or caregivers may manipulate extended-release (ER) opioid formulations to facilitate oral dosing due to a lack of therapeutic options that allow for sprinkle or enteral feeding tube administration. If crushed or broken, current oral ER opioids can be associated with adverse sequelae, including risk of potentially fatal overdose...
September 26, 2016: Current Medical Research and Opinion
Howard D Chilcoat, Paul M Coplan, Venkatesh Harikrishnan, Louis Alexander
BACKGROUND: Doctor-shopping (obtaining prescriptions from multiple prescribers/pharmacies) for opioid analgesics produces a supply for diversion and abuse, and represents a major public health issue. METHODS: An open cohort study assessed changes in doctor-shopping in the U.S. for a brand extended release (ER) oxycodone product (OxyContin) and comparator opioids before (July, 2009 to June, 2010) versus after (January, 2011 to June, 2013) introduction of reformulated brand ER oxycodone with abuse-deterrent properties, using IMS LRx longitudinal data covering >150 million patients and 65% of retail U...
August 1, 2016: Drug and Alcohol Dependence
Theodore J Cicero, Matthew S Ellis, Zachary A Kasper
The introduction of extended-release opioid analgesics helped initiate an epidemic of prescription opioid abuse in the United States. To make access to the drug by crushing or dissolution more difficult, abuse-deterrent formulations (ADFs) of OxyContin (Purdue Pharma, Stamford, CT) and Opana ER (Endo Pharmaceuticals Inc., Malvern, PA), which use the same foundation technology (Intac, Grunenthal, Aachen, Germany), were introduced in 2010 and 2012, respectively. To examine their relative effectiveness, we used a structured survey of 12,124 individuals entering treatment for opioid use disorder followed by a more focused online survey with a subset of these patients (N = 129) using both structured and open-ended questions...
June 2016: Pain
Kuan Gandelman, Michael Lamson, Candace Bramson, Kyle Matschke, Joanne Salageanu, Bimal Malhotra
ALO-02 capsules (ALO-02) contain pellets that consist of extended-release oxycodone that surrounds sequestered naltrexone. The primary objective was to characterize the pharmacokinetics (PK) of oxycodone following single- and multiple-dose oral administration of ALO-02 40 mg BID in healthy volunteers. Secondary objectives were to characterize (1) the PK of oxycodone following single- and multiple-dose administration of a comparator OxyContin (OXY-ER) 40 mg BID as well as an alternate regimen of ALO-02 80 mg QD, and (2) the safety and tolerability assessments...
September 2015: Clinical Pharmacology in Drug Development
Srinivas Nalamachu, Ernest A Kopecky, Robert Taylor, Ben Vaughn, Melinda O'Connor
BACKGROUND: Abuse deterrent formulations (ADF) are designed to prevent the misuse of opioids by tampering (e.g. physical and chemical manipulation) in order to ingest the opioid in a manner other than intended. Extended-release (ER) formulations are formulated with a larger drug load than immediate-release (IR) formulations, which makes ER opioids more desirable to drug abusers than I.R. formulations. ADFs, therefore, are particularly useful with ER opioid agents, which are designed to produce consistent analgesia over prolonged dosing intervals...
July 2016: Current Medical Research and Opinion
Alison B Fleming, Todd A Scungio, Michael P Grima, Stephen P Mayock
OBJECTIVE: Abuse of prescription analgesics is a well-recognized problem, with nearly 2 million people aged 12 years or older initiating nonmedical use of pain relievers in 2012. The prevalence of opioid abuse via intravenous (IV) injection has led to the development of dosage forms designed to deter abuse using different inactive ingredients and formulation strategies. This study evaluated the IV abuse potential for a novel, microsphere-encapsulated abuse-deterrent formulation of oxycodone, Xtampza™ ER (referred to as "oxycodone DETERx")...
January 2016: Journal of Opioid Management
Nobushige Yabe, Shinji Murai, Yoko Harada, Takahiro Yokose, Takamichi Yokoe, Ippei Oto, Takahisa Yoshikawa, Kenjiro Kitasato, Hirotomo Shimizu, Hiromitsu Jinno, Yuko Kitagawa
A 51-year-old woman had previously received treatment for breast cancer at another hospital but had refused early and aggressive treatment. Therefore, she was treated with symptomatic therapy. As her disease progressed, the patient wished to receive palliative care, and was transferred to a palliative care hospital. However, based on her general condition, it was determined that aggressive treatment should not be abandoned, and she was referred to our hospital for treatment. During her initial visit, the patient was found to have left breast cancer with chest wall invasion, right breast metastasis, multiple liver and lung metastases, left pleural effusion accompanied by pleural dissemination, and left upper limb edema...
November 2015: Gan to Kagaku Ryoho. Cancer & Chemotherapy
David M Biondi, Jim Xiang, Mila Etropolski, Bruce Moskovitz
OBJECTIVE: Management of chronic pain in elderly adult patients is often complicated by analgesic medication-related side effects. This post hoc analysis of pooled data evaluated the tolerability and analgesic efficacy of tapentadol extended release (ER) compared with oxycodone controlled release (CR) in elderly adult patients (≥ 75 years of age) with moderate to severe, chronic osteoarthritis knee or low back pain. METHODS: Data were pooled from three similarly designed, randomized, doubleblind, placebo- and active-controlled, phase 3 studies of tapentadol ER for moderate to severe, chronic osteoarthritis knee (NCT00421928, NCT00486811) or low back (NCT00449176) pain, and data for patients ≥ 75 years of age were evaluated...
September 2015: Journal of Opioid Management
Mary Hanna Bekhit
This article provides a historical and pharmacological overview of a new opioid analgesic that boasts an extended-release (ER) formulation designed to provide both immediate and prolonged analgesia for up to 12 hours in patients who are experiencing acute pain. This novel medication, ER oxycodone/acetaminophen, competes with current US Food and Drug Administration (FDA)-approved opioid formulations available on the market in that it offers two benefits concurrently: a prolonged duration of action, and multimodal analgesia through a combination of an opioid (oxycodone) with a nonopioid component...
2015: Journal of Pain Research
Robert Buynak, Stephen A Rappaport, Kevin Rod, Pierre Arsenault, Fabian Heisig, Christine Rauschkolb, Mila Etropolski
PURPOSE: Tapentadol extended release (ER) has demonstrated efficacy and safety for the management of moderate to severe, chronic pain in adults. This study evaluated the long-term safety and tolerability of tapentadol ER in patients with chronic osteoarthritis or low back pain. METHODS: Patients were enrolled in this 1-year, open-label extension study after completing one of two 15-week, placebo-controlled studies of tapentadol ER and oxycodone controlled release (CR) for osteoarthritis knee pain (NCT00421928) or low back pain (NCT00449176), a 7-week crossover study between tapentadol immediate release and tapentadol ER for low back pain (NCT00594516), or a 1-year safety study of tapentadol ER and oxycodone CR for osteoarthritis or low back pain (NCT00361504)...
November 1, 2015: Clinical Therapeutics
Ryan M Franke, Terri Morton, Krishna Devarakonda
This analysis evaluated the single-dose population pharmacokinetics (PK) of biphasic immediate-release (IR)/extended-release (ER) oxycodone (OC)/acetaminophen (APAP) 7.5/325 mg tablets administered under fasted conditions and the effects of a meal on their single-dose population PK. Data were pooled from four randomized, single-dose crossover trials enrolling healthy adult (18-55 years old) participants (three trials) and nondependent recreational users of prescription opioids (one trial) with a body weight of ≥59 kg...
2015: Drug Design, Development and Therapy
Thomas Barrett, Kenneth Kostenbader, Srinivas Nalamachu, Michael Giuliani, Jim L Young
OBJECTIVES: To characterize the safety of immediate-release (IR)/extended-release (ER) oxycodone (OC)/acetaminophen (APAP). METHODS: Data were assessed from 9 phase 1 trials in healthy volunteers and recreational users of prescription opioids (N = 405), including 5 single-dose and 3 multidose open-label pharmacokinetic studies of IR/ER OC/APAP and active comparators; and 1 randomized, controlled, single-dose human abuse potential (HAP) study comparing IR/ER OC/APAP, IR OC/APAP, and placebo in recreational users of opioids; and 2 phase 3 trials (N = 701) including a 48-hour placebo-controlled safety and efficacy study in patients with moderate to severe postbunionectomy pain with a 14-day open-label safety extension and a long-term (≤ 35 days) open-label safety study in patients with chronic osteoarthritis pain or chronic low back pain...
September 2016: Pain Practice: the Official Journal of World Institute of Pain
Nathaniel Katz, Ernest A Kopecky, Melinda OʼConnor, Robert H Brown, Alison B Fleming
Opioid analgesics are commonly used for the treatment of chronic low back pain (CLBP); however, abuse potential is a major concern. This study used a randomized, double-blind, placebo-controlled, enriched-enrollment randomized-withdrawal study design to evaluate the safety, tolerability, and analgesic efficacy of an abuse-deterrent formulation of extended-release oxycodone, Xtampza ER, in opioid-naive and opioid-experienced adults with moderate-to-severe CLBP. Patients entered an open-label titration phase (N = 740); those who were successfully titrated on Xtampza ER (≥40 to ≤160 mg oxycodone hydrochloride equivalent per day) were randomized to active drug (N = 193) or placebo (N = 196) for 12 weeks...
December 2015: Pain
Terri Morton, Ryan Franke, Krishna Devarakonda
OBJECTIVE: To examine whether biphasic immediate-release (IR)/extended-release (ER) oxycodone (OC)/acetaminophen (APAP) 7.5/325-mg tablets have clinically relevant variability in population pharmacokinetics (PK). DESIGN: Post hoc analysis of 2 phase 1 randomized, open-label, multiple-dose crossover studies. SETTING: Single contract research organization clinic. SUBJECTS: Men and women aged 18 to 55 years with a body mass index of 19 to 30 kg/m(2) and body weight ≥ 59 kg...
July 2016: Pain Practice: the Official Journal of World Institute of Pain
Tiffani D Eisenhauer, Mike Matchett, Ralph Heasley, Terri Morton, Krishna Devarakonda, Michael Giuliani, Jim L Young, Thomas Barrett
CONTEXT: Abuse potential of extended-release (ER) opioid tablets increases if tampering causes rapid opioid release. OBJECTIVE: To evaluate the susceptibility to tampering of biphasic immediate-release (IR)/ER oxycodone (OC)/acetaminophen (APAP) tablets compared with IR OC/APAP tablets. MATERIALS AND METHODS: IR/ER OC/APAP and IR OC/APAP tablets were tested at room temperature and after heating, freezing and microwaving. Resistance to crushing was tested using manual and powered tools (e...
July 6, 2015: Drug Development and Industrial Pharmacy
Lisa E MacDonald, Jennifer E Onsrud, Rita Mullins-Hodgin
Oxymorphone, a semisynthetic μ-opioid receptor agonist, is the major active metabolite of oxycodone. It is a highly potent narcotic analgesic due to its high lipid solubility, which allows it to readily cross the blood-brain barrier and enter the central nervous system. It is available as both an immediate-release and extended-release (ER) formulation. Oxymorphone can be abused by injection or inhalation of crushed tablets; thus, in 2011, the manufacturer of ER oxymorphone reformulated the drug with crush-resistant technology to deter its misuse and abuse...
July 2015: Pharmacotherapy
Jeff Gudin, Naama Levy-Cooperman, Ernest A Kopecky, Alison B Fleming
OBJECTIVE: Oxycodone DETERx® is an extended-release (ER), microsphere-in-capsule abuse-deterrent-formulation designed to retain its extended-release properties following tampering or misuse (e.g., chewing, crushing). This study assessed the safety and pharmacokinetics of orally administered intact and crushed Oxycodone DETERx® capsules compared with intact and crushed reformulated OxyContin® tablets and crushed immediate-release oxycodone tablets (IR oxycodone). METHODS: This was a randomized, open-label, active-controlled, cross-over study...
November 2015: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
Joseph V Pergolizzi, Robert Taylor, Robert B Raffa
Acute pain, prevalent as part of postoperative and traumatic pain, is often sub-optimally or inadequately treated. Fixed-dose combination analgesic products that combine a reduced amount of opioid with a nonopioid analgesic such as acetaminophen (paracetamol) in a single tablet offer potential pharmacodynamic and/or pharmacokinetic benefits, and may also result in an opioid-sparing effect. A new analgesic product (XARTEMIS™ XR, Mallinckrodt Brand Pharmaceuticals, Dublin, Ireland) combines oxycodone (7.5 mg) with acetaminophen (325 mg) in an immediate-release/extended-release (ER) formulation that is indicated for the treatment of acute pain...
June 2015: Advances in Therapy
Gary Eichenbaum, Karin Göhler, Mila Etropolski, Ilona Steigerwald, Joseph Pergolizzi, Myoung Kim, Gary Vorsanger
OBJECTIVES: Opioid-induced androgen deficiency (OPIAD) affects patients treated with opioid analgesics. The norepinephrine reuptake inhibitor (NRI) and µ-opioid receptor (MOR) agonist activities of tapentadol may result in tapentadol having less effect on serum androgen concentrations than analgesics acting through the MOR alone, such as morphine and oxycodone. The objectives of this publication are to 1) evaluate the effects of tapentadol (NUCYNTA and NUCYNTA extended release [ER]) on sex hormone concentrations in healthy male volunteers (vs placebo and morphine) and patients with osteoarthritis (vs placebo and oxycodone), and 2) present a mechanistic hypothesis explaining how the combined MOR agonist and NRI activities of tapentadol may result in less impact on androgen concentrations...
May 2015: Journal of Opioid Management
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