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Supportive Care in Cancer : Official... Feb 2006Oxymorphone (oxymorphone hydrochloride) (14-hydroxy-dihydromorphinone), a semisynthetic mu-opioid agonist, was first approved by the US Food and Drug Administration in... (Review)
Review
Oxymorphone (oxymorphone hydrochloride) (14-hydroxy-dihydromorphinone), a semisynthetic mu-opioid agonist, was first approved by the US Food and Drug Administration in 1959. Oxymorphone is considered a more potent opioid than its parent compound, morphine. Recently, an immediate-release and long-acting oral formulation of this drug was developed that makes oxymorphone a new option in treating moderate to severe pain. This article reviews the pharmacodynamics, pharmacology, and clinical efficacy for this new option in treating moderate to severe pain.
Topics: Analgesics, Opioid; Drug Administration Schedule; Drug Interactions; Humans; Neoplasms; Oxymorphone; Pain
PubMed: 16317569
DOI: 10.1007/s00520-005-0917-1 -
Anesthesiology Clinics Jun 2017Pain remains a tremendous burden on patients and for the health care system, with uncontrolled pain being the leading cause of disability in this country. There are a... (Review)
Review
Pain remains a tremendous burden on patients and for the health care system, with uncontrolled pain being the leading cause of disability in this country. There are a variety of medications that can be used in the treatment of pain, including ketorolac, oxymorphone, tapentadol, and tramadol. Depending on the clinical situation, these drugs can be used as monotherapy or in conjunction with other types of medications in a multimodal approach. A strong appreciation of pharmacologic properties of these agents and potential side effects is warranted for clinicians.
Topics: Analgesics, Opioid; Anti-Inflammatory Agents, Non-Steroidal; Humans; Ketorolac; Oxymorphone; Pain; Pain Measurement; Phenols; Tapentadol; Tramadol
PubMed: 28526155
DOI: 10.1016/j.anclin.2017.01.001 -
Journal of Opioid Management 2013Oxymorphone (14-hydroxydihydromorphinone), a pyridine ring unsubstituted pyridomorphinan, a semisynthetic opioid analgesic derived from thebaine, first developed in the... (Review)
Review
Oxymorphone (14-hydroxydihydromorphinone), a pyridine ring unsubstituted pyridomorphinan, a semisynthetic opioid analgesic derived from thebaine, first developed in the year 1914 and has been available as oxymorphone hydrochloride parenteral forms in the United States since 1959, when the US Food and Drug Administration approved it. Over the years, it has been used for the alleviation of moderate-to-severe pain. Pharmacological considerations, new and traditional formulations, clinical indications, and recent study populations are examined in this review. Specific considerations for oxymorphone interactions are focused on as well as specific side effects and end organ considerations. Although discovered many decades ago and used as parenteral formulation, the newer oral preparations of oxymorphone (immediate release and extended release) that were approved in 2006 can provide additional options for customizing therapy to accommodate various patient needs. This newer oral formulation could make this powerful agent an important drug in the armamentarium of the healthcare provider caring for patients with pain.
Topics: Administration, Oral; Analgesics, Opioid; Chemistry, Pharmaceutical; Humans; Molecular Structure; Oxymorphone; Pain Management; Structure-Activity Relationship; Treatment Outcome
PubMed: 24481932
DOI: 10.5055/jom.2013.0186 -
Journal of Opioid Management 2008The treatment of chronic pain remains an enormous challenge in the United States. Opioid analgesics are an important component of pharmacotherapy for chronic pain and... (Review)
Review
The treatment of chronic pain remains an enormous challenge in the United States. Opioid analgesics are an important component of pharmacotherapy for chronic pain and have proven efficacy in the management of cancer and noncancer chronic pain. The newest addition to oral opioid pharmacotherapy is oral oxymorphone, a semisynthetic opioid agonist that is now available in oral immediate-release (IR) and extended-release (ER) formulations. This review discusses the pharmacology, pharmacokinetics, pharmacodynamics, pharmacotherapeutics, and clinical use of oral oxymorphone IR and ER formulations for the management of moderate to severe pain for different types of patients in a variety of settings. Two published studies evaluated the efficacy and safety of oxymorphone IR in patients with moderate to severe postoperative pain and demonstrated that it provides rapid and effective analgesia and is generally well tolerated. Six published randomized controlled trials and three published open-label studies evaluated the efficacy and safety of oxymorphone ER for chronic cancer or noncancer pain. These trials found analgesic efficacy and tolerability comparable to that provided by morphine controlled release (CR) or oxycodone CR; treatment effects with oxymorphone ER were durable for treatment periods of 12 weeks at the same dose or up to 1 year with little dose escalation. Titrated doses of oxymorphone ER were effective and generally well tolerated in both opioid-experienced and opioid-naïve patients. Aspects of oxymorphone metabolism and limited protein binding may simplify treatment in certain populations.
Topics: Analgesics, Opioid; Chronic Disease; Clinical Trials as Topic; Delayed-Action Preparations; Drug Interactions; Follow-Up Studies; Food-Drug Interactions; Humans; Oxymorphone; Pain
PubMed: 18717508
DOI: 10.5055/jom.2008.0018 -
The Annals of Pharmacotherapy Jul 2007To describe the pharmacology, safety and efficacy, and rationale for use of oral oxymorphone for the management of acute and chronic moderate-to-severe pain. (Review)
Review
OBJECTIVE
To describe the pharmacology, safety and efficacy, and rationale for use of oral oxymorphone for the management of acute and chronic moderate-to-severe pain.
DATA SOURCES
A PubMed/MEDLINE search (1966-March 2007) was conducted using the following terms: oral oxymorphone, oxymorphone, EN 3202, EN 3203, Opana, and Opana ER. Manufacturer-provided data (package inserts) and abstracts presented at the American Pain Society meetings (2003-2006) were also reviewed.
STUDY SELECTION AND DATA EXTRACTION
Human studies evaluating the safety and efficacy of oral oxymorphone in pain management were considered; animal and non-English-language data were excluded.
DATA SYNTHESIS
Oral oxymorphone is a semisynthetic opioid agonist that is specific for the mu-opioid receptor and approved to treat both acute and chronic pain. Unlike other opioids, such as oxycodone, oxymorphone does not bind to the kappa-opioid receptor. Due to extensive liver metabolism, oral oxymorphone is contraindicated in patients with moderate-to-severe hepatic impairment; however, no clinically significant CYP3A4, 2C9, or 2D6 mediated drug-drug interactions have been noted. Elderly patients may experience a 40% increase in plasma concentrations, while renally impaired patients may have a 57-65% increase in bioavailability. Food can increase the rate of absorption by as much as 50%, necessitating dosing either 1 hour before or 2 hours after a meal. Oxymorphone's primary adverse effects are similar to those of other opioids: nausea, vomiting, pruritus, pyrexia, and constipation.
CONCLUSIONS
Oxymorphone is an oral therapeutic option approved for the treatment of acute and chronic moderate-to-severe pain. Oxymorphone has a safety and efficacy profile similar to that of other commonly used pure opioids (morphine, oxycodone, hydromorphone). Like oxycodone and morphine, oxymorphone also has immediate-release and extended-release formulations. Since cost alone is not yet favorable for oxymorphone over oxycodone or morphine, further studies of comparative efficacy targeting potential advantages of oxymorphone over other opioids are necessary before considering it for addition to a formulary.
Topics: Administration, Oral; Delayed-Action Preparations; Disease Management; Humans; Oxymorphone; Pain; Pain Measurement
PubMed: 17595308
DOI: 10.1345/aph.1H451 -
Drugs of Today (Barcelona, Spain : 1998) Oct 2008The undertreatment of acute and chronic pain continues to be a significant health concern in the U.S. Opioids are recommended for the treatment of acute or chronic pain... (Review)
Review
The undertreatment of acute and chronic pain continues to be a significant health concern in the U.S. Opioids are recommended for the treatment of acute or chronic pain of moderate to severe intensity that is not responsive to other pharmacologic agents, such as nonsteroidal antiinflammatory drugs. A high level of interindividual responses to the analgesic effects and side effects of opioids necessitates the availability of multiple treatment options. Extended-release and immediate-release oral formulations of oxymorphone hydrochloride were recently approved by the U.S. Food and Drug Administration and may provide new options for patients who have not achieved adequate and well-tolerated analgesia with their current opioid. This review provides an overview of the basic pharmacology (including pharmacokinetic and pharmacodynamic profiles), clinical efficacy and tolerability of both oral oxymorphone formulations.
Topics: Analgesics, Opioid; Half-Life; Humans; Molecular Structure; Morphine; Oxymorphone; Pain; Randomized Controlled Trials as Topic; Receptors, Opioid, mu; Tablets
PubMed: 19137130
DOI: 10.1358/dot.2008.44.10.1279154 -
Drugs in R&D 2003Penwest Pharmaceuticals and Endo Pharmaceuticals are jointly developing an oral, controlled-release opioid analgesic oxymorphone [EN 3202] using Penwest's TIMERx... (Review)
Review
Penwest Pharmaceuticals and Endo Pharmaceuticals are jointly developing an oral, controlled-release opioid analgesic oxymorphone [EN 3202] using Penwest's TIMERx proprietary drug delivery technology. The product is being developed for twice-a-day dosing in patients with moderate to severe pain. TIMERx is a controlled-release technology based on an agglomerated hydrophilic matrix, which consists of the polysaccharides locust bean gum and xanthan gum. The technology provides a full spectrum of controlled-release profiles lasting >/=4 h. In February 2003, the US FDA has announced that it accepted the NDA for oxymorphone extended-release tablets, oxymorphone ER, for the treatment of moderate to severe pain in patients requiring continuous opioid therapy for an extended period of time. Late in 2002, the Oxymorphone formulation successfully completed a phase III clinical trial in patients with osteoarthritis pain. Another randomised, double-blind, placebo-controlled trial was completed in 127 patients with moderate to severe pain resulting from surgery in the knee. Results demonstrated that patients receiving EN 3202 treatment had significantly superior pain relief compared with placebo recipients. An immediate-release formulation of oxymorphone (EN 3203) has also been accepted by the US FDA.
Topics: Analgesics, Opioid; Clinical Trials, Phase III as Topic; Delayed-Action Preparations; Drugs, Investigational; Humans; Oxymorphone
PubMed: 12757410
DOI: 10.2165/00126839-200304030-00012 -
Expert Opinion on Drug Safety Sep 2009Pain among the elderly is pervasive, under-treated and can be properly managed by judiciously using analgesics in the armamentarium. For severe pain, opioids generally... (Review)
Review
BACKGROUND
Pain among the elderly is pervasive, under-treated and can be properly managed by judiciously using analgesics in the armamentarium. For severe pain, opioids generally provide the most effective pain relief, but concerns about safety and tolerability have limited, often unnecessarily, their utilization in the geriatric population.
OBJECTIVE
It is common for geriatric patients to be taking more than one medicine. Oxymorphone might be particularly well suited for use in geriatric patients, in that its metabolism is mainly through non-CYPP450 pathways, thereby posing less risk of interaction with the many drugs that are metabolized by the CYPP450 system. However, oxymorphone is not as familiar to clinicians as morphine or some other opioids. We review here the clinical studies on oxymorphone to outline the key considerations for use of oxymorphone in the geriatric population.
METHODS
Nine available clinical trials of oxymorphone alone or comparing oxymorphone with placebo or other active agents were analyzed with respect to the safety and tolerability findings. These studies included geriatric patients but were not designed to evaluate oxymorphone exclusively in this population.
RESULTS
Based on the results from nine published clinical studies, oxymorphone is an effective opioid analgesic with a safety profile at least comparable to other opioid drugs. At low starting doses and individual titration, oxymorphone should be considered for appropriate geriatric patients, particularly in whom there is concern about interaction with drugs that are metabolized by CYPP450 enzymes.
Topics: Aged; Aged, 80 and over; Arthralgia; Biotransformation; Clinical Trials as Topic; Constipation; Drug Interactions; Glucuronosyltransferase; Humans; Liver; Narcotics; Nausea; Neoplasms; Opioid-Related Disorders; Oxymorphone; Pain; Pain, Postoperative; Polypharmacy; Receptors, Opioid, mu; Sleep Stages; Vomiting
PubMed: 19614559
DOI: 10.1517/14740330903153854 -
Journal of Pain and Symptom Management Feb 2010Opioids are recommended for control of moderate-to-severe, chronic, malignant, and nonmalignant pain. A controlled-release formulation of the opioid oxymorphone has... (Meta-Analysis)
Meta-Analysis Review
Opioids are recommended for control of moderate-to-severe, chronic, malignant, and nonmalignant pain. A controlled-release formulation of the opioid oxymorphone has recently been launched. The aim of this review was to assess the effectiveness of oxymorphone as an analgesic in chronic pain. A systematic search for published studies of oral oxymorphone in the management of chronic pain was conducted. The studies were evaluated for their internal validity according to standard criteria. They were also evaluated for their external validity and research ethic aspects. A meta-analysis was performed to examine the effect of oxymorphone compared with placebo. Nine studies were evaluated; three were excluded because of low quality. Six controlled studies (duration 2-12 weeks) included a total of 1489 subjects suffering from chronic low back pain, chronic pain from osteoarthritis, and chronic cancer pain. Three of the studies were of high quality and three of medium quality. External validity was assessed to be high, medium, and low (in one, three, and two studies, respectively). The meta-analysis suggests that daily doses of 40-100mg are superior to placebo; however, the estimate (reduction of pain intensity compared with placebo) of the treatment effect is imprecise (95% confidence interval -17.08, -8.69). Limited evidence suggests that oxymorphone is effective for pain control in patients with cancer. No significant differences between oxymorphone and oxycodone at equipotent doses were found. In conclusion, oxymorphone is superior to placebo. There is no evidence that the efficacy of oxymorphone differs from other opioids.
Topics: Analgesics, Opioid; Chronic Disease; Humans; Low Back Pain; Neoplasms; Osteoarthritis; Oxymorphone; Pain; Randomized Controlled Trials as Topic
PubMed: 20152592
DOI: 10.1016/j.jpainsymman.2009.07.010 -
Journal of Medical Toxicology :... Jun 2013
Review
Topics: Adult; Analgesics, Opioid; Diagnosis, Differential; Drug Overdose; Emergency Medical Services; Hearing Loss, Sensorineural; Humans; Insufflation; Internet; Male; Massachusetts; Oxymorphone; Receptors, Opioid, mu; Treatment Outcome
PubMed: 23435934
DOI: 10.1007/s13181-013-0293-z