Oxymorphone and oxymorphone extended release: A pharmacotherapeutic review

2018 ◽  
Vol 4 (3) ◽  
pp. 131 ◽  
Author(s):  
Paul Alexander Sloan, MD ◽  
Robert L. Barkin, PharmD, MBA
Keyword(s):  
Chronic Pain ◽  
Extended Release ◽  
Analgesic Efficacy ◽  
Opioid Analgesics ◽  
Immediate Release ◽  
The United States ◽  
Efficacy And Safety ◽  
Open Label ◽  
Opioid Agonist ◽  
Noncancer Pain

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.

A multicenter, 12-month, open-label, single-arm safety study of oxycodone-hydrochloride/naltrexone-hydrochloride extended-release capsules (ALO-02) in patients with moderate-to-severe chronic noncancer pain

2014 ◽  
Vol 10 (6) ◽  
pp. 423 ◽  
Author(s):  
Samir Arora, MD ◽  
Beatrice Setnik, PhD ◽  
Michael Drass, MD ◽  
John D. Hudson, MD ◽  
Ray Clemmer, MS ◽  
...  
Keyword(s):  
Extended Release ◽  
Short Form ◽  
Analgesic Efficacy ◽  
Opiate Withdrawal ◽  
Open Label ◽  
Chronic Noncancer Pain ◽  
Naltrexone Hydrochloride ◽  
Severity Scores ◽  
Oxycodone Hydrochloride ◽  
Noncancer Pain

Objective: To evaluate the long-term safety of oxycodone-hydrochloride and sequestered naltrexone-hydrochloride (ALO-02) administered for up to 12 months.Design: Open-label, single-arm safety study.Setting: Thirty-two US research centers (ClinicalTrials.gov identifier NCT01428583). Patients: Three hundred ninety-five adults (opioid experienced and opioid naïve) with moderate-to-severe chronic noncancer pain (CNCP). Interventions: Open-label, oral ALO-02 capsules, daily dose ranging from 20 to 160 mg oxycodone for up to 12 months.Main outcome measures: Number and type of adverse events (AEs) and drug-related AEs, including assessments of withdrawal (Clinical Opiate Withdrawal Scale; COWS), pharmacokinetics, efficacy, and aberrant behaviors (Current Opioid Misuse Measure).Results: A total of 193 (48.9 percent) patients received ALO-02 for ≥181 days and 105 (26.6 percent) patients for ≥361 days. The most common treatment-emergent AEs were nausea (25.3 percent), constipation (21.3 percent), vomiting (13.9 percent), and headache (11.6 percent). The most common drug-related AEs were constipation (18.0 percent), nausea (14.9 percent), somnolence (8.4 percent), fatigue (6.8 percent), dizziness (5.6 percent), and vomiting (5.1 percent). A majority of patients (86.6 percent) had a maximum COWS total score below the level for mild withdrawal symptoms at every visit throughout the study. Pain severity scores as measured by the short Form of the Brief Pain Inventory (BPI-SF) decreased over time.Conclusions: Repeat dosing of ALO-02 for up to 12 months is safe and well tolerated in a CNCP population of both opioid-experienced and opioid-naïve patients. ALO-02 demonstrated a safety profile consistent with extended-release opioids and the expected analgesic efficacy. The addition of sequestered naltrexone had no significant clinical effect on patients when taken as directed.

scholarly journals Abuse and Diversion of Immediate Release Opioid Analgesics as Compared to Extended Release Formulations in the United States

PLoS ONE ◽  
2016 ◽  
Vol 11 (12) ◽  
pp. e0167499 ◽  
Author(s):  
Janetta L. Iwanicki ◽  
S. Geoff Severtson ◽  
Heather McDaniel ◽  
Andrew Rosenblum ◽  
Chunki Fong ◽  
...  
Keyword(s):  
United States ◽  
Extended Release ◽  
Opioid Analgesics ◽  
Immediate Release ◽  
The United States ◽  
Extended Release Formulations

Limited Access to On-Label Formulations of Buprenorphine for Chronic Pain as Compared with Conventional Opioids

Pain Medicine ◽  
2019 ◽  
Vol 21 (5) ◽  
pp. 1005-1009
Author(s):  
Michael A Fishman ◽  
Ashley Scherer ◽  
Jacob Topfer ◽  
Philip S H Kim
Keyword(s):  
United States ◽  
Chronic Pain ◽  
Analgesic Efficacy ◽  
Immediate Release ◽  
The United States ◽  
Prescription Opioid ◽  
Web Searches ◽  
Online Tool ◽  
Unrestricted Access ◽  
Long Acting

Abstract Importance Buprenorphine is a Schedule III analgesic that is recommended as the firstline long-acting opioid for the treatment of chronic pain due to its ceiling effect on respiratory depression, adverse effect profile, and analgesic efficacy. However, prescription drug coverage policies commonly require that patients try and fail multiple Schedule II conventional opioids before approval of on-label use of buprenorphine for chronic pain. Design A retrospective review was performed looking at coverage of buprenorphine in the forms of Butrans and Belbuca. Patient denial letters, web searches of insurance and pharmacy benefit managers (PBMs), and an online tool (formularylookup.com) were used to assess the coverage and availability of buprenorphine for chronic pain. Results Unrestricted access to Butrans was reported for 42% of commercial lives and 11% of Medicare lives in all locations. Unrestricted access to Belbuca was reported for 53% of commercial lives and 23% of Medicare lives in all locations. Oxycodone immediate-release has unrestricted access for 84% of commercial plans and 97% of Medicare plans. Morphine extended-release has unrestricted access for 62% of commercial lives and 65% of Medicare lives. Conclusions and Relevance There are >17,000 prescription opioid–involved deaths each year in the United States. By substituting buprenorphine as the firstline treatment for chronic and even acute pain, there may be fewer prescribed conventional opioids in the United States. Schedule III buprenorphine formulations for chronic pain should be given unrestricted access for appropriate patients before considering a Schedule II opioid as a public health priority.

Review on the Clinical Pharmacology of Hydroxychloroquine Sulfate for the Treatment of COVID-19

2020 ◽  
Vol 21 (6) ◽  
pp. 427-435 ◽  
Author(s):  
Cheng Cui ◽  
Siqi Tu ◽  
Valerie Sia Jie En ◽  
Xiaobei Li ◽  
Xueting Yao ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Clinical Efficacy ◽  
Relevant Literature ◽  
The United States ◽  
Efficacy And Safety ◽  
Open Label ◽  
Infected People ◽  
Treatment Regimens ◽  
Therapeutic Drugs

Background: As the number of severe acute respiratory syndrome coronavirus 2 (SARS-COV-2) infected people is greatly increasing worldwide, the international medical situation becomes very serious. Potential therapeutic drugs, vaccine and stem cell replacement methods are emerging, so it is urgent to find specific therapeutic drugs and the best treatment regimens. After the publications on hydroxychloroquine (HCQ) with anti- SARS-COV-2 activity in vitro, a small, non-randomized, open-label clinical trial showed that HCQ treatment was significantly associated with reduced viral load in patients with coronavirus disease-19 (COVID-19). Meanwhile, a large prophylaxis study of HCQ sulfate for COVID-19 has been initiated in the United States. HCQ offered a promising efficacy in the treatment of COVID-19, but the optimal administration is still being explored. Methods: We used the keyword "hydroxychloroquine" to conduct a literature search in PubMed to collect relevant literature on the mechanism of action of HCQ, its clinical efficacy and safety, pharmacokinetic characteristics, precautions for clinical use and drug interactions to extract and organize information. Results: This paper reviews the mechanism, clinical efficacy and safety, pharmacokinetic characteristics, exposureresponse relationship and precautions and drug interactions of HCQ, and summarizes dosage recommendations for HCQ sulfate. Conclusion: It has been proved that HCQ, which has an established safety profile, is effective against SARS-CoV-2 with sufficient pre-clinical rationale and evidence. Data from high-quality clinical trials are urgently needed worldwide.

scholarly journals ANalgesic Efficacy and safety of MOrphiNe versus methoxyflurane in patients with acute myocardial infarction: the rationale and design of the ANEMON-SIRIO 3 study: a multicentre, open-label, phase II, randomised clinical trial

BMJ Open ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. e043330
Author(s):  
Aldona Kubica ◽  
Agata Kosobucka ◽  
Piotr Niezgoda ◽  
Piotr Adamski ◽  
Katarzyna Buszko ◽  
...  
Keyword(s):  
Myocardial Infarction ◽  
Analgesic Efficacy ◽  
Randomised Clinical Trial ◽  
Ethical Standards ◽  
Loading Dose ◽  
Efficacy And Safety ◽  
Open Label ◽  
Analgesic Treatment ◽  
Open Label Phase ◽  
St Elevation

IntroductionThe unfavourable influence of morphine on the pharmacokinetics of ticagrelor resulting in weaker and retarded antiplatelet effect in patients with acute coronary syndrome (ACS) has been previously shown. Replacing morphine with methoxyflurane, a potent, non-opioid analgesic agent, that does not weaken or delay the effect of antiplatelet agents may improve the clinical efficacy of treatment of patients with ACS.MethodsThe ANEMON-SIRIO 3 study was designed as a multicentre, open-label, phase II, randomised clinical trial aimed to test the analgesic efficacy and safety of methoxyflurane in patients with ACS. The study population will comprise patients with ST-elevation myocardial infarction or non-ST-elevation ACS admitted to the study centres with typical chest pain requiring analgesic treatment. Before percutaneous coronary intervention (PCI) for the patients with index ACS will be randomly assigned in 1:1 ratio to receive methoxyflurane administered by inhalation, or to obtain morphine administered intravenously. Analgesic treatment will be followed by 300 mg loading dose of aspirin and 180 mg loading dose of ticagrelor. Patients will be assessed with regard to pain intensity according to the Numeric Pain Rating Scale at baseline, 3 min after study drug administration and immediately after PCI. Moreover, patients will be actively monitored with regard to the occurrence of side effects of evaluated therapies, as well as adverse events that may be related to insufficient platelet inhibition (no-reflow phenomenon assessed immediately after PCI, administration of GPIIb/IIIa inhibitors during PCI, acute stent thrombosis).Ethics and disseminationThe study will be conducted in six Polish clinical centres from the beginning of in accordance with the ethical standards of the institutional research committee and with the 1964 Helsinki declaration and its later amendments or comparable ethical standards.Trial registration detailsClinicalTrials.gov, NCT04476173.

An Open-Label, Analgesic Efficacy and Safety of Pituitary Radiosurgery for Patients With Opioid-Refractory Pain: Study Protocol for a Randomized Controlled Trial

Neurosurgery ◽  
2017 ◽  
Vol 83 (1) ◽  
pp. 146-153 ◽  
Author(s):  
Pierre-Yves Borius ◽  
Stéphanie Ranque Garnier ◽  
Karine Baumstarck ◽  
Frédéric Castinetti ◽  
Anne Donnet ◽  
...  
Keyword(s):  
Quality Of Life ◽  
Pain Relief ◽  
Cancer Pain ◽  
Controlled Trial ◽  
Analgesic Efficacy ◽  
Standards Of Care ◽  
Control Group ◽  
Efficacy And Safety ◽  
Open Label

Abstract BACKGROUND Hypophysectomy performed by craniotomy or percutaneous techniques leads to complete pain relief in more than 70% to 80% of cases for opioid refractory cancer pain. Radiosurgery could be an interesting alternative approach to reduce complications. OBJECTIVE To assess the analgesic efficacy compared with standard of care is the primary goal. The secondary objectives are to assess ophthalmic and endocrine tolerance, drug consumption, quality of life, and mechanisms of analgesic action. METHODS The trial is multicenter, randomized, prospective, and open-label with 2 parallel groups. This concerns patients in palliative care suffering from nociceptive or mixed cancer pain, refractory to standard opioid therapy. Participants will be randomly assigned to the control group receiving standards of care for pain according to recommendations, or to the experimental group receiving a pituitary GammaKnife (Elekta, Stockholm, Sweden) radiosurgery (160 Gy delivered in pituitary gland) associated with standards of care. Evaluation assessments will be taken at baseline, day0, day4, day7, day14, day28, day45, month3, and month6. EXPECTED OUTCOMES We could expect pain improvement in 70% to 90% of cases at day4. In addition we will assess the safety of pituitary radiosurgery in a vulnerable population. The secondary endpoints could show decay of opioid consumption, good patient satisfaction, and improvement of the quality of life. DISCUSSION The design of this study is potentially the most appropriate to demonstrate the efficacy and safety of radiosurgery for this new indication. New recommendations could be obtained in order to improve pain relief and quality of life.

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