Analgesic Efficacy and Safety of Oxycodone in Combination With Naloxone as Prolonged Release Tablets in Patients With Moderate to Severe Chronic Pain

Vondráčková, Dana; Leyendecker, Petra; Meißner, Winfried; Hopp, Michael; Szombati, István; Hermanns, Kai; Ruckes, Christian; Weber, Susanne; Grothe, Benedikt; Fleischer, Wolfgang; Reimer, Karen

doi:10.1016/j.jpain.2008.06.014

Cited by 196 publications

(216 citation statements)

References 25 publications

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“…The appearance of pain events was comparable for PR OXN as against PR OX, confirming that the addition of N to OX in a combination tablet did not negatively affect analgesic efficacy of the opioid. In constipated patients with high bowel function index, complete spontaneous bowel movement significantly increased with PR OXN and was associated with lower use of laxative in comparison with PR OX group [14]. In a randomized, double-blind, double-dummy 12-week trial of 322 patients with chronic non-cancer pain, PR OXN and PR OX were compared, after a run-in phase with doses of PR OX ranging 20 --50 mg/day.…”

Section: Clinical Efficacymentioning

confidence: 99%

Combined oral prolonged-release oxycodone and naloxone in chronic pain management

Mercadante

Giarratano

2012

Expert Opinion on Investigational Drugs

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Section: Clinical Efficacymentioning

confidence: 99%

Combined oral prolonged-release oxycodone and naloxone in chronic pain management

Mercadante

Giarratano

2012

Expert Opinion on Investigational Drugs

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“…In patients with chronic pain, oral naloxone improved symptoms of laxation (24), but because of its very narrow therapeutic index, doses that reverse gut symptoms can often cause reversal of analgesia (25). However, there has been a resurgence of interest in naloxone in a prolonged-release preparation, which shows evidence of analgesic efficacy and safety when used in combination with oxycodone (prolonged release) for moderate-to-severe chronic pain (26) and improved bowel function when compared with oral oxycodone (prolonged release) alone (27). This effiacy continues for up to 52 weeks in patients with non-cancer chronic pain (28).…”

Section: Naloxonementioning

confidence: 99%

Opioid Induced Constipation

Aurilio¹,

Pace²,

Pota³

et al. 2012

Constipation - Causes, Diagnosis and Treatment

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“…24,25 While there is some evidence that prototypical μ opioid receptor antagonists, such as naltrexone and naloxone, attenuate POI and chronic opioid-induced bowel dysfunction (OBD), [26][27][28] their clinical value in these GI disorders is limited given that these drugs cross the blood brain barrier readily, and thus can attenuate opioid-induced analgesia and provoke an opioid behavioral withdrawal syndrome. 28,29 However, it is noteworthy that Targin ® , a combination of oxycodone and naloxone, is effi cacious in the treatment of moderate to severe pain without signifi cant constipation; 30,31 its value in POI therapy remains to be determined.…”

Section: Mechanism Of Action Of Alvimopanmentioning

confidence: 99%

Safety and efficacy update: Alvimopan in postoperative ileus

Beattie

2009

Clinical Medicine. Therapeutics

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Postoperative ileus (POI) in patients undergoing abdominal surgery is associated with signifi cant morbidity. In 2008, alvimopan (Entereg ® ) was approved by the Food and Drug Administration (FDA), and is the only available POI therapy in the United States for patients undergoing bowel resection. Data from preclinical studies demonstrate that alvimopan and its primary metabolite, ADL 08-0011, behave as potent μ opioid receptor antagonists. In animals, alvimopan and ADL 08-0011 attenuate opioid agonist-induced reductions in gastrointestinal (GI) transit. Higher doses of alvimopan are required to inhibit opioid-induced analgesia as a result of its inability to penetrate the central nervous system (CNS). ADL 08-0011 is also peripherally selective, although to a lesser degree than alvimopan. In multiple species, including humans, alvimopan has low oral bioavailability, while ADL 08-0011, following its generation by human gut microfl ora, is more readily absorbed and achieves higher exposures. Three Phase 2 and fi ve Phase 3 clinical trials have been conducted to investigate the effi cacy and tolerability of alvimopan in patients undergoing bowel resection. An additional Phase 3 study was conducted in hysterectomy patients. In the majority of the studies, statistically signifi cant, and clinically meaningful, acceleration of GI recovery has been demonstrated. Consistent with animal data, alvimopan has no effect on opioid agonist-induced analgesia in healthy human subjects and POI patients. Clinical experience to date in POI patients indicates that alvimopan is well tolerated when used according to its approved dosing regimen (12 mg b.i.d. for up to 7 days). In this article, the preclinical and clinical properties of alvimopan are reviewed.

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Analgesic Efficacy and Safety of Oxycodone in Combination With Naloxone as Prolonged Release Tablets in Patients With Moderate to Severe Chronic Pain

Cited by 196 publications

References 25 publications

Combined oral prolonged-release oxycodone and naloxone in chronic pain management

Combined oral prolonged-release oxycodone and naloxone in chronic pain management

Opioid Induced Constipation

Safety and efficacy update: Alvimopan in postoperative ileus

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