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PubMed1977

Comparisons of the analgesic effects of oral and intramuscular oxymorphone and of intramuscular oxymorphone and morphine in patients with cancer.

The relative analgesic potency of oral and intramuscular oxymorphone was evaluated in a double-blind crossover comparison of graded single doses in patients with chronic pain due to cancer. When both duration and intensity of analgesia are considered (total effect), oral oxymorphone was 1/6 as potent as the intramuscular form. In terms of peak effect, however, oral oxymorphone was only 1/14 as potent. These values are almost identical to those obtained in a previous study comparing oral with intramuscular morphine. The analgesic effect of oral oxymorphone rose to a peak later and had a longer duration than the effect of intramuscular oxymorphone. Intramuscular oxymorphone and morphine were also compared in a similar patient group. Intramuscular oxymorphone proved to be 8.7 times as potent as morphine in terms of total analgesic effect and 13 times as potent in terms of peak effect. In roughly equinalgesic doses, the occurrence of side effects was qualitatively and quantitatively similar for oral and intramuscular oxymorphone and for intramuscular oxymorphone and morphine.

Administration, Oral↗
PubMed1998

End tidal halothane concentration and postoperative analgesia requirements in dogs: a comparison between intravenous oxymorphone and epidural bupivacaine alone and in combination with oxymorphone.

The purpose of this study was to compare the effects of epidural bupivacaine (BUP) and oxymorphone/bupivacaine (O/B) and intravenous (i.v.) oxymorphone (IVO) on halothane requirements during hind end surgery and postoperative analgesia in 24 dogs. Dogs were randomly assigned to treatment groups: O/B--oxymorphone (0.1 mg/kg) in 0.75% bupivacaine (1 mg/kg for a total volume of 0.2 ml/kg); BUP--0.5% bupivacaine (1 mg/kg for a total volume of 0.2 ml/kg) with i.v. oxymorphone (0.05 mg/kg) postoperatively; and IVO--oxymorphone (0.05 mg/kg) pre- and postoperatively. Heart rate (HR), respiratory rate, arterial blood pressure, end-tidal carbon dioxide and halothane, and arterial blood gases were recorded prior to treatment and every 15 minutes thereafter. Once surgery had begun, end-tidal halothane concentrations were decreased as low as possible while still maintaining a stable anesthetic plane. Data were analyzed using ANOVA with P < 0.05 considered significant. End-tidal halothane requirements did not differ significantly among treatments. Respiratory depression was increased and HR was decreased in the O/B and IVO groups. Postoperative analgesic requirements were significantly less in dogs receiving O/B.

Adjuvants, Anesthesia↗
PubMed1999

Cardiovascular effects of epidurally administered oxymorphone and an oxymorphone-bupivacaine combination in halothane-anesthetized dogs.

OBJECTIVE: To evaluate cardiovascular effects of epidurally administered oxymorphone (OXY) and an OXY-bupivacaine combination (O/B) in halothane-anesthetized dogs. ANIMALS: 6 dogs. PROCEDURE: In a randomized crossover design study, dogs were anesthetized with halothane and given OXY, O/B, and saline solution (SAL). Eucapnia and end-tidal halothane concentration of 1.2% were established. Heart rate (HR), systemic and pulmonary arterial pressures, central venous pressure (CVP), and cardiac output were measured at baseline and 5, 15, 30, 45, 60, and 75 minutes after treatment. At 90 minutes, glycopyrrolate was administered IV, and measurements were repeated at 95 minutes. Cardiac index (CI), stroke volume, stroke index, systemic vascular resistance (SVR), and left ventricular work were calculated. End-tidal halothane concentration was decreased to 0.8% from 17 to 45 minutes and to 0.5% from 47 to 95 minutes for OXY and O/B, whereas for SAL, it was maintained at 1.5 and 1.2%, respectively. Samples were obtained at 0, 2, 5, 15, 30, 45, 60, and 95 minutes for measurement of serum opiate concentration and comparison with values after IM administration of OXY. RESULTS: HR decreased, but CVP and SVR increased in response to OXY and O/B. These changes were reversed after IV administration of glycopyrrolate, resulting in significant increase in CI, compared with that in response to SAL. Serum opiate concentration increased markedly and peaked within 15 minutes after OXY and O/B administration but did not differ from values after IM administration. CONCLUSIONS: Epidural administration of OXY results in rapid systemic uptake and decreased HR. Glycopyrrolate administration improves HR, resulting in improved CI at equipotent halothane concentrations.

Analgesia, Epidural↗
PubMed2006

A 2-week, multicenter, randomized, double-blind, placebo-controlled, dose-ranging, phase III trial comparing the efficacy of oxymorphone extended release and placebo in adults with pain associated with osteoarthritis of the hip or knee.

BACKGROUND: Oxymorphone extended release (ER) is a tablet formulation of the mu-opioid agonist oxymorphone designed to achieve a low peak-to-trough fluctuation in plasma concentrations over a 12-hour dosing period. OBJECTIVE: This study compared the analgesic efficacy, dose response, and tolerability of 3 doses of oxymorphone ER given every 12 hours with those of placebo in patients with pain related to osteoarthritis (OA) of the hip or knee. METHODS: This was a 2-week, multicenter, randomized, double-blind, placebo-controlled, dose-ranging, Phase III trial. Patients with OA of the hip or knee who were receiving an opioid medication for chronic, moderate to severe pain or who were judged by the investigator to have received suboptimal analgesia with nonopioid analgesics entered a 2- to 7-day washout of analgesic medication. When pain in the index joint was >40 mm on a 100-mm visual analog scale (VAS), patients were randomized to receive 1 of 4 regimens: oxymorphone ER 10 mg q12h during weeks 1 and 2; oxymorphone ER 20 mg q12h in week 1 and 40 mg q12h in week 2; oxymorphone ER 20 mg q12h in week 1 and 50 mg q12h in week 2; or placebo q12h during weeks 1 and 2. The primary end point was the change in VAS score for arthritis pain intensity. Other assessments included the Western Ontario and McMaster Universities (WOMAC) OA Index subscales for pain, stiffness, and physical function and the composite index; the Medical Outcomes Study 36-Item Short-Form Health Survey (SF-36) physical health component summary (PCS) score; the Chronic Pain Sleep Inventory (CPSI) score; vital signs; clinical laboratory parameters; and adverse events (AEs). AEs were recorded at each clinic visit. RESULTS: Three hundred seventy patients were randomized to treatment (95 oxymorphone ER 10 mg, 93 oxymorphone ER 40 mg, 91 oxymorphone ER 50 mg, and 91 placebo), and 198 completed the study. Least squares mean changes from baseline in the VAS arthritis pain intensity score were -21, -28, -29, and -17 mm in the oxymorphone ER 10, 40, and 50 mg and placebo groups, respectively (P = 0.002, modified Tukey linear trend test). Oxymorphone ER 40 and 50 mg produced significant improvements from baseline compared with placebo in the WOMAC subscale scores for pain (least squares mean change: -85.1, -108.0, and -42.5, respectively; P < or = 0.025 for 40 mg, P < or = 0.001 for 50 mg), stiffness (-40.5, -48.1, and -17.0; both, P < or = 0.001), and physical function (-256.8, -310.8, and -116.5; P < or = 0.01 and P < or = 0.001, respectively); the SF-36 PCS score (4.6, 3.6, and -0.1; P < 0.001); and the CPSI score (-21.2, -22.2, and -10.7; P < 0.05). The 10-mg dose also was associated with significant improvements compared with placebo in the WOMAC pain (-83.6; P < or = 0.025) and physical function subscales (-232.9; P < or = 0.025) and the SF-36 PCS score (3.9; P < 0.001). The most frequently reported AEs (> or =5% of patients) in the oxymorphone ER groups were nausea (39.4%), vomiting (23.7%), dizziness (22.6%), constipation (22.2%), somnolence (17.6%), pruritus (16.5%), and headache (15.0%). The majority of AEs with oxymorphone ER were mild or moderate in intensity. Three serious AEs (urinary retention, central nervous system depression, and pancreatitis) were considered possibly or probably related to study medication. CONCLUSION: In these patients with chronic, moderate to severe pain related to OA of the hip or knee, oxymorphone ER administered twice daily for 2 weeks produced dose-related reductions in arthritis pain intensity and improvements in physical function.

Analgesics, Opioid↗
PubMed2005

Single- and multiple-dose pharmacokinetic and dose-proportionality study of oxymorphone immediate-release tablets.

INTRODUCTION: Oxymorphone hydrochloride (referred to as oxymorphone), a semisynthetic mu-opioid agonist, is known to produce a more rapid onset of action and greater analgesic potency compared with its parent compound, morphine. Until recently, oxymorphone has been available only in suppository and intravenous formulations. This study examined the pharmacokinetics and dose proportionality of a new immediate-release (IR) tablet formulation of oxymorphone and its metabolites (6-OH-oxymorphone and oxymorphone-3-glucuronide) following single- and multiple-dose administration in healthy volunteers. STUDY DESIGN: A randomised, three-way crossover design was employed, with a target sample size of 24 healthy men and women. METHODS: A single dose of oxymorphone IR (5, 10 and 20mg) was administered on day 1. After drug washout on day 2, study participants then received the same dose every 6 hours (22 total doses) on days 3 to 8. Treatment periods were separated by a 7-day washout. Naltrexone hydrochloride was coadministered to prevent opioid-related adverse events. Blood was collected up to 48 hours after day 1 to determine single-dose pharmacokinetics and up to 6 hours after the last dose for determination of pharmacokinetics at steady state. RESULTS: Twenty-three of 24 enrolled subjects (12 men, 11 women) completed the study. Following a single dose of 5, 10 or 20mg, the oxymorphone IR mean area under the plasma concentration versus time curve from time zero to infinity ([AUC(infinity)] 4.5, 9.1 and 20.1 microg . h/L, respectively) and maximum plasma concentration ([C(max)] 1.1, 1.9 and 4.4 microg/L, respectively) confirmed dose proportionality. 6-OH-oxymorphone and oxymorphone-3-glucuronide also increased in an approximate 2-fold fashion. Similar results were observed for AUC and C(max) of oxymorphone and its metabolites at steady state. Steady state was achieved within 3 days of 6-hourly administration. The median t(max) (time to reach C(max)) was 0.5 hours for all single doses of oxymorphone and at steady state, and the terminal elimination half-life (t(1/2)) was approximately 7.3-9.4 hours. Adverse events were generally mild, and no clinically significant changes in laboratory or other safety variables were noted. DISCUSSION: Because successful pain management often requires careful drug titration across a wide therapeutic dose range, it is important that opioid formulations provide predictable increases in drug concentration with increasing dose. The single-dose and steady-state pharmacokinetic profiles of oxymorphone IR tablets were linear and dose proportional across the dose range from 5 to 20mg.

Adult↗
PubMed2006

Evidence that oxymorphone-induced increases in micronuclei occur secondary to hyperthermia.

Oxymorphone is a potent opioid analgesic. Oral administration of oxymorphone to rats at doses >or= 20 mg/kg and mice at 500 mg/kg produced an increase in micronucleated polychromatic erythrocytes (MPCEs). Oxymorphone does not produce chromosome aberrations in vitro, suggesting that the increased MPCEs in vivo may involve indirect mechanisms. Opioids are known to affect thermoregulatory mechanisms. Changes in body temperature can increase the incidence of MPCEs in rodents. Studies were conducted to examine the relationship between increased MPCEs in rats given oxymorphone and changes in body temperature. Single oral doses of oxymorphone associated with increased MPCEs (20 and 40 mg/kg) also produced a marked, rapid increase in body temperature. When animals were pretreated with sodium salicylate, peak body temperature was lower and returned to baseline more quickly than when oxymorphone was given alone. MPCEs were evaluated in rats after administration of oxymorphone (40 mg/kg) alone or following pretreatment with an oral dose of sodium salicylate. Oxymorphone alone produced a statistically significant increase in the incidence of MPCEs (3.6 per 1000 polychromatic erythrocytes vs. 0.4 in controls). The number of MPCEs in animals pretreated with sodium salicylate was similar to controls. Sodium salicylate alone had no effect on the number of MPCEs. Systemic oxymorphone exposure was not affected by sodium salicylate pretreatment; maximum plasma concentration (C(max)) and area-under-the-curve values were similar after administration of oxymorphone alone or following pretreatment with sodium salicylate. These results indicate that the increased incidence of MPCEs following oxymorphone administration is directly related to increased body temperature.

Analgesics, Non-Narcotic↗
PubMedDate not supplied

Antinociceptive effects of oxymorphone-butorphanol-acepromazine combination in cats.

OBJECTIVE: To determine the antinociceptive effects of oxymorphone, butorphanol, and acepromazine individually and in combination to a noxious visceral stimulus in cats. STUDY DESIGN: Randomized, blinded controlled study. ANIMALS: Eight healthy mixed-breed cats (four male, four female) weighing 4.4 +/- 1.2 kg and aged 1 to 2 years old. METHODS: A silastic balloon catheter was inserted per rectum and inflated at various pressures. Physiological parameters (respiratory rate, pulse rate, and blood pressure) were also recorded. Subjects were administered individual and combined intravenous (i.v.) doses of 0.025, 0.05, 0.10, and 0.20 mg/kg oxymorphone and 0.025, 0.05, 0.10, and 0.20 mg/kg butorphanol. A further study of various ratios of butorphanol and oxymorphone (3:1, 2:1, 1:1, 1:2, and 1:3), at a combined equivalent dose of 0.1 mg/kg, was performed in four cats per dose combination. In a separate study, four cats were administered combined i.v. doses of 0.05 mg/kg each of oxymorphone and butorphanol or 0.05 mg/kg each of oxymorphone, butorphanol, and acepromazine. RESULTS: Combined doses of 0.05 and 0.10 mg/kg of oxymorphone and butorphanol showed mainly additive with some synergistic antinociceptive interactions and the combined dose of 0.2 mg/kg of each agent demonstrated additional antinociceptive effects, P < .05. Additional studies showed that various ratios of the two agents at a total combined dose of 0.10 mg/kg i.v. did not produce levels of antinociception that were significantly different from each other, P > .05. Acepromazine (ACE) significantly increased the magnitude of antinociception at 15 minutes when administered in combination with oxymorphone and butorphanol, P < .05. Also, physiological variables were unaffected by these drug combinations. CONCLUSIONS: Low doses of oxymorphone and butorphanol in combination can produce greater levels of antinociception than when used individually. ACE, in conjunction with oxymorphone and butorphanol, produced even greater levels of antinociception than the two-opioid drug combination. CLINICAL RELEVANCE: Oxymorphone, butorphanol, and ACE can be used in combination to produce additive or synergistic effects without adverse effects in cats. These data suggest that ACE and butorphanol at low doses given as preanesthetic medication followed by a mu opioid (eg, oxymorphone) after surgery at low doses may provide an effective method of pain management in the cat.

Acepromazine↗
PubMed1997

Comparison of ketoprofen, oxymorphone hydrochloride, and butorphanol in the treatment of postoperative pain in dogs.

OBJECTIVE: To compare analgesic effects of ketoprofen, oxymorphone hydrochloride, and butorphanol when used to control postoperative pain associated with elective orthopedic surgery in dogs. DESIGN: Prospective randomized clinical trial. ANIMALS: 70 dogs undergoing orthopedic surgery on a hind limb. PROCEDURE: Dogs were randomly assigned to 1 of 4 postoperative analgesic treatment groups: ketoprofen alone, oxymorphone alone, butorphanol alone, or ketoprofen-oxymorphone. Drugs were given IM at the end of anesthesia. Pain score, sedation score, arterial blood pressures, arterial blood gas partial pressures, and plasma cortisol concentration were measured for 12 hours after surgery. If the pain score was > or = 9, supplemental oxymorphone was administered IM. RESULTS: The proportion of dogs that did not require supplemental treatment with oxymorphone was significantly higher for the ketoprofen alone and ketoprofen-oxymorphone groups than for the oxymorphone alone group. During the first hour after surgery, pain score was lower for oxymorphone alone and ketoprofen-oxymorphone groups than for ketoprofen or butorphanol alone groups. Significant differences were not detected among groups in regard to pain score 2 and 3 hours after surgery or in regard to arterial blood pressures at any time. From 4 to 12 hours after surgery, pain score was significantly lower for the ketoprofen alone group than for other groups. Plasma cortisol concentration was significantly higher for the oxymorphone alone group 6 and 8 hours after surgery, compared with other groups. CLINICAL IMPLICATIONS: Except during the first hour after surgery, dogs given ketoprofen alone after elective orthopedic surgery had a greater level of, and longer-lasting, analgesia than did dogs given oxymorphone or butorphanol alone.

Analgesics, Opioid↗
PubMed2003

Liposome-encapsulated oxymorphone hydrochloride provides prolonged relief of postsurgical visceral pain in rats.

Adequate pain control is necessary for optimal postsurgical recovery and humane treatment of laboratory and companion animals. Opioid drugs are currently the most potent analgesic agents available in human and veterinary medicine. Long-acting formulations of opioid drugs confer several important advantages over standard pharmaceutical preparations, especially for use in animals. A long-acting formulation of oxymorphone hydrochloride was produced by encapsulation into liposomes. Liposome-encapsulated (LE) oxymorphone was tested in a rat model of visceral postoperative pain. Rats were given one subcutaneous injection of LE oxymorphone (1.2 or 1.6 mg/kg of body weight) or standard oxymorphone (0.3 mg/kg) at the time of intestinal transection or resection. A single administration of LE oxymorphone hydrochloride was as effective for relief of postoperative pain in rats (P = 0.18), as were multiple (q4 h or q8 h) injections of 0.3 mg/kg of the standard pharmaceutical preparation. The rats given LE oxymorphone prior to intestinal resection also had significantly higher body weight at three and seven days after surgery than did rats that were given standard oxymorphone. In conclusion, LE oxymorphone was effective in treating visceral pain associated with intestinal surgery in rats. On the basis of body weight gain, rats treated with LE oxymorphone had improved recovery outcome, compared with rats treated with repeated injections of standard oxymorphone.

Abdominal Pain↗
PubMed2004

Effectiveness and safety of oral extended-release oxymorphone for the treatment of cancer pain: a pilot study.

GOALS OF WORK: Inadequate analgesia and/or unmanageable adverse events frequently result in the need to rotate patients with cancer pain to a different opioid. The availability of a novel oral extended-release (ER) formulation of oxymorphone provides clinicians with another treatment option. In this study, we assessed the analgesic effectiveness and safety of the new oral ER formulation of oxymorphone following treatment with controlled-release (CR) morphine sulfate or oxycodone. PATIENTS AND METHODS: Adults with moderate to severe cancer pain were stabilized for > or =3 days on morphine CR or oxycodone CR, and then treated for 7 days at their stabilized dose. Drug selection was based upon patients' previous use or investigator preference. Patients were then crossed over for 7 days of treatment at an estimated equianalgesic dosage of oxymorphone ER. Pain was assessed using a visual analog scale, and adverse events were recorded. MAIN RESULTS: A total of 86 patients entered open-label treatment. Of 34 patients assigned to morphine CR and 52 assigned to oxycodone CR, 21 (61.8%) and 42 (80.8%) completed stabilization and began treatment with oxymorphone ER, respectively; 59 of 63 (93.7%) completed treatment with oxymorphone. There were no significant differences in daily pain intensity scores between oxymorphone ER and comparators (paired t -test). Rescue medication use, expressed as the percent of the daily dose of scheduled opioid, was greater during morphine CR treatment than after crossover to oxymorphone ER (25.2% vs 13.3%; P <0.05, Wilcoxon's test). The tolerability/safety profiles (e.g., nausea, drowsiness, somnolence) were similar for all opioids. CONCLUSIONS: Cancer patients stabilized on morphine CR or oxycodone CR were safely and rapidly converted to a lower milligram dose of oxymorphone ER that provided adequate pain relief with comparable tolerability. These results justify additional trials with oxymorphone ER.

Adolescent↗
PubMed2006

Oxymorphone hydrochloride, a potent opioid analgesic, is not carcinogenic in rats or mice.

Despite their long history of chronic use, little information is available regarding the carcinogenicity of opioid analgesics. Oxymorphone is a potent morphinan-type mu-opioid analgesic used for treatment of moderate-to-severe pain. Oxymorphone was tested for carcinogenicity in Crl:CD IGS BR rats and CD-1 mice. Oxymorphone hydrochloride was administered orally once daily for 2 years to rats at doses of 2.5, 5 and 10 mg/kg/day (males) and 5, 10 and 25 mg/kg/day (females), and mice at 10, 25, 75 and 150 mg/kg/day (65 animals per sex per group; 100 animals per sex in controls). In rats, survival was generally higher than controls in oxymorphone-treated groups, attributable to lower body weight gain. In mice, survival was generally higher than controls in females at all doses and males given < or = 25 mg/kg/day but lower in males given > or = 75 mg/kg/day due to a high incidence of obstructive uropathy. Opioid-related clinical signs and reduced body weight gain occurred in both species throughout the study. Nonneoplastic findings associated with oxymorphone pharmacology included ocular and pulmonary changes in rats considered secondary to inhibition of blinking and mydriasis, and antitussive activity, respectively, and urinary tract and renal findings in mice considered secondary to urinary retention. There was no target organ toxicity, and no increase in any neoplastic lesions attributed to oxymorphone. Plasma oxymorphone levels achieved in these studies exceeded those in patients taking high therapeutic doses of oxymorphone (Area under the curve [AUC(0-24 h)] values up to 5.6-fold and 64-fold in rats and mice, respectively). Oxymorphone is not considered to be carcinogenic in rats or mice under the conditions of these studies.

Analgesics, Opioid↗
PubMedDate not supplied

Oxymorphone extended-release tablets relieve moderate to severe pain and improve physical function in osteoarthritis: results of a randomized, double-blind, placebo- and active-controlled phase III trial.

OBJECTIVE: To compare oxymorphone extended release (ER) and placebo on indices of pain, function, and safety in patients with chronic osteoarthritis (OA) pain. DESIGN: In this multicenter, double-blind, placebo- and active-controlled, parallel-group, dose-ranging study, patients were randomized to oxymorphone ER 20 mg (N = 121), oxymorphone ER 40 mg (N = 121), oxycodone controlled release 20 mg (N = 125), or placebo (N = 124) every 12 hours. The primary efficacy end point was change in arthritis pain intensity (visual analog scale, 0-100) from baseline to week 3 for the oxymorphone ER 40 mg group versus placebo. RESULTS: The primary end point was achieved: the week 3 oxymorphone ER least squares mean difference (LSMD) from placebo was -9.0 (95% confidence interval [CI]: -16.2 to -1.8; P = 0.015). Secondary efficacy analysis showed similar improvements at week 4 (LSMD from placebo, -10.3 [95% CI: -17.7 to -2.8]; P = 0.007) and with oxymorphone ER 20 mg at week 3 (LSMD from placebo, -7.7 [95% CI: -15.0 to -0.4]; P = 0.039) and week 4 (LSMD from placebo, -7.5 [95% CI: -15.0 to 0.0]; P = 0.050). Weeks 3 and 4 pain intensity decreased by approximately 30-40%. Oxymorphone ER 20 and 40 mg improved from baseline on the Western Ontario and McMaster Universities Osteoarthritis Composite Index and pain and physical function subscales at week 4. Adverse events in all opioid groups included mild to moderate nausea, constipation, and somnolence. CONCLUSIONS: In this short-term study, oxymorphone ER was superior to placebo for relieving pain and improving function in patients with moderate to severe chronic OA pain, and is an alternative to other sustained-release opioids.

Analgesics, Opioid↗
PubMed2005

Efficacy and safety of oxymorphone immediate release for the treatment of mild to moderate pain after ambulatory orthopedic surgery: results of a randomized, double-blind, placebo-controlled trial.

OBJECTIVE: To assess the analgesic efficacy and safety of 5 mg of oxymorphone immediate release (IR) for mild to moderate pain. DESIGN: Multicenter, double-blind, randomized, placebo-controlled study. SETTING: Ambulatory surgical centers. PARTICIPANTS: Outpatients (age, > or = 18 y) undergoing knee arthroscopy. INTERVENTION: Randomization to 5 mg of oxymorphone IR or placebo hourly as needed for up to 8 hours. MAIN OUTCOME MEASURE: Sum of pain intensity difference (SPID) from baseline to 8 hours. RESULTS: Among 122 patients randomized, 70.5% and 28.7% had moderate or mild postsurgical pain at baseline, respectively. The mean SPID score was significantly greater in the oxymorphone IR group, showing greater pain relief, compared with the placebo group (least squares mean difference +/- standard error, 76.9+/-28.09; 95% confidence interval, 21.26-132.59; P=.007). More placebo patients (48.4%) required rescue medication than oxymorphone IR patients (16.7%), with median times to use of rescue medication of 6 hours 54 minutes and more than 8 hours, respectively (P<.001). More patients (47.4%) rated oxymorphone IR "very good" or "excellent" for pain relief versus placebo (25.0%). No oxymorphone IR-treated patients discontinued because of adverse events (AEs) or experienced serious AEs. CONCLUSIONS: Five milligrams of oxymorphone IR was well tolerated and effective at relieving mild or moderate postsurgical pain after outpatient knee surgery.

Adult↗
PubMed2004

The efficacy and safety of oral immediate-release oxymorphone for postsurgical pain.

In this double-blind, parallel-group study, we compared 3 oxymorphone immediate-release (IR) doses with placebo for efficacy and with oxycodone IR and placebo for safety in patients with acute moderate-to-severe postsurgical pain. During the single-dose phase (n = 300), patients received oxymorphone IR 10, 20, or 30 mg; oxycodone IR 10 mg; or placebo. All oxymorphone IR doses were superior for providing pain relief for 8 h (P < 0.05), with a significant analgesic dose response (P < 0.001). Significant pain intensity differences occurred by 45 min (20- and 30-mg doses; P < 0.05). Discontinuations for lack of efficacy totaled 42% among placebo-treated patients and 27% among those treated with oxymorphone IR. Patients requiring rescue medication after 3 h were allowed to receive additional study drug every 4 to 6 h as needed for the multiple-dose phase (n = 164). All oxymorphone groups maintained analgesia for 48 h. The median dosing interval was >9.5 h for oxymorphone IR 30 mg and > or =7 h for the other groups. Opioid-related adverse events, similar among groups, were generally mild or moderate. Oxymorphone IR 10, 20, or 30 mg provided significant dose-related pain relief compared with placebo, and this relief was maintained over several days with a safety profile comparable to that of oxycodone IR.

Adolescent↗
PubMed2003

A single dose of liposome-encapsulated oxymorphone or morphine provides long-term analgesia in an animal model of neuropathic pain.

An extended-release formulation of oxymorphone was produced by encapsulation into liposomes, using a novel technique. Liposome-encapsulated morphine was produced, using a standard technique These preparations were tested in an animal model of neuropathic pain. Male Sprague-Dawley rats (approx. 300 g) were allotted to control (non-loaded liposomes) and treatment (liposome-encapsulated oxymorphone or morphine) groups. Drugs were administered subcutaneously to all rats immediately prior to sciatic nerve ligation. Thermal withdrawal latencies were measured at baseline and daily for seven days after sciatic nerve ligation. A second experiment involved subcutaneous administration of non-loaded liposomes, morphine, or oxymorphone to rats that did not undergo sciatic nerve ligation. Thermal withdrawal latencies in sciatic nerve-ligated rats given non-loaded liposomes decreased significantly by day four, with maximal decrease at day seven after surgery, indicating development of full hyperalgesia. In contrast, ligated rats given liposome-encapsulated morphine or liposome-encapsulated oxymorphone had no decrease in thermal withdrawal latency by day four, indicating that these long-acting preparations prevented development of hyperalgesia after a single injection. This treatment effect persisted to day seven. Non-ligated rats treated with vehicle or liposome-encapsulated morphine had no change in thermal withdrawal latencies. Non-ligated rats treated with liposome-encapsulated oxymorphone had a small, but significant increase in thermal withdrawal latency from day four through day seven. One subcutaneous injection of liposome-encapsulated oxymorphone or morphine was effective in preventing hyperalgesia in this pain model for up to seven days. These results suggest that liposome-encapsulation of oxymorphone offers a novel, convenient, and effective means to provide long-term analgesia.

Analgesics, Opioid↗
PubMed1987

Oxymorphone: cardiovascular, pulmonary, and behavioral effects in dogs.

Cardiovascular, pulmonary, and behavioral effects of multiple doses of oxymorphone in 10 nonanesthetized, spontaneously breathing, healthy dogs were studied. Oxymorphone (0.4 mg/kg of body weight) was administered IV, and at 20, 40, and 60 minutes after the first injection was given, 0.2 mg of oxymorphone/kg was administered. Cardiovascular and pulmonary variables were measured before (base line) and at 5, 15, 35, 55, 75, 100, 120, 150, 180, 210, 240, 270, and 300 minutes after the first oxymorphone injection. Degree of sedation and behavioral effects also were recorded. Naloxone (0.04 mg/kg, IV) was administered 4.5 hours after the 4th oxymorphone injection, and behavioral changes were recorded. Oxymorphone induced mild respiratory depression. After transient apnea developed, respiratory rate increased to a pant, tidal volume decreased, and minute ventilation increased, but these values were not significantly (P = 0.05) different from base line. The PaCO2, physiologic dead space, and base deficit increased; alveolar tidal volume decreased; and alveolar minute ventilation did not change. The PaO2 decreased, hemoglobin and arterial O2 content increased, and O2 transport did not change. Venous admixture transiently increased. Oxymorphone induced minimal cardiovascular depression. Mean arterial blood pressure, stroke volume, central venous pressure, pulmonary artery pressure, and pulmonary wedge pressure increased. Heart rate decreased, systemic vascular resistance transiently increased, and cardiac output transiently decreased. Because the dogs moved spontaneously, responded to sound with sudden, vigorous movements, and breathed with excessive effort, oxymorphone alone was considered inadequate as a general anesthetic.

Animals↗
PubMed1989

Naloxone reversal of oxymorphone effects in dogs.

Oxymorphone was administered IV to dogs 4 times at 20-minute intervals (total dosage, 1 mg/kg of body weight, IV) on 2 separate occasions. Minute ventilation, mixed-expired carbon dioxide concentration, arterial and mixed-venous pH and blood gas tensions, arterial, central venous, pulmonary arterial, and pulmonary wedge pressures, and cardiac output were measured. Physiologic dead space, base deficit, oxygen transport, and vascular resistance were calculated before and at 5 minutes after the first dose of oxymorphone (0.4 mg/kg) and at 15 minutes after the first and the 3 subsequent doses of oxymorphone (0.2 mg/kg). During 1 of the 2 experiments in each dog, naloxone was administered 20 minutes after the last dose of oxymorphone; during the alternate experiment, naloxone was not administered. In 5 dogs, naloxone was administered IV in titrated dosages (0.005 mg/kg) at 1-minute intervals until the dogs were able to maintain sternal recumbency, and in the other 5 dogs, naloxone was administered IM as a single dose (0.04 mg/kg). Naloxone (0.01 mg/kg, IV or 0.04 mg/kg, IM) transiently reversed most of the effects of oxymorphone. Within 20 to 40 minutes after IV naloxone administration and within 40 to 70 minutes after IM naloxone administration, most variables returned to the approximate values measured before naloxone administration. The effects of oxymorphone outlasted the effects of naloxone; cardiovascular and pulmonary depression and sedation recurred in all dogs. Four hours and 20 minutes after the last dose of oxymorphone, alertness, responsiveness, and coordination improved in all dogs after IM administration of naloxone. Cardiac arrhythmia, hypertension, or excitement was not observed after naloxone administration.

Animals↗
PubMedDate not supplied

A comparison of the analgesic effect of oxymorphone by rectal suppository and intramuscular injection in patients with postoperative pain.

The relative analgesic potency of oxymorphone by rectal suppository and intramuscular injection was evaluated in a double-blind, twin-crossover comparison of graded single doses in 136 patients with postoperative pain. The time-effect curves of the two routes of administration differed substantially; rectal resulted in lower and more delayed peak analgesia and a longer duration of action than intramuscular administration. When both duration and intensity of analgesia are considered (total effect), rectal oxymorphone was 1/10 as potent as the intramuscular form; in peak effect, it was only 1/16 to 1/20 as potent. However, because intramuscular oxymorphone is nine to ten times as potent as intramuscular morphine, 5 to 10 mg oxymorphone by suppository provides analgesia comparable to that provided by the usually used doses of parenteral narcotics. Rectal oxymorphone produced no more, and perhaps somewhat fewer, side effects than doses of intramuscular oxymorphone producing equivalent total analgesic effect. None of the patients objected to the rectal route of analgesic administration. This study demonstrates the feasibility of well-controlled analgesic assays employing the double-dummy technique to compare suppositoreis with oral or parenteral analgesic dosage forms. Our observations also suggest that the rectal route is an acceptable and practical way of administering potent analgesics and is probably being underutilized by physicians in the control of moderate to severe pain.

Adult↗