-
Veterinary Surgery : VS 1992Oxymorphone (0.2 mg/kg, maximum 4.5 mg) or butorphanol (0.2 mg/kg, maximum 4.5 mg), with acepromazine (0.05 mg/kg) and atropine (0.02 mg/kg), was administered... (Comparative Study)
Comparative Study
Oxymorphone (0.2 mg/kg, maximum 4.5 mg) or butorphanol (0.2 mg/kg, maximum 4.5 mg), with acepromazine (0.05 mg/kg) and atropine (0.02 mg/kg), was administered intravenously to 106 healthy dogs undergoing radiographic examination of the pelvis. The dogs were returned to their owners after the examination and opioid reversal with naloxone (0.02 mg/kg intravenously, maximum 0.4 mg). Questionnaires were completed by the radiology staff and owners of the dogs, and results were coded by one person, all of whom were unaware of the treatment used. There was a lower incidence of temporary excitement upon injection and less panting in dogs sedated with butorphanol than with oxymorphone. There were no significant differences in degree of sedation, response to noise or manipulation, vocalization, defecation, heart rate, reversibility, sedation after reversal, or personality. Both forms of chemical restraint were satisfactory for radiographic examination of the pelvis, with no significant side effects in healthy dogs.
Topics: Acepromazine; Animals; Butorphanol; Dogs; Drug Combinations; Female; Immobilization; Injections, Intravenous; Male; Oxymorphone; Random Allocation; Surveys and Questionnaires
PubMed: 1413474
DOI: 10.1111/j.1532-950x.1992.tb01720.x -
Veterinary Surgery : VS 1998To determine the antinociceptive effects of oxymorphone, butorphanol, and acepromazine individually and in combination to a noxious visceral stimulus 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.
Topics: Acepromazine; Analgesia; Analgesics, Opioid; Animals; Butorphanol; Cats; Dopamine Antagonists; Dose-Response Relationship, Drug; Drug Combinations; Female; Male; Oxymorphone
PubMed: 9749518
DOI: 10.1111/j.1532-950x.1998.tb00158.x -
Drugs in R&D 2005Oxymorphone hydrochloride (referred to as oxymorphone), a semisynthetic mu-opioid agonist, is known to produce a more rapid onset of action and greater analgesic potency... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
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.
Topics: Adult; Chemistry, Pharmaceutical; Cross-Over Studies; Dose-Response Relationship, Drug; Female; Humans; Male; Oxymorphone; Tablets
PubMed: 15777102
DOI: 10.2165/00126839-200506020-00004 -
Comparative Medicine Oct 2004The use of mice in biomedical research is increasing, largely due to the production and use of genetically engineered animals. Providing postoperative pain control in...
The use of mice in biomedical research is increasing, largely due to the production and use of genetically engineered animals. Providing postoperative pain control in mice presents many challenges, and long-acting analgesic preparations would be advantageous for this species. A single subcutaneous injection of a liposome-encapsulated (LE) preparation of oxymorphone was compared with multiple injections of buprenorphine or saline in outbred mice undergoing splenectomy. Control groups were given isoflurane alone or isoflurane and an injection of LE oxymorphone but did not undergo surgery. The following parameters were evaluated for 5 days after surgery and were compared with presurgical baseline data for each group: food and water consumption, body weight, ethographic score, and voluntary exercise on a running wheel. Ethographic scores indicated less postsurgical pain in both groups of mice that received either analgesic preparation compared with mice that received only saline. However, mice given LE oxymorphone had superior postoperative recovery, as measured by wheel-running distance and body weight gain, compared with mice given buprenorphine or saline. Mice undergoing splenectomy had significant decreases in body weight, food and water consumption, voluntary exercise, and other normal behaviors. Administration of liposomal oxymorphone at the time of surgery improved postsurgical recovery as measured by these parameters compared with multiple injections of buprenorphine or saline alone. Administration of LE oxymorphone at the time of surgery improved postsurgical recovery, as measured by these parameters.
Topics: Analgesics, Opioid; Animals; Animals, Outbred Strains; Behavior, Animal; Body Weight; Buprenorphine; Drinking; Eating; Injections, Subcutaneous; Laboratory Animal Science; Liposomes; Male; Mice; Mice, Inbred ICR; Oxymorphone; Pain; Pain Measurement; Physical Conditioning, Animal; Specific Pathogen-Free Organisms; Splenectomy
PubMed: 15575370
DOI: No ID Found -
Journal of Veterinary Pharmacology and... Jun 2014Buccal administration of buprenorphine is commonly used to treat pain in cats. It has been argued that absorption of buprenorphine through the buccal mucosa is high, in... (Randomized Controlled Trial)
Randomized Controlled Trial
Buccal administration of buprenorphine is commonly used to treat pain in cats. It has been argued that absorption of buprenorphine through the buccal mucosa is high, in part due to its pKa of 8.24. Morphine, methadone, hydromorphone, and oxymorphone have a pKa between 8 and 9. This study characterized the bioavailability of these drugs following buccal administration to cats. Six healthy adult female spayed cats were used. Buccal pH was measured prior to drug administration. Morphine sulfate, 0.2 mg/kg IV or 0.5 mg/kg buccal; methadone hydrochloride, 0.3 mg/kg IV or 0.75 mg/kg buccal; hydromorphone hydrochloride, 0.1 mg/kg IV or 0.25 mg/kg buccal; or oxymorphone hydrochloride, 0.1 mg/kg IV or 0.25 mg/kg buccal were administered. All cats received all treatments. Arterial blood was sampled immediately prior to drug administration and at various times up to 8 h thereafter. Bioavailability was calculated as the ratio of the area under the time-concentration curve following buccal administration to that following IV administration, each indexed to the administered dose. Mean ± SE (range) bioavailability was 36.6 ± 5.2 (12.7-49.5), 44.2 ± 7.9 (18.7-70.5), 22.4 ± 6.9 (6.4-43.4), and 18.8 ± 2.0 (12.9-23.5)% for buccal administration of morphine, methadone, hydromorphone, and oxymorphone, respectively. Bioavailability of methadone was significantly higher than that of oxymorphone.
Topics: Administration, Buccal; Analgesics, Opioid; Animals; Biological Availability; Cats; Female; Hydromorphone; Methadone; Morphine; Oxymorphone
PubMed: 24236993
DOI: 10.1111/jvp.12090 -
JAMA Ophthalmology Jun 2014
Topics: Counseling; Disease Progression; Fluorescein Angiography; Follow-Up Studies; Fundus Oculi; Humans; Injections, Intravenous; Ischemia; Male; Middle Aged; Ophthalmoscopy; Oxymorphone; Radiography; Retina; Retinal Vessels; Risk Assessment; Substance Abuse, Intravenous; Vision Disorders
PubMed: 24921173
DOI: 10.1001/jamaophthalmol.2014.324 -
Journal of Clinical Anesthesia 1989The safety and efficacy of two potent opiate analgesics, fentanyl and oxymorphone, used as adjuncts in general anesthesia, were studied in 39 patients undergoing... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
The safety and efficacy of two potent opiate analgesics, fentanyl and oxymorphone, used as adjuncts in general anesthesia, were studied in 39 patients undergoing elective gynecologic surgery of at least 2 hours duration. Based on a potency ratio of 10:1, patients received either fentanyl 6.5 micrograms/kg or oxymorphone 65 micrograms/kg prior to a thiopental 2 to 3 mg/kg succinylcholine induction and endotracheal intubation. Additional maintenance narcotic and isoflurane were administered as required by the "blinded" anesthesiologist in response to hemodynamic alterations 15% above a presurgical baseline. Overall analysis included hemodynamic response at preset intraoperative intervals, total anesthetic requirements, and stability of vital signs in the recovery room. Blood pressure and heart rate were reliably controlled with either agent; however, less narcotic (ml) and recovery room analgesics were required in the oxymorphone-treated group (p less than 0.05). Decreased naloxone requirements (p less than 0.05) and a more rapid emergence suggested that fentanyl was a safer agent when administered in relatively unrestricted fashion.
Topics: Anesthesia, General; Double-Blind Method; Drug Evaluation; Female; Fentanyl; Genital Diseases, Female; Hemodynamics; Humans; Hydromorphone; Oxymorphone; Randomized Controlled Trials as Topic
PubMed: 2483328
DOI: 10.1016/0952-8180(89)90022-6 -
Journal of Opioid Management 2012The aging population generally has greater need for analgesics and is best served by having as many good therapeutic options as possible. Geriatric analgesia requires...
OBJECTIVE
The aging population generally has greater need for analgesics and is best served by having as many good therapeutic options as possible. Geriatric analgesia requires special consideration of age-associated physiologic changes that can affect drug dosing. The study of extended-release (ER) oxymorphone in older (≥ 65 years of age) versus younger (18-40 years of age) male and female volunteers was described.
METHODS
In this multiple-dose, parallel-group, open-label trial, healthy volunteers received a single oral dose of 20 mg oxymorphone ER on day 1, followed by a 48-hour washout period, then two oral doses of 20 mg oxymorphone ER tablets every 12 hours from day 3 to day 8, and a single oral dose of 20 mg oxymorphone ER on day 9. Naltrexone was administered each day to the subjects.
RESULTS
The elderly had significantly higher plasma levels of oxymorphone, 6-OH-oxymorphone, and oxymorphone-3-glucuronide than the younger group (1.36-fold higher area under the concentration versus time curve [AUC] and 1.45-fold higher C(max)) when they were treated with a single dose (20 mg) of oxymorphone. Steady-state AUC and C(max) also were higher in the older group. Following adjustment for body weight, AUC values for oxymorphone and its metabolites were about 40 percent higher and the mean C(max) values were 30-35 percent higher in the older group compared to the younger group.
CONCLUSION
The results of the current study of an ER formulation revealed no pharmacokinetic features that would preclude dosing in the elderly. As with any drug and any age group (but particularly the elderly), oxymorphone ER should be initiated at lower doses in elderly compared to younger patients and titrated to optimal level.
Topics: Adolescent; Adult; Age Factors; Aged; Analgesics, Opioid; Area Under Curve; Delayed-Action Preparations; Female; Glucuronides; Humans; Male; Naltrexone; Narcotic Antagonists; Oxymorphone; Tablets; Young Adult
PubMed: 23264316
DOI: 10.5055/jom.2012.0138 -
Experimental Biology and Medicine... Nov 2023The opioid epidemic has become a serious national crisis in the United States. An indepth systematic analysis of opioid-related adverse events (AEs) can clarify the...
The opioid epidemic has become a serious national crisis in the United States. An indepth systematic analysis of opioid-related adverse events (AEs) can clarify the risks presented by opioid exposure, as well as the individual risk profiles of specific opioid drugs and the potential relationships among the opioids. In this study, 92 opioids were identified from the list of all Food and Drug Administration (FDA)-approved drugs, annotated by RxNorm and were classified into 13 opioid groups: buprenorphine, codeine, dihydrocodeine, fentanyl, hydrocodone, hydromorphone, meperidine, methadone, morphine, oxycodone, oxymorphone, tapentadol, and tramadol. A total of 14,970,399 AE reports were retrieved and downloaded from the FDA Adverse Events Reporting System (FAERS) from 2004, Quarter 1 to 2020, Quarter 3. After data processing, Empirical Bayes Geometric Mean (EBGM) was then applied which identified 3317 pairs of potential risk signals within the 13 opioid groups. Based on these potential safety signals, a comparative analysis was pursued to provide a global overview of opioid-related AEs for all 13 groups of FDA-approved prescription opioids. The top 10 most reported AEs for each opioid class were then presented. Both network analysis and hierarchical clustering analysis were conducted to further explore the relationship between opioids. Results from the network analysis revealed a close association among fentanyl, oxycodone, hydrocodone, and hydromorphone, which shared more than 22 AEs. In addition, much less commonly reported AEs were shared among dihydrocodeine, meperidine, oxymorphone, and tapentadol. On the contrary, the hierarchical clustering analysis further categorized the 13 opioid classes into two groups by comparing the full profiles of presence/absence of AEs. The results of network analysis and hierarchical clustering analysis were not only consistent and cross-validated each other but also provided a better and deeper understanding of the associations and relationships between the 13 opioid groups with respect to their adverse effect profiles.
Topics: Analgesics, Opioid; Bayes Theorem; Data Mining; Fentanyl; Hydrocodone; Hydromorphone; Meperidine; Oxycodone; Oxymorphone; Tapentadol; United States
PubMed: 38158803
DOI: 10.1177/15353702231211860 -
The Canadian Veterinary Journal = La... Jun 1998The 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... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
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.
Topics: Adjuvants, Anesthesia; Analgesia; Anesthetics, Combined; Anesthetics, Inhalation; Anesthetics, Local; Animals; Blood Gas Analysis; Blood Pressure; Bupivacaine; Carbon Dioxide; Dogs; Female; Halothane; Heart Rate; Injections, Epidural; Injections, Intravenous; Male; Oxymorphone; Pain, Postoperative; Respiration
PubMed: 9635170
DOI: No ID Found