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Evaluation of oxycodone and acetaminophen in treatment of postoperative dental pain.

Although both acetaminophen and oxycodone are commonly used analgesics, they were not available as a combination until recently. Since oxycodone is not available as a single entity, there is no archival or even anectodal information on the efficacy and safety of this combination. The purpose of this study was to evaluate the relative efficacy of various doses of the combination that could be used in dental situations. The single-dose efficacy and safety of acetaminophen 500 mg., oxycodone 5 mg., acetaminophen 500 mg. + oxycodone 5 mg., acetaminophen 1,000 mg. + oxycodone 5 mg., acetaminophen 1,000 mg. + oxycodone 10 mg., and placebo were compared in outpatients who experienced moderate to severe pain after surgical removal of inpacted third molars. Analgesic data were analyzed by analysis of variance and Duncan's multiple range test. All active treatments were superior to placebo, with the high-ratio combination being the most efficacious. This treatment also had the highest incidence of limiting side effects. A positive dose-effect relationship was evident for both acetaminophen 500 mg. and 1,000 mg. and for oxycodone 5 mg. and 10 mg.

Acetaminophen↗

Attenuation of morphine-induced delirium in palliative care by substitution with infusion of oxycodone.

We have observed among patients of the Southern Community Hospice Programme that up to 25% experience acute delirium when treated with morphine and improve when the opioid is changed to oxycodone or fentanyl. This study aimed to confirm by a prospective trial that oxycodone produces less delirium than morphine in such patients. Oxycodone was administered by a continuous subcutaneous infusion, as this allowed more flexible and reliable dosing, and patients were monitored for any adverse reactions to the drug. Thirteen patients completed the study. Statistically significant improvements in mental state and nausea and vomiting occurred following a change from morphine to oxycodone. Pain scores improved but did not reach a level of statistical significance. The phenotype status of the patients was tested to establish their capacity to metabolize oxycodone. One patient who did not achieve adequate pain control proved to be a poor metabolizer. These results show that oxycodone administered by the subcutaneous route can provide effective analgesia without significant side effects in patients with morphine-induced delirium. This treatment allows patients to remain more comfortable and lucid in their final days. A small proportion of patients who do not metabolize oxycodone effectively may not receive this benefit.

Aged↗

Combination oxycodone 5 mg/ibuprofen 400 mg for the treatment of pain after abdominal or pelvic surgery in women: a randomized, double-blind, placebo- and active-controlled parallel-group study.

BACKGROUND: The sensation of pain arises from both central and peripheral sites, and inflammation may be one of its underlying causes. Combination therapy with analgesic agents having multimodal mechanisms of action and complementary pharmacokinetic properties enhances pain relief by addressing the different pathways of pain while limiting individual drug doses and, therefore, the potential for adverse effects caused by any single agent. Oxycodone and ibuprofen each have been used effectively as monotherapy and in other combinations for the treatment of acute pain; a fixed combination of these analgesics may improve pain relief in the setting of abdominal or pelvic surgery, where trauma and any resultant inflammation may be present at the same time. OBJECTIVE: This study evaluated and compared the analgesic efficacy and tolerability of a single-dose combination tablet containing oxycodone 5 mg/ibuprofen 400 mg with either agent alone and with placebo in women who had undergone abdominal or pelvic surgery. METHODS: In this multicenter, randomized, double-blind,placebo- and active-controlled, parallel-group trial, women experiencing moderate to severe pain between 14 and 48 hours after surgery were randomized per protocol to receive a single dose of study medication in a 3:3:1:1 ratio (combination oxycodone/ibuprofen, ibuprofen, oxycodone, and placebo, in that order). Over a 6-hour study period, patients recorded their assessments of pain intensity (100-mm visual analog scale and 4-point scale), relief from starting pain, and overall evaluation of study drug based on prespecified definitions and rating scales. Based on these data, the following primary efficacy end points were determined: total pain relief 6 hours after dosing (TOTPAR6) and sum of pain intensity differences 6 hours after dosing (SPID6). Other end points included the time to onset of pain relief, time to use of rescue medication, and patient's global rating of analgesic effectiveness. Tolerability was evaluated on the basis of observed and patient-reported adverse events and findings on physical examination. RESULTS: Four hundred fifty-six women participated in the study. They were primarily white and had a mean age of 41.6 years and a mean body weight of 171.5 pounds. Combination treatment was associated with significantly better TOTPAR6 and SPID6 scores compared with ibuprofen alone (P < 0.02 and P < 0.015, respectively), oxycodone alone (P < 0.009 and P < 0.001), or placebo (both, P < 0.001). Fewer patients receiving combination treatment required rescue medication, and the time to use of rescue medication was significantly longer in the combination-treatment group compared with the other groups (P < 0.05). Patients' global ratings of analgesic efficacy were significantly higher in the combination-treatment group compared with all other groups (P < 0.044 vs ibuprofen alone; P < 0.001 vs oxycodone alone and placebo). The onset of pain relief occurred within 15 minutes of dosing with all 4 regimens. Nausea was the most frequently reported treatment-emergent adverse event in all 4 groups. The incidence of treatment-emergent adverse events was highest with placebo (55.0%), followed by oxycodone alone (44.2%), ibuprofen alone (42.3%), and combination treatment (40.8%). CONCLUSIONS: In this population of women who had undergone abdominal or pelvic surgery, the combination of oxycodone 5 mg/ibuprofen 400 mg was significantly more effective than either agent alone or placebo in the treatment of moderate to severe postoperative pain.

Abdomen↗

Oxycodone.

Oxycodone has been in clinical use since 1917. Parenteral oxycodone was used mainly for the treatment of acute postoperative pain whereas combinations, for example, oxycodone and acetaminophen, were used for moderate pain. Since the introduction of controlled-release oxycodone, it has been used to manage cancer-related pain and chronic non-cancer-related pain problems. Controlled studies have been performed in postoperative pain, cancer pain, osteoarthritis-related pain, and neuropathic pain due to postherpetic neuralgia and diabetic neuropathy. The pharmacodynamic effects of oxycodone are typical of a mu-opioid agonist. Oxycodone closely resembles morphine but it has some distinct differences, particularly in its pharmacokinetic profile. Being an old drug, the basic pharmacology of oxycodone has been a neglected field of research.

Analgesics, Opioid↗

A comparative study of oxycodone and morphine in a multi-modal, tissue-differentiated experimental pain model.

Visceral pain can be difficult to treat with classical mu-opioid agonists and it has been suggested to use opioids with distinct pharmacological profiles. In animal experiments, oxycodone has shown different effects compared to morphine, and clinical observations have shown that oxycodone may occasionally be superior to, e.g., morphine in the treatment of visceral pain. In the current study, we randomised 24 healthy subjects to treatment with either morphine (30 mg), oxycodone (15 mg) or placebo in a crossover study. The experimental pain model involved multi-modal (mechanical, thermal and electrical) pain tests in the skin, muscles and viscera. The pain tests were carried out at baseline and 30, 60 and 90 min after oral administration of the drugs. The model showed effect of the two opioids compared to placebo on all stimulus modalities in all three types of tissues (all P values <0.001). Both opioids attenuated the sensory response mainly to painful stimulations. Morphine and oxycodone were equipotent in pain modulation of the skin and muscles, but oxycodone had superior analgesic effect to both morphine and placebo on the mechanical (P<0.001) and thermal (P<0.001) stimulations of the oesophagus. In conclusion, the multi-modal and tissue-differentiated pain model could link findings from animal experiments to clinical findings. A different pharmacological profile of oxycodone compared to that of morphine was shown, and thus oxycodone may be a useful alternative to morphine in the treatment of visceral pain syndromes.

Adult↗

Pharmacokinetic-pharmacodynamic relationships of controlled-release oxycodone.

Plasma concentrations of oxycodone, oxymorphone, and noroxycodone were determined after administration of 20 mg oral controlled-release oxycodone tablets to four subject groups: young (aged 21 to 45 years) men, elderly (aged 65 to 79 years) men, young women, and elderly women. Area under the oxycodone and noroxycodone concentration-time curve (AUC) values were comparable among the four groups. Compared with oxycodone, the oxymorphone AUC values were small, with significant differences between subject groups. AUC values were also calculated for the pharmacodynamic variable "drug effect," scored on a 100 mm visual analog scale. The two groups with the highest oxycodone AUC values (young and elderly women) had the lowest oxymorphone AUC values and the greatest drug effect AUC values. The two groups with the lowest oxycodone AUC values (young and elderly men) had the highest oxymorphone AUC values and the lowest drug effect AUC values. These results support oxycodone, and not oxymorphone, as being primarily responsible for pharmacodynamic and analgesic effects.

Administration, Oral↗

Pharmacokinetics and ventilatory effects of oxycodone before and after liver transplantation.

The pharmacokinetics and ventilatory effects of oxycodone were studied in six volunteer patients with end-stage liver cirrhosis before and after orthotopic liver transplantation. Plasma samples and urine were collected for 24 hours after intravenous administration of 0.05 mg/kg oxycodone hydrochloride. Concentrations of oxycodone and its metabolites, noroxycodone and oxymorphone, were measured in plasma and urine. THe median elimination half-life of oxycodone was 13.9 hours (range, 4.6 to 24.4 hours) in patients with cirrhosis before transplantation and 3.4 hours (range, 2.6 to 5.1 hours) after transplantation (p < 0.05). Correspondingly, oxycodone clearance increased from 0.26 L/min (range, 0.15 to 0.73 L/min) before transplantation to 1.13 L/min (range, 0.71 to 3.98 L/min) after transplantation (p < 0.05). Oxycodone depressed ventilation more strongly before transplantation than after transplantation (p < 0.05). Care should be exercised when oxycodone is used in patients with end-stage disease.

Analgesics, Opioid↗

Controlled-release oxycodone relieves neuropathic pain: a randomized controlled trial in painful diabetic neuropathy.

BACKGROUND: Painful neuropathy is one of the most common long-term complications of diabetes mellitus and often proves difficult to relieve. METHODS: Patients with diabetic neuropathy with moderate or greater pain for at least 3 months, were evaluated for efficacy, safety and health-related quality of life (QOL) while receiving controlled-release (CR) oxycodone (OxyContin) or active placebo. Patients underwent washout from all opioids 2-7 days before randomization to 10 mg CR oxycodone or active placebo (0.25 mg benztropine) q12h. The dose was increased, approximately weekly, to a maximum of 40 mg q12h CR oxycodone or 1 mg q12h benztropine, with crossover to the alternate treatment after a maximum of 4 weeks. Acetaminophen, 325-650 mg q4-6h prn was provided as rescue. RESULTS: Thirty-six patients were evaluable for efficacy (21 men, 15 women, mean age 63.0+/-9.4 years). CR oxycodone resulted in significantly lower (P=0.0001) mean daily pain (21.8+/-20.7 vs. 48.6+/-26.6 mm VAS), steady pain (23.5+/-23.0 vs. 47.6+/-30.7 mm VAS), brief pain (21.8+/-23.5 vs. 46.7+/-30.8 mm VAS), skin pain (14.3+/-20.4 vs. 43.2+/-31.3 mm VAS), and total pain and disability (16.8+/-15.6 vs. 25.2+/-16.7; P=0.004). Scores from 6 of the 8 SF-36 domains and both summary scales, Standardized Physical Component (P=0.0002) and Standardized Mental Component (P=0.0338) were significantly better during CR oxycodone treatment. The number needed to treat to obtain one patient with at least 50% pain relief is 2.6 and clinical effectiveness scores favoured treatment with CR oxycodone over placebo (P=0.0001). CONCLUSION: CR oxycodone is effective and safe for the management of painful diabetic neuropathy and improves QOL.

Aged↗

Controlled-release oxycodone and morphine in cancer related pain.

Controlled-release (CR) formulations of oxycodone and morphine were compared in 45 patients with chronic cancer pain. The study was started with an open-label, randomised titration phase to achieve stable pain control for at least 48 h, followed by a double-blind, randomised, crossover phase in two periods, 3-6 days each. To blind the study using available tablet strengths, the dose ratio of oxycodone to morphine was set at 2:3. A daily telephone contact was maintained between the patient and the investigator. The patients were asked to assess pain intensity four times a day and acceptability of therapy twice daily, and to record possible adverse effects. Pharmacodynamic evaluations were performed at the end of each double-blind period. The patients were allowed to use escape analgesic (respective opioid as oral solution) as needed. Twenty-seven patients were evaluable for both safety and efficacy. Pain was well-controlled during both stable phases. When the period effect was taken into account the two opioids provided comparable analgesia. If the results of the two periods were combined, the patients consumed significantly more escape doses and the mean pain intensities were significantly greater with CR oxycodone. The total opioid consumption ratio of oxycodone to morphine was 2:3 when oxycodone was administered first, and 3:4 when oxycodone was administered after morphine. The total incidence of adverse experiences reported by the patients was similar, but significantly more vomiting occurred with morphine, whereas constipation was more common with oxycodone.

Adult↗

The relative potency between high dose oral oxycodone and intravenous morphine: a case illustration.

Oxycodone is an effective opioid analgesic for cancer pain. In the United States, it is available exclusively as an oral formulation, predominantly in fixed dose combination with acetaminophen or aspirin. The latter limits its use in cancer pain due to the potential toxicity of the nonopioid component. Oxycodone is now available as a single agent, controlled release formulation. The following case report of an opioid tolerant cancer patient taking repeated high doses of oral oxycodone supports the use of a 1:1 milligram conversion ratio for oral morphine and oral oxycodone. This patient's clinical course indicates that oral oxycodone can be used safely and to good effect at high dose, that the milligram relative potency ratio for oral oxycodone to parenteral morphine during repeated dosing is 3:1, and suggests that availability of multiple formulations of oxycodone may benefit cancer patients.

Administration, Oral↗

Can coadministration of oxycodone and morphine produce analgesic synergy in humans? An experimental cold pain study.

AIMS: The coadministration of subantinociceptive doses of oxycodone with morphine has recently been shown to result in a synergistic antinociceptive effect in rats. The present study was aimed to investigate the possibility that coadministration of morphine and oxycodone can produce a similar synergistic effect in humans exposed to an experimental model of cold pressor test (CPT). METHODS: The enriched enrollment design was used to exclude 'stoic' and 'placebo responders' in a single-blind fashion. 'Nonstoic', placebo 'nonresponder' female volunteers (n = 30) were randomly assigned to receive 0.5 mg kg(-1) oral morphine sulphate, 0.5 mg kg(-1) oral oxycodone hydrochloride, and the combination of 0.25 mg kg(-1) morphine sulphate with 0.25 mg kg(-1) oxycodone hydrochloride, 1 week apart from each other, in a double-blind crossover design. Latency to pain onset (threshold), pain intensity (VAS), and pain tolerance (time until removal of the hand from the water) were measured six times over a 3-h period, subsequent to the administration of each medication, and were used to assess their antinociceptive effect. RESULTS: The combination produced a significantly higher effect on latency to pain onset than that of morphine alone [difference in mean postbaseline value 2.2; 95% confidence interval (CI) 0.48, 3.9; P = 0.01] but the effect was nonsignificantly smaller that that of oxycodone alone. Similarly, the effect of the combination on pain tolerance was significantly larger than that of morphine alone (combination difference 8.4; 95% CI 2.5, 14.3; P = 0.007), whereas oxycodone alone caused a nonsignificantly larger effect than that of the combination treatment. Comparisons of pain magnitude failed to show any significant differences between the three treatments. CONCLUSIONS: These results indicate that at the doses tested, morphine and oxycodone do not produce synergistic antinociceptive effects in healthy humans exposed to the CPT.

Adolescent↗

Diclofenac and oxycodone in treatment of postoperative pain: a double-blind trial.

The effects of a prostaglandin synthesis inhibitor (diclofenac, Voltaren) and an opiate (oxycodone, Oxanest) on postoperative pain were compared. Included in the study were 85 candidates for various operations. Patients requesting an analgesic were given either 75 mg of diclofenac or 10 mg of oxycodone as an intramuscular injection. The onset of analgesic effect occurred within 13 +/- 4 min with oxycodone and within 16 +/- 8 min with diclofenac. The analgesic effect of diclofenac was slightly weaker than that of oxycodone (on a pain scale of 1-4, 1.6/2.1 after 0.5 h and 1.5/1.8 after 1 h). The patients again asked for an analgesic after an average of 4.6 h in the oxycodone group and after an average of 6.1 h in the diclofenac group. The average number of injections required until the first postoperative morning was 2.5 in the oxycodone group and 1.8 in the diclofenac group. Side-effects: 21 patients in the oxycodone group reported a total of 39 side-effects and eight patients in the diclofenac group a total of 10 side-effects. Diclofenac is an alternative to opiates in the management of postoperative pain. It is especially useful in patients in whom opiates cause side-effects.

Adult↗

Buprenorphine as premedication and as analgesic during and after light isoflurane-N2O-O2 anaesthesia. A comparison with oxycodone plus fentanyl.

Sixty patients undergoing gynaecological laparotomies under isoflurane anaesthesia received 0.4 mg of buprenorphine sublingually or 0.12 mg/kg of oxycodone intramuscularly in random order for preanaesthetic medication. Patients premedicated with buprenorphine were given buprenorphine before, during and after anaesthesia and patients premedicated with oxycodone received fentanyl before and during anaesthesia and oxycodone after anaesthesia. Buprenorphine premedication produced less drowsiness and sedation and alleviated patients' apprehension significantly (P less than 0.05) less than oxycodone. Systolic and diastolic blood pressure and heart rate were significantly (P less than 0.05 to P less than 0.01) higher after intubation in the buprenorphine group when compared with the oxycodone plus fentanyl group. After anaesthesia, spontaneous respiration started rapidly; the return of consciousness and immediate recovery occurred at the same rate in both groups. In the recovery room moderate to severe pain was more common (P less than 0.05) in the oxycodone plus fentanyl group than in the buprenorphine group. The respiratory rate in the recovery room was lower among patients given buprenorphine, and two patients given buprenorphine developed severe respiratory depression. In the ward (2 to 24 h after operation) sublingual buprenorphine provided pain relief as good as intramuscularly administered oxycodone. No differences were noted in the incidence or severity of emetic symptoms between the groups. It is concluded that buprenorphine can provide good postoperative pain relief for gynaecological laparotomies performed under light isoflurane anaesthesia, but patients need to be monitored carefully after operation because of the possibility of respiratory depression.

Adult↗

Liposolubility and protein binding of oxycodone in vitro.

The liposolubility and protein-binding of oxycodone were studied in vitro and compared with other opioids. Liposolubility was assessed by three different methods: 1) the shake-flask method with n-octanol at pH 4-9, 2) measuring the retention time in reversed-phase high-performance liquid chromatography (RP-HPLC) with a LiChrosorb RP-18 and 3) studying the solubility in human epidural and subcutaneous fat. Human fat was obtained from patients undergoing surgery for herniated intervertebral disc. After incubation, pieces of fatty tissue immersed in a buffer solution containing oxycodone, morphine, pethidine or fentanyl for 10-40 min.; tissue pieces were homogenated, opioids extracted and opioid concentrations measured by gas- and high-performance liquid chromatography. The binding of oxycodone, morphine and fentanyl in plasma proteins was studied by ultrafiltration (Amicon-kit). The mean apparent partition coefficients Papp of oxycodone, morphine, pethidine and fentanyl in n-octanol at pH 7 were 0.7, 0.5, 10.5 and 399, respectively. The retention times in RP-HPLC for oxycodone, morphine, pethidine, fentanyl and buprenorphine were 0.6 min., 0.2 min., 2.4 min., 2.3 min. and 10.5 min., respectively. Only buprenorphine and fentanyl appeared to be highly lipophilic in the human fat tissue experiments; no difference was found between epidural or subcutaneous fat in this respect. The in vitro protein binding of oxycodone was 38%, of morphine 31% and of fentanyl 87% in average. It is concluded that, in terms of physiochemical properties, liposolubility and protein-binding, oxycodone resembles morphine more than it does fentanyl.

Adipose Tissue↗

Pharmacokinetics of oxycodone after intravenous, buccal, intramuscular and gastric administration in children.

OBJECTIVE: To evaluate the pharmacokinetics of four administration routes of oxycodone parenteral liquid (10 mg/mL), single intravenous and intramuscular injections and buccal and gastric administration, in children. PATIENTS AND PARTICIPANTS: Forty generally healthy children, aged 6-93 months, undergoing inpatient surgery. METHODS: After induction of anaesthesia, children received a single dose of oxycodone 0.1 mg/kg intravenously (n = 9), intramuscularly (n = 10), buccally (n = 11) or via an orogastric tube into the stomach (n = 10). Regular blood samples were collected up to 12 hours, and plasma was analysed for oxycodone using gas chromatography-mass spectrometry (limit of quantification 1 microg/L). RESULTS: The peak drug concentration observed was 57-110 (mean 82) microg/L after intravenous administration, 23-54 (34) microg/L after intramuscular administration, 3.9-14 (9.8) microg/L after buccal administration and 1.7-15 (9.2) microg/L after gastric administration. The time to peak concentration was 2-30 (16) minutes in the intramuscular group, 30-480 (221) minutes in the buccal group and 60-360 (193) minutes in the gastric group. The terminal elimination half-lives were closely similar in the four groups: 124-208 (163) minutes in the intravenous group, 162-227 (150) minutes in the intramuscular group, 73-234 (150) minutes in the buccal group and 80-246 (147) minutes in the gastric group. Area under the concentration-time curve (AUC) was 5037-8954 (6612) microg x min/L in the intravenous group, 3084-5524 (4473) microg x min/L in the intramuscular group, 1444-5560 (3658) microg x min/L in the buccal group and 692-3843 (2436) microg x min/L in the gastric group. The estimated bioavailability (AUC/mean intravenous AUC) of intramuscular oxycodone was 0.47-0.84 (0.68), that of buccal oxycodone 0.22-0.84 (0.55) and that of gastric oxycodone 0.10-0.58 (0.37). CONCLUSION: The pharmacokinetics of intravenous oxycodone in children aged 6-93 months are fairly similar to those reported in adults. Intramuscular administration provides relatively constant drug absorption, but after buccal and gastric administration the interindividual variation in the rate and extent of absorption is large.

Administration, Buccal↗

Comparison of oxycodone pharmacokinetics after buccal and sublingual administration in children.

OBJECTIVE: We evaluated and compared the pharmacokinetics of two oral administration routes of oxycodone parenteral liquid (10 mg/mL)--single buccal and sublingual administration--in 30 generally healthy awake children, aged 6-91 months. METHODS: Two groups of children undergoing inpatient surgery were enrolled. In a randomised fashion, children received a single dose of oxycodone 0.2 mg/kg buccally (n = 15) or sublingually (n = 15). Regular blood samples were collected for up to 12 hours, and plasma was analysed for oxycodone, oxymorphone and noroxycodone using gas chromatography-mass spectrometry. RESULTS: Bioavailability was similar after administration at the two instillation sites. The area under the plasma concentration-time curve from time zero extrapolated to infinity (AUCinfinity) was 2400-8000 ng x min/mL (median 4200 ng x min/mL) in the buccal group and 2700-7900 ng x min/mL (median 5500 ng x min/mL) in the sublingual group. After buccal administration, maximum plasma concentration (Cmax) was 5.4-39 ng/mL (16 ng/mL) after buccal and 5.5-42 ng/mL (22 ng/mL) after sublingual administration. Twelve of the 15 children in both groups reached the oxycodone analgesic concentration of 12 ng/mL, which was sustained for 43-209 minutes (median 160 minutes) in the children with buccal oxycodone and for 32-262 minutes (median 175 minutes) in the children with sublingual oxycodone. The terminal elimination half-lives were closely similar in the two groups: 104-251 minutes (median 140 minutes) in the buccal group and 110-190 minutes (150 minutes) in the sublingual group. CONCLUSION: The results of this study show that in young children the absorption of oxycodone is similar after buccal and sublingual instillation.

Administration, Buccal↗

Screening postmortem whole blood for oxycodone by ELISA response ratios.

The objective of this study was to investigate the accuracy of screening postmortem whole blood for oxycodone using the ratio of the oxycodone immunoassay response to the response for the specimen obtained with a general opiate-class immunoassay. Fifty eight specimens which were negative for opiates and 158 postmortem whole blood specimens positive for opiates including 66 specimens known to contain oxycodone were assayed. Specimens were diluted 1:5 with assay buffer and analyzed by both the Neogen Oxymorphone/Oxycodone ELISA and the Neogen Opiate Group ELISA (Neogen Corporation, Lexington KY). The oxycodone equivalents in ng/mL from the Oxymorphone/Oxycodone ELISA were divided by the morphine equivalents in ng/mL from the Opiates ELISA to obtain an Oxycodone/Opiates Response Ratio. This ratio was compared with the GC/MS data for all specimens and for opiate positive specimens. Receiver Operating Characteristic (ROC) analysis suggested that optimum relative response ratio was 2.0. The sensitivity of the ELISA response ratio for the presence of oxycodone at a response ratio cutoff of 2.0 was 89.4% +/- 3.8% and the specificity was 88.1% +/- 3.2%. Specimens with a ratio of 2.0 or higher had a greater than 50% probability (positive predictive value) of containing oxycodone in a population with a greater than 15% prevalence of oxycodone.

Analgesics, Opioid↗

The influence of pharmacogenetics on opioid analgesia: studies with codeine and oxycodone in the Sprague-Dawley/Dark Agouti rat model.

In the Sprague-Dawley (SD) rat, the O-demethylation of codeine to morphine is catalyzed by cytochrome P4502D1 (CYP2D1), which is absent in the female Dark Agouti (DA) rat. Oxycodone is similar in structure to codeine but, in contrast, has an analgesic potency in humans similar to morphine. The aim of the study was to test whether the DA rat and the SD rat pretreated with the CYP2D1 inhibitor quinine showed attenuation in analgesia to codeine and oxycodone. With the use of the tail flick model, dose-response curves were constructed to codeine, morphine, oxycodone and oxymorphone (the O-demethylated metabolite of oxycodone) in both rat strains. Codeine did not induce analgesia in the DA rat and there was a 60% reduction in codeine analgesia in the SD rat pretreated with quinine in comparison to the untreated SD rat. In the DA rat, the ED50 to oxycodone was increased 10-fold but there was a significant (P = .0001) prolongation in the duration of analgesia in comparison to that in the untreated SD rat. In the quinine-pretreated SD rat, there was no reduction in oxycodone analgesia but the duration of analgesia was also prolonged. It was concluded that 1) codeine-mediated analgesia requires the formation of morphine through the functional activity of CYP2D1 and 2) oxycodone-mediated analgesia may only be partly dependent on CYP2D1.

Analgesia↗