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PubMed1993

Inhibition by fluoxetine of cytochrome P450 2D6 activity.

Potent inhibition of cytochrome P450 2D6 (CYP2D6) in human liver microsomes by fluoxetine and its major metabolite norfluoxetine was confirmed (apparent inhibition constant values, 0.2 mumol/L). Several other serotonergic agents were also found to be competitive inhibitors of this genetically polymorphic enzyme. The O-demethylation ratio of dextromethorphan that expressed CYP2D6 activity in 19 patients receiving fluoxetine fell in the region of the antimode separating the O-demethylation ratio values observed in 208 extensive metabolizers from 15 poor metabolizers of a control group of healthy subjects. Inhibition of CYP2D6 activity in patients undergoing treatment with fluoxetine or other serotonin uptake inhibitors could contribute to toxicity or attenuated response from concurrent medications that are substrates of this enzyme. Other in vitro studies indicated that CYP2D6 catalyzes the O-demethylation of oxycodone to form oxymorphone. This reaction was inhibited by fluoxetine and its normetabolite in liver microsomes from both extensive and poor metabolizer individuals, indicating that these compounds are not selective inhibitors of CYP2D6 activity.

Adult↗

PubMed2002

OxyContin and neonatal abstinence syndrome.

Opioids are a commonly abused class of drugs. OxyContin abuse, a long-acting oxycodone derivative, has been increasingly identified as a potent narcotic resulting in drug dependence, overdose and even death. Use during pregnancy may result in withdrawal symptoms in the neonate. However, detection of the drug and its metabolites needs special methods in order to initiate appropriate therapy.

Analgesics, Opioid↗

PubMed2000

Kinetics and inhibition of the formation of 6beta-naltrexol from naltrexone in human liver cytosol.

AIMS: To determine the kinetics of the formation of 6beta-naltrexol from naltrexone in human liver cytosol, and to investigate the role of potential inhibitors. METHODS: The kinetics of the formation of 6 beta-naltrexol from naltrexone were examined in eight human liver cytosol preparations using h.p.l.c. to quantify 6 beta-naltrexol and, the extent of inhibition of 6 beta-naltrexol formation was determined using chemical inhibitors. The formation of 6 beta-naltrexol and the back reaction of 6 beta-naltrexol to naltrexone were also examined in a microsomal preparation. RESULTS: The Vmax, Km and CLint values for the formation of 6 beta-naltrexol from naltrexone were in the ranges of 16-45 nmol mg-1 protein h-1, 17-53 microM and 0.3-2.2 ml h-1 mg-1 protein, respectively. The steroid hormones testosterone (Ki = 0.3 +/- 0.1 microM) and dihydrotestosterone (Ki = 0.7 +/- 0.4 microM) were the most potent competitive inhibitors of 6 beta-naltrexol formation, with naloxone, menadione and corticosterone also producing > 50% inhibition at a concentration of 100 microM. The opioid agonists morphine, oxycodone, oxymorphone and hydromorphone, and a range of benzodiazepines showed < 20% inhibition at 100 microM. In the microsomal preparation, there was no formation of naltrexone from 6beta-naltrexol nor any formation of 6beta-naltrexol from naltrexone. CONCLUSIONS: The intersubject variability in the kinetic parameters of 6beta-naltrexol formation could play a role in the efficacy of and patient compliance with naltrexone treatment. This variability could be due in part to a genetic polymorphism of the dihydrodiol dehydrogenase DD4, one of the enzymes reported to be responsible for the formation of 6beta-naltrexol from naltrexone. DD4 also has hydroxysteroid dehydrogenase activity which could account for the potent inhibition by the steroid hormones testosterone and dihydrotestosterone. The clinical significance of the latter finding remains to be established.

Adult↗

PubMed2003

Effectiveness and safety of new oxycodone/acetaminophen formulations with reduced acetaminophen for the treatment of low back pain.

OBJECTIVE: To evaluate the analgesic effectiveness/safety of the new oxycodone 7.5- and 10-mg/acetaminophen 325-mg (Percocet) formulations in patients with low back pain (LBP) suboptimally responsive to nonsteroidal anti-inflammatory drugs, muscle relaxants, tramadol, cyclo-oxygenase-2 inhibitors, and/or prn opioids. DESIGN: Prospective, open-label, nonrandomized, 4-week trial. SETTING: Multicenter. PATIENTS: Thirty-three men and women (mean age: 52.2 years) with LBP (mean duration: 10.9 years). INTERVENTIONS: All prior analgesics were discontinued, and oxycodone/acetaminophen was dosed three times a day (TID), titrated to clinically meaningful pain relief. Initial oxycodone/acetaminophen dose: 2.5/325 mg TID; maximum: 20/650 mg TID. OUTCOME MEASURES: Effectiveness: Brief Pain Inventory (BPI) and Neuropathic Pain Scale 4 score (sharp, hot, dull, and deep pain). Quality of life: BPI and North American Spine Society Lumbar Spine questionnaire. SAFETY: Adverse events, physical/neurologic examinations, vital signs, and clinical laboratory tests. RESULTS: In all, 28 of 33 patients (85%) completed the study; discontinuations were for adverse events (N=3), patient choice (N=1), and lack of effectiveness (N =1). The mean oxycodone/acetaminophen dose at the end of treatment was 8.2/325 mg TID. After 4 weeks, treatment significantly reduced BPI pain intensity and improved pain relief (P < 0.0005), improved Neuropathic Pain Scale 4 score (P =0.007), reduced pain interference with quality of life (P < 0.0004), and reduced disability (P < 0.0001). Treatment was found to be safe and well tolerated. Adverse events were those most commonly expected from an opioid, and most were of mild-to-moderate intensity. CONCLUSIONS: The primary purpose of this study was to preliminarily test the effectiveness of the new formulations of oxycodone/acetaminophen with reduced acetaminophen in the clinical practice setting. The results from this trial suggest that these formulations are effective in the treatment of moderate-to-severe chronic LBP. Most patients (67%) reported significant pain relief/tolerable side effects with a TID dosing frequency or less (mean: 3.04 doses/day), suggesting chronic pain patients can experience meaningful pain relief with around-the-clock dosing of oxycodone/acetaminophen and minimal risk of hepatotoxicity. Further long-term, controlled studies of the efficacy/safety of the new formulations of oxycodone/acetaminophen in LBP are warranted to fully characterize efficacy in this patient population and corroborate the findings from our study.

Acetaminophen↗

PubMed2003

Supplemental oxygen is not required in trauma patients treated with IV opiates.

The risk of respiratory depression can prevent the proper use of opioids in trauma patients and lead to use of supplemental oxygen. However, high FiO(2) might contribute to atelectasis formation and consequently to relative hypoxia. Supplemental oxygen also can cause a risk of fire. In a randomized, controlled study we evaluated the need and effects of supplemental oxygen in 13 patients with extremity trauma who were treated pain-free with an intravenous opioid, oxycodone (dose range 6.75-13.6 mg). After opioid injection, 7 patients received 40% supplemental oxygen and 6 were breathing room air. Pulse oxygen saturation (SpO(2)), arterial blood gases, and hemodynamic parameters were monitored for 30 minutes. Atelectasis formation was evaluated with a computed tomography scan. No hypoxia, hypoventilation, or significant atelectasis formation was detected in any of the patients. Accordingly, routinely given supplemental oxygen was not considered necessary in these patients because no complications were seen.

Adult↗

PubMed2001

Opioid formulations: tailoring to the needs in chronic pain.

Opioids are one of the standard therapies used in the management of chronic pain. They were first widely adopted for the treatment of chronic pain associated with cancer and are now considered important in the alleviation of non-cancer and neuropathic pain. Around-the-clock (ATC) medication has been found to be an effective approach in treating chronic pain. Guidelines issued by the American Pain Society (1999) note that in most cases the preferred route of administering opioids is oral, because of convenience, flexibility, and relative steadiness of the opioid concentrations in the blood. The advantages of ATC therapy and oral medication are some of the reasons for the development of controlled-release, oral formulations of opioids (e.g. morphine, oxycodone, hydromorphone, and hydrocodone). The reduced dosing frequency makes the oral medication more convenient for patients, making it easier for them to comply with the dosing regimen. ATC therapeutic coverage and the possible increased compliance afforded by controlled-release formulations can make opioids even more effective in managing chronic pain.

Analgesics, Opioid↗

PubMed2005

Bedside femoral block performed on the first postoperative day after unilateral total knee arthroplasty: a randomized study of 49 patients.

This randomized study compared the effectiveness of a femoral nerve block with other methods of pain control on the first postoperative day after total knee arthroplasty. The femoral block consisted of a single injection administered at patients' bedside during the surgeon's hospital rounds. Compared with control group patients, femoral block patients reported less pain on a visual analog scale and required one half the amount of oxycodone (P = .021). Additional femoral block or continued epidural analgesia was required more frequently by control group patients. Thus, pain management with femoral blocks resulted in less work for nursing staff (P = .004). Performing a femoral nerve block as needed during the surgeon's hospital rounds is quick and requires minimal additional time without any special equipment. Bedside femoral block is a useful adjunct to other pain control methods following primary total knee arthroplasty.

Aged↗

PubMed2006

[Post-operative pain therapy of a chronic pain patient].

Post-operative pain therapy of chronic pain patients poses a challenge. Here we report the perioperative management of a 39-year-old male under chronic therapy with oxycodon, gabapentin and tolperison. Particular the pharmacointeractions regarding premedication and postoperative dose finding of opioids with intravenous PCIA are discussed.

Adult↗

PubMedDate not supplied

A solid phase extraction technique for the isolation and identification of opiates in urine.

A quantitative method was developed for the simultaneous analysis of morphine, codeine, hydromorphone, hydrocodone, and oxycodone in urine by gas chromatography/mass spectrometry. Samples were hydrolyzed with beta-glucuronidase and then extracted by solid phase extraction on Bond Elute Certify cartridges at pH 6.8. Nalorphine was used as the internal standard. The opiates were analyzed by full-scan electron impact GC/MS after derivatization with acetic anhydride-pyridine. The standard curves for all five drugs were linear between 50 and 1000 ng/mL, with correlation coefficients exceeding 0.99. Coefficients of variation were less than 7%. The method was applied to the analysis of postmortem urines positive by EMIT opiate assay, and the effect of the hydrolysis procedure on recovery of each drug was measured. The results indicate that the hydrolysis procedure is effective in increasing the recovery of all five drugs from urine. The described method enables the laboratory to identify the five opiates most commonly encountered in forensic and clinical laboratories. Its sensitivity for all five drugs is well below GC/MS cutoffs for codeine and morphine employed in NIDA laboratories, and it provides for conclusive full-scan drug identification.

Chemistry Techniques, Analytical↗

PubMedDate not supplied

Evidence of morphine metabolism to hydromorphone in pain patients chronically treated with morphine.

Minor metabolic pathways in human subjects have been shown to exist for the conversion of codeine to hydrocodone but have not been reported for the metabolic conversion of morphine to hydromorphone. In this study, urine specimens were collected in an out-patient setting from 13 pain patients who were chronically treated with morphine and other opioids (methadone, oxycodone, and fentanyl). The chronic pain patients were chosen for study because they were treated with high-dose morphine and had no personal or family history of addiction. Results of the initial evaluation and follow up of these patients with random urine tests did not indicate opioid misuse. The specimens were analyzed by GC-MS for the presence of hydromorphone. The reporting limit for hydromorphone was 100 ng/mL. Ten of the 13 morphine-treated patients excreted hydromorphone in minor amounts ranging 120 to 1400 ng/mL. Concurrent morphine concentrations were exceedingly high in these 10 patients and frequently exceeded the upper limit of linearity (> 10,000 ng/mL) of the assay. The ratio of hydromorphone to morphine ranged from 0.015 to 0.024. Morphine concentrations in the three patients in which hydromorphone was not detected tended to be lower than those observed in other patients. For comparison, one additional patient was included in the study, who was prescribed both morphine and hydromorphone. Concentrations of hydromorphone in this patient were in the range of 3400-13,000 ng/mL, while concurrent morphine concentrations were in the range of 3200-6600 ng/mL. These data are highly suggestive that hydromorphone can be produced as a minor metabolite of morphine in humans. Although additional studies in more restricted settings are needed, it is recommended that interpretation of low urinary concentrations of hydromorphone in combination with high concentrations of morphine in morphine-treated pain patients should not be considered as conclusive evidence of hydromorphone misuse.

Adult↗

PubMed1995

The effect of intrinsic efficacy on opioid tolerance.

BACKGROUND: The intrinsic efficacy of opioid analgesics has been suggested to play a role in the development of tolerance to these agents. However, the effect of differences in dosing protocol on tolerance to opioid analgesics of high or low efficacy has not been addressed. Therefore, the effect of opioid intrinsic efficacy on tolerance in mice was determined in protocols of continuous and intermittent administration of equieffective doses of opioid agonists. METHODS: Initial antinociceptive median effective doses (ED50s) for five opioid agonists that vary in intrinsic efficacy were estimated in untreated mice. Groups of mice received continuous infusions of morphine, fentanyl, or etorphine for 72 h or 7 days from osmotic minipumps implanted subcutaneously. The infusion doses were calculated as multiples of the initial antinociceptive ED50. An inert placebo was implanted subcutaneously in controls. At the end of treatment, the pumps and placebos were removed, and 4-24 h later, mice were tested in dose-response studies (tail flick) using the same drug that had been chronically administered. In another study using intermittent dosing, mice received subcutaneous injections every 24 h for 3 days of saline or morphine, etorphine, fentanyl, oxycodone, or meperidine, or received subcutaneous injections every 24 h for 7 days of saline or morphine, etorphine, or fentanyl. Daily doses were calculated as multiples of the initial antinociceptive ED50. Twenty-four hours after the last injection, mice were tested in dose-response studies. RESULTS: High-intrinsic-efficacy compounds (e.g., etorphine and fentanyl) produced less tolerance than a lower-intrinsic-efficacy drug (morphine) in 72-h and 7-day infusion studies. Tolerance for all compounds after intermittent treatment with equieffective doses was similar, and intrinsic efficacy had no effect on the magnitude of tolerance after intermittent dosing. CONCLUSIONS: These results indicate that the intrinsic efficacy of opioid analgesics is inversely related to the degree of tolerance after continuous infusion, but that intrinsic efficacy does not significantly affect tolerance after once-daily intermittent administration of these agents. These findings may be of clinical utility in understanding the development of tolerance to the antinociceptive effects of opioids.

Animals↗

PubMedDate not supplied

Acetaminophen, aspirin, or Ibuprofen in combination analgesic products.

Pain of multiple etiologies remains a substantial problem for many patients presenting in the clinical setting. Improved pain relief can be demonstrated, and adverse effects minimized, by multimodal analgesic combinations as the method to improve pain treatment. Substantial evidence supports combining analgesics for the management of pain and, in some instances, they have a heterogeneous pharmacologic sparing effect. Fixed-dose combination analgesics with demonstrated efficacy and safety are widely useful for pain management. However, work needs to continue to further explore which analgesics at which doses can be combined with a coanalgesic in a patient-specific manner to achieve additive, if not synergistic, multimodal pain relief with the fewest possible adverse consequences. Unsupervised consumption of over-the-counter drugs that contain acetaminophen, aspirin, or ibuprofen offers clinical challenges to both the patient and health care providers. Couple this often undisclosed over-the-counter medication consumption event with prescription medications, which many contain similar combination ingredients, and the potential for a therapeutic misadventure may precipitate. This article will address the safety and efficacy of acetaminophen, aspirin, and ibuprofen independently and in combination with currently available prescription dosage forms with a focus on pharmacology, pharmacotherapeutics, pharmacodynamics, and pharmacokinetics, including drug interactions at the CYP450 system. Patient-specific cautions are presented for opiate/opioid combinations, codeine, hydrocodone, oxycodone, and propoxyphene, and there is a discussion of COX I/COX II agents.

Acetaminophen↗

PubMed2006

The validity of the neuropathic pain scale for assessing diabetic neuropathic pain in a clinical trial.

OBJECTIVES: In controlled trials of analgesics for the treatment of neuropathic pain, the primary outcome variable is most often a measure of global pain intensity. However, because neuropathic pain is associated with a variety of pain sensations, the effects of analgesic treatments on different sensations could go undetected if specific pain qualities are not assessed. This study sought to evaluate the utility of assessing the multiple components of neuropathic pain in an analgesic clinical trial. METHODS: One hundred fifty-nine subjects with diabetes-related foot pain were randomly assigned to receive an active analgesic (controlled-release oxycodone) or matching placebo for 6 weeks. A multidimensional measure of neuropathic pain, the Neuropathic Pain Scale (NPS), was administered before, during, and after study treatment. RESULTS: Relative to placebo, the opioid analgesic produced statistically significantly greater decreases in global pain intensity, pain unpleasantness, and sharp, dull, and deep pain sensations. Responder analyses indicated a higher rate of responding to the opioid condition, relative to placebo, for intense, unpleasant, deep, and surface pain. The opioid analgesic did not significantly reduce hot, cold, itchy, or sensitive pain sensations compared with placebo in either analysis. CONCLUSIONS: These findings support the utility of the NPS for characterizing the multidimensional nature of the neuropathic pain experience and for detecting changes in neuropathic pain with treatment.

Adult↗

PubMed1984

Comparison of intramuscular analgesia, intercostal block, epidural morphine and on-demand-i.v.-fentanyl in the control of pain after upper abdominal surgery.

Eighty patients undergoing upper abdominal surgery were randomly allocated to four groups according to the postoperative pain treatment. All patients had a standardized balanced anaesthesia and for postoperative analgesia either intramuscular oxycodone and/or metamizol (IM), intercostal block with 0.5% bupivacaine (IC), epidurally 4 mg morphine (EM) or i.v. infusion of fentanyl 0.54-0.99 micrograms min-1 + on-demand boluses of 7.2-13.5 micrograms (ODAC) were given. The pain intensity 2 h postoperatively was similar in all groups, mean score ranging from 3.2-4.3 on a scale from 0-10. At 24 h also, when additional intramuscular analgesics had been administered if needed, the mean pain scores did not vary much; 2.4 in the ODAC group to 3.4 in the IC group. The time until the first request for additional analgesia was longer in the EM group than in the IM group (7.5 h vs. 3.5 h). There were no differences between the groups in chest X-ray, peak expiratory flow or respiratory rate postoperatively, but in the capillary blood-gas analyses there was a greater number of slightly elevated PCO2 values (6.0-7.3 kPa) in the ODAC group than in the others. The amount of fentanyl infused in 24 h to the ODAC patients varied considerably, 814-2233 micrograms, as did the number of on-demand boluses, 3-155. At 24 h, an efficacy rating "good" was distributed as follows: IM 9/20, IC 11/20, EM 11/20 and ODAC 13/20. In the whole patient material 92.5% rated their condition as "good" or "fair".

Abdomen↗

PubMed1992

Pain after thoracic surgery.

In order to evaluate postoperative pain treatment following thoracic surgery, 214 medical records of patients who were operated during 1986-1988 were examined. Nurses' comments concerning pain and the amounts of analgesics given during the 2 postoperative days were recorded. The 150 patients who were still alive in December 1989 were sent a postal questionnaire which asked about the pain and the efficacy of pain relief they had received after their operation. They were also asked if they still had pain which they connected to the thoracotomy and if any attempts had been made to treat that pain. The mean consumption of intramuscular oxycodone was 38 mg during the 1st and 33 mg during the 2nd postoperative day. The administration of nonsteroidal anti-inflammatory drugs significantly reduced the opioid consumption on the second but not on the first postoperative day. In 30% of the patients' charts there were no remarks on pain, in 10% there was a mention of no pain, in 40% pain was mentioned and in 20% the patient was reported to have severe pain. During the first postoperative week little pain was experienced by 60% of the patients, considerable pain by 35% and excruciating pain by 5% of the patients being interviewed. The postoperative pain relief was rated as good in 60% of the answers, satisfactory in 38% and poor in 2%. Persistent post-thoracotomy pain lasting for more than 6 months was reported by 44% of the patients, of whom 66% had received treatment for the pain.

Acute Disease↗

PubMed1994

Propofol vs isoflurane for gynaecological laparoscopy.

Propofol (n = 15) and isoflurane (n = 15), both administered by clinical and haemodynamic criteria, proved to be equally feasible as sole maintenance anaesthetics (combined with 0.5 mg alfentanil and suxamethonium) for gynaecologic laparoscopies. Two min postextubation, the number of patients awake and responsive to commands was higher in the group given propofol. Later recovery till 2 h postanaesthesia was similar for the groups, except that the propofol patients more frequently required oxycodone for pain relief, and that three of them (NS) were bradycardic. Emesis was rare in both groups. The rapid recovery without emesis qualifies these two anaesthetics for gynaecologic laparoscopies.

Adult↗

PubMed2005

Postoperative analgesic requirements - total laparoscopic hysterectomy versus vaginal hysterectomy.

BACKGROUND: There is limited information available on the requirement for postoperative analgesic drugs in patients submitted to total laparoscopic hysterectomy (TLH) compared with patients undergoing vaginal hysterectomy (VH). AIM: To compare the postoperative analgesic requirements in patients who underwent a TLH with patients who had a VH. METHODS: Chart review of 53 patients who had TLH and 47 who had VH and were seen postoperatively by an acute pain management service in order to assess postoperative analgesic requirements. Patient controlled analgesia (PCA) was part of the standard protocol for postoperative pain management. Analgesic requirement was recorded as the mean doses of morphine and number of days that patients used non-steroidal anti-inflammatory drugs (NSAIDs), oxycodone and tramadol. RESULTS: The requirement for total morphine was approximately half the dose in patients who had a TLH (10.8 +/- 12.6 mg) compared with patients who had a VH (19.4 +/- 21.9 mg) (P 0.017). The length of use of NSAIDs was significantly reduced in patients who had undergone a TLH (2.0 +/- 0.95 days) as compared with patients who had a VH (2.85 +/- 1.1 days) (P < 0.0001). CONCLUSIONS: Patients submitted to TLH require less postoperative analgesic drugs when compared with patients who had VH. Prospective randomised trials are warranted to compare analgesic requirements between patients submitted to TLH and VH.

Adult↗

PubMed1999

Transformations of codeine to important semisynthetic opiate derivatives by Pseudomonas putida m10.

A biotransformation mixture which contained codeine and washed cells of Pseudomonas putida M10 gave rise to a number of transformation products that are of clinical importance which included hydrocodone, dihydrocodeine and 14beta-hydroxycodeine. Incubations with the same organism and codeinone gave rise to 14beta-hydroxycodeinone and 14beta-hydroxycodeine. Cell-free extracts and membrane fractions of P. putida M10 were shown to catalyse the 14beta-hydroxylation of codeinone. In addition, the potent analgesic oxycodone was shown to be produced from 14beta-hydroxycodeinone.

Alcohol Oxidoreductases↗