Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The three-step analgesic ladder, originally proposed for cancer pain relief by the World Health Organization (WHO), is now widely employed for all types of pain, including the chronic pain of musculoskeletal disease. Tramadol, an analgesic with weak opioid receptor affinity and possessing monoaminergic activity, has proved suitable for use at Step 2 of the WHO ladder. Owing to its pharmacological properties, tramadol is more appropriate than NSAIDs for patients suffering from gastrointestinal and renal problems. Importantly, the analgesic potency of tramadol is greater than that of NSAIDs and of other weak opioids (codeine, dextropropoxyphene). It also causes fewer opioid-type adverse effects, e.g. nausea, drowsiness, vomiting, dry mouth and constipation. In chronic musculoskeletal pain it is recommended that tramadol should be given by mouth and by the clock; the initial dose should be titrated upward gradually to reach the individual level required for suitable pain control. This dosage strategy will also minimise the usual opioid-type adverse effects encountered with tramadol. Four recent publications are reviewed to illustrate the efficacy of tramadol, alone or in conjunction with an NSAID, in the management of low back pain, osteoarthritis pain and breakthrough pain.
 ...
PMID:Tramadol in musculoskeletal pain--a survey. 1195 1

(1) Some cancer patients suffer occasional breakthrough pain despite well-conducted opiate treatment, warranting the use of immediate-release oral morphine. (2) A fentanyl preparation for oral transmucosal administration has just been granted this indication in France. (3) The evaluation file mainly contains results from a randomised double-blind cross-over trial comparing transmucosal fentanyl with oral morphine tablets in cancer patients. It showed a small gain in terms of rapidity and efficacy of pain relief with fentanyl relative to morphine, but this was of dubious clinical relevance. (4) The adverse effects of oral transmucosal fentanyl are those of all opiates, such as drowsiness, dizziness, nausea, vomiting and confusion. (5) The oral transmucosal fentanyl preparation has the taste and appearance of a lollipop, and may therefore be attractive to children. The packaging seems to take this risk into account, but precautions must be taken to keep this treatment away from children, especially after opening. (6) Immediate-release oral morphine remains the standard treatment for breakthrough pain in patients receiving opiate therapy. If it is inadequate, oral transmucosal fentanyl may sometimes be slightly better.
 ...
PMID:Oral transmucosal fentanyl: new preparation. For breakthrough cancer pain when morphine fails. 1219 62

Breakthrough pain in patients with cancer is common, often unpredictable, and can rapidly become severe. Treatment using the oral administration of opioids is not optimal due to the slow onset of pain relief. Nasal administration of analgesics potentially offers more rapid pain relief. This study investigates the tolerability and efficacy of a novel morphine-chitosan formulation. Twenty episodes of breakthrough pain were observed in 14 patients with cancer who received 5-80 mg of nasal morphine-chitosan. Nasal symptoms, sedation, giddiness, nausea, and other volunteered symptoms, along with pain scores (pain intensity and pain relief), were recorded at baseline and at regular intervals up to 4 hours after administration, together with an overall satisfaction rating. The formulation was acceptable to patients, generally well tolerated, and had an onset of pain relief 5 minutes after dosing. This formulation warrants further study.
 ...
PMID:Pilot study of nasal morphine-chitosan for the relief of breakthrough pain in patients with cancer. 1255 10

We compared the efficacy of rofecoxib and ketorolac in controlling postoperative pain after outpatient surgery. Patients were randomly assigned to receive either rofecoxib or ketorolac preoperatively and every morning for 5 postoperative days. Patients in both groups received oxycodone as needed for breakthrough pain. After 5 postoperative days, patients were asked for information-pain score; number of supplemental analgesics used; and severity of any incision-site bleeding, nausea, or diarrhea. Rofecoxib and ketorolac did not differ on these measures. Rofecoxib and ketorolac are equally effective in controlling postoperative pain.
 ...
PMID:Comparison of efficacy of oral rofecoxib and ketorolac in controlling early postoperative outpatient orthopedic surgical pain. 1554 Aug 52

Sixty-six patients with cancer-related pain entered an open multicentre study to examine the safety and efficacy of oral transmucosal fentanyl citrate (OTFC) in the treatment of breakthrough pain. Patients were eligible for the study if they were stabilized on a long-acting opioid but were experiencing up to four episodes of breakthrough pain a day and achieving at least partial relief from breakthrough pain using conventional medication (normal release oral morphine in the majority of patients). The efficacy of the conventional medication was documented in a run-in phase and patients then changed to OTFC. All patients were treated initially with a 200 mcg unit of OTFC and the dose was increased if necessary to a level that produced relief of breakthrough pain without troublesome adverse effects. Fifty-eight patients completed the run-in phase using their usual medication and entered the dose titration phase with OTFC and 57 patients received at least one dose of OTFC. Forty-two patients (72%) found a successful dose of OTFC. The primary outcome measures were the Summed Pain Intensity Differences (SPID) and Total Pain Relief (TOTPAR) scores at 60 min. There was a significant difference in both measures in favour of OTFC compared with conventional medication in these patients. Twenty-eight of the 42 patients (67%) preferred OTFC to their usual medication. The most common adverse effects attributed to OTFC were nausea, stomatitis, vomiting and dizziness but there were no unpredicted or severe problems. Thirty-seven patients continued into the long-term study and 12 of these completed six months treatment. Most drop-outs in this phase were associated with progression of the underlying disease. No patient stopped using OTFC because of dissatisfaction with the drug. OTFC appears to be a safe and effective treatment for breakthrough pain in cancer patients and may have advantages over currently available opioid formulations.
 ...
PMID:Oral transmucosal fentanyl citrate in the management of breakthrough pain in cancer: an open, multicentre, dose-titration and long-term use study. 1562 66

In this randomized, controlled, dose-ranging study, we evaluated the analgesic efficacy of a novel single-dose extended-release epidural morphine (Depodur) in patients undergoing lower abdominal surgery. Five-hundred-forty-one patients were randomly assigned to one of six epidural treatments administered approximately 30 min before surgery. The 6 treatments were 5 mg of standard epidural morphine sulfate (MS) (active comparator); 5 mg of single-dose extended-release epidural morphine (EREM) (dose control); and 10, 15, 20, and 25 mg of single-dose EREM. The main study objective was to assess the efficacy of single-dose EREM 10, 15, 20, or 25 mg versus single-dose EREM 5 mg for the management of postoperative pain. This was done by plotting a linear dose-response relationship to assess postoperative IV patient-controlled analgesia (PCA) fentanyl consumption for breakthrough pain for 48 h after surgery. Secondary safety and efficacy analyses compared the 10-, 15-, 20-, and 25-mg single-dose EREM groups with the 5-mg single-dose EREM group and compared each single-dose EREM group with 5 mg of MS. As shown by the dose-response relationship, there was a dose-related reduction in the use of postoperative IV fentanyl through 48 h (estimated slope, -22.2; P = 0.0002). Patients treated with 10, 20, and 25 mg of single-dose EREM used significantly less IV fentanyl (mean +/- sd: 995 +/- 987 microg, P = 0.0446; 972 +/- 982 microg, P = 0.0221; and 683 +/- 620 microg, P < 0.0001, respectively) through 48 h after surgery compared with the 5-mg single-dose EREM group (1218 +/- 894 microg). At 48 h postdose, significantly more single-dose EREM patients (13%) than MS patients (2%) had required no IV fentanyl (P < 0.01). Although all treatment groups had access to PCA fentanyl and there was more frequent PCA fentanyl use in the MS group, patients in the single-dose EREM 15, 20, and 25 mg groups reported significantly lower pain-intensity scores and greater satisfaction with their pain relief. Overall, single-dose EREM was well tolerated, with 97% of adverse events rated as mild to moderate. As expected, the adverse events reported were consistent with those of other epidural opioids (i.e., nausea, vomiting, pruritus, and hypotension). In conclusion, this controlled study demonstrated that single-dose EREM can provide up to 48 h of postoperative analgesia, but supplementation for breakthrough pain is still required in most patients. Within the context of this study, the side effect profile of single-dose EREM was acceptable and predictable.
 ...
PMID:A comparison of Depodur, a novel, single-dose extended-release epidural morphine, with standard epidural morphine for pain relief after lower abdominal surgery. 1578 24

The physiochemical characteristics of the potent synthetic opioid agonist fentanyl make it ideal for noninvasive transmucosal delivery. Studies of oral transmucosal fentanyl citrate (OTFC), a candied matrix formulation administered orally as a palatable lozenge on a stick, have investigated and determined this analgesic's pharmacokinetics and pharmacodynamics in a number of clinical settings, including premedication before surgery, acute analgesia for painful medical procedures, and, most recently, for the control of breakthrough cancer pain. The onset to meaningful pain relief in patients with acute pain from surgery or breakthrough pain from cancer is between 5 and 10 minutes after initiating OTFC use, equivalent to intravenous morphine. Analgesic dose equivalency studies suggest that OTFC is, on average, about 10 times more potent than morphine, although, in randomized, controlled, and blinded studies, many patients who were using relatively high doses of opioid anlagesics on an around the- clock schedule for control of cancer pain reported that even a low dose of OTFC (i.e., 200 microg) provided adequate relief from breakthrough pain. Side effects from OTFC are similar in character and frequency to other opioids, including sedation, nausea, and pruritus. These effects appear to wane rapidly with repeated use of this medication. To date there have been no reported serious adverse events in any of the population groups studied or treated with OTFC.
 ...
PMID:A review of oral transmucosal fentanyl citrate: potent, rapid and noninvasive opioid analgesia. 1585 72

Drugs are indispensable for the management of symptoms in palliative care patients, and account for a significant proportion of expenditures on a Tertiary Palliative Care Unit (TPCU). Drug expenditures for Edmonton's TPCU increased by 40% in 2002 compared to 2001. Fifty-five percent of the increase was attributable to injectable fentanyl, oral and injectable ondansetron, and total parenteral nutrition (TPN). As there was no increase in the unit cost of these drugs between 2001 and 2002, the increased expenditures reflected increased utilization. The hypothesis of this study was that the increased utilization of these drugs reflected appropriate prescribing. The objective was to compare the indications for prescribing these drugs in 2002 against evidence- and consensus-based criteria. Patients who received these drugs while admitted to the TPCU from January 1 to December 31, 2002 were identified through the pharmacy database. Evidence- and consensus-based criteria for drug utilization were developed. Prescribing indications were retrospectively compared against the criteria. Drug prescriptions were categorized as follows: (1) meeting criteria, (2) not meeting criteria, or (3) uncertain. The drugs under study were prescribed during 48 out of 234 admissions to the TPCU in 2002. Prescriptions for fentanyl met criteria in 26 of 29 cases. Indications were unsuccessful therapy with morphine, hydromorphone, and oxycodone (20), requirement for rapid titration from fentanyl patch (5), renal failure (2), and sublingual administration for breakthrough pain (1). Prescriptions for ondansetron met criteria in 19 of 21 cases. Indications were nausea refractory to metoclopramide and dexamethasone (13), and nausea related to radiotherapy or chemotherapy (6). Prescriptions for TPN met criteria for initiation in only one of five cases. However, in all cases, TPN had been started prior to admission. In cases where death was considered imminent, TPN was continued pending consultation with the patient and family regarding discontinuation. These data indicate that the increased prescribing of fentanyl and ondansetron on the TPCU satisfied evidence- and consensus-based criteria in most cases, apparently justifying the associated increase in drug expenditures. This type of analysis may be useful whenever increased drug utilization requires review. A cost effectiveness analysis would be the next step in evaluating the costs vs. the benefits. The issue of discontinuing TPN in palliative care patients requires further investigation.
 ...
PMID:Drug utilization review on a tertiary palliative care unit. 1671 76

Tramadol, a centrally acting analgesic, consists of two enantiomers, both of which contribute to analgesic activity via different mechanisms. (+) Tramadol and the metabolite (+) -O- desmethyl-tramadol (M1) are agonists of the mu opioid receptor. (+) Tramadol also stimulates presinaptic release of serotonin and inhibits serotonin reuptake whereas (-) tramadol inhibits norepinephrine reuptake. Thus tramadol enhances inhibitory effects on pain transmission both by opioid and monoaminergic mechanisms. The complementary and synergistic actions of the two enantiomers improve the analgesic efficacy and tolerability profile of the racemate. Following oral administration the bioavailability of tramadol is high and with new slow release preparations twice daily administration enables effective pain control. The recommended maximum daily dose of tramadol is 400 mg/day. Tramadol is characterised by low plasma protein binding and quite extensive tissue distribution. Elimination is primarily by the hepatic route (metabolism by CYP2D6) and partly by the renal route. It is effective in different types of moderate-to-severe acute and chronic pain, including neuropathic pain, low back pain, osteoarthritis pain and breakthrough pain. It also causes fewer opioid-type adverse effects, e.g. nausea, drowsiness, vomiting, dry mouth and constipation. Although trials in literature demonstrate immune-stimulating effects of tramadol, there are also trials suggesting immunesuppressive effects that are lesser than morphine. Owing to its pharmacological properties, tramadol is more appropriate than NSAIDs for patients suffering from gastrointestinal and renal problems. Besides its proven clinical efficacy tramadol is a safe drug as respiratory depression, cardiovascular side effects, drug abuse and dependence are of minor clinical relevance, unlike some other opioids.
 ...
PMID:[An atypical opioid analgesic: tramadol]. 1678 63

Fentanyl buccal tablets (FBT) are designed to manage the breakthrough pain associated with chronic pain with an enhanced rate and extent of fentanyl absorption through the buccal mucosa. The formulation incorporates an effervescent reaction to produce large shifts in pH that enhance absorption. Results from studies of safety and tolerability have shown FBT to be effective and well tolerated in opioid-tolerant chronic pain patients. Adverse events were similar to those seen with other opioids and included nausea and somnolence. Adverse events were common but mild or moderate in most cases and did not cause a high drop-out rate. In addition to the treatment of breakthrough pain, FBT could be clinically efficacious for the treatment of brief, anticipated painful events. The abuse liability of FBT is unknown and caution should be used in prescribing FBT to patients with histories of substance abuse.
 ...
PMID:Fentanyl buccal tablets. 1704 Feb 4


<< Previous 1 2 3 4 Next >>