Gene/Protein Disease Symptom Drug Enzyme Compound
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9,689 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The administration of single oral doses of delta-9-tetrahydrocannabinol (THC) to patients with cancer pain demonstrated a mild analgesic effect. At a dose of 20 mg, however, THC induced side effects that would prohibit its therapeutic use including somnolence, dizziness, ataxia, and blurred vision. Alarming adverse reactions were also observed at this dose. THC, 10 mg, was well tolerated and, despite its sedative effect, may analgesic potential.
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PMID:The analgesic properties of delta-9-tetrahydrocannabinol and codeine. 5 Jan 59

Fifty-one patients with moderate (11/51) and severe (40/51) cancer pain were given a new non-narcotic analgesic -Tromadol HCL capsule (THC). In 42 of these patients, partial relief was obtained with an average relief time (ART) of 4.1 hours. The average starting time was 58 minutes. Pain relief rate (PRR) in moderate and severe pain was 82% (P = 0.945), and the ARTs were 7.4 hr. and 3.2 hr., respectively (P = 0.005). In 43 patients who were entered into a randomized study with control drugs of AT-237 (36 cases) or Anfendein (7 cases), the PRR was 60.4% (26/43), ART was 1.3 hours. The PRR and ART of THC and control drugs were statistically significant (P less than 0.001 and P = 0.023). Within adequate dose range, increase of THC dose could improve its analgesic effect (P = 0.011). The main side-effects were: somnolence (37.3%), nausea (35.3%), dizziness (33.3%), palpitation and anorexia (25.5%) and constipation (9.8%) which did not necessitate the suspension of THC administration.
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PMID:[Pain-relief effect of tramadol HCL capsule for moderate and severe cancer pain]. 139 64

One hundred and three patients with moderate and severe cancer pain were given a sublingual analgesic agent--dihydroetorphine hydrochloride (DHE). Relief of cancer pain was moderate or complete in 89.3% (92/103). The average relief time (ART) was 3.9 hours and the average time before effectiveness was 20 minutes. In patients with acute or chronic cancer pain, moderate and complete pain-relief rates were 91.3% and 82.2% (P = 0.237). Difference of ART between them was insignificant (P = 0.299). The main clinical side-effects were somnolence (60%), dizziness (72%), nausea (30%), vomiting (16.5%), constipation (5%) and shortness of breath (8%). In two of the patients, the administration of DHE had to be stopped due to its side-effects. Age, sex and site of cancer pain were not related to the analgesic effects of DHE, but the pain-relief in patients with bladder cancer was poor (P less than 0.001). Within certain range, increase in dose was able to enhance its analgesic effect (P less than 0.001) and reduce drug resistance (P less than 0.001).
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PMID:[Dihydroetorphine hydrochloride for moderate and severe cancer pain]. 188 41

Twenty-eight cancer patients were treated with intramuscular butorphanol tartrate, a new non-narcotic analgesic, for investigating its clinical benefits in controlling cancer pain. Remarkable analgesic effects were observed approximately 30 minutes after administration by the single dose of either 1 or 2 mg of butorphanol. The effects lasted actively for 3 to 4 hours. Tolerance or drug dependency was rarely recognized even in the cases receiving repeated injections of the drug. Adverse effects, such as dizziness, nausea, thirst, numbness of the hands etc, observed in 5 patients were transient and required no medication. The above results may warrant a long-term administration of the drug for controlling varieties of pain in the cancer patients.
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PMID:[Clinical trial of butorphanol tartrate in cancer patients: evaluation for analgesic effects and safety on the basis of long term administration]. 634 86

Fourteen patients with chronic pain of malignant origin were treated with escalating doses of THIP intramuscularly 5-30 mg in an open phase 1 study. Analgesic activity was demonstrated in 60% of the patients at the level of 20 mg THIP and a dose response relation was present. Side effects, sedation, dizziness, euphoria, nausea, and blurred vision were present in up to 80% of the patients and were dose limiting. The maximum serum concentration was reached within 1 h after dosing in 87% of all administrations. Mean t1/2 was 1.52 +/- 0.63 h and the clearance was 0.49 +/- 0.181 min. Significant correlations were demonstrated between serum concentration, dose of THIP, analgesic effect and side effects. It is concluded that THIP cannot be used for the treatment of chronic cancer pain, not because of insufficient analgesic effect but because of unacceptable side effects.
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PMID:The analgesic effect of the GABA-agonist THIP in patients with chronic pain of malignant origin. A phase-1-2 study. 663 33

Flupirtine is a novel non-opiate centrally acting analgesic agent with muscle relaxant properties, advocated for use in a number of pain states. Preliminary evidence suggests that flupirtine 100 to 200mg orally or 150mg rectally 3 to 4 times daily (maximum daily dose 600mg) is more effective than placebo in relieving moderate acute pain of various types. For the relief of pain due to surgery, traumatic injury, dental procedures, headache/migraine and abdominal spasms, flupirtine has proved at least as effective as the opiate analgesics codeine, dihydrocodeine and pentazocine, the nonsteroidal anti-inflammatory agents suprofen, diclofenac and ketoprofen, as well as dipyrone and paracetamol (acetaminophen). Although evidence to support a role in the treatment of chronic pain is limited, flupirtine has been found as effective as pentazocine in short term trials of patients with muscular or neuralgiform pain, dysmenorrhoea, soft tissue rheumatism or cancer pain. The safety profile of flupirtine has not yet been fully established, although initial evidence suggests that adverse reactions, while frequent, are usually minor in nature. The most common reactions are drowsiness, dizziness, dry mouth and various gastrointestinal complaints. In comparison with opiate drugs, flupirtine appears to produce fewer central nervous system effects, no respiratory or cardiovascular depression, and no overt tolerance or physical dependence on prolonged administration. If these initially favourable results are confirmed in larger long term trials, then flupirtine would appear to represent an effective analgesic for the relief of moderate pain, particularly that of musculoskeletal origin.
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PMID:Flupirtine. A review of its pharmacological properties, and therapeutic efficacy in pain states. 768 75

Tramadol is a centrally acting analgesic which possesses opioid agonist properties and activates monoaminergic spinal inhibition of pain. It may be administered orally, rectally, intravenously or intramuscularly. In patients with moderate to severe postoperative pain, intravenous or intramuscular tramadol has generally proved to be of equivalent potency to pethidine (meperidine) and one-fifth as potent as nalbuphine. Intravenous tramadol 50 to 150mg was equivalent in analgesic efficacy to morphine 5 to 15mg in patients with moderate pain following surgery; however, when administered epidurally tramadol was one-thirtieth as potent as morphine. Tramadol has demonstrated efficacy in a few studies in the short term treatment of chronic pain of various origins. Orally administered tramadol was found to be an effective analgesic in step 2 of the World Health Organization's guidelines for the treatment of patients with cancer pain. Tramadol is well tolerated in short term use with dizziness, nausea, sedation, dry mouth and sweating being the principal adverse effects. Respiratory depression has been observed in only a few patients after tramadol infusion anaesthesia. When used for pain relief during childbirth, intravenously administered tramadol did not cause respiratory depression in neonates. The tolerance and dependence potential of tramadol during treatment for up to 6 months appears to be low, although the possibility of dependence with long term use cannot be entirely excluded. Thus, evidence to date of the analgesic effectiveness of tramadol combined with a low respiratory depressant effect and low dependence potential in short term use, suggests that the drug may become a useful alternative to the opioid analgesics currently available for the treatment of patients with moderately severe acute or chronic pain.
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PMID:Tramadol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute and chronic pain states. 769 19

Two separate trials compared controlled-release (CR) oral oxycodone (administered every 12 hours) with immediate-release (IR) oxycodone (4 times a day) to determine whether patients with chronic pain could be titrated to stable pain control as readily with the CR as with the IR formulation. In one study, 48 patients with cancer pain were randomized to open-label titration with either CR or IR oxycodone (maximum dose, 400 mg/day) for a period of up to 21 days. In a study of similar design, 57 patients with low back pain were titrated with either CR or IR oxycodone (maximum dose, 80 mg/day) for a period of up to 10 days. The majority of patients in both studies were converted to oxycodone from other opioid analgesics. Results of both studies showed no difference between CR and IR oxycodone with respect to both the percentage of patients achieving stable pain control, the time to achieve stable pain control, and the degree of pain control achieved. Among cancer patients, 85% achieved stable analgesia, 92% with the CR formulation and 79% with the IR formulation. Among noncancer patients, 91% achieved stable pain control, 87% with the CR formulation and 96% with the IR formulation. The most commonly reported adverse effects in both studies were similar for the two formulations and were those anticipated with opioids: nausea, vomiting, constipation, somnolence, dizziness, and pruritus. Nausea and vomiting were the most frequently cited reasons for treatment discontinuations. These studies suggest that dose titration can be accomplished as readily with oral CR oxycodone as with IR oxycodone in patients with chronic, moderate to severe pain.
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PMID:Can a controlled-release oral dose form of oxycodone be used as readily as an immediate-release form for the purpose of titrating to stable pain control? 1053 67

Patients with moderate to severe cancer pain and insufficient pain relief from nonopioid analgesics were treated with slow-release tramadol for initial dose finding and as a long-term treatment. Immediate-release tramadol was provided for the treatment of breakthrough pain and a standard nonopioid analgesic (1000 mg naproxen daily) was given as suggested for step 2 of the WHO analgesic ladder. Ninety of 146 patients (62%) completed the 6-week trial period. Drop-outs were due to adverse events (20%), inadequate pain relief (9%), or both (2.5%), death due to the underlying disease (4%), low patient compliance (2%) or other reasons. Average and maximal pain intensity decreased from day 1 to day 4. The number of patients with good and complete pain relief increased from 43% after week 1 to 71% after week 6 with maximum daily doses of tramadol up to 650 mg. However, 70% of the patients still needed less than 400 mg tramadol per day in week 6. Most patients (86%) experienced adverse events during the study period. Some common side effects of opioids, such as fatigue, dizziness, and constipation, decreased in frequency over the 6 weeks. The frequency of other adverse events such as nausea, vomiting and sweating did not change. Slow-release tramadol provided fast and efficient pain relief in almost two-thirds of patients both during initial dose finding and during long-term treatment, improving treatment options in step 2 of the WHO analgesic ladder.
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PMID:Slow-release tramadol for treatment of chronic malignant pain--an open multicenter trial. 1114 43

Oral transmucosal fentanyl citrate (OTFC); Actiq) is a drug delivery formulation used for management of breakthrough cancer pain. Previous studies with open-label comparisons indicated OTFC was more effective than patients' usual opioid for breakthrough pain. The objective of this study was to compare OTFC and morphine sulfate immediate release (MSIR) for management of breakthrough pain in patients receiving a fixed scheduled opioid regimen. This double-blind, double-dummy, randomized, multiple crossover study was conducted at 19 US university- and community-based hospitals and clinics and comprised 134 adult ambulatory cancer patients. Patients were receiving a fixed scheduled opioid regimen equivalent to 60-1000 mg/day oral morphine or 50-300 microg/h transdermal fentanyl, were using a 'successful' MSIR dose (15-60 mg) as defined by entry criteria, and were experiencing 1-4 episodes of breakthrough pain per day. In open-label fashion, OTFC was titrated such that a single unit (200-1600 microg) provided adequate pain relief with acceptable side effects. Successfully titrated patients entered the double-blind phase of the study and received ten prenumbered sets of randomized capsules and oral transmucosal units. Five sets were the successful OTFC dose paired with placebo capsules, and five sets were placebo OTFC paired with capsules containing the successful MSIR dose. Patients took one set of study medication for each episode of target breakthrough pain. Pain intensity (PI), pain relief (PR) and global performance of medication (GP) scores were recorded. Pain intensity differences (PID) were calculated and 15-min PID was the primary efficacy variable. Adverse events were recorded. Sixty-nine percent of patients (93/134) found a successful dose of OTFC. OTFC yielded outcomes (PI, PID, and PR) at all time points that were significantly better than MSIR. GP also favored OTFC and more patients opted to continue with OTFC than MSIR following the study. Somnolence, nausea, constipation, and dizziness were the most common drug-associated side effects. In conclusion, OTFC was more effective than MSIR in treating breakthrough cancer pain.
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PMID:Breakthrough cancer pain: a randomized trial comparing oral transmucosal fentanyl citrate (OTFC) and morphine sulfate immediate release (MSIR). 1124 84


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