Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0030193 (pain)
261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Dezocine is an agonist-antagonist opiate that acts at the mu receptor, and is used for management of pain. Monkeys will readily press a lever to receive an injection of dezocine, and in former opiate addicts dezocine produces positive subjective effects similar to those of morphine. It is not clear, however, what its subjective effects are in people who do not have a history of opiate abuse. To answer this question, a within-subjects design was used in which 10 normal healthy volunteers (six men, four women) were injected with 0, 2.5, 5.0, and 10 mg/70 kg of dezocine in a double-blind fashion. Subjects completed several questionnaires (e.g., Addiction Research Center Inventory) commonly used in abuse liability testing before and at periodic intervals for up to 5 h after drug injection. We also assessed psychomotor performance (e.g., eye-hand coordination) and several physiologic measures (e.g., pupil size, respiration rate) at these times. Dezocine produced increases in ratings of drug liking (P less than 0.001), as well as other subjective effects that might be considered as pleasant ("good mood," "drunken," "coasting," "happy" ratings) (all P less than 0.05). At the same time, the drug had effects (increased dysphoria and sedation) that typically are not reported by addicts. Dezocine produced psychomotor impairment and miosis (constriction of the pupils) in a dose-dependent fashion. The observation that dezocine produces euphoria and increased drug-liking ratings in individuals without histories of drug abuse suggests that hospitals and surgicenters should have strict accountability procedures with this drug.
...
PMID:Subjective, behavioral, and physiologic responses to intravenous dezocine in healthy volunteers. 134 68

Dezocine is an analgesic agent with opioid agonist and antagonist activity. After parenteral administration of therapeutic doses it is approximately equipotent with morphine, and has proved at least as effective an analgesic as morphine, pethidine (meperidine) and butorphanol in moderate to severe postoperative pain. However, preliminary pharmacodynamic data indicate that the ceiling of analgesic activity of dezocine occurs at a higher level of analgesia than that of reference agonist/antagonist agents. Also, the drug exhibited a morphine-like degree of anaesthetic-sparing activity in animals. Although long term data are very limited, single doses of dezocine are well tolerated, with mild and transient sedation and gastrointestinal upset the principal adverse effects. As with some other agonist/antagonist analgesics, a 'ceiling' effect to dezocine-induced respiratory depression occurs with increasing dosage, beyond which further depression has not been observed. In single analgesic doses, however, dezocine is a slightly more potent respiratory depressant than morphine. Clinically important haemodynamic changes have not been observed with usual analgesic doses of dezocine. As an agonist/antagonist opioid, the dependence liability of dezocine would be expected to be lower than that of pure agonist opioids, but extended clinical use is required before more definitive conclusions can be drawn in this regard. Unlike older drugs of its type, dezocine produced opiate-like subjective effects and was identified as morphine-like by drug abusers. Thus, provided the promising conclusions of currently available clinical studies are confirmed with its wider use, dezocine should be a useful additional agent for the treatment of moderate to severe postoperative pain.
...
PMID:Dezocine. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. 267 May 17

Dezocine, a new mixed agonist-antagonist-type opioid analgesic, was compared in a double-blind trial with placebo and 10 mg of morphine in 190 patients with acute postoperative pain. The medications were given intramuscularly. Dezocine was administered at three dose levels (5, 10, and 15 mg). Pain relief scores, sedation, and side effects were recorded at 15, 30, 60, 120 and 240 min after injection. Significantly higher pain relief scores (p less than 0.05) were reported for the groups receiving dezocine 10 and 15 mg than the placebo group at all observation times, except for dezocine 15 mg at four hours. Morphine produced significantly better pain relief than placebo only between the second and fourth hour after administration. Significantly better pain relief was obtained with dezocine (10 and 15 mg) than with morphine during the first hour. The mean four-hour cumulative pain relief scores (TOTPAR) were significantly (p less than 0.05) higher than placebo for all active treatment groups. Side effects were few with no significant differences between the treatment groups. Seventy-nine per cent of the patients in the dezocine 15 mg group, and 73, 68, 58 and 50 per cent respectively, of the patients in the dezocine 10 mg, dezocine 5 mg, morphine 10 mg and placebo group had a satisfactory clinical response. Significantly (p less than 0.05) more patients in the groups receiving dezocine 10 and 15 mg than in the placebo group had a satisfactory clinical response; the difference was not significant for the dezocine 5 mg and morphine 10 mg groups.(ABSTRACT TRUNCATED AT 250 WORDS)
...
PMID:Double-blind placebo-controlled comparison of dezocine and morphine for post-operative pain relief. 286 30

Dezocine, a new mixed agonist-antagonist opioid analgesic, and morphine were compared in a double-blind study in 206 patients with postoperative pain. The analgesic efficacy of single intravenous injections of dezocine (2.5, 5.0, and 10.0 mg), morphine (5.0 mg), and placebo was assessed by verbal and visual scales at regular intervals for six hours after administration. All active treatments provided greater pain relief than placebo. Pain relief with dezocine 5 and 10 mg was significantly greater (P less than .05) than with placebo for up to four and five hours, respectively, and with morphine up to one hour. Pain relief scores were significantly higher (P less than .05) with morphine than with placebo at all observations except that of the fifth hour, and higher with dezocine 2.5 mg than with placebo for the first 30 minutes. Doses of 5 and 10 mg of dezocine produced approximately the same peak analgesic effect, with the larger dose having a longer duration of effect. All active treatments produced mild to moderate sedation. Side effects were few and mild or moderate with all of the treatments. The physician's and the patients' evaluations favored dezocine in a dose-dependent order, with morphine 5 mg rated lower than dezocine 5 mg and higher than dezocine 2.5 mg.
...
PMID:Intravenous dezocine for postoperative pain: a double-blind, placebo-controlled comparison with morphine. 287 Oct 49

Sixty hospitalized subjects with chronic moderate to severe pain as a result of advanced cancer were enrolled in a randomized, parallel, double-blind trial comparing single doses and multiple doses of intramuscular dezocine (10 mg) with butorphanol (2 mg) and placebo. During the initial 6-hour efficacy evaluation, analgesia was measured using verbal and visual scriptors and vital signs, and acute toxicity information was recorded. Subjects with initial pain relief entered the 7-day multidose portion of the trial, and efficacy and toxicity data were recorded daily. After the initial dose the peak analgesia of the active agents was similar, but the duration of analgesia was longer with dezocine. After multiple doses, dezocine was superior to butorphanol in terms of length of treatment. Dezocine had less toxicity than had butorphanol after both single and repeated doses, further suggesting that dezocine may be beneficial in managing chronic cancer pain. The described study design is unique in that it compares the analgesic efficacy and toxicity of several analgesics with placebo after both single and multiple doses in the same subject. This method may prove to be an alternative pain model to evaluate chronic cancer pain.
...
PMID:Comparison of intramuscular dezocine with butorphanol and placebo in chronic cancer pain: a method to evaluate analgesia after both single and repeated doses. 330 Nov 54

The respiratory depressant and analgesic effects of intravenous dezocine were evaluated in six healthy volunteers. Single 0.15 mg/kg doses were compared with identical amounts of morphine, and the two drugs were given in combination. Five successive 0.15 mg/kg doses of dezocine also were given to identify dose-effect relationships. Respiratory center sensitivity was monitored by carbon dioxide (CO2) rebreathing and mouth occlusion pressure (P0.1) measurement, while analgesia to experimental pain was tested with submaximal tourniquet ischemia. Single 0.15 mg/kg doses of dezocine produced significantly more tolerance to experimental pain and greater respiratory depression than a comparable dose of morphine in the first hour, but effects of both drugs were similar thereafter. Multiple doses of dezocine progressively increased pain tolerance from 46 +/- 14% above control with the first dose to 70 +/- 18% above control with the second dose (cumulative total 0.30 mg/kg). Additional dezocine doses did not result in significantly more analgesia. Depression of CO2 sensitivity followed a similar pattern. Morphine 0.15 mg/kg, when given to subjects who had received a prior dose of dezocine, produced no additional effect beyond that observed with dezocine. With the reverse sequence, dezocine increased the respiratory depression of morphine but also produced a dramatic increment in analgesia, which suggested an additive action. Dezocine is therefore an effective analgesic with morphine-like effects. In human subjects it appears to be a slightly more potent analgesic than morphine in identical clinical doses (0.15 mg/kg). Dezocine is similar to other agonist-antagonist analgesics in that it exhibits a ceiling effect for respiratory depression that parallels its analgesic activity.
...
PMID:Ventilatory and analgesic effects of dezocine in humans. 615 Jun 61

We assessed the analgesic effectiveness of a single intramuscular injection of dezocine, 10 mg or 15 mg; morphine, 10 mg; or a placebo in 160 patients with moderate to severe postoperative pain. Dezocine, 10 mg, was as effective as and had approximately the same duration of action as morphine, 10 mg. Dezocine, 15 mg, was more effective than 10 mg of either dezocine or morphine as assessed by three efficacy scales (verbal and analog pain intensity and pain relief), and both drugs were significantly (p less than 0.05) more effective than placebo as assessed by the three efficacy scales and the overall evaluation of the investigator. A small percentage of patients suffered nausea and became sedated; the drugs and placebo, however, did not differ statistically with respect to the side effects. Blood pressure, heart rate, and respiratory rate generally were slightly decreased by both drugs.
...
PMID:Dezocine for postoperative wound pain. 638 79

Dezocine (Wy 16225), a new analgesic was compared randomly and double-blind with morphine 10 mg in 160 female patients complaining of moderate (group I) or severe (group II) pain after elective lower abdominal surgery; both drugs were given i.m. In group I, pain relief with dezocine 10 and 15 mg was significantly greater than dezocine 5 mg; dezocine 10 mg appeared equipotent with morphine 10 mg. Similar, but statistically insignificant differences were observed in group II. Patient sedation was minimal and untoward side-effects infrequent with all doses of the trial drugs.
...
PMID:WY 16225 (dezocine), a new synthetic opiate agonist-antagonist and potent analgesic: comparison with morphine for relief of pain after lower abdominal surgery. 700 57

Adult patients who had arthroscopic surgery under general anesthesia and requested postoperative pain relief were randomized to receive treatment in a double-blind protocol with 5 mg of intravenous dezocine (20 patients), morphine (22 patients), nalbuphine (18 patients), or saline (24 patients). At 10-min intervals, starting with the first dose of analgesic, patients could choose up to three additional doses of the primary treatment, or choose an alternative analgesic if the primary drug was unsatisfactory. One to four doses of morphine were given as the alternate treatment if the initial treatment was dezocine or nalbuphine, and one to four doses of dezocine were given if the initial treatment was saline or morphine. The proportion of patients treated successfully by the initial treatments (i.e., not requesting alternate treatment), with P value for difference from placebo treatment, were saline 25%, nalbuphine 33% (P = 0.048), morphine 54% (P = 0.04), and dezocine 75% (P = 0.003). Dezocine and morphine are more efficacious than nalbuphine in the management of early postoperative pain. As an alternate analgesic in this study, dezocine required fewer doses to achieve patient satisfaction and was thus more efficacious than morphine. The incidence of treatment-related, adverse effects was different from that of saline or other treatments only for nalbuphine-related pain or burning on injection and dezocine-related facial itching. With respect to analgesic actions and side effects, dezocine seems more like morphine than nalbuphine.
...
PMID:Serial intravenous doses of dezocine, morphine, and nalbuphine in the management of postoperative pain for outpatients. 836 52

Postoperative pain is the most common complaint after laparoscopic cholecystectomy. This study was carried out to evaluate whether preoperative administration of intramuscular dezocine can provide postoperative analgesia and reduce postoperative opioid consumption in patients undergoing laparoscopic cholecystectomy. Patients (ASA I or II) scheduled for laparoscopic cholecystectomy were randomly assigned into intramuscular dezocine group (group 1) or intramuscular normal saline group (group 2). Dezocine and equal volume normal saline were administered intramuscularly 10 min before the induction of anesthesia. After operation, the severity of postoperative pain, postoperative fentanyl requirement, incidence and severity of side-effects were assessed. Postoperative pain and postoperative patient-controlled fentanyl consumption were reduced significantly in group 1 compared with group 2. The incidence and severity of side effects were similar between the two groups. Preoperative single-dose administration of intramuscular dezocine 0.1 mg/kg was effective in reducing postoperative pain and postoperative patient-controlled fentanyl requirement in patients undergoing laparoscopic cholecystectomy.
...
PMID:Preoperative administration of intramuscular dezocine reduces postoperative pain for laparoscopic cholecystectomy. 2355 11


1 2 Next >>