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Buprenorphine, a new powerful analgesic agent, was used to treat chest pain in patients with suspected myocardial infarction. Initial studies showed no significant changes in systemic or pulmonary artery blood pressure or in heart rate after intravenous buprenorphine. Sublingual buprenorphine also appeared effective in relieving pain, but its onset of action was considerably delayed compared with the intravenous route. A randomised double-blind controlled trial of equivalent doses of buprenorphine and diamorphine showed no significant difference between the drugs in terms of pain relief and duration of action. The occurrence of nausea, vomiting, and other side effects was similar in the two groups. The onset of action of buprenorphine was slightly but significantly slower than that of diamorphine. Since buprenorphine seems to be comparable with diamorphine in action and is not a controlled drug, it may prove useful in both general and hospital practice.
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PMID:Randomised trial comparing buprenorphine and diamorphine for chest pain in suspected myocardial infarction. 38 95

Epidural anaesthesia with local anaesthetics has become a standard method of pain relief during labour. In recent years, spinal opiates, alone and in combination with local anaesthetics, have also been tried with varying degrees of success. Buprenorphine, a potent lipophilic opiate with long duration of action, has been used in several trials for caesarean section [3, 4, 6], but not yet in spontaneous labour. The aim of the present investigation was to evaluate epidural anaesthesia with bupivacaine alone and with bupivacaine+buprenorphine in comparison with no anaesthetic treatment in control parturients. METHODS. A total of 80 healthy women during labour at full term (age 18-38 years, weight 54-107 kg) were studied to evaluate the influence of 0.3 mg buprenorphine (group BB) vs placebo (group B) added to an initial dose of 15 ml plain bupivacaine 0.33% for lumbar catheter epidural anaesthesia. Plain bupivacaine 0.25% (10 ml) without any opiate admixture was used for reinjections. The control group was made up of 48 untreated parturients. After every injection, blood pressure, heart rate and respiratory rate were measured repeatedly, as were time intervals between injections, extent of blockade, duration of labour, actual and retrospective visual analogue pain score, and side effects such as pruritus, shivering or nausea and emesis. Maternal capillary blood gases were analysed three times during labour, and Apgar scores and venous and arterial umbilical blood gas analyses were obtained immediately after delivery. RESULTS. Admixture of buprenorphine 0.3 mg significantly increased the time interval between the first and second epidural doses (B: 162 +/- 47 vs BB: 224 +/- 64 min; mean, SD; Table 2) and significantly reduced the incidence of shivering (Table 9). The incidence of instrumental delivery was comparable in all groups (bupivacaine 32.5%, bupivacaine+buprenorphine 27.5%, control 21%; n.s.). No clinically relevant differences were observed between the epidural patients in onset and duration of the block (Fig. 1), analgesic efficacy (Fig. 2), duration of spontaneous labour (BB: 8.6 +/- 3.1 h, B: 8.5 +/- 2.9 h; n.s.) and vital functions of mothers and newborns. Although some statistically significant differences between the three groups were found in some parameters of the blood gas analyses (Table 7), the clinical condition of the newborns was always acceptable; Apgar scores were not significantly different. DISCUSSION AND CONCLUSIONS. The addition of buprenorphine to bupivacaine resulted in some advantages to the mother (reduced incidence of shivering) and the anaesthetist (time lapse before first reinjection was necessary) without jeopardizing the situation of the baby. Compared with untreated control parturients, retrospective pain scores during epidural anaesthesia with bupivacaine (with or without buprenorphine) were significantly lower. No clinically relevant disadvantages of epidural anaesthesia were observed. More studies are required to evaluate whether buprenorphine admixture allows a dose reduction of bupivacaine and could then claim clearer advantages than were found in the present investigation.
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PMID:[Obstetrical peridural anesthesia with bupivacaine and buprenorphine. A randomized double-blind study in comparison with untreated controls]. 149 32

Patient-controlled analgesia (PCA) was studied during the early postoperative period. Subjects were 40 ASA I-III patients recovering from elective major and minor surgery. Buprenorphine doses of 40 micrograms each were available whenever the patients felt pain relief necessary, and were delivered by a microprocessor-controlled injection pump (On-Demand Analgesia Computer). The hourly maximum dose was set at 320 micrograms with a lockout time of 1 minute. A continuous low-dose buprenorphine infusion (5 micrograms/h) was additionally administered in order to prevent catheter obstruction. The duration of the PCA period was 16.9 +/- 5.1 h (mean +/- SD). During this time, 16.1 +/- 11.3 demands per patient were recorded resulting in individual buprenorphine consumptions of 0.63 +/- 0.59 micrograms/kg/h. More buprenorphine was needed following abdominal surgery compared with orthopedic patients, although pain relief was found slightly less in the former group. Buprenorphine consumption was significantly higher in female than in male patients. Overall efficacy and patient acceptance proved to be excellent. The effectiveness of PCA was judged superior by about 93% of patients when compared with previously experienced postoperative analgesia. Side-effects (sweating, nausea, emesis) occurred in about 10% of cases but were usually of minor intensity. No circulatory or respiratory problems were observed during the PCA period.
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PMID:[Postoperative on-demand analgesia with buprenorphine]. 336 65

The analgesic potency, efficacy, duration of action and side-effects of buprenorphine (Temgesic) 0.3 mg and 0.6 mg were compared with those of pentazocine (Sosegon) 30 mg and 60 mg in 100 male patients who had undergone orthopaedic surgical procedures. The drugs were given by intramuscular injection 30 minutes before completion of the surgical procedure, and the quality of pain relief and incidence of side-effects were assessed at 30-minute intervals for at least 6 hours. Buprenorphine was shown to be safe, to be more potent and to have a longer duration of action than pentazocine, and to result in less nausea, vomiting and euphoria, but it was associated with a higher incidence of postoperative sedation than pentazocine.
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PMID:A comparison of buprenorphine and pentazocine for the relief of postoperative pain. 351 Apr 58

Pharmacological properties of buprenorphine were compared with those of morphine and pentazocine. Buprenorphine scarcely showed any effects on spontaneous EEGs and sleep-wakefulness cycles. Buprenorphine tended to depress the recruiting and augmenting responses and the spindle burst, and it also inhibited the hypothalamic arousal response. Buprenorphine had weaker emetic action than morphine and protected against apomorphine-induced emesis in the same manner as morphine. Buprenorphine scarcely affected respirations, blood pressure, heart rate, blood flow, ECG, cardiac contractile force, cornary flow, and intracranial pressure. However, morphine and pentazocine caused depressed respiration, decreased blood pressure, increased blood flow and cardiac contractile force, and elevated intracranial pressure. Buprenorphine, morphine, and pentazocine did not affect bile secretion, but produced contraction of the sphincter of Oddi. Buprenorphine had very little effect on renal function, but morphine and pentazocine reduced this function to depress urine flow. Buprenorphine and morphine inhibited carrageenin-induced edema. Buprenorphine had no effect on blood histamine level, but morphine increased the concentration of histamine. These results indicate that buprenorphine has little effect on the central nervous system, respiratory and cardiovascular system, and renal function.
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PMID:[Pharmacological properties of buprenorphine, a new analgesic agent. Part II. (author's transl)]. 612 75

Epidural buprenorphine was investigated as a postoperative analgesic in a randomized double-blind study of 158 patients given epidural analgesia with mepivacaine or bupivacaine for orthopedic surgery of the lower extremity. At the end of surgery, patients were given either 0.15 mg of epidural buprenorphine (n = 38), 0.3 mg (n = 37) in 15-ml saline, or no further epidural injections (n = 47, control group) after 2% mepivacaine for intraoperative anesthesia. A fourth group (n = 36) received 0.3 mg of buprenorphine in 15-ml saline, after the intraoperative use of 0.5% bupivacaine. The patients rated postoperative pain. The need for additional analgesics as well as side effects were recorded. Analgesia after 0.15 mg buprenorphine was superior to that after no reinjection for 6 hr after surgery (P less than 0.05). Buprenorphine (0.3 mg) was superior both to no reinjection and to 0.15 mg of buprenorphine until the twelfth hour (P less than 0.05). Analgesia after bupivacaine followed by 0.3 mg of buprenorphine was not significantly different than analgesia seen after mepivacaine followed by 0.3 mg of buprenorphine. There was an increase of PaCO2 of 2-5 mm Hg between 1.5-3.5 hr after 0.3 mg of buprenorphine without any evidence for late respiratory depression. Other side effects, e.g., disturbances of micturition, pruritus, nausea, vomiting, fatigue, and headache, were comparably common in all groups. The epidural administration of 0.3 mg buprenorphine may be recommended for postoperative analgesia following orthopedic surgery of the lower extremity.
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PMID:Epidural buprenorphine--a double-blind study of postoperative analgesia and side effects. 637 65

Eighty fit adults having elective abdominal hysterectomy or cholecystectomy received buprenorphine or morphine intravenously at the start of peritoneal closure, in a randomised double-blind trial. The anaesthetic sequence precluded the use of other narcotic analgesics. Pain scores were lower in patients who received buprenorphine, as were the cumulative numbers of patients withdrawn from the trial at each interval because of pain, statistical significance being achieved at all intervals from one to seven hours after administration. Unexpectedly, patients having the upper abdominal procedure were more likely to receive satisfactory analgesia than those having abdominal hysterectomy. Vomiting occurred more commonly after buprenorphine, and mean respiratory rates were slightly lower. However, the differences were not statistically significant. One patient with protracted drowsiness and slow respiratory rate after buprenorphine received naloxone. No serious side-effects were noted. Buprenorphine 4-6 micrograms/kg provided adequate postoperative analgesia of greater duration than could be achieved with morphine, and the potency of buprenorphine when administered in this way was at least 33 times that of morphine.
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PMID:A comparison of morphine and buprenorphine for analgesia after abdominal surgery. 639 18

Two groups of 20 patients each were given immediately after hip-operation an epidural injection of 0,15 or 0,3 mg buprenorphine. Effects and side effects are compared with those observed in two groups of patients having the same type of operation, and given either 4 mg of morphine or saline (placebo) by epidural injection. Buprenorphine in both doses produced a shorter duration of analgesia than 4 mg of morphine. In no case did respiratory depression occur. Urinary retention after buprenorphine was barely more frequent than in the placebo group. Nausea and vomiting occurred in 35-45% of patients. We do not see an advantage in replacing morphine by buprenorphine for epidural opiate-analgesia, because the same high rate of nausea/vomiting is associated with a significantly shorter duration of analgesia after buprenorphine. We are convinced that epidural opiate-analgesia is most valuable for postoperative pain relief but should be reserved for selected cases.
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PMID:[Epidural buprenorphine for postoperative analgesia after hip operations]. 661 22

The therapeutic value of buprenorphine was investigated in 31 patients suffering from moderate to severe cancer pain by intramuscular administration at the single doses of 0.2 mg and 0.3 mg in comparison with pentazocine 30 mg. Analgesic effect of buprenorphine 0.3 mg was significantly superior to buprenorphine 0.2 mg and pentazocine 30 mg. The duration of analgesia with buprenorphine was 9 hours at 0.2 mg and 11 hours at 0.3 mg, which were markedly longer than pentazocine's 6 hours. Side effects most commonly observed in the three groups were nausea, vertigo, oral dryness, urinary retention, vomiting, sweating, and headache. The frequency of side effects was 54.8% for buprenorphine 0.2 mg, 50.0% for buprenorphine 0.3 mg and 58.3% for pentazocine 30 mg respectively, indicating no significant difference between the three groups. Blood pressure, heart rate and respiratory rate did not change appreciably, thereby suggesting a little effect of buprenorphine on the respiratory and cardiovascular systems. Buprenorphine was found a useful or extremely useful in 58% at 0.2 mg and 87.5% at 0.3 mg. As the result it was concluded that buprenorphine could be valuable as an analgesic for cancer pain.
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PMID:[Effect of a long-acting analgesic, buprenorphine on cancer pain--a single-blind crossover comparison with pentazocine]. 718 1

Side-effects of increasing doses of morphine (0.100, 0.150, 0.200 mg/kg) and buprenorphine (0.0015, 0.003, 0.006 mg/kg), given intramuscularly, are clinically observed in conscient subjects suffering from intense pain in the facial or trigeminal nerves territory. Buprenorphine induces a drop in ventilation even with the lower doses, which persists for 120-180 minutes. This effect is more important after the injection of an equianalgesic dose of morphine. The same phenomenon is observed for the drop in heart rate and for the hypotension, which remained in all cases very slight. The central side-effects are of the same nature with buprenorphine and with morphine. On the whole this phenomenon appears with the same frequency with both drugs, especially for drowsiness and sleep, for nausea, vomiting and dizziness. Yet, the patient under buprenorphine becomes more frequently confused and agitated. Lastly, a state of euphoria can occur which might be feared to be related to a drug-addict activity of buprenorphine.
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PMID:[Comparison between the side-effects of buprenorphine and morphine in conscious man (author's transl)]. 745 48


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