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A double-blind randomised, placebo-controlled trial evaluating the influence of oral long-acting muscle relaxant (Mebeverine MR), and insufflation with CO(2) on pain associated with barium enema.

Previous investigators have shown significant benefit using CO(2) for bowel insufflation. Others have suggested that the long-acting smooth muscle relaxant, Mebeverine, may be of benefit. We subjected this to a randomised double-blind trial. A total of 181 outpatients were randomised to receive either Mebeverine or placebo as pre-medication, and either air or CO(2) for bowel insufflation, thus creating four treatment groups. Visual-analogue lines were used to record pain scores before, during, and up to 8 h following the enema. All groups showed increased pain scores during the enema, with peak pain scores at the end of the examination, falling to baseline scores by 8 h. Patients receiving the combination of C0(2) and placebo had significantly lower pain scores at 1 and 4 h ( P=0.00 and P=0.014, respectively; Kruskal-Wallis test) compared with all other groups. Having Mebeverine as a pre-medication did not significantly lower pain scores compared with placebo, and decreased the amount of benefit received from the CO(2). We confirm that CO(2) is of benefit in decreasing pain during barium enema, and we recommend its routine use to improve the comfort of patients. Mebeverine is not of benefit, and its use as a pre-medication for enemas is not recommended.

Administration, Oral↗

Vascular smooth muscle relaxation by nitro compounds: reduced relaxation and cGMP elevation in tolerant vessels and reversal of tolerance by dithiothreitol.

Smooth muscle preparations obtained from bovine mesenteric artery were incubated with high concentrations of nitroglycerin (NG) or nitroprusside (NP) at elevated pH. This treatment was found to make the vessels tolerant towards both the relaxant and cGMP elevating action of a challenging dose of nitrocompounds when tested on the histamine contracted vessels. Also, some cross-tolerance between NP and NG could be found since pretreatment of the vessels with NP caused a reduction in both the relaxant and the cGMP elevating action of NG. The NG induced tolerance could be partly reversed by treatment with the disulfide reducing agent dithiothreitol (DTT). These results are suggested to strengthen the evidence for cGMP as a mediator of vascular smooth muscle relaxation induced by nitrocompounds. The ability of DTT to partly reverse this tolerance indicates the existence of critical tissue sulfhydryl groups with which the nitrocompounds interact. There also seemed to exist certain differences in the mechanism of action between NG and NP since the tolerance induced against NG was much more pronounced than was the case for NP.

Animals↗

Treatment of insomnia in cancer patients using muscle relaxation training.

Mean sleep onset latency was reduced from 124 to 29 min in 15 patients suffering from insomnia secondary to cancer; 15 subjects receiving routine care had means of 116 and 104 min in comparison. Muscle relaxation training was administered in individual sessions on three consecutive days. With 26 subjects available for follow-up 3 months later, the mean differences in sleep latency continued. The relatively greater success in this study than previously reported for a behavioral treatment of insomnia is discussed in light of possible differences between primary insomniacs and those subjects with insomnia secondary to a medical disease.

Adult↗

Intubating conditions with propofol under muscle relaxation with vecuronium bromide. A time-related comparison with thiopental.

In the present study a comparison has been made between intubating condition obtainable after anesthesia induction with Thiopental or Propofol, using Vecuronium Bromide to achieve muscle relaxation. Data were collected about hemodynamic parameters, vocal cords position, coughing or bucking, and involuntary movements. Three-hundred patients, males and females, ASA classes I and II, not premedicated, were included in the study; they all had to undergo surgery requiring tracheal intubation. The patients were divided in six different groups, and in each of them intubation was performed at different times from injection of inducing agents (2-2, 30-3-4-5-6 minutes). Overall results show a lack of satisfying intubating conditions on the extreme of selected times (2 and 5-6 minutes), with no significant difference between Thiopental and Propofol, except for a minimal unlike behaviour in hemodynamics. Therefore, on the basis of our data, as far as intubating conditions are considered, we can conclude that there is no reason to prefer one of the two inducing agents.

Adolescent↗

Newer neuromuscular blockers. Is the practitioner ready for muscle relaxants?

Current research on the development of new neuromuscular blocking agents is directed towards producing agents that have a rapid onset of action and predictable duration of action and recovery times, with minimal hemodynamic effects. For the veterinary practitioner, these newer agents should be considered when muscle relaxation is required for certain surgical procedures. Care must be taken to monitor paralyzed patients appropriately to ensure adequate ventilation and anesthetic depth. Vigilant monitoring should exist during the recovery period for the development of muscle weakness from residual blockade and the ability to reverse the effects of neuromuscular blockade. The use of neuromuscular blocking agents in veterinary patients should continue to increase as newer drugs and better monitoring techniques are developed.

Anesthesia↗

Biotransformation of 3-(2',4',5'-triethoxybenzoyl) propionic acid, a new biliary smooth muscle relaxant with choleretic activity, in rats.

1. By the combined use of deuterium labelling and gas chromatographic-mass spectrometric analysis, the metabolite pattern of 3-[2',4',5'-triethoxybenzoyl) propionic acid (triethoxybenzoylpropionic acid), a new biliary smooth muscle relaxant with choleretic activity, has been determined in the rat. 2. The metabolites excreted in urine and/or bile were isolated and characterized as follows: the parent drug, 3-(2',5'-diethoxy-4'-hydroxybenzoyl)propionic acid (metabolite II),3-(2'-ethoxy-4'-hydroxy-5'-methoxybenzoyl)propionic acid or 3-(2'-ethoxy-5'-hydroxy-4'-methoxybenzoyl)propionic acid (III), 3-(2',4'-diethoxy-5'-hydroxybenzoyl)propionic acid (V) and 3-[2',4'-diethoxy-5'-(2-hydroxyethoxy)benzoyl]propionic acid (VI). 3. The primary route of biotransformation of triethoxybenzoylpropionic acid in the rat was either O-de-ethylation at the C-4' and C-5' positions or beta-hydroxylation of the ethoxy group at the C-5' position in the parent molecule. 4. All these excreted products except metabolite VI were eliminated both unconjugated and in conjugates (probably glucuronides and/or sulphates). 5. The rat excreted mainly metabolites V and VI in the urine and parent drug, metabolites V and VI in the bile.

Animals↗