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At least 919 records · Page 51Linked to original sources
PubMed1981

A comparative clinical study of dioxonium and pancuronium as muscle relaxants in small children.

Dioxonium (30, 40, and 60 microgram/kg i.v.), a new depolarizing agent, weas compared with pancuronium (0.05 and 0.1 mg/kg i.v.) as a muscle relaxant in combination anesthesia during general surgical operations in small children. Generally, the conditions during intubation, maintenance of anesthesia, and in the recovery room were comparable after both drugs. There were no differences in the cardiovascular responses either. However, a wider intra- and interindividual variation in the drug response was observed after dioxonium, especially after repeated administrations.

Anesthesia↗
PubMed1998

Inhibitory mechanisms for cross-bridge cycling: the nitric oxide-cGMP signal transduction pathway in smooth muscle relaxation.

Relaxation follows sequestration of Ca2+ mobilized by an excitatory stimulus in striated muscle. Removal of excitatory stimuli also relaxes smooth muscle in vitro after reductions in the myoplasmic [Ca2+] and dephosphorylation of the myosin regulatory light chains. However, there are several experimental procedures that produce relaxation in the presence of excitatory stimuli and elevated Ca(2+)-dependent cross-bridge phosphorylation. Of potential widespread physiological importance are treatments that increase myoplasmic [cGMP] owing to the ubiquity of nitric oxide (NO) as a signalling molecule for endothelial-mediated vasodilation and inhibitory nerves in most types of smooth muscle. Several mechanisms are implicated in the NO-cGMP mediated relaxation. Most studies support reductions in myoplasmic Ca2+. However, there is evidence that increases in cGMP also lower the Ca(2+)-sensitivity of cross-bridge phosphorylation. This would contribute to a decline in force through actions on the myosin light chain kinase/phosphatase system. In addition, changes in the dependence of force on phosphorylation are observed in tissues partially relaxed by treatments that elevate cGMP. This demonstrates that either the attachment and cycling of phosphorylated cross-bridges is impaired or blocked, or that the formation of dephosphorylated, force-generating cross-bridges ('latch-bridges') is reduced. Protein kinase G-catalysed phosphorylation of either a thin filament protein that blocks attachment of cross-bridges or a protein that inhibits myosin light chain phosphatase may explain the NO-induced relaxation with elevated cross-bridge phosphorylation.

Animals↗
PubMedDate not supplied

[Comparison of the double burst stimulus with the train-of-four stimuli in monitoring muscle relaxation during anesthesia].

OBJECTIVE: To compare double burst stimulus (DBS) and the train-of-four stimuli (TOF) for monitoring neuromuscular blockade during anesthesia in terms of muscle relaxation requirements, dose of anticholinesterase agents and the possibility of postanesthetic residual relaxation. PATIENTS AND METHODS: Patients were randomly assigned to two groups according to type of monitoring (DBS group, n = 29; and TOF group, n = 28), and were given an adjusted infusion of vecuronium to obtain response to stimulation with both methods of monitoring. When the block was considered to be sufficiently reversed in the operating theater, the patients were transferred to the postanesthesia recovery unit (PARU), where the coefficient between the fourth and first responses to TOF (T4/T1r) was obtained by electromyography and the patients were given the dose of neostigmine needed to obtain a T4/T1r > 70% RESULTS: Vecuronium was infused at a faster rate during anesthesia in the DBS group than in the TOF group (1.0 +/- 0.19 microgram.kg-1.min-1 and 0.8 +/- 0.24 microgram. kg-1.min-1, respectively, p = 0.005). T4/T1r was less than 70% upon arrival at the PARU in 10 DBS patients and in 2 TOF patients (p = 0.02). No differences were found in neostigmine doses given. CONCLUSIONS: The use of DBS increased the vecuronium dose required during anesthesia and risk in those patients who arrived at the PARU with residual muscle block (T4/T1r < 70%).

Anesthesia Recovery Period↗
PubMed1999

Characterization of beta-adrenoceptor mediated smooth muscle relaxation and the detection of mRNA for beta1-, beta2- and beta3-adrenoceptors in rat ileum.

1. Functional and molecular approaches were used to characterize the beta-AR subtypes mediating relaxation of rat ileal smooth muscle. 2. In functional studies, (-)-isoprenaline relaxation was unchanged by CGP20712A (beta1-AR antagonist) or ICI118551 (beta2-AR antagonist) but shifted by propranolol (pKB=6.69). (+/-)-Cyanopindolol, CGP12177 and ICID7114 did not cause relaxation but antagonized (-)-isoprenaline relaxation. 3. BRL37344 (beta3-AR agonist) caused biphasic relaxation. The high affinity component was shifted with low affinity by propranolol, (+/-)-cyanopindolol, tertatolol and alprenolol. CL316243 (beta3-AR agonist) relaxation was unaffected by CGP20712A or ICI118551 but blocked by SR58894A (beta3-AR antagonist; pA2 = 7.80). Enhanced relaxation after exposure to forskolin and pertussis toxin showed that beta3-AR relaxation can be altered by manipulation of components of the adenylate cyclase signalling pathway. 4. The beta-AR agonist RO363 relaxed the ileum (pEC50=6.18) and was blocked by CGP20712A. Relaxation by the beta2-AR agonist zinterol (pEC50=5.71) was blocked by SR58894A but not by ICI118551. 5. In rat ileum, beta1-, beta2- and beta3-AR mRNA was detected. Comparison of tissues showed that beta3-AR mRNA expression was greatest in WAT>colon=ileum >cerebral cortex>soleus; beta1-AR mRNA was most abundant in cerebral cortex > WAT > ileum = colon > soleus; beta2-AR mRNA was expressed in soleus > WAT > ileum = colon > cerebral cortex. 6. These results show that beta3-ARs are the predominant beta-AR subtype mediating rat ileal relaxation while beta1-ARs may produce a small relaxation. The beta2-AR agonist zinterol produces relaxation through beta3-ARs and there was no evidence for the involvement of beta2-ARs in relaxation despite the detection of beta2-AR mRNA.

Adenylate Cyclase Toxin↗
PubMed1983

[Study of allergy to general anesthetics and muscle relaxants using the lymphoblast transformation test].

This study aims to test the lymphocyte response in normal subjects and patients who presented an anaphylactoid shock to various anaesthetic and muscle relaxant drugs, by using the lymphoblast transformation test (LTT). The results show that, although the LTT is a specific test, which can be carried out in vitro, it is badly adapted to the biological diagnosis of anaphylactic drug accidents on the whole, because of a possible non specific lymphoblastic transformation in controls or, on the contrary, of false negative results in anaphylaxis. As a consequence of this, and some comparative studies, the diagnosis of drug induced anaphylaxis must rely on skin tests, human basophil degranulation test (HBDT) and the Prausnitz-Küstner test.

Adult↗
PubMed2001

Meta-analysis of smooth muscle relaxants in the treatment of irritable bowel syndrome.

AIM: To update previous overviews of placebo-controlled double-blind trials assessing the efficacy and tolerance of smooth muscle relaxants in irritable bowel syndrome. METHODS AND TRIALS: A total of 23 randomized clinical trials were selected for meta-analyses of their efficacy and tolerance. Six drugs were analysed: cimetropium bromide (five trials), hyoscine butyl bromide (three trials), mebeverine (five trials), otilium bromide (four trials), pinaverium bromide (two trials) and trimebutine (four trials). The total number of patients included was 1888, of which 945 received an active drug and 943 a placebo. RESULTS: The mean percentage of patients with global improvement was 38% in the placebo group (n=925) and 56% in the myorelaxant group (n=927), in favour of myorelaxants with a mean odds ratio of 2.13, P < 0.001 (95% CI: 1.77--2.58) and a mean risk difference of 22% P < 0.001 (95% CI: 13--32%). The percentage of patients with pain improvement was 41% in the placebo group (n=568) and 53% in the myorelaxant group (n=567): odds ratio 1.65, P < 0.001 (95% CI: 1.30--2.10) and risk difference 18%, P < 0.001 (95% CI: 7--28%). There was no significant difference for adverse events. CONCLUSION: Myorelaxants are superior to placebo in the management of irritable bowel syndrome.

Abdominal Pain↗
PubMed2002

[Tracheal intubation in a case of idiopathic pulmonary fibrosis using remifentanil and propofol without muscle relaxants].

The anesthetic management of a 58 year-old-male suffering from idiopathic pulmonary fibrosis associated with a previous experience of altered dose-response relationship to muscle relaxants is reported. He underwent a gastroendoscopic surgical procedure. After intravenous atropine, remifentanil 3.0 microg kg(-1) was injected over 90 sec. Sixty seconds after the start of remifentanil bolus dose, propofol 2.0 mg kg(-1) was injected and intubation was performed 1 min after the administration of propofol. Anesthesia was maintained by N(2)O, oxygen, sevoflurane (0.5-0.8%) and remifentanil titrated infusion (mean dose of 0.15 mg kg(-1) min(-1)) under spontaneous respiration or assisted ventilation, if the patient was apnoic. The intubating conditions were good, a 30 per cent reduction in MAP was observed after propofol administration. The patient regained consciousness 5 minutes after the end of remifentanil administration and his trachea was extubated without any troubles. Recovery was uneventful without the need of long-term intensive therapy.

Anesthetics, Intravenous↗
PubMed1986

Smooth muscle relaxant effect of dehydroindicolactone.

Dehydroindicolactone, a novel linear furanocoumarin with an 8-substituted side chain carrying a 5-member ring lactone, showed spasmolytic activity in a number of smooth muscle preparations. The spasmolytic activity seems to lie in its ability to block the dihydropyridine-sensitive calcium channel.

Animals↗
PubMed1976

[On the molecular mechanism of action of galanthamine, an antagonist of nondepolarizing muscle relaxants (author's transl)].

In clinical anaesthesia, galanthamine hydrobromide (Nivalin), an alkaloid of galanthus nivalis (common snowdrop) is used to reverse the neuromuscular blocking effect of curare-type muscle relaxants. A comparative study of the inhibition by galanthamine of acetylcholinesterase (AChE; PH 7,2; substrate; acetylthiocholine) and of pseudocholinesterase (ChE; ph 7,7; substrate: butyrylthiocholine) was carried out by means of a colorimetric assay technique at 25 degrees C. AChE (pI50 = 5.5; Ki = 5.2 X 10(-8) M) has an approximately 100-fold higher affinity to galanthamine than has ChE (pI50 = 3.7; Ki = 2.9 X 10(-6) M). The kinetic analysis of the inhibition which is instantaneously reversible upon dilution revealed a pure competitive mechanism of action for both enzymes. Supported by a calculation of the change in free binding energy (AChE: delta F = 9.9 kcal X mole-1; ChE: delta F = -7.6 kcal X mole-1), galanthamine is thought to decrease the rate of hydrolysis by a reversible binding to the anionic site of the active centre ("prosthetic inhibitor") thus impairing the formation of the enzyme-substrate complex.

Chemical Phenomena↗