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PubMed2003

Overestimation of Bispectral Index in sedated intensive care unit patients revealed by administration of muscle relaxant.

BACKGROUND: Electromyographic activity has previously been reported to elevate the Bispectral Index (BIS) in patients not receiving neuromuscular blockade while under sedation in the intensive care unit. This study aimed to investigate the magnitude of the decrease of BIS following administration of muscle relaxant in sedated intensive care unit patients. METHODS: The authors prospectively investigated 45 patients who were continuously sedated with midazolam and sufentanil to achieve a Sedation-Agitation Scale value equal to 1 and who required administration of muscle relaxant. BIS (BIS version 2.10), electromyography, and acceleromyography at the adductor pollicis muscle were recorded simultaneously before and after neuromuscular blockade. Sixteen of these 45 patients were also studied simultaneously with the new BIS XP. RESULTS: After administration of a muscle relaxant, BIS (67 +/- 19 vs. 43 +/- 10, P < 0.001) and electromyographic activity (37 +/- 9 vs. 27 +/- 3 dB, P < 0.001) significantly decreased. Multiple regression analysis showed that the decrease of BIS following administration of myorelaxant was significantly correlated to BIS and electromyographic baseline values. Using standard BIS range guidelines, the number of patients under light or deep sedation versus general anesthesia or deep hypnotic state was markedly overestimated before administration of myorelaxant (53 vs. 2%, P < 0.001). CONCLUSIONS: The BIS in sedated intensive care unit patients may be lower with paralysis for an equivalent degree of sedation because of high muscular activity. The magnitude of BIS overestimation is significantly correlated to both BIS and electromyographic activity before neuromuscular blockade. The authors conclude that clinicians who determine the amount of sedation in intensive care unit patients only from BIS monitoring may expose them to unnecessary oversedation.

Anesthetics, Intravenous↗
PubMed1994

Membrane fusion of erythrocytes as a model study of the effects of muscle relaxants on presynaptic exocytosis.

The exact mechanism by which synaptic vesicles fuse with the presynaptic nerve terminal membrane has not been determined. We therefore investigated the effects of muscle relaxants on membrane fusion using the human red blood cell as a model membrane. The kinetics of calcium-phosphate-induced membrane fusion were monitored continuously by noting the relief of fluorescence self-quenching of octadecyl-rhodamine B chloride (R18)-labeled and unlabeled membranes. The nondepolarizing muscle relaxants, vecuronium and pancuronium, inhibited membrane fusion of ghosts, inside-out vesicles (IOVs), and phosphatidylserine (PS)-loaded IOVs, whereas succinylcholine did not affect membrane fusion. The inhibitory effect of nondepolarizing muscle relaxants on membrane fusion suggests the prejunctional involvement of nondepolarizing muscle relaxants.

Erythrocytes↗
PubMed1981

Clinical pharmacology of ORG NC45 (NorcuronTM): a new nondepolarizing muscle relaxant.

To determine the neuromuscular effects of a new muscle relaxant, ORG NC45 (Norcuron), a monoquaternary homologue of pancuronium, 84 ASA Class I or II patients were studied under halothane and nitrous oxide anesthesia. The ED50 (dose of muscle relaxant causing a 50% depression of twitch tension) of pancuronium and ORG NC45 was 0.022 mg/kg (r = 0.90) and 0.015 mg/kg (r =0.80), respectively, for a potency ratio of 1.5 (0.022/0.015). The duration of action (time from injection to 90% recovery of control twitch tension) was 27 +/- 5 min with ORG NC45, 0.02 mg/kg, and 65 +/- 16 min with pancuronium in an equivalent dose of 0.03 mg/kg. The increase in duration of neuromuscular blockade from repetitive doses was greater with pancuronium than with ORG NC45. Reversal of an ORG NC45 neuromuscular blockade was accomplished with doses of neostigmine slightly less than those required for pancuronium. Under thiopental-nitrous oxide anesthesia, endotracheal intubation was easily performed using ORG NC45, 0.07-0.14 mg/kg. The duration of action of ORG NC45, 0.07 mg/kg, was about one-third that of pancuronium (0.1 mg/kg). It was concluded that ORG NC45 is more potent and has a shorter duration of action with both initial and repetitive doses than does pancuronium. With these characteristics and the reported lack of cardiovascular effects, the authors believe further clinical trials are warranted.

Adult↗
PubMed1994

Centrally acting skeletal muscle relaxants and associated drugs.

A review of available studies supports a role for muscle relaxants in the treatment of painful musculoskeletal disorders. The utility of these drugs is limited by sedation and other side effects, as well as by the potential for abuse and dependency. Other drugs can also be used in the treatment of muscle spasm, specifically diazepam, baclofen, dantrolene sodium, and quinine sulfate. The pharmacology of the muscle relaxants and these other agents is discussed and practical suggestions for use are offered.

Animals↗
PubMed1997

Pharmacological properties of the new centrally acting muscle relaxant (R)-(+)-3-phenyl-5-[2-(1-pyrrolidinylmethyl)butyryl]isoxazole hydrochloride.

The pharmacological properties of (R)-(+)-3-phenyl-5-[2-(1-pyrrolidinylmethyl)butyryl]isoxazole hydrochloride (CAS 144576-50-1, MS-322), a new centrally acting muscle relaxant, were investigated and compared with those of eperisone-HCl (CAS 56839-43-1) in experimental animals. MS-322 (1.5-6 mg/kg i.v.) reduced both anemic and intercollicular decerebration-induced rigidity in rats. Similar doses were required for these effects. The activity of MS-322 (200 mg/kg p.o.) against intercollicular decerebration-induced rigidity was greater and longer lasting than that of the same dose of eperisone-HCl. MS-322 (0.75-6 mg/ kg i.v.) inhibited the flexor reflex in anesthetized cats in a dose-dependent manner and more strongly than eperisone-HCl. MS-322 had no effect on the neuromuscular junction in anesthetized rats. The muscle relaxant activity of MS-322 in mice, demonstrated by the traction and rota-rod tests was stronger than that of eperisone-HCl, whereas MS-322 affected spontaneous motor activity in mice less than eperisone-HCl. The results of this study suggest that MS-322 is a potent centrally acting muscle relaxant with relatively weak depressant activity at other central nervous system pathways.

Animals↗
PubMed1988

Effect of benzazole-related centrally acting muscle relaxants on HPNS.

A series of benzazole-related, centrally acting muscle relaxants, comprising benzimidazole, chlorzoxazone, and zoxazolamine, were found to give substantial protection against the tremors and convulsions associated with the high pressure neurologic syndrome (HPNS) in the mouse. In this respect they represent a new class of nonanesthetic, anti-HPNS agents. Their anti-HPNS properties, like those previously established for the mephenesin group of centrally acting muscle relaxants, seem to be related to their ability to antagonize the convulsive action of strychnine. These findings are consistent with the suggestion that one of the principal effects of pressure, expressed as HPNS, arises from a perturbation of strychnine-sensitive mechanisms.

Animals↗
PubMed2003

Tracheal intubation without muscle relaxants: remifentanil or alfentanil in combination with propofol.

BACKGROUND AND OBJECTIVE: In some situations, the use of muscle relaxants (neuromuscular blocking drugs) are undesirable or contraindicated. We compared intubating conditions without muscle relaxants in premedicated patients receiving either alfentanil 40 microg kg(-1) or remifentanil 2, 3 or 4 microg kg(-1) followed by propofol 2 mg kg(-1). METHODS: In a randomized, double-blind study, 80 healthy patients were assigned to one of four groups (n = 20). After intravenous atropine, alfentanil 40 microg kg(-1) or remifentanil 2, 3 or 4 microg kg(-1) were injected over 90 s followed by propofol 2 mg kg(-1). Ninety seconds after administration of the propofol, laryngoscopy and tracheal intubation were attempted. Intubating conditions were assessed as excellent, good or poor on the basis of ease of lung ventilation, jaw relaxation, laryngoscopy, position of the vocal cords, and patient response to intubation and slow inflation of the endotracheal tube cuff. RESULTS: Seven patients who received remifentanil 2 microg kg(-1) and one patient who received remifentanil 3 microg kg(-1) could not be intubated at the first attempts. Excellent intubating conditions (jaw relaxed, vocal cords open and no movement in response to tracheal intubation and cuff inflation) were observed in those who received either alfentanil 40 microg kg(-1) (45% of patients) or remifentanil in doses of 2 microg kg(-1) (20%), 3 microg kg(-1) (75%) or 4 microg kg(-1) (95%). Overall, intubating conditions were significantly better (P < 0.05), and the number of patients showing excellent conditions were significantly higher (P < 0.05) in patients who received remifentanil 4 microg kg(-1) compared with those who received alfentanil 40 microg kg(-1) or remifentanil 2 microg kg(-1). No patient needed treatment for hypotension or bradycardia. CONCLUSIONS: Remifentanil 4 microg kg(-1) and propofol 2 mg kg(-1) administered in sequence intravenously provided good or excellent conditions for tracheal intubation in all patients without the use of muscle relaxants.

Adolescent↗
PubMed2000

Anaphylactic reactions during induction of anaesthesia using rocuronium for muscle relaxation: a report including 3 cases.

Anaphylaxis during induction of anaesthesia is a dreaded complication with a mortality rate of 3-6%, most frequently associated with the use of muscle relaxants. Current knowledge on this matter is reviewed in relation to the presentation of 3 cases of anaphylaxis and bronchospasm associated with the use of the recently released nondepolarizing muscle relaxant rocuronium. Bronchospasm may be the sole sign of a serious drug reaction, triggered by precipitation of insoluble thiopental crystals when mixed with a muscle relaxant in the intravenous (iv) line. It is recommended that these drugs are administered via different injection ports. The hypotension requires immediate treatment with oxygen, epinephrine and large amounts of iv fluids. Epinephrine infusion may be needed for hours. It is recommended that serum tryptase is measured approximately 2 h after debut of the serious drug reaction. Allergy testing should be performed for all the drugs the patient was exposed to, 4-8 weeks after the incident, and due to cross-reactivity, including all available muscle relaxants. Doctors are urged to inform their patients, and systematically register adverse drug reactions.

Adult↗
PubMed1990

Vascular smooth muscle relaxation induced by epidermal growth factor is endothelium-dependent.

Epidermal growth factor (EGF) is released from platelets during aggregation. Because we thought that EGF played a role in vascular tone, we investigated its vascular reactivity using isolated rat aortic strips with and without the endothelium. In the presence of endothelium, EGF relaxed vascular smooth muscle precontracted with 40 mM K+, 10(-5) M prostaglandin F2 alpha or 10(-6) M norepinephrine. The relaxation induced by EGF was more prominent on the prostaglandin F2 alpha- and norepinephrine-induced contractions than on the K(+)-induced contraction. Atropine (10(-5) M) and aspirin (10(-5) M) had no effect on the EGF-induced relaxation, but methylene blue (10(-5) M) partly abolished the relaxation evoked by EGF. These results suggest that EGF relaxes vascular smooth muscle in the presence of the endothelium. They also suggest that EGF has an effect on the endothelium to produce relaxing factor independent of cyclooxygenase; the releasing factor activates soluble guanylate cyclase, resulting in relaxation of vascular smooth muscle through the production of cyclic GMP.

Animals↗
PubMed1991

Heterogeneity of human mast cells and basophils in response to muscle relaxants.

The authors studied the effects of increasing concentrations 10(-5)-10(-3) M) of four muscle relaxants (succinylcholine, d-tubocurarine, vecuronium, and atracurium) on histamine release from peripheral blood basophils and mast cells isolated from human lung parenchyma, skin tissues, and heart fragments. Basophil granulocytes released less than 5% of their histamine content when incubated with any one of the muscle relaxants tested. In contrast, mast cells showed a significant heterogeneity in response to different muscle relaxants. Succinylcholine did not induce histamine release from any type of mast cell, and only high concentrations of d-tubocurarine (10(-3) M) caused histamine release from skin and lung mast cells. Vecuronium concentration-dependently induced histamine release from skin and lung--but not from heart mast cells--to a maximum of 7.2 +/- 2.1% and 4.9 +/- 1.4%, respectively. Atracurium concentration-dependently caused significant histamine release from skin and lung mast cells to a maximum of 46.2 +/- 15.1% and 30.6 +/- 6.0%, respectively. Atracurium (5 x 10(-5) - 2 x 10(-4) M) also induced histamine release from heart mast cells. The histamine release process from both lung and skin mast cells caused by atracurium and vecuronium was extremely rapid (t1/2 = less than 1 min). The releasing activity of atracurium and vecuronium on lung and skin mast cells was not reduced, and not abolished, by lowering the temperature of the incubation buffer to 22 degrees C and 4 degrees C. Extracellular calcium did not affect the capacity of atracurium and vecuronium to induce histamine release from lung and skin mast cells.(ABSTRACT TRUNCATED AT 250 WORDS)

Basophils↗
PubMed2006

Thrombospondin-1 limits ischemic tissue survival by inhibiting nitric oxide-mediated vascular smooth muscle relaxation.

The nitric oxide (NO)/cGMP pathway, by relaxing vascular smooth muscle cells, is a major physiologic regulator of tissue perfusion. We now identify thrombospondin-1 as a potent antagonist of NO for regulating F-actin assembly and myosin light chain phosphorylation in vascular smooth muscle cells. Thrombospondin-1 prevents NO-mediated relaxation of precontracted vascular smooth muscle cells in a collagen matrix. Functional magnetic resonance imaging demonstrated that an NO-mediated increase in skeletal muscle perfusion was enhanced in thrombospondin-1-null relative to wild-type mice, implicating endogenous thrombospondin-1 as a physiologic antagonist of NO-mediated vasodilation. Using a random myocutaneous flap model for ischemic injury, tissue survival was significantly enhanced in thrombospondin-1-null mice. Improved flap survival correlated with increased recovery of oxygen levels in the ischemic tissue of thrombospondin-1-null mice as measured by electron paramagnetic resonance oximetry. These findings demonstrate an important antagonistic relation between NO/cGMP signaling and thrombospondin-1 in vascular smooth muscle cells to regulate vascular tone and tissue perfusion.

Actins↗
PubMed1977

Comparative effects of nondepolarizing muscle relaxants on succinycholine-induced fasciculations and postoperative pain.

The effectiveness of pancuronium (1.0 to 1.5 mg), d-tubocurarine (3 mg), and gallamine (20 mg) administered three minutes before succinylcholine (1 mg/kg) in preventing muscle fasciculations and postoperative muscle pains was compared in 100 patients. Pretreatment with pancuronium abolished fasciculations and produced rapid and excellent muscle relaxation for endotracheal intubation. Both d-tubocurarine (dTc) and gallamine administered prior to succinylcholine (SCh) were inconsistent in prevention fasciculations. Muscle relaxation was significantly delayed in onset, shorter in duration, and was inadequate for intubation in the majority of patients. The 45% incidence of postoperative muscle pains in the control group decreased after pretreatment with gallamine, dTc, and pancuronium to 20%, 15%, and less than 5%, respectively. It was concluded from the present study that pancuronium is superior to dTc and gallamine for preventing SCh-induced fasciculations and postoperative muscle pains without compromising the muscle relaxation for intubation. However, pancuronium administered for pretreatment may significantly prolong the action of succinylcholine and caution is to be exercised in patients having short surgical procedures and when additional doses of muscle relaxants may be required.

Adolescent↗
PubMed1975

Actions of a new muscle relaxant (AH8165) on neuromuscular transmission.

The effects of a new muscle relaxant, AH8165, on miniature endplate potential (MEPP) amplitude and frequency, endplate sensitivity to acetylcholine, and muscle twitch tension were studied in vitro in the frog sartorius muscle. Nerve terminal effects were studied in vivo in the cat soleus muscle and its ventral root fibers. AH8165 stimulates the nerve terminal, as evidenced by increased MEPP frequency and the appearance of post-drug repetitive activity. In the same concentration range at which MEPP frequency is increased, MEPP amplitude, endplate sensitivity to acetylcholine, and twitch tension are decreased. This suggests that AH8165 produces muscle relaxation by blocking postsynaptic cholinergic receptors. (Key works: Neuromuscular relaxants, AH8165.).

Acetylcholine↗
PubMed2004

Inhibition of mouth skeletal muscle relaxation by flavonoids of Cistus ladanifer L.: a plant defense mechanism against herbivores.

Cistus ladanifer exudate is a potent inhibitor of the sarcoplasmic reticulum Ca2+-ATPase (Ca2+-pump) of rabbit skeletal muscle, a well-established model for active transport that plays a leading role in skeletal muscle relaxation. The low concentration of exudate needed to produce 50% of the maximum inhibition of the sarcoplasmic reticulum Ca2+-ATPase activity, 40-60 microg/ml, suggests that eating only a few milligrams of C. ladanifer leaves can impair the relaxation of the mouth skeletal muscle of herbivores, as the exudate reaches up to 140 mg/g of dry leaves in summer season. The flavonoid fraction of the exudate accounts fully for the functional impairment of the sarcoplasmic reticulum produced by the exudate (up to a dose of 250-300 microg/ml). The flavonoids present in this exudate impair the skeletal muscle sarcoplasmic reticulum function at two different levels: (i) by inhibition of the Ca2+-ATPase activity, and (ii) by decreasing the steady state ATP-dependent Ca2+-accumulation. Among the exudate flavonoids, apigenin and 3,7-di-O-methyl kaempferol are the most potent inhibitors of the skeletal muscle sarcoplasmic reticulum. We conclude that the flavonoids of this exudate can elicit an avoidance reaction of the herbivores eating C. ladanifer leaves through impairment of mouth skeletal muscle relaxation.

Animals↗
PubMed1999

Muscle relaxant activity of methocarbamol enantiomers in mice.

Documented studies support the emerging idea that drug enantiomers could have different pharmacological activity. Our bibliographical data have shown that so far no report has been published on the pharmacological activity of individual enantiomers of methocarbamol. This study was conducted to characterize the muscle relaxant activity of methocarbamol enantiomers. The rotarod test was used to compare the muscle relaxant activity of racemic methocarbamol and pure enantiomers after intraperitoneal administration of the enantiomers to mice. The results show that (+)-R-methocarbamol has higher muscle relaxant activity compared with racemic methocarbamol or (-)-S-methocarbamol.

Animals↗
PubMed2006

Arginase strongly impairs neuronal nitric oxide-mediated airway smooth muscle relaxation in allergic asthma.

BACKGROUND: Using guinea pig tracheal preparations, we have recently shown that endogenous arginase activity attenuates inhibitory nonadrenergic noncholinergic (iNANC) nerve-mediated airway smooth muscle relaxation by reducing nitric oxide (NO) production--due to competition with neuronal NO-synthase (nNOS) for the common substrate, L-arginine. Furthermore, in a guinea pig model of allergic asthma, airway arginase activity is markedly increased after the early asthmatic reaction (EAR), leading to deficiency of agonist-induced, epithelium-derived NO and subsequent airway hyperreactivity. In this study, we investigated whether increased arginase activity after the EAR affects iNANC nerve-derived NO production and airway smooth muscle relaxation. METHODS: Electrical field stimulation (EFS; 150 mA, 4 ms, 4 s, 0.5-16 Hz)-induced relaxation was measured in tracheal open-ring preparations precontracted to 30% with histamine in the presence of 1 microM atropine and 3 microM indomethacin. The contribution of NO to EFS-induced relaxation was assessed by the nonselective NOS inhibitor Nomega-nitro-L-arginine (L-NNA, 100 microM), while the involvement of arginase activity in the regulation of EFS-induced NO production and relaxation was investigated by the effect of the specific arginase inhibitor Nomega-hydroxy-nor-L-arginine (nor-NOHA, 10 microM). Furthermore, the role of substrate availability to nNOS was measured in the presence of exogenous L-arginine (5.0 mM). RESULTS: At 6 h after ovalbumin-challenge (after the EAR), EFS-induced relaxation (ranging from 3.2 +/- 1.1% at 0.5 Hz to 58.5 +/- 2.2% at 16 Hz) was significantly decreased compared to unchallenged controls (7.1 +/- 0.8% to 75.8 +/- 0.7%; P < 0.05 all). In contrast to unchallenged controls, the NOS inhibitor L-NNA did not affect EFS-induced relaxation after allergen challenge, indicating that NO deficiency underlies the impaired relaxation. Remarkably, the specific arginase inhibitor nor-NOHA normalized the impaired relaxation to unchallenged control (P < 0.05 all), which effect was inhibited by L-NNA (P < 0.01 all). Moreover, the effect of nor-NOHA was mimicked by exogenous L-arginine. CONCLUSION: The results clearly demonstrate that increased arginase activity after the allergen-induced EAR contributes to a deficiency of iNANC nerve-derived NO and decreased airway smooth muscle relaxation, presumably via increased substrate competition with nNOS.

Animals↗
PubMed1999

Smooth muscle relaxant activity of pterosin Z and related compounds.

The natural products pterosin Z, acetylpterosin Z, originally from the fern Pteridium aquilinum, and their isopterosin analogues have been synthesized and their smooth muscle relaxation activity has been measured. All of the test compounds show activity with pterosin Z being the most active (EC50 = 1.3 +/- 0.1 x 10(-6) M), exhibiting 100 times the activity reported for the related fern metabolites onitin (EC50 = 1 x 10(-4) M), onotisin (EC50 = 2 x 10(-3) M) and otninoside (EC50 = 7 x 10(-4) M). The smooth muscle relaxant activity of pterosin Z is approximately equipotent with that of the related fungal pterosin (EC50 of 2.9 +/- 1.6 x 10(-6) M). These results suggest that smooth muscle relaxant activity is reduced when a phenol group is present in the pterosin nucleus and when one of the dimethyl groups is derivatized.

Animals↗
PubMed1989

A model for determining the influence of hepatic uptake of nondepolarizing muscle relaxants in the pig.

Hepatic uptake and distribution of nondepolarizing muscle relaxants in pigs was investigated. A portocaval shunt preparation enabled the determination of the pharmacodynamics of nondepolarizing muscle relaxants both during temporary liver exclusion and intraportal injection in the same animal. To demonstrate the validity of the model in pigs, in a pilot study the influence of hepatic uptake on neuromuscular blockade by pancuronium (n = 3) and its congener Org 6368 (n = 3) was determined. Thereafter, the influence of hepatic uptake on neuromuscular blockade by gallamine (3.4 mg/kg, n = 5), Org 6368 (0.3 mg/kg, n = 5), and vecuronium (0.1 mg/kg, n = 4 and 0.15 mg/kg, n = 5) was studied in pigs anesthetized with pentobarbital. Each pig received one relaxant, which was injected four consecutive times under different conditions. The first injection was into the jugular vein (iv) the second into the portal vein, the third was iv while the liver was excluded for 10 min and the fourth was iv (control). After each injection the onset time, intensity, recovery rate, and total duration of neuromuscular blockade were measured. These variables were compared between the four injections for each relaxant. In the pilot study the influence of hepatic uptake on neuromuscular blockade was similar for pancuronium and Org 6368. For gallamine the onset time, intensity, recovery rate, and duration of action were similar after all four injections. For Org 6368 the variables of neuromuscular blockade were similar after iv and intraportal injection, but exclusion of the liver prolonged the neuromuscular block.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗