Neuromuscular Pharmacology of TAAC3, a New Nondepolarizing Muscle Relaxant with Rapid Onset and Ultrashort Duration of Action

2002 ◽  
Vol 94 (4) ◽  
pp. 879-885 ◽  
Author(s):  
Laszlo Gyermek ◽  
Chingmuh Lee ◽  
Young-Moon Cho ◽  
N. Nguyen ◽  
S. K. Tsai
1997 ◽  
Vol 25 (2) ◽  
pp. 133-137
Author(s):  
L. Cade ◽  
P. Kakulas

Laparoscopy is commonly performed as a daycase procedure and requires satisfactory but brief and readily reversible muscle relaxation with good intubating conditions. We have examined the use of the new nondepolarizing muscle relaxant, mivacurium, in this setting and compared it with the two most commonly used such drugs in day surgery, atracurium and vecuronium, in a prospective randomized trial of 107 patients. Mivacurium provided a significantly more rapid onset and briefer duration of muscle relaxation, which was readily reversible with or without pharmacological antagonism.


2003 ◽  
Vol 98 (5) ◽  
pp. 1042-1048 ◽  
Author(s):  
Bertrand Debaene ◽  
Benoît Plaud ◽  
Marie-Pierre Dilly ◽  
François Donati

Background Residual neuromuscular blockade remains a problem even after short surgical procedures. The train-of-four (TOF) ratio at the adductor pollicis required to avoid residual paralysis is now considered to be at least 0.9. The incidence of residual paralysis using this new threshold is not known, especially after a single intubating dose of intermediate-duration nondepolarizing relaxant. Therefore, the aim of the study was to determine the incidence of residual paralysis in the postanesthesia care unit after a single intubating dose of twice the ED(95) of a nondepolarizing muscle relaxant with an intermediate duration of action. Methods Five hundred twenty-six patients were enrolled. They received a single dose of vecuronium, rocuronium, or atracurium to facilitate tracheal intubation and received no more relaxant thereafter. Neuromuscular blockade was not reversed at the end of the procedure. On arrival in the postanesthesia care unit, the TOF ratio was measured at the adductor pollicis, using acceleromyography. Head lift, tongue depressor test, and manual assessment of TOF and DBS fade were also performed. The time delay between the injection of muscle relaxant and quantitative measurement of neuromuscular blockade was calculated from computerized anesthetic records. Results The TOF ratios less than 0.7 and 0.9 were observed in 16% and 45% of the patients, respectively. Two hundred thirty-nine patients were tested 2 h or more after the administration of the muscle relaxant. Ten percent of these patients had a TOF ratio less than 0.7, and 37% had a TOF ratio less than 0.9. Clinical tests (head lift and tongue depressor) and manual assessment of fade showed a poor sensitivity (11-14%) to detect residual blockade (TOF < 0.9). Conclusion After a single dose of intermediate-duration muscle relaxant and no reversal, residual paralysis is common, even more than 2 h after the administration of muscle relaxant. Quantitative measurement of neuromuscular transmission is the only recommended method to diagnose residual block.


1996 ◽  
Vol 84 (5) ◽  
pp. 1083-1091 ◽  
Author(s):  
Shahpoor S. Sorooshian ◽  
Michael A. Stafford ◽  
Nigel B. Eastwood ◽  
Alastair H. Boyd ◽  
Christopher J. Hull ◽  
...  

Background The effects of a muscle relaxant may differ in elderly compared with young adult patients for a variety of reasons. The authors compared the effects of a new muscle relaxant (cisatracurium) in young and elderly adults and used pharmacokinetic/pharmacodynamic modeling to identify factors explaining differences in time course of effect. Methods Thirty-one young (18-50 yr) and 33 elderly ( > 65 yr) patients anesthetized with nitrous oxide, isoflurane, and fetanyl were studied. Cisatracurium (0.1 mg/kg) was given after induction of anesthesia and later additional boluses of 0.025 mg/kg or an infusion of cisatracurium was given. Neuromuscular transmission was measured using the first twitch of the train-of-four response at the adductor pollicis after supramaximal stimulation of the ulnar nerve at 2 Hz every 15 s. Five venous blood samples were obtained for plasma drug concentration at intervals ranging from 2 to 120 min from every patient. Three additional samples were obtained from those who received an infusion. A population pharmacokinetic/pharmacodynamic model was fitted to the plasma concentration and effect data. The parameters of the model were permitted to vary with age to identify where differences existed between young and elderly adults. Results Onset of block was delayed in the elderly; values being mean 3.0 (95% confidence interval 1.75-11.4) min and 4.0 (2.4-6.5) min in the young and elderly, respectively (P < 0.01). Duration of action was similar in the two groups. Plasma clearance was 319 (293-345) ml/min in the study population and did not differ between young and elderly patients. Apparent volume of distribution was 13.28 (9.9-16.7) 1 and 9.6 (7.6-11.7) 1 in the elderly and young adults, respectively (P < 0.05). There also were differences in pharmacodynamic parameters between the young and elderly; the predominant change being a slower rate of biophase equilibration (ke0) in the elderly (0.060 [0.052-0.068])/min compared with the young (0.071 [0.065-0.077]/min; P < 0.05). Conclusions The pharmacokinetics of cisatracurium differ only marginally between young and elderly adults. Onset is delayed in the elderly because of slower biophase equilibration.


2021 ◽  
Vol 18 (2) ◽  
pp. 66-76
Author(s):  
Alexander V. Emelyanov ◽  
Galina R. Sergeeva ◽  
Evgenia V. Leshenkova

The second generation of H1-antihistamines is approved for the stepwise treatment of seasonal and perennial allergic rhinitis in adults and children by international and national guidelines. They reduce the severity of nasal and ocular symptoms of rhinitis and improve the quality of life of patients. Bilastine, a piperidine derivative, is a novel H1-antihistamine. It has a potent and selective effect on H1- receptors and a rapid onset and long duration of action and substantially reduces nasal and ocular symptoms of seasonal and perennial allergic rhinitis. Bilastine has no clinically substantial hepatic metabolism and has a high safety profile: it has no sedative effect, does not affect cognitive functions, has no cardiotoxic effects, and does not interact with alcohol and benzodiazepines in normal and high doses. Tachyphylaxis does not develop despite long-term (up to 1 year) use. Bilastine is registered for clinical use in adults and children aged 12 years. The results of clinical and experimental studies have demonstrated that bilastine has many of the features of modern H1-antihistamines recommended by international guidelines.


Peptides ◽  
1992 ◽  
pp. 88-90 ◽  
Author(s):  
H. B. Long ◽  
J. C. Baker ◽  
R. M. Belagaje ◽  
R. D. DiMarchi ◽  
B. H. Frank ◽  
...  

1993 ◽  
Vol 26 (1) ◽  
pp. 50
Author(s):  
Jin Seung Lee ◽  
Jang Weon Lee ◽  
Si Young Ok ◽  
Yoo Jae Kim ◽  
Wook Park ◽  
...  

1997 ◽  
Vol 84 (5) ◽  
pp. 1011-1018 ◽  
Author(s):  
Raymond Kahwaji ◽  
David R. Bevan ◽  
George Bikhazi ◽  
Colin A. Shanks ◽  
Robert J. Fragen ◽  
...  

1976 ◽  
Vol 4 (3) ◽  
pp. 239-244 ◽  
Author(s):  
L. T. Seow ◽  
H. H. Chiu ◽  
C. Y. Tye

A randomized double-blind trial compared 1·0% etidocaine and 1·5% lignocaine (both with 1/200,000 adrenaline), for caudal anaesthesia for pelvic floor repair. Etidocaine was highly effective for the surgical procedure, with rapid onset of action, adequate muscle relaxation and longer duration of action. Its use for post-operative analgesia may be hindered by the concomitant immobilization of the legs. The problem of tachyphylaxis with etidocaine needs further investigation.


1987 ◽  
Vol 1 (2) ◽  
pp. 87-94 ◽  
Author(s):  
John T. Connell ◽  
M. Ines Linzmayer

Oxymetazoline (Afrin) and pseudoephedrine (Sudafed) were compared by rhinomanometric measurements using nasal airflow, a parameter of nasal airway patency, and therefore airway congestion. Oxymetazoline had a more rapid onset and duration of action, greater improvement in airway patency, and longer action than pseudoephedrine, the best of the oral decongestants. The decongestive effect was more reliable for oxymetazoline with 28 of 29 subjects experiencing some degree of decongestion compared to 21 of 30 for pseudoephedrine. Utilizing a combination of oral and topical decongestants may result in the most logical regimen for treatment of nasal congestion. Oxymetazoline is the drug of choice for night time decongestion.


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