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At least 829 records · Page 46Linked to original sources
PubMed1996

[Acid base changes and muscle relaxants].

Previous publications have provided conflicting results concerning the effects of respiratory and metabolic acid base changes on the neuromuscular effects of nondepolarizing muscle relaxants. The varying results can be attributed not only to experimental design or species difference, but also to the accompanying changes in the pharmacokinetics in vivo. Using the phrenic nerve-hemidiaphragm preparation of rats, in which many variables of in vivo studies can be eliminated, respiratory and metabolic acid-base changes were induced by varying carbon dioxide (PCO2) and bicarbonate (HCO3) concentrations in the Krebs' solution and their effects on the potencies of muscle relaxants were compared. Decreasing pH by increasing Pco2 or by decreasing HCO3 increased the potencies of the monoquaternary relaxants (d-tubocurarine, vecuronium and rocuronium), while pH changes did not affect the potencies of the bisquaternary relaxants (metocurine, pancuronium and pipecuronium). Above difference between mono- and bisquaternary relaxants may reflect pH-induced changes in the ionization of the tertiary ammonium and resulting in changes in the sensitivity to the anionic nicotinic receptors. Neostigmine-induced antagonism was not affected by acid-base changes. These results in vitro were compared and correlated with the previous results in vivo.

Acid-Base Equilibrium↗
PubMed1998

[Advances in anesthesiology in the 90's].

Author looks over the novelties in anaesthesiology in the 90-ies; (1) effort to relief not only the postoperative, but in general, every kind of pain; (2) publication of evidence based guidelines; (3) standpoints according to perioperative risk factors; (4) conception of preemptive analgesia; (5) usage of modern brain imaging techniques in anaesthesiology also; (6) researches about the sites, where general anaesthetics exert their effect; (7) new volatile anaesthetics (desflurane, sevoflurane); (8) researches, targeting the use of xenon; (9) new i.v. anaesthetics-analgesics (propofol, remifentanil, S(+)-ketamine, eltanolone) and their administration (TCI); (10) potential interactions between NO and anaesthetic agents; (11) new neuromuscular blocking drugs (mivacurium, rocuronium, cis-atracurium) and the new possibilities of neuromuscular monitoring; (12) question of difficult intubation (McCoy and bullard laringoscopes, laryngeal mask); (13) synthesis of the new elements for the challenges of the surgical practice: the anaesthesiological solution of laparoscopic surgery, one-day surgery, minimally invasive heart-surgery; (14) TIVA (recognition of awareness during operation); (15) closed circuit anaesthesia; (16) reduction of expenses; (17) application of computer and data management techniques; (18) organizational steps in order to achieve an integrated standard throughout the country.

Anesthesia↗
PubMedDate not supplied

[Postsynaptic nondepolarizing muscle relaxants in clinical practice].

Several postsynaptic nondepolarizing muscle relaxants are used today mainly for maintenance of muscular relaxation in surgical operations. They possess a highly selective effect on the cholinoceptors (CC) of the skeletal muscle postsynaptic membrane. Aminosteroid derivatives are important among them. The first to be suggested was pancuronium, and later pipecurium and the monoquaternary aminosteroid derivatives vecoronium and rocuronium. Highly selective muscle relaxants are atracurium and its isomers, cisatracurium in particular, as well as some atracurium derivatives: mivacurium and doxacurium. Tercuronium also has a highly selective effect on the CC of the skeletal muscles.

Adult↗
PubMedDate not supplied

[Cisatracurium].

Cisatracurium is one of ten isomers that form the racemic mix of atracurium (51W89 or 1 R-cis, 1'R-cis atracurium). It is three times more potent than atracurium itself and hemodynamically stable thanks to its scarce release of histamine. Cisatracurium is hydrolyzed mainly by the pathway of Hofmann (77%) and to a lesser degree it is metabolized by organ-dependent modes (mainly by the kidney (16%)). Dose therefore hardly needs to be changed for elderly patients or those with liver, kidney or cardiovascular disease. The calculated ED95 is 0.05 mg.kg-1 (0.04 mg.kg-1 in children), although a dose two to four times greater is used under clinical conditions to shorten tracheal intubation time because of low onset of blockade, particularly in comparison with rocuronium. The period of deep blockade (lack of response to neurostimulation) is prolonged by the higher dose, but recovery is dose-independent and recovery indices are similar. Cisatracurium has proven useful in intensive care because of its hemodynamic stability, which is comparable to that of steroid derivatives but with faster recovery from blockade once administration is discontinued. Its metabolism predominantly through Hofmann's pathway, with less laudanosine formation than is produced by atracurium, is also appreciated. Cisatracurium is described as the nondepolarizing muscle relaxant of choice for medium-to-long-term surgery on hemodynamically unstable patients or those with kidney or liver disease, and for neuromuscular blockade in intensive care.

Aged↗
PubMed2004

Effects of isoflurane on the actions of neuromuscular blockers on the muscle nicotine acetylcholine receptors.

In this study, we tested the hypothesis that volatile anesthetic enhancement of muscle relaxation is the result of combined drug effects on the nicotinic acetylcholine receptors. The poly A m RNA from muscle by isolation were microinjected into Xenopus oocytes for receptor expression. Concentration-effect curves for the inhibition of Ach-induced currents were established for vecuronium, rocuranium, and isoflurane. Subsequently, inhibitory effects of NDMRs were studied in the presence of the isoflurane at a concentration equivalent to half the concentration producing a 50% inhibition alone. All tested drugs produced rapid and readily reversible concentration-dependent inhibition. The 50% inhibitory concentration values were 889 micromol/L (95% CI: 711-1214 micromol). 33.4 micromol (95% CI: 27.1-41.7 nmol) and 9.2 nmol (95% CI: 7.9-12.3 nmol) for isoflurane. rocuranium and vecuronium, respectively. Coapplication of isoflurane significantly enhanced the inhibitory effects of rocuranium and vecuronium, and it was especially so at low concentration of NMDRs. Isoflurane increases the potency of NDMRs, possibly by enhancing antagonist affinity at the receptor site.

Androstanols↗
PubMed1991

The pharmacodynamics and pharmacokinetics of Org 9426, a new non-depolarizing neuromuscular blocking agent, in patients anaesthetized with nitrous oxide, halothane and fentanyl.

The pharmacodynamics and pharmacokinetics of a new non-depolarizing neuromuscular blocking agent, Org 9426, were investigated. Ten patients undergoing elective head and neck surgery and anaesthetized with nitrous oxide, halothane and fentanyl, received a bolus dose of Org 9426 (1 mg.kg-1, 3 x ED90). The isometric contractions of the adductor pollicis muscle following ulnar nerve stimulation (0.1 Hz and intermittent TOF) were measured. Blood and urine were sampled over 8 and 24 hr, respectively. Concentrations of Org 9426 and its possible metabolites in plasma and urine were determined using HPLC. Pharmacokinetic variables were calculated by iterative linear least square regression analysis. Intubation conditions were excellent one minute after administration at a neuromuscular block of 88 (13)% (Mean (CV]. Onset time until maximum block, duration until 25% recovery of twitch height, and recovery from 25 until 75% of twitch height were 1.7 (32), 53 (19) and 20 (37) min, respectively. The TOF reached a ratio of 0.7 after 87 (19) min. Half lives were 1.8 (33), 19 (34), 131 (62) min, respectively, in a three exponential decay; distribution volume at steady-state and plasma clearance were 0.264 (56) L.kg-1 and 4.0 (21) ml.kg-1.min-1, respectively. Plasma concentration at 25% recovery of the twitch height was 1.0 mg.L-1. Within 24 h, 33 (37)% of Org 9426 was excreted unchanged in the urine. Metabolites were absent both in plasma and urine. We conclude that the difference in potency between Org 9426 and vecuronium is similar to the difference between their effective concentrations.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1992

Estimation of the potency of ORG 9426 using two different modes of nerve stimulation.

The potency of ORG 9426, a new nondepolarising muscle relaxant, has been estimated using two different modes of nerve stimulation in patients anaesthetised with thiopentone, nitrous oxide-oxygen and intravenous fentanyl. The force of contraction of adductor pollicis was measured following a single twitch (ST) at 0.1 Hz or a train-of-four (TOF) mode of stimulation at 2 Hz every ten seconds. Dose-response curves were constructed using a single-dose method. The ED50, ED90 and ED95 were 147,272 and 305 micrograms.kg-1 respectively using the ST mode and 125,230 and 257 micrograms.kg-1 using the TOF mode of stimulation. The ED50S were not significantly different but the differences between ED90S and ED95S were significant (P less than 0.05) indicating greater sensitivity of the neuromuscular junction using TOF stimulation. The results of this study suggest that the information obtained by single-twitch stimulation is not the same as that obtained from the first response of the TOF stimulation, suggesting apparently increased sensitivity (and apparently greater potency) with the TOF mode of stimulation. Org 9426 appears to be a drug with relatively low potency.

Adolescent↗
PubMed2004

Bilateral sixth cranial nerve palsy after unintentional dural puncture.

PURPOSE: Bilateral sixth nerve palsy is a known though uncommon complication following dural puncture. The recommended treatment consists of hydration and alternate monocular occlusion. The value and the timing of an epidural blood patch (EBP) for sixth nerve palsy remains controversial as some authors have demonstrated benefits in performing an EBP early in course of the nerve palsy whereas others have not found any advantage when an EBP was performed later. CLINICAL FEATURES: A 40-yr-old woman developed bilateral sixth nerve palsy ten days after an unintentional dural puncture. An EBP was done within 24 hr after the onset of the symptoms and immediate improvement of the diplopia was noted by the patient and confirmed by an ophthalmologist. Complete resolution of the diplopia occurred 36 days after the dural puncture. CONCLUSION: Blood patching within 24 hr of the onset of diplopia may be a reasonable treatment for ocular nerve palsy as it relieved the postdural puncture headache and produced partial improvement of the diplopia.

Abdominal Pain↗
PubMed2002

Full remission of tardive dyskinesia following general anaesthesia.

A 44 year old woman with a severe drug induced tardive dyskinesia had previously been treated with a left thalamotomy and right deep brain stimulation. Thalamotomy abolished the right hemiballismus. Deep brain stimulation caused a moderate reduction of the remaining involuntary movements on the left side. After a minor orthopaedic operation under general anaesthesia, the dyskinesia disappeared completely, even with the deep brain stimulation turned off. The remission has now lasted for 41 months.

Adult↗
PubMed1992

Uptake of taurocholate, a vecuronium-like organic cation, ORG 9426, and ouabain into carcinogen-induced diploid and polyploid hepatocytes obtained by centrifugal elutriation.

Bile acid uptake, an important function of differentiated hepatocytes, is decreased in hepatocellular carcinomas and gamma-glutamyltranspeptidase-positive, putatively preneoplastic hepatocytes. Whether hepatic uptake is also changed in carcinogen-induced diploid hepatocytes versus polyploid hepatocytes is unknown. The present study has determined whether the hepatic uptake of three model compounds, an anionic bile acid, an organic cation and a neutral organic compound, into diploid cells is different from that in polyploid hepatocytes. These two hepatocyte populations were separated from the parent freshly isolated hepatocyte suspension by centrifugal elutriation. Flow cytometric analysis indicated that the diploid fraction contained approximately 83% diploid cells and that the polyploid fraction had about 84% polyploid hepatocytes. Initial uptake velocity was determined for taurocholate (1-50 microM), ORG 9426 (20-400 microM), a vecuronium-like cation, and ouabain (20-500 microM). Apparent Km was not different between diploid and polyploid cells for the three tested substrates, whereas apparent Vmax was decreased in diploid hepatocytes for taurocholate and ouabain by 42 and 55%, respectively. There were no changes in the hepatic uptake of ORG 9426. These data indicate that uptake by the bile acid/multispecific carrier is compromised in carcinogen-induced diploid cells.

Androstanols↗
PubMed1992

A multispecific uptake system for taurocholate, cardiac glycosides and cationic drugs in the liver.

To test the hypothesis of multiplicity in carrier-mediated uptake mechanisms for organic cations in the liver and to study the possible relation with bile acid and cardiac glycoside uptake mechanisms, mutual interaction during uptake of various radiolabeled quaternary amines has been studied in isolated rat hepatocytes. Inhibition patterns at low concentrations (1 microM) of the presumed type I monovalent organic cation tri-n-butylmethylammonium were markedly different from those at relatively high concentrations (25 microM). Both the cardiac glycoside K-strophantoside and the bile acid taurocholate clearly reduced the uptake rate of tri-n-butylmethylammonium at 25 microM whereas these agents completely failed to reduce the uptake at low concentrations of the cation. Subsequently, inhibition of uptake of some multivalent amphipathic organic cations (muscle relaxants) for the type II uptake system was investigated. It was found that the uptake of these muscle relaxants both at tracer concentrations (< 1 microM) and at relatively high concentrations (25 microM) was decreased in the presence of low concentrations of the cardiac glycoside K-strophantoside, while taurocholate only inhibited the uptake at the concentration range > 25 microM of the muscle relaxants. Procainamide ethobromide, a typical type I organic cation, did not affect the uptake either at the low or high concentration range of the muscle relaxants. It is concluded that for each of the type I-like compounds and type II-like compounds tested at least two systems are involved in uptake into hepatocytes: tri-n-butylmethylammonium in a concentration range < or = 1 microM is mainly taken up by the type I uptake system and at concentrations > or = 25 microM also by system(s) that can be inhibited by taurocholate and K-strophantoside. Bulky amphipathic organic (type II) cations at concentrations < 1 microM are also transported by an uptake system that is inhibitable by cardiac glycosides but not by bile salts. At concentrations > 25 microM these compounds are predominantly accommodated by an uptake system that possibly mediates uptake of both cardiac glycosides and bile acids. This concept was supported by the observation that both type II organic cations and bile salts can inhibit ouabain uptake, while type II organic cations as well as the cardiac glycosides reduce taurocholate uptake rate. The present data support the idea that the liver seems to be equipped with a "multispecific" uptake system that transports hydrophobic compounds irrespective of charge, including some type I and type II organic cations at relatively high substrate concentrations.

Androstanols↗
PubMedDate not supplied

Neuromuscular blocking agents in the emergency department.

Neuromuscular blocking agents (NMBAs) are utilized frequently in the emergency department (ED). We begin with a brief history of neuromuscular blockade, then review the indications and guidelines for its use in the emergency department setting. The relevant agents will be discussed focusing on dosage, side effects, and adverse reactions. Special attention will be paid to succinylcholine, the drug most commonly employed in the ED setting, followed by a summary of the nondepolarizing agents currently available, in particular the four shorter-acting agents that are most appropriate for administration in the ED.

Androstanols↗
PubMedDate not supplied

Pharmacodynamic effects of three doses of ORG 9426 used for endotracheal intubation in humans.

STUDY OBJECTIVE: To determine the pharmacodynamic characteristics of three incremental doses of ORG 9426 used for endotracheal intubation in patients. DESIGN: Double-blind, randomized administration of one of three doses of intravenous ORG 9426. SETTING: Inpatients requiring surgery at Georgetown University Medical Center. PATIENTS: Thirty-six patients, ages 18 to 65, ASA physical status I, II, and III, scheduled for general surgery. INTERVENTIONS: After Georgetown University Institutional Review Board approval and patient consent, patients were premedicated with midazolam or droperidol. Anesthesia was induced with thiopental sodium and fentanyl. Anesthesia was maintained with 60% nitrous oxide in oxygen. The ulnar nerve was stimulated supramaximally with a 2 Hz train-of-four (TOF) every 20 seconds. Thumb contractions were measured with a force transducer. When TOF and anesthesia were stable, 2, 2.5, or 3 times the ED95 of ORG 9426 (570 micrograms/kg, 710 micrograms/kg, or 850 micrograms/kg) was administered randomly. Tracheal intubation was attempted at maximal depression of the first TOF response (T1). MEASUREMENTS AND MAIN RESULTS: The following parameters were measured: time interval from the injection of ORG 9426 to 90% depression of T1 (T1 90% block), maximal T1 depression (onset time), intubating conditions, clinical duration (time for return of T1 to 25% of control), heart rate (HR), blood pressure (BP), and any adverse clinical experience. ORG 9426 provided adequate intubating conditions in all patients but two, independent of the dose used. Its onset time was rapid, but increasing the dose did not shorten the onset. T1 90% block was achieved rapidly (75 +/- 25 seconds to 78 +/- 18 seconds, means +/- SD). The clinical duration of ORG 9426 was relatively short and lengthened with increasing doses (from 36 +/- 18 minutes at 570 micrograms/kg to 42 +/- 10 minutes at 850 micrograms/kg. Spontaneous twitch recovery from 10% to 25% was similar in all dosage groups (5 +/- 1 minutes to 6 +/- 4 minutes). No clinically significant changes in HR and BP and no adverse clinical experiences were noted in any group. CONCLUSION: These findings warrant further clinical evaluation of ORG 9426 for induction and maintenance of muscle relaxation in humans.

Adolescent↗