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Biomedical subjects

L H Booij

Publications and source records attributed to L H Booij.

140 records · Page 8Linked to original sources
PubMed1980

Intubation conditions and reversibility of a new non-depolarizing neuromuscular blocking agent, Org-NC45.

We describe the clinical use, for intubation purposes, of Org-NC45, a new non-depolarizing neuromuscular blocking agent. Administration of 50 and 72 microgram/kg of this drug allowed good to excellent endotracheal intubation conditions within 3 and 2 min, respectively. In none of the cases ws a significant change in blood pressure or heart rate seen after the injection of Org-NC45. The resulting block was of short duration and, if necessary, was easily reversed with neostigmine or pyridostigmine.

Adult↗
PubMed1980

The comparative neuromuscular blocking effects of some aminoglycoside antibiotics.

The neuromuscular blocking effects of aminoglycoside antibiotics were tested in the isolated phrenic nervediaphragm preparation of the rat. The neuromuscular blocking potencies were netilmicin equals sisomicin much greater than neomycin much greater than gentamicin much greater than tobramycin. The EC 50's (concentration resulting in 50 percent depression of the original twitch tension) were respectively 13.3 x 10(-4); 13.4 x 10(-4); 13.6 x 10(-4); 15.1 x 10(-4); and 95.3 x 10(-4) Mol/l for netilmicin, sisomicin, neomycin, gentamicin and tobramycin. When a threshold dose of pancuronium was added to the bathing fluid the EC 50's were diminished respectively by a factor of 0.4 (sisomicin and neomycin) 0.5 (tobramycin) and 0.6 (netilmicin and gentamicin). Addition of a threshold dose of Org-NC45, a new steroidal non-depolarizing muscle relaxant, diminished the EC 50's to the same extent. The neuromuscular blocking effects of pancuronium and Org-NC45 themselves were potentiated by pretreatment of the preparations with a threshold dose of the aminoglycoside. Comparison of the results demonstrated the following potentiating effects: netilmicin equals sisomicin much greater than neomycin much greater than gentamicin greater than tobramycin. Which is in the same sequence s the neuromuscular blocking potencies of these drugs.

Aminoglycosides↗
PubMed1980

Cardiovascular and neuromuscular effects of Org NC 45, pancuronium, metocurine, and d-tubocurarine in dogs.

We compared the cardiovascular and neuromuscular effects of Org NC 45 with those of pancuronium, metocurine, and d-tubocurarine in six dogs anesthetized with halothane. The ED90 (dose of drug which produced a 90% depression of twitch tension) of Org NC 45, pancuronium, metocurine, and d-tubocurarine was 14 +/- 3, 22 +/- 3, 63 +/- 19, and 130 +/- 19 micrograms/kg, respectively. All subsequent neuromuscular and cardiovascular effects were determined from a dose equal to 3 times the ED90 of muscle relaxant. Org NC 45, pancuronium, metocurine, and d-tubocurarine produced a neuromuscular blockade with a during (time from relaxant administration until recovery 50% of the original twitch tension) of 42 +/- 2, 108 +/- 10, 109 +/- 21, and 100 +/- 19 minutes, respectively. Org NC 45 caused no significant cardiovascular changes. Pancuronium increased heart rate, mean arterial blood pressure, cardiac output, and pulmonary wedge pressure, and it decreased systemic vascular resistance (p less than 0.05). Although metocurine also increased heart rate and cardiac output (p less than 0.05), mean arterial blood pressure and pulmonary wedge pressure did not change. d-Tubocurarine decreased all cardiovascular parameters except heart rate which increased significantly (p less than 0.05). We conclude that Org NC 45 produces a neuromuscular blockade of shorter duration with fewer cardiovascular changes than that of pancuronium, metocurine, or d-tubocurarine.

Animals↗
PubMed1980

Antagonism of Org NC 45 neuromuscular blockade by neostigmine, pyridostigmine, and 4-aminopyridine.

The antagonism of Org NC 45 neuromuscular blockade by neostigmine, pyridostigmine, 4-aminopyridine, and their combinations was studied in the in vivo rat sciatic nerve anterior tibialis preparation using the constant infusion of Org NC 45 technique. The ED50 (dose of drug which produced a 50% antagonism) of neostigmine, pyridostigmine, and 4-aminopyridine were 14.5, 75, and 466 micrograms/kg, respectively. The addition of 100 microgram/kg of 4-aminopyridine, which produced no antagonism by itself, decreased neostigmine ED50 to 9.8 micrograms/kg. The addition of 200 micrograms/kg of 4-aminopyridine, which produced a 14.8% antagonism by itself, decreased the ED50 of pyridostigmine to 17.5 micrograms/kg. We concluded that neostigmine, pyridostigmine, and 4-aminopyridine effectively antagonize an Org NC 45 neuromuscular blockade. Neostigmine and pyridostigmine interact with 4-aminopyridine in a synergistic manner. The doses of antagonists were very similar to those required to antagonize a pancuronium neuromuscular blockade.

Aminopyridines↗
PubMed1980

Continuous infusion of etomidate as a method for outpatient anesthesia.

Fourteen, ASA class 1 or 2, outpatients of either sex, admitted for elective arthroscopy of the knees, were anesthetized by continuous infusion of etomidate. After a mean infusion time +/- SD of 38.2 +/- 11.6 min., the awakening time was 4.96 +/- 3.29 min. Five patients (37.7%) had mild pain on the injection side and 3 (21.5%) showed myoclonic movements. Postanesthetically 6 patients (42%) were nauseated and 4 (28.5%) were vomiting. After 130.4 +/- 38.33 min. all patients could be sent home. It is concluded that continuous infusion of etomidate is unless these side effects a good alternative anesthesia technique for outpatients. (Acta anaesth. belg., 1980, 31, 39-43).

Adult↗
PubMed1979

4-Aminopyridine potentiates neostigmine and pyridostigmine in man.

To elucidate the interaction of 4-aminopyridine with neostigmine and pyridostigmine, the authors studied 57 anesthetized surgical patients using a technique of constant infusion of pancuronium to quantitate antagonist activity. 4-Aminopyridine, 0.15 or 0.35 mg/kg, produced no antagonism, while 0.5 mg/kg produced a mean 24 +/- 6 per cent (peak) antagonism. The dose that produced 50 per cent antagonism (ED50) of neostigmine alone was 22 micrograms/kg; with 0.35 mg/kg 4-aminopyridine, it was 7 micrograms/kg. The ED50 of pyridostigmine alone was 110 micrograms/kg; with 0.35 mg/kg 4-aminopyridine, it was 27 micrograms/kg. 4-Aminopyridine prolonged the onset times of both neostigmine and pyridostigmine, but prolonged the duration of action of neostigmine only. At a given level of antagonism of pancuronium, adding 4-aminopyridine 0.35 mg/kg, to neostigmine and to pyridostigmine decreased the amounts of atropine needed to prevent a change in heart rate by 68 and 70 per cent, respectively. The authors conclude that 4-aminopyridine potentiates antagonism of a pancuronium-induced neuromuscular blockade by neostigmine or pyridostigmine. Also, less atropine is needed to prevent cardiac muscarinic stimulation when 4-aminopyridine is used with either neostigmine or pyridostigmine.

Adult↗
PubMed1979

Effect of different anesthetics on the pharmacokinetics and pharmacodynamics of pancuronium in the cat.

To investigate the effect of different anesthetics on the pharmacokinetics and pharmacodynamics of pancuronium, 120 microgram/kg i.v., cats were anesthetized with either pentobarbital (N = 4), ketamine (N = 4), enflurane (N = 5), or halothane (N = 5). A longer onset time and duration of neuromuscular blockade occurred during enflurane and halothane anesthesia. The apparent elimination half-life was longer and the total voluem of distribution at steady state larger during halothane anesthesia. The plasma concentration of pancuronium required for neuromuscular blockades was less during enflurane than during the other three anesthetics. We conclude that inhalation anesthetics may prolong a neuromuscular blockade by altering both the pharmacokinetics and pharmacodynamics of pancuronium.

Adjuvants, Anesthesia↗
PubMed1979

The comparative influence of gamma-hydroxy butyric acid, althesin and etomidate on the neuromuscular blocking potency of pancuronium in man.

The potentiating effect of gamma-hydroxy butyric acid (GHB), Althesin and etomidate on pancuronium was studied in man. GHB proved to influence pancuronium the least whereas Althesin and etomidate potentiate considerably. It is concluded that the amount of non-depolarizing relaxant needed depends on the type of anesthesia given. For neuromuscular blocking studies, GHB and/or thiopentone anesthesia seem to be preferable.

Alfaxalone Alfadolone Mixture↗
PubMed1978

Potentiation of neostigmine and pyridostigmine by 4-aminopyridine in the rat.

The interaction between 4-aminopyridine and neostigmine or pyridostigmine was studied in vivo in the rat sciatic nerve-anterior tibialis preparation using the constant infusion of pancuronium technique. The ED50 (dose of drug which produced a 50% antagonism) of neostigmine, pyridostigmine and 4-aminopyridine were 18, 49 and 440 microgram kg(-1) respectively. The addition of 100 microgram kg(-1) of 4-aminopyridine, which produced no antagonism by itself, decreased the neostigmine ED50 to 7.4 microgram kg(-1). The addition of 200 microgram kg(-1) of 4-aminopyridine, which produced a 30% antagonism by itself, decreased the ED50 of pyridostigmine to 11 microgram kg(-1). We conclude that both neostigmine and pyridostigmine interact with 4-aminopyrine synergistically.

Aminopyridines↗
PubMed1978

Hypothermia and the pharmacokinetics and pharmacodynamics of pancuronium in the cat.

We tested the effect of hypothermia on the pharmacokinetics and pharmacodynamics of pancuronium in the cat. In 14 cats given pancuronium, 120 microgram/kg i.v., we found that neuromuscular block lasted between 2.5 and 3.0 times longer at 29 degrees C (N = 5) than at 34 degrees C (N = 5) or 39 degrees C (N = 4). The apparent plasma elimination half-life was 46 +/- 7 min (S.E.) at 29 degrees C as compared to 21 +/- 2 and 25 +/- 6 min at 34 and 39 degrees C, respectively. The volume of distribution of the central compartment and total volume of distribution at steady state were less at 29 and 34 dgrees C than at 39 degrees C. Total plasma clearance was 4.3 +/- 0.4 ml/kg/min at 29 degrees C and 10.7 +/- 0.9 and 10.9 +/- 1.5 ml/kg/min at 34 and 39 degrees C, respectively. The reduced plasma clearance resulted at least in part from a markedly reduced biliary and urinary excretion of pancuronium at 29 degrees C as compared to 34 and 39 degrees C. In four other cats, the plasma concentration of pancuronium was correlated with depression of twitch tension under steady-state conditions. The ED50 of pancuronium (plasma concentration required for a 50% depression of twitch tension) was 0.035 and 0.073 microgram/ml at 29 and 38 degrees C, respectively. We conclude that a pancuronium neuromuscular block is prolonged at 29 degrees C because of an increased sensitivity of the neuromuscular junction to pancuronium and delayed biliary and urinary excretion.

Animals↗
PubMed1978

The comparative potency and pharmacokinetics of pancuronium and its metabolites in anesthetized man.

To determine the potency of pancuronium and its metabolites, 3-OH-, 17-OH- and 3,17-OH-pancuronium, cumulative dose-response curves were determined in five anesthetized patients with each drug. Pancuronium (ED50 = 0.041 mg/kg) was 2 times more potent than 3-OH-pancuronium (ED50 = 0.082 mg/kg), 50 times more potent than 17-OH-pancuronium (ED50 = 2.0 mg/kg) and 54 times more potent than 3,17-OH--pancuronium (ED50 = 2.15 mg/kg). In 21 other patients, one equipotent dose of either pancuronium or one of its metabolites was given as an i.v. bolus. Onset time and duration of neuromuscular blockade from 3-OH- and 3,17-OH-pancuronium did not differ significantly from that of pancuronium; 17-OH-pancuronium had a shorter duration of action than did pancuronium. Although pancuronium tended to have a slightly longer elimination half-life, the pharmacokinetics of the four drugs did not differ significantly. The elimination half-lifes were 110, 68, 73 and 71 min for pancuronium and its 3-OH, 17-OH and 3,17-OH derivatives, respectively. We conclude that although pancuronium is more potent than its 3-OH, 17-OH and 3,17-OH metabolites, the pharmacokinetics of these three metabolites do not differ from each other and from that of pancuronium.

Dose-Response Relationship, Drug↗
PubMedDate not supplied

Neostigmine and 4-aminopyridine antagonism of lincomycin-pancuronium neuromuscular blockade in man.

Seven anesthetized patients were studied to determine the interaction between pancuronium and lincomycin and the ability of neostigmine and 4-aminopyridine to antagonize the block. Lincomycin 600 mg given IV alone did not decrease twitch tension. An 8 to 10% decrease in twitch tension occurred when lincomycin was given after neostigmine antagonism of pancuronium. Lincomycin augmented a partial pancuronium neuromuscular blockade. The combined lincomycin-pancuronium neuromuscular blockade was effectively antagonized by both neostigmine and 4-aminopyridine although the latter produced a slower rate of antagonism. The authros conclude that lincomycin, 600 mg IV, augments a pancuronium neurovascular blockade. 4-Aminopyridine offers no advantage over neostigmine and, in fact, may offer a disadvantage because of a slower rate of antagonism.

Adolescent↗
PubMedDate not supplied

Antagonism of pancuronium and its metabolites by neostigmine in cats.

Antagonism by neostigmine of neuromuscular blockade produced by pancuronium or its metabolites was studied in the cat anterior or tibialis muscle-peroneal nerve preparation using constant infusions of muscle relaxants. The ED50 of neostigmine (dose which caused a 50% antagonism) was 16, 11, 29, and 26 micrograms/kg for pancuronium, 3-hydroxypancuronium, 17-hydroxypancuronium, and 3, 17-hydroxypancuronium, respectively. Times of onset of neostigmine action were shorter when antagonizing 17-hydroxypancuronium neuromuscular blockade. Duration of neostigmine action when antagonizing 17- or 3, 17-hydroxypancuronium blockade was shorter than with pancuronium or 3-hydroxypancuronium. We conclude that more neostigmine is required to antagonize 17- or 3,17-hydroxypancuronium neuromuscular blockade than is required to antagonize pancuronium. Conversely, less neostigmine was required to antagonize 3-hydroxypancuronium blockade.

Animals↗