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Biomedical subjects

L H Booij

Publications and source records attributed to L H Booij.

At least 127 records · Page 7Linked to original sources
PubMed1982

Org-NC45: a new steroidal non-depolarizing muscle relaxant.

Although pancuronium has fewest side effects compared to other currently used non-depolarizing muscle relaxants, it is still not the ideal relaxant. Its structural analogues have been studied to derive such an ideal relaxant. Org-NC45 meets the requirements for such a relaxant best and is therefore extensively studied. It is more potent than pancuronium, has a shorter onset and duration of action and is free from cardiovascular side effects. Histamine release could not be demonstrated. It can be easily reversed by neostigmine, pyridostigmine or 4-aminopyridine. Interaction with antibiotics and anaesthetic drugs is not different from that of pancuronium.

Humans↗
PubMed1982

The influence of halothane and enflurane on the reversibility of an Org NC45 neuromuscular blockade in cats.

The pharmacodynamics of neostigmine 20 micrograms kg-1 reversing a constant neuromuscular blockade from continuous infusion of Org NC 45 was studied in 17 cats. Six cats received only intravenous thiopental anaesthesia, another five received a 1 MAC (0.73%) inhalational concentration of halothane, and the remaining six cats received 1 MAC (1.68%) enflurane. In the enflurane group statistically significantly less Org NC 45 was needed to maintain the blockade (p less than 0.05). There was no difference in the degree of reversal or in the time course of the neostigmine activity between the 3 groups (p greater than 0.05). Only the duration of action of neostigmine was prolonged under halothane anaesthesia.

Animals↗
PubMed1982

Pharmacodynamics of vecuronium and pancuronium in cats with and without ligated renal pedicles.

The pharmacodynamic behaviour upon continuous infusion and bolus administration of pancuronium and vecuronium was studied in cats with and without ligated renal pedicles. In all circumstances vecuronium had a shorter time course of action than pancuronium. Ligation of the renal pedicles, i.e. acute renal failure, did not significantly influence the time course of the respective neuromuscular blockades. It is suggested that uptake by aspecific binding sites of the compounds is the main determining factor in termination of the blockade. A difference between acute and chronic renal failure is expected to exist.

Acute Kidney Injury↗
PubMed1982

Continuous infusion of alfentanil.

The administration of alfentanil by continuous infusion as supplementation to nitrous oxide for shortlasting anesthesias has been studied in 51 patients. Anesthesia was induced with thiopental 4 to 5 mg/kg-1. Analgesia was performed by a continuous infusion of alfentanil (0.1 mg.ml-1 in glucose 5%) preceded by a bolus injection of 0.5 mg alfentanil i.v. Supplementations of 0.25 mg alfentanil i.v. were given if indicated. The patients were divided into 4 groups, according to the rate of infusion (group I: 4 mg.hr-1; group II: 5 mg.hr-1) and to the addition of either droperidol (group III) or domperidone (group IV). Anesthesia was satisfactory in all cases. Alfentanil given by continuous infusion (4 mg/hr-1) preceded by a bolus injection (0.5 mg) provided a good basic analgesia. With this method of administration the awakening time was shorter and less analgesic was needed than after incremental dosages of alfentanil. Droperidol, almost abolished nausea and vomiting postoperatively. It, however, clearly potentiated the effect of alfentanil. Domperidone given instead of droperidol had no or little effect on postoperative nausea and vomiting.

Adult↗
PubMed1982

Comparison of diazepam and midazolam as oral premedicants for bronchoscopy under local anesthesia.

A randomized double blind comparison between diazepam 10 mg, and midazolam 15 mg as oral premedicants in diagnostic fiber optic bronchoscopy under local anesthesia was made. The subjective assessments by the patient, the observer and the bronchoscopist showed that midazolam 15 mg orally gives an at least comparable degree of sedation, relief of anxiety and patient's tolerance as diazepam 10 mg orally. Midazolam 15 mg gives some degree of anterograde amnesia where diazepam 10 mg completely fails. Psychomotor recovery after 4 hours is better after midazolam 15 mg than after diazepam 10 mg. No adverse reactions were seen with both premedicants.

Amnesia↗
PubMed1981

Pharmacokinetics and pharmacodynamics of the muscle relaxant drug Org NC-45 and each of its hydroxy metabolites in dogs.

The pharmacodynamics and pharmacokinetics of Org NC-45 and each of its metabolites were studied in anaesthetized dogs. Only Org NC-45 and C3-deacetylated NC-45 produced neuromuscular blockade at the doses studied. The plasma half-lives varied from 3 to 15 min, and are about one third of that of the structurally-related compound pancuronium. Renal excretion was of the order 5-20% and the biliary excretion 7-20% 6 h after administration of each of the 4 compounds. The apparent volume of distribution after a 1 1/2 h infustion was of the same order as the extracellular fluid volume. It seems that no significant entero-hepatic recirculation occurs. Thus, long term continuous infusions of Org NC-45 may be safe.

Animals↗
PubMed1981

Simultaneous determination and pharmacokinetics of midazolam and its hydroxymetabolites in plasma and urine of man and dog by means of high-performance liquid chromatography.

A HPLC (high performance liquid chromatography) method for the determination of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) and its hydroxy metabolites has been developed. The half-life of elimination of midazolam and the glucuronides of the metabolites 1-hydroxymethyl-midazolam, 4-hydroxy-midazolam and 1-hydroxymethyl-4-hydroxy-midazolam are identical, 53 min in dogs and 90 min in man.

Aged↗
PubMed1981

Midazolam as a sedative on regional anesthesia. Preliminary results.

Diazepam is widely used as a sedative for loco-regional anesthesia. The venous irritation and long duration of action and hangover may be a drawback. We compared 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum), a new water-soluble benzodiazepine, with diazepam for cardio-respiratory changes, onset time, duration of action, amnesia and venous irritation after a single i.v. shot in loco-regional anesthesia.

Anesthesia, Conduction↗
PubMed1980

Do neostigmine and 4-aminopyridine inhibit the antibacterial activity of antibiotics?

Neostigmine and 4-aminopyridine are used to antagonize the neuromuscular blockade induced by antibiotics or an antibiotic-non depolarizing blocker combination. They may also counteract the antibacterial activity of antibiotics. It was found that neostigmine and 4-aminopyridine do not interfere with antibacterial activity of antibiotics in bacterial cultures using an agar solution method. It is concluded that neostigmine and 4-aminopyridine may bae used to antagonize neuromuscular blockade induced by antibiotics alone or in combination with non-depolarizing agents.

4-Aminopyridine↗
PubMed1980

Relative potency of ORG NC 45, pancuronium, alcuronium and tubocurarine in anaesthetized man.

The relative potency, time-course of action and cardiovascular effects of Org NC 45, a new non-depolarizing neuromuscular blocking agent, have been compared with those of pancuronium, alcuronium and tubocurarine in 64 anaesthetized patients. The relative potency (ED50) to Org NC 45 was 1.74, 3.69 and 8.57 respectively. In doses which caused useful surgical relaxation, duration of action of Org NC 45 was 34%, 39% and 26% that of pancuronium, alcuroniuym and tubocurarine. After administration of repeated doses no cumulation was seen for Org NC 45. The new drug was free from any effect on arterial pressure and heart rate.

Adult↗
PubMed1980

Pharmacology of ORG NC 45 compared with other non-depolarizing neuromuscular blocking drugs.

From results of pharmacological tests on the neuromuscular and autonomic blocking actions of a series of pancuronium analogues, Org NC 45, the C16 monoquaternary analogue of pancuronium, was selected for detailed study. Org NC 45 has a non-depolarizing mechanism of action, is more rapid in onset and shorter in duration of action than pancuronium. It shows less cumulation than pancuronium or tubocurarine, and is easily antagonized by anticholinesterases and aminopyridines. Org NC 45 exhibits a low propensity to release histamine. Its ability to inhibit cholinesterases is not likely to be important at neuromuscular blocking doses. Org NC 45 possesses negligible ganglion-blocking activity and there is a wide margin between neuromuscular and vagal blocking doses. Thus cardiovascular side-effects are unlikely to occur with the use of Org NC 45. It will hydrolyse mainly to its 3-hydroxy analogue which, like Org NC 45, possesses a wide margin between neuromuscular and vagal blocking doses. Org NC 45 has a high selectivity for the neuromuscular junction and represents a potentially useful addition to the armamentarium of clinically useful muscle relaxants.

Aminopyridines↗
PubMed1980

Preliminary review of the interactions of ORG NC 45 with anaesthetics and antibiotics in animals.

In vitro (rat hemidiaphragm) and in vivo (rat and cat tibialis anterior muscle preparation) studies of the interactions between Org NC 45 and some i.v. anaesthetics and antibiotics were carried out. With the exception of ketamine 1 mg kg-1 none of the drugs tested in vivo significantly changed the time course of an Org NC 45 bolus injection. All of the drugs caused an enhancement of the neuromuscular block using infusions in vivo and also in the in vitro preparations. Org NC 45 seems to be potentiated in a manner similar to pancuronium.

Anesthetics↗
PubMed1980

First clinical experiences with ORG NC 45.

The new short-acting steroid muscle relaxant Org NC 45 was tested clinically in 18 patients and compared with a similar application of pancuronium bromide in 22 patients. Onset, duration and slope of recovery were significantly shorter for Org NC 45. No cumulative effects were noticed over several consecutive doses of Org NC 45. No tachycardia or arterial pressure changes were noticed with doses of Org NC 45 up to 130 microgram kg-1, which was three times the 95% blocking dose.

Adult↗
PubMed1980

Intradermal histamine releasing effect caused by Org-NC 45. A comparison with pancuronium, metocurine and d-tubocurarine.

Histamine release caused by Org-NC 45, pancuronium, metocurine and d-tubocurarine was determined by measuring the diameter of the redness and skin induration following the intradermal injection of these drugs. d-Tubocurarine and metocurine caused the largest diameter of redness and induration, followed by pancuronium. Org-NC 45 caused the smallest reaction. We conclude that Org-NC 45 may be the drug of choice in patients with asthma and allergic reactions.

Adult↗