Arzneimittel Forsch
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Arzneimittel Forsch · Jan 1980
The effect of the steroid muscle relaxant pipecurium bromide on the acetylcholinesterase activity of red blood cells in vitro.
The acetylcholinesterase (AchE) inhibitory effect of a muscle relaxant 2 beta,16 beta-bis-(4'-dimethyl-1'-piperazino)-3 alpha,17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), was studied in vitro. The inhibition of AchE activity of human red blood cells, expressed as pI50, was 3.99, whereas that of serum cholinesterase (ChE) was 4.33. ⋯ The combined effect of pipecurium bromide and of some other diamino-azasteroid agent proved to be additive. Pipecurium bromide showed mixed-type inhibitory effect both on AchE and ChE.
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Arzneimittel Forsch · Jan 1980
Randomized Controlled Trial Comparative Study Clinical TrialComparative clinical study of pipecurium bromide and pancuronium bromide.
The properties and the effects of a new steroid muscle relaxant preparation 2 beta,16 beta-bis(4'-dimethyl-1'-piperazino)-3 alpha,17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan) were compared to those of pancuronium bromide in a controlled randomized clinicopharmacological study using ataranalgesic anaesthesiological technique. In 45 cases pipecurium bromide, in other 45 cases pancuronium bromide was used as long-acting muscle relaxant in anaesthesia for general surgical procedures. According to the results, pipecurium bromide is approximately 20% more potent than pancuronium bromide, it induces mechanical response characteristic for non-depolarizing muscle relaxants, and the residual neuromuscular blockade can be antagonized completely by neostigmine. ⋯ LDH) level changes observed. Pipecurium bromide did not influence blood pressure but in contrast to the heart rate increasing effect of pancuronium bromide, it caused mild bradycardia. On the basis of the study the drug can be used for further wide scale clinical investigations.
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The effect of oral N-(4-chlorophenyl)-N-[1-(1-methylethyl)-4-piperidinyl]benzene acetamide (lorcainide) was studied in 12 patients with frequent and stable ventricular arrhythmias resistant to a number of other antiarrhythmic agents. Ambulatory electrocardiograms were obtained before and during treatment with lorcainide and in some patients after discontinuation of the drug. Lorcainide suppressed ventricular premature contractions by more than 90% in all but one patient. ⋯ Plasma concentrations of lorcainide and of the dealkylated metabolite ranged from 0.13 to 0.27 microgram/ml and 0.25 to 0.95 microgram/ml, respectively. Side effects such as insomnia and excessive perspiration were seen in 7 and 3 patients, respectively. Lorcainide is an effective antiarrhythmic agent against ventricular arrhythmias otherwise difficult to treat.
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Arzneimittel Forsch · Jan 1980
On some properties of a new steroid curare-like compound pipecurium bromide.
In experiments on cats it has been shown that 2 beta, 16 beta-bis (4'-dimethyl-1'-piperazino)-3 alpha, 17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), is a non-depolarizing muscular blocker. The order of myorelaxation evoked by this agent is characteristic: first the chewing and limb muscles, then abdominal muscles and diaphragm and at the end intercostal muscles are relaxed. ⋯ No acetylcholinesterase inhibiting action of the compound was seen. It does not affect the central nervous system.
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The actions of the new depolarization-blocking muscle relaxant agent; 2 beta,16-beta-bis-(4'-dimethyl-1'-piperazino)-3 alpha,17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), were studied in fentanyl-N2O, in halothane-N2O and in methoxy-flurane-N2O anaesthesia in a total of 94 patients. The drug in a dose of 0.05 mg/kg body weight (recommended by the manufacturer), elicited complete muscle relaxation, which was satisfactory even for performing abdominal operations. ⋯ Transient fall of blood pressure and bradycardia (in 40.4% of the cases) were observed as side effects. Further studies are needed for the determination of the pathomechanism of bradycardia and to judge to what extent the inhalation anaesthetic agents influence the duration of action of pipecurium bromide.