Arzneimittel Forsch
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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.
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Arzneimittel Forsch · Jan 1980
Clinical experience with a new steroid muscle relaxant: pipecurium bromide.
Experience gained in applying to 102 surgery patients a steroid 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) is reported. Pipercurium bromide proved to be a potent muscle relaxant with a medium duration of action. ⋯ Residual relaxation can be antagonized with neostigmine. Pipecurium bromide did not influence circulation, is free of side effects and can be applied in anaesthesiologically high-risk patients.
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Arzneimittel Forsch · Jan 1980
Pharmacological study of a new competitive neuromuscular blocking steroid, pipecurium bromide.
2 beta, 16 beta-Bis-(4'-dimethyl-1'-piperazino)-3 alpha, 17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), a newly synthetized bisquaternary steroid, produces competitive neuromuscular blockade in chicks, rats, cats, rabbits and dogs. The onset of paralysis is rapid. Pipecurium bromide is 2-4 times as potent as pancuronium bromide. ⋯ Many times higher doses than the effective dose administered for 20 days, do not cause any toxic damage to respirated beagle dogs. According to examinations in rats, the placentary transfer of pipecurium bromide is lower than 0.1%. According to preliminary clinical examinations pipecurium bromide is free from side effects, and elicits as well controllable muscle relaxation.
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Arzneimittel Forsch · Jan 1979
Carcinogenic N-nitrosodimethylamine as a contamination in drugs containing 4-dimethylamino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one (amidopyrine, aminophenazone).
A total of 68 commercially available drugs containing amidopyrine were investigated for contamination with the strong carcinogen N-nitrosodimethylamine (NDMA). All samples contained varying amounts of NDMA. About half of the drugs contained 1--10 micrograms/kg, 40% contained 11--50 micrograms/kg, 7% contained 51--10 micrograms/kg and one sample had 370 micrograms/kg. ⋯ NDMA concentrations in the samples were inhomogenously distributed. It could be demonstrated that amidopyrine in substance reacts extremely rapidly with nitrogen oxides from the air to form NDMA. Ascorbic acid, which prevents nitrosamine formation in aqueous-acidic solution, under these conditions had no protective effect.