Die Abh�ngigkeit der letalen Dosis von der Infusionsgeschwindigkeit am Beispiel des g-Strophanthin und des The vetin B

Kraupp, O.; Obenaus, H.; Pillat, B.; Stumpf, Ch.

doi:10.1007/bf00246587

Cited by 5 publications

(3 citation statements)

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“…(Hobbiger, 1957a Protection against Lethal Poisoning by Neostigmine and Related Anticholinesterases.-Neostigmine, the bisneostigmine (BC-48) and the bispyridostigmine (BC-51) are potent anticholinesterases which do not inhibit cholinesterase by phosphorylation. The biochemical and pharmacological actions of the last two have been described in detail by Kraupp, Stumpf, Herzfeld, and Pillat (1955) and Herzfeld, Kraupp, Pateisky, and Stumpf (1957). To test the specificity of the antidotal action of oximes of polymethylenebispyridinium compounds in organophosphate poisoning 0.095 m.mole/kg.…”

Section: Resultsmentioning

confidence: 99%

“…of compound 16 against lethal poisoning by the bisneostigmine and the bispyridostigmine (BC-51) respectively. The latter, like organophosphates, inhibit cholinesterase for much longer periods than does neostigmine (Kraupp, Stumpf, Herzfeld and Pillat, 1955;Herzfeld, Kraupp, Pateisky, and Stumpf, 1957), and thus it is questionable whether the mechanism responsible for protection against lethal neostigmine poisoning contributes significantly to protection against lethal organophosphate poisoning. In this connexion the findings of Grob and Johns (1958a and b) must be mentioned.…”

Section: Resultsmentioning

confidence: 99%

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Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Hobbiger

Sadler

1959

British Journal of Pharmacology and Chemotherapy

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The effect of 18 pyridinium aldoximes on diethylphosphoryl-acetocholinesterase in vitro and the protection against lethal poisoning by ethyl pyrophosphate (TEPP) in mice pretreated with 0.095 m.mole/kg. of these oximes was investigated. Monoximes and dioximes of polymethylenebispyridinium compounds were studied in greater detail since they were up to 22 times more potent than pyridine-2-aldoxime methiodide (2-hydroxyiminomethyl-N-methylpyridinium iodide) in reactivating diethylphosphoryl-acetocholinesterase in vitro and protected mice against lethal poisoning by up to 15 LD100 of ethyl pyrophosphate. These oximes were also up to 52 times more potent than pyridine-2-aldoxime methiodide in reactivating di-isopropylphosphorylacetocholinesterase in vitro and were effective in preventing lethal poisoning by dyflos (di-isopropyl phosphorofluoridate). The antidotal action against diethyl phosphostigmine (Ro 3-0340) was even greater than that against ethyl pyrophosphate. Some of the most effective oximes had antidotal actions in poisoning by ethyl pyrophosphate, diethyl phosphostigmine and dyflos when given in 0.0095 m.mole/kg. and this effect was enhanced by 1 mg./kg. atropine sulphate. In vivo reactivation of diethylphosphoryl-acetocholinesterases by 0.0095 or 0.095 m.mole/kg. of oximes of polymethylenebispyridinium compounds was demonstrated in blood but not in brain. Atropine-like and neuromuscular blocking activities were studied on isolated organs and protection against lethal doses of neostigmine and related anticholinesterases were also investigated. Some of the oximes of polymethylenebispyridinium compounds have, relative to pyridine-2-aldoxime methiodide, a higher therapeutic ratio in mice and considerably greater water-solubility. The possible advantages to be gained from their use in preference to pyridine-2-aldoxime methiodide are discussed.The interaction between anticholinesterases of the organophosphate type and acetocholinesterase (also often referred to as true cholinesterase or acetylcholinesterase) yields phosphorylated acetocholinesterase which is enzymatically inactive and in many instances has a half-life ranging from several days to weeks. While cholinesterase is in a phosphorylated form acetylcholine accumulates and thus the administration of organophosphates is followed by muscarinic and nicotinic symptoms of acetylcholine poisoning.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Hobbiger

Sadler

1959

British Journal of Pharmacology and Chemotherapy

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“…Infusion of the cardiac glycosides resp. aglycones was carried out via the arteria carotis by the method of Kraupp et al (1959) resp. Bach and Reiter (1964) using the Braun Infusor apparatus (Braun, Germany).…”

Section: A Acute Infusion Toxicitymentioning

confidence: 99%

The influence of reduced serum potassium level on the toxicity of some cardenolides in guinea pigs

Fricke

Klaus

1981

Basic Res Cardiol

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Recent experiments on the pharmacological properties of the semisynthetic cardiotonic steroid strophanthidin-3-bromoacetate (SBA) have challenged the well-known potassium digitalis antagonism in isolated heart muscle preparations. In order to establish these results in vivo, the minimum lethal doses (LDmin) of ouabain (OUA), digoxin (DO), digotoxin (DT), k-strophanthidin (STR) and SBA were determined by the infusion toxicity method in guinea pigs at normokalemia and hypokalemia. The experimentally induced decrease of the serum potassium concentration (5.0 mmoles/l vs. 3.3 mmoles/l) significantly reduced the LDmin of DO (1.42 vs. 1.05 mumoles/kg), DT (1.78 vs. 1.24 mumoles/kg) and STR (20.16 vs. 15.98 mumoles/kg), whereas the LDmin of OUA (0.37 vs. 0.34 mumoles/kg) was not altered. Contrary, the LDmin of SBA was even slightly, but not significantly increased during hypokalemia (16.77 vs. 19.04 mumoles/kg). In addition, from the experimental data an optimum time of infusion (Topt), corresponding to the LDmin, can be derived, which is equivalent to the time for optimum "utilization" of the drug. The obtained sequence: STR less than OUA less than DO less than DT less than SBA represents the well-known differences in the onset of the pharmacological action in man resp. animal. Hypokalemia in general resulted in a shortening of the Topt, thus indicating a more rapid "utilization" of the drug tested. The above differences of the cardenolide action at reduced serum potassium concentration may be dependent on the recently reported divergent influence of potassium on the association- resp. dissociation rate constants for the interaction of these drugs with their binding site at the Na+-K+-ATPase.

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?-Methyl-digoxin

Voigtländer¹,

Schaumann²,

Koch³

et al. 1972

Naunyn-Schmiedeberg's Arch. Pharmacol.

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Die Abh�ngigkeit der letalen Dosis von der Infusionsgeschwindigkeit am Beispiel des g-Strophanthin und des The vetin B

Cited by 5 publications

References 28 publications

Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

The influence of reduced serum potassium level on the toxicity of some cardenolides in guinea pigs

?-Methyl-digoxin

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