N-dimethyl-di-guanide and its biological properties
Supniewski, J.; Chrusciel, T.
Archivum Immunologiae et Therapiae Experimentalis 2: 1-15
1954
ISSN/ISBN: 0004-069X PMID: 13269290 Document Number: 9410
N-di-methyl-di-guanide was observed to cause death in 50 per cent of mice used for experiments, when administered subcutaneously in doses of 0,23 g/kg. A dose of 0,24 g/kg is lethal for all mice. Death occurs with symptoms of dizziness; it is caused by respiration paralysis and is often preceded by convulsions. A dose of 5 g/kg administered into the lymphatic sac induced death in 50 per cent of frogs used for experiments. A dose of 5,5 g/kg is lethal for all frogs, the symptoms being similar to those described for mice. The drug at a dilution of 1 per cent causes slight haemolysis of rabbit blood cells. Doses of 25-30 mg/kg of the drug, administered subdurally into the spinal canal do not affect the medulla and brain; 0,2 ml of the drug at a concentration of 2 per cent, injected into thelateral ventricle of rabbit's brain, induces no pathological effects. N-di-methyl-di-guanide, even at a concentration of 200 pg/ml, has no growth-inhibiting effect on St. aureus, E. coli, B. subtilis. Doses as high as 100 Mg/kg, given subcutaneously, have no therapeutic effect on the infection caused by Trypanosoma equiperdum in mice. A daily dose of 100 mg/kg of the drug, administered subcutaneously. cures influenza infection of the lungs in mice. The drug has no destructive effect on influenza virus in vitro. N-di-methyl-di-guanide, given intravenously, causes a decrease in the blood pressure, due to dilatation of the vessels. In perfusion experiments it was observed to induce dilatation of the blood vessels of the extremities, intestines and lung in the cat, and a slight dilatation of extremities in the frog. The drug reduces the heart activity, at first stimulating its contractions, then' reducing them, and finally causing slouching of the walls, volume increase, irregularities of the heart-beat and cardiac block. This effect may be observed on the hearts of mammals in situ, as well as on isolated ones. Similar action was observed on the hearts of frogs with the exception that there was no reduction of pulsation. Even high doses of di-methyl-di-guanide do not cause any appreciable stimulation of the breathing centre. The drug has a depressing effect on the striated muscles of mammals and frogs, decreasing their contractions when given in larger doses. This action occurs on the muscles in situ as well as on the isolated ones. The drug produces a depressive effect on the tension and movements of isolated small - intestine in rabbits and rectum in frogs. High doses enhance the, tension of these organs. The drug causes contractions of mammal bronchi both in situ and after isolation, and stimulates the contraction of the urine bladder in situ. N-di-methyl-di-guanide does not affect the blood sugar level, has no antipyretic effect, and displays but a slight diuretic action. When given intraperitoneally to rats it has a slight anaesthetic effect. N-di-methyl-di-guanide was tested in virus diseases in man, by subcutaneous administration in doses of 0,05-0,1 g every four hours. Some therapeutic effect was observed in cases of varicella, viral jaundice, influenza and parotitis. In the case of lung inflammation due to measles, resistant -to other drugs, the administration of N-di-methyl-di-guanide resulted in a rapid fall of temperature and resolution of lung consolidations.
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