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Biomedical subjects

J M de Suray

Publications and source records attributed to J M de Suray.

4 recordsLinked to original sources
PubMed1985

Pharmacological properties of the new potent diuretic torasemide in rats and dogs.

Torasemide, a pyridine-3-sulfonylurea derivative, has potent diuretic activity in rats and dogs. In both species urinary volume and electrolyte excretion increased linearly with the logarithm of the dose, thus resembling the profile of a high ceiling diuretic. The minimum effective dose by oral route was 0.2 mg/kg in the rat and less that 0.1 mg/kg in the dog. Maximal effect was obtained with about 10 mg/kg. Experiments by oral and i.v. routes in the rat indicated that torasemide was equally potent by both oral and parenteral administration. In both rats and dogs, urinary excretions induced by torasemide were similar to those obtained with furosemide. However, for the same natriuretic effect, potassium losses with torasemide were significantly less than with furosemide. On a weight basis, torasemide was 9-40 times more potent than furosemide in the rat and about 10 times in the dog. After oral administration the diuretic effects of torasemide started within 20 min and lasted approximately 2 h in the rat and more than 8 h in the dog. The activity of torasemide was not decreased after a repeated daily oral dose of 10 mg/kg for 15 days in the rat. Torasemide at a daily oral dose of 5 mg/kg for 12 days effectively reduced the arterial blood pressure in desoxycortone induced hypertension in the rat. Besides the diuretic and antihypertensive effects no other significant pharmacological effects were observed with torasemide in the different in vitro and in vivo experiments. Torasemide was practically fully absorbed by the gastrointestinal tract, its bioavailability by oral route ranged from 80 to 100%.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1981

Pharmacokinetic study of aprindine and moxaprindine in dogs.

Moxaprindine and aprindine were each administered to a group of six dogs at a single dose of 5.5 mg/kg by intravenous injection and at the same dose 14 days later by oral route. In each series the sequence of route of administration was randomized. In a second experiment, 8 to 12 weeks later, the dogs were treated for 5 successive days with the same drug at the dose of 5.5 mg/kg twice daily. Moxaprindine and aprindine are similar in several of their pharmacokinetic characteristics. Their plasma levels are suitably explained by a two-compartment open model. No significant differences are found between their respective terminal plasma half-lives nor their k12, k21 and kel values; on multiple dosing, the steady state is reached within 3 days with both drugs. However, the plasma levels of moxaprindine are twice as high as those of aprindine. Consequently the distribution volume of moxaprindine is half as small as that of aprindine. Moxaprindine is 95.3% protein bound at 1 microgram/ml and 93.6% at 2 microgram/ml; the corresponding values for aprindine are 98.3% and 98.1%. These differences may be of clinical significance as regards therapeutic effectiveness and safety of these two substances.

Administration, Oral↗
PubMed1979

Bioavailability study of gitoxin in a solid dosage form.

Although the cardiotonic activity of gitoxin is known for almost half a century, this digitalis glycoside has never been used in therapy, due to its apparent lack of resorption after administration by oral route. Recent studies have demonstrated that the bioavailability of gitoxin could be upraised to 100% provided it be given as a hydroalcoholic solution. The present paper deals with the development of a solid dosage form (tablets) using a physical association of gitoxin and sodium escinate.

Adult↗