[Pharmacologic profile of dithiadenoxide, a potential non-sedating H1-antihistaminic].

Dithiadenoxide, a product of metabolic S-oxidation of the H1-antihistaminic agent dithiaden (bisulepin, Dithiaden), is also an effective histaminic H1-antagonist in pharmacological experiments in in vivo conditions. In contrast to dithiaden, dithiadenoxide exerts a demonstrable inhibitory action as much as the subtoxic or sublethal dosage in experiments in mice and rats. Its acute toxicity in mice and guinea-pigs substantially decreases; acute toxicological findings in rats are not unambiguous.

[Nonsedative H1 antihistaminics].

Recent research provided evidence that effective H1-antihistaminic drugs need not exert a central and sedative action. Non-sedative H1-antihistaminics can aptly replace older combined preparations of classical H1-antihistaminics, motivated by an effort to weaken their sedative action by the concurrent administration of pharmaceutical preparations with a central stimulating action (e.g.

[A comparative pharmacologic study of histamine H-1 antagonists].

In a representative group of 10 conventional antihistaminic agents, a comparison of their H1-antagonistic efficacy was carried out in a series of pharmacological tests. A very good correlation of findings obtained under in vivo conditions in guinea-pigs (tests of detoxication of histamine and histamine aerosol) and a test in rats, which examined the influence on local changes induced by histamine in the dermal region, was demonstrated. No statistically significant correlation of in vivo findings and receptor binding studies on membranes of the rat brain (displacement of (3H)-mepyramine) was found.