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Biomedical subjects

A Rastelli

Publications and source records attributed to A Rastelli.

29 records · Page 2Linked to original sources

Comparative study of the vasoconstrictor activity of halopredone acetate in a modified McKenzie test.

The vasoconstrictor activity of four steroids, administered in solution and in the commercially available form, were compared in healthy volunteer subjects. Evaluation was based on conventional visual observations and photometric measurement of reflectance. Statistical analysis showed that halopredone acetate had less vasoconstrictor action on healthy skin than fluocinolone acetonide, beta-methasone valerate and hydrocortisone acetate. The halopredone acetate results were identical to those of th excipient, although it was found that halopredone acetate cream (Topicon) had a marked anti-inflammatory effect in animals and on human dermatoses. The validity of the McKenzie test, as an unequivocal screening procedure for the potency of topical steroids is discussed, and the accuracy and precision of photometric evaluation is emphasized.

Administration, Topical↗

Electronic aspects of the antibacterial action of sulfanilamides.

Intramolecular interactions in N1-substituted sulfanilamides (SA) can rationalize the trend of their antibacterial powers with the use of a resonance scheme, derived from d orbital symmetry and tested with an extensive spectroscopic investigation on amidic, imidic, and anionic SA. On quantitative grounds, a good relationship is presented between the antibacterial power and the proton chemical shift of the p-amino group. The electronic features for high activity are described.

Bacteria↗

Antibacterial activity and chemical reactivity of sulphanylamides. Rate constants of alkaline hydrolysis of N4-acetylsulphanylamides.

The alkaline deacylation rate constants of a collection of N4-acetylderivatives of acidic and non-acidic sulphonamides (SA) clearly show a definite trend due to the intramolecular effects induced by the different substitutions on the N1 nitrogen. The rate constant is interpreted as a reactivity index of the corresponding non-acetylated compound, and is found to be strictly correlated with the electron-availability of the p-amino group; thus providing an interesting correlation with the antibacterial activity of these drugs. Moreover, the reported experiments corroborate early predictions that the greatest reactivity of the p-amino group pertains to p-aminobenzoate (PAB) in the series of chemically related compounds, and that SA anions show the highest chemical and electronic resemblance to the essential metabolite (PAB); thus the high antibacterial activity of SA anions correctly corresponds to its close resemblance to the metabolite.

Alkalies↗

Preliminary clinical evaluation of a new topical corticosteroid, halopredone acetate, as compared to fluocinonide.

17,21-Bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-diene-3,20-dione (halopredone acetate; Topicon), a new corticosteroid for topical use, was compared with fluocinonide in a double blind sequential study. The tests were made on a total of 16 patients affected with psoriasis and exudative dermatitis. In each patient, the symmetrically distributed skin lesions were separately treated with either halopredone acetate or the reference compound. The two active substances were in the same concentration (0.05%) in the same carrier (cream), and both reduced the subjective and objective symptoms of these skin conditions. No statistically significant differences were observed between the two medicated areas. Haloperidone acetate, the excipients of the cream and the reference compound were all excellently tolerated.

Administration, Topical↗

Clinical study of the relationship between dose and response to halopredone acetate in dermatoses.

A comparative clinical investigation with three different concentrations of 17,21-bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-diene-3,20-dione (halopredone acetate; Topicon), a new topical corticosteroid, has been made to assess the optimum concentration of active substance to be incorporated into cream on the basis of the therapeutic effects achieved in dermatologic patients. The remarkable therapeutical effectiveness of the new steroid, however, has made it impossible to ascertain statistically significant differences between preparations containing either 0.01%, 0.025% or 0.05% of active substance, and to gain thereby a clear answer concerning the relationship between dose and response. Numerous haematochemical controls were made during the trials. In particular, we determined the plasma cortisol levels in patients suffering from large lesions requiring prolonged occlusive medication. No significant alterations of the basal values were observed. As already observed in animals, halopredone, acetate is devoid in humans also of the wellknown effects on the hypophysial-adrenal axis due to transcutaneous absorption of steroids.

Administration, Topical↗

[The Guidance Center. Evaluation after a year of activity].

The C.H.U. of Grenoble started a child Guidance Clinic for assuming the education of handicapped children from 2 to 6 (years of age). A whole organization for medical advice, training for walk, psychotherapy, orthophony, together with a day hospital can be found there--the working of whith is provided by a pluridisciplinary team of 15 members (among whom educators, psychanalistes, psychiatristes, psychologistes, pediatristes). The parents may profit by interviews with the educators, with a conjugal adviser, or by parents groups who meet twice a month. An average of 25 children are registered, and 15 are present, among whom most are trisomic 21, or psychotics. The day price is 257 F and 100% returned by the social Security. At last, besides the therapeutic function, the clinic also plays a pedagogic part by receiving probationers coming from different places.

Child↗

The role of anionic, imidic and amidic forms in structure-activity relationships. Conjugation and bacteriostatic activity in sulphonamides.

The electronic structures of anionic, imidic and amidic forms of sulphonamides were investigated and compared by means of I.R., Raman and U.V. spectroscopy. Indices reflecting the electronic situation of the common moiety p-H2N-C6H4-SO2 was a whole, although not necessarily related, physically, to any event taking place in the biological processes, were found to correlate with the in vitro bacteriostatic activity of the specific individual forms. The influence of N1-substituents both on the SO2 electronic features and on the coupling between the para amino group and the phenyl ring was discussed. It resulted that the most active chemical species, in this class of compounds, are characterized, electronically, by the most electron-rich common moiety and, in particular, by the most negative oxygens in the SO2 group and the most available (less engaged) lone-pair in the rho-amino group. These conclusions give a new settlement both to the problem of resonance and to the relation between resonance effects and bacteriostatic activity in this class of compounds.

Amides↗