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At least 109 records · Page 6Linked to original sources
PubMed1981

A comparison of the effects of tixocortol pivalate (JO 1016), hydrocortisone acetate and beclomethasone dipropionate on collagen synthesis and degradation.

The effects of a corticosteroid substitute pregn-4-ene-3,20-dione-11 beta,17 alpha-dihydroxy-21-pivalate (tixocortol, JO 1016, Pivalone), hydrocortisone acetate and beclomethasone dipropionate on collagen metabolism in mouse calvariae were compared by histological and biochemical determination of collagen content, and by radio-assays of collagenase and collagenase inhibitor. Hydroxyproline assay revealed dose-related increases in collagen content/wet wt. tissue. These were greatest in explants treated with beclomethasone dipropionate, tixocortol pivalate being effective only at much higher concentrations than the other 2 drugs. Hydrocortisone acetate and beclomethasone dipropionate stimulated collagenase production at the lowest levels tested whereas tixocortol pivalate was only slightly stimulatory at the highest treatment level. These results suggest that in clinical use tixocortol pivalate would be much less likely than hydrocortisone acetate or beclomethasone dipropionate to cause degenerative changes in connective tissue.

Administration, Topical↗
PubMed1981

Pharmacological study of a new anti-inflammatory steroid, tixocortol pivalate (JO 1016).

Some pharmacological activities of pregn-4-ene-3,20-dione-21-thiol-11 beta,17 alpha-dihydroxy-21-pivalate (tixocortol pivalate, JO 1016 Pivalone), a new steroidal anti-inflammatory compound, are described. The anti-inflammatory activity of tixocortol pivalate has been clearly demonstrated in various tests using adrenalectomised and intact animals. Of particular interest is the dissociation of its local and systemic activities. Comparison with hydrocortisone acetate indicates a similar or greater anti-inflammatory activity, by either the local or topical routes, but tixocortol pivalate is between 60 and 300 times less active than hydrocortisone acetate after oral or subcutaneous administration. Glucocorticoid activity was only detected at very high oral doses of tixocortol pivalate and the highest tested subcutaneous dose (300 mg/kg) failed to induce significant activity. Hydrocortisone acetate exerted glucocorticoid effects at much lower doses. It is possible therefore the local or topical use of tixocortol pivalate in therapy may not cause the unwanted side effects of many of the corticosteroids in current use.

Administration, Oral↗
PubMed1981

A comparison of the effects of tixocortol pivalate (JO 1016), beclomethasone dipropionate and hydrocortisone acetate on the activation of lymphocytes.

A comparative study was made of the effects of hydrocortisone acetate, beclomethasone dipropionate and a corticosteroid substitute (pregn-4-ene-3,20-dione-21-thiol-11 beta,17 alpha-dihydroxy-21-pivalate, tixocortol pivalate, JO 1016, Pivalone) on lymphocyte activation. The response measured in vivo was the production of heamagglutinating antibody by mice in response to immunization with sheep erythrocytes. The in vitro response tested was the blastocytic transformation of T cells in mixed lymphocyte culture. All three compounds suppressed T cell activation in vitro. Tixocortol pivalate however, was non-toxic and non-immunosuppressive when administered to mice, in contrast to hydrocortisone acetate and beclomethasone dipropionate, which were toxic and immuno-suppressive at the highest dose levels tested. These results indicated that tixocortol pivalate would, by virtue of its low toxicity and absence of general immunosuppression, have potential advantages over both hydrocortisone acetate and beclomethasone dipropionate in the topical treatment of allergic conditions of mucous membranes.

Administration, Topical↗
PubMed1981

A comparison of the effects of tixocortol pivalate (JO 1016), hydrocortisone acetate and beclomethasone dipropionate on the phagocytosis and lysis of microorganisms by alveolar macrophages.

A comparison was made of the ability of guinea pig alveolar macrophages, which had been pretreated with hydrocortisone acetate, beclomethasone dipropionate or a corticosteroid substitute pregn-4-ene-3,20-dione-21-thiol-11 beta,17 alpha-dihydroxy-21-pivalate (tixocortol pivalate, JO 1016, Pivalone), to phagocytose and lyse Staphylococcus aureus or Candida albicans. The three drugs had different patterns of effect on phagocytosis and lysis. Hydrocortisone acetate had little effect on the phagocytosis of Staph. aureus at any dose level tested, but the two higher concentrations slightly inhibited intracellular lysis; phagocytosis of C. albicans was inhibited initially but increased at 5 h. Both beclomethasone dipropionate and tixocortol pivalate caused an initial stimulation of phagocytosis and lysis of Staph. aureus. Ingestion of C. albicans was increased in macrophages pretreated with beclomethasone dipropionate, but their fungicidal activity was unchanged. Pretreatment with tixocortol pivalate stimulated the initial phagocytosis of C. albicans but continued uptake on prolonged incubation was inhibited. Lysis of the ingested organisms was not markedly affected. Since the production of any effect on the phagocytic and lytic activity of alveolar macrophages required much higher levels of tixocortol pivalate than of either of the other two drugs, it is suggested that in clinical use correspondingly higher doses of tixocortol pivalate could be given without danger of affecting either phagocytic activity or the immune response.

Administration, Topical↗