hoe-777 and Dermatitis

In an open multi-center study on 1,286 patients aged 60 years and more, we tested the efficacy and compatibility of prednicarbate (Dermatop) in various vehicles. The eczemas and erythematosquamous dermatoses of 857 patients (66.6%) disappeared within three weeks treatment. In 142 patients (11%), it took more than 3 weeks (62 day at the most) to achieve a complete healing. A very good or good tolerance was observed in 97.1% of the patients. Only in 1.5% the study had to be broken off because of a change for the worse. Prednicarbate, therefore, is especially suitable in the treatment of eczemas and chronic erythematosquamous dermatoses of aged skin.

Topics: Aged; Anti-Inflammatory Agents, Non-Steroidal; Dermatitis; Eczema; Female; Humans; Male; Middle Aged; Multicenter Studies as Topic; Pharmaceutical Vehicles; Prednisolone; Skin Aging

We report on the results of an openly conducted multicenter study concerning efficacy and tolerance of a new prednisolone derivative free from halogenic groups (prednicarbate 0.25%, Dermatop) prepared as a) emulsifiable greasy ointment without water, b) w/o emulsion (ointment), and c) o/w emulsion (cream). These preparations were therapeutically applied in eczema (allergic, seborrheic, microbic), psoriasis, and atopic dermatitis. The study was carried out in close team work between a clinic and 37 practicing dermatologists and included 383 patients. After 3 weeks therapy, 4% of the patients did not reveal any satisfying results; 16% showed medium outcome with some persisting symptoms; in 80% of the patients, we observed good to very good therapeutic results.

Topics: Administration, Topical; Adolescent; Adult; Aged; Anti-Inflammatory Agents; Berlin; Child; Child, Preschool; Clinical Trials as Topic; Dermatitis; Dermatitis, Atopic; Dermatitis, Seborrheic; Eczema; Female; Humans; Male; Middle Aged; Pharmaceutical Vehicles; Prednisolone; Psoriasis

There is a continuous need for methods to evaluate the biologic effects of topically applied drugs in the skin. Irritation of the epidermis with sodium dodecyl sulfate leads to an upregulation of E-selectin on endothelial cells and E-selectin mRNA can be detected in vivo within a short time. This study was aimed to investigate whether this biologic response can be used as a read-out for the anti-inflammatory effect of topically administered corticosteroids. We investigated skin of healthy volunteers treated according to the two following experimental protocols: (i) topical application of different corticosteroids (versus basic ointments as controls) for 12 h and irritation with sodium dodecyl sulfate 1% for 4 h; (ii) irritation with sodium dodecyl sulfate 1% for 12 h and application of the corticosteroids for 5 h. The biopsy specimens were subjected to RNA extraction and reverse transcription and competitive reverse transcriptase-polymerase chain reaction was performed using defined concentrations of a pre-constructed mimic DNA. As result, we found strong positive signals for wild-type E-selectin mRNA in all biopsies pretreated with basic ointments, whereas in biopsies from areas pretreated with corticosteroids the bands for wild-type E-selectin DNA could be detected at 10-1000 lower levels of mimic DNA concentrations. The reverse experiment, application of corticosteroids after the irritation, again yielded significantly reduced signals for E-selectin mRNA. In both experimental settings, the different strength of the topical corticosteroids used was reflected by significant differences in the amount of E-selectin mRNA found in the biopsies. This study demonstrates the pharmacologic effect of topical corticosteroids on the irritation-induced E-selectin mRNA expression on dermal endothelial cells in vivo using very small tissue samples and this approach may be of value for further pharmaceutical studies.

Topics: Administration, Topical; Adult; Anti-Inflammatory Agents; Biopsy; Dermatitis; Drug Eruptions; E-Selectin; Female; Humans; Hydrocortisone; Male; Prednisolone; Premedication; RNA, Messenger; Skin; Sodium Dodecyl Sulfate; Triamcinolone; Up-Regulation

Topics: Administration, Topical; Adrenal Cortex Hormones; Anti-Inflammatory Agents; Cytokines; Dermatitis; Glucocorticoids; Humans; Macrophages; Prednisolone; Receptors, Thyroid Hormone

Prednicarbate (Dermatop) was topically applied in 50 children suffering from inflammatory dermatoses. In 12 children, the courses of therapy were documented by photographs. Its rapid onset of action, its lacking suppression of the endogenic biosynthesis of cortisol, as well as its small antiproliferative effect on cutaneous fibroblasts suggest that prednicarbate bears only minor risks especially for children's skin.

Topics: Administration, Topical; Anti-Inflammatory Agents; Child; Child, Preschool; Dermatitis; Dermatitis, Atopic; Dermatitis, Contact; Dermatitis, Seborrheic; Eczema; Female; Humans; Male; Prednisolone

Topics: Administration, Topical; Anti-Inflammatory Agents; Dermatitis; Humans; Prednisolone

Prednicarbate (Hoe 777) is a corticoid without halogenic groups (see formula Fig. 1), showing a remarkably favorable split between topical and systemic anti-inflammatory or rather corticoid effects, which could be proved by means of various animal experiments after dermal and systemic application. The topical efficacy resembles that of current corticoid preparations containing fluorine, but its systemic influence is definitely less.

Topics: Administration, Topical; Animals; Anti-Inflammatory Agents; Biotransformation; Chemical Phenomena; Chemistry; Dermatitis; Humans; Mice; Prednisolone; Rats

In 20 patients suffering from acute or chronic inflammatory dermatoses, topical treatment with prednicarbate (Dermatop) was photographically documented and evaluated. Because of the rapid and pronounced anti-inflammatory and anti-edematous effect of prednisolone-17-ethyl carbonic ester without halogenic groups, therapy took only 7 to 21 days. Since there was practically no suppression of the endogenic biosynthesis of cortisol and no atrophogenic potency, we expected a minimum of side effects along with a maximum of therapeutic results.

Topics: Administration, Topical; Adult; Aged; Anti-Inflammatory Agents; Dermatitis; Dermatitis, Atopic; Dermatitis, Contact; Eczema; Female; Follow-Up Studies; Humans; Male; Middle Aged; Prednisolone; Psoriasis

The corticoid prednicarbate (test name: Hoe 777) is derived from prednisolone having no halogenic groups (chemical name: prednisolone-17-ethyl carbonate-21-propionate). Because of the specific physical and chemical properties of prednicarbate, galenic research strove to optimize the vehicle. Further development was only performed on those drug-containing bases showing especially good drug release (granting the most favorable action) in a) the vasoconstriction test and b) the UV erythema test practiced on volunteers with healthy skin. Exemplarily dealing with the special preparations predicarbate cream, ointment, and greasy ointment, we give some details of studies on drug dosage, vehicle selection, and the optimum water/lipid ratio.

Topics: Administration, Topical; Anti-Inflammatory Agents; Chemical Phenomena; Chemistry; Dermatitis; Dose-Response Relationship, Drug; Humans; Pharmaceutical Vehicles; Prednisolone; Skin Absorption; Sunburn; Vasoconstriction

Prednisolone-17-ethyl carbonate-21-propionate (PrEP, Hoe 777) was tested for antiinflammatory activity in various animal models by topical and systemic administration. In those models being indicative of topical efficacy, the potency of PrEP was the same as that of desoximetasone. However, systemic effects after topical administration of PrEP in shaved skin of the dorsum of rats were relatively weak compared with the reference compound. Moreover, there were less systemic corticoid effects after s.c. administration of PrEP than after desoximetasone. Thus, PrEP is obviously a compound with a considerable split of topical and systemic activity, suggesting its testing in man for systemic effects after topical administration.

Topics: Administration, Topical; Animals; Anti-Inflammatory Agents; Dermatitis; Desoximetasone; Gluconeogenesis; Granuloma; Mice; Mice, Inbred Strains; Prednisolone; Rats; Rats, Inbred Strains; Skin

We report on the clinical efficacy of the local corticoid prednicarbate (chemical name: prednisolone-17-ethyl carbonate-21-propionate). In a concentration of 0.25%, it can be assigned to corticoid force class III. We think it's remarkable that even extensive application of 20 g daily in patients with affected skin and 30 g daily in healthy persons does not cause any suppression of plasma cortisol. Extreme long-term application (12 months) in 4 test persons did not result in any clinical, histological, or electron microscopical signs of topical atrophy; only one case showed slight hypertrichosis. These studies show that we may regard the original opinion as disproved that efficacy and side effects of corticoids are always inseparably linked together. To our minds, this preparation constitutes an essential step towards solving the problem of long-term application of a topical corticoid wherever it may be necessary from the dermatologic point of view, e.g. especially in atopic dermatitis and psoriasis.

Topics: Administration, Topical; Adolescent; Adult; Aged; Anti-Inflammatory Agents; Betamethasone Valerate; Child; Cortisone; Dermatitis; Dermatitis, Atopic; Dermatitis, Contact; Desoximetasone; Double-Blind Method; Drug Evaluation; Female; Humans; Male; Middle Aged; Prednisolone; Psoriasis