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Biomedical subjects

H Wendt

Publications and source records attributed to H Wendt.

At least 19 recordsLinked to original sources
PubMed1992

Dose-response relationship of topically applied methylprednisolone aceponate (MPA) in healthy volunteers.

Topical glucocorticosteroids are useful in the treatment of various skin diseases. Although many corticosteroids are available today, there is still a need for highly potent compounds with minimal adverse effects. Methylprednisolone aceponate (MPA) has recently been synthesized. Its activity has been evaluated using the vasoconstrictor assay and the poison ivy test (rhus dermatitis) in 19/20 healthy volunteers of either sex. Comparable blanching was found with MPA in a cream vehicle, in an ointment and a fatty ointment. Vasoconstriction and suppression of experimentally-induced poison ivy contact dermatitis were dose-dependent in the concentration range 0.01% to 0.5% MPA. Concentrations of MPA of at least 0.05% were significantly active. Following the highest dose, blanching was close to the maximum which can be obtained. This finding, and the improvement of rhus dermatitis, suggest that MPA belongs to the highly potent local glucocorticosteroids.

Administration, Topical↗
PubMed1979

The pharmacokinetics and biotransformation of the new benzodiazepine lormetazepam in humans. I. Absorption, distribution, elimination and metabolism of lormetazepam-5-14C.

The pharmacokinetics and metabolism of the new benzodiazepine lormetazepam were investigated in five male volunteers using the 14C-labelled drug (position 5). Lormetazepam was administered intravenously and orally, at a dose of 0.2 and 2 mg respectively, to each of the test subjects. Measurements of total radioactivity showed that the drug was absorbed completely and eliminated almost exclusively by the renal route. Maximum plasma level of active ingredient and total radioactivity were observed about 2 hours and 5 hours following oral administration. As early as 30 min following oral administration, concentration of active ingredient amounted to 80% of the maximum values. After both treatments the terminal half-life of total radioactivity and lormetazepam glucuronide in plasma corresponded to the half-life of elimination in urine of about 13 hours. After enzymatic hydrolysis with beta-glucuronidase/arylsulphatase, an average of 90% of total radioactivity from various urine and plasma samples was extractable with ether. Extracts from plasma contained only unchanged drug, indicating free and conjugated lormetazepam as ingredients of total radioactivity. Extracts from urine could be separated into lormetazepam and its N-demethylation derivative lorazepam. The relative amount of excreted lorazepam conjugate was demonstrated to be time-dependent, probably due to enterohepatic circulation. Since less than 6% of the total dose was demethylated by both routes of administration, it can be assumed that lormetazepam is the active product.

Absorption↗
PubMed1979

Investigations of pharmacokinetics of ethinyloestradiol to specific consideration of a possible first-pass effect in women.

Ethinyloestradiol-3H was given intravenously and orally to four and three women, respectively, in a dose of 60 micrograms and 3 mg. To another three female volunteers, 100 micrograms of ethinyloestradiol was administered by both routes in succession. Drug concentration in plasma and total radioactivity in plasma, urine and faeces were measured for different periods of time. Intraindividual comparison of the area under the drug level vs. time curve after intravenous and oral administration of 100 micrograms showed that ethinyloestradiol is subject to an about 60% first-pass effect in women. The time course of ethinyloestradiol concentration in plasma can be described by a 3-compartment model after intravenous injection and by a 2-compartment model after oral administration, because an early disposition phase with a half-life of about 15 minutes only becomes visible after i.v. injection. On an average, the terminal half-life of unchanged ethinyloestradiol level and total radioactivity was calculated to be about 1 day. However, a high variability was found with this parameter as well as with the rate and degree of elimination in urine.

Absorption↗
PubMed1979

Plasma levels of active ingredients after single and repeated administration of a new oral contraceptive containing 2 mg of cyproterone acetate and 50 micrograms of ethinyl estradiol (DIANE) to five young women.

Peripheral plasma from five young women was analyzed for cyproterone acetate and ethinyl estradiol during a period of 96 hours duration after single oral intake of a coated tablet of DIANE (2 mg of cyproterone acetate + 50 micrograms of ethinyl estradiol), and during a treatment cycle of 21 days during which the formulation was given daily. Radioimmunoassays were utilized for quantifications. A maximum concentration of 11.0 +/- 3.4 ng of cyproterone acetate/ml plasma was found 1.6 +/- 0.6 hours after a single administration of DIANE. Postmaximal disposition took place in two phases with half-lives of 1.9 +/- 0.6 hours and 2.2 +/- 0.2 days. The maximum level of 0.08 +/- 0.03 ng of ethinyl estradiol/ml plasma was found 1.6 +/- 0.6 hours after such single administration. Following commencement of a daily oral intake of DIANE a steady state was reached by the 5th to 8th days, during which 24 hours after each dose cyproterone acetate concentrations were found to be 2.4 +/- 0.7 times higher than at the corresponding time after a single administration. Accordingly, after the first third of the 21 day treatment cycle an almost constant plasma level was reached indicating an equilibrium of intake and elimination. Except for a change in the mean terminal half life after multiple dosing, there was evidently no change in the kinetics of cyproterone acetate. No pointers to an accumulation of ethinyl estradiol upon daily administration of DIANE could be found.

Adult↗
PubMed1979

[Antimicrobial activity of the broad spectrum antimycotic isoconazole nitrate in humans (author's transl)].

A comparative study (occlusion test according to Marples and Kligman) was conducted in 100 test subjects with several formulations of isoconazole nitrate. The following results were obtained: 1. There are no differences in efficacy between the free base, isoconazole, and the nitrate. 2. Increasing the active substance concentration of isoconazole nitrate above 1% produced a noticeable increase in its effect so that 2% and 4% preparations are appropriate for particular uses. 3. 1% isoconazole nitrate (Travogen cream, Gyno-Travogen cream) is more effective than a commercial cream containing 1% clotrimazole. 4. The addition of a corticosteroid (diflucortolone-21-valerate 0.1%, Travocort cream) does not influence the action of isoconazole nitrate.

Clotrimazole↗
PubMed1978

A study of the comparative efficacy of diflucortolone valerate 0.3% ointment and clobetasol propionate 0.05% ointment.

Three hundred and fifty-four patients with symmetrical dermatoses took part in a multicentre, doubleblind, half-side study in order to compare the efficacy of a new topical steroid, diflucortolone valerate 0.3% (Nerisone Forte) against that of an established, potent topical steroid, clobetasol propionate 0.05% (Dermovate). The assessment of overall response, as judged by the physicians' preference for one side or another, showed no difference between the two compounds. However, when the results were examined by separate diagnostic category, the number of preferences was greater for diflucortolone valerate 0.3% in eczema, and for clobetasol propionate 0.05% in psoriasis, although neither of these differences reached levels of statistical significance. The graded assessments of response indicated that both compounds were highly effective, potent, topical steroids. Eighty-one percent of all patients showed marked improvement or healing with diflucortolone valerate 0.3%, and 84% showed marked improvement or healing with clobetasol propionate 0.05%. This difference was not statistically significant. Analysis of response, either by diagnosis or grade of severity, showed no statistically significant differences between the two compounds. No significant differences in the incidence of severity of side-effects were observed. It was concluded that the two compounds were of equal clinical efficacy.

Adrenal Cortex Hormones↗
PubMed1978

Prolactin-lowering effect of low doses of lisuride in man.

Lisuride, a new semisynthetic ergot derivative, effectively decreased the TRH-induced hyperprolactinaemia in healthy female volunteers at a dose of 300 microgram given orally. Basal prolactin levels were suppressed after a single dose of 100 and 200 microgram lisuride. This effect was still present 6 h after administration. Two hundred microgram lisuride also decreased the high serum prolactin levels produced by im injection of 50 mg sulpiride, and conversely, sulpiride injection abolished the prolactin lowering effect of lisuride. These results demonstrate that in man too lisuride is a very potent prolactin-lowering agent. In addition, the data support the hypothesis of a predominant role of dopaminergic mechanisms in the regulation of prolactin secretion.

Administration, Oral↗
PubMed1977

[Clinico-pharmacological studies on the acne-inducing action of fluocortin butylester (author's transl)].

The acne-inducing effect of butyl 6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) 0.75% was compared with that of hydrocortisone acetate 1.0% and diflucortolone valerate 0.1% in a model established by Plewig and Kligman. The steroid and the cream base uniformly used in all preparations were applied to the backs of 20 volunteers over 4 weeks. Dome-shaped red papules developed in the third week of occlusive treatment, and were counted in an area of 16 cm2 at the maximum of their development and graded according to a scale. The degree of papulation under diflucortolone valerate 0.1% was 2.15+/-0.75. No differences were observed between fluocortin butylester 0.75% (0.2+/-0.42), hydrocortisone acetate and the cream base (0.15+/-0.37).

Acne Vulgaris↗
PubMed1977

[The effect of fluocortin butylester on adrenal function in man (author's transl)].

The systemic corticoid effects of butyl 6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-regnadien-21-oate (fluocortin butylester, Vaspit) in the form of 0.75% fluocortin butylester cream were tested under conditions which permit maximum absorption of the active principle. Over 8 days 40 g cream daily were applied to the entire body surface of 6 subjects and the trunk, thighs and upper arms covered with polythene foil. The plasma cortisol levels, elimination of free cortisol in the 24-h urine and eosinophilic leucocytes were compared intraindividually with the values before and three days after treatment. In addition 6 further subjects were treated with 0.1% hydrocortisone-17-butyrate cream, a preparation considered to have little systemic action. Fluocortin butylester showed no systemic corticoid effects. Cortisol secretion and eosinophilic leucocytes remained unaffected. In contrast the inhibiting effect of hydrocortisone-17-butyrate was evident in all parameters, especially in the morning plasma cortisol values. Under treatment with hydrocortisone-17-butyrate these dropped from 361 to 11 nmol/l. Under occlusion treatment with fluocortin butyl they remained constant (357 before, 320 nmol/l after treatment). The relevance of the method of examination is discussed.

Administration, Topical↗
PubMed1977

[Studies on phototoxic and photoallergic effects of cream, ointment and fatty ointment of fluocortin butylester (author's transl)].

The phototoxic action of ointment and fatty ointment of butyl 6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) was examined by means of the epicutaneous test with subsequent UV-irradiation (Kromeyer lamp with Schott filter DG 18) in 20 patients with skin disorders. Photoallergic effects of fluocotrin butylester cream, ointment and fatty ointment were tested in a modified Draize test in which 198 subjects with normal skin participated. The subjects were sensitized in 10 epicutaneous tests conducted at intervals of 24 h and followed by irradiation (1500 W xenon lamp) with 2 MED. Treatment and irradiation were then repeated after a 2-week interval. This proceding permitted additional statements an phototoxicity of the administered preparations. No positive reactions occurred in either of the tests so that phototoxic effects can be excluded and a photoallergic potential is improbable.

Adolescent↗