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At least 19 recordsLinked to original sources
PubMed2000

Determination of fluocortolone pivalate and fluocortolone hexanoate in suppositories using reverse-phase HPLC.

Fluocortolone and its esters are synthetic corticosteroids used topically in the treatment of various skin disorders. A method that can be successfully used for the separation and determination of fluocortolone pivalate and fluocortolone hexanoate in suppositories was developed. This method is based on reverse-phase HPLC on Supelcosil LC-18 (25 cm x 4.6 mm, 5 microns), using methanol-acetonitrile-water-glacial acetic acid (17:46:37:0.4 v/v/v/v) as mobile phase at a flow rate of 3.0 ml/min. Detection was carried out using a UV detector at 238 nm. The method developed was validated, and calibration curves were established dependent on peak area. The validated ranges for fluocortolone pivalate and fluocortolone hexanoate are 15-305 micrograms/ml (r = 0.9995) and 15-315 micrograms/ml (r = 0.9996), respectively. The limits of detection and the limits of quantification for both esters were also determined.

Administration, Topical↗
PubMed1977

Allergic contact dermatitis from fluocortolone, flucocortolone pivalate and fluocortolone caproate.

Two patients with contact allergy to Ultralan preparations are reported. Each Ultralan preparation contains two of three related fluocortolone derivatives. The first patient reacted to all three derivatives. The second patient reacted to flucortolone and when retested 4 months later also to fluocortolone pivalate but ot to flucortolone caproate. The negative reaction to fluocortolone pivalate at the first examination was probably false negative due to a low test concentration. In order to avoid false negative patch test reactions the fluorinated steroids should possibly be applied in concentrations higher than 1%. No cross sensitivity to the other steroids for topical use was found.

Aged↗
PubMed1983

A comparative multicentre trial of halometasone ointment and fluocortolone plus fluocortolone caproate ointment in the treatment of psoriasis.

A multicentre, between-patient, comparative trial was carried out by nine dermatologists in the Federal Republic of Germany to compare the efficacy and tolerability of 0.05 halometasone ointment with those of an ointment, containing 0.25% fluocortolone + 0.25% fluocortolone caproate, in patients with psoriasis vulgaris. The evaluable trial population consisted of 182 patients, 115 males and sixty-seven females. Halometasone ointment yielded a higher success rate ('good' to 'very good' results), namely 56.4% than that obtained with the comparative ointment (45.4%). Halometasone ointment also produced a higher cure rate, namely 26.6%, than that reported with the comparative preparation (19.3%). An improvement of one score over the pre-treatment clinical status of the psoriatic lesions reported at the Day 10 visit was significantly higher (p = 0.04), namely 48.9%, with halometasone ointment than that with the comparative preparation (35.2%). The percentages of patients obtaining an early cure, i.e. in less than 30 days, and onset of action were practically identical in both treatment groups. No adverse effects were reported in any of the ninety-four patients treated with halometasone ointment, while unwanted reactions were observed in three of the eighty-eight patients treated with the comparative preparation.

Administration, Topical↗
PubMed1986

Pharmacokinetics of fluocortolone in man.

The kinetics of the synthetic corticoid fluocortolone was determined in 9 healthy female volunteers after a single oral dose of 20 mg. The maximal plasma level fluocortolone (Cmax) of 202 +/- 70 ng/ml occurred within 85 +/- 32 min of oral intake after which it declined monoexponentially. Total plasma clearance was 6.48 +/- 2.07 ml/min X kg and the clearance of unbound fluocortolone was 60.38 +/- 26.67 ml/min X kg. Plasma protein binding was 83 to 95%. The volume of distribution at steady-state was 1.01 +/- 0.341/kg for total fluocortolone and 11.21 +/- 3.771/kg for unbound drug. The results of the study characterize the kinetics of unbound fluocortolone for the first time. In addition, the kinetics of total fluocortolone presented here confirm values calculated previously.

Adult↗
PubMed1986

[Pharmacokinetics of fluocortolone in long term therapy of patients with rheumatic and hematologic diseases].

The pharmacokinetics of fluocortolone (Ultralan oral) and its effect on plasma cortisol levels were investigated during long-term treatment of patients with rheumatic and haematological diseases with different doses of fluocortolone. Fluocortolone was administered in the morning and plasma levels of fluocortolone and cortisol were measured in samples obtained 1.5, 3, 4, and 5 h p. adm. by means of specific radioimmunoassays. Maximum concentrations of fluocortolone in plasma (Cmax) and areas under the fluocortolone plasma level curves (AUC) increased linearly with the dose. The peak time (tmax = 2.04 +/- 0.85 h) and the plasma half-life (t1/2 = 1.53 +/- 0.52 h) were independent of the dose administered. Cortisol suppression as indicated by morning cortisol levels below 50 ng/ml plasma was not observed with doses below 10 mg/d.

Adult↗
PubMed1986

Fluocortolone: pharmacokinetics and effect on plasma cortisol level.

The pharmacokinetics of fluocortolone and its effect on plasma cortisol levels are described after oral administration of 20, 50 and 100 mg to 9 healthy adults. The concentrations of fluocortolone and cortisol in plasma were measured simultaneously by HPLC with UV detection. Fluocortolone was rapidly absorbed after all doses, giving the maximum plasma level after 1.4-2.1 h. After ingestion of 20, 50 and 100 mg, the peak levels were 199, 419 and 812 ng/ml, respectively. The maximum plasma levels and areas under the plasma level-time curves increased in proportion to the dose. Post-maximum plasma levels declined monoexponentially with a half-life of 1.76 h. Plasma half-life (t1/2 = 1.76 h), volume of distribution (1.03 l/kg) and oral clearance (6.9 ml/min/kg) were independent of the dose. The intensity and duration of adrenal suppression was dose dependent. Maximum suppression was observed 8 hours after fluocortolone. Clearcut suppression of cortisol levels after 24 hours was only seen following 100 mg fluocortolone.

Adult↗
PubMed1988

Fluocortolone: pharmacokinetics and effect on ACTH and cortisol secretion during daily and alternate-day administration.

The pharmacokinetics of fluocortolone and its effect on the circadian rhythm of plasma cortisol and ACTH have been studied during different schedules of oral administration. Groups of 6 healthy male adults were given a single daily dose of fluocortolone 5, 10 and 20 mg, and another group received 20 mg every second day. Administration to all groups was continued for 8 days. Pharmacokinetic parameters of fluocortolone (half lives of absorption-t1/2a and elimination t1/2e, volume of distribution V and oral clearance (CL/f) were independent of the duration of treatment and dose. Areas under the plasma level curves, AUC and Cmax values increased in proportion to the dose, indicating dose linearity of fluocortolone pharmacokinetics. A normal morning cortisol peak occurred during all treatment schedules, which indicates that circadian cortisol secretion was not seriously affected by the glucocorticoid treatment. On the other hand, when the level of circulating fluocortolone was high the 12.00 a.m. and 4.00 p.m. cortisol levels were diminished compared to the pre and posttreatment values. There was no definite correlation between the ACTH and cortisol levels, either on treatment or on control days. ACTH levels were suppressed by daily treatment with the 20 mg dose. Thus, even during administration of a high dose of a glucocorticoid, the circadian secretion of cortisol can be preserved if the treatment is adjusted according to the half-life of the drug.

Administration, Oral↗
PubMed2000

Treatment of erythrodermic cutaneous T-cell lymphoma with intermittent chlorambucil and fluocortolone therapy.

BACKGROUND: Erythrodermic cutaneous T-cell lymphomas (CTCL) including Sézary syndrome have been successfully treated with daily administration of chlorambucil and prednisone (Winkelmann regimen). OBJECTIVES: Our purpose was to determine the efficacy and safety of a low-dose pulse chemotherapy with chlorambucil and fluocortolone in this stage of the disease. Fluocortolone has the same potency as prednisone but lacks a mineralocorticoid effect. PATIENTS/METHODS: Thirteen patients with erythrodermic CTCL (stages III-IVb) were treated with chlorambucil and fluocortolone therapy (chlorambucil 10-12 mg day-1 for 3 days and fluocortolone, first day 75 mg, second day 50 mg and third day 25 mg) as primary therapy in an uncontrolled pilot study. Treatment was started with pulses every 2 weeks; subsequently, the intervals were prolonged according to the clinical status. Clinical outcome, side-effects and long-term survival were assessed. RESULTS: Seven patients achieved a complete remission and six had a partial response (improved significantly). The mean duration of remissions was 16.5 (median 12) months. The mean number of cycles necessary during the first year was one cycle every 5 weeks. No treatment-related severe side-effects occurred. The long-term follow-up (mean 31.5, median 27 months) showed that six patients remained in complete remission and three showed a stable partial remission. Four patients died, two of them from their lymphoma. CONCLUSIONS: We conclude that pulse chemotherapy with chlorambucil and fluocortolone is effective and safe in the treatment of erythrodermic CTCL and should be considered as an alternative to the classical Winkelmann treatment scheme.

Aged↗
PubMed1987

Differential effects of hydrocortisone, fluocortolone, and aldosterone on nocturnal sleep in humans.

Previous experiments have suggested that sleep processes are sensitive to influences of corticosteroids. The present experiment was designed to compare effects of three different corticosteroids on human sleep: fluocortolone (a synthetic pure glucocorticoid), cortisol which possesses glucocorticoid and mineralocorticoid activity, and aldosterone (the major mineralocorticoid). Ten male adult subjects were tested in four experimental nights according to a double-blind latin-square design under conditions of either 1.0 mg of aldosterone, 20 mg of fluocortolone, 80 mg of hydrocortisone, or placebo. Substances were administered orally (fluocortolone, 23.00 h) or infused iv throughout the night (hydrocortisone, aldosterone) starting at 23.00 h. Hydrocortisone and fluocortolone induced a substantial reduction of rapid eye movement sleep. Hydrocortisone increased slow wave sleep activity. No such effect was observed after fluocortolone. Effects on sleep processes of aldosterone, in general, seemed to be neglegible. The results demonstrate differential effects of synthetic glucocorticoid, cortisol, and aldosterone on sleep in humans, which may be attributed to the heterogeneity of corticosteroid receptors in the brain.

Administration, Oral↗
PubMed1984

The pharmacokinetics of fluocortolone and prednisolone after intravenous and oral administration.

The pharmacokinetics of fluocortolone and of prednisolone were examined following a single intravenous injection of 5 mg and oral administrations of 10 and 20 mg to five healthy male volunteers. After intravenous injection the plasma levels of fluocortolone decreased biexponentially with half-lives of 9 +/- 5 min and 1.3 +/- 0.3 h. Total plasma clearance of fluocortolone was calculated to be 7.0 +/- 1.5 ml/min/kg. Oral administrations of fluocortolone revealed maximum plasma levels of 86 +/- 12 ng/ml (10-mg dose) and 174 +/- 34 ng/ml (20-mg dose) after 1.4 +/- 0.2 h. Intravenously administered prednisolone was rapidly distributed (t 1/2 alpha = 5 +/- 3 min) but more slowly eliminated from plasma than fluocortolone (t1/2 beta = 3.1 +/- 0.8 h). Correspondingly a total plasma clearance of 2.2 +/- 0.2 ml/min/kg was calculated. Oral administrations revealed maximum prednisolone plasma levels of 172 +/- 25 ng/ml (10-mg dose) and 278 ng/ml (20-mg dose) after 1.6 +/- 0.7 h. The absolute bioavailability of both corticosteroids was higher than 80% and independent of both dose levels investigated.

Administration, Oral↗
PubMed1980

[Penetration kinetics of fluocortolone from a new base for ointment and creme (author's transl)].

The penetration of fluocortolone from topically administered Syracort ointment and creme was investigated in guinea pigs. Two fluocortolone standards were tested as reference preparations (ointment and creme). 1. Fluocortolone liberation from the ointments and Syracort Creme within 24 h varied between 55% and 62% of the administered dose. The reference creme gave lower drug liberation values (39%). 2. The penetration profile of fluocortolone changed gradually. Non-absorbed portions and the concentrations in the upper layers of the stratum corneum decreased during inunction up to 24 h. Within the same time concentrations in the deeper layers of the skin increased. 3. The two ointments showed comparably good penetration properties, whereas Syracort creme gave flux values higher than those obtained from the reference creme. 4. 24 h after removal of the non-absorbed portion of the ointments a further persistence of the drug could be observed within the skin: 14.3% to 18.5% after additional 6 days. The mean renal elimination rate was found to be 3 days, a total amount between 28% to 30% of the dose was excreted via urine and feaces. Consequently, fluocortolone can be considered a fast penetrating topical which is accumulated especially in the layers of the epidermis and cutis.

Animals↗
PubMed1988

Lack of impairment of fluocortolone disposition in oral contraceptive users.

Seven healthy women chronically (greater than 6 months) treated with oral contraceptives and 7 age- and weight-matched female controls were studied. Each subject was given 20 mg fluocortolone orally and the plasma concentrations of total and unbound fluocortolone in multiple samples obtained during the following 24 h were determined by HPLC and equilibrium dialysis. In the subjects on oral contraceptives there was no significant change in total clearance, unbound clearance or volume of distribution at steady-state of total and unbound fluocortolone, but there was a significant increase in hydrocortisone concentration compared to the control subjects. It appears that the elimination of the synthetic corticoid fluocortolone was not impaired by chronic administration of contraceptive steroids.

Adult↗
PubMed1977

[Binding of cortisol, fluocortolone and difluocortolone to human plasma proteins (author's transl)].

The binding properties of [3H]cortisol, [3H]fluocortolone and [3H]difluocortolone by human plasma, human albumin, human- beta- and gamma-globulins have been studied by equilibrium dialysis. Cortisol, in physiological concentrations (0,4 micromol/l), is 98% bound in human plasma at 25 degrees C, fluocortolone 96% and diflucortolone 85%. Uncer physiological conditions cortisol is mainly bound to the corticosteroid binding globulin (transcortin). 2/3 of fluocortolone is bound to transcortin and 1/3 to albumin and globulins, whereas difluocortolone is mainly bound to albumin and to globulins but not to transcortin. The binding affinities of beta- and gamma-globulins are -ery low for the corticoids investigated, but they are higher for fluocortolone and difluocortolone than for cortisol.

Carrier Proteins↗
PubMed1996

Pharmacokinetic/pharmacodynamic modeling of cortisol suppression after oral administration of fluocortolone.

Fluocortolone is a potent corticosteroid used orally for the treatment of rheumatic diseases, asthma, and immunosuppression. A clinical study of nine healthy volunteers was conducted to determine the pharmacokinetics and cortisol suppression after administration of single oral doses of 20 mg, 50 mg, and 100 mg of fluocortolone. Blood samples were collected at 8:00 AM, 12:00 PM, and 4:00 PM on the day before treatment, and 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 28, 32, 48, 52, and 56 hours after administration of the drug. Concentrations of fluocortolone and cortisol were measured in plasma by a reversed phase high-performance liquid chromatography system. Cortisol suppression was chosen as the pharmacodynamic parameter. Total concentrations were converted into unbound concentrations using a two-protein, one-ligand equation. The unbound concentrations were fitted using a one-compartment body model equation with first-order absorption. A linear release-rate model was used to characterize the cortisol data. The data were fitted using a common E50 value of 0.95 +/- 0.22 ng/mL for the mean data. The value of E50 was in close agreement with the prediction based on relative glucocorticoid receptor affinity.

Administration, Oral↗
PubMed1993

Pharmacodynamic modeling of cortisol suppression from fluocortolone.

The effect of fluocortolone on cortisol suppression was characterized using a 'direct suppression pharmacodynamic model'. The model incorporates the physiologic circadian secretion of cortisol under normal and treatment conditions, together with pharmacokinetic data from single fluocortolone doses of 20, 50, and 100 mg. A mean IC50 value (fluocortolone plasma concentration at which the circadian secretion of cortisol is inhibited by 50%) of 15.5 ng.ml-1 was found. This analysis shows how use of pharmacodynamic modeling can characterize dose-proportionality data to provide an in vivo measure of drug potency.

Depression, Chemical↗