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At least 19 recordsLinked to original sources
PubMed2000

Spironolactone versus placebo or in combination with steroids for hirsutism and/or acne.

BACKGROUND: Hirsutism is the presence of excessive hair growth in women and is an important cosmetic condition often resulting in severe distress. Hirsutism is most often caused by increased production of male sex hormones also known as androgens. It is also affected by increased sensitivity to androgens in the hair follicles, and the secretory glands around the hair follicles, called sebaceous glands. Spironolactone is an antiandrogen and aldosterone antagonist used to treat hirsutism. Since 1978, many studies have been conducted to determine its effectiveness. OBJECTIVES: The objective of this review was to investigate the effectiveness of spironolactone and/or in combination with steroids (oral contraceptive pill included) in reducing excess hair growth and/or acne in women. SEARCH STRATEGY: All publications of randomised controlled trials of spironolactone versus placebo and/or in combination with steroids (oral contraceptive pill included) were identified. Search strategy was developed by the Menstrual Disorder Group. All accessable electronic databases were searched. In addition, all reference lists of relevant trials were searched and drug companies contacted for details of unpublished trials. SELECTION CRITERIA: All randomised controlled comparisons of spironolactone versus: placebo steroids (oral contraceptive pill included)) spironolactone of varying dosages or spironolactone and steroids versus steroids alone when used to reduce hair growth and acne in women. DATA COLLECTION AND ANALYSIS: Four trials were included in the review, seven trials were excluded. Two other trials are awaiting assessment. All included trials were small (no more than 31 participants) randomised and controlled. Only one trial studied acne as an outcome, the remaining three were concerned with hirsutism. One trial investigated spironolactone versus placebo; one trial was a dosage studies of spironolactone; one trial compared spironolactone with spironolactone in combination with dexamethasone; the remaining trial used topical spironolactone for the treatment of acne. Major outcome measures include the following: - subjective observations - Ferriman and Gallwey hair scores - hormonal and biochemical parameters - side effects - sebum production measurement MAIN RESULTS: All sample populations were small and confidence intervals were wide. There was no significant difference between treatments for any of the observed outcomes. REVIEWER'S CONCLUSIONS: The effectiveness of treatment for either acne vulgaris or hirsutism cannot be determined due to the small sample populations involved in the trials. Its value in clinical practice is difficult to assess from currently available research.

Acne Vulgaris↗
PubMed1998

Water-soluble beta-cyclodextrins in paediatric oral solutions of spironolactone: preclinical evaluation of spironolactone bioavailability from solutions of beta-cyclodextrin derivatives in rats.

Water-soluble derivatives of beta-cyclodextrin have been considered for solubilization of spironolactone in the formulation of a safe liquid preparation for premature infants. The oral absorption of spironolactone was studied in rats to evaluate the need to adjust spironolactone dosage in prospective clinical studies. Spironolactone was administered in solutions of sulphobutyl ether beta-cyclodextrin (SBE7) or dimethyl-beta-cyclodextrin (DM-beta-CyD) and also as spironolactone-containing powder papers (reference preparation). Spironolactone in SBE7 solution was administered intravenously to assess the extent of intestinal absorption from the different formulations. Spironolactone and the metabolites 7alpha-thiospirolactone, 7alpha-thiomethylspirolactone and canrenone were determined in rat serum after intravenous administration of spironolactone. Half-lives for spironolactone, 7alpha-thiomethylspirolactone and canrenone were 0.72 +/- 0.17, 1.5 +/- 0.3 and 2.2 +/- 0.3 h, respectively. Although, according to Cmax values, 7alpha-thiomethylspirolactone was the major serum metabolite in rats, higher AUC (area under the serum concentration-time curve) values were obtained for canrenone. After oral administration of spironolactone the bioavailabilities evaluated from the AUC values of 7alpha-thiomethylspirolactone were 27.5 +/- 9.3%, 81.3 +/- 28.8% and 82.8 +/- 28.6% for powder papers, DM-beta-CyD and SBE7 solutions, respectively. The oral absorption of spironolactone by rats was better after administration of spironolactone in SBE7 and DM-beta-CyD solutions than after administration as powder papers. Both cyclodextrin formulations enhanced spironolactone bioavailability to a similar extent despite some deacetylation of spironolactone in the presence of SBE7. A reduction of spironolactone dosage would be recommended during clinical studies with premature infants. These results indicate that SBE7 could be a safe and suitable excipient for the solubilization of spironolactone in paediatric formulations.

Animals↗
PubMed2000

[Treatment of hirsutism with spironolactone and with spironolactone plus dexamethasone].

BACKGROUND: Spironolactone has an anti androgenic effect, inhibiting the binding of androgens to their receptor. This antagonistic effect is the basis for the use of spironolactone in the treatment of hirsutism. AIM: To study the effectiveness and safety of spironolactone in the treatment of hirsute women and of the association of spironolactone plus dexamethasone in the treatment of hirsutism with glucocorticoid sensitive hyperandrogenism. PATIENTS AND METHOD: Sixteen women (group 1) with peripheral hirsutism (defined as those with normal androgens levels, normal menstrual cycles and ovulation) and 24 women (group 2) with glucocorticoid sensitive hyperandrogenic hirsutism were studied. Group 1 was treated with spironolactone 50 mg hid and group 2 with same spironolactone dose plus dexamethasone 0.5 mg at 23 h during one month and 0.25 mg thereafter. Patients were followed during one year. RESULTS: After one year of treatment, a 54% reduction in Moncada hirsutism escore was observed in group 1 and 52% reduction in group 2. Observed secondary effects of spironolactone were increases in diuresis, fatigability, acne aggravation and seborrhea in two patients. Two additional patients had spotting. No secondary effect attributable to glucocorticoid use were observed. CONCLUSIONS: Spironolactone is effective and safe in the treatment of hirsutism. Androgenic supression did no increases its effectiveness, underscoring the peripheral anti androgenic activity os spironolactone.

Adolescent↗
PubMedDate not supplied

Readministration of spironolactone in the spironolactone-intolerant patient.

We report a successful practical protocol for readministration of spironolactone in a patient with cirrhosis and severe ascites whose initial exposure to spironolactone resulted in erythema multiforme. Because salt and water restriction and other diuretics were ineffective, readministration of spironolactone was considered appropriate. In the absence of in vitro or in vivo diagnostic tests for drug allergy to spironolactone, serial increasing doses from 1 mg to 400 mg were administered over a 14 day period and tolerated uneventfully. A mild maculopapular rash appeared a month later but resolved despite continuation of spironolactone. The patient has now received spironolactone successfully for a total of 20 months without evidence of subsequent drug hypersensitivity. Although proven drug hypersensitivity attributable to spironolactone is very rare, when allergic manifestations have occurred in a patient who may require readministration of spironolactone, we believe that the suggested protocol for test-dosing be considered.

Drug Hypersensitivity↗
PubMed2004

A comparison between spironolactone and spironolactone plus finasteride in the treatment of hirsutism.

OBJECTIVE: To compare the clinical efficacy and safety of the combination of spironolactone (100 mg/day) plus finasteride (5 mg/day) and spironolactone (100 mg/day) alone in the treatment of hirsutism. PATIENTS AND MEASUREMENTS: Sixty-five hirsute women were randomly assigned to one of these two treatment groups. Hirsutism score was measured according to the modified Ferriman-Gallwey scoring system. Baseline and post-treatment assessments were carried out in each subject by an investigator blinded to the therapy. Both groups had similar demographic properties at baseline. The serum levels of total and free testosterone, dehydroepiandrosterone sulphate and sex hormone-binding globulin were measured at the beginning and after 1 year of therapy. Blood chemistry and side-effects were evaluated during the study. Hirsutism scores were decreased significantly in both groups at the end of the year. RESULTS: The mean percentage change in hirsutism scores from baseline in the spironolactone plus finasteride-treated group (51.3%) was significantly (P<0.005) higher than in the group treated with spironolactone alone (36.6%). Patients from both treatment groups experienced similar side-effects. CONCLUSIONS: We have concluded that a combination of spironolactone plus finasteride is a safe and effective therapy in the treatment of hirsutism.

Adult↗
PubMed1977

Renin levels and spironolactone treatment in general practice: similar blood pressure lowering effect of spironolactone in low and normal renin patients.

We examined the predictive value of plasma renin activity (PRA) in ambulatory patients in the selection of hypertensive patients for treatment with spironolactone. The patients were classified as frusemide responders or non-responders according to their PRA response to 80 mg frusemide orally. After an initial 4 weeks placebo period forty-five patients with the clinical diagnosis of benign hypertension (WHO stage I-II) entered a 4 X 4 week double blind treatment period during which they received spironolactone (Aldactone) 400, 300, 200 and 100 mg/day, respectively. Five out of the forty-five patients who started the trial were withdrawn on account of side-effects and five patients for other reasons. Of the thirty-five patients who completed the study eighteen belonged to the group of non-responders to frusemide, seventeen to the responders. A gradual and significant decrease in mean blood pressure occurred during the period with the high doses of spironolactone, without any significant difference between the groups. The blood pressure lowering effect obtained with the initial high doses was maintained during the consecutive periods when the doses was reduced to a half or even a fourth, in both groups. We conclude that PRA measurement in ambulatory patients is of little, if any, value for the selection of hypertensives for spironolactone treatment; this in contrast to similar selections performed on hospitalized patients.

Adult↗
PubMed1976

A comparison of the dissolution and bioavailability characteristics of three spironolactone tablet formulations, including preliminary data on two spironolactone metabolites.

The bioavailabilities of three spironolactone tablet formulations specially selected for major differences in in vitro dissolution tests were compared in normal male volunteers by measuring plasma and urinary levels of the pharmacologically active spironolactone metabolite canrenone. It was possible to demonstrate small but statistically significant differences in plasma canrenone concentration-time curves derived from the three formulations together with significant differences in the time course of urinary canrenone excretion. The bioavailabilities of the three formulations did not differ significantly although the tablet with the poorest in vitro dissolution produced a significant delayed peak canrenone concentration. The dissolution rate methodology and results are described and an approach to the development of improved in vitro dissolution tests for spironolactone is suggested. The use of a new method for canrenone estimation resulted in the incidental detection of two other quantitatively significant spironolactone metabolites and preliminary information is given on these.

Adolescent↗
PubMed2004

Novel spironolactone-analogs as impurities in spironolactone.

Six novel spironolactone-analogs steroids (3-8) were isolated from spironolactone by using various chromatographic methods. Their structures were elucidated by spectrometric analysis. Two of the analogs (3 and 7) were confirmed by X-ray crystallography. The A-ring of compounds 3-7 is opened at C-2C-3 bond, and compound 7 is an organic polysulfide, which has a rare, nine-membered ring with a five sulfur atom bridge.

Crystallography, X-Ray↗
PubMed2005

The effect of spironolactone on experimental periodontitis in rats.

BACKGROUND: Elevated levels of tumour necrosis factor (TNF) have been found in patients with adult periodontitis. Animal studies have shown that TNF plays an important role in the pathogenesis of periodontitis. New findings suggest that the aldosterone-inhibitor spironolactone possesses an anti-TNF effect. The purpose of the study was to determine the anti-TNF effect of spironolactone in an endotoxic shock rat model and to disclose the effect of oral administration of spironolactone on the development of experimental periodontitis in rats. METHODS: The study was divided in two parts. Part 1: oral administration of spironolactone (100 mg/kg) followed by intravenous lipopolysaccharide (1 mg/kg) infusion 45 min later. Blood samples were taken before and 90 min after lipopolysaccharide infusion to determine the TNF levels in spironolactone treated and non-treated rats. Part 2: oral administration of spironolactone [100 mg/(kg day)] starting 2 days prior to induction of experimental periodontitis established by peridental ligatures. Morphometrical and radiographical registrations of alveolar bone destruction were carried out to determine the effect of spironolactone on the progression of experimental periodontitis. RESULTS: In part 1 the endotoxic shock model showed a significant reduction in TNF levels in the spironolactone-treated group compared to the non-treated group, suggesting that spironolactone acts as a TNF inhibitor. In part 2 spironolactone-treated rats did not demonstrate significantly less alveolar bone destruction compared to non-treated rats. CONCLUSIONS: The insignificant effect of spironolactone treatment could be explained by the fast metabolism of spironolactone and that spironolactone does not completely inhibit TNF production in rats. Moreover, many other cytokines and mediators involved in alveolar bone destruction may account for the lacking response to spironolactone.

Administration, Oral↗
PubMed2003

Potential beneficial as well as detrimental effects of chronic treatment with lisinopril and (or) spironolactone on isolated hearts following low-flow ischemia in normal and infarcted rats.

This study was designed to demonstrate potential beneficial as well as detrimental effects of lisinopril and spironolactone given in combination. In patients with congestive heart failure or myocardial infarction, the use of angiotensin-converting enzyme (ACE) inhibitors may inhibit aldosterone production. Spironolactone, a specific aldosterone receptor antagonist may exert other independent and additive effects to those of ACE inhibitors. Given the consequences of aldosterone on ischemic hearts, we evaluated the protective effects of spironolactone or lisinopril and combined spironolactone-lisinopril therapy during low-flow ischemia and reperfusion in isolated rat hearts. Normal and infarcted (left coronary artery ligature) male Wistar rats were submitted to chronic action of drugs (0.8 mg.kg-1.day-1 for lisinopril and 8 or 50 mg.kg-1.day-1 for spironolactone) for 1 month. Hearts were rapidly excised and perfused (constant pressure) for a 40-min period of stabilization followed by a 25-min period of global low-flow ischemia and a 30-min reperfusion. In normal rats, spironolactone decreased ischemic and reperfusion contracture, reduced ventricular tachycardia, suppressed action-potential duration dispersion, and increased reactive hyperemia leading to an improvement of contractile recovery. Lisinopril also decreased ventricular tachycardia and action-potential duration dispersion concomitantly with increased reactive hyperemia and better contractile recovery. These beneficial effects of the drugs were lost when the two treatments were combined (lisinopril and 50 mg.kg-1.day-1 spironolactone), despite a synergistic effect on plasmatic K+ and Mg2+. However, an interaction between the ACE inhibitor and spironolactone potentiating the effects of either drug alone was observed with a lower dose of spironolactone (lisinopril and 8 mg.kg-1.day-1 spironolactone). Similar beneficial effects have been noted in infarcted rat hearts on reactive hyperemia, ventricular tachycardia, and contractile recovery with the combined treatment and for both spironolactone concentrations (8 or 50 mg). Chronic spironolactone treatment produces similar beneficial effects to ACE inhibitor treatment on normal rat hearts during an ischemia-reperfusion protocol. Synergistic effects have been observed with the combined therapy when a lower dose of spironolactone was utilized in normal and infarcted rats. However, in the case of a high dose of spironolactone, the two effective drugs seem to cancel each other but only in normal rats.

Action Potentials↗