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PubMed1996

[Mepartricin 150.000 (40 mg) vs mepartricin 50.000 U (13 mg) in the treatment of BIP. Double blind clinical trial].

A group of 25 patients with uncomplicated BPH was treated mepartricin 150,000 U (40 mg) once in the evening for 60 days and the results were compared with those obtained in 25 patients treated with mepartricin 50,000 U (13 mg) t.d.s. Efficacy and tolerance of both treatment schemes were good. In the group treated with on single dose at night some symptoms such as nocturia and pollakiuria regressed more rapidly.

Aged↗
PubMed2006

Mepartricin long-term administration regulates steroid hormone and adrenergic receptor concentrations in the prostate of aged rats.

Mepartricin is a semi-synthetic macrolide antibiotic developed as a drug for the treatment of benign prostatic hyperplasia (BPH) in human patients. In the present study, aged rats are used as an experimental model to evaluate the effects of mepartricin on circulating hormone concentrations and prostate receptor concentrations, to compare these possible effects with clinical findings observed in long-term treated dogs. Fifty-six aged male rats were randomly divided into four experimental groups treated orally with 0 (group 1), 2 mg (group 2), 5 mg (group 3) and 20 mg (group 4) mepartricin/kg of body weight. for 28 days respectively. Serum oestradiol and testosterone concentrations were measured by radio-immune-assays methods. Binding assays were used to measure the prostate concentrations of oestrogen receptors (ER), androgen receptors (AnR), alpha(1)-adrenergic receptor (alpha(1)-AR), and beta-adrenerergic receptor (beta-AR) subtypes. Mepartricin induced a significant reduction of prostate weight and serum oestradiol concentrations. Serum testosterone concentrations were unaffected. The treatment induced a significant down-regulation of ER concentrations (P < 0.05) and a significant up-regulation of AnR (P < 0.05) in rat prostate. Mepartricin induced a significant (P < 0.05) dose-dependent up-regulation of alpha(1)-AR and beta(2)-AR. In contrast, the concentration of beta(3)-ARs was significantly decreased (P < 0.05) in treated animals. The increase in prostate beta(2)-AR concentrations observed in subjects treated with mepartricin may be a favourable element in the evolution of BPH, because of the role exerted by these receptors in the control of prostatic smooth muscle relaxation. Curiously, beta(3)-AR concentrations were significantly reduced in treated animals. Data collected suggest that the prostatic beta-AR expression might be strongly influenced by oestrogen deprivation (mepartricin treatment); therefore, the combination of oestrogen suppression (mepartricin) and adrenergic suppression (alpha(1)-AR blockers) may be proposed as a possible nonhormonal therapeutic strategy for the treatment of benign prostatic hyperplasia in dogs.

Administration, Oral↗
PubMed1998

Double-blind, placebo-controlled trial to assess the efficacy and tolerability of mepartricin in the treatment of BPH.

BACKGROUND: Mepartricin, a semisynthetic polyene derivative with a favorable effect on urethro-prostatic function, was clinically evaluated, adopting the diagnostic and research criteria recommended by the First International Consultation on BPH. METHODS: A multicenter, randomized, double-blind, parallel-group study compared mepartricin 40 mg/daily to placebo in the treatment of 196 patients with newly diagnosed BPH and mild-to-moderate symptomatology. International Prostate Symptom Score (I-PSS), quality of life (QoL) index and maximum urinary flow-rate (Qmax) were determined every 4 weeks for 6 months; postvoiding volume, prostate volume, and prostate-specific antigen (PSA) were assessed after 3 and 6 months of therapy. RESULTS: Mepartricin was shown to determine a statistically significant improvement over placebo in I-PSS and QoL index from month 2 onwards, and a significant linear increase in Qmax over the study period. At month 6, the improvement in the mepartricin and placebo groups in I-PSS, QoL index, and Qmax was 6.3 (standard error (SE) 0.51) and 4.2 (SE 0.60) points (P = 0.003), 0.99 (SE 0.14) and 0.62 (SE 0.12) points (P = 0.036), and 2.7 (SE 0.46) and 1.2 (SE 0.46) ml/sec (P = 0.051), respectively. No significant differences were noted in postvoiding residual volume, prostate volume, or PSA. Mepartricin tolerability was good, showing no adverse events on sexual function. CONCLUSIONS: Mepartricin proved to be an effective treatment of benign prostatic hyperplasia, determining an improvement in symptoms, quality of life, and peak urinary flow.

Aged↗
PubMed1998

Estrogen suppression as a pharmacotherapeutic strategy in the medical treatment of benign prostatic hyperplasia: evidence for its efficacy from studies with mepartricin.

Estrogen suppression has been introduced as a pharmacotherapeutic strategy in the medical treatment of benign prostatic hyperplasia. Recent negative results obtained in placebo-controlled trials with the aromatase inhibitor atamestane raised doubts about the efficacy of estrogen reduction. However, inhibition of aromatase not only reduces estrogens but also increases androgens which promote prostatic growth. In order to reevaluate the therapeutic efficacy of estrogen suppression, we summarize clinical trials investigating the therapeutic effects of mepartricin in the treatment of uncomplicated benign prostatic hyperplasia. Mepartricin has been reported to lower the levels of circulating estrogens without causing changes in other hormones such as androgens. By applying stringent inclusion criteria, 23 studies (including 7 placebo-controlled trials, 3 post-marketing surveillance studies, and 13 open trials) published between 1982 and 1996 were selected to be included in this report. In 79.9% of 4635 patients treated with mepartricin, its therapeutic effect was rated "good" or "excellent". In 6 out of 7 placebo-controlled trials, the therapeutic efficacy of mepartricin was significantly superior to that of placebo. Comparison of these data with results obtained with alpha 1-adrenoceptor antagonists or with the 5 alpha-reductase inhibitor finasteride indicates that mepartricin is as efficient as these widely accepted medical treatments for benign prostatic hyperplasia. Since mepartricin acts selectively upon estrogens, the present results show that estrogen suppression may be considered an efficient pharmacotherapeutic strategy in the medical treatment of uncomplicated benign prostatic hyperplasia.

Clinical Trials as Topic↗
PubMed2001

Effects of mepartricin on estradiol and testosterone serum levels and on prostatic estrogen, androgen and adrenergic receptor concentrations in adult rats.

The effects induced by oral administration of 0, 5 and 20 mg of meparticin kg(-1)of body weight for 28 days (group 1, 2 and 3, respectively) upon prostatic estrogen, androgen, alpha(1)- and beta-adrenergic receptor concentrations and on estradiol and testosterone serum levels in adult male rats were studied. The effects produced by mepartricin treatments on the weight and dimension of the gland were investigated. Both mepartricin dosages induced significant decreases (P< 0.05) of the absolute and relative weights and of the dimensions of the prostate. A significant dose-dependent decrease (P< 0.05) in estradiol serum levels was observed in treated rats, whereas no significant modifications were found in testosterone serum levels. As far as prostatic steroid receptor concentrations were concerned, a significant (P< 0.05) decrease in estrogen receptor number was observed in both treated groups, whilst a significant increase (P< 0.05) of androgen receptor concentrations was recorded only in rats treated with 20 mg mepartricin kg(-1). Conversely, a dose-dependent up-regulation of both prostatic alpha(1)- and beta-AR was found. Data obtained suggest that the prostatic alpha(1)-AR expression may be strongly influenced by estrogen deprivation (mepartricin treatment), therefore the combination of estrogen suppression (mepartricin) and adrenergic suppression (alpha(1)-AR blockers) may be suggested as a possible pharmacotherapeutic strategy for the treatment of benign prostatic hyperplasia.

Administration, Oral↗
PubMed2005

Effects of mepartricin, a polyene macrolide antibiotic, on estrogen-induced hyperplastic growth of the dorsolateral prostate and seminal vesicle in immature castrated rats.

OBJECTIVE: To investigate the effects of mepartricin, a polyene macrolide antibiotic, on estrogen-induced hyperplastic prostate and seminal vesicle (SV) growth in castrated rats. MATERIAL AND METHODS: Immature rats aged 3 weeks were castrated and left untreated for 1 week. Then, 17beta-estradiol benzoate (E(2)-BA) was subcutaneously injected at a dose of 10 microg/day twice weekly, and mepartricin was orally administered at doses of 2.5, 5 and 10 mg/kg once daily for 3 weeks. The weights and hydroxyproline contents of the prostate and SV, the activity of growth factors (GFs) in the dorsolateral prostate (DLP) and the serum estrogen level were measured. Histological examination of the prostate and SV was also performed. RESULTS: Mepartricin dose-dependently suppressed the increase in the serum estrogen level, the weights and hydroxyproline contents of the DLP and SV and the elevation of GF activity in the DLP induced by E(2)-BA treatment. Histological examination also revealed that treatment with mepartricin reduced collagen accumulation and thickening of the smooth muscle layer in the DLP and SV, and proliferation of the glandular epithelium in the DLP. CONCLUSIONS: These results suggest that mepartricin suppresses hyperplastic growth of the DLP and SV induced by estrogen in immature castrated rats, the underlying mechanism being a reduction in the serum estrogen level, thereby suppressing stromal cell proliferation and activation.

Animals↗
PubMed2001

[Mepartricin in the treatment of male pelvic pain syndrome secondary to chronic nonbacterial prostatitis/prostatodynia].

BACKGROUND: The aim of this paper is to compare the activity of mepartricin vs placebo in male pain pelvic syndrome secondary to chronic nonbacterial prostatitis/prostatodynia. METHODS: Forty-two patients have been tested (mean age: 35 years; range 29-44), these proved affected by male pain pelvic syndrome secondary to chronic nonbacterial prostatitis/prostatodynia, and were randomized into 2 groups: the 1st treated with mepartricin 40 mg/die for 60 days, the 2nd with placebo (C vitamin 500 mg/die) for 60 days. The following patterns were examined: spontaneous and rectal examination pain, diurnal and nocturnal urinary frequency and prostatic volume. Side effects in course of therapy were examined as well. RESULTS: Mepartricin proved significantly more active than placebo in reducing spontaneous pain, rectal examination pain, diurnal urinary frequency, nicturia and prostatic volume. No significant difference proved to emerge between placebo and mepartricin in terms of side effects. CONCLUSIONS: These data allow us to substain that mepartricin may be a useful and safe drug for the therapy of male pain pelvic syndrome secondary to chronic nonbacterial prostatitis/prostatodynia.

Adult↗
PubMed2004

Role of mepartricin in category III chronic nonbacterial prostatitis/chronic pelvic pain syndrome: a randomized prospective placebo-controlled trial.

OBJECTIVES: To verify the efficacy of mepartricin versus placebo with regard to symptom improvement in patients with chronic nonbacterial prostatitis/chronic pelvic pain syndrome (CPPS) and to verify a relation between hormonal levels and clinical improvement in these patients. METHODS: Twenty-six patients with CPPS were included in our study and randomized into two groups of 13 subjects each. Group 1 patients were treated with mepartricin (40 mg daily) and group 2 patients with placebo. All patients underwent treatment for 60 days. At the beginning and end of therapy, all patients underwent evaluation, including a standardized history, physical examination, luteinizing hormone, follicle-stimulating hormone, testosterone, and beta-estradiol measurements, and a National Institutes of Health-Chronic Prostatitis Symptom Index (NIH-CPSI) questionnaire. RESULTS: We observed a decrease in the total NIH-CPSI score from 25.0 to 10.0 in group 1 and from 25.0 to 20.0 in group 2, revealing a 60% and 20% improvement in groups 1 and 2, respectively. A statistically significant decrease was observed with regard to pain (from 11.0 to 4.0 and from 10.0 to 8.0, respectively) and quality of life (from 10.0 to 5.0 and 10.0 to 9.0, respectively). No statistically significant difference was observed in urinary dysfunctions. The luteinizing hormone, follicle-stimulating hormone, and testosterone values were similar in both groups before and after treatment; the 17-beta-estradiol levels were significantly lower in group 1 compared with group 2 at the end of the study. CONCLUSIONS: Mepartricin provides significant symptomatic improvement in men with CPPS compared with placebo. The role of mepartricin in decreasing estrogen plasmatic levels and their concentration in the prostate may account for this clinical improvement.

Adult↗
PubMed1985

A comparison of the activity of mepartricin and amphotericin B against yeasts.

An in-vitro comparison was made of the activity of mepartricin and amphotericin B against yeasts both in the presence and absence of pooled human plasma. The methods used included minimum inhibitory concentrations (MICs), liquid cultures and scanning electron microscopy (SEM). Mepartricin was found to be consistently more active than amphotericin B and to exhibit a partial inhibitory action over a wider range of concentrations below the MIC. In the presence of plasma, amphotericin B had increased activity but there was a slight reduction for mepartricin. By electron microscopy both drugs exhibited a rapid effect on Candida albicans and the cell membrane was found to be their primary target. Mepartricin was found to have the additional effect of causing a delayed separation of dividing cells and damage on both sides of the septum between mother and daughter cells. This suggests interference with the enzymatic mechanism of septum formation or chitin synthesis.

Amphotericin B↗
PubMed2001

[Mepartricine and prostatitis. Clinical experience and rationale for use].

BACKGROUND: The purpose of this study was to report our experience on the use of Mepartricine in the treatment of chronic and sub-acute prostatitis and to analyse, on the basis of the literature, the role of estrogens, the target of Mepartricine in the development and maintenance of prostatic inflammatory reactions. METHODS: In a retrospective study the data of 110 patients who presented with lower urinary tract symptoms suggestive of prostatitis, from January 1994 to February 1999 have been evaluated: 65 of this patients had an abacterial prostatitis, and 45 a bacterial prostatitis. The Mearers-Stamey test was used to localize inflammation and pathogens to prostate. The clinical symptoms presented were essentially pelvic and perineal pain and irritative and obstructive voiding symptoms. The treatment was based on antibiotic therapy indicated by the sensitivity to antibiotic assay. In abacterial prostatitis, in cases of Chlamidia, Mycoplasma and Ureaplasma positivity, the treatment was based on macrolides and tetracycline use. All the patients received Mepartricine by oral supply, 1 daily tablet (40 mg) for 60 days. RESULTS: After two months of treatment remarkable improvements in symptoms were obtained despite the persistent bacteriological positivity in the prostatic secretion in 68% of cases. Therefore antinflammatory antiedemic and decongestant effects of Mepartricine on prostatic inflammation, are observed. CONCLUSIONS: The data of the literature show data estrogens modulate inflammatory reactions: it is possible that their decrease can produce, at prostatic level, antinflammatory effects improving urethro-prostatic bladder functions. Personal experience seems to confirm this supposition and so we think that Mepartri-cine can be considered and excellent coadjuvant in the treatment of prostate inflammation, independent of etiology.

Adult↗
PubMed1991

[The effects of mepartricin on the symptomatology of prostatic hypertrophy--double-blind controlled trial].

Seventy one patients were treated with mepartricin or placebo in three urological centres for a mean duration of 102 days (extremes: 60 and 142 days). An analysis of the results was carried out for 34 patients in the placebo group and 36 patients in the mepartricin group. The results indicate a significant improvement in both the placebo group and the mepartricin group. The irritative and obstructive symptoms are improved in the active treatment group with a response rate of the order of 70%, compared to approx. 45% in the placebo group. An improvement of the values on the flow meter, though not statistically significant, is observed following treatment with mepartricin, compared to the placebo group. There were no significant differences in the evolution of the prostate gland volume, determined by ultrasound in the placebo group and the active treatment group. Side-effects were minor and only one patient reported epigastric pain.

Aged↗
PubMed1978

Mepartricin, a polyene active on both Trichomonas and Candida. Lack of mutagenic activity.

Mepartricin, the methyl ester of partricin, is a new polyene antibiotic with antifungal and antiprotozoal activity. The antitrichomonas activity in vitro is comparable to that of metronidazole, the widely used drug recently demonstrated to possess mutagenic activity and thus to be used with caution in therapy. Clinical investigations have shown that mepartricin can be successfully used in the topic treatment of vaginal trichomoniasis and candidiasis. The mutagenic activity of mepartricin has been evaluated using the Ames' test and compared to that of metronidazole. No mutagenic activity was detected for mepartricin. The drug can thus be proposed as a safer and efficient alternative to metronidazole.

Administration, Topical↗
PubMed1999

Effects of mepartricin, a polyene macrolide agent, on fecal excretion and serum concentration of estrogen and number of prostatic estrogen receptors in immature rats.

BACKGROUND: Mepartricin, an antifungal agent, was investigated for effects on fecal excretion and serum concentration of sex steroids and the number of sex steroid prostatic receptors in immature rats. METHODS: Mepartricin was orally administered at 2.5, 5, and 10 mg/kg once daily for 2 weeks. Fecal estrogen and testosterone excretions, serum estrogen, testosterone and luteinizing hormone concentrations, and numbers of prostatic estrogen and androgen receptors were assayed. Prostate weight was also monitored. RESULTS: Fecal estrogen excretion showed a dose-dependent increase, which was significant for the two higher dosages. Conversely, the serum estrogen concentration and prostatic estrogen receptors were significantly decreased. No significant changes in fecal testosterone excretion, serum testosterone and luteinizing hormone concentrations, and prostatic androgen receptors were observed. Prostate weight was significantly reduced at 5 mg/kg, but we did not observe dose-dependency. CONCLUSIONS: Mepartricin increases fecal excretion of estrogen by binding with it in the intestinal tract, which results in reducing the serum estrogen concentration and number of prostatic estrogen receptors.

Administration, Oral↗
PubMed2001

Binding of mepartricin to sex hormones, a key factor of its activity on benign prostatic hyperplasia.

Androgens and estrogens, mainly testosterone (TES) and dihydrotestosterone (DHT) and 17 beta-estradiol (EST), are widely recognized to regulate the prostate growth and their imbalance with aging, leading to reduction of androgens and relative increase of estrogens, may be responsible for the development of benign prostatic hyperplasia (BPH). Mepartricin (CAS 11121-32-7), a polyene drug for medical treatment of BPH, was assayed in vitro for its ability to bind with 14C-labelled sex hormones, by incubation in buffered saline, serum and bile, followed by centrifugation and dosing of the radioactivity in the supernatant. It proved effective in complexing up to 90% of TES and DHT in buffered saline and up to 80% of EST in bile. Due to minimal absorption of oral mepartricin and to much higher enterohepatic circulation for estrogens than for androgens, the binding effect of mepartricin on EST in the gut should be of particular pharmacological relevance to explain its mechanism of action on BPH.

Animals↗
PubMedDate not supplied

Changes in the plasma pattern of sex steroids in patients with liver cirrhosis treated with mepartricin.

Mepartricin was given to cirrhotic patients in order to evaluate its effect on the imbalance of sex steroids which is typical of this disorder. Patients were divided into two group: one group received placebo (n = 19) and the other received 150,000 IU/day mepartricin for 30 days (n = 19). The patients were evaluated by separate medical staff who were unaware of the treatment. Mepartricin significantly decreased the plasma concentration of testosterone, oestradiol and prolactin as compared with the values at the start of the trial, while no significant changes were seen in the occurrence of gynaecomastia. No relevant changes were seen in patients receiving the control, except for a slight increase in the peripheral concentration of androstenedione, aldosterone and follicle stimulating hormone.

Aldosterone↗
PubMedDate not supplied

Faecal elimination of steroids in rats after oral administration of mepartricin.

Treatment of both male and female rats with 5 IU/day mepartricin for 7-10 days administered by gastric tubing resulted in an increased faecal excretion of some steroids. Mean rate of elimination of total oestrogens was enhanced by 45% in male rats and by 14% in female rats, and the average excretion of conjugated oestrogen was also increased in the female animals. Faecal elimination of cholesterol was 37% and 42% higher in male and female rats, respectively, after mepartricin treatment, and in male rats plasma concentrations of cholesterol were reduced following treatment. It is suggested mepartricin acts either by changing the intestinal flora or by acting directly on the steroid moieties, and it is speculated that a similar mechanism may occur in man.

Administration, Oral↗