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.

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.

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.

[Multicenter clinical study of the effects of once daily administration of mepartricin 150.000 U. in benign prostatic hypertrophy]. / Studio clinico multicentrico degli effetti dell'ipertrofan cpr. nella IPB con monosomministrazione giornaliera di 150.000 U.

The effects of partricin methyl ester, administered to 481 BPH patients at the dose of 150.000 U as a single administration at night for 90 days were studied in the course of a multicentre study. The favourable evolution of the objective and subjective symptomatologic parameters taken into consideration confirmed the efficacy of the substance used even by this mode of administration. The size of the patient sample ensured that reliable findings were obtained as regards the excellent safety of this form of dosage.

[The effects of mepartricin on the symptomatology of prostatic hypertrophy--double-blind controlled trial]. / Etude de l'effect de la mépartricine sur la symptomatologie de l'hypertrophie prostatique--expérimentation contrôlée en double aveugle.

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.

[Correction of hyperdyslipidemia using polyene-structure substances. Controlled clinical trial]. / Correzione degli stati iperdislipidemici mediante una sostanza a struttura polienica. Ricerca clinica controllata.

Mepartricin (SPA-S-160 enteric-coated tablets) fat-lowering effect was evaluated in 20 patients with lipids disorders of various type. The cross-over trial was carried out with clofibrate as reference drug. Posology consisted, in both treatments, of 3 tablets/die. All subjects received each drug for a 30-day period, with a drug-free interval of 30 days. The results proved positive for both drugs but mepartricin showed a better therapeutical index. Local and systemic tolerance was good for both drugs even though the transaminases values were found to be sensibly higher after the therapeutic cycle with clofibrate.

[Short-term treatment of vaginal trichomoniasis and moniliasis. Clinical trial of a soluble complex of mepartricin]. / Trattamento "short-term" delle trichomoniasi e delle moniliasi vaginali. Ricerche cliniche con un complesso solubile della mepartricina.

The efficacy and tolerance of mepartricin sodium lauryl sulphate (SPA-S-222) was evaluated in patients with vaginal trichomoniasis and/or moniliasis. One group received 4 tablets/day for 3 days (group "A"), and the other (group "B") 1 tablet/8 hr for 4 days. A lasting microbiological cure was obtained in all cases. Tolerance was better in group "B" and it is felt that this protocol should be preferred.