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), α1-adrenergic receptor (α1-AR), and β-adrenerergic receptor (β-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 α1-AR and β2-AR. In contrast, the concentration of β3-ARs was significantly decreased (P < 0.05) in treated animals. The increase in prostate β2-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, β3-AR concentrations were significantly reduced in treated animals. Data collected suggest that the prostatic β-AR expression might be strongly influenced by oestrogen deprivation (mepartricin treatment); therefore, the combination of oestrogen suppression (mepartricin) and adrenergic suppression (α1-AR blockers) may be proposed as a possible nonhormonal therapeutic strategy for the treatment of benign prostatic hyperplasia in dogs.

Pharmacokinetics of tramadol in cats undergoing neutering / P. Cagnardi, A. Zonca, S. Carli, D. Fonda, G. Ravasio, R. Villa. - In: JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS. - ISSN 0140-7783. - 29:S1(2006), pp. 289-290. ((Intervento presentato al 10. convegno EAVPT International Congress tenutosi a Grugliasco nel 2006.

Pharmacokinetics of tramadol in cats undergoing neutering

P. Cagnardi
Primo
;
A. Zonca
Secondo
;
S. Carli;D. Fonda;G. Ravasio
Penultimo
;
R. Villa
Ultimo
2006

Abstract

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), α1-adrenergic receptor (α1-AR), and β-adrenerergic receptor (β-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 α1-AR and β2-AR. In contrast, the concentration of β3-ARs was significantly decreased (P < 0.05) in treated animals. The increase in prostate β2-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, β3-AR concentrations were significantly reduced in treated animals. Data collected suggest that the prostatic β-AR expression might be strongly influenced by oestrogen deprivation (mepartricin treatment); therefore, the combination of oestrogen suppression (mepartricin) and adrenergic suppression (α1-AR blockers) may be proposed as a possible nonhormonal therapeutic strategy for the treatment of benign prostatic hyperplasia in dogs.
Settore VET/09 - Clinica Chirurgica Veterinaria
Settore VET/07 - Farmacologia e Tossicologia Veterinaria
2006
European Association of Veterinary Pharmacology and Toxicology
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/32243
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