RESUMO
BACKGROUND: Terazosin and tamsulosin are drugs currently used in the treatment of benign prostatic hypertrophy (BPH). The potency of these two alpha(1) receptor antagonists and that of prazosin to inhibit contractions induced by noradrenaline and the binding of [(3)H]-prazosin in human prostate and four different human arterial and venous vessels (saphenous and umbilical veins, renal and mesenteric arteries) was studied. METHODS: By bioassay and binding studies, we examined the receptor affinities of different alpha(1) receptor antagonists in different human tissues. RESULTS: pKb of terazosin, tamsulosin, and prazosin obtained in the prostatic tissues (8.15, 9.64, and 8.59, respectively) were not different from those obtained in the umbilical veins (8.07, 9.56, and 8.30, respectively), in the mesenteric artery (8.27, 10.29, and 9.01, respectively), renal artery (8.35, 10.13, and 8.76, respectively) and saphenous vein (7.8, 10.3, and 9.32, respectively). IC(50) (nM) of prazosin, terazosin, and tamsulosin obtained from binding studies in membrane preparations from prostate tissue were similar to those from umbilical veins, saphenous vein, and renal artery. CONCLUSIONS: All of the evaluated drugs showed similar selectivity for prostatic vs. vascular tissues. Thus, different clinical profiles of the present drugs should not result from their differential affinity for prostatic versus vascular alpha(1)-adrenoceptors.
Assuntos
Antagonistas de Receptores Adrenérgicos alfa 1 , Antagonistas Adrenérgicos alfa/farmacologia , Músculo Liso Vascular/efeitos dos fármacos , Próstata/efeitos dos fármacos , Antagonistas Adrenérgicos alfa/metabolismo , Relação Dose-Resposta a Droga , Feminino , Humanos , Cinética , Masculino , Artérias Mesentéricas/efeitos dos fármacos , Contração Muscular/efeitos dos fármacos , Músculo Liso Vascular/metabolismo , Músculo Liso Vascular/fisiologia , Norepinefrina/fisiologia , Prazosina/análogos & derivados , Prazosina/metabolismo , Prazosina/farmacologia , Próstata/metabolismo , Próstata/fisiologia , Receptores Adrenérgicos alfa 1/metabolismo , Receptores Adrenérgicos alfa 1/fisiologia , Artéria Renal/efeitos dos fármacos , Veia Safena/efeitos dos fármacos , Sulfonamidas/metabolismo , Sulfonamidas/farmacologia , Tansulosina , Veias Umbilicais/efeitos dos fármacosRESUMO
Metastatic Crohn's disease (MCD) is a cutaneous granulomatous reaction which affects patients with bowel disease in areas of the skin distant from the affected bowel. Penile involvement is a very uncommon observation. We report a case of penile ulcerative MCD in a 37-year-old man, which requested surgical management. The lesion developed during reactivation of the bowel disease.