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Clinical application of 5alpha-reductase inhibitors.

机译:5α-还原酶抑制剂的临床应用。

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The inhibitors of 5alpha-reductase isoenzymes (1 and 2) can be schematically divided in three groups according they substrate specificity: a) pure or preferential inhibitor of 5alpha-reductase 1; b) pure or preferential inhibitor of 5alpha-reductase 2; c) dual inhibitors. Despite the fact that several steroidal and non-steroidal inhibitors have been synthesized and experimented in pharmacological models, only finasteride has been extensively used for clinical purposes. The largest application of finasteride in man has been human benign prostative hyperplasia (BPH). In addition, finasteride has been recently used for treatment of male baldness with a 50% of objective response. In women, finasteride has been used in some control trials for treatment of hirsutism with an objective favorable response. In conclusion, finasteride appears be useful for BPH, baldness and hirsutism (with caution) treatment. On the basis of experimental observations on distribution of 1 and 2 isoenzymes in human skin, scalp and prostate, the dual inhibitors should be more indicated for treatment of BPH and baldness. Similarly, the dual inhibitors seem indicated in attempting to prevent prostatic cancer. The pure 5alpha-reductase 1 inhibitors seem the ideal drugs for treatment of acne and hirsutism.
机译:5α-还原酶同工酶的抑制剂(1和2)可根据其底物特异性分为三类:a)5α-还原酶1的纯或优先抑制剂; b)5α-还原酶2的纯或优先抑制剂; c)双重抑制剂。尽管已经合成了几种甾体和非甾体抑制剂并在药理模型中进行了实验,但只有非那雄胺被广泛用于临床目的。非那雄胺在人类中的最大应用是人类良性前列腺增生症(BPH)。此外,非那雄胺最近已用于治疗男性脱发,客观反应率为50%。在女性中,非那雄胺已用于一些对照试验中,以客观有利的方式治疗多毛症。总之,非那雄胺似乎可用于BPH,秃发和多毛症(慎用)治疗。根据对人皮肤,头皮和前列腺中1和2种同工酶分布的实验观察,应更进一步指出使用双重抑制剂治疗BPH和脱发。类似地,双重抑制剂似乎在试图预防前列腺癌中被表明。纯5α-还原酶1抑制剂似乎是治疗痤疮和多毛症的理想药物。

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