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Dopamine agonists, anti-progestins, anti-androgens, long-term-release GnRH agonists and anti-estrogens in canine reproduction: a review

机译:多巴胺激动剂,抗孕激素,抗雄激素,长期释放的GnRH激动剂和抗雌激素在犬繁殖中的应用

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Over the last 10 years, new drugs have been applied to canine reproduction, widening the spectrum of therapeutic possibilities for diseases that were previously surgically treated, and facilitating better control of the estrous cycle and fertility. Some are not approved for use in dogs; their use is experimental and further clinical trials are necessary. Dopamine agonists such as cabergoline, bromocriptine or metergoline are ergoderivative alkaloids that exert an anti-prolactinergic effect via stimulation of D2 pituitary receptors or inhibition of central serotoninergic ones. Their main indication is suppression of lactation. Anti-prolactinergic compounds have also been successfully used for pregnancy termination and shortening of interestrous intervals. Anti-progestins, (e.g. mifepristone and aglepristone) are synthetic steroids that bind with high affinity to progesterone (P4) receptors, preventing P4 from exerting its biological effects. Anti-progestins have been indicated in P4-dependent conditions, such as pregnancy termination, induction of parturition and the medical treatment of pyometra. Several groups of drugs have been described to have anti-androgenic properties through different mechanisms of action: progestins, receptor binding anti-androgens (e.g. flutamide), competitive enzyme inhibitors (e.g. finasteride), aromatase inhibitors, and GnRH agonists. Their main application is medical treatment of benign prostatic hyperplasia. Long-term release formulations of GnRH agonists (e.g. leuprolide or deslorelin acetate) postponed puberty and reversibly suppressed reproductive function in male and female dogs for periods exceeding 1 year. Anti-estrogens (e.g. clomiphene and tamoxifen citrate) are synthetic non-steroidal type I anti-estrogenic compounds that competitively block estrogen receptors with a combined antagonist-agonistic effect. In dogs, their action is more agonistic than antagonistic.
机译:在过去的十年中,新药已用于犬类繁殖,拓宽了以前通过外科手术治疗的疾病的治疗可能性范围,并有助于更好地控制发情周期和生育能力。有些不被允许在狗中使用。它们的使用是实验性的,需要进一步的临床试验。多巴胺激动剂,如卡麦角林,溴隐亭或美特古林是麦角生物碱,通过刺激D2垂体受体或抑制中枢5-羟色胺能发挥抗催乳激素作用。它们的主要指征是抑制泌乳。抗催乳激素化合物也已成功用于终止妊娠和缩短间隔时间。抗孕激素(例如米非司酮和阿格列酮)是合成类固醇,与孕激素(P4)受体具有高亲和力,可阻止P4发挥其生物学作用。抗孕激素已在P4依赖的疾病中显示出来,例如终止妊娠,分娩诱导和脓疱病的药物治疗。已经描述了几类通过不同作用机理具有抗雄激素特性的药物:孕激素,结合受体的抗雄激素(例如氟他胺),竞争性酶抑制剂(例如非那雄胺),芳香酶抑制剂和GnRH激动剂。它们的主要应用是良性前列腺增生的医学治疗。 GnRH激动剂的长期释放制剂(例如亮丙瑞林或醋酸去甲肾上腺素)可延缓青春期并可逆地抑制雄性和雌性狗的生殖功能超过1年。抗雌激素(例如克罗米芬和柠檬酸他莫昔芬)是合成的非类固醇I型抗雌激素化合物,可竞争性阻断雌激素受体并具有拮抗拮抗作用。在狗中,它们的作用比拮抗作用更激动。

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