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Transdermal hormone therapy in postmenopausal women: A review of metabolic effects and drug delivery technologies

机译:绝经后妇女的经皮激素治疗:代谢作用和药物递送技术的综述

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Abstract: Vasomotor symptoms (VMS) associated with menopause can cause significant discomfort and decrease the quality of life for women in the peri-menopausal and post-menopausal stages of life. Hormone therapy (HT) is the mainstay of treatment for menopausal symptoms and is currently the only therapy proven effective for VMS. Numerous HT options are available to treat VMS, including estrogen-only and estrogen-progestogen combination products to meet the needs of both hysterectomized and nonhysterectomized women. In addition to selecting an appropriate estrogen or estrogen-progestogen combination, consideration should be given to the route of administration to best suit the needs of the patient. Delivery systems for hormone therapy include oral tablets, transdermal patches, transdermal topical (nonpatch) products, and intravaginal preparations. Oral is currently the most commonly utilized route of administration in the United States. However, evidence suggests that oral delivery may lead to some undesirable physiologic effects caused by significant gut and hepatic metabolism. Transdermal drug delivery may mitigate some of these effects by avoiding gut and hepatic first-pass metabolism. Advantages of transdermal delivery include the ability to administer unmetabolized estradiol directly to the blood stream, administration of lower doses compared to oral products, and minimal stimulation of hepatic protein production. Several estradiol transdermal delivery technologies are available, including various types of patches, topical gels, and a transdermal spray.
机译:摘要:与绝经有关的血管舒缩症状(VMS)可能导致绝经前后和绝经后妇女的严重不适并降低其生活质量。激素疗法(HT)是更年期症状的主要治疗手段,目前是唯一被证明对VMS有效的疗法。可以使用多种HT治疗VMS,包括仅使用雌激素和结合雌激素-孕激素的产品,以满足子宫切除和非子宫切除妇女的需求。除了选择合适的雌激素或雌激素-孕激素组合外,还应考虑最适合患者需求的给药途径。激素治疗的递送系统包括口服片剂,透皮贴剂,透皮局部(非贴剂)产品和阴道内制剂。口服是目前美国最常用的给药途径。但是,有证据表明,口服给药可能会由于明显的肠道和肝脏代谢而导致某些不良的生理影响。透皮给药可以避免肠道和肝脏的首过代谢,从而减轻某些影响。透皮递送的优点包括将未代谢的雌二醇直接施用到血流中的能力,与口服产品相比施用更低剂量的剂量以及对肝蛋白产生的最小刺激。现有几种雌二醇透皮递送技术,包括各种类型的贴剂,局部用凝胶剂和透皮喷雾剂。

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