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Drug Des Devel Ther. 2009 Feb 06;2:193-202. doi: 10.2147/dddt.s4146.

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

Drug design, development and therapy

Nathan W Kopper, Jennifer Gudeman, Daniel J Thompson

Affiliations

  1. KV Pharmaceutical, 2503 South Hanley Road, St. Louis, MO 63144, USA. [email protected]

PMID: 19920906 PMCID: PMC2761184 DOI: 10.2147/dddt.s4146

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.

Keywords: estradiol; hormone therapy; menopause; transdermal drug delivery; vasomotor symptoms

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