Estrogeni i gestageni u transdermalnim terapijskim sustavima

Professional paper - Review paper

• Author: Zrinka Rajić
• Author's institution: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of medicinal chemistry)
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract (english)

Estrogen replacement therapy is effective in relieving typical postmenopausal symptoms; it prevents osteoporosis and reduces the risk of cardiovascular diseases. Various delivery forms and routes of administration of estradiol are currently available, but transdermal delivery is getting increasingly popular. It bypasses the hepatic first-pass metabolism,
eliminates poor absorption during gastrointestinal disturbances, minimizes the potential of drug interactions and allows delivery of constant levels ofhormones.
Transdermal delivery systems (TDS) enable fast hormone release in blood circulation.
There are two different TDS - the transdermal reservoir patch and matrix patch. The
transdermal matrix system may be preferable because its use is associated with a lower
incidence of side effects, more stabile plasma estrogen concentrations, delivery of consistent therapeutic serum levels of estradiol and better bioavailability. Results obtained by
comparing several matrix systems show that different TDS with the same declared
amount of hormones released in bio od circulation do not have equal bioavailability and
pharmacokinetic profile. Comparison is made of absorption and bioavailability of estradiol between TDS and different therapeutic forms, i.e. gel. Pharmacokinetic profiles of
estradiol are different, but bioavailability and Cmax do not differ significantly. There is a
big difference in cmin (lower for TDS). Fluctuations in plasma concentrations are therefore higher for TDS.
TDS is also used as a contraceptive. Dosing schedule is simple to follow, user-controlled, and easily reversed. Comparison is made between 3 contraceptive methods: combined oral contraceptive, TDS and vagina! ring. Individua! serum levels with combined
oral contraceptive showed the highest variability as a result of its dosing regimen and
exposure to ethinylestradiol was the highest. Vaginal administration ofhormones affords
much lower, more stable and far more precise dosing than either the transdermal or oral routes.

• Keywords (croatian): estrogeni; gestageni; transdermalni terapijski sustavi; adhezivni flasteri
• Language: croatian
• Publication type: Professional paper - Review paper
• Publication status: Published
• Peer review: Peer review - domestic
• Publication version: Published version
• Journal title: Farmaceutski glasnik
• Numbering: vol. 63, no. 9, pp. 505-517
• p-ISSN: 0014-8202
• URN:NBN: urn:nbn:hr:163:333254
• Publication: 2007
• Type of resource: Text
• Access conditions: Open access
• Created on: 2020-11-20 09:29:19