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Combined methods
Published in Suzanne Everett, Handbook of Contraception and Sexual Health, 2020
Evra releases 150 micrograms of norelgestromin and 20 micrograms of ethinylestradiol per 24 hours; norelgestromin is the primary active metabolite of norgestimate (the progestogen contained in the combined pill Cilest). Evra is a transdermal patch which lasts seven days. A patch is used for three weeks, changed each week with a new patch and followed by a hormone-free interval of seven days in the fourth week where a withdrawal bleed occurs. Evra prevents pregnancy by inhibiting ovulation, altering cervical mucus so that it is impenetrable to sperm and by making the endometrium unfavourable to implantation.
Dermal and Transdermal Drug Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Kenneth A. Walters, Majella E. Lane
The introduction of a hormonal patch for female contraception was seen as a significant advance in the avoidance of unwanted pregnancies, especially in younger women where there was a risk of missing the daily oral dose (Graziottin, 2008). Ortho-Evra® is a combination transdermal contraceptive patch containing 6 mg norelgestromin and 0.75 mg ethinyl estradiol. The patch is a 20 cm2 drug-in-adhesive matrix with a standard backing membrane of polyethylene and polyester. The adhesive is polyisobutylene/polybutene and this carries the two active ingredients together with crospovidone and lauryl lactate, the adhesive layer being protected during storage by a release liner of polyethylene terephthalate with a polydimethylsiloxane coating. The patch is designed to deliver 150 µg norelgestromin and 20 µg ethinyl estradiol daily and is applied to the buttocks, lower abdomen, upper torso (excluding breasts) or the upper arm on the first day of menstruation and left in place for a week. The patch is removed and replaced with a new patch on a weekly basis for a further two weeks. The fourth week is patch free.
Contraception
Published in James M. Rippe, Lifestyle Medicine, 2019
The Ortho Evra patch, or Xulan, is a 4.5 cm2, three-layer system, with an outer protective, water-resistant layer, a middle medicated adhesive layer, and a clear release liner inner layer, which is removed at the time of patch application. Each patch delivers a total of 20 mg of EE and 150 mcg of norelgestromin, the primary metabolite of norgestimate.17 This results in a sustained release of hormonal contraception over several days, thereby avoiding peak and trough hormone levels and the need for daily administration. The patch is applied once a week for three weeks in a different discrete location, followed by a patch-free week during which menses occurs. The patch is more forgiving of dosing errors than pills. Even if a scheduled patch change is missed for two days during weeks two and three of a four-week cycle, clinical efficacy is maintained, and backup contraception is not needed.18
Effects of progestin-only contraceptives on the endometrium
Published in Expert Review of Clinical Pharmacology, 2020
Carlo Bastianelli, Manuela Farris, Vincenzina Bruni, Elena Rosato, Ivo Brosens, Giuseppe Benagiano
Their starting point was an investigation of decidual cell regulation of hemostasis at the time of menstruation, leading to the transformation of the local hemostatic environment into a hemorrhage-promoting milieu [22]. Within this context, enhanced expression of matrix metalloproteinase (MMP) 1 evoked by steroid withdrawal, would mediate endometrial extra-cellular matrix (ECM) degradation, leading to sloughing of its superficial layer at menstruation [23]. Indeed, back in 2000, Galant et al. [24] came-up with the hypothesis that MMPs initiate bleeding episodes. However, it was later shown, at least in vitro and using Ishikawa endometrial cancer cells, that MMP expression is not regulated by 2 of the third-generation progestins: norgestimate (NGS) and its 17-deacetylated derivative, norelgestromin (NGM) [25].
Effects of anatomical location on in vivo percutaneous penetration in man
Published in Cutaneous and Ocular Toxicology, 2020
Jordan L. Bormann, Howard I. Maibach
A contraceptive patch containing ethinyl oestradiol and gestodene was tested at three location sites: upper outer arm, buttocks, and abdomen. There was no significant difference in percutaneous absorption at any of the sites (Table 8)37. Stanczyk et al.38 found less absorption at the abdomen compared to back and buttocks of a low-dose ethinyl oestradiol patch (Table 8). However, therapeutically, all three patch application sites were similar. Abrams et al.22 collected absorption data on a patch containing ethinyl oestradiol and norelgestromin also showing decreased absorption of both hormones, yet still within therapeutic range (Table 8). Yet another study regarding 17-B-oestradiol absorption showed 88% of the AUC0-last for an abdominal patch location compared to the buttock (Table 8)39.
Migraine, hormones and the menopausal transition
Published in Climacteric, 2018
M. A. Hipolito Rodrigues, L. Maitrot-Mantelet, G. Plu-Bureau, A. Gompel
Although studies showed conflicting results – worsening, improving or having no effect on headache in COC use, correct usage of COCs can prevent or reduce some kinds of migraine such as estrogen withdrawal headache39. In a large, population-based, cross-sectional study, Aegidius and colleagues40 observed a mildly increased prevalence of migraine among former users of COCs (OR 1.2, 95% CI 1.1–1.3) and current users. There was no significant relation between frequency of headache and oral contraceptive use. The prevalence increased only in those who used pills containing estrogen, were current users and without a relationship between the dosage of estrogen and occurrence of headache. It is important to highlight that estrogen doses used in COCs were between 30 and 50 µg. Progestin-only contraceptives were not linked to increased prevalence of headache40. La Guardia and colleagues41 observed that the mean number of headache days per week was higher in the extended group (84 days) compared with the cyclic group (28 days) during the patch-on weeks with ethinylestradiol 20 µg + norelgestromin 150 µg, but both regimens resulted in a linear decrease over time in headache frequency. More important, in most women, the extended use of a transdermal regimen of contraception delayed menses and reduced the mean number of headache days during the hormone-free interval (p < 0.0001). Similarly, Sulak and colleagues42, extending the COC regimen (168 days with 30 µg ethinylestradiol +3 mg drospirenone), observed a decrease in headache severity (p < 0.001), daily headache scores (p < 0.05) and improvement of working productivity, one of the serious problems of absences from work in migraineur women. Nappi and colleagues43, in a prospective pilot study with 32 women with MRM, administered estradiol valerate and dienogest with 2 hormone-free days. They noticed a significantly reduced number of migraine attacks (p < 0.001), duration (p < 0.001) and severity of head pain (p < 0.001) at the sixth cycle. And more, a significant reduction in number of analgesics used was observed at the sixth cycle (p < 0.001).