Article

The transdermal contraceptive patch: a new approach to hormonal contraception.

Department of Obstetrics and Gynecology, Baystate Medical Center, Springfield, Massachusetts, USA.
International journal of fertility and women's medicine (Impact Factor: 0.56). 01/2002; 47(2):69-76.
Source: PubMed

ABSTRACT The transdermal contraceptive patch delivers ethinyl estradiol and norelgestromin (17-deacetylnorgestimate) at a rate over seven days that results in efficacy paralleling that achieved with oral contraceptives. Due to the pharmacokinetics of the system, adequate steroid levels are maintained for two days beyond the recommended duration of use of an individual patch, with resulting maintenance of efficacy. With perfect use, the failure rate is 0.70 pregnancies per 100 woman-years and for typical use, the rate is 0.88 pregnancies per 100 woman-years. Body weight above 90 kilograms (198 pounds) is associated with lower efficacy. Cycle control is similar to that achieved by oral contraceptives. With the exception of a transient increase in breast tenderness, the side effect profile is similar to that noted by oral contraceptive users. A major advantage of this method compared to oral contraceptives is a nearly 90% perfect adherence to the dosing schedule across all age groups. Partial or total detachment of the patch occurs at an overall rate of 3.8%. This rate is not affected by warm humid climates, vigorous exercise, or exposure to saunas or water baths.

0 Followers
 · 
142 Views
  • [Show abstract] [Hide abstract]
    ABSTRACT: Many contraceptive methods have been developed for fertility regulation, either reversible or irreversible, in males and females. Oral contraceptives have been considered the most popular form of reversible contraception. However, they must be taken consistently, on a daily basis for 21 or 28 days of each menstrual cycle, in order to achieve the maximal outcomes of contraception. Moreover, their contraceptive efficacy has been reportedly affected by their interactions with many drug products taken concurrently for other conditions. To resolve the dilemma of daily compliance and the risk of potential interactions with drugs taken orally, several non-traditional delivery systems have been developed to permit contraceptive agents and their combinations to be administered via a non-oral route, and also at a lesser frequency of administration, so as to enhance treatment compliance, maximize therapeutic outcomes, and minimize adverse effects. One typical example is the successful development of the ethinylestradiol/norelgestromin patch for achieving contraception in females via transdermal delivery. With topical application on intact skin, each patch delivers a combination of norelgestromin and ethinylestradiol for a week. With a treatment schedule of 3 weeks with a patch on and 1 week without a patch for each menstrual cycle, the ethinylestradiol/norelgestromin patch has achieved a clinical efficacy that is considered bioequivalent to oral contraceptives (with an unintended pregnancy rate of 0.8% per woman-year for the patch versus 0.1% per woman-year for the combined oral contraceptive).Stimulated by the marketing success of the ethinylestradiol/norelgestromin transdermal contraceptive patch, and a growing recognition of the therapeutic benefits realized by delivering an orally inactive progestin via a transdermal route, other transdermal drug delivery systems (DDS), such as transdermal gels and a metered-dose transdermal spray system, have also been developed. Further transdermal contraceptive patches have also been developed. One of these is similar to the ethinylestradiol/norelgestromin patch, in that it is fabricated from an adhesive polymer matrix diffusion-controlled DDS; however, it has a two times smaller patch size (to minimize localized reactions at the application site). This was made possible by substituting norelgestromin with a more potent progestin called gestodene, that has a higher skin permeation rate. The other transdermal patch that has been developed employs a microreservoir partition-controlled delivery system, to provide dual-controlled delivery of estradiol (a natural estrogen) and levonorgestrel (another potent synthetic progestin) at constant rates (zero-order kinetics). Clinical studies have demonstrated that these two new patch systems may be attractive alternative forms of contraception, since ovulation inhibition has been achieved in all subjects who wear the transdermal patch for 3 weeks, replacing it on a weekly basis.A transdermal gel has been formulated to contain elcometrine, which has a progestational potency that is 100 times that of progesterone but is orally inactive, in an alcoholic solution. Preliminary clinical studies have indicated that suppression of ovulation was achieved in the majority of subjects receiving daily application of the transdermal gel. To address the problems associated with the dosing accuracy of the transdermal gel, due to difficulty controlling the area and size of the application site, the feasibility of delivering the transdermal gel from a metered-dose transdermal spray system is currently under evaluation by the Population Council.
    American Journal of Drug Delivery 12/2005; 4(4):201-213.
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: The range of contraceptive options and consumer awareness of new contraceptive methods have both increased significantly over the past 10 years. New methods available in Australia include lower-dose oral contraceptive pills, new oral progestogens, progestogen implants, a progestogen-bearing intrauterine device and polyurethane female condoms. Contraceptive options which may soon be introduced in Australia include novel methods of administering combined (oestrogen-progestogen) contraception, such as dermal patches and vaginal rings.
    The Medical journal of Australia 07/2003; 178(12):616-20. · 3.79 Impact Factor
  • [Show abstract] [Hide abstract]
    ABSTRACT: Long-term efficacy and tolerability data are not yet available for patch formulations of dopamine agonists in restless legs syndrome. Efficacy and safety of rotigotine (0.5-4mg/24h), formulated as a once-daily transdermal system (patch), were investigated in an open extension (SP710) of a preceding 6-week placebo-controlled trial (SP709, 341 randomized patients) in patients with idiopathic restless legs syndrome. For efficacy assessment the international RLS severity scale (IRLS), the RLS-6 scales, the clinical global impressions (CGI) and the QoL-RLS questionnaire were administered. In addition, long-term tolerability and safety were assessed. Of 310 patients who finished the controlled trial, 295 (mean age 58+/-10 years, 66% females) with a mean IRLS score of 27.8+/-5.9 at baseline of SP709 were included. We report results after one year of this ongoing long-term trial. Two hundred twenty patients (retention rate=74.6%) completed the 12-month follow-up period. The mean daily dose was 2.8+/-1.2mg/24h with 4mg/24h (40.6%) being the most frequently applied dose; 14.8% were sufficiently treated with 0.5 or 1.0mg/24h. The IRLS total score improved by ?17.4+/-9.9 points between baseline and end of Year 1 (p<0.001). The other measures of severity, sleep satisfaction and quality of life supported the efficacy of rotigotine (p<0.001 for pre-post-comparisons of all efficacy variables). The tolerability was described as "good" or "very good" by 80.3% of all patients. The most common adverse events were application site reactions (40.0%), which led to withdrawal in 13.2%. Further relatively frequent adverse events were nausea (9.5%) and fatigue (6.4%). Two drug-related serious adverse events, nausea and syncope, required hospitalization. Symptoms of augmentation were not reported by the patients. Rotigotine provided a stable, clinically relevant improvement in all efficacy measures throughout one year of maintenance therapy. The transdermal patch was safe and generally well tolerated by the majority of patients. Comparable to any transdermal therapy, application site reactions were the main treatment complication.
    Sleep Medicine 09/2008; 9(8):865-73. DOI:10.1016/j.sleep.2008.04.012 · 3.10 Impact Factor