Clinical performance and endocrine profiles of contraceptive vaginal rings releasing 3-keto-desogestrel and ethinylestradiol

Apter, Dan; Cacciatore, Bruno; Stenman, Ulf‐Hǎkan; Alapiessa, U.; Assendorp, R.

doi:10.1016/0010-7824(90)90016-o

Cited by 19 publications

(4 citation statements)

References 9 publications

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“…There is, however, no evidence for an exclusive causality. On the contrary, the rapid rise in the KDG levels within 3 days after insertion of a vaginal ring releasing daily 15 pg EE and 75 pg KDG to a steady state, which is only reached after 12 days of oral intake of 30EE/DG [28], cannot be explained solely by binding to SHBG [32], Similarly, the higher steady-state concentrations of norcthisterone during the 6th cycle of treatment with 30 pg EE + 0.6 mg norethisterone as compared to the 1st treat ment cycle cannot be due to binding to SHBG, the levels of which were similar [22]. Moreover, an increase in the lcvonorgestrel levels has been observed during multiple intake of 30 pg EE + 150 pg levonorgestrel, although SHBG scrum concentrations remained unchanged [33].…”

Section: Discussionmentioning

confidence: 98%

Oral Contraceptives Containing 20 or 30 μg Ethinylestradiol and 150 μg Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Jung-Hoffmann

Fitzner²,

Kühl³

1991

Horm Res

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The serum concentrations of ethinylestradiol (EE) and 3-keto-desogestrel (KDG) were compared during treatment with a combination of 20 µg EE + 150 µg DG (20EE/DG) or of 30 µg EE + 150 µg DG (30EE/DG). During intake of both preparations, the peak levels and the areas under the curve (AUC) of EE increased significantly by approximately 100% between days 1 and 10. In the steady state, the maximal EE levels were 75 ± 34 pg/ml (20EE/DG) and 136 ± 55 pg/ml (30EE/DG), and the AUC were 464 ± 236 pg·h/ml and 840 ± 492 pg·h/ml. The KDG levels, which were identical with both preparations, increased between days 1 and 21 by approximately 300% up to values of 4.5 ± 1.6 ng/ml. There were large interindividual variations in the AUC of EE and KDG and no correlation between the levels of EE and KDG. On day 21 of intake of 30EE/DG, the serum concentrations of sex-hormone- and corticosteroid-binding globulin were higher by 16% and 12%, respectively than with 20EE/DG. Although the morning peak levels of cortisol did not differ, the decrease which occurred thereafter, according to the circadian rhythm, was slower with 30EE/DG. There was no relationship between the serum concentrations of EE and/or KDG and the occurrence of irregular bleedings, which was similar during treatment with both preparations. As most of the women who bled had bleedings both with 20EE/DG and 30EE/DG, an influence of predisposition can be assumed. It is concluded that the increase in the EE levels and partly of progestogen levels during multiple intake of the pill is probably caused by an inhibition of hepatic steroid metabolism by the contraceptive steroids.

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Section: Discussionmentioning

confidence: 98%

Oral Contraceptives Containing 20 or 30 μg Ethinylestradiol and 150 μg Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Jung-Hoffmann

Fitzner²,

Kühl³

1991

Horm Res

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“…(4B) [39]. When used as recommended (21 consecutive days followed by a week without the device) this formulation completely inhibits ovulation, thus permitting a good control of the menstrual cycle [40].…”

Section: Contraceptive Vaginal Ringmentioning

confidence: 99%

Is the Vagina an Adequate Route for the Administration of Hormonal Contraceptives?

Lete

Dueñas²,

Esplugues³

et al. 2010

CDM

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The vaginal route of drug administration provides women with a valid alternative to more conventional methods of contraception. Drugs absorbed in the upper part of the vagina can bypass the liver and, if metabolized, are subject to a reduced hepatic first-pass effect. Current vaginally-administered contraceptive formulations deliver similar doses of gestagens to those provided by oral methods but release lower amounts of oestrogens. This results in a systemic exposure to gestagens similar to that achieved via other routes, thereby maintaining contraceptive efficacy while limiting systemic, but not uterine, exposure to oestrogen. In this way, the probability of systemic oestrogen-related adverse effects are theoretically reduced without compromising cycle control. In addition, the fact that the effects of a contraceptive ring last a complete cycle makes it more user-friendly than other methods and results in better patient compliance. The present review will explain in detail the specificities of this route of delivery of hormonal contraception and will compare it to more classic forms of contraception received via the oral (pill), intramuscular (injected), transdermic (patch) and subcutaneous (implants) routes of administration.

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“…Apter et al 30 reported a dose-finding study of a 3-month cyclic-use core design CVR with an outer diameter of 60 mm and inner diameter of 55 mm containing varying doses of ethinyl estradiol and etonogestrel. They demonstrated a dose-response relationship between etonogestrel and ovulation suppression and bleeding patterns.…”

Section: Etonogestrel + Ethinyl Estradiolmentioning

confidence: 99%

Contraceptive Vaginal Rings

Harwood¹,

Mishell²

2001

Semin Reprod Med

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Contraceptive vaginal rings (CVRs) contain sex steroids that diffuse through a plastic polymer ring at a constant rate and are absorbed directly through the vaginal epithelium into the systemic circulation. This delivery system provides many advantages over oral contraceptives (OCs), including avoidance of the first-pass effect through the liver, constant serum steroid levels, longer duration of use, and greater bioavailability of the hormones. CVRs containing progestin only are designed for continuous use for 3 to 6 months. Those containing progesterone alone are indicated for use in women who are breastfeeding. Large clinical trials of progestin-containing CVRs demonstrated good efficacy and safety of the CVR, with continuation rates similar to that of OCs. CVRs containing a combination of estrogen and progestin are designed to be used for 1 to 12 months in a cyclic manner similar to OCs, with withdrawal bleeding in the fourth week of each cycle. In clinical trials these CVRs have typical use efficacies similar to OCs, with an acceptable pattern of bleeding.

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Clinical performance and endocrine profiles of contraceptive vaginal rings releasing 3-keto-desogestrel and ethinylestradiol

Cited by 19 publications

References 9 publications

Oral Contraceptives Containing 20 or 30 μg Ethinylestradiol and 150 μg Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Oral Contraceptives Containing 20 or 30 μg Ethinylestradiol and 150 μg Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Is the Vagina an Adequate Route for the Administration of Hormonal Contraceptives?

Contraceptive Vaginal Rings

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Clinical performance and endocrine profiles of contraceptive vaginal rings releasing 3-keto-desogestrel and ethinylestradiol

Cited by 19 publications

References 9 publications

Oral Contraceptives Containing 20 or 30 &mu;g Ethinylestradiol and 150 &mu;g Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Oral Contraceptives Containing 20 or 30 &mu;g Ethinylestradiol and 150 &mu;g Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Is the Vagina an Adequate Route for the Administration of Hormonal Contraceptives?

Contraceptive Vaginal Rings

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Product

Resources

About

Oral Contraceptives Containing 20 or 30 μg Ethinylestradiol and 150 μg Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters

Oral Contraceptives Containing 20 or 30 μg Ethinylestradiol and 150 μg Desogestrel: Pharmacokinetics and Pharmacodynamic Parameters