A comparison of a new graduated formulation with three constant-dosed oral contraceptives

Appel, Theodore B.; Arman, Kambi A.; Birdsall, C.K.; Christenson, David A.; Clark, Douglas O.; DeKoning, Joel R.; Dreisbach, Leonard A.; Frost, John F.; Gustin, Alan E.; Halikis, Michael; Hart, Thomas J.; Hlayackek, James H.; Hoffpauir, Norris S.; Hubbell, William S.; Kangayappan, Sivakami; Kuk, Dennis S.; Lackey, O. Monty; Lesko, Clarence A.; Levision, Judy; Levitan, Dean B.; Lucca, Paul A.; Maxymiv, George W.; McWhorter, James R.; Melton, Russell W.; Minard, William D.; Polich, Joseph J.; Ries, T.; Stewart, Stephen K.; Thornton, Thomas L.; White, William R.

doi:10.1016/s0010-7824(87)80013-6

Cited by 19 publications

(5 citation statements)

References 17 publications

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“…Twenty years ago, 50 pg EE had been regarded as the minimal dose, while in modern pills, 30 pg have been suggested as the lowest acceptable dosage. Indeed, a combination of 20 gg EE and 1 mg norethisterone caused a relatively high rate of irregular bleedings [6], There is, however, considerable evidence that the type and dose of the progestogen component is the critical factor [7,8], The experience with a new for mulation containing 20 gg EE and 150 gg desogestrel actually demonstrated that the cycle control is not differ ent from that during treatment with a combination con taining 30 gg EE and 150 gg desogestrel (DG) [9][10][11][12][13]. The present report describes the results of two compara tive studies on the pharmacokinetics and some pharma codynamic parameters of two oral contraceptives con taining 150 gg DG and 20 or 30 gg EE.…”

Section: Introductionmentioning

confidence: 99%

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: Introductionmentioning

confidence: 99%

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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“…9 -12 Due to characteristics of their classes, levonorgestrel and norethindrone acetate have distinct biochemical differences: levonorgestrel has higher bioavailability, a longer serum half-life, and a higher relative binding affinity in humans. [13][14][15][16][17] The primary hypothesis of this study was that characteristics of individual progestins, or estrogen dose, may influence the breakthrough bleeding rates with continuously dosed OCs. The ethinyl estradiol (E2) dose may also influence cycle control by counterbalancing the progestin component and stabilizing the endometrium.…”

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confidence: 99%

Continuous Oral Contraceptives

Edelman

Koontz

Nichols

et al. 2006

Obstetrics & Gynecology

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“…At first, they were not widely used, as clinicians worried that there would be more breakthrough bleeding as a result of the lower estrogen dose. However, it soon became clear that this was not the case for doses of 30–35 μg ethinylestradiol, although there is some evidence of more breakthrough bleeding with oral contraceptives containing 20 μg ethinylestradiol (1, 3). The doses of progestins also fell from typical doses of up to 10 mg in the original first‐generation combined oral contraceptives to <1 mg by the late 1980s as it became clear that the same contraceptive efficacy was achieved, but with fewer unwanted progestogenic effects such as acne and weight gain (102, 103).…”

Section: Three Generations a Pill Scare And Legal Wranglingsmentioning

confidence: 99%

Oral contraceptives and the periodontium

Preshaw¹

2012

Periodontology 2000

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Oral contraceptives are a safe and effective means of contraception for millions of women worldwide. The first formulations of these drugs contained much higher doses of estrogens and progestins than those available today, and these were associated with an unacceptably high rate of unwanted effects including serious cardiovascular events. In addition, a number of case reports and clinical studies suggested that use of the first generation oral contraceptives was also associated with an increased risk for gingival and/or periodontal disease. Unfortunately, many of these early studies suffered from significant methodological flaws which throw their findings into question. Nonetheless, these studies provided the basis for a perception among the dental profession that oral contraceptives increase the risk for gingivitis and/or periodontitis. Realisation that the adverse events profile of oral contraceptives was dose dependant led to the development of the modern low dose formulations that are in use today. There have been far fewer studies to investigate whether modern oral contraceptives have any impact on the periodontium compared to studies of the early contraceptive formulations, but the quality of the more recent research is undoubtedly better. Following extensive review of the relevant literature and consideration of the historical perspective, the best available evidence strongly supports that oral contraceptives no longer place users at any increased risk for gingivitis or periodontitis. Oral contraceptives should not be viewed as a risk factor for gingival or periodontal disease.

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A comparison of a new graduated formulation with three constant-dosed oral contraceptives

Cited by 19 publications

References 17 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

Continuous Oral Contraceptives

Oral contraceptives and the periodontium

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A comparison of a new graduated formulation with three constant-dosed oral contraceptives

Cited by 19 publications

References 17 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

Continuous Oral Contraceptives

Oral contraceptives and the periodontium

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Product

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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