COMPARATIVE EFFECTS OF ETHINYL ESTRADIOL, 17α-Ethyl-19-Nortestosterone AND METHYLTESTOSTERONE ON THE PLASMA CLEARANCE OF INFUSED CORTISOL

Marks, Leon J.; Benjamin, G. Andrew H.; Duncan, Frederick J.; O'sullivan, James V. I.

doi:10.1210/jcem-21-7-826

Cited by 19 publications

(2 citation statements)

References 9 publications

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“…It was suggested that binding to CBG is respon sible for the increase in the cortisol levels during intake of oral contraceptives. On the other hand, an inhibition of hepatic metabolism of corticosteroids by contracep tive steroids seems to be involved in the rise of cortisol levels [37][38][39][40], The circadian rhythm of cortisol with a maximum at 6-8 h and a continuous decrease thereafter is maintained at a higher level during pill intake [41]. In the present study, there was no difference in the serum concentrations of cortisol at the time of intake (0 h) between both preparations, possibly due to the variation in the lime of blood sampling which was started between 8 and 10 h. The steep fall in the cortisol levels thereafter ( fig.…”

Section: Discussionmentioning

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: Discussionmentioning

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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“…Thus testosterone and its esters, which are not hepatotoxic (Foss & Simpson, 1959), lower urinary corticoid excretion (Venning & Browne, 1947;Bartter, Forbes, Jefferies, Carroll & Albright, 1949) and inhibit the normal rise in 17-OHCS caused by surgical stress but not that caused by ACTH (Gemzell & Notter, 1956). Methyltestosterone also has been shown to decrease urinary steroid excretion (Reifenstein, Forbes, Albright, Donaldson & Carroll, 1945;Venning & Browne, 1947;Bartter et al 1949) but, although this drug is known to affect hepatic function and occasionally causes jaundice (Foss & Simpson, 1959), it does not prolong the half-hfe of infused cortisol (Marks, Benjamin, Duncan & O'Sullivan, 1961). The finding that methandienone reduced urinary steroid excretion while lowering the plasma levels of cortisol and corticosterone in two patients with Cushing's syndrome in the present study is 219 difficult to explain on a hepatic basis and was considered to indicate a direct hypo¬ thalamic or pituitary inhibitory effect.…”

Section: Discussionmentioning

confidence: 99%

Effect of an Anabolic Steroid (Methandienone) on the Metabolism of Cortisol in the Human

James¹,

Landon²,

Wynn³

1962

Journal of Endocrinology

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Possible mechanisms whereby the anabolic steroid methandienone lowers the urinary excretion of 17-KS and 17-OHCS have been studied in eight patients. Administration of the drug was associated with a delayed catabolism of infused cortisol and of endogenous cortisol, and a fall in cortisol production rate. In several patients, treatment was accompanied by a rise in certain serum enzyme levels and abnormal bromsulpthalein retention, but in others, these liver function tests were unaffected. Methandienone may thus inhibit the hepatic detoxification of cortisol without necessarily inducing changes in conventional liver function tests. The suppression of adrenocortical secretion was considered to be in part secondary to the effect of delayed cortisol catabolism, but evidence is also given suggesting a direct effect of the drug on the hypothalamus or pituitary, inhibiting the production or release of ACTH.

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Interactions between Androgenic-Anabolic Steroids and Glucocorticoids

Linet

1970

Progress in Drug Research / Fortschritte Der Arzneimittelforschung / Progrès Des Recherches Pharmaceutiques

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COMPARATIVE EFFECTS OF ETHINYL ESTRADIOL, 17α-Ethyl-19-Nortestosterone AND METHYLTESTOSTERONE ON THE PLASMA CLEARANCE OF INFUSED CORTISOL

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

Effect of an Anabolic Steroid (Methandienone) on the Metabolism of Cortisol in the Human

Interactions between Androgenic-Anabolic Steroids and Glucocorticoids

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COMPARATIVE EFFECTS OF ETHINYL ESTRADIOL, 17α-Ethyl-19-Nortestosterone AND METHYLTESTOSTERONE ON THE PLASMA CLEARANCE OF INFUSED CORTISOL

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

Effect of an Anabolic Steroid (Methandienone) on the Metabolism of Cortisol in the Human

Interactions between Androgenic-Anabolic Steroids and Glucocorticoids

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Product

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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