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Desogestrel (DSG) is a third-generation 19-nortestosterone derivative progestogen. It is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP). Its principal metabolite (etonogestrel, ETN) is the only progestin used for intravaginal combined contraception and one of the most used for subdermal hormonal contraception.This is a review of the available data on the pharmacokinetics of DSG and ETN in hormonal contraception. The material included was searched and obtained via Medline, PubMed, and EMBASE up to July 2013 using the search terms 'pharmacokinetics, metabolism' in combination with 'desogestrel, etonogestrel, and progestins.'DSG and its metabolite ETN are very suitable molecules for use in hormonal contraception. For the oral use the molecule used is DSG, while for parenteral routes (intravaginal, subdermal) its metabolite ETN is the compound of choice. In both cases (oral and parenteral) the active molecule in the organism is the latter (ETN), due to the rapid in vivo metabolism of oral DSG. The contraceptive efficacy and tolerability of all the formulations present on the market (mono/multiphasic EE/DSG COCs, DSG POP, EE/ETN vaginal ring, ETN implant) are reassuring, permitting a long-term use. The estrogenic component increases the contraindications, forcing the prescription to the safer only-progestin preparations, DSG POP or ETN implant.

Editor,—We were pleased to see the publication on behalf of the UK Steering Group “Recommendations for the management of galactosaemia”.1 In particular, we were pleased to see the emphasis on the management of adult women and the prevention of osteoporosis. We have, however, some concerns about the advice on the use of Loestrin 20 (an oral contraceptive preparation containing 20 μg ethinyl oestradiol and a progestogen) for long term oestrogen replacement. None of the combined oral …

A 26-year-old woman who had been taking an oral contraceptive preparation for two years developed malignant hypertension. Investigation failed to elicit any renal or other cause for her hypertension, but control of blood pressure was obtained by withdrawal of the oral contraceptive agent and antihypertensive therapy. Subsequently, after withdrawal of therapy, the blood pressure remained near normal. The patient had a previous history of hypertension during pregnancy; she was also overweight.

Three oral contraceptive preparations were studied in 60 healthy women. This randomized, comparative, baseline controlled study was designed to investigate the effects of the preparations on plasma lipids and lipoproteins. The following formulations were studied: a monophasic preparation containing ethinylestradiol and desogestrel (M-DSG) and two triphasic formulations containing ethinylestradiol and gestodene or levonorgestrel respectively (T-GSD and T-LNG). These preparations were studied for six treatment cycles. Total cholesterol and apoprotein B did not change in any group. Low density lipoprotein (LDL) cholesterol was significantly decreased in the groups of women treated with M-DSG and T-GSD respectively. No changes were observed in the T-LNG group. With M-DSG, significant increases were observed in high-density lipoprotein (HDL) cholesterol and HDL3 cholesterol, whilst HDL2 cholesterol did not change. With both T-GSD and T-LNG, no changes were observed in HDL cholesterol, whilst a significant increase in HDL3 cholesterol together with a trend to decrease in HDL2 cholesterol were observed. Apolipoprotein AI increased with the following ranking M-DSG greater than T-GSD greater than T-LNG. The LDL/HDL cholesterol ratio significantly decreased with both M-DSG and T-GSD. In the T-LNG group there was no change in this ratio. Triglycerides increased to the same extent in all treatment groups. As far as concerns the risk of arterial diseases, these three oral contraceptive formulations mostly induced negligible and/or partly favorable changes in plasma lipids and lipoproteins; however, the lipoprotein pattern during M-DSG treatment resulted better than during T-GSD, and the latter turned out to be better than during T-LNG.3 oral contraceptive (OC) preparations were studied in 60 healthy women. This randomized, comparative, baseline controlled study was designed to investigate the effects of the preparations on plasma lipids and lipoproteins. The following formulations were studied: a monophasic preparation containing ethinyl estradiol and desogestrel (M-DSG) and 2 triphasic formulations containing ethinyl estradiol and gestodene or levonorgestrel respectively (T-GSD and T-LNG). These preparations were studied for 6 treatment cycles. Total cholesterol and apoprotein B did not change in any group. Low density lipoprotein (LDL) cholesterol was significantly decreased in the groups of women treated with M-DSG and T-GSD respectively. No changes were observed in the T-LNG group. With M-DSG, significant increases were observed in the high density lipoprotein (HDL) and HDL3 cholesterols, while HDL2 cholesterol did not change. With both T-GSD and T-LNG, no changes were observed in HDL3 cholesterol together with a trend to decrease in HDL2 cholesterol were observed. Apolipoprotein AI increased with the following ranking M-DSG T-GSD T-LNG. The LDL/HDL cholesterol ratio significantly decreased with both M-DSG and T-GSD. In the T-LNG group there was no change in this ratio. Triglycerides increased to the same extent in all treatment groups. As far as the risk of arterial diseases, these 3 OC formulations mostly induced negligible and/or partly favorable changes in plasma lipids and lipoproteins; however, the lipoprotein pattern during M-DSG treatment was better than during T-GSD, and the latter was better than during T-LNG.

To determine the comparative metabolic effects of ethinyl estradiol and norgestrel in oral contraceptive preparations 45 women were administered these steroids in differing combinations for 21 days after which plasma protein levels were determined from blood samples. 11 women received .05 mg ethinyl estradiol alone daily and 15 received .25 mg d-norgestrel with it daily; 9 women received .03 mg ethinyl estrodiol daily and 10 women received .25 mg of d-norgestrel with it daily. The presence of norgestrel was found to significantly reduce the increased plasma protein concentration that results from estrogen administration (p less than .001). No significant difference was found between the .03- and .05-mg ethinyl estradiol doses in their effects in plasma protein levels with or without the norgestrel.

To determine the effect of oral contraceptives on mitotic indices in the peripheral blood leucocyte cultures of mothers and their progeny 70 women who had previously taken various oral contraceptive preparations (Ovulen-21 Anovlar-21 Gynovlar-21 Norinyl-1 Conovid-E Lyndiol-1 and Minovlar-21) were studied. Blood samples were collected at time of delivery from the mother and newborn and the percentage of mitoses was calculated from examination of 500 cells from each subject. No significant difference was found between the mitotic indices in treated subjects and appropriate controls. Providing the hormonal constituents of these pills are still effective after discontinuation of use for up to 60 months it is concluded that oral contraceptives have no appreciable adverse effect on the mitotic activity of peripheral blood cells.