Desogestrel, Norgestimate, and Gestodene: The Newer Progestins

@article{Kaplan1995DesogestrelNA,
  title={Desogestrel, Norgestimate, and Gestodene: The Newer Progestins},
  author={Barbara Kaplan},
  journal={Annals of Pharmacotherapy},
  year={1995},
  volume={29},
  pages={736 - 742}
}
  • B. Kaplan
  • Published 1 July 1995
  • Medicine
  • Annals of Pharmacotherapy
Objective: To review and compare the newer progestins desogestrel, norgestimate, and gestodene with regard to chemistry, pharmacokinetics, efficacy, and tolerability. Data Sources: Primary literature on desogestrel, norgestimate, and gestodene was identified from a comprehensive MEDLINE English-literature search from 1984 through 1994, with additional studies selected by review of the references. Indexing terms included progestins, desogestrel, gestodene, norgestimate, levonorgestrel, and… 
Uniqueness of oral contraceptive progestins.
TLDR
The current, informal method for classifying oral contraceptives as old, first generation, or second generation on the basis of their date of introduction obscures the fact that each of the gonane progestins has unique biologic properties.
Hormonelle Antiandrogene in der Aknetherapie
TLDR
F females with acne tarda, persistent acne recalcitrant to treatment, with parallel wish of contraception, and as a requirement for a systemic isotretinoin treatment can be treated with hormonal antiandrogen treatment, but this is not a primary monotherapy for uncomplicated acne.
Triphasic oral contraceptives: review and comparison of various regimens.
  • M. Cedars
  • Medicine
    Fertility and sterility
  • 2002
TLDR
Both triphasics and monophasics have minimal effects on carbohydrate and lipid metabolism and hemostasis parameters, and therefore comparable low risks of coronary heart disease.
Clinical profile of contraceptive progestins
  • G. Benagiano, F. Primiero, M. Farris
  • Medicine
    The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception
  • 2004
TLDR
It has been amply proven that - even when administered in doses that do not constantly inhibit ovulation - a progestin can still remain effective as a contraceptive by acting at the level of the cervical mucus and, at least in part, of the endometrium.
A comparative study of the effects of gestodene 60 microg/ethinylestradiol 15 microg and desogestrel 150 microg/ethinylestradiol 20 microg on hemostatic balance, blood lipid levels and carbohydrate metabolism.
TLDR
The 24-day GTD 60 microg/EE 15 microg formulation and DSG/EE produced similar effects on hemostatic balance, lipid metabolism and glucose tolerance, and exhibited comparable efficacy and tolerability.
Pharmacokinetics of an oral contraceptive containing oestradiol valerate and dienogest
TLDR
Treatment with an OC containing E2V and DNG was well tolerated and was associated with stable E2 concentrations over 28 days, and the pharmacokinetics of DNG were consistent with previous findings.
Investigation of the Hemostatic Effect of a Transdermal Patch Containing 0.55 mg Ethinyl Estradiol and 2.1 mg Gestodene Compared with a Monophasic Oral Contraceptive Containing 0.03 mg Ethinyl Estradiol and 0.15 mg Levonorgestrel: An Open-Label, Randomized, Crossover Study
TLDR
A COC containing 0.03 mg EE and 0.15 mg levonorgestrel and the novel Bayer patch have comparable influence on hemostatic endpoints, and both treatments were well-tolerated by subjects.
[Treatment of acne with antiandrogens--an evidence-based review].
  • C. Zouboulis
  • Medicine
    Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG
  • 2003
TLDR
Antiandrogen treatment should be limited to female patients with additional signs of peripheral hyperandrogenism or hyper androgenemia, and Gestagens or estrogens as monotherapy, spironolactone, flutamide, gonadotropin-releasing hormone agonists, and inhibitors of peripheral androgen metabolism cannot be endorsed based on current knowledge.
Berberine and Monacolin Effects on the Cardiovascular Risk Profile of Women with Oestroprogestin-Induced Hypercholesterolemia
TLDR
It appears that the tested combined lipid-lowering nutraceutical is able to equally improve lipid metabolism in oral contraceptive induced hypercholesterolemia in women affected or not by PCOS.
Pharmacokinetic Drug Interactions Between Oral Contraceptives and Second-Generation Anticonvulsants
TLDR
On the basis of available study data in women receiving concomitant OC preparations, gabapentin, lamotrigine, tiagabine and vigabatrin may be administered without significant pharmacokinetic interactions that potentially diminish contraceptive efficacy.
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TLDR
The new formulations were found to be comparable in efficacy to each other and to established agents and appeared to be less androgenic than current OCs and to have less impact on carbohydrate and lipoprotein metabolism.
Pharmacokinetics of desogestrel.
TLDR
3-keto-desogestrel has a lower affinity for sex hormone-binding globulin, which results in markedly lower plasma levels after administration, and is generally comparable with those of levonorgestrel and norethindrone.
New progestins—Clinical experiences: Gestodene
TLDR
Gestodene, one of three new gonane progestins, is the most potent on a per weight basis in regard to progestational effects and has little or no estrogenic effect, and consequently is a competitive aldosterone inhibitor, leading to speculation that it may be beneficial in hypertensive patients.
Progestational and androgenic receptor binding affinities and in vivo activities of norgestimate and other progestins.
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Evidence of the selectivity of norgestimate based on minimal androgenicity is provided, indicating an improvement over other progestins used in oral contraceptives.
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TLDR
Serum concentrations of gestagens were compared after single doses and after multiple doses (steady-state conditions) of four widely used oral contraceptives containing norethisterone, levonorgestrel, desogestrel and gestodene to suggest that the concentrations of unbound gestagen in serum are similar but may be higher for NET whose half-life of elimination is about half that of the other three gestagen.
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TLDR
The safety and efficacy of the triphasic oral contraceptive agent containing norgestimate and ethinyl estradiol were evaluated in a 12‐month study of 661 women and the incidence of dysmenorrhea and premenstrual syndrome was sharply reduced.
Clinical and hormonal effects of two contraceptives: correlation to serum concentrations of levonorgestrel and gestodene.
TLDR
Serum levels of FSH, LH, estradiol and progesterone were all depressed with both preparations, and depression was more marked in the GES group, despite lower progestogen ingestion and similar serum concentrations.
Pharmacokinetics and serum protein binding of gestodene and 3-keto-desogestrel in women after single oral administration of two different contraceptive formulations.
TLDR
Two low-dose oral contraceptives, both containing the same dose of ethinyl estradiol but different progestins--gestodene and desogestrel--were administered to 18 women in a single dose, cross-over study, finding GEST was mainly bound to SHBG, while KDG was predominantly bound to albumin.
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TLDR
Multicentric clinical trials with a combination of only 75 mcg gestoden combined with 30 mcg EE confirm a reliable contraceptive efficacy combined with excellent cycle control and tolerance in 1,095 women over 14,281 treatment cycles.
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TLDR
The higher EE levels with EE/GSD as compared to EE/DG seem to be due to a retardation of the inactivation and elimination of EE caused by the progestogen component, and the rise in the EE levels during each cycle seems to be a reduction in the oxidative metabolism by EE itself.
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