The pharmacological profile of dienogest

Oettel, M; Breitbarth, H; Elger, W.; Gräser, T; Hübler, D; Kaufmann, G.; Moore, C.; Patchev, Vladimir K.; Römer, Wolfgang; Schröder, Johann Michael; Sobek, Lothar; Zimmermann, H.

doi:10.3109/13625189909085259

Cited by 56 publications

(54 citation statements)

References 16 publications

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“…Also, it has been approved as a monotherapy for the treatment of this pathology in various countries [26]. Dienogest binds to the progesterone receptor with high specificity and produces a powerful progestogenic effect [41]. When administered continuously, it results in anti-ovulatory activity [42], inhibitory effects on cytokine production of endometriotic cells [43], a hypoestrogenic endocrine environment, and decidualization of endometrial tissue and consequent atrophy of the endometriotic lesions [26] without androgenic effects and with minimal changes in lipid and carbohydrate levels [44,45].…”

Section: Discussionmentioning

confidence: 99%

Oral contraceptives in the prevention of endometrioma recurrence: does the different progestins used make a difference?

Cucinella

Granese²,

Calagna

et al. 2013

Arch Gynecol Obstet

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Objective The primary aim of the study was to analyze the endometrioma recurrence rate in patients who underwent laparoscopic excision followed by postoperative longterm regimen of oral contraceptives (OCs). Materials and methods 168 patients who underwent a conservative laparoscopic surgery for endometrioma, during the period between September 2009 and August 2010 in three university hospitals were studied. A long-term OCs therapy was offered to all women following surgery. Patients were randomly divided into three groups according to different progestins used (desogestrel, gestodene, dienogest). Women who refused a postoperative hormonal therapy served as control. Follow-up visits and transvaginal scan were planned at 1, 3, 6, 12, and 24 months after surgery. All patients who showed an ultrasound persistence of the endometrioma at 1 month follow-up were excluded from clinical analysis.Results Of the 168 patients, 131 completed the 24 months follow-up. Endometrioma recurrence was found in 21 (12.5 %) of all patients, it was unilateral in 17 cases while bilateral in 4 cases. The rate of recurrent endometrioma was statistically significant in non-users compared to the long-term OCs treated patients. Conclusion The current data suggest the usefulness of long-term OCs regimen after conservative surgery for the prevention of ovarian endometrioma recurrence. As a statistical significant difference could not be observed between OCs groups, further study on the individual molecules is required in order to really understand the effect of each of them.

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Section: Discussionmentioning

confidence: 99%

Oral contraceptives in the prevention of endometrioma recurrence: does the different progestins used make a difference?

Cucinella

Granese²,

Calagna

et al. 2013

Arch Gynecol Obstet

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“…Estradiol valerate is considerably less potent than ethinylestradiol in terms of hepatic protein synthesis induction, as demonstrated in clinical studies assessing SHBG, angiotensinogen, and hemostatic parameters. [26][27][28][29] However, changes observed with COCs reflect not only influences of the estrogen component, but also those of the progestogen component; indeed, progestogen can affect the binding of testosterone or cortisol to transport proteins [33] and the clearance time from serum. [34] The findings of the current study are also consistent with those of a study that compared the Table III.…”

Section: Discussionmentioning

confidence: 99%

Hemostatic Effects of a Novel Estradiol-Based Oral Contraceptive

Klipping¹,

Duijkers²,

Parke

et al. 2011

Drugs R D

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Background: A novel estradiol-based combined oral contraceptive (COC) is currently available in many countries worldwide, including Europe and the US. Based on previous studies, it is expected that this estradiol-based COC will have a reduced hepatic effect compared with COCs containing ethinylestradiol with regard to proteins controlling the hemostatic balance. Objective: The aim of this study was to compare the hemostatic effects of the estradiol valerate/dienogest COC with a monophasic low-estrogen dose COC containing ethinylestradiol/levonorgestrel. Study Design: Healthy women aged 18-50 years were randomized to receive a COC containing estradiol valerate/dienogest (2 days estradiol valerate 3 mg, 5 days estradiol valerate 2 mg/dienogest 2 mg, 17 days estradiol valerate 2 mg/dienogest 3 mg, 2 days estradiol valerate 1 mg, 2 days placebo) or ethinylestradiol 0.03 mg/levonorgestrel 0.15 mg in a crossover study design. Women received each treatment for three cycles, with two washout cycles between treatments. The primary efficacy variables were the intra-individual absolute changes in prothrombin fragment 1 + 2 and D-dimer from baseline to cycle three. Results: Data from 29 women were assessed. Intra-individual absolute changes in prothrombin fragment 1 + 2 and D-dimer from baseline to cycle three were less pronounced with estradiol valerate/dienogest than with ethinylestradiol/ levonorgestrel. Conclusion: The novel COC containing estradiol valerate/dienogest had similar or less pronounced effects on hemostatic parameters than ethinylestradiol/levonorgestrel.

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“…Выраженный периферический гестагенный эффект диеногеста в составе КОК Силуэт об-условлен специфическим трансформирующим влиянием на эндометрий по сравнению с другими прогестагенами. Доказано антипролиферативное действие диеногеста в отношении эндометриоидных гетеротопий (оказывает прямое воздействие на подавление роста эндометриоид-ных имплантатов) [27][28][29][30], что важно при лечении хрони-ческой тазовой боли. КОК с диеногестом относятся к пре-паратам с низкими тромборисками, а доза эстрогенового компонента в 20 или 30 мкг не имеет существенного зна-чения для прогнозирования рисков тромбоза.…”

Section: кок прогестины и врвмтunclassified

Varicose veins of the small pelvis and pelvic congestion syndrome. A differentiated approach: the choice of method of contraception, treatment, prevention

Григоренко¹,

Гордийчук²

2017

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The article considers the main points that affect the quality of life of women with varicose veins of small pelvis with congestion and without it, in particular the use of hormonal methods of contraception, and also discussed the issues of diagnostics, prevention and treatment of these diseases. Algorithms of clinical tactics for conducting such patients are presented. Particular attention is focused on the features of the appointment of hormonal drugs in this category of women. You can determine the methods of treatment and avoid long-term unreasonable prescription of various medicine (especially hormones that will mask or worsen the course of the disease) if you select groups of women with varicose veins of the small pelvis without congestion and with it (reflux).Varicose veins of the small pelvis and pelvic congestion syndrome are conditions that require an interdisciplinary and differentiated approach. Symptoms of these conditions can be put on a mask of various gynecological, urological, traumatological diseases. Anatomical and physiological features of the structure of the veins and the regulation of their venous tone explain the possibility of forming a venous congestive syndrome in women. This can be due to two reasons: due to the violation of the outflow of venous blood or due to the obstruction of any vein of the ovary, any increase in intravascular pressure not controlled by the venous tone at the level of the pelvis.Varicose veins of the small pelvis and pelvic congestion syndrome remain unexplored until the end. There are no uniform standards for their diagnostics. Varicose veins of the small pelvis and pelvic congestion syndrome are different diseases which requiring an understanding of the mechanisms of their development and consequences. If a pelvic varicose veins are suspected, the first diagnostic test is usually ultrasound. Modern ultrasound technique can evaluate blood flow in various veins. To study the blood flow in the veins, laparoscopy, venography in combination with CT or MRI can also be performed.

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The pharmacological profile of dienogest

Cited by 56 publications

References 16 publications

Oral contraceptives in the prevention of endometrioma recurrence: does the different progestins used make a difference?

Oral contraceptives in the prevention of endometrioma recurrence: does the different progestins used make a difference?

Hemostatic Effects of a Novel Estradiol-Based Oral Contraceptive

Varicose veins of the small pelvis and pelvic congestion syndrome. A differentiated approach: the choice of method of contraception, treatment, prevention

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