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Clinical Obstetrics and Gynecology Dec 1995Desogestrel is a new, potent progestogen with very low androgenic properties. When used as a contraceptive, it is a strong antiovulatory compound, even at low doses. The... (Review)
Review
Desogestrel is a new, potent progestogen with very low androgenic properties. When used as a contraceptive, it is a strong antiovulatory compound, even at low doses. The clinical efficacy is as good as that of the old progestogens. It has a low incidence of side effects and complications, similar to other progestogens. It may have a role as an anti-androgen in women with hyperandrogenic symptoms in need of adequate oral contraception.
Topics: Clinical Trials as Topic; Contraceptives, Oral, Synthetic; Desogestrel; Female; Humans; Progesterone Congeners
PubMed: 8616978
DOI: 10.1097/00003081-199538040-00017 -
Drug and Therapeutics Bulletin Oct 2021
Topics: Contraceptives, Oral, Combined; Desogestrel; Female; Humans
PubMed: 34426511
DOI: 10.1136/dtb.2021.000049 -
The Annals of Pharmacotherapy 1995To review and compare the newer progestins desogestrel, norgestimate, and gestodene with regard to chemistry, pharmacokinetics, efficacy, and tolerability. (Comparative Study)
Comparative Study Review
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 norgestrel.
STUDY SELECTION
Only human clinical and pharmacokinetic trials performed in Europe, Canada, and the US were included.
DATA EXTRACTION
All available data from human studies were reviewed; both comparative and noncomparative studies were included because of the paucity of direct comparative information available.
DATA SYNTHESIS
The newer progestins were designed to minimize the adverse effects (e.g., acne, hirsuitism, nausea, carbohydrate and lipid metabolism changes) observed with older oral contraceptives (OCs) while maintaining efficacy and good menstrual cycle control. Desogestrel, norgestimate, and gestodene have minimal amounts of androgenicity and antiestrogenic potential. All of these agents are pharmacokinetically similar to older agents: they are highly bioavailable when administered orally, hepatically metabolized, and obtain steady-state concentrations after 8-10 days of continuous administration. The newer agents have similar Pearl Indexes and slightly better cycle control. Furthermore, the new progestins appear to cause fewer adverse effects, such as acne and hirsuitism, and similar rates of weight gain, blood pressure changes, and lipid and carbohydrate metabolism changes.
CONCLUSIONS
Desogestrel, norgestimate, and gestodene appear to offer clinical advantages because of their decreased androgenicity. Women whose cycles are currently well controlled with other OCs should not be switched to a newer progestin. However, any of the combination OC products that contain these progestins may be prescribed for women intolerant of older agents or to first-time users of OCs. The newer progestins appear to be efficacious and offer similar cycle control, improved safety and tolerability profiles, and comparable price with the older agents.
Topics: Clinical Trials as Topic; Contraceptives, Oral; Desogestrel; Drug Interactions; Female; Humans; Norgestrel; Norpregnenes; Progesterone Congeners
PubMed: 8520092
DOI: 10.1177/106002809502907-817 -
American Journal of Obstetrics and... Mar 1993Associated with progesterone and the synthetic progestins used in oral contraceptives is a dose-dependent impairment of carbohydrate metabolism. It is well known that in... (Review)
Review
Associated with progesterone and the synthetic progestins used in oral contraceptives is a dose-dependent impairment of carbohydrate metabolism. It is well known that in the general population hyperinsulinemia and alterations in glucose metabolism are significant risk factors for the development of cardiovascular disease. Studies that use curve analysis of glucose tolerance tests have demonstrated insulin resistance, rises in plasma insulin, and relative glucose intolerance in women using oral contraceptives. Desogestrel, a new progestin, has been demonstrated to have generally less pronounced effects on these parameters of carbohydrate metabolism.
Topics: Animals; Blood Glucose; Carbohydrate Metabolism; Contraceptives, Oral, Synthetic; Coronary Disease; Desogestrel; Female; Humans; Insulin; Insulin Resistance; Male; Risk Factors
PubMed: 8447358
DOI: 10.1016/0002-9378(93)90335-g -
American Journal of Obstetrics and... Mar 1993Improvement in oral contraceptive formulations was originally achieved through dose reduction of the estrogen and progestogen components. Recently, further improvement... (Review)
Review
Improvement in oral contraceptive formulations was originally achieved through dose reduction of the estrogen and progestogen components. Recently, further improvement was achieved by increasing the selectivity of contraceptive progestins. The ratio between the affinity for the progesterone receptor and the affinity for the androgen receptor is an indicator of progesterone (or androgen) selectivity of a progestin. This ratio (selectivity index) reflects the relative amount of androgenic or progestational effect at a given dose. Relative selectivity can be characterized with in vitro receptor-binding studies and animal pharmacologic experiments. In comparison with levonorgestrel, desogestrel displays markedly lower androgenicity and slightly increased relative progestational activity. In receptor-binding experiments and animal pharmacologic studies, 3-keto-desogestrel, the active metabolite of desogestrel, shows the highest selectivity index. The favorable effect of desogestrel-containing oral contraceptives on lipoprotein metabolism and preexisting androgen-dependent skin disorders and the absence of adverse effects on blood pressure and body weight are attributed to the increased progestin selectivity of desogestrel.
Topics: Animals; Desogestrel; Female; Humans; Male; Ovulation; Progesterone Congeners; Prostate; Receptors, Androgen; Receptors, Progesterone
PubMed: 8447353
DOI: 10.1016/0002-9378(93)90330-l -
The Journal of Family Planning and... Jul 2003
Topics: Contraception; Contraceptives, Oral, Combined; Contraceptives, Oral, Synthetic; Desogestrel; Drug Prescriptions; Female; Humans; Intrauterine Devices; Ovulation; Patient Education as Topic; Practice Patterns, Physicians'; Progesterone Congeners; United Kingdom; Women's Health
PubMed: 12885316
DOI: 10.1783/147118903101197593 -
American Journal of Obstetrics and... Mar 1993Desogestrel is a gonane progestogen that in early studies had an improved ratio between desired progestational effects and undesired androgenic effects. A review of more... (Review)
Review
Desogestrel is a gonane progestogen that in early studies had an improved ratio between desired progestational effects and undesired androgenic effects. A review of more than 50 clinical studies suggests that desogestrel differs from progestins currently used in oral contraception in that it does not interfere with the estrogen effects on lipoprotein metabolism. This profile is attributable to the high selectivity of desogestrel.
Topics: Animals; Contraceptives, Oral, Combined; Desogestrel; Ethinyl Estradiol; Female; Humans; Lipid Metabolism
PubMed: 8447357
DOI: 10.1016/0002-9378(93)90334-f -
Expert Opinion on Drug Safety May 2013Desogestrel (DSG) is a third-generation progestin. It is commonly used in various formulations for hormonal contraception including combinations with ethinyl estradiol... (Review)
Review
INTRODUCTION
Desogestrel (DSG) is a third-generation progestin. It is commonly used in various formulations for hormonal contraception including combinations with ethinyl estradiol (EE), progestin-only pill and subdermal implants. DSG is also used in menopausal patients for hormone replacement therapy (HRT).
AREAS COVERED
The current manuscript aims to review the available data on safety and tolerability of DSG in oral contraception and HRT. The material included in the manuscript was searched and obtained via Medline, PubMed and EMBASE up to September 2012 using the search terms 'adverse events, side effects, tolerability' in combination with 'desogestrel and progestins'.
EXPERT OPINION
DSG is frequently used as contraceptive and it shows good contraceptive efficacy as demonstrated by the Pearl indexes reported in the studies reviewed in this manuscript. It is a versatile compound; in fact, it can be used either as progestin-only contraceptive or in combination with EE, and different formulations are available (such as the subdermal implant). In contraception, DSG is generally well tolerated but its use is associated with doubled risk of venous thromboembolism compared to second-generation progestins. Although DSG is efficacious in HRT, it may not represent the best choice due to the potential higher risk of breast cancer compared with progesterone or dydrogesterone.
Topics: Breast Neoplasms; Contraceptives, Oral, Combined; Desogestrel; Drug Therapy, Combination; Female; Hormone Replacement Therapy; Humans
PubMed: 23560561
DOI: 10.1517/14740338.2013.788147 -
Expert Opinion on Drug Metabolism &... Jan 2014Desogestrel (DSG) is a third-generation 19-nortestosterone derivative progestogen. It is contained in many oral contraceptive preparations, both combined (COCs) to... (Review)
Review
INTRODUCTION
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.
AREAS COVERED
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.'
EXPERT OPINION
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.
Topics: Administration, Oral; Animals; Contraceptive Agents, Female; Desogestrel; Drug Evaluation, Preclinical; Female; Humans; Randomized Controlled Trials as Topic
PubMed: 24102478
DOI: 10.1517/17425255.2013.844229 -
Journal of Pediatric and Adolescent... Oct 2021Adolescent menstrual dysfunction (AMD) is a common cause of iron deficiency anemia and absences from school. The management of AMD with single- and double-dose...
STUDY OBJECTIVE
Adolescent menstrual dysfunction (AMD) is a common cause of iron deficiency anemia and absences from school. The management of AMD with single- and double-dose desogestrel is largely on the basis of anecdotal evidence. Our aim was to describe the effectiveness and safety of both dosing strategies in our clinic cohort to help guide future management.
DESIGN
Local service evaluation with retrospective analysis of clinic notes.
SETTING
Adolescent gynecology clinic in a tertiary pediatric center in the North West of England.
PARTICIPANTS
Adolescent girls (10-18 years of age) with AMD (n = 129).
INTERVENTIONS
Single-dose (75 µg) desogestrel vs double-dose (150 µg) desogestrel.
MAIN OUTCOME MEASURES
Prevalence of amenorrhea and light spotting, side effects, and discontinuation rates of both dosing regimens.
RESULTS
Forty-three of 87 (49%) adolescent girls who started treatment with a double dose of desogestrel were amenorrheic/experienced light spotting, compared with 7/40 (18%) of girls who started treatment with a single dose (P = .001). Patients taking a double dose of desogestrel were less likely to discontinue overall (double: 45/89 [51%]; vs single: 35/40 [88%]; P < .001) and there was no evidence of an increase in nonbleeding side effects (double: 30/89 [34%]; vs single: 15/40 [38%]; P = .68).
CONCLUSION
Our findings provide evidence that a double dose of desogestrel is associated with a higher prevalence of amenorrhea and light spotting compared with a single dose in adolescent girls with AMD. However, larger studies are needed to further inform clinical guidelines.
Topics: Adolescent; Amenorrhea; Child; Desogestrel; Ethinyl Estradiol; Female; Humans; Metrorrhagia; Retrospective Studies
PubMed: 33989805
DOI: 10.1016/j.jpag.2021.04.015