Pharmacokinetic evaluation of desogestrel as a female ... Last Answer : C. It has additional androgenic acitivity. Fourth Generation Progestin - FPnotebook.com Newer progestogens Desogestrel is a prodrug of etonogestrel (3-ketodesogestrel), and, via this active metabolite, it has progestogenic activity, antigonadotropic effects, very weak androgenic activity, very weak glucocorticoid activity, and no other hormonal activity. For androgenicity, it would be 0.15 X 3.4 = .51 or half as androgenic as a pill containing 1 mg of norethindrone. These effects help counter the androgenic effects. It has both strong progestational and strong antiovulatory activities C. It has additional androgenic acitivity D. It does not counteract the beneficial effect of estrogen on lipid profile. Medroxyprogest-erone acetate. The distinctive features of desogestrel include the following except: A. Desogestrel. Norethisterone acetate. I started Yaz, an anti-androgen birth control, 3 months ago in addition to adopting a healthier diet. Levonorgestrel. 91,92 The relevance of this latter finding in humans is unknown. Desogestrel bioavailability was determined by the measurement of 3-ketodesogestrel plasma concentration. Norethindrone acetate is another first-generation progestin with low progestational activity and slight estrogenic effects. It tends to be less androgenic than the second-generation progestins, but more androgenic than newer progestins, like desogestrel. Some have antiandrogenic activity but not as much as cyproterone acetate has. 4th generation progesterone. Femilon controls hyperandrogenic states very efficiently by Ethinyl estradiol’s ability to raise SHBG as well as desogestrel’s inherent anti-androgenic activity. ... particularly norgestimate, desogestrel, and gestodene. No clinical data on efficacy and safety are available in adolescents below 18 years. Furthermore, all three progestins exhibited weak GR-mediated antagonistic activity. Desogestrel and Etonogestrel. New birth control pill formulations contain progestins with less androgenic activity. For example, desogestrel is a very potent and androgenic progestin but its usual oral contraceptive dose is 0.15 mg instead of 1.00 mg for norethindrone. Desogestrel is a synthetic progestogen. None of them bind to sex hormone-binding globulin (SHBG). It is a prodrug B. The androgenic and the progestational activity of norgestimate (NORG) and levonorgestrel (LNG) were compared in two animal studies. In 1969 I discovered that it was the progestogens with inherent oestrogenic activity, norethisterone acetate and ethynodiol diacetate, The degree to which progestational activity is maximized and androgenic activity is minimized is a measure of a progestin's selectivity. I’d definitely say I’ve noticed less shedding. This difference in androgenicity may be responsible for observed differences in metabolic effects between oral contraceptive (OC) formulations containing almost equivalent estrogen doses but with either DSG or LNG as a progestogen. Serum LDL-C 59.2 ± 12.7 61.7 ± 13.6 Ĺ 4.22 Not significant. The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism Levonorgestrel. They have developed norgestimate (NGM) which is a progestin with improved selectivity. Desogestrel (3.4) Progestins with least Androgenic Activity. It has a low incidence of side effects and complications, similar to other progestogens. Indications: Progestin component in vaginal ring contraceptive - (NuvaRing-combined with ethinyl estradiol) Side Effects: active metabolite of desogestrel - minimal androgenic activity norelgestromin Synthetic progestin (progesterone agonist) It's usually used in low dose combination pills, meaning that the pill has less than 50 mcg of synthetic estrogen, ethinyl estradiol. Desogestrel (DSG) is a highly effective progestin with low androgenic activity and high antigonadotrophic activity (De Bastos et al., 2014). A hormone which is found in birth control tablets that can cause hair loss is progestin. no androgenic activity. It is a prodrug B. Desogestrel, norgestimate and drospirenone (3rd / 4th generation) have the least androgenic activity. Description : The distinctive features of desogestrel include the following except: A. Those that find birth control pills promote excess hair growth or hair loss usually find switching to another formulation helps. OVARIES -- prevention of follicular development & … For androgenicity, it would be 0.15 X 3.4 = .51 or half as androgenic as a pill containing 1 mg of norethindrone. Gestodene has relatively high affinity for the glucocorticoid receptor, about 27% of that of the corticosteroid dexamethasone. Oral DSG in combination with various TE doses produced 100% azoospermia (Table I). When used as a contraceptive, it is a strong antiovulatory compound, even at low doses. In the last three decades, new progestins have been developed in order to reduce androgenic side effects . lower oestrogen or higher progestogen pill or pill with some androgenic activity . Am Fam Physician. A Comparative Study of Drospirenone and Desogestrel: An Overview of Benefits and Side Effects. Desogestrel (DSG) is a highly effective progestin with low androgenic activity and high antigonadotrophic activity (De Bastos et al., 2014). Receptor binding studies, as well as studies in animals, have shown that 3-keto-desogestrel, the biologically active metabolite of desogestrel, combines high progestational activity with minimal intrinsic androgenicity. Correlation with nuclear magnetic resonance signals. Serum LDL-C 59.2 ± 12.7 61.7 ± 13.6 Ĺ 4.22 Not significant. The progestins of this class retain varying degrees of androgenic activity that possibly accumulate with that of the exogenous androgen. i.e., extent of maximization of progestational … A selective progestin has progestational effects at relatively low concentrations or doses and androgenic effects at only relatively high concentrations or doses. It has a weak androgenic activity, which can not be shown. Reprint request to: Mr Srithean Lertvikool, Department of Obstetrics and Gynecology, Faculty of Medicine Ramathibodi Hospital, Mahidol University, 270 Rama 6 Road, Ratchatawee, Bangkok 10400, Thailand. 3rd generation little androgenic activity C11 substitution increase activity. Accepted: July 31 2014. It has both strong progestational and strong antiovulatory activities C. It has additional androgenic acitivity D. It does not counteract the beneficial effect of estrogen on lipid profile. Progestin Generations . V. Progestins with least Androgenic Activity. Moreover, the androgenic activity of progestins within the testosterone derivatives also varies, and while some may have high or moderate androgenic activity, others have only low or no such activity. The least 'androgenic' progestins often added to OCPs include norethindrone, norethindrone actetate, desogestrel, norgestimate and drosperisone.The most 'androgenic' progestins in OCPs have names like levonorgestrel and norgestrel. Glucocorticoid activity. It is a prodrug B. ... selective progestogen with low androgenic activity [3]. [A higher estrogen content is also recommended] Desogestrel 0.15 mg/EE 30 mcg Desogen® Drospirenone 3 mg/EE 20 mcg Yaz® Drospirenone 3 mg/EE 30 mcg Yasmin® Norgestimate 0.25 mg/EE 35 mcg Ortho-Cyclen® Bloating Switch progestin to drospirenone which has weak potassium-sparing diuretic effets. More... Desogestrel is a synthetic progestogen structurally related to levonorgestrel, with progesterone hormone receptor agonistic activity, used as a contraceptive and hormone replacement agent. Desogestrel (DSG) is a less-androgenic progestogen than levonorgestrel (LNG). Pregestational only … Its progestin potency compared to norethindrone would be 0.15 X 9.0 = 1.35 times. and the boost in estrogen I believe is working to keep my hairs in the growth (anagen) phase longer. Last … Preparations: Good Triphasic Initial Choices. Newer progestins (norgestimate and desogestrel) have little or no androgenic activity, whereas other progestins (cyproterone acetate, drospirenone, and dienogest) have antiandrogenic activity . The varying progestational “potencies” attributed to different COC preparations are based on pharmacological experimental models. These results demonstrate the synergistic action of this steroid … Description : he distinctive features of desogestrel include the following except: A. The decreased androgenic activity is thought to be related to the 5α-reduced metabolite of testosterone, dihydrotestosterone, having greater AR potency than testosterone, but the 5α-reduced metabolites of 19-nortestosterone derivatives having diminished AR agonist potency relative to their parent steroids. no androgenic or estrogenic activity. Desogestrel is a new, potent progestogen with very low androgenic properties. Description : The distinctive features of desogestrel include the following except: A. The androgenic properties of progestins determine their biological activity in the breast epithelium and reveal an unexpected role for AR activity in breast epithelial cell proliferation. Desogestrel | C22H30O | CID 40973 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more. Pregnane Progestin (0) Norethynodrel (0) Ethynodiol Diacetate (0.6) Norethindrone (1.0): Lower limit reference. Desogestrel (DSG) is an oral third-generation progestogen with potent progestational activity and lower androgenicity. It has both strong progestational and strong antiovulatory activities C. It has additional androgenic acitivity D. It does not counteract the beneficial effect of estrogen on lipid profile. androgenic activity. Oral Contraceptive Androgenic Activity (low to high) Andogen activity based on Methytestosterone mg/28 days. desogestrel: [ des″o-jes´trel ] a progestational agent having little androgenic activity; used in combination with an estrogen component as an oral contraceptive . Progestational activity is usually tested using the McPhail Index in immature rabbits, and also the pregnancy maintenance and the ovulation inhibition tests in rats.2 In contrast to progesterone, which showed antiandrogenic activity, gestodene and 3-keto-desogestrel both exhibited androgenic activity. Desogestrel Progestational Activity: 9.0 Norgestimate Progestational Activity: Estrogenic Activity: 0 Androgenic Activity: 1.3 Estrogenic Activity: 0 3.4 AndrogenicActivity: Desogen (0.15/30) Ortho-Cept(0.15/30) Androgenic Activity: 1.9 Cept (0.15/30) Ortho-Cyclen (0.15/30) Mircette (0.15/20) Cyclessa (0.100 - A synthetic progestogen structurally related to levonorgestrel, with progesterone hormone receptor agonistic activity, used as a contraceptive and hormone replacement agent. This means it has low progestational and estrogenic activity and also tends to be less androgenic than second generation progestins. Its progestin potency compared to norethindrone would be 0.15 X 9.0 = 1.35 times. DMPA is a long-acting, reversible progestational contraceptive without any estrogenic or androgenic activity. For androgenicity, it would be 0.15 X 3.4 = .51 or half as androgenic as a pill containing 1 mg of norethindrone. 4th generation. For example, levonorgestrel has a high androgenic index, which can cause adverse reactions in women who are sensitive to androgenic activity. Desogestrel (DSG) is an oral third-generation progestogen with potent progestational activity and lower androgenicity. It has … In contrast to progesterone, which showed antiandrogenic activity, gestodene and 3-keto-desogestrel both exhibited androgenic activity. For example norgestimate or desogestrel are non-androgenic progestins used in modern birth control pill formulations. The distinctive features of desogestrel include the following except: A. Desogestrel is a progestin, or a synthetic progestin, and therefore is a progesterone receptor agonist, the biological target of progestogens like progesterone. Although approved by the US Food and Drug Administration (FDA) in 1959 as a treatment for endometrial and renal cancers, it is now primarily used for contraception because of its ability to inhibit follicular maturation and ovulation. The least 'androgenic' progestins often added to OCPs include norethindrone, norethindrone actetate, desogestrel, norgestimate and drosperisone.The most 'androgenic' progestins in OCPs have names like levonorgestrel and norgestrel. The endocrine activities measured are those most closely related to the clinically important actions of contraceptives. In Table below, the first column is the micrograms of oestrogen. For example, desogestrel is a very potent and androgenic progestin but its usual oral contraceptive dose is 0.15 mg instead of 1.00 mg for norethindrone. Lots of progestational and some androgenic -Ortho-cept, Desogen 3rd generation. Birth control pills’ androgenic action can result in a variety of side effects, including hair loss. https://www.verywellhealth.com/different-progestin-types-906936 Pharmacokinetics Desogestrel is rapidly and almost completely absorbed from the gastrointestinal tract and immediately metabolized in the liver and in the intestinal wall in the 3-keto-desogestrel, which is the biologically active metabolite of desogestrel.

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