[18], Drospirenone is the generic name of the drug and its INN, USAN, BAN, and JAN, while drospirénone is its DCF. [31][32] Due to its antimineralocorticoid activity, drospirenone opposes estrogen-induced salt and water retention and maintains or slightly reduces body weight. Taking drospirenone with cobicistat may increase drospirenone serum concentrations. Drospirenone counteracts the estrogen-induced stimulation of the renin-angiotensin-aldosterone system and blocks testosterone from binding to androgen receptors. [44] The incidence is about 4-fold higher on average than in women not taking a birth control pill. Mechanism of Action Estrogen receptor agonists; Mineralocorticoid receptor antagonists; Progesterone receptor agonists; Testosterone congener inhibitors Orphan Drug Status Orphan designation is assigned by a regulatory body to encourage companies to develop drugs for rare diseases. 14.1 . Drospirenone prevents pregnancy primarily by suppressing ovulation. 21733. Contact Supplier. [1], Common side effects include acne, headache, breast tenderness, weight increase, and menstrual changes. Taking drospirenone and ethinyl estradiol can increase your risk of blood clots, stroke, or heart attack. [1][2][3][58] The medication is more potent as an antiandrogen than spironolactone, but is less potent than cyproterone acetate, with about 30% of its antiandrogenic activity in animals. Estradiol/drospirenone (E2/DRSP), sold under the brand name Angeliq, is a combination of estradiol (E2), an estrogen, and drospirenone (DRSP), a progestin, antimineralocorticoid, and antiandrogen, which is used in menopausal hormone therapy, specifically the treatment of menopausal syndrome and osteoporosis, in postmenopausal women. [8][47], Different progestins in ethinylestradiol-containing birth control pills have been associated with different risks of VTE. [2][4], Drospirenone, also known as 1,2-dihydrospirorenone or as 17β-hydroxy-6β,7β:15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid, γ-lactone, is a synthetic steroidal 17α-spirolactone, or more simply a spirolactone. [21] Drospirenone was introduced for use as a progestogen-only birth control pill in 2019. Product Presentation. Drospirenone side effects. [4] Symptoms that may occur in the event of an overdose may include nausea, vomiting, and vaginal bleeding. [4] This may increase the risk of hyperkalemia (high potassium levels). [2] Progesterone and drospirenone counteract these undesirable effects via their antimineralocorticoid activity. Action . [4] Elimination of drospirenone is virtually complete 10 days after the last dose. [2] The medication does not inhibit the effects of ethinylestradiol on sex hormone-binding globulin (SHBG) and serum lipids, in contrast to androgenic progestins like levonorgestrel but similarly to other antiandrogenic progestins like cyproterone acetate. USDMF . [63][62][64], These have been no reports of serious adverse effects with overdose of drospirenone. [4][8] Drospirenone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It is an agonist of the PR and an antagonist of the MR and AR, and hence is a progestogen, antimineralocorticoid, and antiandrogen. [2] Similar effects occur during the luteal phase of the menstrual cycle due to increased progesterone levels and the resulting antagonism of the MR.[2] Estrogens, particularly ethinylestradiol, activate liver production of angiotensinogen and increase levels of angiotensinogen and angiotensin II, thereby activating the renin–angiotensin–aldosterone system. Website. Drospirenone is a progestin medication which is used in birth control pills to prevent pregnancy and in menopausal hormone therapy, among other uses. [79][4] It has been said that the pharmacological profile of drospirenone more closely resembles that of progesterone than other progestins due to its antimineralocorticoid activity. [105] It includes prasterone (dehydroepiandrosterone; DHEA), an oral androgen prohormone, to replace testosterone and avoid testosterone deficiency caused by suppression of testosterone by ethinylestradiol and drospirenone. [41][43] Persistent hyperkalemia that required discontinuation occurred in 2 out of around 1,000 women (0.2%) with 4 mg/day drospirenone alone in clinical trials. Global leader in steroidal APIs. 15 REFERENCES 16 HOW SUPPLIED/STORAGE AND HANDLING . Oral Contraceptive Clinical Trial 14.2 . Update your events Sterling Spa. [104], A combination of ethinylestradiol, drospirenone, and prasterone is under development by Pantarhei Bioscience as a combined birth control pill for prevention of pregnancy in women. [8][56], In the early 2010s, the FDA updated the label for birth control pills containing drospirenone and other progestins to include warnings for stopping use prior to and after surgery, and to warn that such birth control pills may have a higher risk of blood clots. drospirenone was devoid of glucocorticoid activity. Folate Supplementation Clinical Trials . Call your doctor or seek emergency medical help if you have severe pain in your lower stomach or side. [44] The absolute risk of VTE with ethinylestradiol-containing birth control pills is small, in the area of 3 to 10 out of 10,000 women per year, relative to 1 to 5 out of 10,000 women per year not taking a birth control pill. [4][2][5][6], Drospirenone is excreted in urine and feces, with slightly more excreted in feces than in urine. [106][107][108][109], O=C7O[C@@]6([C@@]3([C@H]([C@@H]2[C@@H]4[C@H](/C1=C/C(=O)CC[C@]1(C)[C@H]2CC3)C4)[C@@H]5C[C@@H]56)C)CC7, InChI=1S/C24H30O3/c1-22-6-3-12(25)9-17(22)13-10-14(13)20-16(22)4-7-23(2)21(20)15-11-18(15)24(23)8-5-19(26)27-24/h9,13-16,18,20-21H,3-8,10-11H2,1-2H3/t13-,14+,15-,16+,18+,20-,21+,22-,23+,24+/m1/s1, Ethinylestradiol 30 μg and drospirenone 3 mg, Ethinylestradiol 30 μg, drospirenone 3 mg, and levomefolate calcium 0.451 mg, Ethinylestradiol 20 μg and drospirenone 3 mg, Estradiol 0.5 or 1 mg and drospirenone 0.25 or 0.5 mg, Conjugated estrogens/medroxyprogesterone acetate, progesterone receptor membrane component-1, List of progestogens § Spirolactone derivatives, List of steroidal antiandrogens § Spirolactone derivatives, List of progestogens available in the United States, ethinylestradiol, drospirenone, and prasterone, Ethinylestradiol/drospirenone/levomefolic acid, "Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects", "Drospirenone/ethinyl estradiol 3 mg/20 μg (24/4 day regimen): hormonal contraceptive choices – use of a fourth-generation progestin", "Pharmacokinetic interaction between the CYP3A4 inhibitor ketoconazole and the hormone drospirenone in combination with ethinylestradiol or estradiol", "Does the Progestogen Used in Combined Hormonal Contraception Affect Venous Thrombosis Risk? [1][4] The two major metabolites of drospirenone are drospirenone acid and 4,5-dihydrodrospirenone 3-sulfate, and are both formed independently of the cytochrome P450 system. Drospirenone has no estrogenic activity and no appreciable glucocorticoid or antiglucocorticoid activity. [1][84][65][71] Progesterone displays antiandrogenic activity in some assays similarly to drospirenone,[2] although this issue is controversial and many researchers regard progesterone as having no significant antiandrogenic activity. YASMINELLE ® is an oral contraceptive consisting of an estrogenic hormone such as ethinyl estradiol and a progestogen such as drospirenone. [89], Spirolactones like drospirenone and spironolactone are derivatives of progesterone, which likewise has progestogenic and antimineralocorticoid activity. [48], In July 2012, Bayer notified its stockholders that there were more than 12,000 such lawsuits against the company involving Yaz, Yasmin, and other birth control pills with drospirenone. [4] There is no antidote for overdose of drospirenone and treatment of overdose should be based on symptoms. Pharmacodynamics 12.3 . Drospirenone has another hormonal mechanism: that of an antiandrogeni c hormone, which exerts its progestatio nal and ant imine raloc ortic oid ef fects b y compe titiv ely in hibit ing [71] The total endometrial transformation dose of drospirenone is about 50 mg per cycle, whereas its daily dose is 2 mg for partial transformation and 4 to 6 mg for full transformation. [7] Its name is a shortened form of the name 1,2-dihydrospirorenone or dihydrospirenone. [45][46] The risk of VTE during pregnancy is 5 to 20 in 10,000 women per year and during the postpartum period is 40 to 65 per 10,000 women per year. The egg can no longer accept a … [21][22][23][24] The drospirenone component in this formulation is included specifically to prevent estrogen-induced endometrial hyperplasia. [41] In women with mild or moderate chronic kidney disease, or in combination with chronic daily use of other potassium-sparing medications (ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics, heparin, antimineralocorticoids, or nonsteroidal anti-inflammatory drugs), a potassium level should be checked after two weeks of use to test for hyperkalemia. Drospirenone + Ethinyl estradiol is a generic medicine name and there are several brands available for it. Please be aware that you should take drospirenone + ethinyl estradiol only if a doctor has recommended or prescribed it. Mechanism of Action 12.2 . 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