[42], Drospirenone has been found to stimulate the proliferation and migration of breast cancer cells in preclinical research, similarly to certain other progestins. Therefore, serum potassium and sodium, and evidence of metabolic acidosis, should be monitored in cases of overdose. Drospirenone prevents pregnancy primarily by suppressing ovulation. [4] Symptoms that may occur in the event of an overdose may include nausea, vomiting, and vaginal bleeding. [58], Many lawsuits have been filed against Bayer, the manufacturer of drospirenone, due to the higher risk of venous thromboembolism (VTE) that has been observed with combined birth control pills containing drospirenone and certain other progestins relative to the risk with levonorgestrel-containing combined birth control pills. Drospirenone is a spironolactone analogue with antimineralocorticoid activity. [4] At least 20 different metabolites can be identified in urine and feces. Please be aware that you should take drospirenone + ethinyl estradiol only if a doctor has recommended or prescribed it. Oral Contraceptive Clinical Trial 14.2 . [7] Its name is a shortened form of the name 1,2-dihydrospirorenone or dihydrospirenone. [7] Among others, it is marketed in combination with ethinylestradiol under the brand names Yasmin and Yaz and in combination with estradiol under the brand name Angeliq. drospirenone was devoid of glucocorticoid activity. [57][58] The combination of estradiol and drospirenone has been found to increase breast density, an established risk factor for breast cancer, in postmenopausal women. Instruct women to report adverse events to their prescribers. [1] For comparison to progesterone, a 200 mg dose of oral progesterone is considered to be approximately equivalent in antimineralocorticoid effect to a 25 to 50 mg dose of spironolactone. Some of the brands for drospirenone + ethinyl estradiol might be better known than drospirenone + ethinyl estradiol itself. You can get this information while placing the order for drospirenone + ethinyl estradiol with the pharmacy. [103] This is in addition to around 10,000 claims that Bayer has already settled without admitting liability. Home delivery services for drospirenone + ethinyl estradiol may be free or they may cost you depending on the pharmacy and the minimum order requirements. [2][1] The apparent volume of distribution of drospirenone is approximately 4 L/kg. [7][88] Drospirenone differs structurally from spironolactone only in that the C7α acetylthio substitution of spironolactone has been removed and two methylene groups have been substituted in at the C6β–7β and C15β–16β positions. [87] Certain other progestins act similarly in this assay, whereas progesterone acts neutrally. Because of these characteristics, it has the potential to reduce body weight, blood pressure, and low-density lipoprotein levels and to enhance high-density lipoprotein levels. The egg can no longer accept a … [65], Drospirenone is an antagonist of the MR, the biological target of mineralocorticoids like aldosterone, and hence is an antimineralocorticoid. [63][62][64], These have been no reports of serious adverse effects with overdose of drospirenone. [62] Progestogen-only birth control is not generally associated with a higher risk of breast cancer. Preclinical studies in animals and . [74] No studies of the antigonadotropic effects of drospirenone or its influence on hormone levels appear to have been conducted in men. [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. Mechanism of Action. Folate Supplementation Clinical Trials . [18], Drospirenone is the generic name of the drug and its INN, USAN, BAN, and JAN, while drospirénone is its DCF. [4][1] Drospirenone has no affinity for sex hormone-binding globulin (SHBG) or corticosteroid-binding globulin (CBG), and hence is not bound by these plasma proteins in the circulation. [3][2][58], Due to its antimineralocorticoid activity, drospirenone increases natriuresis, decreases water retention and blood pressure, and produces compensatory increases in plasma renin activity as well as circulating levels and urinary excretion of aldosterone. [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. 3. Drospirenone. [4], Drospirenone binds with high affinity to the progesterone receptor (PR) and mineralocorticoid receptor (MR), with lower affinity to the androgen receptor (AR), and with very low affinity to the glucocorticoid receptor (GR). Drospirenone + Ethinyl estradiol is a generic medicine name and there are several brands available for it. [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. (2020). YASMINELLE ® is an oral contraceptive consisting of an estrogenic hormone such as ethinyl estradiol and a progestogen such as drospirenone. [1][72][71] The medication acts as a contraceptive by activating the PR, which suppresses the secretion of luteinizing hormone, inhibits ovulation, and alters the cervical membrane and endometrium. [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. Drospirenone is a gestagen-only drug. [68][69][1][70] Inhibition of ovulation occurred in about 90% of women at a dose of 0.5 to 2 mg/day and in 100% of women at a dose of 3 mg/day. [4] This may increase the risk of hyperkalemia (high potassium levels). You are even more at risk if you have high blood pressure, diabetes, high cholesterol, or if you are overweight.Your risk of stroke or blood clot is highest during your first year of taking birth control pills. [25] Drospirenone has also been used in combination with an estrogen as a component of hormone therapy for transgender women. [2] It is metabolized into the acid form of drospirenone by opening of its lactone ring. in vitro. 14 CLINICAL STUDIES . [7], Drospirenone has been categorized as a "fourth-generation" progestin. [7][88][98][99][100][101], Drospirenone is marketed in combination with an estrogen under a variety of brand names throughout the world. [13][14] The medication was approved for use in menopausal hormone therapy in combination with estradiol in 2005. Pharmacology For Drospirenone + Ethinyl estradiol, directory of Pharmacies, Chemists and Druggists, branded alternatives for drospirenone + ethinyl estradiol, Ministry of Health & Family Welfare-Government of India, Department of Health Research (DHR), Government of India, Department of Indian Systems of Medicine and Homoeopathy, Pharmacopoeial Laboratory for Indian Medicine (PLIM). [2] Drospirenone and its metabolites are excreted in urine about 38% as glucuronide conjugates, 47% as sulfate conjugates, and less than 10% in unconjugated form. Call your doctor or seek emergency medical help if you have severe pain in your lower stomach or side. Taking drospirenone with cobicistat may increase drospirenone serum concentrations. [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. [4] With the combination of 30 μg/day ethinylestradiol and 3 mg/day drospirenone, peak levels of drospirenone after a single dose are 35 ng/mL, and levels at steady state are 60 to 87 ng/mL at peak and 20 to 25 ng/mL at trough. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge. Pharmacodynamics 12.3 . [96][97] It was introduced for medical use in combination with ethinylestradiol as a combined birth control pill in 2000. Description: Ethinylestradiol and drospirenone suppress ovulation by negative feedback mechanism on the hypothalamus that changes the normal gonadotropin secretion pattern of FSH and LH by the anterior pituitary gland, thereby blocking the follicular FSH phase and midcycle surge of gonadotropins. Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.. As far as the mechanism of action is concerned, the literature has been sustaining the direct role of COCs in hsCRP determination by affecting the latter’s metabolic and genetic regulation . Drospirenone has no estrogenic activity and no appreciable glucocorticoid or antiglucocorticoid activity. Update your events Sterling Spa. [4] Drospirenone may interact with potassium-sparing medications such as ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics, potassium supplements, heparin, antimineralocorticoids, and nonsteroidal anti-inflammatory drugs to further increase potassium levels. [1][65][66][3] It is an agonist of the PR and an antagonist of the MR and AR, and hence is a progestogen, antimineralocorticoid, and antiandrogen. [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. [7][4] The medication is taken by mouth. [8][47], Different progestins in ethinylestradiol-containing birth control pills have been associated with different risks of VTE. Italy. [8] Birth control pills containing progestins such as desogestrel, gestodene, drospirenone, and cyproterone acetate have been found to have 2- to 3-fold the risk of VTE of birth control pills containing levonorgestrel in retrospective cohort and nested case–control observational studies. [1][74][2] Drospirenone alone at 4 mg/day has been found to suppress estradiol levels in premenopausal women to about 40 to 80 pg/mL depending on the time of the cycle. [105] As of August 2018, the formulation is in phase II/III clinical trials. Drospirenone side effects. [2][1] As a result, they can produce undesirable side effects including increased sodium excretion, water retention, weight gain, and increased blood pressure. [65][71][78] Accordingly, 3 to 4 mg drospirenone is said to be equivalent to about 20 to 25 mg spironolactone in terms of antimineralocorticoid activity. Ethinyl … Global leader in steroidal APIs. [1][65][3][58] Drospirenone has no estrogenic activity and no appreciable glucocorticoid or antiglucocorticoid activity. [4] Since drospirenone has antimineralocorticoid activity, levels of potassium and sodium should be measured and signs of metabolic acidosis should be monitored. Mechanism of Action 12.2 . Website. [1][7] It is available both alone under the brand name Slynd and in combination with an estrogen under the brand name Yasmin among others. [75], Drospirenone has been studied in forms for parenteral administration. Drospirenone is devoid of any estrogenic, glucocorticoid and antiglucocorticoid activity, which provides a pharmacological profile very close to the profile of the natural hormone progesterone. The presence of drospirenone, a synthetic progestin with antimineralocorticoid activity useful for reducing the accumulation of sodium and water and associated pathologies, is instead justified by the direct action on the endometrium, useful for controlling the growth of endometrial cells induced by estradiol, potentially dangerous for the development of neoplastic diseases. [73][4], Due to its antigonadotropic effects, drospirenone inhibits the secretion of the gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and suppresses gonadal sex hormone production, including of estradiol, progesterone, and testosterone. [90][91][92] The loss of the C7α acetylthio group of spironolactone, a compound with negligible progestogenic activity,[93][94] appears to be involved in the restoration of progestogenic activity in drospirenone, as SC-5233, the analogue of spironolactone without a C7α substitution, has potent progestogenic activity similarly to drospirenone. [28][29] E2/DRSP has been found to increase bone mineral density and to reduce the occurrence of bone fractures in postmenopausal women. [49] Systematic reviews and meta-analyses of all of the data in the mid-to-late 2010s found that birth control pills containing cyproterone acetate, desogestrel, drospirenone, or gestodene overall were associated with a risk of VTE of about 1.3- to 2.0-fold compared to that of levonorgestrel-containing birth control pills. [1][2] It has about 1 to 65% of the affinity of the synthetic anabolic steroid metribolone for the AR. [1][2][3] Peak levels occur 1 to 6 hours after an oral dose. [4], Drospirenone is an antimineralocorticoid with potassium-sparing properties, though in most cases no increase of potassium levels is to be expected. [75][76][77] In male cynomolgus monkeys however, 4 mg/kg/day oral drospirenone strongly suppressed testosterone levels. 11 DESCRIPTION. the cervical mucus (which increases the difficulty of sperm entry into the uterus) and the : endometrium (which reduces the likelihood of implantation). Drospirenone counteracts the estrogen-induced stimulation of the renin-angiotensin-aldosterone system and blocks testosterone from binding to androgen receptors. [4] Drospirenone also undergoes oxidative metabolism by CYP3A4. [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. [13][14] It is available as a generic medication. [62] Conversely, combined birth control and menopausal hormone therapy with an estrogen and a progestogen are associated with higher risks of breast cancer. [8][45] However, this area of research is controversial, and confounding factors may have been present in these studies. [11][12] It is available widely throughout the world. [4], Birth control pills containing ethinylestradiol and a progestin are associated with an increased risk of venous thromboembolism (VTE), including deep vein thrombosis (DVT) and pulmonary embolism (PE). [21] Drospirenone was introduced for use as a progestogen-only birth control pill in 2019. Ahead of Print. [103] These claims of VTE have amounted to US$1.97 billion. Once Bound To The Receptor, Progestins Slow The Frequency Of Release Of Gonadotropin Releasing Hormone (GnRH) From The Hypothalamus And Blunt The Pre-ovulatory LH … [1][65][3][58], Drospirenone is an agonist of the PR, the biological target of progestogens like progesterone. [1][65] It has about 35% of the affinity of promegestone for the PR and about 19 to 70% of the affinity of progesterone for the PR. Contact Supplier. [26][27], Studies have found that EE/DRSP is superior to placebo in reducing premenstrual emotional and physical symptoms while also improving quality of life. 14.1 . primary mechanism of this action is inhibition of ovulation, other alterations include changes in . [4][41][42] Renal impairment, hepatic impairment, and adrenal insufficiency are contraindicated because they increase exposure to drospirenone and/or increase the risk of hyperkalemia with drospirenone. [102] They also noted that the company by then had settled 1,977 cases for US$402.6 million, for an average of US$212,000 per case, while setting aside US$610.5 million to settle the others. [2] Progesterone and drospirenone counteract these undesirable effects via their antimineralocorticoid activity. Mechanism of Action of Drospirenone Drospirenone diffuse freely into target cells in the female reproductive tract, mammary gland, hypothalamus, and the pituitary and bind to the progesterone receptor. 15 REFERENCES 16 HOW SUPPLIED/STORAGE AND HANDLING . Before taking this medicine. [4][2] Neither of these metabolites are known to be pharmacologically active. [4], Inhibitors and inducers of the cytochrome P450 enzyme CYP3A4 may influence the levels and efficacy of drospirenone. [8][56] Conversely, this would be the case less or not at all with progestins that are less androgenic, like desogestrel and gestodene, as well as progestins that are antiandrogenic, like drospirenone and cyproterone acetate. [4], The distribution half-life of drospirenone is about 1.6 to 2 hours. Drospirenone is a spironolactone analogue which has antimineralocorticoid properties. Mechanism of Action. [2][81][1] This has been shown to occur at doses of 2 to 4 mg/day. [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. [1][2][58] Drospirenone has antigonadotropic and functional antiestrogenic effects as a result of PR activation. 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. It would be best to get this clarified while placing the order. [8][45][48] Other observational studies, specifically prospective cohort and case control studies, have found no differences in risk between different progestins, including between birth control pills containing drospirenone and birth control pills containing levonorgestrel. Mechanism of Action of Drospirenone Drospirenone diffuse freely into target cells in the female reproductive tract, mammary gland, hypothalamus, and the … [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. [62], The oral bioavailability of drospirenone is between 66 and 85%. USDMF . [1][65] The ovulation-inhibiting dosage of drospirenone is 2 to 3 mg/day. [103] Bayer also reached a settlement for arterial thromboembolic events, including stroke and heart attacks, for US$56.9 million. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for drospirenone + ethinyl estradiol before they complete the sale. [4] Rare side effects may include high potassium levels and blood clots, among others. [104] As of October 2019, it is in phase III clinical trials. [59][60][61], Data on risk of breast cancer in women with newer progestins like drospirenone are lacking at present. [4] There is no antidote for overdose of drospirenone and treatment of overdose should be based on symptoms. 2012-02-17. However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. Taking drospirenone and ethinyl estradiol can increase your risk of blood clots, stroke, or heart attack. [4], Adverse effects of drospirenone alone occurring in more than 1% of women may include unscheduled menstrual bleeding (breakthrough or intracyclic) (40.3–64.4%), acne (3.8%), metrorrhagia (2.8%), headache (2.7%), breast pain (2.2%), weight gain (1.9%), dysmenorrhea (1.9%), nausea (1.8%), vaginal hemorrhage (1.7%), decreased libido (1.3%), breast tenderness (1.2%), and irregular menstruation (1.2%). [7] The medication is sometimes referred to as a "fourth-generation" progestin. [2][1] The pharmacokinetics of oral drospirenone are linear with a single dose across a dose range of 1 to 10 mg.[4][2] Intake of drospirenone with food does not influence the absorption of drospirenone. Product Presentation. [33], Drospirenone is available in the following formulations, brand names, and indications:[34][35], Contraindications of drospirenone include renal impairment or chronic kidney disease, adrenal insufficiency, presence or history of cervical cancer or other progestogen-sensitive cancers, benign or malignant liver tumors or hepatic impairment, undiagnosed abnormal uterine bleeding, and hyperkalemia (high potassium levels). [11][12] Schering AG of Germany has been granted several patents on the production of drospirenone, including WIPO and US patents, granted in 1998 and 2000, respectively. [31][32] Due to its antimineralocorticoid activity, drospirenone opposes estrogen-induced salt and water retention and maintains or slightly reduces body weight. Drospirenone counteracts the estrogen-induced stimulation of the renin-angiotensin-aldosterone system and blocks testosterone from binding to … [4] There is 1.5- to 2-fold accumulation in drospirenone levels with continuous administration, with steady-state levels of drospirenone achieved after 7 to 10 days of administration. Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including drospirenone + ethinyl estradiol. [9][10], Drospirenone was patented in 1976 and introduced for medical use in 2000. [1][4] The medication is also metabolized by reduction of its double bond between the C4 and C5 positions and subsequent sulfation. [4][1] It is bound to albumin and 3 to 5% circulates freely or unbound. Target: Progesterone Receptor Drospirenone is a novel progestin under clinical development that is similar to the natural hormone progesterone, combining potent progestogenic with antimineralocorticoid and antiandrogenic activities. 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility . [4] Only trace amounts of unchanged drospirenone can be found in urine and feces. [105], Drospirenone has been suggested for potential use as a progestin in male hormonal contraception. [1] It has additional antimineralocorticoid and antiandrogenic activity and no other important hormonal activity. [7][88] Drospirenone is also known by its developmental code names SH-470 and ZK-30595 (alone), BAY 86-5300, BAY 98-7071, and SH-T-00186D (in combination with ethinylestradiol), and BAY 86-4891 (in combination with estradiol). 13 NONCLINICAL TOXICOLOGY . [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. [1], Common side effects include acne, headache, breast tenderness, weight increase, and menstrual changes. 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. [95], Drospirenone was patented in 1976 and introduced for medical use in 2000. [1][4][2] Peak levels of drospirenone at steady state with 4 mg/day drospirenone are about 41 ng/mL. In a therapeutic dose, drospirenone also has antiandrogenic and weak antimineralocorticoid activity. It appears to suppress ovulation more consistently than norethindrone. [80] Both drospirenone and progesterone are actually weak partial agonists of the MR in the absence of mineralocorticoids. [8] In contrast to ethinylestradiol-containing birth control pills, neither progestogen-only birth control nor the combination of transdermal estradiol and an oral progestin in menopausal hormone therapy is associated with an increased risk of VTE. [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. Status. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for drospirenone + ethinyl estradiol and other medicines and health products. [50][51][45], Androgenic progestins have been found to antagonize to some degree the effects of ethinylestradiol on coagulation. [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. The combined oral contraceptive pill (COC) consisting of drospirenone 3 mg/ethinyl estradiol 20 μg (3 mg DRSP/20 μg EE-24/4) supplies 24 days of pills with hormones followed by 4 days of hormone-free pills. Drospirenone(Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone. DROSPIRENONE NON MICRONIZED AND MIC... Drospirenone Issue/Submission Date. [15] In 2017, a formulation of drospirenone with ethinylestradiol was the 98th most commonly prescribed medication in the United States, with more than eight million prescriptions. It is a birth control pill that contains two types of hormones, ethinyl estradiol and drospirenone, and when taken properly, prevents pregnancy. [4] The plasma protein binding of drospirenone is 95 to 97%. 21733. It works by stopping a woman's egg from fully developing each month. [2][1][70] SHBG levels are significantly higher with ethinylestradiol and cyproterone acetate than with ethinylestradiol and drospirenone, owing to the more potent antiandrogenic activity of cyproterone acetate relative to drospirenone. Although the primary mechanism of this action is inhibition of ovulation, other alterations include changes in the cervical mucus (which increases the difficulty of sperm entry into the uterus) and the endometrium (which reduces the likelihood of implantation). [19][20] For use in menopausal hormone therapy, E2/DRSP is specifically approved to treat moderate to severe vasomotor symptoms (hot flashes), vaginal atrophy, and postmenopausal osteoporosis. [4] Drospirenone does not appear to influence the metabolism of omeprazole (metabolized via CYP2C19), simvastatin (metabolized via CYP3A4), or midazolam (metabolized via CYP3A4), and likely does not influence the metabolism of other medications that are metabolized via these pathways. Virtual Booth. [4][2][5][6], Drospirenone is excreted in urine and feces, with slightly more excreted in feces than in urine. [16][17], Drospirenone (DRSP) is used by itself as a progestogen-only birth control pill, in combination with the estrogen ethinylestradiol (EE), with or without supplemental folic acid (vitamin B9), as a combined birth control pill, and in combination with the estrogen estradiol (E2) for use in menopausal hormone therapy.
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