[62] Progestogen-only birth control is not generally associated with a higher risk of breast cancer. [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). [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. Ethinyl estradiol: Reduces LHRH release from hypothalamus, reduces gonadotropin release from pituitary; increases synthesis of DNA, RNA, and various proteins in target tissues; other possible mechanisms include changes in cervical mucus that cause inhibition of sperm penetration and endometrial changes that reduce likelihood of implantation . [4] Since drospirenone has antimineralocorticoid activity, levels of potassium and sodium should be measured and signs of metabolic acidosis should be monitored. 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. It is a birth control pill that contains two types of hormones, ethinyl estradiol and drospirenone, and when taken properly, prevents pregnancy. Update your events Sterling Spa. 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. [82][83], Drospirenone is an antagonist of the AR, the biological target of androgens like testosterone and dihydrotestosterone (DHT). [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. 21733. [1][2] It has about 1 to 65% of the affinity of the synthetic anabolic steroid metribolone for the AR. [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. [4] This may increase the risk of hyperkalemia (high potassium levels). [75][76][77] In male cynomolgus monkeys however, 4 mg/kg/day oral drospirenone strongly suppressed testosterone levels. [1], Common side effects include acne, headache, breast tenderness, weight increase, and menstrual changes. [96][97] It was introduced for medical use in combination with ethinylestradiol as a combined birth control pill in 2000. [1][2][58] Drospirenone has antigonadotropic and functional antiestrogenic effects as a result of PR activation. Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.. [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. [59][60][61], Data on risk of breast cancer in women with newer progestins like drospirenone are lacking at present. 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. Application Number. Drospirenone has no estrogenic activity and no appreciable glucocorticoid or antiglucocorticoid activity. [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. [18], Drospirenone is the generic name of the drug and its INN, USAN, BAN, and JAN, while drospirénone is its DCF. [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. It is an agonist of the PR and an antagonist of the MR and AR, and hence is a progestogen, antimineralocorticoid, and antiandrogen. [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. [13][14] It is available as a generic medication. [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. It would be best to get this clarified while placing the order. [11][12] It is available widely throughout the world. [65] It has about 100 to 500% of the affinity of aldosterone for the MR and about 50 to 230% of the affinity of progesterone for the MR.[1][2][67][58] Drospirenone is about 5.5 to 11 times more potent as an antimineralocorticoid than spironolactone in animals. 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. Drospirenone (6R,7R,8R,9S,10R,13S,14S,15S,16S,17S)-1,3’,4’,6,6a,7,8,9,10,11, 12,13,14,15,15a,16-hexadecahydro-10,13-dimethylspiro-[17H-dicyclopropa- [6,7:15,16]cyclopenta[a]phenanthrene-17,2’(5H)-furan]-3,5’(2H)-dione) is a synthetic progestational compound and has a molecular weight of 366.5 and a molecular formula of C24H30O3. [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. 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 A Latin American perspective for oestrogen-free oral contraception weak partial agonists of the MR in the of! Not generally associated with different risks of VTE have amounted to US $ 56.9 million actually weak partial of... Amounts of unchanged drospirenone can be identified in urine and feces amounted to US 1.97. 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