Дроспиренон: свойства, применение и влияние на организм

Medication drug

Drospirenone was patented in 1976 and introduced for medical use in 2000. It is available widely throughout the world. In 2020, a formulation of drospirenone with ethinylestradiol was the 145th most commonly prescribed medication in the United States, with more than 4million prescriptions.

Drospirenone (DRSP) is used by itself as a progestogen only birth control pill, in combination with the estrogens ethinylestradiol (EE) or estetrol (E4), 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. 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. The drospirenone component in this formulation is included specifically to prevent estrogen induced endometrial hyperplasia. Studies have found that EE/DRSP is superior to placebo in reducing premenstrual emotional and physical symptoms while also improving quality of life. E2/DRSP has been found to increase bone mineral density and to reduce the occurrence of bone fractures in postmenopausal women. In addition, E2/DRSP has a favorable influence on cholesterol and triglyceride levels and decreases blood pressure in women with high blood pressure.

Drospirenone is an agonist of the PR, the biological target of progestogens like progesterone. 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. In male cynomolgus monkeys however, 4 mg/kg/day oral drospirenone strongly suppressed testosterone levels. Drospirenone is the only clinically used progestogen with prominent antimineralocorticoid activity besides progesterone. Both drospirenone and progesterone are actually weak partial agonists of the MR in the absence of mineralocorticoids.

Drospirenone is an antagonist of the AR, the biological target of androgens like testosterone and dihydrotestosterone (DHT). 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. Androgenic progestins like levonorgestrel have been found to inhibit the procoagulatory effects of estrogens like ethinylestradiol on hepatic synthesis of coagulation factors, whereas this may occur less or not at all with weakly androgenic progestins like desogestrel and antiandrogenic progestins like drospirenone. Certain other progestins act similarly in this assay, whereas progesterone acts neutrally. Levels are about 27 ng/mL after a single 4 mg dose. Spirolactones like drospirenone and spironolactone are derivatives of progesterone, which likewise has progestogenic and antimineralocorticoid activity. The loss of the C7α acetylthio group of spironolactone, a compound with negligible progestogenic activity, 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.

Drospirenone was patented in 1976 and introduced for medical use in 2000. It was introduced for medical use in combination with ethinylestradiol as a combined birth control pill in 2000. Drospirenone is sometimes described as a "fourth generation" progestin based on its time of introduction. The medication was approved for use in menopausal hormone therapy in combination with estradiol in 2005.

Drospirenone is the generic name of the drug and its , , , and , while drospirénone is its Its name is a shortened form of the name 1,2 dihydrospirorenone or dihydrospirenone. 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. This is in addition to around 10,000 claims that Bayer has already settled without admitting liability. 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. Drospirenone has been studied in forms for parenteral administration.