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Drospirenone

Generic Name
Drospirenone
Brand Names
Angeliq 0.25/0.5 28 Day, Beyaz 28 Day, Gianvi 28-day, Jasmiel 28 Day, Lo-zumandimine 28 Day, Loryna, Nextstellis 28 Day, Nikki 28 Day, Ocella 28 Day, Safyral 28 Day, Slynd, Syeda 28 Day, Tydemy 28 Day, Vestura, Yasmin, Yasmin 28 Day, Yaz 28 Day, Yaz Plus, Zarah, Zumandimine 28 Day
Drug Type
Small Molecule
Chemical Formula
C24H30O3
CAS Number
67392-87-4
Unique Ingredient Identifier
N295J34A25
Background

Drospirenone is a synthetic progestin commonly found in the popular oral contraceptive, Yaz in combination with Ethinyl estradiol. Most recently, it was approved by both Health Canada and the FDA in combination with Estetrol as an oral contraceptive therapy. Aside from its contraceptive effects, drospirenone is used with estrogens to control acne and premenstrual dysphoric disorder (PMDD).

Drospirenone has been the subject of widespread safety concern due to the possibility of an increased risk of venous thromboembolism associated with its use. In 2012, however, a safety statement by the FDA concluded that the increase in the risk of thromboembolism resulting from the use of drospirenone remains unclear, as studies regarding this risk are conflicting. Some studies have demonstrated a significantly increased risk and some demonstrating no risk of thromboembolic events. In its statement, the FDA has mentioned that increased risk of venous thromboembolism with oral contraceptives such as drospirenone exists but remains lower than the risk of this condition during pregnancy and during the postpartum period, and this should be considered when assessing potential risks of hormonal contraceptive use.

Indication

Drospirenone, in combination with ethinyl estradiol or estetrol, is indicated as an oral contraceptive for the prevention of pregnancy. In addition to its use for contraceptive effects, this combination is used to treat moderate acne vulgaris and the symptoms of premenstrual dysphoric disorder. The drug has approved indications for combination with estrogens for the treatment of menopause-associated symptoms, such as vasomotor symptoms and vulvovaginal atrophy. Drospirenone combined with estrogen may also may aid in the prevention of osteoporosis in women who have been post-menopausal for at least a year and are not candidates for other therapies. It can sometimes be found in preparations containing estrogen and folic acid for folic acid replenishment during oral contraception.

When used for the treatment of acne vulgaris, drospirenone-containing contraceptives should only be used in women ≥14 years of age who have experienced menarche, desire oral contraception, and do not have any contraindications to oral contraceptives. Off-label uses for this drug include the treatment of menstrual irregularities, dysmenorrhea, hirsutism, and endometriosis.

Associated Conditions
Atrophy of vulva, Moderate to Severe Vasomotor Symptoms, Neural Tube Defects (NTDs), Premenstrual Dysphoric Disorder (PMDD), Vulvo Vaginal Atrophy, Moderate Acne vulgaris
Associated Therapies
Contraception, Folate supplementation therapy

Acurx Pharmaceuticals Advances Ibezapolstat for C. difficile Infection

• Acurx Pharmaceuticals presented Phase 2 clinical trial results of ibezapolstat for *C. difficile* infection (CDI) at the Anaerobe Society of the Americas, highlighting its clinical efficacy. • The USPTO granted Acurx a new patent for ibezapolstat, expiring in June 2042, covering the treatment of CDI while reducing recurrence and improving gut microbiome health. • Acurx is planning a Phase 3 clinical program and NDA submission for ibezapolstat, with ongoing preclinical programs for other gram-positive infections like MRSA and VRE. • Phase 2b trial data presented at IDWeek showed ibezapolstat had comparable clinical cure and sustained cure rates to vancomycin, with no recurrence in followed patients.
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