Description

The combination product of Ethinyl Estradiol and Drospirenone is a widely used oral contraceptive. It contains Ethinyl Estradiol, a synthetic estrogen, and Drospirenone, a unique synthetic progestin that is an analog of spironolactone. This combination is known for its contraceptive efficacy and its additional therapeutic benefits related to the anti-androgenic and anti-mineralocorticoid properties of drospirenone.

Indication

This combination is indicated for a range of uses beyond standard contraception. Its main indications include:

• Oral Contraception: To prevent pregnancy.

• Moderate Acne Vulgaris: For the treatment of moderate acne in women who are at least 14 years old and have already started menstruating, and who desire an oral contraceptive for birth control.

• Premenstrual Dysphoric Disorder (PMDD): For the treatment of the emotional and physical symptoms of PMDD.

Mechanism of Action

The therapeutic effects of this combination are a result of the synergistic actions of its two components:

1. Ethinyl Estradiol

• Inhibition of Ovulation: Ethinyl Estradiol works to suppress the release of follicle-stimulating hormone (FSH) from the pituitary gland. This prevents the development of ovarian follicles.
• Hormonal Regulation: The presence of a constant level of estrogen and progestin throughout the cycle disrupts the normal hormonal feedback loop, preventing the hormonal fluctuations that lead to ovulation.

2. Drospirenone

• Contraceptive Action: As a progestin, drospirenone provides several contraceptive effects:

• • It suppresses the luteinizing hormone (LH) surge required for ovulation.

• • It causes the cervical mucus to become thick and hostile to sperm penetration.

• • It thins the endometrial lining, making it unsuitable for implantation.

• Anti-androgenic Properties: Drospirenone has a unique structure that gives it the ability to block androgen receptors. Androgens (like testosterone) are hormones that can contribute to conditions like acne and excessive hair growth. By blocking these receptors, drospirenone helps to reduce the activity of androgens in the skin, which is the mechanism behind its effectiveness in treating acne.
• Anti-mineralocorticoid Properties: Drospirenone also has an anti-mineralocorticoid effect, similar to spironolactone. It blocks the aldosterone receptor, which promotes the excretion of sodium and water while retaining potassium. This helps to reduce symptoms of bloating, fluid retention, and breast tenderness that can be associated with hormonal fluctuations, making it effective in treating the physical symptoms of PMDD.

Synergistic Effect

The combination provides highly effective contraception through the combined suppression of ovulation and the alteration of cervical mucus and the uterine lining. The unique properties of drospirenone provide the added benefits of reducing acne (due to its anti-androgenic effect) and alleviating symptoms of fluid retention (due to its anti-mineralocorticoid effect), making it a valuable option for women seeking these additional benefits.