Diane 35 is a combined oral contraceptive that is widely used in many countries for its anti-androgenic effects. The answer to the question, 'Is Diane 35 an anti-androgen?' is unequivocally yes. Its anti-androgenic activity is the primary reason it is prescribed for conditions caused by an overproduction or increased sensitivity to androgens (male hormones) in women. While it also serves as an effective contraceptive, this is often considered a secondary benefit for patients taking it to manage severe acne, hirsutism, or symptoms of Polycystic Ovary Syndrome (PCOS). The medication's potency and dual mechanism distinguish it from other hormonal therapies.
The Anti-androgenic Mechanism of Diane 35
Diane 35, also known generically as co-cyprindiol, contains two active ingredients: cyproterone acetate (CPA) and ethinylestradiol (EE). These two components work synergistically to exert a powerful anti-androgenic effect through two primary pathways.
The Role of Cyproterone Acetate (CPA)
CPA is a progestin with potent anti-androgenic properties. It is the main driver of Diane 35's androgen-blocking capability. CPA works in two ways to combat the effects of androgens:
- Competitive Androgen Receptor Blockade: CPA directly competes with androgens like testosterone and dihydrotestosterone (DHT) for binding to androgen receptors on target cells. By occupying these receptors, it prevents the natural androgens from initiating their effects, such as stimulating sebaceous glands or hair follicles.
- Suppression of Androgen Production: CPA also has an anti-gonadotropic effect, meaning it suppresses the release of luteinizing hormone (LH) from the pituitary gland through negative feedback. Reduced LH levels lead to a decrease in the production of androgens by the ovaries and adrenal glands.
The Synergistic Effect of Ethinylestradiol (EE)
The estrogen component, ethinylestradiol, enhances the anti-androgenic effects of CPA. EE primarily works by increasing the hepatic synthesis of Sex Hormone-Binding Globulin (SHBG). Here’s how it helps:
- Increased SHBG: SHBG is a protein that binds to androgens in the bloodstream, effectively making them inactive.
- Reduced Free Androgens: By increasing the level of SHBG, EE reduces the amount of free, biologically active androgens circulating in the plasma. This further diminishes the androgenic stimulation of target tissues.
Clinical Applications and Indications
The combined anti-androgenic and contraceptive properties of Diane 35 make it a treatment of choice for several androgen-dependent conditions in women.
Treating Androgen-Sensitive Conditions
Healthcare providers may prescribe Diane 35 for specific conditions where excess androgens are a problem:
- Severe Acne: For women with moderate to severe acne that is unresponsive to other treatments, such as topical therapies or systemic antibiotics, Diane 35 has shown significant improvement. It reduces the activity of the sebaceous glands, decreasing oil production.
- Hirsutism: This refers to the excessive growth of dark or coarse hair in a male-like pattern on a woman's body. Diane 35 has been clinically proven to reduce hirsutism, with noticeable improvement often appearing within 9 to 12 months of treatment.
- Polycystic Ovary Syndrome (PCOS): For women with PCOS who experience hyperandrogenism (high androgen levels), Diane 35 helps regulate hormonal imbalances, improve acne, and manage irregular periods. It can also reduce the size and number of ovarian cysts over time.
Contraceptive Functionality
When used as prescribed, Diane 35 also provides effective oral contraception. It works by inhibiting ovulation and altering the cervical mucus and endometrium, making it difficult for sperm to reach and fertilize an egg. However, it is important to note that due to its elevated risk profile, particularly for thromboembolism, it is not indicated for use as a contraceptive alone. Patients on Diane 35 should not take any additional hormonal contraceptives.
Comparison with Other Anti-androgenic Therapies
Diane 35 is just one of several options for treating androgen-related conditions. Other medications, like spironolactone and finasteride, work through different mechanisms and have varying efficacy and side effect profiles.
| Feature | Diane 35 (Cyproterone Acetate + Ethinylestradiol) | Spironolactone | Finasteride |
|---|---|---|---|
| Mechanism | Dual action: CPA blocks androgen receptors and suppresses androgen production; EE increases SHBG, reducing free androgens. | Blocks androgen receptors and inhibits enzymes in the testosterone synthesis pathway. | Inhibits 5α-reductase, which prevents the conversion of testosterone to the more potent DHT. |
| Indications | Severe acne, hirsutism, PCOS; also provides contraception. | Hirsutism, acne, and androgenetic alopecia in women. | Hirsutism and androgenetic alopecia in women. |
| Efficacy | Highly effective for acne and hirsutism. Can provide faster clinical improvement when combined with other anti-androgens. | Less potent anti-androgen than cyproterone acetate for testosterone suppression. | May be less effective than CPA or spironolactone for treating hirsutism. |
| Side Effects | Increased risk of venous thromboembolism (VTE), mood changes, weight gain, breast tenderness. | Menstrual irregularities, breast tenderness, hyperkalemia risk. | Lower risk of serious side effects compared to flutamide. |
| Contraceptive? | Yes, also provides reliable contraception. | No, not a contraceptive; requires additional birth control. | No, not a contraceptive; requires additional birth control. |
| Availability | Widely available internationally, but not in the United States. | Widely available. | Widely available. |
How Treatment with Diane 35 Works
When a doctor prescribes Diane 35, they will provide specific instructions for its use. Typically, a patient takes one tablet daily for 21 days, followed by a 7-day tablet-free interval, during which a withdrawal bleed occurs.
The Timeline for Results
Patients should manage their expectations regarding the timeline for seeing results, as improvements are not immediate.
- Acne: Improvements can often be noticed within 3 to 4 weeks of starting treatment. Significant improvement is typically seen by the ninth cycle, with 80-90% of women experiencing success.
- Hirsutism: Results take longer to manifest. A reduction in unwanted hair growth is usually observed after 9 to 12 months of therapy. Patience is crucial for this indication.
Conclusion
In summary, Diane 35 is indeed an effective anti-androgen that combines a direct androgen receptor blocker (cyproterone acetate) with an estrogen (ethinylestradiol) that increases SHBG, further reducing free androgen levels. Its efficacy in treating severe acne, hirsutism, and symptoms of PCOS is well-documented, and it also provides reliable contraception. However, its use is associated with serious risks, most notably venous thromboembolism, which is why it is reserved for specific patient populations and not for general contraceptive use. Patients considering Diane 35 should have a thorough discussion with their doctor to weigh the benefits against the risks and to ensure proper monitoring. For more information, patients can consult product information from authorized distributors, such as this example from Bayer.
