What are the anti-androgenic oral contraceptives available in the market, including their scientific and trade names?

Anti-Androgenic Oral Contraceptives in the Market: Scientific and Trade Names

The most effective anti-androgenic oral contraceptives available in the market are those containing drospirenone or norgestimate as the progestin component, with drospirenone having the strongest anti-androgenic properties. 1, 2

Mechanism of Anti-Androgenic Action

Oral contraceptives work as anti-androgens through several mechanisms:

• Decreasing ovarian androgen production
• Increasing sex hormone-binding globulin (SHBG)
• Reducing 5α-reductase activity
• Blocking androgen receptors 1, 2

Progestin Generations and Anti-Androgenic Properties

Progestins in oral contraceptives can be categorized by generation and their androgenic/anti-androgenic properties:

Fourth Generation (Strongest Anti-Androgenic)

• Drospirenone: A spironolactone analogue not derived from testosterone, with potent anti-androgenic and anti-mineralocorticoid properties 1, 2
  • Trade names: Yasmin, YAZ, Loryna (with 30 μg ethinyl estradiol)
  • Newer formulations: Yasminelle (with 20 μg ethinyl estradiol) 3, 4

Third Generation (Moderate Anti-Androgenic)

• Norgestimate: Has peripheral anti-androgenic properties 1, 2
  • Trade name: Sprintec (with ethinyl estradiol) 2
• Desogestrel: Less androgenic than earlier generations 1, 5
  • Trade name: Various generic formulations

Second Generation (Minimal to No Anti-Androgenic)

• Levonorgestrel: Has androgenic potential 1
  • Trade names: Various generic formulations
• Norgestrel: Higher androgenic activity 1, 2
  • Trade names: Various generic formulations

First Generation (Androgenic)

• Norethindrone: Has androgenic effects 1
• Ethynodiol diacetate: Has androgenic effects 1

FDA-Approved Anti-Androgenic Oral Contraceptives

Four combined oral contraceptives are FDA-approved for treatment of acne, indicating their anti-androgenic properties:

1. Norgestimate/ethinyl estradiol
2. Norethindrone acetate/ethinyl estradiol/ferrous fumarate
3. Drospirenone/ethinyl estradiol
4. Drospirenone/ethinyl estradiol/levomefolate 1

Newest Formulations with Enhanced Properties

Drospirenone-Containing Formulations

• Drospirenone 3 mg/ethinyl estradiol 20 μg (24/4): YAZ - approved for contraception, PMDD treatment, and moderate acne 3, 6
• Drospirenone 3 mg/ethinyl estradiol 30 μg: Yasmin - effective for acne and fluid-related symptoms 7, 4

Natural Estrogen Formulations

• Estradiol valerate/dienogest: Newer formulation with potentially fewer adverse effects 1
• Estetrol/drospirenone: Newer formulation with potentially fewer adverse effects 1

Clinical Considerations

Safety Profile

• Drospirenone-containing COCs may have a slightly higher risk of venous thromboembolism (VTE) compared to levonorgestrel-containing formulations (approximately 10 per 10,000 woman-years vs. 3-9 per 10,000 woman-years) 1, 8
• Norgestimate has one of the lowest VTE risks among combined oral contraceptives 2

Specific Benefits

• Drospirenone: Most beneficial for women with PMDD, fluid retention issues, and more severe androgenic symptoms 2, 3, 6
• Norgestimate: Better option for women with higher VTE risk factors or PCOS 2

Contraindications

Common contraindications for all COCs include:

• Age ≥35 years with smoking
• History of deep vein thrombosis or pulmonary embolism
• Ischemic heart disease
• History of cerebrovascular accident
• Migraines with aura
• Active viral hepatitis or severe liver disease 2, 8

Monitoring and Expected Results

• Improvement in androgenic symptoms may take at least 3 months to become noticeable
• Regular monitoring of blood pressure is recommended, especially with drospirenone due to its anti-mineralocorticoid effects 2

Anti-androgenic oral contraceptives represent an important therapeutic option for women who need contraception while also addressing androgenic symptoms such as acne, hirsutism, or female pattern hair loss.