What is the best antiandrogen birth control pill?

Best Antiandrogen Birth Control Pills for Women

Drospirenone-containing combined oral contraceptives (COCs) are the best antiandrogen birth control pills due to their unique antiandrogenic properties and favorable clinical outcomes. 1, 2

Mechanism of Action of Antiandrogen COCs

• All COCs provide antiandrogenic effects through multiple mechanisms:

  • Decrease ovarian androgen production 1
  • Increase sex hormone-binding globulin, reducing free testosterone 1, 2
  • Reduce 5α-reductase activity 1, 2
  • Block androgen receptor activation 1

• These mechanisms lead to improvement in androgen-related conditions such as acne and hirsutism while providing contraception 1

FDA-Approved COCs with Antiandrogen Properties

There are four FDA-approved COCs for acne treatment, all with antiandrogenic properties:

1. Drospirenone-containing COCs (strongest antiandrogen effect):

   • Ethinyl estradiol/drospirenone 1, 2
   • Ethinyl estradiol/drospirenone/levomefolate 1, 2

2. Other FDA-approved options:

   • Ethinyl estradiol/norgestimate 1
   • Ethinyl estradiol/norethindrone acetate/ferrous fumarate 1

Comparing Antiandrogen Potency of COCs

• Drospirenone is a fourth-generation progestin derived from spironolactone with unique antimineralocorticoid and antiandrogenic properties 1, 3

  • Not derived from testosterone (unlike other progestins) 1
  • Has intrinsic antiandrogenic activity similar to endogenous progesterone 3
  • May help prevent water retention and weight gain 4, 3

• Norgestimate (third-generation) and norethindrone (first-generation) have less antiandrogenic activity than drospirenone but still provide net antiandrogenic effects when combined with ethinyl estradiol 1

• Studies have shown drospirenone-containing COCs to be as effective as cyproterone acetate (a potent antiandrogen not available in the US) for treating acne 5

Clinical Decision Algorithm

1. First-line option: Drospirenone-containing COCs for women with moderate acne or other androgenic symptoms who desire contraception 2, 3

   • Particularly beneficial for women concerned about fluid retention or weight gain 4, 3

2. Alternative options if drospirenone is contraindicated:

   • Norgestimate-containing COCs 1, 2
   • Norethindrone acetate-containing COCs 1, 2

3. Avoid: Progestin-only contraceptives as they may worsen acne 1

Safety Considerations

• VTE risk:

  • Baseline risk (non-pregnant, non-COC users): 1-5 per 10,000 woman-years 1
  • Standard COCs: 3-9 per 10,000 woman-years 1
  • Drospirenone-containing COCs: approximately 10 per 10,000 woman-years 1
  • Pregnancy: 5-20 per 10,000 woman-years 1

• Contraindications for all COCs include:

  • History of deep vein thrombosis or pulmonary embolism 1
  • Ischemic heart disease 1
  • Severe liver disease 1
  • Migraine with aura at any age or without aura if ≥35 years 1
  • Active smokers over age 35 1

Important Clinical Pearls

• A comprehensive medical history and blood pressure measurement should be performed before prescribing any COC 2

• Improvement in acne may take 3-6 months to become fully apparent 5, 6

• All COCs have a net antiandrogenic effect when combined with estrogen, regardless of progestin type, but drospirenone provides the strongest antiandrogenic activity 1, 2

• For women with PCOS and hirsutism, combining an antiandrogen COC with other treatments may provide the most effective approach 1

• Avoid cyproterone acetate in women with hereditary angioedema as it may worsen symptoms 1