What are the trade names of hormonal Oral Contraceptive Pills (OCPs) with antiandrogenic effects?

Trade Names of Hormonal OCPs with Antiandrogenic Effects

The FDA-approved combined oral contraceptive pills (COCs) with antiandrogenic effects include Yaz/Yasmin (ethinyl estradiol/drospirenone), Ortho Tri-Cyclen (ethinyl estradiol/norgestimate), Estrostep Fe (ethinyl estradiol/norethindrone acetate/ferrous fumarate), and Beyaz (ethinyl estradiol/drospirenone/levomefolate). 1

Antiandrogenic Mechanisms of OCPs

• All combined oral contraceptives have some degree of antiandrogenic effect through multiple mechanisms 1:

  • Decrease ovarian androgen production
  • Increase sex hormone-binding globulin (SHBG), binding free testosterone
  • Reduce 5-alpha-reductase activity
  • Block androgen receptors

• The net effect of all COCs when combined with ethinyl estradiol is antiandrogenic, regardless of the specific progestin used 1

OCPs with Strongest Antiandrogenic Properties

• Drospirenone-containing pills (Yaz, Yasmin, Beyaz):

  • Drospirenone is a fourth-generation progestin with specific antiandrogenic properties 2
  • Contains 3mg drospirenone with 20μg ethinyl estradiol in a 24/4 day regimen 2
  • Drospirenone is a spironolactone analogue with both antimineralocorticoid and antiandrogenic activity 3
  • FDA-approved specifically for acne treatment 1

• Norgestimate-containing pills (Ortho Tri-Cyclen):

  • Second-generation progestin with antiandrogenic effects 1
  • FDA-approved for acne treatment 1
  • Effective in reducing inflammatory and comedonal acne lesions 1

• Norethindrone acetate-containing pills (Estrostep Fe):

  • First-generation progestin with moderate antiandrogenic effects 1, 4
  • FDA-approved for acne treatment 1
  • Contains ferrous fumarate to supplement iron during menstruation 1

Other OCPs with Antiandrogenic Effects (Not FDA-approved for acne)

• Desogestrel-containing pills (Marvelon):

  • Third-generation progestin considered less androgenic than earlier generations 5, 6
  • Contains 30μg ethinyl estradiol, placing it in the mid-range of estrogen dosing 5
  • Shown to have antiandrogenic effects but less pronounced than drospirenone 6

• Dienogest-containing pills:

  • Potent antiandrogenic progestin that blocks androgen receptors 7
  • Reduces activity of skin 5-alpha-reductase enzyme 7

• Chlormadinone acetate-containing pills:

  • Potent antiandrogenic progestin 7
  • Suppresses gonadotropin secretion, reducing ovarian and adrenal androgen production 7
  • Improvement or resolution of seborrhea in 80% of users 7

Clinical Efficacy for Acne and Other Androgenic Conditions

• Drospirenone-containing OCPs have been shown to reduce acne lesions by approximately 62.5% after 9 treatment cycles 8
• OCPs containing cyproterone acetate (not available in US) reduced acne lesions by 58.8% 8
• All FDA-approved antiandrogenic OCPs demonstrate significant reduction in both inflammatory and comedonal acne lesions 1
• Clinical improvements are also seen in:
  • Seborrhea (80% improvement) 7
  • Hirsutism (36% improvement) 7
  • Androgen-related alopecia (up to 86% improvement) 7

Contraindications and Precautions

• OCPs with antiandrogenic effects carry the same contraindications as other combined hormonal contraceptives 1, 2:

  • History of deep vein thrombosis or pulmonary embolism
  • Uncontrolled hypertension
  • Smoking in women over 35 years of age
  • History of breast cancer or other estrogen/progestin-sensitive cancers
  • Active liver disease
  • Migraine with aura

• Drospirenone-containing pills may have a slightly higher VTE risk (approximately 10 per 10,000 person-years) compared to other combined oral contraceptives 5

• When prescribing OCPs for antiandrogenic effects, the benefits must be weighed against the risks, particularly in women with risk factors for venous thromboembolism 1