What are the most commonly prescribed oral combined contraception pills?

Most Commonly Prescribed Oral Combined Contraception Pills

The most commonly prescribed oral combined contraception pills (COCs) are those containing 30-35 μg of ethinyl estradiol combined with a progestin such as levonorgestrel or norgestimate. 1

Composition and Types of COCs

• COCs contain both estrogen and progestin components, with ethinyl estradiol (EE) being the most common estrogen, typically ranging from 10-50 μg 1

• Progestins in COCs are categorized by generations:

  • First-generation: norethindrone and ethynodiol diacetate 2, 1
  • Second-generation: levonorgestrel and norgestrel 2, 1
  • Third-generation: norgestimate and desogestrel 2, 1
  • Fourth-generation: drospirenone and dienogest 2, 1

• Low-dose pills (containing ≤35 μg ethinyl estradiol) are now the standard of care and are considered first-line options 3

FDA-Approved COCs for Acne Treatment

Four specific COC formulations have FDA approval for treating acne in women who desire contraception:

• Norgestimate/ethinyl estradiol 2
• Norethindrone acetate/ethinyl estradiol/ferrous fumarate 2
• Drospirenone/ethinyl estradiol 2
• Drospirenone/ethinyl estradiol/levomefolate 2

Mechanism of Action

• COCs prevent pregnancy by inhibiting gonadotropin-releasing hormone, follicle-stimulating hormone, and luteinizing hormone 2
• They also decrease ovarian androgen production, increase sex hormone-binding globulin, and reduce free testosterone 2

Safety Considerations

• The risk of venous thromboembolism (VTE) with COC use is estimated to be 3-9 per 10,000 woman-years, with the highest risk during the first year of use 4
• DRSP-containing COCs may be associated with a higher risk of VTE than COCs containing levonorgestrel or some other progestins 4
• The American Academy of Pediatrics notes that the most serious adverse event associated with COC use is the increased risk of blood clots, which increases from 1 per 10,000 to 3-4 per 10,000 woman-years during COC use 1

Prescribing Patterns and Recommendations

• For most women, providers typically begin with a COC containing 30-35 μg of ethinyl estradiol and a progestin such as levonorgestrel or norgestimate 1
• Pills containing levonorgestrel or norethisterone in combination with ethinyl estradiol 35 μg or less are considered first-line options 3
• For women with specific needs:
  • Women with acne may benefit from COCs containing drospirenone, which has anti-androgenic properties 5
  • Women concerned about weight gain may prefer formulations with drospirenone, which has antimineralcorticoid effects 5
  • Women with headaches may benefit from lower estrogen doses (20 μg or less) 5

Drug Interactions

• COCs may have reduced effectiveness when taken with certain medications, particularly some antiretroviral agents 2
• Ritonavir-boosted protease inhibitors, nevirapine, and efavirenz can reduce hormonal levels of COCs 2
• COCs do not have significant interactions with nucleoside reverse transcriptase inhibitors, integrase inhibitors such as raltegravir and dolutegravir, entry inhibitors, or fusion inhibitors 2

Common Pitfalls and Considerations

• The risk of VTE is highest during the first 6 months of COC use 4
• Known risk factors for VTE include smoking, obesity, and family history of VTE 4
• COCs containing drospirenone should be prescribed with caution in women with risk factors for VTE 4
• COCs should be discontinued if an arterial or venous thrombotic event occurs 4
• Estrogen-free progestin-only pills (POPs) are valuable alternatives for women who are ineligible for or choose not to use COCs 6

Evolution of COC Formulations

• Most current COC formulations contain 50 μg or less of ethinyl estradiol and 1 mg or less of various progestins 7
• Newer generation progestins (norgestimate, desogestrel, and gestodene) allow for effective contraception at lower doses than previous progestins 7
• Estradiol 17-β, the natural estrogen in women, is now being used in some COCs as an alternative to ethinyl estradiol, potentially offering a better metabolic and vascular profile 8