Citations for: Stanczyk, F. Z.; Archer, D. F.; Bhavnani, B. R., Ethinyl estradiol and 17 beta-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception 2013, 87 (6), 706-727.

Entry Type

Name

Value

Parent Entry

Pharmacology Data Field

Serum Protein Binding

97% bound. Mainly to serum albumin. No binding to SHBG, but induces SHBG synthesis.

Ethinyl Estradiol (API)

Pharmacology Data Field

Mineralocorticoid Receptor Activity

Antagonist (antimineralocorticoid or aldosterone antagonist). Agonist reports vary: "weak" (Africander) to "strong" (Bartsch).

Drospirenone (API)

Pharmacology Data Field

Elimination Half-Life (t_1/2)

7-8 h (Stanczyk, Goodman & Gilman)
4.8 - 12.8 h (Toxnet)

Norethindrone (API)

Pharmacology Data Field

Bioavailability

< 5%

Estradiol (API)

Pharmacology Data Field

Elimination Half-Life (t_1/2)

Oral: 13-30 h (Stanczyk)
36 h (DrugBank)
20.1 h from oral administration (Toxnet)

Estradiol (API)

Pharmacology Data Field

Serum Protein Binding

60% to albumin, 38% to SHBG.

Estradiol (API)

Pharmacology Data Field

Glucocorticoid Receptor Activity

Pronounced as "unknown" by Stanczyk in 2013, but previously claimed as not active (Ruan, Lello). Recently (2015) defined as full antagonist with low affinity (Paris).

Norgestimate (API)

Pharmacology Data Field

Excretion

54% in urine, 6% in feces.

Estradiol (API)

Pharmacology Data Field

Androgen Receptor Activity

Potent antagonist

Cyproterone Acetate (API)