Trust Pill Mechanism of Action

Pharmacotherapeutic group: Progestogen and Estrogens, fixed combinations. ATC code: G03AA07.
Pharmacology: Pharmacodynamics: Overall Pearl Index (method failure + patient failure): 0.59 (upper tow-sided 95% confidence limit: 0.85).
The contraceptive effect of COCs is based on the interaction of various factors. The most important are the inhibition of ovulation and changes in cervical mucus.
Mechanism of action: Ethinylestradiol + Levonorgestrel + Ferrous Fumarate (TRUST PILL) works primarily by preventing the release of eggs from the ovaries. Also, Ethinylestradiol acts synergistically with levonorgestrel to provide regular and consistent suppression of ovulation.
Pharmacokinetics: Absorption: Ethinylestradiol and Levonorgestrel are absorbed with maximum plasma concentrations occurring within 2 hours after Ethinylestradiol + Levonorgestrel + Ferrous Fumarate (TRUST PILL) administration. Levonorgestrel reaches a bioavailability of nearly 100% after oral administration and is not subject to first-pass metabolism. Ethinylestradiol reaches a bioavailability of approximately 43% principally due to first pass metabolism.
The mean plasma pharmacokinetic parameters after daily exposure to Levonorgestrel & Ethinylestradiol remain statistically similar on day 21, 84, and 91.
The effect of food on the rate and the extent of Levonorgestrel and Ethinylestradiol absorption following oral administration Ethinylestradiol + Levonorgestrel + Ferrous Fumarate (TRUST PILL) has not been evaluated.
Distribution: Levonorgestrel is about 97.5-99% bound principally to sex hormone binding globulin (SHBG) and, to a lesser extent, serum albumin. Ethinylestradiol is about 95%-97% bound to serum albumin. Ethinylestradiol induces SHBG synthesis, which leads to decreased Levonorgestrel clearance.
Metabolism: Following absorption, Levonorgestrel is conjugated at the 17β-OH position to form sulfate and glucuronide conjugates in plasma. Significant amounts of conjugated and unconjugated 3α,5β-tetrahydrolevonorgestrel are also present in plasma. Levonorgestrel and its phase I metabolites are excreted primarily as glucuronide conjugates. Metabolism of Ethinylestradiol involves formation of Ethinylestradiol-3-sulfate in the gut wall, followed by 2-hydroxylation of a portion of the remaining untransformed Ethinylestradiol by hepatic cytochrome P-450 3A4 (CYP3A4). Hydroxylation at the 4-,6-, and 16- positions may occur. The various hydroxylated metabolites are subject to further methylation and/or conjugation.
Excretion: About 45% of Levonorgestrel and its metabolites are excreted in the urine and about 32% are excreted in feces, mostly as glucuronide conjugates. The terminal elimination half-life for Levonorgestrel was about 34 hours. Ethinylestradiol is excreted in the urine and feces as glucuronide and sulfate conjugates, and it undergoes enterohepatic recirculation. The terminal elimination half-life of Ethinylestradiol was about 18 hours.
Race: The effect of race on the pharmacokinetics of Ethinylestradiol + Levonorgestrel + Ferrous Fumarate (TRUST PILL) has not been evaluated.