Clomiphene
Clomiphene. Mixture of zuclomiphene + enclomiphene isomers. Antagonizes estrogen receptor at the hypothalamus, removing negative feedback → increased GnRH → increased…
Mixture of zuclomiphene + enclomiphene isomers. Antagonizes estrogen receptor at the hypothalamus, removing negative feedback → increased GnRH → increased FSH/LH → increased gonadal steroid output. In women, induces ovulation; in men, raises endogenous testosterone without exogenous androgen exposure.
PK: STRIPPED. THE STORED HALF-LIFE APPEARS NOWHERE — its citation offers only the qualitative "The active Z isomer attained peak blood levels later than the inactive E isomer and was eliminated much more slowly, significant plasma concentrations still being detected up to 1 month after treatment" — and the stored figure is a label statement in days converted to hours. A PUBLISHED SENTENCE DECLARES THE RECORD UNAUTHORABLE OUTRIGHT: "The conventional model-dependent pharmacokinetics of clomiphene citrate isomers COULD NOT BE DETERMINED due to a very flat terminal half-life and the long-tailed residence time." The feasibility test agrees and does so for BOTH isomers at once: one needs an exposure-to-peak ratio of at least 173 h and observes 86, the other observes 4.3 — two orders apart — SO NOTHING REPRODUCES BOTH, and a mixture record must reproduce both. With the solver defaults the record was predicting a peak roughly forty-fold above the published total. The doses go too: only the lowest has any human data, the highest is off-label, and the typical figure is a computed artefact of the other two.
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Sources: PMID:3091405