SERMs

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CLOMIPHENE
50MG/TAB * 24TAB

Pharmacology
Clomiphene is a racemic mixture consisting of zuclomiphene (~38%) and enclomiphene (~62%), each with distinct pharmacologic properties. Clomiphene acts at the level of the hypothalamus, occupying cell surface and intracellular estrogen receptors (ERs) for longer durations than estrogen. This interferes with receptor recycling, effectively depleting hypothalamic ERs and inhibiting normal estrogenic negative feedback. Impairment of the feedback signal results in increased pulsatile GnRH secretion from the hypothalamus and subsequent pituitary gonadotropin (FSH, LH) release, causing growth of the ovarian follicle, followed by follicular rupture (ASRM 2013; Dickey, 1996).

Absorption
Readily absorbed.


Metabolism
Hepatic; undergoes enterohepatic recirculation (Goldstein 2000).


Time to Peak
~6 hours (Goldstein 2000).


Half-Life Elimination
~5 days (Goldstein 2000).


Detection Time
~60 days.

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EVISTA
60MG/TAB * 28TAB

Pharmacology
Raloxifene is an estrogen agonist/antagonist (a selective estrogen receptor modulator [SERM]); selective binding activates estrogenic pathways in some tissues and antagonizes estrogenic pathways in other tissues. Raloxifene acts like an estrogen agonist in the bone to prevent bone loss and has estrogen antagonist activity to block some estrogen effects in the breast and uterine tissues. Raloxifene decreases bone resorption, increasing bone mineral density and decreasing fracture incidence.

Absorption
Rapid; ~60%


Metabolism
Hepatic, extensive first-pass metabolism; metabolized to glucuronide conjugates.


Half-Life Elimination
27.7 hours (following a single dose); 32.5 hours (following multiple doses).

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NOLVADEX, Rx
10MG/TAB * 100TAB - 20MG/TAB * 100TAB

Pharmacology
Tamoxifen competitively binds to estrogen receptors on tumors and other tissue targets, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects; nonsteroidal agent with potent antiestrogenic properties which compete with estrogen for binding sites in breast and other tissues; cells accumulate in the G0 and G1 phases; therefore, tamoxifen is cytostatic rather than cytocidal.

Absorption
Well absorbed.


Metabolism
Hepatic; via CYP2D6 to 4-hydroxytamoxifen and via CYP3A4/5 to N-desmethyl-tamoxifen. Each is then further metabolized into endoxifen (4-hydroxy-tamoxifen via CYP3A4/5 and N-desmethyl-tamoxifen via CYP2D6); both 4-hydroxy-tamoxifen and endoxifen are 30- to 100-fold more potent than tamoxifen.


Time to Peak
Serum: ~5 hours.


Half-Life Elimination
Tamoxifen: ~5 to 7 days; N-desmethyl tamoxifen: ~14 days


Detection Time
~60 days.

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NOLVADEX-D
20MG/TAB * 30TAB

Pharmacology
Tamoxifen competitively binds to estrogen receptors on tumors and other tissue targets, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects; nonsteroidal agent with potent antiestrogenic properties which compete with estrogen for binding sites in breast and other tissues; cells accumulate in the G0 and G1 phases; therefore, tamoxifen is cytostatic rather than cytocidal.

Absorption
Well absorbed.


Metabolism
Hepatic; via CYP2D6 to 4-hydroxytamoxifen and via CYP3A4/5 to N-desmethyl-tamoxifen. Each is then further metabolized into endoxifen (4-hydroxy-tamoxifen via CYP3A4/5 and N-desmethyl-tamoxifen via CYP2D6); both 4-hydroxy-tamoxifen and endoxifen are 30- to 100-fold more potent than tamoxifen.


Time to Peak
Serum: ~5 hours.


Half-Life Elimination
Tamoxifen: ~5 to 7 days; N-desmethyl tamoxifen: ~14 days


Detection Time
~60 days.

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$25.00
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