Triptorelin

Status

FDA-approved. FDA-approved labeling exists as Trelstar for palliative treatment of advanced prostate cancer and as Triptodur for central precocious puberty. Labels document initial transient surges in testosterone, spinal cord compression and urinary obstruction risk in prostate cancer, and reductions in bone mineral density.

What it is

A GnRH agonist used clinically, with a strong initial hormone surge.

What published research measured

A gonadotropin-releasing hormone agonist with a long duration of action. Its clinical behaviour follows directly from the pulsatile-versus-continuous principle: after an initial surge in gonadotropins and sex hormones — the flare, which can transiently worsen hormone-sensitive disease — continuous receptor occupation downregulates the pituitary and produces profound suppression of testosterone or oestradiol. That suppression is the therapeutic purpose in advanced prostate cancer, endometriosis and central precocious puberty, all supported by randomized evidence. Used in a physique context to restart the axis, the flare is the intended effect and the sustained suppression that follows is the unintended one, which is the opposite of what is usually assumed. Bone density loss with prolonged use is well documented.

Source

FDA labeling for Trelstar and Triptodur

Sources

No linked primary source is on file for this entry yet.

Educational use only, never medical advice. No doses.