For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
Used in the palliative treatment of advanced prostate cancer. Leuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.
mechanism of action
Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
In rats subcutaneous administration of 250 to 500 times the recommended human dose, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a clinical counterpart of this phenomenon. In early clinical trials with leuprolide acetate doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose.
Primarily degraded by peptidase and not by cytochrome P450 enzymes.
Bioavailability by subcutaneous administration is comparable to that by intravenous administration.
route of elimination
Excretion in urine